REVIEW article

Front. Pharmacol., 30 October 2019

Sec. Ethnopharmacology

Volume 10 - 2019 | https://doi.org/10.3389/fphar.2019.01236

Actinidia chinensis Planch.: A Review of Chemistry and Pharmacology

  • XH

    Xirui He 1*

  • JF

    Jiacheng Fang 2

  • XC

    Xufei Chen 2

  • ZZ

    Zefeng Zhao 2

  • YL

    Yongsheng Li 3

  • YM

    Yibing Meng 3

  • LH

    Linhong Huang 3

  • 1. Department of Bioengineering, Zhuhai Campus Zunyi Medical University, Zhuhai, China

  • 2. The College of Life Sciences, Northwest University, Xi’an, China

  • 3. Honghui Hospital, Xi’an Jiaotong University, Xi’an, China

Abstract

Actinidia chinensis Planch. (A. chinensis), commonly known as Chinese kiwifruit, is a China native fruit, which becomes increasingly popular due to attractive economic, nutritional, and health benefits properties. The whole plant including fruits, leaves, vines, and roots of A. chinensis are used mainly as food or additive in food products and as folk medicine in China. It is a good source of triterpenoids, polyphenols, vitamin C, carbohydrate, amino acid, and minerals. These constituents render the A. chinensis with a wide range of pharmacological properties including antitumor, antioxidant, anti-inflammatory, immunoregulatory, hypolipemic, antidiabetic, and cardiovascular protective activities, suggesting that it may possibly be value in the prevention and treatment of pathologies associated to cancer, oxidative stress, and aging. This minireview provides a brief knowledge about the recent advances in chemistry, biological activities, utilization, and storage of Chinese kiwifruit. Future research directions on how to better use of this crop are suggested.

Introduction

Actinidia chinensis Planch. (A. chinensis), commonly known as “Chinese kiwifruit” (English), “中华猕猴桃” (Chinese), and characterized by excessive vegetative vigor, is a woody perennial, deciduous, and functionally dioecious medicinal plant in the family Actinidiaceae (; The Plant List, 2013). It is native to China and has been cultivated in New Zealand, United States, Greece, Italy, Chile, France, Japan, and Korea (Li and Zhu, 2017; Ma et al., 2017). In China, they are mainly distributed in temperate to warm-temperate zones such as Shaanxi, Gansu, Henan, Guangdong, Guangxi, Fujian, Guizhou, Yunnan, Sichuan, as well as the middle and lower reaches of the Yangtze River basin, especially in Yiling district in Yichang city, Hubei province (Figure 1) (). There are 13 A. chinensis cultivars, especially “Hongyang,” “Jintao,” and “Huayou,” are developed for commercial production in China (Sharon, 2016), and more than three ones such as “Sungold,” “Charm,” and “Hort16A” developed in New Zealand () (Table 1).

Figure 1

; https://www.newasp.net/soft/105257.html).

Table 1

Origin countryCultivarFruit shapeAvg. weightFruit skinFruit flesh
ChinaCuiyu (Liangmei No. 1)Ovoid90 gGreenish brown with short hairsGreen
Wuzhi No. 3 (Wuzhi 81-36)Ellipsoid85 gDark green with soft hairsBright green
Chuhong (Panda™
Forest Red Kiwi)
Long ellipsoid80 gDark green and hairlessGreen with red flesh around white core
QihongCylindric100 gGreen with sparse or absent hairsLight green to yellow
Hongyang (Red Sun, RS1)Obovoid60-70 gDark green or greenish brown with fine hairsGreen-yellow to yellow, circle of red around white core
Jintao (C6, WIB-C6, Jingold™)Long cylindric90 gYellow with brown hairsGreen-yellow to orange-yellow
Huayou (Panda™ Golden Kiwi)Ellipsoid90 gEllipsoidLight green to yellow
Ganmi No. 1 (Zaoxian
No. 1, FT-79-5)
Cylindric85 gGreen-brown to pale brown with soft hairsGreenish-yellow to yellow
Ganmi No. 3
(Jinfeng, FT 79-3)
Ellipsoid80-90 gYellow-brown or dark brown with short, fine hairsYellow
JinyanCylindrical100-110 gYellow brown with short, fine hairsYellow
Ganmi No. 2 (Kuimi, FY 79-1)Apple shaped100 gGreen-brown to dark brown with fine hairsYellow-green to yellow
Hort16AOvoid95-100gGreen-brown to brown with soft hairsYellow-green to bright yellow
WanhongCylindrical110-140gGreen-brown with rare hairsYellow-green to bright yellow
New ZealandCharm (Zespri® Charm)OvoidBrown with soft hairsYellow
Sungold (Zespri® Sungold)Brown with smooth skinYellow
Hort16A (Zespri®
Gold, Earligold)
Ovoid95-100gGreen-brown to brown with soft hairsYellow-green to bright yellow
ItalySoreli (Ac 171.76)Oblong> 100gBrown with sparse hairsYellow
JapanSanuki GoldSquat160-180gBrown with soft hairsBright yellow

A. chinensis cultivars developed for commercial production ().

There are two varieties accepted by The Plant List that include A. chinensis and A. chinensis var. setosa H.L.Li (The Plant List, 2013). The fruit of A. chinensis is the largest one in Actinidia genus, and it has the greatest economic, medicinal, and edible significance in terms of production and utilization. Its relevant pictures are showed in Figure 2. Generally, Chinese kiwifruit with a cross-sectional radius of about 3 cm is oval-shaped densely covered with yellowish-brown hairs. The flesh color of fruit skin is green to yellow, and the average fruit weight is 20–120 g. The fruit is a tasty, nutritious food that can be eaten fresh directly. Today, a range of kiwifruit processed products with the attractive eating quality and nutritional benefits has been developed including juice, preserved fruit, yogurt, wine, canned fruit, dried kiwi slices, fruit vegetable juice drinks, milk beverage, and vinegar. Apart from being a food and natural health product, the whole plant (fruits, branches and leaves, vines and roots) of A. chinensis has been used as traditional folk medicine in China (; Wei et al., 2018; ). The ripe kiwifruit, tastes sweet and sour, acts on the spleen, stomach, and kidney meridians, has improving properties on dyspepsia, loss of appetite, and vomiting. The branches and leaves have been used to treat arthronalgia, bleeding, empyrosis, and ulcer. The vine has appetizing, heat clearing, and wind-dampness dispelling effects and is used to treat indigestion, aundice, and urolithiasis. The root and bark of A. chinensis taste bitter and astringent, and they have various medical effects such as wind and heat dispelling, blood circulation improving, and detumescence properties, and are used for the treatment of rheumatoid arthritis, bruises, furuncle, swelling, filariasis, hepatitis, and dysentery (Xie, 1975). However, people with weak spleen and stomach should be cautious in taking A. chinensis (Xie, 1975). To date, only very few modern studies have been done on potential toxic and side effects of A. chinensis, which should be highlighted in future research.

Figure 2

The principal chemical composition of the whole plant of A. chinensis include polyphenol, triterpenoids and derivatives, carotenoids, polysaccharides, amino acids, vitamins, essential oils, and microelements. (Papunidze et al., 2001; ; Ma et al., 2017; Wang et al., 2017; Twidle et al., 2018). Among these ingredients, the main bioactive constituents are phenolic compounds, triterpenes, and the major nutritional composition are vitamin C, vitamin E, dietary fiber, and microelements, which make up a relatively significant share of the daily value (Table 2). Pharmacological results have revealed various promising bioactivities to A. chinensis including antitumor, antioxidant, anti-inflammatory, antimicrobial, immunoregulatory, hypolipemic and antidiabetic, cardiovascular protective, hypnotic effects, and ACE inhibitory activities (; Niu et al., 2016; Sun et al., 2017; Xia et al., 2017; ; ; ). Much of these bioactivities of A. chinensis are consistent with those observed in traditional folk medicine. More importantly, A. chinensis showed significantly antitumor and antioxidant properties, and these effects could be depended on the presence of a range of triterpenoids, polysaccharide, and phenolic compounds (; Wei et al., 2018; ). However, the information on the chemical and biological activities of A. chinensis is scattered. In this review, we intend to systematically summarize the recent advances in nutritional composition, chemistry, and biological activities of A. chinensis and also provide future research directions for better utilize and develop it as a sustainable crop.

Table 2

NutrientUnitKiwifruit 81gValue per 100 g
Proximates
Waterg66.7882.44
Energykcal5163
Proteing0.831.02
Total lipid (fat)g0.230.28
Carbohydrate, by differenceg12.7915.79
Fiber, total dietaryg1.11.4
Sugars, totalg9.9612.3
Minerals
Calcium, Camg1417
Iron, Femg0.170.21
Magnesium, Mgmg1012
Phosphorus, Pmg2025
Potassium, Kmg255315
Sodium, Namg23
Zinc, Znmg0.060.08
Vitamins
Vitamin C, total ascorbic acidmg130.7161.3
Thiaminmg0.0000.000
Riboflavinmg0.0600.074
Niacinmg0.1870.231
Vitamin B-6mg0.0640.079
Folate, DFEµg2531
Vitamin B-12µg0.060.08
Vitamin A, RAEµg11
Vitamin A, IUIU1923
Vitamin E (alpha-tocopherol)mg1.131.40
Vitamin D (D2 + D3)µg0.00.0
Vitamin DIU00
Vitamin K (phylloquinone)µg4.96.1
Lipids
Fatty acids, total saturatedg0.0530.065
Fatty acids, total monounsaturatedg0.0190.023
Fatty acids, total polyunsaturatedg0.0900.111
Fatty acids, total transg00
Cholesterolmg00

Nutritional composition of Zespri® sun-gold kiwifruit.

Source: USDA Food Composition Databases, https://ndb.nal.usda.gov/ndb/ Accessed on April, 2018.

Chemical Composition

Nutritional Composition

Chinese kiwifruit, known as the “king of fruits,” is a fruit with high-pulp juices, thick flesh, delicious taste, and rich nutrition and has a higher commercial and economic value. It is a rich source of various nutrients including vitamins, carbohydrate, sugar, minerals, amino acids, protein, fatty acids (e.g., linoleic acid), and carotenoids. Table 2 lists the nutritional composition of sun-gold kiwifruit reported from the USDA Food Composition Database (United States Department of Agriculture, USDA Food Composition Databases, 2018). Table 3 shows the chemical content of A. chinensis fruit (; ; Zhou et al., 2009; Xu et al., 2010; ; ; ; Xu et al., 2016; Twidle et al., 2018; Sivakumaran et al., 2018; Wei et al., 2018; Zhang et al., 2018). Of particular note, nutritional composition in kiwifruit is vitamin C (1.61 mg/g) and minerals K (3.15 mg/g). The average vitamin C content of Huayou, Jintao, Ganmi-1, Ganmi-2, Ganmi-3, Wuzhi-3, and Cuiyu cultivated in China are 1.59, 1.49, 0.86, 1.34, 0.97, 2.88, and 1.18 mg/g, respectively. Meanwhile, the vitamin C in SunGold was 1.61 mg/g edible flesh, followed by other varieties Sweet Green (1.5 mg/g) and green “Hayward” (0.85 mg/g) (Sivakumaran et al., 2018). Especially, the vitamin C content in kiwifruit is higher than that determined in lemon, orange, strawberry, and grapefruits (Ma et al., 2017).

Table 3

CompositionCultivar locationGenotypeMethodPlant partContentRef.
Vitamin C (ascorbic acid)ColomictaA. chinensisHPLCRipe fruits0.82 mg/g FW; 4.34 mg/g DWKvesitadze et al., 2001
Vitamin CCardinalA. chinensisHPLCRipe fruits0.74 mg/g FW; 4.30 mg/g DWKvesitadze et al., 2001
Vitamin CBrunoA. chinensisHPLCRipe fruits0.76 mg/g FW; 4.28 mg/g DWKvesitadze et al., 2001
Vitamin CMontiA. chinensisHPLCRipe fruits0.76 mg/g FW; 4.33 mg/g DWKvesitadze et al., 2001
Vitamin CPurpuriaA. chinensisHPLCRipe fruits0.78 mg/g FW; 4.27 mg/g DWKvesitadze et al., 2001
Vitamin CGaivardA. chinensisHPLCRipe fruits0.72 mg/g FW; 4.14 mg/g DWKvesitadze et al., 2001
Vitamin CGaivardA. chinensisHPLCSkin0.21 mg/g FW; 0.63 mg/g DWKvesitadze et al., 2001
Vitamin CGaivardA. chinensisHPLCPulp0.85 mg/g FW; 4.75 mg/g DWKvesitadze et al., 2001
Vitamin CGaivardA. chinensisHPLCCore0.48 mg/g FW; 2.67 mg/g DWKvesitadze et al., 2001
Vitamin CGaivardA. chinensisHPLCFresh juice0.55 mg/g FW; 3.44 mg/g DWKvesitadze et al., 2001
Vitamin CGaivardA. chinensisHPLCJuice after 24 h0.55 mg/g FW; 3.44 mg/g DWKvesitadze et al., 2001
Vitamin CShaanxi, ChinaHuayou2,6-dichloroindophenol titration methodRipe fruits1.59 mg/g FWMa et al., 2017
Total starch content in tissuePukekoheZespri® SunGold KiwifruitTotal starch assay kitOuter pericarp38.6% DWLi and Zhu, 2017
Total starch content in tissueAucklandGold9Total starch assay kitOuter pericarp51.8% DWLi and Zhu, 2017
Total starch content in tissueNew ZealandHort16ATotal starch assay kitOuter pericarp44.8% DWLi and Zhu, 2017
Apparent amylose contentPukekoheZespri® SunGold KiwifruitTotal starch assay kitOuter pericarp27.5% DWLi and Zhu, 2017
Apparent amylose contentAucklandGold9Total starch assay kitOuter pericarp24.5% DWLi and Zhu, 2017
Apparent amylose contentNew ZealandHort16ATotal starch assay kitOuter pericarp25.3% DWLi and Zhu, 2017
True amylose contentPukekoheZespri® SunGold KiwifruitTotal starch assay kitOuter pericarp17.8% DWLi and Zhu, 2017
True amylose contentAucklandGold9Total starch assay kitOuter pericarp15.7% DWLi and Zhu, 2017
True amylose contentNew ZealandHort16ATotal starch assay kitOuter pericarp15.5% DWLi and Zhu, 2017
Total dietary fibreNew ZealandHort 16AMegazyme methodpuree34.1 mg/g FWYuliarti et al., 2008
Total dietary fibreNew ZealandHort 16AMegazyme methodSkin and cores13.84% DWYuliarti et al., 2008
Insoluble dietary fibreNew ZealandHort 16AMegazyme methodPuree26.1 mg/g FWYuliarti et al., 2008
Insoluble dietary fibreNew ZealandHort 16AMegazyme methodSkin and cores11.39% DWYuliarti et al., 2008
Soluble dietary fibreNew ZealandHort 16AMegazyme methodPuree8 mg/g FWYuliarti et al., 2008
Soluble dietary fibreNew ZealandHort 16AMegazyme methodSkin and cores2.45% DWYuliarti et al., 2008
Nonstarch polysaccharideNew Zealandgold kiwifruitAcid extractionPomace77.59% DWYuliarti et al., 2015a
Nonstarch polysaccharideNew Zealandgold kiwifruitAcid extractionEarly-harvested
Fruits
69.14% DWYuliarti et al., 2015b
Nonstarch polysaccharideNew Zealandgold kiwifruitAcid extractionMain-harvested
fruits
64.49% DWYuliarti et al., 2015b
Nonstarch polysaccharideNew Zealandgold kiwifruitWater extractionPomace79.16% DWYuliarti et al., 2015a
Nonstarch polysaccharideNew Zealandgold kiwifruitWater extractionEarly-harvested
fruits
60.74% DWYuliarti et al., 2015b
Nonstarch polysaccharideNew Zealandgold kiwifruitWater extractionMain-harvested
fruits
63.77% DWYuliarti et al., 2015b
Nonstarch polysaccharideNew Zealandgold kiwifruitEnzymatic extractionPomace80.12% DWYuliarti et al., 2015a
Nonstarch polysaccharideNew Zealandgold kiwifruitEnzymatic extractionEarly-harvested
fruits
39.21% DWYuliarti et al., 2015b
Nonstarch polysaccharideNew Zealandgold kiwifruitEnzymatic extractionMain-harvested
fruits
64.02% DWYuliarti et al., 2015b
Total free amino acidsShaanxi, ChinaHort16AHitachi L-8900 amino acid analyzerRipe fruits8.31 mg/g FWMa et al., 2017
Total free amino acidsNew ZealandHort16AHitachi L-8900 amino acid analyzerRipe fruits8.01 mg/g FWMa et al., 2017
Total free amino acidsShaanxi, ChinaHuayouHitachi L-8900 amino acid analyzerRipe fruits7.15 mg/g FWMa et al., 2017
Total essential amino acidsShaanxi, ChinaHuayouHitachi L-8900 amino acid analyzerRipe fruits1.55 mg/g FWMa et al., 2017
Total essential amino acidsShaanxi, ChinaHort16AHitachi L-8900 amino acid analyzerRipe fruits2.09 mg/g FWMa et al., 2017
Total essential amino acidsNew ZealandHort16AHitachi L-8900 amino acid analyzerRipe fruits2.06 mg/g FWMa et al., 2017
Nonessential amino acidsNew ZealandHort16AHitachi L-8900 amino acid analyzerRipe fruits5.95 mg/g FWMa et al., 2017
Nonessential amino acidsShaanxi, ChinaHort16AHitachi L-8900 amino acid analyzerRipe fruits6.22mg/g FWMa et al., 2017
Nonessential amino acidsShaanxi, ChinaHuayouHitachi L-8900 amino acid analyzerRipe fruits5.60 mg/g FWMa et al., 2017
Total phenolicNew ZealandZespri® SunGold KiwifruitFolin-Ciocalteu methodThinned young fruits (20 days)∼80 mg GAE/g FDWJiao et al., 2019
Total phenolicShanxi ProvinceRed sunFolin-Ciocalteu methodRipe fruits0.87 mg GAE/g FWWang et al., 2018
Total phenolicShanxi ProvinceCuiyuFolin-Ciocalteu methodRipe fruits0.83 mg GAE/g FWWang et al., 2018
Total flavonoidNew ZealandZespri® SunGold KiwifruitUV/VisThinned young fruits (20days)∼30 mg CE/g FDWJiao et al., 2019
Total flavanolNew ZealandZespri® SunGold KiwifruitUV/VisThinned young fruits (20days)∼20 mg CE/g FDWJiao et al., 2019
Total flavonoidShanxi ProvinceRed sunUV/VisRipe fruits0.68 mg CE/g FWWang et al., 2018
Total flavonoidShanxi ProvinceCuiyuUV/VisRipe fruits0.68 mg CE/g FWWang et al., 2018
Total carotenoidNew ZealandHort16AHPLCMain-harvested
fruits
0.62 mg/100 g FWMcGhie and Ainge, 2002
Total chlorophyllsNew Zealandgold kiwifruitHPLCOuter Pericarp0.07 mg/100 g FWMontefiori et al., 2005
Total anthocyaninsNew ZealandHongyangHPLCPericarp2.99 mg/100 g FWMontefiori et al., 2005
Total organic acidsChinaHongyangHPLCRipe Fruits39.86 mg/g FWMontefiori et al., 2005
Total organic acidsChinaCuiyuHPLCRipe Fruits29.65 mg/g FWMontefiori et al., 2005

The nutritional composition or phytochemicals content of A. chinensis fruit.

The data show evidence that the sun-gold kiwifruit is high in carbohydrate (15.79%) and sugars (12.3%). The total starches contents were found for outer pericarp and core tissues ranged from 38.6% to 51.8% and 34.6% to 40.7% DW in three harvesting A. chinensis varieties, and the starches in core have higher amylose content (20.7%–23.3%) and enzyme susceptibility. However, the crystallinity degree, granule size, and gelatinization parameters of starches in core are somewhat lower (Li and Zhu, 2017). The kiwifruit peel contains a higher total pectin content (3.7%–4.2%) than that of pulp (1.6%–2.1%) (Meng et al., 2017). Xia et al. (2017) analyzed the polysaccharide from Hongyang using water extraction, followed by column chromatography, high performance gel permeation chromatography, HPLC, and Fourier transform infrared spectroscopy. The results indicated that the polysaccharide of Hogyang fruit consisted of the following monosaccharides: D-galactose (25.45%), D-galacturonic acid (25.25%), L-arabinose (20.51%), L-rhamnose (17.78%), D-glucose (6.14%), D-mannose (2.13%), D-xylose (1.03%), D-glucuronic acid (0.97%), and D-fucose (0.74%). These studies confirmed the utilization potential of Chinese kiwifruit as an incredibly healthy food and loaded with important nutrients and health benefits for human consumption.

Kiwifruit contained 18 free amino acids. Briefly, the total essential amino acid contents in Jintao, Hongyang, Huayou, and Hort16A cultivated in China are 2.59, 1.55, 2.0, and 2.09 mg/g FW, whereas the total essential amino acid in Hort16A cultivated in New Zealand was 2.06 mg/g FW. Meanwhile, Jintao, Hort16A and Hongyang also had a high amount of nonessential amino acid and total free amino acid. The most abundant amino acids detected in the kiwifruit were arginine, glutamic acid, lysine, phenylalanine, aspartic acid, and tyrosine (Ma et al., 2017). There are a number of total saturated lipids including C8:0, C10:0, C12:0, C14:0, C16:0, and C18:0 with the content of 1.49, 0.05, 0.14, 0.14, 0.09, 0.9, and 0.14 mg/g in edible flesh portion of A. chinensis. Meanwhile, the content of monounsaturated fatty acids C16:1 and C18:1 are 0.09 and 0.27 mg/g, and the polyunsaturated fatty acids C18:2 and C18:3 are 1.13 and 0.77 mg/g (). In fact, the kiwifruit seed oil is rich in unsaturated fatty acids (89.92%), notably linolenic acid, which accounts for 60.59% of total seed oil (Luan et al., 2017). Υ-tocopherol, Υ-tocotrienol, and ƍ-tocotrienol are identified in kiwifruit seed oil (). Besides, minerals like calcium, iron, potassium, magnesium, sodium, phosphorus, copper, manganese, zinc, iodine, selenium, and vitamins including vitamin A, β-carotene, lutein, zeaxanthin, riboflavin, niacin, pantothenic acid, vitamin B6, folate, tocopherol, vitamin E, vitamin K, and choline are identified in kiwifruit (Sivakumaran et al., 2018). Thus, these data suggest that kiwifruit is an interesting fruit for daily nutrition and energy suppliers.

Phytochemicals

A range of phytochemicals, including triterpenoids, saponins, and phenolic compounds (flavonoids, polyphenols, anthraquinones, and coumarins) varying in structures, were found and identified in A. chinensis. The major constituents isolated and identified in leaves and roots of A. chinensis are listed in Table 4.

Table 4

NONameCasFormulaSourceRef.
Triterpenoids
1.(2α,​3β,​4α)​-​2,​3,​23-​Trihydroxyursa-​12,​20(30)​-​dien-​28-​oic acid; Actinidic acid341971-45-7C30 H46 O5roots, unripe fruitJi and Liang, 1985; Lahlou et al., 2001
2.Maslinic acid4373-41-5C30 H48 O4roots
3.Ursolic acid acetate7372-30-7C32 H50 O4roots
4.23-​Hydroxyursolic acid94414-19-4C30 H48 O4roots
5.Ergosta-​4,​6,​8(14)​,​22-​tetraen-​3-​one19254-69-4C28 H40 Oroots
6.2α,​3β,​24-​Trihydroxyurs-​12-​en-​28-​oic acid143839-02-5C30 H48 O5rootsJi and Liang, 1985
7.2α,​3α,​24-​Trihydroxyurs-​12,​20(30)​-​dien-​28-​oic acid341503-22-8C30 H46 O5rootsJi and Liang, 1985
8.Pygenic acid A (3- epi-corosolic acid)52213-27-1C30 H48 O4roots
9.2α,3β-Dihydroxyurs-12-en-28,30-olide1198363-27-7C30 H46 O4rootsZhou et al., 2009
10.2α,3β,24-Trihydroxyurs-12-en-28,30-olide1198363-28-8C30 H46 O5rootsZhou et al., 2009
11.3β-Hydroxyurs-12,18-dien-28-oic acid14021-14-8C30 H46 O3rootsZhou et al., 2009
12.2α,3α,23-Trihydroxyursa-12, 20(30)-dien-28-oic acid1187824-97-0C30 H46 O5rootsZhou et al., 2009
13.2α,3α,19α,23, 24-Pentahydroxyurs-12-en-28-oic acid1309360-33-5C30 H48 O7rootsXu et al., 2010
14.Ursolic acid74984-66-0C30 H48 O3rootsXu et al., 2010
15.Pseudotaraxasterol464-98-2C30 H50 OrootsXu et al., 2010
16.2α,3α,23-Trihydroxyurs-12-en-28-oic acid103974-74-9C30 H48 O5rootsXu et al., 2010
17.2α,3β,24-Trihydroxyurs-12-en-28-oic acid475631-15-3C30 H48 O5rootsXu et al., 2010
18.2α,3β,19α, 23-Tetrahydroxyurs-12-en-28-oic acid70868-78-9C30 H48 O6rootsXu et al., 2010
19.2α,3α,19α, 24- Tetrahydroxyurs-12-en-28-oic acid 28-O-β-D-glucopyranoside153753-66-3C36 H58 O11rootsXu et al., 2010
20.Oleanolic acid acetate4339-72-4C32 H50 O4rootsZhu et al., 2013
21.Corosolic acid4547-24-4C30 H48 O4rootsZhu et al., 2013
22.Arjunic acid31298-06-3C30 H48 O5rootsZhu et al., 2013
23.Euscaphic acid53155-25-2C30 H48 O5rootsZhu et al., 2013
24.Oleanolic acid508-02-1C30 H48 O3roots
25.2α,​3α,​24-​Trihydroxyolean-​12-​en-​28-​oic acid150821-16-2C30 H48 O5roots
26.2α,​3α,​19α,​24-​Tetrahydroxyurs-​12-​en-​28-​oic acid153753-65-2C30 H48 O6roots
27.Jacoumaric acid63303-42-4C39 H54 O6roots
28.3β-​Hydroxystigmast-​5-​en-​7-​one2034-74-4C29 H48 O2rootsXu et al., 2016
29.(2α,​3α)​-​2,​3,​23,​24-​Tetrahydroxyurs-​12-​en-​28-​oic acid; 2α,​3α,​23,​24-​Tetrahydroxy ursan-​12-​en-​28-​acid143773-49-3C30 H48 O6rootsXu et al., 2016
30.Oleanan-​28-​oic acid, 12-​chloro-​2,​3,​13,​23-​tetrahydroxy-​, γ-​lactone, (2α,​3β,​4α,​12α)​-1309360-32-4C30 H47 Cl O5rootsXu et al., 2016
31.Urs-​13(18)​-​en-​28-​oic acid, 2,​3,​23-​trihydroxy-​, (2α,​3β,​4α)​-1980812-62-1C30 H48 O5rootsXu et al., 2016
32.Urs-​13(18)​-​en-​28-​oic acid, 2,​3,​19,​23-​tetrahydroxy-​, β-​D-​glucopyranosyl ester, (2α,​3β,​4α)​-1980812-63-2C36 H58 O11rootsXu et al., 2016
33.Pygenic acid B (2α,3α,24-trihydroxyurs-12-en-28-oic acid)89786-83-4C30 H48 O5rootsXu et al., 2016
34.2α,3α,23,24-Tetrahydroxyursa-12, 20(30)-dien-28-oic acid2220160-45-0C30 H46 O6rootsWei et al., 2018
35.2α,3β,23,24-Tetrahydroxyurs-12-en-28-oic acid116787-94-1C30 H48 O6rootsWei et al., 2018
36.2α,3β,23-Trihydroxyurs-12-en-28-oic acid114580-55-1C30 H48 O5rootsWei et al., 2018
37.3β-Hydroxyurs-12-en-28-oic acid77-52-1C30 H48 O3rootsWei et al., 2018
38.3β-Hydroxyolean-12-en-28-oic acid28283-45-6C35 H56 O7rootsWei et al., 2018
39.2β,3α,23-Trihydroxyurs-12-en-28-oic acid175132-32-8C30 H48 O5rootsWei et al., 2018
40.2β,3β,23-Trihydroxyurs-12-en-28-oic acid116348-15-3C3o H48 O5rootsWei et al., 2018
41.Spathodic acid 28-O-β-glucopyranoside870559-41-4C36 H58 O10root barksZhang et al., 2018
42.Fupenzic acid119725-20-1C3o H44 O5root barksZhang et al., 2018
Phenols
43.Planchol A883238-17-3C14 H14 O6roots
44.Planchol B883238-19-5C15 H16 O6roots
45.Planchol C883238-20-8C16 H18 O6roots
46.Planchol D883238-21-9C16 H16 O7roots
47.Benzeneacetic acid, 2-​[(3,​4-​dihydroxybenzoyl)​oxy]​-​4,​6-​dihydroxy-​, methyl ester911315-93-0C16 H14 O8leavesWurms and Cooney, 2006
48.Tachioside (methoxyhydroquinone-3-O-β-D-glucopyranoside)109194-60-7C13 H18 O8rootsZhou et al., 2010
49.Isotachioside (methoxyhydroquinone-1-O-β-D-glucopyranoside)31427-08-4C13 H18 O8rootsZhou et al., 2010
50.Vanillic acid121-34-6C8 H8 O4rootsZhou et al., 2010
51.1-O-(β-D-glucosyl)-2-[2-methoxy-4-(ω-hydroxypropyl)-phenoxy]-propan-3-ol68340-35-2C19 H30 O10rootsZhou et al., 2010
52.Protocatechualdehyde139-85-5C7 H6 O3roots
53.rel-​(1R,​2R)​-​1,​2-​Bis(4-​hydroxy-​3-​methoxyphenyl)​-​1,​3-​propanediol69887-40-7C17 H20 O6roots
54.rel-​(1R,​2S)​-​1,​2-​Bis(4-​hydroxy-​3-​methoxyphenyl)​-​1,​3-​propanediol69887-41-8C17 H20 O6roots
55.p-​Hydroxyl benzoic acid99-96-7C7 H6 O3roots
56.Chlorogenic acid327-97-9C16 H18 O9roots
57.Caffeic acid331-39-5C9 H8 O4roots
58.Cryptochlorogenic acid905-99-7C16 H18 O9roots
59.Neochlorogenic acid906-33-2C16 H18 O9roots
60.5-​O-​Coumaroylquinic acid87099-71-6C16 H18 O8roots
61.Dihydroxy-​dihydrochalcone-​2’-​O-​β-​D-​glucopyranoside23140-78-5C21 H24 O9rootsXu et al., 2016
Flavonoids
62.Epicatechin490-46-0C15 H14 O6unknownMichaud and Ane-Margail, 1977
63.epi-​Afzelechin24808-04-6C15 H14 O5unknownMichaud and Ane-Margail, 1977
64.Procyanidin C137064-30-5C45 H38 O18unknownMichaud and Ane-Margail, 1977
65.2-​(3,​4-​Dihydroxyphenyl)​-​3,​4-​dihydro-​4-​[(phenylmethyl)​thio]​-​2H-​1-​benzopyran-​3,​5,​7-​triol66052-27-5C22 H20 O6 SunknownMichaud and Ane-Margail, 1977
66.2,​2’-​Bis(3,​4-​dihydroxyphenyl)​-​3,​3’,​4,​4’-​tetrahydro-​4’-​[(phenylmethyl)​thio]​[4,​8’-​bi-​2H-​1-​benzopyran]​-​3,​3’,​5,​5’,​7,​7’-​hexol66293-44-5C37 H32 O12 SunknownMichaud and Ane-Margail, 1977
67.Afzelechin2545-00-8C15 H14 O5roots
68.Procyanidin B323567-23-9C30 H26 O12roots
69.Procyanidol B229106-49-8C30 H26 O12roots
70.Afzelechin-​(4α→8)​-​afzelchin101339-37-1C30 H26 O10roots
71.(2R,​2’R,​3R,​3’R,​4R)​-​3,​3’,​4,​4’-​Tetrahydro-​2,​2’-​bis(4-​hydroxyphenyl)​[4,​8’-​bi-​2H-​1-​benzopyran]​-​3,​3’,​5,​5’,​7,​7’-​hexol114715-48-9C30 H26 O10roots
72.Quercetin117-39-5C15 H10 O7fruitsLee et al., 2010
73.(+)-Catechin154-23-4C15H14O6rootsZhou et al., 2010
74.(-​)​-​Epicatechin-​5-​O-​β-​D-​glucopyranoside131831-20-4C21 H24 O11roots
Anthraquinones
75.Emodic acid478-45-5C15 H8 O7rootsJi and Liang, 1985
76.Hydroxyemodin481-73-2C15 H10 O6rootsJi and Liang, 1985
77.Emodin518-82-1C15 H10 O5rootsJi and Liang, 1985
78.Emodin 3-​methyl ether521-61-9C16 H12 O5rootsJi and Liang, 1985
79.Questin3774-64-9C16 H12 O5rootsJi and Liang, 1985
Coumarins
80.5-Hydroxy-6-methoxy-7-O-β-D-glucosyl coumarin141238-32-6C16 H18 O10rootsZhou et al., 2010
81.Fraxin524-30-1C16 H18 O10rootsZhou et al., 2010
82.Esculin531-75-9C15 H16 O9roots
83.Isofraxoside24778-11-8C16 H18 O10roots
Other compouds
84.β-​Sitosterol83-46-5C29 H50 OrootsJi and Liang, 1985
85.Butyl β-D-fructopyranoside67884-27-9C10 H20 O6rootsZhou et al., 2010
86.Lignoceric acid557-59-5C24 H48 O2roots
87.(-​)​-​Quinic acid γ-​lactone665-27-0C7 H10 O5roots
88.Stearyl-β-D-glucopyranoside76739-16-7C24 H48 O6roots
89.Daucosterol474-58-8C35 H60 O6roots
90.Indole-​3-​carboxylic acid771-50-6C9 H7 N O2roots
91.Stigmastane-3,6-diol112244-29-8C29 H52 O2roots
92.Sitoindoside Ⅰ18749-71-8C51 H90 O7roots

Chemical constituents isolated from A. chinensis.

Triterpenoids

Currently, triterpenoids have been the major research focus of A. chinensis components due to their promising antitumor properties. To date, 42 triterpenoids have been isolated and identified mainly from roots of A. chinensis. The commonly triterpenoids found in roots of A. chinensis are 12-en-28-oic acids of oleanane and ursane type. It is noteworthy that some of these triterpenoids (1-2, 7, 15-18, 21, 25-26, 29-30, and 34-40) have significant antitumor activity and deserve further research and development.

Phenolic Compounds

The phenolic compounds abundantly presented in different botanical parts of A. chinensis, and they have drawn increasing attention. These compounds include phenols, flavonoids, and flavanols are characterized by antitumor, antioxidant, and free radicals scavenging properties. HPLC-PAD and UPLC-QqQ-MS/MS-based methods have been used generally for the identification and quantification of these phenolic compounds (Ma et al., 2017; Jiao et al., 2019). The total phenolic, flavonoid, and flavanol contents from young A. chinensis kiwifruits “Zespri® SunGold Kiwifruit” growing in 20 days are 82.84 mg GAE/g FDW, 30.08 catechin/g equivalents FDW, and 20.20 catechin/g equivalents FDW. Meanwhile, the total phenolic, flavonoid, and flavanol contents presented in young A. chinensis kiwifruits growing in 60 days and mature kiwifruits are gradually decreasing, indicating polyphenol content possesses a decreasing pattern during fruit ripening (Jiao et al., 2019). The major chemical composition of phenolics detected in young “Zespri® SunGold Kiwifruit” are epicatechin, quercitrin, rutin, catechin, chlorogenic acid, ferulic acid, and vanillic acid. Based on UPLC-TOF/MS and UPLC-QqQ/MS method, Zhao et al., 2014 showed that the radix A. chinensis contained catechin derivatives, quinic acid derivatives, coumarin derivatives, caffeic acid, and p-coumaric acid (Zhao et al., 2014), showing that A. chinensis appears to be a good source of phenolics.

Volatile Compound and Essential Oil

The volatile components of A. chinensis var. chinensis fruit and flowers have been profiled by GC-MS. The dominant volatile components of eating-ripe firmness fruit are straight-chain aldehydes, alcohols, and esters, such as hexanal, decanal, octanal, nonanal, benzaldehyde, acetaldehyde, hex-E2-enal, 1,8-cineole, ethanol, hexanol, methyl butanoate, and ethyl octanoate (Wang et al., 2011). The volatile components of flowers included (3E,6E)-α-farnesene (38.8%), pentadecane (12.49%), (+)-germacrene D (8.55%), heptadecane (8.01%), (8Z)-heptadecene (7.72%), 2-phenylethano (4.69%), (3Z,6Z,9Z)-heptadecatriene (2.54%), and nonadecane (1.98%) (Twidle et al., 2018). It can be found that terpenes and straight chain alkenes were dominant in flowers of A. chinensis var. chinensis, which contained nearly >92% of the total ion counts. Importantly, many of these compounds possess strong and interesting aroma. However, the volatile components gradually changed during maturation. The essential oil of roots of A. chinensis have been profiled by GC-MS, and the major essential oil in roots are dodecane (29.39%), octane (5.16%), decane (2.94%), paeonal (2.81%), camphor (2.77%), n-decanoic acid (2.64%), 4-Methyldodecane (2.45%), undecane (2.16%), and linalool oxide (2.1%) (Yu et al., 2009).

Carotenoid and Chlorophyll

Carotenoids and chlorophyll are responsible for the color and attractiveness of kiwifruit fruits, as well as provide nutritional values. The carotenoids detected in the red-fleshed genotypes of A. chinensis fruit (Hort16A) are 9′-cis-neoxanthin, violaxanthin, antheraxanthin, lutein, zeaxanthin, β-cryptoxanthin, and β-carotene (McGhie and Ainge, 2002; Montefiori et al., 2005). Chlorophylls a and b are the dominant chlorophylls in Hort16A (McGhie and Ainge, 2002).

Quality Determination

Ripe kiwifruit is susceptible to environmental and itself. Usually, human sensory evaluation method can directly identify the fruit shape, color, surface, pulp, and flavor, but there is little information about swelling, ripening, and other agents present in fruit. Physical and chemical method including firmness and microbial are used effectively to determine the quality condition of kiwifruit. Some new instrument detection methods with accurate analysis ability such as GC, GC-MS, HPLC, UPLC-QqQ-MS/MS, and electronic nose combined with surface acoustic wave resonator are developed for the fruit and its products quality rapid analysis (Kvesitadze et al., 2001; Montefiori et al., 2005; Liu and Hui, 2015; Jiao et al., 2019). As to radix A. chinensis, the systematical method like UPLC-TOF/MS and UPLC-QqQ/MS is commonly applied to quality evaluation and active components analysis for A. chinensis (Zhao et al., 2014). Therefore, there are many high accurate analysis methods for rapid quality evaluation, but there is a lack of effective and standardized quality and safety standard for kiwifruit in China. Thus, there is an urgent demand for developing specific functional components and quality evaluation indicators for standardization and quality control of the fruit and its products.

Biological Activities

A. chinensis contains a range of bioactive compounds accounting for natural pharmacological properties including antitumor, antioxidant, anti-inflammatory, immunoregulatory, hypolipemic, antidiabetic, and cardiovascular protective activities, and most of these biological activities support its traditional use. Table 5 shows the major biological activities of compound or extract from A. chinensis.

Table 5

EffectCompound/ExtractClass of compoundsIn vitroIn vivoRef.
a1AShowed cytotoxicities against HepG2, A549, MCF-7, and SK-OV-3 with IC50 (48 h) values of 36.4, 40.37, 44. 3, and 16.33 μM.Wei et al., 2018
2AShowed cytotoxicities against A549, LoVo, and HepG2 with IC50 (48 h) values of 23.2, 6, and 34.9 μg/ml.Wei et al., 2018; Xu et al., 2010
7AShowed cytotoxicities against A549, MCF-7, SK-OV-3, and HeLa with IC50 (48 h) values of 16.63, 47.93, 22.91, and 15.27 μM.Wei et al., 2018
15AShowed cytotoxicities against LoVo, and HepG2 with IC50 (48 h) values of 31.1, and 33.9 μg/ml.Xu et al., 2010
16AShowed cytotoxicities against HepG2, MCF-7, SK-OV-3, and HeLa with IC50 (48 h) values of 12.22, 36.29, 45.13, and 49.71 μM.Wei et al., 2018
17AShowed cytotoxicities against A549, MCF-7, SK-OV-3, and HeLa with IC50 (48 h) values of 39.3, 11.01, 40.9 and 41.6 μM.Wei et al., 2018
18AShowed cytotoxicities against HepG2, A549, MCF-7, and HeLa with IC50 (48 h) values of 19.08, 32.08, 35.74, and 15.05 μM.Wei et al., 2018
21AInhibited HCC cells migration by targeting the VEGFR2/Src/FAK pathway.Ku et al., 2015
21AShowed cytotoxicities against A549, LoVo, and HepG2 with IC50 (48 h) values of 34.6, 2.9, and 9.2 μg/ml.Xu et al., 2010
25AShowed cytotoxicities against A549 and SK-OV-3 with IC50 (48 h) values of 42.74 and 25.83 μM.Wei et al., 2018
26AShowed cytotoxicities against A549 and HeLa with IC50 (48 h) values of 22.6 and 29.35 μM.Wei et al., 2018
29AShowed cytotoxicities against A549 and SK-OV-3 with IC50 (48 h) values of 31.3 and 37.9 μM.Wei et al., 2018
30AShowed cytotoxicities against A549, LoVo, and HepG2 with IC50 (48 h) values of 30.4, 31.1, and 25.5 μg/ml.Xu et al., 2010
34AShowed cytotoxicities against HepG2, A549, MCF-7, and HeLa with IC50 (48 h) values of 19.62, 18.86, 45.94 and 28.74 μM.Wei et al., 2018
35AShowed cytotoxicities against HepG2, MCF-7, and SK-OV-3 with IC50 (48 h) values of 11.76, 12, and 10.3 μM.Wei et al., 2018
36AShowed cytotoxicities against HepG2, MCF-7, and SK-OV-3 with IC50 (48 h) values of 14.22, 16.99, 28.9 μM.Wei et al., 2018
37AShowed cytotoxicities against HepG2, A549, MCF-7, and SK-OV-3 with IC50 (48 h) values of 48.4, 12.7, 11.2, and 31.7 μM.Wei et al., 2018
38AShowed cytotoxicities against A549, MCF-7, and SK-OV-3 with IC50 (48 h) values of 34.45, 42.2 and 49.55 μM.Wei et al., 2018
39AShowed cytotoxicities against HepG2 with IC50 (48 h) values of 32.5 μM.Wei et al., 2018
40AInhibited NCI-H460 cell proliferation by decreasing NF-κB expression. Showed cytotoxicities against SK-OV-3 with IC50 of 37.21 μM.; Wei et al., 2018
43BShowed cytotoxic activity against P-388 and A-549 cell lines with IC50 of 2.5 and 1.42 μM.
44BShowed cytotoxic activity against P-388 and A-549 cell lines with IC50 of 3.85 and 2.88 μM.
45BShowed cytotoxic activity against P-388 and A-549 cell lines with IC50 of 5.02 and 4.5 μM.
46BShowed cytotoxic activity against P-388 and A-549 cell lines with IC50 of 3.52 and 2.6 μM.
bvitamin E (ƍ-Tocomonoenol)CRadical-scavenging capacities on DPPH and O2 were 23.96 and 29.20%; hydroperoxide conjugate dienes formation and TBARS were 26.88 and 46.70%.
vitamin E (α-tocopherol)CRadical-scavenging capacities on DPPH and O2 were 25.21 and 27.07%. hydroperoxide conjugate dienes formation and TBARS were 33.08 and 53.01%.
vitamin E (ƍ-tocopherol)CRadical-scavenging capacities on DPPH and O2 were 23.4 and 29.273%; hydroperoxide conjugate dienes formation and TBARS were 25.48 and 43.2%.
polymeric proanthocyanidins fractionated by methanol- water (80:20, v/v)D
IC50 for DPPH, ABTS were 105.3 and 74.7μg/ml; FRAP values is 7.4 mM VCE/g.
polymeric proanthocyanidins fractionated by acetone-methanol-water (40:40:20, v/v/v)DIC50 for DPPH, ABTS were 67.7 and 60.1 μg/ml; FRAP values is 9.6 mM VCE/g.
polymeric proanthocyanidins fractionated by acetone-water (70:30, v/v)DIC50 for DPPH, ABTS were 69.3 and 39.5 μg/ml; FRAP values is 9.6 mmol VCE/g.
polyphenols compounds (55.10 mg GAE/g DW), contain p-hydroxybenzoic acid, protocatechuic acid, and p-coumaric acid.B10-50 µg/ml showed DPPH free radical scavenging.
seed oil rich in unsaturated fatty acid from HongyangEIC50 for DPPH, HO·scavenging capacity were 31.4 and 1.09; FRAP and ORAC values were 107.3 mg and 1.09 Trolox/kg.
seed oil rich in unsaturated fatty acid from HuayouEIC50 for DPPH, HO·scavenging capacity were 33.7 and 1.12; FRAP and ORAC values were 72.0 mg and 1.72 Trolox/kg.
seed oil rich in unsaturated fatty acid from Hort 16AEIC50 for DPPH, HO·scavenging capacity were 32.4 and 1.04; FRAP and ORAC values were 3.3 mg and 1.69 Trolox/kg.
water-soluble polysaccharidesF0.5-3 mg/ml showed DPPH radical scavenging activity, protection of the HEK 293 cells from H2O2 damage.Zhang et al., 2015
cpolymeric proanthocyanidins fractionated by methanol- water (80:20, v/v)DInhibited monophenolase and diphenolase activity with IC50 of 180.2 and 390.2 μg/ml.
polymeric proanthocyanidins fractionated by acetone-methanol- water (40:40:20, v/v/v)DInhibited monophenolase activity with IC50 of 80.1 and 192.6 μg/ml.
polymeric proanthocyanidins fractionated by acetone-water (70:30, v/v)DInhibited monophenolase activity with IC50 of 48.9 and 64.9 μg/ml.
dpolyphenols compounds (55.10 mg GAE/g DW), contain p-hydroxybenzoic acid, protocatechuic acid, p-coumaric acid, etc.B20, 40, 60 µg/ml for 12 h inhibit IL-1β and TNF-α secretion in LPS-induced RAW 264.7 cells.
seed oil rich in fatty acidsE1.0 and 3.0 ml/kg/day for 84 days down-regulated TNF-α, IL-6, IL-1β, COX-2 and iNOS in high-fat diet induced mice.Qu et al., 2019
water-soluble polysaccharidesF50, 100, 200, 300 μg/ml reduce NO production of RAW 264.7 cells, and 100, 200 and 300 μg/ml enhanced phagocytic activity of RAW 264.7 cells.Zhang et al., 2015
eseed oil rich in fatty acidsE1.0 and 3.0 mL/kg/day for 84 days decreased bodyweight and ameliorated serum TC, TG, HDL-C, and LDL-C levels in high-fat diet treated mice.Qu et al., 2019
fflavonoid-rich extractGIC50 of ACE inhibitory activity was 12.81 mg/ml.
gactinidinHEnhanced gastric protein α-, β-, and κ-caseins digestion under simulated gastric conditions.Kaur et al., 2010
hthaumatin-like proteinHInhibited Botrytis cinereal, Mycosphaerella arachidicola and Coprinus comatus, inhibit HIV-1 reverse transcriptase.Wang and Ng, 2002
i41A100 μg/ml inhibited tobacco mosaic virus with inhibition rate of 45.70%.Zhang et al., 2018
j21A50 μg/ml showed inhibitory effects on CYP2C19, CYP2D6, and CYP3A4 with 69.3,71.0 and 39.3 of remaining activity.Xu et al., 2016
25A10 μg/ml showed inhibitory effects on CYP2C9, CYP2C19, CYP2D6, and CYP3A4 with 28.3, 59.9, 31.8, and 37.1% of remaining activity.Xu et al., 2016
30A10 μg/ml showed inhibitory effects on CYP2C9 and CYP3A4 with 67.1 and 9.8% of remaining activity.Xu et al., 2016
33A50 μg/ml showed inhibitory effects on CYP2C19 and CYP3A4 with 75.0 and 35.0 of remaining activityXu et al., 2016
61B10 μg/ml showed inhibitory effects on CYP2C9 with 69.0% of remaining activity.Xu et al., 2016

Biological activities of compounds or extracts of A. chinensis.

a, Antitumor effects; b, Antioxidant activity; c. Antityrosinase activity; d, Anti-inflammatory activity; e, Hypolipidemic activity; f, ACE inhibitory activity; g, Digestive activity; h, Antifungal activity; i, Antiviral activity; j, Cytochrome P450 enzyme inhibitory activity. A, Triterpenoid; B, Phenols; C, Vitamin; D, Proanthocyanidins; E, Oil; F, Polysaccharides; G, Flavonoids; H, Protein.

Antitumor Activity

Crude extracts, fractions, and isolated compounds from A. chinensis exhibited strong inhibition against tumor growth in various forms of human cancer cells. These cancer cells were hepatocellular carcinoma cells HepG2 (Xu et al., 2010; Zuo et al., 2012), Hep3B, SMMC7721, MHCC97L, MHCC97H, HCCLM3 (), HL-7702 (), Huh7 (), lung cancer cells NCI-H460 and NCI-H1299 (Lv et al., 2018), colon cancer cells HT-29, LoVo, and SW480, pharyngeal carcinoma cell lines Fadu and HEP-2, gastric cancer cells SGC-7901, BGC-823, MKN-49P, and MFC, as well as other cancer cells like A549, P-388, MCF-7, SK-OV-3, and HeLa (; Xu et al., 2010; Xu et al., 2010; Zuo et al., 2012; Shen et al., 2014; Xia et al., 2017; ; Wang et al., 2017; Wei et al., 2018). These reported antitumor activities are consistent with the traditional usage such as liver cancer, lung cancer, colon cancer, esophagus cancer, and gastric cancer.

A large number of triterpenoids in roots of A. chinensis especially those with carboxyl group showed marked cytotoxicity against various types of cancer cells in vitro. Especially, compounds 1-2, 7, 15-18, 21, 25-26, 29-30, 34-40, and 43-46 exhibited remarkable antitumor activity against on A549, HepG2, LVOV, MCF-7, HeLa, and/or HepG2 in vitro (Table 5). Additionally, the polysaccharide of Hogyang fruit showed notable inhibitory against tumor cells lines SGC7901, MCF-7, HT29, HepG2, and NCI-H460 with IC50 of were 0.28, 0.31, 0.58, 0.64, and 0.65 µM, respectively (Xia et al., 2017). In vivo, a polysaccharide isolated from the roots of A. chinensis showed antitumor activity by prolonging the life of EAC or P388 cells-induced tumor mice and inhibiting the DNA synthesis in EAC cells (Lin, 1988). Early treatment and long-term treatment with water extracts of roots from A. chinensis with 2 g/kg/day strongly attenuated the malignant behavior of HCC in mice by decreasing DLX2 expression ().

The molecular mechanism of the inhibition against tumor growth and the apoptosis promoting of the fractions and isolated compounds were due to downregulate DLX2 gene expression and VEGFR2/Src/FAK pathway, inhibit cholesterol metabolism by upregulating PCSK9 signaling pathway, regulate gene encoding laminin subunit beta-3 pathways, and decreased NF-κB and EP3 expression. Meanwhile, the antioxidation and anti-inflammation are also important and possible mechanisms. The triterpenoids, polysaccharides, and phenolic compounds were identified as the major bioactive compounds in the extract from A. chinensis roots with antitumor properties (; Wei et al., 2018), which provides new way to search for treating cancers with natural therapeutic compounds. Overall, A. chinensis has prominent antitumor potential and has a good health benefit for people, however, the further in vivo and clinical studies on antitumor properties of A. chinensis are needed for confirmation.

Antioxidant Activity

Antioxidant activity of bioactive compounds of A. chinensis have been the mostly studied by various in vitro and in vivo assays. These in vitro assays consisted of both chemical and biological assays like DPPH, ABTS, FRAP, HO·, ORAC, oxidative stress by H2O2, and lipid oxidation (; Lee et al., 2015; Hwang et al., 2017; ). The in vivo assays were based on SOD, GSH, ALT, AST, oxidative DNA damage, and lipid oxidation (Iwasawa et al., 2011; Sun et al., 2017; ; Wang et al., 2018). The above results showed that A. chinensis is a good source of bioactive compounds with antioxidant properties to various extents. The antioxidant capacities of kiwifruit are greatly attributed to polyphenols, flavonoid, unsaturated fatty acid, and vitamin C. In addition, the different extraction methods, different plant parts, and genetic diversity of kiwifruit demonstrated different antioxidant activities. The peel showed the strongest antioxidant activity, followed by the pulp and the core. The antioxidant activity of kiwifruit peel was mainly depended on plenty of phenolic substances, and the antioxidant activity of the pulp was mainly attributed to the existence of a large amount of vitamin C (Zhang et al., 2016). The seed oil of Hort 16A and Hongyang are attractive materials rich in unsaturated fatty acid demonstrated radical scavenging capacities for FRAP, DPPH, HO·, and ORAC with IC50 of 3.3 mgTrolox/kg, 32.4 mg/ml, 1.04 mg/ml, 1.69 mgTrolox/kg, and 107.3 mgTrolox/kg, 31.4 mg/ml, 1.09 mg/ml, 1.99 mgTrolox/kg, respectively (). The radical scavenging capacities of fresh and freeze-dried Hort 16A rich in phenolics and flavonoids for ABTS, DPPH, and ORAC were 8.8, 8.8, 98.3, and 6.0, 5.0, and 40.3 mg VCE/g, respectively (Hwang et al., 2017). The radical scavenging capacities of Red sun and Cuiyu rich in phenolics and flavonoids for ABTS, DPPH, ORAC, and FRAP were 1.35, 1.01, 10.78, 1.50 and 1.32, 0.9, 8.87, 1.28 mg VCE/g, respectively (Wang et al., 2018). Oral administration of kiwifruit protected lymphocytes against oxidative DNA damage, inhibit lipid oxidation in mice, increased SOD and GSH, and lowered ALT and AST levels in the patients (Sun et al., 2017). Therefore, A. chinensis possess confirmed antioxidant capacity and it seems that appropriate extraction methods, appropriate genotypes, and plant parts can be screened to maximize the antioxidant properties of A. chinensis.

Anti-Inflammatory Activity

Anti-inflammatory activity of A. chinensis has been proved in vivo and in vitro models. On high-fat diet-induced obese C57BL/6 mice models, consecutive consumption the seeds oil of A. chinensis with 1.0 and 3.0 ml/kg·bw ameliorated obesity-induced inflammation by down-regulating the mRNA expression of related to inflammation adipokines, such as TNF-α, IL-6, IL-1β, COX-2, and iNOS (Qu et al., 2019). The aqueous and ethyl acetate extracts demonstrated anti-inflammatory activity in inflammatory bowel disease models of the IL-10 gene-deficient mice (). In patients with type-2 diabetes mellitus, the fruit juice of A. chinensis showed preventative activity on inflammation by activating Keap1 and Nrf2 via upregulating miR-424 (Sun et al., 2017). On the cellular level, polyphenols mainly composed of protocatechuic acid, p-hydroxybenzoic acid, p-coumaric acid, caffeic acid, and ferulic acid from seeds of A. chinensis at concentration of 40 and 60 μg/ml for 12 h decreased the secretion of pro-inflammatory cytokines IL-1β and TNF-α in LPS-induced RAW 264.7 cells (). Therefore, the anti-inflammatory potential A. chinensis seeds mainly depend on the synergetic effect of these polyphenols, and it may be used to prevent a variety of inflammation related diseases.

Antibacterial Activity

All the extracts including skin, pulp, seeds, and stems showed bactericidal against Staphylococcus aureus, Streptococcus pyogenes, S. faecalis, Salmonella typhi, Proteus mirabilis, Pseudomonas aeruginosa, Escherichia coli, and Klebsiella pneumonia. The skin and pulp extracts showed inhibition activity against S. aureus and S. pyogenes with MIC values of 8 and 4 μg/ml, but they showed moderate inhibition activity against S. faecalis, S. typhi, P. mirabilis, P. aeruginosa, E. coli, and K. pneumonia with MIC values ranging from 16 to 128 μg/ml. The leaves and stems extract just inhibited S. pyogenes and P. aeruginosa with MIC values of both 64 and 32 μg/ml. The seeds extracts showed an exclusively bacteriostatic activity against these selected strains of bacteria with MIC values of between 1 and 8 μg/ml (). Polyphenol from seeds of A. chinensis showed significant bactericidal against Bacillus cereus, B. subtilis, Shigella flexneri, and Salmonella Typhi, and bacteriostatic against B. thuringiensis. We can find that the antimicrobial activity of the polyphenol extract on gram-positive bacteria is higher than that of gram-negative bacteria (). Therefore, kiwifruit seeds are potential food processing material for their antimicrobial activity.

Immunoregulatory Activity

Consumption of the aqueous extracts of whole fresh fruit of Hort16Aat 375 mg/kg for 12 days enhanced both innate and acquired immunity in cholera vaccine and tetanus/diphtheria vaccine models in Balb/c mice, showing a beneficial effect on healthy (Shu et al., 2008). The homopolysaccharide derivatived by O-sulfation from the roots of A. chinensis at concentration of 10 and 50 μg/ml activated phagocytic activity and increased NO production of RAW 264.7 macrophages, and the activity of sulfated polysaccharides is strongly related to the degree of the sulfation (Niu et al., 2016), and treatment with 50-300 μg/ml water-soluble polysaccharides dose-dependently stimulated NO production and phagocytic activity of RAW 264.7macrophages (Zhang et al., 2015). It remains to clarify the detailed mechanism of immunoregulatory activity and the responsible compositions for this valid action.

Hypolipemic and Antidiabetic Activities

Administered the seed oil of A. chinensis rich in fatty acids at 1.0 and 3.0 ml/kg·bw daily over 12 consecutive weeks significantly lowered bodyweight gain, inguinal fat tissue weight, and the accumulation of TC, TG, HDL-C, and LDL-C in liver of the high-fat diet-induced obese C57BL/6 mice. Meanwhile, long-term consumption of the seed oil of A. chinensis up-regulated the expression of thermogenesis-related genes like PPAR-γ, UCP1, PGC1-α, and PRDM16, down-regulated FAS expression, and altered the gut microbiota by decreasing the Firmicutes-to-Bacteroidetes ratio (Qu et al., 2019). In addition, the seed oil from A. chinensis supplementation improved insulin resistance and alleviated hyperglycemia by reducing HOMA-IR index and blood glucose in high fat diet-induced obese mice (Qu et al., 2019). Thus, the lipid lowering potential of A. chinensis seed provide a basis theory for food industries.

Cardiovascular Protective Effects

In H9c2 rat cardiac myocytes cells induced by hypoxia in cardiomyocytes treated with angiotensin II, treatment with 1.25 and 2.5 mg/ml polysaccharide of A. chinensis alleviated cardiac hypertrophy, decreased mitochondrial dysfunction and reduced cardiomyocytes apoptosis by decreasing the apoptosis-associated genes expression like mitochondria associated-1 and caspases3/8/9, and cleaving caspases-3/8/9. Additionally, the protective effects of polysaccharide against hypoxia-induced apoptosis may be attributable to inactivate the ERK1/2 and PI3K/AKT signaling pathways (Wang et al., 2018). The polysaccharide of A. chinensis can be potentially used in the treatment of heart disease. However, it is noteworthy that polysaccharide at high dose (10 mg/ml) suppressed the cardiomyocytes viability.

Hypnotic Effects

Oral administration of ethanol extracts from A. chinensis peel at dose of 250, 500, and 1,000 mg/kg dose-dependently decreased sleep latency and increased sleep duration in pentobarbital-treated mice. Especially, the sequentially partitioned with ethyl acetate fraction rich in flavonoids (1.63 mg QE/g) at 250 mg/kg exert significantly hypnotic effects and this sedative-hypnotic activity could be inhibited by GABAA-BZD receptor antagonist flumazenil. The flavonoids may be attributable to hypnotic activity via allosteric GABAA-BZD receptor modulation, but the precise mechanisms and the existing individual flavonoids are needed to be evaluated in the future (Yang et al., 2013).

Ace Inhibitory Activity

The 70% aqueous acetone extracts partitioning with hexane rich in flavonoid from Hort 16A dose-dependently inhibited ACE activity with IC50 of 12.81 mg/ml using a fluorescence-based biochemical assay. LC-MS/MS showed that the higher total phenolic and total flavonoid contents are identified in this extract. UPLC-MS/MS showed that polyphenols (231.32 µg/g DW) in the extract are mainly flavonols, flavanols, and phenolic acids. Specifically, quercetin-3-O-galactoside (205.19 µg/g DW), quercetin-3-O-glucoside (0.45 µg/g DW), quercetin-3-O-rhamnoside (0.61 µg/g DW), quercetin-3-O-rutinoside (0.29 µg/g DW), epicatechin (5.15 µg/g DW), catechin (0.75 µg/g DW), epigallocatechin (0.61 µg/g DW), phloridzin (2.03 µg/g DW), and isoferulic acid (15.12 µg/g DW) are major compounds in the extract (). These compounds could be responsible for the observed in vitro ACE inhibitory activity of Hort 16A fruit, though the active compounds identifying and in vivo animal studies remain to be investigated and conducted.

Dermatological Activity

The raw polysaccharides with >90% carbohydrate and 5.2% residual protein from the fresh fruit of A. chinensis at 10 μg/ml showed a significantly proliferation-promoting on cell proliferation rates of HaCaT cell line and primary keratinocytes (NHK), and it also significantly promoted proliferation of human dermal fibroblasts at 132 and 198 μg/ml. Meanwhile, treatment of the polysaccharides at 200 μg/ml significantly stimulated ATP-synthesis, promoted mitochondrial activity and energy metabolism of HaCaT keratinocytes, and significantly increased collagen synthesis in dermal skin equivalents (). Kiwifruit pericarp proanthocyanidins mainly contained B-type propelargonidins, procyanidins, procyanidins gallate, and prodelphinidins showed strongly inhibition activity on tyrosinase, indicating that it can be used as whitening agents ().

Cytochrome P450 Enzyme Inhibitory Activities

Cytochrome P450 system in liver plays an important role in drug metabolism. It transforms drug from hydrophobic to hydrophilic, which is easier to excrete. The 90% EtOH extract of A. chinensis root at 50 μg/ml exhibited inhibition activities on CYP2C9, CYP2D6, and CYP3A4 in human liver tissue with the 69.0, 76.3, and 53.3% of remaining activity, respectively. The inhibitory effect of the crude extract could be largely attributed to the presence of triterpenoids (Xu et al., 2016). It is worth noting that the combination of crude extracts or these triterpenoids with other medical herbs or drugs may lead to drug interaction with cytochrome CYPs at pharmacokinetic and pharmacodynamic levels, which indicates that people should cautiously consume A. chinensis fruit when taken medicine.

Processing and Utilization

Chinese kiwifruit is a very high nutritional value of nourishing and consumers’ favorite fruit, which has shown application potential in food, medicine, and health products industry. China is the largest kiwifruit producer in the world. In 2016, kiwifruit production in China reached 2.41 million tons per year, accounting for 56.0% of the world’s total kiwifruit production (United Nations Food and Agriculture Organization, 2016). To date, a series of commercially available products has been processed due to abundant nutrient substance and claimed health benefits. These Chinese kiwifruit related products include sliced fruit, juice, preserved fruit, yogurt, wine, canned fruit, dried kiwi slices, fruit vegetable juice drinks, biscuits, milk beverage, whipped cream, baked goods, vinegar, and oil capsule. Furthermore, various different parts of A. chinensis showed different uses. Briefly, the leaves contain protein, starch, and polyphenols, which may be developed as an excellent source of natural products. The beautiful and fragrant of Chinese kiwifruit flowers rich in honey juice and volatiles can be used as high-quality honey source. Kiwifruit peel residue as sources of high-quality pectin can be used as functional ingredient for food products. Chinese kiwifruit seeds rich in essential fatty acids, protein, and dietary fiber can be used in food and health products industry (Xie, 1975; ). The roots and barks contain ursolic acid, oleanolic acid, and quercetin, which have antitumor effect against liver cancer, lung cancer, gastric cancer, esophageal cancer, colorectal cancer, and cervical cancer (; Xu et al., 2010; Wei et al., 2018). The different parts of A. chinensis are widely used as pharmaceutical raw materials in medicine for prevention and treatment of tumors. In addition, the various claimed nutritional and pharmacological properties including strong antitumor, antioxidation, and anti-inflammatory potential of various extracts or active compounds of A. chinensis indicated that they could be further developed for functional food with added-commercial value or effective and safe drug formulations.

Storage Methods

Chinese kiwifruit has a short postharvest life because of fast softening and serious decay. Preservation of Chinese kiwifruit for prolonged periods is particularly important. Freezing and frozen storage is currently the most common method, which can effectively inhibit the softening of kiwifruit and prolong its postharvest life. However, kiwifruit is cold-sensitive and very susceptible to chilling injury when storage at the temperature between −2°C and 2.5°C for a long time (; Ma et al., 2014). Interestingly, dipped by water for 10 min at 45°C to low temperature storage can prevent chilling injury development to kiwifruit. Meanwhile, the kiwifruit pretreated at 45°C and then stored at 0°C for 90 days showed higher firmness and soluble solids content, and MDA content and lipoxygenase activity in kiwifruit are reduced. However, pretreated at 20 and 55°C were ineffective at alleviating chilling tolerance (Ma et al., 2014). Various other treatments including preharvest calcium chloride sprays (), putrescine (Yang et al., 2016), preharvest chilling (Sfakiotakis et al., 2005), and gradual cooling (Yang et al., 2013) have also been used to alleviate chilling injury in kiwifruit.

After harvest, kiwifruit is highly perishable, and its nutritional ingredients and quality decline rapidly due to the influence of internal biochemical reactions and external environment. The modified atmosphere packaging, chitosan, 1-methylcyclopropene, ClO2, ozone, tea polyphenols, protein, lipid composite film, oxalate, salicylic acid, and citric acid have been used individually or combined to alleviate physicochemical quality changes for postharvest of kiwifruit (). The ozone treatment induced the ripening process, delayed the microbial growth, and influenced the content of vitamin C, polyphenols, flavonoids, and carotenoids (). The chitosan combined with salicylic acid treatment during storage at room temperature for 14 days provides a significantly effective preservative effect by delayed vitamin C and soluble solids decomposition, inhibiting moisture loss and acidity change, and maintaining texture and surface color of Chinese kiwifruit in 14 days of storage at room temperature ().

Conclusions

Chinese kiwifruit and related products are increasingly popular throughout the world due to the remarkably economic, nutritional, and health benefits values. It is a good source of phenolic compounds, vitamin C, carbohydrates, sugars, amino acids, and minerals. Of particular note in kiwifruit is vitamin C and minerals K. The phenolic compounds present in Chinese kiwifruit are organic acids and flavonoids, and fruit peel and flesh, leaf, vine, and roots also contain a variety of these phenolic components. The major components of the roots are triterpenoids characterized by 12-en-28-oic acids of oleanane and ursane type. Terpenes, straight chain alkenes, alcohols, and esters were dominant volatile components in flowers and roots of A. chinensis. These chemical compounds render the A. chinensis with a range of sensory quality, nutritional, and pharmacological properties as proved by in vitro and in vivo studies. The claimed biological activity of isolated compounds, fractions, or crude extracts include antitumor, antioxidant, anti-inflammatory, antibacterial, immunoregulatory, hypolipemic, antidiabetic, and cardiovascular protective effects. Of particular note is that these claimed biological activities such as antitumor, antioxidant, and immunoregulatory may be greatly attributed to the existence of triterpenoids, polyphenols, flavonoid, polysaccharide, unsaturated fatty acid, and vitamin C. These findings suggest that Chinese kiwifruit can be useful in the prevention and treatment of pathologies associated to cancer, oxidative stress, and aging.

There are also research opportunities to better development, utilization, and protection kiwifruit for human consumption. Cytochrome P450 inhibitory activities, toxicity analysis, qualitative and quantitative metabolite research, effective and standardized quality standard building, and clinical studies should be encouraged to conducted for safe daily consumption. Meanwhile, the synergism and attenuation effects, metabolic behavior of various ingredients, as well as the in vivo and molecular mechanisms studies responsible for the observed biological properties should be conducted. It is also found that some of the A. chinensis cultivars were only supported by a few studies, and confirmative studies should be conducted to verify their health effects. Apart from the fruit, other plant parts of kiwifruit including leaves and roots should also be explored for effective utilization. The effective method and technology for the storage and preservation of kiwifruit during preharvest and postharvest remain to be explored to avoid the frequent chilling damage, soft rot, and mildew, and also decrease and improve the change of the chemical profile and bioactivity properties during storage.

Statements

Author contributions

XC and YM obtained the literatures. JF, ZZ, and XH wrote the manuscript. XH, LH, and YL gave ideas and edited the manuscript. All authors approved the paper for publication.

Conflict of interest

The authors declare that the research was conducted in the absence of any commercial or financial relationships that could be construed as a potential conflict of interest.

Abbreviations

A549, Human alveolar basal epithelial cells; ABTS, 2′-azino-bis (3-ethylbenzthiazoline-6-sulfonic acid; ACE, Angiotensin converting enzyme; ALT, Alanine aminotransferase; AST, Aspartate aminotransferase; CE, Catechin equivalents; COX-2, Cyclooxygenase-2; CYP2C9, Cytochrome P450 2C9; CYP2D6, Cytochrome P450 2D6; CYP3A4, Cytochrome P450 3A4; CYPs, Cytochrome P450; DLX2, Distal-less-like homeobox protein; DPPH, 2,2-diphenyl-1-picrylhydrazyl; DW, Dry weight; EP3, Prostaglandin E2 receptor subtype 3; ERK1/2, Extracellular regulated protein kinases; FAS, Fatty acid synthase; FDW, Freeze-dried weight; FRAP, Ferric ion reducing antioxidant power; FW, flesh weight; GABA-BZD, γ-aminobutyric acid-benzodiazepine; GAE, Gallic acid equivalents; GC-MS, Gas chromatography-mass spectrometer; GSH, Glutathione; HaCaT, Human immortalized keratinocytes; HCC, Hepatocellular carcinoma; HDL-C, High density lipoprotein cholesterol; HEK 293, Human embryonic kidney 293 cells; HepG2, Liver hepatocellular cells; HO·, Hydroxyl radical; HOMA-IR, Homeostasis model assessment for insulin resistance; HPLC, High-performance liquid chromatography; IC50, Half maximal inhibitory concentration; IL-1β, Interleukin-1β; IL-6, Interleukin-6; iNOS, Inducible nitric oxide synthase; Keap1, Kelch-like ECH-associated protein 1; LC-MS/MS, Liquid chromatography-tandem mass spectrometry; LDL-C, Low density lipoprotein cholesterol; LoVo, Colorectal cancer cell line; MCF-7, Human breast adenocarcinoma cell line; MDA, Malondialdehyde; MIC, Minimum inhibitory concentration; NCI-H460, Large cell lung cancer cells; NF-κB, Nuclear factor-kappa B; NO, Nitric oxide; Nrf2, Nuclear factor (erythroid-derived 2)-like 2; ORAC, Oxygen radical absorbance capacity; P-388, Mouse leukemia cells; PGC1-α, Peroxisome proliferator-activated receptor gamma coactivator 1-alpha; PI3K/AKT, Phosphatidylinositol 3-kinase/protein kinase B; PPAR-γ, Peroxisome proliferators-activated receptors; PRDM16, PR domain containing 16; QE, Quercetin equivalents; RAW 264.7, Mouse leukaemic monocyte macrophage cell line; SK-OV-3, Human ovarian epithelial cancer cells; SOD, Superoxide dismutase; TC, Total cholesterol; TG, Triglyceride; TNF-α, Tumor necrosis factor alpha; UCP1, Uncoupling protein 1; UPLC-MS/MS, Ultra-high-performance liquid chromatography-tandem mass spectrometry; UPLC-QqQ-MS/MS, Ultra-high-performance hydrophilic interaction liquid chromatography-triple quadrupole tandem mass; UPLC-TOF/MS, Ultra-performance liquid chromatography quadrupole-time of flight mass spectrometry; USDA, United States Department of Agriculture; UV/Vis, Ultraviolet-visible spectroscopy; VCE, Vitamin C equivalents; VEGFR2/Src/FAK, Vascular endothelial growth factor receptor 2/Src/focal adhesion kinase.

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Summary

Keywords

Actinidia chinensis, nutritional composition, chemistry, pharmacological properties, antitumor, antioxidant

Citation

He X, Fang J, Chen X, Zhao Z, Li Y, Meng Y and Huang L (2019) Actinidia chinensis Planch.: A Review of Chemistry and Pharmacology. Front. Pharmacol. 10:1236. doi: 10.3389/fphar.2019.01236

Received

10 April 2019

Accepted

27 September 2019

Published

30 October 2019

Volume

10 - 2019

Edited by

Monique S.J. Simmonds, Royal Botanic Gardens, Kew, United Kingdom

Reviewed by

Marinella De Leo, University of Pisa, Italy; Jianping Chen, Shenzhen Traditional Chinese Medicine Hospital, China

Updates

Copyright

*Correspondence: Xirui He,

This article was submitted to Ethnopharmacology, a section of the journal Frontiers in Pharmacology

Disclaimer

All claims expressed in this article are solely those of the authors and do not necessarily represent those of their affiliated organizations, or those of the publisher, the editors and the reviewers. Any product that may be evaluated in this article or claim that may be made by its manufacturer is not guaranteed or endorsed by the publisher.

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