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Original Research ARTICLE Provisionally accepted The full-text will be published soon. Notify me

Front. Pharmacol. | doi: 10.3389/fphar.2019.01020

Micro-PET imaging demonstrates 3-O-β-D-glucopyranosyl platycodigenin as an effective metabolite affects permeability of cell membrane and improves dosimetry of [18F]-phillygenin in lung tissue

 Fukui Shen1, Wenbo Wu1, Man Zhang1, Xiaoyao Ma1,  Qingxin Cui1, Zhongyao Tang1, 2, Hao Huang2,  Tiantian Tong2,  LeeFong Yau2,  ZhiHong Jiang2,  Yuanyuan Hou1* and  Gang Bai1*
  • 1College of Pharmacy, Nankai University, China
  • 2State Key Laboratory of Quality Research in Chinese Medicines, Macau University of Science and Technology, China

Platycodon grandiflorum, as a traditional medicinal plant, is commonly used in the treatment of pulmonary disease. Platycodon saponins are proposed as active ingredients. However, the role of secondary saponin metabolites (SSM) in the traditional use of Platycodon has not yet been fully clarified. In this study, [18F]-phillygenin ([18F]-PH) probe was synthesized and thereby used as a tracer for micro-positron emission tomography scanning to explore the effects of platycodon saponins. The membrane permeability with different SSM was evaluated in vitro based on the dye carrying capacity of fluorescein isothiocyanate. The results showed that total platycodon saponins improved the dosimetry of [18F]-PH in the lung tissue, and an SSM named 3-O-β-D-glucopyranosyl platycodigenin (GPD682) appreciably changed the distribution of drugs both in vitro and in vivo. We propose that GPD682 could be utilized as an important ingredient to help drug delivery to the lung tissue and improve the treatment of respiratory disease.

Keywords: Platycodon grandiflorum, secondary saponin, 3-O-β-D-glucopyranosyl platycodigenin, [18F]-phillygenin, micro-positron emission tomography

Received: 19 Jun 2019; Accepted: 12 Aug 2019.

Copyright: © 2019 Shen, Wu, Zhang, Ma, Cui, Tang, Huang, Tong, Yau, Jiang, Hou and Bai. This is an open-access article distributed under the terms of the Creative Commons Attribution License (CC BY). The use, distribution or reproduction in other forums is permitted, provided the original author(s) and the copyright owner(s) are credited and that the original publication in this journal is cited, in accordance with accepted academic practice. No use, distribution or reproduction is permitted which does not comply with these terms.

* Correspondence:
Prof. Yuanyuan Hou, College of Pharmacy, Nankai University, Tianjin, China, houyy@nankai.edu.cn
Prof. Gang Bai, College of Pharmacy, Nankai University, Tianjin, China, gangbai@nankai.edu.cn