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Front. Pharmacol. | doi: 10.3389/fphar.2018.00155

Liposome-Encapsulated Baicalein Suppressed Lipogenesis and Extracellular Matrix formation in Hs68 Human Dermal Fibroblasts

Chien-Liang Fang1,  Kevin H. Tsai2, Yiwei Wang3 and  Chang Hsin-I2*
  • 1Division of Plastic and Reconstructive Surgery, Department of Surgery, Ditmanson Medical Foundation Chia-Yi Christian Hospital, Taiwan
  • 2Department of Biochemical Science and Technology, National Chiayi University, Taiwan
  • 3Burns Research Group, Anzac Research Institute, Australia

The dermis of human skin contains large numbers of fibroblasts that are responsible for the production of the extracellular matrix (ECM) that supporting skin integrity, elasticity and wound healing. Previously, an in vivo study demonstrated that dermal fibroblasts siting in the lower dermis are capable to convert into skin adipose layer and hence fibroblast lipogenesis may vary the structure and elasticity of dermis. In the present study, Hs68 human dermal fibroblasts were utilized as an in vitro model to study the lipogenesis via using adipogenic differentiation medium (ADM). Baicalein, isolated from Scutellaria baicaleinsis, is one of the flavonoids to inhibit adipocyte differentiation due to high antioxidant activity in vitro. In order to develop a suitable formulation for baicalein (a poorly water-soluble drug), soybean phosphatidylcholine (SPC) was used to prepare baicalein-loaded liposomes to enhance drug bioavailability. Our results demonstrated that liposome-encapsulated baicalein protected cell viability and increased cellular uptake efficiency of Hs68 fibroblasts. Lipid accumulation, triglyceride synthesis and gene expressions of lipogenesis enzymes (FABP4 and LPL) were significantly increased in ADM-stimulated Hs68 fibroblasts but subsequently suppressed by liposome-encapsulated baicalein. In addition, ADM-induced TNF-α expression and related inflammatory factors was down-regulated by liposome-encapsulated baicalein. Through ADM-induced lipogenesis, the protein expression of elastin, type I and type III collagens increased remarkably, whereas liposome-encapsulated baicalein can down-regulate ADM-induced ECM protein synthesis. Taken together, we found that liposome-encapsulated baicalein can inhibit ADM-induced lipid accumulation and ECM formation in Hs68 fibroblasts through the suppression of lipogenesis enzymes and inflammatory responses. Liposome-encapsulated baicalein may have the potential to improve wound healing and restore skin structure after skin injury.

Keywords: Baicalein, Liposomes, human dermal fibroblast, adipogenic differentiation, Lipogenesis

Received: 09 Nov 2017; Accepted: 13 Feb 2018.

Edited by:

Sherry Y. Wu, The University of Queensland, Australia

Reviewed by:

Amirali Popat, The University of Queensland, Australia
CRISTIAN RODRIGUEZ-AGUAYO, University of Texas MD Anderson Cancer Center, United States  

Copyright: © 2018 Fang, Tsai, Wang and Hsin-I. 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 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: Dr. Chang Hsin-I, National Chiayi University, Department of Biochemical Science and Technology, 300 University Road, Chiayi, 300 University Road, Chiayi, 600, -- Select One --, Taiwan, hchang@mail.ncyu.edu.tw