Fang Chien-Liang, Wang Yiwei, Tsai Kevin H-Y, Chang Hsin-I
Division of Plastic and Reconstructive Surgery, Department of Surgery, Ditmanson Medical Foundation Chia-Yi Christian Hospital, Chiayi City, Taiwan.
Burns Research Group, ANZAC Research Institute, Concord Hospital, University of Sydney, Concord, NSW, Australia.
Front Pharmacol. 2018 Mar 6;9:155. doi: 10.3389/fphar.2018.00155. eCollection 2018.
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 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 model to study the lipogenesis via using adipogenic differentiation medium (ADM). Baicalein, isolated from , is one of the flavonoids to inhibit adipocyte differentiation due to high antioxidant activity . 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.
人类皮肤的真皮层含有大量成纤维细胞，这些细胞负责产生细胞外基质（ECM），维持皮肤的完整性、弹性并促进伤口愈合。此前，一项研究表明，位于真皮下层的真皮成纤维细胞能够转化为皮肤脂肪层，因此成纤维细胞的脂肪生成可能会改变真皮的结构和弹性。在本研究中，Hs68人真皮成纤维细胞被用作模型，通过使用成脂分化培养基（ADM）来研究脂肪生成。从[植物名称未给出]中分离出的黄芩苷是一种黄酮类化合物，因其具有高抗氧化活性而能抑制脂肪细胞分化。为了开发一种适合黄芩苷（一种水溶性差的药物）的制剂，大豆磷脂酰胆碱（SPC）被用于制备载黄芩苷脂质体，以提高药物的生物利用度。我们的结果表明，脂质体包裹的黄芩苷可保护细胞活力，并提高Hs68成纤维细胞的细胞摄取效率。在ADM刺激的Hs68成纤维细胞中，脂质积累、甘油三酯合成以及脂肪生成酶（FABP4和LPL）的基因表达显著增加，但随后被脂质体包裹的黄芩苷所抑制。此外，脂质体包裹的黄芩苷下调了ADM诱导的TNF-α表达及相关炎症因子。通过ADM诱导的脂肪生成，弹性蛋白、I型和III型胶原蛋白的蛋白表达显著增加，而脂质体包裹的黄芩苷可下调ADM诱导的ECM蛋白合成。综上所述，我们发现脂质体包裹的黄芩苷可通过抑制脂肪生成酶和炎症反应，抑制ADM诱导的Hs68成纤维细胞中的脂质积累和ECM形成。脂质体包裹的黄芩苷可能具有改善伤口愈合和修复皮肤损伤后皮肤结构的潜力。
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