Phloroglucinol derivatives from Hypericum species induce in vitro proliferation of cells involved in the wound healing process

The genus Hypericum (Hypericaceae) is a recognized source of therapeutic agents, being some species widely used due to their wound healing properties. In a previous study, south Brazilian species H. caprifoliatum, H. carinatum, H. connatum, H. myrianthum and H. polyanthemum demonstrated potential to induce proliferation of keratinocytes. In the present study, the effect of phloroglucinol derivatives isolated from Hypericum on cell proliferation of human keratinocytes, fibroblasts and stem cells was investigated. The best results, determined by the MTT assay, were achieved with cariphenone B at concentrations of 0.01 and 0.1 µM (122.3% and 114%, respectively) on HaCaT cells. Uliginosin B was able to induce the proliferation of mesenchymal stem cells (129% at 10 µM) and MRC5 fibroblasts (152.5% at 5 µM). These findings confirm the capacity of phloroglucinol derivatives to induce the in vitro cellular proliferation and reinforce the importance of Hypericum species as potential sources of wound healing compounds.

金丝桃属（Hypericum，Hypericaceae）是公认的药用活性成分来源，部分物种因其伤口愈合特性而被广泛应用。既往研究显示，巴西南部的H. caprifoliatum、H. carinatum、H. connatum、H. myrianthum及H. polyanthemum等物种，已被证实具备诱导角质形成细胞增殖的潜力。本研究针对从金丝桃属植物中分离得到的间苯三酚衍生物（phloroglucinol derivatives），对人角质形成细胞、成纤维细胞及干细胞的增殖影响展开了探究。经MTT检测法（MTT assay）验证，卡里芬酮B（cariphenone B）在0.01与0.1 µM浓度下对HaCaT细胞的促增殖效果最佳，分别可达122.3%与114%；乌里吉诺辛B（Uliginosin B）则可诱导间充质干细胞（mesenchymal stem cells）在10 µM浓度下增殖率达129%，以及MRC5成纤维细胞（MRC5 fibroblasts）在5 µM浓度下增殖率达152.5%。上述研究结果证实了间苯三酚衍生物具备诱导体外细胞增殖（in vitro cellular proliferation）的能力，同时进一步凸显了金丝桃属植物作为伤口愈合活性成分潜在来源的重要价值。