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山核桃叶五糖苷 I 通过改善皮肤屏障和抑制 5α-还原酶来抗寻常痤疮。

Anti-acne vulgaris effect including skin barrier improvement and 5α-reductase inhibition by tellimagrandin I from Carpinus tschonoskii.

机构信息

Laboratory of Pharmacognosy and Natural Product derived Medicine, College of Pharmacy, Chung-Ang University, Seoul, 156-756, Republic of Korea.

出版信息

BMC Complement Altern Med. 2019 Nov 21;19(1):323. doi: 10.1186/s12906-019-2734-y.

Abstract

BACKGROUND

Carpinus tschonoskii (CT) has been previously studied for various activities in the improvement of skin diseases. In the present study, we examined the in vitro anti-acne vulgaris (AV) effect of CT leaves (CTL) and tellimagrandin I (TI), one of the main ellagitannins from CT, including skin barrier improvement and 5α-reductase inhibitory activity.

METHODS

To test the anti-AV activities of CTL and TI, firstly, anti-oxidative and anti-inflammatory activities including DPPH radical scavenging activity, nitric oxide (NO) inhibitory activity, and cytokines [interleukin (IL)-6 and IL-8] were tested. Skin barrier improvement experiments were tested using developing cornified envelope (CE) formation, and filaggrin mRNA expression level was determined by RT-PCR. The 5α-reductase inhibitory activity was determined by measuring the testosterone levels in rat liver microsomes.

RESULTS

CTL and TI showed potent anti-oxidative activity and anti-inflammatory activities. Especially, the cytokine production inhibitory activities of TI were found to be similar to the positive control, epigallocatechin gallate (EGCG). CTL and TI enhanced the CE formation and filaggrin mRNA expression levels and showed potent activities compared to that in the positive control, 1.5 mM Ca. In additionally, CTL and TI showed 5α-reductase inhibitory activities in a dose-dependent manner.

CONCLUSION

The results showed that CTL and TI inhibit AV endogenous factors such as 5α-reductase and inflammatory cytokines and affect exogenous factors such as developing skin barrier function (CE and filaggrin levels). Therefore, CTL and TI may be plant-derived agent, promising in the treatment of acne vulgaris.

摘要

背景

胡颓子(CT)已被用于研究各种改善皮肤疾病的活性。在本研究中,我们研究了胡颓子叶(CTL)和Tellimagrandin I(TI)的体外抗寻常痤疮(AV)作用,TI 是胡颓子中的主要鞣花单宁之一,包括改善皮肤屏障和 5α-还原酶抑制活性。

方法

为了测试 CTL 和 TI 的抗 AV 活性,首先测试了其抗氧化和抗炎活性,包括 DPPH 自由基清除活性、一氧化氮(NO)抑制活性和细胞因子[白细胞介素(IL)-6 和 IL-8]。通过测定 RT-PCR 中的颗粒蛋白前体(filaggrin)mRNA 表达水平,检测了开发中的角蛋白包膜(CE)形成的皮肤屏障改善实验。5α-还原酶抑制活性通过测量大鼠肝微粒体中的睾酮水平来确定。

结果

CTL 和 TI 表现出强大的抗氧化和抗炎活性。特别是,TI 的细胞因子产生抑制活性与阳性对照表没食子儿茶素没食子酸酯(EGCG)相似。CTL 和 TI 增强了 CE 的形成和颗粒蛋白前体 mRNA 的表达水平,与阳性对照 1.5mM Ca 相比,表现出更强的活性。此外,CTL 和 TI 表现出剂量依赖性的 5α-还原酶抑制活性。

结论

结果表明,CTL 和 TI 抑制 AV 内源性因素,如 5α-还原酶和炎症细胞因子,并影响外源性因素,如发育中的皮肤屏障功能(CE 和颗粒蛋白前体水平)。因此,CTL 和 TI 可能是植物来源的治疗寻常痤疮的有希望的药物。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/8fbb/6869165/ae21867d0df0/12906_2019_2734_Fig1_HTML.jpg

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