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毛蕊花和锯叶棕提取物对双氢睾酮诱导的人LNCaP前列腺上皮细胞中前列腺特异性抗原分泌的抑制作用。

Inhibition of the DHT-induced PSA secretion by Verbascum xanthophoeniceum and Serenoa repens extracts in human LNCaP prostate epithelial cells.

作者信息

Marcoccia D, Georgiev M I, Alipieva K I, Lorenzetti S

机构信息

Istituto Superiore di Sanità - ISS, Department of Food Safety and Veterinary Public Health, Food and Veterinary Toxicology Unit, viale Regina Elena 299, 00161 Rome, Italy; University Roma Tre, Department of Biology, Viale Guglielmo Marconi 446, I-00146 Rome, Italy.

Bulgarian Academy of Sciences, The Stephan Angeloff Institute of Microbiology, Laboratory of Applied Biotechnologies, Ruski 139 Boulevard, 4000 Plovdiv, Bulgaria.

出版信息

J Ethnopharmacol. 2014 Aug 8;155(1):616-25. doi: 10.1016/j.jep.2014.06.003. Epub 2014 Jun 11.

Abstract

ETHNOPHARMACOLOGICAL RELEVANCE

Verbascum xanthophoeniceum is a mullein plant, typical of Balkan region and some parts of Turkey, traditionally used as phytotherapeutic agent due to its anti-inflammatory properties. It is rich in phenylethanoid and iridoid metabolites whose anti-inflammatory properties are under characterization.

MATERIALS AND METHODS

The role of Verbascum xanthophoeniceum crude methanolic extract and its isolated phenylethanoid glycoside verbascoside have been evaluated, in comparison to a saw palmetto extract, on a human in vitro model of androgen-regulated prostate epithelium, the LNCaP cell line. Cytotoxicity and DHT-induced free and total PSA secretion have been thoroughly studied.

RESULTS

We have found that similar to saw palmetto, Verbascum xanthophoeniceum extract and its isolated phenylethanoid glycoside verbascoside have no cytotoxicity in human LNCaP prostate epithelial cells, whereas an inhibitory effect on the DHT-induced free and total PSA secretion, a recognized anti-androgen like activity, has been shown in case of both Verbascum xanthophoeniceum extract and pure verbascoside. Furthermore, in the absence of the endogenous androgen DHT, an androgen-like activity in Verbascum xanthophoeniceum is detectable as it is for saw palmetto, suggesting that a mixed androgen-antiandrogen activity is present.

CONCLUSIONS

For the first time, Serenoa repens and Verbascum xanthophoeniceum extracts have shown an absence of cytotoxicity and an inhibitory effect on DHT-induced PSA secretion in an in vitro model of human prostate epithelium, whereas the phenylethanoid glycoside verbascoside appeared to explain only part of the Verbascum xanthophoeniceum inhibitory activity on PSA secretion.

摘要

民族药理学相关性

黄褐毛蕊花是一种毛蕊花属植物,原产于巴尔干地区和土耳其部分地区,因其抗炎特性而传统上用作植物治疗剂。它富含苯乙醇和环烯醚萜类代谢物,其抗炎特性正在研究中。

材料与方法

与锯叶棕提取物相比,在雄激素调节的前列腺上皮细胞系LNCaP细胞的体外人模型上,评估了黄褐毛蕊花粗甲醇提取物及其分离出的苯乙醇苷类毛蕊花糖苷的作用。对细胞毒性以及双氢睾酮(DHT)诱导的游离和总前列腺特异性抗原(PSA)分泌进行了深入研究。

结果

我们发现,与锯叶棕类似,黄褐毛蕊花提取物及其分离出的苯乙醇苷类毛蕊花糖苷对人LNCaP前列腺上皮细胞无细胞毒性,而黄褐毛蕊花提取物和纯毛蕊花糖苷均显示出对DHT诱导的游离和总PSA分泌有抑制作用,这是一种公认的抗雄激素样活性。此外,在缺乏内源性雄激素DHT的情况下,黄褐毛蕊花中可检测到类似锯叶棕的雄激素样活性,表明存在混合的雄激素 - 抗雄激素活性。

结论

首次发现锯叶棕和黄褐毛蕊花提取物在人前列腺上皮细胞体外模型中无细胞毒性,且对DHT诱导的PSA分泌有抑制作用,而苯乙醇苷类毛蕊花糖苷似乎仅解释了黄褐毛蕊花对PSA分泌抑制活性的一部分。

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