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塞内加尔番荔枝中的儿茶素是潜在的勃起功能障碍抑制剂:用于男性性功能增强的意义。

Catechin from Anonna senegalensis is a Potential Inhibitor of Erectile Dysfunction: Implication for Its Use in Male Sexual Enhancement.

机构信息

Faculty of Basic Medical Sciences, Department of Physiology, Ladoke Akintola University of Technology, Ogbomosho, P.M.B. 4000, Nigeria.

Faculty of Basic Medical Sciences, College of Medicine, Ekiti State University, Ado-Ekiti, Nigeria.

出版信息

Appl Biochem Biotechnol. 2023 Aug;195(8):4936-4964. doi: 10.1007/s12010-023-04557-z. Epub 2023 Apr 28.

Abstract

Erectile dysfunction (ED) is a major challenge for men. The drugs for its treatment are associated with side effects. Hence, in phytomedicinal research, where Anonna senegalensis (A. senegalensis) is a candidate with abundant phytochemicals possessing various pharmacological properties, but the sex-enhancing phytochemical is elusive in the literature. This study aimed to understand the molecular interaction of its potent molecule mediating male sexual enhancement. A library of 69 compounds from A. senegalensis was docked against the ED-targeted proteins. Sildenafil citrate was used as the reference standard. Thereafter, the lead compound was screened for drug-likeness by applying the Lipinski rule of 5 (RO5), pharmacokinetic properties, and bioactivity using SwissADME and Molinspiration web servers, respectively. The results show catechin as the lead phytochemical compound with a stronger binding affinity for most of the proteins of ED. Also, catechin demonstrates good compliance with the RO5, great pharmacokinetic profiles, and could be said to be a polypharmacological molecule with good bioactivity scores. The research findings unravel the potential of catechin (a phytochemical belonging to the flavonoids class) from A. senegalensis leaf as a potential male sexual enhancement molecule via its high binding affinity for most erectile dysfunction-targeted proteins. They may require further toxicity and therapeutic evaluations in vivo.

摘要

勃起功能障碍(ED)是男性面临的主要挑战。治疗这种疾病的药物会产生副作用。因此,在植物药研究中,非洲木瓜(A. senegalensis)是一种候选植物,它含有丰富的具有多种药理学特性的植物化学物质,但在文献中仍未发现具有增强性功能的植物化学物质。本研究旨在了解介导男性性增强的其有效分子的分子相互作用。从非洲木瓜中提取了 69 种化合物的文库,并对 ED 靶向蛋白进行了对接。枸橼酸西地那非被用作参考标准。此后,通过应用 Lipinski 规则 5(RO5)、瑞士 ADME 和 Molinspiration 网络服务器分别进行药物相似性、药代动力学特性和生物活性筛选,筛选出先导化合物。结果表明,儿茶素是一种主要蛋白具有较强结合亲和力的植物化学物质。此外,儿茶素与 RO5 具有良好的一致性,具有良好的药代动力学特征,可以说是一种具有良好生物活性评分的多效性分子。研究结果表明,来自非洲木瓜叶的儿茶素(属于类黄酮类的一种植物化学物质)作为一种潜在的男性性增强分子,具有很高的结合亲和力,可针对大多数 ED 靶向蛋白。它们可能需要进一步进行体内毒性和治疗评估。

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