Withanolides的抗癌作用:药理性质的计算机预测。

IF 4.2 2区 化学 Q2 BIOCHEMISTRY & MOLECULAR BIOLOGY
Gustavo Werneck de Souza E Silva, André Mesquita Marques, André Luiz Franco Sampaio
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引用次数: 0

摘要

Withanolides是一类天然存在的具有丰富生物活性的C-28麦角甾体内酯,其成员是抗肿瘤药物开发的有希望的候选者。withanolides的ADMET性质在很大程度上仍然是未知的,而在计算机上的预测可以在药物开发中发挥关键作用,突出这些特征,缩短开发药物先导物的时间和资源。在这项工作中,评估了有前途的抗肿瘤的金甾醇类化合物的ADMET特性。每个化学结构提交到预测工具:SwissADME, pkcms -药代动力学,admetSAR v2.0和Molinspiration化学信息学。结果表明,该药物具有良好的胃肠道吸收率,不能穿过血脑屏障,CYP3A4代谢,不抑制其他P450细胞色素,与核受体高度相互作用,毒性低。还预测其对药代动力学转运蛋白的抑制作用和一定的生态毒性。这证明了口服药物开发的可行性,副作用的可能性很低。
本文章由计算机程序翻译,如有差异,请以英文原文为准。
Anticancer Effects of Withanolides: In Silico Prediction of Pharmacological Properties.

Withanolides are a class of naturally occurring C-28 ergostane steroidal lactones with an abundance of biological activities, and their members are promising candidates for antineoplastic drug development. The ADMET properties of withanolides are still largely unknown, and in silico predictions can play a crucial role highlighting these characteristics for drug development, shortening time and resources spent on the development of a drug lead. In this work, ADMET properties of promising antitumoral withanolides were assessed. Each chemical structure was submitted to the prediction tools: SwissADME, pkCSM-pharmacokinetics, admetSAR v2.0, and Molinspiration Cheminformatics. The results indicate a good gastrointestinal absorption rate, inability to cross the blood-brain barrier, CYP3A4 metabolization, without inhibition of other P450 cytochromes, high interaction with nuclear receptors, and a low toxicity. It was also predicted for the inhibition of pharmacokinetics transporters and some ecotoxicity. This demonstrates a viability for oral drug development, with low probabilities of side effects.

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来源期刊
Molecules
Molecules 化学-有机化学
CiteScore
7.40
自引率
8.70%
发文量
7524
审稿时长
1.4 months
期刊介绍: Molecules (ISSN 1420-3049, CODEN: MOLEFW) is an open access journal of synthetic organic chemistry and natural product chemistry. All articles are peer-reviewed and published continously upon acceptance. Molecules is published by MDPI, Basel, Switzerland. Our aim is to encourage chemists to publish as much as possible their experimental detail, particularly synthetic procedures and characterization information. There is no restriction on the length of the experimental section. In addition, availability of compound samples is published and considered as important information. Authors are encouraged to register or deposit their chemical samples through the non-profit international organization Molecular Diversity Preservation International (MDPI). Molecules has been launched in 1996 to preserve and exploit molecular diversity of both, chemical information and chemical substances.
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