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睡茄内酯的抗癌作用:药理特性的计算机模拟预测

Anticancer Effects of Withanolides: In Silico Prediction of Pharmacological Properties.

作者信息

Silva Gustavo Werneck de Souza E, Marques André Mesquita, Sampaio André Luiz Franco

机构信息

Laboratório de Farmacologia Molecular, Farmanguinhos, Fundação Oswaldo Cruz (FIOCRUZ), Rua Sizenando Nabuco 100, Manguinhos, Rio de Janeiro 21041-250, Brazil.

Laboratório de Tecnologia Para Biodiversidade em Saúde/TecBio, Farmanguinhos, Fundação Oswaldo Cruz (FIOCRUZ), Rua Sizenando Nabuco 100, Manguinhos, Rio de Janeiro 21041-250, Brazil.

出版信息

Molecules. 2025 Jun 4;30(11):2457. doi: 10.3390/molecules30112457.

Abstract

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.

摘要

睡茄内酯是一类具有丰富生物活性的天然存在的C-28麦角甾烷甾体内酯,其成员是抗肿瘤药物开发的有前途的候选物。睡茄内酯的ADMET性质在很大程度上仍然未知,而计算机模拟预测可以在突出这些特性以促进药物开发方面发挥关键作用,从而缩短药物先导物开发所花费的时间和资源。在这项工作中,评估了有前景的抗肿瘤睡茄内酯的ADMET性质。每个化学结构都提交给了预测工具:SwissADME、pkCSM-药代动力学、admetSAR v2.0和Molinspiration化学信息学。结果表明其具有良好的胃肠道吸收率、无法穿过血脑屏障、CYP3A4代谢、不抑制其他P450细胞色素、与核受体有高相互作用以及低毒性。还预测了其对药代动力学转运体的抑制作用和一些生态毒性。这表明了口服药物开发的可行性,副作用可能性较低。

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