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利用计算机模拟筛选和鉴定印度人参的植物成分作为BRCA1突变体的有效抑制剂:一种乳腺癌治疗方法。

In silico screening and identifying phytoconstituents of Withania somnifera as potent inhibitors of BRCA1 mutants: A therapeutic against breast cancer.

作者信息

Panda Smita Manjari, Tripathy Umakanta

机构信息

Department of Physics, Indian Institute of Technology (Indian School of Mines), Dhanbad 826004, Jharkhand, India.

Department of Physics, Indian Institute of Technology (Indian School of Mines), Dhanbad 826004, Jharkhand, India.

出版信息

Int J Biol Macromol. 2024 Dec;282(Pt 3):136977. doi: 10.1016/j.ijbiomac.2024.136977. Epub 2024 Oct 28.

DOI:10.1016/j.ijbiomac.2024.136977
PMID:39490493
Abstract

Breast CAncer gene 1 (BRCA1) is an anti-oncogene that helps the cell repair damaged DNA and preserve genetic material. BRCA1 also acts as a cell growth suppressor and produces tumor suppressor gene (TSG) proteins, i.e., BRCA1 protein. Remarkably, BRCA1 mutations account for 90% of hereditary breast cancer and a majority of hereditary ovarian cancer. Hence, we have considered three mutants of BRCA1 (R1699W, R1699Q, T1700A) in this study and adopted an in-silico approach to find the best possible phytochemical to inhibit these mutated proteins, enabling early breast cancer diagnosis. Perceiving the importance, many natural molecules from ancient medicinal plants are considered for molecular docking. Our findings suggest that though many molecules bind actively with the receptor's active site, the top three phytoconstituents (27-Deoxy-14-hydroxywithaferin A, Withacoagulin, Somniferanolide) of Withania somnifera, commonly known as Ashwagandha, have high binding affinities and suitable pharmacokinetic properties, making these natural compounds potential drug candidates. Further, molecular dynamics (MD) simulation and the binding free energy calculation show stability and thermodynamically favourable. We can, therefore, draw the conclusion that these lead compounds act as potential inhibitors against BRCA1. However, wet lab experiments and clinical trials are recommended to ascertain its efficacy, hence the development of novel BRCA1 inhibitors.

摘要

乳腺癌基因1(BRCA1)是一种抗癌基因,可帮助细胞修复受损的DNA并保存遗传物质。BRCA1还作为细胞生长抑制剂发挥作用,并产生肿瘤抑制基因(TSG)蛋白,即BRCA1蛋白。值得注意的是,BRCA1突变占遗传性乳腺癌的90%和大多数遗传性卵巢癌。因此,在本研究中我们考虑了BRCA1的三种突变体(R1699W、R1699Q、T1700A),并采用计算机模拟方法寻找能够抑制这些突变蛋白的最佳植物化学物质,以实现早期乳腺癌诊断。鉴于其重要性,许多来自古代药用植物的天然分子被用于分子对接研究。我们的研究结果表明,虽然许多分子与受体的活性位点有积极结合,但印度人参(Withania somnifera)的前三种植物成分(27-脱氧-14-羟基维A、Withacoagulin、睡茄内酯)具有高结合亲和力和合适的药代动力学特性,使这些天然化合物成为潜在的候选药物。此外,分子动力学(MD)模拟和结合自由能计算显示其具有稳定性和热力学优势。因此,我们可以得出结论,这些先导化合物可作为BRCA1的潜在抑制剂。然而,建议进行湿实验室实验和临床试验以确定其疗效,从而开发新型BRCA1抑制剂。

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