Kumari Reshmi, Banerjee Satarupa
Department of Biotechnology, School of Biosciences and Technology, VIT University Vellore, Vellore, Tamil Nadu, 632014, India.
BMC Mol Cell Biol. 2025 Jul 30;26(1):24. doi: 10.1186/s12860-025-00548-6.
Triple-negative breast cancer (TNBC) presents a significant therapeutic challenge due to its aggressive nature, lack of hormone receptors, and limited targeted treatment options. The complexity of the disease is further compounded by mutations in high-penetrance genes such as BRCA1, BRCA2, and BAX, along with other apoptotic genes involved in tumorigenesis, apoptosis, and drug resistance. Targeting these genes through innovative therapeutic approaches is crucial for improving treatment outcomes. This in-silico study explores the potential of phytochemicals as natural, multi-targeted therapeutic agents against high-penetrance and apoptotic genes implicated in TNBC. Using the IMPPAT 2.0 database, 300 phytochemicals were systematically screened based on their pharmacokinetic properties and toxicity profiles to identify promising candidates. Among them, Bayogenin exhibited strong binding to BRCA2 (-9.3 kcal/mol) and PALB2 (-8.7 kcal/mol), surpassing the FDA-approved drug Olaparib in molecular docking studies. Molecular dynamics simulations over 200 ns further confirmed the stability of these phytochemical-protein complexes, showing consistent root mean square deviation, hydrogen bonding, and free energy profiles. These findings highlight the therapeutic potential of phytochemicals and their possible advantages over existing TNBC treatments. By targeting key molecular pathways, this study provides insights into the development of natural, multi-targeted therapeutic strategies, emphasizing their translational relevance for TNBC therapy.
三阴性乳腺癌(TNBC)因其侵袭性、缺乏激素受体以及靶向治疗选择有限而带来了重大的治疗挑战。高穿透性基因如BRCA1、BRCA2和BAX以及其他参与肿瘤发生、凋亡和耐药性的凋亡基因发生突变,进一步加剧了该疾病的复杂性。通过创新治疗方法靶向这些基因对于改善治疗效果至关重要。这项计算机模拟研究探索了植物化学物质作为针对TNBC中涉及的高穿透性和凋亡基因的天然多靶点治疗剂的潜力。利用IMPPAT 2.0数据库,根据300种植物化学物质的药代动力学特性和毒性概况进行了系统筛选,以确定有前景的候选物。其中,白杨素在分子对接研究中显示出与BRCA2(-9.3千卡/摩尔)和PALB2(-8.7千卡/摩尔)有很强的结合力,超过了FDA批准的药物奥拉帕尼。超过200纳秒的分子动力学模拟进一步证实了这些植物化学物质-蛋白质复合物的稳定性,显示出一致的均方根偏差、氢键和自由能概况。这些发现突出了植物化学物质的治疗潜力及其相对于现有TNBC治疗方法可能具有的优势。通过靶向关键分子途径,本研究为天然多靶点治疗策略的开发提供了见解,强调了它们在TNBC治疗中的转化相关性。