非洲异叶草木犀草素、芹菜素及其衍生物作为疟疾靶点plasmepsin II潜在抑制剂的计算分析。

IF 4.3 2区 化学 Q2 CHEMISTRY, MULTIDISCIPLINARY
Ismail Abubakari, Lucas P Kwiyukwa, Lucas Paul
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引用次数: 0

摘要

疟疾仍然是一项重大的全球卫生挑战,特别是在撒哈拉以南非洲,耐药菌株加剧了对新的治疗战略的需要。Plasmepsin II是疟疾生命周期中的关键酶,是新型抗疟疾药物的一个有希望的靶点。本研究采用分子对接、分子动力学模拟和自由能计算等方法研究非洲异叶草木犀草素、芹菜素及其苷类衍生物与PMII靶点的相互作用。木犀草素衍生物,特别是木犀草素-7- o -葡萄糖苷和木犀草素-3′,7-二- o -葡萄糖苷与PMII的结合能分别为-9.1和-9.5 kcal/mol,而在芹菜素衍生物中,芹菜素-6,8-二- c -己糖糖苷的结合能最显著(-10.2 kcal/mol)。自由能计算进一步证实了其与芹菜素-8- c -己糖苷的强结合亲和力,得到了最佳的结合自由能(-86.646 kJ/mol)。该研究强调了这些化合物作为抗疟疾药物开发的有希望的候选者的潜力,尽管需要进一步的实验验证。
本文章由计算机程序翻译,如有差异,请以英文原文为准。
Computational analysis of luteolin, apigenin and their derivatives from Allophylus africanus as potential inhibitors of plasmepsin II a malaria target.

Malaria remains a critical global health challenge, especially in Sub-Saharan Africa, with drug-resistant strains heightening the need for new treatment strategies. Plasmepsin II, a key enzyme in the life cycle of malaria presents a promising target for novel antimalarial drugs. This study investigates the interaction of luteolin, apigenin and their glycoside derivatives from Allophylus africanus with PMII target using molecular docking, molecular dynamics simulation and free energy calculations. Luteolin derivatives, particularly luteolin-7-O-glucoside and luteolin-3',7-di-O-glucoside showed strong binding with PMII at -9.1 and -9.5 kcal/mol, respectively, while in apigenin derivatives apigenin-6,8-di-C-hexoside exhibited the most significant binding energy (-10.2 kcal/mol). The free energy calculations further confirmed the strong binding affinity with the apigenin-8-C-hexoside, demonstrating the best binding free energy (-86.646 kJ/mol). The study highlights the potential of these compounds as promising candidates for antimalarial drug development, although further experimental validation is needed.

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来源期刊
BMC Chemistry
BMC Chemistry Chemistry-General Chemistry
CiteScore
5.30
自引率
2.20%
发文量
92
审稿时长
27 weeks
期刊介绍: BMC Chemistry, formerly known as Chemistry Central Journal, is now part of the BMC series journals family. Chemistry Central Journal has served the chemistry community as a trusted open access resource for more than 10 years – and we are delighted to announce the next step on its journey. In January 2019 the journal has been renamed BMC Chemistry and now strengthens the BMC series footprint in the physical sciences by publishing quality articles and by pushing the boundaries of open chemistry.
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