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从植物和海洋化合物中识别出Mycobacterial CYP124的多种配体

Leonid Kaluzhskiy¹, Evgeniy Yablokov¹, Tatsiana Varaksa²

¹Institute of Biomedical Chemistry, 10 Building 8, Pogodinskaya Street, 119121 Moscow, Russia.

|February 28, 2026

概括

研究人员确定了抑制CYP124的新型天然化合物,该化合物是结核病的潜在药物标. 这些化合物可能会通过向细菌毒性来导致抗药结核病的新疗法.

科学领域:

生物化学生物化学
微生物学微生物学
药物发现药物发现药物发现

背景情况:

结核病仍然是一个重大的全球卫生挑战,耐药菌株加剧了这一问题.
来自Mycobacterium tuberculosis的细胞染色体P450 124家族 (CYP124) 是一个有前途的治疗点,因为它在毒性和宿主固醇代谢中的作用.

研究的目的:

从自然化合物中识别CYP124的新型非azole配体.
研究CYP124抑制剂作为治疗多药耐药结核病的潜力.

主要方法:

使用表面等离子体共振和UV-Vis光谱定位对32种植物衍生和海洋天然化合物的选.
在基分子对接和结构相似性分析.

主要成果:

对CYP124发现了9种新的非azole配体.
两种化合物,15β-octaol和亨利化物H2 (HD-4) 与CYP124.4形成了长期存在的抑制复合物.
分子对接揭示了在CYP124活性部位中对联体结合至关重要的保存水残留物.
结构分析表明,CYP124配体与人体内源性固醇之间存在相似之处,这表明宿主-病原体相互作用.

结论:

发现了针对CYP124的新型天然化合物,为开发新的抗结核治疗药物提供了基础.
了解CYP124连接体相互作用可能会揭示宿主-病原体界面的固醇介导机制.
这些发现为针对耐药结核病的基于机制的CYP124抑制剂铺平了道路.

关键词:

在CYP124中.海洋天然产品海洋天然产品其他非阿醇抑制剂.植物化合物植物化合物谱位定位的光谱定位.表面的等离子体共振.

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