通过植物化学物质触发安福特里辛B孔形成活动
Svetlana S Efimova1, Anna I Malykhina1, Olga S Ostroumova1
1Laboratory of Membrane and Ion Channel Modeling, Institute of Cytology of Russian Academy of Sciences, Tikhoretsky 4, 194064 Saint Petersburg, Russia.
Membranes
|July 28, 2023
概括
植物化合物可以通过增加其在真菌膜中的毛孔形成活性来增强抗真菌药物安二乙 (AmB). 这种方法可以减少AMB的毒性,并提高系统性真菌菌的治疗疗效.
科学领域:
- 药理学和毒理学 药理学和毒理学
- 菌类学和传染病的研究
- 自然产品化学 自然产品化学
背景情况:
- 氨酸B (AmB) 是系统性真菌病的关键抗真菌剂,因其广泛性和低耐药性发展而受到重视.
- AmB的临床效用受到显著的毒性限制,包括脏病和血液溶解,往往需要降低治疗剂量.
- 探索AmB与天然化合物的强化提供了一种策略,以保持有效性,同时减轻毒性.
研究的目的:
- 调查植物性多和类的潜力,以增强安福特乙的抗真菌活性.
- 评估这些植物化学物质对AmB孔隙形成能力和膜相互作用的影响.
- 评估AmB-植物化学组合的治疗潜力,以减少药物毒性.
主要方法:
- 利用脂质双层 (棕烯酸和埃尔戈斯特) 的跨膜电流测量来评估AmB活性.
- 选了各种植物多和类化合物,以检测它们对AmB诱导的跨膜电流的影响.
- 采用吸收光谱和差异扫描微热度计来研究AmB-膜相互作用和脂质特性.
主要成果:
- 一些植物化学物质,包括佛洛,奎尔和复星,在含有厄戈斯特的膜中显著增加了AMB诱导的跨膜电流.
- 其他化合物,如卡达摩宁和黄素,抑制了AMB活性,而一些化合物没有显著影响.
- 当用胆固醇取代厄戈斯特醇时,增强效应在很大程度上消失了,这表明对哺乳动物细胞的毒性潜力降低了.
结论:
- 特定的植物多和类可以通过改变膜性质来增强安二B的孔形成和抗真菌活性.
- 这些协同作用似乎是丰富于ergosterol的真菌膜的特征,表明减少宿主毒性的潜在机制.
- 雄乙与已识别的植物分子的组合代表了开发更安全,更有效的抗真菌疗法的有希望的途径.
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