在实验室中,拉帕科尔和β-拉帕对Leishmania amazonensis的作用
Á C F H Ramos-Milaré1, B G Sydor1, A Á Brustolin1
1Programa de Pós-graduação em Ciências da Saúde, Universidade Estadual de Maringá, Maringá, PR, Brasil.
概括
拉帕霍尔和β-拉帕显示出显著的抗莱什马尼亚活性,抑制了寄生虫的生长和生存. 这些天然化合物对开发新的莱什曼病治疗有前途.
科学领域:
- 自然产品化学 自然产品化学
- 寄生虫学的寄生虫学
- 药物发现 药物发现 药物发现
背景情况:
- 莱什曼病是一种被忽视的热带疾病,治疗选择有限.
- 现有的药物面临着诸如低粘附度和耐药性等挑战.
- 自然产品是新型抗莱什曼病药物的潜在来源.
研究的目的:
- 评估lapachol和β-lapachone对Leishmania amazonensis的体外活性.
- 评估这些纳夫托金对寄生虫生存能力和细胞完整性的影响.
主要方法:
- 在实验室中对拉帕霍尔和β-拉帕对莱什马尼亚亚马逊菌的前性和前性形式的评估.
- 确定致命剂量50 (LD50) 的值.
- 评估线粒体膜潜力,膜完整性和类似于亡的变化.
- 测量促炎性细胞因子 (TNF-α和IL-6) 的产生.
主要成果:
- 乙-拉帕对LD50值较低的前列腺细胞具有强烈的活性.
- 拉帕霍尔和β-拉帕都显著抑制了莱什曼亚马逊虫 (Leishmania amazonensis) 的虫存活率.
- 化合物诱导了线粒体膜潜力的丧失和膜损伤,表明了细胞亡.
- 观察到瘤亡因子-α (TNF-α) 和互白素-6 (IL-6) 生产的抑制.
结论:
- 拉帕霍尔和β-拉帕具有显著的抗莱什曼病活性.
- 这些纳夫托金具有涉及线粒体功能障碍和亡诱导的作用机制.
- 像拉帕霍尔和β-拉帕这样的天然产品是开发新型抗莱什曼病药物的有希望的候选者.
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