3-烯和状成份对Leishmania (Leishmania) amazonensis的影响
Audrey Rouse Soares Tavares Silva1, Amanda Mendonça Barros Costa1, Ricardo Scher2
1Departamento de Farmácia, Universidade Federal de Sergipe, São Cristóvão 49100-000, Sergipe, Brazil.
Tropical medicine and infectious disease
|June 27, 2023
概括
波洛克萨默407微粒有效地输送了3-烯 (3CR),增强了其对抗莱什曼尼亚寄生虫的抗莱什曼尼亚活性. 这种新的纳米系统显示出治疗被忽视的热带疾病,如莱什曼病的希望.
科学领域:
- 寄生虫学的寄生虫学
- 纳米技术 纳米技术
- 药用化学 医学化学
背景情况:
- 莱什曼病是被忽视的热带疾病,由于当前药物的高成本,毒性和可变疗效,治疗选择有限.
- 一种单烯的3-烯 (3CR) 在体外表现出抗莱什曼的活性,但其水溶性差,挥发性高.
- 开发有效的药物输送系统对于克服现有抗莱什曼治疗方法的局限性至关重要.
研究的目的:
- 为了配制和表征Poloxamer 407 (P407) 微粒,以提供3 - 烯 (3CR).
- 评估P407-3CR小粒细胞增强的抗莱什曼病毒活性和安全概况.
- 探索P407微粒作为可行的纳米系统在莱什曼病治疗中提供3CR的潜力.
主要方法:
- 构成的Poloxamer 407微粒封装3 - 烯 (P407-3CR) 的配方.
- 微粒大小,多分散性和质性行为的表征.
- 在体外对抗L. (L.) amazonensis*前列腺菌和细胞内前列腺菌的抗莱什曼活性进行评估,包括对哺乳动物细胞的细胞毒性测试.
主要成果:
- P407-3CR微粒表现出纳米尺寸和有利的质性质.
- 3CR和P407-3CR都抑制了*L. (L.) amazonensis*前子的生长,P407-3CR的疗效略有改善.
- 传输电子显微镜揭示了寄生虫中3CR诱导的形态变化.
- 与自由3CR (>1.5 mM) 相比,P407-3CR菌根对细胞内巨乳细胞具有显著增强的活性 (IC50/72h = 0.7 ± 0.1 mM),对宿主细胞无细胞毒性.
结论:
- 波洛克萨默407微粒作为一个有效的纳米系统提供3-carene.
- P407-3CR菌根增强了抗莱什曼病毒的活性,特别是对细胞内巨菌的活性.
- 这种P407-3CR菌根系统值得进一步研究,作为莱什曼病的潜在治疗策略.
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