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二萜类多花瓜馥木酸联合两性霉素B的体外抗菌效果。

Efficacy of Diterpene Polyalthic Acid Combined with Amphotericin B against In Vitro.

作者信息

Candido Ana Carolina Bolela Bovo, Pagotti Mariana Cintra, Santos Daiane Albino Dos, Paula Lucas Antonio de Lima, Veneziani Rodrigo Cássio Sola, Bastos Jairo Kenupp, Ambrósio Sérgio Ricardo, Magalhães Lizandra Guidi

机构信息

Research Group on Natural Products, Center for Research in Sciences and Technology, University of Franca, Avenida Dr. Armando Salles of Oliveira, Franca 14404-600, SP, Brazil.

Animal Science Post Graduation, University of Franca, Franca 14404-600, SP, Brazil.

出版信息

Pharmaceuticals (Basel). 2024 Sep 21;17(9):1243. doi: 10.3390/ph17091243.

Abstract

Leishmaniasis, a neglected disease caused by spp. including , urgently requires new treatments. Polyalthic acid (PA), a natural diterpene from spp., has previously demonstrated significant antiparasitic potential. This study evaluated the leishmanicidal effects of polyalthic acid (PA), alone and with amphotericin B (AmpB), on promastigote and amastigote forms. PA showed significant activity against promastigotes, with 50% effective concentration (EC) values of 2.01 μM at 24 h and an EC of 3.22 μM against amastigotes after 48 h. The PA and AmpB combination exhibited a synergistic effect on both forms without inducing cytotoxicity or hemolysis. Morphological changes in promastigotes, including vacuole formation and cell rounding, were more pronounced with the combination. These findings suggest that PA and AmpB together could form a promising new treatment strategy against infections, offering enhanced efficacy without added toxicity.

摘要

利什曼病是一种由包括 属在内的 属物种引起的被忽视疾病,迫切需要新的治疗方法。多花山竹子酸(PA)是一种从 属植物中提取的天然二萜,此前已显示出显著的抗寄生虫潜力。本研究评估了多花山竹子酸(PA)单独以及与两性霉素B(AmpB)联合使用对 前鞭毛体和无鞭毛体形式的杀利什曼原虫作用。PA对前鞭毛体显示出显著活性,在24小时时50%有效浓度(EC)值为2.01 μM,48小时后对无鞭毛体的EC为3.22 μM。PA和AmpB联合使用对两种形式均表现出协同作用,且不诱导细胞毒性或溶血。联合使用时,前鞭毛体的形态变化,包括液泡形成和细胞变圆,更为明显。这些发现表明,PA和AmpB共同可形成一种有前景的抗 感染新治疗策略,在不增加毒性的情况下提高疗效。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/e6c8/11434928/96b926a3e2b0/pharmaceuticals-17-01243-g001.jpg

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