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

IF 4.3 3区医学 Q2 CHEMISTRY, MEDICINAL Pharmaceuticals Pub Date : 2024-09-21 DOI:10.3390/ph17091243

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

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Abstract

Background/Objectives: Leishmaniasis, a neglected disease caused by Leishmania spp. including L. amazonensis, urgently requires new treatments. Polyalthic acid (PA), a natural diterpene from Copaifera spp., has previously demonstrated significant antiparasitic potential. This study evaluated the leishmanicidal effects of polyalthic acid (PA), alone and with amphotericin B (AmpB), on L. amazonensis promastigote and amastigote forms. Results: PA showed significant activity against promastigotes, with 50% effective concentration (EC₅₀) values of 2.01 μM at 24 h and an EC₅₀ 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. Conclusions: These findings suggest that PA and AmpB together could form a promising new treatment strategy against Leishmania infections, offering enhanced efficacy without added toxicity.

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二萜多硫酸与两性霉素 B 联合使用对亚马逊利什曼病的体外疗效。

背景/目标：利什曼病是由包括亚马逊利什曼病在内的利什曼属引起的一种被忽视的疾病，迫切需要新的治疗方法。聚硫酸（PA）是一种来自科帕菲拉属植物的天然二萜，以前曾被证明具有显著的抗寄生虫潜力。本研究评估了多杀菌素（PA）单独或与两性霉素 B（AmpB）一起对亚马逊原虫和非原虫的利什曼杀灭作用。结果：PA对原生体有明显的活性，24小时后的50%有效浓度（EC50）值为2.01 μM，48小时后对非原生体的EC50值为3.22 μM。联合使用时，原变形体的形态变化（包括空泡形成和细胞变圆）更为明显。结论：这些研究结果表明，PA 和 AmpB 可共同组成一种治疗利什曼病感染的新策略，在不增加毒性的情况下提高疗效。

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