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通过MMV病原体药物盒发现针对……的新型化学工具

Discovery of New Chemical Tools against via the MMV Pathogen Box.

作者信息

López-Arencibia Atteneri, Sifaoui Ines, Reyes-Batlle María, Bethencourt-Estrella Carlos J, San Nicolás-Hernández Desirée, Lorenzo-Morales Jacob, Piñero José E

机构信息

Instituto Universitario de Enfermedades Tropicales y Salud Pública de Canarias, Campus de Anchieta, Universidad de La Laguna, Avda. Astrofísico Fco. Sánchez, S/N, 38203 La Laguna, Spain.

Departamento de Obstetricia y Ginecología, Pediatría, Medicina Preventiva y Salud Pública, Toxicología, Medicina Legal y Forense y Parasitología, Universidad de La Laguna, 38203 La Laguna, Spain.

出版信息

Pharmaceuticals (Basel). 2021 Nov 24;14(12):1219. doi: 10.3390/ph14121219.

DOI:10.3390/ph14121219
PMID:34959620
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC8708704/
Abstract

The protozoan parasite causes a spectrum of diseases and there are over 1 million infections each year. Current treatments are toxic, expensive, and difficult to administer, and resistance to them is emerging. In this study, we screened the antileishmanial activity of the Pathogen Box compounds from the Medicine for Malaria Venture against , and compared their structures and cytotoxicity. The compounds MMV676388 (3), MMV690103 (5), MMV022029 (7), MMV022478 (9) and MMV021013 (10) exerted a significant dose-dependent inhibition effect on the proliferation of promastigotes and intracellular amastigotes. Moreover, studies on the mechanism of cell death showed that compounds 3 and 5 induced an apoptotic process while the compounds 7, 9 and 10 seem to induce an autophagic mechanism. The present findings underline the potential of these five molecules as novel therapeutic leishmanicidal agents.

摘要

这种原生动物寄生虫会引发一系列疾病，每年有超过100万例感染病例。目前的治疗方法有毒、昂贵且给药困难，并且对这些治疗方法的耐药性正在出现。在本研究中，我们筛选了疟疾药物风险投资公司的病原体盒化合物对[寄生虫名称未给出]的抗利什曼原虫活性，并比较了它们的结构和细胞毒性。化合物MMV676388（3）、MMV690103（5）、MMV022029（7）、MMV022478（9）和MMV021013（10）对[寄生虫名称未给出]前鞭毛体和细胞内无鞭毛体的增殖具有显著的剂量依赖性抑制作用。此外，对细胞死亡机制的研究表明，化合物3和5诱导凋亡过程，而化合物7、9和10似乎诱导自噬机制。本研究结果强调了这五种分子作为新型治疗利什曼原虫药物的潜力。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/e6a9/8708704/70c8ff5c3ec7/pharmaceuticals-14-01219-g005.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/e6a9/8708704/6fc8e4ad3336/pharmaceuticals-14-01219-g001.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/e6a9/8708704/d75029917828/pharmaceuticals-14-01219-g002.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/e6a9/8708704/c6bc84a76a7f/pharmaceuticals-14-01219-g003.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/e6a9/8708704/a9eb1cc2627e/pharmaceuticals-14-01219-g004.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/e6a9/8708704/70c8ff5c3ec7/pharmaceuticals-14-01219-g005.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/e6a9/8708704/6fc8e4ad3336/pharmaceuticals-14-01219-g001.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/e6a9/8708704/d75029917828/pharmaceuticals-14-01219-g002.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/e6a9/8708704/c6bc84a76a7f/pharmaceuticals-14-01219-g003.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/e6a9/8708704/a9eb1cc2627e/pharmaceuticals-14-01219-g004.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/e6a9/8708704/70c8ff5c3ec7/pharmaceuticals-14-01219-g005.jpg

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