Fundação Oswaldo Cruz, Instituto Oswaldo Cruz, Laboratório de Biologia Molecular e Doenças Endêmicas, Rio de Janeiro, RJ, Brazil.
Fundação Oswaldo Cruz, Centro de Desenvolvimento Tecnológico em Saúde, Rio de Janeiro, RJ, Brazil; Universidade Iguaçu, Nova Iguaçu, RJ, Brazil.
Braz J Infect Dis. 2023 Mar-Apr;27(2):102743. doi: 10.1016/j.bjid.2023.102743. Epub 2023 Jan 31.
Natural products and their derivatives have been sources of search and research for new drugs for the treatment of neglected diseases. Naphthoquinones, a special group of quinones, are products of natural metabolites with a wide spectrum of biological activities and represent a group of interesting molecules for new therapeutic propositions. Among these compounds, lapachol stands out as a molecule from the heartwood of Tabebuia sp. whose structural changes resulted in compounds considered promising, such as epoxy-α-lapachone (ELAP). The biological activity of ELAP has been demonstrated, so far, for parasitic protozoa such as Leishmania spp., Trypanosoma cruzi and Plasmodium spp., species causing diseases needing new drug development and adequate health policy. This work gathers in vitro and in vivo studies on these parasites, as well as the toxicity profile, and the probable mechanisms of action elucidated until then. The potential of ELAP-based technology alternatives for a further drug is discussed here.
天然产物及其衍生物一直是寻找和研究治疗被忽视疾病的新药的来源。萘醌类化合物是一类特殊的醌类化合物，是天然代谢产物的产物，具有广泛的生物活性，代表了一组有趣的用于新治疗方案的分子。在这些化合物中，拉帕醇是 Tabebuia sp.心材中的一种分子，其结构变化导致了一些被认为有前途的化合物的产生，如环氧-α-拉帕酮（ELAP）。到目前为止，ELAP 的生物活性已在寄生原生动物如 Leishmania spp.、Trypanosoma cruzi 和 Plasmodium spp.等物种中得到证实，这些物种导致需要新药物开发和适当卫生政策的疾病。这项工作汇集了关于这些寄生虫的体外和体内研究，以及到目前为止阐明的毒性概况和可能的作用机制。本文还讨论了基于 ELAP 的技术替代物进一步开发药物的潜力。
