Immunoparasitology Laboratory, Department of Clinical and Toxicological Analysis, Health Sciences Center, Federal University of Rio Grande do Norte, 59012-570 Natal, Brazil.
Postgraduate Program in Pharmaceutical Sciences, Health Sciences Center, Federal University of Rio Grande do Norte, 59012-570 Natal, Brazil.
Molecules. 2020 Jun 3;25(11):2602. doi: 10.3390/molecules25112602.
Neglected tropical diseases such as Chagas disease and leishmaniasis affect millions of people around the world. Both diseases affect various parts of the globe and drugs traditionally used in therapy against these diseases have limitations, especially with regard to low efficacy and high toxicity. In this context, the class of bisphosphonate-based compounds has made significant advances regarding the chemical synthesis process as well as the pharmacological properties attributed to these compounds. Among this spectrum of pharmacological activity, bisphosphonate compounds with antiparasitic activity stand out, especially in the treatment of Chagas disease and leishmaniasis caused by and spp., respectively. Some bisphosphonate compounds can inhibit the mevalonate pathway, an essential metabolic pathway, by interfering with the synthesis of ergosterol, a sterol responsible for the growth and viability of these parasites. Therefore, this review aims to present the information about the importance of these compounds as antiparasitic agents and as potential new drugs to treat Chagas disease and leishmaniasis.
被忽视的热带病,如恰加斯病和利什曼病,影响着全球数百万人。这两种疾病都影响着全球的各个地区,而传统用于治疗这些疾病的药物存在局限性,尤其是在疗效低和毒性高方面。在这种情况下,基于双膦酸盐的化合物类在化学合成过程以及归因于这些化合物的药理学特性方面取得了重大进展。在这种药理活性范围内,具有抗寄生虫活性的双膦酸盐化合物尤为突出,特别是在治疗恰加斯病和利什曼病方面,分别针对 和 spp.。一些双膦酸盐化合物可以通过干扰麦角固醇的合成来抑制甲羟戊酸途径,该途径是一种必需的代谢途径,而麦角固醇是这些寄生虫生长和存活所必需的固醇。因此,本综述旨在介绍这些化合物作为抗寄生虫药物以及作为治疗恰加斯病和利什曼病的潜在新药的重要性。