Bethencourt-Estrella Carlos J, Nocchi Nathalia, López-Arencibia Atteneri, San Nicolás-Hernández Desirée, Souto María L, Suárez-Gómez Blanca, Díaz-Marrero Ana R, Fernández José J, Lorenzo-Morales Jacob, Piñero José E
Instituto Universitario de Enfermedades Tropicales y Salud Pública de Canarias (IUETSPC), Universidad de La Laguna (ULL), Avenida Astrofísico Francisco 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 (ULL), Avenida Astrofísico Francisco Sánchez s/n, 38203 La Laguna, Spain.
Pharmaceuticals (Basel). 2021 Oct 28;14(11):1095. doi: 10.3390/ph14111095.
Leishmaniasis and Chagas disease are neglected tropical diseases that cause problems in developing countries. The causative agents, spp. and , produce a clinical picture that can be fatal for the patient, such as Chagas heart disease, visceral leishmaniasis and megacolon, among others. Current treatments for these diseases are not very effective and highly toxic, since they require very prolonged treatments. The development of innovative, effective and safe drugs to fight infections caused by these parasites remains a challenge. For this reason, in recent years, there has been an increase in the search for new therapies. In this study, the antikinetoplastid activity of 13 sesquiterpene lactones obtained from was screened against , and . The results revealed that the sesquiterpene lactones anhydroartemorin (), -costunolide-14-acetate () and 4-hydroxyarbusculin A () were the most selective against the kinetoplastid species studied. These molecules seem to induce the mechanisms involved in an apoptotic-like death or programmed cell death (PCD) in the kinetoplastids, and since they do not cause necrosis, the inflammatory events associated with this type of cell death will not be triggered.
利什曼病和恰加斯病是在发展中国家引发问题的被忽视热带病。病原体锥虫属物种和利什曼原虫属物种会导致如恰加斯心脏病、内脏利什曼病和巨结肠症等对患者可能致命的临床症状。这些疾病目前的治疗方法效果不佳且毒性很强，因为它们需要非常长时间的治疗。研发创新、有效且安全的药物来对抗这些寄生虫引发的感染仍然是一项挑战。因此，近年来对新疗法的探索有所增加。在本研究中，针对克氏锥虫、杜氏利什曼原虫和巴西利什曼原虫，筛选了从[植物名称未给出]中获得的13种倍半萜内酯的抗动质体活性。结果显示，倍半萜内酯脱水青蒿素（[具体编号未给出]）、β-木香烯内酯-14-乙酸酯（[具体编号未给出]）和4-羟基紫铆素A（[具体编号未给出]）对所研究的动质体物种具有最高的选择性。这些分子似乎诱导了动质体中类似凋亡死亡或程序性细胞死亡（PCD）所涉及的机制，并且由于它们不会导致坏死，所以不会引发与这种细胞死亡相关的炎症事件。
