PDF(Pubmed)
Abstract：
Current treatment for visceral leishmaniasis is based on drugs such as pentavalent antimony and amphotericin B. However, this treatment remains mostly ineffective and expensive, resulting in several side effects and generating resistance. Apigenin, a flavonoid present in fruits and vegetables, has demonstrated several biological functions. In the present study, we observed a concentration-dependent inhibition of the L. infantum promastigote in the presence of apigenin, exhibiting an IC50 value of 29.9 µM. Its effect was also evaluated in L. infantum-infected murine peritoneal macrophages, presenting an C50 value against intracellular amastigotes of 2.3 µM and a selectivity index of 34.3. In a murine model of visceral leishmaniasis, the in vivo effect of apigenin was measured using short-term and long-term treatment schemes. Treatment with apigenin demonstrated 99.7% and 94% reductions in the liver parasite load in the short-term and long-term treatment schemes, respectively. Furthermore, no alterations in serological and hematological parameters were observed. Taken together, these results suggest that apigenin is a potential candidate for visceral leishmaniasis chemotherapy by oral administration.
摘要：
目前内脏利什曼病的治疗基于五价锑和两性霉素B等药物。这种治疗方法仍然大多无效且昂贵，导致几个副作用和产生阻力。芹菜素,一种存在于水果和蔬菜中的类黄酮，已经证明了几种生物学功能。在本研究中,我们观察到在芹菜素的存在下，对婴儿前乳牛的浓度依赖性抑制，IC50值为29.9µM。其效果也在L.infantum感染的鼠腹膜巨噬细胞中进行了评估，针对细胞内amastigotes的C50值为2.3µM，选择性指数为34.3。在内脏利什曼病的鼠模型中，使用短期和长期治疗方案测量芹菜素的体内作用。在短期和长期治疗方案中，芹菜素治疗显示肝脏寄生虫负荷减少99.7%和94%。分别。此外，未观察到血清学和血液学参数的改变.一起来看,这些结果提示芹菜素是利什曼病口服化疗的潜在候选药物。
