PDF(Pubmed)
Abstract：
UNASSIGNED: Leishmaniasis, a neglected tropical parasitic disease, is regarded as a major public health problem worldwide. The first-line drugs for leishmaniasis suffer from limitations related to toxicity and the development of resistance in certain parasitic strains. Therefore, the discovery of alternative treatments for leishmaniasis is imperative, and natural products represent a valuable source of potential therapeutic agents.
UNASSIGNED: The present study aimed at finding new potential antileishmanial agents from the aerial parts of the medicinal plant Momordica charantia. This study was based on bioassay-guided fractionation of the M. charantia extract against promastigotes and amastigotes of Leishmania (Leishmania) amazonensis. The cytotoxicity of the extract, fractions, and isolated compounds were evaluated against peritoneal murine macrophages by employing the MTT assay for assessing cell metabolic activity.
UNASSIGNED: Antileishmanial assay-guided fractionation of the M. charantia extract led to the bioactive cucurbitacin-enriched fraction and the isolation of four bioactive cucurbitacin-type triterpenoids, which exhibited significant antileishmanial activity, with IC50 values between 2.11 and 3.25 μg.mL-1 against promastigote and amastigote forms, low toxicity and selectivity indexes ranging from 8.5 to 17.2.
UNASSIGNED: Our findings demonstrate that the fractions and cucurbitacin-type triterpenoids obtained from the aerial parts of M. charantia are promising natural leishmanicidal candidates.
UNASSIGNED: The present study aimed at finding new potential antileishmanial agents from the aerial parts of the medicinal plant Momordica charantia. This study was based on bioassay-guided fractionation of the M. charantia extract against promastigotes and amastigotes of Leishmania (Leishmania) amazonensis. The cytotoxicity of the extract, fractions, and isolated compounds were evaluated against peritoneal murine macrophages by employing the MTT assay for assessing cell metabolic activity.
UNASSIGNED: Antileishmanial assay-guided fractionation of the M. charantia extract led to the bioactive cucurbitacin-enriched fraction and the isolation of four bioactive cucurbitacin-type triterpenoids, which exhibited significant antileishmanial activity, with IC50 values between 2.11 and 3.25 μg.mL-1 against promastigote and amastigote forms, low toxicity and selectivity indexes ranging from 8.5 to 17.2.
UNASSIGNED: Our findings demonstrate that the fractions and cucurbitacin-type triterpenoids obtained from the aerial parts of M. charantia are promising natural leishmanicidal candidates.
摘要：
■利什曼病，一种被忽视的热带寄生虫病,被认为是世界范围内的重大公共卫生问题。利什曼病的一线药物受到与毒性和某些寄生菌株的耐药性发展有关的限制。因此,发现利什曼病的替代疗法势在必行，和天然产物代表了潜在治疗剂的宝贵来源。
■本研究旨在从药用植物苦瓜的地上部分中寻找新的潜在的抗红霉病剂。这项研究是基于黑麦提取物对利什曼原虫（Leishmania）amazonensis的前鞭毛和amastigotes的生物测定指导的分馏。提取物的细胞毒性，分数，和分离的化合物针对腹膜鼠巨噬细胞通过使用MTT测定法评估细胞代谢活性。
■苦参素提取物的抗利什曼酶测定指导的分级分离导致富含生物活性葫芦素的部分和四种生物活性葫芦素型三萜类化合物的分离，表现出显著的抗利什曼原虫活性，IC50值在2.11和3.25μg之间。mL-1对抗前受精卵和阿马斯蒂戈特形式，低毒性和选择性指数范围从8.5到17.2。
■我们的发现表明，从苦参素的地上部分获得的馏分和葫芦素型三萜类化合物是有希望的天然利什曼杀菌剂。
■本研究旨在从药用植物苦瓜的地上部分中寻找新的潜在的抗红霉病剂。这项研究是基于黑麦提取物对利什曼原虫（Leishmania）amazonensis的前鞭毛和amastigotes的生物测定指导的分馏。提取物的细胞毒性，分数，和分离的化合物针对腹膜鼠巨噬细胞通过使用MTT测定法评估细胞代谢活性。
■苦参素提取物的抗利什曼酶测定指导的分级分离导致富含生物活性葫芦素的部分和四种生物活性葫芦素型三萜类化合物的分离，表现出显著的抗利什曼原虫活性，IC50值在2.11和3.25μg之间。mL-1对抗前受精卵和阿马斯蒂戈特形式，低毒性和选择性指数范围从8.5到17.2。
■我们的发现表明，从苦参素的地上部分获得的馏分和葫芦素型三萜类化合物是有希望的天然利什曼杀菌剂。
