Singh Nasib, Kumar Awanish, Gupta Prasoon, Chand Kailash, Samant Mukesh, Maurya Rakesh, Dube Anuradha
Division of Parasitology, Central Drug Research Institute, Lucknow 226 001, India.
Parasitol Res. 2008 Feb;102(3):561-5. doi: 10.1007/s00436-007-0822-2. Epub 2007 Dec 13.
The chemotherapeutic interventions against visceral leishmaniasis (VL) are limited and facing serious concerns of toxicity, high cost, and emerging drug resistance. There is a greater interest in new drug developments from traditionally used medicinal plants which offers unprecedented diversity in structures and bioactivity. With this rationale, ethanolic extract of Tinospora sinensis Linn and its four fractions were tested in vitro against promastigotes and intracellular amastigotes and in vivo in Leishmania donovani infected hamsters. Ethanolic extract exhibited an appreciable activity against promastigotes (IC(50) 37.6+/-6.2 microg/ml) and intracellular amastigotes (IC(50) 29.8+/-3.4 microg/ml). In hamsters, it resulted in 76.2+/-9.2% inhibition at 500 mg/kg/day x 5 oral dose level. Among fractions, n-butanol imparted highest in vitro and in vivo activities. Ethanolic extract and butanol fraction also enhances reactive oxygen species (ROS) and nitric oxide (NO) release. The results indicate that T. sinensis may provide new lead molecules for the development of alternative drugs against VL.
针对内脏利什曼病(VL)的化疗干预措施有限,且面临毒性、高成本和新出现的耐药性等严重问题。人们对来自传统药用植物的新药开发兴趣更大,这些植物在结构和生物活性方面具有前所未有的多样性。基于这一原理,对中华青牛胆的乙醇提取物及其四个馏分进行了体外抗前鞭毛体和细胞内无鞭毛体的测试,并在感染杜氏利什曼原虫的仓鼠体内进行了测试。乙醇提取物对前鞭毛体(IC50 37.6±6.2微克/毫升)和细胞内无鞭毛体(IC50 29.8±3.4微克/毫升)表现出明显的活性。在仓鼠中,以500毫克/千克/天×5口服剂量给药时,其抑制率为76.2±9.2%。在各馏分中,正丁醇的体外和体内活性最高。乙醇提取物和丁醇馏分还能增强活性氧(ROS)和一氧化氮(NO)的释放。结果表明,中华青牛胆可能为开发抗VL的替代药物提供新的先导分子。