背景:由于其在热带国家的社会经济影响,动物锥虫病是一个主要的牲畜问题。目前使用的杀锥虫剂是有毒的,贵,寄生虫对现有药物产生了抗药性,这就要求迫切需要新的有效和安全的化疗药物从替代来源,如药用植物。在埃塞俄比亚传统医学中,多裂毛毛藻福斯克的新鲜叶子,用于治疗动物锥虫病。本研究旨在评估多裂R.的鲜叶及其主要化合物白头翁素对锥虫田间分离物的抗锥虫活性。
方法:用80%甲醇浸渍和加氢蒸馏法提取多裂红豆根的鲜叶,以获得相应的提取物。通过制备型TLC从水蒸馏的提取物中分离白头翁素。对于体外测定,将0.1、0.4、2和4mg/ml的测试物质与寄生虫一起孵育,并监测寄生虫运动的停止或下降,总持续时间为1小时。在体内测定中,每天腹膜内给药受试物质,持续7天。将双咪唑烯乙酸盐和1%二甲基亚砜(DMSO)用作阳性和阴性对照,分别。
结果:两种提取物均显示抗锥虫活性,尽管与水醇提取物相比,水蒸馏提取物显示出优异的活性。在浓度为4mg/ml时,水蒸馏提取物在20分钟内大大降低了锥虫的运动性。同样,相同浓度的白头翁素在孵育5分钟内完全固定锥虫,而醋酸地米那嗪(28.00mg/kg/天)在10分钟内固定了寄生虫。在体内抗锥虫试验中,白头翁素在所有测试剂量(8.75,17.00和35.00毫克/千克/天)消除寄生虫,并防止复发,而在用乙酸二烯丙嗪治疗的小鼠中,寄生虫在第12至14天再次出现。
结论:当前的研究表明,多裂R.的新鲜叶子具有真正的抗锥虫活性,支持将该植物用于治疗传统医学中的动物锥虫病。此外,白头翁素似乎是该活性的原因,表明其作为开发安全且具有成本效益的抗锥虫剂的支架的潜力。
BACKGROUND: Animal trypanosomiasis is a major livestock problem due to its socioeconomic impacts in tropical countries. Currently used trypanocides are toxic, expensive, and the parasites have developed resistance to the existing drugs, which calls for an urgent need of new effective and safe chemotherapeutic agents from alternative sources such as medicinal plants. In Ethiopian traditional medicine fresh leaves of Ranunculus multifidus Forsk, are used for the treatment of animal trypanosomiasis. The present study aimed to evaluate the antitrypanosomal activity of the fresh leaves of R. multifidus and its major compound anemonin against Trypanosoma congolense field isolate.
METHODS: Fresh leaves of R. multifidus were extracted by maceration with 80% methanol and hydro-distillation to obtain the corresponding extracts. Anemonin was isolated from the hydro-distilled extract by preparative TLC. For the in vitro assay, 0.1, 0.4, 2 and 4 mg/ml of the test substances were incubated with parasites and cessation or drop in motility of the parasites was monitored for a total duration of 1 h. In the in vivo assay, the test substances were administered intraperitoneally daily for 7 days to mice infected with Trypanosoma congolense. Diminazene aceturate and 1% dimethylsulfoxide (DMSO) were used as positive and negative controls, respectively.
RESULTS: Both extracts showed antitrypanosomal activity although the hydro-distilled extract demonstrated superior activity compared to the hydroalcoholic extract. At a concentration of 4 mg/ml, the hydro-distilled extract drastically reduced motility of trypanosomes within 20 min. Similarly, anemonin at the same concentration completely immobilized trypanosomes within 5 min of incubation, while diminazene aceturate (28.00 mg/kg/day) immobilized the parasites within 10 min. In the in vivo antitrypanosomal assay, anemonin eliminates parasites at all the tested doses (8.75, 17.00 and 35.00 mg/kg/day) and prevented relapse, while in diminazene aceturate-treated mice the parasites reappeared on days 12 to 14.
CONCLUSIONS: The current study demonstrated that the fresh leaves of R. multifidus possess genuine antitrypanosomal activity supporting the use of the plant for the treatment of animal trypanosomiasis in traditional medicine. Furthermore, anemonin appears to be responsible for the activity suggesting its potential as a scaffold for the development of safe and cost effective antitrypanosomal agent.