Marango Sylvia Naliaka, Khayeka-Wandabwa Christopher, Makwali Judith Alice, Jumba Bernard Ngoitsi, Choge Joseph K, Adino Eric Onyango, Anjili Christopher O
Department of Biological Science (Parasitology), University of Eldoret, P.O Box 1125, Eldoret, 30100, Kenya.
School of Pharmaceutical Science and Technology (SPST), Health Sciences Platform, Tianjin University, Tianjin, 300072, China.
BMC Res Notes. 2017 Dec 6;10(1):698. doi: 10.1186/s13104-017-3022-x.
Conventional targeted leishmanicidal chemotherapy has persistently remained prohibitive for most economically deprived communities due to costs, associated time to accessing health services and duration for successful treatment programme. Alternatives are bound to be incorporated in rational management of leishmaniasis by choice or default due to accessibility and cultural beliefs. Therefore, there is need to rigorously investigate and appraise the activity of medicinal compounds that may have anti-leishmanicidal activity especially in the context of products that are already being utilized by the populations for other ailments but have limited information on their therapeutic value and possible cytoxicity. Hence, the study examined both in vivo and in vitro response of L. major infection to Tephrosia vogelii extracts in BALB/c mice as the mouse model.
A comparative study design was applied for the in vivo and in vitro assays of the extract with Pentostam (GlaxoSmithKline, UK) and Amphotericin B [Fungizone™, X-Gen Pharmaceuticals (US)] as standard drugs.
In BALB/c mice where the chemotherapeutic extract was administered intraperitoneally, there was significantly (p < 0.05) larger reduction in lesion size and optimal control of parasite burden than those treated orally. However, standard drugs showed better activity. Tephrosia vogelii had 50% inhibitory concentration (IC) and IC of 12 and 68.5 μg/ml respectively, while the standard drugs had IC and IC of 5.5 and 18 μg/ml for Pentostam and 7.8 and 25.5 μg/ml for Amphotericin B in that order. In the amastigote assay, the infection rates decreased with increase in chemotherapeutic concentration. The multiplication indices for L. major amastigotes in macrophages treated with 200 µg/ml of the standard drugs and extract were significantly different (p < 0.05). 200 µg/ml of T. vogelii extract showed a multiplication index of 20.57, 5.65% for Amphotericin B and 9.56% for Pentostam. There was also significant difference (p < 0.05) in levels of Nitric oxide produced in the macrophages.
The findings demonstrated that T. vogelii extract has anti-leishmanial activity and further assays should be done to ascertain the active compounds responsible for anti-leishmanial activity.
由于成本、获得医疗服务所需的相关时间以及成功治疗方案的持续时间,传统的靶向利什曼原虫化疗对大多数经济贫困社区来说一直难以承受。由于可及性和文化信仰,替代方案必然会被纳入利什曼病的合理管理中。因此,有必要严格研究和评估可能具有抗利什曼原虫活性的药用化合物的活性,特别是在那些已经被人们用于治疗其他疾病但对其治疗价值和可能的细胞毒性信息有限的产品背景下。因此,本研究以BALB/c小鼠为模型,研究了大劣按蚊感染对非洲山毛豆提取物的体内和体外反应。
采用比较研究设计,以喷他脒(葛兰素史克公司,英国)和两性霉素B [Fungizone™,X-Gen制药公司(美国)]作为标准药物,对提取物进行体内和体外试验。
在腹腔注射化疗提取物的BALB/c小鼠中,与口服给药的小鼠相比,病变大小的减少显著更大(p < 0.05),对寄生虫负荷的控制也更理想。然而,标准药物显示出更好的活性。非洲山毛豆的50%抑制浓度(IC)和IC分别为12和68.5μg/ml,而标准药物中喷他脒的IC和IC分别为5.5和18μg/ml,两性霉素B的IC和IC依次为7.8和25.5μg/ml。在无鞭毛体试验中,感染率随着化疗浓度的增加而降低。用200μg/ml标准药物和提取物处理的巨噬细胞中大劣按蚊无鞭毛体的增殖指数有显著差异(p < 0.05)。200μg/ml的非洲山毛豆提取物的增殖指数为20.57,两性霉素B为5.65%,喷他脒为9.56%。巨噬细胞中产生的一氧化氮水平也有显著差异(p < 0.05)。
研究结果表明非洲山毛豆提取物具有抗利什曼原虫活性,应进一步进行试验以确定负责抗利什曼原虫活性的活性化合物。