Falade M O, Akinboye D O, Gbotosho G O, Ajaiyeoba E O, Happi T C, Abiodun O O, Oduola A M J
Cellular Parasitology Programme, Cell Biology and Genetics Unit, Department of Zoology, University of Ibadan, Ibadan, Nigeria ; Malaria Research Laboratories, Institute for Advanced Medical Research and Training, College of Medicine, University of Ibadan, Ibadan, Nigeria.
Department of Public and Allied Health, Babcock University, Ilishan-Remo, Ogun State, Nigeria.
J Parasitol Res. 2014;2014:972853. doi: 10.1155/2014/972853. Epub 2014 May 14.
Drug resistance in Plasmodium falciparum requires that new drugs must be developed. Plants are a potential source for drug discovery and development. Two plants that used to treat febrile illnesses in Nigeria were tested for in vitro and in vivo antimalarial activity and cytotoxicity in cancer cell lines. Methanol, hexane, and ethyl acetate leaf extracts of Ficus thonningii and Lophira alata were active in in vitro assays against P. falciparum NF54 (sensitive) and K1 (multiresistant) strains. Hexane extracts of F. thonningii and L. alata were the most effective extracts in in vitro assays with IC50 of 2.7 ± 1.6 μg/mL and 2.5 ± 0.3 μg/mL for NF54 and 10.4 ± 1.6 μg/mL and 2.5 ± 2.1 μg/mL for K1 strain. All extracts were nontoxic in cytotoxicity assays against KB human cell line with IC50 of over 20 μg/mL, demonstrating selectivity against P. falciparum. In vivo analysis shows that hexane extracts of both plants reduced parasitaemia. At the maximum dose tested, L. alata had a 74.4% reduction of parasitaemia while F. thonningii had a reduction of 84.5%, both extracts prolonged animal survival in mice infected with P. berghei NK65 when compared with vehicle treated controls. The antiplasmodial activity observed justifies the use of both plants in treating febrile conditions.
恶性疟原虫的耐药性问题使得必须研发新的药物。植物是药物发现和开发的潜在来源。对尼日利亚两种过去用于治疗发热性疾病的植物进行了体外和体内抗疟活性以及对癌细胞系的细胞毒性测试。托宁榕(Ficus thonningii)和翅籽树(Lophira alata)的甲醇、己烷和乙酸乙酯叶提取物在体外试验中对恶性疟原虫NF54(敏感)和K1(多耐药)菌株具有活性。托宁榕和翅籽树的己烷提取物是体外试验中最有效的提取物,对NF54菌株的IC50分别为2.7±1.6μg/mL和2.5±0.3μg/mL,对K1菌株的IC50分别为10.4±1.6μg/mL和2.5±2.1μg/mL。在针对KB人细胞系的细胞毒性试验中,所有提取物均无毒,IC50超过20μg/mL,表明对恶性疟原虫具有选择性。体内分析表明,两种植物的己烷提取物均能降低疟原虫血症。在测试的最大剂量下,翅籽树的疟原虫血症降低了74.4%,而托宁榕降低了84.5%,与载体处理的对照组相比,两种提取物均延长了感染伯氏疟原虫NK65的小鼠的存活时间。观察到的抗疟活性证明了这两种植物在治疗发热病症中的应用价值。