METHODS: The compounds were isolated from Clausena anisata using column chromatography and their structures elucidated using NMR spectroscopy. The anti-malarial activity was determined by measuring the trophozoitocidal, schizonticidal and gametocytocidal activities of the compounds using the SYBR green assay. Cytotoxicity was evaluated using the tetrazolium-based colorimetric assay.
RESULTS: Heptaphylline and imperatorin produced trophozoitocidal, schizonticidal and gametocytocidal activities with IC50s of 1.57 (0.2317)-26.92 (0.3144) µM with those of artesunate (the standard drug) being 0.00024 (0.0036)-0.0070 (0.0013) µM. In the cytotoxicity assay, the compounds produced CC50S greater than 350 µM and SI of 13.76-235.90. Also, the trophozoitocidal and schizonticidal activities of the compounds were more pronounced than their gametocytocidal activity. Imperatorin was 42.04% more trophozoitocidal than hepthaphyline. However, hepthaphyline has more schizonticidal and gametocytocidal properties than imperatorin.
CONCLUSIONS: Heptaphylline and imperatorin are promising anti-malarial agents, since they possess potent anti-malarial activity with weak cytotoxicity on RBCs. However, imperatorin is a better anti-malarial prophylactic agent whereas heptaphylline is a better malaria treatment agent.
方法:使用柱色谱法从Clausenaanisata中分离化合物,并使用NMR光谱阐明其结构。抗疟疾活性是通过测量的滋养杀动物,使用SYBR绿色测定法对化合物的杀分裂和杀配子细胞活性。使用基于四唑的比色测定法评估细胞毒性。
结果:七叶树素和欧前胡素产生了滋养杀动物,杀生和杀配子细胞活性,IC50为1.57(0.2317)-26.92(0.3144)µM,青蒿琥酯(标准药物)的IC50为0.00024(0.0036)-0.0070(0.0013)µM。在细胞毒性试验中,化合物产生的CC50S大于350µM,SI为13.76-235.90。此外,化合物的杀虫和杀裂殖子活性比其杀配子细胞活性更明显。Imperatorin比hepthaphenline高出42.04%。然而,hepthaphine比欧前胡素具有更多的杀分裂子和杀配子细胞特性。
结论:七肽和欧前胡素是有前途的抗疟疾药,因为它们具有有效的抗疟疾活性,对红细胞具有弱的细胞毒性。然而,欧前胡素是一种更好的抗疟疾预防剂,而七茶碱是一种更好的疟疾治疗剂。