Heptyl prodigiin是一种细菌代谢物,体内抗疟,体外无诱变作用。

Journal of natural toxins Pub Date : 2002-12-01
J Enrico H Lazaro, Josiane Nitcheu, Rey Z Predicala, Gina C Mangalindan, Fabrice Nesslany, Daniel Marzin, Gisela P Concepcion, Bertrand Diquet
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引用次数: 0

摘要

Heptyl prodigiosin是从菲律宾三宝鄢收集的海洋被囊动物α -变形菌中分离出来的培养物中纯化出来的,作为筛选天然产物抗寄生虫活性计划的一部分。对氯喹敏感的恶性疟原虫3D7具有与奎宁相似的体外抗疟活性。体外抗疟活性约为体外抗L5178Y小鼠淋巴细胞毒活性的20倍。单次皮下给药5和20 mg/kg可显著延长伯氏单胞杆菌ANKA菌株感染小鼠的存活时间,但也会在注射部位引起硬化性病变。单次灌胃给药50 mg/kg不增加生存时间。体外微方法对Ames鼠伤寒沙门菌试验和L5178Y小鼠淋巴瘤细胞微核试验均未发现该化合物具有致突变性。
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Heptyl prodigiosin, a bacterial metabolite, is antimalarial in vivo and non-mutagenic in vitro.

Heptyl prodigiosin was purified from a culture of alpha-proteobacteria isolated from a marine tunicate collected in Zamboanga, Philippines, as part of a program to screen natural products for antiparasitic activity. An in vitro antimalarial activity similar to that of quinine was found against the chloroquine-sensitive strain Plasmodium falciparum 3D7. The in vitro antimalarial activity was about 20 times the in vitro cytotoxic activity against L5178Y mouse lymphocytes. A single subcutaneous administration of 5 and 20 mg/kg significantly extended survival of P. berghei ANKA strain-infected mice but also caused sclerotic lesions at the site of injection. A single administration by gavage of 50 mg/kg did not increase survival time. The compound was not found to be mutagenic using in vitro micromethods for the Ames Salmonella typhimurium assay and the micronucleus assay using L5178Y mouse lymphoma cells.

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