Lazaro J Enrico H, Nitcheu Josiane, Predicala Rey Z, Mangalindan Gina C, Nesslany Fabrice, Marzin Daniel, Concepcion Gisela P, Diquet Bertrand
INSERM U511, Immuno-Biologie Cellulaire et Moléculaire des Infections Parasitaires, Centre Hospitalo-Universitaire Universitaire Pitié-Salpêtriére, Université Pierre et Marie Curie, 75013 Paris, France.
J Nat Toxins. 2002 Dec;11(4):367-77.
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.
从菲律宾三宝颜采集的一种海洋被囊动物中分离出的α-变形菌培养物中纯化出庚基灵菌红素,这是筛选具有抗寄生虫活性天然产物计划的一部分。发现其对氯喹敏感的恶性疟原虫3D7菌株具有与奎宁相似的体外抗疟活性。其体外抗疟活性约为对L5178Y小鼠淋巴细胞体外细胞毒性活性的20倍。单次皮下注射5和20mg/kg可显著延长感染伯氏疟原虫ANKA株小鼠的存活时间,但也会在注射部位引起硬化性病变。单次灌胃50mg/kg并未增加存活时间。使用体外微方法进行鼠伤寒沙门氏菌Ames试验和使用L5178Y小鼠淋巴瘤细胞进行微核试验,未发现该化合物具有致突变性。