Fournet A, Barrios A A, Muñoz V, Hocquemiller R, Cavé A
Institut Franłcais de Recherche Scientifique pour le Dévelopement en Coopération (ORSTOM), Département Santé, Paris, France.
Trop Med Parasitol. 1992 Dec;43(4):219-22.
Plumbagin, 3,3'-biplumbagin and 8,8'-biplumbagin are naphthoquinones isolated by activity-directed fractionation from a Bolivian plant, Pera benensis, used in folk medicine as treatment of cutaneous leishmaniasis caused by Leishmania braziliensis. BALB/c mice were infected with L. mexicana or L. venezuelensis and treated 24 h after the parasitic infection with plumbagin (5 or 2.5 mg/kg/day), 3,3'-biplumbagin, 8,8'-biplumbagin (25 mg/kg/d) or Glucantime (200 mg/kg/d). Lesion development was the criteria employed to evaluate the inhibitory effect. The bis-naphthoquinones were less potent than Glucantime against L. amazonensis and L. venezuelensis. Plubagin and Glucantime delayed the development of L. amazonensis and L. venezuelensis. Assays of a single local treatment on foot-pad infection two weeks after the parasitic inoculation with L. amazonensis showed that 8,8'-biplumbagin (50 mg/kg/d) was as potent as Glucantime (400 mg/kg/d).
白花丹醌、3,3'-双白花丹醌和8,8'-双白花丹醌是通过活性导向分级分离从一种玻利维亚植物贝氏佩雷木中分离得到的萘醌，该植物在民间医学中用于治疗由巴西利什曼原虫引起的皮肤利什曼病。将BALB/c小鼠感染墨西哥利什曼原虫或委内瑞拉利什曼原虫，并在寄生虫感染后24小时用白花丹醌（5或2.5毫克/千克/天）、3,3'-双白花丹醌、8,8'-双白花丹醌（25毫克/千克/天）或葡糖胺锑钠（200毫克/千克/天）进行治疗。以病变发展情况作为评估抑制效果的标准。双萘醌对亚马逊利什曼原虫和委内瑞拉利什曼原虫的效力低于葡糖胺锑钠。白花丹醌和葡糖胺锑钠延缓了亚马逊利什曼原虫和委内瑞拉利什曼原虫的发展。在用亚马逊利什曼原虫进行寄生虫接种两周后，对足垫感染进行单次局部治疗的试验表明，8,8'-双白花丹醌（50毫克/千克/天）的效力与葡糖胺锑钠（400毫克/千克/天）相当。
