阿塔拉菲林宁及相关吖啶酮生物碱对啮齿类动物疟疾的体外和体内活性
In vitro and in vivo activities of atalaphillinine and related acridone alkaloids against rodent malaria.
作者信息
Fujioka H, Nishiyama Y, Furukawa H, Kumada N
机构信息
Department of Medical Zoology, Nagoya University School of Medicine, Japan.
出版信息
Antimicrob Agents Chemother. 1989 Jan;33(1):6-9. doi: 10.1128/AAC.33.1.6.
Abstract
Thirty acridone alkaloids obtained from Citrus, Glycosmis, or Severinia plants (members of the family Rutaceae) were tested for their antimalarial activities in vitro and in vivo. At a concentration of 10 micrograms/ml in vitro, seven of these alkaloids suppressed 90% or more of Plasmodium yoelii, which causes malaria in rodents. Atalaphillinine, when injected intraperitoneally in a daily dose of 50 mg/kg for 3 days into mice infected with 10(7) erythrocytes parasitized with Plasmodium berghei or Plasmodium vinckei, completely suppressed the development of malaria parasites, with there being no obvious acute toxic effects from the tested dose.
摘要
从柑橘属、山小桔属或酒饼簕属植物（芸香科成员）中获得的30种吖啶酮生物碱进行了体外和体内抗疟活性测试。在体外浓度为10微克/毫升时，其中7种生物碱抑制了90%或更多的约氏疟原虫，该疟原虫可导致啮齿动物患疟疾。当以50毫克/千克的日剂量腹腔注射3天，给感染了10⁷个被伯氏疟原虫或文氏疟原虫寄生的红细胞的小鼠注射阿他拉菲林宁时，可完全抑制疟原虫的发育，且测试剂量没有明显的急性毒性作用。
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