Characterization of the major metabolite of sampangine in rats.
Characterization of the major metabolite of sampangine in rats.
复制标题
大鼠体内桑潘金主要代谢物的表征。
DOI：
10.1021/np990552z
复制
发表时间：
2000
影响因子：
5.1
通讯作者：
Hufford,CD
中科院分区：
文献类型：
--
作者：
Orabi,KY;Walker,LA;Clark,AM;Hufford,CD
Sampangine (1) is a plant-derived antifungal copyrine alkaloid extracted from the stem bark ofCananga odorata. Although it possesses potent in vitro antifungal activity,1is devoid of significant and reproducible in vivo activity in a mouse model of cryptococcosis. Speculating that the lack of in vivo activity could be due to metabolism, a study was undertaken to begin to develop an understanding of the pharmacokinetics, and particularly metabolism of1. Following intraperitoneal administration of1to rats, urine was collected, extracted, and chromatographed over a reversed-phase C18silica column to yield the major metabolite, SAM MM1 (2), which was identified by NMR and MS to be anO-glucuronide conjugate of sampangine. In addition, two other unstable, structurally uncharacterized minor metabolites were produced, as evidenced by HPLC analysis. Evaluation of the antifungal and antibacterial activities of2showed it to have remarkable in vitro activity againstCryptococcus neoformans.
