Fötsch G, Pfeifer S
Sektion Chemie-Wissenschaftsbereich Pharmazie, Humboldt-Universität zu Berlin.
Pharmazie. 1989 Oct;44(10):710-2.
After parenteral administration of leiocarposide (1, 3-beta-D-glucopyranosyloxy-2-methoxy-6-hydroxybenzoic acid-2'-beta-D-glucopyranosyloxybenzylester) and salicin to the rat the glycosides were mostly excreted unchanged in urine. In contrast to the oral administration (see [1]) only small amounts of metabolites [1: 0.2% of the dose as leiocarpic acid and 0.1% salicylic acid; 2: 0.05% 5] were observed. By in vitro experiments could be shown, that the hydrolysis of ester and glycosidic bonds from 1 to 3 and saligenin and from 2 to 4 took place microbially mostly in the cecum and colon of the rats. The reactions are also visible in the homogenate of kidney. Präparations of liver, lung and serum showed no activity. 4 in the homogenates of liver, kidney and lung, in the gut-wall and the serum was oxidized to 5. The further product of oxidation of 5, gentisic acid, arise only in liver homogenate.
将紫茎泽兰苷(1,3-β-D-吡喃葡萄糖氧基-2-甲氧基-6-羟基苯甲酸-2'-β-D-吡喃葡萄糖氧基苄酯)和水杨苷经肠胃外途径给予大鼠后,这些糖苷大多以原形经尿液排泄。与口服给药情况(见[1])不同,仅观察到少量代谢产物[1:剂量的0.2%为紫茎泽兰酸,0.1%为水杨酸;2:0.05% 5]。通过体外实验可以表明,从1到3的酯键和糖苷键以及从2到4的水杨苷配基的水解大多在大鼠的盲肠和结肠中由微生物进行。这些反应在肾脏匀浆中也可见。肝脏、肺和血清的制剂未显示活性。4在肝脏、肾脏和肺的匀浆中、肠壁和血清中被氧化为5。5的进一步氧化产物龙胆酸仅在肝脏匀浆中产生。