BACKGROUND & AIMS:
We investigated the effects of escins Ia, Ib, and IIb isolated from horse chestnut, the seeds of Aesculus hippocastanum L., and desacylescins I and II obtained by alkaline hydrolysis of escins on acute inflammation in animals (p.o.). Escins Ia, Ib, IIa, and IIb (50-200 mg/kg) inhibited the increase of vascular permeability induced by both acetic acid in mice and histamine in rats. Escins Ib, IIa, and IIb (50-200 mg/kg) also inhibited that induced by serotonin in rats, but escin Ia didn't. Escins Ia, Ib, IIa, and IIb (200 mg/kg) inhibited the hind paw edema induced by carrageenin at the first phase in rats. Escin Ia (200 mg/kg) and escins Ib, IIa, and IIb (50-200 mg/kg) inhibited the scratching behavior induced by compound 48/80 in mice, but escin Ia was weakest. Desacylescins I and II (200 mg/kg) showed no effect. With regard to the relationship between their chemical structures and activities, the acyl groups in escins were essential. Escins Ib, IIa, and IIb with either the 21-angeloyl group or the 2'-O-xylopyranosyl moiety showed more potent activities than escin Ia which had both the 21-tigloyl group and the 2'-O-glucopyranosyl moiety.
背景与目标:
我们研究了从七叶树,七叶树的种子以及通过碱性水解七叶树获得的desacylescins I和II中分离出的esscins Ia,Ib和IIb对动物急性炎症 (p.o.) 的影响。Esscins Ia,Ib,IIa和IIb (50-200 mg/kg) 抑制小鼠中乙酸和大鼠中组胺引起的血管通透性增加。Esscins Ib,IIa和IIb (50-200 mg/kg) 也抑制大鼠中5-羟色胺诱导的浓度,但esscin Ia没有。Esscins Ia,Ib,IIa和IIb (200 mg/kg) 在大鼠第一阶段抑制角叉菜胶诱导的后爪水肿。Escin Ia (200 mg/kg) 和escin Ib,IIa和IIb (50-200 mg/kg) 抑制了由化合物48/80诱导的小鼠抓挠行为,但Escin Ia最弱。Desaylescins I和II (200 mg/kg) 没有效果。关于它们的化学结构和活性之间的关系,escins中的酰基是必不可少的。具有21-当归酰基或2 '-O-吡喃木糖基部分的Escins Ib,IIa和IIb比具有21-替格洛基和2'-O-吡喃葡萄糖基的escin Ia表现出更有效的活性。