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,七叶欧洲七叶树的种子中分离出的七叶皂素Ia,Ib和IIb以及通过七叶皂素碱水解获得的去甲壳素I和II对动物急性炎症的影响(p.o.)。 Escins Ia,Ib,IIa和IIb(50-200 mg / kg)抑制了小鼠乙酸和组胺引起的血管通透性的增加。 Escins Ib,IIa和IIb(50-200 mg / kg)也能抑制5-羟色胺对大鼠的刺激,但escin Ia却没有。 Escins Ia,Ib,IIa和IIb(200 mg / kg)在大鼠的第一阶段抑制了角叉菜胶诱导的后爪水肿。 Escin Ia(200 mg / kg)和escins Ib,IIa和IIb(50-200 mg / kg)抑制化合物48/80诱导的小鼠抓挠行为,但escin Ia最弱。 Desacylescins I和Desacylescins(200 mg / kg)没有作用。关于它们的化学结构和活性之间的关系,七叶皂苷中的酰基是必不可少的。具有21-邻苯二甲酰基或2'-O-吡喃吡喃糖基部分的Escins Ib,IIa和IIb显示出比具有21-tigloyl和2'-O-吡喃葡糖基部分的escin Ia更有力的活性。 >