Matsuda H, Li Y, Murakami T, Ninomiya K, Yamahara J, Yoshikawa M
Kyoto Pharmaceutical University, Japan.
Biol Pharm Bull. 1997 Oct;20(10):1092-5. doi: 10.1248/bpb.20.1092.
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.
我们研究了从欧洲七叶树(Aesculus hippocastanum L.)种子中分离得到的七叶皂苷Ia、Ib和IIb以及通过七叶皂苷碱水解得到的去酰基七叶皂苷I和II对动物急性炎症(口服给药)的影响。七叶皂苷Ia、Ib、IIa和IIb(50 - 200 mg/kg)可抑制小鼠醋酸和大鼠组胺诱导的血管通透性增加。七叶皂苷Ib、IIa和IIb(50 - 200 mg/kg)也可抑制大鼠血清素诱导的血管通透性增加,但七叶皂苷Ia无此作用。七叶皂苷Ia、Ib、IIa和IIb(200 mg/kg)可抑制大鼠角叉菜胶诱导的后爪水肿第一阶段。七叶皂苷Ia(200 mg/kg)以及七叶皂苷Ib、IIa和IIb(50 - 200 mg/kg)可抑制小鼠48/80诱导的搔抓行为,但七叶皂苷Ia作用最弱。去酰基七叶皂苷I和II(200 mg/kg)无作用。关于它们的化学结构与活性之间的关系,七叶皂苷中的酰基至关重要。具有21 - 当归酰基或2'-O - 吡喃木糖基部分的七叶皂苷Ib、IIa和IIb比同时具有21 - 惕各酰基和2'-O - 吡喃葡萄糖基部分的七叶皂苷Ia活性更强。