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药用榆皮(芦丁)在便秘和腹泻中的应用的药理学基础。

Pharmacological basis for the medicinal use of psyllium husk (Ispaghula) in constipation and diarrhea.

机构信息

Natural Product Research Division, Department of Biological and Biomedical Sciences, Aga Khan University Medical College, Karachi, 74800, Pakistan.

出版信息

Dig Dis Sci. 2011 May;56(5):1460-71. doi: 10.1007/s10620-010-1466-0. Epub 2010 Nov 17.

DOI:10.1007/s10620-010-1466-0
PMID:21082352
Abstract

BACKGROUND

The objective of this study was to determine the pharmacological basis of the medicinal use of psyllium husk (Ispaghula) in gastrointestinal motility disorders.

METHODS

In-vivo studies were conducted on mice, and isolated rabbit jejunum and guinea-pig ileum were used in in-vitro experiments.

RESULTS

The crude extract of Ispaghula (Po.Cr) had a laxative effect in mice at 100 and 300 mg/kg, which was partially sensitive to atropine or SB203186 (5-HT(4) antagonist). At higher doses (500 and 1,000 mg/kg), Po.Cr had antisecretory and antidiarrheal activity. In guinea-pig ileum, Po.Cr (1-10 mg/ml) had a stimulatory effect, which was partially sensitive to atropine or SB203186. In rabbit jejunum, Po.Cr had a partially atropine-sensitive stimulatory effect followed by relaxation at 10 mg/ml. The relaxation was inhibited by the presence of L-NAME, a nitric oxide (NO) synthase inhibitor, or methylene blue, a guanylyl cyclase inhibitor. Similarly, the relaxant effect of Po.Cr on K(+) (80 mM)-induced contractions, was attenuated in the presence of L-NAME or methylene blue. Activity-directed fractionation of Po.Cr revealed that the gut stimulatory and inhibitory constituents were widely distributed in the aqueous and organic fractions.

CONCLUSION

This study demonstrates that Ispaghula has a gut-stimulatory effect, mediated partially by muscarinic and 5-HT(4) receptor activation, which may complement the laxative effect of its fiber content, and a gut-inhibitory activity possibly mediated by blockade of Ca(2+) channels and activation of NO-cyclic guanosine monophosphate pathways. This may explain its medicinal use in diarrhea. It is, perhaps, also intended by nature to offset an excessive stimulant effect.

摘要

背景

本研究旨在确定洋车前子壳(Psyllium)在胃肠动力障碍中的药用基础。

方法

在体内实验中使用了小鼠,在体外实验中使用了兔空肠和豚鼠回肠。

结果

洋车前子壳粗提物(Po.Cr)在 100 和 300mg/kg 时对小鼠有通便作用,对阿托品或 SB203186(5-HT4 拮抗剂)部分敏感。高剂量(500 和 1000mg/kg)时,Po.Cr 具有抗分泌和止泻作用。在豚鼠回肠中,Po.Cr(1-10mg/ml)具有刺激作用,对阿托品或 SB203186 部分敏感。在兔空肠中,Po.Cr 先产生部分阿托品敏感的刺激作用,随后在 10mg/ml 时松弛。一氧化氮(NO)合酶抑制剂 L-NAME 或鸟苷酸环化酶抑制剂亚甲蓝存在时,松弛作用被抑制。同样,Po.Cr 对 K+(80mM)诱导收缩的松弛作用在 L-NAME 或亚甲蓝存在时也减弱。Po.Cr 的活性导向分离显示,肠道刺激和抑制成分广泛分布于水相和有机相。

结论

本研究表明,洋车前子具有肠道刺激作用,部分通过毒蕈碱和 5-HT4 受体激活介导,这可能补充其纤维含量的通便作用,以及可能通过阻断 Ca2+通道和激活 NO-环鸟苷酸途径介导的肠道抑制活性。这可以解释其在腹泻中的药用用途。也许这也是大自然为了抵消过度刺激作用而有意为之。

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