Natural Product Research Division, Department of Biological and Biomedical Sciences, Aga Khan University Medical College, Karachi, 74800, Pakistan.
Dig Dis Sci. 2011 May;56(5):1460-71. doi: 10.1007/s10620-010-1466-0. Epub 2010 Nov 17.
The objective of this study was to determine the pharmacological basis of the medicinal use of psyllium husk (Ispaghula) in gastrointestinal motility disorders.
In-vivo studies were conducted on mice, and isolated rabbit jejunum and guinea-pig ileum were used in in-vitro experiments.
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.
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.
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。
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。
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。
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。