关键词: Anticholinergic Antihistaminergic Apigenin Apigenin (PubChem CID: 5280704) Diosmetin Diosmetin (PubChem CID: 5281612) IBS Potassium channel opener Rosmarinus officinalis Rutin Rutin (PubChem CID: 5280805)

Mesh : Animals Guinea Pigs Rosmarinus / chemistry Plant Extracts / pharmacology chemistry Mice Male Gastrointestinal Motility / drug effects Rabbits Anti-Anxiety Agents / pharmacology isolation & purification chemistry Ileum / drug effects metabolism physiology Antidiarrheals / pharmacology isolation & purification Flavonoids / pharmacology Parasympatholytics / pharmacology isolation & purification Laxatives / pharmacology isolation & purification Jejunum / drug effects metabolism Diarrhea / drug therapy Female

来  源:   DOI:10.1016/j.jep.2024.118395

Abstract:
BACKGROUND: Rosmarinus officinalis L. (Rosemary) is a popular herb with reported effectiveness against diarrhea, anxiety and constipation, albeit with limited pharmacological evidence.
OBJECTIVE: The current study was aimed at evaluating the therapeutic potential, possible pharmacological mechanisms of action and active constituents of hydro-ethanolic extract of rosemary (Rs.Cr), as potential anti-diarrheal, laxative and anxiolytic agent.
METHODS: Rs.Cr was analyzed through reverse-phase high pressure liquid chromatography (RP-HPLC). Laxative, antidiarrheal, and anxiolytic activities were assessed using in vivo models. Spasmogenic and spasmolytic mechanisms were studied on isolated guinea pig ileum and rabbit jejunum tissues, respectively. Possible role of diosmetin, one of the active constituents of Rs.Cr was also evaluated.
RESULTS: RP-HPLC analysis revealed presence of diosmetin, rutin and apigenin in Rs.Cr. Laxative effect was seen at low doses, which was partially reversed in atropinized mice. The spasmogenic mechanism was mediated by cholinergic and histaminergic receptors stimulation. At higher doses, antidiarrheal activity was evident, with reduction in gastrointestinal motility and secretions using charcoal meal and enteropooling assays, respectively. Rs.Cr also showed dose-dependent anxiolytic effect. The antispasmodic mechanisms were mediated by anti-muscarinic and K+ channel opening-like effect (predominant KATP-dependent). Diosmetin exhibited antidiarrheal and antispasmodic activities, but spasmogenic effect was not seen.
CONCLUSIONS: Rosemary leaves have dual antidiarrheal and laxative effects, and as well as anxiolytic activity. In addition, the possible modulation of muscarinic and histaminergic receptors, and KATP channels show it as potential herb to be explored for irritable bowel syndrome. Diosmetin is possibly one of its constituents that contributes to its antidiarrheal activity.
摘要:
背景:迷迭香(迷迭香)是一种据报道对腹泻有效的烹饪草药,焦虑和便秘,尽管药理学证据有限。
目的:本研究旨在评估治疗潜力,迷迭香水乙醇提取物的可能药理作用机制和活性成分(Rs.Cr),一种潜在的止泻药,抗便秘和抗焦虑剂。
方法:Rs.通过反相高压液相色谱(RP-HPLC)分析Cr。泻药,止泻药,使用体内模型评估抗焦虑活性。在分离的豚鼠回肠和兔空肠组织上研究了痉挛和痉挛机制,分别。Diosmetin的可能作用,R.的活性成分之一还评估了Cr。
结果:RP-HPLC分析显示,芦丁和芹菜素在R.Cr.在低剂量下观察到泻药效果,在阿托品化小鼠中部分逆转。痉挛机制由胆碱能和组胺能受体刺激介导。在更高的剂量下,止泻活性明显,使用木炭餐和肠池化测定法减少胃肠蠕动和分泌物,分别。RS.Cr还显示出剂量依赖性抗焦虑作用。抗痉挛机制是由抗毒蕈碱和K通道开放样作用(主要是KATP依赖性)介导的。Diosmetin表现出抗腹泻和抗痉挛活性,但没有看到痉挛效应。
结论:迷迭香叶具有止泻和泻药双重作用,以及抗焦虑活性。此外,毒蕈碱和组胺能受体的可能调节,和KATP通道显示它是一种潜在的治疗肠易激综合征的草药。Diosmetin可能是其有助于其抗腹泻活性的成分之一。
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