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这些物质的平滑肌松弛、支气管扩张和血管舒张作用可以用抗毒蕈碱和钙拮抗机制来解释。

The Spasmolytic, Bronchodilator, and Vasodilator Activities of Are Explained by Anti-Muscarinic and Calcium Antagonistic Mechanisms.

机构信息

Faculty of Pharmacy, The Islamia University of Bahawulpur, Bahawulpur 63100, Pakistan.

Faculty of Pharmacy, Bahauddin Zakariya University, Multan 66000, Pakistan.

出版信息

Molecules. 2021 Oct 20;26(21):6348. doi: 10.3390/molecules26216348.

Abstract

is traditionally used in different areas of Pakistan to treat gastrointestinal, respiratory, and vascular diseases. This study evaluates the underlying mechanisms for traditional uses of in diarrhea, asthma, and hypertension. In vitro pharmacological studies were conducted using isolated jejunum, trachea, and aortic preparations, while the cytotoxic study was conducted in mice. Crude extract of (Pp.Cr), comprising appreciable quantities of alkaloids and flavonoids, relaxed spontaneously contracting jejunum preparation, K (80 mM)-induced, and carbachol (1 µM)-induced jejunum contractions in a concentration-dependent manner similar to dicyclomine and dantrolene. Pp.Cr showed a rightward parallel shift of concentration-response curves (CRCs) of Cch after a non-parallel shift similarto dicyclomine and shifted CRCs of Ca to rightward much likeverapamil and dantrolene, demonstrating the coexistence of antimuscarinic and Ca antagonistic mechanism. Furthermore, Pp.Cr, dicyclomine, and dantrolene relaxed K (80 mM)-induced and Cch (1 µM)-induced tracheal contractions and shifted rightward CRCs of Cch similar to dicyclomine, signifying the dual blockade. Additionally, Pp.Cr also relaxed the K (80 mM)-induced and phenylephrine (1 µM)-induced aortic contraction, similarly to verapamil and dantrolene, suggesting Ca channel antagonism. Here, we explored for the first time thespasmolytic and bronchodilator effects of Pp.Crand whether they maybe due to the dual blockade of Ca channels and muscarinic receptors, while the vasodilator effect might be owing to Ca antagonism. Our results provide the pharmacological evidence that could be a new potential therapeutic option to treat gastrointestinal, respiratory, and vascular diseases. Hence, there is a need for further research to explore bioactive constituent of as well as further investigation by suitable experimental models are required to further confirm the importance and usefulness of in diarrhea, asthma, and hypertension treatment.

摘要

在巴基斯坦的不同地区, traditionally used 被用于治疗胃肠道、呼吸道和血管疾病。本研究评估了 在腹泻、哮喘和高血压的传统用途中的潜在机制。使用离体空肠、气管和主动脉制剂进行了体外药理学研究,而细胞毒性研究则在小鼠中进行。包含相当数量的生物碱和类黄酮的 粗提物(Pp.Cr)以类似于双环胺和丹曲林的浓度依赖性方式松弛自发收缩的空肠制剂、K(80 mM)诱导的和 carbachol(1 µM)诱导的空肠收缩。Pp.Cr 显示 Cch 的浓度-反应曲线(CRC)向右平行移动,类似于双环胺,并且 Ca 的 CRC 向右移动类似于 verapamil 和 dantrolene,表明存在抗毒蕈碱和 Ca 拮抗机制的共存。此外,Pp.Cr、双环胺和丹曲林松弛 K(80 mM)诱导和 Cch(1 µM)诱导的气管收缩,并向右移动 Cch 的 CRC,类似于双环胺,表明双重阻断。此外,Pp.Cr 还松弛了 K(80 mM)诱导和 phenylephrine(1 µM)诱导的主动脉收缩,类似于 verapamil 和 dantrolene,表明 Ca 通道拮抗作用。在这里,我们首次探索了 Pp.Cr 的平滑肌松弛和支气管扩张作用,以及它们是否可能是由于 Ca 通道和毒蕈碱受体的双重阻断,而血管扩张作用可能是由于 Ca 拮抗作用。我们的结果提供了药理学证据,表明 可能是治疗胃肠道、呼吸道和血管疾病的新的潜在治疗选择。因此,需要进一步研究以探索 的生物活性成分,并且需要通过适当的实验模型进行进一步研究,以进一步确认 在腹泻、哮喘和高血压治疗中的重要性和有用性。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/37d2/8588472/e4806f1e3c55/molecules-26-06348-g001a.jpg

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