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马郁兰(L.)的钙通道抑制作用:其在腹泻和肠道过度活动中的药用用途。

Calcium Channel Inhibitory Effect of Marjoram ( L.): Its Medicinal Use in Diarrhea and Gut Hyperactivity.

机构信息

Department of Pharmacology & Toxicology, College of Pharmacy, Prince Sattam Bin Abdulaziz University, Al-Kharj 11942, Saudi Arabia.

Department of Pharmacy, Mohammed Al-Mana College for Medical Sciences, Dammam 34222, Saudi Arabia.

出版信息

Front Biosci (Landmark Ed). 2024 Feb 4;29(2):47. doi: 10.31083/j.fbl2902047.

DOI:10.31083/j.fbl2902047
PMID:38420828
Abstract

BACKGROUND

The leaves of () are traditionally renowned for treating diarrhea and gut spasms. This study was therefore planned to evaluate its methanolic extract.

METHODS

Gas chromatography-mass spectrometry (GC-MS) was used to identify the phytochemicals, and Swiss albino mice were used for an antidiarrheal assay. Isolated rat ileum was used as an assay model to study the possible antispasmodic effect and its mechanism(s).

RESULTS

The GC-MS analysis of detected the presence of 21 compounds, of which alpha-terpineol was a major constituent. In the antidiarrheal experiment, showed a substantial inhibitory effect on diarrheal episodes in mice at an oral dosage of 200 mg/kg, resulting in 40% protection. Furthermore, an oral dosage of 400 mg/kg provided even greater protection, with 80% effectiveness. Similarly, loperamide showed 100% protection at oral doses of 10 mg/kg. caused complete inhibition of carbachol (CCh, 1 µM) and high K+ (80 mM)-evoked spasms in isolated ileal tissues by expressing significantly higher potency ( < 0.05) against high K+ compared to CCh, similar to verapamil, a Ca++ antagonist. The verapamil-like predominant Ca++ ion inhibitory action of was further confirmed in the ileal tissues that were made Ca++-free by incubating the tissues in a physiological salt solution having ethylenediaminetetraacetic acid (EDTA) as a chelating agent. The preincubation of at increasing concentrations (0.3 and 1 mg/mL) shifted towards the right of the CaCl2-mediated concentration-response curves (CRCs) with suppression of the maximum contraction. Similarly, verapamil also caused non-specific suppression of Ca++ CRCs towards the right, as expected.

CONCLUSIONS

Thus, this study conducted an analysis to determine the chemical constituents of the leaf extract of and provided a detailed mechanistic basis for the medicinal use of in hyperactive gut motility disorders.

摘要

背景

()的叶子自古以来就以治疗腹泻和肠道痉挛而闻名。因此,本研究旨在评估其甲醇提取物。

方法

采用气相色谱-质谱联用(GC-MS)鉴定植物化学成分,并用瑞士白化小鼠进行抗腹泻试验。分离的大鼠回肠用作研究可能的抗痉挛作用及其机制的试验模型。

结果

GC-MS 分析检测到()的存在 21 种化合物,其中α-松油醇是主要成分。在抗腹泻实验中,()在 200mg/kg 的口服剂量下对小鼠腹泻发作有显著抑制作用,保护率为 40%。此外,口服剂量为 400mg/kg 时提供了更大的保护作用,有效率为 80%。同样,洛哌丁胺在 10mg/kg 的口服剂量下达到 100%的保护作用。()以更高的效力(<0.05)完全抑制了乙酰胆碱(CCh,1µM)和高 K+(80mM)诱发的分离回肠组织痉挛,与钙拮抗剂维拉帕米相似。在将组织孵育在含有乙二胺四乙酸(EDTA)作为螯合剂的生理盐溶液中使组织无钙的情况下,()的维拉帕米样主要钙离子抑制作用在回肠组织中得到进一步证实。用递增浓度(0.3 和 1mg/mL)预孵育()使 CaCl2 介导的浓度反应曲线(CRC)向右移位,最大收缩受到抑制。同样,维拉帕米也如预期的那样导致 Ca++CRC 向右非特异性抑制。

结论

因此,本研究对()叶提取物的化学成分进行了分析,并为()在过度活跃的肠道运动障碍中的药用提供了详细的机制基础。

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