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作为一种通过 sGC 和前列腺素合成途径发挥降压和血管舒张作用的药物。

Acts as an Antihypertensive and Vasorelaxant Agent Through sGC and Prostaglandin Synthesis Pathways.

机构信息

Team of Ethnopharmacology and Pharmacognosy, Faculty of Sciences and Techniques Errachidia, Moulay Ismail University of Meknes, BP 509, Boutalamine, Errachidia, 52000, Morocco.

Energy, materials and sustainable development (EMDD) Team- Higher School of Technology-SALE, Center for Water, Natural Resources Environment and Sustainable Development (CERNE2D), Mohammed V University in Rabat, Avenue Ibn Battouta, B.P. 1014, Rabat, 10000, Morocco.

出版信息

Cardiovasc Hematol Agents Med Chem. 2023;21(3):177-192. doi: 10.2174/1871525721666221209161605.

Abstract

BACKGROUND

is a medicinal plant used in traditional medicine to treat various ailments, including hypertension.

AIMS

The study aimed to determine the antihypertensive activity of .

OBJECTIVE

The study aimed to investigate the antihypertensive and vasorelaxant activities of the aqueous extract of fruits (ALAE) in rats.

METHODS

ALAE was prepared to study its antihypertensive effect in L-NAME (Nω-L-arginine methyl ester)-induced hypertensive rats and its vasorelaxant activity in isolated thoracic aortas of rats. The acute and subchronic effects of ALAE on systolic, diastolic, mean arterial pressure, and heart rate (HR) were evaluated after oral administration of ALAE (60 and 100 mg/kg body weight) for 6 h for the acute experiment and over 7 days for the subchronic test. Isolated thoracic aortic rings were prepared to examine the vasorelaxant action of ALAE. Several common pharmacological agents were used to test potential pathways implicated in vasorelaxant action.

RESULTS

The results showed that ALAE reduced blood pressure parameters (systolic, mean, and diastolic blood pressure) in L-NAME-induced hypertension rats after repeated oral treatment over seven days without affecting normotensive rats. Furthermore, in thoracic aortic rings pre-contracted with epinephrine (EP) (10 μM) or KCl (80 mM), ALAE (0.250-1.625 mg/ml) showed a vasorelaxant effect. In isolated rat thoracic aortas, blockage of soluble guanylyl cyslase with blue methylene (P < 0.01) partially decreased this vasorelaxant effect. In addition, blockage of the prostaglandin synthesis pathway with indomethacin (P<0.05) also reduced the vasorelaxant activity of ALAE. Pretreatment of aortic rings with glibenclamide, propanolol, L-NAME, MLN-4760, or nifedipine did not affect ALAE-induced vasorelaxation.

CONCLUSION

is a prescient medicinal plant, able to act as an antihypertensive agent. Moreover, the results suggest that the extract increased cGMP in NO-independent manner.

摘要

背景

是一种药用植物,在传统医学中用于治疗各种疾病,包括高血压。

目的

本研究旨在确定 的降压活性。

目的

本研究旨在研究 果实水提物(ALAE)在大鼠中的降压和血管舒张活性。

方法

制备 ALAE 研究其在 L-NAME(Nω-L-精氨酸甲酯)诱导的高血压大鼠中的降压作用及其对大鼠离体胸主动脉的血管舒张活性。急性和亚慢性实验中,ALAE(60 和 100 mg/kg 体重)经口给予 6 h 后,评价 ALAE 对收缩压、舒张压、平均动脉压和心率(HR)的急性影响,亚慢性试验中连续 7 天给予。制备离体胸主动脉环以检测 ALAE 的血管舒张作用。使用几种常用的药理学药物来测试血管舒张作用涉及的潜在途径。

结果

结果表明,ALAE 降低了反复口服治疗 7 天后 L-NAME 诱导的高血压大鼠的血压参数(收缩压、平均压和舒张压),而对正常血压大鼠没有影响。此外,在预先用肾上腺素(EP)(10 μM)或氯化钾(80 mM)收缩的胸主动脉环中,ALAE(0.250-1.625 mg/ml)显示出血管舒张作用。在离体大鼠胸主动脉中,用蓝亚甲基(P<0.01)阻断可溶性鸟苷酸环化酶部分降低了这种血管舒张作用。此外,用吲哚美辛(P<0.05)阻断前列腺素合成途径也降低了 ALAE 的血管舒张活性。用格列本脲、普萘洛尔、L-NAME、MLN-4760 或硝苯地平预处理主动脉环不影响 ALAE 诱导的血管舒张。

结论

是一种有前途的药用植物,能够作为一种降压剂。此外,结果表明,该提取物以非一氧化氮依赖的方式增加 cGMP。

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