Bukhari Syed Nasir Abbas, Saeed Sumera, Asim Mulazim Hussain, Irfan Hafiz Muhammad, Ejaz Hasan, Elsherif Mervat A, Junaid Kashaf
Department of Pharmaceutical Chemistry, College of Pharmacy, Jouf University, Sakaka, Al Jouf 72388, Saudi Arabia.
Punjab University College of Pharmacy, University of the Punjab, 54000 Lahore, Pakistan.
Evid Based Complement Alternat Med. 2022 May 20;2022:5871424. doi: 10.1155/2022/5871424. eCollection 2022.
Linn. fruit, a natural dietary item, has long been used traditionally to treat hypertension in Pakistan. The current research work aims to explore the effect on blood pressure and its mechanisms.
The aqueous methanol extract of plant fruit was used to evaluate hypotensive/antihypertensive, vasorelaxation, and safety profiles. Moreover, the inhibitory effect of AMECA on phosphodiesterase was also evaluated.
In hypotensive studies, extracts of fruit exhibited a concentration-dependent reduction in SBP, DBP, MAP, and heart rate. A similar effect has been observed on anesthetized rats, but the effects exerted by the extract were not altered significantly in the presence of L-NAME, atropine, captopril, and propranolol. Moreover, in coronary arteries, the extract significantly potentiated relaxations induced by cGMP- and cAMP-dependent relaxing agonists. When exposed to PDEs, the extract concentration dependently subdued cGMP-hydrolyzing activity of different PDEs with IC50 values of 40-130 g/mL.
It is conceivable that extracts obtained from fruit produced hypotensive and antihypertensive effects in rats. The extract elicited endothelium-independent vasorelaxation, possibly by acting directly on smooth muscles of the coronary artery and by increasing cGMP and cAMP via nonselective inhibition of vascular PDEs.
Linn.果实是一种天然的膳食成分,在巴基斯坦长期以来一直被传统用于治疗高血压。当前的研究工作旨在探索其对血压的影响及其机制。
使用植物果实的甲醇水提取物来评估其降压/抗高血压、血管舒张和安全性概况。此外,还评估了AMECA对磷酸二酯酶的抑制作用。
在降压研究中,果实提取物使收缩压、舒张压、平均动脉压和心率呈浓度依赖性降低。在麻醉大鼠身上也观察到了类似的效果,但在L-精氨酸甲酯、阿托品、卡托普利和普萘洛尔存在的情况下,提取物产生的效果没有显著改变。此外,在冠状动脉中,提取物显著增强了由环鸟苷酸(cGMP)和环腺苷酸(cAMP)依赖性舒张激动剂诱导的舒张作用。当暴露于磷酸二酯酶时,提取物浓度依赖性地抑制了不同磷酸二酯酶的cGMP水解活性,半数抑制浓度(IC50)值为40 - 130μg/mL。
可以想象,从果实中获得的提取物在大鼠中产生了降压和抗高血压作用。该提取物引起了不依赖内皮的血管舒张,可能是通过直接作用于冠状动脉平滑肌,并通过非选择性抑制血管磷酸二酯酶来增加cGMP和cAMP。