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银杏叶新成分组的制备及其对自发性高血压大鼠降压作用的研究。

Preparation of a new component group of Ginkgo biloba leaves and investigation of the antihypertensive effects in spontaneously hypertensive rats.

作者信息

Liang Hongbao, Yuan Xiaomei, Sun Chenghong, Sun Ying, Yang Min, Feng Shuai, Yao Jingchun, Liu Zhong, Zhang Guimin, Li Feng

机构信息

Shandong University of Traditional Chinese Medicine, Jinan, China; Shandong New Time Pharmaceutical Co., Ltd., Linyi, China; Lunan Pharmaceutical Group Co., Ltd. State Key Laboratory of Generic Manufacture Technology of Chinese Traditional Medicine, Linyi, China.

Lunan Pharmaceutical Group Co., Ltd. State Key Laboratory of Generic Manufacture Technology of Chinese Traditional Medicine, Linyi, China.

出版信息

Biomed Pharmacother. 2022 May;149:112805. doi: 10.1016/j.biopha.2022.112805. Epub 2022 Mar 8.

DOI:10.1016/j.biopha.2022.112805
PMID:35276465
Abstract

Ginkgo (Ginkgo biloba L.) is a traditional economic tree species in China. Ginkgo biloba extract (GBE) is widely used in combination to treat hypertension and complications in clinical practice. However, the antihypertensive effect of GBE alone is weak and it is also difficult to study the mechanism because of its complex composition. This study was to prepare a new component group of Ginkgo biloba leaves (GBLCG) with clear chemical structures, and to investigate its effect on reducing blood pressure and improving myocardial hypertrophy in spontaneously hypertensive rats with GBE and amlodipine as positive controls. The results showed that total flavonoid aglycones (TFAs) of GBLCG was mainly composed of quercetin (QCT), kaempferol (KMF) and isorhamnetin (ISR); Total terpenoid lactones (TTLs) of GBLCG might be a novel cocrystal composed of Ginkgolide A (GA), Ginkgolide B (GB) Ginkgolide C (GC), Ginkgolide J (GJ) and bilobalide (BB). The hypotensive activity of GBLCG (4.4 mg/kg) group was better than that of GBE group (p < 0.05), and the effect of improving myocardial hypertrophy was better than that of amlodipine besylate group (p < 0.01). GBLCG might reduce blood pressure and improve myocardial hypertrophy by promoting the synthesis and release of NO in endothelial cells, reducing oxidative stress, inhibiting platelet aggregation and promoting lesion circulation. Eventually, we hope to introduce GBLCG as a new drug for hypertension.

摘要

银杏(Ginkgo biloba L.)是中国一种传统的经济树种。银杏叶提取物(GBE)在临床实践中广泛用于联合治疗高血压及并发症。然而,GBE单独的降压作用较弱,且由于其成分复杂,其作用机制也难以研究。本研究旨在制备化学结构明确的银杏叶新组分群(GBLCG),并以GBE和氨氯地平作为阳性对照,研究其对自发性高血压大鼠降低血压和改善心肌肥厚的作用。结果表明,GBLCG的总黄酮苷元(TFAs)主要由槲皮素(QCT)、山柰酚(KMF)和异鼠李素(ISR)组成;GBLCG的总萜内酯(TTLs)可能是由银杏内酯A(GA)、银杏内酯B(GB)、银杏内酯C(GC)、银杏内酯J(GJ)和白果内酯(BB)组成的新型共晶体。GBLCG(4.4 mg/kg)组的降压活性优于GBE组(p < 0.05),改善心肌肥厚的效果优于苯磺酸氨氯地平组(p < 0.01)。GBLCG可能通过促进内皮细胞中NO的合成与释放、减轻氧化应激、抑制血小板聚集和促进病变循环来降低血压和改善心肌肥厚。最终,我们希望将GBLCG作为一种治疗高血压的新药推出。

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