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银杏叶提取物 EGb 761 中原花青素的详细观察。

A Detailed View on the Proanthocyanidins in Ginkgo Extract EGb 761.

机构信息

Department of Preclinical Research and Development, Dr. Willmar Schwabe GmbH & Co. KG, Karlsruhe, Germany.

Department of Analytical Development, Dr. Willmar Schwabe GmbH & Co. KG, Karlsruhe, Germany.

出版信息

Planta Med. 2022 Apr;88(5):398-404. doi: 10.1055/a-1379-4553. Epub 2021 Apr 16.

Abstract

The Ginkgo extract EGb 761 manufactured with leaves of has been continuously produced over decades at a large scale and is used as a clinically proven remedy for, among other things, the improvement of age-associated cognitive impairment and quality of life in patients with mild dementia. It belongs to the class of extracts addressed as quantified extracts according to the European Pharmacopeia. Accordingly, several compounds (e.g., flavone glycosides and terpene trilactones) are acknowledged to contribute to its clinical efficacy. Covering only about 30% of the mass balance, these characterized compounds are accompanied by a larger fraction of additional compounds, which might also contribute to the clinical efficacy and safety of the extract. As part of our systematic research to fully characterize the constituents of Ginkgo extract EGb 761, we focus on the structural class of proanthocyanidins in the present study. Structural insights into the proanthocyanidins present in EGb 761 and a quantitative method for their determination using HPLC are shown. The proanthocyanidins were found to be of oligomeric to polymeric structure, which yield delphinidin and cyanidin as main building blocks after acidic hydrolysis. A validated HPLC method for quantification of the anthocyanidins was developed in which delphinidin and cyanidin were detected after hydrolysis of the proanthocyanidins. The content of proanthocyanidins in Ginkgo extract EGb 761 was found to be approximately 7%.

摘要

银杏叶提取物 EGb 761 已连续数十年大规模生产,被临床证明可用于改善与年龄相关的认知障碍和轻度痴呆患者的生活质量等。它属于欧洲药典中称为定量提取物的一类提取物。因此,几种化合物(如类黄酮糖苷和三萜内酯)被认为对其临床疗效有贡献。这些有特征的化合物仅占质量平衡的约 30%,其伴随的是更大比例的其他化合物,这些化合物也可能对提取物的临床疗效和安全性有贡献。作为我们对银杏叶提取物 EGb 761 进行全面特征分析的系统研究的一部分,我们在本研究中重点关注原花青素这一结构类别。本研究展示了 EGb 761 中原花青素的结构特征,并提供了一种使用 HPLC 定量测定其含量的方法。原花青素的结构为低聚到聚合体,经酸性水解后得到翠雀素和矢车菊素作为主要结构单元。建立了一种经过验证的 HPLC 方法,用于定量分析原花青素,其中在水解原花青素后检测到翠雀素和矢车菊素。银杏叶提取物 EGb 761 中原花青素的含量约为 7%。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/a593/9020886/1c3371ec1bda/10-1055-a-1379-4553-ie0784pm01ad.jpg

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