Kwon Sunbeom, Jeong Suji, Lee Seulah
Department of Convergent Biotechnology and Advanced Materials Science, College of Life Sciences, Kyung Hee University, Yongin, Republic of Korea.
BK21 Interdisciplinary Program in IT-Bio Convergence System, Kyung Hee University, Yongin, Republic of Korea.
J Pharm Pharm Sci. 2025 Aug 26;28:14614. doi: 10.3389/jpps.2025.14614. eCollection 2025.
The development of cognitive-enhancing drugs from extract is actively pursued worldwide. This study compares the chemical compositions of different extracts and their formulated drugs, highlighting the distinguishing characteristics and potential benefits of optimized extract, EGb 761.
We analyzed three extracts and fifteen formulated drugs using HPLC, principal component analysis, and LC-MS/MS to identify key compositional differences. Molecular docking analysis was conducted to evaluate the binding affinity of the key component with a target protein involved in cognitive enhancement. CYP inhibition assays were performed on selected extracts and their derived products to examine drug-drug interactions.
EGb 761 and its formulated drugs displayed a unique composition, characterized by a significantly higher level of protocatechuic acid (PCA). PCA demonstrated strong interactions with the M receptor, acetylcholinesterase, glycogen synthase kinase-3, which are the key targets for cognitive enhancement. CYP inhibition assays indicated that EGb 761 and the drugs derived from EGb 761 had lower inhibitory activity compared to other samples.
The high PCA content in EGb 761 may contribute to cognitive benefits. With low CYP inhibition, it suggests minimal interference with drug metabolism, highlighting its potential as a safer cognitive enhancer. Ultimately, this study indicates that the composition of EGb 761 can be effectively leveraged for its pharmacological benefits.
全球都在积极致力于从提取物中开发认知增强药物。本研究比较了不同提取物及其制成药物的化学成分,突出了优化提取物EGb 761的显著特征和潜在益处。
我们使用高效液相色谱法(HPLC)、主成分分析和液相色谱-质谱/质谱联用技术(LC-MS/MS)分析了三种提取物和十五种制成药物,以确定关键的成分差异。进行分子对接分析以评估关键成分与参与认知增强的靶蛋白的结合亲和力。对选定的提取物及其衍生产品进行细胞色素P450(CYP)抑制试验,以检查药物相互作用。
EGb 761及其制成药物呈现出独特的成分,其特征是原儿茶酸(PCA)水平显著更高。PCA与M受体、乙酰胆碱酯酶、糖原合酶激酶-3表现出强烈相互作用,这些都是认知增强的关键靶点。CYP抑制试验表明,与其他样品相比,EGb 761及其衍生药物的抑制活性较低。
EGb 761中高含量的PCA可能有助于认知益处。由于其CYP抑制作用较低,这表明对药物代谢的干扰最小,突出了其作为更安全的认知增强剂的潜力。最终,本研究表明EGb 761的成分可有效地用于其药理学益处。