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鉴定和定量具有内皮保护活性的废弃叶提取物中的生物活性成分。

Identification and Quantitation of the Bioactive Components in Wasted Leaves Extract with Endothelial Protective Activity.

机构信息

Institute of Chinese Materia Medica, China Academy of Chinese Medical Sciences, Beijing 100700, China.

College of Pharmacy, Chungnam National University, Daejeon 34134, Republic of Korea.

出版信息

Molecules. 2023 Aug 6;28(15):5907. doi: 10.3390/molecules28155907.

Abstract

, a renowned medicinal plant with a rich history in traditional medicine, has gained attention for its potential therapeutic applications. However, the leaves of this plant have been largely overlooked and discarded due to limited knowledge of their biological activity and chemical composition. To bridge this gap, a comprehensive study was conducted to explore the therapeutic potential of the 70% ethanol extract derived from leaves (LAE) for the treatment of cardiovascular disease (CVD). Initially, the cytotoxic effects of LAE on human umbilical vein endothelial cells (HUVECs) were assessed, revealing no toxicity within concentrations up to 5 μg/mL. This suggests that LAE could serve as a safe raw material for the development of health supplements and drugs aimed at promoting cardiovascular well-being. Furthermore, the study found that LAE extract demonstrated anti-inflammatory properties in HUVECs by modulating the PI3K/Akt and MAPK signaling pathways. These findings are particularly significant as inflammation plays a crucial role in the progression of CVD. Moreover, LAE extract exhibited the ability to suppress the expression of adhesion molecules VCAM-1 and ICAM-1, which are pivotal in leukocyte migration to inflamed blood vessels observed in various pathological conditions. In conjunction with the investigation on therapeutic potential, the study also established an optimal HPLC-PDA-ESI-MS/MS method to identify and confirm the chemical constituents present in 24 samples collected from distinct regions in South Korea. Tentative identification revealed the presence of 14 saponins and nine phenolic compounds, while further analysis using PCA and PLS-DA allowed for the differentiation of samples based on their geographical origins. Notably, specific compounds such as chlorogenic acid, isochlorogenic acid A, and quercitrin emerged as marker compounds responsible for distinguishing samples from different regions. Overall, by unraveling its endothelial protective activity and identifying key chemical constituents, this research not only offers valuable insights for the development of novel treatments but also underscores the importance of utilizing and preserving natural resources efficiently.

摘要

作为一种在传统医学中具有悠久历史的著名药用植物, 因其潜在的治疗应用而受到关注。然而,由于对其生物活性和化学成分的了解有限,这种植物的叶子在很大程度上被忽视和丢弃。为了弥补这一空白,我们进行了一项全面的研究,探索 70%乙醇提取物(LAE)对心血管疾病(CVD)治疗的潜在治疗作用。首先,我们评估了 LAE 对人脐静脉内皮细胞(HUVEC)的细胞毒性,结果表明在浓度高达 5μg/mL 时没有毒性。这表明 LAE 可以作为开发促进心血管健康的保健品和药物的安全原料。此外,研究发现 LAE 提取物通过调节 PI3K/Akt 和 MAPK 信号通路在 HUVECs 中具有抗炎作用。这些发现非常重要,因为炎症在 CVD 的发展中起着关键作用。此外,LAE 提取物还能够抑制粘附分子 VCAM-1 和 ICAM-1 的表达,这在各种病理条件下白细胞向炎症血管迁移中起着关键作用。在研究治疗潜力的同时,我们还建立了一种优化的 HPLC-PDA-ESI-MS/MS 方法,用于鉴定和确认从韩国不同地区收集的 24 个样本中的化学成分。初步鉴定表明存在 14 种皂甙和 9 种酚类化合物,而使用 PCA 和 PLS-DA 进行的进一步分析允许根据地理来源对样品进行区分。值得注意的是,绿原酸、异绿原酸 A 和槲皮苷等特定化合物被鉴定为区分不同地区样品的标记化合物。总的来说,通过揭示其内皮保护活性和鉴定关键化学成分,这项研究不仅为开发新型治疗方法提供了有价值的见解,还强调了有效利用和保护自然资源的重要性。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/efe3/10421206/455191c19eed/molecules-28-05907-g001.jpg

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