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从琴叶榕中分离得到的卡莎二萜生物碱及其抗血管生成作用。

Cassaine diterpene alkaloids from Erythrophleum fordii and their anti-angiogenic effect.

机构信息

College of Pharmacy, Catholic University of Daegu, Gyeongbuk 712-702, Republic of Korea.

College of Pharmacy, Kyungpook National University, Daegu 702-701, Republic of Korea.

出版信息

Bioorg Med Chem Lett. 2014 Jan 1;24(1):168-72. doi: 10.1016/j.bmcl.2013.11.048. Epub 2013 Nov 27.

Abstract

Angiogenesis plays a critical role in embryonic development and various physiological processes. However, excessive angiogenesis is associated with several pathological conditions including cancer. Angiogenesis is closely related to tumor growth, invasion and metastasis, and is considered a prime target for anticancer therapy. In this study, two new mono cassaine diterpenoid amides (1, 5) and four known compounds (2-4, 6) were isolated from the bark of Erythrophleum fordii (Leguminosae). Their chemical structures were established mainly by 1D and 2D NMR techniques and mass spectrometry. The effects of isolates on endothelial tube formation on Matrigel were investigated. Among them, compound 3 was found to have the most potent inhibitory effect on the capillary-like structure formation of human umbilical vein endothelial cells (HUVECs).

摘要

血管生成在胚胎发育和各种生理过程中起着关键作用。然而,过度的血管生成与包括癌症在内的多种病理状况有关。血管生成与肿瘤的生长、侵袭和转移密切相关,被认为是抗癌治疗的主要靶点。在这项研究中,从豆科的 E. fordii 的树皮中分离得到了两种新的单卡山二萜酰胺(1、5)和四种已知化合物(2-4、6)。它们的化学结构主要通过 1D 和 2D NMR 技术和质谱法确定。研究了分离物对 Matrigel 上内皮管形成的影响。其中,化合物 3 对人脐静脉内皮细胞(HUVEC)毛细血管样结构形成的抑制作用最强。

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