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菖蒲新 J-K:一种新型抗血管生成倍半萜类化合物,来源于.

Calamusins J-K: new anti-angiogenic sesquiterpenes from .

机构信息

Chemistry of Natural Compounds Department, Pharmaceutical and Drug Industries Research Division, National Research Centre, Dokki-Cairo, Egypt.

Institute of Organic and Biomolecular Chemistry, University of Göttingen, Göttingen, Germany.

出版信息

Nat Prod Res. 2021 Dec;35(24):5720-5731. doi: 10.1080/14786419.2020.1828404. Epub 2020 Oct 5.

DOI:10.1080/14786419.2020.1828404
PMID:33019814
Abstract

Chemical investigation of the organic extract of the marine soft coral from Red Sea, Egypt, afforded two new hydroazulenes; calamusin J () and its hydroperoxide derivative calamusin K () in addition to eight known compounds. Structure of compounds were confirmed by intensive NMR and mass spectrometry studies. The coral extract and the obtained compounds were examined against a set of diverse microorganisms. The anti-cancer properties were assessed against colon (Caco-2) and breast (MCF-7) cell lines together with their exerted cytotoxicity on the immortalized normal epithelium (hTERT-RPE1) cell type. The anti-angiogenic power was also highlighted through suppressing MCF-7 cell migration and the significant inactivation of VEGFR2 enzyme. Compounds are the most potent angiogenic inhibitors (represented by 1.2- and 1.4-fold enzyme inactivation, respectively) relative to sorafenib. The polyhydroxy sterol; 5-3,6,11-trihydroxy-24-methyl-9,11-seco-5a-cholest-7-en-9-one () inhibited effectively the growth of Caco-2 and MCF-7 with GI of 0.62 and 2.3 µM, respectively.

摘要

从埃及红海的海洋软珊瑚中提取的有机提取物进行了化学研究,得到了两种新的氢化蓝烯:菖蒲素 J()及其过氧化物衍生物菖蒲素 K(),此外还有八种已知化合物。通过深入的 NMR 和质谱研究确定了化合物的结构。对珊瑚提取物和获得的化合物进行了一系列不同微生物的检测。评估了它们的抗癌特性,针对结肠(Caco-2)和乳腺癌(MCF-7)细胞系,以及对永生化正常上皮(hTERT-RPE1)细胞类型的细胞毒性。还通过抑制 MCF-7 细胞迁移和对 VEGFR2 酶的显著失活,突出了抗血管生成能力。化合物()是最有效的血管生成抑制剂(分别代表 1.2 倍和 1.4 倍的酶失活),相对于索拉非尼。多羟基甾醇;5-3,6,11-三羟基-24-甲基-9,11-降-5a-胆甾-7-烯-9-酮()有效地抑制了 Caco-2 和 MCF-7 的生长,GI 分别为 0.62 和 2.3 μM。

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