Atta-ur-Rahman Institute for Natural Product Discovery , Universiti Teknologi MARA Selangor Branch, Puncak Alam Campus , 42300 Bandar Puncak Alam , Selangor Malaysia.
Department of Chemistry, Faculty of Science , University Malaya , 50603 Kuala Lumpur , Malaysia.
J Nat Prod. 2019 Sep 27;82(9):2430-2442. doi: 10.1021/acs.jnatprod.8b01067. Epub 2019 Aug 21.
Eight new bis-styryllactones, goniolanceolatins A-H (-), possessing a rare α,β-unsaturated δ-lactone moiety with a (6)-configuration, were isolated from the CHCl extract of the stembark and roots of Miq., a plant endemic to Malaysia. Absolute structures were established through extensive 1D- and 2D-NMR data analysis, in combination with electronic dichroism (ECD) data. All of the isolates were evaluated for their cytotoxicity against human lung and colorectal cancer cell lines. Compounds and showed cytotoxicity, with IC values ranging from 2.3 to 4.2 μM, and were inactive toward human noncancerous lung and colorectal cells. Compounds , , , , and showed moderate to weak cytotoxicity. Docking studies of compounds and showed that they bind with EGFR tyrosine kinase and cyclin-dependent kinase 2 through hydrogen bonding interactions with the important amino acids, including Lys721, Met769, Asn818, Arg157, Ile10, and Glu12.
八种新的双苯乙烯内酯,goniolanceolatins A-H (-),从马来西亚特有植物 Miq. 的茎皮和根的 CHCl 提取物中分离出来,具有罕见的α,β-不饱和 δ-内酯部分,且构型为 (6)-。通过广泛的 1D 和 2D-NMR 数据分析,结合电子二色性 (ECD) 数据,确定了所有化合物的绝对结构。对所有分离物进行了人肺癌和结直肠癌细胞系的细胞毒性评估。化合物 和 表现出细胞毒性,IC 值范围为 2.3 至 4.2 μM,对人非癌细胞的肺癌和结直肠细胞无活性。化合物 、 、 、 、 和 表现出中等至弱的细胞毒性。化合物 和 的对接研究表明,它们通过与重要氨基酸(包括 Lys721、Met769、Asn818、Arg157、Ile10 和 Glu12)的氢键相互作用与 EGFR 酪氨酸激酶和细胞周期蛋白依赖性激酶 2 结合。