Chemistry Department, College of Natural and Applied Sciences, University of Dar es Salaam, Dar es Salaam, Tanzania.
Department of Chemistry-BMC, Uppsala University, SE-751 23 Uppsala, Sweden.
J Nat Prod. 2021 Dec 24;84(12):3080-3089. doi: 10.1021/acs.jnatprod.1c00811. Epub 2021 Nov 21.
Five new cyclohexene derivatives, dipandensin A and B ( and ) and pandensenols A-C (-), and 16 known secondary metabolites (-) were isolated from the methanol-soluble extracts of the stem and root barks of . The structures were characterized by NMR spectroscopic and mass spectrometric analyses, and that of 6-methoxyzeylenol () was further confirmed by single-crystal X-ray crystallography, which also established its absolute configuration. The isolated metabolites were evaluated for antibacterial activity against the Gram-positive bacteria and and the Gram-negative bacteria , , , , and , as well as for cytotoxicity against the MCF-7 human breast cancer cell line. A mixture of uvaretin () and isouvaretin () exhibited significant antibacterial activity against (EC 8.7 μM) and (IC 7.9 μM). (8'α,9'β-Dihydroxy)-3-farnesylindole () showed strong inhibitory activity (EC 9.8 μM) against , comparable to the clinical reference ampicillin (EC 17.9 μM). None of the compounds showed relevant cytotoxicity against the MCF-7 human breast cancer cell line.
从杜仲茎皮和根皮的甲醇可溶性提取物中分离得到了五个新的环己烯衍生物，即二潘定 A 和 B（和）和潘登醇 A-C（-），以及 16 个已知的次生代谢产物（-）。通过 NMR 光谱和质谱分析鉴定了结构，6-甲氧基泽兰醇（）的结构进一步通过单晶 X 射线晶体学确定，其绝对构型也得到了确定。对分离得到的代谢产物进行了抗菌活性评价，针对革兰氏阳性菌和革兰氏阴性菌、、、、和 ，以及对 MCF-7 人乳腺癌细胞系的细胞毒性。乌瓦雷汀（）和异乌瓦雷汀（）的混合物对（EC8.7μM）和（IC7.9μM）表现出显著的抗菌活性。（8'α,9'β-二羟基）-3-法呢基吲哚（）对（EC9.8μM）显示出强烈的抑制活性，与临床参考氨苄西林（EC17.9μM）相当。这些化合物对 MCF-7 人乳腺癌细胞系均无相关的细胞毒性。
