G.B. Elyakov Pacific Institute of Bioorganic Chemistry, Far Eastern Branch of the Russian Academy of Sciences, Pr. 100-let Vladivostoku 159, 690022 Vladivostok, Russia.
Far Eastern Federal University, Sukhanova Str. 8, 690000 Vladivostok, Russia.
Mar Drugs. 2018 Nov 1;16(11):420. doi: 10.3390/md16110420.
New marine glycoconjugates-the steroidal glycosides designated as anthenosides V⁻X (⁻)-and the seven previously known anthenosides E (), G (), J (), K (), S1 (), S4 (), and S6 () were isolated from the extract of the tropical starfish . The structures of ⁻ were elucidated by extensive NMR and ESIMS techniques. Glycoside contains a rare 5α-cholest-8(14)-ene-3α,7β,16α-hydroxysteroidal nucleus. Compounds and were isolated as inseparable mixtures of epimers. All investigated compounds (⁻) at nontoxic concentrations inhibited colony formation of human melanoma RPMI-7951, breast cancer T-47D, and colorectal carcinoma HT-29 cells to a variable degree. The mixture of and possessed significant anticancer activity and induced apoptosis of HT-29 cells. The molecular mechanism of the proapoptotic action of this mixture was shown to be associated with the regulation of anti- and proapoptotic protein expression followed by the activation of initiator and effector caspases.
从热带海星中分离得到了新的海洋糖缀合物——命名为 anthenosides V⁻X（⁻）和之前已知的 7 种 anthenosides E（）、G（）、J（）、K（）、S1（）、S4（）和 S6（）。通过广泛的 NMR 和 ESIMS 技术阐明了⁻的结构。糖苷含有一个罕见的 5α-胆甾-8(14)-烯-3α,7β,16α-羟甾核。化合物和作为非对映异构体的不可分离混合物被分离出来。所有研究的化合物（⁻）在非毒性浓度下不同程度地抑制了人黑色素瘤 RPMI-7951、乳腺癌 T-47D 和结肠直肠癌细胞 HT-29 的集落形成。和的混合物具有显著的抗癌活性，并诱导 HT-29 细胞凋亡。该混合物促凋亡作用的分子机制被证明与抗凋亡和促凋亡蛋白表达的调节有关，随后是起始和效应半胱天冬酶的激活。
