摘要
为了研究滇产南方红豆杉中紫杉烷二萜类成分及具骨髓瘤细胞毒活性,运用正相、反相以及排阻色谱等分离手段对南方红豆杉枝叶提取物的化合物进行分离和纯化,通过NMR等波谱手段鉴定化合物结构,并采用CCK-8法分析化合物体外抑制NEK2过表达骨髓瘤细胞增殖作用.从该植物中分离鉴定了 16个紫杉烷二萜类化合物,分别为13-肉桂酰基-1-脱羟基巴卡丁 Ⅳ(1)、紫杉素(2)、5α-桂皮酰氧基-9α,10,13α-三乙酰氧基紫杉-4(20),11-二烯(3)、紫杉宁 E(4)、hongdoushan A(5)、11-diene-2α,5α,9α,10β,13β-pentol-2α,9α,10β,13α-tetraacetate-5α-cinnamate(6)、taxezopidine H(7)、紫杉素 B(8)、taxuyunnanine C(9)、1-deoxybaccatin Ⅵ(10)、19-羟基巴卡丁 Ⅲ(11)、巴卡丁 Ⅲ(12)、7,9,13-三去乙酰基巴卡丁 Ⅵ(13)、10-脱乙酰基巴卡丁 Ⅲ(14)、紫杉醇(15)、7-表紫杉醇(16),其中化合物1为新化合物,化合物5、13为首次从南方红豆杉中分离得到,化合物2、6、7、11有明显的抑制NEK2过表达骨髓瘤细胞增殖作用(IC50=24.0、23.5、26.1、18.3 μmol/L),化合物 16 的抑制作用尤为显著(IC50=0.6 μmol/L).
Abstract
This study aims to investigate the taxane diterpenoid constituents of Taxus chinensis var.mairei from Yunnan Prov-ince and their myeloma cytotoxic activities.Compounds were isolated and purified from the extract of the leaves and branches of Taxus chinensis var.mairei by using normal-phase,reversed-phase and size exclusion chromatography,and their structures were identified by NMR spectroscopic methods.The isolated compounds were screened for activity against NEK2 over expres-sion myeloma cell proliferation using a CCK-8 assay.Sixteen taxane diterpenoids were obtained and identified as 13-cin-namoyloxy-1-dehydroxy baccatin Ⅳ(1),taxusin(2),5α-cinnamoyloxy-9α,10β,13α-triacetoxytaxa-4(20),11-diene(3),7-deacetoxy taxinine J(4),hongdoushan A(5),11-diene-2α,5α,9α,10β,13β-pentol-2α,9α,10β,13α-tetraacetate-5α-cin-namate(6),taxezopidine H(7),taxinine B(8),taxuyunnanine C(9),1-deoxybaccatin Ⅵ(10),19-hydroxybaccatin Ⅲ(11),baccatin Ⅲ(12),7,9,13-trideacetyl baccatin Ⅵ(13),10-deacetylbaccatin Ⅲ(14),taxol(15),7-epi-taxol(16).Compound 1 was a new taxane diterpenoid,while compounds 5 and 13 were isolated from Taxus chinensis var.mairei for the first time.The results indicated that compounds 2,6,7 and 11 had notable inhibitory activity on NEK2 over expression myelo-ma cell proliferation(IC50=24.0,23.5,26.1,18.3μmol/L),and compound 16(IC50=0.6 μmol/L)had a significant effect.
维普
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