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目的研究有毒药用植物金刚纂Euphorbia neriifolia茎皮的二萜类化学成分及其抗HIV-1活性。方法利用硅胶、ODS、MCI CHP-20P、Sephadex LH-20等柱色谱和高效液相色谱技术进行系统分离,通过理化性质和NMR、MS波谱数据鉴定化合物结构;采用HIV-1病毒株NL4-3感染的人淋巴MT-4细胞作为细胞检测模型对所得化合物进行抗HIV-1活性测试。结果从金刚纂茎皮的丙酮水提取物的醋酸乙酯萃取部分分离得到9个二萜类化合物,分别被鉴定为12α-乙酰氧基-3β,7α-二羟基-8α-甲氧基续随子烷(1)、3β,8α,12α-三乙酰氧基-7α-苯甲酰氧基续随子烷(2)、3β,8α,12α-三乙酰氧基-7α-巴豆酰氧基续随子烷(3)、对映-3-氧代阿替生烷-16α,17-缩丙酮(4)、13β-羟基-3,15-二氧代阿替生烷-16-烯(5)、对映-3β,(13S)-二羟基阿替生烷-16-烯-14-酮(6)、3β,13(S)-二羟基阿替生烷-16-烯-14-酮(7)、对映-(13S),18-二羟基阿替生烷-16-烯-3,14-二酮(8)、4,13β-二羟基-14-氧代-3,4-开环阿替生烷-16-烯-3-酸甲酯(9)。结论化合物1为新天然产物,化合物2~4、6~8为首次从该植物中分离得到,药理实验结果表明化合物4具有一定的抗HIV-1活性,EC50为8.7μg/m L(SI=1.92)。
Objective To study the diterpenoid constituents and their anti-HIV-1 activity in the bark of Euphorbia neriifolia, a poisonous medicinal plant. Methods The compounds were separated by silica gel, ODS, MCI CHP-20P, Sephadex LH-20 column chromatography and high performance liquid chromatography (HPLC). The structures of compounds were identified by physico-chemical properties and NMR and MS spectral data. Infected human lymphoid MT-4 cells were used as a cell assay model to test the anti-HIV-1 activity of the compounds obtained. Results Nine diterpenoids were isolated from the ethyl acetate extracts of the acetone extracts of the rhizome of Elaeagnus angustifolia and were identified as 12α-acetoxy-3β, 7α-dihydroxy-8a-methoxy (1), 3β, 8α, 12α-triacetoxy-7α-benzoyloxycalazane (2), 3β, 8α, 12α-triacetoxy-7α-crotonyloxy (4), 13β-hydroxy-3,15-dioxometamido-16-ene (5 ), 3β, (13S) -dihydroxybutenal-16-en-14-one (6), 3β, 13 (S) -dihydroxystren-16- (8), 4,13β-dihydroxy-14-oxo-3,4- Ring opening of alane-16-ene-3-carboxylic acid methyl ester (9). Conclusion Compound 1 is a new natural product. Compounds 2 ~ 4 and 6 ~ 8 were isolated from this plant for the first time. Pharmacological results show that compound 4 has anti-HIV-1 activity with EC50 of 8.7μg / m L (SI = 1.92).