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8.7 μg/mL（SI=1.92）。

Objective To investigate the diterpenes from the stem bark of Euphorbia neriifolia L. and their anti-HIV-1 activity. Methods The chemical constituents were isolated and purified by column chromatography over silica gel, ODS, MCI CHP-20P, Sephadex LH-20, and preparative HPLC. Their structures were identified by the analysis of their physicochemical properties and the spectral data of NMR and MS. The anti-HIV-1 activity of the compounds was tested by cell detection models established by HIV-1 NL4-3 infected MT-4 cells. Results Nine compounds were isolated from the stem bark of the plant, namely 12α-acetoxy-3β,7α-dihydroxy-8α-methoxyingol (1), 3β,8α,12α-triacetoxy-7α-benzoyloxyingol (2), 3β,8α,12α-triacetoxy-7α-tigloyloxyingol (3), ent-3-oxoatis-16α,17-acetonide (4), 13β-hydroxy-3,15-dioxoatis-16-ene (5), ent-3β,(13S)-dihydroxyatis-16-en-14-one (6), atis-16-en-14-oxo-3β,13(S)-diol (7), ent-(13S),18-dihydroxyatis-16-ene-3,14-dione (8), 4,13β-dihydroxy-14-oxo-3,4-secoatis-16-en-3-oic acid methyl ester (9). Conclusion Compound 1 is a new natural product. Compounds 2-4, and 6-8 are isolated from the plant for the first time. Furthermore, compound 4 exhibited moderate anti-HIV-1 activities, with EC₅₀ values of 8.7 μg/mL (SI=1.92).

国家自然科学基金资助项目（21572082）