目的 研究假蒟Piper sarmentosum的化学成分及其抗神经炎活性。方法 运用多种柱色谱技术进行分离纯化，并采用波谱数据和理化数据鉴定化合物结构。同时对化合物进行抗神经炎活性的测试。结果 从假蒟95%乙醇提取物中分离得到18个化合物，分别鉴定为 (Z)-3-(3,4-二甲氧基苯基)-1-(1-吡咯烷基)-2-丙烯-1-酮（1）、金色酰胺醇酯（2）、sarmentamide B（3）、N-对香豆酰酪胺（4）、piperlotine D（5）、piperlotine C（6）、墙草碱（7）、假蒟亭碱（8）、piperlotine J（9）、马兜铃内酰胺BII（10）、piperolactam B（11）、tatarinoid C（12）、1-(2,4,5-三甲氧苯基)-1,2-丙二酮（13）、3-羟基-β-二氢大马酮（14）、(3E)-4-[(3R,4S)-3,4-二羟基-2,6,6-三甲基-1-环己烯-1-基]-3-丁烯-2-酮（15）、吐叶醇（16）、6,7-dehydro-7,8-dihydro-3-oxo-α-ionol（17）、3-氧代-α-紫罗兰醇（18）。化合物2对脂多糖（lipopolysaccharide，LPS）刺激的BV2细胞释放NO具有抑制作用，其半数抑制浓度（half maximal inhibitory concentration，IC₅₀）值为（10.77±3.19）μmol/L；化合物4和8对乙酰胆碱酯酶抑制活性的IC₅₀值分别为（48.82±3.40）μmol/L和（45.62±5.32）μmol/L。结论 化合物1为新的酰胺生物碱类化合物，命名为假蒟葶碱B；化合物11和12为首次从假蒟中分离得到。化合物2具有显著NO释放抑制活性，化合物4和8具有一定的乙酰胆碱酯酶抑制活性。

Objective This study aims to investigate the chemical constituents of Piper sarmentosum and their anti-neuroinflammatory activities. Methods A variety of column chromatographic techniques were used to separate and purify, and the structure of the compounds was identified by spectral and physiochemical data, and the anti-neuroinflammatory activity of these compounds was tested. Results A total of 18 compounds were isolated from 95% ethanol extract of P. sarmentosum and were identified as (Z)-3-(3,4-dimethoxyphenyl)-1-(pyrrolidin-1-yl)prop-2-en-1-one (1), aurantiamide acetate (2), sarmentamide B (3), N-p-coumaroyltyramine (4), piperlotine D (5), piperlotine C (6), pellitorine (7), sarmentine (8), piperlotine J (9), cepharanone B (10), piperolactam B (11), tatarinoid C (12), 1-(2,4,5-trimethoxyphenyl)-1,2-propanedione (13), 3-hydroxy-β-damascone (14), (3E)-4-[(3R,4S)-3,4-dihydroxy-2,6,6-trimethyl-1-cyclohexen-1-yl]-3-buten-2-one (15), vomifoliol (16), 6,7-dehydro-7,8-dihydro-3-oxo-α-ionol (17), 3-oxo-α-ionol (18). Compound 2 had inhibitory effect on NO release of LPS-stimulated BV2 cells with IC₅₀ value of (10.77 ±3.19) μmol/L. Compounds 4 and 8 inhibited acetylcholinesterase with IC₅₀ values of (48.82 ±3.40) and (45.62 ±5.32) μmol/L, respectively. Conclusion Compound 1 was a new amide alkaloid and named as piperine B. Compounds 11 and 12 were isolated from P. sarmentosum for the first time. Compound 2 showed significantly inhibited NO release activity, and compounds 4 and 8 had certain acetylcholinesterase inhibitory activity.

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国家自然科学基金资助项目(U2202213);浙江中医药大学校级科研项目人才专项(2023RCZXZK27)