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假蒟化学成分及抗神经炎活性研究

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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。
Chemical constituents of Piper sarmentosum and their anti-neuroinflammatory activity
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.

Piper L.Piper sarmentosum Roxb.camide alkaloidspiperine BN-p-coumaroyltyramineanti-neuroinflammatory activity

周漫佳、郭佳琪、周新哲、吕嘉晖、李华强、蒙雄裕、施琦、秦路平

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浙江中医药大学药学院,浙江 杭州 311403

胡椒属 假蒟 酰胺生物碱 假蒟葶碱B N-对香豆酰酪胺 抗神经炎活性

2025

中草药
天津药物研究院,中国药学会

中草药

北大核心
影响因子:1.632
ISSN:0253-2670
年,卷(期):2025.56(1)