[关键词]
[摘要]
目的 研究裕丹参Salvia miltiorrhiza(主产于河南南阳的丹参)的化学成分及其抗哮喘活性。方法 利用硅胶柱色谱、凝胶柱以及制备液相色谱进行分离纯化,根据波谱数据及理化性质鉴定化合物结构;采用β-氨基己糖苷酶释放试验及RBL-2H3细胞脱颗粒模型评价所得化合物的抗哮喘活性。结果 从裕丹参醋酸乙酯部位中分离得到7个化合物,分别鉴定为 (S)-3-(3-hydroxy-4-methoxyphenyl)-1-methoxy-1-oxopropan-2-yl (2S,3S)-2-(3,4-dihydroxyphenyl)-4-((E)-3-(((S)-3-(3,4-dihydroxyphenyl)-1- ethoxy-1-oxopropan-2-yl)oxy)-3-oxoprop-1-en-1-yl)-7-hydroxy-2,3-dihydrobenzofuran-3-carboxylate(1)、迷迭香酸(2)、亚油酸甲酯(3)、4-oxononanoic acid(4)、(Z)-9-octadecenoic acid(5)、(9Z,12Z)-nonadeca-9,12-dienoic acid(6)、n-13,16-nonadecadienoic acid(7)。活性实验结果显示,化合物1能够抑制β-氨基己糖苷酶的释放,降低肥大细胞蛋白酶1(mouse mast cell protease-1,mMCP-1)、β-类胰蛋白酶(β-mast cell tryptase,β-MCT)、组胺(histamine,HIS)和白三烯C4(leukotriene C4,LTC4)水平,显著改善RBL-2H3细胞脱颗粒现象。结论 化合物1为新的水溶性酚酸类化合物,命名为9ʺ′-丹酚酸B单乙酯;其可能通过抑制肥大细胞脱颗粒发挥抗哮喘作用。
[Key word]
[Abstract]
Objective To study the chemical constituents of Salvia miltiorrhiza and their anti-asthma activity. Methods The compounds were isolated and purified by silica gel column chromatography, gel column chromatography and preparative liquid chromatography. Their structures were identified based on spectroscopic data and physicochemical properties. The anti-asthma activity of the obtained compounds was evaluated using β-hexosaminidase release assay and RBL-2H3 cell degranulation model. Results Seven compounds were isolated from the ethyl acetate fraction of S. miltiorrhiza and identified as (S)-3-(3-hydroxy-4-methoxyphenyl)-1-methoxy-1-oxopropan-2-yl (2S,3S)-2-(3,4-dihydroxyphenyl)-4-((E)-3-(((S)-3-(3,4-dihydroxyphenyl)-1-ethoxy-1-oxopropan-2-yl)oxy)-3-oxoprop-1-en-1-yl)-7-hydroxy-2,3-dihydrobenzofuran-3-carboxylate (1), rosmarinic acid (2), methyl linoleate (3), 4-oxononanoic acid (4), (Z)-9-octadecenoic acid (5), (9Z,12Z)-nonadeca-9,12-dienoic acid (6), and n-13,16-nonadecadienoic acid (7). The bioactivity results showed that compound 1 inhibited the release of β-hexosaminidase, reduced the levels of mouse mast cell protease-1 (mMCP-1), β-mast cell tryptase (β-MCT), histamine (HIS) and leukotriene C4 (LTC4), and significantly ameliorated the degranulation of RBL-2H3 cells. Conclusion Compound 1 is a new water-soluble phenolic acid, named 9′ʺ-ethyl salvianolate B, that may exert anti-asthma effect by inhibiting mast cell degranulation.
[中图分类号]
R284.1
[基金项目]
国家自然科学基金资助项目(82505008);河南省自然科学基金(252300421631);河南省卫生健康委员会国家中医药传承创新中心联合共建科研专项(2024ZXZX1185);河南省中医药科研专项(2025ZY3007);河南省博士后科研项目资助(HN2026087);河南中医药大学第一附属医院博士科研启动基金(2023BSJJ030)