目的 研究秦艽Gentiana macrophylla干燥根部的化学成分及抗炎保肝活性。方法 采用多种色谱学方法对秦艽正丁醇和水层萃取物进行系统的分离纯化；采用脂多糖（lipopolysaccharide，LPS）诱导的RAW 264.7巨噬细胞中炎症因子白细胞介素-6（interleukin-6，IL-6）的表达为指标，评价各化合物的抗炎活性；采用对乙酰氨基酚（paracetamol，APAP）诱导人肝细胞（LO2）为模型，研究对APAP诱导LO2细胞损伤的抑制作用，以评价各化合物的保肝活性。结果 从秦艽70%乙醇提取物中分离鉴定11个化合物，分别为 (＋)-秦艽酸甲（1a）、(−)-秦艽酸甲（1b）、gentiananoside A（2）、3′-O-β-D-葡萄糖基龙胆苦苷（3）、chinshanol A（4）、8-羟基-落叶松脂醇-4'-O-β-D-葡萄吡喃糖苷（5）、berchemol（6）、6-去甲氧基茵陈色原酮（7）、1-(β-D-ribofuranosyl)-1H-1,2,4-triazone（8）、尿嘧啶苷（9）、β-D-吡喃葡萄糖基苯甲酸酯（10）和2-苯乙基-β-D-吡喃葡萄糖（11）。活性研究显示，化合物1b对IL-6的分泌抑制效果明显；化合物1、1a、1b、2、8可降低APAP诱导的LO2细胞损伤中的丙氨酸转氨酶（alanine transaminase，ALT）和天冬氨酸转氨酶（aspartate aminotransferase，AST）水平。结论 化合物1a和1b为1对新的苯并二氢吡喃光学异构体，化合物2～3为环烯醚萜类化合物，化合物4～6为木脂素类化合物，还含有黄酮、苯环衍生物等，化合物4～5、8、10为首次从该属植物中分离得到，化合物9为首次从该植物中分离得到；部分化合物显示出良好的抗炎保肝作用前景。

Objective To investigate the chemical compositions and anti-inflammatory and hepatoprotective activities of the dried root of Qinjiao (Gentiana macrophylla). Methods Sequential chromatographic methods were employed to systematically separated the compounds of the butanol and water extracts of G. macrophylla. The anti-inflammatory activity of the compounds was evaluated by measuring the expression of interleukin-6 (IL-6), an inflammatory cytokine, in lipopolysaccharide (LPS)-induced RAW 264.7 macrophage cells. The hepatoprotective activity of the compounds was assessed using an acetaminophen (APAP)-induced liver cell (LO2) damage model. Results Eleven compounds were successfully isolated from the 70% ethanol extract of G. macrophylla. and identified as (+) cajachromane D (1a), (−) cajachromane D (1b), gentiananoside A (2), 3′-O-β-D-glucopyranosyl-gentiopicroside (3), chinshanol A (4), 8-hydroxy-lariciresinol-4'-O-β-D-glucopyranoside (5), berchemol (6), 6-demethoxycapillarisin (7), 1-(β-D-ribofuranosyl)-1H-1,2,4-triazole (8), uridine (9), β-D-glucopyranosyl benzoic acid ester (10), and 2-phenylethyl-β-D-glucopyranoside (11). Research into the capabilities demonstrated that compound 1b exerted a remarkable suppression effect on the secretion of IL-6, while compounds 1, 1a, 1b, 2 and 8 suppressed ALT and AST levels in LO2 cells damage induced by APAP. Conclusion Compounds 1a and 1b were identified as novel enantiomers of 2H-benzopyran derivatives, compounds 2—3 are iridoid terpenoids, while compounds 4—6 are lignans, along with flavonoids and phenolic derivatives. While compound 9 was initially isolated from G. macrophylla for the first time, compounds 4—5, 8, and 10 were isolated from the genus Gentiana for the first time. Notably, several of these compounds exhibited promising anti-inflammatory and hepatoprotective potential.

R284.1

云南省科技厅项目（202202AA100009，202302AA310006）；云南省高校工程研究中心（2020YGG01）；云南省教育厅重点实验室（2020YGG01）