旋覆花中酚酸类化合物的降脂活性研究

doi:10.12122/j.issn.1673-4254.2026.06.17

南方医科大学学报 ›› 2026, Vol. 46 ›› Issue (6): 1374-1384.doi: 10.12122/j.issn.1673-4254.2026.06.17

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旋覆花中酚酸类化合物的降脂活性研究

陈玉婷¹^,²^,⁵(), 游艳婷¹^,²^,⁴^,⁵, 黄宇舒²^,⁵, 贺飞²^,⁵(), 邱峰¹(), 杜庆锋²^,³^,⁴^,⁵()

^1.南方医科大学第七附属医院医学检验科，广东佛山 528244
^2.南方医科大学中医药学院，广东广州 510515
^3.中西医结合防治情志病基础研究卓越中心，广东广州 510515
^4.南方医科大学中西医结合医院，广东广州 510315
^5.广东省中药制剂重点实验室，广东广州 510515

收稿日期:2026-02-05 出版日期:2026-06-20 发布日期:2026-06-24
通讯作者: 贺飞,邱峰,杜庆锋 E-mail:13533207732@139.com;hefei8131@smu.edu.cn;qiufeng3079@smu.edu.cn;dqf1689@smu.edu.cn
作者简介:陈玉婷，在读硕士研究生，E-mail: 13533207732@139.com
基金资助:
国家科技重大专项(2024ZD0523400);广州市卫生健康科技重大项目(2024A031007);胰岛素抵抗相关代谢性慢病中西医结合防治创新团队(2022KCXTD003)

Hypolipidemic activity of phenolic acids from Inula japonica Thunb.

Yuting CHEN¹^,²^,⁵(), Yanting YOU¹^,²^,⁴^,⁵, Yushu HUANG²^,⁵, Fei HE²^,⁵(), Feng QIU¹(), Qingfeng DU²^,³^,⁴^,⁵()

^1.Department of Laboratory Medicine, The Seventh Affiliated Hospital, Southern Medical University, Foshan 528244, China
^2.School of Traditional Chinese Medicine, Southern Medical University, Guangzhou 510515, China
^3.Guangdong Basic Research Center of Excellence for Integrated Traditional and Western Medicine for Qingzhi Diseases, Guangzhou 510515, China
^4.Hospital of Integrated Traditional Chinese and Western Medicine, Southern Medical University, Guangzhou 510315, China
^5.Guangdong Provincial Key Laboratory of Chinese Medicine Pharmaceutics, Guangzhou 510515, China

Received:2026-02-05 Online:2026-06-20 Published:2026-06-24
Contact: Fei HE, Feng QIU, Qingfeng DU E-mail:13533207732@139.com;hefei8131@smu.edu.cn;qiufeng3079@smu.edu.cn;dqf1689@smu.edu.cn

摘要/Abstract

摘要：

目的分离与鉴定旋覆花甲醇提取部位中的酚酸类化学成分，并评估其对代谢相关脂肪性肝病的降脂活性。方法运用硅胶、十八烷基硅烷键合硅胶柱及半制备高效液相色谱技术对旋覆花甲醇提取物进行分离纯化；通过理化性质与波谱数据分析鉴定化合物结构；采用游离脂肪酸（FFA）诱导的AML12细胞脂质沉积模型，对所得化合物进行降脂活性初筛；对活性化合物进一步通过油红O、尼罗红、BODIPY染色观察脂质变化，并检测活性氧和线粒体膜电位水平评估细胞功能。结果从旋覆花中分离得到11个酚酸类化合物，分别为二氢红花菜豆酸（1）、原儿茶醛（2）、绿原酸（3）、隐绿原酸（4）、1，3-O-二咖啡酰基奎宁酸（5）、2，3-二羧基-67-二羟基-1-（3'，4'-二羟基）苯基-1，2-二氢萘-10-甲酸甲酯（6）、咖啡酸（7）、原儿茶酸（8）、3-羧基-6，7-二羟基-1-（3'，4'-二羟基苯-萘（9）、对羟基苯甲酸（10）、4-羟基苯乙酸（11）。其中，化合物1和9为首次从旋覆花属中分离，化合物6为首次从该植物中分离。活性筛选表明，化合物6和9在FFA模型中表现出降脂活性，且能显著降低细胞内总胆固醇、总甘油三酯、谷丙转氨酶和谷草转氨酶水平（P<0.05），有效减少脂质积累，并调节氧化应激与线粒体功能。结论旋覆花富含结构多样的酚酸类成分，其中化合物6和化合物9通过抑制脂质蓄积、改善氧化应激及线粒体功能障碍发挥降脂活性，可作为缓解代谢相关脂肪性肝病的潜在先导化合物。

关键词: 旋覆花, 酚酸类化合物, 降脂活性, 代谢相关脂肪性肝病

Abstract:

Objective To isolate and identify phenolic acid constituents from methanol extract of Inula japonica Thunb. and evaluate their lipid-lowering activity in vitro. Methods The methanol extract of Inula japonica Thunb. was purified using silica gel, ODS, and semi-preparative HPLC. The compound structures were determined using physicochemical and spectroscopic analyses, and their hypolipidemic activities were assessed in an AML12 cell model of free fatty acids (FFA)-induced lipid deposition. The active compounds were further assessed for their effects on lipid deposition, reactive oxygen species (ROS) production and mitochondrial membrane potential (MMP) of the cell model. Results A total of 11 phenolic acid compounds were isolated from Inula japonica Thunb., namely dihydrocaffeic acid (1), protocatechualdehyde (2), chlorogenic acid (3), cryptochlorogenic acid (4), 1,3-O-dicaffeoylquinic acid (5), 2,3-dicarboxy-6,7-hydroxy-l-(3',4'-dihydroxy)-phenyl -1,2-dihydronaphthalene-10-methyl ester (6), caffeic acid (7), protocatechuic acid (8), 3-carboxy-6,7-dihydroxy-1-(3',4'-dihydroxyphenyl)-naphthalene (9), p-hydroxybenzoic acid (10), and 4-hydroxyphenylacetic acid (11). Among them, compounds 1 and 9 were isolated for the first time from the genus Inula, and compound 6 was isolated for the first time from this plant. Compounds 6 and 9 showed lipid-lowering effects in FFA-induced AML12 cells, significantly lowered cellular levels of total cholesterol, triglyceride, alanine aminotransferase, and aspartate aminotransferase, reduced lipid accumulation, and alleviated oxidative stress and mitochondrial function. Conclusion Inula japonica Thunb. contains diverse phenolic acids, and among them compounds 6 and 9 show hypolipidemic activities via inhibiting lipid accumulation and improving oxidative stress and mitochondrial function and can potentially serve as lead compounds for treatment of metabolic dysfunction-associated steatotic liver disease.

Key words: Inula japonica Thunb, phenolic acids, hypolipidemic activity, metabolic dysfunction-associated steatotic liver disease

陈玉婷, 游艳婷, 黄宇舒, 贺飞, 邱峰, 杜庆锋. 旋覆花中酚酸类化合物的降脂活性研究[J]. 南方医科大学学报, 2026, 46(6): 1374-1384.

Yuting CHEN, Yanting YOU, Yushu HUANG, Fei HE, Feng QIU, Qingfeng DU. Hypolipidemic activity of phenolic acids from Inula japonica Thunb.[J]. Journal of Southern Medical University, 2026, 46(6): 1374-1384.

图/表 6

图1 旋覆花中分离得到的化合物1-11的结构

Fig.1 Chemical structures of compounds 1-11 isolated from Inula japonica Thunb. 1: dihydrocaffeic acid; 2: protocatechualdehyde; 3: chlorogenic acid; 4: cryptochlorogenic acid; 5: 1,3-O-dicaffeoylquinic acid; 6: 2,3-dicarboxy-6,7-hydroxy-l-(3',4'-dihydroxy)-phenyl-1,2-dihydronaphthalene-10-methyl ester; 7: caffeic acid; 8: protocatechuic acid; 9: 3-carboxy-6,7-dihydroxy-1-(3',4'-dihydroxyphenyl)-naphthalene; 10: p-hydroxybenzoic acid; 11: 4-hydroxyphenylacetic acid.

图2 化合物1-11对AML-12细胞的细胞毒性作用

Fig.2 Cytotoxic effect of the compounds 1–11 in AML12 cells (Mean±SD, n=8). A-K: Cytotoxic effect of compounds 1-11 in AML12 cells, respectively. #P<0.05, ##P<0.01, ###P<0.001, ####P<0.0001 vs CON group.

图3 化合物1-11对FFA诱导的AML12细胞MASLD模型生化指标的影响

Fig.3 Effects of compounds 1-11 on biochemical indicators in free fatty acid (FFA)-induced AML12 cells (n=3). ##P<0.01, ####P<0.001 vs CON group; *P<0.05, **P<0.01, ***P<0.001, ****P<0.0001 vs FFA group.

图4 化合物6、化合物9对FFA诱导的AML12细胞MASLD模型生化指标的影响

Fig.4 Effects of compounds 6 and 9 on biochemical indicators in FFA-induced AML12 cells (Mean±SD, n=3). A-D: Levels of TC, TG, ALT and AST contents in AML12 cells treated with FFA and different concentrations of compound 6. E-H: Levels of TC, TG, ALT and AST contents in AML12 cells treated with FFA and different concentrations of compound 9. ###P<0.001, ####P<0.0001 vs CON group; *P<0.05, **P<0.01, ***P<0.001, ****P<0.0001 vs FFA group.

图5 化合物6、化合物9对FFA诱导的AML12细胞MASLD脂滴积累的影响

Fig.5 Effects of compounds 6 and 9 on lipid droplet accumulation in FFA-induced AML12 cells (Mean±SD, n=3). A: Oil Red O staining of AML12 cells treated with FFA and different concentrations of compound 6 and compound 9 (Original magnification: ×800). B, C: Quantitative analysis of results of Oil Red O staining. D: Nile Red staining of AML12 cells treated with FFA and different concentrations of compound 6 and compound 9 (×400). E: BODIPY staining of AML12 cells treated with FFA and different concentrations of compound 6 and compound 9 (×400). F, G: Quantitative analysis of results of Nile Red staining. H, I: Quantitative analysis of results of BODIPY staining. ####P<0.0001 vs CON group; *P<0.05, **P<0.01, ***P<0.001, ****P<0.0001 vs FFA group.

图6 化合物6、化合物9对FFA诱导的AML12细胞MASLD模型ROS和MMP的影响

Fig.6 Effects of compounds 6 and 9 on ROS and mitochondrial membrane potential (MMP) in FFA-induced AML12 cells (Mean±SD, n=3). A, B: ROS levels examined by flow cytometry in AML12 cells treated with FFA and different concentrations of compound 6 and compound 9. C, D: MMP examined by flow cytometry in AML12 cells treated with FFA and different concentrations of compound 6 and compound 9. ####P<0.0001 vs CON group; *P<0.05, ***P<0.001, ****P<0.0001 vs FFA group.

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旋覆花中酚酸类化合物的降脂活性研究

Hypolipidemic activity of phenolic acids from Inula japonica Thunb.

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