柴胡的化学成分、药理作用、炮制和毒性研究进展

doi:10.19803/j.1672-8629.20240996

摘要/Abstract

摘要： 目的总结柴胡化学成分、药理作用、炮制和毒性等最新研究进展,为其进一步研究与开发利用提供参考。方法通过文献调研与数据整合,分析临床应用、化学成分、药理作用、炮制现状、毒理性质等。结果根据柴胡的炮制方法,可将其分为生柴胡、醋柴胡、酒柴胡、鳖血柴胡、蜜柴胡等,不同炮制品之间药效有一定的差异,现代主要应用生柴胡和醋柴胡。柴胡临床应用广泛,现代药理研究表明其在解热、镇痛、抗炎、免疫调节、抗抑郁、保肝护肝、抗肿瘤等方面具有一定作用。柴胡临床药效显著,但是运用不当会造成肺毒性、肝毒性,故临床应用应避免超量、长期服用。结论未来,柴胡炮制致化学成分结构变化、多种炮制饮片药理作用和物质基础综合比较及柴胡炮制品毒理学研究是可供选择的研究方向;还可进一步探讨柴胡对心脏保护、肾脏保护、缓解胃溃疡、抗过敏、减轻阿尔茨海默病等疾病防治研究。

关键词: 柴胡, 化学成分, 药理作用, 炮制, 毒理性质, 临床应用

Abstract: Objective To summarize the latest progress in research on the chemical composition, pharmacological effects, Chinese materia medica processing and toxicological properties of BUPLEURI RADIX so as to provide a reference for applications and development of this drug. Methods Based on literature review and data integration, the clinical applications, chemical composition, pharmacological effects, processing methods, and toxicological properties of BUPLEURI RADIX were analyzed. Results Different processing methods yielded varying forms, such as raw BUPLEURI RADIX, vinegar-processed BUPLEURI RADIX, wine-processed BUPLEURI RADIX, turtle blood-processed BUPLEURI RADIX and honey-fried BUPLEURI RADIX, each with distinct therapeutic properties. Raw and vinegar forms were predominantly used in clinical settings. Pharmacological studies demonstrated its antipyretic, analgesic, anti-inflammatory, immunoregulatory, antidepressant, hepatoprotective, and antitumor activities. Despite its clinical efficacy, improper use could lead to pulmonary and hepatic toxicity, necessitating careful dosage and duration management. Conclusion In the future, the changes in the chemical composition structure caused by the processing of BUPLEURI RADIX, a detailed comparison of the pharmacological effects and material basis of various processed decoction pieces, and the toxicological research on processed products of BUPLEURI RADIX will be good options for research. Further research can be conducted on the role of Bupleurum chinense in heart protection, kidney protection, relief of gastric ulcers, anti-allergy treatment, and alleviation of Alzheimer’s disease.

Key words: BUPLEURI RADIX, Chemical Composition, Pharmacological Effects, Chinese Materia Medica Processing, Toxicological Properties, Clinical Application

中图分类号:

R994.11

牛源菲, 刘美婷, 时宇静, 荣文双, 马丽娜, 郑长辉, 富尧, 王连嵋, 曹俊岭. 柴胡的化学成分、药理作用、炮制和毒性研究进展[J]. 中国药物警戒, 2025, 22(9): 1073-1080.

NIU Yuanfei, LIU Meiting, SHI Yujing, RONG Wenshuang, MA Lina, ZHENG Changhui, FU Yao, WANG Lianmei, CAO Junling. Research Progress in Chemical Composition, Pharmacological Effect, Chinese Materia Medica Processing and Toxicological Properties of BUPLEURI RADIX[J]. Chinese Journal of Pharmacovigilance, 2025, 22(9): 1073-1080.

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链接本文: https://zgywjj.magtechjournal.com/CN/10.19803/j.1672-8629.20240996

https://zgywjj.magtechjournal.com/CN/Y2025/V22/I9/1073

参考文献

[1] National Pharmacopoeia Commission.Pharmacopoeia of the People's Republic of China I(中华人民共和国药典一部)[M]. Beijing: China Pharmaceutical Science Press, 2020.
[2] YANG QT, WANG YX, WU YN, et al.Analysis of 13 Chemical Constituents in the Aqueous Extract of Bei Chai Hu and Their Protective Effects against Liver Injury[J]. Central South Pharmacy(中南药学), 2022, 20(1): 74-79.
[3] WANG ZC, WANG MZ, ZHANG SY, et al. Research Progress on Compound Preparations of Classical Prescriptions[J/OL]. Asia-Pacific Traditional Medicine(亚太传统医药), (2025-06-19)[2025-08-27]. https://link.cnki.net/urlid/42.1727.R.20250618.1608.008.
[4] DONG SY, DU LJ, WANG AQ, et al.HPLC Fingerprint and Effective Component Analysis of Bupleuri Radix from Different Habitats[J]. Journal of Beijing University of Agriculture(北京农学院学报), 2021, 36(2): 95-100.
[5] National Pharmacopoeia Commission.Pharmacopoeia of the People's Republic of China I(中华人民共和国药典一部)[M]. Beijing: China Pharmaceutical Science Press, 2025.
[6] YANG X, YANG J, WANG A, et al.Saikosaponin a Ameliorates Ulcerative Colitis by Targeting the CH25H/25-OHC Axis to Inhibit NLRP3 Inflammasome in Macrophages[J]. Phytomedicine: International Journal of Phytotherapy and Phytopharmacology, 2025, 143: 156844.
[7] CHEN D, LI R, SHE F, et al.Saikosaponin C Ameliorates Tau-Related Pathology by Modulating Oxidative Stress and MAPK Axis in Alzheimer's Disease[J]. Journal of Ethnopharmacology, 2025, 352: 120221.
[8] DENG C, YANG Y, BAI Q X, et al.Saikosaponin C Ameliorates Renal Injury and Fibrosis Via Suppression of the HK2/PKM2/LDHA Signaling Mediated Glycolysis in CKD[J]. Journal of Ethno-pharmacology, 2025, 353(Pt A): 120283.
[9] YIN M, HAN X.Saikosaponin D Inhibits the Inflammatory Response of Secretory Otitis Media Through FTO-Mediated N6-Methyladenosine Modification of TLR4 mRNA[J]. BMC Pharmacology and Toxicology, 2025, 26(1): 79.
[10] DUAN Q, WANG M, CUI Z, et al.Saikosaponin D suppresses Esophageal Squamous Cell Carcinoma via the PI3K-AKT Signaling Pathway[J]. Naunyn-Schmiedeberg's Archives of Pharmacology, 2025, 398(5): 6059-6070.
[11] LUO F, YANG J, YANG X, et al.Saikosaponin D Potentiates the Antineoplastic Effects of Doxorubicin in Drug-Resistant Breast Cancer through Perturbing NQO1-Mediated Intracellular Redox Balance[J]. Phytomedicine, 2024, 133: 155945.
[12] CHEN Y, ZHANG G, LIANG R, et al.Protective Effect of Saikosaponin D against Streptozotocin-Induced Diabetic Nephropathy in Rats by Regulating the Oxidative Stress and Inflammatory Markers[J]. Indian Journal of Pharmaceutical Education and Research, 2024, 58(3): 882-889.
[13] DONG HY, SUN JM, YE TX, et al.Saikosaponin b1 Induces HCC Cells Apoptosis by Inhibiting STAT3/HSP90 and Negatively Regulating MCL1[J]. Modern Chinese Medicine(现代中医药), 2025, 45(4): 125-132.
[14] GAO HY, ZHANG JC, CHEN X, et al.Effect of Saikosaponin B2 on Renal Interstitial Fibrosis in Rats with Unilateral Ureteral Obstruction Based on TLR4/NF-κB/NLRP3 Signaling Pathway[J]. Chinese Traditional Patent Medicine(中成药), 2024, 46(6): 2053-2057.
[15] LIU YF, YAN YN, WU Y, et al.GC-MS Analysis of Chemical Components of the Volatile Oil from the Aerial Part of Bupleurum Chinense[J]. Journal of Beijing University of Traditional Chinese Medicine(北京中医药大学学报), 2004(5): 59-61.
[16] WANG SL, ZHU JJ, LU Q, et al.Study on Common Volatile Substances of Bupleurum Scorzonerifolium and Bupleurum Chinense Roots[J]. Journal of Chinese Medicinal Materials(中药材), 2024, 47(4): 927-933.
[17] ZHU XL, DU XW, ZHU SJ, et al.Antipyretic Effect of Dodecanal, the Main Chemical Constituent of the Volatile Oils from Bupleurum scorzonerifolium Willd. Roots[J]. Chinese Journal of Modern Applied Pharmacy(中国现代应用药学), 2025, 42(2): 209-214.
[18] SHI Z, CHEN RS, CHEN Y.Study on the Chemical Composition of the Essential Oil Extracted from Bupleuri Chinese by Different Methods[J]. Journal of Nanjing University of Traditional Chinese Medicine(南京中医药大学学报), 2015, 31(6): 576-578.
[19] CHANG P, LI Q.Flavonoid Biosynthetic Pathways of Bupleurum Scorzonerifolium and B. Chinense[J]. Subtropical Plant Science(亚热带植物科学), 2025, 54(2): 158-167.
[20] HU JR, LI P, ZHAO HM, et al.Anti-Inflammatory and Antioxidant Activities of Total Flavonoids from Radix Bupleuri[J]. China Food Additives(中国食品添加剂), 2023, 34(9): 82-88.
[21] WANG H, LIU ZG, HUANG XF, et al.Antioxidation in vitro of Four Active Components from Bupleurum Chinense[J]. Herald of Medicine(医药导报), 2023, 42(9): 1318-1325.
[22] GUO F.Study on the Protective Effect of Bupleurum Flavanone on Oxidative Damage in Mice after Progressive Load Exercise[D]. Jinan: Shandong Normal University, 2022.
[23] YANG XW, HU WK, JIANG X, et al.Research Progress on Chemical Composition and Pharmacological Effects of Bupleuri Radix[J]. Frontiers in Pharmaceutical Sciences(药学前沿), 2024, 28(11): 507-522.
[24] YU HJ, DOU Y, ZHU BY.Review on Chemical Constituents and Pharmacological Effects of Bupleuri Radix[J]. Special Economic Animals and Plants(特种经济动植物), 2024, 27(11): 107-109.
[25] CHEN YC, PENG DH, SUN YP, et al.Study on Protective Effect and Mechanism of Bupleurum Chinense Polysaccharides on Acute Liver Injury in Mice[J]. China Pharmacy(中国药房), 2024, 35(19): 2352-2357.
[26] LUO XK, HUANG LL.Physicochemical Properties and Antagonistic Capacity against Cell Adhesion of Polysaccharide Isolated from Bupleurum Scorzonerifolium[J]. China Modern Doctor(中国现代医生), 2023, 61(30): 51-55.
[27] ZHAO ZW.Structural Characterization and Antioxidant Activity in vitro of Polysaccharides from Bupleuri Radix[D]. Shenyang: ShenYang University of Chemical Technology, 2025.
[28] LIU ZF, WANG XS, LI P, et al.Isolation,Purification and Synergistic Anti-Liver Cancer Activity of Polysaccharide from Vinegar-Baked Bupleuri Radix[J]. Natural Product Research and Development(天然产物研究与开发), 2025, 37(1): 40-51.
[29] LIU LP, ZHANG XT, WANG FQ, et al.Study on Extraction and Purification of Phytosterol from Bupleurum chinense[J]. Feed Industry(饲料工业), 2025, 46(2): 123-128.
[30] WU LN, ZHAO L, YE G, et al.Influence of α-Spinasterol on Expression of P-gp and PEPT1 in Small Intestine of Mice[J]. Acta Agriculturae Zhejiangensis(浙江农业学报), 2016, 28(6): 944-950.
[31] XIAO GL.Protective Effect of β-sitosterol on Pentyltetrazole-Induced Epileptic Model in Mice[D]. Ganzhou: Gannan Medical University, 2025.
[32] XIN Y, LI X, LIN XZ, et al.Stigmasterol Attenuates Inflammatory Injury in Steatotic Hepatocytes Induced by Oleic Acid and Low-Density Lipoprotein Cholesterol[J]. Acta Nutrimenta Sinica(营养学报), 2025, 47(1): 46-51, 59.
[33] ZHANG R, SUO X, ZHANG HW, et al. Research Progress on Processing History Evolution, Chemical Composition and Pharmacologic Effects of Bupleuri Radix[J/OL]. Chinese Archives of Traditional Chinese Medicine(中华中医药学刊), (2025-08-12)[2025-08-28]. https://link.cnki.net/urlid/21.1546.R.20250812.1047.002.
[34] CAI Q, GE YQ, XU LJ, et al.Protective Effect of Scoparone on MCD Diet Induced Liver Fibrosis in Mice[J]. Shaanxi Journal of Traditional Chinese Medicine(陕西中医), 2021, 42(11): 1511-1516, 1521.
[35] HE N, LI LP, TAN XN, et al.Mechanism of Esculetin Promoting Ferroptosis of Mouse Breast Cancer 4T1 Cells Based on p53/SLC7A11/GPX4 Axis[J]. Chinese Journal of Pathophysiology(中国病理生理杂志), 2024, 40(2): 282-290.
[36] GAO LP.Effective Constituents and Pharmacological Action of Bupleuri Radix[J]. Electronic Journal of Clinical Medical Literature(临床医药文献电子杂志), 2017, 4(70): 13853-13854.
[37] YANG L, WANG XY, LIU C, et al.Progress in Chemical Constituents and Pharmacological Action of Bupleurum Chinense[J]. Information on Traditional Chinese Medicine(中医药信息), 2012, 29(3): 143-145.
[38] LIU DX.Effect of Different Processing Methods of Traditional Chinese Medicine on Clinical Curative Effect of Chinese Herbal Pieces[J]. Renowned Doctor(名医), 2024(17): 12-14.
[39] WU JY, YI B, XUE YH, et al.Study on the Processing and Quality Standard of Jianchangbang Wine-Processed RadixBupleuri[J]. Journal of Jiangxi University of Chinese Medicine(江西中医药大学学报), 2025, 37(1): 73-81.
[40] AN Y, YANG TS, LIU YQ.Optimization of Processing Technology of Bupleurum Chinense by Orthogonal Test[J]. Ningxia Medical Journal(宁夏医学杂志), 2013, 35(6): 557-559.
[41] DONG R, LU Y, WANG P.The Process Optimization of Vinegar Roasting of Bupleurum Chinense by Entropy Weight Method Combined with Box-Behnken Response Surface Method and Its Protective Effect on Mice Liver Injury[J]. Science and Technology of Food Industry(食品工业科技), 2021, 42(23): 209-217.
[42] SUN HM.Chemical and Pharmacological Comparison of Bupleurum chinense Before and After Vinegar Processing[D]. Taiyuan: Shanxi University, 2015.
[43] NING YM, YANG T.Comparative Research on the Antipyretic and Analgesic Effects of Processed Products of Soft-Shelled Turtle Blood-Baked Bupleurum in Different Proportions[J]. Journal of Gansu University of Chinese Medicine(甘肃中医学院学报), 2014, 31(6): 5-8.
[44] HUANG W, SUN R, YIN JW, et al.Comparative Study on Mice's Acute Toxicity of Different Components of Radix Bupleuri and Radix Bupleuri Scorzoneraefoli[J]. Chinese Journal of Pharmacovigilance(中国药物警戒), 2010, 7(8): 454-457.
[45] ZHANG Y, SHI ZC, SHI JQ, et al.Discussion on "Ancient Prescription not Coping with Modern Diseases" from Xiaochaihu Decoction Incident[J]. Acta Chinese Medicine(中医学报), 2021, 36(6): 1172-1175.
[46] HSU LM, HUANG YS, TSAY SH, et al.Acute Hepatitis Induced by Chinese Hepatoprotective Herb, Xiao-Chai-Hu-Tang[J]. Journal of the Chinese Medical Association: JCMA, 2006, 69(2): 86-88.
[47] LEE CH, WANG JD, CHEN PC.Risk of Liver Injury Associated with Chinese Herbal Products Containing Radix Bupleuri In 639 779 Patients with Hepatitis B Virus Infection[J]. PLoS One, 2011, 6(1): e16064.
[48] SUN R, HUANG W, YIN JW, et al.Effect of Jinchai Antivirus Capsules on Prevention and Treatment of Influenza A H1N1 Virus in Immunodeficiency Mouse[J]. Chinese Journal of Experimental Traditional Medical Formulae(中国实验方剂学杂志), 2010, 16(13): 190-193.