| 2,387 | 42 | 142 |
| 下载次数 | 被引频次 | 阅读次数 |
高良姜素是主要存在于中药高良姜、蜂胶中的一种天然黄酮类化合物。现代研究表明,高良姜素具有抗炎、抗肿瘤、皮肤保护、抗糖尿病及其并发症、抗纤维化、抗病原微生物、神经保护等多种药理活性,应用前景广阔。本文对高良姜素的药理作用及作用机制进行综述,以期为高良姜素在医药领域的开发应用提供理论依据。
Abstract:Galangin is a natural flavonoid compound mainly existing in Chinese medicinal materials Rhizoma Alpiniae Officinarum and Propolis. Modern studies show that galangin has pharmacological activities such as anti-inflammation, anti-tumor, skin protection, anti-diabetes and its complications, anti-fibrosis, microbial resistance, and neuroprotection, with a broad application prospect. In this paper, the pharmacological activities and mechanism of galangin were summarized, in order to provide a theoretical basis for the development and application of galangin in the field of medicine.
[1]国家药典委员会.中华人民共和国药典.一部[S].北京:中国医药科技出版社,2020:300.
[2]MA Y L,ZHAO F,YIN J T,et al.Two Approaches for Evaluating the Effects of Galangin on the Activities and mRNA Expression of Seven CYP450[J].Molecules,2019,24(6):1171.
[3]LU H,YAO H,ZOU R,et al.Galangin Suppresses Renal Inflammation via the Inhibition of NF-κB,PI3K/AKT and NLRP3 in Uric Acid Treated NRK-52E Tubular Epithelial Cells[J].Biomed Res Int,2019,2019:3018357.
[4]FU Q,GAO Y,ZHAO H,et al.Galangin protects human rheumatoid arthritis fibroblast like synoviocytes via suppression of the NF κB/NLRP3 pathway[J].Molecular medicine reports,2018,18(4):3619-3624.
[5]Choi M J,Lee E J,Park J S,et al.Anti-inflammatory mechanism of galangin in lipopolysaccharide-stimulated microglia:Critical role of PPAR-γ signaling pathway[J].Biochem Pharmacol,2017,144:120-131.
[6]Sangaraju R,Nalban N,Alavala S,et al.Protective effect of galangin against dextran sulfate sodium (DSS)-induced ulcerative colitis in Balb/c mice[J].Inflamm Res,2019,68(8):691-704.
[7]Gerges S H,Tolba M F,Elsherbiny D A,et al.The natural flavonoid galangin ameliorates dextran sulphate sodium-induced ulcerative colitis in mice:Effect on Toll-like receptor 4,inflammation and oxidative stress[J].Basic Clin Pharmacol Toxicol,2020,127(1):10-20.
[8]SONG H Y,KIM W S,HAN J M,et al.Galangin treatment during dendritic cell differentiation confers tolerogenic properties in response to lipopolysaccharide stimulation[J].J Nutr Biochem,2021,87:108524.
[9]ZHU L,LUO Q,BI J,et al.Galangin inhibits growth of human head and neck squamous carcinoma cells in vitro and in vivo[J].Chem Biol Interact,2014,224:149-156.
[10]Tolomeo M,Grimaudo S,Di Cristina A,et al.Galangin increases the cytotoxic activity of imatinib mesylate in imatinib-sensitive and imatinib-resistant Bcr-Abl expressing leukemia cells[J].Cancer Lett,2008,265(2):289-297.
[11]Murray T J,Yang X,Sherr D H.Growth of a human mammary tumor cell line is blocked by galangin,a naturally occurring bioflavonoid,and is accompanied by down-regulation of cyclins D3,E,and A[J].Breast Cancer Res,2006,8(2):R17.
[12]Lee C C,Lin M L,Meng M,et al.Galangin Induces p53-independent S-phase Arrest and Apoptosis in Human Nasopharyngeal Carcinoma Cells Through Inhibiting PI3K-AKT Signaling Pathway[J].Anticancer Res,2018,38(3):1377-1389.
[13]SONG W,YAN C Y,ZHOU Q Q,et al.Galangin potentiates human breast cancer to apoptosis induced by TRAIL through activating AMPK[J].Biomed Pharmacother,2017,89:845-856.
[14]LIU D,YOU P,LUO Y,et al.Galangin Induces Apoptosis in MCF-7 Human Breast Cancer Cells Through Mitochondrial Pathway and Phosphatidylinositol 3-Kinase/Akt Inhibition[J].Pharmacology,2018,102(1-2):58-66.
[15]ZOU W W,XU S P.Galangin inhibits the cell progression and induces cell apoptosis through activating PTEN and Caspase-3 pathways in retinoblastoma[J].Biomed Pharmacother,2018,97:851-863.
[16]朱敏,郗雪艳,杜伯雨.LncRNA H19在肿瘤发病中的作用机制研究进展[J].中国免疫学杂志,2021,37(7):883-887.
[17]ZHONG X,HUANG S,LIU D,et al.Galangin promotes cell apoptosis through suppression of H19 expression in hepatocellular carcinoma cells[J].Cancer Med,2020,9(15):5546-5557.
[18]Kumar R,Tiku A B.Galangin induces cell death by modulating the expression of glyoxalase-1 and Nrf-2 in HeLa cells[J].Chem Biol Interact,2018,279:1-9.
[19]Russo M,Russo G L.Autophagy inducers in cancer[J].Biochem Pharmacol,2018,153:51-61.
[20]WANG Y,WU J,LIN B,et al.Galangin suppresses HepG2 cell proliferation by activating the TGF-β receptor/Smad pathway[J].Toxicology,2014,326:9-17.
[21]梁晓晖,余明珠,石海莲,等.高良姜素抑制胃癌MGC803细胞NF-κB通路促进自噬[J/OL].中国中药杂志,1-9[2021-06-02].
[22]LI X,WANG Y,XIONG Y,et al.Galangin Induces Autophagy via Deacetylation of LC3 by SIRT1 in HepG2 Cells[J].Sci Rep,2016,6:30496.
[23]CHOU C W,HUANG Y K,KUO T T,et al.An Overview of ADAM9:Structure,Activation,and Regulation in Human Diseases[J].Int J Mol Sci,2020,21(20):7790.
[24]LEI D,ZHANG F,YAO D,et al.Galangin increases ERK1/2 phosphorylation to decrease ADAM9 expression and prevents invasion in A172 glioma cells[J].Mol Med Rep,2018,17(1):667-673.
[25]HUANG H.Matrix Metalloproteinase-9 (MMP-9) as a Cancer Biomarker and MMP-9 Biosensors:Recent Advances[J].Sensors (Basel),2018,18(10):3249.
[26]Chien S T,Shi M D,Lee Y C,et al.Galangin,a novel dietary flavonoid,attenuates metastatic feature via PKC/ERK signaling pathway in TPA-treated liver cancer HepG2 cells[J].Cancer Cell Int,2015,15:15.
[27]ZOU Y,LI R,KUANG D,et al.Galangin Inhibits Cholangiocarcinoma Cell Growth and Metastasis through Downregulation of MicroRNA-21 Expression[J].Biomed Res Int,2020,2020:5846938.
[28]ZHANG W,TANG B,HUANG Q,et al.Galangin inhibits tumor growth and metastasis of B16F10 melanoma[J].J Cell Biochem,2013,114(1):152-161.
[29]CAO J,WANG H,CHEN F,et al.Galangin inhibits cell invasion by suppressing the epithelial-mesenchymal transition and inducing apoptosis in renal cell carcinoma[J].Mol Med Rep,2016,13(5):4238-4244.
[30]CHEN D,LI D,XU X B,et al.Galangin inhibits epithelial-mesenchymal transition and angiogenesis by downregulating CD44 in glioma[J].J Cancer,2019,10(19):4499-4508.
[31]HUANG H,CHEN A Y,YE X,et al.Galangin,a Flavonoid from Lesser Galangal,Induced Apoptosis via p53-Dependent Pathway in Ovarian Cancer Cells[J].Molecules,2020,25(7):1579.
[32]YU S,GONG L S,LI N F,et al.Galangin (GG) combined with cisplatin (DDP) to suppress human lung cancer by inhibition of STAT3-regulated NF-κB and Bcl-2/Bax signaling pathways[J].Biomed Pharmacother,2018,97:213-224.
[33]沈存思,杨福州,项莹颖,等.中药活性化合物高良姜素与吉非替尼抗非小细胞肺癌的协同增效作用及机制研究[J].南京中医药大学学报,2021,37(1):72-76.
[34]贺文煜,张海明,袁昌劲.高良姜素通过PI3K/Akt及p38-MAPK信号通路增强胃癌SGC-7901细胞对阿帕替尼的敏感性[J].天津医药,2019,47(10):1020-1025.
[35]赵艳姣,范浩,廉斌.高良姜素通过PTEN/AKT信号通路抑制乳腺癌发展并增加曲妥珠单抗抗肿瘤活性[J].天然产物研究与开发,2021,33(5):819-830.
[36]Madduma Hewage S R,Piao M J,Kim K C,et al.Galangin (3,5,7-trihydroxyflavone) shields human keratinocytes from ultraviolet B-induced oxidative stress[J].Biomol Ther (Seoul),2015,23(2):165-173.
[37]Madduma Hewage S R K,Piao M J,Kang K A,et al.Galangin Activates the ERK/AKT-Driven Nrf2 Signaling Pathway to Increase the Level of Reduced Glutathione in Human Keratinocytes[J].Biomol Ther (Seoul),2017,25(4):427-433.
[38]Ye-Jin Kim et al.Protective effects of galangin against UVB irradiation-induced photo-aging in CCD-986sk human skin fibroblasts[J].Applied Biological Chemistry,2019,62(1):1-8.
[39]WEN S Y,CHEN J Y,CHEN C J,et al.Protective effects of galangin against H2O2-induced aging via the IGF-1 signaling pathway in human dermal fibroblasts[J].Environ Toxicol,2020,35(2):115-123.
[40]Chung K W,Jeong H O,Lee E K,et al.Evaluation of Antimelanogenic Activity and Mechanism of Galangin in Silico and in Vivo[J].Biol Pharm Bull,2018,41(1):73-79.
[41]Sangaraju Rajendra et al.Galangin ameliorates Imiquimod-Induced psoriasis-like skin inflammation in BALB/c mice via down regulating NF-κB and activation of Nrf2 signaling pathways[J].International Immunopharmacology,2021,96:107754.
[42]Choi J K,Kim S H.Inhibitory effect of galangin on atopic dermatitis-like skin lesions[J].Food Chem Toxicol,2014,68:135-141.
[43]Aloud A A,Chinnadurai V,Chandramohan G,et al.Galangin controls streptozotocin-caused glucose homeostasis and reverses glycolytic and gluconeogenic enzyme changes in rats[J].Arch Physiol Biochem,2020,126(2):101-106.
[44]Aloud A A,Chinnadurai V,Govindasamy C,et al.Galangin,a dietary flavonoid,ameliorates hyperglycaemia and lipid abnormalities in rats with streptozotocin-induced hyperglycaemia[J].Pharm Biol,2018,56(1):302-308.
[45]Kalhotra P,Chittepu VCSR,Osorio-Revilla G,et al.Discovery of Galangin as a Potential DPP-4 Inhibitor That Improves Insulin-Stimulated Skeletal Muscle Glucose Uptake:A Combinational Therapy for Diabetes[J].Int J Mol Sci,2019,20(5):1228.
[46]Aloud A A,Veeramani C,Govindasamy C,et al.Galangin,a dietary flavonoid,improves antioxidant status and reduces hyperglycemia-mediated oxidative stress in streptozotocin-induced diabetic rats[J].Redox Rep,2017,22(6):290-300.
[47]Aloud A A,Veeramani C,Govindasamy C,et al.Galangin,a natural flavonoid reduces mitochondrial oxidative damage in streptozotocin-induced diabetic rats[J].Redox Rep,2018,23(1):29-34.
[48]LIU Y,LIANG X,ZHANG G,et al.Galangin and Pinocembrin from Propolis Ameliorate Insulin Resistance in HepG2 Cells via Regulating Akt/mTOR Signaling[J].Evid Based Complement Alternat Med,2018,2018:7971842.
[49]ZHANG T,MEI X,Ouyang H,et al.Natural flavonoid galangin alleviates microglia-trigged blood-retinal barrier dysfunction during the development of diabetic retinopathy[J].J Nutr Biochem,2019,65:1-14.
[50]LIAO J,LIU B,CHEN K,et al.Galangin attenuates oxidative stress-mediated apoptosis in high glucose-induced renal tubular epithelial cells through modulating renin-angiotensin system and PI3K/AKT/mTOR pathway[J].Toxicol Res (Camb),2021,10(3):551-560.
[51]Abukhalil M H,Althunibat O Y,Aladaileh S H,et al.Galangin attenuates diabetic cardiomyopathy through modulating oxidative stress,inflammation and apoptosis in rats[J].Biomed Pharmacother,2021,138:111410.
[52]Xiong Y,Lu H,Xu H.Galangin Reverses Hepatic Fibrosis by Inducing HSCs Apoptosis via the PI3K/Akt,Bax/Bcl-2,and Wnt/β-Catenin Pathway in LX-2 Cells[J].Biol Pharm Bull,2020,43(11):1634-1642.
[53]杨晶晶,王辉波,廖海含,等.高良姜素减轻压力负荷诱导的心脏纤维化[J].武汉大学学报(医学版),2020,41(6):889-893.
[54]Thangaiyan R,Arjunan S,Govindasamy K,et al.Galangin Attenuates Isoproterenol-Induced Inflammation and Fibrosis in the Cardiac Tissue of Albino Wistar Rats[J].Front Pharmacol,2020,11:585163.
[55]WANG L,LIU H,HE Q,et al.Galangin ameliorated pulmonary fibrosis in vivo and in vitro by regulating epithelial-mesenchymal transition[J].Bioorg Med Chem,2020,28(19):115663.
[56]ZHANG Y F,SHAN S,WANG J,et al.Correction to:Galangin inhibits hypertrophic scar formation via ALK5/Smad2/3 signaling pathway[J].Molecular and Cellular Biochemistry,2020,468(1-2):195-196.
[57]Echeverría J,Opazo J,Mendoza L,et al.Structure-Activity and Lipophilicity Relationships of Selected Antibacterial Natural Flavones and Flavanones of Chilean Flora[J].Molecules,2017,22(4):608.
[58]Ouyang J,Sun F,Feng W,et al.Antimicrobial Activity of Galangin and Its Effects on Murein Hydrolases of Vancomycin-Intermediate Staphylococcus aureus (VISA) Strain Mu50[J].Chemotherapy,2018,63(1):20-28.
[59]ZOU M,LIU H,LI J,et al.Structure-activity relationship of flavonoid bifunctional inhibitors against Zika virus infection[J].Biochem Pharmacol,2020,177:113962.
[60]Kilic F S,Kaygisiz B,Aydin S,et al.The effects and mechanisms of the action of galangin on spatial memory in rats[J].Bratisl Lek Listy,2019,120(12):881-886.
[61]张赫,郑焱.β淀粉样蛋白级联假说相关的阿尔茨海默病发病机制及防治策略研究进展[J].中国医学科学院学报,2019,41(5):702-708.
[62]ZENG H,HUANG P,WANG X,et al.Galangin-induced down-regulation of BACE1 by epigenetic mechanisms in SH-SY5Y cells[J].Neuroscience,2015,294:172-181.
[63]HUANG L,LIN M,ZHONG X,et al.Galangin decreases p tau,Aβ42 and β secretase levels,and suppresses autophagy in okadaic acid induced PC12 cells via an Akt/GSK3β/mTOR signaling dependent mechanism[J].Mol Med Rep,2019;19(3):1767-1774.
[64]CHEN G,LIU J,JIANG L,et al.Galangin Reduces the Loss of Dopaminergic Neurons in an LPS-Evoked Model of Parkinson's Disease in Rats[J].Int J Mol Sci,2017,19(1):12.
[65]LI X,JIANG J,YANG Z,et al.Galangin suppresses RANKL-induced osteoclastogenesis via inhibiting MAPK and NF-κB signalling pathways[J].J Cell Mol Med,2021,25(11):4988-5000.
[66]ZHANG X,DENG Y,XIANG J,et al.Galangin Improved Non-Alcoholic Fatty Liver Disease in Mice by Promoting Autophagy [J].Drug design,development and therapy,2021,15:231-231.
[67]Henry L J K,Ramar M K,Palanisamy S,et al.Mechanistic investigation of PPARγ-facilitated anti-asthmatic effects of Galangin (Norizalpinin):Insights from in silico and in vivo analyses[J].Biochem Biophys Res Commun,2020,526(3):833-840.
[68]张欣,陈曦文,卢昊,等.高良姜素自微乳大鼠在体肠吸收和体内药动学研究[J].中药新药与临床药理,2021,32(11):1699-1704.
[69]陈曦文,卢昊,张欣,等.单纯形网格法优化设计高良姜素自微乳处方[J].中药材,2020,43(11):2753-2758.
[70]Sabry Shereen,El hakim Ramadan Abd,Abd elghany Mahmoud,et al.Formulation,characterization,and evaluation of the anti-tumor activity of nanosized galangin loaded niosomes on chemically induced hepatocellular carcinoma in rats[J].Journal of Drug Delivery Science and Technology,2020:102163.
[71]YAO H,LU H,ZHANG J,et al.Preparation of Prolonged-Circulating Galangin-Loaded Liposomes and Evaluation of Antitumor Efficacy In Vitro and Pharmacokinetics In Vivo[J].Journal of Nanomaterials,2019,2019:1-9.
[72]赵玲,吴斐华.高良姜素结构修饰及对K562细胞的抑制活性[J].武汉轻工大学学报,2016,35(4):31-36.
基本信息:
DOI:10.13412/j.cnki.zyyl.20220424.001
中图分类号:R285
引用信息:
[1]王晓晴,孙允红,赵方舒,等.高良姜素的药理作用及机制研究进展[J].中药药理与临床,2023,39(08):115-120.DOI:10.13412/j.cnki.zyyl.20220424.001.
基金信息:
山东省自然科学基金(编号:ZR2019QH007); 山东省重点研发计划(重大科技创新工程)(编号:2020CXGC010505、2021CXGC010511); 山东省中医药科技项目(编号:2020M009)
2022-04-25
2022-04-25
2022-04-25