槲皮素对心血管系统疾病的影响及其新剂型研究进展
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摘要
槲皮素广泛存在于双子叶植物的根、茎、叶中。槲皮素具有较好的止咳平喘的作用,对心血管疾病也有较好的治疗作用,如降血压、降血脂、抗动脉粥样硬化、抗心肌缺血、扩张冠状动脉、增加冠状动脉血流量等。然而,槲皮素的水溶性极低,具有口服吸收差,生物利用度低的缺点。文章总结了槲皮素对心血管系统疾病的影响,并对其新剂型进行概述,以期为槲皮素的进一步研究与开发提供参考。
Quercetin was found in the roots, stems and leaves of dicotyledonous plants. It has the pharmacological effects of relieving cough and relieving asthma and treating cardiovascular diseases, such as lowering blood pressure, lowering blood lipid, anti-atherosclerosis, anti-myocardial ischemia, dilating coronary artery, increasing coronary blood flow, etc. However, quercetin has the disadvantages of low water solubility, poor oral absorption, low bioavailability, etc. The article summarizes the effect of quercetin on cardiovascular diseases and summarizes its new dosage form, aimed to provide references for the further research and development of quercetin.
Quercetin was found in the roots, stems and leaves of dicotyledonous plants. It has the pharmacological effects of relieving cough and relieving asthma and treating cardiovascular diseases, such as lowering blood pressure, lowering blood lipid, anti-atherosclerosis, anti-myocardial ischemia, dilating coronary artery, increasing coronary blood flow, etc. However, quercetin has the disadvantages of low water solubility, poor oral absorption, low bioavailability, etc. The article summarizes the effect of quercetin on cardiovascular diseases and summarizes its new dosage form, aimed to provide references for the further research and development of quercetin.
引文
[1] Ablajan K, Abliz Z, Shang X Y, et al. Structural characterization of flavonol 3,7-di- O -glycosides and determination of the glycosylation position by using negative ion electrospray ionization tandem mass spectrometry[J]. J Mass Spectrom,2006, 41(3):352.
[2] 倪湾, 李敬双, 于洋. 洋葱槲皮素对脂多糖诱导的小鼠腹腔巨噬细胞炎症反应抑制作用[J]. 食品工业科技, 2017(23):284.
[3] 沈宇. 关于黄酮类物质的心血管保护作用及其机制的研究[D]. 南京大学博士学位论文, 2012.
[4] 郑俊媛, 曾悦, 吴江红,等. 不同剂量槲皮素对高甘油三酯血症相关性急性胰腺炎大鼠胰腺病理的影响[J]. 世界华人消化杂志, 2015,23(20):3195.
[5] Lu Y, Wang R H, Guo B B, et al. Quercetin inhibits angiotensin II induced apoptosis via mitochondrial pathway in human umbilical vein endothelial cells[J]. Eur Rev Med Pharmacol Sci, 2016, 20(8):1609.
[6] Perez A, Gonzalez-Manzano S, Jimenez R, et al. The flavonoid quercetin induces acute vasodilator effects in healthy volunteers: Correlation with beta-glucuronidase activity[J]. Pharmacol Res,2014,89:11.
[7] 李春阳, 付琳, 黄午阳,等. 蓝莓叶槲皮素和金丝桃苷的HPLC-MS鉴定及在内皮细胞中的舒血管和抗炎作用研究[J]. 现代食品科技, 2017,33(1):20.
[8] 闫磊. 芩丹胶囊及其有效成分槲皮素逆转自发性高血压大鼠心室肥厚的实验研究[D]. 山东大学博士学位论文, 2014.
[9] 侯国军, 秦小江, 侯晓敏,等. 槲皮素对肾性高血压大鼠的降压作用及机制研究[J]. 中西医结合心脑血管病杂志, 2016, 14(2):137.
[10] Li C, Wang T, Zhang C, et al. Quercetin attenuates cardiomyocyte apoptosis via inhibition of JNK and p38 mitogen-activated protein kinase signaling pathways.[J]. Gene, 2016, 577(2):275.
[11] Kumar M, Kasala E R, Bodduluru L N, et al. Molecular and biochemical evidence on the protective effects of quercetin in isoproterenol‐induced acute myocardial injury in rats[J]. J Biochem Mol Toxicol, 2017, 31(1):1.
[12] 刘慧, 张薇, 卢少平. 槲皮素在大鼠心肌损伤中的抗氧化作用[J]. 陕西医学杂志, 2017, 46(8):995.
[13] 李冬梅, 张元媛, 徐丽,等. 槲皮素对心肌缺血再灌注损伤的保护作用及机制研究[J]. 实用药物与临床, 2016, 19(4):410.
[14] Jin H B, Yang Y B, Song Y L, et al. Protective roles of quercetin in acute myocardial ischemia and reperfusion injury in rats[J]. Mol Biol Rep, 2012, 39(12):11005.
[15] 汤蕾, 彭易安, 胥甜甜,等. PKCε信号通路介导槲皮素拮抗心肌细胞缺氧/复氧损伤[J]. 中国病理生理杂志, 2013, 29(9):1567.
[16] 张雪梅, 骞秀芳. 槲皮素对大鼠心肌缺血再灌注损伤的保护作用[J]. 中国药师, 2015,18(11):1895.
[17] 刘亮. 槲皮素对动脉粥样硬化的保护作用及其机制研究[D]. 华中科技大学博士学位论文, 2014.
[18] 侯晓敏, 张明升, 赵良渊,等. 槲皮素改善高糖损伤大鼠冠脉肌原性反应的机制研究[J]. 中国病理生理杂志, 2017, 33(10):1801.
[19] 吕丽. 基于PI3K/Akt/NF-κb信号通路槲皮素抗动脉粥样硬化作用研究[D]. 吉林大学博士学位论文, 2017.
[20] 查克岚. 槲皮素对ApoE-/-小鼠动脉粥样硬化形成及SDF-1/CXCR4表达的影响研究[D]. 泸州医学院硕士学位论文, 2013.
[21] Chekalina N I, Shut S V, Trybrat T A, et al. Effect of quercetin on parameters of central hemodynamics and myocardial ischemia in patients with stable coronary heart disease[J]. Wiad Lek,2017, 70(4):707.
[22] Suri S, Liu X H, Rayment S, et al. Quercetin and its major metabolites selectively modulate cyclic GMP-dependent relaxations and associated tolerance in pig isolated coronary artery[J] .Br J Pharmacol, 2010, 159(3):566.
[23] 李丽, 冯健, 李家富. 槲皮素对大鼠心脏成纤维细胞纤维连接蛋白和转化生长因子β_1表达的影响[J]. 世界最新医学信息文摘, 2018(3):111.
[24] 章春, 冯健, 李家富. 槲皮素对TNF-α诱导的乳鼠心肌成纤维细胞增殖及P38MAPK、HMGB1蛋白表达的影响[J]. 重庆医学, 2017, 46(23):3189.
[25] 陈奎香, 李素娟, 罗健东,等. 槲皮素通过抑制蛋白酶体活性减轻心肌细胞肥大[J]. 中国病理生理杂志, 2015, 31(8):1352.
[26] Chen K, Rekep M, Wei W, et al. Quercetin Prevents In Vivo and In Vitro Myocardial Hypertrophy Through the Proteasome-GSK-3 Pathway[J]. Cardioasc Drugs Ther,2018,32(4):1.
[27] Aluani D, Tzankova V, Kondevaburdina M, et al. Еvaluation of biocompatibility and antioxidant efficiency of chitosan-alginate nanoparticles loaded with quercetin[J]. Int J Biol Macromol, 2017, 103:771.
[28] Hatahet T, Morille M, Hommoss A, et al. Liposomes, lipid nanocapsules and smart Crystals: A comparative study for an effective quercetin delivery to the skin[J]. Int J Pharm,2018,542(1-2):176.
[29] Caddeo C, Pons R, Carbone C, et al. Physico-chemical characterization of succinyl chitosan-stabilized liposomes for the oral co-delivery of quercetin and resveratrol[J]. Carbohydr Polym, 2017, 157:1853.
[31] Anwer M K, Almansoor M A, Jamil S, et al. Development and evaluation of PLGA polymer based nanoparticles of quercetin[J]. Int J Biol Macromol,2016, 92:213.
[32] 卢贞, 翟光喜. 槲皮素纳米结晶混悬剂灌胃给药大鼠体内药物动力学研究[J]. 泰山医学院学报, 2012, 33(3):202.
[33] Silva W, Torres-Gatica M F, Oyarzun-Ampuero F, et al. Double emulsions as potential fat replacers with gallic acid and quercetin nanoemulsions in the aqueous phases[J]. Food Chem,2018, 253:71.
[34] 阮婧华, 杨付梅, 张金洁,等. 槲皮素纳米结构脂质载体增加口服吸收机制研究[J]. 中国药学杂志, 2013, 48(5):368.
[35] Chen YG, Chun FY, Qi LL,et al. Development of a quercetin-loaded nanostructured lipid carrier formulation for topical delivery[J]. Int J Pharm,2012, 430(1-2):292.
[36] 张伟玲, 刘晓娟. 槲皮素自微乳制剂的制备[J]. 山东大学学报(医学版), 2016, 54(3):41.
[37] 黄瑞雪, 茅玉炜, 黎翊君,等. 姜黄素-槲皮素复方自微乳制备与评价研究[J]. 辽宁中医药大学学报, 2017,19(10):33.
[38] Murgia S, Falchi A M, Meli V, et al. Cubosome formulations stabilized by a dansyl-conjugated block copolymer for possible nanomedicine applications.[J]. Coll Surf B Biointerf,2015, 129:87.
[39] 侯天凌, 张琦, 刘丽花,等. 聚维酮联用轻质碳酸钙用于槲皮素固体分散体的制备及评价[J]. 中国实验方剂学杂志, 2017,23(10):17.
[40] Patra A, Satpathy S, Shenoy A K, et al. Formulation and evaluation of mixed polymeric micelles of quercetin for treatment of breast, ovarian, and multidrug resistant cancers[J]. Int J Nanomed,2018,13:2869.
[41] 夏晓静, 胡英, 金江,等. N-(4-咪唑甲基)-羟乙基壳聚糖自组装胶束载槲皮素的研究[J]. 中国药科大学学报, 2017, 48(1):46.
[2] 倪湾, 李敬双, 于洋. 洋葱槲皮素对脂多糖诱导的小鼠腹腔巨噬细胞炎症反应抑制作用[J]. 食品工业科技, 2017(23):284.
[3] 沈宇. 关于黄酮类物质的心血管保护作用及其机制的研究[D]. 南京大学博士学位论文, 2012.
[4] 郑俊媛, 曾悦, 吴江红,等. 不同剂量槲皮素对高甘油三酯血症相关性急性胰腺炎大鼠胰腺病理的影响[J]. 世界华人消化杂志, 2015,23(20):3195.
[5] Lu Y, Wang R H, Guo B B, et al. Quercetin inhibits angiotensin II induced apoptosis via mitochondrial pathway in human umbilical vein endothelial cells[J]. Eur Rev Med Pharmacol Sci, 2016, 20(8):1609.
[6] Perez A, Gonzalez-Manzano S, Jimenez R, et al. The flavonoid quercetin induces acute vasodilator effects in healthy volunteers: Correlation with beta-glucuronidase activity[J]. Pharmacol Res,2014,89:11.
[7] 李春阳, 付琳, 黄午阳,等. 蓝莓叶槲皮素和金丝桃苷的HPLC-MS鉴定及在内皮细胞中的舒血管和抗炎作用研究[J]. 现代食品科技, 2017,33(1):20.
[8] 闫磊. 芩丹胶囊及其有效成分槲皮素逆转自发性高血压大鼠心室肥厚的实验研究[D]. 山东大学博士学位论文, 2014.
[9] 侯国军, 秦小江, 侯晓敏,等. 槲皮素对肾性高血压大鼠的降压作用及机制研究[J]. 中西医结合心脑血管病杂志, 2016, 14(2):137.
[10] Li C, Wang T, Zhang C, et al. Quercetin attenuates cardiomyocyte apoptosis via inhibition of JNK and p38 mitogen-activated protein kinase signaling pathways.[J]. Gene, 2016, 577(2):275.
[11] Kumar M, Kasala E R, Bodduluru L N, et al. Molecular and biochemical evidence on the protective effects of quercetin in isoproterenol‐induced acute myocardial injury in rats[J]. J Biochem Mol Toxicol, 2017, 31(1):1.
[12] 刘慧, 张薇, 卢少平. 槲皮素在大鼠心肌损伤中的抗氧化作用[J]. 陕西医学杂志, 2017, 46(8):995.
[13] 李冬梅, 张元媛, 徐丽,等. 槲皮素对心肌缺血再灌注损伤的保护作用及机制研究[J]. 实用药物与临床, 2016, 19(4):410.
[14] Jin H B, Yang Y B, Song Y L, et al. Protective roles of quercetin in acute myocardial ischemia and reperfusion injury in rats[J]. Mol Biol Rep, 2012, 39(12):11005.
[15] 汤蕾, 彭易安, 胥甜甜,等. PKCε信号通路介导槲皮素拮抗心肌细胞缺氧/复氧损伤[J]. 中国病理生理杂志, 2013, 29(9):1567.
[16] 张雪梅, 骞秀芳. 槲皮素对大鼠心肌缺血再灌注损伤的保护作用[J]. 中国药师, 2015,18(11):1895.
[17] 刘亮. 槲皮素对动脉粥样硬化的保护作用及其机制研究[D]. 华中科技大学博士学位论文, 2014.
[18] 侯晓敏, 张明升, 赵良渊,等. 槲皮素改善高糖损伤大鼠冠脉肌原性反应的机制研究[J]. 中国病理生理杂志, 2017, 33(10):1801.
[19] 吕丽. 基于PI3K/Akt/NF-κb信号通路槲皮素抗动脉粥样硬化作用研究[D]. 吉林大学博士学位论文, 2017.
[20] 查克岚. 槲皮素对ApoE-/-小鼠动脉粥样硬化形成及SDF-1/CXCR4表达的影响研究[D]. 泸州医学院硕士学位论文, 2013.
[21] Chekalina N I, Shut S V, Trybrat T A, et al. Effect of quercetin on parameters of central hemodynamics and myocardial ischemia in patients with stable coronary heart disease[J]. Wiad Lek,2017, 70(4):707.
[22] Suri S, Liu X H, Rayment S, et al. Quercetin and its major metabolites selectively modulate cyclic GMP-dependent relaxations and associated tolerance in pig isolated coronary artery[J] .Br J Pharmacol, 2010, 159(3):566.
[23] 李丽, 冯健, 李家富. 槲皮素对大鼠心脏成纤维细胞纤维连接蛋白和转化生长因子β_1表达的影响[J]. 世界最新医学信息文摘, 2018(3):111.
[24] 章春, 冯健, 李家富. 槲皮素对TNF-α诱导的乳鼠心肌成纤维细胞增殖及P38MAPK、HMGB1蛋白表达的影响[J]. 重庆医学, 2017, 46(23):3189.
[25] 陈奎香, 李素娟, 罗健东,等. 槲皮素通过抑制蛋白酶体活性减轻心肌细胞肥大[J]. 中国病理生理杂志, 2015, 31(8):1352.
[26] Chen K, Rekep M, Wei W, et al. Quercetin Prevents In Vivo and In Vitro Myocardial Hypertrophy Through the Proteasome-GSK-3 Pathway[J]. Cardioasc Drugs Ther,2018,32(4):1.
[27] Aluani D, Tzankova V, Kondevaburdina M, et al. Еvaluation of biocompatibility and antioxidant efficiency of chitosan-alginate nanoparticles loaded with quercetin[J]. Int J Biol Macromol, 2017, 103:771.
[28] Hatahet T, Morille M, Hommoss A, et al. Liposomes, lipid nanocapsules and smart Crystals: A comparative study for an effective quercetin delivery to the skin[J]. Int J Pharm,2018,542(1-2):176.
[29] Caddeo C, Pons R, Carbone C, et al. Physico-chemical characterization of succinyl chitosan-stabilized liposomes for the oral co-delivery of quercetin and resveratrol[J]. Carbohydr Polym, 2017, 157:1853.
[31] Anwer M K, Almansoor M A, Jamil S, et al. Development and evaluation of PLGA polymer based nanoparticles of quercetin[J]. Int J Biol Macromol,2016, 92:213.
[32] 卢贞, 翟光喜. 槲皮素纳米结晶混悬剂灌胃给药大鼠体内药物动力学研究[J]. 泰山医学院学报, 2012, 33(3):202.
[33] Silva W, Torres-Gatica M F, Oyarzun-Ampuero F, et al. Double emulsions as potential fat replacers with gallic acid and quercetin nanoemulsions in the aqueous phases[J]. Food Chem,2018, 253:71.
[34] 阮婧华, 杨付梅, 张金洁,等. 槲皮素纳米结构脂质载体增加口服吸收机制研究[J]. 中国药学杂志, 2013, 48(5):368.
[35] Chen YG, Chun FY, Qi LL,et al. Development of a quercetin-loaded nanostructured lipid carrier formulation for topical delivery[J]. Int J Pharm,2012, 430(1-2):292.
[36] 张伟玲, 刘晓娟. 槲皮素自微乳制剂的制备[J]. 山东大学学报(医学版), 2016, 54(3):41.
[37] 黄瑞雪, 茅玉炜, 黎翊君,等. 姜黄素-槲皮素复方自微乳制备与评价研究[J]. 辽宁中医药大学学报, 2017,19(10):33.
[38] Murgia S, Falchi A M, Meli V, et al. Cubosome formulations stabilized by a dansyl-conjugated block copolymer for possible nanomedicine applications.[J]. Coll Surf B Biointerf,2015, 129:87.
[39] 侯天凌, 张琦, 刘丽花,等. 聚维酮联用轻质碳酸钙用于槲皮素固体分散体的制备及评价[J]. 中国实验方剂学杂志, 2017,23(10):17.
[40] Patra A, Satpathy S, Shenoy A K, et al. Formulation and evaluation of mixed polymeric micelles of quercetin for treatment of breast, ovarian, and multidrug resistant cancers[J]. Int J Nanomed,2018,13:2869.
[41] 夏晓静, 胡英, 金江,等. N-(4-咪唑甲基)-羟乙基壳聚糖自组装胶束载槲皮素的研究[J]. 中国药科大学学报, 2017, 48(1):46.
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