根皮苷的分离纯化及药理研究进展
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摘要
根皮苷是广泛存在于苹果根、茎、叶和果实中的一种二氢查耳酮类物质,在多种植物中均有发现,国内外先后有近3 000篇文献对根皮苷的相关信息进行报道,广泛受到多个领域研究人员的关注,这很可能因为它具降血糖、抗氧化、保护视网膜、保护肝脏、美白、杀菌等多种生物活性,这暗示着根皮苷在医药、美容、农业等多个领域都具有潜在的开发价值。文章对有关根皮苷最近几年的提取合成、分离纯化以及多种生物活性及其药效作用机制进行了整理分析概括,希望对根皮苷的进一步广泛研究和在各个领域被快速开发运用提供一些帮助。
Phlorizin is a dihydrochalcone widely found in the roots, stems, leaves and fruits of apples. It has been found in a variety of plants. There have been nearly 3 000 papers about phlorizin at home and abroad. It has received extensive attention from researchers in different fields, which is probably for the reason that it has hypoglycemic, antioxidation, retina and liver protection, whitening, bactericidal and other biological activities. It is suggested that there is potential development value for phlorizin in medicine, cosmetology, agriculture and other fields. This paper analyzes and summarizes the extraction and synthesis,isolation and purification as well as its various biological activities and pharmacodynamic mechanisms of phlorizin in recent years,hoping to provide some help in further extensive research on phlorizin and its rapid development and application in various fields.
Phlorizin is a dihydrochalcone widely found in the roots, stems, leaves and fruits of apples. It has been found in a variety of plants. There have been nearly 3 000 papers about phlorizin at home and abroad. It has received extensive attention from researchers in different fields, which is probably for the reason that it has hypoglycemic, antioxidation, retina and liver protection, whitening, bactericidal and other biological activities. It is suggested that there is potential development value for phlorizin in medicine, cosmetology, agriculture and other fields. This paper analyzes and summarizes the extraction and synthesis,isolation and purification as well as its various biological activities and pharmacodynamic mechanisms of phlorizin in recent years,hoping to provide some help in further extensive research on phlorizin and its rapid development and application in various fields.
引文
[1]胡莎.根皮苷对果蝇抗衰老的机理研究.天津:天津科技大学,2011
[2]Gosch C,Halbwirth H,Stich K.Phloridzin:biosynthesis,distribution and physiological relevance in plants.Phytochemistry,2010,71(8/9):838-843
[3]董华强,宁正祥.根皮苷与糖尿病防治.食品科技,2006,31(12):192-195
[4]谭飔,周志钦.根皮苷研究进展.食品与发酵工业,2013,39(8):182-186
[5]王奇志,王新为,李文雅,等.根皮苷的研究进展及其应用.中药与天然药高峰论坛暨全国中药和天然药物学术研讨会,2012
[6]Gosch C,Halbwirth H,Kuhn J,et al.Biosynthesis of phloridzin in apple(Malus domestica Borkh.).Plant Science,2009,176(2):223-231
[7]Dare A P,Tomes S,Cooney J M,et al.The role of enoylreductase genes in phloridzin biosynthesis in apple.Plant Physiology and Biochemistry,2013,72:54-61
[8]朱珊,王文倩,李赫宇,等.根皮苷标准品的研制.中药饮片质量分析与中药鉴别技术交流研讨会论文集,2009
[9]徐凯,吕海涛.正交实验优选苹果皮中根皮苷提取工艺.中南药学,2009,7(7):497-499
[10]丰金玉,秦昱,段继春,等.超声波辅助提取多穗石柯根皮苷研究.中国农学通报,2015,31(10):251-255
[11]秦昱,丰金玉,段继春,等.大孔吸附树脂分离纯化多穗石柯根皮苷.中国农学通报,2015,31(36):269-275
[12]杨大坚,钟炽昌.甜茶化学成分研究Ⅰ.甜味成分.中草药,1991,22(3):99-101
[13]冯雪娇,曹学丽,李艳,等.根皮苷的应用及分离纯化研究进展.食品科学技术学报,2008,26(4):13-16
[14]李胜华,伍贤进,牛有芽.D-101大孔树脂纯化多穗柯中根皮苷的工艺研究.食品科技,2010,35(7):217-221
[15]Sun L,Liu D,Sun J,et al.Simultaneous separation and purification of chlorogenic acid,epicatechin,hyperoside and phlorizin from thinned young Qinguan,apples by successive use of polyethylene and polyamide resins.Food Chemistry,2017,230:362-371
[16]Sun L,Guo Y,Fu C,et al.Simultaneous separation and purification of total polyphenols,chlorogenic acid and phlorizin from thinned young apples.Food Chemistry,2013,136(2):1022-1029
[17]王慧莹.多穗柯根皮苷的提取纯化研究.长沙:中南大学,2014
[18]李荣涛,焦中高,刘杰超,等.高效离心分配色谱(HPCPC)分离纯化苹果树枝中的根皮苷.果树学报,2010,27(4):645-649
[19]吕朝磊,雷巧灵,张宪宝,等.基于基因调控网络的糖肾方治疗糖尿病肾病作用机理解析.中华中医药杂志,2018,33(4):1320-1324
[20]Mudaliar S,Polidori D,Zambrowicz B,et al.Sodium-glucose cotransporter inhibitors:Effects on renal and intestinal glucose transport:From bench to bedside.Diabetes Care,2015,38(12):2344
[21]Coady M J,Wallendorff B,Lapointe J Y.Characterization of the transport activity of SGLT2/MAP17,the renal low-affinity Na+/glucose cotransporter.Am J Physiol Renal Physiol,2017,313(2):F467-F474
[22]袁璐,李倩,高谷,等.钠葡萄糖协同转运子2抑制剂:糖尿病治疗的新选择.国际内分泌代谢杂志,2010,30(5):321-323
[23]Powell D R,Dacosta C M,Gay J,et al.Improved glycemic control in mice lackingSglt1 and Sglt2.American Journal of Physiology Endoc A rinology&Metabolism,2013,304(2):E117-E130
[24]Yamaguchi K,Kato M,Suzuki M,et al.Pharmacokinetic and pharmacodynamic modeling of the effect of an sodium-glucose cotransporter inhibitor,phlorizin,on renal glucose transport in rats.Drug Metabolism&Disposition the Biological Fate of Chemicals,2011,39(10):1801
[25]Rossetti L,Shulman G I,Zawalich W,et al.Effect of chronic hyperglycemiaon in vivo insulin secretion in partially pancreatectomized rats.J Clin Invest,1987,80(4):1037-1044
[26]RossettiL,SmithD,ShsulmanGI,etal.Correctionof hyperglycemiawith phlorizin normalizes tissue sensitivity toinsulin in diabetic rats.J Clin Invest,1987,79(5):1510-1515
[27]Mei X,Zhang X,Wang Z,et al.Insulin Sensitivity-enhancing activity of phlorizin is associated with lipopolysaccharide decrease and gut microbiota changes in obese and type 2 diabetes(db/db)mice.Journal of Agricultural&Food Chemistry,2016,64(40):7502
[28]申婷婷,花尔并,马娜,等.根皮苷对饲喂高脂高胆固醇饲料仓鼠肝脏中胆固醇代谢调控基因表达的影响.营养学报,2014,36(2):159-163
[29]沈琳.根皮苷对db/db小鼠主动脉的保护作用机制研究.济南:山东大学,2013
[30]蔡茜.根皮苷对db/db小鼠糖尿病心肌病变保护机制的定量蛋白质组学研究.济南:山东大学,2013
[31]郭建茹.根皮苷对肥胖小鼠糖脂代谢的影响及作用机制的初步研究.广州:广州中医药大学,2013
[32]Zhao S,Bomser J,Joseph E L,et al.Intakes of apples or apple polyphenols decease plasma values for oxidized low-density lipoprotein/beta 2-glycoprotein I complex.Journal of Functional Foods,2013,5(1):493-497
[33]伍春,李彦龙,张帆.中医药抗皮肤衰老的研究进展.中华中医药杂志,2014,29(9):2889-2891
[34]Magwere T,West M,Riyahi K,et al.The effects of exogenous antioxidants on lifespan and oxidative stress resistance in Drosophila melanogaster.Mechanisms of Ageing&Development,2006,127(4):356-370
[35]Yu H,Qin C,Zhang P,et al.Antioxidant effect of apple phenolic on lipid peroxidation in Chinese-style sausage.Journal of Food Science&Technology,2015,52(2):1032-1039
[36]Ana Milisavljevi?,Marija Stojanovi?,Milica Carevi?,et al.Lipasecatalyzed esterification of phloridzin:Acyl donor effect on enzymatic affinity and antioxidant properties of esters.Industrial&Engineering Chemistry Research,2014,53(43):16644-16651
[37]王建新,周忠,王建国.根皮素抑酪氨酸酶活性研究.香料香精化妆品,2002(2):4-5
[38]Lin Y P,Hsu F L,Chen C S,et al.Constituents from the Formosan apple reduce tyrosinase activity in human epidermal melanocytes.Phytochemistry,2007,68(8):1189-1199
[39]翟一淼.根皮苷保护表皮细胞抵抗UVB损伤的作用及分子机制研究.上海:华东师范大学,2014
[40]赵江,陈纯,马娜,等.根皮苷对雄性果蝇抗衰老活性的研究.营养学报,2015(4):372-375
[41]贺军花,马利菁,周会玲.根皮苷对苹果采后灰霉病的影响.咸阳:西北农林科技大学,2017
[42]张世阳.根皮苷对db/db小鼠视网膜保护机制的研究.济南:山东大学,2013
[43]Ehrenkranz J R,Lewis N G,Kahn C R,et al.Phlorizin:a review.Diabetes/Metabolism Research&Reviews,2005,21(1):31-38
[44]冯天艳,方荣,邓改改,等.根皮苷对小鼠CCl4急性肝损伤的保护作用.中药药理与临床,2010(5):47-50
[45]张硕,袁希平,王庆林.根皮苷对血吸虫病肝纤维化小鼠肝脏中TGF-β1和PDGF-BB表达的影响.华西药学杂志,2015,30(1):42-46
[46]Khalifa M,Bakr A G,Osman A T.Protective effects of phloridzin against methotrexate-induced liver toxicity in rats.Biomedicine&Pharmacotherapy,2017,95:529-535
[47]Ikumi Y,Kida T,Sakuma S,et al.Polymer-phloridzin conjugates as an anti-diabetic drug that Inhibits glucose absorption through the Na+/glucose cotransporter(SGLT1)in the small intestine.Journal of Controlled Release,2008,125(1):42-49
[2]Gosch C,Halbwirth H,Stich K.Phloridzin:biosynthesis,distribution and physiological relevance in plants.Phytochemistry,2010,71(8/9):838-843
[3]董华强,宁正祥.根皮苷与糖尿病防治.食品科技,2006,31(12):192-195
[4]谭飔,周志钦.根皮苷研究进展.食品与发酵工业,2013,39(8):182-186
[5]王奇志,王新为,李文雅,等.根皮苷的研究进展及其应用.中药与天然药高峰论坛暨全国中药和天然药物学术研讨会,2012
[6]Gosch C,Halbwirth H,Kuhn J,et al.Biosynthesis of phloridzin in apple(Malus domestica Borkh.).Plant Science,2009,176(2):223-231
[7]Dare A P,Tomes S,Cooney J M,et al.The role of enoylreductase genes in phloridzin biosynthesis in apple.Plant Physiology and Biochemistry,2013,72:54-61
[8]朱珊,王文倩,李赫宇,等.根皮苷标准品的研制.中药饮片质量分析与中药鉴别技术交流研讨会论文集,2009
[9]徐凯,吕海涛.正交实验优选苹果皮中根皮苷提取工艺.中南药学,2009,7(7):497-499
[10]丰金玉,秦昱,段继春,等.超声波辅助提取多穗石柯根皮苷研究.中国农学通报,2015,31(10):251-255
[11]秦昱,丰金玉,段继春,等.大孔吸附树脂分离纯化多穗石柯根皮苷.中国农学通报,2015,31(36):269-275
[12]杨大坚,钟炽昌.甜茶化学成分研究Ⅰ.甜味成分.中草药,1991,22(3):99-101
[13]冯雪娇,曹学丽,李艳,等.根皮苷的应用及分离纯化研究进展.食品科学技术学报,2008,26(4):13-16
[14]李胜华,伍贤进,牛有芽.D-101大孔树脂纯化多穗柯中根皮苷的工艺研究.食品科技,2010,35(7):217-221
[15]Sun L,Liu D,Sun J,et al.Simultaneous separation and purification of chlorogenic acid,epicatechin,hyperoside and phlorizin from thinned young Qinguan,apples by successive use of polyethylene and polyamide resins.Food Chemistry,2017,230:362-371
[16]Sun L,Guo Y,Fu C,et al.Simultaneous separation and purification of total polyphenols,chlorogenic acid and phlorizin from thinned young apples.Food Chemistry,2013,136(2):1022-1029
[17]王慧莹.多穗柯根皮苷的提取纯化研究.长沙:中南大学,2014
[18]李荣涛,焦中高,刘杰超,等.高效离心分配色谱(HPCPC)分离纯化苹果树枝中的根皮苷.果树学报,2010,27(4):645-649
[19]吕朝磊,雷巧灵,张宪宝,等.基于基因调控网络的糖肾方治疗糖尿病肾病作用机理解析.中华中医药杂志,2018,33(4):1320-1324
[20]Mudaliar S,Polidori D,Zambrowicz B,et al.Sodium-glucose cotransporter inhibitors:Effects on renal and intestinal glucose transport:From bench to bedside.Diabetes Care,2015,38(12):2344
[21]Coady M J,Wallendorff B,Lapointe J Y.Characterization of the transport activity of SGLT2/MAP17,the renal low-affinity Na+/glucose cotransporter.Am J Physiol Renal Physiol,2017,313(2):F467-F474
[22]袁璐,李倩,高谷,等.钠葡萄糖协同转运子2抑制剂:糖尿病治疗的新选择.国际内分泌代谢杂志,2010,30(5):321-323
[23]Powell D R,Dacosta C M,Gay J,et al.Improved glycemic control in mice lackingSglt1 and Sglt2.American Journal of Physiology Endoc A rinology&Metabolism,2013,304(2):E117-E130
[24]Yamaguchi K,Kato M,Suzuki M,et al.Pharmacokinetic and pharmacodynamic modeling of the effect of an sodium-glucose cotransporter inhibitor,phlorizin,on renal glucose transport in rats.Drug Metabolism&Disposition the Biological Fate of Chemicals,2011,39(10):1801
[25]Rossetti L,Shulman G I,Zawalich W,et al.Effect of chronic hyperglycemiaon in vivo insulin secretion in partially pancreatectomized rats.J Clin Invest,1987,80(4):1037-1044
[26]RossettiL,SmithD,ShsulmanGI,etal.Correctionof hyperglycemiawith phlorizin normalizes tissue sensitivity toinsulin in diabetic rats.J Clin Invest,1987,79(5):1510-1515
[27]Mei X,Zhang X,Wang Z,et al.Insulin Sensitivity-enhancing activity of phlorizin is associated with lipopolysaccharide decrease and gut microbiota changes in obese and type 2 diabetes(db/db)mice.Journal of Agricultural&Food Chemistry,2016,64(40):7502
[28]申婷婷,花尔并,马娜,等.根皮苷对饲喂高脂高胆固醇饲料仓鼠肝脏中胆固醇代谢调控基因表达的影响.营养学报,2014,36(2):159-163
[29]沈琳.根皮苷对db/db小鼠主动脉的保护作用机制研究.济南:山东大学,2013
[30]蔡茜.根皮苷对db/db小鼠糖尿病心肌病变保护机制的定量蛋白质组学研究.济南:山东大学,2013
[31]郭建茹.根皮苷对肥胖小鼠糖脂代谢的影响及作用机制的初步研究.广州:广州中医药大学,2013
[32]Zhao S,Bomser J,Joseph E L,et al.Intakes of apples or apple polyphenols decease plasma values for oxidized low-density lipoprotein/beta 2-glycoprotein I complex.Journal of Functional Foods,2013,5(1):493-497
[33]伍春,李彦龙,张帆.中医药抗皮肤衰老的研究进展.中华中医药杂志,2014,29(9):2889-2891
[34]Magwere T,West M,Riyahi K,et al.The effects of exogenous antioxidants on lifespan and oxidative stress resistance in Drosophila melanogaster.Mechanisms of Ageing&Development,2006,127(4):356-370
[35]Yu H,Qin C,Zhang P,et al.Antioxidant effect of apple phenolic on lipid peroxidation in Chinese-style sausage.Journal of Food Science&Technology,2015,52(2):1032-1039
[36]Ana Milisavljevi?,Marija Stojanovi?,Milica Carevi?,et al.Lipasecatalyzed esterification of phloridzin:Acyl donor effect on enzymatic affinity and antioxidant properties of esters.Industrial&Engineering Chemistry Research,2014,53(43):16644-16651
[37]王建新,周忠,王建国.根皮素抑酪氨酸酶活性研究.香料香精化妆品,2002(2):4-5
[38]Lin Y P,Hsu F L,Chen C S,et al.Constituents from the Formosan apple reduce tyrosinase activity in human epidermal melanocytes.Phytochemistry,2007,68(8):1189-1199
[39]翟一淼.根皮苷保护表皮细胞抵抗UVB损伤的作用及分子机制研究.上海:华东师范大学,2014
[40]赵江,陈纯,马娜,等.根皮苷对雄性果蝇抗衰老活性的研究.营养学报,2015(4):372-375
[41]贺军花,马利菁,周会玲.根皮苷对苹果采后灰霉病的影响.咸阳:西北农林科技大学,2017
[42]张世阳.根皮苷对db/db小鼠视网膜保护机制的研究.济南:山东大学,2013
[43]Ehrenkranz J R,Lewis N G,Kahn C R,et al.Phlorizin:a review.Diabetes/Metabolism Research&Reviews,2005,21(1):31-38
[44]冯天艳,方荣,邓改改,等.根皮苷对小鼠CCl4急性肝损伤的保护作用.中药药理与临床,2010(5):47-50
[45]张硕,袁希平,王庆林.根皮苷对血吸虫病肝纤维化小鼠肝脏中TGF-β1和PDGF-BB表达的影响.华西药学杂志,2015,30(1):42-46
[46]Khalifa M,Bakr A G,Osman A T.Protective effects of phloridzin against methotrexate-induced liver toxicity in rats.Biomedicine&Pharmacotherapy,2017,95:529-535
[47]Ikumi Y,Kida T,Sakuma S,et al.Polymer-phloridzin conjugates as an anti-diabetic drug that Inhibits glucose absorption through the Na+/glucose cotransporter(SGLT1)in the small intestine.Journal of Controlled Release,2008,125(1):42-49