两色金鸡菊提取物中3种黄酮苷在大鼠胃肠道的水解代谢研究
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摘要
目的研究两色金鸡菊(CCT)中马里苷(CCT-1)、异奥卡宁-7-O-β-D-吡喃葡萄糖苷(CCT-2)和花旗松素-7-O-β-D-吡喃葡萄糖苷(CCT-3)在大鼠胃肠道内是否发生水解代谢。方法采用体外孵育法,筛选底物质量浓度、酶质量浓度及孵育时间,再通过测定的苷元质量浓度分析3种黄酮苷在大鼠胃肠道的水解代谢程度。结果孵育体系中,质量浓度为36μg·mL-1的黄酮苷与蛋白质量浓度为1.5mg·mL-1的组织提取物孵育45min,发现CCT-1、CCT-2和CCT-3的水解代谢率在大鼠十二指肠中依次为4.8%,7.1%和0%;在空肠中依次为61.8%,35.3%和13.7%;在回肠中依次为64.8%,29.7%和20.5%;在胃、结肠和盲肠组织提取物中无水解。结论 CCT-1、CCT-2和CCT-3在大鼠小肠中均发生去糖基水解代谢,生成苷元,三者水解程度依次为:CCT-1>CCT-2>CCT-3。此3种黄酮苷及其苷元可能是两色金鸡菊潜在的药效物质基础。
Objective To study the hydrolysis of marein(CCT-1),flavanomarein(CCT-2)and taxifolin-7-O-β-D-glucopyranoside(CCT-3)from capitula of Coreopsis tinctoria(CCT)in rat gastrointestinal tracts(GIT).Methods Substrate concentration,enzyme concentration and incubating time were optimized by incubation in vitro,and the hydrolyzation ratio was determined for evaluating whether CCT-1,CCT-2 and CCT-3 were hydrolyzed in GIT.Results After 36μg·mL-1 of flavonoid glycosides being added to cell-free extract(1.5 mg·mL-1 of protein)and incubated for 45 min,the hydrolyzation ratio of CCT-1,CCT-2 and CCT-3 were4.8%,7.1% and 0% in duodenum,61.8%,35.3% and 13.7% in jejunum,64.8%,29.7% and 20.5% in ileum,respectively,while there was no hydrolyzation happened in stomach,colon and cecum.Conclusion CCT-1,CCT-2 and CCT-3 could be hydrolyzed only in rat small intestine(duodenum,jejunum and ileum)cell-free extract,the hydrolyzation extent order was:CCT-1>CCT-2>CCT-3.The results will help us to clarify the real functional components of CCTin vivo.
Objective To study the hydrolysis of marein(CCT-1),flavanomarein(CCT-2)and taxifolin-7-O-β-D-glucopyranoside(CCT-3)from capitula of Coreopsis tinctoria(CCT)in rat gastrointestinal tracts(GIT).Methods Substrate concentration,enzyme concentration and incubating time were optimized by incubation in vitro,and the hydrolyzation ratio was determined for evaluating whether CCT-1,CCT-2 and CCT-3 were hydrolyzed in GIT.Results After 36μg·mL-1 of flavonoid glycosides being added to cell-free extract(1.5 mg·mL-1 of protein)and incubated for 45 min,the hydrolyzation ratio of CCT-1,CCT-2 and CCT-3 were4.8%,7.1% and 0% in duodenum,61.8%,35.3% and 13.7% in jejunum,64.8%,29.7% and 20.5% in ileum,respectively,while there was no hydrolyzation happened in stomach,colon and cecum.Conclusion CCT-1,CCT-2 and CCT-3 could be hydrolyzed only in rat small intestine(duodenum,jejunum and ileum)cell-free extract,the hydrolyzation extent order was:CCT-1>CCT-2>CCT-3.The results will help us to clarify the real functional components of CCTin vivo.
引文
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[10]Haixia Han,Zhiyuan Ma,Wei Wang,et al.Deglycosylation and absorption of marein,flavanomarein and taxifolin-7-O-β-D-glucopyranoside from capitula of Coreopsis tinctoriain rats and humans[J].J Funct Foods,2016,27(12):178-188.
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[12]Kim H,Kong H S,Choi B,et al.Metabolic and pharmacological properties of rutin,a dietary quercetin glycoside,for treatment of inflammatory bowel disease[J].Pharm Res-dordr,2005,22(9):1499-1509.
[13]Li Z,Jiang H,Xu C,et al.A review:Using nanoparticles to enhance absorption and bioavailability of phenolic phytochemicals[J].Food Hydrocolloid,2015,43:153-164.
[14]Tribolo S,Berrin J G,Kroon P A,et al.The crystal structure of human cytosolic beta-glucosidase unravels the substrate aglycone specificity of a family 1glycoside hydrolase[J].J Mol Biol,2007,370(5):964-975.
[15]Chang Q,Zuo Z,Chow M,et al.Difference in absorption of the two structurally similar flavonoid glycosides,hyperoside and isoquercitrin,in rats[J].Eur J Pharm Biopharm,2005,59(3):549-555.
[16]Ma Z,Zheng S,Han H,et al.The bioactive components of Coreopsis tinctoria(Asteraceae)capitula:antioxidant activity in vitro and profile in rat plasma[J].J Funct Food,2016,20:575-586.
[17]Dias T,Liu B,Jones P,et al.Cytoprotective effect of Coreopsis tinctoria extracts and flavonoids on tBHP and cytokine-induced cell injury in pancreatic MIN6cells[J].J Ethnopharmacol,2012,139(2):485-492.
[18]Dias T,Bronze M R,Houghton P J,et al.The flavonoidrich fraction of Coreopsis tinctoria promotes glucose tolerance regain through pancreatic function recovery in streptozotocin-induced glucose-intolerant rats[J].J Ethnopharmacol,2010,132(2):483-490.
[19]Shen S,Tang H,Zhang X,et al.Targeting mesoporous silica-encapsulated gold nanorods for chemo-photothermal therapy with near-infrared radiation[J].Biomaterials,2013,34(12):3150-3158.
[20]Guo J,Qian F,Li J,et al.Identification of a new metabolite of astilbin,3′-O-methylastilbin,and its immuncisuppressive activity against contact dermatitis[J].Clin Chem,2007,53(5):997.
[2]姚新成,田丽萍,秦冬梅,等.两色金鸡菊化学成分及生物活性研究进展[J].西北药学杂志,2014,29(6):655-658.
[3]Wang T,Xi M,Guo Q,et al.Chemical components and antioxidant activity of volatile oil of a Compositae tea(Coreopsis tinctoria Nutt.)from Mt.Kunlun[J].Ind Crop Prod,2015,67:318-323.
[4]兰怡,卢伟,李琳琳,等.两色金鸡菊醇提物对实验性糖尿病大鼠血糖血脂的影响[J].中国药物应用与监测,2014,(5):272-275.
[5]Zhang Y,Shi S,Zhao M,et al.Coreosides A-D,C-14-polyacetylene glycosides from the capitula of Coreopsis tinctoria and its anti-inflammatory activity against COX-2[J].Fitoterapia,2013,87:93-97.
[6]姜保平.两色金鸡菊茶饮对2型糖尿病胰岛素抵抗的预防作用及机制研究[D].北京:北京协和医学院,2015:162.
[7]张雅,方贺,李佳,等.两色金鸡菊总黄酮对大鼠心肌缺血再灌注损伤保护作用的研究[J].石河子大学学报:自然科学版,2016,(1):1-5.
[8]Li Y,Chen X,Xue J,et al.Flavonoids from Coreopsis tinctoria adjust lipid metabolism in hyperlipidemia animals by down-regulating adipose differentiation-related protein[J].Lipids Health Dis,2014,13:193.
[9]邓凯,李新霞,李琳琳,等.两色金鸡菊醇提物的质量标准研究[J].西北药学杂志,2016,31(6):554-560.
[10]Haixia Han,Zhiyuan Ma,Wei Wang,et al.Deglycosylation and absorption of marein,flavanomarein and taxifolin-7-O-β-D-glucopyranoside from capitula of Coreopsis tinctoriain rats and humans[J].J Funct Foods,2016,27(12):178-188.
[11]Kim D H,Jung E A,Sohng I S,et al.Intestinal bacterial metabolism of flavonoids and its relation to some biological activities[J].Arch Pharm Res,1998,21(1):17-23.
[12]Kim H,Kong H S,Choi B,et al.Metabolic and pharmacological properties of rutin,a dietary quercetin glycoside,for treatment of inflammatory bowel disease[J].Pharm Res-dordr,2005,22(9):1499-1509.
[13]Li Z,Jiang H,Xu C,et al.A review:Using nanoparticles to enhance absorption and bioavailability of phenolic phytochemicals[J].Food Hydrocolloid,2015,43:153-164.
[14]Tribolo S,Berrin J G,Kroon P A,et al.The crystal structure of human cytosolic beta-glucosidase unravels the substrate aglycone specificity of a family 1glycoside hydrolase[J].J Mol Biol,2007,370(5):964-975.
[15]Chang Q,Zuo Z,Chow M,et al.Difference in absorption of the two structurally similar flavonoid glycosides,hyperoside and isoquercitrin,in rats[J].Eur J Pharm Biopharm,2005,59(3):549-555.
[16]Ma Z,Zheng S,Han H,et al.The bioactive components of Coreopsis tinctoria(Asteraceae)capitula:antioxidant activity in vitro and profile in rat plasma[J].J Funct Food,2016,20:575-586.
[17]Dias T,Liu B,Jones P,et al.Cytoprotective effect of Coreopsis tinctoria extracts and flavonoids on tBHP and cytokine-induced cell injury in pancreatic MIN6cells[J].J Ethnopharmacol,2012,139(2):485-492.
[18]Dias T,Bronze M R,Houghton P J,et al.The flavonoidrich fraction of Coreopsis tinctoria promotes glucose tolerance regain through pancreatic function recovery in streptozotocin-induced glucose-intolerant rats[J].J Ethnopharmacol,2010,132(2):483-490.
[19]Shen S,Tang H,Zhang X,et al.Targeting mesoporous silica-encapsulated gold nanorods for chemo-photothermal therapy with near-infrared radiation[J].Biomaterials,2013,34(12):3150-3158.
[20]Guo J,Qian F,Li J,et al.Identification of a new metabolite of astilbin,3′-O-methylastilbin,and its immuncisuppressive activity against contact dermatitis[J].Clin Chem,2007,53(5):997.