UPLC—ESI—Q—TOF—MS/MS分析槲皮苷在大鼠(1)
[摘要]该试验主要研究槲皮苷在大鼠肠道菌群中的代谢情况及其可能的生物转化途径，为中药糖苷类成分的代谢机制奠定基础。建立超高效液相色谱串联电喷雾飞行时间质谱测定槲皮苷及其代谢产物的分析方法，流动相为01%甲酸水01%甲酸乙腈，梯度洗脱，流速为03 mL·min-1，扫描方式为电喷雾负离子模式，将大鼠肠道菌群在体外与槲皮苷共同孵育使其发生代谢，采用此方法对其代谢产物进行检测分析，结合Metabolite ToolsTM，质量亏损过滤(MDF)等技术，对代谢产物进行筛查分析以及推测代谢产物化学式。结果显示，槲皮苷发生脱糖、脱氧、乙酰化等反应，脱糖生成的苷元槲皮素进一步发生羟基化、脱氧、还原、开环等反应，得到槲皮素脱氧代谢产物山柰酚、槲皮素C2C3双键加氢还原产物花旗松素、槲皮苷脱糖基产物槲皮素等。研究结果表明槲皮苷能够在大鼠肠道菌群中发生代谢，增加了化合物的疏水性和化学多样性。
[关键词]槲皮苷； 肠道菌群； UPLCQTOFMS/MS； 代谢
Analysis of metabolites of quercitrin in rat intestinal flora by using
, 百拇医药
UPLCESIQTOFMS/MS
QIN Xiaoli1，2，4， SUN Huiyuan1，2 ， YANG Wu1，2 ， LI Yongjun3， ZHENG Lin1 ， LIU Ting1， HUANG Yong1*
(1 Guizhou Provincial Key Laboratory of Pharmaceutics， Guiyang 550004， China；
2 School of Pharmacy， Guizhou Medical University， Guiyang 550004， China，3 Engineering Research Center for the Development and Application of Ethnic Medicine and Traditional Chinese Medicine，Ministry of Education， Guiyang 550004， China，4 National Engineering Research Center of Miao′s Medicines， Guiyang 550004， China)
, 百拇医药
[Abstract]To investigate the metabolism of quercitrin in rat intestinal flora and possible biological pathways， laying the foundation for the metabolic mechanism of traditional Chinese medicine glycosides ingredients UPLCQTOFMS/MS method was established to detect the quercitrin and its metabolites with 01% formic acid solution(A)01% formic acid acetonitrile(B) as the mobile phase for gradient elution at a flow rate of 03 mL·min-1 Electrospray negative ion mode was applied to analyze the metabolites of quercitrin in rat intestinal flora Metabolite ToolsTM， mass defect filter(MDF) and other technologies were used to screen， analyze the metabolites and infer the chemical formula of the metabolites The results showed that quercitrin would have degalactoside， deoxygenation and acetylation reactions， and the aglycone quercetin resulted from degalactoside would have further reactions such as hydroxylation， deoxygenation， reduction， and ring opening to achieve deoxygenation metabolite kaempferol， C2C3 double bonds hydrogenation and reduction product taxifolin， and degalactoside product quercetin The research results showed that quercitrin can be metabolized by rat intestinal flora， which could increase their hydrophobicity and chemical diversity
, 百拇医药
[Key words]quercitrin； intestinal flora； UPLCQTOFMS/MS； metabolism
中药糖苷类成分是中药中一类重要的活性成分，其突出的药效活性受到广泛关注，相关研究表明，糖苷类成分在肠道较难吸收，生物利用度低，在体内难直接发挥作用[1]，然而却能发挥药效，这可能是肠道中存在大量的细菌[2]，使糖苷代谢成各种代谢产物，其代谢产物可能才是真正起药理活性的成分，因此口服中药糖苷类成分的活性与肠道菌群密不可分。而槲皮苷是由槲皮素和鼠李糖基组成的糖苷，具有中枢抑制、抗动脉粥样硬化、抗肿瘤、抗炎镇痛等作用[3]，在三七、银杏叶、荭草花、头花蓼等药材中均含有此成分。目前国内研究槲皮苷的藥理药效[3]、吸收[46]等较多，但是关于槲皮苷在大鼠肠道菌群中的代谢情况尚不明确，因此本文采用UPLCQTOFMS/MS联用技术，并在厌氧环境下研究槲皮苷在大鼠肠道菌群中的代谢规律，对槲皮苷及其类型的糖苷代谢机制具有十分重要的意义。, 百拇医药(覃小丽 孙慧园 杨武 李勇军 郑林 刘亭 黄勇)
[关键词]槲皮苷； 肠道菌群； UPLCQTOFMS/MS； 代谢
Analysis of metabolites of quercitrin in rat intestinal flora by using
, 百拇医药
UPLCESIQTOFMS/MS
QIN Xiaoli1，2，4， SUN Huiyuan1，2 ， YANG Wu1，2 ， LI Yongjun3， ZHENG Lin1 ， LIU Ting1， HUANG Yong1*
(1 Guizhou Provincial Key Laboratory of Pharmaceutics， Guiyang 550004， China；
2 School of Pharmacy， Guizhou Medical University， Guiyang 550004， China，3 Engineering Research Center for the Development and Application of Ethnic Medicine and Traditional Chinese Medicine，Ministry of Education， Guiyang 550004， China，4 National Engineering Research Center of Miao′s Medicines， Guiyang 550004， China)
, 百拇医药
[Abstract]To investigate the metabolism of quercitrin in rat intestinal flora and possible biological pathways， laying the foundation for the metabolic mechanism of traditional Chinese medicine glycosides ingredients UPLCQTOFMS/MS method was established to detect the quercitrin and its metabolites with 01% formic acid solution(A)01% formic acid acetonitrile(B) as the mobile phase for gradient elution at a flow rate of 03 mL·min-1 Electrospray negative ion mode was applied to analyze the metabolites of quercitrin in rat intestinal flora Metabolite ToolsTM， mass defect filter(MDF) and other technologies were used to screen， analyze the metabolites and infer the chemical formula of the metabolites The results showed that quercitrin would have degalactoside， deoxygenation and acetylation reactions， and the aglycone quercetin resulted from degalactoside would have further reactions such as hydroxylation， deoxygenation， reduction， and ring opening to achieve deoxygenation metabolite kaempferol， C2C3 double bonds hydrogenation and reduction product taxifolin， and degalactoside product quercetin The research results showed that quercitrin can be metabolized by rat intestinal flora， which could increase their hydrophobicity and chemical diversity
, 百拇医药
[Key words]quercitrin； intestinal flora； UPLCQTOFMS/MS； metabolism
中药糖苷类成分是中药中一类重要的活性成分，其突出的药效活性受到广泛关注，相关研究表明，糖苷类成分在肠道较难吸收，生物利用度低，在体内难直接发挥作用[1]，然而却能发挥药效，这可能是肠道中存在大量的细菌[2]，使糖苷代谢成各种代谢产物，其代谢产物可能才是真正起药理活性的成分，因此口服中药糖苷类成分的活性与肠道菌群密不可分。而槲皮苷是由槲皮素和鼠李糖基组成的糖苷，具有中枢抑制、抗动脉粥样硬化、抗肿瘤、抗炎镇痛等作用[3]，在三七、银杏叶、荭草花、头花蓼等药材中均含有此成分。目前国内研究槲皮苷的藥理药效[3]、吸收[46]等较多，但是关于槲皮苷在大鼠肠道菌群中的代谢情况尚不明确，因此本文采用UPLCQTOFMS/MS联用技术，并在厌氧环境下研究槲皮苷在大鼠肠道菌群中的代谢规律，对槲皮苷及其类型的糖苷代谢机制具有十分重要的意义。, 百拇医药(覃小丽 孙慧园 杨武 李勇军 郑林 刘亭 黄勇)