The absorption profiles of Schisandra chinensis were evaluated using the human Caco-2 cell monolayer and rat everted gut sac models,as well as in rat plasma.By analyzing the chromatographic and MSn characteristics of ...The absorption profiles of Schisandra chinensis were evaluated using the human Caco-2 cell monolayer and rat everted gut sac models,as well as in rat plasma.By analyzing the chromatographic and MSn characteristics of individual peak acquired by HPLC-DAD-APCI-MS^(n) determination,thirteen lignans were identified as the major in vitro absorbable components of the Schisandra extract.Most of these compounds were also detected and identified in rat plasma after an oral administration of the Schisandra extract,except for angeloyl(tigloyl)gomisin H and angeloyl(tigloyl)gomisin Q,whose structures possess an ester group at the cyclooctadiene ring.In addition,four metabolites,corresponding to the hydroxylation and demethylation products of schisandrin and the hydrolysis derivative of angeloyl(tigloyl)gomisin Q,were tentatively identified.The results demonstrate that Schisandra lignans are the major absorbable components of this crude drug,and hydroxylation,demethylation and hydrolysis are important metabolic transformations of the absorbable lignans.展开更多
为探讨芍药甘草汤配伍机制与适宜的配伍比例,采用大鼠外翻肠囊模型、在体单向肠灌流模型,从肠吸收角度研究芍药甘草汤SG11(白芍-炙甘草1∶1)、SG31(白芍-炙甘草3∶1)、白芍水煎液S及炙甘草水煎液(G)中主要指标成分在大鼠离体、在体肠吸...为探讨芍药甘草汤配伍机制与适宜的配伍比例,采用大鼠外翻肠囊模型、在体单向肠灌流模型,从肠吸收角度研究芍药甘草汤SG11(白芍-炙甘草1∶1)、SG31(白芍-炙甘草3∶1)、白芍水煎液S及炙甘草水煎液(G)中主要指标成分在大鼠离体、在体肠吸收情况,并进行比较。以HPLC测定上述供试品以及肠囊吸收样品、肠灌流样品中芍药苷(paeoniflorin,PF)、甘草苷(liquiritin,LQ)、甘草酸单铵盐(glycyrrhizin single ammonium salt,GL)的浓度,并计算肠吸收量及吸收参数。发现在外翻肠囊模型中,3种成分在十二指肠、空肠和回肠均有吸收,最佳吸收部位均为空肠,且SG11中相应成分的吸收率均显著高于单煎(P<0.05),与SG31比较无显著性差异。在单向在体肠灌流模型中,SG11中相应成分的吸收速率常数Ka、表观吸收系数Papp和吸收率均显著高于各单煎液,SG11中PF,GL的各参数均显著高于SG31,LQ,各参数无差异。说明白芍炙甘草配伍有助于PF,LQ和GL的肠吸收,SG11较SG31各指标成分的吸收好。展开更多
基金supported by an International Center for Complementary and Alternative Medicine(ICRC)Grant(1-U19-AT003266PI:Brian Berman,University of Maryland)of the National Center for Complementary and Alternative Medicine(NCCAM),USA.
文摘The absorption profiles of Schisandra chinensis were evaluated using the human Caco-2 cell monolayer and rat everted gut sac models,as well as in rat plasma.By analyzing the chromatographic and MSn characteristics of individual peak acquired by HPLC-DAD-APCI-MS^(n) determination,thirteen lignans were identified as the major in vitro absorbable components of the Schisandra extract.Most of these compounds were also detected and identified in rat plasma after an oral administration of the Schisandra extract,except for angeloyl(tigloyl)gomisin H and angeloyl(tigloyl)gomisin Q,whose structures possess an ester group at the cyclooctadiene ring.In addition,four metabolites,corresponding to the hydroxylation and demethylation products of schisandrin and the hydrolysis derivative of angeloyl(tigloyl)gomisin Q,were tentatively identified.The results demonstrate that Schisandra lignans are the major absorbable components of this crude drug,and hydroxylation,demethylation and hydrolysis are important metabolic transformations of the absorbable lignans.
文摘为探讨芍药甘草汤配伍机制与适宜的配伍比例,采用大鼠外翻肠囊模型、在体单向肠灌流模型,从肠吸收角度研究芍药甘草汤SG11(白芍-炙甘草1∶1)、SG31(白芍-炙甘草3∶1)、白芍水煎液S及炙甘草水煎液(G)中主要指标成分在大鼠离体、在体肠吸收情况,并进行比较。以HPLC测定上述供试品以及肠囊吸收样品、肠灌流样品中芍药苷(paeoniflorin,PF)、甘草苷(liquiritin,LQ)、甘草酸单铵盐(glycyrrhizin single ammonium salt,GL)的浓度,并计算肠吸收量及吸收参数。发现在外翻肠囊模型中,3种成分在十二指肠、空肠和回肠均有吸收,最佳吸收部位均为空肠,且SG11中相应成分的吸收率均显著高于单煎(P<0.05),与SG31比较无显著性差异。在单向在体肠灌流模型中,SG11中相应成分的吸收速率常数Ka、表观吸收系数Papp和吸收率均显著高于各单煎液,SG11中PF,GL的各参数均显著高于SG31,LQ,各参数无差异。说明白芍炙甘草配伍有助于PF,LQ和GL的肠吸收,SG11较SG31各指标成分的吸收好。
