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20.0 mg/mL),different intestinal segments(duodenum,jejunum,ileum,colon),P-glycoprotein(P-gp)inhibitors(verapamil)
and bile on the intestinal absorption of each constituent were explored. RESULTS:The linear ranges of concentrations of
kaempferol, isokaempferol, vitexin, protocatechuic acid, kaempferol-3-O-β-D-glucoside and quercetin were 3.15-50.40,
3.21-51.31,1.63-52.43,1.60-50.94,1.31-20.97,8.07-129.25 µg/mL(r>0.999). The lower limits of quantification were 7.86,
8.45,6.52,4.00,3.28,16.14 ng/mL,respectively. RSDs of precision,matrix effect and stability tests were all lower than 11%;
the accuracy were 85.64%-107.65%,which were in line with the requirements of biological sample quantification analysis. Except
for there was no statistical significance in the absorption of kaempferol absorption in duodenum of model group at different
concentrations,absorption of other five constituents in duodenum of normal and model rats increased with the increase of the
concentration of active constituents,and absorption of medium- and/or high- concentration active constituents(except quercetin)in
model group was significantly lower than normal group(P<0.05). In normal group,the absorption of kaempferol was more in
jejunum,ileum and colon,isokaempferol was more in ileum,vitexin and protocatechuic acid were more in jejunum and ileum,
kaempferin-3-O- β-D-glucoside was more in duodenum,jejunum and colon,quercetin was more in colon;in the model group,the
absorption of Polygonum orientale in jejunum and colon was more,the absorption of isokaempferol in 4 intestinal segments was
little different,vitexin was mainly absorbed in ileum,protocatechuic acid and kaempferol-3-O-β-D-glucoside was mainly absorbed
in jejunum,quercetin was mainly absorbed in duodenum and ileum;in the same intestine,the absorption of constituents in the
model group was less than normal group. After adding verapamil,absorption of all constituents in the normal group increased,but
the difference was not statistically significant(P>0.05);absorption of kaempferol,isokaempferol,vitexin,protocatechuic acid
and kaempferol-3-O-β-D-glucoside were all increased significantly in model group (P<0.05),while there was no statistical
significance in the increase of quercetin(P>0.05). After the bile flowed into the duodenum,absorption of protocatechuic acid was
increased significantly in normal group(P<0.05);absorption of other active constituents were increased significantly in model
group,except for isokaempferol and quercetin(P<0.05). CONCLUSIONS:Six active constituents of P. orientale were absorbed
in the whole intestine of normal and MI model rats,and the absorption of above constituents may be enhanced more significantly
by P-gp inhibitor and bile under pathological condition.
KEYWORDS Myocardial ischemia;Polygonum orientale;Active constituent;Intestinal absorption;Intestinal perfusion;Rat
荭草为蓼科植物荭草(Polygonum orientale L.)的干 内的肠吸收特征差异,从而为荭草体内过程的深入研究
燥果穗及带叶茎枝,具有祛风除湿、活血消肿的功效,用 提供实验依据。
[1]
于治疗风湿性关节炎、冠心病等 。相关研究表明,荭草 1 材料
具有抗急性心肌缺血、增加心肌血流量、抗菌、抗血栓等 1.1 仪器
[2]
药理活性 。本课题组前期通过对荭草药用部位、化学 Acquity UPLC-TQD 型超高效液相色谱-三重四极
成分、药理活性及血清谱效关系等方面的研究发现,荭 杆质谱联用仪(美国Waters公司);Allegra 64R型低温高
草水溶性部位有较好的抗心肌缺血和抗缺氧作用,其含 速离心机(美国Beckman公司);BT100-2J型恒流泵(保
量较高的活性成分主要为原儿茶酸、异荭草素、荭草素、 定兰格恒流泵有限公司);DK-98-Ⅱ型恒温水浴锅(天津
牡荆素、山柰素-3-O-β-D-葡萄糖苷、槲皮苷等酚酸类和 泰斯特有限公司);SHB-Ⅲ型循环水式多用真空泵(郑州
黄酮类化合物 。 长城科工贸有限公司);WP-UP-Ⅱ-20型超纯水机(四川
[3]
口服给药是中药常用的临床给药方式,中药经口服 沃特尔科技发展有限公司);ZH-2型涡旋混合器(天津药
后主要在胃肠道被吸收,各活性成分进入血液后随体循 典标准仪器厂);MTN-2800D 型氮吹浓缩装置(天津奥
环分布到各个组织器官并发挥疗效。据研究报道,机体 特塞恩斯仪器有限公司);CQ 250A-TS型超声波清洗机
在病理状态下,其体内药物代谢酶、转运蛋白、肠道菌 (上海跃进医用光学器械厂)。
群、细胞膜通透性等较在正常生理状态时有所改变,进 1.2 药品与试剂
而影响中药在机体内的吸收过程 [4-5] ,故研究中药在病理 荭草药材购自贵州省盘州市丹霞镇,由贵州医科
状态下的吸收特征对于阐明其药效物质基础具有重要 大学刘春花副教授鉴定为荭草的带叶茎枝。荭草素、
意义。 异荭草素、牡荆素、原儿茶酸、山柰素-3-O-β-D-葡萄糖
本研究通过皮下注射大剂量盐酸异丙肾上腺素制 苷、槲皮苷对照品(四川省维克奇生物科技有限公司,
备心肌缺血模型大鼠 [6-8] ,采用在体肠循环灌流法研究荭 批号分别为:wkq16041301、wkq16080404、wkq16031003、
草提取物中6个活性成分(荭草素、异荭草素、牡荆素、原 wkq16012105、wkq16022301、wkq16080402,纯度:均不
儿茶酸、山柰素-3-O-β-D-葡萄糖苷、槲皮苷)在不同条件 低于 98%);葛根素对照品(内标,批号:S02M9B54875,
下[不同药物质量浓度、不同肠段、P-糖蛋白(P-gp)抑制 纯度:≥98%)、盐酸维拉帕米原料药(批号:Y05J6C2,纯
剂作用下、胆汁作用下]在正常和心肌缺血模型大鼠体 度:≥98%)均购自上海源叶生物科技有限公司;盐酸异
中国药房 2020年第31卷第13期 China Pharmacy 2020 Vol. 31 No. 13 ·1563 ·