Liu Chun-Hua, Wang Ming-Jin, Yang Shu-Ting, Li Na, Lu Yuan, Pan Jie, Li Yong-Jun, Wang Yong-Lin, Sun Jia
State Key Laboratory of Functions and Applications of Medicinal Plants, Engineering Research Center for the Development and Application of Ethnic Medicine and Traditional Chinese Medicine (Ministry of Education), Guizhou Medical University Guiyang 550004, China Guizhou Provincial Key Laboratory of Pharmaceutics, Guizhou Medical University Guiyang 550004, China.
Guizhou Provincial Key Laboratory of Pharmaceutics, Guizhou Medical University Guiyang 550004, China School of Pharmacy, Guizhou Medical University Guiyang 550004, China.
Zhongguo Zhong Yao Za Zhi. 2021 Jan;46(1):196-205. doi: 10.19540/j.cnki.cjcmm.20201010.201.
The present study is to investigate the absorption characteristics of the main components in Polygonum orientale extract in normal and isoproterenol-induced myocardial ischemia model rats with everted intestinal sac models. Intestinal sac fluid samples were collected in different part of intestine(duodenum, jejunum, ileum, colon) at different time after administration of different concentration of P. orientale extract(5.0,10.0, 20.0 mg·mL~(-1)). An UPLC-TQD method was employed for the determination of six components including orientin, isoorientin, vitexin, protocatechuic acid, kaempferol-3-O-β-D-glucoside and quercitrin in the intestinal sac samples. The absorption rate and cumulative absorption were calculated to analyze the intestinal absorption characteristics of six components in normal and myocardial ischemia model rats. The P-glycoprotein(P-gp) inhibitor was applied to investigate influence of intestinal absorption of six components in P. orientale extract. The results showed that the main absorption sites were concentrated on the duodenum at low concentration, while they were the colon at the medium concentration and the ileum at high concentration in control groups. In the condition of myocardial ischemia model, the main absorption sites focus on the ileum and jejunum at low concentration; the main absorption sites were in the ileum at the medium concentration and main absorption sites were the duodenum and ileum at high concentration. Compared with the normal group, the absorption rate and cumulative absorption of the six components significantly decreased in the model group. P-gp inhibitor markedly increased the absorption rate and cumulative absorption of six components in the model group, inferring that the 6 components may be the substrates of P-gp, and the mechanism needs further study. In this study, it is revealed that the six components of P. orientale extract can be absorbed into the intestinal sac, and it is an effective method to assess the intestinal absorption characteristics of P. orientale extract through everted intestinal sac model, providing data support for the clinical application and further development of P. orientale.
本研究旨在采用外翻肠囊模型，考察水红花子提取物中主要成分在正常及异丙肾上腺素诱导的心肌缺血模型大鼠中的吸收特性。给予不同浓度（5.0、10.0、20.0 mg·mL⁻¹）的水红花子提取物后，于不同时间在肠道不同部位（十二指肠、空肠、回肠、结肠）采集肠囊液样本。采用超高效液相色谱 - 串联四极杆质谱法（UPLC - TQD）测定肠囊样本中包括荭草苷、异荭草苷、牡荆素、原儿茶酸、山柰酚 - 3 - O - β - D - 葡萄糖苷和槲皮苷在内的6种成分。计算吸收速率和累积吸收量，以分析正常及心肌缺血模型大鼠中6种成分的肠道吸收特性。应用P - 糖蛋白（P - gp）抑制剂考察其对水红花子提取物中6种成分肠道吸收的影响。结果表明，对照组中低浓度时主要吸收部位集中在十二指肠，中浓度时主要吸收部位为结肠，高浓度时主要吸收部位为回肠。在心肌缺血模型条件下，低浓度时主要吸收部位集中在回肠和空肠；中浓度时主要吸收部位在回肠，高浓度时主要吸收部位为十二指肠和回肠。与正常组相比，模型组中6种成分的吸收速率和累积吸收量显著降低。P - gp抑制剂显著提高了模型组中6种成分的吸收速率和累积吸收量，推测这6种成分可能是P - gp的底物，其机制有待进一步研究。本研究表明，水红花子提取物中的6种成分可被吸收进入肠囊，通过外翻肠囊模型评估水红花子提取物的肠道吸收特性是一种有效方法，为水红花子的临床应用和进一步开发提供了数据支持。
