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Abstract：
OBJECTIVE: To explore the therapeutic effect of transdermal patches containing Cassia seed extract applied at the navel on slow transit constipation (STC) in rats and explore the spectrum-effect relationship of the patches.
METHODS: In a STC rat model established by gavage of compound diphenoxylate suspension for 14 days, the transdermal patches containing low, medium and high doses of Cassia seed extract (41.75, 125.25, and 375.75 mg/kg, respectively) were applied at the Shenque acupoint on the abdomen for 14 days after modeling, with constipation patches (13.33 mg/kg) as the positive control. After the treatment, fecal water content and intestinal propulsion rate of the rats were calculated, the pathological changes in the colon were observed with HE staining. Serum NO and NOS levels and the total protein content and NO, NOS and AChE expressions in the colon tissue were determined. HPLC fingerprints of the transdermal patches were established, and the spectrum-effect relationship between the common peaks of the patches and its therapeutic effect were analyzed.
RESULTS: Treatment with the transdermal patches containing Cassia seed extract significantly increased fecal water content and intestinal propulsion rate of the rat models, where no pathological changes in the colon tissue were detected. The treatment also suppressed the elevations of serum and colonic NO and NOS levels and reduction of AChE in STC rats. Twenty-eight common peaks were confirmed in the HPLC fingerprints of 6 batches of Cassia seed extract-containing patches. Analysis of the spectrum-effect relationship showed that autrantio-obtusin had the greatest contribution to the therapeutic effect of the patches in STC rats.
CONCLUSIONS: The Cassia seed extract-containing patches alleviates STC in rats via synergistic actions of multiple active ingredients in the extract, where autrantio-obtusin, rhein, chrysoobtusin, obtusin, obtusifolin, emodin, chrysophanol, and physcion are identified as the main active ingredients.
METHODS: In a STC rat model established by gavage of compound diphenoxylate suspension for 14 days, the transdermal patches containing low, medium and high doses of Cassia seed extract (41.75, 125.25, and 375.75 mg/kg, respectively) were applied at the Shenque acupoint on the abdomen for 14 days after modeling, with constipation patches (13.33 mg/kg) as the positive control. After the treatment, fecal water content and intestinal propulsion rate of the rats were calculated, the pathological changes in the colon were observed with HE staining. Serum NO and NOS levels and the total protein content and NO, NOS and AChE expressions in the colon tissue were determined. HPLC fingerprints of the transdermal patches were established, and the spectrum-effect relationship between the common peaks of the patches and its therapeutic effect were analyzed.
RESULTS: Treatment with the transdermal patches containing Cassia seed extract significantly increased fecal water content and intestinal propulsion rate of the rat models, where no pathological changes in the colon tissue were detected. The treatment also suppressed the elevations of serum and colonic NO and NOS levels and reduction of AChE in STC rats. Twenty-eight common peaks were confirmed in the HPLC fingerprints of 6 batches of Cassia seed extract-containing patches. Analysis of the spectrum-effect relationship showed that autrantio-obtusin had the greatest contribution to the therapeutic effect of the patches in STC rats.
CONCLUSIONS: The Cassia seed extract-containing patches alleviates STC in rats via synergistic actions of multiple active ingredients in the extract, where autrantio-obtusin, rhein, chrysoobtusin, obtusin, obtusifolin, emodin, chrysophanol, and physcion are identified as the main active ingredients.
摘要：
目的：探讨肚脐含决明子提取物的透皮贴剂对大鼠慢传输性便秘(STC)的治疗作用及其谱效关系。
方法：用复方苯乙氧基化物混悬液灌胃14天建立STC大鼠模型，透皮贴剂的含量低，中高剂量的决明子提取物（41.75、125.25和375.75mg/kg，分别）在建模后14天，在腹部的神雀穴处涂抹，以便秘贴剂(13.33mg/kg)作为阳性对照。治疗后,计算大鼠的粪便含水量和肠推进率，HE染色观察结肠病理变化。血清NO和NOS含量和总蛋白含量,测定结肠组织中NOS和AChE的表达。建立了透皮贴剂的HPLC指纹图谱,并分析了贴片的公共峰与治疗效果之间的频谱-效应关系。
结果：用含决明子提取物的透皮贴剂治疗可显著提高大鼠模型的粪便含水量和肠推进率，其中未检测到结肠组织的病理变化。该治疗还抑制了STC大鼠血清和结肠NO和NOS水平的升高以及AChE的降低。在6批含有决明子种子提取物的贴剂的HPLC指纹图谱中确认了28个共同峰。对光谱-效应关系的分析表明，自交尿肽对STC大鼠贴片的治疗作用贡献最大。
结论：含决明子提取物的贴剂通过提取物中多种活性成分的协同作用减轻大鼠的STC，在那里，rhein,chrysobtusin,obtusin,obtusifolin,大黄素,大黄酚,和physcion被确定为主要活性成分。
方法：用复方苯乙氧基化物混悬液灌胃14天建立STC大鼠模型，透皮贴剂的含量低，中高剂量的决明子提取物（41.75、125.25和375.75mg/kg，分别）在建模后14天，在腹部的神雀穴处涂抹，以便秘贴剂(13.33mg/kg)作为阳性对照。治疗后,计算大鼠的粪便含水量和肠推进率，HE染色观察结肠病理变化。血清NO和NOS含量和总蛋白含量,测定结肠组织中NOS和AChE的表达。建立了透皮贴剂的HPLC指纹图谱,并分析了贴片的公共峰与治疗效果之间的频谱-效应关系。
结果：用含决明子提取物的透皮贴剂治疗可显著提高大鼠模型的粪便含水量和肠推进率，其中未检测到结肠组织的病理变化。该治疗还抑制了STC大鼠血清和结肠NO和NOS水平的升高以及AChE的降低。在6批含有决明子种子提取物的贴剂的HPLC指纹图谱中确认了28个共同峰。对光谱-效应关系的分析表明，自交尿肽对STC大鼠贴片的治疗作用贡献最大。
结论：含决明子提取物的贴剂通过提取物中多种活性成分的协同作用减轻大鼠的STC，在那里，rhein,chrysobtusin,obtusin,obtusifolin,大黄素,大黄酚,和physcion被确定为主要活性成分。
