Huang L, Cheng S, Liu Z, Zou C, Yan H
School of Pharmacy, Wannan Medical College, Wuhu 241002, China.
Nan Fang Yi Ke Da Xue Xue Bao. 2024 Apr 20;44(4):720-726. doi: 10.12122/j.issn.1673-4254.2024.04.14.
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.
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.
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.
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.
探讨脐部贴敷含决明子提取物的透皮贴剂对大鼠慢传输型便秘(STC)的治疗作用,并探索该贴剂的谱效关系。
通过灌胃复方地芬诺酯混悬液14天建立STC大鼠模型,造模后在腹部神阙穴贴敷低、中、高剂量决明子提取物(分别为41.75、125.25和375.75 mg/kg)的透皮贴剂14天,以便秘贴剂(13.33 mg/kg)作为阳性对照。治疗后,计算大鼠粪便含水量和肠推进率,采用HE染色观察结肠的病理变化。测定血清一氧化氮(NO)和一氧化氮合酶(NOS)水平以及结肠组织中的总蛋白含量、NO、NOS和乙酰胆碱酯酶(AChE)表达。建立透皮贴剂的高效液相色谱(HPLC)指纹图谱,并分析贴剂共有峰与其治疗效果之间的谱效关系。
含决明子提取物的透皮贴剂治疗显著提高了大鼠模型的粪便含水量和肠推进率,且未检测到结肠组织的病理变化。该治疗还抑制了STC大鼠血清和结肠中NO和NOS水平的升高以及AChE的降低。在6批含决明子提取物贴剂的HPLC指纹图谱中确认了28个共有峰。谱效关系分析表明,橙黄决明素对该贴剂治疗STC大鼠的效果贡献最大。
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缓解大鼠STC,其中橙黄决明素、大黄酸、金黄决明素、决明素、钝叶决明素、大黄素、 Chrysophanol和大黄酚被确定为主要活性成分。