Department of Pharmacology, PES College of Pharmacy, Bangalore 560050.
Asian Pac J Trop Med. 2011 Jun;4(6):451-6. doi: 10.1016/S1995-7645(11)60124-7.
To evaluate antidiarrheal activity of the fractions of aqueous extract from stem barks of Thespesia populnea (Malvaceae).
From the aqueous extract three fractions namely ethyl acetate fraction (EAF), methanolic fraction (MF) and residue fraction (RF) were made and studied for antidiarrheal activity. Antidiarrheal activity of the fractions were evaluated in castor oil induced diarrhea, prostaglandin E(2) (PG-E(2)) induced diarrhea and charcoal meal test as in vivo models and the most potent fraction was further evaluated with in vitro models to determine the possible antimotility effect.
In castor oil induced diarrhea model, the RF (10, 25, 50 and 100 mg/kg, po.) and MF (100 mg/kg, po.) has significantly reduced the cumulative wet faecal mass, where as the EAF have not shown any significant antidiarrheal activity, RF was found to be more potent than MF. Based on these results and percentage yield, only RF was evaluated in PG-E(2) induced enteropooling and charcoal meal test. RF (10, 25 and 50 mg/kg) had shown significant inhibition of PG-E(2) induced secretions (antisecretory) and decreased the movement of charcoal in charcoal meal test indicating its antimotility activity. Furthermore, RF has showed significant inhibition of acetylcholine, histamine and BaCl(2) induced contractions on rat colon, guinea pig ileum and rabbit jejunum with EC(50) values of 241.7, 303.1 and 286.1 μg/mL, respectively indicating the antimotility effect of RF. The phytochemical analysis of RF showed presence of gums and mucilages and the possible mechanism may be the combination inhibition of elevated prostaglandin biosynthesis and reduced propulsive movement of the intestine.
RF possesses good antidiarrheal activity comparing with other two fractions and the possible mechanism thought to be associated with combination of antisecretory and antimolity.
评价朱槿（锦葵科）茎皮水提物的各馏分的止泻活性。
从水提物中得到三种馏分，即乙酸乙酯馏分（EAF）、甲醇馏分（MF）和残渣馏分（RF），并对其进行了研究。采用蓖麻油诱导腹泻、前列腺素 E（2）（PG-E（2））诱导腹泻和炭末试验作为体内模型评价馏分的止泻活性，选择最有效的馏分进一步用体外模型评价其可能的抗蠕动作用。
在蓖麻油诱导腹泻模型中，RF（10、25、50 和 100 mg/kg，po.）和 MF（100 mg/kg，po.）显著减少了累积湿粪便质量，而 EAF 没有显示出任何显著的止泻活性，RF 比 MF 更有效。基于这些结果和产率，仅对 RF 进行了 PG-E（2）诱导肠液积聚和炭末试验的评估。RF（10、25 和 50 mg/kg）显示出对 PG-E（2）诱导分泌（抗分泌）的显著抑制作用，并减少了炭末试验中炭的运动，表明其具有抗蠕动活性。此外，RF 对大鼠结肠、豚鼠回肠和兔空肠的乙酰胆碱、组胺和 BaCl（2）诱导的收缩具有显著抑制作用，其 EC（50）值分别为 241.7、303.1 和 286.1 μg/mL，表明 RF 具有抗蠕动作用。RF 的植物化学分析表明存在胶和黏液，可能的机制可能是结合抑制升高的前列腺素生物合成和减少肠的推进运动。
RF 与其他两种馏分相比具有良好的止泻活性，其可能的机制与抗分泌和抗蠕动的结合有关。
