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Colitis is an inflammatory disease of the intestine with unknown etiology involving multiple immune, genetic, and environmental factors. We were interested to examine the effect of total extract from Dracocephalum kotschyi (D. kotschyi) Boiss. on the experimental colitis. D. kotschyi hydroalcoholic extract (10, 20, and 40 mg/kg) or apigenin (5, 10, and 20 mg/kg) were administered orally 2 h prior to induction of colitis which was induced by intrarectal administration of acetic acid (4%) in rats. Prednisolone (4 m/kg) was used as the standard drug for comparison. Biochemical evaluation of inflamed colon was performed by measuring myeloperoxidase (MPO) activity. After 5 days treatment, mucosal ulceration was evaluated. Intrarectal instillation of acetic acid caused significant inflammatory reactions as indicated by macroscopic and microscopic changes. The activity of MPO increased in vehicle treated groups while recovered to normal level by pretreatment of animals with D. kotschyi extract, apigenin, or prednisolone. D. kotschyi and apigenin-treated groups showed significantly lower score values of macroscopic and microscopic characters when compared with the vehicle-treated negative control group. The beneficial effect of apigenin was comparable with that of prednisolone. This research has shown the anti-inflammatory potential of D. kotschyi extract and apigenin in experimentally induced colitis.

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1 The ability of several potassium (K+) channel openers to inhibit spasm of the uterus of the nonpregnant rat and their susceptibility to antagonism by glibenclamide was assessed in vitro and in vivo. 2 In the isolated uterus exposed to oxytocin (0.2 nM), cromakalim, RP 49356 and pinacidil were of similar potency (mean pD2 = 6.4, 6.0 and 6.2 respectively) while minoxidil sulphate was of lower potency (pD2 = 4.7). Glibenclamide antagonized cromakalim and RP 49356 with the interactions consistent with competitive antagonism (mean pA2 of 6.57 and 7.00 respectively). Glibenclamide also antagonized pinacidil (pA2 = 6.22) but the slope of the Schild plot was significantly greater than -1. Neither salbutamol nor minoxidil sulphate was antagonized by glibenclamide (10p1M). (0.01-1lpM) inhibited spasm evoked by all concentrations of KCl (10-80mM). Suppression of spasm evoked by KCI (10-80mM) by cromakalim (100pM) and pinacidil (100pMm) was insensitive to glibenclamide (10pM).4 Cromakalim (0.1mgkg-1) and RP 49356 (0.1mgkg-1), given by i.v. bolus injection, inhibited uterine contractions, produced a fall in blood pressure and a slight tachycardia in the conscious ovariectomized rat. Glibenclamide (20mgkg-'), given by i.v. infusion, antagonized the vascular and uterine smooth muscle relaxant properties of cromakalim and RP 49356. 5 Several K+ channel openers are uterine relaxants. The antagonism of cromakalim, RP 49356 and pinacidil, at low concentrations, by glibenclamide suggests their actions may involve an ATP-sensitive K+ channel. High concentrations of pinacidil (10 and 100puM) and cromakalim (100pM) may exert an additional action in the uterus. The low potency of minoxidil sulphate and its insensitivity to glibenclamide in the isolated uterus suggests that its mechanism of action may differ from that of the other K+ channel openers.

Dracocephalum kotschyi Boiss. is a traditional medicine with antispasmodic activities. The objective of this research was to study antispasmodic activities of hydroalcoholic extract of D. kotschyi on rat isolated uterus contractions for comparison with isolated ileum. Hydroalcoholic extract was obtained from aerial part of D. kotschyi using percolation method. A portion of rat ileum or uterus was suspended in Tyrode's solution at 37°C and gassed with O2. Effect of D. kotschyi extract was assessed on ileum or uterus contractions induced by KCl (80 mM), acetylcholine (ACh, 500 nM), electrical field stimulation (EFS) or oxytocin (0.0005 IU/mL). The extract of D. kotschyi concentration-dependently inhibited ileum responses to KCl (IC50 = 65 ± 18 μg/mL), ACh (IC50 = 102 ± 18 μg/mL) and EFS (IC50 = 117 ± 29 μg/mL). The extract of D. kotschyi also concentration-dependently inhibited uterus responses to KCl (IC50 = 453 ± 64μg/mL), ACh (IC50 = 58 ± 9 μg/mL), EFS (IC50 = 22 ± 3 μg/mL) as well as oxytocin (IC50 = 70 ± 11 μg/mL). From this experiment it was concluded that D. kotschyi extract possesses antispasmodic activities on both smooth muscle of ileum and uterus. In comparison, the extract was more effective inhibitor of ACh and EFS responses in rat uterus than on the ileum. On the other hand, the extract was a more potent inhibitor of KCl response on rat ileum. However, the extract was found to be a potent inhibitor of oxytocin-induced contraction of rat uterus. These results indicate that D. kotschyi extract may contain components that might be useful lead compounds for prevention of uterus spasm.

Implication for health policy/practice/research/medical education:This paper provides pharmacological evidence for antimotility of apigenin and luteolin two component of Dracocephalum kotschyi in vivo. In addition it was revealed that inactive apigenin-4'-galactoside in the gastrointestinal tract is converted to active apigenin.Please cite this paper as: Sadraei H, Ghanadian SM, Moazeni S. Inhibitory effect of hydroalcoholic and flavonoids extracts of Dracocephalum kotschyi, and its components luteolin, apigenin and apigenin-4'-galactoside on intestinal transit in mice. J Introduction: Dracocephalum kotschyi is an Iranian indigenous herbal plant which has been reported to have antispasmodic activity in vitro. The antispasmodic activity of hydroalcoholic extract of D. kotschyi is reported to be due to its flavonoids constituents including apigenin and luteolin. The objective of this research was to compare antispasmodic activities of hydroalcoholic and flavonoids extracts of D. kotschyi on ileum contractions in vivo. In addition, spasmolytic activity of apigenin, luteolin and apigenin-4'-galactoside were compared. Methods: The hydroalcoholic extract was prepared by percolation method. Flavonoids extract was obtained by solvent-solvent extraction. Antispasmodic effect of the test compounds was assessed by measurement of percent small intestine transit following oral administration of a charcoal meal and compared with control group and standard drug loperamide. Results: Biochemical assessment of flavonoids content of the extracts showed that ethyl-acetate fraction contained higher quantity of flavonoids. Loperamide (2.5 mg/kg) reduced charcoal meal movement by 58% in comparison to control group. Hydroalcoholic extract of D. kotschyi (20 mg/kg) and its ethyl-acetate fraction (20 mg/kg) reduced the intestinal charcoal meal transit by 32% and 90%, respectively. Apigenin, luteolin and apigenen-4'-galactoside with oral dose of 20 mg/kg inhibited intestinal movement of the charcoal meal 93%, 89% and 45%, respectively in comparison with the vehicle treated control groups. Conclusion: This study confirms that both the hydroalcoholic and flavonoids extracts of D. kotschyi have antispasmodic properties in vivo. Antimotility of apigenen-4'-galactoside in mice is probably due to release of apigenin in the gastrointestinal tract.

Apigenin and luteolin, two active ingredients of Dracocephalum kotschyi extract, are responsible for its antispasmodic activity and might be used for this purpose in patients having abdominal spasm.