Effects of flavone on the contractile activity of the circular smooth muscle of the rabbit middle colon in vitro.

The circular smooth muscles of the middle colon of the rabbit generate giant contractions of high amplitude and low frequency. Flavone, at various concentrations, reduces the giant contractions and the tonic contraction induced by 10 µM carbachol and 80 mM KCl. The contractions induced by dequalinium and tetraethylammonium are reduced by flavone (30 µM). At 100 µM, flavone decreases the contraction induced by 100 µM methylene blue and 1mM orthovanadate. These results suggest that flavone inhibit the giant contractions by (1) inhibition of voltage-dependent Ca(2+) channels, (2) activation of guanyl cyclase, (3) opening of K(+) channels and (4) inhibition of tyrosines kinases.

The spontaneous mechanical activity of the circular smooth muscle of the rabbit colon in vitro.

The spontaneous mechanical activity of the proximal, middle and distal colon of the rabbit shows in vitro two types of contractions: phasic contractions with low amplitude and high frequency, giant contractions (GCs) with high amplitude and low frequency. Both patterns of contractions did not present differences according to the region. Investigations on the neural control of giant contractions in the middle colon gave the following results. (1) GCs are insensitive to muscarinic antagonism by atropine and ganglionic blockade by hexamethonium; (2) GCs are converted into phasic contractions following the inhibition of acetylcholinesterase by neostigmine, and are abolished for a short period by dimethyl-phenyl-piperazinium, a ganglionic nicotinic receptor agonist; (3) application of L-arginine, the substrate of nitric oxide (NO) synthase prolonged the duration of GCs without affecting their amplitude; sodium nitroprusside, a donor of NO, reduced both the amplitude and frequency of GCs; (4) inhibition of guanylate cyclase by methylene blue converted GCs into phasic contractions; (5) blockade of K(+) channels with the non-selective blocker, tetraethylammonium, or with the more selective apamin-sensitive Ca(2+)-dependent K(+) channels blocker, dequaliniun, increased the resting tone and decreased the amplitude of contractions; whereas opening of ATP-sensitive K(+) channels by diazoxide abolished any rhythmic contractile activity. These data taken together suggest that the amplitude and frequency of GCs are controlled by the endogenous release of NO which activates guanylate cyclase, the subsequent formation of cGMP activates in turn the opening of Ca(2+)-dependent K(+) channels. The cholinergic input seems to be responsible of the resting tone, and an increase of this tone is prone to impose the phasic contractions pattern to the tissue.

Effect of tannins from Quercus suber and Quercus coccifera leaves on ethanol-induced gastric lesions in mice.

The gastroprotective effects of 70% acetone extracts of Quercus suber and Quercus coccifera leaves and of tannins (pedunculagin, castalagin, phillyraeoidin A, and acutissimin B) purified from these extracts were examined in the mouse using the ethanol-induced gastric ulcer model. Both extracts (25, 50, and 100 mg/kg), given orally, prevented the formation of ethanol-induced lesions in the stomach. The percent protection varied between 68 and 91%. Purified tannins (50 mg/kg) were also effective in protecting the stomach against ethanol, and the percent protection varied from 66 to 83%. Castalagin was the most potent. Both extracts and all of the tannins tested (10, 25, and 50 microg/mL) strongly inhibited (55-65%) the lipid peroxidation of rabbit brain homogenate. These results suggest that the gastroprotective effects of extracts of Q. suber and Q. coccifera leaves and the purified tannins in this experimental model are related to their anti-lipoperoxidant properties.