Cistus incanus and Cistus monspeliensis inhibit the contractile response in isolated rat smooth muscle.

The lyophilized aqueous extracts from Cistus incanus L. (CI) and Cistus monspeliensis L. (CM) collected in Sicily were studied in order to evaluate their myorelaxant activity by using isolated smooth muscle of rat ileum and rat aorta. Both CI and CM extracts concentration-dependently inhibited the contractile response to acetylcholine (ACh), phenylephrine (PE) and to 100 mM KCl. The concentration-contraction curves to ACh in ileum and to PE in aorta, were displaced to the right by Cistus extracts in a non-competitive manner, with a depression of the maximum contractile response. The EC50 (microg/ml) of CM and CI were: ileum/KCl, CM 457+/-99, CI 681+/-80; ileum/ACh 100 microM, CM 297+/-66, CI 335+/-41; aorta/KCl, CM 360+/-21, CI 843+/-36; and aorta/PE 10 microM, CM 287+/-33, CI 451+/-58. The two extracts resulted almost equi-active in ileum, whereas CM was more active than CI in aorta. These data indicate that Cistus extracts act as spasmolytic on intestinal and vascular smooth muscle. The antagonism they exert on ACh-, PE- and KCl-evoked contractions seems to be functional, because it is not specifically directed toward any particular receptor; furthermore, a calcium-antagonist activity seems unlikely, since the extracts are capable of completely block the contractile response to agonists.

Antioxidant activity and protective effect on DNA cleavage of extracts from Cistus incanus L. and Cistus monspeliensis L.

The genus Cistus includes many typical species of Mediterranean flora; Cistus species are used as antidiarrhetics, as general remedies for treatment of various skin diseases in folk medicine and as anti-inflammatory agents. These species contain flavonoids that are considered to be chain-breaking antioxidants. In this work, we have investigated the effects of crude aqueous extracts from Cistus incanus and Cistus monspeliensis on DNA cleavage and their free-radical scavenging capacity. In addition, their effect on lipid peroxidation in rat liver microsomes was evaluated. These extracts showed a protective effect on DNA cleavage and a dose-dependent free-radical scavenging capacity; Cistus monspeliensis was more active than Cistus incanus; these results were confirmed by a significant inhibition of lipid peroxidation in rat liver microsomes. The experimental evidence, therefore, suggests that because of their antioxidant activity these extracts may offer excellent photoprotection for skin and may be useful in the treatment of human diseases where oxidative stress plays a key role.

Gastroprotective effect of aqueous extract of Cistus incanus L. in rats.

The antiulcer activity of a short-boiled aqueous extract from aerial parts of Cistus incanus was studied in rats against gastric lesions induced by necrotizing agents (1N HCl and absolute ethanol), indomethacin, serotonin and reserpine. The extract, containing bioflavonoids, was orally administered in the range from 0.25 to 0.50 g kg-1. It was found to have significant dose-related protective effects in all these experimental models, and was more effective against reserpine- and serotonin-induced mucosal congestion and haemorrhagic ulcers. These data suggest that the active constituents of the crude extract could be responsible for its protective effect by maintaining an efficient gastric mucosal microvascular supply.

Influence of sodium valproate and carbamazepine on GSH levels in rat cerebral cortex.

The effects of sodium valproate (150 mg/kg) and carbamazepine (300 mg/kg), alone and in combination, on the content of glutathione (GSH) were investigated in the rat cerebral cortex. No modification was found either 4, 12 or 16 hours after treatment, suggesting that sodium valproate and carbamazepine do not affect the cortical GSH metabolism in rats.

Pharmacological properties and toxicology of MED-15, a prodrug of tolmetin.

In this study the pharmacological evaluation of MED-15, a non-acidic prodrug of tolmetin, is described. After oral administration the new compound shows a marked anti-inflammatory activity similar to that of tolmetin, but with minor ulcerogenic action and lower acute toxicity.

Antioxidant enzymatic systems and oxidative stress in erythrocytes with G6PD deficiency: effect of deferoxamine.

In the present study we have assayed the effect of divicine in G6PD-deficient red blood cells in the presence of deferoxamine (iron-chelating drug) and NaN3 (inhibitor of catalase). The effect of divicine has been compared to oxidative stress by H2O2; haemolysis is regarded as an index of cellular toxicity. In addition, we have tested antioxidant enzymatic systems. No significant change in antioxidant enzymatic systems was found in RBCs from subjects with G6PD deficiency when compared to the control group, either in oxidative haemolysis by divicine or by H2O2; a significant decrease in oxidative haemolysis by H2O2 was observed in the presence of deferoxamine, whereas no change was found in oxidative haemolysis by divicine. The replacement of incubation medium by homologous plasma or the supplementation with bovine serum albumin resulted in a marked decrease of percentage of haemolysis by divicine.

Synthesis and pharmacological activity of 6H-thiazolo [3',2': 1,2]-5-oxopyrimido[5,4-b]indole derivatives, a new heterocyclic ring system.

In the outline of the investigations concerning the analgesic and antiinflammatory activity of new fused heterocyclic compounds containing the pyrimidine ring, a series of 6H-thiazolo[3',2': 1,2]-5-oxopyrimido[5,4-b]indole derivatives was synthesized. Pharmacological results are reported and discussed.

Papaver somniferum L. var. album D.C. cultivated in Sicily: phytochemical investigation and use.

The authors evaluated the vegetative growth and alkaloid content of the Papaver somniferum L. var. album D.C. capsules cultivated in Assoro (Enna) Sicily, in relation to the geographical position, environmental conditions and soil type. Gas chromatography revealed low alkaloid opiate producing capacity which makes cultivation for therapeutic and toxicologic purposes uneconomic. On the contrary, the elevated production of capsules containing numerous seeds justifies its cultivation for extraction of oil for the food industry and paint production. The results suggest that the cultivation of Papaver somniferum studied is used for baking traditional cakes and bread.

New heterocyclic ring systems--V synthesis and pharmacological activity of 6H-1,3,4-thiadiazolo [3',2':1,2]-5-oxopyrimido [5,4-b] indole derivatives and of 1-phenyl-6H-1,2,4-triazolo [1',5':1,2]-5-oxopyrimido[5,4-b] indole.

As a part of a study on analgesic and antiinflammatory active condensed heterocyclic compounds containing the pyrimidinic ring, a number of 6H-1,3,4-thiadiazolo [3',2':1,2]-5-oxopyrimido [5,4-b]indole and 1-phenyl-6H-1,2,4-triazolo [1',5':1,2]-5-oxopyrimido [5,4-b] indole were synthesized and tested. The results of pharmacological assays are reported and discussed.