Bronchodilatory and mast cell stabilising activity of Cressa cretica L.:Evaluation through in vivo and in vitro experimental models

Objective:To evaluate the effect of ethylacetate fraction(Fr-Et) and methanolic fraction(FrMe) obtained from Cressa cretica L.(C.crelica) L on experimental models for bronchodilatory activity and mast cell stabilising activity.Methods:The effect of Fr-Et and Fr-Me were studied on acetylcholine and histamine aerosol-induced broncospasm using guinea pigs as experimental animals.Also,the effects of these fractions were evaluated on the isolated guinea pig tracheal preparations.Besides this mast cell degranulation effect was assessed using egg albumin and compound 48/80 on rat peritoneal mast cells.Results:Significant increase in nreconvulsion time was observed due to pretrealment with the fractions when guinea pigs were exposed to histamine and acetylcholine aerosol.Fr-Et and Fr-Me significantly increased the preconvulsion in a dose depended manner that suggestive of bronchodilating activity.Fr-Et and Fr-Me exhibited a significant concentration dependant relaxant effect on guinea pig trachea pre-contracted with CCh,K^+ and histamine.The results revealed that Fr-Et to be more potent than Fr-Me in relaxing histamine and K^+ and calcium induced contraction than CCh induced conlractions.Studies on the fractions in protecting mast cell degranulation,which were elicited by the egg albumin as well as synthetic compound 48/80 revealed both the fractions significantly protect the mast cell degranulation,which release mediators such as histamine and proinflammatory cytokines through various stimuli in a dose depended manner.Conclusions:Thus our study established the bronchodilator activity,and mast cell stabilizing activity which are important mediators that provoke or sustain in asthma.

Synthesis and Bronchodilatory Activities of New Pyrazolo[4,3-d]pyrimidin-7-ones

Twelve novel pyrazolo [4,3-d] pyrimidin-7-ones were synthesized and their structures were confirmed by IR, 1H NMR and MS. Their in vitro bronchodilatory activities were tested in guinea-pigs. The pharmacological results show that compound 11c has more potent activity than aminophylline.

Anti-inflammatory and bronchodilatory constituents of leaf extracts of Anacardium occidentale L. in animal models

Objective： Anocardium occidentale L. leaf is useful in the treatment of inflammation and asthma, but the bioactive constituents responsible for these activities have not been characterized. Therefore, this study was aimed at identifying the bioactive constituent（s） ofA. occidentale ethanolic leaf extract （AOEL） and its solvent-soluble portions, and evaluating their effects on histamine-induced paw edema and bronchocon- striction. Methods： The bronchodilatory effect was determined by measuring the percentage protection provided by plant extracts in the histamine-induced bronchoconstriction model in guinea pigs. The anti- inflammatory effect of the extracts on histamine-induced paw edema in rats was determined by measur- ing the increase in paw diameter, after which the percent edema inhibition was calculated. The extracts were analyzed using gas chromatography-mass spectrometry to identify the bioactive constituents. Column chromatography and Fourier transform infrared spectroscopy were used respectively to isolate and characterize the constituents. The bronchodilatory and anti-inflammatory activities of the isolated bioactive constituent were evaluated. Results： Histamine induced bronchoconstriction in the guinea pigs and edema in the rat paw. AOEL, hexane-soluble portion of AOEL, ethyl acetate-soluble portion of AOEL, and chloroform-soluble portion of AOEL significantly increased bronchodilatory and anti-inflammatory activities （P 〈 0.05）. Oleamide （9-octadecenamide） was identified as the most abundant compound in the extracts and was isolated. Oleamide significantly increased bronchodilatory and anti-inflammatory activities by 32.97% and 98.41%, respectively （P 〈 0.05）. Conclusion： These results indicate that oleamide is one of the bioactive constituents responsible for the bronchodilatory and anti-inflammatory activity of A. occidentale leaf, and can therefore be employed in the management of bronchoconstriction and inflammation.