Pharmacological evaluation for anti-asthmatic and anti-inflammatory potential of Woodfordia fruticosa flower extracts.

CONTEXT: Woodfordia fruticosa Kurz. (Lythraceae) flowers are ethnopharmacologically acclaimed in the Indian medicinal system to treat asthma. OBJECTIVE: To evaluate W. fruticosa flower extracts for anti-asthmatic effect. MATERIALS AND METHODS: Ethyl acetate, acetone, methanol, and hydro-alcohol extracts of W. fruticosa flowers were obtained successively and standardized. Ability of extracts to stabilize free radicals and compound-48/80-induced mast cell degranulation was evaluated. In vitro anti-inflammatory potential of extracts at 100 and 200 µg/ml by membrane stabilization and in vivo inhibition of rat paw edema up to 5 h (100 and 200 mg/ml; p.o.) was evaluated. In vitro bronchorelaxant effect was examined against histamine- and acetylcholine (1 µg/ml; independently)-induced guinea pig tracheal contraction. Extracts were evaluated for bronchoprotection (in vivo) ability against 0.1% histamine- and 2% acetylcholine-induced bronchospasm in guinea pigs at 100 and 200 mg/ml; p.o. RESULTS: Standardization studies revealed that the methanol extract exhibited highest polyphenolic (62.66 GAE), and flavonoid (6.32 RE) content and HPLC fingerprinting confirmed the presence of gallic acid (Rt 1.383). IC50 values for DPPH scavenging and metal chelation by the methanol extract were 40.42 and 31.50 µg/ml. Methanol and ethyl acetate extracts at 100 µg/ml exhibited 06.52 and 07.12% of histamine release. Methanol, ethyl acetate, and hydro alcohol extracts at 200 mg/kg demonstrated 32.73, 29.83, 26.75% and 32.46, 9.38, 26.75% inhibition of egg albumin and carrageenan-induced inflammation, respectively. Methanol extract exhibited 100% bronchorelaxation and 48.83% bronchoprotection. CONCLUSION: Woodfordia fruticosa flower (WFF) extracts exhibited anti-asthmatic effect by demonstrating bronchoprotection, bronchorelaxation, anti-inflammatory, antioxidant, and mast cell stabilization ability.

Bronchorelaxant, mast cell stabilizing, anti-inflammatory and antioxidant activity of Randia dumetorum (Retz.) Lamk. extracts.

Randia dumetorum (RD) fruits in different form have been ethnopharmacologically reported to possess antiasthmatic property. Therefore, present study was undertaken to evaluate two different extracts of RD i.e., ethyl acetate (RD-EA) and methanol (RD-ME) for bronchorelaxant, anti-inflammatory, mast cell stabilizing and antioxidant effect along with safety margin, according to OECD guidelines for toxicity. RD-ME and RD-EA (1 mg/mL) exhibited 68.75 and 57.39% inhibition of contraction against acetylcholine, while against histamine induced contraction, inhibition observed was 100 and 78.13%, respectively. Moreover, extracts attenuated the experimentally induced inflammation at 200 mg/kg with % inhibition of 41.62 by RD-ME and 30.36 by RD-EA in carrageenan model, while in egg albumin model RD-ME and RD-EA exhibited % inhibition of 48.31 and 33.75, respectively. In addition, RD-ME and RD-EA at 100 microg/mL demonstrated significant decrease in histamine release of 08.31 and 16.71 in C-48/80 induced mast cell degradation. RD extracts also exhibited antioxidant activity in DPPH, reducing power and metal chelation method, along with safe margin for oral administration as observed in acute toxicity evaluation.

Synthesis, antihypertensive activity, and 3D-QSAR studies of some new p-hydroxybenzohydrazide derivatives.

p-Hydroxybenzohydrazide 2 on treatment with aromatic/aliphatic aldehyde followed by cyclization with carbon disulphide afforded compounds 4a-4n. Also, compound 2 by treatment of substituted isothiocyanate followed by the treatment of chloroacetic acid yields the corresponding compounds 6a-6i. All the test compounds were assayed for antihypertensive activity by non-invasive blood pressure measurement and invasive blood pressure measurement methods. The test compounds showed significant antihypertensive activity. The intact compounds were subjected to 3D-QSAR studies. The 3D-QSAR analysis was carried out by PHASE program and a statistically reliable model with good predictive power (r(2) = 0.98, q(2) = 0.74) was achieved. The 3D-QSAR plots illustrated insights into the structure-activity relationship of these compounds which may aid in the design of potent p-hydroxybenzohydrazide derivatives as antihypertensive agents.