Antipyretic and Anticonvulsant Activity of Polygonatum verticillatum: Comparison of Rhizomes and Aerial Parts

The current study was undertaken to explore the antipyretic and anticonvulsant profile of the Polygonatum verticillatum in established pharmacological paradigms. The crude methanol extract of rhizomes (PR) and aerial parts (PA) of the plant were tested in Brewer's‐yeast‐induced pyrexia and pentylenetetrazole‐induced convulsion test. PR and PA both evoked prominent antipyretic activity (p < 0.01) in a dose‐dependent manner during all assessment times at the dose of 50, 100, and 200 mg/kg intraperitoneally. The protection elicited by PR (82.20%) at 200 mg/kg was comparable with aspirin (88.48%) as a standard drug at 100 mg/kg. However, PA was less potent, and maximum protection was 64% at 200 mg/kg. Both PR and PA were devoid of any anticonvulsant activity. Our results demonstrated prominent evidence of antipyretic activity of P. verticillatum that is consistent with the folk uses of the plant. In addition from a biodiversity point of view, PA of the plant can also be used as an alternate of PR. Copyright © 2012 John Wiley & Sons, Ltd.     

Piroxicam sulfonates biology-oriented drug synthesis (BIODS), characterization and anti-nociceptive screening

The present study was designed to synthesize aryl/alkyl sulfonyl substituted derivatives of piroxicam. The structures were elucidated through various spectroscopic procedures like ¹H-NMR, ¹³C-NMR, MS, IR, UV and elemental analysis. The synthesized derivatives (I–VI) were screened for anti-nociceptive activity in BALB-c mice by dividing them in five groups (n = 6) for each compound. Test compounds significantly reduced the number of writhes in acetic acid test for peripheral analgesia, but no effect was observed in hot plate test for central analgesia. The compounds possessed good peripheral analgesic effect but no central effect. These compounds were also assessed for acute toxicity in different doses at 50, 100 and 150 mg/kg i.p., and no mortality was observed in animals. In conclusion, the piroxicam derivatives exhibited marked peripheral anti-nociceptive effect with considerable safety.     

Molecular simulations of bergenin as a new urease inhibitor

Bergenin is well-established and potent antioxidant compound with known gastro-protective effects. Main aim of the current investigation was to study the urease inhibitory potential of bergenin both experimentally and computationally. The target compound bergenin was isolated from acetone extract of Mallotus philippinensis bark. Bergenin inhibited the Bacillus pasteurii urease (IC₅₀ value: 21.7?±?0.2?μM). Thiourea was used as standard inhibitor (IC₅₀ value: 25?±?0.09?μM). Molecular docking studies revealed the potential binding mode of bergenin, according to which, Bergenin penetrated deeply into the active catalytic site of urease and was found in close interaction with nickel ions and the various important amino acid residues surrounding the catalytic site of B. pasteurii urease. This might be an additional gastro-protective mechanism by which, bergenin inhibits urease released by various urease producing bacterial strains especially Helicobacter pylori.