According to a survey, non-steroidal anti-inflammatory agents were the most popular analgesic used in South Africa for management of peri-operative pain, acute post-operative pain and chronic pain. The most popular non-steroidal anti-inflammatory agents are flunixin meglumine and phenylbutazone. The most popular opioid type drug is buprenorphine, followed by morphine. In the peri-operative sett...

Structure-activity relationship translation offers an expeditious means for discovery of new active series. This approach was applied to discover tetrahydroisoquinoline (THIQ)-based steroidomimetic microtubule disruptors. The two A-ring elements of a three-point steroidal pharmacophore were incorporated into a THIQ-based A,B-ring mimic to which an H-bond acceptor was attached as the third motif...

The aglycon form of the steroidal sapogenin furost -5-ene-3 beta, 22,26-triol, 3 beta- chacotrioside 26 beta-D-glucopyranoside was isolated from cell suspension cultures of Dioscorea deltoidea and its molecular structure was determined by mass spectrometry and 1H and 13C n.m.r. spectroscopy. From kinetic studies and incorporation experiments with [1-14C]acetate it was concluded that the steroid...

Non-steroidal anti-inflammatory drugs have been clearly shown to increase the chances of peptic ulcer and its complications. Risk factors associated with this propensity are as yet poorly and inconsistently defined. Clinicians have long accepted that non-steroidal anti-inflammatory drug (NSAID) treatment may cause peptic ulcer and its complications. In assessing the chances it is necessary to d...

The configurational and conformational analyses of α-methylene-γ-butyro steroidal spirolactones have been accomplished using 2D COSY, NOESY, ROESY and HETEROCOSY in conjunction with 1D H NMR. The analyses indicate that the major or the only spirolactones formed at positions 2, 3 and 6 of the steroids have the steroidal ring bearing the spirolactone in a chair conformation with an axial disposit...

Structure-based drug design approach is used to design and analyze cytochrome P450 inhibitors for the treatment of prostate cancer. The structural efficiency of inhibitors is measured by the ability of the designed inhibitors to form interactions with atoms in the active site of cytochrome P450 that includes a heme group. Docking studies are conducted to analyze the structural effectiveness of ...

A new steroidal saponin was isolated from the leaves of Agave attenuata Salm-Dyck. Its structure was established as (3beta,5beta,22alpha,25S)-26-(beta-D-glucopyranosyloxy)-22-methoxyfurostan-3-yl O-beta-D-glucopyranosyl-(1-->2)-beta-D-glucopyranosyl-(1-->2)-O-[beta-D-glucopyranosyl-(1-->3)]-beta-D-glucopyranosyl-(1-->4)-beta-D-galactopyranoside. The structural identification was performed using...

Drug histories were obtained from 76 patients at the time of initial Eder-Puestow dilatation for benign oesophageal stricture. Six patients had consumed drugs known to cause oesophageal ulceration (emepronium bromide and potassium preparations). Of the remaining 70 patients, 22 had regularly taken a non-steroidal anti-inflammatory drug before the onset of dysphagia compared with 10 patients in ...

The effects of three non-steroidal anti-inflammatory drugs, ibufenac, sulindac and mepirizole, on the renal excretion of sulfamethizole in rats were investigated, in order to clarify the mechanisms involved. The clearance ratio of sulfamethizole was markedly decreased after infusion of ibufenac, while sulindac or mepirizole had no effect on the clearance ratio of sulfamethizole. From this resul...

A new steroidal saponin, named pumilum A (1), and a new phenolic glycoside, threo-1-(4'-hydroxy-2'-methoxyphenyl)-2-(2",4"-dihydroxyphenyl)-1,3-propanediol-4'-O-β-D-glucopyranoside (7) were isolated from the methanolic extract of the bulbs of Lilium pumilum DC, along with five known steroidal saponins. Their chemical structures were elucidated on the basis of detailed spectroscopic analysis, in...