PEGylated systems in pharmaceutics

This review addresses the use of poly(ethylene glycol) (PEG) and PEG conjugation for the design of novel dosage forms and the modification of biomolecules. The peculiarities of PEGylated nanoparticles, liposomes, proteins, enzymes, and small drug and polyelectrolyte molecules and their influence on systemic drug delivery, including overcoming of various biological barriers and adhesion to mucosal tissues (mucoadhesion), are considered

Synthesis of trihydroxy quinolizidine alkaloids: 1,3-addition reaction of allylmagnesium bromide to a sugar nitrone

The synthesis of (1R,2R,3S,9aR) and (1R,2R,3S,9aS) trihydroxy quinolizidine alkaloids 3a and 3b from D-glucose derived nitrone 4 is described. The key transformation involves the 1,3-addn. of allylmagnesium bromide to nitrone 4 that afforded high diastereoselectivity in the presence of TMSOTf. The N-O bond reductive cleavage, N-Cbz protection, ozonolysis, Wittig olefination, lactam formation and reductive amination cascade afforded the target compds. 3a and 3b in good overall yield

Rotenoids from <i>Boerhaavia diffusa</i> as Potential Anti-inflammatory Agents

Five new (<b>2</b>, <b>3</b>, <b>5</b>, <b>7</b>, and <b>9</b>) and four known rotenoids (<b>1</b>, <b>4</b>, <b>6</b>, and <b>8</b>) were isolated from a methanol extract of <i>Boerhaavia diffusa</i> roots. The structures of the new rotenoids were elucidated by spectroscopic data interpretation. The 70% ethanol extract, a rotenoid-rich fraction, and all isolated rotenoids were evaluated for their COX-1 and COX-2 inhibitory activities. Among the rotenoids tested, compound <b>7</b> showed the most potent COX-1 and COX-2 inhibition, with IC₅₀ values of 21.7 ± 0.5 and 25.5 ± 0.6 μM, respectively. Boeravinone B (<b>6</b>) exhibited significant anti-inflammatory activity (56.6% at 50 mg/kg) when evaluated in an in vivo carrageenan-induced rat paw model