Design, synthesis and evaluation of 2,4-diarylpyrano[3,2-c]chromen-5(4H)-one as a new class of non-purine xanthine oxidase inhibitors.

Abstract Keeping in view the recent success of molecular hybridization technique in drug design, 2,4-diarylpyrano[3,2-c]chromen-5(4H)-ones as conjugates of coumarins and chalcones have been designed and synthesized in the present study. The catalytic efficiency of various Lewis acids for the synthesis of designed conjugates under neat conditions was investigated, and SiO (200-400 mesh)-ZnCl was optimized as the best catalyst among the tested ones. The conjugates were evaluated for in-vitro xanthine oxidase activity.

Implications of minocycline, platelet-derived growth factor, and transforming growth factor-beta on inflammatory repair potential in the periodontium.

Background: Semisynthetic tetracyclines used in the adjunctive treatment of inflammatory periodontal disease enhance collagen expression in induced periodontal lesions of rats. Polypeptide growth factors regulate key cellular events in tissue repair. The physiologically active androgen 5 alpha-dihydrotestosterone (DHT) stimulates bone and connective tissue turnover.

The uptake of two androgen substrates by cultured human gingival fibroblasts in response to minocycline and metabolic studies using a cell-free system.

The uptake of two androgen substrates by cultured fibroblasts and the anabolic response of homogenates of cultured gingival fibroblasts to minocycline were investigated. Monolayer cultures of confluent fibroblasts were incubated with [14C]testosterone/[14C]4-androstenedione for timed intervals in the presence or absence of optimal concentrations of minocycline. The intracellular uptake of androgens was quantified by radio-isotope counts on cell digests.

Effects of the anti-androgen finasteride on 5alpha-reductase activity in human gingival fibroblasts in response to minocycline.

In addition to their antimicrobial properties, tetracyclines have antiinflammatory and pro-anabolic effects on the reparatory potential of connective tissue and bone. The physiologically active androgen 5alpha-dihydrotestosterone (DHT) implicated in matrix synthesis is formed in gingivae from androgen substrates. The aim of this investigation is to study the androgen metabolic response of gingivae to minocycline, in the presence or absence of the anti-androgen finasteride.