Anti‐inflammatory R‐prostaglandins from Caribbean Colombian soft coral Plexaura homomalla. (14th October 2013)

• Record Type: Journal Article
• Authors: Reina, Eduardo; Ramos, Freddy A.; Castellanos, Leonardo; Aragón, Marcela; Ospina, Luis F.
• Is Part Of: Journal of pharmacy and pharmacology. Volume 65:Number 11(2013:Nov.)
• Page Start: 1643
• Page End: 1652
• Publication Date: 2013-10-14
• Subjects: Pharmacy -- Periodicals; Pharmacology -- Periodicals; 615.1
• DOI: 10.1111/jphp.12138
• Languages: English
• ISSNs: 0022-3573

Abstract

<abstract abstract-type="main"> <title>Abstract</title> <sec id="jphp12138-sec-0001" sec-type="section"> <title>Objectives</title> <p>This study aims to evaluate the effect of prostaglandins isolated from soft coral <italic>Plexaura homomalla</italic>, collected in Colombian Caribbean Sea, on in vivo and in vitro inflammation models.</p> </sec> <sec id="jphp12138-sec-0002" sec-type="section"> <title>Methods</title> <p>Extracts from <italic>P</italic><italic>. homomalla</italic> were fractionated and sequentially chromatographed to obtain the prostaglandins: (15<italic>R</italic>)‐PGA<sub>2</sub> (<bold>1</bold>), (15<italic>R</italic>)‐PGA<sub>2</sub>‐Me (<bold>2</bold>), (15<italic>R</italic>)‐<italic>O</italic>‐Ac‐PGA<sub>2</sub> (<bold>3</bold>), (15<italic>R</italic>)‐<italic>O</italic>‐Ac‐PGA<sub>2</sub>‐Me (<bold>4</bold>) and (15<italic>R</italic>)‐PGE<sub>2</sub> (<bold>5</bold>) in addition to three semi‐synthetic prostaglandins obtained by transformations of the natural products. The anti‐inflammatory properties of natural and semi‐synthetic compounds were determined <italic>in vivo</italic> using 12‐<italic>O</italic>‐tetradecanoylphorbol‐13‐acetate (TPA)‐induced mouse ear oedema model and in vitro leucocyte degranulation, myeloperoxidase (MPO) and elastase enzymatic activities from human polymorphonuclear cells (PMNs). The cell viability was evaluated by the 3‐(4, 5‐dimethylthiazol‐2‐yl)‐2, 5‐diphenyltetrazolium bromide assay.</p> </sec> <sec id="jphp12138-sec-0003" sec-type="section"> <title>Key findings</title> <p>In the in vivo assay, (15<italic>R</italic>)‐PGE<sub>2</sub> (<bold>1</bold>) and (15<italic>R</italic>)‐<italic>O</italic>‐Ac‐PGA<sub>2</sub> (<bold>3</bold>) showed anti‐inflammatory activity, as well as in vitro inhibition of elastase release from PMNs. In the PMNs degranulation assay, (15<italic>R</italic>)‐PGE<sub>2</sub> (<bold>5</bold>), was the most active compound in the inhibition of MPO release. Finally, all the tested prostaglandins showed moderate inhibition for elastase enzyme activity, whereas none of the prostaglandins exhibit significative inhibition on MPO activity.</p> </sec> <sec id="jphp12138-sec-0004" sec-type="section"> <title>Conclusion</title> <p>(15<italic>R</italic>)‐PGE<sub>2</sub> (<bold>1</bold>) and (15<italic>R</italic>)‐<italic>O</italic>‐Ac‐PGA<sub>2</sub> (<bold>3</bold>) present significant inhibition on three important events related to the topical inflammatory response induced by TPA: the oedema formation, the PMNs degranulation, events that modulate MPO and elastase levels at inflammation site, and the inhibition of the enzyme activity.</p> </sec> </abstract>