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In vitro COX-1 and COX-2 enzyme inhibitory activities of iridoids from Penstemon barbatus, Castilleja tenuiflora, Cresentia alata and Vitex mollis

2015; Elsevier BV; Volume: 25; Issue: 20 Linguagem: Inglês

10.1016/j.bmcl.2015.08.075

1464-3405

M. Ángeles Ramírez‐Cisneros, Marı́a Yolanda Rios, A. Berenice Aguilar‐Guadarrama, Praveen P. N. Rao, Rola Aburto-Amar, Verónica Rodríguez-López,

Natural product bioactivities and synthesis

A group of sixteen iridoids isolated from plants used as anti-inflammatory remedies in Mexican folk medicine were evaluated for their potential to inhibit cyclooxygenase-1 (COX-1) and cyclooxygenase-2 (COX-2) enzymes. From these assays, loganic acid (10) was identified as the most promising compound with both COX-1 (36.0 ± 0.6%) and COX-2 (80.8 ± 4.0%) inhibition at 10 μM. Compound 10 shows a better inhibition against the COX-2 enzyme. Other iridoids tested in the present study showed weak or no inhibition against these enzymes. Furthermore, herein are presented key interactions of iridoid 10 with COX-1 and COX-2 enzymes through molecular docking studies. These studies suggest that 10 exhibits anti-inflammatory activity due to COX inhibition.