In vivo and in vitro anti-inflammatory potential of pentahydroxy-pregn-14-ol, 20-one-beta-D-thevetopyranoside in rats

Abstract

Polyhydroxy pregnane glycoside (PPG), a steroidal glycoside was isolated from Wattakaka volubilis Linn. (Stap.f.). PPG was evaluated for in vivo and in vitro anti-inflammatory activity using acute inflammation and chronic model of inflammation in rats and LPS-induced RAW 264.7 macrophage cells. PPG seemed to be responsible for the anti-inflammatory activity in the studied models. PPG at dose level of both 5 and 10 mg/kg significantly reduced the edema induced by the carrageenan in acute model of inflammation. It also showed significant anti-proliferative effect (dry pellet weight basis) in chronic model of inflammation. Cellular content of granuloma was measured by assaying activity of N-acetyl glucosaminidase (NAG) and total nucleic acid content. PPG at 5 and 10 mg/kg significantly suppressed the cellular infiltration measured by total nucleic acid content. In contrast, NAG activity decreased over a period of 10 days resulting in inhibition of granuloma weight gain. PPG had a more effective response than the reference drug diclofenac sodium in both the models of inflammation. Wattakaka volubilis steroidal glycoside mixture (WVSM) and PPG (1-50 mu M) significantly inhibited the COX-2 and iNOS enzymes resulting in low levels of PGE(2) and NO in LPS-induced RAW 264.7 macrophage cells. Hence the study supports the traditional use of Wattakaka volubilis and its constituent PPG in treatment of inflammatory disorders. (C) 2013 Elsevier GmbH. All rights reserved.