Anti-Inflammatory and Analgesic Activities of Ilex

Biol Pharm Bull. 2008 Apr;31(4):643-50.
In vivo anti-inflammatory and analgesic activities of a purified saponin fraction derived from the root of Ilex pubescens.
Wang JR, Zhou H, Jiang ZH, Wong YF, Liu L.
School of Chinese Medicine, Hong Kong Baptist University, Kowloon Tong, Kowloon, Hong Kong, People's Republic of China.

The root of Ilex pubescens (Mao-Dong-Qing in Chinese, MDQ) has been commonly used for treatment of cardiovascular and inflammatory diseases in the Chinese medical system. The current studies aimed to investigate the anti-inflammatory and analgesic effects as well as the underlying mechanisms of a purified saponin fraction (PSF) derived from MDQ. PSF was found to significantly suppress the paw edema of rats induced by histamine given intraperitoneally at dosages ranging from 12.5-100 mg/kg. Meanwhile, PSF given orally at dosages of 200 and 100 mg/kg significantly inhibited acetic acid-induced abdominal writhing response of mice and prolonged the time required for mouse tail flick after exposure to a source of radiant heat. The mechanistic studies showed that cyclooxygenase-2 (COX-2) protein expression in carrageenan-injected paw tissues of rats was markedly attenuated by intraperitoneal injection of PSF at dosages of 12.5 to 100 mg/kg. PSF could also markedly inhibit production of proinflammatory cytokines, especially IL-1 beta, IL-6 and TNF-alpha, but enhance production of anti-inflammatory cytokines of IL-4 and IL-10 in the carrageenan-injected paw tissues in rats. These effects resulted in an overall attenuation of the ratio of proinflammatory/anti-inflammatory cytokines and, ultimately suppression of the paw edema. In conclusion, the current study has demonstrated the in vivo anti-inflammatory and analgesic effects of PSF, and suggested that the molecular mechanisms might be associated with inhibition of the elevated expression of COX-2 protein and the overproduction of the proinflammatory cytokines, as well as augmentation of the anti-inflammatory cytokines IL-4 and IL-10 in the carrageenan-injected paw tissues of rats.