Sanguinarine-Chelerythrine from <i>Coptis chinensis</i> Offers Analgesic and Anti-Inflammatory Effects Without Gastrotoxicity

Background: Pain is a major clinical and socioeconomic problem worldwide and existing therapies are not always effective and are often associated with the burden of adverse effects that limit their usage. Natural compounds are an important group of pharmaceuticals that may be used in pain management. We aimed to investigate the analgesic activity of the sanguinarine-chelerythrine from C. chinensis. Methods: The analgesic and anti-inflammatory activity of sanguinarine-chelerythrine fraction of C. chinensis (SC 5 and10mg/kg), sanguinarine (SAN 1 and 2 mg/kg) and chelerythrine (CHEL 4 and 8 mg/kg ) was assessed in the tail-flick and formalin tests. Microscopic and macroscopic examination of stomach mucosae was performed. TNF&alpha; and MMP-9 levels were measured with ELISA kits. Results: Morfine (MORF), CHEL and SC prolongated the tail withdrawal latency and with comparable analgesic activity of MRF and CHEL 8 mg/kg. MORF, CHEL 8 mg/kg, and SAN 2 mg/kg ameliorated the pain reaction in the neurogenic phase of the formalin test. In the inflammatory phase of the formalin test, all tested substances exerted analgesic activity. SAN, CHEL and SC reduced additionally TNF&alpha; and MMP-9 secretion.. Conclusions: Our results confirmed analgesic effects of CHEL and SC with CHEL analgesic activity comparable to MORF. All investigated substances exerted significant anti-inflammatory activity without concomitant gastrotoxicity.