Sanguinarine-Chelerythrine from Coptis chinensis Offers Analgesic and Anti-Inflammatory Effects Without Gastrotoxicity.

Abstract

Background: Pain is a major clinical and socioeconomic problem worldwide. The available therapies are not always effective and are often associated with the multiple adverse effects that reduce their clinical application. 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 Coptis chinensis. Methods: The analgesic and anti-inflammatory activity of the sanguinarine-chelerythrine fraction of C. chinensis extract (SC 5 and 10 mg/kg), sanguinarine (SAN 1 and 2 mg/kg) and chelerythrine (CHEL 4 and 8 mg/kg) was assessed in tail flick and formalin tests. A microscopic and macroscopic examination of stomach mucosae was performed. TNFα and MMP-9 levels were measured with ELISA kits. Results: Morphine (MORF), CHEL and SC prolongated the tail withdrawal latency, with comparable analgesic activity between MORF 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 additionally reduced TNFα 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.