Abstract

Structural modification of active natural compounds   which   were   originated from   Traditional Chinese Medicine (TCM) have showed   great advantages   in the   development   of new drugs . In TCM, “Huangqin   -   Huanglian” is a classic “medicine couple”   that   has been used to treat intestinal diseases for thousands of   years, while baicalin   and berberine are the major active compounds   of Huangqin and Huanglian   respectively. Based on   this   “medicine couple”,   we   designed   and synthesized   a new   baicalin and berberine hybrid compound (BBH).   Its molecular structure was   confirmed   by spectroscopy .   The antibacterial activity of BBH was detected in vitro.   Results indicated   that the new hybrid compound exhibited the best antibacterial activity for   proteobacteria as compared with its original synthetic materials (baicalin and   berberine). In vivo, the effect of BBH   on ulcerative colitis   was also   investigated.   BBH treatment significantly ameliorated the disease symptoms and   prevented   the colon damage of ulcerative colitis. Furthermore, BBH showed a   significant anti-inflammatory effect through regulating activities of SOD , MPO   and   expressions of pro-inflammatory cytokines (TNF-α, IL-1β and IL-6) in colon   tissue. Data also suggested that BBH was more superior than baicalin and berberine in   ameliorating colonic damage. This indicated that the new hybrid compound BBH   showed enhanced efficacy in treating ulcerative colitis.