机构：[1]Guangzhou General Pharmaceutical Research Institute, Guangzhou, Guangdong 510240, PR China[2]Integrated Chinese and Western Medicine, Post-doctoral Research Station, Jinan University, Guangzhou, PR China[3]Shenzhen Second People’s Hospital/the First Affiliated Hospital of Shenzhen University Health Science Center, Shenzhen 518035, PR China深圳市第二人民医院深圳医学信息中心[4]Shenzhen Institute of Geriatrics, Shenzhen 518020, PR China[5]Basic Medical School, Guangzhou University of Chinese Medicine, Guangzhou 510006, PR China[6]Academy of Traditional Chinese Medicine, Guangzhou University of Chinese Medicine, Guangzhou 510006, PR China[7]Xiyuan Hospital, China Academy of Chinese Medical Scineces, Beijing 100000, PR China[8]Labortary of Cardiovascular Diseases, Xiyuan Hospital, China Academy of Chinese Medical Scineces, Beijing 100000, PR China
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-alpha, IL-1 beta 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.
基金：
Shenzhen Basic Discipline Layout Project [JCYJ20170413161352000]; Science and Technology Foundation of Guangdong Province of China [2017A050506007]
第一作者机构：[1]Guangzhou General Pharmaceutical Research Institute, Guangzhou, Guangdong 510240, PR China[2]Integrated Chinese and Western Medicine, Post-doctoral Research Station, Jinan University, Guangzhou, PR China[4]Shenzhen Institute of Geriatrics, Shenzhen 518020, PR China
共同第一作者：
通讯作者：
通讯机构：[2]Integrated Chinese and Western Medicine, Post-doctoral Research Station, Jinan University, Guangzhou, PR China[3]Shenzhen Second People’s Hospital/the First Affiliated Hospital of Shenzhen University Health Science Center, Shenzhen 518035, PR China[4]Shenzhen Institute of Geriatrics, Shenzhen 518020, PR China[6]Academy of Traditional Chinese Medicine, Guangzhou University of Chinese Medicine, Guangzhou 510006, PR China[*1]232 Outer Ring Road, Guangzhou Higher Education Mega Center, Guangzhou, PR China[*2]No. 2008 Sungang West Road, Futian District, Shenzhen, PR China[*3]No. 601 HuangpuAvenue West, Tianhe District, Guangzhou, PR China
推荐引用方式(GB/T 7714)：
Jia Dan,Dou Yonghui,Li Ziwen,et al.Design, synthesis and evaluation of a baicalin and berberine hybrid compound as therapeutic agent for ulcerative colitis[J].BIOORGANIC & MEDICINAL CHEMISTRY.2020,28(20):doi:10.1016/j.bmc.2020.115697.
APA：
Jia, Dan,Dou, Yonghui,Li, Ziwen,Zhou, Xinxin,Gao, Ying...&Li, Weimin.(2020).Design, synthesis and evaluation of a baicalin and berberine hybrid compound as therapeutic agent for ulcerative colitis.BIOORGANIC & MEDICINAL CHEMISTRY,28,(20)
MLA：
Jia, Dan,et al."Design, synthesis and evaluation of a baicalin and berberine hybrid compound as therapeutic agent for ulcerative colitis".BIOORGANIC & MEDICINAL CHEMISTRY 28..20(2020)
