当前位置: X-MOL 学术Bioorg. Med. Chem. › 论文详情
Our official English website, www.x-mol.net, welcomes your feedback! (Note: you will need to create a separate account there.)
Design, synthesis and evaluation of a baicalin and berberine hybrid compound as therapeutic agent for ulcerative colitis
Bioorganic & Medicinal Chemistry ( IF 3.3 ) Pub Date : 2020-08-06 , DOI: 10.1016/j.bmc.2020.115697
Dan Jia 1 , Yonghui Dou 2 , Ziwen Li 3 , Xinxin Zhou 4 , Ying Gao 4 , Keji Chen 5 , Weihong Cong 6 , Min Ma 7 , Zhengzhi Wu 3 , Weimin Li 4
Affiliation  

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.



中文翻译:

黄ical素和小ber碱杂合化合物作为溃疡性结肠炎治疗剂的设计,合成和评价

源自中药(TCM)的活性天然化合物的结构修饰在新药的开发中显示出巨大的优势。在中医中,“黄勤-黄连”是经典的“药对”,已经用于治疗肠道疾病已有数千年的历史,而黄ical苷和小ber碱分别是黄q和黄连的主要活性成分。基于这种“药物对”,我们设计并合成了一种新的黄ical素和小ber碱杂化化合物(BBH)。其分子结构通过光谱法确认。在体外检测到BBH的抗菌活性。结果表明,与原始合成材料(黄ical素和小ber碱)相比,新的混合化合物对蛋白菌具有最佳的抗菌活性。体内,还研究了BBH对溃疡性结肠炎的影响。BBH治疗显着改善了疾病症状,并预防了溃疡性结肠炎的结肠损伤。此外,BBH通过调节结肠组织中的SOD,MPO活性和促炎性细胞因子(TNF-α,IL-1β和IL-6)的表达而显示出显着的抗炎作用。数据还表明,BBH在改善结肠损伤方面比黄ical苷和小ber碱更优越。这表明新的杂合化合物BBH在治疗溃疡性结肠炎中显示出增强的功效。MPO和结肠组织中促炎性细胞因子(TNF-α,IL-1β和IL-6)的表达。数据还表明,BBH在改善结肠损伤方面比黄ical苷和小ber碱更优越。这表明新的杂合化合物BBH在治疗溃疡性结肠炎中显示出增强的功效。MPO和结肠组织中促炎性细胞因子(TNF-α,IL-1β和IL-6)的表达。数据还表明,BBH在改善结肠损伤方面比黄ical苷和小ber碱更优越。这表明新的杂合化合物BBH在治疗溃疡性结肠炎中显示出增强的功效。

更新日期:2020-08-11
down
wechat
bug