Gu Ting, Zhong Yue, Lu Yu-Ting, Sun Ying, Dong Ze-Xi, Wu Wen-Yu, Shi Zhi-Hao, Li Nian-Guang, Xue Xin, Fang Fang, Li He-Min, Tang Yu-Ping
National and Local Collaborative Engineering Center of Chinese Medicinal Resources Industrialization and Formulae Innovative Medicine, Nanjing University of Chinese Medicine, Nanjing, Jiangsu 210023, China.
Department of Medicinal Chemistry, Nanjing University of Chinese Medicine, Nanjing, Jiangsu 210023, China.
Molecules. 2017 Jun 21;22(6):1028. doi: 10.3390/molecules22061028.
Scutellarin () has been widely used to treat acute cerebral infarction in clinic, but poor aqueous solubility decreases its bioavailability. Interestingly, scutellarin () could be metabolized into scutellarein () in vivo. In this study, a sulfonic group was introduced at position C-8 of scutellarein () to enhance the aqueous solubility of the obtained derivative (). DPPH (1,1-diphenyl-2-picrylhydrazyl)-radical scavenging ability and antithrombic activity were also conducted to determine its bioactivity. The result showed that scutellarein derivate () could be a better agent for ischemic cerebrovascular disease treatment.
灯盏花素()已在临床上广泛用于治疗急性脑梗死,但水溶性差降低了其生物利用度。有趣的是,灯盏花素()在体内可代谢为灯盏乙素()。在本研究中,在灯盏乙素()的C-8位引入磺酸基团以提高所得衍生物()的水溶性。还进行了DPPH(1,1-二苯基-2-苦基肼)自由基清除能力和抗血栓活性测定以确定其生物活性。结果表明,灯盏乙素衍生物()可能是治疗缺血性脑血管疾病的更好药物。