中文摘要
申请人近年来从事“中药药效物质与中药代谢”研究,以生物转化为纽带,将中药化学与中药代谢相结合,在中药作用物质明晰及指导科学配伍方面取得了系统的创新性成果:1.利用组合生物转化技术,构建代谢产物制备鉴定的新方法,解决中药代谢研究的瓶颈问题,首次全解析中药蟾酥人体代谢通路。2.建立中药代谢稳定性研究体系,揭示关键药效物质和药代/药效靶点,从中药蟾酥中发现新型抗肿瘤先导化合物。3.首次发现CYP3A4,SULT2A1等关键代谢酶的高选择性探针;并基于代谢酶,阐明中药配伍规律;构建计算模型预测潜在配伍关系,指导中药安全用药。上述成果在阐明中药关键物质,开发新型天然药物,指导合理配伍方面具有重要科学价值。主持国家自然科学基金4项,入选辽宁省特聘教授, 省百人。第一完成人获辽宁省科技进步二等奖。编写教材论著11部,发表SCI论文105篇,第一作者15篇,通讯作者50篇,其中6篇IF>5,5篇IF>4。
英文摘要
Xiaochi Ma has engaged in the research fields of medicinal material base and metabolism of traditional Chinese medicines (TCMs) for recent years. By using biotransformation technology as an important bridge to combine the chemistry of TCMs with TCMs metabolism, the great achievements in clarification of key medicinal material base in TCMs and vital guides for reasonable usage of TCMs in clinic, were developed. 1. By combinatorial biotransformation technology as the supplementary mean, a novel method was developed for effective preparation and accurate identification of metabolites of TCMs, which successfully resolved the rate-limiting step of TCMs metabolism research. By this approach, it is first time to fully figure out the metabolic profiles of common Chinese medicine, Chansu, in human. 2. The systematic research model of metabolism stability was established to evaluate the metabolism stability regulation of bufadienolides to reveal the key material base and potential pharmacological targets of Chansu, then we exploited the novel anticancer leading compound from Chansu. Additionally, using this metabolism stability research model, we found the several highly selective probes from Chansu, for the key human metabolic enzymes such as CYP3A4,SULT2A1,UGT1A3/1A4. 3. Base on the metabolic enzymes, we successfully explained the compatibility relationship of TCMs in clinic, and developed the advanced computer model to predict the potential compatibility interaction, which was vital for guide the safe medication of TCMs in practices. These research findings would give the important scientific significances in elucidating the key material substances of TCMs, developing the novel natural leading compounds, guiding reasonable usage of TCM in clinic and provide the vital information for the modernization and globalization of TCMs. In recent years, Xiaochi Ma was awarded multiple projects including four national Natural Science foundation of China, Distinguished Professor of Liaoning Province, Liaoning BaiQianWan Talents Program, and won the second prize of Liaoning provincial scientific and technological progress award as the first completed person. Xiaochi Ma had published more than 103 academic articles, including the first author of 15 publications, and corresponding author of 50 publications, including IF>5 (six publications ) and IF>4 (5 publications ) in the investigation of TCMs.
