Important progress has been made in the original research of triterpenoid chemistry in China

[Zhang Wenwen, Science Times] Recently, researchers in China discovered more than 80 triterpenoids with 8 skeleton types and novel structures for the first time after studying the chemical and biological activities of 5 plants of Schisandraceae/KLOC-0. Some new skeleton triterpenoids and lignans have good anti-HIV activity, and one lignan compound (SM 10) is under preclinical study, which has low toxicity and can be used as an adjuvant drug against HIV, with broad prospects. At the same time, through computer virtual screening, it is found that a series of triterpenoids with novel structures bind to many important targets related to neurodegenerative diseases, such as β -secretase The project has applied for five patents, four of which have obtained patent certificates.

This research achievement was made by an innovative research team led by Academician Sun, State Key Laboratory of Phytochemistry and Sustainable Utilization of Plant Resources in Western China, Kunming Institute of Botany, Chinese Academy of Sciences, after nearly 65,438+00 years of hard work. This research was supported by the National Natural Science Foundation of China, China Academy of Sciences and Yunnan Natural Science Foundation. At present, 35 research papers have been published in many internationally renowned magazines, and 34 papers have been included in SCI. Eight new compounds were listed as "research hotspots" by the internationally renowned organic biochemistry review magazine "Natural Products Report". In addition, in 2008, the journal also published a review article "Triterpenoids in Schisandraceae".

According to reports, this study will not only look for lead compounds with higher activity and lower toxic and side effects, but also focus on Schisandraceae plants and their important functions and chemical basis in neurodegenerative diseases and the targets of related diseases. This research not only has important academic value, but also provides a scientific basis for the research and development of new drugs with independent intellectual property rights in China, which is of great significance for the rational development and utilization of this unique plant resource in China and the promotion of economic development in poverty-stricken areas of ethnic minorities. At the same time, it will further enrich and promote the content and development of triterpenoids in chemistry, and maintain its international leading position in this field, which is also one of the real original contributions of China scholars in the world terpenoid chemistry field.

Schisandra chinensis is a famous traditional Chinese medicine in China, which has the function of calming the nerves and calming the mind, but the relationship between its nature and taste and the chemical basis of its function have not been deeply studied and clarified so far. According to Sun, Schisandraceae is divided into two genera: Schisandra and Schisandra. There are about 50 species in the world, distributed in East Asia, Southeast Asia and southern North America. There are about 30 species belonging to two genera in China, which are mainly produced in southwest and central south. Since the 1960s, scholars at home and abroad have been very active in studying the chemical constituents of this family, and accumulated a large number of biological activity data.

According to reports, in the future, researchers will use modern separation and analysis technology to conduct a comprehensive and systematic study on the famous Chinese medicine Schisandra chinensis and Schisandraceae 12, in order to find more compounds with new skeletons and new structures, and provide a solid chemical material basis for in-depth discussion on the biological activities of plants in this family in neurodegenerative diseases. At the same time, we will cooperate with China Academy of Sciences, Shanghai Institute of Materia Medica, Kunming Institute of Zoology, Shanghai Jiaotong University School of Medicine and other domestic units engaged in pharmaceutical research, and screen the related parts and monomer compounds isolated from 12 Schisandraceae plants for cytotoxicity, anti-HIV, HBV and HCA, and in vitro antioxidant activity, so as to lay a solid foundation for clarifying the pharmacological effects of Schisandraceae plants and finding drug lead compounds or drug candidate structures with important biological activities.

Science Times (2008- 10-22 A 1 Highlights)