1. Phytochemical investigations on the plant distributed in southwest of China

Natural products are the largest pool of chemically diverse and physiologically interesting metabolites. There are rich plant resources in southwest of China. With an aim to find structurally interesting and bioactive natural products, intense chemical and bioactive study on the plants distributed in southwest of China has been conducted over the past five years in our laboratory. Forty plants mainly involved in Fern,Salvia,and Viburnum specieshave been studied thoroughly.

1.1 Phytochemical investigations on Fern

1.2. Phytochemical investigations on Salvia plants

2. Bioactivity

By collaborations with research group worldwide,broad bioactivity screening on the isolated natural products has led to the discovery of hundreds of compounds with various promising bioactivity, such as antitumor, anti-HIV, anti-inflamatiory, anti-HIV activities, hypoglycemic effects and so on. Among these bioactive compounds, two classes of lead compounds are especially promising, that is natural inhibitors of 11ß-HSD1 and differentiation inducers in treating leukemia.

2.1. Inhibitors of 11ß-HSD1*

2.2 Differentiation inducers in treating leukemia*

3. Natural Medicinal Chemistry

Natural products have long been excellent source of novel active agents that may serve as the leads and scaffolds for elaboration into efficacious drugs. According to a review of New Chemical Entities (NCE) from 1940 to 2006, approximately 65% of drugs were delivered from natural products, or mimicked them in one form or another. Through the medicinal chemistry approach, natural products can be modified synthetically to improve their pharmacological profiles.

During the past five years, the modification, structure-activity relationship (SAR), and drug discovery from natural product have been studied. Erioclyxin B, taxoids,cheliensisin A,abietane andso on were selected as starting material because of their potent bioactivity, unique structure or high content in plants.

3.1. Synthesis and structure-activity relationship of eriocalyxing B and its derivatives

3.2. Synthesis, cytotoxic activity, and SAR analysis of the derivatives of taxchinin A

3.3 Development of novel conformation-constrained cytotoxic derivatives of cheliensisin A by embedment of small heterocycles