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The Family Moraceae and the Genus Rhododendron as Important Source of Drug Discovery and Development
发布时间:2015-11-01 来源:

Ai-Jun Hou
School of Pharmacy, Fudan University, 826 Zhang Heng Road, Shanghai 201203, China
Moraceae is a large family, including some important groups such as Morus, Artocarpus, Ficus, and Cudrania. The moraceous plants are of important economic and medicinal values and are rich in prenylated phenolics with structural and biological diversity.
A series of new compounds were isolated from some moraceous plants by our group, including some new skeletons, novel 2-arylbenzofuran dimers, bioflavonoids, and Diels-Alder adducts. It is more important that some compounds promoted adipogenesis and induced up-regulation of the expression of glucose transporter 4 (GLUT4) and that some compounds showed inhibition on pancreatic lipase (PL) and protein tyrosine phosphatase 1B (PTP1B). This will be of significance for exploring new lead compounds against diabetes and obesity. Furthermore, the antitumor constituents of Cudrania tricuspidata were explored, an antitumor traditional Chinese medicine. Mechanism of the active compound was investigated. Based on the investigations on C. tricuspidata, a new antitumor drug candidate is undergoing preclinical studies. In addition, the total syntheses of some bioactive isoprenylated flavonoids from the family Moraceae were also completed.
The genus Rhododendron (Ericaceae) comprises about 1000 species mainly distributed in East and Southeast Asia and China is considered to be the Rhododendron distribution center in the world with 571 species. Many Rhododendron plants have been used as folk medicine in China and some other countries. Recently, some enantiomeric pairs of meroterpenoids and novel grayanane diterpenoids with PTP1B inhibition were discovered by our group.


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