Details

Autor(en) / Beteiligte

• Dao, Trong Tuan
• Le, Thi Van
• Nguyen, Phi Hung
• Thuong, Phuong Thien
• Minh, Pham Thi
• Woo, Eun-Rhan
• Lee, Kwang Youl
• Oh, Won Keun

Titel

SIRT1 inhibitory diterpenoids from the Vietnamese medicinal plant Croton tonkinensis

Ist Teil von

• Planta medica, 2010-07, Vol.76 (10), p.1011-1014

Ort / Verlag

Germany

Erscheinungsjahr

2010

Quelle

MEDLINE

Beschreibungen/Notizen

• Silent information regulator two ortholog 1 (SIRT1) is a member of the sirtuin deacetylase family of enzymes that removes acetyl groups from the lysine residues in histones and other proteins. It has been suggested that SIRT1 inhibitors might be beneficial in the treatment of cancer and neurodegenerative diseases. Bioassay-guided fractionation of the MeOH extract of the leaves of CROTON TONKINENSIS resulted in the isolation of a new ENT-kaurane diterpenoid (1) along with 11 known compounds (2- 12). The structure of the new compound 1 was determined to be ENT-11 alpha-acetoxy-7 beta-hydroxykaur-16-en-15-one based on spectroscopic analyses. Compounds 3, 4, 6- 9, 11, and 12 exhibited SIRT1 inhibitory activity in an IN VITRO assay, with IC (50) values ranging from 16.08 +/- 0.11 to 44.34 +/- 2.32 microM. This is the first report showing the potential of ENT-kaurane diterpenoids as a new class of natural SIRT1 inhibitors.