Benzamides and quinazolines from a mangrove actinomycetes Streptomyces sp. (No. 061316) and their inhibiting caspase-3 catalytic activity in vitro |
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| Authors: | Chen Guodong Gao Hao Tang Jinshan Huang Yuanfan Chen Ying Wang Ying Zhao Huinan Lin Haipeng Xie Qingyi Hong Kui Li Jia Yao Xinsheng |
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| Institution: | Institute of Traditional Chinese Medicine and Natural Products, College of Pharmacy/Guangdong Province Key Laboratory of Pharmacodynamic Constituents of TCM and New Drugs Research, Jinan University, Guangzhou, People’s Republic of China. |
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| Abstract: | One new benzamide, 3-hydroxyl-2-N-iso-butyryl-anthranilamide (1), together with two known benzamides (2, 3) and three known quinazolines (4-6), was isolated from a mangrove actinomycetes Streptomyces sp. (No. 061316), which displayed inhibiting Caspase-3 activity in vitro. The structure of 1 was elucidated by electrospray ionization (ESI)-MS, NMR spectroscopies and X-ray crystal diffraction. After evaluation of all compounds for their inhibitory effect on Caspase-3 in vitro, 3-hydroxyl-anthranilamide (2) and 8-hydroxyl-2,4-dioxoquinazoline (6) showed activity against Caspase-3 with IC(50) values of 32 and 36 μM, respectively. |
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