Anti-tubercular agents from Ammannia baccifera (Linn.)

作者：Upadhyay Harish C; Thakur Jay Prakash; Saikia Dharmendra; Srivastava Santosh K^*

来源：Medicinal Chemistry Research, 2013, 22(1): 16-21.

DOI：10.1007/s00044-012-9998-9

• A. baccifera
• Lythraceae
• Anti-tubercular
• SAR
• MDR
• Tetralone

Ammannia baccifera is an important component of various traditional Chinese herbal formulations. The samples of A. baccifera were extracted with methanol and the methanolic extract was successively fractionated with n-hexane, chloroform and n-butanol. The serial chromatographic separation of chloroform and n-butanol fractions resulted in the isolation and characterization of betulinic acid (1), 4-hydroxy-alpha-tetralone (2), tetralone-4-O-beta-D-glucopyranoside (3) and ellagic acid (4). Further, the compound 2 was chemically modified into its five semi-synthetic acyl and aryl derivatives (2A-2E) namely; 4-O-m-anisoyl-alpha-tetralone (2A), 4-O-benzoyl-alpha-tetralone (2B), 4-O-palmitoyl-alpha-tetralone (2C), 4-O-(3,4,5-trimethoxybenzoyl)-alpha-tetralone (2D) and 4-O-myricitoyl-alpha-tetralone (2E). The tetralone group compounds 2, 3 and semi-synthetic derivatives 2A-2E were evaluated for their in vitro anti-tubercular activity against Mycobacterium tuberculosis H37Rv by BACTEC-460 radiometric susceptibility assay. The compounds 2 and 2E have shown significant anti-tubercular activity (MIC 50 mu g/ml) while 2B was moderate active (MIC 100 mu g/ml) against the pathogen. The results of SAR study indicated that substitutions in alpha hydroxyl group of 4-hydroxy-alpha-tetralone either retards or have no increasement in in vitro anti-tubercular potential.

• 出版日期2013-1
• 单位河北医科大学