Bioassay-Guided Isolation and Structural Modification of the Anti-TB Resorcinols fromArdisia gigantifolia
| Autor: | Nguyen Van Hung, Hongjie Zhang, Nguyen Manh Cuong, Xun Song, Ming-Hua Qiu, Yi Fu Guan, Scott G. Franzblau, Djaja D. Soejarto, Zhendan He, Sheng Hong Li, Shi-Hong Luo, Bao Jie Wang, Harry H. S. Fong |
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| Rok vydání: | 2016 |
| Předmět: |
0301 basic medicine
Spectrometry Mass Electrospray Ionization Magnetic Resonance Spectroscopy Tuberculosis Stereochemistry 030106 microbiology Antitubercular Agents Microbial Sensitivity Tests Resorcinol 01 natural sciences Biochemistry Ardisia Mycobacterium tuberculosis 03 medical and health sciences chemistry.chemical_compound Drug Discovery medicine Bioassay Pharmacology biology Plant Extracts 010405 organic chemistry Organic Chemistry Resorcinols biology.organism_classification medicine.disease 0104 chemical sciences chemistry Mic values Mycobacterium tuberculosis H37Rv Molecular Medicine Biological Assay Ardisia gigantifolia |
| Zdroj: | Chemical Biology & Drug Design. 88:293-301 |
| ISSN: | 1747-0277 |
| Popis: | Tuberculosis (TB) is a highly contagious disease mainly caused by Mycobacterium tuberculosis H37 RV . Antitubercular (anti-TB) bioassay-guided isolation of the CHCl3 extract of the leaves and stems of the medicinal plant Ardisia gigantifolia led to the isolation of two anti-TB 5-alkylresorcinols, 5-(8Z-heptadecenyl) resorcinol (1) and 5-(8Z-pentadecenyl) resorcinol (2). We further synthesized 15 derivatives based on these two natural products. These compounds (natural and synthetic) were evaluated for their anti-TB activity against Mycobacterium tuberculosis H37 RV . Resorcinols 1 and 2 exhibited anti-TB activity with MIC values at 34.4 and 79.2 μm in MABA assay, respectively, and 91.7 and 168.3 μm in LORA assay, respectively. Among these derivatives, compound 8 was found to show improved anti-TB activity than its synthetic precursor (2) with MIC values at 42.0 μm in MABA assay and 100.2 μm in LORA assay. The active compounds should be regarded as new hits for further study as a novel class of anti-TB agents. The distinct structure-activity correlations of the parent compound were elucidated based on these derivatives. |
| Databáze: | OpenAIRE |
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