期刊
CHEMICAL BIOLOGY & DRUG DESIGN
卷 88, 期 2, 页码 293-301出版社
WILEY-BLACKWELL
DOI: 10.1111/cbdd.12756
关键词
Ardisia gigantifolia; isolation and structure identification; resorcinols; anti-TB activity; Mycobacterium tuberculosis H37RV; structural modification
资金
- Hong Kong Baptist University (HKBU) [RC-IRMS/12-13/03]
- Natural Science Foundation of China [21402166]
- NIH [3U01TW001015-10S1, 2U01TW001015-11A1]
- NSF
- Foreign Agricultural Service of the USDA
- Shenzhen strategic emerging industry development project [CXZZ20150601110000604, ZDSYS201506031617582, Shenfagai (2013) 180]
Tuberculosis (TB) is a highly contagious disease mainly caused by Mycobacterium tuberculosis H37RV. 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 H37RV. Resorcinols 1 and 2 exhibited anti-TB activity with MIC values at 34.4 and 79.2 mu M in MABA assay, respectively, and 91.7 and 168.3 mu M 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 mu M in MABA assay and 100.2 mu M 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.
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