Journal
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
Volume 74, Issue -, Pages -Publisher
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmcl.2022.128924
Keywords
Mogrol; Anti -proliferative; Anti-inflammatory; Indole; ?-unsaturated ketone
Categories
Funding
- National Natural Science Foundation of China [U20A2004]
- Basic research fund of Guangxi Academy of Sciences [CQZ-C-1901]
- Key -Area Research and Develop- ment Program of Guangdong Province [2020B1111110003]
- Guilin Scientific and Technological Project [20190210-3]
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A class of novel mogrol derivatives has been synthesized and found to exhibit promising activity in anti-inflammatory and anti-proliferative effects. One derivative showed superior inhibitory activity against cell secretions and antioxidants through a specific pathway, while other derivatives displayed broad-spectrum activity in suppressing different types of lung cancer cell proliferation.
A class of novel mogrol derivatives modified on A ring were synthesized. The screening result showed that indole-fused derivatives exhibited lower toxicity and better anti-inflammatory activity in LPS-induced RAW 264.7 cells model than mogrol and other compounds. Derivative B8 exerted superior inhibitory result of NO production (IC50 = 5.05 mu M) and inhibitory ability of TNF-alpha and IL-6 secretion to mogrol through iNOS/NF--KB pathway. Besides, the CCK8 assay was performed to evaluate their anti-proliferative activity against non-small cell lung cancer including A549, NCI-H460, H1299 and H1975 cells. Compared with mogrol, compound B8 showed moderate anti-proliferative activities against A549 and H1975 cells, while derivatives bearing alpha, beta-unsaturated ketone scaffold displayed broad-spectrum growth inhibition against four cell lines. Among them, compound A9 showed 12-fold higher activity than mogrol against H1299 and H1975 cells. The suppressive effect on expression level of p-p65 might account for the compound A9-induced growth inhibition and cell cycle arrest at G1 phase.
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