Chemical constituents of Plectranthus amboinicus and the synthetic analogs possessing anti-inflammatory activity
Chen, Y.-S.; Yu, H.-M.; Shie, J.-J.; Cheng, T.-J.R.; Wu, C.-Y.; Fang, J.-M.; Wong, C.-H. (2014). Chemical constituents of Plectranthus amboinicus and the synthetic analogs possessing anti-inflammatory activity. Bioorg. Med. Chem. 22(5): 1766-1772. https://dx.doi.org/10.1016/j.bmc.2014.01.009
In: Bioorganic & Medicinal Chemistry. Elsevier: Amsterdam. ISSN 0968-0896; e-ISSN 1464-3391, more
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| Author keywords |
Plectranthus amboinicus; Anti-inflammation; Rosmarinic acid; Thymoquinone; 2-Alkylidenyl-4-cyclopentene-1,3-diones |
| Authors | | Top |
- Chen, Y.-S.
- Yu, H.-M.
- Shie, J.-J.
- Cheng, T.-J.R.
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- Wu, C.-Y.
- Fang, J.-M.
- Wong, C.-H.
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| Abstract |
This study demonstrates that compounds 1–4 from an extract of Plectranthus amboinicus inhibit the binding of AP-1 to its consensus DNA sequence. Thymoquinone (5) was further identified as a nonpolar ingredient from the hexane extract of P. amboinicus to suppress the expression of lipopolysaccharide-induced tumor necrosis factor-alpha (TNF-α). We then synthesized 2-alkylidenyl-4-cyclopentene-1,3-diones as the designed biomimetics of thymoquinone, and found that compounds 8a, 8b and 8dwere more potent TNF-α inhibitors. |
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