1. Synthesis and biological evaluation of novel curcuminoid derivatives.
- Author
-
Cao YK, Li HJ, Song ZF, Li Y, and Huai QY
- Subjects
- Anti-Bacterial Agents pharmacology, Antineoplastic Agents pharmacology, Antioxidants pharmacology, Cell Line, Tumor, Cell Proliferation drug effects, Escherichia classification, Escherichia drug effects, Hep G2 Cells, Humans, Staphylococcus classification, Staphylococcus drug effects, Anti-Bacterial Agents chemical synthesis, Antineoplastic Agents chemical synthesis, Antioxidants chemical synthesis, Curcumin analogs & derivatives
- Abstract
Curcuminoids have been reported to possess multiple bioactivities, such as antioxidant, anticancer and anti-inflammatory properties. Three novel series of curcuminoid derivatives (11a-h, 15a-h and 19a-d) with enhanced bioactivity have been synthesized. Among the synthesized compounds, 11b exhibited the most significant activity with an MIC of 0.5 µM /mL against selected medically important Gram-positive cocci (S. aureus and S. viridans) and Gram-negative bacilli (E. coli and E. cloacae). The derivatives exhibited remarkable results in an antioxidant test with an IC50 2.4- to 9.3-folder smaller than curcuminoids. With respect to antiproliferative activity against Hep-G2, LX-2, SMMC7221 and MDA-MB-231, the derivatives exhibited an effect stronger than curcuminoids with an IC50 ranging from 0.18 to 4.25 µM.
- Published
- 2014
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