Protein kinase inhibitors from Indonesian Sponge Axynissa sp.
A combination of a chemically-and biologically driven approach for drug discovery was employed. Sponge extracts were tested by protein kinase inhibitory assay by in vitro method in parallel to the usage of TLC, and HPLC coupled to UV spectrophotometry and mass spectrometry to isolate the chemically most interesting substances. Structure identification of active compounds was performed by using NMR spectroscopy and mass
This study showed that only Axynissa sp. fractions were found active in protein kinase inhibitory assay. Two bisabolene type sesquiterpenoids, (+)- curcuphenol (1) and (+)-curcudiol (2) were identified as active compounds from the sponge. Compound 1 showed SRC protein kinase inhibition with an IC50value of 7.8 μg/mL while 2 inhibited FAK with an IC50 value of 9.2 μg/mL.
Key words: protein kinase inhibitor, Axynissa sp.
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