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Inhibitor protein kinese dari spons Indonesia Axynissa sp. (Protein kinase inhibitors from Indonesian sponge Axynissa sp)
A research about inhibitory activity on various cancer related protein kinases of several marine sponges collected in Indonesia was performed. This study aims were to isolate and to identify structures of biologically active sponge metabolites.
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 isolated the chemically most interesting substance. Structure identification of active compounds was performed by using NMR spectroscopy and mass spectrometry methods.
This study showed that only axynisca sp. Fractions were found active in protein kinase inhibitory assay. Two bisabolance type sesquiterpenoids (+)- curcuphenol (1) and (+) – curcudiol (2) were identified as active compounds from the sponge. Compound 1 showed SRC protein kinase inhibition with an IC50 value of 7,8 μg/mL while 2 inhibited FAK with and IC50 value 0f 9,2 μg/mL.
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