INDONESIAN JOURNAL OF PHARMACY
Vol 19 No 2, 2008

Protein kinase inhibitors from Indonesian Sponge Axynissa sp.

Triana Hertiani (Institut für Pharmazeutische Biologie and Biotechnologie, Henrich-Heine Universität Düsseldorf, Universitätsstrasse 1 Geb. 26.23, 40225 Düsseldorf, Germany Department of Biological Pharmacy, Faculty of Pharmacy, Universitas Gadjah Mada. Yogyakarta, I)
Ru Angelie Edrada-Ebel (Strathclyde Institute of Pharmacy and Biomedical Science, University of Strathclyde, The John Arbuthnott Building, 27 Taylor Street, Glasgow G4 0NR, United Kingdom)
Michael Kubbutat (ProQinase GMBH, Breisacher Str. 117, 79106 Freiburg im Breisgau, Germany)
rob W.M. van Soest (Institute for Systematics and Ecology, University of Amsterdam, P.O. Box 94766, 1090 GT Amsterdam, The Netherlands)
peter Proksch (Institut für Pharmazeutische Biologie and Biotechnologie, Henrich-Heine Universität Düsseldorf, Universitätsstrasse 1 Geb. 26.23, 40225 Düsseldorf, Germany)



Article Info

Publish Date
01 Apr 2008

Abstract

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 isolate the chemically most interesting substances. Structure identification of active compounds was performed by using NMR spectroscopy and massspectrometry methods.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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Journal Info

Abbrev

3

Publisher

Subject

Medicine & Pharmacology

Description

Indonesian Journal of Pharmacy (ISSN-e: 2338-9486, ISSN-p: 2338-9427), formerly Majalah Farmasi Indonesia (ISSN: 0126-1037). The journal had been established in 1972, and online publication was begun in 2008. Since 2012, the journal has been published in English by Faculty of Pharmacy Universitas ...