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All Journal INDONESIAN JOURNAL OF PHARMACY
rob W.M. van Soest
Institute for Systematics and Ecology, University of Amsterdam, P.O. Box 94766, 1090 GT Amsterdam, The Netherlands
Medicine & Pharmacology

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Protein kinase inhibitors from Indonesian Sponge Axynissa sp. Triana Hertiani; Ru Angelie Edrada-Ebel; Michael Kubbutat; rob W.M. van Soest; peter Proksch
Indonesian Journal of Pharmacy Vol 19 No 2, 2008
Publisher : Faculty of Pharmacy Universitas Gadjah Mada, Yogyakarta, Skip Utara, 55281, Indonesia

Show Abstract | Download Original | Original Source | Check in Google Scholar | Full PDF (221.985 KB) | DOI: 10.14499/indonesianjpharm0iss0pp78-85

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.
Chemical investigation on Pseudoceratina purpurea collected from Banyuwangi Indonesia Triana Hertiani; RuAngelie Edrada; Rob W.M. Van Soest; Werner E.G. Muller; Sudarsono .; Peter Proksch
Indonesian Journal of Pharmacy Vol 20 No 1, 2009
Publisher : Faculty of Pharmacy Universitas Gadjah Mada, Yogyakarta, Skip Utara, 55281, Indonesia

Show Abstract | Download Original | Original Source | Check in Google Scholar | Full PDF (448.691 KB) | DOI: 10.14499/indonesianjpharm0iss0pp17-26

Abstract

Chemical investigation on marine sponge Pseudoceratina purpurea collected from Banyuwangi, Indonesia has been performed. This study was aimed to isolate and to identify structures of the sponge secondary metabolites as well as to test their cytotoxicity activity on mouse lymphoma cell line L5178Y.Isolation procedure was performed by using different chromatography techniques. NMR spectroscopy and mass spectrometry methods were used to identify the compounds chemical structures. Cytotoxicity of the isolates was tested on mouse lymphoma cell line L5178Y by using the microculture tetrazolium (MTT) assay.This study yielded five known tyrosine-derived alkaloids, two of which, aplysamine-2 (1) and aeroplysinin-1 (2) showed growth inhibition of mouse lymphoma cell line L5178Y with IC50 value of 1.7 mg/mL and 0.57 mg/mL, respectively.Key words: Pseudoceratina purpurea, sponge, alkaloids.
Co-Authors Michael Kubbutat peter Proksch Peter Proksch Ru Angelie Edrada-Ebel RuAngelie Edrada Sudarsono . Triana Hertiani Werner E.G. Muller