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A Flow Cytometry-Based Cell Surface Protein Binding Assay for Assessing Selectivity and Specificity of an Anticancer Aptamer

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Cytotoxic aaptamines from Malaysian Aaptos aaptos.

Khozirah Shaari¹, Kee Cheng Ling, Zalilawati Mat Rashid

¹Laboratory of Natural Products, Institute of Bioscience, University Putra Malaysia, 43400 Serdang, Selangor, Malaysia. khozirah@yahoo.com.my

|April 17, 2009

Summary

Marine sponge Aaptos aaptos yielded new cytotoxic alkaloids. Researchers identified two novel aaptamine derivatives, 3-(phenethylamino)demethyl(oxy)aaptamine and 3-(isopentylamino)demethyl(oxy)aaptamine, alongside known aaptamine, highlighting their potential in cancer research.

Keywords:

Aaptos aaptos Marine sponge aaptaminoids alkaloids cytotoxicity

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Area of Science:

Marine Natural Products Chemistry
Pharmacology
Organic Chemistry

Background:

Marine sponges are a rich source of bioactive compounds.
The sponge Aaptos aaptos has demonstrated preliminary cytotoxic activity.
Bioassay-guided isolation is crucial for identifying active natural products.

Purpose of the Study:

To isolate and identify cytotoxic compounds from Aaptos aaptos.
To characterize novel alkaloid derivatives.
To evaluate the cytotoxic potential of isolated alkaloids against cancer cell lines.

Main Methods:

Preliminary cytotoxic screening of Aaptos aaptos extract.
Bioassay-guided fractionation using chloroform extraction.
Structure elucidation using Nuclear Magnetic Resonance (NMR) and mass spectroscopy.
Cytotoxicity evaluation against CEM-SS cells.

Main Results:

Aaptos aaptos extract exhibited significant cytotoxic activity.
Two new aaptamine derivatives, 3-(phenethylamino)demethyl(oxy)aaptamine and 3-(isopentylamino)demethyl(oxy)aaptamine, were isolated.
The known alkaloid aaptamine was also identified.
The cytotoxic activities of all three isolated alkaloids were assessed.

Conclusions:

Aaptos aaptos is a source of novel cytotoxic alkaloids.
The identified aaptamine derivatives possess significant cytotoxic properties.
Further investigation into these compounds may lead to new therapeutic agents.