Abstract
In this paper, eight new galaxamide analogues (Z-1~Z-8) were synthesized and evaluated for their cytotoxic activities against five cancer cell lines, MCF-7, MD-MBA-231, HepG2, Hela, and A549, using MTT assays. The modified analogue Z-6 displayed broad spectrum cytotoxic activity toward each tested cell line with IC50 values of 1.65 ± 0.30 (MCF-7), 2.91 ± 0.17 (HepG2), 4.59 ± 0.27 (MD-MBA-231), 5.69 ± 0.37 (Hela), and 5.96 ± 0.41 (A549) μg/mL, respectively. The galaxamides Z-3 and Z-6 induced concentration-dependent apoptosis of the MCF-7 cells after 72 h as evaluated by the flow cytometry experiment. The results showed that these compounds could induce MCF-7 cell apoptosis by arresting the G0/G1 phase of the cell cycle and finally achieving the effect of inhibiting the proliferation of MCF-7 cells.
Highlights
IntroductionCyclopeptides mainly isolated from various marine species, which exhibited antitumor, [1,2,3] antiviral, [4] anti-inflammatory [5,6] and antibacterial [7,8,9] activities
[11] To enhance the antitumor activity of cyclopeptides, they were always modified by changing the configurations of amino acid residues
5 μL of Annexin V-fluorescein isothiocyanate (FITC) and 5 μL of propidium iodide (PI) were added for dual staining of the cells for analysis by FACS flow cytometry
Summary
Cyclopeptides mainly isolated from various marine species, which exhibited antitumor, [1,2,3] antiviral, [4] anti-inflammatory [5,6] and antibacterial [7,8,9] activities. Previous phytochemical investigation on the alga of Galaxaura filamentosa had led to the isolation of a novel cyclic pentapeptide, galaxamide (Figure 1) It was composed of five L-leucines including two N-methylated ones, which showed significant antitumor activities against GRC-1 and HepG2 cell lines. [13] In the preliminary work, the galaxamide analogues had been synthesized by replacing one of the leucines with penylalanine and changing the configuration of amino acids, which showed potential antitumor activities. A great majority of the synthesized compounds showed strong antitumor activities. They showed weak inhibitory effects on the strong antitumor activities On thethe other they showed weak effectscancer on the non-neoplastic cells.
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