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Syntheses, anti-cancer activity of CO-releasing molecules with targeting galactose receptor


CO-releasing molecules (CORMs ) containing cobalt have many bioactivities,but most of them do not dissolve in water and have no selectivity to tissue and organs. On the basis of the specific recognition of galactose or sialic acid to its receptor, a series of CORMs based on carbohydrates were synthesized and evaluated. The testing results show all the complexes displayed anticancer activity. Among them, the effects of the complexes of galactose (1), GalNAc (8) and sialic acid (10) were very distinct. Complex 1 displayed higher activity against HeLa, HePG2, MCF-7 and HT-29 cells proliferation than cis-platin (DDP), and its selectivity was far much better than DDP compared with normal cell W138. Furthermore, the uptakes of complexes 1, 8 and 10 by HePG2, HT-29, A549 and RAW264.7 cell lines were studied. The uptake ratio of each cell line for complex 1 was different, the order of uptake ratio in four cell lines was HePG2 > HT-29 > RAW264.7 > A549. The HePG2 cells absorbed beyond 60% complex 1 after incubation for 8 h, while A549 only 27.8%. For complex 8, the uptake trend was similar to that of complex 1 absorbed by all the four cancer cells, but the uptake rate was lower. However, differently, complex 10 was absorbed heavily by macrophage RAW264.7, followed by HePG2; after 8h incubation later, the uptake rate of RAW264.7 was over 50%. In addition, the mechanism of action was explored, the results show the complexes inhibited cell cycle arrest at G2/M phase; and complex 1 up-regulated the expression levels of caspase-3 and Bax, down-regulated the Bcl-2 expression, by which giving rise to HePG2 cell apoptosis.

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Publication details

The article was received on 07 Aug 2018, accepted on 09 Oct 2018 and first published on 09 Oct 2018

Article type: Paper
DOI: 10.1039/C8OB01921E
Citation: Org. Biomol. Chem., 2018, Accepted Manuscript
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    Syntheses, anti-cancer activity of CO-releasing molecules with targeting galactose receptor

    J. li, Q. Y. zhao, J. zhang, Q. zhang, Z. bai, D. he, Z. wang, Y. chen and B. liu, Org. Biomol. Chem., 2018, Accepted Manuscript , DOI: 10.1039/C8OB01921E

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