Related Experiment Video
Updated: Sep 9, 2025
11:14
Anticancer Metal Complexes: Synthesis and Cytotoxicity Evaluation by the MTT Assay
Published on: November 10, 2013
57.9K
Acetylated monosaccharide functionalized co-ligand based strong anticancer Pt(II) complexes: Synthesis
Na Wang1, Ning Yuan2, Zhimin Lv1
1Inner Mongolia University, Research Center for Glycochemistry of Characteristic Medicinal Resources, Department of Chemistry and Chemical Engineering, Hohhot, People's Republic of China.
Journal of Inorganic Biochemistry
|September 4, 2025
Summary
Novel platinum(II) complexes with sugar-modified ligands show potent anticancer activity, especially against cisplatin-resistant cancer cells. These complexes target GLUT1, offering a promising new therapeutic strategy with reduced toxicity to normal cells.
Area of Science:
- Organometallic Chemistry
- Medicinal Chemistry
- Cancer Biology
Background:
- Platinum(II) complexes are established anticancer agents.
- Development of novel platinum(II) complexes is crucial to overcome drug resistance and improve therapeutic index.
- Salicylaldimine ligands offer a versatile scaffold for designing platinum(II) complexes.
Purpose of the Study:
- To synthesize and characterize novel Pt(II) complexes incorporating monosaccharide-functionalized pyridine co-ligands.
- To evaluate the in vitro anticancer potency of these complexes against various human cancer cell lines, including cisplatin-resistant ones.
- To elucidate the mechanism of action, including GLUT1 dependence and apoptotic pathways.
Main Methods:
- Synthesis of Pt(II) complexes (C1-C12) via a two-step reaction involving silver(I) tetrafluoroborate and acetylated β-d-glucose conjugated pyridine.
- In vitro anticancer activity assessment using gastric (MKN 45), colon (RPMI 4788), and lung (A549) cancer cell lines.
- Evaluation in cisplatin-resistant A549/DDP cells and normal gastric (GES) and colonic (NCM 460) epithelial cells.
- GLUT1 inhibitor (quercetin) studies, cell morphology analysis (bright field, Hoechst 33342 staining), flow cytometry, and Western blot analysis (PARP, caspase 3, BCL-2).
Main Results:
- Complexes C9 and C12 demonstrated significant in vitro anticancer potency.
- These complexes exhibited superior efficacy in cisplatin-resistant lung cancer cells and lower toxicity in normal cells.
- GLUT1-dependent anticancer activity was observed for C9 and C12, unlike the control oxaliplatin.
- Mechanistic studies confirmed induction of apoptosis via PARP, caspase 3, and BCL-2 pathways.
Conclusions:
- The novel Pt(II) complexes with sugar-modified ligands show promising anticancer properties, particularly against resistant cancer types.
- The observed GLUT1-dependent mechanism suggests a targeted approach for cancer therapy.
- These findings highlight the potential of these complexes as next-generation platinum-based anticancer drugs with an improved safety profile.
Keywords:
ApoptosisFluorescenceGLUT1 inhibitionPt(II) complexesSugar conjugated Pt(II) complexesTumor spheres formationMore Related Videos
Related Concept Videos
00:43Complexometric Titration: Ligands
1.1K
Different monodentate and polydentate ligands are used as complexing agents in complexometric titration reactions. The formation of complexes by mono- and bidentate ligands involves two or more intermediate steps, limiting their use as complexing agents. In comparison, polydentate ligands can form complexes with metal ions in a single-step process, facilitating sharper end points. This means polydentate ligands, such as amino carboxylic acid derivatives, are most commonly employed in...
1.1K
01:22EDTA: Chemistry and Properties
2.2K
Polydentate ligands are most widely used in complexometric titrations because they form more stable complexes with the metal ions than mono- or bidentate ligands due to the chelate effect. Examples of polydentate ligands are ethylenediaminetetraacetic acid (EDTA), crown ethers, and cryptands. The most important feature of optimal polydentate ligands is the ability to form 1:1 complexes in a single-step process. Amino carboxylic acid derivatives are frequently used as complexing agents. EDTA is...
2.2K
02:52Stereoisomerism
12.4K
Isomerism in Complexes
Isomers are different chemical species that have the same chemical formula.
Transition metal complexes often exist as geometric isomers, in which the same atoms are connected through the same types of bonds but with differences in their orientation in space. Coordination complexes with two different ligands in the cis and trans positions from a ligand of interest form isomers. For example, the octahedral [Co(NH3)4Cl2]+ ion has two isomers (Figure 1) In the cis...
Isomers are different chemical species that have the same chemical formula.
Transition metal complexes often exist as geometric isomers, in which the same atoms are connected through the same types of bonds but with differences in their orientation in space. Coordination complexes with two different ligands in the cis and trans positions from a ligand of interest form isomers. For example, the octahedral [Co(NH3)4Cl2]+ ion has two isomers (Figure 1) In the cis...
12.4K