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Synthesis and In Vitro Antitumor Activity of Two Mixed-Ligand Oxovanadium(IV) Complexes of Schiff Base and Phenanthroline.

Zhang Y, Wang X, Fang W, Cai X, Chu F, Liao X, Lu J - Bioinorg Chem Appl (2013)

Bottom Line: Two oxovanadium(IV) complexes of [VO(msatsc)(phen)], (1) (msatsc = methoxylsalicylaldehyde thiosemicarbazone, phen = phenanthroline) and its novel derivative [VO (4-chlorosatsc)(phen)], (2) (4-chlorosatsc = 4-chlorosalicylaldehyde thiosemicarbazone), have been synthesized and characterized by elemental analysis, IR, ES-MS, (1)H NMR, and magnetic susceptibility measurements.Both 1 and 2 decreased significantly the ΔΨm, causing the depolarization of the mitochondrial membrane.Complex 2 showed greater antitumor efficiency than that of complex 1.

View Article: PubMed Central - PubMed

Affiliation: Department of Biology, School of Basic Courses, Guangdong Pharmaceutical University, Guangzhou, Guangdong 510006, China.

ABSTRACT
Two oxovanadium(IV) complexes of [VO(msatsc)(phen)], (1) (msatsc = methoxylsalicylaldehyde thiosemicarbazone, phen = phenanthroline) and its novel derivative [VO (4-chlorosatsc)(phen)], (2) (4-chlorosatsc = 4-chlorosalicylaldehyde thiosemicarbazone), have been synthesized and characterized by elemental analysis, IR, ES-MS, (1)H NMR, and magnetic susceptibility measurements. Their antitumor effects on BEL-7402, HUH-7, and HepG2 cells were studied by MTT assay. The antitumor biological mechanism of these two complexes was studied in BEL-7402 cells by cell cycle analysis, Hoechst 33342 staining, Annexin V-FITC/PI assay, and detection of mitochondrial membrane potential (ΔΨm). The results showed that the growth of cancer cells was inhibited significantly, and complexes 1 and 2 mainly caused in BEL-7402 cells G0/G1 cell cycle arrest and induced apoptosis. Both 1 and 2 decreased significantly the ΔΨm, causing the depolarization of the mitochondrial membrane. Complex 2 showed greater antitumor efficiency than that of complex 1.

No MeSH data available.


Related in: MedlinePlus

Distribution map of mitochondrial membrane potential with complex 1 (bottom) and complex 2 (top) for 48 h.
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fig11: Distribution map of mitochondrial membrane potential with complex 1 (bottom) and complex 2 (top) for 48 h.

Mentions: As shown in Figure 11 and Table 4 upon increasing the concentrations of complexes 1 and 2 (60, 90, and 135 μM), the mean value of green fluorescence intensity obtained from the flow cytometry on BEL-7402 cells increases steadily after treated for 48 h. It is indicated that a lot of Rhodamine 123 from mitochondria matrix was released to the cytoplasm in a dose dependent manner, complexes 1 and 2 can affect the mitochondrial function and causing the depolarization of the mitochondrial membrane, and lead to the ΔΨm value significantly decreased. The percentage relative to control of the complex 2 is stronger than that of the complex 1 (Table 4). These results imply that the induction of apoptosis by the complexes may be associated with the mitochondrial pathway [17, 22, 43–47]. However, further mechanism researches involved in the induction of apoptosis remain to be elucidated.


Synthesis and In Vitro Antitumor Activity of Two Mixed-Ligand Oxovanadium(IV) Complexes of Schiff Base and Phenanthroline.

Zhang Y, Wang X, Fang W, Cai X, Chu F, Liao X, Lu J - Bioinorg Chem Appl (2013)

Distribution map of mitochondrial membrane potential with complex 1 (bottom) and complex 2 (top) for 48 h.
© Copyright Policy
Related In: Results  -  Collection

License
Show All Figures
getmorefigures.php?uid=PMC3569890&req=5

fig11: Distribution map of mitochondrial membrane potential with complex 1 (bottom) and complex 2 (top) for 48 h.
Mentions: As shown in Figure 11 and Table 4 upon increasing the concentrations of complexes 1 and 2 (60, 90, and 135 μM), the mean value of green fluorescence intensity obtained from the flow cytometry on BEL-7402 cells increases steadily after treated for 48 h. It is indicated that a lot of Rhodamine 123 from mitochondria matrix was released to the cytoplasm in a dose dependent manner, complexes 1 and 2 can affect the mitochondrial function and causing the depolarization of the mitochondrial membrane, and lead to the ΔΨm value significantly decreased. The percentage relative to control of the complex 2 is stronger than that of the complex 1 (Table 4). These results imply that the induction of apoptosis by the complexes may be associated with the mitochondrial pathway [17, 22, 43–47]. However, further mechanism researches involved in the induction of apoptosis remain to be elucidated.

Bottom Line: Two oxovanadium(IV) complexes of [VO(msatsc)(phen)], (1) (msatsc = methoxylsalicylaldehyde thiosemicarbazone, phen = phenanthroline) and its novel derivative [VO (4-chlorosatsc)(phen)], (2) (4-chlorosatsc = 4-chlorosalicylaldehyde thiosemicarbazone), have been synthesized and characterized by elemental analysis, IR, ES-MS, (1)H NMR, and magnetic susceptibility measurements.Both 1 and 2 decreased significantly the ΔΨm, causing the depolarization of the mitochondrial membrane.Complex 2 showed greater antitumor efficiency than that of complex 1.

View Article: PubMed Central - PubMed

Affiliation: Department of Biology, School of Basic Courses, Guangdong Pharmaceutical University, Guangzhou, Guangdong 510006, China.

ABSTRACT
Two oxovanadium(IV) complexes of [VO(msatsc)(phen)], (1) (msatsc = methoxylsalicylaldehyde thiosemicarbazone, phen = phenanthroline) and its novel derivative [VO (4-chlorosatsc)(phen)], (2) (4-chlorosatsc = 4-chlorosalicylaldehyde thiosemicarbazone), have been synthesized and characterized by elemental analysis, IR, ES-MS, (1)H NMR, and magnetic susceptibility measurements. Their antitumor effects on BEL-7402, HUH-7, and HepG2 cells were studied by MTT assay. The antitumor biological mechanism of these two complexes was studied in BEL-7402 cells by cell cycle analysis, Hoechst 33342 staining, Annexin V-FITC/PI assay, and detection of mitochondrial membrane potential (ΔΨm). The results showed that the growth of cancer cells was inhibited significantly, and complexes 1 and 2 mainly caused in BEL-7402 cells G0/G1 cell cycle arrest and induced apoptosis. Both 1 and 2 decreased significantly the ΔΨm, causing the depolarization of the mitochondrial membrane. Complex 2 showed greater antitumor efficiency than that of complex 1.

No MeSH data available.


Related in: MedlinePlus