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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

Synthesis of [VO(msatsc)(phen)] 1, X = –OCH3 and [VO(4-chlorosatsc)] 2, X = Cl.
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sch1: Synthesis of [VO(msatsc)(phen)] 1, X = –OCH3 and [VO(4-chlorosatsc)] 2, X = Cl.

Mentions: Because V(IV) complexes have no charge, they are perceived to be candidates for easy bioabsorption. On the other hand, vanadyl(IV) complexes incorporating thiosemicarbazones have been studied extensively for their insulin-like effects which result in the inhibition of glycerol release and enhancement of glucose uptake by rat adipocytes and have been used in the treatment of tuberculosis [16–20]. In view of inquisitive response of oxovanadium(IV) in biology, we have reported that four oxidovanadium(IV) complexes present highly cytotoxic activities against Myeloma cell (Ag8.653) and Gliomas cell (U251) lines [21]. To continue our research in this project, in the present paper, an oxovanadium complex [VO(msatsc)(phen)] 1 (msatsc = methoxylsalicylaldehyde thiosemicarbazone, phen = phenanthroline) and its novel derivative [VO (4-chlorosatsc)(phen)] and (2) (4-chlorosatsc = 4-chlorosalicylaldehyde thiosemicarbazone) (Scheme 1) 2 have been synthesized and characterized. Their antitumor effects on BEL-7402 human liver (Bel7402), HUH-7, HepG2 cells were studied by MTT assay. The reported compounds may be an addition of new class of compounds as the metal-based drugs.


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)

Synthesis of [VO(msatsc)(phen)] 1, X = –OCH3 and [VO(4-chlorosatsc)] 2, X = Cl.
© Copyright Policy
Related In: Results  -  Collection

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

sch1: Synthesis of [VO(msatsc)(phen)] 1, X = –OCH3 and [VO(4-chlorosatsc)] 2, X = Cl.
Mentions: Because V(IV) complexes have no charge, they are perceived to be candidates for easy bioabsorption. On the other hand, vanadyl(IV) complexes incorporating thiosemicarbazones have been studied extensively for their insulin-like effects which result in the inhibition of glycerol release and enhancement of glucose uptake by rat adipocytes and have been used in the treatment of tuberculosis [16–20]. In view of inquisitive response of oxovanadium(IV) in biology, we have reported that four oxidovanadium(IV) complexes present highly cytotoxic activities against Myeloma cell (Ag8.653) and Gliomas cell (U251) lines [21]. To continue our research in this project, in the present paper, an oxovanadium complex [VO(msatsc)(phen)] 1 (msatsc = methoxylsalicylaldehyde thiosemicarbazone, phen = phenanthroline) and its novel derivative [VO (4-chlorosatsc)(phen)] and (2) (4-chlorosatsc = 4-chlorosalicylaldehyde thiosemicarbazone) (Scheme 1) 2 have been synthesized and characterized. Their antitumor effects on BEL-7402 human liver (Bel7402), HUH-7, HepG2 cells were studied by MTT assay. The reported compounds may be an addition of new class of compounds as the metal-based drugs.

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