Inorganic pharmaceuticals

Holder, Alvin A.

doi:10.1039/c1ic90005f

Cited by 11 publications

(7 citation statements)

References 149 publications

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“…Therefore, we began to look into using a TA derivative, specifically, a metallodrug. Metal complexes have been found to have a synergistic activity with their original drugs which enhance the drug’s bioactivity [28–34]. Recently, a copper (II)-Tolfenamic acid has been synthesized and published [35].…”

Section: Introductionmentioning

confidence: 99%

Novel Survivin Inhibitor for Suppressing Pancreatic Cancer Cells Growth via Downregulating Sp1 and Sp3 Transcription Factors

Hurtado

Sankpal

Kaba

et al. 2018

Cell Physiol Biochem

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Background/Aims: Targeting survivin, an anti-apoptotic protein and mitotic regulator, is considered as an effective therapeutic option for pancreatic cancer (PaCa). Tolfenamic acid (TA) showed anti-cancer activity in pre-clinical studies. A recent discovery demonstrated a copper(II) complex of TA (Cu-TA) can result in higher activity. In this study, the ability of Cu-TA to inhibit survivin and its transcription factors, Specificity protein (Sp) 1 and 3 in PaCa cell lines and tumor growth in mouse xenograft model were evaluated. Methods: Cell growth inhibition was measured in MIA PaCa-2 and Panc1 cells for 2 days using CellTiter-Glo kit. Sp1, Sp3 and survivin expression (by Western blot and qPCR), apoptotic cells and cell cycle phase distribution (by flow cytometry) were evaluated. A pilot study was performed using athymic nude mice [treated with vehicle/Cu-TA (25 or 50 mg/kg) 3 times/week for 4 weeks. Results: The IC₅₀ value for Cu-TA was about half than TA.Both agents repressed the protein expression of Sp1/Sp3/survivin, Cu-TA was more effective than TA. Especially effect on survivin inhibition was 5.2 (MIA PaCa-2) or 6.4 (Panc1) fold higher and mRNA expression of only survivin was decreased. Apoptotic cells increased with Cu-TA treatment in both cell lines, while Panc1 showed both effect on apoptosis and cell cycle (G₂/M) arrest. Cu-TA decreased the tumor growth in mouse xenografts (25 mg/kg: 48%; 50 mg/kg: 68%). Additionally, there was no change observed in mice body weights, indicating no overt toxicity was occurring. Conclusion: These results show that Cu-TA can serve as an effective survivin inhibitor for inhibiting PaCa cell growth.

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Section: Introductionmentioning

confidence: 99%

Novel Survivin Inhibitor for Suppressing Pancreatic Cancer Cells Growth via Downregulating Sp1 and Sp3 Transcription Factors

Hurtado

Sankpal

Kaba

et al. 2018

Cell Physiol Biochem

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“…Bipyridine 2,2′-bipyridine is a chelating component. The 2,2′-bipyridyl moiety has been extensively used as a chelating donor site within such bridging ligands due to its robust redox stability [24]. This allows ligands containing multiple 2,2′-bipyridine units to be synthesized and the interconnection of metal centres to be achieved with well-defined spatial arrangements.…”

Section: Nitrogen Heterocyclesmentioning

confidence: 99%

Dynamics of Transition Metal and their Application in Biomedical Industry

Malpaharia¹,

Pandey²

2020

Int.J.Curr.Microbiol.App.Sci

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“…For the development of vanado drugs, much work has been done for vanadyl ion coordinated to various organic ligands which show insulinmimetic effects. [11][12][13] Vanadium complexes exert preventive action against chemical carcinogenesis by the arrest of cell-cycle through the process of DNA fragmentation and cleavage. 14 Vanadium penetrates to the cells in the form of vanadate VO -3 which is then reduced to VO 2+ (vanadyl)ion at physiological pH.…”

Section: Introductionmentioning

confidence: 99%