Evaluation of anticancer potency of Cu-isatin-1-(2-pyridyl) piperazine thiosemicarbazone (Cu-Istpypz) against epidermoid carcinoma cell line (A431)
A series of Isatin thiosemicarbazones and their copper(II) complexes were synthesized and evaluated for their anti-cancer activities to develop potent chemotherapeutic agents. Among the compounds synthesized, copper conjugated isatin-thiosemicarbazone derivative, Cu-Istpypz, showed considerable anti...
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| Main Authors: | , , , , |
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| Format: | Article |
| Language: | English |
| Published: |
Elsevier
2025-01-01
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| Series: | Results in Chemistry |
| Subjects: | |
| Online Access: | http://www.sciencedirect.com/science/article/pii/S2211715624006891 |
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| Summary: | A series of Isatin thiosemicarbazones and their copper(II) complexes were synthesized and evaluated for their anti-cancer activities to develop potent chemotherapeutic agents. Among the compounds synthesized, copper conjugated isatin-thiosemicarbazone derivative, Cu-Istpypz, showed considerable anti-proliferative activity against A431 (Skin Cancer) and A549 (Lung Cancer) cell lines. Cell viability assay using crystal violet dye exhibited the effects of the compounds against those cell lines. Cu-Istpypz was highly effective in inhibiting A431 cell proliferation at lower concentrations. The compound Cu-Istpypz also suppressed the colony formation of A431 cells in a concentration-dependent manner, as demonstrated by the clonogenic assay. Additionally, at higher concentrations, Cu-Istpypz slowed down the migration and wound-healing capabilities of A431 cells. RT-PCR and western blot analysis indicated that the compound induced the expression of pro-apoptotic Bax and inhibited anti-apoptotic Bcl-2 and Bcl-xl in a concentration-dependent manner. Further, the compound induces intrinsic apoptosis in A431 cells by activating the JNK signalling pathway and suppressing the PI3K/AKT pathway. DNA fragmentation assay further confirms the onset of apoptosis in the presence of the compound. All these confirm that Cu-Istpypz thiosemicarbazone has the potential to be developed as a future chemotherapeutic agent in the treatment of skin cancer. |
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| ISSN: | 2211-7156 |