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Pyrazole (1, 2-diazole) induce apoptosis in lymphoma cells by targeting BCL-2 and BCL-XL genes and mitigate murine solid tumour development by regulating cyclin-D1 and Ki-67 expression.
Vishnu, Walsan Kalarikkal; Abeesh, Prathapan; Guruvayoorappan, Chandrasekharan.
Afiliación
  • Vishnu WK; Laboratory of Immunopharmacology and Experimental Therapeutics, Division of Cancer Research, Regional Cancer Centre (Research Centre, University of Kerala), Thiruvananthapuram, 695011 Kerala, India.
  • Abeesh P; Laboratory of Immunopharmacology and Experimental Therapeutics, Division of Cancer Research, Regional Cancer Centre (Research Centre, University of Kerala), Thiruvananthapuram, 695011 Kerala, India.
  • Guruvayoorappan C; Laboratory of Immunopharmacology and Experimental Therapeutics, Division of Cancer Research, Regional Cancer Centre (Research Centre, University of Kerala), Thiruvananthapuram, 695011 Kerala, India. Electronic address: guruvayoorappan@rcctvm.gov.in.
Toxicol Appl Pharmacol ; 418: 115491, 2021 05 01.
Article en En | MEDLINE | ID: mdl-33737021
ABSTRACT
Pyrazole or 1,2-Diazole is a five-membered heteroaromatic ring with two nitrogen atoms which is widely used in pharmacological research and organic synthesis. Several natural and synthetic pyrazole derivatives possess anti-cancer potential and some of them have underwent clinical trials. In this aspect, an investigation into the efficiency of the pyrazole nucleus to inhibit the growth and progression of various cancer cell lines/ experimental tumours would help in giving a better clarity to the anti-cancer behaviour of pyrazole containing drugs. This paper investigates the efficiency of pyrazole against Dalton's Lymphoma Ascites (DLA) cell line. Pyrazole inhibited the growth of DLA cells in vitro by committing them towards apoptosis. In vitro results were consistent in DLA induced murine solid tumour in vivo systems. Drug-treatment improved survival, reduced tumour loads, stabilized body weights and improved the haematological and serum biochemical parameters of DLA solid tumour bearing mice, thereby improving their overall survivability. Drug administration contained the aggravation of solid tumour by targeted downregulation of Cyclin-D1 and Ki-67. In addition, the mRNA expression levels of anti-apoptotic genes, BCL-2 and BCL-XL were downregulated in solid tumours, corroborating the in vitro results that pyrazole encourage apoptotic cell death in DLA cells. The new findings establish pyrazole as a potential anti-cancer drug candidate. The results must encourage future investigations into the efficacy of the drug against various cancer types.
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Texto completo: 1 Bases de datos: MEDLINE Asunto principal: Ascitis / Pirazoles / Apoptosis / Antígeno Ki-67 / Proteínas Proto-Oncogénicas c-bcl-2 / Ciclina D1 / Proteína bcl-X / Linfoma / Antineoplásicos Límite: Animals Idioma: En Revista: Toxicol Appl Pharmacol Año: 2021 Tipo del documento: Article País de afiliación: India

Texto completo: 1 Bases de datos: MEDLINE Asunto principal: Ascitis / Pirazoles / Apoptosis / Antígeno Ki-67 / Proteínas Proto-Oncogénicas c-bcl-2 / Ciclina D1 / Proteína bcl-X / Linfoma / Antineoplásicos Límite: Animals Idioma: En Revista: Toxicol Appl Pharmacol Año: 2021 Tipo del documento: Article País de afiliación: India