Apigenin potentiates the antitumor activity of 5-FU on solid Ehrlich carcinoma: Crosstalk between apoptotic and JNK-mediated autophagic cell death platforms

Toxicol Appl Pharmacol. 2017 Feb 1:316:27-35. doi: 10.1016/j.taap.2016.12.012. Epub 2016 Dec 23.

Abstract

Background: Although 5- Fluorouracil (5-FU) has exhibited effectiveness against cancer, novel therapeutic strategies are needed to enhance its antitumor efficiency and modulate its cytotoxity. Apigenin, a flavonoid present in fruits and vegetables, is a potent dietary phytochemical effective in cancer chemoprevention.

Aim: This study was undertaken to investigate the potential synergistic antitumor activity of apigenin and 5-FU on Solid Ehrlich carcinoma (SEC).

Methods: Eighty Swiss albino male mice were divided into four equal groups: vehicle treated control SEC, SEC+5-FU, SEC+apigenin, SEC+ 5-FU+apigenin. Beclin-1 and caspases 3, 9 and JNK activities were estimated by ELISA; mRNA expression levels of the antiapoptotic gene Mcl-1 were estimated using quantitative real-time RT-PCR, while tissue malondialdehyde (MDA), glutathione peroxidase and total antioxidant capacity were evaluated spectrophotometrically. A part of the tumor was examined for histopathological and Ki-67 immunohistochemistry analysis.

Results: 5-FU and/or apigenin caused significant increase in tissue levels of Beclin-1, caspases 3, 9 and JNK activities, MDA with significant decrease in tumor volume, Mcl-1expression, tissue glutathione peroxidase and total antioxidant capacity and alleviated the histopathological changes with significant decrease of Ki-67 proliferation index compared to vehicle treated SEC control group.

In conclusion: The combination of 5-FU and apigenin had a greater effect than each of 5-FU or apigenin alone against solid Ehrlich carcinoma in mice.

Keywords: 5-FU; Apigenin; Apoptosis; Autophay; Ehrlich tumor; JNK activity.

MeSH terms

  • Animals
  • Antimetabolites, Antineoplastic / administration & dosage
  • Antineoplastic Combined Chemotherapy Protocols / administration & dosage
  • Apigenin / administration & dosage*
  • Apoptosis / drug effects*
  • Apoptosis / physiology
  • Carcinoma, Ehrlich Tumor / drug therapy*
  • Carcinoma, Ehrlich Tumor / metabolism*
  • Cell Death / drug effects
  • Cell Death / physiology
  • Drug Synergism
  • Fluorouracil / administration & dosage*
  • Ki-67 Antigen / biosynthesis
  • MAP Kinase Kinase 4 / metabolism*
  • Male
  • Mice
  • Myeloid Cell Leukemia Sequence 1 Protein / biosynthesis
  • Tumor Burden / drug effects
  • Tumor Burden / physiology
  • Xenograft Model Antitumor Assays / methods

Substances

  • Antimetabolites, Antineoplastic
  • Ki-67 Antigen
  • Mcl1 protein, mouse
  • Mki67 protein, mouse
  • Myeloid Cell Leukemia Sequence 1 Protein
  • Apigenin
  • MAP Kinase Kinase 4
  • Fluorouracil