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Screening of cytoprotectors against methotrexate-induced cytogenotoxicity from bioactive phytochemicals

Shaobin Gu1, Ying Wu2, Jianbo Yang3

  • 1College of Food and Bioengineering, Henan University of Science and Technology, Luoyang, China; Luoyang Engineering and Technology Research Center of Microbial Fermentationon, Luoyang, China.

Peerj
|May 19, 2016
PubMed

Insights

Certain plant compounds can protect against the genotoxicity of methotrexate (MTX), a chemotherapy drug. Combinations of these phytochemicals show significant antimutagenic effects, reducing MTX-induced DNA damage and offering potential as cytoprotective agents.

Area of Science:

  • Pharmacology
  • Toxicology
  • Natural Product Chemistry

Background:

  • Methotrexate (MTX) is an anti-neoplastic drug with known cytogenotoxicity.
  • Increased risk of secondary cancers necessitates the development of cytoprotectors against MTX side effects.

Purpose of the Study:

  • To evaluate the cytoprotective and antimutagenic effects of ten bioactive phytochemicals and their combinations against MTX-induced genotoxicity.
  • To identify potent phytochemical combinations for potential use as cytoprotectors.

Main Methods:

  • An umu test and a micronucleus assay were used to assess the antimutagenic activities of various phytochemicals.
  • Phytochemical combinations were tested for their efficacy in suppressing MTX genotoxicity in vitro and in vivo (Kunming mice).

Main Results:

  • Allicin, proanthocyanidins, polyphenols, eleutherosides, and isoflavones demonstrated significant antimutagenic activities.
  • Combinations of grape seed proanthocyanidins with eleutherosides, and green tea polyphenols with eleutherosides showed the highest inhibition rates (74.7% and 71.8%, respectively).
  • In vivo studies confirmed reduced micronucleus and sperm abnormality rates, with improved thymus and spleen indices in MTX-exposed mice pretreated with phytochemical combinations.

Conclusions:

  • Bioactive phytochemicals, particularly in specific combinations, exhibit potent antimutagenic properties against methotrexate.
  • These phytochemical combinations show promise as novel cytoprotectors to mitigate MTX-induced genotoxicity and associated risks.
Keywords:
CytoprotectorMethotrexatePhytochemicalUmu test

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