In Vitro Cytotoxic Activity and Phytochemical Characterization (UPLC/T-TOF-MS/MS) of the Watermelon (Citrullus lanatus) Rind Extract

Molecules. 2022 Apr 12;27(8):2480. doi: 10.3390/molecules27082480.

Abstract

Reusing food waste is becoming popular in pharmaceutical industries. Watermelon (Citrullus lanatus) rind is commonly discarded as a major solid waste. Here, the in vitro cytotoxic potential of watermelon rind extracts was screened against a panel of human cancer cell lines. Cell cycle analysis was used to determine the induction of cell death, whereas annexin V-FITC binding, caspase-3, BAX, and BCL-2 mRNA expression levels were used to determine the degree of apoptosis. VEGF-promoting angiogenesis and cell migration were also evaluated. Moreover, the identification of phytoconstituents in the rind extract was achieved using UPLC/T-TOF-MS/MS, and a total of 45 bioactive compounds were detected, including phenolic acids, flavonoids aglycones, and their glycoside derivatives. The tested watermelon rind extracts suppressed cell proliferation in seven cancer cell lines in a concentration-dependent manner. The cytotoxicity of the rind aqueous extract (RAE) was higher compared with that of the other extracts. In addition to a substantial inhibitory effect on cell migration, the RAE triggered apoptosis in HCT116 and Hep2 cells by driving the accumulation of cells in the S phase and elevating the activity of caspase-3 and the BAX/BCL-2 ratio. Thus, a complete phytochemical and cytotoxic investigation of the Citrullus lanatus rind extract may identify its potential potency as an anticancer agent.

Keywords: Citrullus lanatus; VEGF; apoptosis; cancer cell lines; cell cycle.

MeSH terms

  • Antineoplastic Agents* / metabolism
  • Caspase 3 / metabolism
  • Citrullus* / chemistry
  • Humans
  • Phytochemicals / metabolism
  • Phytochemicals / pharmacology
  • Plant Extracts / pharmacology
  • Proto-Oncogene Proteins c-bcl-2 / metabolism
  • Tandem Mass Spectrometry
  • bcl-2-Associated X Protein / metabolism

Substances

  • Antineoplastic Agents
  • Phytochemicals
  • Plant Extracts
  • Proto-Oncogene Proteins c-bcl-2
  • bcl-2-Associated X Protein
  • Caspase 3