In vitro bioactivity approach of unripe genipap (Genipa americana L., Rubiaceae) fruit extract and its solid lipid microparticle

Food Res Int. 2020 Jan:127:108720. doi: 10.1016/j.foodres.2019.108720. Epub 2019 Oct 9.

Abstract

Growing awareness in favor of innovative and healthier alternatives is creating a noticeable shift from synthetic colorants to natural additives. And, such a swing in the consumer market is growing slowly but noticeably. In this context, genipap (Genipa americana L.) fruit represents an emerging source of blue colorants in Latin America with extensive application possibilities. This is despite the fact that there are few studies concerning its toxicity predictive factors. In this early-stage study we propose to investigate safety issues around genipap extract (IBBP); we also attempt to identify fingerprint profiling of both IBBP extract and solid lipid microparticles containing IBBP extract (SLM-IBBP) using in vitro assays. The main compounds identified were genipin, and genipin 1-β-gentiobioside. Results indicated that IBBP extract, at 25 µg/mL, was able to promote DNA damage in CHO-K1 cells, suggesting a genotoxic effect. On the other hand, the SLM-IBBP inhibited almost all cancer cell lines with GI50 ranging from 0.25 μg/mL to 43.5 μg/mL. Also, IBBP-SLM seems to exert a desirable apoptosis induction (at 25 µg/mL dosage). The next steps for our work, therefore, will focus on other nanoparticle formulation approaches, in particular with the use of natural Brazilian starch. An evaluation of the metabolism and distribution of microparticles, and their safety for food and pharmaceutical purposes, are also required.

Keywords: 6′-O-p-Coumaroyl-geniposidic acid (PubChem CID: 44255335); 6′-O-p-Feruloyl-geniposidic acid (PubChem CID: not found); 6″-O-p-Coumaroyl-1-β-gentibioside geniposidic acid (PubChem CID: not found); 6″-O-p-Coumaroylgenpin-gentiobioside (PubChem CID: 101408305); Gardenoside (PubChem CID: 442423); Genipin; Genipin (PubChem CID: 442424); Genipin 1-β-gentiobioside (PubChem CID: 3082301); Geniposide; Geniposide (PubChem CID: 107848); Geniposidic acid (PubChem CID: 16020046); Iridoid glucosides; Metabolic activation (S9(+)/S9(−)); Natural blue colorants; Phosphatidylserine exposure.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Animals
  • Apoptosis / drug effects
  • Chromatography, High Pressure Liquid
  • Chromatography, Liquid
  • Fruit / chemistry*
  • Humans
  • Lipids
  • Mass Spectrometry
  • Microscopy, Electron
  • Plant Extracts / pharmacology*
  • Rubiaceae / chemistry*

Substances

  • Lipids
  • Plant Extracts