Abstract

Given the alarming increase in colorectal cancer (CRC) worldwide, novel therapies are urgently needed. Plant-derived extracts have gained considerable interest in the last years due to their strong anticancer effect mediated by their unique bioactive compounds. Specifically, rosehips from Rosa canina have been successfully tested against several cancer models, including colon cancer. Moreover, gold derivatives are a promising alternative to the current platinum-based drugs commonly used in CRC chemotherapy due to their lack of affinity for DNA. Herein we have investigated the antitumor potential of a drug combination made of acidic polyphenols extracted from R. canina and the gold complex (Au(C≡C-2-NC5H4) (PTA)) in Caco-2 cell line as a model of CRC. The combination triggered strong apoptosis mediated by a blockage of the autophagic flux, which might be a consequence of a reactive oxygen species (ROS) increase and mitochondrial dysfunctionality. Our results suggest that the clinical application of plant polyphenols might enhance the anticancer effect of metallodrugs and reduce drug exposure time and therefore its side effects.

Highlights

  • The high incidence of cancer worldwide, along with the incomplete efficacy of current therapies, drives the development of novel clinical strategies to reduce mortality and improve patients’ quality of life

  • Results obtained showed the key role of acidic polyphenols (AP) concentration on the antiproliferative effect of drug combination, since all the tested concentration values decreased cell viability in comparison to both negative control and cells treated with the gold complex as a single agent (p < 0.05)

  • We have investigated the anticancer potential of a novel drug combination made from the acidic polyphenols extracted from rosehips of the wild plant Rosa canina and the gold complex (Au(C≡C-2-NC5 H4 )(PTA))

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Summary

Introduction

The high incidence of cancer worldwide, along with the incomplete efficacy of current therapies, drives the development of novel clinical strategies to reduce mortality and improve patients’ quality of life. The use of whole-plant extracts and/or isolated fractions that contain more than one bioactive compound might be a better approach to cancer therapy due to the additive effect of single agents. In line with this thinking, plant extracts have been proposed as promising adjuvants for chemotherapeutic drugs in order to enhance their effectiveness [3,4] as well as to improve its cytotoxicity on healthy tissue [5,6]. Rosehips from R. canina have been successfully tested on various cancer cell lines including colon, lung and prostate, suggesting their potential role on chemotherapy [8]

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