Abstract

Tropical forests constitute a prolific sanctuary of unique floral diversity and potential medicinal sources, however, many of them remain unexplored. The scarcity of rigorous scientific data on the surviving Mascarene endemic taxa renders bioprospecting of this untapped resource of utmost importance. Thus, in view of valorizing the native resource, this study has as its objective to investigate the bioactivities of endemic leaf extracts. Herein, seven Mascarene endemic plants leaves were extracted and evaluated for their in vitro antioxidant properties and antiproliferative effects on a panel of cancer cell lines, using methyl thiazolyl diphenyl-tetrazolium bromide (MTT) and clonogenic cell survival assays. Flow cytometry and comet assay were used to investigate the cell cycle and DNA damaging effects, respectively. Bioassay guided-fractionation coupled with liquid chromatography mass spectrometry (MS), gas chromatography-MS, and nuclear magnetic resonance spectroscopic analysis were used to identify the bioactive compounds. Among the seven plants tested, Terminalia bentzoë was comparatively the most potent antioxidant extract, with significantly (p < 0.05) higher cytotoxic activities. T. bentzoë extract further selectively suppressed the growth of human hepatocellular carcinoma cells and significantly halted the cell cycle progression in the G0/G1 phase, decreased the cells’ replicative potential and induced significant DNA damage. In total, 10 phenolic compounds, including punicalagin and ellagic acid, were identified and likely contributed to the extract’s potent antioxidant and cytotoxic activities. These results established a promising basis for further in-depth investigations into the potential use of T. bentzoë as a supportive therapy in cancer management.

Highlights

  • The plant kingdom is known to be a prolific sanctuary of phytochemicals with unique therapeutic potential

  • While the proanthocyanidin content prevailed in the E. sideroxyloides leaf, both the S. lineata leaf and T. bentzoë leaf had a remarkably negligible amount of proanthocyanidin detected by the butanol/HCl assay

  • The cytotoxic nature of T. bentzoë leaf extract against cancerous cells indicated that the T. bentzoë leaf has the potential to be repurposed in the mitigation of cancer as part of traditional medicine

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Summary

Introduction

The plant kingdom is known to be a prolific sanctuary of phytochemicals with unique therapeutic potential. At least 25% of the 1562 clinical drugs approved by the US Food and Drugs Administration are known to have been derived from terrestrial plants [1,2]. An estimated 28,187 plant taxa, globally, are documented to have medicinal values, with over 3000 species reported with the ethnomedicinal application against cancer [3,4]. The continued dependence of mankind on plants was further evidenced during the recent outbreak of the COVID-19 pandemic, whereby herbal medicines were used in an attempt to mitigate the symptoms of the novel coronavirus infection [5,6,7]. Untapped endemic plant species from these niche areas broaden the structural variation of novel chemotypes [9,10]. The market value of vincristine alone was estimated to be USD 15 million per kilogram, in the year 2016 [13]

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