Abstract

BackgroundSutherlandia frutescens (L.) R. Br is endemic to Southern Africa where it has been traditionally used for cancer and diabetes. In recent times it has been marketed for its reputed (but not proven) anticancer, antidiabetic and anti-HIV properties. Little is known about the mutagenic and antimutagenic potential of extracts and common marker compounds of Sutherlandia frutescens. Therefore this study aimed to investigate the putative efficacy and possible long-term adverse effects of using this herb.MethodsEthylacetate (EA) and 50% Methanol (MeOH) extracts were screened for mutagenic and antimutagenic activity using the Ames assay utilising TA97a, TA98, TA100 and TA102 in the presence and absence of metabolic activation. Four compounds, L-arginine, L-canavanine, GABA and D-pinitol known to occur in sutherlandia were also included. The total polyphenolic content of the both extracts was determined using the Folin-Ciocalteau method and FRAP and ABTS were used to determine the anti-oxidant potential of the extracts.ResultsThe extracts and the standards did not show any cytotoxicity except in TA97a. The EA extract exhibited antimutagenicity against all the bacterial strains at all concentrations tested. The MeOH extract showed both pro-mutagenic and antimutagenic activities with 2-acetamidofluorene and aflatoxin B1 in the presence of metabolic activation of TA98 and TA100, respectively. All compounds, except L-canavanine exhibited antimutagenic activity against all strains. L-canavanine, on the other hand showed co-mutagenicity with 9-aminoacridine on TA97a, at all test concentrations. The extracts and pure compounds exhibited their antimutagenic activity in a dose response manner. L-arginine and GABA showed an some antimutagenic response. EA extract had three times the total phenolic content (12.56 μg GE / mg) observed in the MeOH extract. There was correlation between total phenolic content, antioxidant potential and antimutagenicity.ConclusionBoth extracts exhibited a protective effect, with the EA extract exhibiting greater potency. L-canavanine acted as a co-mutagen in a dose response manner without metabolic activation. It is suggested that the EA extract be priotized for future development work as it showed a better risk profile and activity.

Highlights

  • Dose response effects Dose response effects were observed in the following two ways: Typical dose response where the inhibitory effect was directly related to the concentration of the extracts and pure compounds against 2-AAF, aflatoxin B1 (AFB1), cumoyl hydroperoxide (CHP) and 9-AA (Tables 1 and 3); and a saturation effect where there was constant inhibition across the three concentrations tested with all pure compounds against CHP and gamma (γ) aminobutyric acid (GABA) against 9-AA (Table 3)

  • Gomes-Carneiro et al [47] demonstrated that in the Salmonella/microsome assay, antimutagenicity generally manifests as a reduction in the number of revertant colonies caused by a known genotoxic agent, and cytotoxicity to tester strains may result in a reduction of revertants

  • The current study is the first report on the mutagenicity and antimutagenicity of S. frutescens crude extracts and comparing its polar and non-polar extracts as well as pure compounds

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Summary

Introduction

(Fabaceae, formerly Leguminosae, sub-family Papilionoideae) known locally as cancer bush, kankerbos (Afrikaans) and unwele (Zulu), is widely marketed in South Africa and elsewhere as sutherlandia tablets or as a leaf decoction or infusion. It is reputed, by various ethnic groups including the Zulus, Khoi-San and Xhosas, to treat a number of different diseases including diabetes mellitus, cancer, stomach complaints, topical wounds, gonorrhea and syphilis [6, 7], stress, depression and inflammation/arthritis [8, 9]. There is little known about its potential for cellular toxicity

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