Abstract

Ethnobotanical and ethnopharmacological studies of many Centaurea species indicated their potential in folk medicine so far. However, investigations of different Centaurea calcitrapa L. extracts in terms of cytotoxicity and antimicrobial activity against phytopathogens are generally scarce. The phenolic profile and broad antimicrobial activity (especially towards bacterial phytopathogens) of methanol (MeOH), 70% ethanol (EtOH), ethyl-acetate (EtOAc), 50% acetone (Me2CO) and dichloromethane: methanol (DCM: MeOH, 1: 1) extracts of C. calcitrapa leaves and their potential toxicity on MRC-5 cell line were investigated for the first time. A total of 55 phenolic compounds were identified: 30 phenolic acids and their derivatives, 25 flavonoid glycosides and aglycones. This is also the first report of the presence of centaureidin, jaceidin, kaempferide, nepetin, flavonoid glycosides, phenolic acids and their esters in C. calcitrapa extracts. The best results were obtained with EtOAc extract with lowest MIC values expressed in µg/mL ranging from 13 to 25, while methicillin resistant Staphylococcus aureus was the most susceptible strain. The most susceptible phytopathogens were Pseudomonas syringae pv. syringae, Xanthomonas campestris pv. campestris and Agrobacterium tumefaciens. The highest cytotoxicity was recorded for EtOAc and Me2CO extracts with the lowest relative and absolute IC50 values between 88 and 102 µg/mL, while EtOH extract was the least toxic with predicted relative IC50 value of 1578 µg/mL. Our results indicate that all tested extracts at concentration considered as non-toxic can be one of great importance in combat towards phytopathogenic and human pathogenic strains, as well as natural sources of antimicrobials.

Highlights

  • In the last few decades, there have been an increased number of resistant pathogens globally due to uncontrolled use of antibiotics for medical and agricultural purposes

  • Methodology applied through using UHPLC-LTQ Orbitrap MS reveals 55 plant metabolites and fragmentation data confirmed the presence of many compounds which are revealed for the first time in C. calcitrapa extracts such as jaceidin and its positional isomer centaureidin

  • Apigenin was the most abundant in our study, which has been identified in other Calcitrapa species such as C. pallescens Delile, C. urvillei, C. affinis Friv., C. cyanus, C. chilensis Bertero ex Hook. & Arn., C. nigra L., C. virgata Lam. (Khammar and Djeddi 2012)

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Summary

Introduction

In the last few decades, there have been an increased number of resistant pathogens globally due to uncontrolled use of antibiotics for medical and agricultural purposes. The genus Centaurea is one of the largest genera in the family Asteraceae which contains approximately 400–700 species (Garcia-Jacas et al 2001). Spp. stepposa Wagenitz, C. pullata L. and C. calcitrapa L. are used in diet, either as raw material or in processed form, and some of the species are used for making beverages and tonics (Lentini 2000; Pieroni et al 2002; Khammar and Djeddi 2012). The presence of natural components such as sesquiterpene lactones, phenolic acids, flavonoids and steroids favors the genus Centaurea over other genera within the Asteraceae family in terms of extended biological activities (Dumlu and Gürkan 2006)

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