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Objective To investigate the chemical composition of a moderately polar extract (CHCl
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OBJECTIVE@#To investigate the chemical composition of a moderately polar extract (CHCl3 soluble part of the MeOH-H2O extract) obtained from the aerial parts (leaves and flowers) of Centaurea diluta Ait. subsp. algeriensis (Coss. & Dur.) Maire, a species endemic to Algeria and Morocco on which no reports are available to date. To evaluate in vitro the cytotoxic, antifungal and antimicrobial activities of this extract and the cytotoxic and antimicrobial activities of its isolated secondary metabolites.@*METHODS@#The cytotoxic effects of the extract were investigated on 3 human cancer cell lines i.e. the A549 non-small-cell lung carcinoma (NSCLC), the MCF7 breast adenocarcinoma and the U373 glioblastoma using a MTT colorimetric assay. Biological data allowed to guide the fractionation of the extract by separation and purification on silica gel 60 (CC and TLC). The isolated compounds which were characterized by spectral analysis, mainly HR-ESIMS, HR-EIMS, UV and NMR experiments ((1)H, (13)C, COSY, ROESY, HSQC and HMBC) and comparison of their spectroscopic data with those reported in the literature, were evaluated for cytotoxic activities on six cancer cell lines (A549, MCF7, U373, Hs683 human glioma, PC3 human prostate and B16-F10 murine melanoma). The direct and indirect antibacterial and antifungal activities were determined using microdilution methods for the raw extract and TLC-bioautography and microdilution methods against standard and clinical strains for the isolated compounds.@*RESULTS@#The raw extract reduced cell viability with IC50s of 27, 25 and 21 μg/mL on A549, MCF7 and U373, respectively. Five secondary metabolites: two phenolic compounds (vanillin 1, paridol 3), a lignan [(-)-arctigenin 2] and two flavonoid aglycones (eupatilin 4 and jaceosidin 5), were then isolated from this extract. Moderate cytotoxic effects were observed for (-)-arctigenin 2 (IC50s: 28 and 33 μM on Hs683 and B16-F10, respectively), eupatilin 4 (IC50s: 33 and 47 μM on B16-F10 and PC3, respectively) and jaceosidin 5 (IC50s: 32 and 40 μM on PC3 and B16-F10, respectively).@*CONCLUSIONS@#All the isolated compounds were described for the first time from this species. Although inactive against 7 tested microorganisms (fungi, bacteria and yeast, human or plant pathogens), the raw extract was able to potentiate the effect of beta-lactam antibiotics on methicillin-resistant Staphylococcus aureus (MRSA), reducing the minimal inhibitory concentrations (MICs) by a factor of 2-32-fold. No synergy was found between the extract and streptomycin. From the five isolated compounds only jaseosidin 5 showed a moderate antimicrobial activity.
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Pharmacovigilance is essential for developing reliable information on the safety of herbal medicines as used in Europe and the US. The existing systems were developed for synthetic medicines and require some modification to address the specific differences of medicinal herbs. Traditional medicine from many different cultures is used in Europe and the US which adds to the complexities and difficulties of even basic questions such as herb naming systems and chemical variability. Allied to this also is the perception that a 'natural' or herbal product must be safe simply because it is not synthetic which means that the safety element of monitoring for such medicines can be overlooked because of the tag associated with such products. Cooperation between orthodox physicians and traditional practitioners is needed to bring together the full case details. Independent scientific assistance on toxicological investigation, botanical verification can be invaluable for full evaluation of any case report. Systematic pharmacovigilance is essential to build up reliable information on the safety of herbal medicines for the development of appropriate guidelines for safe effective use.
