RESUMO
Sideritis scardica Griseb. (ironwort, mountain tea), an endemic plant of the Balkan Peninsula, has been used in traditional medicine in the treatment of gastrointestinal complaints, inflammation, and rheumatic disorders. This study aimed to evaluate its gastroprotective and anti-inflammatory activities. Besides, continuously increasing interest in assessing the role of the plant active constituents preventing the risk of cancer was a reason to make a detailed examination of the investigated ethanol, diethyl ether, ethyl acetate, and N-butanol extracts regarding cytotoxicity. Oral administration of the investigated extracts caused a dose-dependent anti-inflammatory effect in a model of carrageenan-induced rat paw edema. Gastroprotective activity of the extracts was investigated using an ethanol-induced acute stress ulcer in rats. The cytotoxic activity of plant extracts was assessed on PBMC, B16, and HL-60 cells and compared to the cytotoxicity of phenolic compounds identified in extracts. Apoptotic and necrotic cell death were analyzed by double staining with fluoresceinisothiocyanate (FITC)-conjugated annexin V and PI. The developed HPLC method enabled qualitative fingerprint analysis of phenolic compounds in the investigated extracts. Compared to the effect of the positive control, the anti-inflammatory drug indomethacine (4 mg/kg), which produced a 50 % decrease in inflammation, diethyl ether and N-butanol extracts exhibited about the same effect in doses of 200 and 100 mg/kg (53.6 and 48.7 %; 48.4 and 49.9 %, respectively). All investigated extracts produced dose-dependent gastroprotective activity with the efficacy comparable to that of the reference drug ranitidine. The diethyl ether extract showed significant dose-dependent cytotoxicity on B16 cells and HL-60 cells, decreasing cell growth to 51.3 % and 77.5 % of control, respectively, when used at 100 µg/mL. It seems that phenolic compounds (apigenin, luteolin, and their corresponding glycosides) are responsible for the diethyl ether extract cytotoxic effect. It also appears that induction of oxidative stress might be involved in its cytotoxicity, since B16 and HL-60 cells increased their ROS production in response to treatment with diethyl ether extract. Neither of the tested extracts nor any phenolic compounds showed significant cytotoxic effect to human PBMC. These results demonstrated the potent anti-inflammatory and gastroprotective activities, as well as the promising cytotoxicity.
Assuntos
Anti-Inflamatórios/administração & dosagem , Flavonoides/administração & dosagem , Fármacos Gastrointestinais/administração & dosagem , Extratos Vegetais/administração & dosagem , Polifenóis/administração & dosagem , Sideritis/química , Administração Oral , Animais , Anti-Inflamatórios/efeitos adversos , Anti-Inflamatórios/química , Anti-Inflamatórios/isolamento & purificação , Apigenina/administração & dosagem , Apigenina/análise , Apigenina/química , Apigenina/isolamento & purificação , Carragenina/farmacologia , Morte Celular , Linhagem Celular Tumoral , Edema/induzido quimicamente , Edema/tratamento farmacológico , Flavonoides/efeitos adversos , Flavonoides/análise , Flavonoides/química , Flavonoides/isolamento & purificação , Sequestradores de Radicais Livres/análise , Sequestradores de Radicais Livres/metabolismo , Fármacos Gastrointestinais/efeitos adversos , Fármacos Gastrointestinais/química , Fármacos Gastrointestinais/isolamento & purificação , Humanos , Luteolina/administração & dosagem , Luteolina/análise , Luteolina/química , Luteolina/isolamento & purificação , Masculino , Medicina Tradicional , Camundongos , Estrutura Molecular , Extratos Vegetais/efeitos adversos , Extratos Vegetais/química , Extratos Vegetais/isolamento & purificação , Polifenóis/efeitos adversos , Polifenóis/análise , Polifenóis/química , Polifenóis/isolamento & purificação , Ratos , Ratos Wistar , Espécies Reativas de Oxigênio/análise , Espécies Reativas de Oxigênio/metabolismo , Taninos/análise , Taninos/metabolismoRESUMO
Sideritis scardica Griseb., Lamiaceae (ironwort, mountain tea), an endemic plant of the Balkan Peninsula, has been used in traditional medicine in the treatment of antimicrobial infections, gastrointestinal complaints, inflammation and rheumatic disorders. This study reports a comparison between conventional (hydrodistillation HD and solvent extraction SE) and alternative (supercritical carbon dioxide SC CO2) extraction methods regarding the qualitative and quantitative composition of the obtained extracts as analyzed by GC and GC-MS techniques and their anitimicrobial activity. Different types of extracts were tested, the essential oil EO obtained by HD, EO-CO2 and AO-CO2 obtained by SC CO2 at different preasures 10 and 30 MPa, at 40 °C, respectively, and the fractions A, B, C and D obtained by successive solvent extraction (SE) A: ethanol, B: diethyl ether, C: ethyl acetate and D: n-butanol). While EO was characterized by the presence of the high percentage of oxygenated monoterpenes and sesquiterpenes (30.01 and 25.54%, respectively), the rest of the investigated samples were the most abundant in fatty acids and their esters and diterpenes (from 16.72 to 71.07% for fatty acids and their esters, and from 23.30 to 72.76%, for diterpenes). Microbial susceptibility tests revealed the strong to moderate activity of all investigated extracts against the tested microorganisms (MIC from 40 to 2,560 µg/mL). Although differences in the chemical compositions determined by GC and GC-MS analysis were established, the displayed antimicrobial activity was similar for the all investigated extracts.
Assuntos
Antibacterianos/isolamento & purificação , Cromatografia com Fluido Supercrítico/métodos , Extratos Vegetais/isolamento & purificação , Sideritis/química , Antibacterianos/farmacologia , Antifúngicos/isolamento & purificação , Antifúngicos/farmacologia , Bactérias/efeitos dos fármacos , Bactérias/isolamento & purificação , Infecções Bacterianas/microbiologia , Candida albicans/efeitos dos fármacos , Candida albicans/isolamento & purificação , Candidíase/microbiologia , Destilação/métodos , Cromatografia Gasosa-Espectrometria de Massas , Humanos , Cinética , Testes de Sensibilidade Microbiana , Óleos Voláteis/isolamento & purificação , Tonsila Palatina/microbiologia , Extratos Vegetais/farmacologia , Extração em Fase Sólida/métodos , Terpenos/isolamento & purificaçãoRESUMO
BACKGROUND/AIM: Recurrent vulvovaginal candidiasis is relatively frequent condition, and may have serious health consequences, like chronic vulvovaginal pain syndrome. The aim of our study was to determine possible risk factors for recurrent vulvovaginal candidiasis in non-pregnant females within the reproductive age. METHODS: The design of our study was of a case-control type. Case and control patients were selected from the gynecological patients at six primary care facilities in Serbia and in Montenegro. The data on the patients' health condition, concomitant therapy and diseases were taken from their records, and the data on habits were obtained by unstructured interview. For potential risk factors crude odds ratios were calculated, and then adjusted by logistic regression. RESULTS: A total of fifty-one patients had four or more episodes of vulvovaginal candidiasis during the last year (cases), and 132 patients with one to three episodes of vulvovaginal candidiasis were sampled as controls, matched by age. The only two significant associations were found between recurrent vulvovaginal candidiasis and continual wearing of panty liners during the last year (Odds ratio - OR adjusted: 3.97; confidence interval--CI: 1.57-10.02;p = 0.004), and between recurrent vulvovaginal candidiasis and predominant use of vaginal tampons during menstruation in the last year (OR adjusted: 4.25; CI: 1.11-16.27;p = 0.035). The synergistic effect was observed for the concurrent continual wearing of panty liners during the last year and self-medication with antimycotics. CONCLUSIONS: Local factors, like wearing of panty liners or use of tampons during menstruation, may promote recurrence of vulvovaginal candidiasis, especially in patients who practice self-medication with antimycotics.