RESUMEN
The objectives of this study were to evaluate the in vitro and in vivo anti-tumor potential of the aqueous gall extract (G extract) from Limoniastrum guyonianum and to elucidate its immunological mechanisms, in part, by assessing its effects on the growth of transplanted tumors and the immune response in these tumor-bearing mice. Here, mice were inoculated with B16F10 mouse tumor cells and then treated intraperitoneally with G extract at 25 or 50 mg extract/kg BW for 7, 14, or 21 days. At each timepoint, effects of the extract on the tumor growth, splenocytes proliferation, NK cell activity, and CTL activity among splenocytes isolated from the mice were measured. G extract-induced tumor growth inhibition was associated with characteristic apoptotic changes in the tumor cells, like nuclear condensation. In addition, the extract inhibited melanin synthesis and tyrosinase activity among melanoma cells in a concentration-related manner. G extract did not only significantly inhibit the growth of the transplantable tumor, but also remarkably increased splenocytes proliferation and both NK and CTL activities in tumor-bearing mice. The extract was also seen to have promoted lysosomal activity of host macrophages and gave rise to enhanced cellular anti-oxidant activity in several cell types in mice.
Asunto(s)
Antineoplásicos Fitogénicos/farmacología , Factores Inmunológicos/farmacología , Melanoma Experimental/tratamiento farmacológico , Extractos Vegetales/farmacología , Plumbaginaceae/química , Animales , Antioxidantes/farmacología , Apoptosis/efectos de los fármacos , Línea Celular Tumoral/efectos de los fármacos , Proliferación Celular/efectos de los fármacos , Células Asesinas Naturales/efectos de los fármacos , Células Asesinas Naturales/inmunología , Macrófagos Peritoneales/efectos de los fármacos , Masculino , Melaninas/biosíntesis , Melanoma Experimental/inmunología , Melanoma Experimental/patología , Ratones Endogámicos BALB C , Monofenol Monooxigenasa/metabolismo , Linfocitos T Citotóxicos/efectos de los fármacosRESUMEN
An aqueous extract of Limoniastrum guyonianum gall (G extract) was tested on Salmonella typhimurium to assess its mutagenic and antimutagenic effects. This extract showed no mutagenicity when tested with S. typhimurium strain TA104 either with or without exogenous metabolic activation mixture (S9), whereas our findings revealed that the aqueous gall extract induced a mutagenic effect in S. typhimurium TA1538 when tested in the presence, as well as in the absence, of S9 activation mixture at the concentration of 500 µg/mL. Thus, the same concentration produced a mutagenic effect, when incubated with S. typhimurium TA100 in the presence of metabolic activation mixture. In contrast, our results showed a weak antimutagenic potential of the same extract against sodium azide in the presence of S. typhimurium TA100 and S. typhimurium TA1538 without metabolic activation (S9), whereas, in the presence of S. typhimurium TA104, we obtained a significant inhibition percentage (76.39%) toward 3.25 µg/plate of methylmethanesulfonate. Antimutagenicity against aflatoxin B1, 4-nitro-o-phenylene-diamine and 2-aminoanthracène was significant, with an inhibition percentage of, respectively, 70.63, 99.3 and 63.37% in the presence of, respectively, S. typhimurium TA100, S. typhimurium TA1538 and S. typhimurium TA104 strains at a concentration of 250 µg/plate after metabolic activation (S9). Antioxidant capacity of the tested extract was evaluated using the enzymatic (xanthine/xanthine oxidase assay) and the nonenzymatic (2,2-diphenyl-1-picrylhydrazyl) system. G extract exhibited high antioxidant activity.
Asunto(s)
Antimutagênicos/farmacología , Antioxidantes/farmacología , Mutágenos/farmacología , Extractos Vegetales/farmacología , Tumores de Planta , Plumbaginaceae/química , Aflatoxina B1/antagonistas & inhibidores , Análisis de Varianza , Antracenos , Compuestos de Bifenilo , Metilmetanosulfonato , Microsomas/efectos de los fármacos , Fenilendiaminas/antagonistas & inhibidores , Picratos , Salmonella typhimurium/efectos de los fármacos , Azida Sódica/metabolismo , Especificidad de la Especie , TúnezRESUMEN
In this report, the ethyl acetate extract and its major constituent, isorhamnetin 3-o-robinobioside (I3-O-Rob), from Nitraria retusa (N. Retusa) leaf extracts were evaluated for their ability to induce apoptosis in human lymphoblastoid cells (TK6). Apoptosis of TK6 cell line was carried out using DNA fragmentation, poly ADP-ribose polymerase (PARP) cleavage with reference to caspase-3 activity. These tested products, from N. Retusa, enhanced the apoptosis effects in the tested cancer cell line. This result was confirmed by DNA fragmentation and PARP cleavage indicating a release of caspase-3 level. Our results indicate that the original ethyl acetate extract and the I3-O-Rob have a great antiproliferative effect on human lymphoblastoid cells (TK6), which may be due to their involvement in the apoptotic pathway.
Asunto(s)
Antineoplásicos/farmacología , Apoptosis/efectos de los fármacos , Flavonoides/farmacología , Magnoliopsida/química , Extractos Vegetales/farmacología , Caspasa 3/metabolismo , Línea Celular Tumoral , Fragmentación del ADN/efectos de los fármacos , Glicósidos/farmacología , Humanos , Hojas de la Planta/química , Poli(ADP-Ribosa) Polimerasas/genética , Poli(ADP-Ribosa) Polimerasas/metabolismo , Quercetina/análogos & derivados , Quercetina/farmacologíaRESUMEN
BACKGROUND: In this report, the isorhamnetin 3-o-robinobioside and its original extract, the ethyl acetate extract, from Nitraria retusa leaves, were evaluated for their ability to induce antioxidant and antigenotoxic effects in human chronic myelogenous leukemia cell line. METHODS: Nitraria retusa products properties were carried out by firstly evaluating their effects against lipid peroxidation induced by H2O2, using the thiobarbituric acid reactive substances species (TBARS) assay, and proceeding to the assay of cellular antioxidant activity, then doing the comet assay. RESULTS: The isorhamnetin 3-o-robinobioside showed a protective effect against lipid peroxidation induced by H2O2. The same natural compound and ethyl acetate extract inhibited oxidation induced by 2,2'-azobis (2-amidinopropane) dihydrochloride in human chronic myelogenous leukemia cells with respectively 50% inhibitory concentration values of 0.225 mg/ml and 0.31 mg/ml, reflecting a significant antioxidant potential. The same two products inhibited the genotoxicity induced by hydroxyl radicals in the same human cell line (by 77.77% at a concentration of 800 µg/ml and by 80.55% at a concentration of 1000 µg/ml respectively). CONCLUSIONS: The isorhamnetin 3- o-robinobioside and its original extract, the ethyl acetate extract, from Nitraria retusa leaves, have a great antioxidant and antigenotoxic potential on human chronic myelogenous leukemia cell line K562.
Asunto(s)
Antimutagênicos/farmacología , Antioxidantes/farmacología , Glicósidos/aislamiento & purificación , Glicósidos/farmacología , Leucemia Mielógena Crónica BCR-ABL Positiva/metabolismo , Peroxidación de Lípido/efectos de los fármacos , Magnoliopsida/química , Extractos Vegetales/farmacología , Quercetina/análogos & derivados , Antimutagênicos/aislamiento & purificación , Antimutagênicos/uso terapéutico , Antioxidantes/aislamiento & purificación , Antioxidantes/uso terapéutico , Línea Celular , Glicósidos/uso terapéutico , Humanos , Peróxido de Hidrógeno , Concentración 50 Inhibidora , Células K562 , Leucemia Mielógena Crónica BCR-ABL Positiva/tratamiento farmacológico , Nigeria , Fitoterapia , Extractos Vegetales/química , Extractos Vegetales/uso terapéutico , Quercetina/aislamiento & purificación , Quercetina/farmacología , Quercetina/uso terapéutico , Sustancias Reactivas al Ácido Tiobarbitúrico/metabolismoRESUMEN
The antioxidant and apoptotic activities of digallic acid, isolated from the fruits of Pistascia lentiscus, were investigated. The study demonstrated that digallic acid possessed pro-apoptotic effects, as shown by provoking DNA fragmentation of K562 cells. It also revealed a significant antioxidant potential and effective scavenging activity against 2,2-diphenyl-1-picrylhdrazyl (DPPH·) and O2·â» radicals, and reduced cupric ions. We conclude that this integrated approach to apoptotic and antioxidant assessment may be useful to maximize the beneficial effects associated with using P. lentiscus derivatives as medicinal and dietary compounds.
Asunto(s)
Antioxidantes/química , Apoptosis , Depsidos/farmacología , Ácido Gálico/análogos & derivados , Pistacia/química , Extractos Vegetales/farmacología , Antineoplásicos Fitogénicos/química , Antineoplásicos Fitogénicos/farmacología , Compuestos de Bifenilo/química , Fragmentación del ADN , Depsidos/química , Frutas/química , Ácido Gálico/química , Ácido Gálico/farmacología , Humanos , Células K562 , Picratos/química , Extractos Vegetales/química , Riboflavina/química , Superóxido Dismutasa/química , Sales de Tetrazolio/químicaRESUMEN
Fractionation of the chloroformic extracts from Teucrium ramosissimum leaves resulted in the isolation of three flavonoids: genkwanin (1), cirsimaritin (2) and 4',7-dimethoxy apigenin (4) and one sesquiterpene: ß-eudesmol (3). The structures were determined using data obtained from (1)H and (13)C NMR spectra, as well as by various correlation experiments (COSY, HMQC and HMBC). The antioxidant activities of the isolated flavonoids from T. ramosissimum leaves were evaluated by measuring their ability to scavenge the radical ABTS(+) and through chemical assays: cupric reducing antioxidant capacity (CUPRAC), reducing power (RP) and ferric reducing antioxidant power (FRAP). Furthermore, the effects of T. ramosissimum isolated molecules, on inhibition of cell proliferation and induction of apoptosis in human leukemia cells, were also examined. Cirsimaritin showed the best activity in the ABTS assay with TEAC value 2.04µM, whereas apigenin and 4',7-dimethoxy apigenin exhibited the highest antioxidant activity using the CUPRAC, RP and FRAP assays with TEAC values 10.5, 1.39 and 0.71µM respectively. The cytotoxic activity revealed that the ß-eudesmol inhibited significantly the proliferation of K562 cells (IC(50)=20µg/ml).
Asunto(s)
Antineoplásicos Fitogénicos/farmacología , Flavonoides/química , Flavonoides/farmacología , Sesquiterpenos/farmacología , Teucrium/química , Antineoplásicos Fitogénicos/química , Antioxidantes/química , Antioxidantes/farmacología , Apoptosis/efectos de los fármacos , Línea Celular Tumoral , Proliferación Celular/efectos de los fármacos , Ensayos de Selección de Medicamentos Antitumorales , Flavonas/química , Flavonas/farmacología , Humanos , Células K562 , Leucemia/tratamiento farmacológico , Leucemia/patología , Espectroscopía de Resonancia Magnética , Estructura Molecular , Hojas de la Planta/química , Plantas Medicinales/química , Sesquiterpenos/química , Relación Estructura-Actividad , TúnezRESUMEN
In our continual course toward the valorization of traditionally used endemic flora through the analysis of its chemobiodiversity, the phytochemical analysis of aerial parts of Marrubium deserti de Noé was undertaken. Dichloromethane and methanol extracts led to the isolation of terpenoid derivatives among which two were new labdane diterpenes named marrulibacetal A and desertine, respectively. Six of them were known compounds (a mixture of the isomers cyllenin A and 15-epi-cyllenin A, marrubiin, marrulactone, marrulibacetal and ß-stigmasterol) and seven known phenolic compounds were also isolated: apigenin and several 7-O-substituted derivatives (apigenin-7-O-ß-neohesperidoside, apigenin-7-O-glucoside, terniflorin and apigenin-7-O-glucuronide) together with two phenylethanoid glucosides (acteoside and forsythoside B). The structures and relative configurations of the new compounds were elucidated by MS and a series of 1D and 2D NMR analyses. Some pure compounds have been evaluated for their antioxidant activities through different methods: DPPH and ABTS assays as well as CUPRAC assay. Genotoxic and antigenotoxic activities of extracts and pure compounds were also evaluated in vitro on Escherichia coli PQ37 cells by the SOS Chromotest. Some of the isolated compounds like phenylethanoid derivatives showed stronger antioxidant capacity than trolox and were also able to significantly inhibit ß-galactosidase induction caused by the mutagen agent nitrofurantoin.
Asunto(s)
Antioxidantes/farmacología , Daño del ADN/efectos de los fármacos , Marrubium/química , Extractos Vegetales/farmacología , Apigenina/aislamiento & purificación , Apigenina/farmacología , Benzotiazoles/análisis , Compuestos de Bifenilo/análisis , Ácidos Cafeicos/aislamiento & purificación , Ácidos Cafeicos/farmacología , Diterpenos/aislamiento & purificación , Diterpenos/farmacología , Flavonas/aislamiento & purificación , Flavonas/farmacología , Glucósidos/aislamiento & purificación , Glucósidos/farmacología , Glicósidos/aislamiento & purificación , Glicósidos/farmacología , Espectroscopía de Resonancia Magnética/métodos , Metanol/metabolismo , Cloruro de Metileno/metabolismo , Fenoles/aislamiento & purificación , Fenoles/farmacología , Picratos/análisis , Ácidos Sulfónicos/análisisRESUMEN
Total oligomer flavonoids (TOF) enriched and ethyl acetate (EA) extracts from Rhamnus alaternus induce apoptotic death in human chronic myelogenous leukaemia K562 cell line, as demonstrated by gel electrophoresis, which demonstrates the characteristic ladder patterns of DNA fragmentation and the proteolytic cleavage of poly(ADP ribose) polymerase (PARP). The effect of R. alaternus extract in reducing oxidative stress was evaluated by anti-lipid peroxidation which was monitored by measuring malondialdehyde level in K562 cultured cells. The TOF and EA extracts were found to be effective to protect against lipid peroxidation. Their IC50 values were 196 and 273 µg mL⻹, respectively. These findings suggest that R. alaternus extracts exhibit potential antioxidant and proapoptotic properties.
Asunto(s)
Leucemia Eritroblástica Aguda/metabolismo , Peroxidación de Lípido/efectos de los fármacos , Extractos Vegetales/farmacología , Rhamnus/química , Apoptosis/efectos de los fármacos , Línea Celular Tumoral , Fragmentación del ADN/efectos de los fármacos , Humanos , Malondialdehído/metabolismo , Estrés Oxidativo/efectos de los fármacos , Extractos Vegetales/química , Poli(ADP-Ribosa) Polimerasas/metabolismoRESUMEN
The antioxidant potency of Acacia salicina extracts was investigated. Total antioxidant capacity was determined using an ABTS(+) assay. Superoxide radical scavenging was measured using riboflavin-light-nitro blue tetrazolium (NBT) assay. In addition, the content of phenols, total flavonoids and sterols were measured in the tested extracts. The petroleum ether exhibited a potent scavenging activity toward ABTS radical cations. Whereas, chloroform extract showed the highest activity against superoxides radicals and was also able to protect pKS plasmid DNA against hydroxyl radicals induced DNA damages. The antimutagenicity of these extracts was assayed using the Ames assay against Salmonella typhimurium TA98 and S. typhimurium TA 1535 tester strains at different concentrations. These extracts decreased significantly the mutagenecity induced by sodium azide (SA) and 4-nitro-o-phenylenediamine (NOP). The antioxidant and antimutagenecity activities exhibited by A. salicina depended on the chemical composition of the tested extracts.
Asunto(s)
Acacia/química , Antioxidantes/farmacología , Daño del ADN/efectos de los fármacos , Radical Hidroxilo/toxicidad , Extractos Vegetales/farmacología , Antimutagênicos/farmacología , Flavonoides/análisis , Flavonoides/farmacología , Fenoles/análisis , Fenoles/farmacología , Fenilendiaminas/toxicidad , Hojas de la Planta/química , Plásmidos/efectos de los fármacos , Salmonella typhimurium/efectos de los fármacos , Azida Sódica/toxicidad , Esteroles/análisis , Esteroles/farmacologíaRESUMEN
Antioxidant activity of isorhamnetin 3-O-neohesperidoside, isolated from the leaves of Acacia salicina, was determined by the ability of this compound to inhibit xanthine oxidase activity and to scavenge the free radical 2,2'-azino-bis (3-ethylbenzthiazoline-6-sulfonic acid) (ABTS(.-)) diammonium salt. Antigenotoxic activity was assessed using the SOS chromotest assay. This compound has the ability to scavenge the ABTS(.+) radical by a hydrogen donating mechanism. We also envisaged the study of the antioxidant effect of this compound by the enzymatic xanthine/xanthine oxidase (X/XOD) assay. Results indicated that isorhamnetin 3-O-neohesperidoside was a potent inhibitor of xanthine oxidase and superoxide anion scavengers. Moreover, this compound induced an inhibitory activity against nifuroxazide and aflatoxine B1 (AFB1) induced genotoxicity. Taken together, these observations provide evidence that isorhamnetin 3-O-neohesperidoside isolated from the leaves of A. salicina is able to protect cells against the consequences of oxidative stress.
Asunto(s)
Acacia/química , Aflatoxina B1/toxicidad , Antimutagênicos/farmacología , Antioxidantes/farmacología , Hidroxibenzoatos/toxicidad , Nitrofuranos/toxicidad , Estrés Oxidativo/efectos de los fármacos , Animales , Antimutagênicos/aislamiento & purificación , Antioxidantes/aislamiento & purificación , Enzimas Reparadoras del ADN/metabolismo , Relación Dosis-Respuesta a Droga , Flavonoles/aislamiento & purificación , Flavonoles/farmacología , Radicales Libres/química , Microsomas Hepáticos/efectos de los fármacos , Pruebas de Mutagenicidad , Extractos Vegetales/aislamiento & purificación , Extractos Vegetales/farmacología , Hojas de la Planta/química , Ratas , Xantina Oxidasa/antagonistas & inhibidoresRESUMEN
Four extracts were prepared from the leaves of Nitraria retusa; methanol, ethyl acetate, chloroform and hexane extracts. An assay for the ability of these extracts to prevent mutations induced by various oxidants in Salmonella typhimurium TA102 and TA 104 strains was conducted. These extracts from leaf parts of N. retusa showed no mutagenicity either with or without the metabolic enzyme preparation (microsome fraction). The highest protection against methylmethanesulfonate induced mutagenicity was observed with chloroform and methanol extracts with inhibition percentages of 44.93% (at 50 microg/plate in the presence of TA102 strain) and 38% (at 10 microg/plate in the presence of TA104 strain), respectively. Whereas Hexane and chloroform extracts reduced the mutagenicity induced by 2-aminoanthracene by 83.4% (using the S. typhimurium TA104 assay system) and 65.3% (using the S. typhimurium TA 102 assay system), respectively. Antioxidant activity of N. retusa extracts was determined by the ability of each extract to protect plasmid DNA against strand scission induced by hydroxyl radicals. Chloroform extract exhibited the highest ability to protect plasmid DNA against hydroxyl radical induced DNA damages and exhibited the highest antioxidant capacity, with 0.95mM trolox equivalent when tested by the ferric reducing/antioxidant method.
Asunto(s)
Antimutagênicos/farmacología , Antioxidantes/química , Magnoliopsida/química , Mutágenos/farmacología , Daño del ADN/efectos de los fármacos , ADN Bacteriano/efectos de los fármacos , ADN Bacteriano/genética , Flavonoides/química , Flavonoides/farmacología , Microsomas/química , Microsomas/metabolismo , Fenoles/química , Fenoles/farmacología , Extractos Vegetales/química , Extractos Vegetales/farmacología , Hojas de la Planta/química , Plásmidos/genética , Polifenoles , Salmonella typhimurium/efectos de los fármacos , Salmonella typhimurium/genética , Esteroles/química , Esteroles/farmacología , Taninos/química , Taninos/farmacología , TúnezRESUMEN
Four extracts were prepared from the leaves of Phlomis mauritanica: lyophilized infusion, total oligomer flavonoids, methanol, and ethyl acetate extracts. The antimutagenic properties of these extracts were investigated by assessing the inhibition of the mutagenic effects of direct-acting mutagens such as sodium azide and 4-nitrophenylenediamine and indirect-acting mutagens like aflatoxin B1 (AFB1) using the Ames assay. The four extracts prepared from P. mauritanica strongly inhibit the mutagenicity induced by AFB1 in both Salmonella typhimurium TA 100 and TA 98 assay systems. Lyophilized infusion and methanol extracts at the dose of 250 microg per plate reduced AFB1 mutagenicity by 93% and 91%, respectively, in S. typhymurium strain TA 100. We examined also the antioxidant effect of these extracts by the enzymatic xanthine/xanthine oxidase assay. Result indicated that total oligomer flavonoids and ethyl acetate and methanol extracts were potent inhibitors of xanthine oxidase activity. In contrast, lyophilized infusion, total oligomer flavonoids, and methanol extracts exhibited a high degree of superoxide anion scavenging. Our findings emphasize the potential of P. mauritanica extracts to prevent mutations and oxidant effects. Furthermore, the results presented here could be an additional argument to support the use of this species as a medicinal and dietary plant.
Asunto(s)
Compuestos de Anilina/farmacología , Antimutagênicos/farmacología , Inhibidores Enzimáticos/farmacología , Depuradores de Radicales Libres/análisis , Mutágenos/farmacología , Phlomis/química , Extractos Vegetales/farmacología , Salmonella typhimurium/efectos de los fármacos , Aflatoxina B1/farmacología , Antimutagênicos/análisis , Inhibidores Enzimáticos/análisis , Depuradores de Radicales Libres/farmacología , Salmonella typhimurium/genética , Azida Sódica/farmacología , Superóxidos/química , Xantina Oxidasa/antagonistas & inhibidores , Xantina Oxidasa/metabolismoRESUMEN
The in vitro antiproliferative, apoptotic, and antioxidant activities from leaf extracts of Moricandia arvensis, which are used in traditional cooking and medicines, were investigated. The MTT assay revealed that only TOF (total oligomer flavonoids), ethyl acetate (EA), chloroform (Chl), and petroleum ether (PE) extracts inhibited the proliferation of K562 cells. Apoptosis plays a very important role in the treatment of cancer by promoting the apoptosis of cancer cells and limiting the concurrent death of normal cells. Thus, the possible effects of M. arvensis extracts on the induction of apoptosis in human leukemic cells (K562 cells) were investigated. The electrophoretic analysis of DNA fragmentation confirms that TOF, Chl, PE, and EA extracts provoke DNA fragmentation. Using the lipid peroxidation inhibitory assay, the antioxidant capacity of M. arvensis extracts was evaluated by the ability of each extract to inhibit malondialdehyde formation. It was revealed that EA and TOF extracts are the most active in scavenging the hydroxyl radicals.
Asunto(s)
Antineoplásicos Fitogénicos/farmacología , Brassicaceae/química , Leucemia Eritroblástica Aguda/tratamiento farmacológico , Extractos Vegetales/farmacología , Antineoplásicos Fitogénicos/aislamiento & purificación , Antioxidantes/metabolismo , Apoptosis/efectos de los fármacos , Proliferación Celular/efectos de los fármacos , Fragmentación del ADN/efectos de los fármacos , Electroforesis en Gel de Agar , Humanos , Células K562 , Leucemia Eritroblástica Aguda/patología , Peroxidación de Lípido/efectos de los fármacos , Malondialdehído/metabolismo , Hojas de la Planta , Solventes/químicaRESUMEN
The Salmonella typhimurium/microsome assay is a widely used bacterial genotoxicity assay to test potential carcinogens. The aim of this work was to evaluate the mutagenic and antimutagenic activities with and without the addition of an extrinsic metabolic activation system of essential oils obtained from an aerial part of Pituranthos chloranthus harvested from different stations in Tunisia. The oils showed no mutagenicity when tested with S. typhimurium strains TA98, TA100, and TA1535. On the other hand, we showed that these essential oils reduced significantly Benzo [a] pyrene (B[a] P) and sodium-azide-induced mutagenicity. The scavenging capacity of these essential oils was also estimated by evaluating the inhibition of DPPH radical. Essential oils harvested at Medenine and Gabes in November were more effective in scavenging activity. The essential oils were tested for their antimicrobial properties against five different bacteria, and were found to be weakly active, with MIC and MBC values in the range 0.6-4 and 2.2-5 mg/mL, respectively.
Asunto(s)
Antibacterianos/farmacología , Antimutagênicos/farmacología , Microsomas Hepáticos/efectos de los fármacos , Mutágenos/farmacología , Aceites Volátiles/química , Antiinfecciosos/farmacología , Bacterias , Depuradores de Radicales Libres/farmacología , Magnoliopsida , Pruebas de Sensibilidad Microbiana , Pruebas de Mutagenicidad , Mutación , Extractos Vegetales/farmacología , Aceites de Plantas/química , Salmonella typhimurium/efectos de los fármacosRESUMEN
The extract enriched in total oligomer flavonoids (TOF), and the aqueous, methanol, and ethyl acetate extracts of Acacia salicina were investigated for their polyphenolic compound content, antioxidative activity in the nitro blue tetrazolium/riboflavin assay system, antibacterial activity against Gram-positive and Gram-negative bacterial reference strains, antigenotoxic activity tested with the Ames assay, and cytotoxic activity against the K562 human chronic myelogenous leukemia cell line and L1210 leukemia murine cells. TOF extract was effective at inhibiting nitro blue tetrazolium reduction by superoxide radical in a nonenzymatic O(2)(*-)-generating system. Significant activity against bacterial reference strains Staphylococcus aureus, Enterococcus faecalis, Salmonella enteritidis, and Salmonella typhimurium was shown with all the tested extracts. These extracts significantly decreased the genotoxicity induced by sodium azide and 4-nitro-o-phenylenediamine. A pronounced cytotoxic effect on both leukemia cell lines was detected in TOF, methanolic and ethyl acetate extracts. The antioxidant, antimicrobial, antigenotoxic, and cytotoxic activities exhibited by A. salicina depended on the chemical composition of the tested extracts.
Asunto(s)
Acacia/química , Antibacterianos/farmacología , Antimutagênicos/farmacología , Antineoplásicos Fitogénicos/farmacología , Antioxidantes/farmacología , Flavonoides/farmacología , Fenoles/farmacología , Extractos Vegetales/farmacología , Antibacterianos/uso terapéutico , Antimutagênicos/uso terapéutico , Antineoplásicos Fitogénicos/uso terapéutico , Antioxidantes/uso terapéutico , Bacterias/efectos de los fármacos , Carcinógenos , Línea Celular Tumoral , Proliferación Celular/efectos de los fármacos , Daño del ADN/efectos de los fármacos , Flavonoides/aislamiento & purificación , Flavonoides/uso terapéutico , Humanos , Leucemia/tratamiento farmacológico , Fenoles/aislamiento & purificación , Fenoles/uso terapéutico , Fenilendiaminas , Fitoterapia , Extractos Vegetales/química , Extractos Vegetales/uso terapéutico , Hojas de la Planta , Polifenoles , Azida SódicaRESUMEN
The genus Phlomis L. belongs to the Lamiaceae family and encompasses 100 species native to Turkey, North Africa, Europe and Asia. It is a popular herbal tea enjoyed for its taste and aroma. Phlomis species are used to treat various conditions such as diabetes, gastric ulcer, hemorrhoids, inflammation, and wounds. This review aims to summarize recent research on the phytochemistry and pharmacological properties of the genus Phlomis, with particular emphasis on its ethnobotanical uses. The essential oil of Phomis is composed of four chemotypes dominated by monoterpenes (alpha-pinene, limonene and linalool), sesquiterpenes (germacrene D and beta-caryophyllene), aliphalic compounds (9,12,15-octadecatrienoic acid methyl ester), fatty acids (hexadecanoic acid) and other components (trans-phytol, 9,12,15-octadecatrien-1-ol). Flavonoids, iridoids and phenylethyl alcohol constitute the main compounds isolated from Phlomis extracts. The pharmacological activities of some Phlomis species have been investigated. They are described according to antidiabetic, antinociceptive, antiulcerogenic, protection of the vascular system, anti-inflammatory, antiallergic, anticancer, antimicrobial and antioxidant properties.
Asunto(s)
Phlomis/química , Extractos Vegetales/farmacología , Analgésicos/farmacología , Etnobotánica , Flavonoides/aislamiento & purificación , Humanos , Iridoides/aislamiento & purificación , Aceites Volátiles/química , Aceites Volátiles/aislamiento & purificación , Alcohol Feniletílico/aislamiento & purificación , Extractos Vegetales/químicaRESUMEN
The lyophilized infusion, the methanol, the ethyl acetate, and the total oligomer flavonoid (TOF)-enriched extracts prepared from the dried leaves of Phlomis crinita Cav. ssp. mauritanica Munby were investigated for the contents of flavonoids, tannins, coumarines and steroids. Antibacterial activity was investigated toward five bacterial strains. An inhibitory effect was observed against Staphyllococcus aureus and Enterococcus feacalis, and the minimal inhibitory concentrations ranged from 2.5 to 5 mg/mL of extract. The tested extracts exhibit an important free radical scavenging activity toward the 1,1-diphenyl 2-picrylhydrazyl (DPPH) free radical; with IC(50) values of 30.5, 6, 32, and 31.5 microg/mL, respectively, in the presence of lyophilized infusion, the TOF, the methanol, and the ethyl acetate extracts. Genotoxic and antigenotoxic properties of the different extracts were studied by using the SOS chromotest with Escherichia coli PQ37. The lyophilized infusion and TOF extracts obtained from P. crinita ssp. mauritanica showed no genotoxicity, whereas methanol and ethyl acetate extracts are considered as marginally genotoxic. On the other hand, we showed that each extract inhibited the mutagenicity induced by aflatoxin B1 (AFB1) (10 microg/assay) and nifuroxazide (NF) (10 microg/assay). The ethyl acetate extract showed the strongest level of protection toward the genotoxicity induced by both directly and indirectly genotoxic NF and AFB1. These tests proved that the lyophilized infusion possesses an antiradical activity likewise, it showed no genotoxic effect; that is why we choose this extract to assess its antiulcerogenic activity by using an ethanol-induced ulcerogenesis model in the rat. This test demonstrates that 300 mg/kg of a P. crinita ssp. mauritanica lyophilized infusion was more effective than the reference compound, cimetidine.
Asunto(s)
Antibacterianos/farmacología , Antiulcerosos/farmacología , Phlomis/química , Extractos Vegetales/farmacología , Animales , Antibacterianos/administración & dosificación , Antibacterianos/aislamiento & purificación , Antiulcerosos/administración & dosificación , Antiulcerosos/aislamiento & purificación , Antimutagênicos/administración & dosificación , Antimutagênicos/aislamiento & purificación , Antimutagênicos/farmacología , Cimetidina/farmacología , Femenino , Depuradores de Radicales Libres/administración & dosificación , Depuradores de Radicales Libres/aislamiento & purificación , Depuradores de Radicales Libres/farmacología , Liofilización , Concentración 50 Inhibidora , Masculino , Pruebas de Sensibilidad Microbiana , Pruebas de Mutagenicidad , Extractos Vegetales/administración & dosificación , Hojas de la Planta , RatasRESUMEN
Antioxidant activity of Acacia salicina extracts was determined by the ability of each extract to inhibit lipid peroxidation, to protect against DNA strand scission induced by hydroxyl radicals, and to scavenge the free radical, 2,2'-azino-bis (3-ethylbenzothiazoline-6-sulfonic acid) (ABTS(*+)). The IC(50) values of the inhibitory activity toward lipid peroxidation of total oligomer flavonoids (TOF), methanol, ethyl acetate, and aqueous extracts were respectively 28, 52, 472, and 480 microg/mL. All extracts have the ability to scavenge the ABTS(*+) radical by a hydrogen-donating mechanism and to protect pKS plasmid DNA against hydroxyl radicals- induced DNA damage. An assay for the ability of A. salicina extracts to prevent mutations induced by various mutagens in Salmonella typhimurium TA102 and TA104 cells was conducted. TOF, methanol, ethyl acetate, and aqueous extracts from leaf parts of A. salicina showed no mutagenicity either with or without the metabolic enzymes preparation (S9). Protection against methylmethanesulfonate-induced mutagenicity was observed for TOF, methanol, and ethyl acetate extracts. Likewise, all extracts exhibited a high inhibition level of the Ames response induced by the indirect mutagen, 2-aminoanthracene. The antigenotoxic activity could be ascribed, at least in part, to their antioxidant properties, but we cannot exclude additionally mechanisms. Thus, A. salicina may serve as an ideal candidate for a cost- effective, readily exploitable natural phytochemical compound.
Asunto(s)
Acacia/química , Antimutagênicos/farmacología , Antioxidantes/farmacología , Peroxidación de Lípido/efectos de los fármacos , Extractos Vegetales/farmacología , Línea Celular Tumoral , Citoprotección/efectos de los fármacos , Relación Dosis-Respuesta a Droga , Flavonoides/farmacología , Depuradores de Radicales Libres , Humanos , Células K562 , Fitoterapia , Sustancias Protectoras/farmacologíaRESUMEN
A Total Oligomers Flavonoids (TOFs) and ethyl acetate extracts of Cyperus rotundus were analyzed, in vitro, for their antioxidant activity using several biochemical assays: the xanthine (X)/xanthine oxidase (XO), the lipid peroxidation induced by H(2)O(2) in K562 human chronic myelogenous leukemia cells and the DNA damage in pKS plasmid DNA assay induced by H(2)O(2)/UV-photolysis and for their apoptotic effect. TOF and ethyl acetate extracts were found to be efficient in inhibiting xanthine oxidase with IC(50) values of 240 and 185 microg/ml and superoxide anion with IC(50) values of 150 and 215 microg/ml, respectively. Also, all the extracts tested were effective in reducing the production of thiobarbituric acid reactive substances (TBARS) and were able to protect against H(2)O(2)/UV-photolysis induced DNA damage. The highest activity, measured as equivalents of MDA concentration, was observed in the ethyl acetate extract (MDA=2.04 nM). In addition, the data suggest that only TOF enriched extract exerts growth inhibition on K562 cells through apoptosis induction. Therefore, these extracts were subjected to further separation by chromatographic methods. Thus, three major compounds (catechin, afzelechin and galloyl quinic acid) were isolated from the TOF enriched extract and five major compounds (luteolin, ferulic acid, quercetin, 3-hydroxy, 4-methoxy-benzoic acid and 6,7-dimethoxycoumarin) from ethyl acetate extract. Their structures were determined by spectroscopic data analysis and comparison with the literature. In addition, we evaluate the biological activities of the catechin, ferulic acid and luteolin. This investigation has revealed that the luteolin was the most active in reducing the production of TBARS (MDA=1.5 nM), inhibiting significantly the proliferation of K562 cells (IC(50)=25 microg/ml) and protecting against H(2)O(2)/UV-photolysis induced DNA damage. In conclusion, the study reveals that the ability of C. rotundus to inhibit the enzyme xanthine oxidase (XO), the lipid peroxidation and to exert apoptotic effect, may explain possible mechanisms by which C. rotundus exhibits its health benefits.
Asunto(s)
Antioxidantes/farmacología , Proliferación Celular/efectos de los fármacos , Cyperus/química , Leucemia Eritroblástica Aguda/patología , Extractos Vegetales/farmacología , Daño del ADN , Electroforesis en Gel de Agar , Humanos , Peróxido de Hidrógeno/toxicidad , Células K562 , Espectroscopía de Resonancia Magnética , Sustancias Reactivas al Ácido Tiobarbitúrico/metabolismo , Rayos UltravioletaRESUMEN
The mutagenic potential of total aqueous, total oligomers flavonoids (TOF), ethyl acetate (EA), chloroform (Chl), petroleum ether (PE) and methanol (MeOH) extracts from aerial parts of Moricandia arvensis was assessed using Ames Salmonella tester strains TA100 and TA1535 with and without metabolic activation (S9), and using plasmid pBluescript DNA assay. None of the different extracts produced a mutagenic effect, except aqueous extract when incubated with Salmonella typhimurium TA100 after metabolic activation. Likewise, the antimutagenicity of the same extracts was tested using the "Ames test". Our results showed that M. arvensis extracts possess antimutagenic effects against sodium azide (SA) in the two tested Salmonella assay systems, except metabolized aqueous and PE extracts when tested with S. typhimurium TA100 assay system. Different extracts were also found to be effective in protecting plasmid DNA against the strand breakage induced by hydroxyl radicals, except PE and aqueous extracts. Antioxidant capacity of the tested extracts was evaluated using the enzymatic (xanthine/xanthine oxidase assay) (X/XOD) and the non enzymatic (NBT/Riboflavine assay) systems. TOF extract was the more effective one in inhibiting both xanthine oxidase activity and NBT reduction.