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1.
Int J Med Mushrooms ; 26(1): 17-26, 2024.
Artículo en Inglés | MEDLINE | ID: mdl-38305259

RESUMEN

In the present investigation methanol and acetone extracts of basidiocarps of mushrooms Laetiporus sulphureus and Meripilus giganteus were evaluated for their antimicrobial, cytotoxic and antioxidant/prooxidant effects. The antimicrobial potential was determined by the microdilution method against ten microorganisms. Cytotoxic effects were evaluated by MTT test, while changes of the redox status parameters (superoxide anion radical, nitrites and reduced glutathione) were determined spectrophotometrically on a human colorectal cancer cell line and human health fibroblasts cells. The results were measured 24 and 72 h after the treatment. Tested extracts exhibited moderate antimicrobial activity with MIC values from 0.004 to 20 mg/mL. The maximum antimicrobial activity was found in the methanol extracts of the M. giganteus against Bacillus subtilis, which was better than positive control. The acetone extract of M. giganteus with IC5072h = 13.36 µg/mL showed significant cytotoxic effect with strong cell selectivity (selectivity index = 37.42) against cancer human colorectal cancer cells. The tested extracts, especially M. giganteus acetone extract, induced an increase in oxidative stress parameters in tested cell lines, but significantly heightened it in human colorectal cancer cells. The obtained results suggest that these extracts, especially M. giganteus acetone extract, can be proposed as a novel source of nutraceuticals and pharmaceuticals.


Asunto(s)
Agaricales , Antiinfecciosos , Antineoplásicos , Ascomicetos , Basidiomycota , Neoplasias Colorrectales , Polyporales , Humanos , Metanol , Acetona , Antioxidantes/farmacología , Antineoplásicos/farmacología , Extractos Vegetales/farmacología
2.
Nat Prod Res ; : 1-11, 2023 Dec 15.
Artículo en Inglés | MEDLINE | ID: mdl-38099357

RESUMEN

This investigation examined the antioxidant, antimicrobial, cytotoxic, and anti-inflammatory activities of the acetone extract of the lichen Platismatia glauca (L.) W.L. Culb. & C.F. Culb. (PGAE). The phytochemical study of PGAE showed presence of seven compounds: salazinic acid, ß-orcinol carboxylic acid, 3-hydroxyphysodalic acid, physodalic acid, physodic acid, atranorin, and chloroatranorin. The antimicrobial potential was determined by microdilution which showed that S. aureus was most sensitive to the effect of PGAE with MIC value 0.312 mg/ml. Antioxidant activity was evaluated by using DPPH method. The obtained IC50 value for PGAE was 194.30 ± 3.32 µg/ml. The cytotoxic effect of the extract was evaluated by MTT test and the strongest activity was towards human epithelial carcinoma cells with IC50 value of 59.10 ± 0.46 µg/ml. The findings revealed that the application of lichen extracts decreased the paw edoema in a dose-dependent manner at 1, 2, 3, and 4 h following carrageenan administration.

3.
Bioorg Med Chem Lett ; 93: 129413, 2023 09 01.
Artículo en Inglés | MEDLINE | ID: mdl-37499986

RESUMEN

Due to the increased resistance to antibiotics, in recent years there has been a growing interest in the discovery of new antimicrobial agents from different sources. Bacteria that are resistant to most antibiotics are a global public health concern. In order to find a new antimicrobial drug, we synthesized a small series of 2,4-diketo esters and tested them on some gram-positive and gram-negative bacterial strains. Two compounds showed very good antibacterial activity against Staphylococcus aureus and Bacillus subtilis, respectively. Trichophyton mentagrophytes proved to be the most sensitive of the tested species regarding antifungal activity. Also, research was conducted on the biomolecule of bovine serum albumin. Examining these interactions, we concluded that all compounds have the appropriate binding affinity for bovine serum albumin, which is vital. Furthermore, to investigate the potential antitumor activity, interactions with DNA were carried out. Examining the interactions between our compounds and DNA using fluorescence, we concluded that all but one of the compounds interacts with the DNA molecule by intercalation. In addition, a molecular docking study was performed to investigate the binding mode of the tested compounds to DNA and bovine serum albumin. In conclusion, all the results indicate a great potential for the future application of these compounds in clinical practice in the future.


Asunto(s)
Antiinfecciosos , Ésteres , Unión Proteica , Simulación del Acoplamiento Molecular , Ésteres/farmacología , Albúmina Sérica Bovina/química , Antibacterianos/química , ADN/química , Pruebas de Sensibilidad Microbiana , Bacterias Grampositivas
4.
Int J Med Mushrooms ; 25(4): 1-15, 2023.
Artículo en Inglés | MEDLINE | ID: mdl-37075080

RESUMEN

Honey mushroom, Armillaria mellea, is an edible and medicinal lignicolous basidiomycete. In this study, we investigated the chemical composition and bioactive properties of its methanolic and acetonic extracts. The chemical characterization of extracts was done with the HPLC-DAD-MS/MS method. The results showed that potassium was the most abundant mineral; chlorogenic acid was the most abundant polyphenol; malic acid was the most abundant organic acid; and among carbohydrates, the most abundant were sorbitol, glucose, fructose, and saccharose. Antioxidative activity was assessed by DPPH (IC50 of the methanolic extract was 608.32 µg/mL and of the acetonic extract 595.71 µg/mL) and reducing power assays (the results ranged between 0.034 and 0.102 µg/mL). Total phenolic content was determined as gallic acid equivalent (methanolic extract: 4.74 mg GAE/g; acetonic extract: 5.68 mg GAE/g). The microdilution assay was used to evaluate the antimicrobial activity of the extracts, and the results ranged from 1.25 to 20 mg/mL. The antidiabetic effect of the extracts was tested by the α-amylase (the results ranged from 34.90% to 41.98%) and α-glucosidase assays (the results were in the range of 0.55-2.79%). The neuroprotective activity was explored by the acetylcholinesterase inhibition assay (the results were in the range of 1.94-7.76%). The microtetrazolium assay was used to investigate the cytotoxic activity of the extracts (the IC50 values ranged from 212.06 to > 400 µg/mL). Although some results suggest that some activities of the extracts are relatively moderate, the honey mushroom can still be considered an excellent source of food and bioactive compounds with medicinal value.


Asunto(s)
Armillaria , Miel , Serbia , Acetilcolinesterasa , Espectrometría de Masas en Tándem , Antioxidantes/farmacología , Antioxidantes/química , Extractos Vegetales/farmacología , Extractos Vegetales/química
5.
Pharmaceutics ; 14(10)2022 Oct 21.
Artículo en Inglés | MEDLINE | ID: mdl-36297686

RESUMEN

In this paper, the synthesis, characterization, and biological evaluation of the novel tetrahydropyrimidines-THPMs are described. THPMs are well-known for wide pharmacological activities such as antimicrobial, anticancer, antiviral, etc. This research includes obtained results of in vitro antimicrobial, anticancer, and α-glucosidase inhibitory activities of the eleven novel THPMs. An antibiotic assessment was done against five bacteria (two Gram-positive and three Gram-negative) and five fungi by determining the minimal inhibitory concentration (MIC), using the broth tube dilution method. The most active antibacterial compounds were 4a, 4b, and 4d, while the best antifungal activity was shown by 4e, 4f, and 4k. The lowest MIC value (0.20 mg/mL) was measured for 4e, 4f, and 4k against the Trichophyton mentagrophytes. Moreover, examining the α-glucosidase inhibitory activity revealed the compound 4g as the one with the best activity. The cytotoxic activity was performed on the tumor cell lines (HeLa, K562, and MDA-MB-231) and normal cells (MRC-5). The best antitumor activity was shown by compounds 4b and 4k against HeLa cell lines. The influence on cell cycle and mechanism of action of the most active compounds were examined too. Compound 4b had good antibacterial and anticancer activities, while 4k showed promising antifungal and anticancer activities.

6.
Int J Med Mushrooms ; 24(7): 21-40, 2022.
Artículo en Inglés | MEDLINE | ID: mdl-35993959

RESUMEN

In this study, we tested the methanolic and acetonic extracts of the edible species Meripilus giganteus for their medicinal properties. Here, we present the chemical composition, as well as the antimicrobial, antioxidant, antidiabetic, neuroprotective, and cytotoxic activities, of the aforementioned extracts. The chemical composition of the extracts was analyzed with high-performance liquid chromatography coupled with diode-array detection and tandem mass spectrometry. The studied extracts contained 13 minerals, 23 polyphenols, 11 organic acids, and 22 carbohydrates. Antimicrobial activity was tested by applying the microdilution assay, and the results ranged from 0.002 to 20 mg/mL. Antioxidant activity was studied with the DPPH assay (half-maximal inhibitory concentration = 673.42 and 712.31 µg/mL for the methanolic and acetonic extracts, respectively) and the reducing power assay (range, 0.042-0.099 µg/mL). Total phenolic content was determined as 4.86 mg gallic acid equivalents (GAE)/g for the methanolic extract and 5.06 mg GAE/g for the acetonic extract. The antidiabetic effect of the extracts was explored with the α-amylase and α-glucosidase assays, and the results ranged from 30.66% to 38.67% and from 11.06% to 17.08%, respectively. The neuroprotective properties of M. giganteus extracts were studied using the acetylcholinesterase inhibition assay, with results ranging from 4.54% to 9.31%. Cytotoxic activity was tested by applying the microtetrazolium assay, with results ranging from 196.24 to 322.83 µg/mL. Although some assays proved relatively limited activities of the M. giganteus extracts studied, they can still be considered as natural sources of bioactive compounds without side effects.


Asunto(s)
Agaricales , Antiinfecciosos , Acetilcolinesterasa , Agaricales/química , Antioxidantes/química , Ácido Gálico/análisis , Hipoglucemiantes/farmacología , Extractos Vegetales/química , Extractos Vegetales/farmacología , Polyporales , Serbia , Coloración y Etiquetado
7.
Med Chem ; 18(7): 784-790, 2022.
Artículo en Inglés | MEDLINE | ID: mdl-35249503

RESUMEN

BACKGROUND: It is known that pyrrolidinone derivates belong to a class of biologically active compounds with a broad spectrum of biological actions. Nowadays, many scientists are making an effort in the discovery of more effective ways to eliminate reactive oxygen species (ROS) that cause oxidative stress or to eliminate the harmful microorganisms from the organism in humans. Therefore, pyrrolidinones seem to be great candidates for the research of this field. METHODS: The antimicrobial activity of tested compounds was estimated by the determination of the minimal inhibitory concentration by the broth micro-dilution method against four species of bacteria and five species of fungi. The antioxidant activity was evaluated by free radical scavenging and reducing power. RESULTS: Among the tested compounds, P22 showed marked antibacterial activity on Staphylococcus aureus with a MIC value of 0.312 mg/mL. Maximum antifungal activity with MIC value 0.625 mg/mL was shown by P23 and P25 compounds against Trichophyton mentagrophytes. Tested samples showed a relatively strong scavenging activity on DPPH radical (IC50 ranged from 166.75- 727.17 µg/mL). The strongest DPPH radical scavenging activity was shown by P3 compound with an IC50 value of 166.75 µg/mL. Moreover, the tested compounds had effective reducing power. Compounds P3, P10, and P13 showed the highest reducing power than those from the other samples. Results of the interactions between DNA and P3 indicated that P3 had the affinity to displace EB from the EB-DNA complex through intercalation [Ksv = (1.4 ± 0.1) × 105 M-1], while Ka values obtained via titration of BSA with P23 or P25 [Ka = (6.2 ± 0.2) and (5.0 ± 0.2) × 105 M-1] indicate that the notable quantity of the drug can be transmitted to the cells. CONCLUSION: Achieved results indicate that our compounds are potential candidates for use as medicaments.


Asunto(s)
Antiinfecciosos , Antioxidantes , Antibacterianos/química , Antibacterianos/farmacología , Antiinfecciosos/farmacología , Antioxidantes/química , Antioxidantes/farmacología , ADN , Humanos , Pruebas de Sensibilidad Microbiana , Extractos Vegetales/farmacología , Piridinolcarbamato
8.
Med Chem ; 17(5): 519-532, 2021.
Artículo en Inglés | MEDLINE | ID: mdl-31696810

RESUMEN

BACKGROUND: In order to make some progress in discovering the more effective way to eliminate ROS which cause the oxidative stress in organism in humans and bearing in mind the fact that ethyl-2-hydroxy-4-aryl(alkyl)-4-oxo-2-butenoates (ß-diketonates) belong to a class of biologically active compounds, series of ß-diketonates were synthesized, characterized, and tested to evaluate there antioxidant activity. Further, to investigate how coordination to copper(II) ion affects the activity of ß-diketonates, appropriate complexes were synthesized and characterized. METHODS: All complexes were characterized by UV-Vis, IR, and EPR spectroscopy, MS spectrometry, and elemental analysis. Fluorescence spectroscopic method was used for investigations of the interactions between biomacromolecules (DNA or BSA) and compound 2E. Viscosity measurements and molecular docking study were performed to confirm the mode of interactions between DNA and BSA and compound 2E. RESULTS: Scavenging activity on DPPH radical revealed that compounds 2A, 2B, and 2E possess largest free radical scavenging, comparable to standard while results of superoxide anion scavenging activities of tested samples showed that maximum scavenging activity (IC50=168.92 µg/mL) was found for 2E, very similar to standard ascorbic acid, followed by 2B and 2G. Results of the interactions between biomacromolecules and 2E indicated that 2E has the affinity to displace EB from the EB-DNA complex through intercalation [Ksv = (3.7 ± 0.1) × 103 M-1], while Ka value obtained via titration of BSA with 2E [Ka = (4.2 ± 0.2) × 105 M-1], support the fact that the significant amount of the drug could be transported and distributed through the cells. CONCLUSION: All ß-diketonates exhibited better scavenging activities than their corresponding copper complexes. Among all the tested compounds, 2E gave the highest reducing power, even higher than standard ascorbic acid, while reducing power for compounds 2A and 2B was also good but lower than standard. DNA and BSA binding study for 2E showed that this compound has the potential to be used as medicament.


Asunto(s)
Complejos de Coordinación/química , ADN/metabolismo , Depuradores de Radicales Libres/química , Cetonas/química , Albúmina Sérica Bovina/metabolismo , Animales , Bovinos , Complejos de Coordinación/síntesis química , Complejos de Coordinación/metabolismo , Cobre/química , ADN/química , Depuradores de Radicales Libres/síntesis química , Depuradores de Radicales Libres/metabolismo , Cetonas/síntesis química , Cetonas/metabolismo , Simulación del Acoplamiento Molecular , Unión Proteica , Viscosidad
9.
Environ Monit Assess ; 192(11): 693, 2020 Oct 10.
Artículo en Inglés | MEDLINE | ID: mdl-33037947

RESUMEN

The subject of this paper is the possibility of using self-organizing map (SOM) in the biomonitoring studies. We used lichens as biomonitors to indicate different degrees of air quality. This research included all of 88 lichen species that was collected at 75 investigated points. These lichen species showed the different responses to air pollution. The air quality was assessed by IAP (index of atmospheric pollution) values. The IAP values were calculated for all of investigated points on the territory of four natural and one urban ecosystem. Calculated IAP values were in range of 10 to 75. On the basis of the lichen data and IAP values, we have employed SOM analysis that distinguished three clusters (A, B, and C). It presented lichen indicator species for each cluster: 16 species for cluster A, 18 species for cluster B, and two species for cluster C. This paper presents a useful method to find indicator species.


Asunto(s)
Contaminación del Aire , Líquenes , Peninsula Balcánica , Ecosistema , Monitoreo del Ambiente , Serbia
10.
J BUON ; 25(2): 1219-1229, 2020.
Artículo en Inglés | MEDLINE | ID: mdl-32521929

RESUMEN

PURPOSE: Sea macroalgae are an important source of biologically highly valuable compounds. The main aim of this study was to investigate the in vitro anticancer properties and chemical composition of the dichloromethane-methanol extract and three fractions of the Fucus spiralis from coastline of Morocco. METHODS: Fractions were made from dichloromethane:methanol (1:1) extract of Fucus spiralis: petroleum-ether, ethyl-acetate and n-butanol. Extract and fractions were screened for in vitro cytotoxicity by MTT assay against human cervical adenocarcinoma (HeLa), colorectal adenocarcinoma (LS-174T), lung carcinoma (A549), and normal human lung fibroblasts (MRC-5). Cell cycle distribution of the HeLa cells was evaluated using flow cytometry. Acridine orange (AO)-ethidium bromide (EB) staining was used to assess morphological changes of HeLa cells under fluorescence microscope. Anti-migration and anti-angiogenic properties were investigated using scratch and tube formation assays against human endothelium-derived permanent EA.hy926 cell line. Antidiabetic activity was tested using anti-α-glucosidase assay. Antimicrobial effect was tested using micro- dilution method. RESULTS: Petroleum-ether fraction оf Fucus spiralis rich in fatty acids exerted the highest cytotoxicity against HeLa cells. Ethyl-acetate and petroleum-ether fractions induced the highest accumulation of the HeLa cells in sub-G1 and G2/M phases. Extract and fractions showed proapoptotic effect on HeLa cells under fluorescent microscope. They exhibited antimigratory and antiangiogenic effects in vitro. IC50 value for α-glucosidase inhibitory activity was much stronger than standard acarbose. n-Butanol fraction exerted the highest antibacterial and antifungal activity. CONCLUSIONS: The investigation of various biological activities of the extract and fractions obtained from Fucus spiralis may suggest a promising anticancer and pharmacological potential of this edible macroalga.


Asunto(s)
Antibacterianos/uso terapéutico , Fucus/química , Microalgas/química , Neoplasias/tratamiento farmacológico , Extractos Vegetales/química , Antibacterianos/farmacología , Células HeLa , Humanos , Microscopía Fluorescente
11.
Int J Med Mushrooms ; 22(4): 347-357, 2020.
Artículo en Inglés | MEDLINE | ID: mdl-32558499

RESUMEN

Antioxidant, antimicrobial, genoprotective, anticancer, and neuroprotective potential of acetone extract of the fruiting bodies of the edible mushroom Lactarius piperatus was studied. The antioxidant activity was evaluated using different methods (DPPH radical scavenging, superoxide anion radicals scavenging, reducing power assay, and determination of total phenolic compounds). The microdilution method was used to reveal the antimicrobial potential. The genoprotective potential was determined by Comet assay. Cytotoxic activity was tested using MTT. The capacity of the extract to inhibit acetylcholinesterase was used for determining its neuroprotective potential. The received results show that L. piperatus extract possessed potent health enhancing effects. In the antioxidant activity, IC50 was 33.97 µg/mL for DPPH radicals scavenging and 22.52 µg/mL for superoxide anion radicals scavenging, whereas the absorbance for the reducing power was from 0.0510 to 0.1451. The total content of phenolic compounds in the extract was 5.08 µg PE/mg. The testing of the antimicrobial activity showed that MIC values were from 0.039 to 10 mg/mL. For Comet assay, all concentrations of extract increased the GDI values from 0.46 ± 0.05 to 0.99 ± 0.31. L. piperatus extract expressed relatively strong cytotoxic activity with IC50 values ranging from 37.83 to 65.94 µg/mL. Finally, the percentage of inhibition of acetylcholinesterase activity of tested extract was within the range 16.75-44.35%. Our results imply that the acetone extract of L. piperatus has rather strong antioxidant, antimicrobial, genoprotective, anticancer, and neuroprotective effects; thus this mushroom represents healthy food that could be used in the pharmaceutical industry and to prevent various diseases.


Asunto(s)
Basidiomycota/química , Extractos Celulares/farmacología , Sustancias Protectoras/farmacología , Antiinfecciosos/química , Antiinfecciosos/farmacología , Antineoplásicos/química , Antineoplásicos/farmacología , Extractos Celulares/química , Línea Celular Tumoral , Supervivencia Celular/efectos de los fármacos , Cuerpos Fructíferos de los Hongos/química , Humanos , Concentración 50 Inhibidora , Pruebas de Sensibilidad Microbiana , Fenoles/análisis , Fenoles/farmacología , Sustancias Protectoras/química , Serbia
12.
EXCLI J ; 19: 442-457, 2020.
Artículo en Inglés | MEDLINE | ID: mdl-32398969

RESUMEN

It is known that many edible mushrooms have important medicinal properties, including effects on different types of cancers. This is the first report regarding the neuroprotective, antimicrobial, antioxidative and anticancer activities of the acetone extract of edible mushroom Hygrophorus eburneus. Neuroprotective potential was evaluated by measuring the capacity of the extract to inhibit acetylcholinesterase. In this assay, the tested extract showed activity against acetylcholinesterase in a dose-dependent manner where the percentage of inhibition ranged from 13.19 to 46.44 %. The antimicrobial potential was determined by the microdilution method against five species of bacteria and eight species of fungi and the results of this method exhibited moderate antimicrobial activity of H. eburneus with MIC values ranging from 6.25 to 25 mg/mL. Antioxidant activity was evaluated by measuring the scavenging capacity of the tested sample on DPPH and superoxide anion radicals, by the reducing power assay and by measuring the amounts of total phenolics in extract. As a result of the study, H. eburneus extract showed a potent antioxidant activity (IC50 were 102.93 µg/mL for DPPH radical scavenging activity and 123.27 µg/mL for superoxide anion radicals scavenging) while absorbances for reducing power assay were from 0.0235 to 0.1161. The total phenolic content in the extract was 9.27 µg PE/mg. Finally, anticancer effects were evaluated by MTT test for cytotoxicity, acridine orange/ethidium bromide staining for detection of the type of cell death and wound healing assay for antimigratory effects on human colorectal cancer cell line (HCT-116) and human breast cancer cell line (MDA-MB-231). The results for cytotoxicity and apoptosis were measured after 24 and 72 h and for anti-migratory effect after 12 and 24 h. The tested H. eburneus mushroom extract expressed cell selectivity, with notable cytotoxic effects observed on HCT-116 cells, with a strong proapoptotic potential. The migration of HCT-116 cells was significantly inhibited, while MDA-MB-231 cells were less sensitive to the treatment. The results of this study revealed that the tested extract had relatively strong neuroprotective, antimicrobial, antioxidant, and anticancer effects. It suggests that this mushroom can be proposed as a novel source of nutraceuticals and pharmaceuticals.

13.
Chem Biodivers ; 14(8)2017 Aug.
Artículo en Inglés | MEDLINE | ID: mdl-28388815

RESUMEN

A small series of 1-acetyl-2-(4-alkoxy-3-methoxyphenyl)cyclopropanes was prepared, starting from dehydrozingerone (4-(4-hydroxy-3-methoxyphenyl)-3-buten-2-one) and its O-alkyl derivatives. Their microbiological activities toward some strains of bacteria and fungi were tested, as well as their in vitro cytotoxic activity against some cancer cell lines (HeLa, LS174 and A549). All synthesized compounds showed significant antimicrobial activity and expressed cytotoxic activity against tested carcinoma cell lines, but they showed no significant influence on normal cell line (MRC5). Butyl derivative is the most active on HeLa cells (IC50 = 8.63 µm), while benzyl one is active against LS174 and A549 cell lines (IC50 = 10.17 and 12.15 µm, respectively).


Asunto(s)
Antiinfecciosos/química , Estirenos/química , Células A549 , Antiinfecciosos/farmacología , Línea Celular Tumoral , Proliferación Celular/efectos de los fármacos , Cristalografía por Rayos X , Ciclopropanos/química , Ensayos de Selección de Medicamentos Antitumorales , Hongos/efectos de los fármacos , Bacterias Gramnegativas/efectos de los fármacos , Bacterias Grampositivas/efectos de los fármacos , Células HeLa , Humanos , Pruebas de Sensibilidad Microbiana , Conformación Molecular , Relación Estructura-Actividad , Estirenos/toxicidad
14.
Dalton Trans ; 45(38): 15067-15077, 2016 Sep 27.
Artículo en Inglés | MEDLINE | ID: mdl-27711668

RESUMEN

A serie of novel square pyramidal copper(ii) complexes [Cu(L)2H2O] (3a-d) with O,O-bidentate ligands [L = ethyl-2-hydroxy-4-aryl-4-oxo-2-butenoate; aryl = 3-methoxyphenyl-2a, (E)-2-phenylvinyl-2b, (E)-2-(4'-hydroxy-3'-methoxyphenyl)vinyl-2c, 3-nitrophenyl-2d, 2-thienyl-2e] were synthesized and characterized by spectral (UV-Vis, IR, ESI-MS and EPR), elemental and X-ray analysis. The antimicrobial activity was estimated by the determination of the minimal inhibitory concentration (MIC) using the broth microdilution method. The most active antibacterial compounds were 3c and 3d, while the best antifungal activity was showed by complexes 3b and 3e. The lowest MIC value (0.048 mg mL-1) was measured for 3c against Proteus mirabilis. The cytotoxic activity was tested using the MTT method on human epithelial carcinoma HeLa cells, human lung carcinoma A549 cells and human colon carcinoma LS174 cells. All complexes showed extremely better cytotoxic activity compared to cisplatin at all tested concentrations. Compound 3d expressed the best activity against all tested cell lines with IC50 values ranging from 7.45 to 7.91 µg mL-1. The type of cell death and the impact on the cell cycle for 3d and 3e were evaluated by flow cytometry. Both compounds induced apoptosis and S phase cell cycle arrest. The interactions between selected complexes (3d and 3e) and CT-DNA or bovine serum albumin (BSA) were investigated by the fluorescence spectroscopic method. Competitive experiments with ethidium bromide (EB) indicated that 3d and 3e have a propensity to displace EB from the EB-DNA complex through intercalation suggesting strong competition with EB [Ksv = (1.4 ± 0.2) and (2.9 ± 0.1) × 104 M-1, respectively]. Ksv values indicate that these complexes bind to DNA covalently and non-covalently. The achieved results in the fluorescence titration of BSA with 3d and 3e [Ka = (2.9 ± 0.2) × 106 and (2.5 ± 0.2) × 105 M, respectively] showed that the fluorescence quenching of BSA is a result of the formation of the 3d- and 3e-BSA complexes. The obtained Ka values are high enough to ensure that a significant amount of 3d and 3e gets transported and distributed through the cells.


Asunto(s)
Antineoplásicos , Complejos de Coordinación , Cobre , Compuestos de Vinilo , Antibacterianos/química , Antibacterianos/farmacología , Antifúngicos/química , Antifúngicos/farmacología , Antineoplásicos/química , Antineoplásicos/farmacología , Apoptosis/efectos de los fármacos , Bacterias/efectos de los fármacos , Bacterias/crecimiento & desarrollo , Ciclo Celular/efectos de los fármacos , Línea Celular Tumoral , Supervivencia Celular/efectos de los fármacos , Complejos de Coordinación/química , Complejos de Coordinación/farmacología , Cobre/química , Cobre/farmacología , ADN/química , Hongos/efectos de los fármacos , Hongos/crecimiento & desarrollo , Humanos , Albúmina Sérica Bovina/química , Compuestos de Vinilo/química , Compuestos de Vinilo/farmacología
15.
Int J Med Mushrooms ; 18(5): 397-404, 2016.
Artículo en Inglés | MEDLINE | ID: mdl-27649601

RESUMEN

The bioactivity of Ganoderma lucidum basidiocarps has been well documented, but there are no data on the medicinal properties of its submerged cultivation broth nor on the other species of the genus Ganoderma. Thus the aim of this study was to test the potential antimicrobial and antioxidant activity of fermentation broth obtained after submerged cultivation of G. applanatum, G. carnosum, and G. lucidum. DPPH· scavenging ability, total phenols, and flavonoid contents were measured to determine the antioxidative potential of Ganoderma spp. fermentation filtrates, whereas their antimicrobial potential was studied using the microdilution method. DPPH· scavenging activity of G. lucidum fermentation filtrates was significantly higher than that of G. applanatum and G. carnosum, with the maximum (39.67%) obtained from strain BEOFB 432. This filtrate also contained the highest concentrations of phenols (134.89 µg gallic acid equivalents/mL) and flavonoids (42.20 µg quercetin equivalent/mL). High correlations between the activity and phenol content in the extracts showed that these compounds were active components of the antioxidative activity. G. lucidum strain BEOFB 432 was the most effective antibacterial agent, whereas strain BEOFB 434 has proven to be the most effective antifungal agent. The study showed that Ganoderma spp. fermentation filtrates are novel potent antioxidative and antimicrobial agents that could be obtained more quickly and cheaper than basidiocarps.


Asunto(s)
Antibacterianos/farmacología , Antifúngicos/farmacología , Antioxidantes/farmacología , Medios de Cultivo/química , Ganoderma/química , Antibacterianos/química , Antifúngicos/química , Antioxidantes/química , Bacterias/efectos de los fármacos , Fermentación , Hongos/efectos de los fármacos , Cetoconazol/farmacología , Estreptomicina/farmacología , Consumo de Alcohol en Menores
16.
J Food Sci Technol ; 53(6): 2804-16, 2016 Jun.
Artículo en Inglés | MEDLINE | ID: mdl-27478237

RESUMEN

The aim of this study was to investigate antioxidant, antimicrobial and anticancerous activity of Melanelia subaurifera and Melanelia fuliginosa. The phytochemical analysis was determined by HPLC-UV method. Antioxidant activity was evaluated by DPPH and reducing power assay while antimicrobial activity was determined by minimal inhibitory concentration. The cytotoxic activity was tested using MTT method. The method for quantification of 2'-O-methyl anziaic acid and lecanoric acid in these lichens using RF-HPLC was also developed and validated. The depsides (lecanoric acid, gyrophoric acid, atranorin, anziaic acid and 2'-O-methyl anziaic acid), and dibenzofurane (usnic acid) were identified in these lichens. The antioxidant activity (IC50) of lichens extracts ranged from 121.52 to 424.51 µg/ml. 2'-O-Methyl anziaic acid showed the highest antimicrobial activity with MIC ranging from 0.0625 to 1 mg/ml. M. subaurifera extract showed the highest cytotoxic activity against the tested cell lines (IC50 = 9.88 to 31.64 µg/ml).

17.
Curr Pharm Biotechnol ; 17(7): 651-8, 2016.
Artículo en Inglés | MEDLINE | ID: mdl-27033512

RESUMEN

This paper studies the phytochemical analysis of the acetone extracts of the Ramalina fraxinea and Ramalina fastigiata lichens and the antioxidant, antimicrobial and antitumour activities of these species and their constituents. The phytochemical analysis of two Ramalina species was evaluated using HPLC-UV test. The depsides (evernic acid, obtusatic acid, sekikaic acid and atranorin), depsidones (protocetraric acid) and dibenzofurane (usnic acid) were identified from these lichens. Antioxidant activity was evaluated by DPPH assay, reducing power assay and by measuring the amounts of total phenolics in extracts. Antimicrobial activity was tested towards five bacterial and 10 fungal species, using broth microdilution method to determine the minimum inhibitory concentration. Cytotoxic activity was tested using MTT method on the human epithelial carcinoma (Hela), human lung carcinoma (A549) and human colon carcinoma (LS174) cells. As a result of the study, tested samples showed strong free radical scavenging activity with I50 values within the range of 285.45-423.51 µg/mL. Absorbance for reducing power was found to be from 0.0043 to 0.1747. The total amount of phenol concentrations in extracts of Ramalina fraxinea and Ramalina fastigiata was 32.63 and 33.49 µg PE/mg, respectively. Methyl evernate showed the strongest antimicrobial properties with the least measured MIC value being 0.125 mg/mL. In addition, all samples exhibited strong anticancer activities against tested cells (I50 values were between 24.63 and 161.37 µg/mL). These results indicate that lichen appears to be a possible natural biopharmaceutical.


Asunto(s)
Glutamatos/metabolismo , Glutamatos/farmacología , Líquenes/metabolismo , Antiinfecciosos/química , Antiinfecciosos/metabolismo , Antiinfecciosos/farmacología , Antineoplásicos Fitogénicos/química , Antineoplásicos Fitogénicos/metabolismo , Antineoplásicos Fitogénicos/farmacología , Antioxidantes/química , Antioxidantes/metabolismo , Antioxidantes/farmacología , Supervivencia Celular/efectos de los fármacos , Supervivencia Celular/fisiología , Hongos/efectos de los fármacos , Glutamatos/química , Células HeLa , Humanos , Pruebas de Sensibilidad Microbiana/métodos , Fenoles/química , Fenoles/metabolismo , Fenoles/farmacología
18.
Cytotechnology ; 68(4): 999-1008, 2016 Aug.
Artículo en Inglés | MEDLINE | ID: mdl-25682053

RESUMEN

The methanol extract of the lichen Lasallia pustulata was tested for genotoxic, antioxidant, antimicrobial and anticancer activities. We did this using a cytokinesis block micronucleus (MN) assay on peripheral blood lymphocytes, by measuring free radical and superoxide anion scavenging activity, reducing power, determining of total phenolic compounds and determining the total flavonoid content, measuring the minimal inhibitory concentration by the broth microdilution method against five species of bacteria and five species of fungi and by using the microculture tetrazolium test on FemX (human melanoma) and LS174 (human colon carcinoma) cell lines. As a result of this study, we found that the methanol extract of L. pustulata did not modify the frequency of the MN and nuclear division index in comparison to untreated cells (p > 0.05). These results revealed that the methanol extract had moderate free radical scavenging activity with IC50 values of 395.56 µg/mL. Moreover, the extract tested had effective reducing power and superoxide anion radical scavenging. The values of the minimum inhibitory concentration against the tested microorganisms ranged from 0.625 to 20 mg/mL. In addition, the extract tested had strong anticancer activity against both cell lines with IC50 values of 46.67 and 71.71 µg/mL.

19.
J Food Drug Anal ; 24(3): 477-484, 2016 07.
Artículo en Inglés | MEDLINE | ID: mdl-28911552

RESUMEN

This study is designed for the determination of metal concentrations, antioxidant, antimicrobial, and anticancer potential of two edible mushrooms Lactarius deliciosus and Macrolepiota procera. Concentrations of nine metals are determined and all metals are present in the allowable concentrations in the tested mushrooms except Cd in M. procera. Antioxidant activity was evaluated by free radical scavenging and reducing power. M. procera extract had more potent free radical scavenging activity (IC50=311.40 µg/mL) than L. deliciosus extract. Moreover, the tested extracts had effective reducing power. The total content of phenol in the extracts was examined using Folin-Ciocalteu reagent and obtained values expressed as pyrocatechol equivalents. Further, the antimicrobial potential was determined with a microdilution method on 15 microorganisms. Among the tested species, extract of L. deliciosus showed a better antimicrobial activity with minimum inhibitory concentration values ranging from 2.5 mg/mL to 20 mg/mL. Finally, the cytotoxic activity was tested using the 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide method on human epithelial carcinoma HeLa cells, human lung carcinoma A549 cells, and human colon carcinoma LS174 cells. Extract of both mushrooms expressed similar cytotoxic activity with IC50 values ranging from 19.01 µg/mL to 80.27 µg/mL.


Asunto(s)
Agaricales , Antiinfecciosos , Antioxidantes , Células HeLa , Humanos , Metales
20.
Acta Biol Hung ; 66(4): 374-84, 2015 Dec.
Artículo en Inglés | MEDLINE | ID: mdl-26616370

RESUMEN

In the present investigation the acetone extracts of three macroalgae, Cystoseira amentacea, Cystoseira barbata and Cystoseira compressa, were tested for antioxidant, antimicrobial and cytotoxic potential. As a result of the study, C. amentacea extract had more potent free radical scavenging activity (IC50 = 409.81 µg/mL) than C. barbata and C. compressa extracts. For reducing power, measured values of absorbance varied from 0.0352 to 0.8873. The IC50 values for superoxide anion scavenging activity for different extracts were 521.45-976.62 µg/mL. Total phenol and flavonoid contents in extracts were 39.96-81.28 µg PE/mg and 20.85-64.58 µg RE/mg respectively. Further, all three Cystoseira species exhibited a similar antimicrobial activity. The lowest MIC value (0.312 mg/mL) was shown in the extract obtained from C. compressa against Bacillus subtilis. Finally, extract of C. amentacea expressed the strongest cytotoxic activity toward tested cell lines with IC50 values ranging from 94.72 to 186.55 µg/mL. Based on these results, it can be stated that the tested macroalgae can be used as potential natural antioxidants and antimicrobial and cytotoxic agents.


Asunto(s)
Antiinfecciosos/química , Antioxidantes/química , Algas Marinas/química , Antiinfecciosos/aislamiento & purificación , Antioxidantes/aislamiento & purificación , Bacillus subtilis/efectos de los fármacos , Línea Celular , Flavonoides/química , Flavonoides/aislamiento & purificación , Humanos , Fenoles/química , Fenoles/aislamiento & purificación
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