RESUMO
Colorectal cancer (CRC) is the third most common type of cancer worldwide. Its treatment options have had a limited impact on cancer remission prognosis. Therefore, there is an ongoing need to discover novel anti-cancer agents. Medicinal plants have gained recognition as a source of anti-cancer bioactive compounds. Recently, ethanolic extract of L. virginicum stems ameliorated dinitrobenzene sulfonic acid (DNBS)-induced colitis by modulating the intestinal immune response. However, no scientific study has demonstrated this potential cytotoxic impact on colon cancer cells. The objective of this study was to evaluate the cytotoxic effect of the methanolic extract of L. virginicum (ELv) on a human colorectal adenocarcinoma cell line (Caco-2) and to identify and quantify the phenolic compounds present in ELv extracts by liquid chromatography-mass spectrometry analysis. The cytotoxic activity was assessed using cell viability assays by reduction in the compound 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide (MTT) and lactate dehydrogenase (LDH). MTT and LDH assays revealed that the ELv decreases cell viability in the Caco-2 cell line in a concentration-dependent manner. Cell death was a result of DNA fragmentation and p53-mediated apoptosis. Eight phenolic acids and five flavonoids were identified and quantified in the stems. In conclusion, our findings demonstrate that the extract of L. virginicum possesses cytotoxic properties on Caco-2 cell line, suggesting that it could be a potential source of new drugs against CRC.
Assuntos
Apoptose , Sobrevivência Celular , Lepidium , Metanol , Extratos Vegetais , Proteína Supressora de Tumor p53 , Humanos , Células CACO-2 , Extratos Vegetais/farmacologia , Extratos Vegetais/química , Apoptose/efeitos dos fármacos , Proteína Supressora de Tumor p53/metabolismo , Sobrevivência Celular/efeitos dos fármacos , Metanol/química , Lepidium/química , Neoplasias Colorretais/tratamento farmacológico , Neoplasias Colorretais/metabolismo , Neoplasias Colorretais/patologia , Antineoplásicos Fitogênicos/farmacologia , Antineoplásicos Fitogênicos/química , Fenóis/farmacologia , Fenóis/químicaRESUMO
PURPOSE: For growth of methylotrophic yeast, glycerol is usually used as a carbon source. Glucose is used in some cases, but not widely consumed due to strong repressive effect on AOX1 promoter. However, glucose is still considered as a carbon source of choice since it has low production cost and guarantees growth rate comparable to glycerol. RESULTS: In flask cultivation of the recombinant yeast, Pichia pastoris GS115(pPIC9K-appA38M), while methanol induction point(OD600) and methanol concentration significantly affected the phytase expression, glucose addition in induction phase could enhance phytase expression. The optimal flask cultivation conditions illustrated by Response Surface Methodology were 10.37 OD600 induction point, 2.02 h before methanol feeding, 1.16% methanol concentration and 40.36µL glucose feeding amount(for 20 mL culture volume) in which the expressed phytase activity was 613.4 ± 10.2U/mL, the highest activity in flask cultivation. In bioreactor fermentation, the intermittent glucose feeding showed several advantageous results such as 68 h longer activity increment, 149.2% higher cell density and 200.1% higher activity compared to the sole methanol feeding method. These results implied that remaining glucose at induction point might exhibit a positive effect on the phytase expression. CONCLUSION: Glucose intermittent feeding could be exploited for economic phytase production and the other recombinant protein expression by P. pastoris GS115.
Assuntos
6-Fitase , Reatores Biológicos , Fermentação , Glucose , Metanol , Proteínas Recombinantes , 6-Fitase/genética , 6-Fitase/metabolismo , Glucose/metabolismo , Proteínas Recombinantes/genética , Proteínas Recombinantes/metabolismo , Metanol/metabolismo , Reatores Biológicos/microbiologia , Meios de Cultura/química , Meios de Cultura/metabolismo , Saccharomycetales/genética , Saccharomycetales/metabolismo , Saccharomycetales/crescimento & desenvolvimento , Pichia/genética , Pichia/metabolismo , Pichia/crescimento & desenvolvimento , Expressão GênicaRESUMO
INTRODUCTION: Justicia pectoralis Jacq. is traditionally applied in folk medicine in Brazil and in several Latin American countries. The leaves are used in tea form, especially in the treatment of respiratory disorders, acting as an expectorant. It also has activity in gastrointestinal disorders, and it is anti-inflammatory, antioxidant, sedative, and estrogenic, among others. AIMS: To investigate the gastroprotective activity of the methanol extract of the leaves of Justicia pectoralis Jacq. (MEJP) in different experimental models of gastric ulcers. MATERIALS AND METHODS: The adult leaves of Justicia pectoralis Jacq. were collected and cultivated in beds, with an approximate spacing of 40 × 40 cm, organic fertilization, irrigation with potable water and without shelter from light. The MEJP was prepared from the dried and pulverized leaves and concentrated under reduced pressure in a rotary evaporator. For the experimental model of gastric ulcer, Swiss male albino mice were used. The inputs used in the experiment were MEJP at three different concentrations (250, 500 and 1000 mg/kg p.o.), cimetidine (50 mg/kg p.o.), indomethacin (50 mg/kg s.c.) and vehicle (10 mL/kg p.o.). RESULTS: MEJP (250, 500 and 1000 mg/kg p.o.) demonstrated gastroprotective activity, with levels of protection of 45.65%, 44.80% and 40.22%, respectively, compared to the control (vehicle). Compared with cimetidine (48.29%), MEJP showed similar gastroprotective activity. CONCLUSIONS: This study demonstrated the gastroprotective activity of MEJP and contributes to validate the traditional use the species for gastric disorders and provides a pharmacological basis for its clinical potential.
Assuntos
Extratos Vegetais , Folhas de Planta , Úlcera Gástrica , Animais , Extratos Vegetais/farmacologia , Camundongos , Úlcera Gástrica/tratamento farmacológico , Úlcera Gástrica/prevenção & controle , Folhas de Planta/química , Masculino , Antiulcerosos/farmacologia , Metanol/química , Justicia/química , Modelos Animais de Doenças , Cimetidina/farmacologia , Acanthaceae/química , Indometacina , Brasil , Mucosa Gástrica/efeitos dos fármacos , Mucosa Gástrica/patologiaRESUMO
In the context of the increasing global use of ethanol biofuel, this work investigates the concentrations of ethanol, methanol, and acetaldehyde, in both the gaseous phase and rainwater, across six diverse urban regions and biomes in Brazil, a country where ethanol accounts for nearly half the light-duty vehicular fuel consumption. Atmospheric ethanol median concentrations in São Paulo (SP) (12.3 ± 12.1 ppbv) and Ribeirão Preto (RP) (12.1 ± 10.9 ppbv) were remarkably close, despite the SP vehicular fleet being â¼13 times larger. Likewise, the rainwater VWM ethanol concentration in SP (4.64 ± 0.38 µmol L-1) was only 26 % higher than in RP (3.42 ± 0.13 µmol L-1). This work demonstrated the importance of evaporative emissions, together with biomass burning, as sources of the compounds studied. The importance of biogenic emissions of methanol during forest flooding was identified in campaigns in the Amazon and Atlantic forests. Marine air masses arriving at a coastal site led to the lowest concentrations of ethanol measured in this work. Besides vehicular and biomass burning emissions, secondary formation of acetaldehyde by photochemical reactions may be relevant in urban and non-urban regions. The combined deposition flux of ethanol and methanol was 6.2 kg ha-1 year-1, avoiding oxidation to the corresponding and more toxic aldehydes. Considering the species determined here, the ozone formation potential (OFP) in RP was around two-fold higher than in SP, further evidencing the importance of emissions from regional distilleries and biomass burning, in addition to vehicles. At the forest and coastal sites, the OFP was approximately 5 times lower than at the urban sites. Our work evidenced that transition from gasoline to ethanol or ethanol blends brings the associated risk of increasing the concentrations of highly toxic aldehydes and ozone, potentially impacting the atmosphere and threatening air quality and human health in urban areas.
Assuntos
Acetaldeído , Poluentes Atmosféricos , Monitoramento Ambiental , Etanol , Metanol , Chuva , Brasil , Acetaldeído/análise , Etanol/análise , Metanol/análise , Poluentes Atmosféricos/análise , CidadesRESUMO
The human head lice Pediculus humanus capitis (De Geer) (Phthiraptera: Pediculidae) are strict, obligate human ectoparasites that spends their entire life cycle in the host and cause skin irritation and derived infections. Despite the health-related importance, few studies have evaluated the chemical communication among these insects. Here, we evaluate the response of lice of both sexes to cuticular extracts using two solvents of different polarity (hexane and methanol). Cuticular extracts that elicited an attraction response towards head lice were analysed by gas chromatography-mass spectrometry (GC-MS) to determine the cuticular lipid profile. Both lice sexes were attracted to the hexane extracts but not the methanol extracts, suggesting the non-polarity of the compounds present in the cuticle. Chemical analyses of hexane extracts from males and females showed high similarity in major compounds. This study provides the first evidence that lice respond to cuticle extracts, which may be important to understand aggregation behaviour.
Assuntos
Hexanos , Pediculus , Animais , Feminino , Masculino , Pediculus/efeitos dos fármacos , Pediculus/química , Hexanos/química , Cromatografia Gasosa-Espectrometria de Massas , Metanol/química , Comportamento Animal/efeitos dos fármacosRESUMO
The objective of the study was to carry out phytochemical prospection through colorimetric tests to determine the groups of secondary metabolites and also to determine the total content of phenolic compounds (TPC) present in plant extracts methanol (ME), ethyl acetate (EAE), hexane (HE) and dichloromethane (DE) from the leaves of Myrsine umbellata, as well as to investigate the antimicrobial activity against twelve standard ATCC strains by the broth microdilution technique; the antioxidant potential by the DPPH method and the ABTS method and the antibiofilm potential on the biofilm biomass of standard bacteria by the crystal violet technique and tetrazolium salt reduction (MTT) assay. Phytochemical prospection detected the presence of saponins, steroids, alkaloids, anthocyanins, anthocyanidins, flavonoids, and tannins. The results of the quantitative phytochemical estimation revealed a higher content of total phenolics in DE (280.24 ± 0.037 µM GAE g ext. -1) followed by ME (159.01 ± 0.031 µM GAE g ext. -1). The ME showed the best biological activities when compared to the other extracts tested. We observed antimicrobial activity against Gram-positive Staphylococcus epidermidis strain (MIC 3.12 and MBC 6.25), antioxidant percentage of 92.58% against the DPPH radical and 420.31 µM Trolox g ext. -1 against the ABTS radical, finally showed antibiofilm action against Gram-positive strain Staphylococcus aureus, with eradication of the biomass in 92.58%. The results suggest that EM from M. umbellata represents an alternative source of plant bioactives for the development of natura products.
Assuntos
Anti-Infecciosos , Benzotiazóis , Myrsine , Ácidos Sulfônicos , Antocianinas , Antioxidantes/farmacologia , Metanol , Fenóis/farmacologia , Compostos Fitoquímicos/farmacologia , Anti-Infecciosos/farmacologiaRESUMO
We report a case of acute methanol toxicity with unique optical coherence tomography findings. A 56-year-old man was referred to our ophthalmology clinic with a history of handmade vodka consumption and vision loss. On ophthalmologic examination, his vision was 20/100 in his right eye and 20/200 in his left eye. Bilateral mild optic disk hyperemia was detected on fundus examination. Because of the severity of systemic symptoms in such cases, it is very difficult to include optical coherence tomography in the ophthalmologic examination. However, we managed to perform optical coherence tomography and recorded shallow subretinal fluid and a prominent middle limiting membrane sign as acute retinal structural changes in the patient. The patient was treated with hemodialysis, intravenous ethanol, and sodium bicarbonate. On the fourth day of treatment, visual acuity improved to 20/20 in both eyes. In addition, the prominent middle limiting membrane sign and subretinal fluid disappeared. In this unusual case, retinal pigment epithelium damage and retinal ischemia may have contributed to the prominent middle limiting membrane and subretinal fluid, which are novel optical coherence tomography findings of methanol toxicity.
Assuntos
Doenças Retinianas , Tomografia de Coerência Óptica , Masculino , Humanos , Pessoa de Meia-Idade , Tomografia de Coerência Óptica/métodos , Metanol , Retina/diagnóstico por imagem , Doenças Retinianas/induzido quimicamente , Doenças Retinianas/diagnóstico por imagem , Fundo de Olho , AngiofluoresceinografiaRESUMO
BACKGROUND: The development of analgesic and anti-inflammatory drugs plays a crucial role in modern medicine, aiming to alleviate pain and reduce inflammation in patients. Opioids and nonsteroidal anti-inflammatory drugs are groups of drugs conventionally used to treat pain and inflammation, but a wide range of adverse effects and ineffectiveness in some pathological conditions leads us to search for new drugs with analgesic and anti-inflammatory properties. OBJECTIVES: In this regard, the authors intend to investigate the ((2s,6s)-6-ethyl-tetrahydro-2h-pyran- 2-yl) methanol compound (LS20) on pain and acute inflammation. METHODS: Male Swiss mice were evaluated using acetic acid-induced abdominal writhing, formalin, and tail-flick as models of nociceptive evaluation and edema paw, air pouch and cell culture as models of inflammatory evaluation besides the rotarod test for assessment of motor impairment. RESULTS: The compound showed an effect on the acetic acid-induced abdominal writhing, formalin and tail-flick tests. Studying the mechanism of action, reversion of the antinociceptive effect of the compound was observed from previous intraperitoneal administration of selective and non-selective opioid antagonists on the tail flick test. In addition, the compound induced an antiedematogenic effect and reduced leukocyte migration and the production of pro-inflammatory cytokines in the air pouch model. LS20 was able to maintain cell viability, in addition to reducing cell production of TNF-α and IL-6. CONCLUSION: In summary, the LS20 compound presented an antinociceptive effect, demonstrating the participation of the opioid system and an anti-inflammatory effect related to the inhibition of pro-inflammatory cytokine production. The compound also demonstrated safety at the cellular level.
Assuntos
Analgésicos , Anti-Inflamatórios , Dor , Piranos , Animais , Masculino , Camundongos , Analgésicos/farmacologia , Analgésicos/uso terapêutico , Piranos/farmacologia , Anti-Inflamatórios/farmacologia , Anti-Inflamatórios/uso terapêutico , Dor/tratamento farmacológico , Humanos , Inflamação/tratamento farmacológico , Metanol/química , Ácido Acético , Edema/tratamento farmacológico , Edema/induzido quimicamente , Citocinas/metabolismoRESUMO
The study aimed to evaluate the insecticidal activity of extracts of edible mushrooms Pleurotus ostreatus and Lentinula edodes against Rhyssomatus nigerrimus. Methanol:water extracts (70:30) of P. ostreatus and L. edodes were made and evaluated in two in vitro tests (exposure and immersion toxic effect) against R. nigerrimus. Subsequently, the toxicity test of the extracts against Artemia salina was evaluated. These extracts were subjected to colorimetric tests and gas chromatography-mass spectrometry. The results showed a mortality effect against R. nigerrimus of 50% for the P. ostreatus 2 extracts at a concentration of 20% in the immersion test. Likewise, in the toxic effect test, 90% mortality was observed after five days of exposure to a concentration of 10%. On the other hand, for the toxicity test, the extract that showed the values with the highest mortality against A. salina was P. ostreatus, starting with 80% mortality at 100µg/mL. The functional groups present in the extracts were saponins, coumarins, and alkaloids. Furthermore, the presence of more than 7 compounds in the mushroom extracts evaluated is reported. This study demonstrates the insecticidal activity of P. ostreatus and L. edodes fungal extracts and indicates the importance of using different in vitro tests to elucidate the mechanism of action for future studies.
Assuntos
Artrópodes , Inseticidas , Pleurotus , Cogumelos Shiitake , Gorgulhos , Animais , Metanol , ArtemiaRESUMO
Colorectal cancer is a widespread neoplasia with high ratios of chemoresistance. Phytochemicals in plant-based extracts could be useful to treat colorectal cancer, and/or reduce chemoresistance. Methanolic extract of avocado mesocarp (MEAM) has demonstrated antitumoral properties, depending on the fruit ripening stage (RS). The aim of this study was to analyze the effects of methanolic extracts of "Hass" avocado fruit at different RS on cytotoxicity, antioxidative, anti-inflammatory, anti-invasive, cell cycle, and epithelial-mesenchymal transition inhibition in colorectal adenocarcinoma cell line HT29. The MEAM showed an increasing concentration of total phenolic compounds as the RS progressed, which was correlated with antioxidant capacity measured by the Ferric Reducing Antioxidant Power assay but not with the 2.2-diphenyl-1-picrylhydrazyl assay. The specific phenolic compounds of MEAM were determined by high-performance liquid chromatography, and it was found that concentrations of epicatechin decreased while concentrations of chlorogenic acid increased as the RS progressed. The HT29 cell line was treated with MEAM for 48 h, and all MEAM had a cytotoxic effect, reported by MTT assay, nevertheless, the strongest effect was associated with the presence of chlorogenic acid. MEAM induced apoptosis and cell cycle arrest in phase G0/G1, reported by flow cytometry. Moreover, MEAM inhibited cell migration evidenced by the wound healing assay. On the other hand, MEAM significantly reduced expression of mRNA of tumor necrosis factor-alpha and cyclooxygenase 2. These effects comprise important inhibition of some hallmarks of cancer. This, in turn, may provide interesting guidelines for developing antitumoral intervention agents.
Assuntos
Antineoplásicos , Neoplasias Colorretais , Persea , Humanos , Frutas/química , Antioxidantes/metabolismo , Persea/química , Metanol , Ácido Clorogênico/análise , Extratos Vegetais/química , Células HT29 , Neoplasias Colorretais/tratamento farmacológicoRESUMO
Renewable resources have stood out as raw materials in producing biofuels. This study aimed to evaluate the parameters of alcohol transesterification (ethanol and methanol) and localization of collection of aquatic macrophyte Eichhornia crassipes (Mart.) Solms in the production of biodiesel by in situ transesterification. E. crassipes was collected in Dourados and Corumbá (Brazil) municipalities. The fatty acid ester composition of the biodiesel was characterized and quantified by gas chromatography. The biodiesel properties were estimated using the BiodieselAnalyzer© program prediction. The ethyl transesterification resulted in higher yields, but the localization of collection was the most relevant parameter in biodiesel production according to the Permutation Multivariate Analysis of Variance. The simulation and comparison of the physical-chemical properties of E. crassipes biodiesel and BD 100 (commercial biodiesel) were promising for commercial application.
Assuntos
Eichhornia , Biocombustíveis , Eichhornia/química , Esterificação , Etanol , MetanolRESUMO
The present study shows the untargeted metabolite profiling and inâ vitro antibacterial, cytotoxic, and nitric oxide (NO) inhibitory activities of the methanolic leaves extract (MLE) and methanolic stem extract (MSE) of Erythroxylum mexicanum, as well as the fractions from MSE. Using ultra-high performance liquid chromatography/quadrupole time-of-flight tandem mass spectrometry (UHPLC-QTOF-MS/MS), a total of 70 metabolites were identified; mainly alkaloids in the MLE, while the MSE showed a high abundance of diterpenoids. The MSE fractions exhibited differential activity against Gram-positive bacteria. Notably, the hexane fraction (HSF) against Streptococcus pyogenes ATCC 19615 (MIC=62.5â µg/mL) exhibited a bactericidal effect. The MSE fractions exhibited cytotoxicity against all cancer cell lines tested, with selectivity towards them compared to a noncancerous cell line. Particularly, the HSF and chloroform fraction (CSF) showed the highest cytotoxicity against prostate cancer (PC-3) cells, with IC50 values of 19.9 and 18.1â µg/mL and selectivity indexes of 3.8 and 4.2, respectively. Both the HSF and ethyl acetate (EASF) fractions of the MSE inhibited NO production in RAW 264.7 macrophages, with NO production percentages of 50.0 % and 51.7 %, respectively, at a concentration of 30â µg/mL. These results indicated that E. mexicanum can be a source of antibacterial, cytotoxic, and anti-inflammatory metabolites.
Assuntos
Antineoplásicos , Espectrometria de Massas em Tandem , Masculino , Humanos , Óxido Nítrico , Extratos Vegetais/química , Cromatografia Líquida de Alta Pressão , Antibacterianos/farmacologia , Antineoplásicos/farmacologia , Metanol/químicaRESUMO
In this study, we specifically focused on the crude methanolic leaf extract of Byrsonima coccolobifolia, investigating its antifungal potential against human pathogenic fungi and its antiviral activity against COVID-19. Through the use of high-performance liquid chromatography coupled with electrospray ionization ion trap tandem mass spectrometry, direct infusion electrospray ionization ion trap tandem mass spectrometry, and chromatographic dereplication procedures, we identified galloyl quinic acid derivatives, catechin derivatives, proanthocyanidins, and flavonoid glycosides. The broth dilution assay revealed that the methanolic leaf extract of B. coccolobifolia exhibits antifungal activity against Cryptococcus neoformans (IC50 = 4 µg/mL). Additionally, docking studies were conducted to elucidate the interactions between the identified compounds and the central residues at the binding site of biological targets associated with COVID-19. Furthermore, the extract demonstrated an in vitro half-maximum effective concentration (EC50 = 7 µg/mL) and exhibited significant selectivity (>90%) toward SARS-CoV-2.
Assuntos
COVID-19 , Extratos Vegetais , Humanos , Extratos Vegetais/farmacologia , Extratos Vegetais/química , Antifúngicos , Estrutura Molecular , SARS-CoV-2 , Espectrometria de Massas por Ionização por Electrospray/métodos , Metanol , Antivirais/farmacologia , Cromatografia Líquida de Alta Pressão/métodosRESUMO
Cost is the crucial impediment in commercializing microalgal biodiesel. Therefore, cultivating microalgae in cost-effective nutrients reduces the upstream process cost remarkably. Thus, in this study, sugar cane bagasse hydrolysate (SBH) as a lucrative carbon supplement for Chlorococcum sp. and subsequent lipid extraction via an optimized solvent system for biodiesel production was investigated. Characterization of SBH revealed the presence of various monosaccharides and other sugar derivatives such as glucose, fructose, xylose, arabinose, etc. The maximum dry cell weight of 1.7 g/L was estimated in cultures grown in 10 mL SBH. Different solvents such as diethyl ether (DEE), chloroform (CHL), ethyl acetate (ETA), hexane (HEX), methanol (MET), ethanol (ETOH), acetone (ACE) and also combination of solvents (2:1 ratio) such as DEE: MET, CHL: MET, HEX: MET, HEX: ETOH was tested for lipid extraction efficacy. Among solvents used, 12.3% and 18.4% of lipids were extracted using CHL and CHL: MET, respectively, from 10 mL SBH amended cultures. However, the biodiesel yield was found to be similar at about 70.16 % in both SBH and no SBH-added cultures. The fatty acid profile of the biodiesel shows palmitic, oleic, linoleic, linolenic, and arachidonic acid as principal fatty acids. Further, the levels of SFAs, MUFAs, and PUFAs in 10 mL SBH-added cells were 24.67, 12.89, and 34.24%, respectively. Eventually, the fuel properties of Chlorococcum sp. biodiesel, satisfying international biodiesel standards, make the biodiesel a viable diesel substitute in the future.
Assuntos
Microalgas , Saccharum , Ácidos Graxos , Solventes , Lipídeos , Biocombustíveis , Carbono , Metanol , BiomassaRESUMO
Background: Litsea glaucencens Kuth is an aromatic plant used for food seasoning food and in Mexican traditional medicine. Among, L. glaucencens leaves properties, it has proven antibacterial activity which can be used against opportunistic pathogens like Listeria monocytogenes, a foodborne bacteria that is the causal agent of listeriosis, a disease that can be fatal in susceptible individuals. The aim of this work was to investigate the antibacterial activity of L. glaucescens Kuth leaf extracts against L. monocytogenes and to identify its bioactive components. Material and Methods: L. glaucences leaves were macerated with four solvents of different polarity (n-hexane, dichloromethane, ethyl acetate, and methanol). To determine the capacity to inhibit bacterial proliferation in vitro, agar diffusion and microdilution methods were used. Next, we determined the minimal bactericidal concentration (MBC). Finally, we determined the ratio of MBC/MIC. Metabolites present in the active methanolic extract from L. glaucescens Kuth (LgMeOH) were purified by normal-phase open column chromatography. The structure of the antibacterial metabolite was determined using nuclear magnetic resonance (1H, 13C, COSY, HSQC) and by comparison with known compounds. Results: The LgMeOH extract was used to purify the compound responsible for the observed antimicrobial activity. This compound was identified as 5,7-dihydroxyflavanone (pinocembrin) by analysis of its spectroscopic data and comparison with those described. The MIC and MBC values obtained for pinocembrin were 0.68 mg/mL, and the ratio MBC/MIC for both LgMeOH and pinocembrin was one, which indicates bactericidal activity. Conclusion: L. glaucences Kuth leaves and its metabolite pinocembrin can be used to treat listeriosis due the bactericidal activity against L. monocytogenes.
Assuntos
Listeria monocytogenes , Listeriose , Litsea , Humanos , Extratos Vegetais/farmacologia , Testes de Sensibilidade Microbiana , Antibacterianos/farmacologia , Listeriose/tratamento farmacológico , MetanolRESUMO
Chiranthodendron pentadactylon Larreat is a tree native to southeastern Mexico and Guatemala. Its flower is used in Mexican folk medicine to treat a variety of diseases, including conditions of blood pressure. However, scientific information on its usefulness in this pathology is lacking. The present study evaluates the effect of a methanolic extract (ME) from the flower and its active constituents on heart rate (HR) and mean arterial pressure (MAP) in anesthetized rats (MAPHR). The study also analyzed the effects on rat-isolated aortic rings (RIAR) and the rat mesenteric arterial bed (MABR). Active fractions were chromatographed, which led to the isolation of cyanidin 3-O-glucoside (C3G) identified through HPLC. The Chiranthodendron pentadactylon flowers produced hypotensive and vasorelaxant effects associated with C3G. The vasorelaxant effect is a mechanism underlying the synthesis and release of nitric oxide (NO). Neither cholinergic receptors nor prostaglandins are involved. ME and C3G cause cardiovascular depression in anesthetized rats via cholinergic and prostanoid mechanisms. Our research expands the scientific understanding of the flowers on the rat cardiovascular system. This amplifies the appreciation of the flower's ethnomedicine employed to control blood pressure. However, researchers need to conduct toxicity studies to determine the safety of this plant.
Assuntos
Hipotensão , Extratos Vegetais , Ratos , Animais , Extratos Vegetais/farmacologia , Hipotensão/induzido quimicamente , Hipotensão/tratamento farmacológico , Vasodilatadores/farmacologia , Metanol , FloresRESUMO
A gas sensor array was developed and evaluated using four high-frequency quartz crystal microbalance devices (with a 30 MHz resonant frequency in fundamental mode). The QCM devices were coated with ethyl cellulose (EC), polymethylmethacrylate (PMMA), Apiezon L (ApL), and Apiezon T (ApT) sensing films, and deposited by the ultrasonic atomization method. The objective of this research was to propose a non-invasive technique for acetone biomarker detection, which is associated with diabetes mellitus disease. The gas sensor array was exposed to methanol, ethanol, isopropanol, and acetone biomarkers in four different concentrations, corresponding to 1, 5, 10, and 15 µL, at temperature of 22 °C and relative humidity of 20%. These samples were used because human breath contains them and they are used for disease detection. Moreover, the gas sensor responses were analyzed using principal component analysis and discriminant analysis, achieving the classification of the acetone biomarker with a 100% membership percentage when its concentration varies from 327 to 4908 ppm, and its identification from methanol, ethanol, and isopropanol.
Assuntos
Diabetes Mellitus , Técnicas de Microbalança de Cristal de Quartzo , Humanos , Acetona/análise , 2-Propanol , Metanol , Biomarcadores , Etanol , Quartzo/química , Diabetes Mellitus/diagnósticoRESUMO
Significant risk factors for atherosclerosis include hyperlipidemia and oxidative stress, which together rank as three of the most significant risk factors for cardiovascular diseases. Securigera securidaca lowers cholesterol levels in diabetic rats' blood. This investigation's objective was to determine how methanolic extracts affected the flowers, leaves, and seeds of plants in rats that were fed a high-fat diet (HFD). Five groups of animals were created (n = 5). A total of 35 days, divided into two intervals, were used for the study. Rats received HFD during the first 15-day interval, while during the second 20-day interval, they also received extracts or the Atorvastatin reference drug. The extract of seeds has a high phenol content as well as DPPH radical antioxidant activity. Extracts were given at a dose of 200 mg/kg; p.o. Methanolic treatment of S. securidaca flowers, leaves, and seeds in HFD-induced hyperlipidemic rats resulted in significant reductions in total cholesterol, triglycerides, LDLC, and VLDL-C levels. HDL-C levels increased significantly because of the leaves. While in hyperlipidemic rats, seeds significantly reduced the activities of the enzymes ALT and ALP. The findings showed that, to a certain extent, seeds, flowers, and leaves may have benefits in reducing hyperlipidemia brought on by HFD in terms of lipid profiles and liver function enzymes. The findings of this study indicate a promising application prospect, but more research is needed to determine the exact mechanism of these novel compounds as antihyperlipidemic agents and to clarify their potential combination effect with synthetic drugs such as Atorvastatin. Combinations can reduce the dose of chemical medications required, which lowers the risk of side effects.
Assuntos
Diabetes Mellitus Experimental , Hiperlipidemias , Securidaca , Ratos , Animais , Hiperlipidemias/induzido quimicamente , Hiperlipidemias/tratamento farmacológico , Hipolipemiantes/farmacologia , Hipolipemiantes/uso terapêutico , Ratos Wistar , Dieta Hiperlipídica/efeitos adversos , Atorvastatina/farmacologia , Atorvastatina/uso terapêutico , Atorvastatina/análise , Diabetes Mellitus Experimental/tratamento farmacológico , Metanol/análise , Metanol/uso terapêutico , Extratos Vegetais/farmacologia , Extratos Vegetais/uso terapêutico , Extratos Vegetais/química , Sementes , Antioxidantes/farmacologia , Antioxidantes/uso terapêutico , Antioxidantes/análise , Flores , ColesterolRESUMO
BACKGROUND: Azithromycin (AZT) is an antimicrobial available in different pharmaceutical forms and many people can have access to this medicine. Therefore, the existence of adequate and reliable analytical methods for evaluating the quality of AZT and AZT-based products is essential. OBJECTIVE/METHODS: The purpose of this review is to discuss the analytical methods for evaluating AZT present in the literature and official compendia in the context of Green Analytical Chemistry (GAC). RESULTS: Among the methods found in the literature for evaluating AZT, the most used method is HPLC (62%) followed by TLC (14%) and the microbiological method by agar diffusion (14%). Even pharmacopoeias recommend the analysis of AZT by HPLC or agar diffusion. Acetonitrile and methanol account for 35% of the most used solvents in the analyses, followed by buffer. CONCLUSION: AZT lacks analytical methods in the context of GAC. Both physical-chemical and microbiological methods can contemplate the environmentally friendly way to analyze AZT and AZT-based products, depending only on the chosen conditions. Ethanol, purified water, acetic acid instead of methanol, acetonitrile, buffer, formic acid in the physical-chemical methods are excellent alternatives. However, in the microbiological method, turbidimetry is a great option instead of agar diffusion.
Assuntos
Anti-Infecciosos , Azitromicina , Humanos , Metanol , Ágar , AcetonitrilasRESUMO
Herein we report an unprecedented and efficient methodology for accessing 6-alkoxy-Δ4,6-diene-3-one derivatives. Such scaffolds were serendipitously obtained in the course of the study of the reaction of Δ4-3-keto steroids with catalytic amounts of iodine in refluxing methanol. A series of 6-methoxy and 6-ethoxy- Δ4,6-diene-3-ones were prepared from easily-available sterols in a two-step sequence; first, oxidation of sterols furnished the Δ4-3-keto steroids, which were then refluxed with ethanol or methanol with I2 as catalyst to obtain a series of ten derivatives. Furthermore, this protocol was also effective for the introduction of a larger carbon chain at C-6. Druglikeliness properties of synthesized compounds were predicted using the SwissADME tool.