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1.
Drug Chem Toxicol ; 46(5): 931-943, 2023 Nov.
Artigo em Inglês | MEDLINE | ID: mdl-35950554

RESUMO

Cervical cancer ranks fourth in incidence among women worldwide. Cisplatin is currently the first-line drug of treatment for cervical cancer; however, it causes serious adverse effects. Therefore, it is crucial to explore natural products for cervical cancer treatment. Prosopis laevigata is a medicinal plant frequently used for ophthalmological and gastrointestinal infections. In this study, we used the MTT cell viability assay to evaluate the cytotoxic effect of a wood extract from Prosopis laevigata (Extract T7) in SiHa, HeLa, Ca Ski, and C-33 A cancer cell lines. Phosphatidylserine translocation and cell cycle evaluations were performed to determine the mechanism of cellular death. The extract's safety was evaluated using the Ames test with Salmonella typhimurium strains, in vivo acute toxicity assay, and repeated dose toxicity assay in mice. We also identified phenolic compounds of Extract T7 through liquid chromatography/mass spectrometry. Naringin, catechin, and eriodictyol demonstrated a higher concentration in Extract T7. Additionally, Extract T7 exhibited a cytotoxic effect against cervical cancer cells, where C-33 A was the most sensitive (IC50= 22.58 ± 1.10 µg/mL and 14.26 ± 1.11 µg/mL at 24 h and 48 h respectively). Extract T7 induced death by apoptosis and cell cycle arrest in the G2 phase in C-33 A. Extract T7 was not mutagenic. No toxicological effects were observed during acute toxicity and repeated dose toxicity for 28 days. Therefore, further evaluations of Extract T7 should be conducted to identify the complete mechanism of action for potential anti-tumoral activity and safety before conducting studies in animal models.


Assuntos
Antineoplásicos , Prosopis , Neoplasias do Colo do Útero , Humanos , Feminino , Animais , Camundongos , Neoplasias do Colo do Útero/tratamento farmacológico , Extratos Vegetais/toxicidade , Extratos Vegetais/uso terapêutico , Madeira , Antineoplásicos/farmacologia , Células HeLa , Apoptose , Linhagem Celular Tumoral
2.
Nutr Cancer ; 73(11-12): 2287-2305, 2021.
Artigo em Inglês | MEDLINE | ID: mdl-32959676

RESUMO

BACKGROUND: Echinacea spp. displays different biological activities, such as antiviral, immunomodulatory, and anticancer activities. Currently, high sales of hydroalcoholic extracts of Echinacea have been reported; hence, the importance of studies on Echinacea. AIM: To establish the effects of Echinacea angustifolia DC extract obtained with ethyl acetate (Ea-AcOEt) in breast cancer cell lines. METHODS: Cytotoxicity, cell cycle arrest, and cell death were evaluated. Besides, the safety of the extract, as well as its effect in combination with paclitaxel were investigated. RESULTS: The echinacoside and caffeic acid content in the Ea-AcOEt extract were quantified by HPLC, and its antioxidant activity was assessed. The Ea-AcOEt extract showed cytotoxic activity on breast cancer MDA-MB-231 cells (IC50 28.18 ± 1.14 µg/ml) and MCF-7 cells (19.97 ± 2.31 µg/ml). No effect was observed in normal breast MCF-10 cells. The Ea-AcOEt extract induced cell cycle arrest in the G1 phase and caspase-mediated apoptosis. No genotoxicity was found in vitro or in vivo, and the extract showed no signs of toxicity or death at 2,000 mg/kg in rodents. In vitro, the combination of Ea-AcOEt extract and paclitaxel showed a synergistic effect on both cancer cell lines. CONCLUSION: The Ea-AcOEt extract is a potential candidate for breast cancer treatment.


Assuntos
Neoplasias da Mama , Echinacea , Apoptose , Neoplasias da Mama/tratamento farmacológico , Neoplasias da Mama/metabolismo , Pontos de Checagem do Ciclo Celular , Linhagem Celular Tumoral , Proliferação de Células , Feminino , Humanos , Células MCF-7 , Paclitaxel/farmacologia , Extratos Vegetais/farmacologia
3.
J Food Sci Technol ; 56(7): 3225-3238, 2019 Jul.
Artigo em Inglês | MEDLINE | ID: mdl-31274890

RESUMO

ABSTRACT: Peltogyne mexicana heartwood might be a novel purple pigment source. The results of the present study demonstrate that the purple pigment is an important source of phenolic compounds (698.22 ± 2.99 mg GAE/g) and flavonoids (48.01 ± 0.51 mg EPE/g). UV-Vis spectrum and color parameters (L* a* b*) showed that purple pigment has different shades of purple-red (H° value 19.32 ± 0.02 in methanol and 22.85 ± 0.01 in ethanol) depending on the solvent and the pH. Also, the purple pigment did not exhibit acute oral toxicity at a single dose (2000 mg/kg body weight). No mutagenicity was observed in the Ames test with three Salmonella typhimurium strains. The purple pigment exhibited considerable coloring properties with a wider range of citric acid-dependent color hues in gelatin (H° from 280.3 to 319.9 and from 68.0 to 88.1), and higher color intensity than commercial anthocyanin. Minor variations in the hue were found in yogurt, for purple pigment with H° values from 317.5 to 315.0, and commercial anthocyanin from 82.6 to 88.7 and 276.9 to 295.5. However, purple pigment required lower concentrations to achieve superior effects. For gelatin and yogurt samples, similar variations in the color parameters L*, a*, b*, and pigment degradation were observed for purple pigment and commercial anthocyanin in the stability assay.

4.
Int J Mol Sci ; 19(12)2018 Nov 27.
Artigo em Inglês | MEDLINE | ID: mdl-30486412

RESUMO

In this study, an ethanol extract of Agave lechuguilla was evaluated against six carcinogenic cell lines (HCT-15, MCF-7, PC-3, U-251, SK-LU-1 and K-562) with an inhibition of 75.7 ± 2.3% against the SK-LU-1 line. Based on the previous result, the extract was hydrolyzed and fractionated, to which the IC50 was determined; the cell line was more sensitive to the fractionated extract with an IC50 6.96 ± 0.15 µg/mL. Characterization by mass spectrometry showed the presence of kaempferol, quercetin and a flavonoid dimer formed by afzelechin-4ß-8-quercetin, according to the generated fragmentation pattern. The fractionated extract presented cell death by apoptosis with 39.8% at 24 h. Molecular docking was performed with the molecules found to try to describe cell death by apoptosis through death receptors such as FasCD95, TNF-R1, DR4/5 and blocking signaling on the EGFR and K-Ras MAPK/ERK pathway, as well as through the intrinsic pathway activating tBID, which promotes the amplification of the apoptotic signal due to the activation of caspase-3, and consequently caspase-7. In addition to the activation of the IIb complex associated with cell death due to necroptosis.


Assuntos
Agave/química , Antineoplásicos Fitogênicos/química , Antineoplásicos Fitogênicos/farmacologia , Apoptose/efeitos dos fármacos , Extratos Vegetais/química , Extratos Vegetais/farmacologia , Adenocarcinoma de Pulmão , Antioxidantes/química , Antioxidantes/farmacologia , Linhagem Celular Tumoral , Proliferação de Células/efeitos dos fármacos , Sobrevivência Celular/efeitos dos fármacos , Humanos , Ligação de Hidrogênio , Modelos Moleculares , Conformação Molecular , Estrutura Molecular , Compostos Fitoquímicos/química , Compostos Fitoquímicos/farmacologia , Relação Estrutura-Atividade
5.
Biochim Biophys Acta ; 1858(8): 1891-903, 2016 08.
Artigo em Inglês | MEDLINE | ID: mdl-27137675

RESUMO

Platelets are small, anucleated cell fragments that activate in response to a wide variety of stimuli, triggering a complex series of intracellular pathways leading to a hemostatic thrombus formation at vascular injury sites. However, in essential hypertension, platelet activation contributes to causing myocardial infarction and ischemic stroke. Reported abnormalities in platelet functions, such as platelet hyperactivity and hyperaggregability to several agonists, contribute to the pathogenesis and complications of thrombotic events associated with hypertension. Platelet membrane lipid composition and fluidity are determining for protein site accessibility, structural arrangement of platelet surface, and response to appropriate stimuli. The present study aimed to demonstrate whether structural and biochemical abnormalities in lipid membrane composition and fluidity characteristic of platelets from hypertensive patients influence the expression of the Epithelial Sodium Channel (ENaC), fundamental for sodium influx during collagen activation. Wb, cytometry and quantitative Reverse Transcription-Polymerase Chain Reaction (qRT-PCR) assays demonstrated ENaC overexpression in platelets from hypertensive subjects and in relation to control subjects. Additionally, our results strongly suggest a key role of ß-dystroglycan as a scaffold for the organization of ENaC and associated proteins. Understanding of the mechanisms of platelet alterations in hypertension should provide valuable information for the pathophysiology of hypertension.


Assuntos
Plaquetas/metabolismo , Canais Epiteliais de Sódio/sangue , Regulação da Expressão Gênica , Hipertensão/sangue , Fluidez de Membrana , Sódio/sangue , Idoso , Aldosterona/sangue , Plaquetas/ultraestrutura , Estudos de Casos e Controles , Caveolina 1/farmacologia , Caveolinas/sangue , Distroglicanas/antagonistas & inibidores , Distroglicanas/biossíntese , Distroglicanas/sangue , Distroglicanas/genética , Canais Epiteliais de Sódio/biossíntese , Canais Epiteliais de Sódio/genética , Feminino , Regulação da Expressão Gênica/efeitos dos fármacos , Humanos , Hidrocortisona/sangue , Transporte de Íons , Masculino , Pessoa de Meia-Idade , Interferência de RNA , RNA Interferente Pequeno/genética
6.
Bioorg Med Chem Lett ; 26(16): 4086-91, 2016 08 15.
Artigo em Inglês | MEDLINE | ID: mdl-27397496

RESUMO

Pyranocoumarins are compounds with an important pharmacological profile, such as anti-inflammatory, antioxidant, cytotoxic, antiviral, antibacterial, and hypoglycemic effects. These molecules have a widespread presence as secondary metabolites in medicinal plants used to treat Diabetes Mellitus (DM). The aim of this work was to evaluate antidiabetic activity in Streptozotocin (STZ)-induced diabetic rats and the antioxidant effects of 3',4'-Di-O-acetyl-cis-khellactone (DOAcK), as well as its toxic potential. We obtained DOAcK with an enantiomeric excess of 70% by chemical synthesis. Our results showed that this compound exerts an important antidiabetic effect: blood glucose decreased in groups treated with DOAcK by 60.9% at dose of 15mg/kg (p<0.05) compared with the diabetic control group, and demonstrated a statistically significant increase in weight gain (45.7±9.7 in the group treated with DOAcK vs. -23.0±33.1 in the group with diabetes). In a biochemical profile, DOAcK did not modify lipid metabolism and did not cause damage at the renal level. DOAcK administration increased the activities of Catalase (CAT), Glutathione Peroxidase (GPx), and Super Oxide Dismutase (SOD) to levels near those of the healthy group. Histopathological analysis exhibited morphology similar to that of the healthy group and the group treated with DOAcK. DOAcK is not mutagenic by Ames test for Salmonella typhimurium strains TA98, TA100, or TA102, and is not genotoxic by Micronucleus assay; median lethal dose (LD50) >2000mg/kg and, at this dose, no signs of toxicity or death were reported after 14days of observation. These results indicate that DOAcK can improve glucose metabolism, which may be due to the increased antioxidant activity of CAT, GPx and SOD. In addition, DOAcK is not toxic in the studies tested.


Assuntos
Antioxidantes/química , Cumarínicos/química , Hipoglicemiantes/química , Animais , Antioxidantes/farmacologia , Antioxidantes/uso terapêutico , Glicemia/análise , Peso Corporal/efeitos dos fármacos , Catalase/metabolismo , Cumarínicos/farmacologia , Cumarínicos/uso terapêutico , Diabetes Mellitus Experimental/induzido quimicamente , Diabetes Mellitus Experimental/tratamento farmacológico , Diabetes Mellitus Experimental/patologia , Glutationa/metabolismo , Glutationa Peroxidase/metabolismo , Hipoglicemiantes/farmacologia , Hipoglicemiantes/uso terapêutico , Insulina/metabolismo , Ilhotas Pancreáticas/metabolismo , Ilhotas Pancreáticas/patologia , Fígado/efeitos dos fármacos , Fígado/patologia , Testes de Mutagenicidade , Estresse Oxidativo/efeitos dos fármacos , Ratos , Salmonella typhimurium/efeitos dos fármacos , Salmonella typhimurium/genética , Estreptozocina/toxicidade , Superóxido Dismutase/metabolismo
7.
Artigo em Inglês | MEDLINE | ID: mdl-37816987

RESUMO

Diabetes mellitus type 2 (DM2) is the most common chronic disease worldwide, characterized mainly by increased glucose concentration in the blood and affecting several organs' functionality. The daily consumption of probiotic bacteria can help control diabetes and reduce the damage caused. Cell immobilization techniques are a powerful tool that provides physical cell protection to such probiotic bacteria against gastrointestinal conditions. We suggest that cell immobilization could be a significant vector for delivering a high quantity of viable probiotics to the gut, helping attenuate hyperglycemia in diabetic rats. Seventy male Wistar rats were used in this work. Nicotinamide was administrated via intraperitoneal injection 15 minutes before inducing type 2 diabetes (DM2), followed by a second intraperitoneal injection of streptozotocin to induce DM2. Rats were divided into seven groups. For 45 days, a specific treatment was applied to each group. The group of rats, supplied with immobilized Lactobacillus casei, showed a serum glucose concentration of 137 mg/dL, which was close to the one observed in the groups of healthy rats (117 mg/dL) and rats treated with metformin (155 mg/dL). The diabetic rats without treatment presented a higher serum glucose concentration (461 mg/dL). In the rats treated with immobilized L. casei, there was no biochemical parameter alteration, and the cell morphology of the analyzed tissues was similar to those of the healthy group. The consumption of immobilized L. casei could allow a high quantity of viable probiotics to be delivered to the gut, reducing serum glucose concentration by up to 70% compared to diabetic rats and reducing organ damage caused by diabetes.

8.
Naunyn Schmiedebergs Arch Pharmacol ; 396(6): 1211-1222, 2023 06.
Artigo em Inglês | MEDLINE | ID: mdl-36694011

RESUMO

Breast cancer (BC) is the leading cause of cancer-related death in women worldwide. Triple negative breast cancer (TNBC) is the most aggressive form of BC being with the worst prognosis and the worst survival rates. There is no specific pharmacological target for the treatment of TNBC; conventional therapy includes the use of non-specific chemotherapy that generally has a poor prognosis. Therefore, the search of effective therapies against to TNBC continues at both preclinical and clinical level. In this sense, the exploration of different pharmacological targets is a continue task that pave the way to epigenetic modulation using novel small molecules. Lately, the inhibition of histone deacetylases (HDACs) has been explored to treat different BC, including TNBC. HDACs remove the acetyl groups from the ɛ-amino lysine resides on histone and non-histone proteins. In particular, the inhibition of HDAC6 has been suggested to be useful for the treatment of TNBC due to it is overexpressed in TNBC. Therefore, in this work, an HDAC6 selective inhibitor, the (S)-4-butyl-N-(1-(hydroxyamino)-3-(naphthalen-1-yl)-1-oxopropan-2-yl) benzamide (YSL-109), was assayed on TNBC cell line (MDA-MB231) showing an antiproliferative activity (IC50 = 50.34 ± 1.11 µM), whereas on fibroblast, it was lesser toxic. After corroborating the in vitro antiproliferative activity of YSL-109 in TNBC, the toxicological profile was explored using combined approach with in silico tools and experimental assays. YSL-109 shows moderate mutagenic activity on TA-98 strain at 30 and 100 µM in the Ames test, whereas YSL-109 did not show in vivo genotoxicity and its oral acute toxicity (LD50) in CD-1 female mice was higher than 2000 mg/kg, which is in agreement with our in silico predictions. According to these results, YSL-109 represents an interesting compound to be explored for the treatment of TNBC under preclinical in vivo models.


Assuntos
Antineoplásicos , Neoplasias de Mama Triplo Negativas , Humanos , Feminino , Animais , Camundongos , Neoplasias de Mama Triplo Negativas/tratamento farmacológico , Neoplasias de Mama Triplo Negativas/metabolismo , Inibidores de Histona Desacetilases , Linhagem Celular Tumoral , Proliferação de Células , Antineoplásicos/farmacologia , Antineoplásicos/uso terapêutico
9.
Biochem Cell Biol ; 90(3): 425-34, 2012 Jun.
Artigo em Inglês | MEDLINE | ID: mdl-22332957

RESUMO

Entamoeba histolytica is the causative agent of amoebiasis, a disease that produces dysentery as a result of the perforation of the large intestine. This parasite often invades other organs, primarily the liver, leading to an amoebic liver abscess (ALA), which can cause death. Metronidazole is the drug of choice for the treatment of ALA; however, it produces toxic side effects in patients. Lactoferrin (Lf) is a glycoprotein of the innate immune response that sequesters iron in the mucosae. Lf possesses immune-regulatory properties, such as antiinflammatory and antioxidant activities. Moreover, the microbicidal activity of apoLf, which lacks bound iron, has been shown. In this study, we evaluated the therapeutic effect of bovine Lf (bLf) against ALA in a model of hepatic amoebiasis in hamsters. Interestingly, hamsters treated intragastrically with Lf (2.5 mg/100 g mass) over a period of 8 days showed no clinical signs of disease and ALA was effectively decreased, with only 0.63% detectable lesion, compared with 63% in untreated animals. Furthermore, liver function and blood cells approached normal levels among those receiving bLf treatment. These results suggest that bLf may aid in the therapy of amoebiasis, likely without producing undesirable effects in patients.


Assuntos
Amebicidas/uso terapêutico , Entamoeba histolytica/efeitos dos fármacos , Lactoferrina/uso terapêutico , Abscesso Hepático Amebiano/tratamento farmacológico , Metronidazol/uso terapêutico , Fosfatase Alcalina/metabolismo , Amebicidas/farmacologia , Animais , Bilirrubina/metabolismo , Bovinos , Cricetinae , Avaliação Pré-Clínica de Medicamentos , Quimioterapia Combinada , Lactoferrina/farmacologia , Fígado/metabolismo , Fígado/parasitologia , Fígado/patologia , Abscesso Hepático Amebiano/parasitologia , Masculino , Mesocricetus , Metronidazol/farmacologia , Valores de Referência
10.
Nat Prod Res ; 36(16): 4293-4309, 2022 Aug.
Artigo em Inglês | MEDLINE | ID: mdl-34459687

RESUMO

The study of medicinal plants for cancer treatment has gained attention due to an increasing incidence of cancer worldwide and antineoplastics-related undesirable secondary effects. Most of the natural products of medicinal plants that have been evaluated for cytotoxic activity, are derived from leaves, bark, roots and flowers. However, natural products derived from wood have demonstrated a cytotoxic effect with promising results. Moreover, some fractions and compounds have been isolated of wood in order to increase the effect. This review presents in vitro experimental evidence of cytotoxic effect of natural products from wood against cancer cell lines. It also provides considerations and recommendations to obtain herbal medicines over time.


Assuntos
Neoplasias , Plantas Medicinais , Madeira , Antineoplásicos/farmacologia , Linhagem Celular Tumoral/efeitos dos fármacos , Humanos , Neoplasias/tratamento farmacológico , Madeira/metabolismo
11.
Nutrients ; 14(18)2022 Sep 09.
Artigo em Inglês | MEDLINE | ID: mdl-36145087

RESUMO

Beef is an excellent source of nutrients; unfortunately, most nutritional recommendations suggest limiting or even avoiding it. Studies have shown that the fatty acid composition of meat influences weight loss. This randomized controlled clinical trial evaluated the anthropometric and serum lipid changes after a food intervention that included frequent beef consumption (120 g consumed four days/week for four weeks). Volunteers were randomly assigned to the commercial or Wagyu-Cross beef groups, with the latter beef possessing higher fat and MUFA contents. Both groups exhibited reductions in body measurements and lipid profiles; however, the Wagyu-Cross group exhibited greater changes in weight (-3.75 vs. -2.90 kg) and BMI (-1.49 vs. -1.03) than the commercial group, without a significant difference between them. No significant group differences in lipid profiles were observed; however, the Wagyu-Cross group exhibited a more favorable change in decreasing the TC concentration (-7.00 mg/dL) and LDL-C concentration (-12.5 mg/dL). We suggest that high MUFA beef could be included in weight-loss programs since it does not affect weight loss and hasn't a negative influence on lipid metabolism.


Assuntos
Ácidos Graxos , Carne , Animais , Bovinos , LDL-Colesterol , Humanos , Voluntários , Redução de Peso
12.
Nutrients ; 13(8)2021 Jul 27.
Artigo em Inglês | MEDLINE | ID: mdl-34444736

RESUMO

Pomegranate juice (Punica granatum) has been used since ancient times in traditional medicine (Unani Medicine, Ayurveda); its main compounds are anthocyanins and ellagic acid, which have anti-inflammatory, antioxidant, hepatoprotective, and cardiovascular health effects. The objective was to evaluate the effect of pomegranate juice on inflammation, blood pressure, and vascular and physiological markers associated with obesity induced by a high-fat diet in a murine model. The results show that pomegranate juice reduces the concentration of low-density lipoprotein cholesterol (cLDL) 39% and increases the concentration of high-density lipoprotein cholesterol (cHDL) by 27%, leading to a 12%-18% decrease in the risk of cardiovascular diseases (CVD). In addition to reducing blood pressure by 24%, it also had an antiatherogenic effect by decreasing sE-selectin levels by 42%. On the other hand, the juice significantly increased adiponectin levels in adipose tissue, decreased levels of inflammation markers (tumor necrosis factor-α (TNF-α), plasminogen activator inhibitor-1 (PAI-1), interleukin-17A (IL-17A), interleukin-6 (IL-6), interleukin-1ß (IL-1ß)), and inhibited the monocyte chemoattractant protein-1 (MCP-1). Pomegranate juice requires clinical studies to prove its immunoregulatory and therapeutic effects on cardiovascular and atherogenic risks.


Assuntos
Tecido Adiposo/metabolismo , Doenças Cardiovasculares/prevenção & controle , Sucos de Frutas e Vegetais , Fatores de Risco de Doenças Cardíacas , Inflamação , Obesidade/fisiopatologia , Punica granatum , Adiponectina/metabolismo , Tecido Adiposo/imunologia , Animais , Biomarcadores/análise , Pressão Sanguínea , Doenças Cardiovasculares/etiologia , Quimiocina CCL2/antagonistas & inibidores , Citocinas/metabolismo , Dieta Hiperlipídica , Ingestão de Energia , Sucos de Frutas e Vegetais/análise , Lipídeos/sangue , Masculino , Obesidade/complicações , Ratos , Ratos Wistar
13.
J Food Sci ; 86(6): 2713-2726, 2021 Jun.
Artigo em Inglês | MEDLINE | ID: mdl-33929040

RESUMO

Beef is considered an excellent source of high-quality protein and micronutrients. The high saturated fatty acid (SFA) composition of beef has been associated with cardiovascular diseases; however, this is a controversial issue because at present, no evidence has scientifically proven such an association. Wagyu cattle have been used as an option to generate high-quality fatty acids (FAs) in beef and have been crossed with local beef cattle (Wagyu-Cross). In Mexico, Wagyu-Cross is marketed assuming the same quality as purebred Wagyu meat without scientific support. This study aimed to determine whether the differences in the FA composition of Wagyu-Cross and commercial beef affected lipid metabolism in frequent consumers of beef. The study is a randomized, controlled, double-blinded phase IV clinical trial. Thirty-four volunteers completed treatments in which 120 g ground beef was consumed 3 days per week for 2 weeks. Volunteers were randomized to the "A" (commercial meat) or "B" (Wagyu-Cross meat) groups. The beef fat content was 87% higher, the SFA content was 2.3% lower, and the monounsaturated fatty acid (MUFA) C18:1 n-9 concentrations were higher in Wagyu-Cross beef than in commercial beef. The B group exhibited a significantly larger change from baseline in the serum lipid profile in total cholesterol (TC) (-4.7% versus +6.9%), low-density lipoprotein (LDL) (-4.1% versus +10.0%), nonhigh-density lipoprotein (non-HDL) (-6.1% versus +4.9%), and the ratio of three atherogenic indexes-TC/HDL (-3.5% versus +6.4%), LDL/HDL (-2.8% versus +14.6%), and non-HDL/HDL (-4.7% versus +9.3%)-than the A group. This result confirms that meat FA composition is a key point for redirecting cattle breeding strategies and promotes beef as a healthful protein source. PRACTICAL APPLICATION: Here, we found new evidence based on a clinical trial that beef with a favorable fatty acid composition (i.e., monounsaturated fatty acid and polyunsaturated fatty acid content) is a key factor in improving parameters associated with consumer health. This information will support the design of cattle breeding strategies as an option to promote beef consumption as a healthier protein source and create opportunities for the development of the functional food industry.


Assuntos
Lipídeos/análise , Carne/análise , Adolescente , Adulto , Animais , Bovinos , HDL-Colesterol/análise , Método Duplo-Cego , Ácidos Graxos Monoinsaturados/análise , Ácidos Graxos Insaturados/análise , Humanos , Lipoproteínas LDL/análise , Masculino , México , Pessoa de Meia-Idade , Adulto Jovem
14.
J Ethnopharmacol ; 222: 133-147, 2018 Aug 10.
Artigo em Inglês | MEDLINE | ID: mdl-29730133

RESUMO

ETHNOPHARMACOLOGICAL IMPORTANCE: Kalanchoe flammea Stapf (Crassulaceae) is a medicinal plant grown in the South of Mexico (State of Tabasco), which is commonly used in traditional medicine for the treatment of fever, wounds, inflammation, and cancer. AIM OF THE STUDY: To establish the potential of K. flammea for the treatment of prostate cancer, evaluating its cytotoxic activity, its probable mechanism of action, and carrying out some toxicological safety studies. MATERIALS AND METHODS: The cytotoxic activity of the ethyl acetate extract of K. flammea (Kf-EtOAc) was evaluated in several cell lines of prostate cancer by MTT viability assay. The cellular death mechanism was studied by evaluating the translocation of phosphatidylserine (Annexin V); overproduction of reactive oxygen species [2'-7'-Dichlorodihydrofluorescein diacetate (DCFH-DA) assay]; release of Cytochrome C; activation of caspase-3 and -9, and regulation of Bcl-2, XIAP, and PKCε proteins by Western Blot analysis. For the evaluation of the safety of Kf-EtOAc, the Ames test, Micronucleus assay, and acute toxicity study were determined. RESULTS: Kf-EtOAc exhibited selective cytotoxic activity against prostate cell lines as follows: PC-3, LNCaP, and PrEC (IC50 = 1.36 ±â€¯0.05; 2.06 ±â€¯0.02, and 127.05 ±â€¯0.07 µg/mL, respectively). The F82-P2 fraction (rich in coumaric acid and palmitic acid) obtained by bioassay-guided fractionation of Kf-EtOAc also demonstrated selective cytotoxic activity against PC-3 cells (IC50 = 1.05 ±â€¯0.06 µg/mL). Kf-EtOAc induces apoptosis by the intrinsic pathway; this mechanism of cell death was confirmed after observing that the extract produces phosphatidylserine translocation, overproduction of reactive oxygen species, release of Cytochrome C at mitochondrial level, and activation of caspase-3 and -9. It was also observed that Kf-EtOAc produces significant downregulation of apoptosis-related proteins Bcl-2, XIAP, and PKCε and induces DNA fragmentation and cell cycle arrest. In addition, Kf-EtOAc is non-genotoxic in vitro by Ames test and non-genotoxic in vivo by Micronucleus assay, and no signs of toxicity or death were reported after the administration of a single acute exposure of 2000 mg/kg. CONCLUSION: K. flammea is a potential candidate for the development of new drugs for the treatment of prostate cancer. However, to propose their use in clinical trials, additional studies are required to understand their pharmacokinetic behavior, as well as the development of a suitable pharmaceutical form.


Assuntos
Antineoplásicos/farmacologia , Kalanchoe , Extratos Vegetais/farmacologia , Animais , Apoptose/efeitos dos fármacos , Linhagem Celular , Linhagem Celular Tumoral , Sobrevivência Celular/efeitos dos fármacos , Células Cultivadas , Humanos , Leucócitos Mononucleares/efeitos dos fármacos , Masculino , Camundongos , Mitocôndrias/efeitos dos fármacos , Mitocôndrias/metabolismo , Testes de Mutagenicidade , Neoplasias da Próstata/metabolismo , Espécies Reativas de Oxigênio/metabolismo , Transdução de Sinais/efeitos dos fármacos , Testes de Toxicidade Aguda
15.
Artigo em Inglês | MEDLINE | ID: mdl-30224932

RESUMO

Diabetes is one the world's most widespread diseases, affecting over 327 million people and causing about 300,000 deaths annually. Despite great advances in prevention and therapy, existing treatments for this disorder have serious side effects. Plants used in traditional medicine represent a valuable source in the search for new medicinal compounds. Hamelia patens Jacq. has been used for treating diabetes and, so far, no reports have been made on the in vivo antihyperglycemic activity of this plant. The present study on H. patens aimed to test the antihyperglycemic effect of repeated administrations of the crude and fractional methanolic extracts (CME and FME, respectively) on rats with hyperglycemia induced by streptozotocin. After 10 administrations (20 days), each extract had lowered blood glucose to a normal level. The extracts produced effects similar to metformin. Of the five compounds identified by chromatographic analysis of the extracts, epicatechin and chlorogenic acid demonstrated antihyperglycemic effect. The antioxidant activity of the extracts was evidenced by their IC50 values (51.7 and 50.7 µg/mL, respectively). The LD50≥2000 mg/Kg suggests low toxicity for both CME and FME. Thus, considering that the antihyperglycemic and antioxidant effects of metformin and extracts from H. patens were comparable, the latter may be efficacious for treating diabetes.

16.
Bol. latinoam. Caribe plantas med. aromát ; 21(5): 646-653, sept. 2022. tab, graf
Artigo em Inglês | LILACS | ID: biblio-1553790

RESUMO

Lippia graveolens HBK (Verbenaceae) is an aromatic herb of economic importance in Mexico, known as oregano. The leaves are used as condiments, and people use this species for respiratory and digestive disorders. The aim of this work was to evaluate the cytotoxic effect of ethanolic extracts obtained from free-oil leaves (L9) and stem (S15), against lung cancer cell line SK-LU-1, through tetrazolium salt (MTT) assay. Extracts concentrations of 0.3 to 300 µg/mL were used and HFF-1 as normal control cells. Both L9 and S15 extracts, showed cytotoxic effect, although stem was stronger than leaves and without damage to normal cell control. The phenolic compounds caffeic acid and acacetin werein higher concentration in L9, whereas naringenin, taxifolin, eriodictyol, luteolin, and apigenin had higher concentrations in S15. The ethanolic extracts of L. graveolens have excellent cytotoxic activity, and have a wide possibility of use in lung cancer treatment.


Lippia graveolens HBK. (Verbenaceae) es una hierba aromática de importancia económica en México, conocida como orégano. Las hojas se usan como condimento y en medicina tradicional se utiliza para aliviar malestares respiratorios y digestivos. El objetivo de este trabajo fue evaluar el efecto citotóxico de extractos etanólicos obtenidos de hojas sin aceite (L9) y tallo (S15), sobre la línea celular de cáncer de pulmón SK-LU-1, mediante el ensayo de la sal de tetrazolium (MTT). Los extractos se aplicaron a concentraciones de 0,3 a 300 µg/mL y se utilizaron células HFF-1 como control normal. Tanto los extractos L9 como S15 mostraron efecto citotóxico, aunque el efecto del tallo fue mayor al de las hojas y sin daño al control celular normal. Los compuestos fenólicos ácido cafeico y acacetina se encontraron en mayor concentración en L9, mientras que naringenina, taxifolina, eriodictyol, luteolina y apigenina tuvieron mayor concentración en S15. Los extractos etanólicos de L. graveolens tienen una excelente actividad citotóxica, con amplia posibilidad de utilizar en el tratamiento de cáncer de pulmón.


Assuntos
Lippia/toxicidade , Lippia/química , Etanol/toxicidade , Neoplasias Pulmonares/tratamento farmacológico , Caules de Planta/química , Folhas de Planta/química , Etanol/química
17.
J Ethnopharmacol ; 152(1): 91-8, 2014 Feb 27.
Artigo em Inglês | MEDLINE | ID: mdl-24373809

RESUMO

ETHNOPHARMACOLOGICAL RELEVANCE: Arracacia tolucensis is a medicinal plant used in northeast of Mexico as a remedy to treat people with Diabetes mellitus (DM); however, there are no scientific studies that support this information. Thus, we evaluated the anti-hyperglycemic effect of the hexane, ethyl acetate and ethanol extracts from aerial parts in streptozotocin-induced diabetic rats. MATERIALS AND METHODS: DM was induced in Wistar male rats by single intraperitoneal injection of streptozotocin (STZ 50mg/kg). After STZ-induction, hyperglycemic rats were treated with all three extracts orally at a single dose (250 mg/kg) each 48 h for 21 days. Glibenclamide (1mg/kg) was used as a reference drug. The fasting blood glucose levels, the hematic biometry and biochemical profiles, and the inhibition of inflammatory cytokines expression were estimated. Histopathology analysis of pancreas, liver, spleen, and kidney tissue was carried out. RESULTS: Ours results showed that ethyl acetate extract decreased blood glucose levels significantly (75%, p< 0.05) when compared to diabetic rats and controlled the body weight loss; the lipids level did not change, but the enzyme levels of aspartate aminotransferase and alanine aminotransferase decreased significantly (60.83% and 66.16%, respectively, p< 0.05) and inhibited the expression of inflammatory cytokines,with respect to diabetic rats. Histopathology injury was not observed; by contrast repair of islet of Langerhans was exhibited. CONCLUSION: These results validate the use of Arracacia tolucensis as a treatment against DM and suggests it is suitable to continue studies for its safe therapeutic use.


Assuntos
Apiaceae/química , Diabetes Mellitus Experimental/tratamento farmacológico , Hipoglicemiantes/farmacologia , Extratos Vegetais/farmacologia , Animais , Glicemia/efeitos dos fármacos , Citocinas/metabolismo , Etnofarmacologia , Hipoglicemiantes/isolamento & purificação , Mediadores da Inflamação/metabolismo , Masculino , México , Componentes Aéreos da Planta , Ratos , Ratos Wistar , Solventes/química , Estreptozocina
18.
Acupunct Med ; 32(6): 486-94, 2014 Dec.
Artigo em Inglês | MEDLINE | ID: mdl-25267728

RESUMO

OBJECTIVE: To investigate the antihyperglycaemic activity of laser acupuncture stimulation at 650 and 980 nm at BL20 in streptozotocin (STZ)-induced diabetic rats. METHODS: Seventy healthy adult male albino Wistar rats weighing 250±50 g were divided into seven groups of 10 animals each. Groups I-III comprised healthy control rats which were untreated (I) or stimulated with laser acupuncture at 650 nm (II) and 980 nm (III), respectively. Groups IV-VII underwent induction of diabetes with a single intraperitoneal administration of STZ at 50 mg/kg. Animals with blood glucose levels of ≥200 mg/dL on the fifth day were used for the experiments and were left untreated (group IV), treated with glibenclamide (group V) or stimulated with laser acupuncture at 650 nm (group VI) and 980 nm (group VII), respectively. Laser acupuncture was applied at BL20 on alternate days for a total of 12 sessions over a 28-day period. RESULTS: After 28 days of treatment, STZ-induced diabetic rats stimulated with laser acupuncture at 650 and 980 nm had significantly lower glucose levels compared with untreated diabetic rats (242.0±65.0 and 129.8±33.2 vs 376.5±10.0 mg/dL, both p≤0.05). Treatment at 980 nm also attenuated the increase in glucose between day 1 and day 28 compared with the glibenclamide-treated diabetic group (41.5±19.6 mg/dL vs 164.1±13.7 g/dL, p<0.05). Laser acupuncture treatment did not affect the blood count or biochemical profile and was not associated with any morphological changes in the pancreas, liver, kidney or spleen. CONCLUSIONS: Stimulation with laser acupuncture at 650 and 980 nm at BL20 in STZ-induced diabetic rats has antihyperglycaemic activity. The results support further evaluation of laser acupuncture as an alternative or complementary treatment for the control of hyperglycaemia.


Assuntos
Terapia por Acupuntura , Glicemia/metabolismo , Diabetes Mellitus Experimental/terapia , Hiperglicemia/terapia , Terapia por Acupuntura/métodos , Animais , Lasers , Masculino , Ratos Wistar
19.
Toxicology ; 314(1): 155-65, 2013 Dec 06.
Artigo em Inglês | MEDLINE | ID: mdl-24012731

RESUMO

Cisplatin remains one of the most effective current chemotherapeutic agents; however, metal complexes synthesis has increased in order to produce new anti-neoplastic drugs with DNA binding and apoptotic activities in tumor cells and less toxicity for patients. In this study, we evaluated the cytotoxic activity of a novel copper(II) complex (LQM402) against cervical cancer cell lines and found that LQM402 exhibited selective cytotoxicity against HeLa and Ca Ski cells. FITC-annexin assay and DNA fragmentation indicated that apoptosis could be involved in HeLa cell death. Caspase 3/7 and cytochrome c analysis by immunoblotting suggest the intrinsic pathway. LQM402 is a lipid peroxidation inductor according to TBARS production. Additionally, the Ames and micronucleus tests demonstrated non-genotoxic activity for this compound in Salmonella typhimurium and CD1 mice, respectively. Therefore, LQM402 may be a promising and safe anti-cervical cancer compound.


Assuntos
Apoptose/efeitos dos fármacos , Complexos de Coordenação/farmacologia , Cobre/química , Mutagênicos/toxicidade , Oxidantes/metabolismo , Neoplasias do Colo do Útero/tratamento farmacológico , Animais , Anexinas , Química Encefálica/efeitos dos fármacos , Caspase 3/metabolismo , Caspase 7/metabolismo , Linhagem Celular Tumoral , Corantes , Complexos de Coordenação/toxicidade , Citocromos c/metabolismo , Citosol/metabolismo , Fragmentação do DNA/efeitos dos fármacos , Feminino , Citometria de Fluxo , Fluoresceína-5-Isotiocianato , Células HeLa , Humanos , Marcação In Situ das Extremidades Cortadas , Peroxidação de Lipídeos/efeitos dos fármacos , Camundongos , Testes para Micronúcleos , Testes de Mutagenicidade , Fosfatidilserinas/metabolismo , Ratos , Salmonella typhimurium/efeitos dos fármacos , Salmonella typhimurium/metabolismo , Sais de Tetrazólio , Tiazóis , Neoplasias do Colo do Útero/metabolismo , Neoplasias do Colo do Útero/patologia
20.
Rev. bras. farmacogn ; 25(1): 22-28, Jan-Feb/2015. tab, graf
Artigo em Inglês | LILACS | ID: lil-746057

RESUMO

Berberis hartwegii Benth., Berberidaceae, Hamelia patens Jacq., Rubiaceae, Dendropanax arboreus (L.) Decne & Planch., Araliaceae, Erythrina herbacea L., Fabaceae, and Zanthoxylum caribaeum Lam., Rutaceae, acetone extracts were selected on the basis of their use in traditional Mexican medicine to treat scabies or skin diseases. Anti-dermatophyte activity in vitro was evaluated using the agar dilution assay, and the therapeutic efficacy of B. hartwegii and Z. caribaeum were tested against experimental tinea pedis. The infected animals were treated intragastrically daily for seven days with 2.5 and 5 mg/kg of acetone extracts. The acetone extract of H. patens exhibited 100% growth inhibition against T. mentagrophytes and E. floccosum at 100.0 and 50.0 µg/ml, respectively, and B. hartwegii inhibited growth of M. canis and T. mentagrophytes at 100.0 µg/ml. Effective treatments with 2.5 mg/kg of Z. caribaeum and B. hartwegii extract were comparable with 1 mg/kg of clotrimazole in mice. Liver profile tests and histological analyses did not exhibit any signs of toxicity and the Ames test indicated that both extracts were safe when evaluated in strains TA98, TA100 and TA102. Our results suggest the potential for the future development of new antifungal drugs from B. hartwegii or Z. caribaeum.

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