RESUMO
This study aimed to investigate the feasibility of a combined treatment of bee venom acupuncture (BVA) and non-steroidal anti-inflammatory drugs (NSAIDs) for the treatment of non-specific chronic neck pain (NCNP). Patients with NCNP for ≥3 months were randomly allocated to a BVA, NSAIDs, or combined group (1:1:1), receiving 6 sessions of BVA, loxoprofen (180 mg daily), or a combination, respectively, for 3 weeks. Recruitment, adherence, and completion rates were calculated to assess feasibility. Bothersomeness, pain, disability, quality of life, depressive status, treatment credibility, and adverse events were assessed. In total, 60 participants were enrolled, and 54 completed the trial. Recruitment, adherence, and completion rates were 100%, 95%, and 90%, respectively. Bothersomeness, pain, disability, and depressive symptoms significantly improved in all groups after treatment (p < 0.05). The combined group showed continuous improvement during the follow-up period (p < 0.05). Quality of life was significantly improved (p < 0.05), and treatment credibility was maintained in the BVA and combined groups. No serious adverse events were reported. Combined treatment of BVA and NSAIDs are feasible for the treatment of NCNP, showing high persistence of the effect, credibility, and safety. Additional trials with longer follow-up are needed to confirm this effect.
Assuntos
Terapia por Acupuntura , Anti-Inflamatórios não Esteroides/uso terapêutico , Venenos de Abelha/uso terapêutico , Dor Crônica/terapia , Cervicalgia/terapia , Fenilpropionatos/uso terapêutico , Adulto , Terapia Combinada , Feminino , Humanos , Masculino , Pessoa de Meia-Idade , Qualidade de Vida , Método Simples-Cego , Resultado do TratamentoRESUMO
Normal brain functioning involves the interaction of interconnected molecular and cellular activities, which appear to alter normal to abnormal brain functioning when worsened, contributing to the emergence of neurological disorders. There are currently millions of people who are living with brain disorders globally and this will rise if suitable prevention strategies are not explored. Nutraceutical intended to treat numerous health goals with little adverse effect possible together can be more beneficial than pharmaceutical monotherapy for fostering balanced brain functioning. Nutraceutical provides a specific composition of effective macronutrients and micronutrients that are difficult to synthesize in the laboratory. Numerous elements of rice fibers in rice bran are characterized as natural anti-oxidant and having potential anti-inflammatory activity. The rice bran captures interest among the researchers as it is widespread, affordable, and rich in nutrients including protein, fat, carbohydrates, bioactive components, and dietary fiber. This review covers the neuroprotective multiplicity of rice bran and its constituents to deter pathological conditions of the brain and to facilitate balanced brain functioning at the same time.
Assuntos
Anti-Inflamatórios/uso terapêutico , Doenças do Sistema Nervoso/dietoterapia , Fármacos Neuroprotetores/uso terapêutico , Oryza , Fenilpropionatos/uso terapêutico , Extratos Vegetais/uso terapêutico , Óleo de Farelo de Arroz/uso terapêutico , Tocotrienóis/uso terapêutico , Animais , Suplementos Nutricionais , Humanos , Serotonina/metabolismoRESUMO
The recent coronavirus disease 2019 (COVID-19) pandemic is a global threat for healthcare management and the economic system, and effective treatments against the pathogenic severe acute respiratory syndrome coronavirus 2 (SARS-CoV-2) virus responsible for this disease have not yet progressed beyond the developmental phases. As drug refinement and vaccine progression require enormously broad investments of time, alternative strategies are urgently needed. In this study, we examined phytochemicals extracted from Avicennia officinalis and evaluated their potential effects against the main protease of SARS-CoV-2. The antioxidant activities of A. officinalis leaf and fruit extracts at 150 µg/mL were 95.97% and 92.48%, respectively. Furthermore, both extracts displayed low cytotoxicity levels against Artemia salina. The gas chromatography-mass spectroscopy analysis confirmed the identifies of 75 phytochemicals from both extracts, and four potent compounds, triacontane, hexacosane, methyl linoleate, and methyl palminoleate, had binding free energy values of -6.75, -6.7, -6.3, and -6.3 Kcal/mol, respectively, in complexes with the SARS-CoV-2 main protease. The active residues Cys145, Met165, Glu166, Gln189, and Arg188 in the main protease formed non-bonded interactions with the screened compounds. The root-mean-square difference (RMSD), root-mean-square fluctuations (RMSF), radius of gyration (Rg), solvent-accessible surface area (SASA), and hydrogen bond data from a molecular dynamics simulation study confirmed the docked complexes' binding rigidity in the atomistic simulated environment. However, this study's findings require in vitro and in vivo validation to ensure the possible inhibitory effects and pharmacological efficacy of the identified compounds.
Assuntos
Avicennia/química , Tratamento Farmacológico da COVID-19 , Compostos Fitoquímicos/uso terapêutico , SARS-CoV-2/metabolismo , Antioxidantes/química , Antioxidantes/metabolismo , Antioxidantes/uso terapêutico , Avicennia/metabolismo , Sítios de Ligação , COVID-19/patologia , COVID-19/virologia , Frutas/química , Frutas/metabolismo , Humanos , Simulação de Acoplamento Molecular , Simulação de Dinâmica Molecular , Álcool Feniletílico/química , Álcool Feniletílico/metabolismo , Álcool Feniletílico/uso terapêutico , Fenilpropionatos/química , Fenilpropionatos/metabolismo , Fenilpropionatos/uso terapêutico , Compostos Fitoquímicos/química , Compostos Fitoquímicos/metabolismo , Folhas de Planta/química , Folhas de Planta/metabolismo , SARS-CoV-2/isolamento & purificação , Proteínas da Matriz Viral/química , Proteínas da Matriz Viral/metabolismoRESUMO
Association to early mortality and sedentarism was already demonstrated in the literature; nevertheless, some possible biochemical mechanisms around physical inactivity still need answers. The use of an invertebrate model, such as Drosophila melanogaster, can reproduce reliable responses in inducing an exercise protocol with exogenous antioxidant supplementation. This study main evaluates the effect of exercise (EXE) associated with γ-oryzanol (ORY) supplementation to improve locomotor behavior, antioxidant defenses, and survival in Drosophila melanogaster. Two-day old flies were submitted to a protocol for seven days, divided into five groups: Control, Movement-Limited Flies (MLF), EXE, ORY [25 µM], and EXE + ORY [25 µM]. The survival rate was evaluated, followed by open field and negative geotaxis. Flies were euthanized and subjected to analysis for acetylcholinesterase (AChE) and antioxidant enzymes activity, glycidic and lipid parameters, body weight, reactive species (RS), and lipid peroxidation. EXE and EXE + ORY flies showed increased survival and locomotor activity, improved glycidic and lipid parameters, with a lower RS production, and increased antioxidant defenses compared to Control, and EXE + ORY when compared to the EXE group, obtained an increase in the ratio of protein levels/body weight, decreased ratio of triglyceride levels/body weight and decreased lipid peroxidation. However, MLF showed less survival and decreased locomotor activity, possibly due to increased AChE activity and reduced antioxidant defenses. The EXE and EXE + ORY demonstrate effective results in maintaining endogenous defenses, with increased locomotor activity, supporting evidence on EXE benefits, and supplementation with antioxidant compounds face of health paradigms.HighlightsNew protocol system of exercise on Drosophila melanogaster model.ORY demonstrates synergistic effect with EXE.Exercise with ORY supplementation increases locomotor behavior.Exercise with ORY supplementation decrease oxidative damages on flies.
Assuntos
Suplementos Nutricionais/normas , Estresse Oxidativo/efeitos dos fármacos , Fenilpropionatos/uso terapêutico , Animais , Drosophila melanogaster , Fenilpropionatos/farmacologia , Condicionamento Físico AnimalRESUMO
The G protein-coupled receptor 109 A (GPR109A) is robustly expressed in osteoclastic precursor macrophages. Previous studies suggested that GPR109A mediates effects of diet-derived phenolic acids such as hippuric acid (HA) and 3-(3-hydroxyphenyl) propionic acid (3-3-PPA) on promoting bone formation. However, the role of GPR109A in metabolic bone homeostasis and osteoclast differentiation has not been investigated. Using densitometric, bone histologic and molecular signaling analytic methods, we uncovered that bone mass and strength were significantly higher in tibia and spine of standard rodent diet weaned 4-week-old and 6-month-old GPR109A gene deletion (GPR109A-/-) mice, compared to their wild type controls. Osteoclast numbers in bone and in ex vivo bone marrow cell cultures were significantly decreased in GPR109A-/- mice compared to wild type controls. In accordance with these data, CTX-1 in bone marrow plasma and gene expression of bone resorption markers (TNFα, TRAP, Cathepsin K) were significantly decreased in GPR109A-/- mice, while on the other hand, P1NP was increased in serum from both male and female GPR109A-/- mice compared to their respective controls. GPR109A deletion led to suppressed Wnt/ß-catenin signaling in osteoclast precursors to inhibit osteoclast differentiation and activity. Indeed, HA and 3-3-PPA substantially inhibited RANKL-induced GPR109A expression and Wnt/ß-catenin signaling in osteoclast precursors and osteoclast differentiation. Resultantly, HA significantly inhibited bone resorption and increased bone mass in wild type mice, but had no additional effects on bone in GPR109A-/- mice compared with their respective untreated control mice. These results suggest an important role for GPR109A during osteoclast differentiation and bone resorption mediating effects of HA and 3-3-PPA on inhibiting bone resorption during skeletal development.
Assuntos
Reabsorção Óssea/prevenção & controle , Hipuratos/farmacologia , Osteogênese/efeitos dos fármacos , Fenilpropionatos/farmacologia , Receptores Acoplados a Proteínas G/metabolismo , Animais , Avaliação Pré-Clínica de Medicamentos , Feminino , Microbioma Gastrointestinal , Hipuratos/uso terapêutico , Masculino , Camundongos Endogâmicos C57BL , Camundongos Knockout , Fenilpropionatos/uso terapêutico , Receptores Acoplados a Proteínas G/antagonistas & inibidores , Receptores Acoplados a Proteínas G/genética , Via de Sinalização WntRESUMO
ETHNOPHARMACOLOGICAL RELEVANCE: Cecropia pachystachya Trécul (Urticaceae) is a medicinal plant popularly known as 'embaúba'. In Brazil, the leaves of this species are used for the treatment of various kidney and cardiovascular diseases. However, there are no detailed studies on the renal and cardiovascular activities of this species. No studies on the anatomy or the quality control of this herbal drug is available thus far. AIM: This study was aimed to investigate the ethnopharmacological properties of the leaves of C. pachystachya. MATERIAL AND METHODS: The leaves of C. pachystachya were analyzed by light and scanning electron microscopy for pharmacobotanical and anatomical characterization. The ethanol-soluble fraction of C. pachystachya leaf extract (ESCP) was characterized by high-performance liquid chromatograph equipped with diode array detector and mass spectrometry (HPLC-DAD-MS). The acute oral toxicity of ESCP on female Wistar rats was assessed. The acute and prolonged diuresis and antioxidant effects of ESCP (30, 100, and 300 mg/kg) were evaluated in male Wistar rats. In addition, the hypotensive effects of the ESCP as well as the vasodilatory activity in isolated and perfused mesenteric vascular beds were investigated. RESULTS: The anatomical markers obtained in this study can help in the identification of C. pachystachya, as well as to distinguish it from the other 'embaúbas'. The metabolites found in the ESCP were phenolic compounds, mainly C- and O-glycosylated flavonoids. The ESCP did not exhibit any toxic effects at a dose of 2000 mg/kg. Significant diuretic activities were observed at the doses of 30, 100, and 300 mg/kg. In addition, a significant modulating activity of the tissue redox state was observed after prolonged treatment. On the other hand, no hypotensive or vasodilator activity was observed. CONCLUSION: The key findings of the present study can contribute to the taxonomy, species identification and quality control of C. pachystachya. Chemical studies have shown the presence of glycosylated flavonoids, phenylpropanoid derivative and proanthocyanidins. The pharmacological studies showed significant diuretic and antioxidant effects of C. pachystachya leaf extract, indicating a possible validation of its popular medicinal use.
Assuntos
Antioxidantes/farmacologia , Antioxidantes/uso terapêutico , Cecropia/química , Diuréticos/farmacologia , Diuréticos/uso terapêutico , Extratos Vegetais/farmacologia , Extratos Vegetais/uso terapêutico , Animais , Pressão Arterial/efeitos dos fármacos , Brasil , Feminino , Flavonoides/farmacologia , Flavonoides/uso terapêutico , Frequência Cardíaca/efeitos dos fármacos , Masculino , Oxirredução/efeitos dos fármacos , Fenilpropionatos/farmacologia , Fenilpropionatos/uso terapêutico , Extratos Vegetais/efeitos adversos , Extratos Vegetais/química , Folhas de Planta/química , Folhas de Planta/citologia , Plantas Medicinais/química , Proantocianidinas/farmacologia , Proantocianidinas/uso terapêutico , Ratos Wistar , Urina/química , Vasodilatadores/farmacologia , Vasodilatadores/uso terapêuticoRESUMO
Gestational diabetes (GDM) is common in pregnancies due to the inflammation and oxidative stress-mediated insulin resistance. In the present study, GDM was induced in the Wistar rats by administering the streptozotocin to elucidate whether the administration of syringin (50 mg/kg/day) during pregnancy could improve maternal glycemia and protect against the complications of GDM. The animals were assessed for their morphological changes in the ß-islets of Langerhans and their insulin-producing ability, inflammatory cytokine markers, and the involvement of TLR4/MyD88/NF-κB signaling pathway using RT-PCR. The results demonstrated that the onset of GDM demonstrated pancreatic tissue degeneration in the islets of Langerhans with a significant increase in oxidative stress and reduced antioxidant enzymes. Besides, the mRNA expression levels of TLR4, MyD88, NF-Kß p65; NLRP3 mRNA were profoundly increased in GDM rats compared to normal pregnant rats. On the other hand, syringin administered GDM rats abrogated the oxidative stress and attenuated the level of the inflammatory cytokines. Intriguingly, the decrease in TLR4 expression and the downstream molecules of MyD88, NF-κB, and NLRP3 were also observed in syringin administered GDM rats that indicate the insulin secretion stimulatory actions of syringin through the suppression of TLR4 signaling. These novel findings of the study provide evidence that syringin could be a probable candidate to be used in the treatment of gestational diabetes in the future.
Assuntos
Diabetes Gestacional/prevenção & controle , Glucosídeos/uso terapêutico , Fator 88 de Diferenciação Mieloide/antagonistas & inibidores , NF-kappa B/antagonistas & inibidores , Estresse Oxidativo/efeitos dos fármacos , Fenilpropionatos/uso terapêutico , Receptor 4 Toll-Like/antagonistas & inibidores , Animais , Animais Recém-Nascidos , Citoproteção/efeitos dos fármacos , Citoproteção/fisiologia , Diabetes Gestacional/metabolismo , Eleutherococcus , Feminino , Glucosídeos/farmacologia , Inflamação/metabolismo , Inflamação/prevenção & controle , Masculino , Fator 88 de Diferenciação Mieloide/metabolismo , NF-kappa B/metabolismo , Estresse Oxidativo/fisiologia , Fenilpropionatos/farmacologia , Gravidez , Ratos , Ratos Wistar , Transdução de Sinais/efeitos dos fármacos , Transdução de Sinais/fisiologia , Receptor 4 Toll-Like/metabolismoRESUMO
The present study assessed the effects of daily supplementation with 33 mg/metabolic weight (MW) of γ-oryzanol on testicular degeneration induced by scrotal insulation in rams. Eight animals were divided into two groups: Control (subjected to scrotal insulation without treatment) and Gamma (subjected to scrotal insulation and γ-oryzanol treatment). The rams were subjected to scrotal insulation by covering the scrotum with a thermal bag for 72â¯h. Animals in the Gamma group received 33â¯mg/MW oral γ-oryzanol once-daily, beginning 7 days before insulation and continuing during insulation and for 20 days afterward, for a total treatment period of 30 days. Samples of semen and blood were collected during the experiment to perform biochemical evaluations of oxidative stress, seminal kinetics and morphology, and plasma testosterone concentrations. Ultrasound examinations of the testicular parenchyma and clinical evaluations of its consistency and the scrotal perimeter were also performed at weekly intervals. Testicular tissue was collected for biochemical analyses of oxidative stress parameters at the end of the experiment by orchiectomy. The results showed that testicular degeneration was induced by scrotal insulation, as was demonstrated by the reduced scrotal perimeter and increased in testicular flaccidity immediately after insulation. Moreover, a delayed increase in the number of hyperechoic points in the parenchyma and a delayed reduction in sperm motility were observed at 10 weeks after insulation by ultrasonography. Treatment with γ-oryzanol reduced levels of reactive oxygen species (ROS) levels in the testes, and increased the total antioxidant potential (assessed based on the ferric reducing ability (FRAP)) in week 10 and levels of lipid peroxidation (TBARS). It also increased the number of intact spermatozoa in week 3, but increased the total number of sperm defects from week 5 onwards. Although γ-oryzanol protected the semen and testes by reducing the levels of the parameters of oxidative stress evaluated herein, the other parameters studied were not improved by the treatment. In addition, supplementation with γ-oryzanol led to more morphological abnormalities in the sperm. This study presented new information on the oral administration of γ-oryzanol to rams with testicular degeneration, and described potential therapies for this pathology, which currently has no established treatment and has important impacts on reproductive health.
Assuntos
Antioxidantes/uso terapêutico , Fenilpropionatos/uso terapêutico , Escroto/efeitos dos fármacos , Ovinos/fisiologia , Testículo/efeitos dos fármacos , Animais , Resposta ao Choque Térmico , Peroxidação de Lipídeos , Masculino , Estresse Oxidativo , Espécies Reativas de Oxigênio/metabolismo , Escroto/patologia , Temperatura , Testículo/patologiaRESUMO
OBJECTIVES: Rice bran oil (RBO) is a major source of monounsaturated fatty acid and gamma-oryzanol, which may assist in lowering blood lipids and oxidative stress. This study examined the effects of RBO containing different amounts of gamma-oryzanol on blood lipid, antioxidant, and inflammatory markers. MATERIALS AND METHODS: A total of 59 hyperlipidemic subjects completed the study. They were divided into four groups: RBO1 (4,000 ppm gamma-oryzanol, n = 14), RBO2 (8,000 ppm gamma-oryzanol, n = 15), RBO3 (11,000 ppm gamma-oryzanol, n = 15), and control (soybean oil, n = 15). The assigned oil (30 mL) was incorporated into three cooked meals each day for 4 weeks. Anthropometrical measurements and blood samples were taken to evaluate body weight, body composition, lipid parameters, antioxidant status, and inflammatory markers before and after the intervention. RESULTS: Compared with the control, consumption of RBO significantly decreased low-density lipoprotein cholesterol (LDL-C) levels (percentage change: -0.8% [control]; -8% [RBO1]; -11.8% [RBO2]; and -12.2% [RBO3], p = 0.012) with the greatest change found in RBO2 and RBO3. In addition, antioxidant status also improved significantly. Levels of oxygen radical absorbance capacity (ORAC) and ferric reducing antioxidant power (FRAP) increased after consumption of a diet with RBO compared with consumption of a diet with soybean oil (ORAC: -2.7% [control]; 4.1% [RBO1]; 8.6% [RBO2]; and 10.1% [RBO3], p < 0.001; FRAP: -4.4% [control]; 4.7% [RBO1]; 7.4% [RBO2]; and 7.6% [RBO3], p < 0.001). CONCLUSIONS: RBO with gamma-oryzanol could decrease LDL-C levels and increase antioxidant capacity in hyperlipidemic subjects. Therefore, RBO consumption may reduce cardiovascular disease risk factors.
Assuntos
Antioxidantes/análise , Hiperlipidemias , Lipídeos/sangue , Fenilpropionatos/uso terapêutico , Óleo de Farelo de Arroz/uso terapêutico , Adulto , Método Duplo-Cego , Humanos , Hiperlipidemias/sangue , Hiperlipidemias/tratamento farmacológico , Pessoa de Meia-Idade , Adulto JovemRESUMO
ETHOPHARMACOLOGICAL RELEVANCE: The propolis is extensively used in folk medicine in natura or to prepare pharmaceutical formulations since ancient time to improve health or prevent diseases, among them gastrointestinal disorders. Aiming to contribute in the scientific validation about the popular use of Brazilian Green propolis (BGP) against gastritis and gastric ulcer, this work evaluated the antiulcer potential of isolated compounds from BGP, three prenylated p-coumaric acid derivatives and two flavonoids, respectively named: 3,5 diprenyl-4-hydroxycinnamic acid (artepillin C) (1), 3-prenyl-4-dihydroxycinnamoiloxy cinnamic acid (baccharin) (2), 3-prenyl-4-hydroxycinnamic acid (drupanin) (3), aromadendrin-4'-O-methyl-ether (4) and kaempferide (5). MATERIAL AND METHODS: The compounds were characterized by nuclear magnetic resonance and mass spectrometry. Their gastroprotective effects were evaluated against ethanol/HCl- and indomethacin-induced ulcer in mice. Further, histological, histochemical, oxidative and inflammatory parameters were analyzed at ulcerated tissue. Acid antisecretory activities also were also assessed. RESULTS: Compound 2 did not reduce the ethanol/HCl- induced ulcer at 30â¯mg/kg (p.o), whereas the minimum oral gastroprotective doses of 1, 3, 4 and 5 were 0.3, 0.3, 3 and 3â¯mg/kg, respectively. Besides, these compounds prevented ethanol/HCl-induced ulcer by intraperitoneal route, as well as indomethacin-induced ulcer by oral route. The gastroprotection was accompanied by normalization of superoxide dismutase, catalase and glutathione-S-transferase activities and reduction in myeloperoxidase activity. Moreover, the compounds 4 and 5 increased the gastric mucin content and 1 reduced TNF amount. Furthermore, 1, 3, 4 and 5 decreased volume, pH, total acidity and pepsin activity of the gastric juice from rats. CONCLUSIONS: Together, our findings showed a diversified mode of action elicited by 1, 3, 4 and 5 on the gastroprotection and contribute to explain the anti-ulcer activity reported for BGP.
Assuntos
Antiulcerosos/uso terapêutico , Própole/química , Úlcera Gástrica/tratamento farmacológico , Animais , Cinamatos/uso terapêutico , Etanol , Flavonoides/uso terapêutico , Ácido Clorídrico , Indometacina , Quempferóis/uso terapêutico , Masculino , Camundongos , Fenilpropionatos/uso terapêutico , Própole/uso terapêutico , Úlcera Gástrica/induzido quimicamenteRESUMO
Risk factors of type 2 diabetes mellitus (T2D) and cardiovascular disease (CVD) cluster together and are termed the metabolic syndrome. Key factors driving the metabolic syndrome are inflammation, oxidative stress, insulin resistance (IR), and obesity. IR is defined as the impairment of insulin to achieve its physiological effects, resulting in glucose and lipid metabolic dysfunction in tissues such as muscle, fat, kidney, liver, and pancreatic ß-cells. The potential of rooibos extract and its major C-glucosyl flavonoids, in particular aspalathin, a C-glucoside dihydrochalcone, as well as the phenolic precursor, Z-2-(ß-D-glucopyranosyloxy)-3-phenylpropenoic acid, to prevent the metabolic syndrome, will be highlighted. The mechanisms whereby these phenolic compounds elicit positive effects on inflammation, cellular oxidative stress and transcription factors that regulate the expression of genes involved in glucose and lipid metabolism will be discussed in terms of their potential in ameliorating features of the metabolic syndrome and the development of serious metabolic disease. An overview of the phenolic composition of rooibos and the changes during processing will provide relevant background on this herbal tea, while a discussion of the bioavailability of the major rooibos C-glucosyl flavonoids will give insight into a key aspect of the bioefficacy of rooibos.
Assuntos
Antioxidantes/uso terapêutico , Aspalathus/química , Suplementos Nutricionais , Flavonoides/uso terapêutico , Glucosídeos/uso terapêutico , Síndrome Metabólica/prevenção & controle , Fenilpropionatos/uso terapêutico , Extratos Vegetais/uso terapêutico , Animais , Anti-Inflamatórios não Esteroides/análise , Anti-Inflamatórios não Esteroides/química , Anti-Inflamatórios não Esteroides/uso terapêutico , Antioxidantes/análise , Antioxidantes/química , Bebidas/análise , Diabetes Mellitus Tipo 2/complicações , Diabetes Mellitus Tipo 2/dietoterapia , Diabetes Mellitus Tipo 2/imunologia , Etnofarmacologia , Flavonoides/análise , Flavonoides/química , Glucosídeos/análise , Glucosídeos/química , Humanos , Isomerismo , Medicinas Tradicionais Africanas , Síndrome Metabólica/complicações , Síndrome Metabólica/etiologia , Obesidade/complicações , Obesidade/dietoterapia , Obesidade/imunologia , Obesidade/fisiopatologia , Fenilpropionatos/análise , Fenilpropionatos/química , Extratos Vegetais/química , Folhas de Planta/química , Caules de Planta/química , África do Sul , Chás de Ervas/análiseRESUMO
The roots of Codonopsis cordifolioidea (classified as campanulaceae cordifolioidea), locally known as Tsoong, have been used as a tonic food. The major components isolated from Tsoong have been demonstrated to present antihuman immunodeficiency virus1 activities and cytotoxicity against various tumor cell lines. However, the possible effects of the novel compound isolated from Tsoong, cordifoliketones A, on pancreatic ductal adenocarcinoma (PDAC) cells, are still unknown. In the present study, cordifoliketones A extractions were prepared from Tsoong, and the possible effects on PDAC cell growth, apoptosis, migration and invasion in vitro and in vivo were exlored. The cytotoxicity assay, apoptosis assay, western blotting, migration and invasion assay, and a PDAC cell (AsPC1, BxPC3 and PANC1) xenograft mice model were employed. The results demonstrated that treatment with cordifoliketones A: i) inhibited proliferation and promoted apoptosis of PDAC cells; ii) significantly induced apoptosis and altered expression of apoptosisassociated proteins in a dosedependent manner; iii) suppressed migration and invasion of PDAC cells in a dosedependent manner; and iv) restrained the growth of PDAC neoplasm in nude mice. Furthermore, cordifoliketones A demonstrated noncytotoxic activity in a panel of normal human cells, including hTERTHPNE, 293, hepatocyte HL7702 and HL1 cells. Therefore, these data indicated that cordifoliketones A may be a potential candidate compound for the prevention of PDAC cell proliferation and metastasis, presumably by induction apoptosis and inhibiting viability, invasion and migration of PDAC cells.
Assuntos
Antineoplásicos Fitogênicos/farmacologia , Apoptose/efeitos dos fármacos , Proliferação de Células/efeitos dos fármacos , Codonopsis/química , Fenilpropionatos/farmacologia , Animais , Antineoplásicos Fitogênicos/química , Antineoplásicos Fitogênicos/uso terapêutico , Proteínas Reguladoras de Apoptose/genética , Proteínas Reguladoras de Apoptose/metabolismo , Carcinoma Ductal Pancreático/tratamento farmacológico , Carcinoma Ductal Pancreático/metabolismo , Carcinoma Ductal Pancreático/patologia , Caspases/metabolismo , Linhagem Celular Tumoral , Movimento Celular/efeitos dos fármacos , Codonopsis/metabolismo , Feminino , Regulação Neoplásica da Expressão Gênica/efeitos dos fármacos , Humanos , Camundongos , Camundongos Endogâmicos BALB C , Camundongos Nus , Neoplasias Pancreáticas/tratamento farmacológico , Neoplasias Pancreáticas/metabolismo , Neoplasias Pancreáticas/patologia , Fenilpropionatos/química , Fenilpropionatos/uso terapêutico , Extratos Vegetais/química , Raízes de Plantas/química , Raízes de Plantas/metabolismo , Transplante HeterólogoRESUMO
OBJECTIVE: To observe the efficacy differences between acupoint catgut embedding combined with auricular point pressure with beans and nilestriol on menopausal syndrome of liver-kidney deficiency type, and to explore their effects on estradiol (E2). METHODS: Sixty patients with menopausal syndrome of liver-kidney deficiency type were randomly divided into an acupoint stimulation group and a medication group, 30 cases in each group. The patients in the acupoint stimulation group were treated by acupoint catgut embedding at Taixi (KI 3), Sanyinjiao (SP 6), Shenshu (BL 23), Ganshu (BL 18) and Taichong (LR 3), combined with auricular point pressure at Gan (CO12), Shen (CO10), Neifenmi (CO18), Shenmen (TF4), Pizhixia (AT4); the treatment was given once a week for consecutive four weeks. The patients in the medication group were treated with oral administration of nilestriol, 1 mg, once a day, combined with oral administration of oryzanol, 20 mg, three times per day for consecutive four weeks. The clinical symptom score was compared between the two groups before and after treatment as well as in follow-up visit. The level of E2 was obserced before and after treatment, and the clinical effect was compared. RESULTS: (1) Compared before treatment, the clinical symptom score in the two groups was significantly reduced after treatment and in follow-up visit (all P<0.05); In follow-up visit, the clinical symptom score in the acupoint stimulation group was significantly lower than that in the medication group (P<0.05). The different value before treatment and at follow-up in the acupoint stimulation group was better than that in the medication group (P<0.05). (2) Compared before treatment, the level of E2 in the two groups were increased after treatment (both P<0.05); compared before and after treatment, the difference in the treatment group was significantly higher than that in the medication group (P<0.05). (3) After treatment, the total effective rate was 93.33% (28/30) in the acupoint stimulation group, which was similar to 90.00% (27/30) in the medication group (P>0.05). CONCLUSIONS: Compared with nilestriol, acupoint catgut embedding combined with auricular point pressure with beans could better improve clinical symptoms for patients with menopausal syndrome of liver-kidney deficiency type, and increased the level of E2.
Assuntos
Pontos de Acupuntura , Acupuntura Auricular/métodos , Categute , Menopausa , Quimioterapia Combinada/métodos , Estradiol/deficiência , Estrogênios/uso terapêutico , Feminino , Humanos , Rim , Fígado , Fenilpropionatos/uso terapêutico , Quinestrol/análogos & derivados , Quinestrol/uso terapêutico , Síndrome , Resultado do Tratamento , Deficiência da Energia Yang/complicaçõesRESUMO
BACKGROUND: Syringin, a major active substance isolated from Eleutherococcus senticosus, has been found to have anti-inflammatory effect. The aim of this study was to investigate the effects and underlying mechanisms of syringin on lipopolysaccharide (LPS)-induced acute lung injury (ALI) in mice. METHODS: We established an LPS-induced ALI model in mice. We also detected the lung wet-to-dry ratio, myeloperoxidase activity, and inflammatory cytokines tumor necrosis factor alpha, interleukin (IL)-1ß, and IL-6 to estimate the index of lung injury in mice. Furthermore, the expression of nuclear factor-erythroid 2-related factor-2 (Nrf2), heme oxygenase-1, and nuclear factor κB (NF-κB) was detected by Western blot analysis. RESULTS: The results showed that the increases in lung wet-to-dry ratio, myeloperoxidase activity, malondialdehyde content, and levels of tumor necrosis factor alpha, IL-1ß, and IL-6 induced by LPS were significantly inhibited by treatment of syringin. The phosphorylation of IκB-α and p65 NF-κB caused by LPS was inhibited by syringin. Furthermore, syringin was found to upregulate the expression of Nrf2 and heme oxygenase 1. CONCLUSIONS: In conclusion, the results suggest that syringin protects against LPS-induced ALI by activating Nrf2 and inhibiting NF-κB signaling pathway.
Assuntos
Lesão Pulmonar Aguda/prevenção & controle , Glucosídeos/uso terapêutico , Fenilpropionatos/uso terapêutico , Lesão Pulmonar Aguda/patologia , Animais , Citocinas/metabolismo , Avaliação Pré-Clínica de Medicamentos , Edema/prevenção & controle , Eleutherococcus , Heme Oxigenase-1/metabolismo , Lipopolissacarídeos , Pulmão/metabolismo , Pulmão/patologia , Masculino , Malondialdeído/metabolismo , Proteínas de Membrana/metabolismo , Camundongos Endogâmicos BALB C , Fator 2 Relacionado a NF-E2/metabolismo , NF-kappa B/metabolismo , Peroxidase/metabolismo , Fitoterapia , Extratos Vegetais/uso terapêuticoRESUMO
Acanthopanax senticosus (previously classified as Eleutherococcus senticosus), commonly known as Ciwujia or Siberian Ginseng, is a traditional Chinese medicine (TCM), widely used for its high medicinal value, such as antifatigue, anti-inflammation, antistress, anti-ulcer and cardiovascular functions, in China, Korea, Japan and Russia. In the past decades, researchers worldwide have conducted systematic investigations on this herb, from chemistry to pharmacology, and a large number of chemical components have been characterized for their significant pharmacological effects. However, reports about the anticancer effects of this plant had been rare until recently, when considerable pharmacological experiments both in vitro and in vivo were conducted to study the anticancer effects of this herb. A. senticosus has been found to have inhibitory effects on malignant tumors, such as those in the lung and liver, suggesting that A. senticosus has potential to be developed as an effective anticancer drug. This paper reviews recent findings on the pharmacological properties of A. senticosus, with a focus on its anticancer effects.
Assuntos
Antineoplásicos Fitogênicos/uso terapêutico , Cumarínicos/farmacologia , Cumarínicos/uso terapêutico , Dioxóis/farmacologia , Dioxóis/uso terapêutico , Eleutherococcus/química , Glucosídeos/farmacologia , Glucosídeos/uso terapêutico , Lignanas/farmacologia , Lignanas/uso terapêutico , Fenilpropionatos/farmacologia , Fenilpropionatos/uso terapêutico , Animais , Anti-Inflamatórios/uso terapêutico , Antioxidantes , Cumarínicos/isolamento & purificação , Dioxóis/isolamento & purificação , Relação Dose-Resposta a Droga , Glucosídeos/isolamento & purificação , Humanos , Fatores Imunológicos/uso terapêutico , Lignanas/isolamento & purificação , Medicina Tradicional Chinesa , Camundongos , Fenilpropionatos/isolamento & purificação , Fitoterapia , RatosRESUMO
OBJECTIVE: Previous studies demonstrated that a phenylpropenoic acid glucoside (PPAG) from rooibos (Aspalathus linearis) extract had anti-hyperglycemic activity and significant protective effects on the pancreatic beta cell mass in a chronic diet-induced diabetes model. The present study evaluated the cytoprotective effect of the phytochemical on beta cells exposed to acute cell stress. METHODS: Synthetically prepared PPAG was administered orally in mice treated with a single dose of streptozotocin to acutely induce beta cell death and hyperglycemia. Its effect was assessed on beta cell mass, proliferation and apoptotic cell death. Its cytoprotective effect was also studied in vitro on INS-1E beta cells and on human pancreatic islet cells. RESULTS: Treatment with the phytochemical PPAG protected beta cells during the first days after the insult against apoptotic cell death, as evidenced by TUNEL staining, and prevented loss of expression of anti-apoptotic protein BCL2 in vivo. In vitro, PPAG protected INS-1E beta cells from streptozotocin-induced apoptosis and necrosis in a BCL2-dependent and independent way, respectively, depending on glucose concentration. PPAG also protected human pancreatic islet cells against the cytotoxic action of the fatty acid palmitate. CONCLUSIONS: These findings show the potential use of PPAG as phytomedicine which protects the beta cell mass exposed to acute diabetogenic stress.