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1.
Braz. j. biol ; 83: e248755, 2023. tab, graf
Article in English | LILACS, VETINDEX | ID: biblio-1350303

ABSTRACT

Abstract Consuming a high-fat diet causes a harmful accumulation of fat in the liver, which may not reverse even after switching to a healthier diet. Different reports dealt with the role of purslane as an extract against high-fat diet; meanwhile, it was necessary to study the potential role of fresh purslane as a hypolipidemic agent. This study is supposed to investigate further the potential mechanism in the hypolipidemic effect of fresh purslane, by measuring cholesterol 7a-hydroxylase (CYP7A1) and low-density lipoprotein receptor (Ldlr). Rats were divided into two main groups: the first one is the normal control group (n=7 rats) and the second group (n=28 rats) received a high fat diet for 28 weeks to induce obesity. Then the high fat diet group was divided into equal four subgroups. As, the positive control group still fed on a high fat diet only. Meanwhile, the other three groups were received high-fat diet supplemented with a different percent of fresh purslane (25, 50 and 75%) respectively. At the end of the experiment, rats were sacrificed and samples were collected for molecular, biochemical, and histological studies. Current study reported that, supplementation of fresh purslane especially at a concentration of 75% play an important role against harmful effects of high-fat diet at both cellular and organ level, by increasing CYP7A1 as well as Ldlr mRNA expression. Also, there were an improvement on the tested liver functions, thyroid hormones, and lipid profile. Fresh purslane plays the potential role as a hypolipidemic agent via modulation of both Ldlr and Cyp7A, which will point to use fresh purslane against harmful effects of obesity.


Resumo O consumo de uma dieta rica em gordura causa um acúmulo prejudicial de gordura no fígado, que pode não reverter mesmo após a mudança para uma dieta mais saudável. Diferentes relatórios trataram do papel da beldroega como um extrato contra uma dieta rica em gordura; entretanto, foi necessário estudar o papel potencial da beldroega fresca como agente hipolipemiante. Este estudo pretende investigar mais profundamente o mecanismo potencial no efeito hipolipidêmico da beldroega fresca, medindo o colesterol 7a-hidroxilase (CYP7A1) e o receptor de lipoproteína de baixa densidade (Ldlr). Os ratos foram divididos em dois grupos principais: o primeiro é o grupo controle normal (n = 7 ratos) e o segundo grupo (n = 28 ratos) recebeu dieta rica em gorduras por 28 semanas para induzir a obesidade. Em seguida, o grupo de dieta rica em gordura foi dividido em quatro subgrupos iguais. Como, o grupo de controle positivo ainda se alimentava apenas com dieta rica em gordura. Enquanto isso, os outros três grupos receberam dieta rica em gordura suplementada com diferentes porcentagens de beldroegas frescas (25%, 50% e 75%), respectivamente. Ao final do experimento, os ratos foram sacrificados e amostras coletadas para estudos moleculares, bioquímica e histológicos. O estudo atual relatou que a suplementação de beldroegas frescas, especialmente a uma concentração de 75%, desempenha papel importante contra os efeitos prejudiciais da dieta rica em gordura em nível celular e orgânico, aumentando a expressão de CYP7A1 e Ldlr mRNA. Além disso, houve melhora nas funções hepáticas testadas, nos hormônios tireoidianos e no perfil lipídico. Beldroegas frescas desempenham papel potencial como agente hipolipemiante por meio da modulação de Ldlr e Cyp7A, o que apontará para o uso de beldroegas frescas contra os efeitos nocivos da obesidade.


Subject(s)
Animals , Rats , Portulaca , Diet, High-Fat/adverse effects , Hypolipidemic Agents , Cholesterol 7-alpha-Hydroxylase , Rats, Sprague-Dawley , Liver
2.
In. Soeiro, Alexandre de Matos; Leal, Tatiana de Carvalho Andreucci Torres; Accorsi, Tarso Augusto Duenhas; Gualandro, Danielle Menosi; Oliveira Junior, Múcio Tavares de; Caramelli, Bruno; Kalil Filho, Roberto. Manual da residência em cardiologia / Manual residence in cardiology. Santana de Parnaíba, Manole, 2 ed; 2022. p.830-834, tab.
Monography in Portuguese | LILACS | ID: biblio-1353529
3.
Braz. J. Pharm. Sci. (Online) ; 58: e191142, 2022. tab, graf
Article in English | LILACS | ID: biblio-1394056

ABSTRACT

A series of N-(benzoylphenyl)-carboxamide derivatives (2a, 2b, 3a, 3b, 4a, 4b, 5a, 5b, 6a and 6b) was prepared with good yields by reacting the corresponding carbonyl chlorides with aminobenzophenones at room temperature. This was followed by evaluating the hypotriglyceridemic and hypocholesterolemic effects of 3b, 5a and 5b. Triton WR-1339 (300 mg/kg) was intraperitoneally administered to overnight-fasted rats to induce hyperlipidemia. Rats were divided into six groups: control, hyperlipidemic, hyperlipidemic plus compounds 3b, 5a and 5b and hyperlipidemic plus bezafibrate. Results showed that after 18 h of treatment at a dose of 15 mg/kg body weight of each of the test compounds, the elevated plasma levels of triglycerides (TG) and total cholesterol (TC) were significantly lowered by compounds 5b and 3b (p < 0.001) and by 5a (p < 0.0001), compared to the hyperlipidemic control group. Compounds 3b and 5a significantly increased levels of high-density lipoprotein cholesterol (HDL-C) by 58 and 71%, respectively. In addition, compounds 3b and 5a caused significant reduction (p < 0.0001) of low-density lipoprotein cholesterol (LDL-C) levels compared to the control group. These results suggest a promising potential for compounds 3b, 5a and 5b as lipid-lowering agents, which may contribute to reducing the risk of atherosclerosis and cardiovascular disease


Subject(s)
Animals , Male , Rats , Pyridines/pharmacology , Hyperlipidemias/chemically induced , Lipids/blood , Hypolipidemic Agents/pharmacology , Polyethylene Glycols , Pyridines/chemical synthesis , Triglycerides/blood , Cholesterol/blood , Rats, Wistar , Disease Models, Animal , Lipoproteins, HDL/drug effects , Lipoproteins, LDL/drug effects , Hypolipidemic Agents/chemical synthesis
4.
Bol. latinoam. Caribe plantas med. aromát ; 20(2): 132-146, 2021. ilus, tab
Article in English | LILACS | ID: biblio-1342208

ABSTRACT

We investigated the effects of dichloromethane extract (DME) from Myrcia splendenson alterations caused by type 2 diabetes in the blood and kidney of rats, in order to reduce side effects caused by synthetic drugs. Rats received streptozotocin (60 mg/kg),15 minutes after nicotinamide (120 mg/kg) or water. After 72 hours, the glycemic levels were evaluated to confirm diabetes and the animals received (15 days) DME (25, 50, 100 or 150 mg/Kg) or water. DME partially reversed hyperglycemia and (100 and 150 mg/kg) reversed hypertriglyceridemia. Histopathological findings elucidated that DME reduced damage to pancreatic islets. DME 150 mg/kgreversed the increases in TBA-RS, the reduction in the sulfhydryl content, 100 and 150 mg/kg increased CAT, reversed the decrease in GSH-Px and increased it activity in the blood. DME 150 mg/kg reversed CAT and GSH-Px reductions in the kidney. We believe that DME effects might be dependent on the presence of phenolic compounds.


Investigamos los efectos del extracto de diclorometano (DME)de Myrcia splendens sobre las alteraciones causadas por la diabetes tipo 2 en la sangre y los riñones de las ratas, para reducir los efectos secundarios causados por las drogas sintéticas. Las ratas recibieron estreptozotocina (60 mg/kg), 15 minutos después de la nicotinamida (120 mg/kg) o agua. Después de 72 horas, se confirmo la diabetes y los animales recibieron (15 días) DME (25, 50, 100 o 150 mg/Kg) o agua. DME revierte parcialmente la hiperglucemia y revierte la hipertrigliceridemia. DME redujo el daño a los islotes pancreáticos. DME revirtió los aumentos en TBA-RS, la reducción en el contenido de sulfhidrilo, aumentó la CAT, revirtió la disminución en GSH-Px y aumentó su actividad en la sangre. Además, DME revirtió las reducciones de CAT y GSH-Px en el riñón. Creemos que los efectos provocados por DME pueden depender de la presencia de compuestos fenólicos.


Subject(s)
Animals , Male , Rats , Plant Extracts/administration & dosage , Myrtaceae/chemistry , Diabetes Mellitus, Experimental/drug therapy , Hypoglycemic Agents/administration & dosage , Methylene Chloride/administration & dosage , Blood Glucose/drug effects , Plant Extracts/chemistry , Chromatography, High Pressure Liquid , Rats, Wistar , Streptozocin , Oxidative Stress/drug effects , Spectrometry, Mass, Electrospray Ionization , Phenolic Compounds/analysis , Hypolipidemic Agents/administration & dosage , Antioxidants/administration & dosage
5.
Braz. J. Pharm. Sci. (Online) ; 57: e18901, 2021. tab, graf
Article in English | LILACS | ID: biblio-1350236

ABSTRACT

The plant, Malva neglecta wallr., is widely consumed for medicinal and nutritional purposes. The current study was carried out to assess the hypoglycemic and antihyperlipidemic potential of aqueous methanolic extract of M. neglecta. Chemical evaluation of the extract was performed by high pressure liquid chromatography. Oral glucose tolerance test (OGTT) was done in diabetic rats pre-exposed to 250, 500 and 750 mg/kg plant extract via the oral route. For hypoglycemic and biochemical study, the same therapy was administered to alloxan induced diabetic rats for 14 days. The standard control group received Glibenclamide (5 mg/kg). Ferulic acid, p-coumaric acid and other phenolic acids were detected and estimated in the extract. Administration of the plant extract significantly reduced blood glucose level in diabetic rats subjected to OGTT. The plant extract lowered the fasting blood glucose and alpha amylase, and prevented the damage to pancreas. It also corrected dyslipidemia in diabetic animals following 14 days therapy. Hence, this experimental study establishes the fact that M. neglecta exhibited significant antidiabetic and antihyperlipidemic activities in alloxan induced diabetic rats.


Subject(s)
Animals , Male , Female , Rats , Plant Extracts/analysis , Malvaceae/classification , Malva/adverse effects , Hyperglycemia/drug therapy , Hyperlipidemias/drug therapy , Hypolipidemic Agents/administration & dosage , Chromatography, High Pressure Liquid/methods
6.
Int. j. cardiovasc. sci. (Impr.) ; 33(4): 371-376, July-Aug. 2020. tab, graf
Article in English | LILACS | ID: biblio-1134382

ABSTRACT

Abstract Background The Adult Treatment Panel III (ATPIII) guidelines aim to reduce cardiovascular morbidity and mortality. In Ecuador, 20% of people have high LDL cholesterol levels, and 39% have high triglyceride levels. Objective To analyze lipid-lowering regimens in Ecuadorian patients and determine the achievement rate of the ATPIII goals for lipid profile. Methods Using a retrospective analysis, 385 subjects older than 30 years, who received pharmacological treatment for dyslipidemia for at least three months was randomly selected from institutions at two large cities in Ecuador. Data were collected from patients' medical records and analyzed by chi-square test or paired t-test; p-values less than 0.05 were considered significant. Results Baseline total cholesterol values were above 200 mg/dL in 75% of subjects, LDL-c values above 129 mg/dL in 83% of subjects and triglycerides values above 150 mg/dL in 79% of subjects. Most (n = 253, 95.8%) patients at very high cardiovascular risk were taking statins, 50% of them atorvastatin. Considering the ATPIII guidelines' goals, only 24 subjects (19%) at high CV risk achieved an LDL-c < 100 mg/dl, while a significantly lower percentage (p = 0.04) of patients at very high risk reached an LDL-c < 70mg/dl (11%; n = 30). Conclusion These data indicate a low rate of compliance with the ATPIII guidelines, independent of the medication used or duration of the treatment. This may be attributed to the prescription of low doses of medication and a therapy targeting isolated lipid fractions rather than a complete lipid profile. (Int J Cardiovasc Sci. 2020; 33(4):371-376)


Subject(s)
Humans , Male , Female , Middle Aged , Aged , Cardiovascular Diseases/prevention & control , Hypolipidemic Agents/therapeutic use , Triglycerides/blood , Cardiovascular Diseases/epidemiology , Cholesterol/blood , Retrospective Studies , Ecuador , Dyslipidemias/epidemiology , Heart Disease Risk Factors
8.
Article in Chinese | WPRIM | ID: wpr-828902

ABSTRACT

OBJECTIVE@#To investigate the triglyceride (TG)-lowering effects of PCSK9 inhibitor in patients with in different baseline triglyceride levels.@*METHODS@#Between February, 2019 and March, 2020, a total of 59 patients were treated with PCSK9 inhibitor (Evolocumab) in 5 hospitals, including Nanfang Hospital, Guangdong Provincial People's Hospital, First Affiliated Hospital of Sun Yat-sen University, Foshan Nanhai District People's Hospital and Yulin First People's Hospital. According to baseline triglyceride levels, the patients were divided into normal TG group (< 1.70 mmol/L, =24), mild hypertriglyceridemia group (1.70-2.29 mmol/L, =11), moderate hypertriglyceridemia group (2.30-5.63 mmol/L, =13), and severe hypertriglyceridemia group (≥5.64 mmol/L, =11), and the changes in TG level after the treatment were compared among the 4 groups.@*RESULTS@#In the groups with normal and mildly elevated baseline TG level, the patients did not show significant changes in TG levels after the treatment. In patients with moderately and severely elevated baseline TG levels, treatment with PCSK9 inhibitor significantly reduced their TG levels ( < 0.005).@*CONCLUSIONS@#PCSK9 inhibitor has a significant TG-lowering effect in patients with moderate to severe hypertriglyceridemia but not in patients with only mildly elevated baseline TG level.


Subject(s)
Humans , Hypertriglyceridemia , Hypolipidemic Agents , Proprotein Convertase 9 , Triglycerides
9.
J. bras. nefrol ; 41(3): 393-399, July-Sept. 2019. graf
Article in English | LILACS | ID: biblio-1040251

ABSTRACT

Abstract Lipoprotein glomerulopathy (LPG) is an uncommon cause of nephrotic syndrome and/or kidney failure. At microscopy, LPG is characterized by the presence of lipoprotein thrombi in dilated glomerular capillaries due to different ApoE mutations. ApoE gene is located on chromosome 19q13.2, and can be identified in almost all serum lipoproteins. ApoE works as a protective factor in atherosclerosis due its interaction with receptor-mediated lipoprotein clearance and cholesterol receptor. Most common polymorphisms include ApoE2/2, ApoE3/2, ApoE3/3, ApoE4/2, ApoE4/3, and ApoE4/4. All age-groups can be affected by LPG, with a discrete male predominance. Compromised patients typically reveal dyslipidemia, type III hyperlipoproteinemia, and proteinuria. LPG treatment includes fenofibrate, antilipidemic drugs, steroids, LDL aphaeresis, plasma exchange, antiplatelet drugs, anticoagulants, urokinase, and renal transplantation. Recurrence in kidney graft suggests a pathogenic component(s) of extraglomerular humoral complex resulting from abnormal lipoprotein metabolism and presumably associated to ApoE.


Resumo A glomerulopatia por lipoproteínas (GLP) é uma patologia rara que causa síndrome nefrótica e/ou insuficiência renal. Na microscopia, a GLP é caracterizada pela presença de trombos de lipoproteínas em capilares glomerulares dilatados devido a diferentes mutações no gene da ApoE. O gene da ApoE está localizado no cromossomo 19q13.2 e pode ser identificado em quase todas as lipoproteínas séricas. A ApoE age como fator de proteção na arterioesclerose por conta de sua interação com a depuração de lipoproteínas mediada por receptores e com o receptor de colesterol. Dentre os polimorfismos mais comuns destacam-se ApoE2/2, ApoE3/2, ApoE3/3, ApoE4/2, ApoE4/3 e ApoE4/4. A GLP pode acometer indivíduos de todas as faixas etárias, com discreta predominância do sexo masculino. Pacientes afetados tipicamente apresentam dislipidemia, hiperlipoproteinemia tipo III e proteinúria. O tratamento da GLP é conduzido com fenofibrato, antilipêmicos, corticosteroides, LDL-aferese, troca de plasma, antiplaquetários, anticoagulantes, uroquinase e transplante renal. Recidiva no enxerto renal indica a existência de componentes patogênicos do complexo humoral extraglomerular resultante de metabolismo lipoproteico anômalo, possivelmente associado a ApoE.


Subject(s)
Humans , Male , Female , Child, Preschool , Adult , Middle Aged , Kidney Diseases/pathology , Kidney Diseases/therapy , Apolipoproteins E/genetics , Sex Factors , Kidney Transplantation , Treatment Outcome , Kidney Diseases/complications , Kidney Diseases/genetics , Kidney Failure, Chronic/surgery , Kidney Failure, Chronic/etiology , Mutation , Hypolipidemic Agents/therapeutic use
10.
Med. UIS ; 32(1): 13-20, ene.-jun. 2019. tab, graf
Article in Spanish | LILACS | ID: biblio-1040390

ABSTRACT

Resumen Introducción: Los estudios de utilización de medicamentos sirven para evaluar la efectividad y seguridad de los fármacos en la práctica real, diferente al contexto del estudio clínico controlado. Los hipolipemiantes actúan sobre el perfil lipídico disminuyendo el riesgo de enfermedades cardiovasculares. Objetivo: Describir el desempeño clínico y seguridad de la utilización de medicamentos hipolipemiantes en la práctica médica real en una cohorte de pacientes con diagnóstico de dislipidemia. Metodología: Estudio observacional de cohorte. Se siguió una cohorte de pacientes con indicación de hipolipemiantes durante 6 meses, en 12 ciudades de Colombia pertenecientes a un registro biomédico de seguimiento de pacientes tratados con medicamentos del portafolio de Abbott. Se midieron variables demográficas y clínicas basales, de seguridad y de desempeño clínico de los medicamentos sobre el perfil lipídico a los 3 y 6 meses. Resultados: Se siguieron 501 pacientes en tratamiento con hipolipemiantes. Las estatinas solas disminuyeron el colesterol de baja densidad de 249 mg/ dL (RIQ=226-268) en la medición basal a 190 (177.6-210) y 170 (108-170) en la segunda y tercera medición, respectivamente. Para estatina + ezetimibe, de 167 mg/dL (RIQ=139-184) a 132 (110-150) y 128.5 (101.5-128.5). El fenofibrato disminuyó los triglicéridos de 275 mg/dL (RIQ=21çj-346) a 201 (172-239) y 150.5 (140-150.5). Conclusiones: la administración de estatinas sola o en combinación disminuyó los niveles de LDL y colesterol total, mientras que el fenofibrato demostró su efectividad al disminuir los triglicéridos. No se reportaron efectos adversos. Hubo una adherencia parcial del médico tratante a la guía de práctica clínica para dislipidemias. MÉD.UIS.2019;32(1):13-20.


Abstract Introduction: Drug use studies are important to evaluate the effectiveness and safety of drugs in daily practice, outside the controlled clinical study. Lipid-lowering drugs act on the lipid profile, decreasing the risk of cardiovascular diseases. Objective: To describe the clinical performance and safety of the use of lipid-lowering drugs in real practice in a group of patients diagnosed with dyslipidemia. Methods: An observational, descriptive cohort study. A cohort of patients with hypolipidemic indication for 6 months was followed in 12 cities of Colombia that belong to the biomedical registry of follow-up of patients treated with medicines from the Abbott portfolio. Baseline demographic and clinical variables, safety and efectivity of the drugs were measured on the lipid profile at 3 and 6 months. Results: 501 patients received lipid-lowering agents. Statins alone decreased the low density (LDL) cholesterol of 249 mg / dL (RIQ = 226-268) at baseline to 190 (177.6-210) and 170 (108-170) at the second and third measurements, respectively. For statin + ezetimibe, from 167 mg / dL (RIQ = 139-184) to 132 (110-150) and 128.5 (101.5-128.5). Fenofibrate decreased triglycerides from 275 mg / dL (RIQ = 219-346) to 201 (172-239) and 150.5 (140-150.5). Conclusions: The administration of statins alone or in combination decreased LDL and total cholesterol levels, while fenofibrate demonstrated its effectiveness in lowering triglycerides. No adverse effects were reported. There was partial adherence of the treating physician to GPC for dyslipidemias. There were no adverse events. MÉD.UIS.2019;32(1):13-20.


Subject(s)
Humans , Male , Female , Middle Aged , Aged , Hypolipidemic Agents , Medical Records , Cholesterol , Dyslipidemias , Pharmacovigilance
11.
Article in Korean | WPRIM | ID: wpr-787467

ABSTRACT

BACKGROUND: Colon cancer is one of the main causes of mortality. Early adenomatous colon polyp is a precursor of colon cancer through the ‘adenomacarcinoma sequence.’ Epidemiological studies suggest that the neutrophil to lymphocyte ratio can be one of useful inflammatory markers in clinical settings. This study aimed to evaluate the association between neutrophil to lymphocyte ratio and development of early adenomatous colon polyps.METHODS: This cross-sectional study retrospectively examined 960 middle-aged and elderly individuals aged ≥45 years who underwent colonoscopy in a health examination program. Multivariate logistic regression was used to analyze the association between neutrophil to lymphocyte ratio and development of early adenomatous colon polyps.RESULTS: Among the 960 subjects, the prevalence of early adenomatous polyps was 20.7% (n=199). The mean age, body mass index, number of current smokers, white blood cell count, triglyceride level, and number of subjects receiving hypolipidemic drugs were higher in the group with early adenomatous polyps than in the multivariate analysis, the odds ratio (95% confidence interval) for the development of early adenomatous polyps was 1.23 (1.01–1.50) with neutrophil to lymphocyte ratio increment after adjusting the confounding variables (P=0.037).CONCLUSION: We found that the neutrophil to lymphocyte ratio was associated with the development of early adenomatous colon polyps among middle-aged and elderly individuals. Accordingly, this result suggests that regular monitoring of early adenomatous colon polyps may be useful among individuals with a higher neutrophil to lymphocyte ratio.


Subject(s)
Adenomatous Polyps , Aged , Body Mass Index , Colon , Colonic Neoplasms , Colonic Polyps , Colonoscopy , Cross-Sectional Studies , Epidemiologic Studies , Humans , Hypolipidemic Agents , Korea , Leukocyte Count , Logistic Models , Lymphocytes , Middle Aged , Mortality , Multivariate Analysis , Neutrophils , Odds Ratio , Polyps , Prevalence , Retrospective Studies , Triglycerides
12.
Article in Chinese | WPRIM | ID: wpr-773713

ABSTRACT

Based on pharmacodynamics-component correlation analysis,the best effective part of hyperlipidemia of Pericarpium Citri Reticulatae( PCR) was screened out to confirm the possible constituents with the lipid regulating effect,in order to provide a basis for the development of new drugs. Hyperlipidemia rats induced by fat emulsion were used to screen out the best hypolipidemic parts of PCR with TC,LDL-c as the index. HPLC-ESI-MS were used to analyze common constituents of the different solvent extracts from PCR. The constituents were classified and identified based on the retention time,m/z and UV spectra. And the HPLC-DAD were used to determine the contents of flavonoids( narirutin,hesperidin,didymin,nobiletin,tangeretin,3,5,6,7,8,3',4'-heptemthoxyflavone).Correlation analysis was conducted on the constituents and efficacy with the method of SPSS ANOVA bivariate correlation. Five extracts could significantly decrease the content of TC,LDL-c of hyperlipemia rats induced by fat emulsion,and the best effective part were95% ethanol and ethyl acetate. There were 19 common peaks in five different solvent extracts from PCR,and 17 flavonoids were identified and classified,including 10 polymethoxyflavonoids and 7 other flavonoids. According to the raw material quantity,the order of content of flavonones arranged from high to low: n-butyl alcohol part> 95% ethanol part> water part> ethyl acetate part> petroleum ether part; and the order of PMFs arranged from high to low: n-butyl alcohol part≈95% ethanol part≈ethyl acetate part > petroleum ether part > water part. The decreased percentage of TC,LDL-c was positively correlated with 10 common PMFs constituents,which suggested that PMFs may be the effective components for reducing blood lipid.


Subject(s)
Animals , Chromatography, High Pressure Liquid , Citrus , Chemistry , Drugs, Chinese Herbal , Pharmacology , Flavonoids , Pharmacology , Hypolipidemic Agents , Pharmacology , Rats
13.
Article in Chinese | WPRIM | ID: wpr-773148

ABSTRACT

To study the binding capacity of active ingredients of Daidai lipid-lowering flavonoid extract and plasma protein,investigate the ways to improve the traditional formula for calculating protein binding rates based on ultrafiltration,and increase the stability and reliability of the experimental results. UPLC-MS/MS was used to establish a quantitative analysis method for simultaneous determination of active ingredients( neohesperidin and narngin) in ultrafiltrate. The protein binding rates were calculated by the traditional ultrafiltration formula. The correction factors( F) were introduced later,and the binding rates calculated with the correction factors were compared with those without the correction factors. The binding capacity of the extract and plasma protein was evaluated. The quantitative analysis method established by UPLC-MS/MS had a good specificity. The standard curve and linear range,method accuracy,precision and lower limit of quantitation all met the requirements. The method met the requirement for quantitative detection of the active ingredients in ultrafiltrate after the rat plasma was filtrated in the ultrafiltration tube. Under the experimental conditions,the binding rates of both active ingredients( neohesperidin and narngin) were higher than 90%. The active ingredients and rat plasma protein were bound in a concentration-dependent manner,with statistically significant differences( P<0. 01). There was no statistically significant difference between the protein binding abilities of the two active ingredients with rat plasma protein. Therefore,the active ingredients of Daidai lipid-lowering flavonoid extract had a relatively strong binding strength with rat plasma protein,and they were bound in a concentration-dependent manner. Additionally,when calculating protein binding rates by the traditional ultrafiltration formula,the correction factors could be introduced to effectively reflect the errors of multiple ingredient groups in traditional Chinese medicine extracts.This correction method could provide a reference thinking and practical reference for the improvement of the determination method of the traditional Chinese medicine plasma protein binding ability based on ultrafiltration.


Subject(s)
Animals , Blood Proteins , Chromatography, High Pressure Liquid , Drugs, Chinese Herbal , Pharmacology , Flavonoids , Pharmacology , Hypolipidemic Agents , Pharmacology , Lipids , Rats , Reproducibility of Results , Tandem Mass Spectrometry
14.
Chinese Journal of Traumatology ; (6): 142-147, 2019.
Article in English | WPRIM | ID: wpr-771620

ABSTRACT

PURPOSE@#To determine the relationship of illnesses and medical drug consumption with the occurrence of traffic accidents among truck and bus drivers.@*METHODS@#This is a cross-sectional study on truck and bus drivers in Tehran, Iran. The criteria for participating in this study were: married males over 30 years old, driving license in grade one, five years of job experience, mental health and non-addiction license. The criterion for not participating in this study was the lack of cooperation in responding to the questions. Six months was spent to collect the latest five years data of driving accidents from 2011 to 2016. A total of 323 truck and bus drivers in Tehran city and the suburbs, Iran were chosen. Among them, 112 were responsible for accidents (accident group) while 211 were not responsible for any accidents or involved in an accident in the last five years (non-accident group). A specially designed questionnaire was used to investigate the demographic information, medical drug consumption, medical backgrounds and history of accidents.@*RESULTS@#The results revealed that compared with healthy subjects, the occurrence of accidents among people with diabetes (OR = 2.3, p = 0.001) and vision weakness (OR = 1.7, p = 0.020) was significantly higher, while that among people with cardiac (OR = 0.5, p = 0.002) and hypertension (OR = 0.9, p = 0.048) problems was remarkably lower. Moreover, consumption of Gemfibrozil (OR = 1.8, p = 0.010) and Glibenclamide (OR = 2.2, p = 0.002) drugs resulted in significantly higher incidence of accidents than those without.@*CONCLUSION@#Frequencies of illnesses like cardiovascular and hypertension were not higher in accident drivers than in non-accident drivers; but diabetes, vision weakness and consumption of Gemfibrozil and Glibenclamide lead to more traffic accidents.


Subject(s)
Accidents, Traffic , Adult , Automobile Driving , Cross-Sectional Studies , Diabetes Mellitus , Epidemiology , Drug Utilization , Gemfibrozil , Glyburide , Humans , Hypolipidemic Agents , Incidence , Iran , Epidemiology , Male , Middle Aged , Surveys and Questionnaires , Vision Disorders , Epidemiology
17.
Article in Chinese | WPRIM | ID: wpr-775385

ABSTRACT

Hypolipidemic polysaccharides have notable activity and safety with a range of diverse sources. In this paper, the classification of hypolipidemic polysaccharides was carried out into polysaccharide sulfate, glycosaminoglycan, homopolysaccharide and heteropolysaccharide. The hypolipidemic activity mechanism and structure-activity relationship hypothesis of those polysaccharides in recent years were briefly reviewed therefore to provide references for the study and product development of polysaccharides.


Subject(s)
Hypolipidemic Agents , Chemistry , Pharmacology , Polysaccharides , Chemistry , Pharmacology , Structure-Activity Relationship
18.
Article in English | WPRIM | ID: wpr-773584

ABSTRACT

Farnesoid X receptor (FXR) is a member of the nuclear receptor superfamily of ligand-activated transcription factors. As a metabolic regulator, FXR plays key roles in bile acid and cholesterol metabolism and lipid and glucose homeostasis. Therefore, FXR is a potential drug target for several metabolic syndromes, especially those related to lipidemia disorders. In the present study, we identified small molecule SIPI-7623, a derivative of an extract from Oriental wormwood (Artemisia capillaris), and found that it specifically upregulated the expression of cholesterol-7-alpha-hydroxylase (CYP7A1), downregulated the expression of sterol-regulatory element-binding protein 1c (SREBP-1c) in the liver, and inhibited the expression of ileal bile acid binding-protein (IBABP) in the ileum of rats. We found that inhibition of FXR by SIPI-7623 decreased the level of cholesterol and triglyceride. SIPI-7623 reduced the levels of cholesterol and triglyceride in in vitro HepG2 cell models, ameliorated diet-induced atherosclerosis, and decreased the serum lipid content on rats and rabbits model of atherosclerosis in vivo. Furthermore, SIPI-7623 decreased the extent of atherosclerotic lesions. Our resutls demonstrated that antagonism of the FXR pathway can be employed as a therapeutic strategy to treat metabolic diseases such as hyperlipidemia and atherosclerosis. In conclusion, SIPI-7623 could be a promising lead compound for development of drugs to treat hyperlipidemia and atherosclerosis.


Subject(s)
Animals , Artemisia , Chemistry , Atherosclerosis , Drug Therapy , Genetics , Metabolism , Cholesterol , Metabolism , Cholesterol 7-alpha-Hydroxylase , Genetics , Metabolism , Drugs, Chinese Herbal , Humans , Hyperlipidemias , Drug Therapy , Genetics , Metabolism , Hypolipidemic Agents , Liver , Metabolism , Male , Rabbits , Rats , Rats, Sprague-Dawley , Receptors, Cytoplasmic and Nuclear , Genetics , Metabolism , Sterol Regulatory Element Binding Protein 1 , Genetics , Metabolism , Triglycerides , Metabolism
19.
Article in Chinese | WPRIM | ID: wpr-771480

ABSTRACT

OBJECTIVE@#To investigate the effects of sera from rats fed with tablets (HGT) on endoplasmic reticulum (ER) stress in a steatotic hepatocyte model of free fatty acids (FFAs)-induced nonalcoholic fatty liver disease (NAFLD) and explore the possible mechanism.@*METHODS@#FFAs prepared by mixing oleic acid and palmitic acid at the ratio of 2:1. HepG2 cells were treated with the sera from rats fed with low-, moderate-or high-dose HGT (HGT sera) or sera of rats fed with fenofibrate (fenofibrate sera), followed by treatment with 1 mmol/L FFAs for 24 h to induce hepatic steatosis. Oil red O staining was used to observe the distribution of lipid droplets in the cells. The biochemical parameters including triglyceride (TG), lactated hydrogenase (LDH), aspartate aminotransferase (AST) and alanine aminotransferase (ALT) were measured using a commercial kit. The morphological changes of the ER in the cells were observed using transmission electron microscopy. The protein/mRNA expressions of ER stress-related signal molecules including GRP78, PERK, p-PERK, ATF6, ATF4, CASPASE-12, CHOP, XBP-1, PKC, and p-PKC-δ were detected using Western blotting and/or quantitative real-time PCR (qRT-PCR). The changes in the protein expressions of GRP78, p-PERK, CASPASE-12 and CHOP were also detected in cells with transient transfection of PKC-δ siRNA for PKC-δ knockdown.@*RESULTS@#Compared with the control cells, the cells treated with FFAs showed significantly increased levels of TG, AST, and ALT ( < 0.05). Compared with FFAs-treated cells, the cells pretreated with HGT sera or fenofibrate sera all showed significantly decreased TG, AST and ALT levels ( < 0.05), reduced accumulation of the lipid droplets ( < 0.05), and lowered protein or mRNA expression levels of GRP78, p-PERK, ATF6, ATF4, CHOP, CASPASE-12, XBP-1 and p-PKC-δ ( < 0.05). PKC-δ knockdown caused significantly reduced protein expressions of GRP78, p-PERK, CASPASE-12 and CHOP in the cells with FFA-induced hepatic steatosis ( < 0.001); treatment with high-dose HGT serum more significantly reduced the expressions of GRP78 ( < 0.001) and P-PERK ( < 0.01) in FFAs-induced cells with PKC-δ knockdown.@*CONCLUSIONS@#HGT serum can effectively prevent FFAs-induced steatosis in HepG2 cells by alleviating ER stress, in which PKC-δ may act as an important target.


Subject(s)
Alanine Transaminase , Blood , Animals , Aspartate Aminotransferases , Blood , Disease Models, Animal , Drugs, Chinese Herbal , Endoplasmic Reticulum , Endoplasmic Reticulum Stress , Fatty Acids, Nonesterified , Fenofibrate , Hep G2 Cells , Humans , Hypolipidemic Agents , Microscopy, Electron, Transmission , Non-alcoholic Fatty Liver Disease , Blood , RNA, Messenger , Blood , Rats , Serum , Tablets , Triglycerides , Blood
20.
Article in English | WPRIM | ID: wpr-812373

ABSTRACT

Farnesoid X receptor (FXR) is a member of the nuclear receptor superfamily of ligand-activated transcription factors. As a metabolic regulator, FXR plays key roles in bile acid and cholesterol metabolism and lipid and glucose homeostasis. Therefore, FXR is a potential drug target for several metabolic syndromes, especially those related to lipidemia disorders. In the present study, we identified small molecule SIPI-7623, a derivative of an extract from Oriental wormwood (Artemisia capillaris), and found that it specifically upregulated the expression of cholesterol-7-alpha-hydroxylase (CYP7A1), downregulated the expression of sterol-regulatory element-binding protein 1c (SREBP-1c) in the liver, and inhibited the expression of ileal bile acid binding-protein (IBABP) in the ileum of rats. We found that inhibition of FXR by SIPI-7623 decreased the level of cholesterol and triglyceride. SIPI-7623 reduced the levels of cholesterol and triglyceride in in vitro HepG2 cell models, ameliorated diet-induced atherosclerosis, and decreased the serum lipid content on rats and rabbits model of atherosclerosis in vivo. Furthermore, SIPI-7623 decreased the extent of atherosclerotic lesions. Our resutls demonstrated that antagonism of the FXR pathway can be employed as a therapeutic strategy to treat metabolic diseases such as hyperlipidemia and atherosclerosis. In conclusion, SIPI-7623 could be a promising lead compound for development of drugs to treat hyperlipidemia and atherosclerosis.


Subject(s)
Animals , Artemisia , Chemistry , Atherosclerosis , Drug Therapy , Genetics , Metabolism , Cholesterol , Metabolism , Cholesterol 7-alpha-Hydroxylase , Genetics , Metabolism , Drugs, Chinese Herbal , Humans , Hyperlipidemias , Drug Therapy , Genetics , Metabolism , Hypolipidemic Agents , Liver , Metabolism , Male , Rabbits , Rats , Rats, Sprague-Dawley , Receptors, Cytoplasmic and Nuclear , Genetics , Metabolism , Sterol Regulatory Element Binding Protein 1 , Genetics , Metabolism , Triglycerides , Metabolism
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