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1.
ADMET DMPK ; 12(2): 335-341, 2024.
Artigo em Inglês | MEDLINE | ID: mdl-38720931

RESUMO

Background and purporse: The combination of alginate and gum acacia in previous studies showed good results in inhibiting ketoconazole precipitation due to the supersaturation phenomenon. Ketoconazole-loaded alginate and gum acacia can produce hydrogel beads through cross-linking with Ca2+ using ionotropic gelation techniques. However, the pharmacokinetic study of the ketoconazole beads loaded to alginate and gum acacia needs further investigation. This study aimed to evaluate pharmacokinetic parameters using rabbits via oral administration. Experimental approach: The drug was administered orally to 2 groups of rabbits: pure ketoconazole (KTZ) and formulation of ketoconazole (AG75) groups. Blood samples were obtained from the ear marginal vein at various time points: 0 (before administration), 15, 30, 45, 60, 90, 120, 150, 180, 240, 300, 360, and 420 minutes after oral dosage. The pharmacokinetic study employed a non-compartment analysis to calculate the area under the curve (AUC), the volume of distribution (Vd F-1), clearance (Cl F-1), maximum concentration (Cmax), and time to reach maximum concentration (tmax). The data obtained from the parameter result was analyzed using the independent-sample T-test. Key result: The results of the KTZ group include AUC of 15.83±0.62 h µg mL-1, VdF-1 of 8.95±1.17 mL, ClF-1 of 3.45±0.3 mL h-1, Cmax of 4.7±0.69 µg mL-1, and tmax of 1.67±0.17 h. The results of the AG75 group include AUC of 27.8±1.01 h µg mL-1, VdF-1 of 11.5±2.4 mL, ClF-1 of 2.15±0.11 mL h-1, Cmax of 4.49±0.52 µg mL-1, and tmax of 2.5±0.5 h. Conclusion: The formulation incorporating ketoconazole beads resulted in a higher AUC0-∞ than the pure ketoconazole. This finding suggests that the created formulation has enhanced the bioavailability of ketoconazole.

2.
Glob Health Sci Pract ; 12(2)2024 Apr 29.
Artigo em Inglês | MEDLINE | ID: mdl-38428996

RESUMO

The Sleman Health and Demographic Surveillance System (HDSS) is a longitudinal survey held routinely since 2014 to collect demographic, social, and health changes in Sleman Regency, Special Region of Yogyakarta, Indonesia. During the COVID-19 pandemic in Indonesia, we needed to adjust our method of conducting data collection from in-person to telephone interviews. We describe the Sleman HDSS data collection strategy used and the opportunities it presented. First, the Sleman HDSS team completed a feasibility study and adjusted the standard operational procedures to conduct telephone interviews. Then, the Sleman HDSS team collected data via a telephone interview in September-October 2020. Ten interviewers were equipped with an e-HDSS data collection application installed on an Android-based tablet to collect data. The sample targeted was 5,064 households. The telephone-based data collection successfully interviewed 1,674 households (33% response rate) in 17 subdistricts. We changed the data collection strategy so that the Sleman HDSS could still be conducted and we could get the latest data from the population. Compared to in-person interviewing, data collection via telephone was sufficiently practical. The telephone interview was a safe and viable data collection method. To increase the response rate, telephone number activation could be checked, ways of building rapport could be improved, and engagement could be improved by using social capital.


Assuntos
COVID-19 , Coleta de Dados , Telefone , Humanos , Indonésia/epidemiologia , COVID-19/epidemiologia , Coleta de Dados/métodos , Vigilância da População/métodos , SARS-CoV-2 , Pandemias , Entrevistas como Assunto , Feminino , Masculino , Adulto , Demografia , Estudos Longitudinais , Pessoa de Meia-Idade
3.
Ann Pharm Fr ; 82(4): 597-617, 2024 Jun.
Artigo em Inglês | MEDLINE | ID: mdl-38354976

RESUMO

Indonesia is the largest archipelagic country in the world, with 70% of its territory covered by oceans that are rich in various types of biological resources. Indonesia's biodiversity has made it possible to develop natural medicine. Marine algae have enormous potential, but the types of marine algae used still need to be more varied. Research on the pharmacology of marine macroalgae has been conducted in Indonesia, but studies on such topic related to diabetes mellitus (DM) still need to be completed. This study provides a comprehensive dataset of pharmacological anti-diabetic potential of marine macroalgae used for managing DM and reports on preclinical trials that provide pharmacological evidence. Data on the Indonesian marine macroalgae used to lower blood glucose were obtained from online sources. The bioactive chemicals of marine macroalgae have been found efficient at blocking several diabetes enzymes in in-vivo and in-vitro studies, and such chemicals have anti-inflammatory, anti-obesity, antioxidant, and other therapeutic benefits. The Google Scholar was used to search for the pharmacological literature with the keywords marine AND macroalgae AND diabetes AND Indonesia. Pharmacological research on the anti-diabetic activity of marine macroalgae has been carried out on five major Indonesian islands, including Sumatra, Kalimantan, Java, Sulawesi, and Papua, which encompassed 12 provinces: Southwest Papua, South Sulawesi, West Kalimantan, Riau Archipelago, Banten, West Java, North Sulawesi, East Java, Yogyakarta, Maluku, Jakarta, and Bengkulu. Articles on preclinical tests (in vitro and in vivo) were also used for the phytochemical problem section. The results briefly describe which class of algae has been widely used in Indonesia as an anti-diabetic. The findings of this research can be utilized to help find DM treatment drugs based on natural resources from marine macroalgae.


Assuntos
Diabetes Mellitus , Hipoglicemiantes , Alga Marinha , Indonésia , Alga Marinha/química , Humanos , Hipoglicemiantes/uso terapêutico , Hipoglicemiantes/farmacologia , Diabetes Mellitus/tratamento farmacológico , Animais
4.
Asian Pac J Cancer Prev ; 24(1): 75-80, 2023 Jan 01.
Artigo em Inglês | MEDLINE | ID: mdl-36708554

RESUMO

OBJECTIVE: Ficus septica is an Indonesian medicinal plant traditionally used to treat various illness, including cancer. The n-hexane insoluble fraction of the ethanolic extract of F. septica leaves (HIFFS) shows a potential anticancer activity against breast cancer cell line T47D. Considering that angiogenesis is a pivotal factor in malignant cancer growth, progression, and invasion, we aimed to investigate the antiangiogenic effect of HIFFS on chicken chorioallantoic membrane (CAM) induced by bFGF. We also evaluated tylophorine, the cytotoxic alkaloid of F. septica. METHODS: Chicken CAM was used to assess the antiangiogenic effect. Fertilized chicken eggs were induced with basic fibroblast growth factor (bFGF) ex ovo. Prior to bFGF induction, HIFFS (2.33, 4.65, 6.98, and 9.30 µg/mL) or tylophorine (9.20 µM) was added (10 µL) to a paper disk and implanted to the CAM. After 48 h of incubation, each treatment group was photographed, and the number of new blood vessel was calculated and compared with that in the solvent-treated group to determine the antiangiogenic activity. Histology of the CAM was evaluated after hematoxylin-eosin and Mallory acid fuchsin staining. RESULTS: We found that HIFFS at low concentrations (2.33, 4.65, 6.98, and 9.30 µg/mL) inhibited angiogenesis activity (31.87, 41.99, 53.65, and 70.08, respectively) in chicken CAM induced by bFGF. Tylophorine (9.20 µM) also showed similar antiangiogenesis activity in the same model. Histopathology analysis revealed that HIFFS and tylophorine reduced the number of new blood vessels in CAM induced by bFGF. CONCLUSION: HIFFS and tylophorine showed antiangiogenic effect on chicken CAM induced by bFGF. This finding emphasized the potential of F. septica as a candidate anticancer agent.


Assuntos
Alcaloides , Antineoplásicos , Ficus , Animais , Galinhas , Membrana Corioalantoide , Fator 2 de Crescimento de Fibroblastos , Alcaloides/farmacologia , Antineoplásicos/farmacologia , Inibidores da Angiogênese/farmacologia , Folhas de Planta
5.
Molecules ; 27(20)2022 Oct 14.
Artigo em Inglês | MEDLINE | ID: mdl-36296494

RESUMO

Co-administered medicinal herbs can modify a drug's pharmacokinetics (PK), effectiveness, and toxicity. Andrographis paniculata (Burm. f.) ethanolic extract (APE) and andrographolide (AND) (a potent CYP2C9 inducer/inhibitor) can alter the pharmacokinetic parameters of glipizide (GLZ). This study aimed to determine the potential pharmacokinetics of herb−drug interactions between GLZ and APE/AND in the plasma of normal and diabetic rats using the HPLC bioanalysis method. The glipizide bioanalytical method established with RP-HPLC/UV instrument was validated following the EMA guidelines. GLZ was administered alone and in combination with APE or AND to normal and diabetic rats. The GLZ pharmacokinetic parameters were estimated according to the correlation between concentration and sampling time using the PK solver program. A simple and rapid GLZ bioanalysis technique with a lower limit of quantitation of 25 ng/mL was developed and presented the following parameters: accuracy (error ≤ 15%), precision (CV ≤ 15%), selectivity, stability, and linearity (R2 = 0.998) at concentrations ranging 25−1500 ng/mL. APE administration significantly improved the Cmax and AUC0−t/AUC0−∞ GLZ values in normal and diabetic rats (p < 0.05). AND significantly reduced the bioavailability of GLZ in diabetic rats with small values of T 1/2, Cmax, and AUC0−t/AUC0−∞ (p < 0.05). This combination can be considered in administering medications because it can influence the pharmacological effects of GLZ.


Assuntos
Andrographis , Diabetes Mellitus Experimental , Diterpenos , Hominidae , Animais , Ratos , Interações Ervas-Drogas , Glipizida , Andrographis paniculata , Cromatografia Líquida de Alta Pressão , Diabetes Mellitus Experimental/tratamento farmacológico , Indutores do Citocromo P-450 CYP2C9 , Extratos Vegetais/farmacologia , Diterpenos/farmacologia
6.
Sci Rep ; 12(1): 4154, 2022 03 09.
Artigo em Inglês | MEDLINE | ID: mdl-35264693

RESUMO

Nonalcoholic fatty liver disease (NAFLD) is usually correlated with metabolic diseases, such as obesity, insulin resistance, and hyperglycemia. Herein, we investigated the inhibitory effects and underlying governing mechanism of clitorin in a western diet (WD)-induced hepatic steatosis mouse model, and in oleic acid-stimulated HepG2 cells. Male C57BL/6 mice were fed a normal diet, WD, WD + 10 or 20 mg/kg orlistat, and WD + 10 or 20 mg/kg clitorin. HepG2 cells were treated with 1 mM oleic acid to induce lipid accumulation with or without clitorin. Clitorin significantly alleviated body weight gain and hepatic steatosis features (NAFLD activity score, micro-, and macro-vesicular steatosis) in WD-induced hepatic steatosis mice. Additionally, clitorin significantly decreased protein expressions of sterol regulatory element-binding protein 1 (SREBP1), peroxisome proliferator-activated receptor γ (PPARγ), and CCAAT/enhancer binding protein α (C/EBPα) in WD-induced hepatic steatosis mice. Moreover, clitorin significantly diminished the mRNA levels of SREBP1, acetyl-CoA carboxylase (ACC), fatty acid synthase (FAS), and hydroxy-3-methylglutaryl coenzyme A reductase (HMGCR) and enhanced the mRNA levels of peroxisome proliferator-activated receptor α (PPARα) and carnitine palmitoyltranserase-1 (CTP-1), as well as adenosine monophosphate-activated protein kinase (AMPK) in the liver of WD-induced hepatic steatosis mice and oleic acid-stimulated HepG2 cells. Overall, our findings demonstrated that clitorin can be a potentially efficacious candidate for NAFLD management.


Assuntos
Lipogênese , Hepatopatia Gordurosa não Alcoólica , Animais , Dieta Hiperlipídica , Dieta Ocidental/efeitos adversos , Glicosídeos , Células Hep G2 , Humanos , Quempferóis , Fígado/metabolismo , Masculino , Camundongos , Camundongos Endogâmicos C57BL , Hepatopatia Gordurosa não Alcoólica/tratamento farmacológico , Hepatopatia Gordurosa não Alcoólica/etiologia , Ácido Oleico/metabolismo , Ácido Oleico/farmacologia , RNA Mensageiro/metabolismo
7.
Adv Pharm Bull ; 11(1): 171-180, 2021 Jan.
Artigo em Inglês | MEDLINE | ID: mdl-33747864

RESUMO

Purpose: Insulin resistance is a characteristic of non-insulin-dependent diabetes mellitus associated with obesity and caused by the failure of pancreatic beta cells to secrete sufficient amount of insulin. Andrographolide (AND) improves beta-cell reconstruction and inhibits fat-cell formation. This research aimed to improve the delivery of water-insoluble AND in self-nanoemulsifying (ASNE) formulation, tested in streptozotocin (STZ)-induced diabetic rats and 3T3-L1 preadipocyte cells. Methods: A conventional formulation of AND in suspension was used as a control. The experimental rats were orally administered with self-nanoemulsifying (SNE) and suspension of AND for 8 days. Measurements were performed to evaluate blood glucose levels in preprandial and postprandial conditions. Immunohistochemistry was used to assess the process of islet beta cell reconstruction. In vitro study was performed using cell viability and adipocyte differentiation assay to determine the delivery of AND in the formulation. Results: ASNE lowered blood glucose levels (day 4) faster than AND suspension (day 6). The histological testing showed that ASNE could regenerate pancreatic beta cells. Therefore, ASNE ameliorated pancreatic beta cells. The in vitro evaluation indicated the inhibition of adipocyte differentiation by both AND and ASNE, which occurred in a time-dependent manner. ASNE formulation had better delivery than AND. Conclusion: ASNE could improve the antidiabetic activity by lowering blood glucose levels, enhancing pancreatic beta cells, and inhibiting lipid formation in adipocyte cells.

8.
World J Gastroenterol ; 27(1): 107-128, 2021 Jan 07.
Artigo em Inglês | MEDLINE | ID: mdl-33505154

RESUMO

BACKGROUND: Shifting on lifestyle, diet, and physical activity contributed on increasing number of obese people around the world. Multiple factors influence the development of obesity. Some research suggested that gut microbiota (GM) plays an important role in nutrient absorption and energy regulation of individuals, thus affecting their nutritional status. Report of Indonesia Basic Health Research showed that the prevalence of obesity in every province tended to increase. Although the root cause of obesity is excessive calorie intake compared with expenditure, the differences in gut microbial ecology between healthy and obese humans may affect energy homeostasis. GM affect body weight, especially obesity. Probiotics that are consumed while alive and able to colonize in the intestine are expected to increase the population of good bacteria, especially Bifidobacteria and Lactobacilli, and suppress pathogens such as Enterobacteriaceae and Staphylococcus. The strain of L. plantarum Dad-13 has been demonstrated to survive and colonize in the gastrointestinal tract of healthy Indonesian adults who consume fermented milk containing L. plantarum Dad-13. The consumption of probiotic L. plantarum Dad-13 powder decreased E. coli and non-E. coli coliform bacteria in school-aged children in Indonesia. L. plantarum is a dominant bacterium in the average Indonesian's GM. For this reason, this bacterium is probably a more suitable probiotic for Indonesians. AIM: To determine the effect of the consumption of indigenous probiotic Lactobacillus plantarum Dad-13 powder in overweight adults in Yogyakarta (Indonesia). METHODS: Sixty overweight volunteers with a body mass index (BMI) equal to or greater than 25 consume indigenous probiotic powder L. plantarum Dad-13 (2 × 109 CFU/gram/sachet) for 90 d. The study was a randomized, double-blind, placebo-controlled study. The volunteers filled in a diary on a daily basis, which consisted of questions on study product intake (only during ingestion period), other food intake, number of bowel movements, fecal quality (consistency and color), any medications received, and any symptom of discomfort, such as diarrhea, constipation, vomiting, gassing, sensation of illness, etc. Fecal samples and the subjects' diaries were collected on the morning of day 10 + 1, which was marked as the end of the baseline period and the start of the ingestion period. During the ingestion period (from day 11 to day 101), several parameters to measure and analyze the results included body weight and height (once a month), the lipid profile, GM analysis using MiSeq, short-chain fatty acid (SCFA) analysis using gas chromatography, and the measurement of fecal pH using a pH meter. RESULTS: The consumption of indigenous probiotic powder L. plantarum Dad-13 caused the average body weight and BMI of the probiotic group to decrease from 84.54 ± 17.64 kg to 83.14 ± 14.71 kg and 33.10 ± 6.15 kg/m2 to 32.57 ± 5.01 kg/m2, respectively. No significant reduction of body weight and BMI in the placebo group was observed. An analysis of the microbiota showed that the number of Bacteroidetes, specifically Prevotella, increased significantly, while that of Firmicutes significantly decreased. No significant change in lipid profile in both groups was found. Also, no significant change in SCFAs (e.g., butyrate, propionate, acetic acid) and pH level was found after the consumption of the probiotic. CONCLUSION: No significant differences in pH before and after ingestion were observed in both the probiotic and placebo groups as well as in the lipid profile of both cholesterol and triglyceride, high-density lipoprotein (HDL), low-density lipoprotein (LDL), and the LDL/HDL ratio. In addition, no significant changes in the concentration of SCFAs (e.g., acetic acid, propionate, and butyrate) were found after con-sumption. Interestingly, a significant decrease in body weight and BMI (P < 0.05) was determined in the treatment group. An analysis of GM shows that L. plantarum Dad-13 caused the Firmicutes population to decrease and the Bacteroidetes population (especially Prevotella) to increase.


Assuntos
Microbioma Gastrointestinal , Lactobacillus plantarum , Probióticos , Adulto , Criança , Método Duplo-Cego , Escherichia coli , Fezes , Humanos , Indonésia/epidemiologia , Pós , Probióticos/uso terapêutico
9.
Biomed Pharmacother ; 135: 111197, 2021 Mar.
Artigo em Inglês | MEDLINE | ID: mdl-33433362

RESUMO

Prostatitis, defined as a pathological inflammatory change in the prostate tissue, is one of the most prevalent urological conditions in men. However, optimal management of prostatitis remains unclear, and treatment outcomes are unsatisfactory owing to adverse effects. Carica papaya leaf extract (PAL) is known for its antioxidant, immunomodulatory, and anticancer properties; however, evidence of its anti-inflammatory effect in prostatic tissues remains elusive. In this study, the therapeutic effects and underlying molecular mechanisms of PAL in mice with experimental autoimmune prostatitis (EAP) and a prostatic cell line (RWPE-1 cells) exposed to inflammatory conditioned medium were investigated. PAL suppressed pathological alterations in EAP and markedly reduced prostate weight in EAP mice. Histological analysis revealed that PAL alleviates prostatic hyperplasia. Furthermore, PAL significantly reduced cyclooxygenase-2 mRNA and protein expression; production of inflammatory cytokines, including interleukin-6, tumor necrosis factor-α, and transforming growth factor-ß; and TRAF6/TAK1/MEK/ERK and NF-κB pathway-related protein expression. TRAF6/TAK1/MEK/ERK and NF-κB pathway-related proteins were upregulated in inflammatory conditioned medium-stimulated RWPE-1 cells, but PAL reduced the expression of these markers. Particularly, PAL treatment suppressed the nuclear translocation of NF-κB p65 and phosphorylation of p65 in RWPE-1 cells exposed to the inflammatory conditioned medium. Collectively, the results demonstrate the anti-proliferative and anti-inflammatory effects of PAL in the experimental prostatitis model, which highlights the potential of PAL as a new therapeutic agent in the treatment of prostatic disease.


Assuntos
Anti-Inflamatórios/farmacologia , Carica , MAP Quinase Quinase Quinases/metabolismo , NF-kappa B/metabolismo , Extratos Vegetais/farmacologia , Próstata/efeitos dos fármacos , Hiperplasia Prostática/prevenção & controle , Prostatite/tratamento farmacológico , Fator 6 Associado a Receptor de TNF/metabolismo , Animais , Anti-Inflamatórios/isolamento & purificação , Carica/química , Linhagem Celular , Proliferação de Células/efeitos dos fármacos , Citocinas/metabolismo , Modelos Animais de Doenças , Finasterida/farmacologia , Mediadores da Inflamação/metabolismo , Masculino , Camundongos Endogâmicos BALB C , Extratos Vegetais/isolamento & purificação , Folhas de Planta , Próstata/enzimologia , Próstata/patologia , Hiperplasia Prostática/enzimologia , Hiperplasia Prostática/patologia , Prostatite/enzimologia , Prostatite/patologia , Ratos Wistar , Transdução de Sinais
10.
Data Brief ; 30: 105611, 2020 Jun.
Artigo em Inglês | MEDLINE | ID: mdl-32395582

RESUMO

The performance of the vortex tube is low compared to a conventional heat pump engine based on Freon refrigerants, and therefore, there is a need for an experiment on how to improve its efficiency. This data article aims to analyze the effect of the new vortex tube design on cold temperature (Tc ), hot temperature (Th ), delta cold temperature (ΔTc ), delta hot temperature (ΔTh ), heat transferred as cooling effect ( Q ˙ c ) , heat transferred as heating effect ( Q ˙ h ) , isentropic efficiency as cooling effect (η isc ), isentropic efficiency as heating effect (η isc ), the coefficient of performance refrigeration (COPref ), and coefficient of performance heat pump (COPh ), which is tested based on pressure and fraction variations. The data were obtained from the experimental measurements. Data were collected at conditions with temperature controlled at 27 ± 0.1°C. All measuring instruments were supposed to be consistent for at least 5 min for data to be collected, although retrieval was conducted 4 times.

11.
Data Brief ; 30: 105521, 2020 Jun.
Artigo em Inglês | MEDLINE | ID: mdl-32420418

RESUMO

This experiment uses the Municipal Solid Waste (MSW) from households and traditional markets as feed materials in the Integrated Downdraft Gasifier and Multi Integrated Gas Cleaner System (IGCS). The IGCS consist of cyclone, rectangular venturi scrubber, and rotary separator. The data from the experiment show the gasification characteristics such as temperature, Low Heating Value (LHV) and tar content. The parameter consists of Air Fuel ration (AFR) at 0.48, 0.5, 0.54 scrubbing water discharge at 1.26, 2.62, 3.33 l/min, and 0.9 rotary separator using suction speed at 0.9, 3.4, 4.4 m/s, respectively. The data also show the power output of the plant and energy balance of the system. This data can be used as reference for the further development of Integrated Downdraft Gasifier and Multi-Integrated Gas Cleaner systems.

12.
J Ethnopharmacol ; 249: 112396, 2020 Mar 01.
Artigo em Inglês | MEDLINE | ID: mdl-31743763

RESUMO

ETHNOPHARMACOLOGICAL RELEVANCE: In silico data revealed that the active compound of ginger (Zingiber officinale Roscoe), 6-shogaol, has strong affinity toward transient receptor potential vanilloid-1 (TRPV-1). TRPV-1 is expressed in nervous tissue and pancreatic ß-cells. Prolonged induction of TRPV-1 is related to the expression of N-methyl-D-aspartate receptor subunit 2B (NMDAR2B). However, there are no data on TRPV-1 and NMDAR2B expressions in nervous tissue after 6-shogaol or ginger extract treatment nor pancreatic islet morphology and insulin expression in mice model of painful diabetic neuropathy (PDN). AIM OF THE STUDY: This study aimed to investigate the mechanism of action of ginger extract and its compound, 6-shogaol, on pancreatic islets as well as on expressions of TRPV-1 and NMDAR2B in the spinal cord of streptozotocin (STZ)-induced mice model of PDN. MATERIALS AND METHODS: Sixty-four 5-6 weeks old male-Balb/C mice were induced with 110 mg/kgBW STZ i.p., while eight mice were used as control group. Mice with blood glucose level ≥200 mg/d, that suffered hyperalgesia and allodynia were classified as PDN mice. Hot plate and von Frey filament tests were performed once a week until termination. At day 28 after considered as PDN, ginger extracts, 6-shogaol or gabapentin as control treatment were given once daily for 21 days until day 49, except for the diabetic control group. Upon termination, mice' pancreas were fixed, processed as paraffin sections and stained with hematoxylin eosin. Total volume of pancreatic islets was estimated using Cavalieri methods. Immunohistochemistry on pancreatic sections were performed to observe insulin expression. mRNA was extracted from lumbar segments of the spinal cord, followed by cDNA preparation and quantitative Real-Time Polymerase Chain Reaction (qRT-PCR) to measure the expressions of TRPV1 and NMDAR2B. The mean differences between groups were analyzed using one-way analysis of variance (ANOVA) with p < 0.05 considered statistically significant. RESULTS: Ginger extracts and 6-shogaol alleviated hyperalgesia and allodynia. The groups that received ginger extract 400 mg/kgBW or 6-shogaol 15 mg/kgBW had significantly lower TRPV1 and NMDAR2B expressions in the spinal cord compared to the diabetic control group (p < 0.001; p < 0.05). However, no differences in volume of pancreatic islets (p > 0.05) nor insulin expression were observed in all PDN groups. CONCLUSION: Ginger extracts and its compound, 6-shogaol, reduced pain symptoms in PDN via its effect on decreasing TRPV1 and NMDAR2B expressions in the spinal cord, with very limited effect on pancreatic islets.


Assuntos
Catecóis/farmacologia , Neuropatias Diabéticas/tratamento farmacológico , Extratos Vegetais/farmacologia , Medula Espinal/efeitos dos fármacos , Zingiber officinale/química , Animais , Catecóis/isolamento & purificação , Diabetes Mellitus Experimental/tratamento farmacológico , Neuropatias Diabéticas/patologia , Hiperalgesia/tratamento farmacológico , Insulina/metabolismo , Ilhotas Pancreáticas/efeitos dos fármacos , Ilhotas Pancreáticas/metabolismo , Masculino , Camundongos , Camundongos Endogâmicos BALB C , Receptores de N-Metil-D-Aspartato/metabolismo , Medula Espinal/metabolismo , Estreptozocina , Canais de Cátion TRPV/metabolismo
14.
Nat Prod Res ; 33(6): 814-821, 2019 Mar.
Artigo em Inglês | MEDLINE | ID: mdl-29224362

RESUMO

Three acacetin triglycosides (compounds 1, 2 and 3) were isolated from the herbs of Elsholtzia ciliata (Labiatae). The structure were identified as 7-O-ß-D-glucopyranosyl-(1 â†’ 2)[α-L-rhamnopyranosyl-(1 â†’ 6)]-ß-D-glucopyranoside (compound 1), 7-O-(6-O-acetyl)-ß-D-glucopyranosyl-(1 â†’ 2)[α-L-rhamnopyranosyl-(1 â†’ 6)]-ß-D-glucopyranoside (compound 2) and 7-O-(6-O-acetyl)-ß-D-glucopyranosyl-(1 â†’ 2)[(4-O-acetyl)-α-L-rhamnopyranosyl-(1 â†’ 6)]-ß-D-glucopyranoside (compound 3) of acacetin. The structures of these compounds were determined on the basis of 2D-NMR spectroscopic data. Compound 3 has not been isolated from a natural source. In addition, the three compounds were quantitatively analysed by HPLC. Acetylcholinesterase (AChE) inhibition activity was assayed to find anti-Alzheimer's activity, since this enzyme increases the concentration of acetylcholine (ACh), a neurotransmitter, responsible for brain's memory. Acacetin, the aglycone of the three compounds, exhibited a potent anti-cholinesterase activity (IC50, 50.33 ± 0.87), though its glycosides (1, 2 and 3) were less active. HPLC analysis demonstrated that the three compounds were contained in the MeOH extract in the order of compounds 2 (12.63 mg/g extract) > 3 (3.10 mg/g) > 1 (2.92 mg/g).


Assuntos
Inibidores da Colinesterase/química , Flavonas/química , Glicosídeos/química , Lamiaceae/química , Acetilcolinesterase , Inibidores da Colinesterase/isolamento & purificação , Cromatografia Líquida de Alta Pressão , Flavonas/isolamento & purificação , Glicosídeos/isolamento & purificação , Espectroscopia de Ressonância Magnética , Estrutura Molecular , República da Coreia
15.
Asian Pac J Cancer Prev ; 19(11): 3065-3069, 2018 Nov 29.
Artigo em Inglês | MEDLINE | ID: mdl-30485942

RESUMO

Background: The effects of tylophorine, a natural alkaloid found in Tylophora indica, administered as a single compound or in combination with doxorubicin on cell cycling and apoptosis were assessed in T47D breast cancer cells, selected as a model system for breast cancer. Methods: Cell cycle distribution and apoptosis were examined by flow cytometry. Caspase 3 and 9 expression was determined by immunocytochemistry.Result: We found that tylophorine did not significantly influence the cell cycle distribution of T47D cells. However, the alkaloid did prevent accumulation of cells in the G2/M phase. In addition, tylophorine increased the number of apoptotic cells. Expression of proapoptotic proteins (caspases 3 and 9) was up-regulated upon administration of tyloporine alone or in combination with doxorubicin. Conclusions: Tylophorine alone or in combination with doxorubicin induced apoptosis in T47D breast cancer cells through modulation of the cell cycle and affecting the expression of caspases 3 and 9.


Assuntos
Alcaloides/farmacologia , Antibióticos Antineoplásicos/farmacologia , Apoptose/efeitos dos fármacos , Neoplasias da Mama/patologia , Ciclo Celular/efeitos dos fármacos , Doxorrubicina/farmacologia , Indolizinas/farmacologia , Fenantrenos/farmacologia , Neoplasias da Mama/tratamento farmacológico , Proliferação de Células/efeitos dos fármacos , Quimioterapia Combinada , Feminino , Humanos , Células Tumorais Cultivadas
16.
Scand J Public Health ; 46(7): 704-710, 2018 Nov.
Artigo em Inglês | MEDLINE | ID: mdl-28752803

RESUMO

BACKGROUND: This paper describes the methodological considerations of developing an urban Health and Demographic Surveillance System (HDSS), in the Sleman District of Yogyakarta, Indonesia. METHODS: 1) The Sleman District was selected because it is mostly an urban area. 2) The minimum sample size was calculated to measure infant mortality as the key variable and resulted in a sample of 4942 households. A two-stage cluster sampling procedure with probability proportionate to size was applied; first, 216 Censuses Blocks (CBs) were selected, and second, 25 households in each CB were selected. 3) A baseline survey was started in 2015, and collected data on demographic and economic characteristics and verbal autopsy (VA); the 2nd cycle collected updated demographic data, VA, type of morbidity (communicable and non-communicable diseases, disability and injury) and health access. 4) The data were collected at a home visit through a Computer-Assisted Personal Interview (CAPI) on a tablet device, and the data were transferred to the server through the Internet. 5) The quality control consisted of spot-checks of 5% of interviews to control for adherence to the protocol, re-checks to ensure the validity of the interview, and computer-based data cleaning. 6) A utilization system was designed for policy-makers (government) and researchers. RESULTS: In total, 5147 households participated in the baseline assessment in 2015, and 4996 households participated in the second cycle in 2016 (97.0% response rate). CONCLUSIONS: Development of an urban HDSS is possible and is beneficial in providing data complementary to the existing demographic and health information system at local, national and global levels.


Assuntos
Vigilância da População/métodos , Saúde da População Urbana , Coleta de Dados , Demografia , Humanos , Indonésia , Estudos Longitudinais , Projetos de Pesquisa , Inquéritos e Questionários
17.
Asian Pac J Trop Med ; 10(11): 1043-1046, 2017 Nov.
Artigo em Inglês | MEDLINE | ID: mdl-29203099

RESUMO

OBJECTIVE: To investigate the effects of friedelin (terpenoid) and 8-hydroxyisocapnolactone-2-3-diol (coumarin) with concentration 10 µM, 30 µM, and 100 µM on inhibiting mast cells (MCs) degranulation. METHODS: The investigation was performed in vitro by administering each compound into rat peritoneal MCs and rat basophilic leukemia-2H3 cells followed by activation with 50 µg/mL of compound 48/80 or 1 µM of ionomycin. The concentration of histamine released from each group was measured by a high-performance liquid chromatography-fluorometry system with post-column derivatization using o-phthalaldehyde. RESULTS: 8-Hydroxyisocapnolactone-2-3-diol inhibited degranulation of compound 48/80 activated-rat peritoneal MCs with the histamine release percentages of 74.57%, 72.21% and 51.79% when the 10 µM, 30 µM and 100 µM concentrations were used, respectively. Where as about 81% histamine was released by the control group. Degranulation inhibition ability was also observed in ionomycin-activated rat basophilic leukemia-2H3 cells. In contrast, friedelin failed to inhibit degranulation in either cell type. The inhibition of 8-hydroxyisocapnolactone-2-3-diol was not related to the depletion of histamine synthesis as implied by the total histamine measurement. CONCLUSIONS: These results exhibit the promising of 8-hydroxyisocapnolactone-2-3-diol is a potential parent structure for developing a MCs stabilizer.

18.
Food Funct ; 8(7): 2611-2620, 2017 Jul 19.
Artigo em Inglês | MEDLINE | ID: mdl-28695925

RESUMO

Although Aster glehni has been reported to prevent diabetes mellitus, hypercholesterolemia, insomnia, and cardiovascular disease, the anti-inflammatory effect of Aster glehni in colonic tissue remains unclear. In this study, we investigated the anti-inflammatory effects and the underlying molecular mechanism of an ethanol extract of Aster glehni (AG) in mice with dextran sulfate sodium (DSS)-induced colitis. AG significantly attenuated DSS-induced DAI scores, which implied that it suppressed diarrhea, gross bleeding, and the infiltration of immune cells. AG administration also effectively prevented shortening of the colon length and enlargement of the spleen size. Histological examinations indicated that AG suppressed colonic damage and the thickness of the muscle layer induced by DSS. In addition, AG inhibited the production of pro-inflammatory cytokines, such as TNF-α, IL-1ß, and IL-6, and the protein expression of COX-2 and iNOS in mice with DSS-induced colitis. Administration with AG suppressed the activation of nuclear factor-κB (NF-κB) including the nuclear translocation of the p65 NF-κB subunit, phosphorylation and degradation of IκB-α. Taken together, these findings suggest that the anti-inflammatory effects of AG are mainly related to the inhibition of the expressions of inflammatory mediators via NF-κB inactivation, and support its possible therapeutic application in colitis.


Assuntos
Anti-Inflamatórios/administração & dosagem , Aster/química , Colite/tratamento farmacológico , NF-kappa B/imunologia , Extratos Vegetais/administração & dosagem , Animais , Colite/induzido quimicamente , Colite/genética , Colite/imunologia , Sulfato de Dextrana/efeitos adversos , Modelos Animais de Doenças , Humanos , Interleucina-1beta/genética , Interleucina-1beta/imunologia , Interleucina-6/genética , Interleucina-6/imunologia , Macrófagos/efeitos dos fármacos , Macrófagos/imunologia , Masculino , Camundongos , NF-kappa B/genética , Fator de Necrose Tumoral alfa/genética , Fator de Necrose Tumoral alfa/imunologia
19.
Artigo em Inglês | MEDLINE | ID: mdl-29644814

RESUMO

Papua is one of five provinces with high malaria incidence in Indonesia. In 2009, the Indonesian Ministry of Health issued decree No 293 on malaria elimination. Socioeconomic, culture and psychological conditions, and perception of malaria are determining factors in seeking treatment. Health seeking behavior also are influenced by enabling factors, such as income and health insurance; and by health providers, such as availability of health care facilities, tariffs and living locationss. Self-care is one form of community participation in knowledge, prevention and early detection of malaria, and in seeking treatment and compliance to malaria treatment, especially among inhabitants in malaria endemic areas. This study was an observation in Nimboran Subdistrict, Jayapura District, Papua Province, Indonesia during 2013. Thirty individuals from 'Pengurus Rukun Tetangga' group were chosen randomly for the survey. Facts evaluated were knowledge of cause of malaria, disease transmission, symptoms and complication, diagnosis, treatment and side effects, medical seeking behavior and treatment, vector breeding sites, and attitude towards compliance of malaria treatment and use of mosquito nets. Self-care against malaria was considered important by 65% of the respondents. All participants had visited health centers and complied with prescribed drug regimen. All respondents with malaria-infected neighbors visited health centers. Regarding antimalarial malaria drugs, the majority of respondents knew of Darplex® and were aware that a common side effect of antimalarials was tinnitus. The majority of respondents identified ponds as malaria vector breeding places and recognized the importance of managing vectors in malaria prevention. The study concludes that malaria self-care was needed for awareness, prevention and treatment of this debilitating disease.


Assuntos
Malária/epidemiologia , Malária/terapia , Autocuidado , Antimaláricos/administração & dosagem , Antimaláricos/efeitos adversos , Antimaláricos/uso terapêutico , Conhecimentos, Atitudes e Prática em Saúde , Humanos , Indonésia/epidemiologia , Malária/prevenção & controle , Controle de Mosquitos/métodos
20.
J Evid Based Complementary Altern Med ; 22(1): 107-113, 2017 Jan.
Artigo em Inglês | MEDLINE | ID: mdl-27313228

RESUMO

The effect of ethanolic extract of Morinda citrifolia leaves and fruit on blood pressure in dexamethasone-induced hypertension rat was evaluated. Total phenolic content of Morinda citrifolia leaves ethanolic extract (MCLEE) and Morinda citrifolia leaves ethanolic extract (MCFEE) was 1.789 ± 0.116 and 1.677 ± 0.051 mg of gallic acid equivalents per gram sample, respectively. Rutin level in MCLEE was 0.92 ± 0.19%, and scopoletin level in MCFEE was 0.46 ± 0.05%. MCLEE, MCFEE, and its extract combination significantly decreased the blood pressure of hypertensive rats. The combination group showed highest hypotensive activity by lowering systolic blood pressure by 16.71 ± 3.95%, diastolic blood pressure by 21.49 ± 7.90%, and mean arterial blood pressure by 19.58% ± 6.35. All extract treatments have not been able to repair or inhibit renal damage caused by dexamethasone induction.


Assuntos
Frutas/química , Hipertensão/tratamento farmacológico , Morinda , Extratos Vegetais , Folhas de Planta/química , Animais , Pressão Sanguínea/efeitos dos fármacos , Peso Corporal/efeitos dos fármacos , Dexametasona/efeitos adversos , Modelos Animais de Doenças , Etanol , Rim/efeitos dos fármacos , Rim/patologia , Masculino , Extratos Vegetais/química , Extratos Vegetais/farmacologia , Extratos Vegetais/uso terapêutico , Ratos , Ratos Wistar , Escopoletina , Timo/efeitos dos fármacos
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