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Antidiabetic Activity of Okra Fruit (Abelmoschus esculentus (L) Moench) Extract and Fractions in Two Conditions of Diabetic Rats
Full text linkOkra (Abelmoschus esculentus (L) Moench) fruit is empirically used in type 2 diabetes mellitus treatment. This research aims to know the antihyperglycemic activity of okra fruit extract and fractions in streptozotocin-nicotinamide (STZ-NA) induced as well as in insulin resistance diabetic rats, the effect on pancreatic cells regeneration, and the effect on immunohistochemical expression of glucose transporter-4. This study used a group of 35 male Wistar rats for STZ-NA induced diabetic model and another group of 35 rats for insulin resistance diabetic model. Gliclazide (0.72mg/kg BW) and metformin (45mg/kg BW) were used as drug control in STZ-NA induced and insulin resistance diabetes, respectively. Okra fruit ethanol extract, n-hexane, ethyl acetate, and water fraction were orally administered with dose of 200; 107; 6 and 86mg/kg BW, respectively, for 28 days after diabetic condition was obtained. Blood glucose level was measured every week. Hematoxylin-eosin staining was used to evaluate the pancreatic cells regeneration, while immunohistochemistry was used to evaluate the expression of glucose transporter-4 in muscle membrane cells, at the end of the treatment. The results revealed that ethyl acetate fraction was the most effective in lowering blood glucose level in both condition of diabetes. Ethyl acetate fraction decreased the necrosis of pancreatic cells in STZ-NA induced diabetic rats and increased the expression of glucose transporter-4 in muscle cell of insulin resistance diabetic rats
The Effect of Brazilin from Caesalpinia sappan on Cell Cycle and Modulation and Cell Senescence in T47D cells
Full text linkEthanolic extract and brazilein-containing fraction of Caesalpinia sappan L., has been reported to inhibit cell proliferation in T47D (ER+ PR+/- cell, Luminal A subtype model). The Luminal A subtype is the most common subtype of breast cancer in Indonesian women. In this study, we explored the activity of the reduced form of brazilein, i.e. brazilin, in T47D cells proliferation and the mechanism that involved. The cytotoxicity activity of brazilin was observed using MTT assay. While the cell cycle modulation analysis was done by using flowcytometry, and the senescence assay was observed using S-A-β-galactosidase assay. The results showed that brazilin inhibited cell growth in a dose-dependent manner with an IC50 value of 50μM (or 14.3μg/mL). That was higher than a brazilein-containing fraction, which was reported previously by our group to have an IC50 value of 68μg/mL against the same cell. Cell cycle analysis showed that cells treated with brazilin were accumulated at the G2/M phase in a dose-dependent manner. Furthermore, cells treated with a combination of brazilin and doxorubicin was accumulated at the G2/M phase and sub G1 phase. Cells accumulation at sub G1 phase indicates that the cells undergo apoptosis. Our data of S-A-β-galactosidase assay showed that cells treated with 1/4IC50, 1/2IC50, and IC50 brazilin had lower senescent cells compared to the untreated cells. The morphology of cells treated with IC50 (50μM) brazilin changed. The cells shape became rounded, cells were shrinkage and detached from the well plate, indicating that cells may undergo apoptosis. These results suggested that brazilin was cytotoxic towards T47D cells and its combination with dox potentially induced apoptosis and decreased cell senescence. The ability of brazilin to decrease cell senescence provides new insight of utilization of C. sappan or its constituents, particularly brazilin, as anti-ageing
Effect of Atorvastatin Treatment on Vascular Aterogenic Factors (Lipid Profiles and VCAM-1) in Patient Diabetes with Dyslipidemia
Full text linkTo analyze effectiveness of atorvastatin 20mg on lipid profiles and adhesion molecule VCAM-1 in patient with diabetes dyslipidemia. An observational prospective cohort study was conducted from November 2016 to March 2017. Patients who fulfilled the inclusion criteria were taken twice for their lipid profiles and VCAM-1 measurements (before initiation of study and after 6 weeks treatment of atorvastatin 20mg). There were 13 patients who met the inclusion criteria. The results of 13 patients showed that after 6 weeks of atorvastatin therapy, there was a 28% decrease in total cholesterol (t0=223.77±49.69, t1=160.92±24.69), 39% LDL decrease (t0=152.59±44.25, t1 =93±21.44), a decrease in TG 38.6% (t0=200.85±101.53, t1=123.30±62.77) and a statistically significant decrease in VCAM-1 7.47% (t0=729.59±208.06, t1=675.06±182.88). The results of the correlation test between total cholesterol and VCAM-1 (p=0.185, r=0.268), LDL and VCAM-1 (p=0.127, r=0.307), TG and VCAM-1 (p=0.198, r=0.261) showed no correlation. Based on the results of the study, it can be concluded that atorvastatin therapy can provide improvements in atherogenic factors such as decreased lipid profile and VCAM-1, and there was no correlation between lipid profile and VCAM-1 in type 2 DM patients with dyslipidemia.
Metabolite Profiling of Eleutherine palmifolia (L.) Merr. By HPTLC-Densitometry and its Correlation with Anticancer Activities and In Vitro Toxicity
No full textEleutherine palmifolia (L.) Merr. (E. palmifolia) is a plant that used as raw material for herbal medicines. The difference of growing location the medicinal plants affects the difference of metabolite content, It also affects the pharmacological activity and toxicity of the plant. This study aims to determine the profile of metabolites (metabolite fingerprinting), anticancer profiles, toxicity/safety profiles from several different regions in Indonesia for the purpose of authentication, efficacy, safety and quality control of these plants. Samples were sampled from 6 different locations in Indonesia, they were West Java, Central Java, East Java, East Borneo, Central Borneo, and South Borneo. Metabolite fingerprinting was determined by HPTLC-densitometry method, the profile of anticancer activity and toxicity was known by the MTT-ELISA method. The difference between metabolite fingerprinting, anticancer profile, toxicity/safety profile was analyzed by Principal Component Analysis (PCA) and Hierarchical Component Analysis (HCA). Whereas the relation between metabolite fingerprinting, anticancer profile, toxicity/safety profile was analyzed by Partial Least Square (PLS). The results of the metabolite profile analysis with PCA showed that E. palmifolia from 6 different locations gave different metabolite profiles and there were 3 metabolites that had a significant effect on cluster formation. samples are Rf 055, 059, and 044. The results of the HCA analysis showed that the 6 regions are in one cluster the same one. The analysis of PLS-DA showed that the metabolites for anticancer activity are found in Rf 059, 076, 093 and Rf 034. While the metabolites for toxicity are Rf 002, Rf 044 and Rf 059
A Study of Psychoactive Medicines and Risk of Falls Among Indonesian Elderly Patients
Full text linkOne of the causes of injury to the elderly is due to falls. Falling can be prevented by identifying and controlling risk factors. One risk factor that can be controlled is the use of fall risk medicines including psychoactive. This study aims to identify the association between the use of psychoactive medicine and its characteristic with the risk of falls among the elderly in Indonesia. The study utilized a case-control study design for a total number of 414 elderly patients, during October until December 2018. Cases were elderly aged 60 years or above with a high risk of falling assessed using the Morse Fall Scale (MFS≥45). Each case was matched with up to two randomly selected controls of the same age who are classified as low to moderate risk of falling (MFS<45). The use of psychoactive medicines was screened from a history of drug use for the past six months. Psychoactive medicine-fall risk associations were estimated via logistic regression. There were 138 cases and 276 controls. The median age of subjects was 66 years old and 54.83% was a woman. Elderly with a high risk of falling had higher psychoactive medicines use when compare with controls (31.16 % vs 21.38 %, p< 0.05). After adjusting for potential confounders, the use of psychoactive medicines was significantly associated with higher fall risk in elderly patients (OR 1.79 95% CI 1.10-2.90). Only the duration of psychoactive medication use over 90 days was significantly associated with a high risk of falling (AOR 3.65 95% CI 1.46-9.14). In elderly patients, the continued use of psychoactive medicines increased the risk of fall. Prescribers need to weigh risk and benefit from the use of psychoactive medicines in the elderly to prevent future fall
Naringenin-Loaded TPGS Polymeric Nanosuspension: In-Vitro and In-Vivo Anti-Inflammatory Activity
Full text linkNaringenin, (NAR) from Citrus grandis(L.) Osbeck, family Rutaceae, exhibit extensive pharmacological action, lacks significance in application due to low aqueous solubility approximately 0.214 mg/ml, which results in low bioavailability of 5.8%. Nanosuspension of NAR (NARNS) was prepared in our previous studies using high pressure homogenization adding various polymers. All these formulations were characterized and as a continuation of our work formulations was further evaluated for their anti-inflammatory activity by in-vitro and in-vivo methods. Denaturation of protein method and membrane stabilization methods were chosen for in-vitro evaluation. In-vivo studies performed were acute inflammatory studies (carrageenan-induced paw oedema) and chronic inflammatory studies (cotton pellet granuloma) on Wistar albino rats. The studies demonstrated that the NAR and NARNS at a dose of 50 mg/kg P.O. have a potent activity compared to the standard drug diclofenac. The percentage protection against inflammation exhibited by NARNS was highly significant compared to NAR
Response Surface Methodology used in the Optimization of RP-HPLC Condition for Quantitative Analysis of Carmine and Rhodamine B
No full textThe objective of this study was to optimize reversed-phase high-performance liquid chromatography (RP-HPLC) using an experimental design approach based on the response surface methodology of Central Composite Design (CCD) for separation and analysis of carmine (CAR) and Rhodamine B (RHO) in lipstick products. Some factors (independent variables) responsible for RP-HPLC separation including pH of buffer phosphate (X1), the acetonitrile ratio (X2), flow rate of mobile phase (X3), and column temperature (X4) were investigated. While, the responses (dependent variables) evaluated were resolution between CAR and RHO (Y1), tailing factor of CAR (Y2), tailing factor of RHO (Y3), retention time of CAR (Y4), retention time of RHO (Y5), peak area of CAR (Y6) and peak area of RHO (Y7). CCD showed that separation of CAR and RHO was influenced by these independent variables (factors). The optimum predicted conditions for the separation of CAR and RHO based on statistical results was pH buffer of 3.4, ACN 55%, the flow rate of 1.1 mL/min and column temperature of 35oC with the desirability of 1. Both CAR and RHO were clearly separated using optimum conditions, as suggested by CCD. The developed techniques were effective for optimizing chromatographic separation, therefore, the time consumption and a large number of running could be hindered
Paricalcitol For CKD-MBD Associated With Secondary Hyperparathyroidism: A Case Series Focus On TRAP5b, b-ALP, and DKK-1
Full text linkChronic kidney disease (CKD) lead to secondary hyperparathyroidism (sHPT) that caused by phosphate retention and hypocalcemia. This condition known as mineral and bone disorder (CKD-MBD). The increase in parathyroid hormone would increase bone turnover that result in an increased risk of bone fractures, and vascular calcification. These will increase the levels of tartrate-resistant acid phosphatase 5b (TRAP5b), and bone-specific alkaline phosphatase (b-ALP), which is a marker of bone turnover, and also dickkopf-related protein 1 (DKK-1), which is an inhibitor of the Wnt pathway. Secondary hyperparathyroidism in CKD also caused by calcitriol deficiency. Paricalcitol is a synthetic calcitrol analogue used to reduce parathyroid hormone (iPTH) with minimal calcemic and phosphatemic activity. Vitamin D receptor activation by paricalcitol will decrease TRAP5b, b-ALP, and DKK-1. In this study we reported 9 cases of CKD-MBD with Hemodialysis (HD) and associated with sHPT. Four of nine cases received 5μg paricalcitol every HD (twice a week) while the others five is not. Level of iPTH, phosphate, calcium, TRAP5b, b-ALP, and DKK-1 were measured before initiation of study and after three months treatment. According to this study, the paricalcol administration suppresses the increase in iPTH level, bone turnover and vascular calcification showed by decreasing or supresses the increase b-ALP, TRAP5b, DKK-1 leves without increasing calcium and phosphate levels
Modeling of Quinoacridinium Derivatives as Antitumor Agents using a QSAR analysis
Full text linkA QSAR analysis has been performed on a compound series of 1-11 quinoacridinium derivatives as internal test compounds, and compounds of 12-15 quinoacridinium derivatives as external test compounds. The electronic descriptors used in this study were atomic net charge (q), dipole moment (μ), ELUMO, EHOMO, polarizability (α), and Log P. They were calculated through HyperChem for Windows 8.0 software using semi-empirical PM3 method. The antitumor activity (IC50) of quinoacridinium derivative compounds was obtained from literature. Furthermore, the model of QSAR equation was analyzed through RML method which produced the best QSAR equation model: Log IC50 = -13.010 + 15.338(qC3) - 4.31(qC4) - 155.308(qC9) + 33.626(qC11) + 26.626(qC12) + 24.631(qC14) - 0.228(μ) - 0.621(ELUMO) - 0.066(α) + 0.233(Log P). The model of QSAR equation has a correlation coefficient n = 11, (r) = 1.00, (r2) = 1.00, SE = 0, and PRESS = 0.003. Among 28 compounds of quinoacridinium derivative which were designed, only 15 compounds, namely 16, 19-20, 22-28, 30-32, 39, and 40 compounds, have been recommended to be synthesized in the laboratory
Profile of Biofilm-Producing Staphylococcus epidermidis from Intravenous Catheter Colonisation at Prof. Dr. Margono Soekarjo Hospital Purwokerto
Full text linkBiofilm- producing Staphylococcus epidermidis has evolved to be a significant human pathogen, particularly in the use of medical devices such as an intravenous catheter. Furthermore, biofilm-producing bacteria 10-1000 fold less susceptible to several antimicrobial agents than free-bacteria. This simple survey aimed to describe the profile of biofilm-producing S. epidermidis from intravenous catheter colonization of some patients in surgical and internal medicine wards at the hospital Margono Soekarjo, Purwokerto, and the antibiotics resistance pattern. A vitek® 2 compact (Enseval Medika Prima) was performed to identify the bacterial species and to examine the 73 antibiotics for understanding the resistance pattern automatically. Microtiter plate biofilm assay with crystal violet staining was performed to measure biofilm optical density (OD) for analyzing the biofilm production capabilities. A scanning electron microscopy (SEM) was done to compare the thickness of ultrastructure of biofilm-producing S. epidermidis visually. The present study found that 2 of 8 Gram-positive bacteria (25%) were biofilm-producing S. epidermidis. One of S. epidermidis was moderate whereas the other was high biofilm-producing bacteria. Images of SEM showed that a high biofilm-producing S. epidermidis has a thicker ultrastructure of biofilm than the moderate biofilm-producing, whereas a control, the weak biofilm-producing S. epidermidis ATCC 12228 has the least biofilm. Both of S. epidermidis strains were sensitive to Gentamicin, Moxifloxacin, Quinupristin/Dalfopristin, Linezolid, Vancomycin, Doxycycline, Minocycline, Tetracycline, Tigecycline, and Nitrofurantoin. Furthermore, both S. epidermidis strains were resistant to the other (63) antibiotics. In conclusion, two strains of S. epidermidis in this study have different capabilities to form the biofilm which were showed that high biofilm-producing strain was thicker than moderate biofilm-producing strain by scanning electron microscopy. However, both of them were resistant to the same number of antibiotics.