Open Journal Systems
Not a member yet
442 research outputs found
Sort by
INHIBITION OF TROPOMYOSIN-RECEPTOR-KINASE B AND PHOSPHOINOSITIDE 3-KINASE/PROTEIN KINASE B SIGNALING CASCADE
Get PDFTrimethyltin (TMT, 2.4mg/kg, i.p) can trigger neuronal damage by inhibiting Tropomyosin receptor kinase B (TrkB receptor) following by phosphoinositide 3-kinase (PI3K)/protein kinase B or Akt signaling cascade. We examined hippocampal changes in TrkA/B phosphorylation on Tyr490/Tyr516 of TMT-treated mice in a time-dependent manner. Phosphorylated PI3K (Tyr508), phosphorylated 3-phosphoinositide-dependent protein kinase 1 (PDK1, Ser241) and phosphorylated Akt (Ser473) were changed following by TMT injury (from 3 hours until 7 days after injury). Treatment with 7,8-dihydroxyflavone (7,8-DHF), a specific agonist of TrkB, significantly attenuated the TMT-caused inhibition of phospho-TrkB, thereby increased in expressions of phospho-PI3K, phospho-PDK1 and phospho-Akt in TMT-treated mice, simultaneously 7,8-DHF showed a neuroprotective effect in observation of nuclear chromatic clumping by Cresyl violet- and terminal deoxynucleotidyltransferase-mediated dUTP-biotin nick end labeling- (TUNEL) staining in the hippocampal dentate gyrus (DG) of TMT-treated mice, as compared to saline-treated group. This finding suggests that inhibition of TrkB receptor following by PI3K/Akt cascade may play a part in the molecular mechanism by which TMT caused neurodegeneration in mice
SYNTHESES AND ANTIOXIDANT ACTIVITIES OF SOME HYDROXY DIMETHOXY CHALCONE DERIVATIVES
Get PDFFour (4) hydroxy dimethoxy chalcones derivatives were synthesized by Claisen-Schmidt condensation of hydroxyacetophenone with 3,4-dimethoxybenzaldehyde using conventional method and grinding technique. The synthesized compounds were characterized by spectroscopy (IR, 1H-NMR and 13C-NMR). Synthesis of the hydroxy dimethoxy chalcone using grinding method is better than the conventional method. The synthesis using grinding method require a low concentration base, shorter reaction (15min) and higher yield (70-84%). The antioxidant activity of the compounds was determined by DPPH method, showed that 2',5'-dihydroxy-3,4-dimethoxy chalcone have the highest antioxidant activity.Key word: hydroxy dimethoxy chalcone, Claisen-Schmidt condensation, grinding, DPPH metho
COMPARATIVE REPELLENCY DURATION OF CITRONELLA OIL LOTION (Cymbopogon nardus L.) BETWEEN Culex sp. WITH Aedes sp. AS LYMPHATIC FILARIASIS VECTOR
Get PDFLymphatic filariasis is a mosquito borne disease, transmitted by mosquitoes such as Culex, Anopheles, Aedes, Mansonia. Filariasis infection resulting in disability. The important method to avoid being bitten from mosquitoes is by using a repellent. The purpose of this study were to compare repellency duration of citronella oil lotion against Culex sp. to Aedes sp. and to compare its repellency duration to N,N-diethyl-m-toluamide (DEET). Laboratory experimental design was conducted at each of five men as subjects using five randomly treatments: 20%, 40% citronella oil lotion (COL), lotion base (negative control), 12.5% DEET lotion with one-day time lag. Repellency duration, since the forearm was inserted into the cage until first mosquito land, was assessed using female Culex sp. and Aedes sp, according to modification of Fradin and Day method. Repellency duration was analyzed using one-way ANOVA, Tukey HSD followed by paired t-test level of significance with a=0.05 level of significance at p<0.05. There were highly significant differences (p<0.01) between average repellency duration (minute) of 20%, 40%, 80% COL against Culex sp. and 40%, 80% against Aedes sp. compared to 12.5% DEET. It was concluded that citronella oil lotion was more effective to Culex sp. than that of Aedes sp. Nevertheless the potency of citronella oil lotion was weaker than 12.5% DEET.Key word: lotion citronelle oil, Culex sp., Aedes sp., Filariasi
INTERACTION STUDY: THE EFFECT OF ORTHOSIPHON STAMINEUS EXTRACT ON HUMAN CYTOCHROME P450
Get PDFHerbal remedies are often used concomitantly with prescribed medication, which leads to an increase in the potential of herb-drug interactions. Orthosiphon stamineus is one of the popular herbal preparations that is traditionally used, especially as a diuretic or for the elimination of kidney stones. The inhibitory effect of O. stamineus extract on human cytochrome P450 isoforms, namely CYP1A2, CYP3A4, CYP2C9 and CYP2D6, has been determined using luminescent methods. The final concentrations of O. stamineus extract tested were 0.01, 0.1, 1, 10, 100 and 1000µg/mL. IC50 value was used to assess the modulation potencies for each CYP isoform. The extract showed a moderate inhibition towards CYP2C9 with the IC50 of 20.12µg/mL and showed IC50 of 49.90, 89.24 and 97.82µg/mL for CYP1A2, CYP2D6 and CYP3A4, respectively. These data suggest that O. stamineus extract may potentiate the herb-drug interaction via CYP inhibition
FORMULATION AND EVALUATION OF DEXTROMETHORPHAN HYDROBROMIDE CONTROLLED RELEASE HOLLOW MICROSPHERES USING NATURAL POLYMER
Get PDFThe objective of this study was to formulate and evaluate gastric floating dosage forms of hollow microspheres for controlled delivery of dextromethorphan hydrobromide (DBM). Hollow microspheres were prepared by emulsion polymerization method using natural polymer gelatin as release retardant and coating agent. Hollow microspheres were characterized by FT-IR, DSC, SEM, and micromeritic properties. FT-IR and DSC studies showed no chemical interaction between the drug and polymers. Hollow microspheres were evaluated for percentage yield, encapsulation efficiency and in vitro release studies. The obtained angle of repose, % Carr’s index, Hausner ratio, and tapped density values were within the limits indicating good flow properties. The surface morphology revealed that microspheres were spherical with minute pores and invert dents on the surface. Among all the formulations, F-3 of hollow microspheres showed highest drug release of 79.69±0.12% at the end of 12h which was considered as the best formulation. The release data was fitted to various mathematical models such as, Higuchi, Korsmeyer-Peppas, First-order, and Zero order to evaluate the release kinetics and mechanism of the drug release. The release kinetics indicated that drug release followed non-fickian diffusion mechanism. Results of the stability studies showed that there were no significant changes in the drug content and physical appearance.
BIOAVAILABILITY STUDY OF SAMBILOTO (Andrographis paniculata) HERBS INFUSION IN RABBIT
Get PDFAndrographis paniculata or sambiloto is one of the most widely used medicinal herbs in Indonesia. The main bioactive chemical constituent, andrographolide, has been reported to have various pharmacological activities. Besides its function for medical purposes, the sambiloto herbs infusion is frequently taken to maintain health. This study was conducted to determine the bioavailability of sambiloto herbs infusion in rabbit plasma, stomach, and liver, calculated as total andrographolide. Fourteen male New Zealand white rabbits were used in this study. Sambiloto herbs infusion were administered orally at the dose 7.04mL/kg body weight to each rabbit. Blood samples were taken at intervals 0.0; 0.5; 1.5; 2.0; 3.0; and 5.0h after infusion administration. Sambiloto herbs infusion, which are calculated as andrographolide, levels in plasma, stomach, and liver were analyzed by high performance liquid chromatography using C-18 column as stationary phase and a mixture of methanol-double distilled water (60:40) as mobile phase. Bioavailability parameters obtained were Cmax 0.5549µg/mL (in stomach), 0.2136µg/mL (in plasma), 0.0051µg/mL (in liver); while tmax 1h (in stomach), 1.5h (in plasma), 2h (in liver); and AUC 1.7451µg.h/mL (in stomach), 0.434µg.h/mL (in plasma), 0.0038µg.h/mL (in liver). These data showed that in healthy animals, sambiloto herbs infusion was fastly absorbed from the stomach, distributed in the circulation system, and metabolized in the liver, in subsequent process. Sambiloto herbs infusion showed good bioavailability in rabbit.
CHIRAL SEPARATION OF CETIRIZINE ENANTIOMERS BY CYCLODEXTRIN MEDIATED CAPILLARY ELECTROPHORESIS
Get PDFChiral separation cetirizine, a second generation H1 antagonist was studied by cyclodextrine (CD) mediated capillary electrophoresis. The influence on the separation of several parameters including pH and concentration of the background electrolyte (BGE), CD type and concentration, applied voltage and temperature were studied and the electrophoretic and analytic parameters were optimized. The best conditions for the chiral separation were obtained using 25mM disodium hydrogeno-phosphate – 25mM sodium didydrogeno-phosphate (1:1) as BGE, 5mM sulfobuthyl ether- β-CD as chiral selector, a voltage of + 20kV, temperature of 20°C, injection pressure/time of 50mbar/ 1sec, UV detection at 230nm. The analytical performance of the method was evaluated. The proposed method was successfully applied to the enantioselective assay of cetirizine in pharmaceutical formula-tions. CE proved to be a rapid, specific, reliable and cost-effective method for the chiral separation of cetirizine enantiomers and can be useful for laboratories performing routine analysis.
OPTIMIZATION OF EXTRACTION CONDITIONS FOR ANDROGRAPHOLIDE USING FRACTIONAL FACTORIAL DESIGN
Get PDFAndrographolide is a major bioctive compound found in king of bitter (Andrographis paniculata). In this study, the extraction method and its condition were investigated in order to get an extract with maximum amount of andrographolide by comparing three other extraction methods, i.e. maceration, soxhletation and ultrasonication and also determination for the optimum condition of the selected extraction method. The highest andrographolide amount was found by maceration, so this method was choosen for further optimization of extraction condition. The optimum condition based on the prediction amount from 27 factor combinations was obtained in 360 times of extraction time, 2g/100mL of sample to solvent ratio, and 3fold of extraction frequency with prediction of andrographolide amount was 3.50%. While by using prediction profile, the optimum condition was obtained in 360min of extraction time, 2 g/100mL of sample and solvent ratio, and 4 times of extraction frequency with the amount was 3.47-3.74%
OPTIMIZATION AND ACESSING THE INFLUENCE OF XANTHAN GUM, EFFERVESCENT COMPONENTS AND HARDNESS ON FLOATATION BEHAVIOR AND DRUG RELEASE OF GASTRO-FLOATING CAPTOPRIL TABLET
Get PDFThis research purposed to optimize, investigate and evaluate the influence of xanthan gum, sodium bicarbonate-citric acid as effervescent components and hardness on floatation behavior and drug release of gastro-floating captopril tablet with floating system. A 23 full factorial design (8 runs) was applied to optimize the floating captopril tablet using xanthan gum (X1), ratio of effervescent components (X2) and hardness (X3) as independent variables. Optimum area was determined by superimposed contour plot of floating lag time (Y1), cumulative drug release at 60min (Q60) (Y2) and drug release constant rate (Y3) using Design Expert® software. Xanthan gum, effervescent components and hardness were affected the floatation behavior and drug release. Hardness was the most dominant factor affected the floatation behavior and drug release. Based on superimposed contour plot, the optimum area was in range of xanthan gum 58–100mg, sodium bicarbonate 45–63mg, citric acid 7–25mg and hardness at 70–98N
IN VITRO EFFECT OF Chloroprocta SP. MAGGOTS SECRETION ON Staphylococcus epidermidis BIOFILM AND THE EXPRESSION LEVEL icaA OF GENE
Get PDFBiofilm formation and the expression of icaA gene can be induced by environment conditions that are potentially toxic for bacterial cells. The effect of green flies maggots secretion to biofilm was studied some years ago to investigate in vitro effect of secretion of Chloroprocta sp. maggots on the formation of Staphylococcus epidermidis biofilm (phenotype) and the expression level of icaA gene (genotype) for indicating its mechanism on bacterial biofilm eradication. Microtiter plate biofilm assay was used to measure the effect of Chloroprocta sp. maggots secretion at various concentration on S. epidermidis biofilm. The expression level of icaA gene was performed by Real TimePCR using lightcycler method. The biofilm susceptibility test was done against maggots excretion/secretion using MTT assay. Whereas planktonic susceptibility testing was carried out using Kirby Bauer method. In the presence of maggots secretion at low concentration (5%), biofilm formation of S. epidermidis 734 was induced. In contrast, the expression level of icaA gene in production of maggots excretion/ secretion at concentration of 5% was lower than that of without maggots secretion (1/2 Fold). Eradication of bacterial biofilm was demonstrated after 48h incubation (MD=-0,011;P<0,05), but planktonic cell. In vitro difference effect of the Chloroprocta sp. maggots secretion at low concentration to phenotype and genotype of S. epidermidis biofilm showed that the possibility of maggots secretion ability to eradicate bacterial biofilm was not mainly due to the expression level of icaA gene