Open Journal Systems
Not a member yet
442 research outputs found
Sort by
Preparation and antibacterial activity of p-Anisyl ethyl fumarate and ethyl n-phenyl fumaramate
Get PDFIn order to generate potent C-9154 antibiotic derivatives, it has been conducted the synthesis and antibacterial activity evaluation of p-anisyl ethyl fumarate and ethyl N-phenyl fumaramate. These target molecules were chosen as the former would be a para-methoxy substituted C-9154 derivative, whereas the latter would be an example of unsubstituted C-9154 derivative bearing an amido-ester fumaric side chain.p-Anisyl ethyl fumarate was synthesized from p-anisaldehyde by reduction with NaBH4, condensation of p-anisyl alcohol with maleic anhydride, and esterification of the resulting p-anisyl maleic acid with ethanol in the presence of benzenesulfonic acid as the catalyst. These reactions gave satisfactorily yields (55-81 %) in all steps involved. In the case of ethyl Nphenyl fumaramate, this molecule was synthesized in 84 % yield through condensation of aniline with maleic anhydride, followed by esterification with ethanol in the presence of concentrated sulfuric acid.The antibacterial activity test showed that the minimum inhibition concentration (MIC) of p-anisyl ethyl fumarate and ethyl N-phenyl fumaramate towards Staphyllococcus aureus were 15 and 25 μg/mL. Interestingly, the MIC values of these two compounds towards Eschericia coliwere also 15 and 25 μg/mL respectively. Thus, the data showed that the two C-9154 derivatives obtained are sufficiently potent and possess antibacterial activities which are comparable to the antibacterial activity of C-9154 itself towards Staphyllococcus aureus (12.5 – 37.5 μg/mL) and Eschericia coli (25 – 50 μg/mL).Key words: synthesis, antibacterial activity, fumarate and fumaramate
ACUTE TOXICITY OF NEW COMPOUNDS 12,13-DIHIDRO--AMYRIN-20,30-en-3-ACETAT ; 12-13-DIHIDRO--AMYRIN-20,30-en-3-ol AND -SITOSTAN-20,30-en-3-ol TO Artemia – Salina Leach
Get PDFAcute toxicity assay of new compound from nature resources is very important to be carried out. This research was to perform an acute toxicity assays of new compound from Eupatorium inulifolium H.B.K. Acute toxicity assays was carried out using Brine Shrimp Bioassay method. The result showed that two compounds, 12,13-dihydro--amyrin-20,30-en-3-ol and -sitostan-20,21-en-3-ol displayed toxicity (LC50 < 1000 g/ml), and LC50 of 12,13-dihydro--amyrin-20,30-en-3-acetate was exceeding 1000 g/ml.Key words: 12,13-dihydro--amyrin-20,30-en-3-ol, 12,13-dihydro--amyrin-20,30-en-3-acetate, -sitostan-20,21-en-3-ol, toxicity assay, Artemia salina Leach
Antioxidant activity of aqueous extract of Sonchus arvensis L. in-vitro
Get PDFAntioxidants are the compounds which have ability to inhibit reactive oxygen species (ROS) and free radicals in human body. Based on this activitiy the antioxidants prevent cell damage and various pathological processess e.q. cardiovascular, diabetes mellitus, atherosclerosis, respiratorydiseases, carcinogenesis, inflammation, cell degenerative. One of the famous Indonesian traditional medicine is tempuyung or S. arvensis L.(Asteraceae). The antioxidant test has been conducted on the dried water extract by measuring the peroxide value (POV) and in-vitro antioxidant activity test was carried out by spectrophotometry applying thiocyanate method at the wave length of 500 nm.The results showed that peroxide value of dried water extract of tempuyung (S. arvensis L. ) by titration iodometric method has a lower value (865.60) compared to positive control -tocoferol (1142.77). In-vitro antioxidant activity test has remarkable results at the various extract concentrations (1, 5 dan 10 %) and had significant differential absorbance(A) with positive control (K+) as well as negative control (K-), and among the extract concentrations (P 0,5). Absorbance value increased along with increasing storage time, in which negative control reached higher value of A (0,987) in the seven days and maximal value after eight days (A 1), while the absorbance value of positive control (K+) was 0.648, and dried water extract of tempuyung 1, 5 & 10 % was 0.576, 0.488 & 0.314 after 14 days, respecticly. The absorbance value of absorbance (A) was inversely compared to extract concentrations. Increasing of extract concentrations resulted in decreasing A value, in other words increasing extract concentration resulted in the increas of antioxidant activity.Key words : Sonchus arvensis L, Asteraceae, POV, antioxidant, thiocyanate method
FORMULATION OF PGV-0 A NEW ANTIINFLAMMATORY AGENT AS A TABLET DOSAGE FORM
Get PDFThe specific objective of this study is to get the best formulation for PGV-0 as a tablet dosage form. By optimation of formulation a more potent and safe antiinflamatory drug could be obtained. This study was started with determination of physical properties which included: appearance, particle size, partition coefficient, and hygroscopicity. In the formulation of PGV-0 6 formulas were chosen with amylum and lactose as fillers, tween 80 as surfactant, solutiogelatine and solutio PVP as binding agent and talc and Mg stearate as lubricants. From these six formulas chosen physical properties of the granules and tablets were determined. PGV-0 powder was not free flowing and has bad compressibility. PGV-0 could not be proccesed by direct compression but should be formulated by wet granulation method. The best formula found was formula V which used solutio PVP 2 % as binding agent and tween 80 0,25 % as wetting agent.Key words: PGV-0, antiinflammation, formulation of tablet dosage form
PROTOPLAST SUSPENSION CULTURE OF LEAVES MESOPHYLOF Centella asiatica (L.) Urban AND QUALITATIVE ANALYSIS ASIATICOSIDE
Get PDFCentella asiatica leaves has been used as diuretic, antihypertensi, anti leprae, skin infection, burning skin and celloid. Cells suspenson culture of mesophyll of Centella asiatica leaves were carried out in three steps: isolation, purification, and cell culture. The aim of this research is to investigate the influences of leaves position (age of leaves) and concentration of macerozyme R-10 for cells number and viability, and the influence of sucrose concentration for cells growth and biosynthesis of asiaticoside. Isolation and purification of mesophyll cell has been performed using factorial completely randomized design. The first factor was leaf position (age of leaves), and the second factor was concentration of macerozyme. Collected data were analysed using Anova and Duncan’s test at 0.0 – 2.5 – 5.0 and 7.5 per cent respectively. Asiaticoside produced by cell biomass were analyzed qualitatively using thin layer chro- matography. The result revealed that mesophyll cells could be used as explant for suspension culture. The highest biomass produced with highest viability were found in cells isolated from second leaves treated with 0.1% macerozyme (1.32 . 107 cells/ml). Addition of sucrose to suspension culture medium produced higher packed cells volume (pcv) percentage than no sucrose was added, (0% sucrose gave pcv 8.5%, 2.5% sucrose pcv 22%, sucrose 5% pcv 21.5%, and 7.5% sucrose pcv 15.75%). The asiaticoside production not only depended on sucrose, because without any sucrose was added, the asiaticoside was also available..Key Words: Cell suspension culture, mesophyll, Centella asiatica (L.) Urban, asiaticosid
The Keto-Enol Tautomerism of Curcumin and Some 4-substituted Curcumin Derivatives : A Theoretical Study Based on Computational Chemistry Approach
Get PDFHeat formation (DHf) for the enol and diketo tautomers of curcumin and some 4-substituted curcumin derivatives has been studied using semiempirical AM1 quantum-chemical calculations. The calculations on curcumin, 4-methylcurcumin, 4-ethylcurcumin, 4-npropylcurcumin, 4-isopropyl-curcumin, 4-n-butylcurcumin, and 4-benzylcurcumin showed that the more steric hindrance resulted from the subtituents, the more stable they were in the form of diketo tautomers than enol tautomers. Whereas, calculations on 4-phenylcurcumin, 4-(o-methoxyphenyl)-curcumin, and 4-(p-methoxyphenyl) curcumin showed that though steric hindrance influenced the keto-enol tautomerism, they were found more stable in the form of enol tautomers. This phenomenon was estimated to be related with conjugation effect of the aromatic groups with the enol moiety of the main bone structure.Keywords : 4-Substituted curcumin, the keto-enol tautomerism, AM1, semiempirical calculations
EFFECT OF ASPIRIN ON RAT LIVER CLASS- GLUTATHIONE S-TRANSFERASE ACTIVITY
Get PDFInflammation is the response of living tissues caused by injury. It involves a complex battery of enzyme activation, mediator release, extravasation of fluid, cell migration, tissue breakdown and repair. Inflammation mediator is synthesized in the body by several steps and catalyzed by several enzymes, such as cyclooxygenase and class- glutathione S-transferases (GSTs) in the cyclooxygenase arachidonic acid cascade. Aspirin, which has been reported as an inhibitor to inflammation mediator synthesis in the cyclooxygenase arachidonic acid cascade, is a non-steroid anti-inflammatory agent. The aim of this research is to study the effect of aspirin on rat liver class- GST activity in vitro. GSTs were isolated from the rat liver cytosolic fraction by centrifugation according to Lundgren. Protein concentration in the cytosol was determined spectrophotometrically using bovine serum albumin as a standard. The GST activity was determined using conjugation reaction rate between glutathione (GSH) and 1,2-dichloro-4-nitrobenzene (DCNB), followed by determining IC50 of aspirin. Then, a study was done to determine the ability of aspirin in inhibition of the rat liver class- GST activity in vitro. It can be concluded that aspirin has no inhibitory effect on rat liver class- GST activity.Key word: Aspirin, anti-inflammatory, glutathione S-transferase
The Anticarcinogenic Activity Of Plants Compounds
Get PDFThe study was conducted to observe the effect of extracts of ngokilo (Gynura procumbens), beluntas (Pluchea indica), murbei (Morus alba) dan tapak doro (Vinca alba) leaves. Showed anticarcinogenic activity on lung tumor growth of mice. In the nex step, compounds having anticarcfinogenic effect was isolated and identified, and evaluated on the cultures of meiloma and Vero cells. The results showed that non-polar fraction of ethanol extract of ngokilo leaves did not have anticarcinogenic activity, whereas the polar fraction show anticarcinogenic activity. At least there were three flavonoids (flavon or flavonol groups) in this polar fraction. It was only two of these flovonoids which could inhibit the growth of myeloma and Vero cells.Key words : ngokilo, Gynura procumbens, anticarcinogenic, flavonoid
Cytotoxicity and antimicrobial test of the bioactive compound isolated from Stylissa flabelliformis sponge
Get PDFA research of cytotoxicity and antimicrobial test of bioactive compound of Stylissa flabelliformis sponge have been done. Cytotoxicity test were conducted on myeloma cells, while antimicrobial test were conducted against Staphylococus aureus,Eschericia coli and Candida albican. The research was initiated with the isolation of bioactive compound from the active fraction of sponge S. Stylissa monitored by Brine shrimp Lethality tes (BST). The active fraction was chromatograped with silica gel as its immobile phase and the mixture of hexane and ethyl acetate (1:1 ) as the mobile phase to obtain compound 1,2,3 and 4.Compound 3 has the most toxic character because it could kill A. salina equal to 100% at dose 25 mg/ml, and has LC50 of 0,9 mg/ml. Cytotoxicity test with direct staining method using tripan blue on myeloma cell at density of 4,5x10 cell / 100.ul showed that the compound 3 had a high activity against myeloma cell, having LC50 equal to 0,08 mg/ml.The result of antimicrobial effect showed that compound 3 was a fungicide against Candida albicans but having no activity on Staphylococcus aureus and Eschericia coliKey words: sponge, Stylissa flabelliformis , cytotoxicity, fungicid
Characterization and dissolution studies of Furosemide solid dispersions using polyethylene glycol (PEG), talc and PEG-talc as dispersion carriers
Get PDFSolid dispersions of furosemide were prepared by melting and solvent methods using polyethylene glycol (PEG) 6000, talc and PEG – talc as dispersion carrier in order to improve furosemide dissolution. The increase of dissolution and physical properties of its powder was evaluated. Only furosemide solid dispersions with combination of PEG – talc 1 : 3 showed a good physical properties. The assay of the effect of PEG – talc ratio on furosemide dissolution showed that the increase of ratio of PEG – talc increased significantly dissolution rate.Key Word : furosemide, solid dispersion, dissolutio