Open Journal Systems
Not a member yet
442 research outputs found
Sort by
Activity of propyl p-benzoyloxybenzoate as mu-class glutathione s-transferase inhibitor
Get PDFNon-steroidal anti-inflammatory drugs (NSAIDs) are the most prescribed medicines. Anti-inflammatory activity was reported to have relationship with the inhibition of prostaglandin synthesis, one of the inflammation mediators. The inhibition mechanism might be through the cyclooxygenase (COX) inhibition, oxygen radical scavenging, and mu-class glutathione S-transferase (GST) inhibition. Aspirin has been used as a NSAID since a hundred years ago and was reported as cyclooxigenase-1 (COX-1) selective inhibitor. The selectivity leds to gastrointestinal ulceration. Propyl p-benzoyloxybenzoate was a new compound which was predicted to have anti-inflammatory activity and would be developed to be an NSAID with minimum side effect.mu-class GST inhibition was examined using formation reaction model of GS-CNB conjugate through conjugation of 1,2-dichloro-4-nitrobenzene (DCNB) and glutathione (GSH) with GST (prepared from rat’s liver) as a catalyst. GSTs were isolated from the rat liver cytosolic fraction by centrifugation according to Lundgren. Protein concentration of the cytosol was determined spectrophotometrically by using bovine serum albumin as a standard. The GST activity was determined using conjugation reaction rate between DCNB and GSH, followed by determination of IC50 of propyl p-benzoyloxybenzoate. The result showed that propyl p-benzoyloxybenzoate has activity as mu-class GST inhibitor with IC50 = 111.77 μM as the result from extrapolation.Key words: Anti-inflammatory, propyl p-benzoyloxybenzoate, inhibitor, mu-class glutathione S-transferase (GST)
Antioxidant activities, total phenolic and flavonoid contents of ethyl acetate extract of Mengkudu (Morinda citrifolia, L) fruit and its fractions
Get PDFThis present study was carried out to evaluate antioxidant activities, total phenolic and total flavonoid contents of ethyl acetate extract of Mengkudu fruit and its fractions. Ethyl acetate extract was fractionated by column chromatography and yielded 15 fractions based on the identical TLC (thin layer chromatography) profile.Antioxidant activities in ethyl acetate extract and its fractions were determined by radical scavenging assay using DPPH (2,2-diphenyl-1- picrylhydrazyl) radical. The total phenolic and total flavonoid contents were determined spectrophotometrically.Among 15 fractions of ethyl acetate extract evaluated, fraction 8 (IC50 5,49 μg/mL) and fraction 7 (IC50 7,90 μg/mL) revealed antioxidant activities that higher than that of vitamin E (IC50 8,27 μg/mL). The total phenolic contents ranged from 5.94 ± 0.08 to 36.52 ± 0.35 g of gallic acid equivalent/100 gram dry material whereas the total flavonoid contents ranged from 1.19 ± 0.02 to 17.65 ± 0.17 g of quercetin equivalent/100 gram dry material.A linier positive relationship existed between the antioxidant activities and total phenolic contents of the tested ethyl acetate extract and its fractions y = -1.220x + 44.022; r2 = 0.67, while the correlation between antioxidant activities and total flavonoid contents revealed a linier regression y = -2.202 x + 35.82; r2 = 0.4278.Key words: antioxidant activity, Morinda citrifolia, L, Fractio
Optimization of theophylline sustained release tablet formula with HPMC, CMC Na and xanthan gum as matrix component
Get PDFTheophylline has a relatively short half-life (8,1 jam) with a narrow therapeutic window (10 – 20 μg/mL). Sustained-release formulation can produce more uniform serum concentrations with less fluctuation in peaktrough levels. The physical properties of tablet mass and the release profileof drug from hydrophilic matrices are influenced by properties of matrix components, i.e. HPMC (gelling agent), CMC-Na (did not show initial burst release), and xanthan gum (free flowing).The research was done with simplex lattice design (SLD) by using 3 component, i.e. HPMC (A), CMC-Na (B), and xanthan gum (C). Seven formula were obtained that are F1 (100% A), F2 (100% B), F3 (100% C), F4 (50% A & 50% B), F5 (50% B & 50% C), F6 (50% A & 50% C), dan F7 (33,33% A, 33,33% B, 33,33% C). The Optimization parameters of theophylline sustained-release were flow rate of the tablet mass, the compactibility of the tablet mass, and the release rate of theophylline.Based on SLD model; equations, contour plots, and superimposed of contour plots were obtained, by which the optimum formula was determined.Xanthan gum was the most dominant factor in increasing flowability and compactibility of theophylline tablet mass. HPMC was the most dominant factor in decreasing the dissolution rate of theophylline. The most dominant interaction effect to increase flowability and compactibility was the interaction of HPMC, CMC-Na, and xanthan gum. The most dominant interaction effect to increase correlation coefficient of zero order kinetics was the interaction HPMC and CMC-Na. Based on the superimposed contour plots, tablet formula consisting of HPMC (2,3 %), CMC-Na (18,6 %), and xanthan gum (79,1 %) is the optimum tablet formula.Key words: theophylline, HPMC, CMC-Na, xanthan gum, sustained-releas
PGV-1 decreases angiogenic factor (VEGF and COX-2) expression on T47D cell induced by estrogen
Get PDFBreast cancer is the most common cancer occurring in women after cervix cancer in Indonesia. Tumor metastasis is the major cause of mortality in breast cancer. For a tumor cell to metastasize effectively, it must induce angiogenesis. 17 β-estradiol has been shown to stimulate the proliferation and angiogenesis of breast cancer cells which express estrogen receptor (ER), T47D (human breast cancer cell line). In the present study Pentagamavunon-1 or PGV-1 [2,5-bis-(4’-hydroxy-3’,5’-dimethylbenzylidene)-cyclopentanone], an analogue of curcumin [1,7-bis-(4’-hydroxy-3’-methoxyphenyl)-1,6-heptadiena-3,5-dion], were tested on their cytotoxicity and suppression effect on angiogenic factors (i.e. VEGF and COX-2) on the breast cancer cell lines (T47D) induced by 17 β-estradiol 10-8 M. The results showed that PGV-1 performed cytotoxicity effect againts T47D cells with IC50 values 3,16 μM. This was more potent than curcumin (IC50 = 19,05 μM). PGV-1 5 μM and curcumin 20 μM decrease VEGF and COX-2 expression. These results suggest both compounds possessed antiangio-genic potensial.Key words : PGV-1, curcumin, 17 β-estradiol, angiogenesi
Effect of protein fraction of Carica papaya L. leaves on the expressions of p53 and Bcl-2 in breast cancer cells line
Get PDFCarica papaya L. leave was known containing Ribosome-inactivating proteins (RIPs), which demonstrated to have an in vitro cytotoxic effect on cancer cell lines. This researh examined the effect of protein fraction containing RIPs isolated from Carica papaya L. on the expressions of p53 and Bcl-2, regulator proteins on apoptosis process, in breast cancer cell lines (T47D).RIPs from Carica papaya L. leaves were isolated by amonium sulfat precipitation. This fraction was analyzed by the activity of cleaving supercoiled double stranded DNA, in order to identify the presence of RIP. The active fraction was then tested of the citotoxic activity on breast cancer cell lines followed by analysing the expressions of p53 and bcl2 using immunohistochemistry technique.The results indicated that the protein fraction possessed cytotoxic activity in breast cancer cell line with the IC50 of 2.8 mg/mL. The expression level of p53 was increased by 59.4%, while Bcl-2 protein was \ decreased by 63%. These results suggested that this protein could induce apoptotic process.Key words : protein fraction, Carica papaya L. , expression of p53 and Bcl-
Synthesis of 4-phenyl-3,4-tetrahydro-indeno [2,1]-pyrimidin-2-one (LR-1)
Get PDFThe synthetic compound 4-phenyl-3,4-tetrahydro-indeno[2,1]- pyrimidin-2-one 20a (LR-1) was synthesised using Biginelli reaction method. The reaction involved benzaldehyde 6, 2-indanone 2 and urea 7 in acid condition. This condensation reaction yielded 15 % of the product 20, at 133,4-135,0oC of melting point and 0.15 (Et2O : CHCl3 = 1 : 3) of Rf value.Keywords : benzaldehyde, indenone-2, ure
Activity of ethanol extracts of seledri (Apium graveolens) herbs and urang aring (Eclipta prostata (L.)L.) leaves against Pityrosporum ovale
Get PDFSeledri (Apium graveolens) and urang aring (Eclipta prostata (L.)L.) have been used traditionally for hair grow. In this study, we want to test wether the both substances have an activity against Pityrosporum ovale as fungi causing dandruff. Anti Pityrosporum ovale activity of ethanol extracts of seledri (Apium graveolens) herbs and urang aring (Eclipta prostata (L.)L.) leaves had been studied using agar diffusion and dilution methods. Anti Pityrosporum ovale activity was shown by both of the two extracts, but seledri herbs extract showed stronger effect with inhibition diameter of as large as 16.33 ± 2.08 at the concentration of 5% w/v whereas that of urang aring leaves showed the inhibition diameter of 12.67 ±1.15 at the same concentration using agar difusion method. With agar dilution method, both of the two extracts still showed the inhibitory effects at the concentration of as low as 0.11 mg/mL.Key words : antifungi, Pityrosporum ovale, seledri, urang arin
Determination of chemical structure of antioxidant compound benzophenon glycoside from n-butanol extract of the fruits of Mahkota Dewa [Phaleria macrocarpa (Scheff) Boerl.]
Get PDFIn continuing of chemical study research on the parts of the fruits of Mahkota dewa, we have done isolated one antioxidant compound benzophenon glycoside from n-butanol extract. Isolation and purification by column chromatography (SiO2, chloroform-methanol) and determination of chemical structure based on interpretation spectra of ultraviolet (UV), infrared (IR) and nuclear magnetic resonance 1 dimension (1H & 13C NMR), 2 dimension (1H-1H COSY, 13C-1H COSY, HMBC). Based on spectrroscopic data, the compound was identified as 6,4’,-dihidroksi-4- metoksibenzofenon-2-O-α-D glucopyranoside.Key words: Mahkota dewa, Phaleria macrocarpa, Thymelaceae, Indonesian medicinal plant, benzophenone glycosid
Simulation of propranolol as antihypertensive agent on hyperglicaemic rabbit
Get PDFDiabetic and hypertention are two common deseases on older people one of fat soluble antihypertensive drugs is propanolol. There for is a study this undertakento observe how propanolol can reduce the blood sugar. This study used 12 male rabbits, divided into 4 grroups. Each group consisted 3 rabbits. The first group was used as negative control (given EDTA sodium liquid 1 % w/v). The second group was the treated group (given EDTA sodium suspension 1.% w/v and propranolol tablet suspension 0,006.% w/v). The third group also the treated group (given EDTA sodium suspension 1% and propranolol tablet suspension 0,02 % w/v). The fourth group was the positive control (given EDTA sodium liquid 1 % w/v only). Blood glucose level was measured before and after treatment by using spektrophotometer (578 nm). The result showed that colloidal CMC sodium liquid 1 % w/v lowered blood glucose level (not significant as 0,7 mg/dL). EDTA sodium liquid 1 % w/v + propranolol suspension 0,006 % w/v significantly lowered blood glucose level as 5,3 mg/dL, EDTA sodium liquid 1 % w/v + propranolol suspension 0,02% w/v also lowered the blood glucose level as 21,7 mg/dL, EDTA sodium liquid 1 % w/v significantly giving the effect on the increasing blood glucose level as 17,4 mg/dL.Key words : Propranolol, glucose, rabbi
Synthesis of 2,5-dibenzilidin cyclopentanone from benzaldehyde and cyclopentanone by solvent variation
Get PDFThe 2,5-dibenzilidine cyclopentanone is a Pentagamavunon-0 analogues (PGV-0) that showed an antiproliferative activity on raji, myeloma and Hella cells. This compound can be synthesized by condensation reaction of a keton and an aldehide by using acid or base as catalyst. The synthesis was carried by reacting cyclopentanone (10 mmol), benzaldehide (20 mmol) and potassium hydroxide 30% (20 mmol) at 5oC, followed by neutralize the reaction product with hydrochloride acid and the compound was obtained by crystalization on CCl4. It showed that rendemen in organic solven: [methanol (96.3 %), ethanol (73.2 %) and isopropanol (67.7%)]. The purity of the product was determined by using melting point and TLC methods . Structural elucidation was carried out by spectroscopic method ( UV-VIS, IR, H1-NMR and MS spectra). It could be concluded that the compound is 2,5-dibenzilidincyclopentanone.Key words: 2,5-dibenzilidincyclopentanone, catalyst, solven