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SYNTHESIS AND SCREENING OF SOME AZOMETHINES BEARING METHYL SALICYLATE MOIETY FOR ANTIBACTERIAL ACTIVITIES
Full text linkIn this study, the series of novel azomethines were synthesized from methyl salicylate and their structural determination was done by IR, NMR and mass spectral data. The screening of these synthesized compounds were done against some Gram positive and Gram negative bacteria in DMF and DMSO solvents by agar disc method. It is observed that solvent and compound structure both affect the inhibition. DMF is found to be good solvent in the present study. Amongst all studied compounds, JB-4 showed maximum zone of inhibition against most of the studied bacterial strains while compound JB-2 is least effective. Thus, substitution affects inhibition and methyl salicylate moiety with cinnamaldehyde side chain is most effective. Further, virtual screening of these compounds was done to evaluate molecular properties and bioactive scores of these compounds.Keywords: azomethines, methyl salicylate, antibacterial activity, agar disc method, DMF, DMS
Methyleugenol, a major metabolite on culture of endophytic fungi isolated from pandan wangi plant
Full text linkTwo kinds of endophytic fungi i.e. Colletotricum sp. PWD2 and Coelomycetes PWA1 isolated from pandan wangi (Pandanus amarylifolius) have been cultivated in a liquid medium, GYP for 3 weeks at room temperature without agitation. The ethyl acetate extracts derived from liquid cultures showed antifungal activity against Saccharomyces cerevisiae. The GC-MS analysis results showed methyleugenol as main metabolite in the ethyl acetate extract of both fungi cultures.Key words: pandan wangi, Pandanus amarylifolius, endophytic fungi, antifungal, methyleugeno
Optimization of piroxicam tablet formula using flowlac, avicel and compritol by Simplex Lattice Design Method
Full text linkPiroksikam is non steroid anti inflammation drug (NSAID) with small dose (10-20 mg daily) with a long time (t1/2) elimination. Piroxicam formulation was expected able to yield a good (quality) tablet to physical characteristic standard. Tablet r component was consisted of Flowlac 100 (filler), Avicel PH-101 (binder) and Compritol 888 ATO (lubricant).The research was done with simplex lattice design (SLD) by using 3 component, i.e. Flowlac (A), Avicel (B), and Compritol (C). Seven formula were needed, I,e, F1 (100 % A), F2 (100 % B), F3 (100 % C), F4 (50 % A and 50 % B), F5 (50 % B and 50 % C), F6 (50 % A and 50 % C),dan F7 (33.33% A, 33.33 % B, 33.33 % C). The optimization parameters of piroxicam tablets were flow rate of the tablet mass, tablet hardness, disintegration time, piroxicam content and the dissolution (C45), on SLD model; equations, contour plots, and superimposed of contour plots were obtained, by which the optimum formula was determined.Based on superimposed contour plot optimum formula was obtained with proportion of Flowlac (89.6 %), Avicel (7.4 %) and Compritol (3 %). The result of flowability was 21.46 g/second; hardness (6.46 kg); disintegration time (6.98 minutes); drug content (10.13 mg) and dissolution C45 (7.35 mg) Interaction of Flowlac-Avicel-Compritol could influence the physical properties and the release profile of tablet. Flowlac was the most dominant factor in increasing flowability, hardness and dissolution of tablet. Compritol was the most dominant factor in increating time of disintegration tablet.Key words: optimization; piroxicam; simplex lattice design
The effect of cauli flower (Brassica oleracea var. botrytis L.) to the change of : cholesterol, MDA level of rats hiperlipide
No full textThe unbalance of oxidant and antioxidant can effect of various diseases, for example atherosclerosis. High total cholesterol level was given the risk factor to atherosclerosis. This research aims to know the effect ofcauliflower (Brassica oleracea var. botrytis L.) juice to change of total cholesterol level and peroxide of lipid (MDA level). A twenty white rats Wistar strain were treated as hiperkolesterolemia with consumed a high fat meal for14 days, then devided in to 4 groups. Group I as positive control was given a green tea leaf infuse through a dosage 0,605 g/ kg BW, group II as negative control was given an aquadestilata. Then Group III and IV as were givencauliflower juice through a dosage 15 mL/ kg BW and 20 mL/ kg BW for 14 days. The result of this research were concluded that cauliflower juice through a dosage 15 mL/ kg BW and 20 mL/ kg BW was decreased of total cholesterol level and lipid peroxide (MDA level). Cauliflower juice through a dosage 20 mL/kg BW was found as an effective dosage to decreased of total cholesterol level and lipid peroxide (MDA level) of male white rats Wistar strain with high fat diet treatment.Key words : Juice, cauliflower, total cholesterol, peroxide of lipid, MDA
Antibacterial activity of ten medicinal plants obtained from some selected villages in the states of Kedah and Penang, Malaysia
No full textThe antimicrobial activities of ten plant extracts showed some degree of variation among Gram positive and Gram negative bacteria. Nineteen crude plant extracts were active against Gram positive bacteria as compared to only 9 against Gram negative bacteria. The most resistant bacteria was K. pneumoniae K6 which showed no sign of susceptibility towards any of the plant extracts. This might be due to the presence of ß-lactamase, which had been reported recently. S. epidermidis* showed susceptibility towards all plants except for M. citrifolia L. The highest zone of inhibition was 14.67 mm which was found in P. guajava extracts against S. epidermidis and this is closely followed by M. indica (at 13.67 mm ) against the same bacteria. Among all the plants which have been studied only M. citrifolia L. extract did not show any sign of antimicrobial activity. The result showed that means of inhibition zones between each plant extract were significantly different.Key words: Antibacterial; Gram positive; Gram negative; medicinal plants
Synthesis of a potential angiogenesis inhibitor compound: 2-benzylidene cyclohexane-1,3-dione
No full textSynthesis of an aromatic cyclic enadione, 2-benzylidene-cyclohexane-1,3-dione (a potential angiogenesis inhibitor), has been done using benzaldehide (50 mmole) and cyclohexane-1,3-dione (50 mmole) as starting materials and NaOH 1.0 N as a catalyst. Odorless and white needle-shape powder has been achieved. The powder was 252.7 mg (2.53 %) and the purity of the powder was 88.81 %. Its melting point was 214.8 oC. The purity of the product was examined by gas chromatography, while the structure elucidation was done using IR spectrometer, 1H-NMR spectrometer, and GC-MS.IR spectrometer showed that the compound had a -C=O bond conjugated to an alkene or a phenyl moiety, methylen groups, and alkene’s -C–H bonds. 1H-NMR spectrometer showed that the compound had benzene moiety and methylen moieties, which were in α and β position to a carbonyl group. GC-MS showed that the molecular weight of the compound was 200 atomic mass unit.Key words: Angiogenesis inhibitor, synthesis, 2-benzylidene-cyclohexane-1,3-dione
Teratogenicity study of combination of ginger rhizome extract and noni fruit extract in Wistar rat
No full textGinger (Zingiber officinale Roscoe var. sunti Val.) extract in combination with noni (Morinda citrifolia Linn.) extract has been proven to be effective in tuberculosis patients. To examine its safety in pregnancy condition, the influence of combination of ethanol extract of ginger and ethanol extract of noni fruit had been studied in pregnant Wistar rat. The ginger and noni extract were administered orally at dose level combination of 50 and 50 mg/kg BW , 500 and 500 mg/kg BW , 1000 and 1000 mg/kg BW on day sixth to fifteenth of gestation. The mother was sacrified on day nineteenth of gestation to observe life fetus, resorption, and growfail fetus. One third of the fetuses eviscerated for skeletal staining with alizarin red and two third of the fetuses were hardened with Bouin’s fixation solution. No malformation were found in the eviscerated group. The combination at all doses did not cause any fetus resorption, growth failure and did not cause malformation in organ and skeleton. The combination dose of 500 and 500 as well as 1000 and 1000 mg/kg BW caused dark red to black color in the liver of rat fetuses of 7.3 and 8.3 % respectively.Key words: teratogenicity study, Zingiber officinale Roscoe var. sunti Val, Morinda citrifolia Linn
n-Butanolic fraction of endofitic fungi of Buah Makasar increases apoptotic effect of doxorubicin on MCF-7 cells
No full textMakassar fruit, Brucea javanica (L.) Merr., showed chemopreventive activity. Secondary metabolites come from B. javanica fruit, brucatol and bruceantine, induced cell differentiation and apoptosis on Leukemia cell, while quassinoid and its derivates acted as antitumor promoter. Butanolic fraction of supernatan of endofitic fungi 1.2.11 isolate fermentation which isolated from B. javanica fruit showed cytotoxycity toward several cancer cells. This fraction has been predicted contain secondary metabolites from B. javanica and has been identified as Bruceosin and Canthin-6-one derivates. Butanolic fraction (FB) of supernatan from endofitic fungi 1.3.11 isolate fermentation is predicted for having similiar cytotoxycity as active as 1.2.11 isolate. This research is aimed to explore cytotoxycity potention and apoptosis induction of BF from 1.3.11 isolate and combination effect of BFdoxorubicinon MCF-7 breast cancer cell.Synergism of BF-doxorubicin combination detect from cell viability inhibition and apoptosis induction on MCF-7, a breast cancer cell lines which shows resistancy toward doxorubicin. Cell viability on single treatment of FB and doxorubicin and its combination were carried out by MTT assay to determine IC50 and combination index (CI). Apoptosis induction of FB, doxorubicin and its combination were carried out by ethidium bromideacridine orange DNA staining.n- Butanolic fraction and doxorubicin showed cell viability inhibition on MCF-7 cell with IC50 48 μg/mL dan 148 nM, respectively. Both of FB and doxorubicin showed apoptosis induction on IC50. Combination of FBdoxorubicin showed synergism and increased apoptosis induction on MCF-7cell.Key words: Brucea javanica, endofitic fungi, MCF-7 cell, synergism, doxorubicin
SYNTHESIS AND ANALGETIC ACTIVITY EVALUATION OF 4-[N-(4-HYDROXYPHENYL)CARBOXYMIDOYL]-2-METHOXYPHENOL
Full text linkParacetamol is an analgesic-antipyretic compound derived from p-aminophenol. Though paracetamol has good efficacy and safety on consumption, parasetamol has hepatotoxic effect as its adverse drug reaction. 4-[N-(4-hydroxyphenyl)carboxymidoyl]-2-methoxyphenol is one of p-aminophenol derivative that was already been determined in silico using molecular docking PLANTS method, and it was known that 4-[N-(4-hydroxyphenyl) carboxymidoyl]-2-methoxyphenol has analgesic effects more potent and has hepatotoxic adverse effect lower than paracetamol. 4-[N-(4-hydroxyphenyl)carboxymidoyl]-2-methoxy-phenol can be synthesized through reaction of p-aminophenol with vanillin under acid condition. The synthesized products were recrytalized, dried, and the purity was determined with melting point determination and Thin Layer Chromatography. The structure of pure crystals were elucidated using IR, 1H-NMR, C-NMR, and Mass Spectroscopy. The analgesic evaluation was carried in vivo using writhing test method. The synthesized compound were divided into three dosage variations, 0,5; 1; and 2 mol equivalent to 100 mg/kgBB of paracetamol (reference drug). 4-[N-(4-hydroxyphenyl)carboxymidoyl]-2-methoxyphenol with 1 mol dosage has analgesic activity better than paracetamol but the difference was not significant.Keywords: 4-[N-(4-hydroxyphenyl)carboxymidoyl]-2-methoxyphenol, p-aminophenol, analgesic, writhing tes
MONOSODIUM GLUTAMATE EXPOSURE AT EARLY DEVELOPMENTAL STAGE INCREASES APOPTOSIS AND STEREOTYPIC BEHAVIOR RISKS ON ZEBRAFISH (DANIO RERIO) LARVAE
Full text linkExcessive glutamate may give neurotoxic effects and contribute to Autism spectrum disorder(ASD). In this study, we investigated prolonged exposure effects of 10 µg/mL Monosodium Glutamate (MSG) on intracellular calcium level, bax, bcl-2, ratio of bax/bcl-2 genes expression, caspase-3, apoptosis of brain cells and stereotypic behavior of Zebrafish (Danio rerio) larvae at early developmental stages. Genes expression were determined by real time PCR, caspase-3 using ELISA, intracellular Ca2+ and apoptotic cells of brain using confocal microscopy, locomotor activity by using crossing lines assay whereas stereotypic behavior by circle swimming. The results indicated that MSG exposure increased brain bax and bcl-2; and caspase-3; intracellular Ca2+; and apoptosis; stereotypic behavior; and decreased locomotor activity. Termination of MSG treatments resulted in recovery of bax, bcl-2, caspase-3 basal levels and stereotypic behavior. In conclusion, MSG exposure at early embryonic stage increased brain cell damage and risk of behavior changes