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REDUCTION ABILITY OF CURCUMIN AND DERIVATIVES ON FERRI : A MOLECULAR DYNAMIC STUDY
Get PDFMolecular dynamics (MD) simulation has been applied to curcumin, 4-methyl curcumin and 4-isopropil curcumin. They have reducting activities on Ferri to Ferro. A computation method used is AM1 (Austin Model 1) semiempiric method. Studying of computation is arranged to theoretical studying of structure and reactivity relationship on these molecules without solvent interaction (in vacuo). The time of simulation is taken from 0 – 10 ps (pico secon) with interval 0,0005 ps on 300oK. The result of experiment that has been proposed from the MD simulation is the structure of conformation trajectory of each molecules. By considering total energy and potential energy changes to time of simulation, along with the change of bonding length, bonding angle, and the atomic charges of -diketon active site to time of simulation. Reactivity of these molecules are analyzed from the geometric shape of the active site indicated that 4-isopropyl curcumin was the most reactive than the other to produce complex with Ferri, while 4-methyl curcumin within the complex was easiest in the reduction of Ferri to Ferro.Key words : molecular dynamic, curcumin, reductio
ANALYSIS OF POLYCYCLIC AROMATIC HYDROCARBON IN SOME MEAT PRODUCTS
Get PDFThe polycyclic aromatic hydrocarbons (PAHs) are a class of organic compounds, composed two or more fused aromatic (benzene) rings, occurred in the environment due to incomplete combustion of organic matters such as forest fires, volcanic eruption, burning of fossil fuels and incorrect process of meat cooking (grilling, smoking, roasting). Healt concerns are focussed on the metabolite transformation of PAHs, which may have mutagenic, carcinogenic and terratogenic activity. Due to their hydophobicity, it is probable the compounds enter human food chain and accumulated in human lipid tissues. Therefore, environment pollution by PAHs must be considered. PAHs gain entry to human body through several routes including respiration, absorpsion through skin surface ang through food consumption that have been polluted with PAHs. In this study concentrations of PAHs (pyrene, perilene, benzo(a)anthracene, benzo(k)fluorantrene and benzo(a)pyrene) in traditional smoked meat, liquid smoked meat and roasted meat are determined. Determination of PAHs used gas chromatograph with OV 17 2% as a stationary phase, nitrogen as carrier gas and flame ionization detector. The results showed that PAHs concentrations in traditional smoked meat were higher than liquid smoked meat (41.19 ppb and 1.03 – 9.26 ppb). In the roasted meat, lipid concentration and roasting time influence PAHs concentration level.Keywords : polycyclic aromatic hydrocarbon, smoked meat, liquid smok
CHEMICAL CONTENT OF TURMERIC ;CURCUMIN AND ITS DERIVATIVES
Get PDFA brief review on turmeric from the stand-point of chemical content are presented. Recent studies on turmeric showed that at least 7 compounds of curcumin derivatives have been found, including cyclocurcumin the newer curcumin derivative.Keywords : curcumin, curcumin derivatives
Synthesis of thiazol derivative compounds from α-bromo asil bromida and thiourea
Get PDFThiazol compounds are mostly used as therapeutics in varies effects. These compounds could be synthesized from starting materials that had been produced by local agrochemical industries i.e. alcohol (from the alcohol factories) and urea (from the fertilizer factory). Yielded bromacylbromide could be used to acylate urea derivatives to form aliphatic bromacylurea. When thiourea was used the cyclization product happened i.e. occurred thiazolon derivatives (without bromine). The lost of bromine could be detected by losing of cluster peak of bromine isotope on MS-spectra. The products of these processes were pure, there were 2-aminothiazol- 4-one 2-amino-5-methyl-thiazol-4-one and 2-amino-5-ethyl-thiazol-4-one.
Key word : alcohol, thiourea, aminothiazol-4-one
SYNTHESIS AND BIOLOGICAL ACTIVITY EVALUATION OF C-9154 ANTIBIOTIC DERIVATIVES FROM VANILLIN
Get PDFThis research was conducted in order to synthesize two derivatives of C-9154 antibiotic from vanillin and to evaluate their biological activities. The synthesis of these C-9154 derivatives was performed through alkylation of vanillin, preparation of the corresponding benzaldoxim, reduction of this benzaldoxim, treatment of the resulting substituted benzilamine with maleic anhydride and esterification of this C-9154 antibiotic derivative. The alkylation of vanillin was carried out using diethylsulfate and NaOH as the base to give 89% yield of ethyl vanillin. The oxim synthesis from ethyl vanillin was performed using hydroxylamine hydrochloride under alkaline condition at 50oC for 2 hours to yield 89% 4-ethoxy-3-methoxybenzaldoxim. Reduction of this benzaldoxim with metallic Na in absolute ethanol afforded 82% yield of 4-ethoxy-3-methoxybenzylamine. This benzylamine derivative was then reacted with maleic anhydride in benzene to give the acid-form of C-9154 antibiotic derivative (6) in 74% yield. Esterification of this acid conducted Jumina using absolute ethanol in the presence of concentrated sulfuric acid at reflux for 4 hours gave the ethyl ester-form of C-9154 antibiotic derivative (7) in 87% yield. Antimicrobial activity evaluation was conducted using Staphyllococcus aureus and Eschericia coli. Based on the minimum inhibition concentration (MIC) data determined using aqueous methanol as the reference, it was observed that the acid-form (6) and the ethyl ester-form (7) of C-9154 antibiotic derivative obtained respectively gave MIC values of 2000-3000 g/ml and 500-1000 g/ml respectively either towards Staphyllococcus aureus or Eschericia coli.Key words: antibiotics, vanillin, oxim, benzylamine, C-9154 derivative, antimicrobe
The influence of Pasak Bumi (Eurycoma longifolia Jack.) root infusa to male white mouse libido
Get PDFPasak Bumi ( Eurycoma Longifolia Jack.) is one of forest plant which have been used as aphrodisiac for many generation by the people in hinterland Kalimantan. The study was aimed to gain information of influence of pasak bumi root infusa to male white mouse libido.The research was pure experimental applying completely randomized design. Sixteen male white mice was divided into 2 groups which first group (negative control) was treated with aquadest by oral and the second group treated with pasak bumi roots infusa which its dosage 100 mg / 100 g body weight of male white mice by oral once a day for 21 days..Data of introduction, climbing, and coitus analysed with one way ANOVA and General Linear Measure model with 95% confidence level. The result indicated that usage period of pasak bumi root infusa (Eurycoma Longifolia Jack.) improving male white mice Iibido, which was showed by the increament amount of introduction and climbing of male white mice to female white mice.Key words: Eurycoma longifolia roots, libido, introduction, climbing, coitu
THE EFFECT OF GINGER RHIZOME JUICE ON ACUTE TOXICITY OF PROPANOLOL AND QUINIDINE IN MICE
Get PDFThe rhizome of ginger (Zingiber officinale, Rosc.) has been consumed by most people, as food ingredient or a traditional drug. In the previous research there was evidence that the ginger juice influenced the pharmacokinetics of propranolol (representative of drugs with high extraction ratio) and of sulfamezathine (as a model of sulfonamide drugs). The aim of this research is to study the effect of juice of ginger on the acute toxicity of propranolol and quinidine (a drug with a narrow therapeutic range). To achieve the aim of this study, mice were divided randomly into two groups, propranolol and quinidine. The each group was divided subsequently into controlled and pretreated groups. Mice in the controlled groups were given propranolol (I: 69 mg/kg BW; II; 82,80 mg/kg BW; III: 99,36 mg/kg BW; IV: 119,23 mg/kg BW) or quinidine (I: 265 mg/kg BW; II; 344,50 mg/kg BW; III: 447,85 mg/kg BW; IV: 582,25 mg/kg BW) through intraperitoneal injection, and those in pretreated group were pretreated with the ginger juice orally (5,6 ml/kg BW) an hour prior administration of propranolol or quinidine. The observations of the effect were done during the first three hours. The mice were killed and the vital organs were taken for histopathologic examination. The values of LD-50 were computed by Miller-Tainter Method (propranolol; LD-50controlled = 89,98 mg/kg BB dan LD-50treated = 87,51 mg/kg BB] [quinidine; LD-50controlled = 418,48 mg/kg BB dan LD-50 treated =331,93 mg/kg BB]. The results of this research showed that the ginger juice influences the acute toxicity of quinidine but the acute toxicity of propranolol.Key words: ginger rhizome, acute toxicity, mice, quinide, propanolo
Quantitative structure-activity relationship of curcumin and its derivatives as μ-class of GST inhibitors
Get PDFThe Quantitative Structure-Activity Relationship (QSAR) study has been performed on curcumin and its derivatives as μ-class glutathione Stransferase inhibitors using atomic net charges as the predictors. The charges were resulted by semiempirical AM1 quantum-chemical calculations using the computational chemistry approach. The inhibition activity was expressed as the concentration that gave 50% inhibition of μ-class GST activity (IC50). The selection of the best QSAR equation models was determined by multiple linear regression analysis. Curcumin and its derivatives were reported as selective μ-class GST inhibitors. The enzyme plays an important role in the process of inflammation and the effectivity of anti lung-cancer compounds. μ-Class GST inhibitors could enhance the effectivity of anti lung-cancer compounds.The result showed that the best QSAR equation model of curcumin and its derivatives as μ-class GST inhibitors was described by.: log (1/IC50) = (-454.686) + (314.235)qC2 + (1593.499)qC3 + (452.563)qC4 + (1057.194)qC5 + (-1.756)qBenzene’ The equation was significant at 95% level with statistical parameters : n = 10, m = 5, F/FTabel = 3.335, R2 = 0.963, SE = 0.150, and PRESS = 0.559.Key words : QSAR analysis, curcumin, μ-class glutathione S-transferase, atomic net charge
Inhibitory potency of some methoxyphenyl derivatives compounds on class mu GST activity in vitro
Get PDFMethoxy phenyl derivative’s compounds i.e. curcumin, ferulic acid, and indomethacin have been reported to have inhibitory effects on rat’s liver glutathione S-transferases (GST) activity. Vaniline and ferulic acid have been known as degradation products of curcumin, and still have methoxy phenyl groups on the structures. Until the recent years, there is no information concerning the influences of methoxy phenyl derivative’s compounds i.e. vaniline, dimethylcurcumin and ethyl-p-methoxycinnamate on GST-activity. The aim of this research is to study the correlation of the inhibitory activity of class mu GST isolated from uninduced and phenobarbital-induced rat liver cytosol by curcumin, dimethylcurcumin, vaniline, indomethacin, ethyl pmethoxycinnamate, and ferulic acid. GST activity was measured spectrophotometrically on the conjugation of DCNB and GSH. The results showed that the inhibitory activity of mu class GST in uninduced or phenobarbital-induced rat liver GST were decreasing as follow : curcumin, dimethylcurcumin, vaniline, indomethacin, ethyl p-methoxycinnamate, and ferulic acid.Key words: methoxyphenyl derivative’s compounds, glutathione S-transferases activity
Isolation and identification artemisinine from product of endophyte microbe cultivation from Artemisia annua. [studies on endophytic microbes of Artemisia spp. (3)]
Get PDFIsolation of the biotransformation product artemisinine from endophitic bacteria is a new alternative for the production of the multidrugresistant antimalaria compounds. The bacteria strain, AT 12, has been proved particularly potential as an artemisinin source.This working was carried out to isolate and to identify the biotransformation product artemisinin as an antimalarial active compound from endophitic bacteria strains of Artemisia annua. The IR spectrum exhibited the characteristic bands for δ-lactone (1750-1735 cm-1, 1250-1111 cm-1) and endoperoxide function (~1115 cm-1, 890-830 cm-1). As a result, the GC-MS gave a positively identification for the majority of GC peaks. The mass spectrum of the peak (Rt 27.94 min) has a molecular ion of artemisinin with one hydrogen loss at m/z 281, representing (M+ - 1).Keywords: Artemisia spp. Artemisia annua, Endophytic, Artemisinine, sesquiterpen