Search results for: ethyl carbamate

Authors: Eunmi Koh, Bogyoung Choi, Dayeon Ryu, Jee-Yeon Lee, Sungok Kwon, Cho-Il Kim

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Ethyl carbamate(EC) is a probable human carcinogen (Group 2A) found in alcoholic beverages and fermented foods. A total of 351 samples including fermented foods and alcoholic beverages were chosen from 734 foods appeared in the pooled intake data of 2008, 2009, 2010, and 2011 Korea National Health & Nutrition Examination Survey (KNHANES). Sampling was carried out from September 2013 to July 2016 in 18 supermarkets of 9 metropolitan cities in Korea. The samples were pooled, prepared according to various cooking methods, and analyzed. A total of 1245 samples were analyzed using gas chromatograph-mass spectrometer. EC was detected in 13 items (1.0%), which ranged from not-detected to 151 g/kg. Alcoholic beverages (maesilju, whisky, and bokbunjaju) and fermented soy products (soy sauce and soybean paste) were the food items with relatively higher EC levels. Dietary intake of EC in the Korean population was estimated to be 2.11 ng/kg body weight (bw) per day for average population and 8.42 ng/kg bw per day for high consumers (the 97.5th percentile). When the estimated average dietary exposure to EC was compared with the Benchmark Dose Lower Confidence Limit 10% (BMDL10) of 0.3 mg/kg bw per day, margin of exposure (MOE) values of 1420000 to 28000000 were observed. This indicates that there is no health concern for the Korean population.

Keywords: ethyl carbamate, total diet study, dietary exposure, margin of exposure

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Authors: Fatih Sonmez

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Alzheimer’s disease (AD) is a progressive neurodegenerative disease and it is the most common form of dementia that affects aged people. Acetylcholinesterase is a hydrolase involved in the termination of impulse transmission at cholinergic synapses by rapid hydrolysis of the neurotransmitter ACh in the central and peripheral nervous system. Carvacrol (5-iso-propyl-2-methyl-phenol) is a main bioactive monoterpene isolated from many medicinal herbs, such as Thymus vulgaris, Monarda punctate and Origanum vulgare spp. It is known that carvacrol has been widely used as an active anti-inflammatory ingredient, which can inhibit the isoproterenol induced inflammation in myocardial infarcted rats. In this paper, a series of 12 carvacrol substituted carbamate derivatives (2a-l) was synthesized and their inhibitory activities on AChE and BuChE were evaluated. Among them, 2d exhibited the strongest inhibition against AChE with an IC50 value of 2.22 µM, which was 130-fold more than that of carvacrol (IC50 = 288.26 µM).

Keywords: Acetylcholinesterase, Butyrylcholinesterase, Carbamate, Carvacrol

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Authors: Hummera Rafique, Aamer Saeed

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Thioureas are highly biologically active compounds, as many important applications are associated with this nucleus. They serve as exceptionally versatile building block for the synthesis of wide variety of heterocyclic systems, which also possess extensive range of bioactivities. These thioureas were converted into five-membered heterocycles with imino moiety like ethyl 4-[2-benzamido-4-methylthiazol-3(2H)-yl)]benzoates (2a-j) by base catalyzed cyclization of corresponding thioureas with 2-bromoacetone and triethylamine in good yields.

Keywords: ethyl 4-[2-benzamido-4-methylthiazol-3(2H)-yl)]benzoates, ethyl 4-(3-benzoylthioureido) benzoates, antibacterial activity

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Authors: M. A. Sedghamiz, S. Raeissi

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This study presents three different approaches to estimate bubble point pressures for the binary system of CO2 and ethyl palmitate fatty acid ethyl ester. The first method involves the Peng-Robinson (PR) Equation of State (EoS) with the conventional mixing rule of Van der Waals. The second approach involves the PR EOS together with the Wong Sandler (WS) mixing rule, coupled with the Uniquac Ge model. In order to model the bubble point pressures with this approach, the volume and area parameter for ethyl palmitate were estimated by the Hansen group contribution method. The last method involved the Peng-Robinson, combined with the Wong-Sandler Method, but using NRTL as the GE model. Results using the Van der Waals mixing rule clearly indicated that this method has the largest errors among all three methods, with errors in the range of 3.96–6.22 %. The Pr-Ws-Uniquac method exhibited small errors, with average absolute deviations between 0.95 to 1.97 percent. The Pr-Ws-Nrtl method led to the least errors where average absolute deviations ranged between 0.65-1.7%.

Keywords: bubble pressure, Gibbs excess energy model, mixing rule, CO2 solubility, ethyl palmitate

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Authors: Shahana Sharmin

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In the present study, the effect of cellulose polymers Ethyl Cellulose and Hydroxy Propyl Methyl Cellulose was evaluated on the release profile of drug from sustained release pellet. Diltiazem Hydrochloride, an antihypertensive, cardio-protective agent and slow channel blocker were used as a model drug to evaluate its release characteristics from different pellets formulations. Diltiazem Hydrochloride sustained release pellets were prepared by drug loading (drug binder suspension) on neutral pellets followed by different percentages of spraying, i.e. 2%,4%, 6%, 8% and 10% coating suspension using ethyl cellulose and hydroxy-propyl methyl cellulose polymer in a fixed 85:15 ratios respectively. The in vitro dissolution studies of Diltiazem Hydrochloride from these sustained release pellets were carried out in pH 7.2 phosphate buffer for 1, 2, 3, 4, 5, 6, 7, and 8 hrs using USP-I method. Statistically, significant differences were found among the drug release profile from different formulations. Polymer content with the highest concentration of Ethyl cellulose on the pellets shows the highest release retarding rate of the drug. The retarding capacity decreases with the decreased concentration of ethyl cellulose. The release mechanism was explored and explained with zero order, first order, Higuchi and Korsmeyer’s equations. Finally, the study showed that the profile and kinetics of drug release were functions of polymer type, polymer concentration & the physico-chemical properties of the drug.

Keywords: diltiazem hydrochloride, ethyl cellulose, hydroxy propyl methyl cellulose, release kinetics, sustained release pellets

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Authors: Rufai Yakubu And Suleiman Kabiru

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Triterpenoids are a diverse class of secondary metabolites with potential antimicrobial properties. In this study, the crude extracts from ethyl acetate was obtained with ultrasonic extraction method. Using a combined chromatographic separation method to isolate squalene (1) stigmasterol (2), stigmasta-5,22-diene-3-ol acetate (3), γ-sitosterol (4), lupeol (5), taraxasterol (6), and betulinic acid (7) from ethyl acetate extracts. Ethyl acetate crude extracts and isolated compounds were both screened for antimicrobial activity and minimum inhibitory concentration (MIC). For ethyl acetate crude extracts with concentrations of (1.5, 0.75, 0.35, & 0.168 mg/mL) indicated marginal antibacterial activity with a range of 17, 20 and 14 mm zone of inhibition for Staphylococcus aureus, Escherichia coli and Candida albicans and lower minimum inhibitory concentrations ranges from 18.75 µg/ml to 150 µg/mL. Butulinic acid showed the highest activity against E. coli and C. albicans at 15 mm and 15 mm followed by Lupeol against S. aureus, E. coli and C. albicans at 13, 12, 12 mm. Moreso, no antimicrobial activity for both S. aureus and C. albicans with squalene except for E. coli which showed activity at 11 mm with 300 µg/mL (MIC). Thus, abundant triterpenoids in Deinbollia pinnata will be another centered area for antimicrobial drug discovery.

Keywords: triterpenoid, antimicrobial potentials, deinbollia pinnata, aerial parts

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Authors: V. Lokesh, M. Manjunathan, S. Sairam, K. Saithsh Kumar, R. Anantharaj

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The densities of pure and its binary mixtures of 1-Butyl-3-methyl imidazolium bis (trifluoro methyl sulfonyl) imide and 1–Ethyl-3-methyl imidazolium ethyl sulphate at different temperature, over the entire composition range were measured at 293.15, 298.15, 303.15, 308.15, 313.15, 318.15, 323.15, 328.15, 33.15, 338.15, 343.15 K. In this study, the liquid-liquid extraction procedure was used. From this experimental data, the excess molar volumes, apparent molar volume, partial molar volumes and the excess partial molar volumes have been calculated for over the whole composition range. Hence, the effect of temperature and composition on all derived thermodynamic properties of this binary mixture will be discussed in terms of intermolecular interactions.

Keywords: ionic liquid, interaction energy, effect of temperature, effect of composition

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Authors: Kiurski S. Jelena, Aksentijević M. Snežana, Oros B. Ivana, Kecić S. Vesna, Djogo Z. Maja

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The paper investigates the effect of light intensity on the formation of two ketones, acetone and methyl ethyl ketone, in working premises of five pad printing departments in Novi Sad, Serbia. Multiple linear regression analysis examined the form of interdependency concentrations of methyl ethyl ketone, acetone and light intensity in five printing presses at seven sampling points, using Statistica software package version 10th. The results show an average stacking variation investigated variable and can be presented by the general regression model: y = b0 + b1xi1 + b2xi2.

Keywords: acetone, methyl ethyl ketone, multiple linear regression analysis, pad printing

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Authors: Asep Sukohar, Ramadhan Triyandi, Muhammad Iqbal, Sahidin, Suharyani

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Introduction: Resveratrol is a class of bioactive chemicals found in melinjo, which has a wide range of biological actions. The purpose of this study is to determine the linarin content of the melinjo fraksi by using preparative-high-performance liquid chromatography (prep-HPLC). Method: Extraction used the soxhletation method with 96% ethanol solvent. Fractionation used ethyl acetate and ethanol in a ratio of 1:1. Tracing of linarin compound used prep-HPLC with a mobile phase ratio of distilled water: methanol (55: 45, v/v). The presence of linarin was detected using a wavelength of 215 nm. Fourier Transform Infrared (FTIR) was used to identify the functional groups of compound. Result: The retention time required to elute the ethyl acetate fraction was 2.601 minutes. Compound separation identification using Fourier Transform Infrared Spectroscopy - Quest Attenuated Total Reflectance (FTIR - QATR) has a similarity value range with standards from 0 to 1000. The elution results of the ethyl acetate fraction have similar values with the standard compounds linarin (668), resveratrol (578), and catechin (455). Conclusion: Tracing for active compound in the ethyl acetate fraction of Gnetum Gnemon L. using prep-HPLC showed a strong suspicion of the presence of linarin compound.

Keywords: Gnetum gnemon L., linarin, prep-HPLC, fraction ethyl acetate

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Authors: Camila da Silva, Simone Belorte de Andrade, Vitor Augusto dos Santos Garcia, Vladimir Ferreira Cabral, J. Vladimir Oliveira Lúcio Cardozo-Filho

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In the present study, the non-catalytic transesterification of soybean oil in continuous mode using supercritical ethanol were investigated. Experiments were performed in a packed-bed tubular reactor (PBTR) and variable studied were reaction temperature (523 K to 598 K), pressure (10 MPa to 20 MPa), oil to ethanol molar ratio (1:10 to 1:40) and water concentration (0 wt% to 10 wt% in ethanol). Results showed that ethyl esters yields obtained in the PBTR were higher (> 20 wt%) than those verified in a tubular reactor (TR), due to improved mass transfer conditions attained in the PBTR. Results demonstrated that temperature, pressure, oil to ethanol molar ratio and water concentration had a positive effect on fatty acid ethyl esters (FAEE) production in the experimental range investigated, with appreciable reaction yields (90 wt%) achieved at 598 K, 20 MPa, oil to ethanol molar ratio of 1:40 and 10 wt% of water concentration.

Keywords: packed bed reactor, ethyl esters, continuous process, catalyst-free process

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Authors: Mohammad Shamim Hasan Mandal, Phu Minh, Do Tan Khang, Phung Thi Tuyen, Tran Dang Xuan

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Rice (Oryza sativa L.) is one of the major crops of Vietnam which has more than thousands of varieties. Many of the local varieties have greater potentiality but they are in danger of extinct. Rice plant contains many secondary metabolites that are allelopathic to other plants. Seven rice varieties were cultivated in the field condition at Hiroshima University, Japan; stems and leaves from each variety were collected later, they were extracted with methanol, hexane, ethyl acetate, butanol, and water. Total phenolic content and total flavonoid contents were high in ethyl acetate extracts. DPPH antioxidant assay results showed that the ethyl acetate extracts had the higher IC50 value. Therefore, the ethyl acetate extracts were selected for laboratory experimentation through petri dish assay. Results showed that the two-local variety Re nuoc and Nan chon completely inhibited the germination of radish seedlings. Further laboratory bioassay and field experimentation will be conducted to validate the laboratory bioassay findings.

Keywords: allelopathy, bioassay, Oryza sativa, Raphanus sativus

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Authors: Nasser R. El-Brollosy, Roberta Loddo

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6-Benzyl-1-(ethoxymethyl)-5-isopropyluracil (Emivirine) and its corresponding 1-benzyloxymethyl analogue (TNK-651) showed high activity against HIV-1. The present study describes synthesis of novel emivirine analogues by reaction of chloromethyl ethyl ether with uracils having 5-ethyl / isopropyl and 6-(3,5-dimethoxybenzyl) substituents. A series of new TNK-651 analogues substituted at N-1 with phenoxyethoxymethyl moiety was prepared on treatment of the corresponding uracils with bis(phenoxyethoxy) methane. The newly synthesized non-nucleosides were tested for biological activity against wild type HIV-1 IIIB as well as the resistant strains N119 (Y181C), A17 (K103N + Y181C), and the triple mutant EFVR (K103R + V179D + P225H) in MT-4 cells. Some of the tested compounds showed good activities. Among them 6-(3,5-dimethylbenzyl)-5-ethyl-1-[2-(phenoxyethyl) oxymethyl]uracil which showed inhibitory potency higher than emivirine against both wild type HIV-1 and the tested mutant strains.

Keywords: Emivirine, HIV, non-nucleoside reverse transcriptase, uracils

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Authors: Paresh M. Patel, Amit A. Patel, R. H. Parikh

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The present investigation was undertaken to fabricate modified transport fluconazole that belongs to BCS class II and have a poor applicability on topical infection. So to improve topical application, transdermal spray could play a vital role by using ethyl cellulose and Eudragit® S100 as film-forming polymers. Concentration of Eudragit® S100, ethyl cellulose and permeation enhancer (camphor and menthol) were selected as independent variables, whereas drying time, viscosity and in-vitro drug release were selected as dependent variables in factorial design. The viscosity, drying time and in-vitro drug release of the optimize batch B15 was 40.1 cps, 47 sec. and 90.79% respectively. The film of optimized batch was flexible and dermal-adhesive.

Keywords: Eudragit, ethyl cellulose, fluconazole, transdermal spray

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Authors: Anıl Dinçer, Dilek Duranoğlu

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Ketones, which are widely used as solvent and chemical intermediates in chemical process industry, are commercially produced by using catalytic dehydrogenation of secondary alcohols at higher temperature (300-500ºC), and pressure (1-5 bar). Although it is possible to obtain high conversion values (60-87%) via gas phase catalytic dehydrogenation, working high temperature and pressure can result in side reactions and shorten the catalyst life. In order to overcome these challenges, catalytic dehydrogenation in the presence of an appropriate liquid solvent has been started to use. Hence, secondary alcohols can be converted to respective ketones at relatively low temperature (150-200ºC) under atmospheric pressure. In this study, methyl ethyl ketone and acetone was produced via catalytic dehydrogenation of appropriate secondary alcohols (isopropyl alcohol and sec-butyl alcohol) in the presence of liquid solvent at 160-190ºC. Obtained methyl ethyl ketone and acetone were analyzed by using FTIR and GC spectrometer. Effects of temperature, amount of catalyst and solvent on conversion and reaction rate were investigated. Optimum process conditions, which gave high conversion and reaction rate, were determined. According to GC results, 70% of secondary butyl alcohol and 42% of isopropyl alcohol was converted to related ketone (methyl ethyl ketone and acetone, respectively) at optimum process conditions. After distillation, 99.13% methyl ethyl ketone and 99.20% acetone was obtained. Consequently, liquid phase dehydrogenation process, which can compete with commercial gas phase process, was developed.

Keywords: dehydrogenation, liquid phase, methyl ethyl ketone, secondary alcohol

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Authors: M. Sivakumar, D. Chamundeeswari

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Glycosmis pentaphylla is one of the medicinally important plants belonging to the family Rutaceae, commonly known as “Anam or Panal” in Tamil. Traditionally, leaves are useful in fever, hepatopathy, eczema, skin disease, helminthiasis, wounds, and erysipelas. The fruits are sweet and are useful in vitiated conditions of vata, kapha, cough, and bronchitis. The roots are good for facial inflammations, rheumatism, jaundice, and anemia. The preliminary phytochemical investigations indicated the presence of alkaloids, terpenoids, flavonoids, tannins, sugar, glycoside, and phenolic compounds. In the present study, the root part of Glycosmis pentaphylla was used, and the root was collected from Western Ghats of South India. The root was sun/shade dried and pulverized to powder in a mechanical grinder. The powder was successively extracted with various solvents, and the ethyl acetate extract of Glycosmis pentaphylla has been subjected to the GC-MS analysis. Amongst the 46 chemical constituents identified from this plant, three major phytoconstituents were reported for the first time. Marmesin, a furanocumarin compound with the chemical structure 7H-Furo (3,2-G) (1)Benzopyran-7-one,2,3–dihydro–2 - (1-Hydroxy-1methylethyl)-(s) is one of the three compounds identified for the first time at the concentration of 11-60% in ethyl acetate extract of Glycosmis pentaphylla. Others include, Beta.-Fagarine (4.71%) and Paverine (13.08%).

Keywords: ethyl acetate extract, Glycosmis pentaphylla, GC-MS analysis, Phytochemicals

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Authors: Sharareh Sharifi, Pargol Ghavam Mostafavi, Ali Mashinchian Moradi, Mohammad Hadi Givianrad, Hassan Niknejad

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Marine organisms such as soft coral, sponge, ascidians, and tunicate containing rich source of natural compound have been studied in last decades because of their special chemical compounds with anticancer properties. The aim of this study was to investigate anti-cancer property of ethyl acetate extracted from marine sea pen Virgularia gustaviana found from Persian Gulf coastal (Bandar Abbas). The extraction processes were carried out with ethyl acetate for five days. Thin layer chromatography (TLC) and high-performance liquid chromatography (HPLC) were used for qualitative identification of crude extract. The viability of HeLa and MDA-Mb-231 cancer cells was investigated using MTT assay at the concentration of 25, 50, and a 100 µl/ml of ethyl acetate is extracted. The crude extract of Virgularia gustaviana demonstrated ten fractions with different Retention factor (Rf) by TLC and Retention time (Rt) evaluated by HPLC. The crude extract dose-dependently decreased cancer cell viability compared to control group. According to the results, the ethyl acetate extracted from Virgularia gustaviana inhibits the growth of cancer cells, an effect which needs to be further investigated in the future studies.

Keywords: anti-cancer, Hela cancer cell, MDA-Md-231 cancer cell, Virgularia gustavina

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Authors: M. N. Ofokansi, Onyemelukwe Chisom, Amauche Chukwuemeka, Ezema Onyinye

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The leaves of Clerodendrumcapitatum(Lamiaceae) is mostly used in the treatment of gastric ulcer in Nigerian folk medicine. The aim of this study was to evaluate the antiulcer activity of its crude methanol leaf extract and its ethyl acetate fraction in white albino rats. The effect of crude methanol leaf extract and its ethyl acetate fraction(250mg/kg, 500mg/kg) was evaluated using an absolute ethanol induced ulcer model. Crude methanol leaf extract and the ethyl acetate fraction was treated with distilled water and 6% Tween 80, respectively. crude methanol leaf extract was further investigated using a pylorus ligation induced ulcer model. Omeprazole was used as the standard treatment. Four groups of five albino rats of either sex were used. Parameters such as mean ulcer index and percentage ulcer protection were assessed in the ethanol-induced ulcer model, while the gastric volume, pH, and total acidity were assessed in the pyloric ligation induced ulcer model. Crude methanol leaf extract of Clerodendrumcapitatum(500mg/kg) showed a very highly significant reduction in mean ulcer index(p<0.001) in the absolute ethanol-induced model. ethyl acetate fraction of crude methanol leaf extract of Clerodendrumcapitatum(250mg/kg,500mg/kg) showed a very highly significant dose-dependent reduction in mean ulcer indices (p<0.001) in the absolute ethanol-induced model. The mean ulcer indices (1.6,2.2) with dose concentration (250mg/kg, 500mg/kg) of ethyl acetate fraction increased with ulcer protection (82.85%,76.42%) respectively when compared to the control group in the absolute ethanol-induced ulcer model. Crude methanol leaf extract of Clerodendrumcapitatum(250mg/kg, 500mg/kg) treated animals showed a highly significant dose-dependent reduction in mean ulcer index(p<0.01) with an increase in ulcer protection (56.77%,63.22%) respectively in pyloric ligated induced, ulcer model. Gastric parameters such as volume of gastric juice, pH, and total acidity were of no significance in the different doses of the crude methanol leaf extract when compared to the control group. The phytochemical investigation showed that the crude methanol leaf extracts Possess Saponins and Flavonoids while its ethyl acetate fraction possess only Flavonoids. The results of the study indicate that the crude methanol leaf extract and its ethyl acetate fraction is effective and has gastro protective and ulcer healing capacity. Ethyl acetate fraction is more potent than crude methanol leaf extract against ethanol-induced This result provides scientific evidence as a validation for its folkloric use in the treatment of gastric ulcer.

Keywords: gastroprotective, herbal medicine, anti-ulcer, pharmacology

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Authors: Sani Abubakar, Oumar Al-Mubarak Adoum

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The leaves extracts of Cassia sieberiana D. C. were screened for antimicrobial bioassay against Staphylococcus aureus, Salmonella typhi, and Escherichia coli and cytotoxicity using Brine Shrimp Test (BST). The crude ethanol extract, Chloroform soluble fraction, aqueous soluble fraction, ethyl acetate soluble fraction, methanol soluble fraction, and n-hexane soluble fraction were tested against antimicrobial and cytotoxicity. The Ethyl acetate fraction obtained proved to be most active in inducing complete lethality at minimum doses in BST and also active on Salmonella typhi. The bioactivity result was used to guide the column chromatography, which led to the isolation of pure compound CSB-8, which was found active in the BST with an LC₅₀ value of 34(722-182)µg/ml and showed remarkable activity on Salmonella typhi (zone of inhibition 25mm) at 10,000µg/ml. The ¹H-NMR, ¹³C NMR, FTIR, and GC-MS spectra of the compound suggested the proposed structure to be 2-pentadecanone.

Keywords: antimicrobial bioassay, cytotoxicity, column chromatagraphy, Cassia sieberiana D.C.

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Authors: K. Fellah, H. Benmehdi, A. Amrouche, H. Malainine, F. Memmou, H. Dalile, W. Siata

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This work aims to evaluate the antioxidant of flavonoids extracted from the leaves of Prunus persica L. A phytochemical screening allowed us to highlight the different phytochemicals present in the leaves of the studied plant. The selective extraction of flavonoids gave yields of 0.71, 1.5, and 4.8% for the fractions ethyl ether, ethyl acetate and n- butanol, respectively. The reading of the antioxidant activity of different extracts of flavonoids by HPLTC method revealed positive reaction (yellow spots) on the TLC plates sprayed with DPPH. Using the DPPH method, the fractions of flavonoids (bunanol, ethyl acetate and Diethyl ether) showed a potent scavenging activity with IC50 = 0.22; 0.27 and 0.76 mg / ml, respectively. Furthermore, our findings revealed the extracts under study exhibited higher reducing potential which depends upon extract concentration. These results obtained from this investigation confirm that the Prunus persica remains a major resource of bioactive molecules.

Keywords: Prunus persica L., phytochemical study, flavonoids, antioxidant activity, TLC bioautographic, FRAP, DPPH

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Authors: Eman Abdullah Morsi, Hend Okasha, Heba Abdel Hady, Mortada El-Sayed, Mohamed Abbas Shemis

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Context: Linum usitatissimum (Linn), known as Flaxseed, is one of the most important medicinal plants traditionally used for various health as nutritional purposes. Objective: Estimation of total phenolic and flavonoid contents as well as evaluate the antioxidant using α, α-diphenyl-β-picrylhydrazyl (DPPH), 2-2'azinobis (3-ethylbenzthiazoline-6-sulphonic acid (ABTS) and total antioxidant capacity (TAC) assay and investigation of anti-inflammatory by Bovine serum albumin (BSA) and anticancer activities of hepatocellular carcinoma cell line (HepG2) and breast cancer cell line (MCF7) have been applied on hexane, ethyl acetate, n-butanol and methanol extracts and also, fractions of methonal extract (hexane, ethyl acetate and n-butanol). Materials and Methods: Phenolic and flavonoid contents were detected using spectrophotometric and colorimetric assays. Antioxidant and anti-inflammatory activities were estimated in-vitro. Anticancer activity of extracts and fractions of methanolic extract were tested on (HepG2) and (MCF7). Results: Methanolic extract and its ethyl acetate fraction contain higher contents of total phenols and flavonoids. In addition, methanolic extract had higher antioxidant activity. Butanolic and ethyl acetate fractions yielded higher percent of inhibition of protein denaturation. Meanwhile, ethyl acetate fraction and methanolic extract had anticancer activity against HepG2 and MCF7 (IC50=60 ± 0.24 and 29.4 ± 0.12µg.mL⁻¹) and (IC50=94.7 ± 0.21 and 227 ± 0.48µg.mL⁻¹), respectively. In Gas chromatography-mass spectrometry (GC-MS) analysis, methanolic extract has 32 compounds, whereas; ethyl acetate and butanol fractions contain 40 and 36 compounds, respectively. Conclusion: Flaxseed contains totally different biologically active compounds that have been found to possess good variable activities, which can protect human body against several diseases.

Keywords: phenolic content, flavonoid content, HepG2, MCF7, hemolysis-assay, flaxseed

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Authors: Soumeya Krimat, Tahar Dob, Mohamed Toumi, Aicha Kesouri, Hafidha Metidji, Chelghoum Chabane

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Lavandula antineae Maire is an endemic medicinal plant of Algeria which is traditionally used for the treatment of chills, bruises, oedema and rheumatism. The present study was designed to investigate the phytochemical screening, total phenolic and antioxidant activity of Lavandula antineae Maire for the first time. Phytochemical screening revealed the presence of different kind of chemical groups (anthraquinones, terpenes, saponins, flavonoids, tannins, O-heterosides, C-heterosides, phenolic acids). The amounts of total phenolics in the extracts (hydromethanolic and ethyl acetate extract) were determined spectrometrically. From the analyses, ethyl acetate extract had the highest total phenolic content (262.35 mg GA/g extract) and antioxidant activity (IC50=7.10 µg/ml) using DPPH method. The ethyl acetate extract was also more potent on reducing power compared to hydromethanolic extract. The results suggested that L. antineae could be considered as a new potential source of natural antioxidant for pharmaceuticals and food preservation.

Keywords: Lavandula antineae, antioxidant activity, phytochemical screening, total phenolics

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Authors: Abdallah Bouguettoucha, Derradji Chebli, Tariq Yahyaoui, Hichem Attout

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The effect of acid -basic treatment of lingocellulosic material (forest wastes wild carob) on Ethyl violet adsorption was investigated. It was found that surface chemistry plays an important role in Ethyl violet (EV) adsorption. HCl treatment produces more active acidic surface groups such as carboxylic and lactone, resulting in an increase in the adsorption of EV dye. The adsorption efficiency was higher for treated of lingocellulosic material with HCl than for treated with KOH. Maximum biosorption capacity was 170 and 130 mg/g, for treated of lingocellulosic material with HCl than for treated with KOH at pH 6 respectively. It was also found that the time to reach equilibrium takes less than 25 min for both treated materials. The adsorption of basic dye (i.e., ethyl violet or basic violet 4) was carried out by varying some process parameters, such as initial concentration, pH and temperature. The adsorption process can be well described by means of a pseudo-second-order reaction model showing that boundary layer resistance was not the rate-limiting step, as confirmed by intraparticle diffusion since the linear plot of Qt versus t^0.5 did not pass through the origin. In addition, experimental data were accurately expressed by the Sips equation if compared with the Langmuir and Freundlich isotherms. The values of ΔG° and ΔH° confirmed that the adsorption of EV on acid-basic treated forest wast wild carob was spontaneous and endothermic in nature. The positive values of ΔS° suggested an irregular increase of the randomness at the treated lingocellulosic material -solution interface during the adsorption process.

Keywords: adsorption, isotherm models, thermodynamic parameters, wild carob

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Authors: Muhammad Ather Nadeem, Bilal Ahmad Khan, Hussam F. Najeeb Alawadi, Athar Mahmood, Aneela Nijabat, Tasawer Abbas, Muhammad Habib, Abdullah

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The global prevalence of Avena fatua infestation poses a significant challenge to wheat sustainability. While chemical control stands out as an efficient and rapid way to control weeds, concerns over developing resistance in weeds and environmental pollution have led to criticisms of herbicide use. Consequently, this study was designed to address these challenges through the chemical synthesis, characterization, and optimization of chitosan-based nanoparticles containing clodinofop Propargyl and fenoxaprop-P-ethyl for the effective management of A. fatua. Utilizing the ionic gelification technique, chitosan-based nanoparticles of clodinofop Propargyl and fenoxaprop-P-ethyl were prepared. These nanoparticles were applied at the 3-4 leaf stage of Phalaris minor weed, applying seven altered doses. These nanoparticles were applied at the 3-4 leaf stage of Phalaris minor weed, applying seven altered doses (D0 (Check weeds), D1 (Recommended dose of traditional-herbicide (TH), D2 (Recommended dose of Nano-herbicide (NPs-H)), D3 (NPs-H with 05-fold lower dose), D4 ((NPs-H) with 10-fold lower dose), D5 (NPs-H with 15-fold lower dose), and D6 (NPs-H with 20-fold lower dose)). Characterization of the chitosan-containing herbicide nanoparticles (CHT-NPs) was conducted using FT-IR analysis, demonstrating a perfect match with standard parameters. UV–visible spectrum further revealed absorption peaks at 310 nm for NPs of clodinofop propargyl and at 330 nm for NPs of fenoxaprop-p-ethyl. This research aims to contribute to sustainable weed management practices by addressing the challenges associated with chemical herbicide use. The application of chitosan-based nanoparticles (CHT-NPs) containing fenoxaprop-P-ethyl and clodinofop-propargyl at the recommended dose of the standard herbicide resulted in 100% mortality and visible injury to weeds. Surprisingly, when applied at a lower dose with 5-folds, these chitosan-containing nanoparticles of clodinofop Propargyl and fenoxaprop-P-ethyl demonstrated extreme control efficacy. Furthermore, at a 10-fold lower dose compared to standard herbicides and the recommended dose of clodinofop-propargyl and fenoxaprop-P-ethyl, the chitosan-based nanoparticles exhibited comparable effects on chlorophyll content, visual injury (%), mortality (%), plant height (cm), fresh weight (g), and dry weight (g) of A. fatua. This study indicates that chitosan/tripolyphosphate-loaded nanoparticles containing clodinofop-propargyl and fenoxaprop-P-ethyl can be effectively utilized for the management of A. fatua at a 10-fold lower dose, highlighting their potential for sustainable and efficient weed control.

Keywords: mortality, chitosan-based nanoparticles, visual injury, chlorophyl contents, 5-fold lower dose.

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Authors: Kasipandi Muniyandi, Parimelazhagan Thangaraj

Abstract:

Plants are important prospective wealth of a country, combination of local health care information about a specific plant together with data published by several groups of scientists, can help in deciding whether it should be considered acceptable for medicinal use. In the developed countries, too, plant-derived drugs may be of importance. The wide variety of ailments that are being treated with Plectranthus is an indication of the medicinal value of the genus. A number of species are not toxic and so may be taken orally, whilst others are used topically on the skin or as enemas. This study was designed to evaluate the different properties of Plectranthus stocksii and the aerial parts were collected and extracted with petroleum ether, chloroform, ethyl acetate, acetone and methanol by Soxhlet apparatus and finally macerated with hot water. The quantification assays revealed that, leaf methanol extract showed higher total phenolic (415.41 mg GAE/ g extract) and tannin (177.53 mg GAE/ g extract) contents whereas leaf ethyl acetate exhibited higher flavonoids (777.11 mg RE/ g extract) content. The antioxidant efficiency of the extracts was analyzed by various radical scavenging assays. Among the different antioxidant assays, leaf ethyl acetate extract showed higher free radical scavenging activities against DPPH (IC50 = 3.46 µg/mL), ABTS (27417.65 µM TE/ g extract), FRAP (152.17 mM Fe(II)E/ mg extract) NO• radical (21.46%) and Superoxide radical (IC50 = 24.16 µg/mL) assays. All the parts P. stocksii extracts showed significant protection against OH• induced DNA damage at 50 µg concentration. The HPLC analysis of leaf ethyl acetate extract revealed the presence of Quercetin (30.29 µg/mg of extract) was the major compound. Anticancer activity of leaf ethyl acetate extract showed better IC50 values were 48.87 and 36.08 µg/ mL against MCF-7 and Caco-2 respectively. From this study, P. stocksii can act as a potent antioxidant and cytotoxic antimicrobial agent. The scope for drug development from this plant is endless and there is undoubtedly a call for further research in pharmaceutical industries.

Keywords: antioxidant, cytotoxicity, phenolics, plectranthus stocksii

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Authors: Adeyi Akindele Oluwatosin, Mustapha Kaosarat Keji, Ajisebiola Babafemi Siji, Adeyi Olubisi Esther, Damilohun Samuel Metibemu, Raphael Emuebie Okonji

Abstract:

Envenoming by Echis ocellatus is potentially life-threatening due to severe hemorrhage, renal failure, and capillary leakage. These effects are attributed to snake venom metalloproteinases (SVMPs). Due to drawbacks in the use of antivenom, natural inhibitors from plants are of interest in studies of new antivenom treatment. Antagonizing effects of bioactive compounds of Moringa oleifera, a known antisnake plant, are yet to be tested against SVMPs of E. ocellatus (SVMP-EO). Ethanol crude extract of M. oleifera was partitioned using n-hexane and ethyl acetate. Each partition was fractionated using column chromatography and tested against SVMP-EO purified through ion-exchange chromatography with EchiTab-PLUS polyvalent anti-venom as control. Phytoconstituents of ethyl acetate fraction were screened against the catalytic site of crystal of BaP1-SVMP, while drug-likeness and ADMET toxicity of compound were equally determined. The molecular weight of isolated SVMP-EO was 43.28 kDa, with a specific activity of 245 U/ml, a percentage yield of 62.83 %, and a purification fold of 0.920. The Vmax and Km values are 2 mg/ml and 38.095 μmol/ml/min, respectively, while the optimal pH and temperature are 6.0 and 40°C, respectively. Polyvalent anti-venom, crude extract, and ethyl acetate fraction of M. oleifera exhibited a complete inhibitory effect against SVMP-EO activity. The inhibitions of the P-1 and P-II metalloprotease’s enzymes by the ethyl acetate fraction are largely due to methanol, 6, 8, 9-trimethyl-4-(2-phenylethyl)-3-oxabicyclo[3.3.1]non-6-en-1-yl)- and paroxypropione, respectively. Both compounds are potential drug candidates with little or no concern of toxicity, as revealed from the in-silico predictions. The inhibitory effects suggest that this compound might be a therapeutic candidate for further exploration for treatment of Ocellatus’ envenoming.

Keywords: Echis ocellatus, Moringa oleifera, anti-venom, metalloproteases, snakebite, molecular docking

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Authors: Hande Taşdemir, Meral Şahin, Mehmet Saçak

Abstract:

Conductive composite materials obtained by physical or chemical mixing of two or more components having conducting and insulating properties have been increasingly attracted. Kaolinite in kaolin clays is one of silicates with two layers of molecular sheets of (Si2O5)2− and [Al2(OH)4]2+ with the chemical composition Al2Si2O5(OH)4. The most abundant hydrophillic kaolinite is extensively used in industrial processes and therefore it is convenient for the preparation of organic/inorganic composites. In this study, conductive poly(N-ethylaniline)/kaolinite composite was prepared by chemical polymerization of N-ethyl aniline in the presence of kaolinite particles using ammonium persulfate as oxidant in aqueous acidic medium. Poly(N-ethylaniline) content and conductivity of composite prepared were systematically investigated as a function of polymerization conditions such as ammonium persulfate, N-ethyl aniline and HCl concentrations. Poly(N-ethylaniline) content and conductivity of composite increased with increasing oxidant and monomer concentrations up to 0.1 M and 0.2 M, respectively, and decreased at higher concentrations. The maximum yield of polymer in the composite (15.0%) and the highest conductivity value of the composite (5.0×10-5 S/cm) was achieved by polymerization for 2 hours at 20°C in HCl of 0.5 M. The structure, morphological analyses and thermal behaviours of poly(N-ethylaniline)/kaolinite composite were characterized by FTIR and XRD spectroscopy, SEM and TGA techniques.

Keywords: kaolinite, poly(N-ethylaniline), conductive composite, chemical polymerization

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Authors: Krutika K. Sawant, Anil Solanki

Abstract:

The present study deals with the preparation and optimization of ethyl cellulose-containing disopyramide phosphate loaded microspheres using solvent evaporation technique. A central composite design consisting of a two-level full factorial design superimposed on a star design was employed for optimizing the preparation microspheres. The drug:polymer ratio (X1) and speed of the stirrer (X2) were chosen as the independent variables. The cumulative release of the drug at a different time (2, 6, 10, 14, and 18 hr) was selected as the dependent variable. An optimum polynomial equation was generated for the prediction of the response variable at time 10 hr. Based on the results of multiple linear regression analysis and F statistics, it was concluded that sustained action can be obtained when X1 and X2 are kept at high levels. The X1X2 interaction was found to be statistically significant. The drug release pattern fitted the Higuchi model well. The data of a selected batch were subjected to an optimization study using Box-Behnken design, and an optimal formulation was fabricated. Good agreement was observed between the predicted and the observed dissolution profiles of the optimal formulation.

Keywords: disopyramide phosphate, ethyl cellulose, microspheres, controlled release, Box-Behnken design, factorial design

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Authors: Syeda Hira, Muhammad Gulfraz

Abstract:

Background: Liver diseases cause serious health issues. Plants contain active compounds that significantly help in the treatment of various diseases. Ficus carica is traditionally used for the treatment of liver diseases. The purpose of the present study was the isolation and identification of active components from F.carica leaves which are responsible for hepatoprotective activity. Methods: The study was designed to identify the most active hepatoprotective sub-fraction from ethyl acetate fraction of Ficus carica by in vitro study and evaluation of its in vivo hepatoprotective effect in animal models. Ethyl acetate fraction was subjected to column, and a total of eight sub-fractions were obtained. In vitro, the hepatoprotective effect of all sub-fractions was determined on HepG2 cell lines. Toxicity was induced by CCl₄ (Carbon tetrachloride), and silymarin was used as a positive control. On the basis of the results, the most active sub-fraction was subjected to LC-MS and FT-IR analysis for the identification of bioactive compounds. In vivo, the hepatoprotective effect was determined in mice. Toxicity was induced by CCl₄; at the end of the experiment, biochemical parameters such as ALT, AST, ALP, bilirubin, and total protein were estimated in serum. Histopathology of liver tissues was also done. Results: Sub-fraction FVI exhibited significant (P<0.05) hepatoprotective activity as compared to other sub-fractions, which was almost similar to the standard drug silymarin. Six known bioactive compounds were identified from this sub-fraction after LC-MS analysis. In vivo, the hepatoprotective activity of sub-fraction FVI was evaluated in CCl₄-induced toxicated mice. Administration of CCl₄ significantly increased level of ALT (Alanine transaminase), AST (Aspartate aminotransferase), ALP (Alkaline phosphatase), and bilirubin and decreased the total protein. Treatment with sub-fraction FVI significantly (p<0.05) reversed the level of these biomarkers toward normal at both doses of 25 mg/kg and 50 mg/kg. Conclusion: Our findings confirmed the hepatoprotective effect of ethyl acetate fraction of F.carica. It could be a good candidate for the development of a natural hepatoprotective drug; pre-clinical investigation on ethyl acetate fraction is recommended.

Keywords: Ficus carica, hepatoprotective, CCl₄, bioactive compounds, liver markers

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Authors: Oluwafemi Ojo, Omotade Oloyede

Abstract:

This study seeks to investigate the antioxidative properties and the ability of aqueous, ethanolic and ethyl acetate extracts from Ocimum gratissimum (OG) leaves to inhibit some pro-oxidants (Fe2+ and sodium nitroprusside) induced lipid peroxidation in rat’s liver homogenates in vitro. The ability of the extracts to inhibit 25 µM FeSO4 and 7.0 µM sodium nitroprusside induced lipid peroxidation in isolated rat’s liver was determined. The results of the study revealed that both pro-oxidants caused a significantly decrease in (p < 0.05) accumulation of lipid peroxides. However, aqueous extract of OG shows a high ability to inhibit lipid production in the liver induced with SNP than Fe2+. Ethanolic and ethyl acetate extract of OG which shows a high ability to inhibit lipid production more when induced with Fe2+ than SNP. However, ethyl acetate fraction of OG shows a higher inhibitory effect on both Fe2+ and SNP induced lipid peroxidation in rat’s liver. This applies to its significantly higher extractable phytochemicals. Therefore, Fe II and sodium nitroprusside induced oxidative stress could be managed by dietary intake of Ocimum gratissimum leaves.

Keywords: antioxidative, pro-oxidants, lipid peroxidation, Ocimum gratissimum

Procedia PDF Downloads 479

Authors: İsmail Çeli̇k, Gülgün Ayhan-Kılcıgi̇l, Arzu Onay-Beşi̇kçi̇

Abstract:

In this study, some 2-(2-phenyl/substitutedphenyl)- lH-benzo[d]'imidazol-l-yl)-N'-(alkylthiosemicarbazide were designed and prepared. Firstly, 2-phenyl/ suhstitutedphenyl-lH-Benzo[d]imidazole was prepared via oxidative condensation of o-phenylenediamine, benzaldehyde and sodium metabisulfite. Treatment of the benzimidazole compound with ethyl chloroacetate in KOH/DMSO gave the ester compound ethyl 2-(2-substitutedphenyl)-1H-benzo[d]imidazol-l-yl)acetate. Hydrazine hydrate and the ester in ethanol were refluxed for 4 h to give 2-(2-phenyl/substitutedphenyl)-1H-benzo[d]imidazol-l-yl)acetohydrazide. Thiosemicarbazides were obtained by condensing acyl hydrazide with the alkylisothiocyanate in ethanol. Following the structure elucidation, benzimidazole compounds were tested for their EGFR kinase inhibitory activities by using ADP-GloTM Kinase Assay.

Keywords: benzimidazole, EGFR kinase inhibitor, synthesis, thiosemicarbazide

Procedia PDF Downloads 257