Search results for: antioxidant compounds

Authors: Arash Jafari, Somaye Bahrami, Mohammad Hossein Razi Jalali

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Dicrocoeliosis, caused by Dicrocoelium dendriticum is a hepatic parasitic disease of clinical and financial significance in ruminant breeding, which causes direct losses due to condemnation of parasitized livers. The purpose of our study was to assess the effects of natural dicrocoeliosis on the antioxidant defense capability of the liver in sheep. For this purpose, livers of 40 infected sheep with D. dendriticumalong with livers of 20 healthy (control) sheep were collected from animals slaughtered in Khuzestan province, Iran. An increase in malondialdehyde concentrations accompanied by decreased activities of SOD and GPX of infected liver was noticed when com-pared with control values. Our data indicate that through dicrocoeliosis insufficient scavenging of reactive oxygen species takes place and caused oxidative liver damage.

Keywords: Dicrocoelium dendriticum, lipid peroxidation, antioxidant enzyme, liver

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Authors: Hoda Sabry Othman, Randa Helmy Swellem, Galal Abd El-Moein Nawwar

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N-cyanoacetyl glycine is a reactive polyfunctional precursor for synthesis of new difficult accessible compounds including pyridones, thiazolopyridine and others. The key step of this protocol is the formation of different ylidines which underwent Michael addition with carbon nucleophiles affording various heterocyclic compounds. Selected compounds underwent pharmacological evaluation, in vitro against two cell lines; breast cell line (MCF-7),and liver cell line(HEPG2). Compounds 14, 15a and 16 showed IC50 values 8.93, 8.18 and 8.03 (µ/ml) respectively for breast cell line (MCF-7), while the standard drug (Tamoxifen) revealed IC50 8.31. With respect to the liver cell line (HEPG2), compounds 14 and 15a revealed IC50 18.4 and 13.6(µ/ml) respectively while the IC50 of the standard drug(5-Flurouracil) is 25(µ/ml). The antimicrobial activity was also screened and revealed that oxime 7 and ylidine 9f showed a broad-spectrum activity.

Keywords: antitumor, cyanoacetyl glycine, heterocycles, pyridones

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Authors: Eric Beyegue, Boris Azantza, Judith Laure Ngondi, Julius E. Oben

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Background: It is clearly that phytochemical constituents of plants in relation exhibit free radical scavenging, antioxidant and glycosylation properties. This study investigated the in vitro antioxidant and free radical scavenging, inhibited activities against α-amylase and invertase enzymes of stem bark extracts C. edulis (Olacaceae). Methods: Four extracts (hexane, dichloromethane, ethanol and aqueous) from the barks of C. edulis were used in this study. Colorimetric in vitro methods were using for evaluate free radical scavenging activity DPPH, ABTS, NO, OH, antioxidant capacity, glycosylation activity, inhibition of α-amylase and invertase activities, phenolic, flavonoid and alkaloid contents. Results: C. edulis extracts (CEE) had a higher scavenging potential on the 2, 2-diphenyl-1-picrylhydrazyl (DPPH), hydroxyl (OH), nitrite oxide (NO), 2, 2-azinobis (3-ethylbenzthiazoline)-6-sulfonic acid (ABTS) radicals and glucose scavenging with the IC50 varied between 41.95 and 36694.43 µg/ml depending on the solvent of extraction. The ethanol extract of C. edulis stem bark (CE EtOH) showed the highest polyphenolic (289.10 + 30.32), flavonoid (1.12 + 0.09) and alkaloids (18.47 + 0.16) content. All the tested extracts demonstrated a relative high inhibition potential against α-amylase and invertase digestive enzymes activities. Conclusion: This study suggests that CEE exhibited higher antioxidant potential and significant inhibition potential against digestive enzymes.

Keywords: Coula edulis, antioxidant, scavenging activity, amylase, invertase

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Authors: Dian Muzdalifah, Anastasia F. Devi, Zatil A. Athaillah, Linar Z. Udin

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Tempe is a functional food prepared from soybeans through Rhizopus spp fermentation. It is well known as functional food, originated from Indonesia. Most studies on tempe functionalities refer to ripe (48 h fermentation) tempe and only limited studies discuss overripe tempe while longer fermentation time possibly increased tempe health benefit. Hence, the present study was performed to investigate the cytotoxic activity againts MCF-7 breast cancer cells and antioxidant property of tempe prepared from 0–156 h of fermentation. Tempe samples were dried and extracted with acetone and ethanol, respectively. Their extracts were used for subsequent analysis. The cytotoxic activity was assessed on MCF 7 breast cancer cells using Alamar Blue method. The antioxidant activity was determined by DPPH free radical scavenging assay. The results indicated that acetone extracts of 108 h tempe had a potent cytotoxic activity against MCF-7 breast cancer cells (IC50 = 2.54 ± 0,30 μg/mL). Ethanol extracts of 108 h tempe also showed the potency, but at slightly higher IC50 (5.20 ± 1.01 μg/mL). Both acetone and ethanol extracts of 108 and 120 h tempe showed high antioxidant activity expressed as percent inhibition with no significant difference. However, acetone extracts of 120 h tempe (81.31 ± 3.70 %) had better ability to inhibit oxidation reaction than that of ethanol extracts (75.77 ± 6.00 %). It can be concluded that the cytotoxic activity of tempe from 0–156 h of fermentation is positively correlated to their corresponding antioxidant property. Longer fermentation time, up to 108 h, increased the ability of tempe to inhibit the growth of MCF-7 breast cancer cells and oxidative reaction. But extended fermentation time, up to 156 h, tends to decrease its ability. Further studies are encouraged to identify the active components contained in each extract.

Keywords: antioxidant property, cytotoxic activity, extracts, overripe tempeh

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Authors: Mohammad Javad Shakori, Esmaeil Babakhanzadeh Sajirani, Vajihe Esmaili

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Today, the increasing contamination is an environmental concern. There is relationship between plants and microorganisms many years ago. In this regard, an experiment was conducted in order to investigate the effect of different levels of lead across three levels ‘zero, 50, and 100 mg/L’ and Trichoderma Harzanium fungus across three levels ‘5, 10, and 15%’ in a factorial design in the form of fully randomized blocks in three replications under form conditions in the climatic conditions of Shahroud in Dehlama Village. This research was performed in 2014-2015 on cauliflower. In this experiment, chlorophyll a, b, total, cartenoid, phenol, flavonoid, and antioxidant properties of cauliflowers were measured. The results indicated that the greatest level of chlorophyll a (75.723 mg/wet weight), chlorophyll b (27.378 mg/wet weight), and total chlorophyll (109.074 mg/wet weight) was related to the interactive effects of 5% treatment of Trichoderma fungus and 0mg/L lead. The results also indicated that the greatest amount of antioxidant (79.88% of free radical) and flavonoides (22.889 mg of coercetin/g of dry weight) was related to the interactive effects of lead 50 mg/L and the treatment of Trichoderma fungus 5%. Further, the greatest level of phenol (21.33 mg of Gaelic acid/ dry weight) was related to the interactive effects of lead 100 mg/L and Trichoderma fungus 5% . As carotenoids are a type of antioxidant and precursor of vitamin A, with the development of alignment effect with other antioxidants such as the total phenol, flavonoid, achieved desirable levels of antioxidant.

Keywords: antioxidant, lead, flavonoid, cauliflower, chlorophyll

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Authors: Mohamed M. Ibrahima, Abdul Aziz A.AL Sahli, Ibrahim A. Alaraidh, Ali A. Al-Homaidan, E.M. Mostafa, G.A. EL-Gaaly

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Traditionally, in Middle Eastern countries, many cultures use chewing sticks of arak for medicinal purposes especially, for oral cleanliness care. It was used by Muslims for the treatment of teeth and highly recommended to be used by muslims during the whole day. Therefore, the present work aimed to determine the total phenolic content and total flavonoids in two Miswak extracts obtained from arak roots collected from two different localities in Saudi Arabia. They were extracted with aqueous ethanol (80%) and used to estimate in vitro their antioxidative abilities. The new findings showed that the two tested extracts contained significantly different amounts of both total phenolic content and total flavonoids. According to the increase of total phenolic contents and total flavonoids obtained from the two extracts, Miswak collected from the southern region was found to contain more contents than those collected from the middle region. The results of antioxidant activities of Miswak root extract obtained by using different in vitro methods were varied depending on the technique used. According to the malondialdehyde (MDA) method, hydrogen peroxide (H2O2) scavenging ability and 1,1-diphenyl-2-picrylhydrazyl (DPPH) methods, the two Miswak extracts exhibited to have high to very high antioxidant activities. Mostly, the values of antioxidant activities of Southern region have been shown to be always the highest.

Keywords: Arak, antioxidant, medicinal plants, Saudi Arabia

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Authors: Houria Djebar, Amina Saib, Malika Berredjem, Khaoula Bechlem, Mohammed-Reda Djebar

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Reactive oxygen species (ROS) have a high potential to damage almost all types of cellular components of the body, which explains their involvement in the induction and/or amplification of several pathologies. Supplementation of the body by exogenous antioxidants is very useful against these harmful species. In this context, we attempted to evaluate the in vitro and in vivo antioxidant activities of three newly synthesized amidophosphonates (AP1, AP2, and AP3). The results relating to the in vitro tests for DPPH radical scavenging activity shows that these amidophosphonates have a modest antiradical power (ARP) less effectively pronounced compared with an analogue marketed in Algeria: (Dursban) Clorpiryphos ethyl. However, in vivo effects were evaluated on some antioxidant systems (LP intensity, CAT activity and GSH content), or in combination with 2, 2-diphenyl-picrylhydrazyle (DPPH) radical in paramecium tetraurelia used as a complementary system to rapidly elucidate the cytotoxicity. On the basis of the results obtained it can be concluded that amidophosphonates studied exhibited a mild protective effect. The mechanism for how they influenced the antioxidant activities was discussed.

Keywords: Paramecium tetraurelia, amidophosphonates, antioxidant activity, DPPH free radical, in vitro experiments, biochemical parameters

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Authors: Siti Rohana Mohd Yatim, Ku Halim Ku Hamid, Kamariah Noor Ismail, Zulkifli Abdul Rashid

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The aim of this study is to investigate odour emission profiles from storage of food waste and to assess the potential health risk caused by exposure to volatile compounds. Food waste decomposition process was conducted for 14 days and kept at 20°C and 30°C in self-made bioreactor. VOCs emissions from both samples were collected at different stages of decomposition starting at day 0, day 1, day 3, day 5, day 7, day 10, day 12 and day 14. It was analyzed using TD-GC/MS. Findings showed that various VOCs were released during decomposition of food waste. Compounds produced were influenced by time, temperature and the physico-chemical characteristics of the compounds. The most abundant compound released was dimethyl disulfide. Potential health risk of exposure to this compound is represented by hazard ratio, HR, calculated at 1.6 x 1011. Since HR equal to or less than 1.0 is considered negligible risk, this indicates that the compound posed a potential risk to human health.

Keywords: volatile organic compounds, decomposition process, food waste, health risk

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Authors: Mervet A. El-sherif, Ginat M El-sherif, Kadry H Tolba

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The objective of this study was to determine, identify and investigate the effects of natural antioxidants of licorice and carob. Besides, their effects as powder and antioxidant extracts addition on refined sunflower oil stability as natural antioxidants were evaluated. Total polyphenol contents as total phenols, total carotenoids and total tannins were 353.93mg/100g (gallic acid), 10.62mg/100g (carotenoids) and 83.33mg/100g (tannic acid), respectively in licorice, while in carob, it was 186.07, 18.66 and 106.67, respectively. Polyphenol compounds of the studied licorice and carob extracts were determined and identified by HPLC. The stability of refined sunflower oil (which determined by peroxide value and Rancimat) was increased with increasing the level of polyphenols extracts addition. Also, our study shows the effect of addition of these polyphenols extracts to El-mewled El-nabawy sweets fortified by full cream milk powder (sesames and folia). We found that, licorice and carob as powder and polyphenols extracts were delayed the rancidity of sesame and peanut significantly. That encourages using licorice and carob as powder and polyphenols extracts as a good natural antioxidants source instead of synthetic antioxidants.

Keywords: licorice, carob, natural antioxidants, antioxidant activity, applications

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Authors: Loreta Serniene, Dalia Sekmokiene, Justina Tomkeviciute, Lina Lauciene, Vaida Andruleviciute, Ingrida Sinkeviciene, Kristina Kondrotiene, Neringa Kasetiene, Mindaugas Malakauskas

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One of the most important areas of product development and research in the dairy industry is the product enrichment with active ingredients as well as leading to increased product safety and sustainability. The most expanding field of the active ingredients is the various plants' CO₂ extracts with aromatic, antioxidant and antimicrobial properties. In this study, 15 plant extracts were evaluated based on their antioxidant, antimicrobial properties as well as sensory acceptance indicators for the development of new dairy products. In order to increase the total antioxidant capacity of the milk products, it was important to determine the content of phenolic compounds and antioxidant activity of CO₂ extract. The total phenolic content of fifteen different commercial CO₂ extracts was determined by the Folin-Ciocalteu reagent and expressed as milligrams of the Gallic acid equivalents (GAE) in gram of extract. The antioxidant activities were determined by 2.2′-azinobis-(3-ethylbenzthiazoline)-6-sulfonate (ABTS) methods. The study revealed that the antioxidant activities of investigated CO₂ extract vary from 4.478-62.035 µmole Trolox/g, while the total phenolic content was in the range of 2.021-38.906 mg GAE/g of extract. For the example, the estimated antioxidant activity of Chinese cinnamon (Cinammonum aromaticum) CO₂ extract was 62.023 ± 0.15 µmole Trolox/g and the total flavonoid content reached 17.962 ± 0.35 mg GAE/g. These two parameters suggest that cinnamon could be a promising supplement for the development of new cheese. The inhibitory effects of these essential oils were tested by using agar disc diffusion method against pathogenic bacteria, most commonly found in dairy products. The obtained results showed that essential oil of lemon myrtle (Backhousia citriodora) and cinnamon (Cinnamomum cassia) has antimicrobial activity against E. coli, S. aureus, B. cereus, P. florescens, L. monocytogenes, Br. thermosphacta, P. aeruginosa and S. typhimurium with the diameter of inhibition zones variation from 10 to 52 mm. The sensory taste acceptability of plant extracts in combination with a dairy product was evaluated by a group of sensory evaluation experts (31 individuals) by the criteria of overall taste acceptability in the scale of 0 (not acceptable) to 10 (very acceptable). Each of the tested samples included 200g grams of natural unsweetened greek yogurt without additives and 1 drop of single plant extract (essential oil). The highest average of overall taste acceptability was defined for the samples with essential oils of orange (Citrus sinensis) - average score 6.67, lemon myrtle (Backhousia citriodora) – 6.62, elderberry flower (Sambucus nigra flos.) – 6.61, lemon (Citrus limon) – 5.75 and cinnamon (Cinnamomum cassia) – 5.41, respectively. The results of this study indicate plant extracts of Cinnamomum cassia and Backhousia citriodora as a promising additive not only to increase the total antioxidant capacity of the milk products and as alternative antibacterial agent to combat pathogenic bacteria commonly found in dairy products but also as a desirable flavour for the taste pallet of the consumers with expressed need for safe, sustainable and innovative dairy products. Acknowledgment: This research was funded by the European Regional Development Fund according to the supported activity 'Research Projects Implemented by World-class Researcher Groups' under Measure No. 01.2.2-LMT-K-718.

Keywords: antioxidant properties, antimicrobial properties, cinnamon, CO₂ plant extracts, dairy products, essential oils, lemon myrtle

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Authors: Kobus-Cisowska Joanna, Flaczyk Ewa, Gramza-Michalowska Anna, Kmiecik Dominik, Przeor Monika, Marcinkowska Agata, Korczak Józef

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The object of this study was to develop recipes and technology of production of functional bread with morus alba fruit addition. There were prepared four samples of functional breads and the control sample also. Bread recipe was designed for supporting the treatment of anemia, diabetes, obesity and cardiovascular diseases. Samples of bread were baked with mixes directly after preparation and after three months' storage, each time preparing the water and methanol extracts. The sensory analysis and nutritional value were estimated. The antioxidant activity were estimated used tests such as the ability to scavenge free radical DPPH, the ability to scavenge the ABTS cation, chelating properties and the total content of polyphenols. The study results showed that the prepared sample of functional breads were characterized by a high nutritional value with high concentration of biologically active compounds which showed antioxidant activity. In addition, the profile sensory of bread samples was highly rated. However, to determine whether they can be considered as a new product preset pro-health properties require additional nutritional studies - clinical trials.

Keywords: functional food, breads, white mulberry, bioactive components

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Authors: Gajanan M. Sonwane

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The computational studies on 2-phenazinamines with their protein targets have been carried out to design compounds with potential anticancer activity. This strategy of designing compounds possessing selectivity over specific tyrosine kinase has been achieved through G-QSAR and molecular docking studies. The objective of this research has been to design newer 2-phenazinamine derivatives as Bcr-Abl tyrosine kinase inhibitors by G-QSAR, molecular docking studies followed by wet-lab studies along with evaluation of their anticancer potential. Computational chemistry was done by using VLife MDS 4.3 and Autodock 4.2 followed by wet-lab experiments for synthesizing 2-phenazinamine derivatives. The chemical structures of ligands in 2D were drawn by employing Chemdraw 2D Ultra 8.0 and were converted into 3D. These were optimized by using a semi-empirical method called MOPAC. The protein structure was retrieved from RCSC protein data bank as a PDB file. The binding interactions of protein and ligands were done by using PYMOL. The molecular properties of the designed compounds were predicted in silico by using Osiris property explorer. The parent compound 2-phenazinamine was synthesized by reduction of 2, 4-dinitro-N-phenyl-benzenamine in the presence of tin chloride followed by cyclization in the presence of nitrobenzene and magnesium sulfate. The derivatization at the amino function of 2-phenazinamine was performed by treating parent compound with various aldehydes in the presence of dicyclohexylcarbodiimide (DCC) and urea to afford 2-(2-chlorophenyl)-3-(phenazine-2-yl) thiazolidine-4-one. Synthesized 39 novel derivatives of 2-phenazinamine and performed antioxidant activity, anti antiproliferative on the bulb of onion and anticancer activity on cell line showing significant competition with marked blockbuster drug imatinib.

Keywords: computer-aided drug design, tyrosin kinases, anticancer, docking

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Authors: Sudha Summarwar, Sudesh Agarwal, Deepali Lall, Nalini Kataria, Jyotsana Pandey

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Assessment of antioxidant status is an effective tool to appraise the presence of oxidative stress. A combination of assays can be used to evaluate the antioxidant status like serum catalase (CAT), superoxide dismutase (SOD) and monoamine oxidase (MAO). In human medicine pregnancy is known to be associated with oxidative stress. Oxidative stress produces harmful effects to the developing foetus. Several metabolic changes occur in the maternal body to meet the demand of energy of developing foetus. Due to these changes susceptibility of maternal body increases to oxidative stress. There is paucity of research work on this aspect in nondescript goats. Therefore, the present study was intended to appraise the oxidative stress in pregnant and non-pregnant non-descript goat. Blood samples were collected for serum separation in otherwise healthy pregnant and non-pregnant nondescript goats. Mean values of serum CAT, SOD and MAO were found on a higher side (p≤0.05) with serum SOD values showing a rise of 2.5 times higher than the control healthy value. Correlations among all the three parameters were found to be highly significant (p≤0.01) especially greatest in youngest group of pregnant animals. Illustration of result enlightened the veracity of bumped up production of free radicals in pregnant animals. Technical savoir-faire of oxidative stress supervision is essential for upholding of health status of foetus. The upshot of present study undoubtedly implied the development of oxidative stress in pregnant goats on the basis of altered antioxidant status. These findings conclude that initially the oxidative stress due to pregnancy is critically combated by the intricate defensive mechanism of natural antioxidant system of the body. It appears that this imbalance between oxidant and antioxidant must be checked in time to prevent cellular damage by regularly appraising the antioxidant status through laboratory methods.

Keywords: antioxidant, oxidative stress, pregnancy, serum catalase

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Authors: M. Y. Maila, H. P. Makhubele

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Roasting is one of the oldest preservation method used in foods such as nuts and seeds. It is a process by which heat is applied to dry foodstuffs without the use of oil or water as a carrier. Groundnut seeds, also known as peanuts when sun dried or roasted, are among the oldest oil crops that are mostly consumed as a snack, after roasting in many parts of South Africa. However, roasting can denature proteins, destroy amino acids, decrease nutritive value and induce undesirable chemical changes in the final product. The aim of this study, therefore, was to evaluate the effect of various roasting times on the food value of the runner groundnut seeds. A constant temperature of 160 °C and various time-intervals (20, 30, 40, 50 and 60 min) were used for roasting groundnut seeds in an oven. Roasted groundnut seeds were then cooled and milled to flour. The milled sundried, raw groundnuts served as reference. The proximate analysis (moisture, energy and crude fats) was performed and the results were determined using standard methods. The antioxidant content was determined using HPLC. Mineral (cobalt, chromium, silicon and iron) contents were determined by first digesting the ash of sundried and roasted seed samples in 3M Hydrochloric acid and then determined by Atomic Absorption Spectrometry. All results were subjected to ANOVA through SAS software. Relative to the reference, roasting time significantly (p ≤ 0.05) reduced moisture (71%–88%), energy (74%) and crude fat (5%–64%) of the runner groundnut seeds, whereas the antioxidant content was significantly (p ≤ 0.05) increased (35%–72%) with increasing roasting time. Similarly, the tested mineral contents of the roasted runner groundnut seeds were also significantly (p ≤ 0.05) reduced at all roasting times: cobalt (21%–83%), chromium (48%–106%) and silicon (58%–77%). However, the iron content was significantly (p ≤ 0.05) unaffected. Generally, the tested runner groundnut seeds had higher food value in the raw state than in the roasted state, except for the antioxidant content. Moisture is a critical factor affecting the shelf life, texture and flavor of the final product. Loss of moisture ensures prolonged shelf life, which contribute to the stability of the roasted peanuts. Also, increased antioxidant content in roasted groundnuts is essential in other health-promoting compounds. In conclusion, the overall reduction in the proximate and mineral contents of the runner groundnuts seeds due to roasting is sufficient to suggest influences of roasting time on the food value of the final product and shelf life.

Keywords: dry roasting, legume, oil source, peanuts

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Authors: Suttijit Sriwatcharakul

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The bioactivity studies from the weed ethanolic crude extracts from leaf, stem, pod and root of wild spider flower; Cleoma viscosa Linn. were analyzed for the growth inhibition of 6 bacterial species; Salmonella typhimurium TISTR 5562, Pseudomonas aeruginosa ATCC 27853, Staphylococcus aureus TISTR 1466, Streptococcus epidermidis ATCC 1228, Escherichia coli DMST 4212 and Bacillus subtilis ATCC 6633 with initial concentration crude extract of 50 mg/ml. The agar well diffusion results found that the extracts inhibit only gram positive bacteria species; S. aureus, S. epidermidis and B. subtilis. The minimum inhibition concentration study with gram positive strains revealed that leaf crude extract give the best result of the lowest concentration compared with other plant parts to inhibit the growth of S. aureus, S. epidermidis and B. subtilis at 0.78, 0.39 and lower than 0.39 mg/ml, respectively. The determination of total phenolic compounds in the crude extracts exhibited the highest phenolic content was 10.41 mg GAE/g dry weight in leaf crude extract. Analyzed the efficacy of free radical scavenging by using DPPH radical scavenging assay with all crude extracts showed value of IC50 of leaf, stem, pod and root crude extracts were 8.32, 12.26, 21.62 and 35.99 mg/ml, respectively. Studied cytotoxicity of crude extracts on human breast adenocarcinoma cell line by MTT assay found that pod extract had the most cytotoxicity CC50 value, 32.41 µg/ml. Antioxidant activity and cytotoxicity of crude extracts exhibited that the more increase of extract concentration, the more activities indicated. According to the bioactivities results, the leaf crude extract of Cleoma viscosa Linn. is the most interesting plant part for further work to search the beneficial of this weed.

Keywords: antimicrobial, antioxidant activity, Cleoma viscosa Linn., cytotoxicity test, total phenolic compound

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Authors: Omoruyi Gold Idemudia, Alexander P. Sadimenko

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The synthesis of N-heterocycles with novel properties, having broad spectrum biological activities that may become alternative medicinal drugs, have been attracting a lot of research attention due to the emergence of medicinal drug’s limitations such as disease resistance and their toxicity effects among others. Acylpyrazolones have been employed as pharmaceuticals as well as analytical reagent and their application as coordination complexes with transition metal ions have been well established. By way of a condensation reaction with amines acylpyrazolone ketones form a more chelating and superior group of compounds known as azomethines. 4-propyl-3-methyl-1-phenyl-2-pyrazolin-5-one was reacted with phenylhydrazine to get a new phenylhydrazone which was further reacted with aqueous solutions of palladium and platinum salts, in an effort towards the discovery of transition metal based synthetic drugs. The compounds were characterized by means of analytical, spectroscopic, thermogravimetric analysis TGA, as well as x-ray crystallography. 4-propyl-3-methyl-1-phenyl-2-pyrazolin-5-one phenylhydrazone crystallizes in a triclinic crystal system with a P-1 (No. 2) space group based on x-ray crystallography. The bidentate ON ligand formed a square planar geometry on coordinating with metal ions based on FTIR, electronic and NMR spectra as well as magnetic moments. Reported compounds showed antibacterial activities against the nominated bacterial isolates using the disc diffusion technique at 20 mg/ml in triplicates. The metal complexes exhibited a better antibacterial activity with platinum complex having an MIC value of 0.63 mg/ml. Similarly, ligand and complexes also showed antioxidant scavenging properties against 2, 2-diphenyl-1-picrylhydrazyl DPPH radical at 0.5mg/ml relative to ascorbic acid (standard drug).

Keywords: acylpyrazolone, antibacterial studies, metal complexes, phenylhydrazone, spectroscopy

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Authors: Ceyda Dadali, Yeşim Elmaci

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Coffee was introduced as an economic crop during the fifteenth century; nowadays it is the most important food commodity ranking second after crude oil. Desirable sensory properties make coffee one of the most often consumed and most popular beverages in the world. The coffee preparation method has a significant effect on flavor and composition of coffee brews. Three different extraction methodologies namely decoction, infusion and pressure methods have been used for coffee brew preparation. Each of these methods is related to specific granulation (coffee grind) of coffee powder, water-coffee ratio temperature and brewing time. Coffee is a mixture of 1500 chemical compounds. Chemical composition of coffee highly depends on brewing methods, coffee bean species and roasting time-temperature. Coffee contains a wide number of very important bioactive compounds, such as diterpenes: cafestol and kahweol, alkaloids: caffeine, theobromine and trigonelline, melanoidins, phenolic compounds. The phenolic compounds of coffee include chlorogenic acids (quinyl esters of hidroxycinnamic acids), caffeic, ferulic, p-coumaric acid. In coffee caffeoylquinic acids, feruloylquinic acids and di-caffeoylquinic acids are three main groups of chlorogenic acids constitues 6% -10% of dry weight of coffee. The bioavailability of chlorogenic acids in coffee depends on the absorption and metabolization to biomarkers in individuals. Also, the interaction of coffee polyphenols with other compounds such as dietary proteins affects the biomarkers. Since bioactive composition of coffee depends on brewing methods effect of coffee brewing method on bioactive compounds of coffee will be discussed in this study.

Keywords: bioactive compounds of coffee, biomarkers, coffee brew, effect of brewing

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Authors: Kirstin Burger, Paul Watts, Nicole Vorster

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Green chemistry focuses on synthesis which has a low negative impact on the environment. This research focuses on synthesizing novel compounds from an all-natural Eucalyptus citriodora oil. Eight novel plasticizer compounds are synthesized and optimized using flow chemistry technology. A precursor to one novel compound can be synthesized from the lauric acid present in coconut oil. Key parameters, such as catalyst screening and loading, reaction time, temperature, residence time using flow chemistry techniques is investigated. The compounds are characterised using GC-MS, FT-IR, 1H and 13C-NMR techniques, X-ray crystallography. The efficiency of the compounds is compared to two commercial plasticizers, i.e. Dibutyl phthalate and Eastman 168. Several PVC-plasticized film formulations are produced using the bio-based novel compounds. Tensile strength, stress at fracture and percentage elongation are tested. The property of having increasing plasticizer percentage in the film formulations is investigated, ranging from 3, 6, 9 and 12%. The diastereoisomers of each compound are separated and formulated into PVC films, and differences in tensile strength are measured. Leaching tests, flexibility, and change in glass transition temperatures for PVC-plasticized films is recorded. Research objective includes using these novel compounds as a green bio-plasticizer alternative in plastic products for infants. The inhibitory effect of the compounds on six pathogens effecting infants are studied, namely; Escherichia coli, Staphylococcus aureus, Shigella sonnei, Pseudomonas putida, Salmonella choleraesuis and Klebsiella oxytoca.

Keywords: bio-based compounds, plasticizer, tensile strength, microbiological inhibition , synthesis

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Authors: Endang Purwati, Ely Vebriyanti, R. Puji Hartini, Hendri Purwanto

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This study aimed to determine the effect of addition cinnamon extract (Cinnamomum burmannii) in making goat milk yogurt product isolates dadih (Pediococcus pentosaceus) to antioxidant activity and cholesterol levels. The method of research was the experimental method by using a Randomized Block Design (RBD), which consists of 5 treatments with 4 groups as replication. Treatment in this study was used of cinnamon extract as A (0%), B (1%), C (2%), D (3%), E (4%) in a goat’s milk yoghurt. This study was used 4200 ml of Peranakan Etawa goat’s milk and 80 ml of cinnamon extract. The variable analyzed were water content, pH value, total lactic acid bacterial colonies, antioxidant activity and cholesterol levels. The average water content ranged from 81.2-85.56%. Mean pH values rang between 4.74–4.30. Mean total lactic acid bacteria colonies ranged from 3.87 x 10⁸ - 7.95 x 10⁸ CFU/ml. The average of the antioxidant activity ranged between 10.98%-27.88%. Average of cholesterol levels ranged from 14.0 mg/ml–17.5 mg/ml. The results showed that the addition of cinnamon extract in making goat milk yoghurt product isolates dadih (Pediococcus pentosaceus) significantly different (P < 0.05) to water content, pH value, total lactic acid bacterial colonies, antioxidant activity and cholesterol levels. In conclusion, the study shows that using of cinnamon extract 4% is the best in making goat milk yoghurt.

Keywords: antioxidant, cholesterol, cinnamon, Pediococcus pentosaceus, yoghurt

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Authors: L. Mallesha, P. Mallu, B. Veeresh

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In the present study, 2, 6-diflurobenzohydrazide and 4-fluorophenylisothiocyanate were used as the starting materials to synthesize 5-phenyl-N3-(4-fluorophenyl)-4H-1, 2, 4-triazole-3, 4-diamine. Further, compound 5-phenyl-N3-(4-fluorophenyl)-4H-1, 2, 4-triazole-3,4-diamine reacted with fluoro substituted benzaldehydes to yield a series of Schiff bases. All the final compounds were characterized using IR, 1H NMR, 13C NMR, MS and elemental analyses. New compounds were evaluated for their antiproliferative effect using the MTT assay method against four human cancer cell lines (K562, COLO-205, MDA-MB231, and IMR-32) for the time period of 24 h. Among the series, few compounds showed good activity on all cell lines, whereas the other compounds in the series exhibited moderate activity.

Keywords: Schiff bases, MTT assay, antiproliferative activity, human cancer cell lines, 1, 2, 4-triazoles

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Authors: Majid Farsadrooh, Mehran Feizi-Dehnayebi

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Serum albumin is the most abundant protein that is present in the circulatory system of a wide variety of organisms. Although it is a significant macromolecule, it can contribute to osmotic blood pressure and also, plays a superior role in drug disposition and efficiency. Molecular docking simulation can improve in silico drug design and discovery procedures to propound a lead compound and develop it from the discovery step to the clinic. In this study, the molecular docking simulation was applied to select a lead molecule through an investigation of the interaction of the two anticancer drugs (Alitretinoin and Abemaciclib) with Human Serum Albumin (HSA). Then, a series of new compounds (a-e) were suggested using lead molecule modification. Density functional theory (DFT) including MEP map and HOMO-LUMO analysis were used for the newly proposed compounds to predict the reactivity zones on the molecules, stability, and chemical reactivity. DFT calculation illustrated that these new compounds were stable. The estimated binding free energy (ΔG) values for a-e compounds were obtained as -5.78, -5.81, -5.95, -5,98, and -6.11 kcal/mol, respectively. Finally, the pharmaceutical properties and toxicity of these new compounds were estimated through OSIRIS DataWarrior software. The results indicated no risk of tumorigenic, irritant, or reproductive effects and mutagenicity for compounds d and e. As a result, compounds d and e, could be selected for further study as potential therapeutic candidates. Moreover, employing molecular docking simulation with the prediction of pharmaceutical properties helps to discover new potential drug compounds.

Keywords: drug design, anticancer, computational studies, DFT analysis

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Authors: Hamdi Belfeki, Belgacem Chandoul, Mnasser Hassouna, Mondher Mejri

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Aqueous and ethanolic extracts of eight Tunisian aromatic and medicinal plants (TAMP) were characterized by studying their composition in polyphenols and also their antiradical and antioxidant capacities. In absence and in the presence of the various extracts, α-amylase from Bacillus subtlis activity, was measured in order to detect a potential inhibition. The total contents of polyphenols and flavonoid vary in function of TAMP and the mobile phase used for the extraction (distilled water or ethanol). The ethanolic extracts showed the most significant antiradical and antioxidant activities. Only the extracts from Coriandrum sativum showed a significant inhibiting effect on the α-amylase activity. This inhibiting capacity could be correlated with the chemical profile of the two extracts, due to the fact that they have the greatest amount of total flavonoid. The ethanolic extract has the most important antioxidant and anti-radicalizing activities among the sixteen extracts studied. The inhibition kinetics of the two coriander extracts were evaluated by pre-incubation method, using Lineweaver-Burk’s equation, obtained by linearization of Michaeilis-Menten’s expression. The results showed that both extracts exercised a competitive inhibition mechanism.

Keywords: α-amylase, antioxidant activity, aromatic and medicinal plants, inhibition

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Authors: M. S. M. Yusof, R. Ramli, S. K. C. Soh, N. Ismail, N. Ngah

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This study presents the synthesis of a series of methoxybenzoylthiourea amino acid derivatives. The compounds were obtained from the reactions between 2/3/4-methoxybenzoyl isothiocyanate with threonine. All of the compounds were characterized via mass spectrometry, ¹H and ¹³C NMR spectrometry, UV-Vis spectrophotometer and FT-IR spectroscopy. Mass spectra for all of the compounds showed the presence of molecular ion [M]⁺ peaks at m/z 312, which are in agreement to the calculated molecular weight. For ¹H NMR spectra, the presence of OCH₃, C=S-NH and C=O-NH protons were observed within range of δ_H 3.8-4.0 ppm, 11.1-11.5 ppm and 10.0-11.5 ppm, respectively. ¹³C NMR spectra in all compounds displayed the presence of OCH₃, C=O-NH, C=O-OH and C=S carbon resonances within range of δ_C 55.0-57.0 ppm, 165.0-168.0 ppm, 170.0-171.0 ppm and 180.0-182.0 ppm, respectively. In UV spectra, two absorption bands have been observed and both were assigned to the n-π* and π-π* transitions. Six vibrational modes of v(N-H), v(O-H), v(C=O-OH), v(C=O-NH), v(C=C) aromatic and v(C=S) appeared in the FT-IR spectra within the range of 3241-3467 cm^-1, 2976-3302 cm^-1, 1720-1768 cm^-1, 1655-1672 cm^-1, 1519-1525 cm^-1 and 754-763 cm^-1, respectively. The antibacterial activity for all of the compounds was screened against Staphylococcus aureus, Staphylococcus epidermidis, Salmonella typhimurium and Escherichia coli. However, no activity was observed.

Keywords: methoxybenzoyl isothiocyanate, amino acid, threonine, antibacterial

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Authors: Stephen Adeniyi Adefegha, Vitor Mostardeiro, Vera Maria Morsch, Ademir F. Morel, Ivana Beatrice Manica Da Cruz, Sabrina Somacal Maria Rosa Chitolina Schetinger

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Moringa stenopetala is often consumed as food and used in folkloric medicine for the management of several diseases. Purpose: This study was set up in order to assess the effect of aqueous extract of Moringa stenopetala on cell viability and oxidative stress biomarkers in BV-2 microglial cells. Aqueous extracts of M. stenopetala were prepared, lyophilized and reconstituted in 0.5% dimethylsulphoxide (DMSO). Cells were treated with M. stenopetala extracts (0.1 - 100 µg/ml) for cell viability and nitric oxide (NO) production tests. However, M. stenopetala extract (50 µg/ml) was used in the treatment of cells for the determination of protein carbonyl content and reactive oxygen species (ROS) level. Incubation of BV-2 microglia cell with M. stenopetala extract maintained cell viability, diminished NO and ROS levels, and reduced protein carbonyl contents Chlorogenic acid, rutin, kaempferol and quercetin derivatives were the main phenolic compounds identified in M. stenopetala leaf extract. These phenolic compounds present in M. stenopetala may be responsible for the mitigation of oxidative stress in BV-2 microglial cells.

Keywords: oxidative stress, BV-2 microglial cell, Moringa stenopetala, cell viability, antioxidant

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Authors: M. Ebrahimi, E. Maroufyan, M. Shakeri, E. Oskoueian, A. F Soleimani, Y. M. Goh

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Lipid peroxidation is a main reason of low quality in meat and meat products. The free radical chain reaction is the major process of lipid peroxidation and reactive oxygen species (ROS) such as hydroxyl radical and hydroperoxyl radical are the main starter of the chain reaction. Papaya leaf contains several secondary metabolites which can be used as a potential antioxidant in broiler feed. Hence, this research was carried out to evaluate the potential of papaya leaf to prevent lipid peroxidation and enhance the antioxidant activity of breast meat of broiler chicken. The results showed that supplementation of papaya leaf at 5%, significantly (p < 0.05) reduced the lipid peroxidation compared to control group. The supplementation of papaya leaf prevented from lipid peroxidation and enhanced the antioxidant activity of the broiler breast meat significantly (p < 0.05) after different storage periods. Papaya leaf reduced the lipid oxidation of meat during storage with strong free radical-scavenging ability. In conclusion, supplementation of papaya leaf in broiler diet to have high quality meat is recommended.

Keywords: antioxidant activity, papaya leaf, breast meat, lipid peroxidation

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Authors: Peramachi Sathiyamoorthy, Jacop Gopas, Avi Golan Goldhirsh

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Corchorus olitorius is a leafy vegetable and an industrial crop. The herb has antioxidant, anti inflammatory, and anti-cancer properties. To assay the pharmaceutical properties, aqueous extracts of leaves and seeds from C. olitorius were tested against drug resistant melanoma cell line. The test showed LC50 of the extract was 0.08µg/ml. Aqueous seed extract exhibited higher melanoma inhibiting activity than leaf extract. Dialysis of seed extract showed that the active compound is less than 12 KDa. The compound with <3 KDa MW separated by microconcentration of seed extract showed 70.5 % inhibition of melanoma cell growth. Among the two fractions obtained by Gel filtration with G10 column, the first fraction at 1:2000 dilutions exhibited 100% inhibition of melanoma growth. The compound with Rf value 0.86 (MA4) isolated by TLC separation showed about 98% cytotoxicity against melanoma at 1: 1000 dilutions. Furthermore, HPLC separation of MA4 compound with Superdex 75 column resulted in 4 compounds. Out of 4, one compound showed melanoma inhibition. The active compound is identified by reagent methods as Strophanthidin. Further toxicological and clinical studies will lead to the development of a potential drug to treat drug resistant melanoma.

Keywords: corchorus olitorius, melanoma, drug development, strophanthidin

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Authors: Daniel Assefa, Engeda Dessalegn, Chetan Chauhan

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Moringa stenopetala is a socioeconomic valued tree that is widely available and cultivated in the Southern part of Ethiopia. The leaves have been traditionally used as a food source with high nutritional and medicinal values. The present work was carried out to evaluate the effect of thermal treatment on the total phenolic content, antioxidant and alpha-amylase inhibition activities of aqueous leaf extracts during maceration and different decoction time interval (5, 10 and 15 min). The total phenolic content was determined by the Folin-ciocalteu methods whereas antioxidant activities were determined by 2,2-diphenyl-1-picryl-hydrazyl(DPPH) radical scavenging, reducing power and ferrous ion chelating assays and alpha-amylase inhibition activity was determined using 3,5-dinitrosalicylic acid method. Total phenolic content ranged from 34.35 to 39.47 mgGAE/g. Decoction for 10 min extract showed ferrous ion chelating (92.52), DPPH radical scavenging (91.52%), alpha-amylase inhibition (69.06%) and ferric reducing power (0.765), respectively. DPPH, reducing power and alpha-amylase inhibition activities showed positive linear correlation (R2=0.853, R2= 0.857 and R2=0.930), respectively with total phenolic content but ferrous ion chelating activity was found to be weakly correlated (R2=0.481). Based on the present investigation, it could be concluded that major loss of total phenolic content, antioxidant and alpha-amylase inhibition activities of the crude leaf extracts of Moringa stenopetala leaves were observed at decoction time for 15 min. Therefore, to maintain the total phenolic content, antioxidant, and alpha-amylase inhibition activities of leaves, cooking practice should be at the optimum decoction time (5-10 min).

Keywords: alpha-amylase inhibition, antioxidant, Moringa stenopetala, total phenolic content

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Authors: Marcela Dvorakova, Lenka Langhansova, Premysl Landa

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A series of quinazoline derivatives bearing aromatic rings in 2- and 4-positions were prepared and tested for their biological activity. Firstly, the compounds were evaluated for their potential to inhibit various kinases, such as autophagy activating kinase ULK1, 3-Phosphoinositide-dependent kinase 1, and TANK-binding kinase 1. None of the compounds displayed any activity on these kinases. Secondly, the compounds were tested for their anti-inflammatory activity expressed as cyclooxygenase (COX) isoforms and 5-lipoxygenase (5-LOX) inhibition. Three of the compounds showed significant selectivity towards COX-1 isoform (COX-2/COX-1 SI = 20-30). They inhibited COX-1 in a single-digit µM range. There was also one compound that exhibited inhibitory activity towards all three tested enzymes in µM range (IC50COX-1 = 1.9 µM; IC50COX-2 and 5-LOX = 10.1µM. COX-1 inhibition was until recently considered undesirable due to COX-1 constitutive expression in most cell types and tissues. Thus, there are not many compounds known with selective COX-1 activity. However, it is now believed that COX-1 plays an important role in the pathophysiology of several acute and chronic disorders, including cancer or neurodegenerative diseases. Thus, the discovery of effective COX-1 selective inhibitors is desirable and important.

Keywords: cyclooxygenases, kinases, lipoxygenases, quinazolines

Procedia PDF Downloads 113

Authors: Niki Mougiou, Spyros Didos, Ioanna Bouzouka, Athina Theodorakopoulou, Michael Kornaros, Anagnostis Argiriou

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Grains from traditional old Greek cereal varieties were evaluated and compared to commercial cultivars, like Simeto and Mexicali 81, in an effort to valorize local products and assess the nutritional benefits of ancient grains. The samples studied in this research included common wheat, durum wheat, emmer (Triticum dicoccum) and einkorn (Triticum monococcum), as well as barley, oats and rye grains. The Internal Transcribed Spacer 2 (ITS2) nuclear region was amplified and sequenced as a barcode for species identification, allowing the verification of the label of each product. After that, the total content of bound and free polyphenols and flavonoids, as well as the antioxidant activity of bound and free compounds, was measured by classic colorimetric assays using Folin- Ciocalteu, AlCl₃ and DPPH‧ (2,2-diphenyl-1-picrylhydrazyl) reagents, respectively. Moreover, the level of variation of fatty acids was determined in all samples by gas chromatography. The results showed that local old landraces of emmer and einkorn had the highest polyphenol content, 2.4 and 3.3 times higher than the average value of 5 durum wheat samples, respectively. Regarding the total flavonoid content, einkorn had 2.6-fold and emmer 2-fold higher values than common wheat. The antioxidant activity of free or bound compounds was at the same level, at about 20-30% higher in both einkorn and emmer compared to common wheat. Five main fatty acids were detected in all samples, in order of decreasing amounts: linoleic (C18:2) > palmitic (C16:0) ≈ , oleic (C18:1) > eicosenoic (C20:1, cis-11) > stearic (C18:0). Emmer and einkorn showed a higher diversity of fatty acids and a higher content of mono-unsaturated fatty acids compared to common wheat. The results of this study demonstrate the high nutritional value of old local landraces that have been put aside by more productive, yet with lower qualitative characteristics, commercial cultivars, underlining the importance of maintaining sustainable agricultural practices to ensure their continued cultivation.

Keywords: biochemical analysis, nutritional value, plant barcoding, wheat

Procedia PDF Downloads 67

Authors: Abdel Rahman Altakhaineh, Mohamma Alaghawat, Hiba Alhendi

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This paper reports an investigation of the comprehension of English compound nouns by sixty Arabic-speaking English Foreign Language (EFL) learners majoring in English at the University of Jordan, Amman. The investigation focused on the problems that these learners may encounter in understanding certain types of compounds and their ability to use their L1 compound noun knowledge to produce the meaning of L2 compound nouns. Participants whose English proficiency level was advanced underwent a test to identify the meaning ofan underlined compound without using a dictionary. Theresponses to the three different types of compounds were analyzed usingTwo-Way repeated measures ANOVA, and the results showed that there were different endocentric and exocentric compound responses within subordinative compounds, with a statistically significant difference between the two in favor of endocentric compounds. We argue that the endocentric, especially subordinative endocentric compounds,weremore easily understood due to its representative nature, i.e., because the head represents the meaning of the whole compound. The study concludes with pedagogical implications for teaching compound nouns.

Keywords: morphology, compounding, SLA, arabic-speaking EFL learners

Procedia PDF Downloads 85