Search results for: selective inhibition of Cdk5/p25

Authors: Muskan Jain, Baiju Gopal

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Objectives: Intimacy in interpersonal relationships is integral to psychological health and everyday wellbeing; the focus is on intimacy, which can be described as feelings of closeness, connection, and belonging within relationships, which is influenced by an individual's gender identity as well as life experiences. The study aims to explore the experiences of intimacy of the non-binary gender; this marginalized community has increased risks of developing the imposter phenomenon. The study explores the influence of IP on the development and sustenance of intimacy in relationships. Methods: The present study accumulates detailed narratives from 10 non-binary young adults ages 18 to 25 in metropolitan cities of India. Thematic analysis was used for the data analysis. Results: Seven major themes have emerged revolving around internalized criticism and self-depreciating behavior, which causes distance between partners. The four themes that result in the internalization of criticism are lack of social stability, invalidation by social units, adverse life experiences, and estrangement due to gender identity. Three themes that encapsulate major difficulties in relationships are limited self-disclosure, inhibition of physical needs, and fear of taking space. The findings have been critically compared and contrasted with the existing body of literature in the domain, which sets the agenda for further inquiry. Conclusion: It is important for future studies to capture the experiences of non-binary genders in India to provide better therapeutic support in order to assist them in forming meaningful and authentic relationships, thus increasing overall wellbeing.

Keywords: imposter phenomenon, intimacy, internalized criticism, marginalized community

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Authors: Salwa M. Elmesallamy, Ahmed A. Farag, Magd M. Badr, Dalia S. Fathy, Ahmed Bakry, Mona A. El-Etre

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The term green environment is an international trend. It is become imperative to treat the corrosion of steel with a green coating to protect the environment. From the potential adverse effects of the traditional materials.A series of polybenzoxazine/henna composites (PBZ/henna), with different weight percent (3,5, and 7 wt % (of henna), were prepared for corrosion protection of carbon steel. The structures of the prepared composites were verified using FTIR analysis. The mechanical properties of the resins, such as adhesion, hardness, binding, and tensile strength, were also measured. It was found that the tensile strength increases by henna loading up to 25% higher than the tidy resin. The thermal stability was investigated by thermogravimetric analysis (TGA) the loading of lawsone (henna) molecules into the PBZ matrix increases the thermal stability of the composite. UV stability was tested by the UV weathering accelerator to examine the possibility that henna can also act as an aging UV stabilizer. The effect of henna content on the corrosion resistance of composite coatings was tested using potentiostatic polarization and electrochemical spectroscopy. The presence of henna in the coating matrix enhances the protection efficiency of polybenzoxazine coats. Increasing henna concentration increases the protection efficiency of composites. The quantum chemical calculations for polybenzoxazine/henna composites have resulted that the highest corrosion inhibition efficiency, has the highest EHOMO and lowest ELUMO; which is in good agreement with results obtained from experiments.

Keywords: polybenzoxazine, corrosion, green chemistry, carbon steel

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Authors: Wei-Chia Huang, Jane Wang

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Damage to nerves is considered one of the most irreversible injuries. The regeneration of nerves has always been an important topic in regenerative medicine. In general, damage to human tissue will naturally repair overtime. However, when the nerves are damaged, healed flesh wound cannot guarantee full restoration to its original function, as truncated nerves are often irreversible. Therefore, the development of treatment methods to successfully guide and accelerate the regeneration of nerves has been highly sought after. In order to induce nerve tissue growth, nerve conduits are commonly used to help reconnect broken nerve bundles to provide protection to the location of the fracture while guiding the growth of the nerve bundles. To prevent the protected tissue from becoming necrotic and to ensure the growth rate, the conduits used are often modified with microstructures or blended with neuron growth factors that may facilitate nerve regeneration. Electrical stimulation is another attempted treatment for medical rehabilitation. With appropriate range of voltages and stimulation frequencies, it has been demonstrated to promote cell proliferation and migration. Biodegradability are critical for medical devices like nerve conduits, while conductive polymers pose great potential toward the differentiation and growth of nerve cells. In this work, biodegradability and conductivity were combined into a novel biodegradable, photocurable, conductive polymer composite materials by embedding conductive nanoparticles in poly(glycerol sebacate) acrylate (PGSA) and 3D-printed into nerve conduits. Rat pheochromocytoma cells and rat neuronal Schwann cells were chosen for the in vitro tests of the conduits and had demonstrate selective growth upon culture in the conductive conduits with built-in microchannels and electrical stimulation.

Keywords: biodegradable polymer, 3d printing, neural regeneration, electrical stimulation

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Authors: Z. Jamalzadeh, A. Niaei, H. Erfannia

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Due to developing industries, the emission of pollutants such as NOx, SOx, and CO2 are rapidly increased. Generally, NOx is attributed to the mono nitrogen oxides of NO and NO2 that is one of the most important atmospheric contaminants. Hence, controlling the emission of nitrogen oxides is environmentally urgent. Selective catalytic reduction of NOx is one of the most common techniques for NOx removal in which zeolites have wide application due to their high performance. In zeolitic processes, the catalytic reaction occurs mostly in the pores. Therefore, investigation of the adsorption phenomena of the molecules in order to gain an insight and understand the catalytic cycle is of important. Hence, in current study, benefiting from molecular simulations, the adsorption phenomena in the nanocatalysts of SCR of NOx process was investigated in order to get a good insight of the catalysts’ behavior. The effect of cation addition to the support in the catalysts’ behavior through adsorption step was explored by Mont Carlo (MC) using Materials Studio Package. Simulation time of 1 Ns accompanying 1 fs time step, COMPASS27 Force Field and the cut off radios of 12.5 Ȧ was applied for performed runs. It was observed that the adsorption capacity increases in the presence of cations. The sorption isotherms demonstrated the behavior of type I isotherm categories and sorption capacity diminished with increase in temperature whereas an increase was observed at high pressures. Besides, NO sorption showed higher sorption capacity than NH3 in H–ZSM5. In this respect, the energy distributions signified that the molecules could adsorb in just one sorption site at the catalyst and the sorption energy of NO was stronger than the NH3 in H-ZSM5. Furthermore, the isosteric heat of sorption data showed nearly same values for the molecules; however, it indicated stronger interactions of NO molecules with H-ZSM5 zeolite compared to the isosteric heat of NH3 which was low in value.

Keywords: Monte Carlo simulation, adsorption, NOx, ZSM5

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Authors: Linda Chularojmontri, Seewaboon Sireeratawong, Suvara Wattanapitayakul

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Terminalia arjuna Roxb. (family Combretaceae) is commonly known as ‘Sa maw thet’ in Thai. The fruit is used in traditional medicine as natural mild laxatives, carminative and expectorant. Aim of the study: This research aims to study the anti-inflammatory, analgesic and antipyretic activities of Terminalia arjuna extract by using animal models in comparison to the reference drugs. Materials and Methods: The anti-inflammatory study was conducted by two experimental animal models namely ethyl phenylpropionate (EPP)-induced ear edema and carrageenan-induced paw edema. The study of analgesic activity used two methods of pain induction including acetic acid and heat-induced pain. In addition, the antipyretic activity study was performed by induced hyperthermia with yeast. Results: The results showed that the oral administration of Terminalia arjuna extract possessed acute anti-inflammatory effect in carrageenan-induced paw edema. Terminalia arjuna extract showed the analgesic activity in acetic acid-induced writhing response and heat-induced pain. This indicates its peripheral effect by inhibiting the biosynthesis and/or release of some pain mediators and some mechanism through Central nervous system. Moreover, Terminalia arjuna extract at the dose of 1000 and 1500 mg/kg body weight showed the antipyretic activity, which might be because of the inhibition of prostaglandins. Conclusion: The findings of this study indicated that the Terminalia arjuna extract possesses the anti-inflammatory, analgesic and antipyretic activities in animals.

Keywords: analgesic activity, anti-inflammatory activity, antipyretic activity, Terminalia arjuna extract

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Authors: Kenia Martínez, Geniel Talavera, Juan Alonso

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Moringa oleifera is a plant containing many nutrients that are mostly concentrated within the leaves. Commonly, the separation process of these nutrients involves solid-liquid extraction followed by evaporation and drying to obtain a concentrated extract, which is rich in proteins, vitamins, carbohydrates, and other essential nutrients that can be used in the food industry. In this work, three drying methods were used, which involved very different temperature and pressure conditions, to evaluate the effect of each method on the vitamin C content and the antioxidant efficiency of the extracts. Solid-liquid extractions of Moringa leaf (LE) were carried out by employing an ethanol solution (35% v/v) at 50 °C for 2 hours. The resulting extracts were then dried i) in a convective oven (CO) at 100 °C and at an atmospheric pressure of 750 mbar for 8 hours, ii) in a vacuum evaporator (VE) at 50 °C and at 300 mbar for 2 hours, and iii) in a freeze-drier (FD) at -40 °C and at 0.050 mbar for 36 hours. The antioxidant capacity (EC₅₀, mg solids/g DPPH) of the dry solids was calculated by the free radical inhibition method employing DPPH˙ at 517 nm, resulting in a value of 2902.5 ± 14.8 for LE, 3433.1 ± 85.2 for FD, 3980.1 ± 37.2 for VE, and 8123.5 ± 263.3 for CO. The calculated antioxidant efficiency (AE, g DPPH/(mg solids·min)) was 2.920 × 10^-5 for LE, 2.884 × 10^-5 for FD, 2.512 × 10^-5 for VE, and 1.009 × 10^-5 for CO. Further, the content of vitamin C (mg/L) determined by HPLC was 59.0 ± 0.3 for LE, 49.7 ± 0.6 for FD, 45.0 ± 0.4 for VE, and 23.6 ± 0.7 for CO. The results indicate that the convective drying preserves vitamin C and antioxidant efficiency to 40% and 34% of the initial value, respectively, while vacuum drying to 76% and 86%, and freeze-drying to 84% and 98%, respectively.

Keywords: antioxidant efficiency, convective drying, freeze-drying, Moringa oleifera, vacuum drying, vitamin C content

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Authors: Lila Boulekbache-Makhlouf, Fatiha Brahmi

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This study was carried out with the aim of enriching fresh cheese with the food by-products, which are the leaves of shallots and the peels of potatoes. Firstly, the conditions for extracting the total polyphenols using ultrasound are optimized. Then, the contents of total polyphenols PPT , flavonoids and antioxidant activity were evaluated for the extracts obtained by adopting the optimal parameter. On the other hand, we have carried out some physicochemical, microbiological and sensory analyzes of the cheese produced. The maximum total polyphenols value of 70.44 mg GAE gallic acid equivalent / g of dry matter DM of shallot leaves was reached with 40% (v/v) ethanol, an extraction time of 90 min and a temperature of 10 °C. While, the maximum TPP total polyphenols content of potato peels of 45.03 ± 4.16 mg gallic acid equivalent / g of dry matter DM was obtained using an ethanol /water mixture (40%, v/v), a time of 30 min and a temperature of 60 °C and the flavonoid contents were 13.99 and 7.52 QE quercetin equivalent/g dry matter DM, respectively. From the antioxidant tests, we deduced that the potato peels present a higher antioxidant power with the concentration of extracts causing a 50% inhibition IC50s of 125.42 ± 2.78 μg/mL for 2,2-diphényl 1-picrylhydrazyle DPPH, of 87.21 ± 7.72 μg/mL for phosphomolybdate and 200.77 ± 13.38 μg/mL for iron chelation, compared with the results obtained for shallot leaves which were 204.29 ± 0.09, 45.85 ± 3,46 and 1004.10 ± 145.73 μg/mL, respectively. The results of the physicochemical analyzes have shown that the formulated cheese was compliant with standards. Microbiological analyzes show that the hygienic quality of the cheese produced was satisfactory. According to the sensory analysis, the experts liked the cheese enriched with the powder and pieces of the leaves of the shallots.

Keywords: shallots leaves, potato peels, ultrasound extraction, phenolics, cheese

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Authors: Pratap Sing, Chaman. K. Jadon, H. P. Meena, D. L.yadav, S. L. Yadav, Uditi Dhakad

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The experiment was conducted at Agricultural Research Station, Agriculture University, Kota, Rajasthan, India during kharif and rabi 2020-21 and 2021-22 to study the biofficacy of diclosulam and its residual effect on succeeding wheat crop. The treatments comprised of Diclosulam 84 % WDG viz. 6.25, 12.50, 25.00 and 37.50 g/ha as pre emergence (PE), Pendimethalin 30% EC 3.33 l/ha, Sulfentrazon 48% SC 750 g/ha, hand weeding at 30 and 45 DAS and weedy check, were evaluated in randomized block design in three replications. The experimental soil was clay in texture and non-calcareous. Experimental field was mainly dominated by grasses-Echinochloa colonum, E.crusgalli,Cynodon dactylon, Sedges-Cyperus rotundus and broad leaved weeds Celosia argentea and Digera arvensis.The result revealed that application of Diclosulam 84 % WDG 25 g/ha PE was found effective in controlling mostly weed species and registered higher weed control efficiency 81.2, 74.3, 69.6 per cent at 30, 45 days after sowing and at harvest. Diclosulam 84 % WDG (6.25-25.0 g/ha) was found selective to the soybean crop as no any phytotoxicity symptoms were observed. Among the herbicidal treatments, Diclosulam 84 % WDG 25 g/ha registered maximum and significantly higher soybean seed yield (1889 and 1431 kg/ha during kharif 2020 and 2021, respectively and was at par with Sulfentrazone 48% SC 750 g/ha and over weedy check( 1027 and 667 kg/ha).The wheat crop growth, yield attributes and seed yield were not influenced due to carry over effect of the Diclosulam 84 % WDG( 6.25-25.0 g/ha) and no any phytotoxicity symptoms were observed. Henceforth, the Diclosulam 84 % WDG 25.0 g/ha as pre emergence may be used in the soybean for effective weed control without carry over effect on succeeding wheat crop.

Keywords: Diclosulam, soybean, carry over effect, succeeding wheat

Procedia PDF Downloads 93

Authors: A. Moawad, K. C. Yao, A. Mansour, R. Gautier

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The detecting of an occupied frequency band is a major issue in cognitive radio systems. The detection process becomes difficult if the signal occupying the band of interest has faded amplitude due to multipath effects. These effects make it hard for an occupying user to be detected. This work mitigates the missed-detection problem in the context of cognitive radio in frequency-selective fading channel by proposing blind channel estimation method that is based on scattering transform. By initially applying conventional energy detection, the missed-detection probability is evaluated, and if it is greater than or equal to 50%, channel estimation is applied on the received signal followed by channel equalization to reduce the channel effects. In the proposed channel estimator, we modify the Morlet wavelet by using its first derivative for better frequency resolution. A mathematical description of the modified function and its frequency resolution is formulated in this work. The improved frequency resolution is required to follow the spectral variation of the channel. The channel estimation error is evaluated in the mean-square sense for different channel settings, and energy detection is applied to the equalized received signal. The simulation results show improvement in reducing the missed-detection probability as compared to the detection based on principal component analysis. This improvement is achieved at the expense of increased estimator complexity, which depends on the number of wavelet filters as related to the channel taps. Also, the detection performance shows an improvement in detection probability for low signal-to-noise scenarios over principal component analysis- based energy detection.

Keywords: channel estimation, cognitive radio, scattering transform, spectrum sensing

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Authors: Chika C. Ogueke, Ijeoma M. Agunwah

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The antimicrobial activities and preservative potentials of crude extracts of Alstonia boonei stem bark and Euphorbia hirta leaves were studied. Soxhlet extraction and cold ethanol extraction methods were used for the extraction of the dried and ground plant samples. Well in agar diffusion method was used for the antimicrobial screening at different concentrations of 25mg/ml, 50mg/ml, 100mg/ml and 200mg/ml on E.coli and B.subtilis. The preservative effects of the extracts at 0.1%, 0.2% and 0.3% singly and in combination were determined in minced meat using E. coli and B. subtilis as test isolates. Phytochemical analysis was also conducted on the extracts using standard analytical methods. E.hirta cold and A.boonei cold extracts gave the highest zone of growth inhibition on E. coli and B.substilis with 20mm zone diameter at 200mg/ml concentration. Phytochemical analysis revealed the presence of alkaloids, flavonoids, tannins, saponins and cardiac glycosides. A.boonei at 0.1, 0.2 and 0.3% produced a log cycle reduction on the growth of E.coli. Mixture of A. boonei and E. hirta extracts (1:1) at 0.1% and 0.2% also produced a log cycle reduction on the growth of E.coli and B. subtilis, however the A. boonei extracts had more significant effect on the isolates. The observed antimicrobial activities are attributed to the phytochemicals identified in the extracts. The results reveal the potentials of plant extracts as natural antimicrobial preservatives in minced meat. Thus the crude extracts can act as inhibitors of bacteria in a food system. Upon further purification better results may be obtained.

Keywords: antimicrobial preservative, crude extracts, minced meat, test isolates

Procedia PDF Downloads 278

Authors: Camille Charlebois-Plante, Marie-Ève Bourassa, Gaelle Dumel, Meriem Sabir, Louis De Beaumont

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To the extent of our knowledge, there has been little interest in the chronic effects of mild traumatic brain injury (mTBI) on cognition during normal aging. This is rather surprising considering the impacts on daily and social functioning. In addition, sustaining a mTBI during late adulthood may increase the effect of normal biological aging in individuals who consider themselves normal and healthy. The objective of this study was to characterize the persistent neuropsychological repercussions of mTBI sustained during late adulthood, on average 12 months prior to testing. To this end, 35 mTBI patients and 42 controls between the ages of 50 and 69 completed an exhaustive neuropsychological assessment lasting three hours. All mTBI patients were asymptomatic and all participants had a score ≥ 27 at the MoCA. The evaluation consisted of 20 standardized neuropsychological tests measuring memory, attention, executive and language functions, as well as information processing speed. Performance on tests of visual (Brief Visuospatial Memory Test Revised) and verbal memory (Rey Auditory Verbal Learning Test and WMS-IV Logical Memory subtest), lexical access (Boston Naming Test) and response inhibition (Stroop) revealed to be significantly lower in the mTBI group. These findings suggest that a mTBI sustained during late adulthood induces lasting effects on cognitive function. Episodic memory and executive functions seem to be particularly vulnerable to enduring mTBI effects.

Keywords: cognitive function, late adulthood, mild traumatic brain injury, neuropsychology

Procedia PDF Downloads 163

Authors: Bercem Kiran-Yildirim, Volker Gaukel

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Ice recrystallization (IR) which occurs especially during frozen storage is an undesired process due to the possible influence on the quality of products. As a result of recrystallization, the total volume of ice remains constant, but the size, number, and shape of ice crystals change. For instance, as indicated in the literature, the size of ice crystals in ice cream increases due to recrystallization. This results in texture deterioration. Therefore, the inhibition of ice recrystallization is of great importance, not only for food industry but also for several other areas where sensitive products are stored frozen, like pharmaceutical products or organs and blood in medicine. Ice-binding proteins (IBPs) have the unique ability to inhibit ice growth and in consequence inhibit recrystallization. This effect is based on their ice binding affinity. In the presence of IBP in a solution, ice crystal growth is inhibited during temperature decrease until a certain temperature is reached. The melting during temperature increase is not influenced. The gap between melting and freezing points is known as thermal hysteresis (TH). In literature, the TH activity is usually investigated under laboratory conditions in IBP buffer solutions. In product applications (e.g., food) there are many other solutes present which may influence the TH activity. In this study, a subset of IBPs, so-called antifreeze proteins (AFPs), is used for the investigation of the influence of sucrose solution concentration on the TH activity. For the investigation, a polarization microscope (Nikon Eclipse LV100ND) equipped with a digital camera (Nikon DS-Ri1) and a cold stage (Linkam LTS420) was used. In a first step, the equipment was established and validated concerning the accuracy of TH measurements based on literature data.

Keywords: ice binding proteins, ice crystals, sucrose solution, thermal hysteresis

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Authors: Ga-Young Lee, Hyun-Man Kim

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The modulation of the cell-cell junction is critical in epithelial-mesenchymal transition during tumorigenesis. As RhoA activity is known to be up-regulated to dissociate cell-cell junction by contracting acto-myosin complex in various cancer cells, the present study investigated if RhoA activity was also associated with the disruption of the cell-cell junction of oral cancer cells. We studied SCC-25 cells which are established from oral squamous cell carcinoma if their E-cadherin junction (ECJ) was under control of RhoA. Interestingly, development of ECJ of SCC-25 cells depended on the amount of fibronectin (FN) coated on the culture dishes. Seeded cells promptly aggregated to develop ECJ on the substrates coated with a low amount of FN, whereas they were retarded in the development of ECJ on the substrates coated with a high amount of FN. However, it was an unexpected finding that total RhoA activity was lower in the dissociated cells on the substrates of high FN than in the aggregated cells on the substrates of low FN. Treating the dissociated cells on the substrates of high FN with LPA, a RhoA activator, promoted the development to ECJ. In contrast, treating the aggregated cells on the substrates of low FN with Clostridium botulinum C3, a toxin decreasing RhoA activity, dissociated cells concomitant with the disruption of ECJ. Genetical knockdown of RhoA expression by transfecting RhoA siRNA also down-regulated the development of ECJ in SCC-25 cells. Furthermore, PMA, an activator of protein kinase C (PKC), down-regulated the development of ECJ junction of SCC-25 cells on the substrates coated with low FN. In contrast, GO6976, a PKC inhibitor, up-regulated the development of ECJ of SCC-25 cells with the activation of RhoA on the substrates coated with high FN. In conclusion, in the present study, we demonstrated unexpected results that the activation of RhoA promotes the development of ECJ, whereas the inhibition of RhoA retards the development of ECJ in SCC-25 cells.

Keywords: E-cadherin junction, oral squamous cell carcinoma, PKC, RhoA, SCC-25

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Authors: Irma Gabriela Lopez-Moreno, Elva Perez-Luque, Herlinda Aguilar-Zavala

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Introduction: Type 2 Diabetes Mellitus (T2DM) is characterized by combination of insulin resistance and deterioration of insulin secretion. Sfrp5 is a protein that antagonizes Wnt5a proteins by preventing it from reaching its receptor and activating the Wnt/β-catenin signaling pathway, this pathway is one of the most important regulators of adipogenesis. Although metformin decreases glucose levels its mechanisms of action are not fully known but it has been implicated in the inhibition of the Wnt/β-catenin signaling pathway. Objective: The objective was evaluating the effects of metformin on serum levels of Sfrp5 in patients with T2DM treated and not treated with metformin. Methods: Two groups of patients were selected: one group of T2DM patients treated with metformin (n = 35) and another group of subjects with recent diagnosis of T2DM untreated (n = 35) with a mean age of 48 ± 9 years. In these subjects anthropometric measures were taken as weight, height, waist and hip circumference, were calculated the percentage of body fat, visceral fat and muscle mass. In addition, were measured glucose levels, lipid profile, adiponectin and Sfrp5. Results: Sfrp5 were higher in metformin-treated patients compared to the untreated group (19.9 vs 13.6 ng/mL p < 0.001), a negative correlation was found between Sfrp5 levels and total cholesterol levels (r= -0.25, p = 0.03) and percentage of visceral fat (r = -0.26, p = 0.03) and a positive correlation with HDL cholesterol levels (r = 0.31, p = 0.01) and adiponectin (r=0.65, p = < 0.001). Conclusions: The findings show that metformin consumption increased levels of Sfrp5, which may lead to a decrease in the activation of the WNT/β-catenin pathway impacting on adipogenesis.

Keywords: adiponectin, diabetes, metformin, Sfrp5

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Authors: Boris Ershov

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Depression is the most common mood disorder experienced by patients who have sustained a traumatic brain injury (TBI) and is associated with poorer cognitive functional outcomes. However, in some cases, similar cognitive impairments can also be observed in depression. There is not enough information about the features of the cognitive deficit in patients with TBI in relation to patients with depression. TBI patients without depressive symptoms (TBInD, n25), TBI patients with depressive symptoms (TBID, n31), and 28 patients with bipolar II disorder (BP) were included in the study. There were no significant differences in participants in respect to age, handedness and educational level. The patients clinical status was determined by using Montgomery–Asberg Depression Rating Scale (MADRS). All participants completed a cognitive battery (The Brief Assessment of Cognition in Affective Disorders (BAC-A)). Additionally, the Rey–Osterrieth Complex Figure (ROCF) was used to assess visuospatial construction abilities and visual memory, as well as planning and organizational skills. Compared to BP, TBInD and TBID showed a significant impairments in visuomotor abilities, verbal and visual memory. There were no significant differences between BP and TBID groups in working memory, speed of information processing, problem solving. Interference effect (cognitive inhibition) was significantly greater in TBInD and TBID compared to BP. Memory bias towards mood-related information in BP and TBID was greater in comparison with TBInD. These results suggest that depressive symptoms are associated with impairments some executive functions in combination at decrease of speed of information processing.

Keywords: bipolar II disorder, depression, neurocognitive deficits, traumatic brain injury

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Authors: Bienvenu Gael Fouda Mbanga

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This study reports a new approach of preparation of carbon nanoparticles coated cerium oxide nanorods (CNPs/CeONRs) nanocomposite and reusing the spent adsorbent of Cd2+- CNPs/CeONRs nanocomposite for latent fingerprint detection (LFP) after removing Cd2+ ions from aqueous solution. CNPs/CeONRs nanocomposite was prepared by using CNPs and CeONRs with adsorption processes. The prepared nanocomposite was then characterized by using UV-visible spectroscopy (UV-visible), Fourier transforms infrared spectroscopy (FTIR), X-ray diffraction pattern (XRD), scanning electron microscope (SEM), Transmission electron microscopy (TEM), Energy-dispersive X-ray spectroscopy (EDS), Zeta potential, X-ray photoelectron spectroscopy (XPS). The average size of the CNPs was 7.84nm. The synthesized CNPs/CeONRs nanocomposite has proven to be a good adsorbent for Cd2+ removal from water with optimum pH 8, dosage 0. 5 g / L. The results were best described by the Langmuir model, which indicated a linear fit (R2 = 0.8539-0.9969). The adsorption capacity of CNPs/CeONRs nanocomposite showed the best removal of Cd2+ ions with qm = (32.28-59.92 mg/g), when compared to previous reports. This adsorption followed pseudo-second order kinetics and intra particle diffusion processes. ∆G and ∆H values indicated spontaneity at high temperature (40oC) and the endothermic nature of the adsorption process. CNPs/CeONRs nanocomposite therefore showed potential as an effective adsorbent. Furthermore, the metal loaded on the adsorbent Cd2+- CNPs/CeONRs has proven to be sensitive and selective for LFP detection on various porous substrates. Hence Cd2+-CNPs/CeONRs nanocomposite can be reused as a good fingerprint labelling agent in LFP detection so as to avoid secondary environmental pollution by disposal of the spent adsorbent.

Keywords: Cd2+-CNPs/CeONRs nanocomposite, cadmium adsorption, isotherm, kinetics, thermodynamics, reusable for latent fingerprint detection

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Authors: Haile F. Darge, Hsieh C. Tsai

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The tumor microenvironment affects the therapeutic outcomes of cancer disease. In a malignant tumor, overexpression of vascular endothelial growth factor (VEGF) provokes the production of pathologic vascular networks. This results in a hostile tumor environment that hinders anti-cancer drug activities and profoundly fuels tumor progression. In this study, we develop a strategy of sequential sustain release of the anti-angiogenic drug: Bevacizumab(BVZ), and anti-cancer drug: Doxorubicin(DOX) which had a synergistic effect on cancer treatment. Poly (D, L-Lactide)- Poly (ethylene glycol) –Poly (D, L-Lactide) (PDLLA-PEG-PDLLA) thermo-sensitive hydrogel was used as a vehicle for local delivery of drugs in a single platform. The in vitro release profiles of the drugs were investigated and confirmed a relatively rapid release of BVZ (73.56 ± 1.39%) followed by Dox (61.21 ± 0.62%) for a prolonged period. The cytotoxicity test revealed that the copolymer exhibited negligible cytotoxicity up to 2.5 mg ml-1 concentration on HaCaT and HeLa cells. The in vivo study on Hela xenograft nude mice verified that hydrogel co-loaded with BVZ and DOX displayed the highest tumor suppression efficacy for up to 36 days with pronounce anti-angiogenic effect of BVZ and with no noticeable damage on vital organs. Therefore, localized co-delivery of anti-angiogenic drug and anti-cancer drugs by the hydrogel system may be a promising approach for enhanced chemotherapeutic efficacy in cancer treatment.

Keywords: anti-angiogenesis, chemotherapy, controlled release, thermo-sensitive hydrogel

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Authors: Austin Jiang, Richard M. Salmon, Nicholas W. Morrell, Wei Li

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BMP10 is highly expressed in the developing heart and plays essential roles in cardiogenesis. BMP10 deletion in mice results in embryonic lethality due to impaired cardiac development. In adults, BMP10 expression is restricted to the right atrium, though ventricular hypertrophy is accompanied by increased BMP10 expression in a rat hypertension model. However, reports of BMP10 activity in the circulation are inconclusive. In particular it is not known whether in vivo secreted BMP10 is active or whether additional factors are required to achieve its bioactivity. It has been shown that high-affinity binding of the BMP10 prodomain to the mature ligand inhibits BMP10 signaling activity in C2C12 cells, and it was proposed that prodomain-bound BMP10 (pBMP10) complex is latent. In this study, we demonstrated that the BMP10 prodomain did not inhibit BMP10 signaling activity in multiple endothelial cells, and that recombinant human pBMP10 complex, expressed in mammalian cells and purified under native conditions, was fully active. In addition, both BMP10 in human plasma and BMP10 secreted from the mouse right atrium were fully active. Finally, we confirmed that active BMP10 secreted from mouse right atrium was in the prodomain-bound form. Our data suggest that circulating BMP10 in adults is fully active and that the reported vascular quiescence function of BMP10 in vivo is due to the direct activity of pBMP10 and does not require an additional activation step. Moreover, being an active ligand, recombinant pBMP10 may have therapeutic potential as an endothelial-selective BMP ligand, in conditions characterized by loss of BMP9/10 signaling.

Keywords: bone morphogenetic protein 10 (BMP10), endothelial cell, signal transduction, transforming growth factor beta (TGF-B)

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Authors: Samira Rostom, Robert Symonds, Robin W. Hughes

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Hydrogen is considered as one of the most important clean and renewable energy carriers for a sustainable energy future. However, its efficient and cost-effective purification remains challenging. This paper presents the potential of using metal–organic frameworks (MOFs) in combination with pressure swing adsorption (PSA) technology for syngas based H2 purification. PSA process analysis is done considering high pressure and elevated temperature process conditions, it reduces the demand for off-gas recycle to the fuel reactor and simultaneously permits higher desorption pressure, thereby reducing the parasitic load on the hydrogen compressor. The elevated pressure and temperature adsorption we present here is beneficial to minimizing overall process heating and cooling demand compared to existing processes. Here, we report the comparative performance of zeolite-5A, Cu-BTC, and the mix of zeolite-5A/Cu-BTC for H2 purification from syngas typical of those exiting water-gas-shift reactors. The MOFs were synthesized hydrothermally and then mixed systematically at different weight ratios to find the optimum composition based on the adsorption performance. The formation of different compounds were characterized by XRD, N2 adsorption and desorption, SEM, FT-IR, TG, and water vapor adsorption technologies. Single-component adsorption isotherms of CO2, CO, CH4, N2, and H2 over single materials and composites were measured at elevated pressures and different temperatures to determine their equilibrium adsorption capacity. The examination of the stability and regeneration performance of metal–organic frameworks was carried out using a gravimetric system at temperature ranges of 25-150℃ for a pressure range of 0-30 bar. The studies of adsorption/desorption on the MOFs showed selective adsorption of CO2, CH4, CO, and N2 over H2. Overall, the findings of this study suggest that the Ni-MOF-74/Cu-BTC composites are promising candidates for industrial H2 purification processes.

Keywords: MOF, H2 purification, high T, PSA

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Authors: O. V. Vyazovska

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Behavioral efficiency is one of the main principles to be successful in nature. Accuracy of visual discrimination is determined by the attention, learning experience, and memory. In the experimental condition, pigeons’ responses to visual stimuli presented on the screen of the monitor are behaviorally manifested by pecking or not pecking the stimulus, by the number of pecking, reaction time, etc. The higher the probability of rewarding is, the more likely pigeons will respond to the stimulus. We trained 8 pigeons (Columba livia) on a stagewise go/no-go visual discrimination task.16 visual stimuli were created from all possible combinations of four binary dimensions: brightness (dark/bright), size (large/small), line orientation (vertical/horizontal), and shape (circle/square). In the first stage, we presented S+ and 4 S-stimuli: the first that differed in all 4-dimensional values from S+, the second with brightness dimension sharing with S+, the third sharing brightness and orientation with S+, the fourth sharing brightness, orientation and size. Then all 16 stimuli were added. Pigeons rejected correctly 6-8 of 11 new added S-stimuli at the beginning of the second stage. The results revealed that pigeons’ behavior at the beginning of the second stage was controlled by probabilities of rewarding for 4 dimensions learned in the first stage. More or fewer mistakes with dimension discrimination at the beginning of the second stage depended on the number S- stimuli sharing the dimension with S+ in the first stage. A significant inverse correlation between the number of S- stimuli sharing dimension values with S+ in the first stage and the dimensional learning rate at the beginning of the second stage was found. Pigeons were more confident in discrimination of shape and size dimensions. They made mistakes at the beginning of the second stage, which were not associated with these dimensions. Thus, the received results help elucidate the principles of dimensional stimulus control during learning compound multidimensional visual stimuli.

Keywords: visual go/no go discrimination, selective attention, dimensional stimulus control, pigeon

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Authors: Azza H. El-Medany, Hanan H. Hagar, Jamila H. El-Medany

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Ulcerative colitis (UC) is one of chronic inflammatory diseases primarily affecting colon with unknown etiology. Some researches papers mentioned the possibility of the use of drugs that affect the angiotensin II in reducing the complication of ulcerative colitis. The aim of the present study is to evaluate the potential protective and therapeutic effects of captopril and valsartan on ulcerative colitis induced experimentally in rats using acetic acid. The results were assessed by histological assessment of colonic tissues and measurement of malondialdehyde (MDA), tumor necrosis factor (TNF-α), transforming growth factor (TGF-1B), angiotensin converting enzyme (ACE), reduced glutathione (GSH) and platelet activating factor (PAF) levels in colonic tissues. Oral pre-treatment with captopril or valsartan in a dose of 30 mgkg-1 body weight for 2 weeks before induction of colitis (prophylactic groups) and continuously for 2 weeks after induction (therapeutic groups) significantly reduce MDA, TNF-α, PAF, TGF-1B and ACE levels in colonic tissues as compared to acetic acid control group. Also, a significant increase in GSH level was observed in colonic tissues. Captopril and valsartan attenuated the macroscopic and microscopic colonic damage induced by acetic acid. These results suggest that either captopril or valsartan may be effective as prophylactic or treatment of UC through inhibition of ACE and scavenging effect on oxygen-derived free radicals.

Keywords: captopril, valsartan, angiotensin converting enzyme, reduced glutathione, tumor necrosis factor

Procedia PDF Downloads 254

Authors: Hicham Amar, Mustapha El Ghorfi, Yassine Taha, Abdellatif Elghali, Rachid Hakkou, Mostafa Benzaazoua

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Phosphate mine waste rock (PMWR) generated during ore extraction is continuously increasing, resulting in a significant environmental footprint. The main objectives of this study consist of i) elaboration of the sampling strategy of PMWR piles, ii) a mineralogical and chemical characterization of PMWR piles, and iii) 3D block model creation to evaluate the potential valorization of the existing PMWR. Destructive drilling using reverse circulation from 13 drills was used to collect samples for chemical (X-ray fluorescence analysis) and mineralogical assays. The 3D block model was created based on the data set, including chemical data of the realized drills using Datamine RM software. The optical microscopy observations showed that the sandy phosphate from drills in the PMWR piles is characterized by the abundance of carbonate fluorapatite with the presence of calcite, dolomite, and quartz. The mean grade of composite samples was around 19.5±2.7% for P₂O₅. The mean grade of P₂O₅ exhibited an increasing tendency by depth profile from bottom to top of PMWR piles. 3D block model generated with chemical data confirmed the tendency of the mean grades’ variation and may allow a potential selective extraction according to %P₂O₅. The 3D block model of P₂O₅ grade is an efficient sampling approach that confirmed the variation of P₂O₅ grade. This integrated approach for PMWR management will be a helpful tool for decision-making to recover the residual phosphate, adopting the circular economy and sustainability in the phosphate mining industry.

Keywords: 3D modelling, reverse circulation drilling, circular economy, phosphate mine waste rock, sampling

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Authors: Violina R. Angelova

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Comparative research has been conducted to allow us to determine the content of macro and microelements in the vegetative and reproductive organs of grass pea and the quality of grass pea seeds, as well as to identify the possibility of grass pea growth on soils contaminated by heavy metals. The experiment was conducted on an agricultural field subjected to contamination from the Non-Ferrous-Metal Works (MFMW) near Plovdiv, Bulgaria. The experimental plots were situated at different distances of 0.5 km and 8 km, respectively, from the source of pollution. On reaching commercial ripeness the grass pea plants were gathered. The composition of the macro and microelements in plant materials (roots, stems, leaves, seeds), and the dry matter content, sugars, proteins, fats and ash contained in the grass pea seeds were determined. Translocation factors (TF) and bioaccumulation factor (BCF) were also determined. The quantitative measurements were carried out through inductively-coupled plasma (ICP). The grass pea plant can successfully be grown on soils contaminated by heavy metals. Soil pollution with heavy metals does not affect the quality of the grass pea seeds. The seeds of the grass pea contain significant amounts of nutrients (K, P, Cu, Fe Mn, Zn) and protein (23.18-29.54%). The distribution of heavy metals in the organs of the grass pea has a selective character, which reduces in the following order: leaves > roots > stems > seeds. BCF and TF values were greater than one suggesting efficient accumulation in the above ground parts of grass pea plant. Grass pea is a plant that is tolerant to heavy metals and can be referred to the accumulator plants. The results provide valuable information about the chemical and nutritional composition of the seeds of the grass pea grown on contaminated soils in Bulgaria. The high content of macro and microelements and the low concentrations of toxic elements in the grass pea grown in contaminated soil make it possible to use the seeds of the grass pea as animal feed.

Keywords: Lathyrus sativus L, macroelements, microelements, quality

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Authors: T. Scattolin, E. Cavarzerani, F. Visentin, F. Rizzolio

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Organopalladium compounds have recently attracted attention for their high stability even under physiological conditions and, above all, for their remarkable in vitro cytotoxicity towards cisplatin-resistant cell lines. Among the organopalladium derivatives, those bearing at least one N-heterocyclic carbene ligand (NHC) and the Pd(II)-η³-allyl fragment have exhibited IC₅₀ values in the micro and sub-micromolar range towards several cancer cell lines in vitro and in some cases selectivity towards cancerous vs. non-tumorigenic cells. Herein, a selection of allyl and indenyl palladates were synthesized using a solvent-free method consisting of grinding the corresponding palladium precursors with different saturated and unsaturated azolium salts. All compounds have been fully characterized by NMR, XRD and elemental analyses. The intramolecular H, Cl interaction has been elucidated and quantified using the Voronoi Deformation Density scheme. Most of the complexes showed excellent cytotoxicity towards ovarian cancer cell lines, with I₅₀ values comparable to or even lower than cisplatin. Interestingly, the potent anticancer activity was also confirmed in a high-serous ovarian cancer (HGSOC) patient-derived tumoroid, with a clear superiority of this class of compounds over classical platinum-based agents. Finally, preliminary enzyme inhibition studies of the synthesized palladate complexes against the model TrxR show that the compounds have high activity comparable to or even higher than auranofin and classical Au(I) NHC complexes. Based on such promising data, further in vitro and in vivo experiments and in-depth mechanistic studies are ongoing in our laboratories.

Keywords: anticancer activity, palladium complexes, organoids, indenyl and allyl ligands

Procedia PDF Downloads 83

Authors: O. U. Nwosu, C. O. Osuagwu, N. Nnawugwu, C. T. Amanze

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Phytoremediation is a green and sustainable approach to decontaminate and restore contaminated sites while maintaining the biological activity and physical structure of soils. A pot experiment was conducted for a period of 70 days to evaluate the remediation potentials of Vetiveira zizanioides, Heianthus annuus L., Zea mays, and Glycine max in concurrent removal of anthracene and Pb in co-contaminated soil. Sandy loam soils were polluted with Pb chloride salt and anthracene at three different levels (50mg/kg of Pb, 100mg/kg of Pb, and 100mg/kg of Pb+100mg/kg of anthracene) and laid out in a completely randomized design with three replicates. Shoot dry matter weight was significantly reduced (p≤0.05) in comparison to control treatments by 33%, 32%, 40%, and 6.7% when exposed to 100mg kg⁻¹ of Pb, respectively in G.max, H.annuus, Z.mays, and vetiver. There was 42%, 41%, 48%, and 7.1% growth inhibition of shoot dry matter weight of G.max, H.annuus, Z.mays, and vetiver relative to control treatments when 100 mg Pb kg⁻¹ was mixed with 100 mgkg⁻¹ anthracene. Root and shoot metal concentration in G.max, H.annuus, Z.mays, and vetiver increased with increasing concentration of Pb. Translocation factor (TF < 1) obtained for G.max, Z.mays, and vetiver suggests that these plant species predominantly retain Pb in the root portion, while the TF value (TF≥1) obtained for H.annuus suggests that it predominantly retains Pb in the shoot portion. The extractable anthracene decreased significantly (p ≤ 0.05) in soil planted with G.max, H.annuus, Z.mays, and vetiver, as well as in pots without plants. This accounted for 53% to 71% of anthracene dissipation in planted soil and 40% dissipation in unplanted soil. This result suggested that the plant species used are a promising candidate for phytoremediation.

Keywords: phytoremediation, heavy metals, polyaromatic hydrocarbon, co-contaminated soil

Procedia PDF Downloads 106

Authors: William L. Whitehouse, Louisa H. Y. Lo, Andrew B. Kinghorn, Simon C. C. Shiu, Julian. A. Tanner

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C-reactive protein (CRP) is an acute-phase reactant and sensitive indicator for sepsis and other life-threatening pathologies, including systemic inflammatory response syndrome (SIRS). Currently, clinical turn-around times for established CRP detection methods take between 30 minutes to hours or even days from centralized laboratories. Here, we report the development of an electrochemical biosensor using redox probe-tagged DNA aptamers functionalized onto cheap, commercially available screen-printed electrodes. Binding-induced conformational switching of the CRP-targeting aptamer induces a specific and selective signal-ON event, which enables single-step and reagentless detection of CRP in as little as 1 minute. The aptasensor dynamic range spans 5-1000nM (R=0.97) or 5-500nM (R=0.99) in 50% diluted human serum, with a LOD of 3nM, corresponding to 2-orders of magnitude sensitivity under the clinically relevant cut-off for CRP. The sensor is stable for up to one week and can be reused numerous times, as judged from repeated real-time dosing and dose-response assays. By decoupling binding events from the signal induction mechanism, structure-switching electrochemical aptamer-based sensors (SS-EABs) provide considerable advantages over their adsorption-based counterparts. Our work expands on the retinue of such sensors reported in the literature and is the first instance of an SS-EAB for reagentless CRP detection. We hope this study can inspire further investigations into the suitability of SS-EABs for diagnostics, which will aid translational R&D toward fully realized devices aimed at point-of-care applications or for use more broadly by the public.

Keywords: structure-switching, C-reactive protein, electrochemical, biosensor, aptasensor.

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Authors: Seyedamirreza Shamsdini, Mohsen Mohammadi

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In this research, 18Ni-300 maraging steel powder particles are investigated by studying particle size distribution along with their morphology and grain structure. The powder analysis shows mostly spherical morphologies with cellular structures. A laser-based additive manufacturing process, selective laser melting (SLM) is used to produce samples for further investigation of mechanical properties and microstructure. Several uniaxial tensile tests are performed on the as-built parts to evaluate the mechanical properties. The macroscopic properties, as well as microscopic studies, are then investigated on the printed parts. Hardness measurements, as well as porosity levels, are measured for each sample and are correlated with microstructures through electron microscopy techniques such as Scanning Electron Microscopy (SEM) and Transmission Electron Microscopy (TEM). The grain structure is studied for the as-printed specimens and compared to the powder particle microstructure. The cellular structure of the printed samples is observed to have dendritic forms with dendrite width dimensions similar to the powder particle cells. The process parameter is changed, and the study is performed for different powder layer thickness, and the resultant mechanical properties and grain structure are shown to be similar. A phase study is conducted both on the powder and the printed samples using X-Ray Diffraction (XRD) techniques, and the austenite phase is observed to at first decrease due to the manufacturing process and again during the uniaxial tensile deformation. The martensitic structure is formed in the first stage based on the heating cycles of the manufacturing process and the remaining austenite is shown to be transformed to martensite due to different deformation mechanisms.

Keywords: additive manufacturing, maraging steel, mechanical properties, microstructure

Procedia PDF Downloads 149

Authors: Hyun Young Kim, Min Jung Kim, Ji Hyun Kim, Sanghyun Lee, Eun Ju Cho

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Oxidative stress that results from overproduction of free radicals can lead to pathogenesis of human diseases including cancer, neurodegenerative diseases, and cardiovascular disease. Aster yomena (Kitam.) Honda (A. yomena) belonging to Compositae family is a perennial plant, and it has anti-inflammatory, anti-asthmatic and anti-obesity effects. In this study, we investigated the antioxidative effect of A. yomena by measuring 2, 2-diphenyl-1-picrylhydrazyl (DPPH), hydroxyl radical (˙OH) and superoxide radical (O₂⁻) scavenging activities in vitro. A. yomena was extracted with ethanol and then partitioned with n-hexane, methylene chloride (CH₂Cl₂), ethyl acetate (EtOAc) and n-butanol (n-BuOH). In DPPH radical scavenging assay, the concentration of A. yomena from 10 to 100μg/mL dose-dependently raised the inhibition of DPPH oxidation. Especially, EtOAc fraction of A. yomena showed the highest DPPH radical scavenging activity among other fractions. The ˙OH radical scavenging activities of the extract and four fractions of A. yomena were increased by over 80% at a concentration of 50μg/mL. Especially, the IC50 value of EtOAc fraction was 0.03 μg/mL that is the lowest value compared with the values of other fractions. In addition, we found that the EtOAc fraction of A. yomena was showed to be better at O₂⁻ radical scavenging than other fractions. Taken together these results, we suggested that A. yomena, especially EtOAc fraction, can be used as a natural antioxidant against free radicals. Acknowledgements: This research was supported by Basic Science Research Program through the National Research Foundation of Korea (NRF) funded by the Ministry of Education, Science and Technology (NRF-2016R1D1A1B03931593).

Keywords: Aster yomena (Kitam.) Honda (A. yomena), free radicals, antioxidant, EtOAc fraction

Procedia PDF Downloads 284

Authors: S. Susanti, V. P. Bintoro, A. Setiadi, S. I. Santoso, D. R. Febriandi

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Meat is a foodstuff of animal origin. It is perishable because a suitable medium for bacterial growth. That is why meat can be a potential hazard to humans. Several ways have been done to inhibit bacterial population in an effort to prolong the meat shelf-life. However, aberration sometimes happens in the practices of meat preservation, for example by using chemical material that possessed strong antibacterial activity like formaldehyde. For health reason, utilization of formaldehyde as a food preservative was forbidden because of DNA damage resulting cancer and birth defects. Therefore, it is important to seek a natural food preservative that is not harmful to the body. This study aims to reveal the potency of cashew apple as natural food preservative by measuring its antibacterial activity and marinating effect on the bacterial growth of beef and chicken meat. Antibacterial activity was measured by The Kirby-Bauer method while bacterial growth was determined by total plate count method. The results showed that inhibition zone of 10-30% cashew apple extract significantly wider compared to 0% extract on the medium of E. coli, S. aureus, S. typii, and Bacillus sp. Furthermore, beef marinated with 20-30% cashew apple extract and chicken meat marinated with 5-15% extract significantly less in the total number of bacteria compared to 0% extract. It can be concluded that marinating with 5-30% cashew apple extract can effectively inhibit the bacterial growth of beef and chicken meat. Moreover, the concentration of extracts to inhibit bacterial populations in chicken meat was reached at the lower level compared to beef. Thus, cashew apple is potential as a natural food preservative.

Keywords: bacterial growth, cashew apple, marinating, meat

Procedia PDF Downloads 261

Authors: Gajanan M. Sonwane

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Nowadays, the entire pharmaceutical industry is facing the challenge of increasing efficiency and innovation. The major hurdles are the growing cost of research and development and a concurrent stagnating number of new chemical entities (NCEs). Hence, the challenge is to select the most druggable targets and to search the equivalent drug-like compounds, which also possess specific pharmacokinetic and toxicological properties that allow them to be developed as drugs. The present research work includes the studies of developing new anticancer heterocycles by using molecular modeling techniques. The heterocycles synthesized through such methodology are much effective as various physicochemical parameters have been already studied and the structure has been optimized for its best fit in the receptor. Hence, on the basis of the literature survey and considering the need to develop newer anticancer agents, new phenazinamine derivatives were designed by subjecting the nucleus to molecular modeling, viz., GQSAR analysis and docking studies. Simultaneously, these designed derivatives were subjected to in silico prediction of biological activity through PASS studies and then in silico toxicity risk assessment studies. In PASS studies, it was found that all the derivatives exhibited a good spectrum of biological activities confirming its anticancer potential. The toxicity risk assessment studies revealed that all the derivatives obey Lipinski’s rule. Amongst these series, compounds 4c, 5b and 6c were found to possess logP and drug-likeness values comparable with the standard Imatinib (used for anticancer activity studies) and also with the standard drug methotrexate (used for antimitotic activity studies). One of the most notable mutations is the threonine to isoleucine mutation at codon 315 (T315I), which is known to be resistant to all currently available TKI. Enzyme assay planned for confirmation of target selective activity.

Keywords: drug design, tyrosine kinases, anticancer, Phenazinamine

Procedia PDF Downloads 105