Search results for: antioxidant compounds

Authors: Ibrahim I. Elshahawy

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The objective of the present study was to investigate the effect of green tea extract on serum oxidant and antioxidant profile, liver and kidney function. 40 Friesian calves are included in this study and allocated into two groups: Group I (n=20) clinically healthy calves showing no clinical abnormalities, not receiving any treatment and served as control; group II (n=20) received green tea extract (GTE) for 30 days. Non-significant changes in blood urea nitrogen (BUN) were detected between groups, on contrary, serum creatinine and activities of liver enzymes aspartate transaminase (AST) and alanine transaminase (ALT) were significantly different between two groups. There were significant increases in the mean values of serum antioxidative parameters (total antioxidant capacity, catalase, superoxide dismutase, reduced glutathione and glutathione peroxidase) in group II. Whereas, the activity of lipid peroxidase significantly decreased in GTE treated calves when compared to control.

Keywords: green tea extract, antioxidants, oxidants, calves

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Authors: Vagolu S. Krishna, Shan Zheng, Estharla M. Rekha, Luke W. Guddat, Dharmarajan Sriram

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Tuberculosis (TB) remains a major threat to human health. This due to the fact that current drug treatments are less than optimal as well as the rising occurrence of multi drug-resistant and extensively drug-resistant strains of the etiological agent, Mycobacterium tuberculosis (Mt). Given the wide-spread significance of this disease, we have undertaken a design and evaluation program to discover new anti-TB drug leads. Here, our attention is focused on ketol-acid reductoisomerase (KARI), the second enzyme in the branched-chain amino acid biosynthesis pathway. Importantly, this enzyme is present in bacteria but not in humans, making it an attractive proposition for drug discovery. In the present work, we used high-throughput virtual screening to identify seventeen potential inhibitors of KARI using the Birla Institute of Technology and Science in-house database. Compounds were selected based on high docking scores, which were assigned as the result of favourable interactions between the compound and the active site of KARI. The Ki values for two leads, compounds 14 and 16 are 3.71 and 3.06 µM, respectively for Mt KARI. To assess the mode of binding, 100 ns molecular dynamics simulations for these two compounds in association with Mt KARI were performed and showed that the complex was stable with an average RMSD of less than 2.5 Å for all atoms. Compound 16 showed an MIC of 2.06 ± 0.91 µM and a 1.9 fold logarithmic reduction in the growth of Mt in an infected macrophage model. The two compounds exhibited low toxicity against murine macrophage RAW 264.7 cell lines. Thus, both compounds are promising candidates for development as an anti-TB drug leads.

Keywords: ketol-acid reductoisomerase, macrophage, molecular docking and dynamics, tuberculosis

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Authors: Jarel Elgin Tolentino, Arby Denise Nera, Mary Rose Roco, Angela Vianca Aspa, Nikko Beltran, Else Dapat

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Drug resistance by cells has been the problem in the medical field for decades now. The use of medicinal plants as a source of creating powerful drugs has been nowadays recognized worldwide to treat such resistant diseases. In the present study, the potential for Diospyros philippinensis A. DC. to inhibit growth of both bacteria and cancer cell line was conducted. The leaf crude extracts were screened for the presence of phytochemicals and examined for potential bioactivities by employing several assays like Kirby-Bauer disc diffusion method, DPPH (2,2-diphenyl-1-picryl-hydrazyl-hydrate) assay and MTT (3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide) tetrazolium assay for the antibacterial, antioxidant and cytotoxic activities of the extract, respectively. Phytochemical test results of the extracts revealed the presence of alkaloids, flavonoids, saponins, phenols, quinones, cardiac glycosides, phlobatannins, carbohydrate, cardenolides and proteins. The leaf extracts were found to exhibit antibacterial activity against gram-positive bacteria, high antioxidant activity (99.22% ± 0.005) but did not show any sign of cytotoxicity towards HCT116 (ATCC CCL-247). The study therefore concludes that D. philippinensis A. DC. leaf extract can be a source of antibacterial and chemopreventive agents. This claim may be used as basis for future investigation.

Keywords: bioassay, medicinal plants, plant crude extracts, phytochemical screening

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Authors: Sijing Xiong, Ran Su, Lit-Hsin Loo, Daniele Zink

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The kidney is a major target for toxic effects of drugs, industrial and environmental chemicals and other compounds. Typically, nephrotoxicity is detected late during drug development, and regulatory animal models could not solve this problem. Validated or accepted in silico or in vitro methods for the prediction of nephrotoxicity are not available. We have established the first and currently only pre-validated in vitro models for the accurate prediction of nephrotoxicity in humans and the first predictive platforms based on renal cells derived from human pluripotent stem cells. In order to further improve the efficiency of our predictive models, we recently developed a high content screening (HCS) platform. This platform employed automated imaging in combination with automated quantitative phenotypic profiling and machine learning methods. 129 image-based phenotypic features were analyzed with respect to their predictive performance in combination with 44 compounds with different chemical structures that included drugs, environmental and industrial chemicals and herbal and fungal compounds. The nephrotoxicity of these compounds in humans is well characterized. A combination of chromatin and cytoskeletal features resulted in high predictivity with respect to nephrotoxicity in humans. Test balanced accuracies of 82% or 89% were obtained with human primary or immortalized renal proximal tubular cells, respectively. Furthermore, our results revealed that a DNA damage response is commonly induced by different PTC-toxicants with diverse chemical structures and injury mechanisms. Together, the results show that the automated HCS platform allows efficient and accurate nephrotoxicity prediction for compounds with diverse chemical structures.

Keywords: high content screening, in vitro models, nephrotoxicity, toxicity prediction

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Authors: A. M. Plante, F. O’Halloran, A. L. McCarthy

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By 2050 it is projected that 2 billion of the global population will be more than 60 years old. Older adults have unique dietary requirements and aging is associated with physiological changes that affect appetite, sensory perception, metabolism, and digestion. Therefore, it is essential that foods recommended and designed for older adults promote healthy aging. To assess cheese as a functional food for the elderly, a range of commercial cheese products were selected and compared for their antioxidant properties. Cheese from various milk sources (bovine, goats, sheep) with different textures and fat content, including cheddar, feta, goats, brie, roquefort, halloumi, wensleydale and gouda, were initially digested with two different simulated in vitro gastrointestinal digestion (SGID) models. One SGID model represented a validated in vitro adult digestion system and the second model, an elderly SGID, was designed to consider the physiological changes associated with aging. The antioxidant potential of all cheese digestates was investigated using in vitro chemical-based antioxidant assays, (2,2-Diphenyl-1-picrylhydrazyl (DPPH) radical scavenging, ferric reducing antioxidant power (FRAP) and total phenolic content (TPC)). All adult model digestates had high antioxidant activity across both DPPH ( > 70%) and FRAP ( > 700 µM Fe²⁺/kg.fw) assays. Following in vitro digestion using the elderly SGID model, full-fat red cheddar, low-fat white cheddar, roquefort, halloumi, wensleydale, and gouda digestates had significantly lower (p ≤ 0.05) DPPH radical scavenging properties compared to the adult model digestates. Full-fat white cheddar had higher DPPH radical scavenging activity following elderly SGID digestion compared to the adult model digestate, but the difference was not significant. All other cheese digestates from the elderly model were comparable to the digestates from the adult model in terms of radical scavenging activity. The FRAP of all elderly digestates were significantly lower (p ≤ 0.05) compared to the adult digestates. Goats cheese was significantly higher (p ≤ 0.05) in FRAP (718 µM Fe²/kg.fw) compared to all other digestates in the elderly model. TPC levels in the soft cheeses (feta, goats) and low-fat cheeses (red cheddar, white cheddar) were significantly lower (p ≤ 0.05) in the elderly digestates compared to the adult digestates. There was no significant difference in TPC levels, between the elderly and adult model for full-fat cheddar (red, white), roquefort, wensleydale, gouda, and brie digestates. Halloumi cheese was the only cheese that was significantly higher in TPC levels following elderly digestion compared to adult digestates. Low fat red cheddar had significantly higher (p ≤ 0.05) TPC levels compared to all other digestates for both adult and elderly digestive systems. Findings from this study demonstrate that aging has an impact on the bioactivity of cheese, as antioxidant activity and TPC levels were lower, following in vitro elderly digestion compared to the adult model. For older adults, soft cheese, particularly goats cheese, was associated with high radical scavenging and reducing power, while roquefort cheese had low antioxidant activity. Also, elderly digestates of halloumi and low-fat red cheddar were associated with high TPC levels. Cheese has potential as a functional food for the elderly, however, bioactivity can vary depending on the cheese matrix. Funding for this research was provided by the RISAM Scholarship Scheme, Cork Institute of Technology, Ireland.

Keywords: antioxidants, cheese, in-vitro digestion, older adults

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Authors: Harpreet Singh Kainth

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Rubidium salts have been commonly used as an electrolyte to improve the efficiency cycle of Li-ion batteries. In recent years, it has been implemented into the large scale for further technological advances to improve the performance rate and better cyclability in the batteries. X-ray absorption spectroscopy (XAS) is a powerful tool for obtaining the information in the electronic structure which involves the chemical state analysis in the active materials used in the batteries. However, this technique is not well suited for the industrial applications because it needs a synchrotron X-ray source and special sample file for in-situ measurements. In contrast to this, conventional wavelength dispersive X-ray fluorescence (WDXRF) spectrometer is nondestructive technique used to study the chemical shift in all transitions (K, L, M, …) and does not require any special pre-preparation planning. In the present work, the fluorescent Lα, Lβ₁ , Lβ₃,₄ and Lγ₂,₃ X-ray spectra of rubidium in different chemical forms (Rb₂CO₃ , RbCl, RbBr, and RbI) have been measured first time with high resolution wavelength dispersive X-ray fluorescence (WDXRF) spectrometer (Model: S8 TIGER, Bruker, Germany), equipped with an Rh anode X-ray tube (4-kW, 60 kV and 170 mA). In ₃₇Rb compounds, the measured energy shifts are in the range (-0.45 to - 1.71) eV for Lα X-ray peak, (0.02 to 0.21) eV for Lβ₁ , (0.04 to 0.21) eV for Lβ₃ , (0.15 to 0.43) eV for Lβ₄ and (0.22 to 0.75) eV for Lγ₂,₃ X-ray emission lines. The chemical shifts in rubidium compounds have been measured by considering Rb₂CO₃ compounds taking as a standard reference. A Voigt function is used to determine the central peak position of all compounds. Both positive and negative shifts have been observed in L shell emission lines. In Lα X-ray emission lines, all compounds show negative shift while in Lβ₁, Lβ₃,₄, and Lγ₂,₃ X-ray emission lines, all compounds show a positive shift. These positive and negative shifts result increase or decrease in X-ray energy shifts. It looks like that ligands attached with central metal atom attract or repel the electrons towards or away from the parent nucleus. This pulling and pushing character of rubidium affects the central peak position of the compounds which causes a chemical shift. To understand the chemical effect more briefly, factors like electro-negativity, line intensity ratio, effective charge and bond length are responsible for the chemical state analysis in rubidium compounds. The effective charge has been calculated from Suchet and Pauling method while the line intensity ratio has been calculated by calculating the area under the relevant emission peak. In the present work, it has been observed that electro-negativity, effective charge and intensity ratio (Lβ₁/Lα, Lβ₃,₄/Lα and Lγ₂,₃/Lα) are inversely proportional to the chemical shift (RbCl > RbBr > RbI), while bond length has been found directly proportional to the chemical shift (RbI > RbBr > RbCl).

Keywords: chemical shift in L emission lines, bond length, electro-negativity, effective charge, intensity ratio, Rubidium compounds, WDXRF spectrometer

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Authors: Jaspal Rana, Alkem Laboratories, Baddi, Himachal Pradesh, India Chitkara University, Punjab, India

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Oxidative stress has been identified as an underlying cause of ischemia-reperfusion (IR) related cognitive dysfunction and brain damage. Therefore, antioxidant based therapies to treat IR injury are being investigated. Allium cepa L. (onion) is used as culinary medicine and is documented to have marked antioxidant effects. Hence, the present study was designed to evaluate the effect of A. cepa outer scale extract (ACE) against IR induced cognition and biochemical deficit in mice. ACE was prepared by maceration with 70% methanol and fractionated into ethylacetate and aqueous fractions. Bilateral common carotid artery occlusion for 10 min followed by 24 h reperfusion was used to induce cerebral IR injury. Following IR injury, ACE (100 and 200 mg/kg) was administered orally to animals for 7 days once daily. Behavioral outcomes (memory and sensorimotor functions) were evaluated using Morris water maze and neurological severity score. Cerebral infarct size, brain thiobarbituric acid reactive species, reduced glutathione, and superoxide dismutase activity was also determined. Treatment with ACE significantly ameliorated IR mediated deterioration of memory and sensorimotor functions and rise in brain oxidative stress in animals. The results of the present investigation revealed that ACE improved functional outcomes after cerebral IR injury, which may be attributed to its antioxidant properties.

Keywords: stroke, neuroprotection, ischemia reperfusion, herbal drugs

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Authors: Harshani Uggallage, Kapila D. Dissanayaka

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A Sulforhodamine-B assay-guided fractionation on Nigella sativa seeds was conducted to determine the presence of cytotoxic compounds against human hepatoma (HepG2) cells. Initially, a freeze-dried sample of Nigella sativa seeds was sequentially extracted into solvents of increasing polarities. Crude extracts from the sequential extraction of Nigella sativa seeds in chloroform and ethyl acetate showed the highest cytotoxicity. The combined mixture of these two extracts was subjected to bioassay guided fractionation using a modified Kupchan method of partitioning, followed by Sephadex® LH-20 chromatography. This chromatographic separation process resulted in a column fraction with a convincing IC50 (half-maximal inhibitory concentration) value of 13.07µg/ml, which is considerable for developing therapeutic drug leads against human hepatoma. Reversed phase High-Performance Liquid Chromatography (HPLC) was finally conducted for the same column fraction, and the result indicates the presence of one or several main cytotoxic compounds against human HepG2 cells.

Keywords: cytotoxic compounds, half-maximal inhibitory concentration, high-performance liquid chromatography, human HepG2 cells, nigella sativa seeds, Sulforhodamine-B assay

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Authors: Md. Shadab, Mariyam N. Nashid, Venkata Srikanth Meka, Thiagarajan Madheswaran

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Naringenin (NAR), is a naturally occurring plant flavonoid, found predominantly in citrus fruits, that possesses a wide range of pharmacological properties including anti-oxidant, anti-inflammatory behaviour, cholesterol-lowering and anticarcinogenic activities. However, despite the therapeutic potential of naringenin shown in a number of animal models, its clinical development has been hindered due to its low aqueous solubility, slow dissolution rate and inefficient transport across biological membranes resulting in low bioavailability. Naringenin nanosuspension were produced using stabilizers Tween® 80 by high pressure homogenization techniques. The nanosuspensions were characterized with regard to size (photon correlation spectroscopy (PCS), size distribution, charge (zeta potential measurements), morphology, short term physical stability, dissolution profile and antioxidant potential. A nanocrystal PCS size of about 500 nm was obtained after 20 homogenization cycles at 1500 bar. The short-term stability was assessed by storage of the nanosuspensions at 4 ◦C, room temperature and 40 ◦C. Result showed that naringenin nanosuspension was physically unstable due to large fluctuations in the particle size and zeta potential after 30 days. Naringenin nanosuspension demonstrated higher drug dissolution (97.90%) compared to naringenin powder (62.76%) after 120 minutes of testing. Naringenin nanosuspension showed increased antioxidant activity compared to naringenin powder with a percentage DPPH radical scavenging activity of 49.17% and 31.45% respectively at the lowest DPPH concentration.

Keywords: bioavailability, naringenin, nanosuspension, oral delivery

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Authors: Strahinja Kovačević, Lidija Jevrić, Miloš Kuzmanović, Sanja Podunavac-Kuzmanović

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In this paper, various derivatives of benzimidazole have been evaluated against Gram-negative bacteria Escherichia coli. For all investigated compounds the minimum inhibitory concentration (MIC) was determined. Quantitative structure-activity relationships (QSAR) attempts to find consistent relationships between the variations in the values of molecular properties and the biological activity for a series of compounds so that these rules can be used to evaluate new chemical entities. The correlation between MIC and some absorption, distribution, metabolism and excretion (ADME) parameters was investigated, and the mathematical models for predicting the antibacterial activity of this class of compounds were developed. The quality of the multiple linear regression (MLR) models was validated by the leave-one-out (LOO) technique, as well as by the calculation of the statistical parameters for the developed models and the results are discussed on the basis of the statistical data. The results of this study indicate that ADME parameters have a significant effect on the antibacterial activity of this class of compounds. Principal component analysis (PCA) and agglomerative hierarchical clustering algorithms (HCA) confirmed that the investigated molecules can be classified into groups on the basis of the ADME parameters: Madin-Darby Canine Kidney cell permeability (MDCK), Plasma protein binding (PPB%), human intestinal absorption (HIA%) and human colon carcinoma cell permeability (Caco-2).

Keywords: benzimidazoles, QSAR, ADME, in silico

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Authors: Xiao-Jing Zhu, Liang Zhou, Shi-Zhong Zheng

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Various studies have shown that diallyl trisulfide (DATS) can protect the liver injury, and DATS has a strong antioxidant property. The aim of this study is to evaluate the in vivo role of DATS in protecting the liver against injury and fibrogenesis and further explores the underlying mechanisms. Our results demonstrated that DATS protected the liver from CCl4-caused injury by suppressing the elevation of ALT and AST activities, and by improving the histological architecture of the liver. Treatment with DATS or colchicine improved the liver fibrosis by sirius red staining and immunofluorescence. In addition, immunohistochemistry, western blot, and RT-PCR analyses indicated that DATS inhibited HSC activation. Furthermore, DATS attenuated oxidative stress by increasing glutathione and reducing lipid peroxides and malondialdehyde. These findings suggest that the protective effect of DATS on CCl4-caused liver injury and liver fibrogenesis was, at least partially, attributed to its antioxidant activity.

Keywords: liver fibrogenesis, liver injury, oxidative stress, DATS

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Authors: Borokini Funmilayo Boede

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B. alba L., commonly called ‘Amunututu’ and Solanecio biafrae called ‘Worowo’ among the Yoruba tribe in the southwest part of Nigeria are reported to be of great ethnomedicinal importance but are among many underutilized green leafy vegetables in the country. Many studies have established the nutritional values of these vegetables, utilization are very poor and indepth information on their chemical profiles is scarce. The aqueous, methanolic and ethanolic extracts of these vegetables were subjected to phytochemical screening and phenolic profiles of the alcoholic extracts were characterized by using high-performance liquid chromatography coupled with diode array detector (HPLC-DAD). Total phenol and flavonoid contents were determined, antioxidant activities were evaluated using five in vitro assays to assess DPPH, nitric oxide and hydroxyl radical-scavenging abilities, as well as reducing power with ferric reducing antioxidant assay and phosphomolybdate method. The antibacterial activities of the extracts against Staphylococcus aureus, Pseudomonas aeruginosa, and Salmonella typhi were evaluated by using agar well diffusion method and the antifungal activity evaluated against food-associated filamentous fungi by using poisoned food technique with the aim of assessing their nutraceutical potentials to encourage their production and utilization. The results revealed the presence of saponnin, steroids, tannin, terpenoid and flavonoid as well as phenolic compounds: gallic acid, chlorogenic acid, caffeic acid, coumarin, rutin, quercitrin, quercetin and kaemferol. The vegetables showed varying concentration dependent reducing and radical scavenging abilities from weak to strong compared with gallic acid, rutin, trolox and ascorbic acid used as positive controls; the aqueous extracts which gave higher concentrations of total phenol displayed higher ability to reduce Fe (lll) to Fe (ll) and stronger inhibiting power against hydroxyl radical than the alcoholic extracts and in most cases exhibited more potency than the ascorbic acids used as positive controls, at the same concentrations, whereas, methanol and / or ethanol extracts were found to be more effective in scavenging 2, 2-diphenyl-1-picryl hydrazyl radical and showed higher ability to reduce Mo (VI) to Mo (V) in total antioxidant assay than the aqueous extracts. However, the inhibition abilities of all the extracts against nitric oxide were comparable with the ascorbic acid control at the same concentrations. There were strong positive correlations with total phenol (mg GAE/g) and total flavonoid (mg RE/g) contents in the range TFC (r=0.857- 0999 and r= 0.904-1.000) and TPC (r= 0.844- 0.992 and r= 0.900 -0.999) for Basella alba and Senecio biafrae respectively. Inhibition concentration at 50 % (IC50) for each extract to scavenge DPPH, OH and NO radicals ranged from 32.73 to 1.52 compared with control (0.846 - -6.42) mg/ml. At 0.05g/ml, the vegetables were found to exhibit mild antibacterial activities against Staphylococcus aureus, Pseudomonas aeruginosa and Salmonella typhi compared with streptomycin sulphate used as control but appreciable antifungi activities against (Trichoderma rubrum and Aspergillus fumigates) compared with bonlate antibiotic positive control. The vegetables possess appreciable antioxidant and antimicrobial properties for promoting good health, their cultivation and utilization should be encouraged especially in the face of increasing health and economic challenges and food insecurity in many parts of the world.

Keywords: antimicrobial, antioxidants, extracts, phytochemicals

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Authors: W. P. Hu, J. V. Kumar, Jeffrey J. P. Tsai

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The inhibition of SH2 domain regulated protein-protein interactions is an attractive target for developing an effective chemotherapeutic approach in the treatment of disease. Molecular simulation is a useful tool for developing new drugs and for studying molecular recognition. In this study, we searched potential drug compounds for the inhibition of SH2 domain by performing structural similarity search in PubChem Compound Database. A total of 37 compounds were screened from the database, and then we used the LibDock docking program to evaluate the inhibition effect. The best three compounds (AP22408, CID 71463546 and CID 9917321) were chosen for MD simulations after the LibDock docking. Our results show that the compound CID 9917321 can produce a more stable protein-ligand complex compared to other two currently known inhibitors of Src SH2 domain. The compound CID 9917321 may be useful for the inhibition of SH2 domain based on these computational results. Subsequently experiments are needed to verify the effect of compound CID 9917321 on the SH2 domain in the future studies.

Keywords: nonpeptide inhibitor, Src SH2 domain, LibDock, molecular dynamics simulation

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Authors: Nura Lawal, Lawal Suleiman Bilbis, Rabiu Aliyu Umar, Anas A. Sabir

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Metabolic syndrome (MS) a high-risk condition involving obesity, dyslipidemia, hypertension, and diabetes mellitus is prevalent in Nigeria. The study aims to formulate an antioxidant-rich nutraceutical from locally available foodstuff (onion, garlic, ginger, tomato, lemon, palm oil, watermelon seeds) and investigate their effects on blood pressure, body weight, serum glucose, lipid profile, insulin and oxidative stress markers in salt-induced rats. The rats were placed on 8% salt diet for 6 weeks and then supplementation and treatment with nutraceutical and nifedipine in the presence of salt diet for additional 4 weeks. Feeding rats with salt diet for 6 weeks increased blood pressure and body weight of the salt-loaded rats relative to control. Significant (P < 0.001) increase in serum blood glucose and lipid profile, and the decrease in high-density lipoprotein-cholesterol (HDL-C) was observed in salt-loaded rats as compared with control. Both supplementation and treatment (nifedipine) lowered the blood pressure but the only supplementation lowered the body weight. Supplementation with nutraceutical resulted in significant (P < 0.001) decrease in the serum blood glucose, lipid profile, malonyldialdehyde (MDA), insulin levels, insulin resistance, and increased HDL-C and antioxidant indices. The percentage protection against atherogenesis was 76.5±2.13%. There is strong positive correlation between blood pressure, body weight and serum blood glucose, lipid profile, markers of oxidative stress and strong negative correlation with HDL-C and antioxidant status. The results suggest that the nutraceuticals are useful in reversing most of the component of metabolic syndrome and might be beneficial in the treatment of patients with metabolic syndrome.

Keywords: metabolic syndrome, hypertension, diabetes mallitus, obesity

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Authors: Krasimir Ivanov, Elitsa Kolentsova, Dimitar Dimitrov, Petya Petrova, Tatyana Tabakova

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This work studies the effect of chemical composition on the activity and selectivity of γ–alumina supported CuO/ MnO2/Cr2O3 catalysts toward deep oxidation of CO, dimethyl ether (DME) and methanol. The catalysts were prepared by impregnation of the support with an aqueous solution of copper nitrate, manganese nitrate and CrO3 under different conditions. Thermal, XRD and TPR analysis were performed. The catalytic measurements of single compounds oxidation were carried out on continuous flow equipment with a four-channel isothermal stainless steel reactor. Flow-line equipment with an adiabatic reactor for simultaneous oxidation of all compounds under the conditions that mimic closely the industrial ones was used. The reactant and product gases were analyzed by means of on-line gas chromatographs. On the basis of XRD analysis it can be concluded that the active component of the mixed Cu-Mn-Cr/γ–alumina catalysts consists of at least six compounds – CuO, Cr2O3, MnO2, Cu1.5Mn1.5O4, Cu1.5Cr1.5O4 and CuCr2O4, depending on the Cu/Mn/Cr molar ratio. Chemical composition strongly influences catalytic properties, this influence being quite variable with regards to the different processes. The rate of CO oxidation rapidly decrease with increasing of chromium content in the active component while for the DME was observed the reverse trend. It was concluded that the best compromise are the catalysts with Cu/(Mn + Cr) molar ratio 1:5 and Mn/Cr molar ratio from 1:3 to 1:4.

Keywords: Cu-Mn-Cr oxide catalysts, volatile organic compounds, deep oxidation, dimethyl ether (DME)

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Authors: Benhouda Afaf, Yahia Massinissa, Paolo Grieco

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Hyoscyamus albus L. is a small genus from Solanaceae family known by its use in old traditional medicine in the east of Algeria. Aim: This study aimed to characterize bioactive molecules from H. albus, evaluate their anticancer activity in several cancer cells and investigate their possible molecular mechanism. Materials and Methods: Different compounds (Peak h of fraction F), (Peak 3 of Fraction F), (Peak 1 of fraction C) were isolated from H.albus L by using high-performance chromatography (HPLC), mass spectrometry (MS) and proton NMR (NMR H1). All isolated compounds were subjected to cytotoxicity and antiproliferative assays against a panel of the four cell lines: DU-145, U-2 OS, U-87 MG and LN-229 cell lines and were determined using MTT assay, Annexin V and propodium iodide were used to evaluate apoptosis. Results: The phytochemical study of H. albus Fractions led to the isolation of quercetin-3-O-β-dglucopyranosyl-( 1 → 6)-β-d-glucopyranosid, N-trans-feruloyltyramine, Hydrocaffeoyl-N8- caffeoylspermidine.The biological results indicated that all cell lines were consistently sensitive to P1 FC in a dose-dependent manner. This difference in cytotoxic sensitivity was more pronounced in osteosarcoma cell line, U-2 OS, when compared to prostate cancer and U-87 MG. Cell viability data also demonstrated that only U-87 MG cells were responsive to treatment with Ph FF. compounds P1 FC and Ph FF have induced necrosis and apoptosis in a large part of LN-229 cells. Conclusion: The overall results of the present study provided evidence that isolated compounds are potential therapeutic entities against cancer.

Keywords: hyoscyamus albus, cancer cells, coumpounds, HPLC

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Authors: Udeshika Yapa Bandara, Chamindri Witharana, Preethi Soysa

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Pomegranate fruits are used in cancer treatment in Ayurveda, Sri Lanka. Due to prevailing therapeutic effects of phytochemicals, this study was focus on anti-cancer properties of the constituents in the parts of Pomegranate fruit. Furthermore, the method of extraction, plays a crucial step of the phytochemical analysis. Therefore, this study was focus on different extraction methods. Five techniques were involved for the peel and the pericarp to evaluate the most effective extraction method; Boiling with electric burner (BL), Sonication (SN), Microwaving (MC), Heating in a 50°C water bath (WB) and Sonication followed by Microwaving (SN-MC). The presence of polyphenolic and flavonoid contents were evaluated to recognize the best extraction method for polyphenols. The total phenolic content was measured spectrophotometrically by Folin-Ciocalteu method and expressed as Gallic Acid Equivalents (w/w% GAE). Total flavonoid content was also determined spectrophotometrically with Aluminium chloride colourimetric assay and expressed as Quercetin Equivalents (w/w % QE). Pomegranate juice was taken as fermented juice (with Saccharomyces bayanus) and fresh juice. Powdered seeds were refluxed, filtered and freeze-dried. 2g of freeze-dried powder of each component was dissolved in 100ml of De-ionized water for extraction. For the comparison of antioxidant activity and total phenol content, the polyphenols were removed by the Polyvinylpolypyrrolidone (PVVP) column and fermented and fresh juice were tested for the 1, 1-diphenyl-2-picrylhydrazil (DPPH) radical scavenging activity, before and after the removal of polyphenols. For the peel samples of Pomegranate fruit, total phenol and flavonoid contents were high in Sonication (SN). In pericarp, total phenol and flavonoid contents were highly exhibited in method of Sonication (SN). A significant difference was observed (P< 0.05) in total phenol and flavonoid contents, between five extraction methods for both peel and pericarp samples. Fermented juice had a greatest polyphenolic and flavonoid contents comparative to fresh juice. After removing polyphenols of fermented juice and fresh juice using Polyvinyl polypyrrolidone (PVVP) column, low antioxidant activity was resulted for DPPH antioxidant activity assay. Seeds had a very low total phenol and flavonoid contents according to the results. Although, Pomegranate peel is the main waste component of the fruit, it has an excellent polyphenolic and flavonoid contents compared to other parts of the fruit, devoid of the method of extraction. Polyphenols play a major role for antioxidant activity.

Keywords: antioxidant activity, flavonoids, polyphenols, pomegranate

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Authors: Li Chun Zhao, Zhi Chao Hu, Xi Qiang Liu, Man Lai Lee, Chak Shing Yeung, Man Fei Xu, Yuen Yee Kwan, Alan H. M. Ho, Nickie W. K. Chan, Bin Deng, Zhong Zhen Zhao, Min Xu

Abstract:

Background: Chuangxiong Rhizoma (Chuangxion, CX) is one of the most frequently used herbs in Chinese medicine because of its wide therapeutic effects such as vasorelaxation and anti-inflammation. Aim: The purposes of this study are (1) to perform non-targeted / targeted analyses of CX methanol extract and water extract, and compare the present data with previously LC-MS or GC-MS fingerprints; (2) to examine the difference between CX methanol extract and water extract for preliminarily evaluating whether current compound markers of methanol extract from crude CX materials could be suitable for quality control of CX water extract. Method: CX methanol extract was prepared according to the Hong Kong Chinese Materia Medica Standards. DG water extract was prepared by boiling with pure water for three times (one hour each). UHPLC-Q-TOF-MS/MS fingerprint analysis was performed by C18 column (1.7 µm, 2.1 × 100 mm) with Agilent 1290 Infinity system. Experimental data were analyzed by Agilent MassHunter Software. A database was established based on 13 published LC-MS and GC-MS CX fingerprint analyses. Total 18 targeted compounds in database were selected as markers to compare present data with previous data, and these markers also used to compare CX methanol extract and water extract. Result: (1) Non-targeted analysis indicated that there were 133 compounds identified in CX methanol extract, while 325 compounds in CX water extract that was more than double of CX methanol extract. (2) Targeted analysis further indicated that 9 in 18 targeted compounds were identified in CX methanol extract, while 12 in 18 targeted compounds in CX water extract that showed a lower lose-rate of water extract when compared with methanol extract. (3) By comparing CX methanol extract and water extract, Senkyunolide A (+1578%), Ferulic acid (+529%) and Senkyunolide H (+169%) were significantly higher in water extract when compared with methanol extract. (4) Other bioactive compounds such as Tetramethylpyrazine were only found in CX water extract. Conclusion: Many new compounds in both CX methanol and water extracts were found by using UHPLC Q-TOF MS/MS analysis when compared with previous published reports. A new standard reference including non-targeted compound profiling and targeted markers functioned especially for quality control of CX water extract (herbal decoction) should be established in future. (This project was supported by Hong Kong Baptist University (FRG2/14-15/109) & Natural Science Foundation of Guangdong Province (2014A030313414)).

Keywords: Chuanxiong rhizoma, fingerprint analysis, targeted analysis, quality control

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Authors: Saleh N. Maodaa

Abstract:

Perinatal exposure to nicotine imbalances the redox status in newborns. This study investigated the effect of Anethum graveolens (dill) extract on oxidative stress and tissue injury in the liver and kidney of mice newborns exposed to nicotine perinatally. Pregnant mice received nicotine (0.25 mg/kg) on gestational day 12 to day 5 after birth and/or A. graveolens extract on a gestational day 1 to day 15 after birth. Newborn mice exposed to nicotine showed multiple histopathological alterations in the kidney and liver, including inflammatory cell infiltration and degenerative changes. Nicotine exposure increased hepatic and renal reactive oxygen species (ROS), lipid peroxidation, tumor necrosis factor (TNF-_), interleukin-6 (IL-6), and inducible nitric oxide synthase (iNOS) (p < 0.001), and decreased antioxidant defenses (p < 0.001). A. graveolens supplementation significantly prevented liver and kidney injury, suppressed ROS generation (p < 0.001), lipid peroxidation (p < 0.001), and inflammatory response (p < 0.001), and enhanced antioxidant defenses. In addition, A. graveolens upregulated hepatic and renal Nrf2 and HO-1 mRNA and increased HO-1 activity in normal and nicotine-exposed mice. In conclusion, A. graveolens protects against perinatal nicotine-induced oxidative stress, inflammation, and tissue injury in the liver and kidney of newborn mice. A. graveolens upregulated hepatic and renal Nrf2/HO-1 signaling and enhanced antioxidant defenses in mice.

Keywords: dill, oxidative stress, cytokines, nicotine

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Authors: Nima Samie, Sekaran Muniandy, Zahurin Mohamed, M. S. Kanthimathi

Abstract:

Although number of indole containing compounds have been reported to have anticancer properties in vitro but only a few of them show potential as anticancer compounds in vivo. The current study was to evaluate the mechanism of cytotoxicity of selected indolic compound in vivo and in vitro. In this context, we determined the potency of the compound in the induction of apoptosis, cell cycle arrest, and cytoskeleton rearrangement. HT-29, WiDr, CCD-18Co, human monocyte/macrophage CRL-9855, and B lymphocyte CCL-156 cell lines were used to determine the IC50 of the compound using the MTT assay. Analysis of apoptosis was carried out using immunofluorescence, acridine orange/ propidium iodide double staining, Annexin-V-FITC assay, evaluation of the translocation of NF-kB, oxygen radical antioxidant capacity, quenching of reactive oxygen species content, measurement of LDH release, caspase-3/-7, -8 and -9 assays and western blotting. The cell cycle arrest was examined using flowcytometry and gene expression was assessed using qPCR array. Results displayed a potent suppressive effect on HT-29 and WiDr after 24 h of treatment with IC50 value of 2.52±0.34 µg/ml and 2.13±0.65 µg/ml respectively. This cytotoxic effect on normal, monocyte/macrophage and B-cells was insignificant. Dipping in the mitochondrial membrane potential and increased release of cytochrome c from the mitochondria indicated induction of the intrinsic apoptosis pathway by the compound. Activation of this pathway was further evidenced by significant activation of caspase-9 and 3/7. The compound was also shown to activate the extrinsic pathways of apoptosis via activation of caspase-8 which is linked to the suppression of NF-kB translocation to the nucleus. Cell cycle arrest in the G1 phase and up-regulation of glutathione reductase, based on excessive ROS production were also observed. These findings were further investigated for inhibitory efficiency of the compound on colonic aberrant crypt foci in male rats. Rats were divided in to 5 groups: vehicle, cancer control, positive control groups and the groups treated with 25 and 50 mg/kg of compounds for 10 weeks. Administration of compound suppressed total colonic ACF formation up to 73.4%. The results also showed that treatment with the compound significantly reduced the level of malondialdehyde while increasing superoxide dismutase and catalase activities. Furthermore, the down-regulation of PCNA and Bcl2 and the up-regulation of Bax was confirmed by immunohistochemical staining. The outcome of this study suggest sthat the indolic compound is a potent anti-cancer agent against colon cancer and can be further evaluated by animal trial.

Keywords: indolic compound, chemoprevention, crypt, azoxymethane, colon cancer

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Authors: Keivan Saeb, Azade Kakouei, Razieh Jafari Hajati, Khalil Pourshamsian, Babak Babakhani

Abstract:

Urtica Diocia L. from the Urticaceae family is a plant of herbal value and of a noticeable distribution in the north of Iran. The growth of different plants in various natural environments and ecosystems seems to be affected by factors such as the height (from sea surface).To investigate the effect of height on Urtica Diocia L. medicine compounds in its natural environment, three areas with the height of zero, 800 and 1800m were selected.The samples were randomly gathered three times and were dried; also, their compounds was extracted using the Clivenger with the water-distilling method. To determine the medicine compounds, the GC-MS as well as the GC machines were used. The analysis of variance was done in the form of the random-full-block design. The results indicated that there was a significant difference between the percent of EOs in the selected heights; however, such difference was not significant within each height. From among the eight flavors of the study, the phytol compound was more in terms of percentage. By increasing the height the percent of EOs would decrease. lower heights could be considered most appropriate for producing the studied effective materials despite of the moistened climate and soil there.

Keywords: Urtica diocia L., height, EOs, medicine

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Authors: Muruvvet Ilgin, Ilknur Agca

Abstract:

Common mulberry (Morus levigate Wall.) and purple mulberry (Morus rubra L.) species which were selected from different regions of Turkey were used as material in order to determine their performance. Therefore, phenological observations, pomological analysis (fruit size, fruit weight, fruit stalk length, acidity and TSS (Total Soluble Solids) and phytochemical properties organic acids (oxalic acid, succinic acid, citric acid, fumaric acid and malic acid) and vitamin C (ascorbic acid) total phenolics and antioxidant capacity values of mulberries) were determined. Phenological observations of seven different periods were also identified. Fruit weight values varied between 3.48 to 4.26 g. TSS contents value were from 14.36 to 21.30%, and fruit acidity was determined between 0.29 to 2.02%. The amount of ascorbic acid of Finger mulberry (Morus levigate Wall.) and purple mulberry (Morus rubra L.) species were identified as 35.60% and 363.28%. The highest value of total phenolic contents belonged to with a finger mulberry genotypes P1 934.80 mg/100g whereas the lowest one was of purple mulberry genotypes 278.70 mg/100g. FRAP and TEAC methods were used for determination of antioxidant capacity of the values of 0.58-22.65 micromol TE/kg and 20.34-31.6 micromol TE/kg. Total phenolics contents and antioxidant capacity strongly depends on fruit color intensity with a positive correlation. The obtained results have been found to be important as a source of future pharmacological studies and pomological and breeding programs.

Keywords: mulberry, phenology, phytochemical property, pomology

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Authors: Shima Dehghan

Abstract:

Aim: imbalance between antioxidant defensive system and increasing production of free radicals caused oxidative stress that can be rolled in cellular damage and occurring some of diseases such as diabetes. The aim of current study was to investigate the effect of eight weeks aerobic training on peroxidant and antioxidants indicators in women with type2 diabetes. Methodology: thirty two inactive women with type 2 diabetes were randomly assigned into four groups: 1. control, 2. Aerobic training, 3. Purslane seed and 4. Aerobic training + Purslane seed groups. Subjects were asked to accomplish eight weeks aerobic training (50 min aerobic exercise, 3 days/week, for to achieve 65-75% maximum of heart rate). Also, subjects in certain groups received purslane seeds for eight weeks. Blood samples were obtained in two sets (one session and after 8 weeks). Data was analyzed using one way ANOVA. A significant difference was accepted at p < 0/05 level. Results: After eight weeks of aerobic training with purslane seeds supplementation, malon dyaldehyde (MDA) concentration in training group were significantly decreased (p < 0/000), but A difference significant was not found in control group. Superoxide dismutase (SOD) and catalase (CAT) concentrations in training group were significantly increased (p < 0/000), while difference significant wasnot found in control group. Conclusion: The finding of the current study indicates that disciplined aerobic training with purslane seeds supplementation can be caused improvement in peroxidant/antioxidant balance in women with type2 diabetes.

Keywords: aerobic training, purslane seed, peroxidant/antioxidant balance, diabetes2

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Authors: Huda Aldossari

Abstract:

Members of the Brassicaceae family, such as rocket species, have high concentrations of glucosinolates (GLSs). GSLs and isothiocyanates (ITCs), the product of GLSs hydrolysis, are the most influential compounds that affect flavour in rocket species. Aside from their contribution to the flavour, GSLs and ITCs are of particular interest due to their potential ability to inhibit the growth of human pathogenic bacteria such as E. coli O157. Quantitative and qualitative analysis of glucosinolate compounds in rocket extracts was obtained by Liquid Chromatography-Mass Spectrometry (LC–MS).Each individual component of non-volatile GLSs and ITCs was isolated by High-Performance Liquid Chromatography (HPLC) fractionation. The identity and purity of each fraction were confirmed using Ultra High-Performance Liquid Chromatography (UPLC). The separation of glucosinolates in the complex rocket extractions was performed by optimizing a HPLC fractionation method through changing the mobile phase composition, solvent gradient, and the flow rate. As a result, six glucosinolates compounds (Glucosativin, 4-Methoxyglucobrassicin, Glucotropaeolin GTP, Glucoiberin GIB, Diglucothiobenin, and Sinigrin) have been isolated, identified and quantified in the complex samples. This step aims to evaluate the antibacterial activity of glucosinolates and their enzymatic hydrolysis against bacterial growth of E.coli k12. Therefore, fractions from this study will be used to determine the most active compounds by investigating the efficacy of each component of GLSs and ITCs at inhibiting bacterial growth.

Keywords: rocket, glucosinolates, E.coli k12., HPLC fractionatio

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Authors: Mehdi Abbasi, Masoumeh Majidi Zolbin

Abstract:

Varicocele is one of the common causes of infertility in 30-50% of married men which occurs within the spermatic cord. It can be considered as an abnormal dilatation and stasis of veins of the pampiniform plexus that drain the testis. It occurs in 15-20% of the male population. Inducible nitric oxide synthase (NOS) activity has been frequently reported in varicose veins. Several studies have considered the relationship between varicocele and semen NO concentrations. NOS isoforms have been shown to regulate a number of functions, e.g., sperm motility and maturation and germ cell apoptosis in the testes. In adult patients with varicocele, the amount of NO levels in the varicose veins are 25 times higher than in serum of peripheral veins. The aim of this study was to review the effect of different antioxidant that we applied so far on sperm parameters as well as sperm DNA fragmentation. The findings of this study suggest that antioxidants improve sperm parameters which are associated with infertility in varicocelized rats, and treatment can reduce damage to sperm DNA and increase the chance of fertility.

Keywords: antioxidant, rat, sperm parameter, varicocele

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Authors: Salma Mirza, Syeda Asma Naqvi, Khalid Mohammed Khan, M. Iqbal Choudhary

Abstract:

In this study twenty-five (25) newly synthesized compounds substituted aryl thiazoles (SAT) 1-25 were synthesized, and in vitro cytotoxicity of these compounds was evaluated against four cancer cell lines namely, MCF-7 (ER+ve breast), MDA-MB-231 (ER-ve breast), HCT116 (colorectal), and, HeLa (cervical) and compared with the standard anticancer drug doxorubicin with IC50 value of 1.56 ± 0.05 μM. Among them, compounds 1, 4-8 and 19 were found to be active against all four cell lines. Compound 20 was found to be selectively active against MCF7 cells with IC50 value of 40.21 ± 4.15 µM, whereas compound 19 was active against only MCF7 and HeLa cells with IC50 values of 46.72 ± 1.8 and 19.86 ± 0.11 μM, respectively. These results suggest that aryl thiazoles 1 and 4 deserve to be investigated further in vivo as anti-cancer agents.

Keywords: anticancer agents, breast cancer cell lines (MCF7, MDA-MB-231), colorectal cancer cell line (HCT-116), cervical cancer cell line (HeLa), Thiazole derivatives

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Authors: Philip Edinger, Christian Ludwig

Abstract:

The formation and control of tars remain one of the major challenges in the implementation of biomass gasification technologies. Robust, on-line analytical methods are needed to investigate the fate of tar compounds when different measures for their reduction are applied. This work establishes an on-line UV-Vis method, based on a liquid quench sampling system, to monitor tar compounds in biomass gasification processes. Recorded spectra from the liquid phase were analyzed for their tar composition by means of a classical least squares (CLS) and partial least squares (PLS) approach. This allowed for the detection of UV-Vis active tar compounds with detection limits in the low part per million by volume (ppmV) region. The developed method was then applied to two case studies. The first involved a lab-scale reactor, intended to investigate the decomposition of a limited number of tar compounds across a catalyst. The second study involved a gas scrubber as part of a pilot scale wood gasification plant. Tar compound quantification results showed good agreement with off-line based reference methods (GC-FID) when the complexity of tar composition was limited. The two case studies show that the developed method can provide rapid, qualitative information on the tar composition for the purpose of process monitoring. In cases with a limited number of tar species, quantitative information about the individual tar compound concentrations provides an additional benefit of the analytical method.

Keywords: biomass gasification, on-line, tar, UV-Vis

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Authors: Dilek Zorlu Kaya, Sena Çenesiz, Utku Duran

Abstract:

Infectious pancreatic necrosis virus is a disease of great concern in aquaculture, causing mortality of 80 - 90% of the stocks in salmonid production. We aimed to investigate the efficacy of quercetin on oxidant and antioxidant parameters of infectious pancreatic necrosis virus, which is important for fish farming and economy in vitro. Quercetin experimental model was used in the cell culture of Oncorhynchus mykiss infected with infectious pancreatic necrosis virus. Malondialdehyde, ceruloplasmin, total oxidant capacity, total antioxidant levels, and glutathione-peroxidase were measured in the samples. As a result of the study, it was observed that quercetin can minimize the damage caused by scavenging free radicals in cells infected with infectious pancreatic necrosis virus. Thus, we think that an important development can be achieved for fish farming and the economy.

Keywords: IPNV, oncorhynchus mykiss, TAS, TOS, quercetin

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Authors: D. Baranova, E. Neborak

Abstract:

Polyphenols, particularly flavonoids like quercetin, fisetin, and kaempferol, have gained significant attention in nutrition due to their antioxidant, senolytic, and anti-inflammatory properties. These compounds are commonly found in various plant-based foods and are represented by diverse subclasses, each with unique health benefits. Understanding their absorption, metabolism, and bioactivity within the human body is crucial for unlocking their full potential. Quercetin, for instance, exists in multiple forms, impacting its solubility and absorption in the intestine. Its intake, often derived from sources like apples, is affected by cooking methods, with medium heat retaining its potency. Fisetin, also present in fruits and vegetables, demonstrates neuroprotective qualities and stability under varied conditions compared to quercetin. Similarly, kaempferol, found in fruits and vegetables, displays antioxidative effects but is influenced by cooking techniques, with specific methods preserving its polyphenolic content better. Overall, these polyphenols offer promising health benefits, yet their optimal dosage and specific dietary recommendations warrant further research to harness their full nutritional potential.

Keywords: polyphenols, flavonoids, absorption, quercetin, kaempferol, fisetin, senolytics, absorption, cooking method

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Authors: Monika Sogani, Zainab Syed, Adrian C. Fisher

Abstract:

Pollution of estrogenic compounds has caught the attention of researchers as the slight increase of estrogens in the water bodies has a significant impact on the aquatic system. They belong to a class of endocrine disrupting compounds (EDCs) and are able to mimic hormones or interfere with the action of endogenous hormones. The microbial electrochemical remediation system (MERS) is employed here for exploiting an electrophototrophic bacterium for evaluating the capacity of biodegradation of ethinylestradiol hormone (EE2) under anaerobic conditions with power generation. MERS using electro-phototrophic bacterium offers a tailored solution of wastewater treatment in a developing country like India which has a huge solar potential. It is a clean energy generating technology as they require only sunlight, water, nutrients, and carbon dioxide to operate. Its main feature that makes it superior over other technologies is that the main fuel for this MERS is sunlight which is indefinitely present. When grown in light with organic compounds, these photosynthetic bacteria generate ATP by cyclic photophosphorylation and use carbon compounds to make cell biomass (photoheterotrophic growth). These cells showed EE2 degradation and were able to generate hydrogen as part of the process of nitrogen fixation. The two designs of MERS were studied, and a maximum of 88.45% decrease in EE2 was seen in a total period of 14 days in the better design. This research provides a better insight into microbial electricity generation and self-sustaining wastewater treatment facilities. Such new models of waste treatment aiming waste to energy generation needs to be followed and implemented for building a resource efficient and sustainable economy.

Keywords: endocrine disrupting compounds, ethinylestradiol, microbial electrochemical remediation systems, wastewater treatment

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