Search results for: protease inhibition.

Authors: Memet Vezir Kahraman, Ferhat Sen

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This study aimed to develop polyelectrolyte structured antimicrobial food packaging materials that do not contain any antimicrobial agents. Cationic hydroxyethyl cellulose was synthesized and characterized by Fourier Transform Infrared, carbon and proton Nuclear Magnetic Resonance spectroscopy. Its nitrogen content was determined by the Kjeldahl method. Polyelectrolyte structured antimicrobial food packaging materials were prepared using hydroxyethyl cellulose, cationic hydroxyethyl cellulose, and sodium alginate. Antimicrobial activity of materials was defined by inhibition zone method (disc diffusion method). Thermal stability of samples was evaluated by thermal gravimetric analysis and differential scanning calorimetry. Surface morphology of samples was investigated by scanning electron microscope. The obtained results prove that produced food packaging materials have good thermal and antimicrobial properties, and they can be used as food packaging material in many industries.

Keywords: antimicrobial food packaging, cationic hydroxyethyl cellulose, polyelectrolyte, sodium alginate

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Authors: Parisa Farzaneh, Azade Harati

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Mushrooms, or macro-fungi, as an important superfood, contain many bioactive compounds, particularly bio-peptides. In this research, mushroom proteins were extracted by buffer or buffer plus salt (0.15 M), along with an ultrasound bath to extract the intercellular protein. As a result, the highest amount of proteins in mushrooms were categorized into albumin. Proteins were also hydrolyzed and changed into peptides through endogenous and exogenous proteases, including gastrointestinal enzymes. The potency of endogenous proteases was also higher in Agaricus bisporus than Terfezia claveryi, as their activity ended at 75 for 15 min. The blanching process, endogenous enzymes, the mixture of gastrointestinal enzymes (pepsin-trypsin-α-chymotrypsin or trypsin- α-chymotrypsin) produced the different antioxidant and antibacterial hydrolysates. The peptide fractions produced with different cut-off ultrafilters also had various levels of radical scavenging, lipid peroxidation inhibition, and antibacterial activities. The bio-peptides with superior bioactivities (less than 3 kD of T. claveryi) were resistant to various environmental conditions (pH and temperatures). Therefore, they are good options to be added to nutraceutical and pharmaceutical preparations or functional foods, even during processing.

Keywords: bio-peptide, mushrooms, gastrointestinal enzymes, bioactivity

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Authors: Mohammed Auwal Ibrahim, Aminu Mohammed

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Stigmasterol has previously been reported to possess antitrypanosomal activity using in vitro and in vivo models. However, the mechanism of antitrypanosomal activity is yet to be elucidated. In the present study, molecular docking was used to decipher the mode of interaction and binding affinity of stigmasterol to three known antitrypanosomal drug targets viz; adenosine kinase, ornithine decarboxylase and triose phosphate isomerase. Stigmasterol was found to bind to the selected trypanosomal enzymes with minimum binding energy of -4.2, -6.5 and -6.6 kcal/mol for adenosine kinase, ornithine decarboxylase, and triose phosphate isomerase respectively. However, hydrogen bond was not involved in the interaction of stigmasterol with all the three enzymes, but hydrophobic interaction seemed to play a vital role in the binding phenomenon which was predicted to be non-competitive like type of inhibition. It was concluded that binding to the three selected enzymes, especially triose phosphate isomerase, might be involved in the antitrypanosomal activity of stigmasterol but not mediated via a hydrogen bond interaction.

Keywords: antitrypanosomal, in silico, molecular docking, stigmasterol

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Authors: Sani Abubakar, Oumar Al-Mubarak Adoum

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

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

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Authors: Gulcan Sahal, Behzad Nasseri, Ali Akbar Ebrahimi, Isil Seyis Bilkay

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Proteus mirabilis strains which are natural colonizers of healthy individuals’ gastrointestinal tract are also known as common causes of catheter-associated urinary tract infections. Nowadays, as a result of an increased resistance to various antimicrobial drugs, there has been a growing interest in natural products. Therefore, the aim of this study is to investigate biofilm formation of P. mirabilis strains on lemongrass oil containing polycaprolactone nanofibers. Polycaprolactone nanofibers with different lemongrass oil concentrations were successfully prepared by electrospinning and biofilm formation of P. mirabilis on these nanofibers were determined by ‘Crystal Violet Staining Assay’. According to our results, polycaprolactone nanofibers with some lemongrass oil concentrations, decreased biofilm formation of P. mirabilis and this effect increased in parallel with the increase in lemongrass oil concentration. Our results indicate that, polycaprolactone nanofibers with some concentrations of lemongrass oil may provide a treatment against catheter-associated urinary tract infections by means of causing an inhibition on biofilm formation of P. mirabilis.

Keywords: anti-biofilm, biofilm formation, essential oils, nanofibers, proteus mirabilis

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Authors: Abdul Hameed, Muhammad Zaheer Ahmed, Salman Gulzar, Bilquees Gul, Jan Alam, Ahmad K. Hegazy, Abdel Rehman A. Alatar, M. Ajmal Khan

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Seed germination and recovery from salt stress of an annual halophyte Suaeda heterophylla (Kar. and Kir.) Bunge to different iso-osmotic concentrations (0, -0.46, -0.92, -1.38, -1.84, and -2.30 MPa) of NaCl and PEG-6000 at 15/25, 20/30 and 25/35°C in both 12-h temperature and light regimes and in complete darkness were studied. Maximum number of seeds germinated in distilled water and increase in concentrations of both NaCl and PEG-6000 decreased germination at all temperature regimes, light and dark conditions, with higher inhibition in NaCl than PEG-6000. Recovery of germination and viability of seeds were lower in NaCl than PEG-6000 both in the light and dark. Moderate alternate temperatures (20/30°C) and 12-h photoperiod were found to be the optimal for seed germination and recovery. Better seed germination of S. heterophylla when osmotic potential caused both by NaCl and PEG 6000 is lower, temperature regime of 20/30°C and light regime is for 12 h.

Keywords: seed germination, abiotic stresses, Suaeda heterophylla, molecular biology

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Authors: Sahar Nasr, Lin Li, Edwin Wang

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Bladder cancer (BLCA) is known as the 13th cause of death among cancer patients worldwide, and ~575,000 new BLCA cases are diagnosed each year. Urothelial carcinoma (UC) is the most prevalent subtype among BLCA patients, which can be categorized into muscle-invasive bladder cancer (MIBC) and non-muscle-invasive bladder cancer (NMIBC). Currently, various therapeutic options are available for UC patients, including (1) transurethral resection followed by intravesical instillation of chemotherapeutics or Bacillus Calmette-Guérin for NMIBC patients, (2) neoadjuvant platinum-based chemotherapy (NAC) plus radical cystectomy is the standard of care for localized MIBC patients, and (3) systematic chemotherapy for metastatic UC. However, conventional treatments may lead to several challenges for treating patients. As an illustration, some patients may suffer from recurrence of the disease after the first line of treatment. Recently, immune checkpoint therapy (ICT) has been introduced as an alternative treatment strategy for the first or second line of treatment in advanced or metastatic BLCA patients. Although ICT showed lucrative results for a fraction of BLCA patients, ~80% of patients were not responsive to it. Therefore, novel treatment methods are required to augment the ICI response rate within BLCA patients. It has been shown that the infiltration of T-cells into the tumor microenvironment (TME) is positively correlated with the response to ICT within cancerous patients. Therefore, the goal of this study is to enhance the infiltration of cytotoxic T-cells into TME through the identification of target genes within the tumor that are responsible for the non-T-cell inflamed TME and their inhibition. BLCA bulk RNA-sequencing data from The Cancer Genome Atlas (TCGA) and immune score for TCGA samples were used to determine the Pearson correlation score between the expression of different genes and immune score for each sample. The genes with strong negative correlations were selected (r < -0.2). Thereafter, the correlation between the expression of each gene and survival in BLCA patients was calculated using the TCGA data and Cox regression method. The genes that are common in both selected gene lists were chosen for further analysis. Afterward, BLCA bulk and single-cell RNA-sequencing data were ranked based on the expression of each selected gene and the top and bottom 25% samples were used for pathway enrichment analysis. If the pathways related to the T-cell infiltration (e.g., antigen presentation, interferon, or chemokine pathways) were enriched within the low-expression group, the gene was included for downstream analysis. Finally, the selected genes will be used to calculate the correlation between their expression and the infiltration rate of the activated CD+8 T-cells, natural killer cells and the activated dendric cells. A list of potential target genes has been identified and ranked based on the above-mentioned analysis and criteria. SUN-1 got the highest score within the gene list and other identified genes in the literature as benchmarks. In conclusion, inhibition of SUN1 may increase the tumor-infiltrating lymphocytes and the efficacy of ICI in BLCA patients. BLCA tumor cells with and without SUN-1 CRISPR/Cas9 knockout will be injected into the syngeneic mouse model to validate the predicted SUN-1 effect on increasing tumor-infiltrating lymphocytes.

Keywords: data analysis, gene expression analysis, gene identification, immunoinformatic, functional genomics, transcriptomics

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Authors: Rohit Thirumdas, Annapure U. S.

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Low-pressure air plasma is used to investigate the antioxidant properties and fatty acid composition of rice bran at different power levels (40 W and 60 W). We observed partial hydrogenation of rice bran oil after the treatment. The fatty acid composition analysis by gas chromatography showed an increase of 28.2% in palmitic acid and a 29.4% decrease in linoleic acid. FTIR spectrum shows no new peak formation, which confirms negligible amounts of trans-fatty acids. There is a decrease in peroxide value and iodine value, which can be correlated to an increase in saturated fatty acids. The total polyphenolic content was observed to be increased by 20.1% after the treatment. There is an increase in reducing power and DPPH % inhibition of rice bran due to plasma treatment. This study shows cold plasma treatment can be considered an alternative technology for the hydrogenation of oils, replacing traditional toxic processes.

Keywords: cold plasma, rice bran, fatty acid composition, hydrogenation of oils, antioxidant properties

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Authors: Amritanshu Shriwastav, Purnendu Bose

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Algal photo bioreactors were operated at incident light intensities of 0.24, 2.52 and 5.96 W L-1 to determine the impact of light on algal growth. Low specific Chlorophyll-a content of algae was a strong indicator of light induced stress on algal cells. It was concluded that long term operation of photo bioreactors in the continuous illumination mode was infeasible under the range of incident light intensities examined and provision of a dark period after each light period was necessary for algal cells to recover from light-induced stress. Long term operation of photo bioreactors in the intermittent illumination mode was however possible at light intensities of 0.24 and 2.52 W L-1. Further, the incident light intensity in the photo bioreactors was found to decline exponentially with increase in algal concentration in the reactor due to algal ‘self-shading’. This may be an important determinant for photo bioreactor performance at higher algal concentrations.

Keywords: Algae, algal growth, photo bioreactor, photo-inhibition, ‘self-shading’

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Authors: Pervin Basaran Akocak

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Food antimicrobials are compounds that are incorporated into food matrixes in order to cause death or delay the growth of spoilage or pathogenic microorganisms. As a result, microbiological deterioration is prevented throughout storage and food distribution. In this study, the effect of natural antimycotic natamycin (C33H47NO13, with a molecular mass of 665.725), a GRAS (Generally Recognized As Safe) commercial compound produced by different strains of Streptomyces sp., was tested against various fermented food contamination fungi and yeast species. At the concentration of 100 µg/ml, natamycin exhibited stronger antifungal activity against fungi than yeast species tested. The exposure time of natamycin for complete inhibition of the species tested were found to be between 100-180 min at 300-750 µg/ml concentration. SEM observations of fungal species demonstrated that natamycin distorted and damaged the conidia and hyphae by inhibiting spore germination and mycelial growth. Natamycin can be considered as a potential candidate in hurdle food treatments for preventing fungal and yeast invasion and resulting deterioration of fermented products.

Keywords: natamycin, antifungal, fermented food, food spoilage fungi

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Authors: Shweta Sinha, Mukesh Doble, Manju S. L.

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Pyrazole scaffold is an important group of compound in heterocyclic chemistry and is found to possess numerous uses in chemistry. Pyrazole derivatives are also known to possess important biological activities including antitumor, antimicrobial, antiviral, antifungal, anticancer and anti-inflammatory. Inflammation is associated with pain, allergy and asthma. Leukotrienes are mediators of various inflammatory and allergic disorders. 5-Lipoxygenase (5-LOX) is an important enzyme involved in the biosynthesis of leukotrienes and metabolism of arachidonic acid (AA) and thus targeted for anti-inflammation. In vitro inhibitory activity of pyrazol-3-yl thiazole 4-carboxylic acid derivatives is tested against enzyme 5-LOX. Most of these compounds exhibit good inhibitory activity against this enzyme. Binding mode study of these compounds is determined by computational tool. Further experiments are being done to understand the mechanism of action of these compounds in inhibiting this enzyme. To conclude, these compounds appear to be a promising target in drug design against 5-LOX.

Keywords: inflammation, inhibition, 5-lipoxygenase, pyrazole

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Authors: Mthokozisi B. C. Simelane

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Despite the various efforts by governmental and non-governmental organizations aimed at eradicating the disease, malaria is said to kill a child every 30 seconds. Traditional healers use different concoctions prepared from medicinal plants to treat malaria. In the quest to bio-prospect plant-derived triterpenes for anti-malaria activity, we report here the in vivo antiplasmodial activity of ursolic acid acetate (ursolic acid isolated from dichloromethane extract of Mimusops caffra was chemically modified to its acetate derivative). The transdermal administration of ursolic acid acetate (UAA) dose dependently showed complete inhibition of the parasites’ growth at the highest concentration of 400 mg/kg after 15 days of Plasmodium berghei infection. UAA prevented the in vitro aggregation of MDH but did not prevent the expression of PfHsp 70 in E. coli XL1 blue cells. It, however, enhanced PfHsp70 ATPase activity with the specific activity of 65 units (amount of phosphate released 73.83 nmolPi/min.mg). Ursolic acid acetate prevented the formation of hemozoin (60 ± 0.02% at 6 mg/ml). The results suggest that Ursolic acid acetate possesses potential anti-malaria properties.

Keywords: Mimusops caffra, ursolic acid acetate, hemozoin, Malaria

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Authors: Hanan Moawad, Naglaa M. Abd EL-Rahman

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Erwinia carotovora var. carotovora is the main cause of soft rot in potatoes. Hyphaene thebaica was studied for biocontrol of E. carotovora which inhibited growth of E. carotovora on solid medium, a comparative study of classical and ultrasound-assisted extractions of Hyphaene thebaica fruit. The use of ultrasound decreased significant the total time of treatment and increase the total amount of crude extract. The crude extract was subjected to determine the in vitro, by a bioassay technique revealed that the treatment of paper disks with ultrasound extraction of Hyphaene thebaica reduced the growth of pathogen and produced inhibition zones up to 38mm in diameter. The antioxidant activity of ultrasound-ethanolic extract of Doum fruits (Hyphaene thebaica) was determined. Data obtained showed that the extract contains the secondary metabolites such as Tannins, Saponin, Flavonoids, Phenols, Steroids, Terpenoids, Glycosides and Alkaloids.

Keywords: ultrasound, classical extract, biological control, Erwinia carotovora, Hyphaene thebaica

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Authors: K. Suresh, R. Arunkumar

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The objective of this study is to investigate the preparation of gramine nano suspension and protective effect of Gramine on the apoptosis of laryngeal cancer cells cell line (HEp-2 and KB). The growth inhibition rate of Hep-2 and KB cells in vitro were measured by MTT assay and apoptosis by, levels of reactive oxygen species, mitochondrial membrane potential, morphological changes and flowcytometry. Based on the results, we determined the effective doses of gramine as 127.23µm/ml for 24 hr and 119.81 µm/ml for 48hr in hep-2 cell line and 147.58 µm ml for 24 hr and 123.74µm µm/ml for 48hr in KB cell line. cytotoxicity effects of gramine were confirmed by treatment of HEp-2 cell and KB cell with IC50 concentration of gramine resulted in sequences of events marked by the enhance the apoptosis accompanied by loss of cell viability, modulation of reactive oxygen species and cell cycle arrest through the induction of G0/G1 phase arrest on HEp-2 cells. Our study suggests that the nanosuspension of gramine possesses the more cytotoxic effect of cancer cells and a novel candidate for cancer chemoprevention.

Keywords: apoptosis, HEp-2 cell line, KB cell line mitochondria, gramine, nanosuspension

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Authors: Rizwan H. Khan, Saima Nusrat

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Despite the fact that amyloid associated neurodegenerative diseases and non-neuropathic systemic amyloidosis have allured the research endeavors, as no curative drugs have been proclaimed up till now except for symptomatic cure. Therapeutic compounds which can diminish or disaggregate such toxic oligomers and fibrillar species have been examined and more are on its way. In the present study, we had reported an extensive biophysical, microscopic and computational study, revealing that L-3, 4-dihydroxyphenylalanine (L-Dopa) possess undeniable potency to inhibit heat induced human lysozyme (HL) amyloid fibrillation and also retain the fibril disaggregating potential. L-Dopa interferes in the amyloid fibrillogenesis process by interacting hydrophobically and also by forming hydrogen bonds with the amino acid residues found in amyloid fibril forming prone region of HL as elucidated by molecular docking results. L-Dopa also disaggregates the mature amyloid fibrils into some unorganised species. Thus, L-Dopa and related compounds can work as a promising inhibitor for the therapeutic advancement prospective against systemic amyloidosis.

Keywords: amyloids, disaggregation, human lysozyme, molecular docking

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Authors: Merve Akca

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Retrieval-induced forgetting (RIF) refers to the phenomenon that selective retrieval of some information impairs memory for related, but not previously retrieved information. Despite age differences in retrieval-induced forgetting regarding retrospective memory being documented, this research aimed to highlight age differences in RIF of the prospective memory tasks for the first time. By using retrieval-practice paradigm, this study comparatively examined RIF effects in retrospective memory and event-based prospective memory in young and old adults. In this experimental study, a mixed factorial design with age group (Young, Old) as a between-subject variable, and memory type (Prospective, Retrospective) and item type (Practiced, Non-practiced) as within-subject variables was employed. Retrieval-induced forgetting was observed in the retrospective but not in the prospective memory task. Therefore, the results indicated that selective retrieval of past events led to suppression of other related past events in both age groups but not the suppression of memory for future intentions.

Keywords: prospective memory, retrieval-induced forgetting, retrieval inhibition, retrospective memory

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Authors: Afifah Nur Aini, Elsa Mega Suryani, Betty Lukiaty

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Drymoglossum piloselloides or more commonly known as sisik naga fern is a member of Polipodiaceae Family that is abundant and widely distributed in nature. That being said, there hasn’t been many studies reporting about the benefits of this fern. The aim of this study was to find out the active compounds and antioxidant activity of water fraction extract of sisik naga leaves. The study will be able to optimize the use of this fern in the future. In this study, phytochemical test was done qualitatively by using Mayer, Dragendorff and Wagner reagent for alkaloid test; FeCl3 for phenolic test; Shinoda test for flavonoid; Liebermann-Burchard test for triterprnoid and Forth test for saponin. Antioxidant activity test was done by using 20D spectronic spectrophotometer to determine the percentage of DPPH free radical inhibition. The results showed that water fraction extract of sisik naga leaves contain phenolic and IC50 = 5.44 μg/ml. This means that sisik naga leaves can be used as an antioxidant.

Keywords: antioxidant activity test, dpph, phytochemical test, drymoglossum piloselloides

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Authors: Salmin K. Alshalmani, Nada H. Zobi, Ismaeel H. Bozakouk

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Marine organisms are potentially prolific sources of highly bio active secondary metabolites that might represent useful leads in the development of new pharmaceutical agents. The Libyan marine biodiversity including macroalgae remains partially unexplored in term of their potential bio activities. The phytochemical analysis of the alcoholic extracts of some commonly occurring seaweed Cystoseira compressa, enteromorpha intestinals, corallina, and Ulva lactuca and their evaluated for antibacterial activity by well diffusion assay were studied. Four different solvents namely water, ethanol 99 %, methanol 99 %, and methylated spirit 95 % were used for extraction. The phytochemical analysis revealed the presence of carbohydrates, steroids, tannin & phenols, saponins, proteins, and glycosides. The extracts were subjected for study of antibacterial activity. The zone of inhibition ranged between 8 to 16 mm in aqueous extract and up to 16 mm in methanol extract. The maximum activity (16 mm) was recorded from methanol extract of Ulva lactuca against Staphylococcus aureus and, minimum activity (8mm) recorded by Cystoseira compressa against S. aureus.

Keywords: macroalgae, phytochemicals, antibacterial activity, methanolic extract

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Authors: Abdullah Bilal Ozturk, Nil Acarali, Hediye Irem Ozgunduz, Hava Gizem Kandilci, Hanifi Sarac

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In this study, zeolite, shellac and different boron chemicals were used as additive to dye and effects were comprehensively investigated. Considering previous studies additive materials that had not used before were determined for produce dye with physical properties. Literature research about the materials provides determining easily sufficient amount of additive materials. Accessible of additives or yearly production amounts are become important issue at selection of materials. Zeolite and boron chemicals are suitable selection in that easy access and has large amount of production in our country. Previous research about boron chemicals shows they have flame retardant effect on textile materials besides numerous usage areas. Also, from previous research, shellac was used widely for protection and insulation of metallic materials. Zeolite added to dye to increase adhesive effect of dye. In this study, corrosion tests were applied to find out if there are positive effects of zeolite, shellac, and boron chemicals to dye’s physical properties.

Keywords: dye, corrosion, zeolite, shellac, boron

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Authors: Borys Stegniy, Anton Gerilovych, Oleksii Solodiankin, Vitaliy Bolotin, Anton Stegniy, Denys Muzyka, Claudio Afonso

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New APMV was isolated from white fronted goose in Ukraine. This isolate was tested serologically using monoclonal antibodies in haemagglutination-inhibition tests against APMV1-9. As the results obtained isolate showed cross reactions with APMV7. Following investigations were provided for the full genome sequencing using random primers and cloning into pCRII-TOPO. Analysis of 100 transformed colonies of E.coli using traditional sequencing gave us possibilities to find only 3 regions, which could identify by BLAST. The first region with the length of 367 bp had 70 % nucleotide sequence identity to the APMV 12 isolate Wigeon/Italy/3920_1/2005 at genome position 2419-2784. Next region (344 bp) had 66 % identity to the same APMV 12 isolate at position 4760-5103. The last region (365 bp) showed 71 % identity to Newcastle disease virus strain M4 at position 12569-12928.

Keywords: APMV, Newcastle disease virus, Ukraine, full genome sequencing

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Authors: Uthumporn Utra, Y. N. Shariffa, M. Maizura, A. S. Ruri

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This research is to study the utilization of pumpkin and winter melon as the main substrate for kefir fermentation in the production of pumpkin and winter melon-based fermented drinks. Optimized temperature and time were chosen for fermentation of pumpkin and winter melon. Physicochemical and microbiological evaluations were conducted to the end products: P (fermented pumpkin juice) and K (fermented winter melon juice). Ethanol content was detected at low concentration of 0.9% (v/wt) in P, and 1.0% (v/wt) in K. Level of glucose and fructose increased significantly (p < 0.05) in both fermented drinks when compared to unfermented pumpkin (CP) and winter melon (CK) juices. Total phenolic content in P & K was higher than CP and CK, while %DPPH inhibition of both decreased significantly. Total Lactobacilli counts in P & K were 8.9 and 7.88 log cfu/ml respectively, while acetic acid bacteria counts were 8.62 and 7.57 log cfu/ml respectively, yeast counts were 4.71 and 5 log cfu/ml, and no E.coli was detected in all samples. Sensory evaluation yield comparable properties in P & K. This concluded that pumpkin and winter melon fermented drinks inoculated by water kefir grains could be promising source of nutrients with probiotic potency.

Keywords: fermented drinks, functional beverage, kefir, pumpkin, winter melon

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Authors: Asma Ben Hmidene, Mizuho Hanaki, Kazuma Murakami, Kazuhiro Irie, Hiroko Isoda, Hideyuki Shigemori

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Type 2 diabetes mellitus (T2DM) and Alzheimer’s disease (AD) are characterized as a peripheral metabolic disorder and a degenerative disease of the central nervous system, respectively. It is now widely recognized that T2DM and AD share many pathophysiological features including glucose metabolism, increased oxidative stress and amyloid aggregation. Amyloid beta (Aβ) is the components of the amyloid deposits in the AD brain and while the component of the amyloidogenic peptide deposit in the pancreatic islets of Langerhans is identified as human islet amyloid polypeptide (hIAPP). These two proteins are originated from the amyloid precursor protein and have a high sequence similarity. Although the amino acid sequences of amyloidogenic proteins are diverse, they all adopt a similar structure in aggregates called cross-beta-spine. Add at that, extensive studies in the past years have found that like Aβ1-42, IAPP forms early intermediate assemblies as spherical oligomers, implicating that these oligomers possess a common folding pattern or conformation. These similarities can be used in the search for effective pharmacotherapy for DM, since potent therapeutic agents such as antioxidants with a catechol moiety, proved to inhibit Aβ aggregation, may play a key role in the inhibit the aggregation of hIAPP treatment of patients with DM. Tamarix gallica is one of the halophyte species having a powerful antioxidant system. Although it was traditionally used for the treatment of various liver metabolic disorders, there is no report about the use of this plant for the treatment or prevention of T2DM and AD. Therefore, the aim of this work is to investigate their protective effect towards T2DM and AD by isolation and identification of α-glucosidase inhibitors, with antioxidant potential, that play an important role in the glucose metabolism in diabetic patient, as well as, the polymerization of hIAPP and Aβ aggregation inhibitors. Structure-activity relationship study was conducted for both assays. And as for α-glucosidase inhibitors, their mechanism of action and their synergistic potential when applied with a very low concentration of acarbose were also suggesting that they can be used not only as α-glucosidase inhibitors but also be combined with established α-glucosidase inhibitors to reduce their adverse effect. The antioxidant potential of the purified substances was evaluated by DPPH and SOD assays. Th-T assay using 42-mer amyloid β-protein (Aβ42) for AD and hIAPP which is a 37-residue peptide secreted by the pancreatic β –cells for T2DM and Transmission electronic microscopy (TEM) were conducted to evaluate the amyloid aggragation of the actives substances. For α-glucosidase, p-NPG and glucose oxidase assays were performed for determining the inhibition potential and structure-activity relationship study. The Enzyme kinetic protocol was used to study the mechanism of action. From this research, it was concluded that polyphenols playing a role in the glucose metabolism and oxidative stress can also inhibit the amyloid aggregation, and that substances with a catechol and glucuronide moieties inhibiting amyloid-β aggregation, might be used to inhibit the aggregation of hIAPP.

Keywords: α-glucosidase inhibitors, amyloid aggregation inhibition, mechanism of action, polyphenols, structure activity relationship, synergistic potential, tamarix gallica

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Authors: Deepak Mohan, Sushma Sharma

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Non-Steroidal Anti-Inflammatory Drugs (NSAIDs) are a group of widely used drugs for the treatment of rheumatoid diseases and to relieve pain and inflammation due to their analgesic anti-pyretic and anti-inflammatory properties. The therapeutic and many of the toxic effects of NSAIDs result from reversible inhibition of enzymes in the cyclooxygenase (COX) group. In the present investigation the effect of the drug on the concentration of lipids, and on the activity of the enzymes i.e. acid and alkaline phosphatase, GOT, GPT and lipid peroxidase were studied. There was a significant enhancement in the activities of both acid and alkaline phosphatase after 21 days of treatment. Proportionate increase in the MDA contents was observed after different days of diclofenac treatment. Cellular damage in the liver resulted in decrease in the activity of both GOT (Glutamate oxaloacetate transaminase) and GPT (Glutamate pyruvate transaminase) in both low and high dose groups. Significant decrease in the liver contents was also observed in both dose groups.

Keywords: anti-inflammatory, cyclooxygenase, glutamate oxaloacetate transaminase, malondialdehyde

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Authors: Rajesh P.P., Md. Tabish Noori, Makarand M. Ghangrekar

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Methanogenic substrate loss is reported to be a major bottleneck in microbial fuel cell which significantly reduces the power production capacity and coulombic efficiency (CE) of microbial fuel cell (MFC). Nitroethane is found to be a potent inhibitor of hydrogenotrophic methanogens in rumen fermentation process. Influence of nitroethane pre-treated sewage sludge inoculum on suppressing the methanogenic activity and enhancing the electrogenesis in MFC was evaluated. MFC inoculated with nitroethane pre-treated anodic inoculum demonstrated a maximum operating voltage of 541 mV, with coulombic efficiency and sustainable volumetric power density of 39.85 % and 14.63 W/m3 respectively. Linear sweep voltammetry indicated a higher electron discharge on the anode surface due to enhancement of electrogenic activity while suppressing methanogenic activity. A 63 % reduction in specific methanogenic activity was observed in anaerobic sludge pre-treated with nitroethane; emphasizing significance of this pretreatment for suppressing methanogenesis and its utility for enhancing electricity generation in MFC.

Keywords: coulombic efficiency, methanogenesis inhibition, microbial fuel cell, nitroethane

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Authors: Ram Sharma, Esha Chatterjee, Santosh Kumar Guru, Kunal Nepali

Abstract:

A tractable anti-lung cancer agent was identified via the installation of a Ring C expanded synthetic analogue of the alkaloid vasicinone [7,8,9,10-tetrahydroazepino[2,1-b] quinazolin-12(6H)-one (TAZQ)] as a surface recognition part in the HDAC inhibitory three-component model. Noteworthy to mention that the candidature of TAZQ was deemed suitable for accommodation in HDAC inhibitory pharmacophore as per the results of the fragment recruitment process conducted by our laboratory. TAZQ was pinpointed through the fragment screening program as a synthetically flexible fragment endowed with some moderate cell growth inhibitory activity against the lung cancer cell lines, and it was anticipated that the use of the aforementioned fragment to generate hydroxamic acid functionality (zinc-binding motif) bearing HDAC inhibitors would boost the antitumor efficacy of TAZQ. Consistent with our aim of applying epigenetic targets to the treatment of lung cancer, a strikingly potent anti-lung cancer scaffold (compound 6) was pinpointed through a series of in-vitro experiments. Notably, the compounds manifested a magnificent activity profile against KRAS and EGFR mutant lung cancer cell lines (IC50 = 0.80 - 0.96 µM), and the effects were found to be mediated through preferential HDAC6 inhibition (IC50 = 12.9 nM). In addition to HDAC6 inhibition, the compounds also elicited HDAC1 and HDAC3 inhibitory activity with an IC50 value of 49.9 nM and 68.5 nM, respectively. The HDAC inhibitory ability of compound 6 was also confirmed from the results of the western blot experiment that revealed its potential to decrease the expression levels of HDAC isoforms (HDAC1, HDAC3, and HDAC6). Noteworthy to mention that complete downregulation of the HDAC6 isoform was exerted by compound 6 at 0.5 and 1 µM. Moreover, in another western blot experiment, treatment with hydroxamic acid 6 led to upregulation of H3 acK9 and α-Tubulin acK40 levels, ascertaining its inhibitory activity toward both the class I HDACs and Class II B HDACs. The results of other assays were also encouraging as treatment with compound 6 led to the suppression of the colony formation ability of A549 cells, induction of apoptosis, and increase in autophagic flux. In silico studies led us to rationalize the results of the experimental assay, and some key interactions of compound 6 with the amino acid residues of HDAC isoforms were identified. In light of the impressive activity spectrum of compound 6, a pH-responsive nanocarrier (hyaluronic acid-compound 6 nanoparticles) was prepared. The dialysis bag approach was used for the assessment of the nanoparticles under both normal and acidic circumstances, and the pH-sensitive nature of hyaluronic acid-compound 6 nanoparticles was confirmed. Delightfully, the nanoformulation was devoid of cytotoxicity against the L929 mouse fibroblast cells (normal settings) and exhibited selective cytotoxicity towards the A549 lung cancer cell lines. In a nutshell, compound 6 appears to be a promising adduct, and a detailed investigation of this compound might yield a therapeutic for the treatment of lung cancer.

Keywords: HDAC inhibitors, lung cancer, scaffold, hyaluronic acid, nanoparticles

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Authors: Sidra Islam, Moin Uddin, Mir A. Rouf

Abstract:

A wide variety of pathological disorders owing to hyperglycemic conditions involves structural rearrangements and condensations of proteins. The implication of methylglyoxal (MG) modified immunoglobulin G (IgG) in the onset and progression of diabetes type 2 (T2DM) is studied in the present study. Using biophysical and biochemical approaches MG was found to perturb the structure of IgG, effect its microenvironment and leads to aggregate formation. Furthermore, MG-IgG was found to be highly immunogenic inducing high titre antibodies in female rabbits. Clinical studies revealed the presence of circulating anti-MG-IgG antibodies as analyzed by direct binding ELISA. The circulating auto antibodies were highly specific for MG-IgG as revealed by inhibition ELISA. Thus it can be concluded that MG is a powerful agent with a high damaging potential. To IgG. It is highly capable of generating immune response that contributes to the immunopathology associated with diabetes. Dicarbonyl adducts may emerge as potential biomarkers for T2DM.

Keywords: immunogenicity, Immunoglobulin G, methylglyoxal, Type 2 Diabetes Mellitus

Procedia PDF Downloads 264

Authors: Miroslava Cuperlovic-Culf, Lipu Wang, Ketty Boyle, Nadine Makley, Ian Burton, Anissa Belkaid, Mohamed Touaibia, Marc E. Surrette

Abstract:

Metabolic changes are one of the major factors in the development of a variety of diseases in various species. Metabolism of agricultural plants is altered the following infection with pathogens sometimes contributing to resistance. At the same time, pathogens use metabolites for infection and progression. In humans, metabolism is a hallmark of cancer development for example. Quantified metabolomics data combined with other omics or clinical data and analyzed using various unsupervised and supervised methods can lead to better diagnosis and prognosis. It can also provide information about resistance as well as contribute knowledge of compounds significant for disease progression or prevention. In this work, different methods for metabolomics quantification and analysis from Nuclear Magnetic Resonance (NMR) measurements that are used for investigation of disease development in wheat and human cells will be presented. One-dimensional 1H NMR spectra are used extensively for metabolic profiling due to their high reliability, wide range of applicability, speed, trivial sample preparation and low cost. This presentation will describe a new method for metabolite quantification from NMR data that combines alignment of spectra of standards to sample spectra followed by multivariate linear regression optimization of spectra of assigned metabolites to samples’ spectra. Several different alignment methods were tested and multivariate linear regression result has been compared with other quantification methods. Quantified metabolomics data can be analyzed in the variety of ways and we will present different clustering methods used for phenotype determination, network analysis providing knowledge about the relationships between metabolites through metabolic network as well as biomarker selection providing novel markers. These analysis methods have been utilized for the investigation of fusarium head blight resistance in wheat cultivars as well as analysis of the effect of estrogen receptor and carbonic anhydrase activation and inhibition on breast cancer cell metabolism. Metabolic changes in spikelet’s of wheat cultivars FL62R1, Stettler, MuchMore and Sumai3 following fusarium graminearum infection were explored. Extensive 1D 1H and 2D NMR measurements provided information for detailed metabolite assignment and quantification leading to possible metabolic markers discriminating resistance level in wheat subtypes. Quantification data is compared to results obtained using other published methods. Fusarium infection induced metabolic changes in different wheat varieties are discussed in the context of metabolic network and resistance. Quantitative metabolomics has been used for the investigation of the effect of targeted enzyme inhibition in cancer. In this work, the effect of 17 β -estradiol and ferulic acid on metabolism of ER+ breast cancer cells has been compared to their effect on ER- control cells. The effect of the inhibitors of carbonic anhydrase on the observed metabolic changes resulting from ER activation has also been determined. Metabolic profiles were studied using 1D and 2D metabolomic NMR experiments, combined with the identification and quantification of metabolites, and the annotation of the results is provided in the context of biochemical pathways.

Keywords: metabolic biomarkers, metabolic network, metabolomics, multivariate linear regression, NMR quantification, quantified metabolomics, spectral alignment

Procedia PDF Downloads 334

Authors: Devasis Ghosh

Abstract:

The main hindrance to total cure of cancer is a) the failure to control continued production of cancer cells, b) its sustenance and c) its metastasis. This review study has tried to address this issue of total cancer cure in a more innovative way. A 10-pronged “CRAB METHOD”, a novel holistic scientific approach of Cancer treatment has been hypothesized in this paper. Apart from available Chemotherapy, Radiotherapy and Oncosurgery, (which shall not be discussed here), seven other points of interference and treatment has been suggested, i.e. 1. Efficient stress management. 2. Dampening of ATF3 expression. 3. Selective inhibition of Platelet Activity. 4. Modulation of serotonin production, metabolism and 5HT receptor antagonism. 5. Auxin, its anti-proliferative potential and its modulation. 6. Melatonin supplementation because of its oncostatic properties. 7. HDAC Inhibitors especially valproic acid use due to its apoptotic role in many cancers. If all the above stated seven steps are thoroughly taken care of at the time of initial diagnosis of cancer along with the available treatment modalities of Chemotherapy, Radiotherapy and Oncosurgery, then perhaps, the morbidity and mortality rate of cancer may be greatly reduced.

Keywords: ATF3 dampening, auxin modulation, cancer, platelet activation, serotonin, stress, valproic acid

Procedia PDF Downloads 268

Authors: Manal E. A Elhalwagy, Nadia Amin Abdulmajeed, Hanan S. Alnahdi, Enas N. Danial

Abstract:

Baron is herbicide includes (48% glyphosate) widely used in Egypt. The present study assesses the cytotoxic and genotoxic effect of baron on rats liver. Two groups of rats were treated orally with 1/10 LD 50, (275.49 mg kg -1) and 1/40 LD 50, (68.86 mg kg-1) glyphosate for 28 days compared with control group. Serum and liver tissues were taken at 14 and 28 days of treatment. An inhibition in Alanine aminotransferase (ALT) and aspartate aminotransferase (AST) activities were recorded at both treatment periods and reduction in total serum protein (TP) and albumin (ALB). However, non-significant changes in serum acetylcholinesterase (AChE). Elevation in oxidative stress biomarker malondyaldehyde (MDA) and the decline in detoxification biomarker total reduced glutathione (GSH), Glutathione S-transferase (GST) and superoxide dismutase (SOD) in liver tissues led to increase in percentage of DNA damage. Destruction in liver tissue architecture was observed . Although, Baron was classified in the safe category pesticides repeated exposure to small doses has great danger effect.

Keywords: glyphosate, liver toxicity, oxidative stress, DNA damage, commet assay

Procedia PDF Downloads 377

Authors: Venoos Iman, Suzita Mohd Noor, Syam Mohan, Mohamad Ibrahim Noordin

Abstract:

Girinimbine, a carbazole alkaloid was isolated from the stem bark and root of Murraya koenigii and its structure and purity was identified by HPLC and LC-MS. Here we report that Girinimbine strongly inhibit angiogenesis activity both in vitro and in vivo. MTT result showed that girinimbine inhibits cell proliferation of the HUVECS cell line in vitro. Result of endothelial cell invasion, migration, tube formation and wound healing assays also demonstrated significant time and does dependent inhibition by girinimbine. Moreover, girinibine mediates its anti-angiogenic activity through up- and down-regulation of angiogenic and anti-aniogenic proteins. Furthermore, anti-angiogenic potential of girinimbine was evidenced in vivo on zebrafish model. Girinimbine inhibited neo-vessels formation in zebrafish embryos during 24 hours exposure time. Together, these results demonstrated for the first time that girinimbine could effectively suppress angiogenesis and strongly suggest that it might be a novel angiogenesis inhibitor.

Keywords: anti-angiogenic, carbazole alkaloid, girinimbine, zebrafish

Procedia PDF Downloads 372