Search results for: enzymatic inhibition activity

Authors: L. Bendifallah, F. Acheuk, M. Djouabi, M. Oukili, R. Ghezraoui, W. Lakhdari, R. Allouane

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Nigella sativa L. (Renunculaceae) native to the Mediterranean region and Western Asia, Black cumin is grown to India, through Sudan and Ethiopia. It is widely cultivated in Egypt, the Middle East, Saudi Arabia, Turkey, Sudan, Afghanistan and Europe. It is among the most important medicinal plants in Algeria that is known for its antifungal and antimicrobial properties. Despite its plethora of uses for treating various diseases, it has garnered very little scientific interest so far, particularly in Algeria. For this study, the seeds of Algerian Nigella sativa L cultivated in the area of Magra (M’sila) in northern Algeria, were collected in summer. In such a propitious context, the aim of this study was to enhance Nigella sativa as a medicinal herb. The phytochemical screening methods are used. For their antimicrobial activity, extracts of tannin and polyphenols were screened against four pathogenic bacterial strains and two pathogenic yeast strains. The phytochemical analysis results showed a remarkable combination of chemical components including a high content in tannins, in flavonoïds, and in alkaloids. The tannins and the polyphenols have strong antimicrobial activity against all the species. The maximum zone of inhibition was noted for polyphenol and tannin extracts against Escerichia coli (14 mm, 12.33 mm) and an antifungic activity against Aspergillus niger (11.66 mm, 9 mm). These results indicate to some benefits of Nigella sativa seeds which can use to treatment the microbial infection.

Keywords: Nigella sativa, phytochemistry, antimicrobial activity, Algeria

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Authors: L. Bendifallah, F.Acheuk, M. Djouabi, M. Oukili, R. Ghezraoui, W. Lakhdari, R. Allouane

Abstract:

Nigella sativa L. (Renunculaceae) native to the Mediterranean region and Western Asia, Black cumin is grown to India, through Sudan and Ethiopia. It is widely cultivated in Egypt, the Middle East, Saudi Arabia, Turkey, Sudan, Afghanistan and Europe. It is among the most important medicinal plants in Algeria that is known for its antifungal and antimicrobial properties. Despite its plethora of uses for treating various diseases, it has garnered very little scientific interest so far, particularly in Algeria. For this study, the seeds of Algerian Nigella sativa L cultivated in the area of Magra (M’sila) in northern Algeria, were collected in summer. In such a propitious context, the aim of this study was to enhance Nigella sativa as a medicinal herb. The phytochemical screening methods are used. For their antimicrobial activity, extracts of tannin and polyphenols were screened against four pathogenic bacterial strains and two pathogenic yeast strains. The phytochemical analysis results showed a remarkable combination of chemical components including a high content in tannins, in flavonoïds, and in alkaloids. The tannins and the polyphenols have strong antimicrobial activity against all the species. The maximum zone of inhibition was noted for polyphenol and tannin extracts against Escerichia coli (14 mm, 12.33 mm) and an antifungic activity against Aspergillus niger (11.66 mm, 9 mm). These results indicate to some benefits of Nigella sativa seeds which can use to treatment the microbial infection.

Keywords: Algeria, antimicrobial activity, Nigella sativa, phytochemistry

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Authors: S. Korkut, M. S. Kilic, E. Erhan

Abstract:

In order to detect and quantify the phenolic contents of a wastewater with biosensors, two working electrodes based on modified Poly (Pyrrole) films were fabricated. Enzyme horseradish peroxidase was used as biomolecule of the prepared electrodes. Various phenolics were tested at the biosensor. Phenol detection was realized by electrochemical reduction of quinones produced by enzymatic activity. Analytical parameters were calculated and the results were compared with each other.

Keywords: carbon nanotube, phenol biosensor, polypyrrole, poly (glutaraldehyde)

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Authors: Vanitha Varadharaj, Vijalakshmi Krishnamurthy

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Annona squamosa Linn, commonly known as Sugar apple, belonging to the family Annonaceae, is said to show varied medicinal effects, including insecticide, antiovulatory and abortifacient. The alkaloid and flavonoids present in Annona squamosa leaf has proved to have antioxidant activity. The present work has been planned to investigate the effect of ethanolic leaf extract of Annona squamosa leaf on Den Induced wistar albino rats. The study was carried out to analyze the biochemical Parmeters like Total Proteins, Bilirubin, Enzymatic and Non –Enzymatic enzymes, Marker enzymes and Tumor markers in serum and also the histopathological studies in liver is carried out in control and DEN induced rats. Supplementation of ELAS (Ethanolic Leaf Extract Of Annona squamosa) reduced the liver weight and also reduced the tumour incidence. Chemoprevention group showed near normal values of bilirubin when compared with the control rats. Total protein was decreased in the cancer bearing group and on treatment with the extract the levels of protein were restored. Both in pre and post treatment group, the activities of enzymatic antioxidants such as superoxide dismutase, catalase, and Glutathione peroxidase were increased but in pre treated animals it was more effective than post treated animals. The non- enzymatic antioxidants such as vitamin C and vitamin E were brought back to normal level significantly in post and pre treated animals. Activities of marker enzymes such as SGOT, SGPT, ALP, γ GT were significantly elevated in the serum of cancer animals and the values returned to normal after treatment with the extract suggesting the hepato protective effect of the extract. Lipid peroxide was found to be elevated in the cancer induced group. This condition was brought back to the normal in the pre and post treated animals with ELAS. Histological examination also confirmed the anti- carcinogenic potential of ELAS, Cancer induced groups had a triple fold increase in their AFP values when compared to other groups. DEN treatment increased the level of AFP expression while ELAS partially counteracted the effect of it. So the scientific validation obtained from this study may pave way to many budding scientists to find new drugs from Annona squamosa for various ailments.

Keywords: annona squamosa, biochemical parmeters, cancer, leaf extract

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Authors: Nusrat Masood, Vijaya Dubey, Suaib Luqman

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Caspase 3, a member of cysteine-aspartic acid protease family, is an imperative indicator for cell death particularly when substantiating apoptosis. Thus, caspase 3 is an interesting target for the discovery and development of anticancer agent. We adopted a four level assessment of both terpenoids and flavonoids and thus experimentally performed the enzymatic assay in cell free system as well as in cancer cell line which was validated through real time expression and molecular interaction studies. A significant difference was observed with both the class of natural products indicating terpenoids as better activators of caspase 3 compared to flavonoids both in the cell free system as well as in cell lines. The expression analysis, activation constant and binding energy also correlate well with the enzyme activity. Overall, terpenoids had an unswerving effect on caspase 3 in all the tested system while flavonoids indirectly affect enzyme activity.

Keywords: Caspase 3, terpenoids, flavonoids, activation constant, binding energy

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Authors: H. Amellal-Chibane, N. Dehdouh, S. Ait-Kaki, F. Halladj

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Kefir is fermented milk that is produced by adding Kefir grains, consisting of bacteria and yeasts, to milk. The aim of this study was to investigate the antioxidant activity of the kefir supernatant and the raw milk. The Antioxidant activity assays of kefir supernatant and raw milk were evaluated by assessing the DPPH radical-scavenging activity. Kefir supernatant demonstrated high antioxidant activity (87.75%) compared to the raw milk (70.59 %). These results suggest that the Algerian kefir has interesting antioxidant activity.

Keywords: antioxidant activity, kefir, kefir supernatant, raw milk

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Authors: Woraprat Amnuaychaichana

Abstract:

Several medicinal plants are well known to contain active constituents such as flavonoids and phenolic compounds with are plausible candidates for therapeutic purposes. An infectious disease caused by microbial infection is the leading cause of death. Antibiotics are typically used to eradicate these microbes, but recent evidence indicates that they are developing antibiotic-resistant effects. This study focused on antimicrobial activities of Phyllanthus emblica and Gracilaria fisheri using the agar disk diffusion method and broth microdilution to determine the minimum inhibitory concentration (MIC) value. The extracts were screened against Staphylococcus aureus. Five concentrations of plant extracts were used to determine the minimum inhibitory concentration (MIC) by 2-fold dilution of plant extract. The results indicated that G. fisheri extract gave the maximum zones of inhibition of 11.7 mm against S. aureus while P. emblica showed no effects. The MIC values of G. fisheri extract against S. aureus was 500 µg/ml. To summarise, G. fisheri extracts demonstrated high efficacy of antibacterial activity against Gram-positive S. aureus, which may pave the way for developing a formulation containing this plant. G. fisheri extract should be subjected to additional investigation in order to determine the mechanism of action of its antimicrobial activity.

Keywords: antibacterial activity, Staphylococcus aureus, gracilaria fishery, Phyllanthus emblica

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Authors: Kira Rysakova, Vitaly Novikov

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An improved method of obtaining enzymatic collagen hydrolysate from the tissues of marine hydrobionts is proposed, which allows to obtain hydrolysate without pre-isolation of pure collagen. The method can be used to isolate enzymatic collagen hydrolysate from the waste of industrial processing of Red King crab and non-traditional objects - marine holothurias. Comparative analysis of collagen hydrolysates has shown the possibility of their use in a number of nutrient media, but this requires additional optimization of their composition and biological tests on wide sets of test strains of microorganisms.

Keywords: collagen hydrolysate, marine hydrobionts, red king crab, marine holothurias, enzymes, exclusive HPLC

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Authors: S. Hallal, Z. Chami, A. Hadji-Lehtihet, S. Sokhal-Boudella, A. Berhoune, L. Yargui

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Gaucher disease is the most common lysosomal storage in our population, it is due to a deficiency of β –glucosidase acid. The enzyme deficiency causes a pathological accumulation of undegraded substrate in lysosomes. This metabolic overload is responsible for a multisystemic disease with hepatosplenomegaly, anemia, thrombocytopenia, and bone involvement. Neurological involvement is rare. The laboratory diagnosis of Gaucher disease consists of phenotypic diagnosis by determining the enzymatic activity of β - glucosidase by fluorimetric method, a study by genotypic diagnosis in the GBA gene, limiting the search recurrent mutations (N370S, L444P, 84 GG); PCR followed by an enzymatic digestion. Abnormal profiles were verified by sequencing. Monitoring of treated patients is provided by the determination of chitotriosidase. Our experience spaning a period of 6 years (2007-2014) has enabled us to diagnose 78 patients out of a total of 328 requests from the various departments of pediatrics, internal medicine, neurology. Genotypic diagnosis focused on the entire family of 9 children treated at pediatric CHU Mustapha, which help define the clinical form; or 5 of them had type III disease, carrying the L444P mutation in the homozygous state. Three others were composite (N370/L444P) (N370S/other unintended mutation in our study), and only in one family no recurrent mutation has been found. This molecular study permits screening of heterozygous essential for genetic counseling.

Keywords: Gaucher disease, mutations, N370S, L444P

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Authors: A. Almohammedi, A. J. Hudson, N. M. Storey

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Following ischaemia/reperfusion injury, as in a myocardial infraction, cardiac myocytes undergo oxidative stress which leads to several potential outcomes including; necrotic or apoptotic cell death or dysregulated calcium homeostasis or disruption of the electron transport chain. Several studies have shown that nitric oxide donors protect cardiomyocytes against ischemia and reperfusion. However until present, the mechanism of cardioprotective effect of nitric oxide donor in isolated ventricular cardiomyocytes is not fully understood and has not been investigated before using Raman spectroscopy. For these reasons, the aim of this study was to develop a novel technique, pre-resonance Raman spectroscopy, to investigate the mechanism of cardioprotective effect of nitric oxide donor in isolated ventricular cardiomyocytes exposed to metabolic inhibition and re-energisation. The results demonstrated the first time that Raman microspectroscopy technique has the capability to monitor the metabolic inhibition of cardiomyocytes and to monitor the effectiveness of cardioprotection by nitric oxide donor prior to metabolic inhibition of cardiomyocytes. Metabolic inhibition and reenergisation were used in this study to mimic the low and high oxygen levels experienced by cells during ischaemic and reperfusion treatments. A laser wavelength of 488 nm used in this study has been found to provide the most sensitive means of observe the cellular mechanisms of myoglobin during nitric oxide donor preconditioning, metabolic inhibition and re-energisation and did not cause any damage to the cells. The data also highlight the considerably different cellular responses to metabolic inhibition to ischaemia. Moreover, the data has been shown the relationship between the release of myoglobin and chemical ischemia where that the release of myoglobin from the cell only occurred if a cell did not recover contractility.

Keywords: ex vivo biospectroscopy, Raman spectroscopy, biophotonics, cardiomyocytes, ischaemia / reperfusion injury, cardioprotection, nitric oxide donor

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Authors: Maxime Merheb, Rachel Matar

Abstract:

Retrieving ancient DNA sequences which in return permit the entire genome sequencing from fossils have extraordinarily improved in recent years, thanks to sequencing technology and other methodological advances. In any case, the quest to search for ancient DNA is still obstructed by the damage inflicted on DNA which accumulates after the death of a living organism. We can characterize this damage into three main categories: (i) Physical abnormalities such as strand breaks which lead to the presence of short DNA fragments. (ii) Modified bases (mainly cytosine deamination) which cause errors in the sequence due to an incorporation of a false nucleotide during DNA amplification. (iii) DNA modifications referred to as blocking lesions, will halt the PCR extension which in return will also affect the amplification and sequencing process. We can clearly see that the issues arising from breakage and coding errors were significantly decreased in recent years. Fast sequencing of short DNA fragments was empowered by platforms for high-throughput sequencing, most of the coding errors were uncovered to be the consequences of cytosine deamination which can be easily removed from the DNA using enzymatic treatment. The methodology to repair DNA sequences is still in development, it can be basically explained by the process of reintroducing cytosine rather than uracil. This technique is thus restricted to amplified DNA molecules. To eliminate any type of damage (particularly those that block PCR) is a process still pending the complete repair methodologies; DNA detection right after extraction is highly needed. Before using any resources into extensive, unreasonable and uncertain repair techniques, it is vital to distinguish between two possible hypotheses; (i) DNA is none existent to be amplified to begin with therefore completely un-repairable, (ii) the DNA is refractory to PCR and it is worth to be repaired and amplified. Hence, it is extremely important to develop a non-enzymatic technique to detect the most degraded DNA.

Keywords: ancient DNA, DNA barcodong, enzymatic repair, PCR

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Authors: Kang-Hyun Leem, Myung-Gyou Kim, Hye Kyung Kim

Abstract:

The prickly pear cactus (Opuntia ficus-indica) has a global distribution and have been used for medicinal benefits such as artherosclerosis, diabetes, gastritis, and hyperglycemia. However, very little information is currently available for their mechanism. The prikly pear variety Opuntia ficus-indica var. Saboten (OFS) is widely cultivated in Cheju Island, southwestern region of Korea, and used as a functional food. Present study investigated the effects of OFS on pancreatic β-cell function using pancreatic islet β cells (HIT cell). Alpha-glucosidase inhibition, glucose uptake, insulin secretion, insulin sensitivity, and pancreatic β cell proliferation were determined. The inhibitory effect of ethanol extract of OFS stem on α-glucosidase enzyme was measured in a cell free system. Glucose uptake was determined using fluorescent glucose analogue, 2-NBDG. Insulin secretion was measured by ELISA assay. Cell proliferation was measured by MTT assay. Ethanol extracts of OFS dose-dependently inhibited α-glucosidase activity as well as glucose uptake. Insulinotrophic effect of OFS extract was observed at high glucose media in pancreatic β-islet cells. Furthermore, pancreatic β cell regeneration was also observed.These results suggest that OFS mediates the antidiabetic activity mainly via α-glucosidase inhibition, glucose uptake, and improved insulin sensitivity.

Keywords: prickly pear cactus, Opuntia ficus-indica var. Saboten, pancreatic islet HIT cells, α-glucosidase, glucose uptake, insulinotrophic

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Authors: T. Sadunishvili, L. Kutateladze, T. Urushadze, R. Khvedelidze, N. Zakariashvili, M. Jobava, G. Kvesitadze

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Multiple repeated soil-climatic zones in Georgia determines the diversity of microorganisms. Hundreds of microscopic fungi of different genera have been isolated from different ecological niches, including some extreme environments. Biosynthetic ability of microscopic fungi has been studied. Trichoderma ressei, representative of the Ascomycetes secrete cellulolytic and xylanolytic enzymes that act in synergy to hydrolyze polysaccharide polymers to glucose, xylose and arabinose, which can be fermented to biofuels. The other mesophilic strains producing cellulases are Allesheria terrestris, Chaetomium thermophile, Fusarium oxysporium, Piptoporus betulinus, Penicillium echinulatum, P. purpurogenum, Aspergillus niger, A. wentii, A. versicolor, A. fumigatus etc. In the majority of the cases the cellulases produced by strains of genus Aspergillus usually have high β-glucosidase activity and average endoglucanases levels (with some exceptions), whereas strains representing Trichoderma have high endo enzyme and low β-glucosidase, and hence has limited efficiency in cellulose hydrolysis. Six producers of stable cellulases and xylanases from mesophilic and thermophilic fungi have been selected. By optimization of submerged cultivation conditions, high activities of cellulases and xylanases were obtained. For enzymes purification, their sedimentation by organic solvents such as ethyl alcohol, acetone, isopropanol and by ammonium sulphate in different ratios have been carried out. Best results were obtained with precipitation by ethyl alcohol (1:3.5) and ammonium sulphate. The yields of enzyme according to cellulase activities were 80-85% in both cases. Cellulase activity of enzyme preparation obtained from the strain Trichoderma viride X 33 is 126 U/g, from the strain Penicillium canescence D 85–185U/g and from the strain Sporotrichum pulverulentum T 5-0 110 U/g. Cellulase activity of enzyme preparation obtained from the strain Aspergillus sp. Av10 is 120 U/g, xylanase activity of enzyme preparation obtained from the strain Aspergillus niger A 7-5–1155U/g and from the strain Aspergillus niger Aj 38-1250 U/g. Optimum pH and temperature of operation and thermostability, of the enzyme preparations, were established. The efficiency of hydrolyses of different agricultural residues by the microscopic fungi cellulases has been studied. The glucose yield from the residues as a result of enzymatic hydrolysis is highly determined by the ratio of enzyme to substrate, pH, temperature, and duration of the process. Hydrolysis efficiency was significantly increased as a result of different pretreatment of the residues by different methods. Acknowledgement: The Study was supported by the ISTC project G-2117, funded by Korea.

Keywords: cellulase, xylanase, microscopic fungi, enzymatic hydrolysis

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Authors: Konstans Ruseva, Kristina Ivanova, Katerina Todorova, Margarita Gabrashanska, Tzanko Tzanov, Elena Vassileva

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Zwitterionic polymers (ZP) are well-known with their ultralow biofouling. They are successfully competing with poly(ethylene glycols) (PEG), which are considered as the “golden standard” in this respect. These unique properties are attributed to their strong hydration capacity, defined by the dipole-dipole interactions, arising between the ZP pendant groups as well as to the dipoles interaction with water molecules. Beside, ZP are highly resistant to bacterial adhesion thus ensuring an excellent anti-biofilm formation ability. Moreover, ZP are able to respond upon external stimuli such as temperature, pH, salt concentration changes which in combination with their anti-biofouling effect render this type of polymers as materials with a high potential in biomedical applications. The present work is focused on the development of zwitterionic hydrogels for efficient treatment of highly exudating and hard-to-heal chronic wounds. To this purpose, two types of ZP networks with different crosslinking degree were synthesized - polysulfobetaine (PSB) and polycarboxybetaine (PCB) ones. They were characterized in terms of their physico-mechanical properties, e.g. microhardness, swelling ability, smart behaviour. Furthermore, the potential of ZP networks to resist biofilm formation towards Staphylococcus aureus and Escherichia coli was studied. Their ability to reduce the high levels of myeloperoxidase and metalloproteinase, two enzymes that are part of the chronic wounds enviroenment, was revealed. Moreover, the in vitro cytotoxic assessment of PSB and PCB networks along with their in vivo performance in rats was also studied to reveal their high biocompatibility.

Keywords: absorption properties, biocompatibility, enzymatic inhibition activity, wound healing, zwitterionic polymers

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Authors: Tania Camarillo Contreras, Yana Kuchirko

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Women’s sexuality, despite it being a core part of human functioning, has historically been stigmatized, silenced, and regulated and silenced across many cultures. The regulation of women’s bodies and desires has often been accomplished via gender ideologies and norms that ascribe power to men over women. Within Latino communities, gender ideologies like marianismo provide scripts by which women are expected to adhere submissiveness, purity, and putting others’ needs before their own. Prior work on sexuality-related topics among Latinas has almost exclusively examined the roles of risky behavior, partner violence, and gender roles on psychological and health outcomes. it know little about positive aspects of Latinas’ sexuality, such as their perspectives on sexual excitation and inhibition. Moreover, we know little about Latina’s sexuality in relation to marianismo. In this study, it ask the following questions (1) What are Latina’s perspectives on sexual excitation/inhibition? Do they vary by demographic variables (e.g., education, religiosity); (2) Does endorsement of marianismo among Latina women predict their perspectives on sexual excitation/sexual inhibition? and (3) Does endorsement of double standard (mediator variable) mediate the relation between marianismo (Independent) and sexual excitation/sexual inhibition? The results of this study shed light on effects of culturally specific gender ideologies like marianismo on women’s sexualities and have implications for culturally informed and gender-affirming policies seeking to better support Latinas’ sexual health.

Keywords: cultural beliefs, latinas, marianismo, sexuality, sexual inhibition

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Authors: Zerrin Erginkaya, Gözde Konuray

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In this study, antimicrobial effect of Greek clover was determined with usage of MIC (minimum inhibition concentration) and agar diffusion method. Moreover, pH, water activity and microbial change were determined during storage of fenugreek paste. At first part of our study, microbial load of spices was evaluated. Two different fenugreek pastes were produced with mixing of Greek clover, spices, garlic and water. Fenugreek pastes were stored at 4 °C. At the second part, antimicrobial effect of Greek clover was determined on Escherichia coli, Staphylococcus aureus, Bacillus subtilis, Debaryomyces hansenii, Aspergillus parasiticus, Candida rugosa, Mucor spp., when the concentrations of Greek clover were 8%, 12% and 16%. According to the results obtained, mould growth was determined at 15^th and 30^th days of storage in first and second fenugreek samples, respectively. Greek clover showed only antifungal effect on Aspergillus parasiticus at previously mentioned concentrations.

Keywords: antimicrobial, fenugreek, Greek clover, minimum inhibition concentration

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Authors: Suthida Panwong, Jeeraporn Pekkoh, Yingmanee Tragoolpua, Aussara Panya

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Dengue virus (DENV) infection is a major public health problem in many countries, especially in tropical and subtropical countries. DENV infection causes dengue fever that can progress to serious conditions of dengue hemorrhagic fever (DHF) or dengue shock syndrome (DSS), relevant to a high risk of mortality. However, there are no effective treatments available against the manifestation and fatalities. Currently, natural extracts have been widely used for the treatment of infectious diseases due to their safety, non-accumulation in the body, or lower side effects. Chlorella spp. is a microalgae with anti-viral activity, but there is not much report to support its ability to inhibit DENV infection. Thus, this study aimed to investigate the inhibitory effect of ethanolic extract from Chlorella sp. AARL G049, which was explored in Thailand on inhibition of DENV-2 infection. The inhibitory effect on viral infection was assessed using a foci-forming assay (FFA), which revealed that a concentration of 125 µg/mL could inhibit viral infection in Vero cells by 75.45±8.06% when treated at the same time as DENV-2 infection. Moreover, the extract at an equal concentration effectively reduced viral protein synthesis by 90.51±5.48% when assessed in human cell lines using enzyme-linked immunosorbent assay (ELISA). Concordantly, the number of infected cells after treatment was reduced as measured by immunofluorescent assay (IFA). Therefore, the finding of this study supports the potential use of Chlorella sp. extract to suppress DENV infection.

Keywords: viral infection, flavivirus, treatment, natural extract

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Authors: A. N. Ukwuani, M. G. Abubakar, S. W. Hassan

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Grewia crenata is used locally in the treatment of fractured bones, wound healing and inflammatory conditions. The anti-inflammatory activity of hydromethanolic extract of G. crenata leaves was investigated using egg albumin induced-hind paw oedema model in albino rat. The extract produced a time-dependent inhibition of egg albumin induced-hind paw oedema at 30th minutes up to 150th minutes in all the groups compared to the control. Significant reduction (p<0.05) of hind paw oedema was observed 150 minutes after egg albumin injection. The percentage inhibition produced by the extract at 200 mg/kg (22.1%) was comparable to that produced by 10 mg/kg indomethacin (24.9%) at the 150th minutes of post-egg albumin injection. Preliminary qualitative phytochemical analysis revealed the presence of saponins, steroids, flavonoids, anthraquinones and glycosides. The results obtained in this study suggest that Grewia crenata can be a potential source of anti-inflammatory agent and validates its use in the treatment of inflammatory conditions.

Keywords: Grewia crenata, anti-inflammatory, hind paw, oedema

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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: Alemu Tadesse Feroche

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In this study, some 2, 3 distributed quinazoline -4 (3H) - one derivative were synthesized using a three-step synthetic route. They were obtained in a good yield (59.5-85%) by applying different chemical reactions like cyclization and condensation reactions. The chemical structure of the final compounds was also verified by spectroscopic methods (IR, ¹HNMR) and elemental microanalysis. The in vivo antimalarial activity of these compounds on P. berghei infected mice was found to be moderate to high at an oral dose of 0.04846 mmol/kg /day. This is equal to 25 mg/kg of chloroquine phosphate, which causes 100% inhibition of the parasite. It is worth mentioning that most active compounds (E) -3 Phenyl -2- [2- (pyridine -4- yl) vinyl] -4 (3H) -quinazolinone IVa (64.02%, (E)-2-[2-(4 - Hydroxy-3 - methoxystyryl) - vinyl) -3 - phenyl -4 (3H ) - quinazolinone IVc (77.25%) and (E)-2 –[2 –(Pyridin -4-yl) –vinyl] -3 phenenylamine -4(3H) quinazolinone IVe (73.54%) showed a dose-dependent increase in present suppression in antimalarial activities. Furthermore, the synthesized compounds were screened for their in vitro antileishmanial activity against L. aethiopica isolate (CL/039/09). All tested compounds (IVa (0.03766 ug/ml), IVb (0.00538 ug/ml, IVc (0.00412 ug/ml, IVd (0.00110 ug/ml), IVe (0.03017 ug/ml) and IVf (0.03894 ug/ml)) showed excellent potency that is much better than amphotericin B (IC50 = 0,04359 ug/ml). The results of acute toxicity indicated that all test compounds (IVa –IVf) proved to be nontoxic and well tolerated by the experimental animals up to 300 mg/kg in oral and 140 mg/kg in parental studies.

Keywords: 4(3H)-quinazolinone, in vivo antimalarial activity, in vitro antileishmanial activity, acute toxicity

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Authors: Paweł Stączek, Tomasz Plech, Aleksandra Strzelczyk, Katarzyna Dzitko, Monika Wujec, Edyta Kuśmierz, Piotr Paneth, Agata Paneth

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In this contribution, we will describe the inhibitory potency of nine thiosemicarbazide derivatives against bacterial type IIA topoisomerases, their antibacterial profile, and molecular modeling evaluation. We have found that one of the tested compounds, 4-benzoyl-1-(2-methyl-furan-3-ylcarbonyl) thiosemicarbazide, remarkably inhibits the activity of S. aureus DNA gyrase with the IC50 below 5 μM. Besides, this compound displays antibacterial activity on Staphylococcus spp. and E. faecalis at non-cytotoxic concentrations in mammalian cells, with minimal inhibitory concentrations (MICs) values at 25 μg/mL. Based on the enzymatic and molecular modeling studies we propose two factors, i.e. geometry of molecule and hydrophobic/hydrophilic balance as important molecular properties for developing thiosemicarbazide derivatives as potent Staphylococcus aureus DNA gyrase inhibitors.

Keywords: bioactivity, drug design, topoisomerase, molecular modeling

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Authors: Ririn Lestari Sri Rahayu, Mustofa Ahda

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The use of synthetic antioxidants often causes a negative effect on health and increases the incidence of carcinogenesis. Development of the natural antioxidants should be investigated. However, natural antioxidants have a low toxicity and are safe for human consumption. Ethanol extract of mangosteen rind (Garcinia mangostana) contains natural antioxidant compounds that have various pharmacological activities. Antioxidants from the ethanol extract of mangosteen rind have free radicals scavenging activities. The scavenging activity of ethanol extract of mangosteen rind was determined by DPPH method. The phenolic compound from the ethanol extract of mangosteen rind is determined with Folin-Ciocalteu method. The results showed that the absolute ethanol extract of mangosteen rind has IC₅₀ of 40.072 ug/mL. The correlation of total phenols content with free radical scavenging activity has an equation y: 5.207x + 205.51 and determination value (R²) of 0.9329. Total phenols content from the ethanol extract of mangosteen rind has a good correlation with free radicals scavenging activity of DPPH.

Keywords: Antioxidant, Garcinia mangostana, Inhibition concentration 50%, Phenolic.

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Authors: Afshin Farahbakhsh, Hoda Khodadadi

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In this paper, we compare five methods of biological fuel cell fabrication by combining a Shewanella oneidensis microbial anode and a laccase-modified air-breathing cathode. As a result of biofuel cell laccase with graphite nanofibers, carbon surface (PAMAN) on the pt/hpg electrode, graphite sheets MWCNT and with (PG) and (MWCNT) showed, respectively. Describes methods for creating controllable and reproducible bio-anodes and demonstrates the versatility of hybrid biological fuel cells. The laccase-based biocathodes prepared either with the crude extract or with the purified enzyme can provide electrochemically active and stable biomaterials. The laccase-based biocathodes prepared either with the crude extract or with the purified enzyme can provide electrochemically active and stable biomaterials. When the device was fed with transdermal extracts, containing only 30μM of glucose, the average peak power was proportionally lower (0.004mW). The result of biofuel cell with graphite nanofibers showed the enzymatic fuel cell reaches 0.5 V at open circuit voltage with both, ethanol and methanol and the maximum current density observed for E2electrode was 228.94mAcm.

Keywords: enzymatic electrode, fuel cell, immobilization, laccase

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Authors: Sifi Ibrahim, Benaddou Fatima Zohra, Yousfi Mohamed

Abstract:

The Marrubium deserti and Ammodaucus leucotrichus L. an Algerian endemic species, has several applications in traditional medicine for example as a remedy for asthma and diabetes, and was found to have antibacterial properties. In this work, an antioxidant and antimicrobial activities was performed on phenolic extracts of Marrubium deserti, Ammodaucus leucotrichus plants. The yield of methanol maceration of these plants is 12.4% and 20.4% respectively. The content of total polyphenols, flavonoids and anthocyanin in methanolic extracts, are varied between 19.52±1.88 and 59.24±3.45 mg/g gallic acid equivalent, and 2.08±0.29 to 1.46±0.39 mg/g quercetin equivalent, and 0.395 to 1.934µmol/g respectively. The total chlorophylls and carotenoids were be ranged from 0.149±0.20 to 1.537±0.20 g/ml and 1.537±0.20 to 0.149 ± 0.20 g/ml, respectively. According to DPPH and FRAP test, the values of EC50 was shows a higher activity of Marrubium deserti than Ammodaucus leucotrichus with EC50 values (DPPH) were 34.53±0.71 μg/mL and 258.60±15.67 mg/ml respectively. The TEAC values of FRAP test was a highly superior for Marrubium deserti 209.66±0.26 mg Equivalent Trolox/g dry residue than Ammodaucus leucotrichus 45.88±2.93 mg Trolox Equivalent/g dry residue. The antimicrobial activity against nine strains of bacteria (Staphylococcus aureus(+), Staphylococcus aureus (-), Bacillus cereus, Enterococcus faecalis, Escherichia coli, Pseudomonas aeruginosa, Klebsiella pneumoniae and Salmonella typhi), was showed that the tested extracts are a significant antibacterial activity with inhibition zones ranging from 10 to 50 mm. the value of CMI were ranging from 0.89 to 14.29 mg/ml.

Keywords: phenolic extract, antioxidant activity, antimicrobial activity, Marrubium deserti, Ammodaucus leucotrichus

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Authors: M. Doyeni, S. Suproniene, V. Tilvikiene

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Agricultural wastes contribute significantly to global climate change through greenhouse gas emissions if not adequately recycled and sustainably managed. A recurring agricultural waste is livestock wastes that have consistently served as feedstock for biogas systems. The objective of this study was to access the influence of digestate fertilization on soil microbial activity and greenhouse gas emissions in agricultural fields. Wheat (Triticum spp. L.) was fertilized with different types of animal wastes digestates (organic fertilizers) and mineral nitrogen (inorganic fertilizer) for three years. The 170 kg N ha⁻¹ presented in digestates were split fertilized at an application rate of 90 and 80 kg N ha⁻¹. The soil microorganism activity could be predicted significantly using the dehydrogenase activity and soil microbial biomass carbon. By combining the two different monitoring approaches, the different methods applied in this study were sensitive to enzymatic activities and organic carbon in the living component of the soil organic matter. The emissions of greenhouse gasses (carbon dioxide (CO₂), methane (CH₄), and nitrous oxide (N₂O) were monitored directly by a static chamber system. The soil and environmental variables were measured to determine their influence on greenhouse gas emissions. Emission peaks was observed in N₂O and CO₂ after the first application of fertilizers with the emissions flattening out over the cultivating season while CH₄ emission was negligible with no apparent patterns observed. Microbial biomass carbon and dehydrogenase activity were affected by the fertilized organic digestates. A significant difference was recorded between the control and the digestate treated soils for the microbial biomass carbon and dehydrogenase. Results also showed individual and cumulative emissions of CO₂, CH₄ and N₂O from the digestates were relatively low suggesting the digestate fertilization can be an efficient method for improving soil quality and reducing greenhouse gases from agricultural sources in temperate climate conditions.

Keywords: greenhouse gas emission, manure digestate, soil microbial activity, yield

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Authors: T. Büyüksırıt, H. Kuleaşan

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Natural antimicrobials are used to preserve foods that can be found in plants, animals, and microorganisms. Antimicrobial substances are natural or artificial agents that produced by microorganisms or obtained semi/total chemical synthesis are used at low concentrations to inhibit the growth of other microorganisms. Food borne pathogens and spoilage microorganisms are inactivated by the use of antagonistic microorganisms and their metabolites. Yeasts can produce toxic proteins or glycoproteins (toxins) that cause inhibition of sensitive bacteria and yeast species. Antimicrobial substance producing phenotypes belonging different yeast genus were isolated from different sources. Toxins secreted by many yeast strains inhibiting the growth of other yeast strains. These strains show antimicrobial activity, inhibiting the growth of mold and bacteria. The effect of antimicrobial agents produced by yeasts can be extremely fast, and therefore may be used in various treatment procedures. Rapid inhibition of microorganisms is possibly caused by microbial cell membrane lipopolysaccharide binding and in activation (neutralization) effect. Antimicrobial agents inhibit the target cells via different mechanisms of action.

Keywords: antimicrobial agents, yeast, toxic protein, glycoprotein

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Authors: Deepak Mohan, Sushma Sharma, Mohammad Asif

Abstract:

Diclofenac sodium being one of the most common non-steroidal anti-inflammatory drugs is normally used as painkiller and to reduce inflammation. The drug is known to alter the enzymatic activities of acid and alkaline phosphatase, glutamate oxaloacetate transaminase and glutamate pyruvate transaminases. The drug also results in change in the concentration of proteins and lipids in the body. The present study is an attempt to study different biochemical changes electrophoretically due to administration of different doses of diclofenac (4mg/kg/body weight and 14mg/kg/body weight) on liver and testes of mice from 7-28 days of investigation. Homogenization of the tissue was done, supernatant separated was loaded in the gel and native polyacrylamide gel electrophoresis was conducted. Diclofenac administration resulted in alterations of all these biochemical parameters which were observed in native polyacrylamide gel electrophoretic studies. The severe degenerative changes as observed during later stages of the experiment showed correlation with increase or decrease in the activities of all the enzymes studied in the present investigation. Image analysis of gel in liver showed a decline of 7.4 and 5.3 % in low and high dose group after 7 days whereas a decline of 9.6 and 7.5% was registered after 28 days of investigation. Similar analysis for testis also showed an appreciable decline in the activity of alkaline phosphatase after 28 days. Gel analysis of serum was also performed to find a correlation in the enzymatic activities between the tissue and blood.

Keywords: diclofenac, inflammation, polyacrylamide, phosphatase

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Authors: Thomas F. Ducey, Kristin M. Trippe, James A. Ippolito, Jeffrey M. Novak, Mark G. Johnson, Gilbert C. Sigua

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The Oronogo-Duenweg mining belt –approximately 20 square miles around the Joplin, Missouri area– is a designated United States Environmental Protection Agency Superfund site due to lead-contaminated soil and groundwater by former mining and smelting operations. Over almost a century of mining (from 1848 to the late 1960’s), an estimated ten million tons of cadmium, lead, and zinc containing material have been deposited on approximately 9,000 acres. Sites that have undergone remediation, in which the O, A, and B horizons have been removed along with the lead contamination, the exposed C horizon remains incalcitrant to revegetation efforts. These sites also suffer from poor soil microbial activity, as measured by soil extracellular enzymatic assays, though 16S ribosomal ribonucleic acid (rRNA) indicates that microbial diversity is equal to sites that have avoided mine-related contamination. Soil analysis reveals low soil organic carbon, along with high levels of bio-available zinc, that reflect the poor soil fertility conditions and low microbial activity. Our study looked at the use of several materials to restore and remediate these sites, with the goal of improving soil health. The following materials, and their purposes for incorporation into the study, were as follows: manure-based biochar for the binding of zinc and other heavy metals responsible for phytotoxicity, locally sourced biosolids and compost to incorporate organic carbon into the depleted soils, effective microorganisms harvested from nearby pristine sites to provide a stable community for nutrient cycling in the newly composited 'soil material'. Our results indicate that all four materials used in conjunction result in the greatest benefit to these mine-impacted soils, based on above ground biomass, microbial biomass, and soil enzymatic activities.

Keywords: locally effective microorganisms, biochar, remediation, reclamation

Procedia PDF Downloads 215

Authors: Abdelkader H. El Debani, Huda Gargoum, Awad G. Abdellatif

Abstract:

The aim of this study is to investigate analgesic and the anti-inflammatory effects Camel Thorn Extract (CTE) in rodents. Male albino mice weighing 20-25 gm. were divided into different groups each of 8 mice. The control was given normal saline i. p., the first group was given normal saline i. p. the 2nd, 3rd, 4th, groups received different doses of CTE (330, 660, and 1300 mg/kg) respectively and the 6th group received 5mg/kg of morphine i. p. All groups (except the control group) were given acetic acid 40 min after receiving the different treatment. The number of writhes was recorded 5 min after acetic acid injection for 15 min and the % of inhibition of writhing were calculated. Different groups of rats weighing 180- 220 gm., were divided into three groups each of 5 rats. At the beginning, the volumes of the right and left paw in animals were measured by using of the plethysmometer. The 1st group was given 660 mg /kg i. p. of CTE, the 2nd group received indomethacin (5 mg/kg i. p.). One hour later, edema was induced by sub planter injection of 0.1 ml of 1 % freshly prepared suspension of carrageenan into the right hind paws of the rats. The volume of the injected paws and contra-lateral paws were measured at 0, 0.5, 1, 2, 3, 4, and 5 hours using plethysmometer. The volume of the left paw of the rat was subtracted from the volume of the right paw of the same animal. Our results showed that 330,660 and 1300 mg/kg produced 14, 49 and 84%of inhibition of writhes, indicating that CTE has a strong analgesic activity. Our data also showed that the % of inhibition of edema at 30, 60, 120, 180, and 240 min was 14,51,71,61, and 56% in the animals given camel thorn extract whereas these figures in animals given endomethacin were 14, 24, 54, 52, and 54%. These results indicate that camel thorn has anti-inflammatory activities. The mechanism of analgesic and anti-inflammatory activities needs further investigations.

Keywords: camel thorn, imdomethacin, morphine, pharmaceutical medicine

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Authors: G. V. Novikov, V. S. Sivozhelezov, S. S. Kolesnikov, K. V. Shaitan

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The study reports about the influence of binding of orthosteric ligands as well as point mutations on the conformational dynamics of β-2-adrenoreceptor. Using molecular dynamics simulation we found that there was a little fraction of active states of the receptor in its apo (ligand free) ensemble corresponded to its constitutive activity. Analysis of MD trajectories indicated that such spontaneous activation of the receptor is accompanied by the motion in intracellular part of its alpha-helices. Thus receptor’s constitutive activity directly results from its conformational dynamics. On the other hand the binding of a full agonist resulted in a significant shift of the initial equilibrium towards its active state. Finally, the binding of the inverse agonist stabilized the receptor in its inactive state. It is likely that the binding of inverse agonists might be a universal way of constitutive activity inhibition in vivo. Our results indicate that ligand binding redistribute pre-existing conformational degrees of freedom (in accordance to the Monod-Wyman-Changeux-Model) of the receptor rather than cause induced fit in it. Therefore, the ensemble of biologically relevant receptor conformations is encoded in its spatial structure, and individual conformations from that ensemble might be used by the cell in conformity with the physiological behaviour.

Keywords: seven-transmembrane receptors, constitutive activity, activation, x-ray crystallography, principal component analysis, molecular dynamics simulation

Procedia PDF Downloads 254