Search results for: p-gp inhibition

Authors: S. N. T. I. Sampath, J. M. S. Jayasinghe, A. P. Attanayake, V. Karunaratne

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Diabetes mellitus is one of the major public health posers throughout the world today that incidence and associated with increasing mortality. Insufficient regulation of the blood glucose level might be serious effects for health and its necessity to identify new therapeutics that have ability to reduce hyperglycaemic condition in the human body. Even though synthetic antidiabetic drugs are more effective to control diabetes mellitus, there are considerable side effects have been reported. Thus, there is an increasing demand for searching new natural products having high antidiabetic activity with lesser side effects. The purposes of the present study were to evaluate different physical parameters and in-vitro and in-vivo antidiabetic potential of the selected combined medicinal plant extracts mixture composed of leaves of Murraya koenigii, cloves of Allium sativum, fruits of Garcinia queasita and seeds of Piper nigrum. The selected plants parts were mixed and ground together and extracted sequentially into the hexane, ethyl acetate and methanol. Solvents were evaporated and they were further dried by freeze-drying to obtain a fine powder of each extract. Various physical parameters such as moisture, total ash, acid insoluble ash and water soluble ash were evaluated using standard test procedures. In-vitro antidiabetic activity of combined plant extracts mixture was screened using enzyme assays such as α-amylase inhibition assay and α-glucosidase inhibition assay. The acute anti-hyperglycaemic activity was performed using oral glucose tolerance test for the streptozotocin induced diabetic Wistar rats to find out in-vivo antidiabetic activity of combined plant extracts mixture and it was assessed through total oral glucose tolerance curve (TAUC) values. The percentage of moisture content, total ash content, acid insoluble ash content and water soluble ash content were ranged of 7.6-17.8, 8.1-11.78, 0.019-0.134 and 6.2-9.2 respectively for the plant extracts and those values were less than standard values except the methanol extract. The hexane and ethyl acetate extracts exhibited highest α-amylase (IC50 = 25.7 ±0.6; 27.1 ±1.2 ppm) and α-glucosidase (IC50 = 22.4 ±0.1; 33.7 ±0.2 ppm) inhibitory activities than methanol extract (IC50 = 360.2 ±0.6; 179.6 ±0.9 ppm) when compared with the acarbose positive control (IC50 = 5.7 ±0.4; 17.1 ±0.6 ppm). The TAUC values for hexane, ethyl acetate, and methanol extracts and glibenclamide (positive control) treated rats were 8.01 ±0.66; 8.05 ±1.07; 8.40±0.50; 5.87 ±0.93 mmol/L.h respectively, whereas in diabetic control rats the TAUC value was 13.22 ±1.07 mmol/L.h. Administration of plant extracts treated rats significantly suppressed (p<0.05) the rise in plasma blood glucose levels compared to control rats but less significant than glibenclamide. The obtained results from in-vivo and in-vitro antidiabetic study showed that the hexane and ethyl acetate extracts of selected combined plant mixture might be considered as a potential source to isolate natural antidiabetic agents and physical parameters of hexane and ethyl acetate extracts will helpful to develop antidiabetic drug with further standardize properties.

Keywords: diabetes mellitus, in-vitro antidiabetic assays, medicinal plants, standardization

Procedia PDF Downloads 136

Authors: Christy Rosaline, Rathankar Roa, Waheeta Hopper

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Persistence of tuberculosis, emergence of multidrug-resistance and extensively drug-resistant forms of the disease, has increased the interest in developing new antitubercular drugs. Developing inhibitors for 3-deoxy-D-arabino-heptulosonate 7-phosphate synthase from Mycobacterium tuberculosis (MtbDAH7Ps), an enzyme involved in shikimate pathway, gives a selective target for antitubercular agents. MtbDAH7Ps was screened against ZINC database, and shortlisted compounds were subjected to induce fit docking. Prime/Molecular Mechanics Generalized Born Surface Area calculation was used to validate the binding energy of ligand-protein complex. Molecular Dynamics analysis for of the lead compounds–MtbDAH7Ps complexes showed that the backbone of MtbDAH7Ps in their complexes were stable. These results suggest that the shortlisted lead compounds ZINC04097114, ZINC15163225, ZINC16857013, ZINC06275603, and ZINC05331260 could be developed into novel drug leads to inhibit DAH7Ps in Mycobacterium tuberculosis.

Keywords: MtbDAH7Ps, Mycobacterium tuberculosis, HTVS, molecular dynamics

Procedia PDF Downloads 184

Authors: Essia Sebai, Amel Abidi, Hayet benyeddem, Akkari Hafidh

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Herbal extracts are of particular interest to the drug industry; essential oil with significant anthelmintic activity has the potential to be used as an alternative to conventional chemical drugs. In the present study, we describe the chemical profile of Laurus nobilis essential oil (EO), the in vitro anthelmintic activity of laurel oil against Haemonchus contortus and its in vivo anthelmintic effect against the murine helminth parasite model Heligmosomoides polygyrus. The chromatographic profile of L. nobilis (EO) extracted from the leaves of L. nobilis has shown the presence of monoterpenes 1,8-cineol (Eucalyptol) (29.47%), D-Limonène (18.51%) and Linalool (10.84%) in high fractions. The in vitro anthelmintic potential was expressed by an ovicidal effect against H. contortus egg hatching with an inhibition value of 3.23 mg/mL and 87.5% of immobility of adult worms after 8 hours of exposure to 8 mg/mL of L. nobilis EO. Regarding the in vivo anthelmintic potential, L. nobilis (EO) at 2400 mg/kg completely eliminated the egg output of H. polygyrus after seven days of oral treatment, together with a 79.2% of reduction in total worm counts. Based on the obtained funding, L. nobilis EO showed promising in vitro and in vivo anthelmintic capacities against gastrointestinal parasites.

Keywords: lauris nobilis, anthelmintic, haemonchus, pylogyrus

Procedia PDF Downloads 109

Authors: A. N. Gornostaeva, P. I. Bobyleva, E. R. Andreeva, L. B. Buravkova

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Multipotent mesenchymal stromal cells (MSCs) possess immunomodulatory properties. The effect of MSCs on the crucial cellular immunity compartment – T-cells is of a special interest. It is known that MSC tissue niche and expected milieu of their interaction with T- cells are characterized by low oxygen concentration, whereas the in vitro experiments usually are carried out at a much higher ambient oxygen (20%). We firstly evaluated immunomodulatory effects of MSCs on T-cells at tissue-related oxygen (5%) after interaction implied cell-to-cell contacts and paracrine factors only. It turned out that MSCs under reduced oxygen can effectively suppress the activation and proliferation of PHA-stimulated T-cells and can provoke decrease in the production of proinflammatory and increase in anti-inflammatory cytokines. In hypoxia some effects were amplified (inhibition of proliferation, anti-inflammatory cytokine profile shift). This impact was more evident after direct cell-to-cell interaction; lack of intercellular contacts could revoke the potentiating effect of hypoxia.

Keywords: MSCs, T-cells, activation, low oxygen, cell-to-cell interaction, immunosuppression

Procedia PDF Downloads 384

Authors: Muhammad Rizwan Tabassum, Ao Xia, Jerry D. Murphy

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The aim of this work is to provide an overview of macroalgae as an alternative feedstock for gaseous fuel production and key innovative technologies. Climate change and continuously depleting resources are the key driving forces to think for alternative sources of energy. Macroalgae can be favored over land based energy crops because they are not in direct competition with food crops. However, some drawbacks, such as high moisture content, seasonal variation in chemical composition and process inhibition limit the economic practicability. Macroalgae, like brown seaweed can be converted into gaseous and liquid fuel by different conversion technologies. Biomethane via anaerobic digestion is the appealing technology due to its dual advantage of a commercially applicable and environment friendly technology. Other technologies like biodiesel and bioethanol conversion technologies from seaweed are still under progress. Screening of high yielding macroalgae species, peak harvesting season and process optimization make the technology economically feasible for alternative source of feedstock for biofuel production in future.

Keywords: anaerobic digestion, biofuels, bio-methane, advanced conversion technologies, macroalgae

Procedia PDF Downloads 310

Authors: Mosaab A. Omar, Mohammad Saleh Al-Aboody, Mohmed A. Rizk, Shimaa M. Elsayed, Ahmed ElSify, Naoaki Yokoyama, Ikuo Igarashi

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Enoxacin is a broad-spectrum 6-fluoronaphthyridinone antibacterial agent (fluoroquinolones) structurally related to nalidixic acid used mainly in the treatment of urinary tract infections and gonorrhea. Also, it has been shown recently that it may have cancer inhibiting effect. The primary antibabesial effect of Enoxacin is due to inhibition of DNA gyrase subunit A, and DNA topoisomerase. In the present study, enoxacin was tested as a potent inhibitor against the in vitro growth of bovine and equine Piroplasms. The in vitro growth of five Babesia species that were tested was significantly inhibited (P<0.05) by micromolar concentrations of enoxacin (IC50 values= 13.5, 7.2, 7.5, and 24.2 µM for Babesia bovis, Babesia bigemina, Babesia caballi, and Theileria equi, respectively). Enoxacin IC50 values for Babesia and Theileria parasites were satisfactory as the drug is a potent antibacterial drug with minimum side effects. Therefore, enoxacin might be used for the treatment of Babesiosis and Theileriosis especially in case of mixed infections with bacterial diseases or in the case of animal sensitivity against diminazin toxicity.

Keywords: enoxacin, Babesia, Theileria, IC50 and dimenazin

Procedia PDF Downloads 472

Authors: Duchel Jeanedvi Kinouani Kinavouidi, Christian Aimé Kayath, Etienne Nguimbi

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Biosurfactants are amphipathic molecules produced by many microorganisms, usually bacteria, fungi, and yeasts. +ey possesses the property of reducing the tension of the membrane interfaces. No studies have been conducted on Shigella species showing the role of biosurfactant-like molecules (BLM) in pathogenicity. +e aim of this study is to assess the ability of Shigella environmental and clinical strains to produce BLM and investigate the involvement of biosurfactants in pathogenicity. Our study has shown that BLM is secreted in the extracellular medium with EI24 ranging from 80% to 100%. +e secretion depends on the type III secretion system (T3SS). Moreover, our results have shown that S. flexneri, S. boydii, and S. sonnei are able to interact with hydrophobic areas with 17.64%, 21.42%, and 22.22% hydrophobicity, respectively. BLM secretion is totally prevented due to the inhibition of T3SS by 100 mM benzoic and 1.5 mg/ml salicylic acids. P. aeruginosa harboring T3SS is able to produce 100% of BLM in the presence or in the absence of both T3SS inhibitors. +e secreted BLM are extractable with an organic solvent such as chloroform, and this could entirely be considered a lipopeptide or polypeptide compound. Secretion of BLM allows some Shigella strains to induce multicellular phenomena like ‘swarming.’

Keywords: shigella flexneri, biosurfactant, T3SS, Lipopeptide

Procedia PDF Downloads 21

Authors: Lyudmila V. Ignatova, Yelena V. Brazhnikova, Togzhan D. Mukasheva, Ramza Zh. Berzhanova, Anel A. Omirbekova

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Endophytic microorganisms are presented in plants of different families growing in the foothills and piedmont plains of Trans-Ili Alatau. It was found that the maximum number of endophytic micromycetes is typical to the Fabaceae family. The number of microscopic fungi in the roots reached (145.9±5.9)×103 CFU/g of plant tissue; yeasts - (79.8±3.5)×102 CFU/g of plant tissue. Basically, endophytic microscopic fungi are typical for underground parts of plants. In contrast, yeasts more infected aboveground parts of plants. Small amount of micromycetes is typical to inflorescence and fruits. Antagonistic activity of selected micromycetes against Fusarium graminearum, Cladosporium sp., Phytophtora infestans and Botrytis cinerea phytopathogens was detected. Strains with a broad, narrow and limited range of action were identified. For further investigations Rh2 and T7 strains were selected, they are characterized by a broad spectrum of fungicidal activity and they formed the large inhibition zones against phytopathogens. Active antagonists are attributed to the Rhodotorula mucilaginosa and Beauveria bassiana species.

Keywords: endophytic micromycetes, fungicidal activity, prevalence, plants

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Authors: Li Yuchen, Wu Qingxin, Jin Yuxing, Yang Qian

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Interleukin-11 (IL-11), a well-known anti-inflammatory factor, helps to protect against intestinal epithelium damage caused by physical or chemical factors. However, little is known about the role of IL-11 during viral infection. Herein, high mRNA and protein levels of IL-11 were found in epithelial cells and jejunum of piglets during porcine epidemic diarrhea virus (PEDV) infection, and IL-11 expression was positively correlated with the level of viral infection. Pretreatment with recombinant porcine IL-11 (pIL-11) suppressed PEDV replication in Vero E6 cells, while IL-11 knockdown promoted viral infection. Furthermore, pIL-11 inhibited viral infection by preventing PEDV-mediated apoptosis of cells through activating the IL-11/STAT3 signal pathway. Conversely, application of a STAT3 phosphorylation inhibitor significantly antagonized the anti-apoptosis function of pIL-11 and counteracted its inhibition of PEDV. Our data suggested that that IL-11 is a novel PEDV-inducible cytokine, and its production enhances the anti-apoptosis ability of epithelial cells against PEDV infection. The potential uses of IL-11 as a novel therapeutic against devastating viral diarrhea in piglets deserves more attention and study.

Keywords: Interleukin-11, Porcine epidemic diarrhea virus, STAT3, anti-apoptosis

Procedia PDF Downloads 142

Authors: Paiwan Buachan, Maneekarn Namsa-Aid, Suchada Jongrungruangchok, Foengchat Jarintanan, Wanlaya Uthaisang-Tanechpongtamb

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Lung cancer or pulmonary carcinoma is the uncontrolled growth of abnormal cells in one or both of the lungs. These abnormal cells can spread to other organs of the body through lymphatic system or bloodstream which is called metastatic stage that leading cause of cancer death. Terrein (C₈H₁₀O₃; MW= 154.06 kDa) is a secondary bioactive fungal metabolite, which was isolated from the Aspergillus terreus. In this study, we investigated the effects of terrein on the inhibition of human lung cancer cell proliferation and metastasis. The A549 human non-small cell lung cancer cell line was used as a model. Terrein significantly inhibited lung cancer cell proliferation measuring by a colorimetric MTT assay (IC₅₀ 0.32 mM) and significantly inhibited metastatic processes including migration, invasion, and adhesion that determined by wound healing assay, transwell assay, and adhesion assay, respectively. These findings indicate that terrein could be a potential therapeutic agent for lung cancer.

Keywords: terrein, lung cancer, anticancer, antimetastatic

Procedia PDF Downloads 173

Authors: Laila H. Abdel-Rahman, Mohamed Shaker S. Adam, Ahmed M. Abu-Dief, Hanan El-Sayed Ahmed

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In this investigation, Cu(II), Pd(II) and Ag(I) complexes with the tetra-dentate DSPH Schiff base ligand were synthesized. The DSPH Schiff base and its complexes were characterized by using different physicochemical and spectral analysis. The results revealed that the metal ions coordinated with DSPH ligand through azomethine nitrogen and phenolic oxygen. Cu(II), Pd(II) and Ag(I) complexes are present in a 1:1 molar ratio. Pd(II) and Ag(I) complexes have square planar geometries while, Cu(II) has a distorted octahedral (Oh) geometry. All investigated complexes are nonelectrolytes. The investigated compounds were tested against different strains of bacteria and fungi. Both prepared compounds showed good results of inhibition against the selected pathogenic microorganism. Moreover, the interaction of investigated complexes with CT-DNA was studied via various techniques and the binding modes are mainly intercalative and grooving modes. Operating Environment MOE package was used to do docking studies for the investigated complexes to explore the potential binding mode and energy. Furthermore, the growth inhibitory effect of the investigated compounds was examined on some cancer cells lines.

Keywords: tetradentate, antimicrobial, CT-DNA interaction, docking, anticancer

Procedia PDF Downloads 245

Authors: Nabila N. El-Maraghy, Amany Essa, Yousra Abdel–Mottaleb, Nada Ismail

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The use of combination of chemotherapy and natural products to influence the cell death with low doses of chemotherapeutic agents and few side effects has recently emerged as a new method of cancer therapy. Aim: Evaluation the modulatory effect of Thymoquinone on HepG2 cells treated with Sorafenib. Methods: Hepatocellular Carcinoma HepG2 cell line was treated with Sorafenib and TQ individually and in combination. The effect of these treatments on cell viability (MTT assay), apoptosis (Expression of Caspase-3) and oxidative markers (GSH content and extent of lipid peroxidation) was determined. Results: When compared the effect of both agents alone and the combination of the IC50 of Sorafenib and the IC50 TQ, the combination resulted in reduction of cell inhibition and apoptosis and antagonize their actions on GSH content and extent of lipid peroxidation which are increased. This study showed potent anti-tumor activity of both TQ and Sorafenib separately on HepG2 but upon combination surprisingly they interacted and give antagonistic effect. Conclusion: Co-treatment resulted in antagonistic interaction between Sorafenib and Thymoquinone.

Keywords: antagonism, hepatocellular carcinoma, sorafenib, thymoquinone

Procedia PDF Downloads 558

Authors: Sunil Kamboj, Vipin Saini, Suman Bala, Gaurav Sharma

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The main aim of the present research was to encapsulate mefenamic acid in niosomes and incorporate the prepared niosomes in the carbopol gel base for sustained therapeutic action. Mefenamic acid loaded niosomes were prepared by thin film hydration technique and evaluated for entrapment efficiency, vesicular size and zeta potential. The entrapment efficiency of the prepared niosomes was found to increase with decreasing the HLB values of surfactants and vesicle size was found to increase with increasing the cholesterol concentration. Niosomal vesicles with good entrapment efficiencies were incorporated in carbopol gel base to form the niosomal gel. The prepared niosomal gel was evaluated for pH, viscosity, spreadability, extrudability and skin permeation study across the rat skin.The results of permeation study revealed that the gel formulated with span 60 niosomes sustained the drug release for 12 h. Further the in vivo study showed the good inhibition of inflammation by the gel prepared with span 60 niosomes.

Keywords: mefenamic acid, niosomal gel, nonionic surfactants, sustained release

Procedia PDF Downloads 413

Authors: Zhongyang Sun, Shu Zhang

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In osteoblasts, L-type voltage sensitive calcium channels (LTCCs), especially the Cav1.2 LTCCs, play fundamental roles in cellular responses to external stimuli including both mechanical forces and hormonal signals. Several lines of evidence have revealed that the density of bone is increased and the resorption of bone is decreased when these calcium channels in osteoblasts are activated. And numerous studies have shown that mechanical loading promotes bone formation in the modeling skeleton, whereas removal of this stimulus in microgravity results in a reduction in bone mass. However, the effect of microgravity on LTCCs in osteoblasts is still unknown. The aim of this study was to determine whether microgravity exerts influence on LTCCs in osteoblasts and the possible mechanisms underlying. In this study, we demonstrate that simulated microgravity substantially inhibits LTCCs in osteoblast by suppressing the expression of Cav1.2. Then we show that the up-regulation of miR-103 is involved in the down-regulation of Cav1.2 expression and inhibition of LTCCs by simulated microgravity in osteoblasts. Our study provides a novel mechanism of simulated microgravity-induced adverse effects on osteoblasts, offering a new avenue to further investigate the bone loss caused by microgravity.

Keywords: L-type voltage sensitive calcium channels, Cav1.2, osteoblasts, microgravity

Procedia PDF Downloads 309

Authors: N. Mezıou-Cheboutı, A. Merabet, N. Behidj, F. Z. Bissaad

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The Algeria by its location, offers a rich and diverse vegetation. A large number of aromatic and medicinal plants grow spontaneously. The interest in these plants has continued to grow in recent years. Their particular properties due to the essential oil fraction can be utilized to treat microbial infections. To this end, and in the context of the valuation of the Algerian flora, we became interested in the species of the family Lamiaceae which is one of the most used as a global source of spices and extracts strong families antimicrobial potency. The plant on which we have based our choice is a species of sage "Salvia officinalis" from the Isser localized region within the province of Boumerdes. This work focuses on the study of the antimicrobial activity of essential oil extracted from the leaves of salvia officinalis. The extraction is carried out by HE hydrodistillation and reveals a yield of 1.06℅. The study of the antimicrobial activity of the essential oil by the method of at aromatogramme shown that Gram positive bacteria are most susceptible (Staphylococcus aureus and Bacillus subtilis) with a strong inhibition of growth. The yeast Candida albicans fungus Aspergillus niger and have shown moderately sensitive.

Keywords: Salvia officinalis, steam distillation, essential oil, aromatogram, anti-microbial activity

Procedia PDF Downloads 321

Authors: Abolfazl Kamkar

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Vegetable oils and fats are recognized as important components of our diet. They provide essential fatty acids, which are precursors of important hormones and control many physiological factors such as blood pressure, cholesterol level, and the reproductive system.Vegetable oils with higher contents of unsaturated fatty acids, especially polyunsaturated fatty acids (PUFAs) are more susceptible to oxidation.Protective effects of Sature jahortensis(SE) extracts in stabilizing soybean oil at different concentrations (200 and 400 ppm) were tested. Results showed that plant extracts could significantly (P< 0.05) lower the peroxide value and thiobarbituric acid value of oil during storage at 60 oC. The IC50 values for methanol and ethanol extracts were 31.5 ± 0.7 and 37.00 ± 0 µg/ml, respectively. In the β- carotene/linoleic acid system, methanol and ethanol extracts exhibited 87.5 ± 1.41% and 74.0 ±2.25 % inhibition against linoleic acid oxidation. The total phenolic and flavonoid contents of methanol and ethanol extracts were (101.58 ± 0. 26m g/ g) and (96.00 ± 0.027 mg/ g), (44.91 ± 0.14 m g/ g) and (14.30 ± 0.12 mg/ g) expressed in Gallic acid and Quercetin equivalents, respectively.These findings suggest that Satureja extracts may have potential application as natural antioxidants in the edible oil and food industry.

Keywords: satureja hortensis, antioxidant activity, oxidative stability, vegetable oil, extract

Procedia PDF Downloads 377

Authors: Asma Meliani, S. Lakehal, F. Z. Benrebiha, C. Chaouia

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There is an increasing interest in phytochemicals as new source of natural antioxidant and antimicrobial agents. Plants essential oils have come more into the focus of phytomedicine. Many researchers have reported various biological and/or pharmacological properties of Artemisia herba alba Asso essential oil. The present study describes antimicrobial and antioxidant properties of Artemisia herba alba Asso essential oil. Artemisia herba alba Asso essential oil obtained by hydrodistillation (using Clevenger type apparatus) growing in Algeria (M’sila) was analyzed by GC-MS. The essential oil yield of the study was 0.7%. The major components were found to be camphor, chrysanthenone et 1,8-cineole. The antimicrobial activity of the essential oil was tested against four bacteria (Gram-negative and Gram-positive) and three fungi using the diffusion method and by determining the inhibition zone. The oil was found to have significant antibacterial activity. In addition, antioxidant activity was determined by 1, 1-diphenyl-1-picrylhydrazyl (DPPH) assay, ferric reducing (FRAP) assay and β-carotene bleaching test, and high activity was found for Artemisia herba-alba oil.

Keywords: Artemisia herba-alba, essential oil, antibacterial activity, antioxidant activity

Procedia PDF Downloads 337

Authors: E. Kuley, M. Durmuş, E. Balikci, G. Ozyurt, Y. Uçar, F. Kuley, F. Ozogul, Y. Ozogul

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Ammonia and biogenic amine production of fish spoilage bacteria in sardine infusion decarboxylase broth and antimicrobial effect of olive by products (olive leaf extract:OL, olive cake: OC and black water:BW) was monitored using HPLC method. Fish spoilage bacteria produced all biogenic amine tested, mainly histamine and serotonin. Ammonia was accumulated more than 13.60 mg/L. Histamine production was in range 37.50 mg/L by Ser. liquefaciens and 86.71 mg/L by Ent. cloacae. The highest putrescine and cadaverine production was observed by Ent. cloacae (17.80 vs. 17.69 mg/L). The presence of OL, OC and BW in the broth significantly affected biogenic amine accumulation by bacteria. The antibacterial effect of olive by products depended on bacterial strains. OL and OC resulted in significant inhibition effect on HIS accumulation by bacteria apart from Ser. liquefaciens and Prot. mirabilis. The study result revealed that usefulness of OL and OC to prevent the accumulation of this amine which may affect human health.

Keywords: Antimicrobials, biogenic amine, fish spoilage bacteria, olive-by products

Procedia PDF Downloads 507

Authors: Asma Meliani, S. Lakehal, F. Z. Benrebiha, C. Chaouia

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There is an increasing interest in phytochemicals as new source of natural antioxidant and antimicrobial agents. Plants essential oils have come more into the focus of phytomedicine. Many researchers have reported various biological and/or pharmacological properties of Artemisia herba alba Asso essential oil. The present study describes antimicrobial and antioxidant properties of Artemisia herba alba Asso essential oil. Artemisia herba alba Asso essential oil obtained by hydrodistillation (using Clevenger type apparatus) growing in Algeria (M’sila) was analyzed by GC-MS. The essential oil yield of the study was 0.7 %. The major components were found to be camphor, chrysanthenone et 1,8-cineole. The antimicrobial activity of the essential oil was tested against four bacteria (Gram-negative and Gram-positive) and one fungi using the diffusion method and by determining the inhibition zone. The oil was found to have significant antibacterial activity. In addition, antioxidant activity was determined by 1,1-diphenyl-1-picrylhydrazyl (DPPH) assay, ferric reducing (FRAP) assay and β-carotene bleaching test, and high activity was found for Artemisia herba-alba oil.

Keywords: Artemisia herba-alba, essential oil, antibacterial activity, antioxidant activity

Procedia PDF Downloads 475

Authors: Antonella Di Sotto, Cinzia Ingallina, Caterina Fraschetti, Simone Circi, Marcello Locatelli, Simone Carradori, Gabriela Mazzanti, Luisa Mannina, Silvia Di Giacomo

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Cannabis sativa L. is one of the oldest cultivated plant species known not only for its voluptuous use but also for the wide application in food, textile, and therapeutic industries. Recently, the progress of biotechnologies applied to medicinal plants has allowed to produce different hemp varieties with low content of psychotropic phytoconstituents (tetrahydrocannabinol < 0.2% w/v), thus leading to a renewed industrial and therapeutic interest for this plant. In this context, in order to discover new potential remedies of pharmaceutical and/or nutraceutical interest, the chemopreventive properties of different organic and hydroalcoholic extracts, obtained from the inflorescences of C. sativa L. var. USO31, collected in June and September harvesting, were assessed. Particularly, the antimutagenic activity towards the oxidative DNA-damage induced by tert-butyl hydroperoxide (t-BOOH) was evaluated, and the DPPH (2,2-diphenyl-1-picrylhydrazyl) and ABTS (2,2'-azino-bis-3-ethylbenzthiazoline-6-sulphonic acid) radical scavenging power of the samples were assessed as possible mechanisms of antimutagenicity. Furthermore, the ability of the extracts to inhibit the glucose-6-phosphate dehydrogenase (G6PD), whose overexpression has been found to play a critical role in neoplastic transformation and tumor progression, has been studied as a possible chemopreventive strategy. A careful phytochemical characterization of the extracts for phenolic and terpenoid composition has been obtained by high performance liquid chromatography (HPLC) and gas chromatography-mass spectrometry (GC-MS) methods. Under our experimental condition, all the extracts were found able to interfere with the tBOOH-induced mutagenicity in WP2uvrAR strain, although with different potency and effectiveness. The organic extracts from both the harvesting periods were found to be the main effective antimutagenic samples, reaching about a 55% inhibition of the tBOOH-mutagenicity at the highest concentration tested (250 μg/ml). All the extracts exhibited radical scavenger activity against DPPH and ABTS radicals, with a higher potency of the hydroalcoholic samples. The organic extracts were also able to inhibit the G6PD enzyme, being the samples from September harvesting the highly potent (about 50% inhibition respect to the vehicle). At the phytochemical analysis, all the extracts resulted to contain both polar and apolar phenolic compounds. The HPLC analysis revealed the presence of catechin and rutin as the major constituents of the hydroalcoholic extracts, with lower levels of quercetin and ferulic acid. The monoterpene carvacrol was found to be an ubiquitarian constituent. At GC-MS analysis, different terpenoids, among which caryophyllene sesquiterpenes, were identified. This evidence suggests a possible role of both polyphenols and terpenoids in the chemopreventive properties of the extracts from the inflorescences of C. sativa var. USO31. According to the literature, carvacrol and caryophyllene sesquiterpenes can contribute to the strong antimutagenicity although the role of all the hemp phytocomplex cannot be excluded. In conclusion, present results highlight a possible interest for the inflorescences of C. sativa var. USO31 as source of bioactive molecules and stimulate further studies in order to characterize its possible application for nutraceutical and pharmaceutical purposes.

Keywords: antimutagenicity, glucose-6-phosphate dehydrogenase, hemp inflorescences, nutraceuticals, sesquiterpenes

Procedia PDF Downloads 161

Authors: Sajjad Negahban, Ruihe Wang, Baojiang Sun

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Gas-lift dual gradient drilling is a solution for deepwater drilling challenges. As well, Continuous development of drilling technology leads to increase employment of mineral oil based drilling fluids and synthetic-based drilling fluids, which have adequate characteristics such as: high rate of penetration, lubricity, shale inhibition and low toxicity. The paper discusses utilization of nitrified mineral oil base drilling for deepwater drilling and for more accurate prediction of pressure in DGD at marine riser, solubility and bubble pressure were considered in steady state hydraulic model. The Standing bubble pressure and solubility correlations, and two models which were acquired from experimental determination were applied in hydraulic model. The effect of the black oil correlations, and new solubility and bubble pressure models was evaluated on the PVT parameters such as oil formation volume factor, density, viscosity, volumetric flow rate. Eventually, the consequent simulated pressure profile due to these models was presented.

Keywords: solubility, bubble pressure, gas-lift dual gradient drilling, steady state hydraulic model

Procedia PDF Downloads 280

Authors: S. Ghalem, M. Mesmoudi, I. Daoudand, H. Allali

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The nitrogen-containing bisphosphonates (N-BPs) are well established as the treatments of choice for disorders of excessive bone resorption, myeloma and bone metastases, and osteoporosis. They inhibit farnesyl pyrophosphate synthase (FFPS), a key enzyme in the mevalonate pathway, resulting in inhibition of the prenylation of small GTP-binding proteins in osteoclasts and disruption of their cytoskeleton, adhesion/spreading, and invasion of cancer cells. A very few examples for synthesis of α-amino bisphosphonates based on several amino acids are known from the literature. In the present work, esters of aminoacid react with ketophsophonate (or their analog acid or acyl) to afford the desired products, α-iminophosphonates. The reaction of imine with dimethyl phosphate in the presence of catalytic amount of I2 give ester of α-aminobisphosphonate as sole product in good yield. Finally, we used computational docking methods to predict how several α-aminobisphosphonates bind to FPPS and how R and X influence. Pamidronate, β-aminobisphosphonate already marketed, was used as reference. These results are of interest since they represent a new and simple way to sythesize α-aminobisphosphonates with a free COOH group increased by R2 functionalisable and opening up the possibility of using the molecular docking to facilitate the design of other, novel FFPS inhibitors.

Keywords: drug research, cancer, α-amino bisphosphonates, molecular docking

Procedia PDF Downloads 274

Authors: Jamie A. Prowse Turner, Jamie I. D. Campbell, Valerie A. Thompson

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The objective of the current research was to use a dual-process theory framework to explain these age-related differences in reasoning. Seventy-two older (M = 80.0 years) and 72 younger (M = 24.6 years) adults were given a variety of reasoning tests (i.e., a syllogistic task, base rate task, the Cognitive Reflection Test, and a perspective manipulation), as well as independent tests of capacity (working memory, processing speed, and inhibition), thinking styles, and metacognitive ability, to account for these age-related differences. It was revealed that age-related differences were limited to problems that required Type 2 processing and were related to differences in cognitive capacity, individual difference factors, and strategy choice. Furthermore, older adults’ performance can be improved by reasoning from another’s’ perspective and cannot, at this time, be explained by metacognitive differences between young and older adults. All of these findings fit well within a dual-process theory of reasoning, which provides an integrative framework accounting for previous findings and the findings presented in the current manuscript.

Keywords: aging, dual-process theory, performance, reasoning ability

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Authors: Benarous Khedidja, Yousfi Mohamed

Abstract:

Infections caused by Candida species manifest in a number of diseases, including candidemia, vulvovaginal candidiasis, endocarditis, and peritonitis. These Candida species have been reported to have lipolytic activity by secretion of lipolytic enzymes such as esterases, lipases and phospholipases. These Extracellular hydrolytic enzymes seem to play an important role in Candida overgrowth. Candidiasis is commonly treated with antimycotics such as clotrimazole and nystatin, which bind to a major component of the fungal cell membrane (ergosterol). This binding forms pores in the membrane that lead to death of the fungus. Due to their secondary effects, scientists have thought of another treatment basing on lipase inhibition but we haven’t found any lipase inhibitors used as candidiasis treatment. In this work, we are interested to lipases inhibitors such as alkaloids as another candidiasis treatment. In the first part, we have proceeded to optimize the alkaloid structures and protein 3D structure using Hyperchem software. Secondly, we have docked inhibitors using Genetic algorithm with GOLD software. The results have shown ten possibilities of binding inhibitor to Candida rugosa lipase (CRL) but only one possibility has been accepted depending on the weakest binding energy.

Keywords: marrubiin, candida rugosa lipase, docking, gold

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Authors: Asieh Abbassi Daloii, Fatemeh Fani, Ahmad Abdi

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Objective: The aim of this study was to determine the effect of 8 weeks endurance training and L-NAME on apelin in adipose tissue, glucose and insulin in elderly male’s rats. Methods: For this purpose, 24 vistar elderly rats with average 20 months old purchased from Razi Institute and transferred to Research Center were randomly divided into four groups: 1. control, 2. training, 3.training and L-NAME and 4. L-NAME. Training protocol performed for 8 weeks and 5 days a week with 75-80 VO2 max. All rats were killed 72 hours after the final training session and after 24 hours of fasting adipose tissue samples were collected and kept in -80. Also, Data was analyzed with One way ANOVA and Tucky in p < 0/05. Results: The results showed that the inhibition of nitric oxide on apelin in adipose tissue of adult male rats after eight weeks of endurance training increased significantly compared to the control group (p < 0.00). Also, the results showed no significant difference between the levels of insulin and glucose groups. Conclusion: It is likely that the increased apelin in adipose tissue in mice independent of insulin and glucose.

Keywords: endurance training, L-NAME, apelin in adipose tissue, elderly male rats

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Authors: Sakshi Chopra, Ashima Nehra, Sumit Sinha, Harsimarpreet Kaur, Ravindra Mohan Pandey

Abstract:

Background: Cognitive rehabilitation aims to retrain brain injured individuals with cognitive deficits to restore or compensate lost functions. As illiterates or people with low literacy levels represent a significant proportion of the world, specific rehabilitation modules for such populations are indispensable. Literacy is significantly associated with all neuropsychological measures and retraining programs widely use written or spoken techniques which essentially require the patient to read or write. So, the aim of the study was to develop and standardize a literacy free neuropsychological rehabilitation program for improving cognitive functioning in patients with mild and moderate Traumatic Brain Injury (TBI). Several studies have pointed out to the impairments seen in memory, executive functioning, and attention and concentration post-TBI, so the rehabilitation program focussed on these domains. Visual item memorization, stick constructions, symbol cancellations, and colouring techniques were used to construct the retraining program. Methodology: The development of the program consisted of planning, preparing, analyzing, and revising the different modules. The construction focussed on areas of retraining immediate and delayed visual memory, planning ability, focused and divided attention, concentration, and response inhibition (to control irritability and aggression). A total of 98 home based retraining modules were prepared in the 4 domains (42 for memory, 42 for executive functioning, 7 for attention and concentration, and 7 for response inhibition). The standardization was done on 20 healthy controls to review, select and edit items. For each module, the time, errors made and errors per second were noted down, to establish the difficulty level of each module and were arranged in increasing level of difficulty over a period of 6 weeks. The retraining tasks were then administered on 11 brain injured individuals (5 after Mild TBI and 6 after Moderate TBI). These patients were referred from the Trauma Centre to Clinical Neuropsychology OPD, All India Institute of Medical Sciences, New Delhi, India. Results: The time was taken, errors made and errors per second were analysed for all domains. Education levels were divided into illiterates, up to 10 years, 10 years to graduation and graduation and above. Mean and standard deviations were calculated. Between group and within group analysis was done using the t-test. The performance of 20 healthy controls was analyzed and only a significant difference was observed on the time taken for the attention tasks and all other domains had non-significant differences in performance between different education levels. Comparing the errors, time taken between patient and control group, there was a significant difference in all the domains at the 0.01 level except the errors made on executive functioning, indicating that the tool can successfully differentiate between healthy controls and patient groups. Conclusions: Apart from the time taken for symbol cancellations, the entire cognitive rehabilitation program is literacy free. As it taps the major areas of impairment post-TBI, it could be a useful tool to rehabilitate the patient population with low literacy levels across the world. The next step is already underway to test its efficacy in improving cognitive functioning in a randomized clinical controlled trial.

Keywords: cognitive rehabilitation, illiterates, India, traumatic brain injury

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Authors: M. N. Hanina, M. Hairul Shahril, I. Ismatul Nurul Asyikin, A. K. Abdul Jalil, M. R. Salina, M. R. Maryam, M. Rosfarizan

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The extracellular proteins secreted by bacteria may be increased in stressful surroundings, such as in the presence of antibiotics. It appears that many antibiotics, when used at low concentrations, have in common the ability to activate or repress gene transcription, which is distinct from their inhibitory effect. There have been comparatively few studies on the potential of antibiotics as a specific chemical signal that can trigger a variety of biological functions. Therefore, this study was carried out to determine the effect of Streptomycin Sulfate in regulating extracellular proteins secreted by Bacillus subtilis ATCC21332. Results of Microdilution assay showed that the Minimum Inhibition Concentration (MIC) of Streptomycin Sulfate on B. subtilis ATCC21332 was 2.5 mg/ml. The bacteria cells were then exposed to Streptomycin Sulfate at concentration of 0.01 MIC before being further incubated for 48h to 72 h. The extracellular proteins secreted were then isolated and analyzed by sodium dodecyl sulfate polyacrylamide gel electrophoresis (SDS-PAGE). Proteins profile revealed that three additional bands with approximate sizes of 30 kDa, 22 kDa and 23 kDa were appeared for the treated bacteria with Streptomycin Sulfate. Thus, B. subtilis ATCC21332 in stressful condition with the presence of Streptomycin Sulfate at low concentration could induce the extracellular proteins secretion.

Keywords: Bacillus subtilis ATCC21332, streptomycin sulfate, extracellular proteins, antibiotics

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Authors: N. A. Kazemi Sefat, M. M. Mohammadi, J. Hadjati, S. Talebi, M. Ajami, H. Daneshvar

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Colorectal cancer metastases result in a significant number of cancer related deaths. Histone deacetylase (HDAC) inhibitors induce growth arrest and apoptosis in a variety of human cancer cells. Sodium butyrate (SB) is a short chain fatty acid, belongs to HDAC inhibitors which is released in the colonic lumen as a consequence of fiber fermentation. In this study, we are about to assess the effect of sodium butyrate on HCT116 human colorectal carcinoma cell line. The viability of cells was measured by microscopic morphologic study and MTT assay. After 48 hours, treatments more than 10 mM lead to cell injury in HCT116 by increasing cell granulation and decreasing cell adhesion (p>0.05). After 72 hours, treatments at 10 mM and more lead to significant cell injury (p<0.05). Our results may suggest that the gene expression which is contributed in cell proliferation and apoptosis has been changed under pressure of HDAC inhibition.

Keywords: colorectal cancer, sodium butyrate, cytotoxicity, MTT

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Authors: Olaitan Akanji, Cleophas Loto, Patricia Popoola, Andrei Kolesnikov

Abstract:

Studies involving performance of corrosion inhibitors had been identified as one of the critical research needs for improving the durability of mild steel used in various industrial applications. This paper investigates the inhibiting effect of calcium gluconate against the corrosion of mild steel in 2.5M magnesium chloride using weight loss method and linear polarization technique, calculated corrosion rates from the obtained weight loss data, potentiodynamic polarization measurements are in good agreement. Results revealed calcium gluconate has strong inhibitory effects with inhibitor efficiency increasing with increase in inhibitor concentration at ambient temperature, the efficiency of the inhibitor increased in the following order of concentrations 2%g/vol,1.5%g/vol,1%g/vol,0.5%g/vol. Further results obtained from potentiodynamics experiments had good correlation with those of the gravimetric methods, the adsorption of the inhibitor on the mild steel surface from the chloride has been found to obey Langmuir, Frumkin and Freudlich adsorption isotherm. Scanning electron microscopy (SEM) observation confirmed the existence of an absorbed protective film on the metal surface.

Keywords: calcium gluconate, corrosion, magnesium chloride, mild steel

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Authors: M. Nasiri

Abstract:

Aim: Considering the hypoglisimic ad hipolipidimic effect of the fenugreek seed and aerobic exercise training, this study was conducted to evaluate the effect of fenugreek and aerobic exercise training on insulin resistance in women with type 2 diabetes. Methodology: 32 patients with type II diabetes were selected and randomly divided into four groups: control, fenugreek, training and fenugreek - training. Fenugreek groups used 10 grams of fenugreek seeds daily for eight weeks on two occasions before noon and evening meal. Training of groups is also performed a regular program of aerobic exercise 65-55% of maximum heart rate (4 days per week).Two days before and after the training period, blood samples were taken from their brachial veins in a fasting state (12 hours prior to the test) in a sitting position. The data was analyzed used of t-independent and ANOVA at a significance level of α < 0.05. Results: Intra-group changes in all experimental groups showed that significant decrease insulin resistance, and the difference between groups showed significant difference between the groups of fenugreek - training than other groups there. Conclusions: According to the research findings to fenugreek combined with aerobic exercise more beneficial effect on the inhibition of insulin resistance in women with diabetes are recommended to them.

Keywords: fenugreek, training, insulin resistance, diabetes

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