Search results for: xanthine oxidase inhibitory activity

Authors: Uc-Cayetano E. G., Ake-Uh O. E., Villanueva-Mena I. E., Ordonez L. C.

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Carbon nanotubes (CNTs) and other graphitic nanostructures are materials with extraordinary physical, physicochemical and electrochemical properties which are being aggressively investigated for a variety of sensing applications. Thus, sensing of biological molecules such as proteins, DNA, glucose and other enzymes using either single wall or multiwall carbon nanotubes (MWCNTs) has been widely reported. Despite the current progress in this area, the electrochemical response of CNTs used in a variety of sensing arrangements still needs to be improved. An alternative towards the enhancement of this CNTs' electrochemical response is to chemically (or physically) modify its surface. The influence of the decoration with iron oxide nanoparticles in different types of MWCNTs on the amperometric sensing of glucose, urea, and cholesterol in solution is investigated. Commercial MWCNTs were oxidized in acid media and subsequently decorated with iron oxide nanoparticles; finally, the enzymes glucose oxidase, urease, and cholesterol oxidase are chemically immobilized to oxidized and decorated MWCNTs for glucose, urease, and cholesterol electrochemical sensing. The results of the electrochemical characterizations consistently show that the presence of iron oxide nanoparticles decorating the surface of MWCNTs enhance the amperometric response and the sensitivity to increments in glucose, urease, and cholesterol concentration when compared to non-decorated MWCNTs.

Keywords: WCNTs, enzymes, oxidation, decoration

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Authors: H. Alijani, M. Jabari, S. Matroodi, H. Zolqarnein, A. Sharafi, I. Zamani

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Actinomycetes, Gram-positive bacteria, are interesting as a main producer of secondary metabolites and are important industrially and pharmaceutically. The marine environment is a potential source for new actinomycetes, which can provide novel bioactive compounds and industrially important enzymes. The aims of this study were to isolate and identify novel actinomycetes from Persian Gulf sediments and screen these isolates for the production of secondary metabolites, especially antibiotics, Using phylogenetic (16S rRNA gene sequence), morphological and biochemical analyses. 15 different actinomycete strains from Persian Gulf sediments at a depth of 5-10 m were identified. DNA extraction was done using Cinnapure DNA Kit. PCR amplification of 16S rDNA gene was performed using F27 and R1492 primers. Phylogenetic tree analysis was performed using the MEGA 6 software. Most of the isolated strains belong to the genus namely Streptomyces (14), followed by Nocardiopsis (1). Antibacterial assay of the isolates supernatant was performed using a standard disc diffusion assay with replication (n=3). The results of disk diffusion assay showed that most active strain against Proteus volgaris and Bacillus cereus was AMJ1 (16.46±0.2mm and 13.78±0.2mm, respectively), against Salmonella sp. AMJ7 was the most effective strain (10.13±0.2mm), and AMJ1 and AHA5 showed more inhibitory activity against Escherichia coli (8.04±0.02 mm and 8.2±0.03 ). The AMJ6 strain showed best antibacterial activity against Klebsiella sp. (8.03±0.02mm). Antifungal activity of AMJ2 showed that it was most active strain against complex (16.05±0.02mm) and against Aspergillus flavus strain AMJ1 was most active strain (16.4±0.2mm) and highest antifungal activity against Trichophyton mentagrophytes, Microsporum gyp serum and Candida albicans, were shown by AHA1 (21.03±0.02mm), AHA3 and AHA7 (18±0.03mm), AMJ6 (21.03±0.2mm) respectively. Our results revealed that the marine actinomycetes of Persian Gulf sediments were potent source of novel antibiotics and bioactive compounds and indicated that the antimicrobial metabolites were extracellular. Most of the secondary metabolites and antibiotics are extracellular in nature and extracellular products of actinomycetes show potent antimicrobial activities.

Keywords: antibacterial activity, antifungal activity, marine actinomycetes, Persian Gulf

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Authors: Ginpreet Kaur, Mohammad Yasir Usmani, Mohammed Kamil Khan

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Diabetes mellitus is a disease with a high global burden and results in significant morbidity and mortality. In India, the number of people suffering with diabetes is expected to rise from 19 to 57 million in 2025. At present, interest in herbal remedies is growing to reduce the side effects associated with conventional dosage form like oral hypoglycemic agents and insulin for the treatment of diabetes mellitus. Our aim was to investigate the antidiabetic activities of combinatorial extract of N. sativa & C. cassia in Streptozotocin induced type-I Diabetic Rats. Thus, the present study was undertaken to screen postprandial glucose excursion potential through α- glucosidase inhibitory activity (In Vitro) and effect of combinatorial extract of N. sativa & C. cassia in Streptozotocin induced type-I Diabetic Rats (In Vivo). In addition changes in body weight, plasma glucose, lipid profile and kidney profile were also determined. The IC50 values for both extract and Acarbose was calculated by extrapolation method. Combinatorial extract of N. sativa & C. cassia at different dosages (100 and 200 mg/kg orally) and Metformin (50 mg/kg orally) as the standard drug was administered for 28 days and then biochemical estimation, body weights and OGTT (Oral glucose tolerance test) were determined. Histopathological studies were also performed on kidney and pancreatic tissue. In In-Vitro the combinatorial extract shows much more inhibiting effect than the individual extracts. The results reveals that combinatorial extract of N. sativa & C. cassia has shown significant decrease in plasma glucose (p<0.0001), total cholesterol and LDL levels when compared with the STZ group The decreasing level of BUN and creatinine revealed the protection of N. sativa & C. cassia extracts against nephropathy associated with diabetes. Combination of N. sativa & C. cassia significantly improved glucose tolerance to exogenously administered glucose (2 g/kg) after 60, 90 and 120 min interval on OGTT in high dose streptozotocin induced diabetic rats compared with the untreated control group. Histopathological studies shown that treatment with N. sativa & C. cassia extract alone and in combination restored pancreatic tissue integrity and was able to regenerate the STZ damaged pancreatic β cells. Thus, the present study reveals that combination of N. sativa & C. cassia extract has significant α- glucosidase inhibitory activity and thus has great potential as a new source for diabetes treatment.

Keywords: lipid levels, OGTT, diabetes, herbs, glucosidase

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Authors: Gourav Jain, Sameer Dixit, Surjeet Kumar Arya, Praveen C. Verma

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Plant cell wall plays a major role in defence mechanism against biotic and abiotic stress as it constitutes the physical barrier between the microenvironment and internal component of the cell. It is a complex structure composed of mostly carbohydrates among which cellulose and hemicelluloses are most abundant that is embedded in a matrix of pectins and proteins. Multiple enzymes have been reported which plays a vital role in cell wall modification, Pectin Methylesterase (PME) is one of them which catalyses the demethylesterification of homogalacturonans component of pectin which releases acidic pectin and methanol. As emitted methanol is toxic to the insect pest, we use PME gene for the better methanol production. In the current study we showed overexpression of PME gene isolated from Withania somnifera under the insect inducible promoter causes enhancement of methanol production at the time of insect feeds to plants, and that provides better insect resistance property. We found that the 85-90% mortality causes by transgenic tobacco in both chewing (Spodoptera litura larvae and Helicoverpa armigera) and sap-sucking (Aphid, mealybug, and whitefly) pest. The methanol content and emission level were also enhanced by 10-15 folds at different inducible time point interval (15min, 30min, 45min, 60min) which would be analysed by Purpald/Alcohol Oxidase method.

Keywords: methanol, Pectin methylesterase, inducible promoters, Purpald/Alcohol oxidase

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Authors: Hana Al-Baghaoi, Kumar Shiva Gubbiyappa, Mayuren Candasamy, Kiruthiga Perumal Vijayaraman

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Acne is a chronic inflammatory disease of the sebaceous glands characterized by areas of skin with seborrhea, comedones, papules, pustules, nodules, and possibly scarring. Propionibacterium acnes (P. acnes), plays a key role in the pathogenesis of acne. Their colonization and proliferation trigger the host’s inflammatory response leading to the production of pro-inflammatory cytokines such as interleukin-8 (IL-8) and tumour necrosis factor-α (TNF-α). The usage of honey and natural compounds to treat skin ailments has strong support in the current trend of drug discovery. The present study was carried out evaluate antimicrobial and anti-inflammatory potential of Doani Sidr honey and its fractions against P. acnes and to screen madecassoside alone and in combination with fractions of honey. The broth dilution method was used to assess the antibacterial activity. Also, ultra structural changes in cell morphology were studied before and after exposure to Sidr honey using transmission electron microscopy (TEM). The three non-toxic concentrations of the samples were investigated for suppression of cytokines IL 8 and TNF α by testing the cell supernatants in the co-culture of the human peripheral blood mononuclear cells (hPBMCs) heat killed P. acnes using enzyme immunoassay kits (ELISA). Results obtained was evaluated by statistical analysis using Graph Pad Prism 5 software. The Doani Sidr honey and polysaccharide fractions were able to inhibit the growth of P. acnes with a noteworthy minimum inhibitory concentration (MIC) value of 18% (w/v) and 29% (w/v), respectively. The proximity of MIC and MBC values indicates that Doani Sidr honey had bactericidal effect against P. acnes which is confirmed by TEM analysis. TEM images of P. acnes after treatment with Doani Sidr honey showed completely physical membrane damage and lysis of cells; whereas non honey treated cells (control) did not show any damage. In addition, Doani Sidr honey and its fractions significantly inhibited (> 90%) of secretion of pro-inflammatory cytokines like TNF α and IL 8 by hPBMCs pretreated with heat-killed P. acnes. However, no significant inhibition was detected for madecassoside at its highest concentration tested. Our results suggested that Doani Sidr honey possesses both antimicrobial and anti-inflammatory effects against P. acnes and can possibly be used as therapeutic agents for acne. Furthermore, polysaccharide fraction derived from Doani Sidr honey showed potent inhibitory effect toward P. acnes. Hence, we hypothesize that fraction prepared from Sidr honey might be contributing to the antimicrobial and anti-inflammatory activity. Therefore, this polysaccharide fraction of Doani Sidr honey needs to be further explored and characterized for various phytochemicals which are contributing to antimicrobial and anti-inflammatory properties.

Keywords: Doani sidr honey, Propionibacterium acnes, IL-8, TNF alpha

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Authors: Sanjay Singh, Swati Jaiswal, Prashant Mishra

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Nanoparticle based formulations of drug delivery systems have shown their potential in improving the performance of existing drugs and have opened avenues for new therapies. Calendula extract is a low cost, wide spectrum bioactive material that has been used for a long term therapy of various infections. Aim: The aim of this study was to develop Calendula officinalis extract based nanoformulations and to study the antibacterial activity of either Calendula extract loaded chitosan nanoparticles or Calendula extract coated silver nanoparticles for increased bioavailability and their long term effect. Methods: Chitosan nanoparticles were prepared by the process of ionotropic gelation, based on interaction between the negative groups of tri polyphosphate (TPP) and positively charged amino groups of chitosan. The size of the Calendula extract-loaded chitosan particles was determined using dynamic light scattering and scanning electron microscopy. Antibacterial activities of these formulations were determined based on minimum inhibitory concentration and time kill studies. In addition, silver nanoparticles were also synthesized in the presence of Calendula extract and characterized by UV visible spectrum, DLS and XRD. Experiments were conducted on 96-plates against two Gram-positive bacteria; Staphylococcus aureus and Bacillus subtilis two Gram-negative bacteria; Escherichia coli and Pseudomonas aeruginosa. Results: Results demonstrated time dependent antibacterial activity against different microbes studied. Both Calendula extract and Calendula extract loaded chitosan nanoparticles have shown good antimicrobial activity against both Gram positive and Gram negative bacteria. Conclusion: Calendula extract loaded chitosan nanoparticles and calendula extract coated silver nanoparticles are potential antibacterial for their long term antibacterial effects.

Keywords: antibacterial, Calendula extract, chitosan nanoparticles, silver nanoparticles

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Authors: Eman Ahmed Alsaleh

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Background: Many studies published in other countries identified certain perceived benefits and barriers to physical activity among patients with coronary heart disease. Nevertheless, there is no data about the issue relating to Jordanian patients with coronary heart disease. Objective: This study aimed to describe the prevalence of level of physical activity, benefits of and barriers to physical activity as perceived by Jordanian patients with coronary heart disease, and the relationship between physical activity and perceived benefits of and barriers to physical activity. In addition, it focused on examining the influence of selected sociodemographic and health characteristics on physical activity and the perceived benefits of and barriers to physical activity. Methods: A cross-sectional design was performed on a sample of 400 patients with coronary heart disease. They were given a list of perceived benefits and barriers to physical activity and asked to what extent they disagreed or agreed with each. Results: Jordanian patients with coronary heart disease perceived various benefits and barriers to physical activity. Most of these benefits were physiologically related (average mean = 5.7, SD = .7). The most substantial barriers to physical activity as perceived by the patients were: feeling anxiety, not having enough time, lack of interest, bad weather, and feeling of being uncomfortable. Sociodemographic and health characteristics that significantly influenced perceived barriers to physical activity were age, gender, health perception, chest pain frequency, education, job, caring responsibilities, ability to travel alone, smoking, and previous and current physical activity behaviour. Conclusion: This research demonstrates that patients with coronary heart disease have perceived physiological benefits of physical activity, and they have perceived motivational, physical health, and environmental barriers to physical activity, which is significant in developing intervention strategies that aim to maximize patients' participation in physical activity and overcome barriers to physical activity.

Keywords: prevalence, coronary heart disease, physical activity, perceived barriers

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Authors: Yılmaz Uçar, Fatih Ozogul, Mustafa Durmuş, Yesim Ozogul, Ali Rıza Köşker, Esmeray Kuley Boğa, Deniz Ayas

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The aim of this study was to purified eicosapentaenoic acid (EPA) and docosahexaenoic acid (DHA), that are essential oils from trout oil, using high-performance liquid chromatography (HPLC) method, bioconverted EPA and DHA into bioconverted EPA (bEPA), bioconverted DHA (bDHA) extracts by P. aeruginosa PR3. Moreover, in vitro antibacterial activity of bEPA and bDHA was investigated using disc diffusion methods and minimum inhibitory concentration (MIC). EPA and DHA concentration of 11.1% and 15.9% in trout oil increased in 58.64% and 40.33% after HPLC optimisation, respectively. In this study, EPA and DHA enriched products were obtained which are to be used as valuable supplements for food and pharmaceutical purposes. The bioconverted EPA and DHA exhibited antibacterial activities against two Gram-positive bacteria (Listeria monocytogenes ATCC 7677 and Staphylococcus aureus ATCC 29213) and six Gram-negative bacteria (Pseudomonas aeruginosa ATCC 27853, Escherichia coli ATCC 25922, Klebsiella pneumoniae ATCC700603, Enterococcus faecalis ATCC 29212, Aeromonas hydrophila NCIMB 1135, and Salmonella Paratyphi A NCTC 13). Inhibition zones and MIC value of bEPA and bDHA against bacterial strains ranged from 7 to 12 mm and from 350 to 2350 μg/mL, respectively. Our results suggested that the crude extracts of bioconversion of EPA and DHA by P. aeruginosa PR3 can be considered as promising antimicrobials in improving food safety by controlling foodborne pathogens.

Keywords: High-Performance Liquid Chromatography (HPLC), docosahexaenoic acid, DHA, eicosapentaenoic acid, EPA, minimum inhibitory concentration, MIC, Pseudomonas aeruginosa PR3

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Authors: Fisseha Shiferie (Bpharm, Mpharm)

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Diarrhea is a common gastrointestinal disorder characterized by an increase in stool frequency and a change in stool consistency. Inspite of the availability of many drugs as antidiarrheal agents, the search for a drug with affordable cost and better efficacy is essential to overcome diarrheal problems. The root extract of Echinops kebericho, is used by traditional practitioners for the treatment of diarrhea. However, the scientific basis for this usage has not been yet established. The purpose of the present study was to evaluate the antidiarrheal and spasmolytic activities of the aqueous extract of the roots of E. kebericho in rodents and isolated guinea-pig ileum preparations. In the castor oil induced intestinal transit test, E. kebericho produced a significant (p < 0.01) dose dependent decrease in propulsion with peristaltic index values of 45.05±3.3, 42.71±2.25 and 33.17±3.3%, respectively at doses of 100, 200 and 400 mg/kg compared with 63.43±7.3% for control. In the castor oil-induced diarrhea test, the mean defecation was reduced from 1.81±0.18 to 0.99 ± 0.21 compared with 2.59 ±0.81 for control. The extract (at doses stated above) significantly decreased the volume of intestinal fluid secretion induced by castor oil (2.31±0.1 to 2.01±0.2) in relation to 3.28±0.3 for control. When tested on a guinea-pig ileum, root extract of Echinops kebericho exhibited a dose dependent spasmolytic effect, 23.07 % being its highest inhibitory effect. The results obtained in this study give some scientific support to the use of Echinops kebericho as an antidiarrheal agent due to its inhibitory effects on the different diarrheal parameters used in this study.

Keywords: antidiarrheal activity, E. kebericho, traditional medicine, diarrhea, enteropooling, and intestinal transit

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Authors: Sobhy El-Sohaimy, Abduvali Toshev, Hanem Mansour

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(1) Objective: The main objective of the current study was to evaluate in an In Vitro and In Vivo, the potential activity of olive leaves extract (OLE) in the treatment and/or preventing the diabetes mellitus type II and related implications; (2) Methodology: Five groups of male rats were used in the current study: group (1)- negative control (normal); group (2)- positive control, streptozotocin (STZ) induced rats; group (3)-diabetic rats treated with metformin (200 mg/kg) plus OLE (200 mg/kg); group 4- diabetic rats treated with metformin (200 mg/kg); group 5- diabetic rats treated with OLE (200 mg/kg). A four-week regime of oral treatment was administered once daily; (3) Results: Diabetic rats treated with metformin + OLE clearly showed normal blood glucose level (121.67 ± 5.49 mg/dl), and glycated hemoglobin (HbA1c) (3.70 ± 0.10%). The combination of metformin + OLE obviously showed a superior improvement in the lipid profile (TG, TC, HDL and LDL) compared to both metformin and OLE individually. The histological examination revealed that the combination of metformin + Olive leaves extract successfully repaired of the liver, kidneys, and pancreatic tissues in diabetic rats to be near to the normal status; (4) Conclusion: Finally, it can be concluded that, the combination of metformin and OLE exhibited a superior improvement than metformin and OLE individually which emphasized the promising adjuvant role of the OLE in the treatment protocol of diabetes mellitus type II.

Keywords: olive (olea europaea) leaves extracts, hypoglycemic agents, cytotoxicity, nitic oxide scavenging activity, α-glucose oxidase inhibitor

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Authors: Yousef M. Abouzeed A. Elfahem, F. Zgheel, M. A. Saad, Mohamed O. Ahmed

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The bioactive properties of phytochemicals indicate their potential as natural drug products to prevent and treat human disease; in particular, compounds with antioxidant and antimicrobial activities may represent a novel class of safe and effective drugs. Following desiccation, grapes (Vitis vinifera) become more resistant to microbial-based degradation, suggesting that raisins may be a source of antimicrobial compounds. To investigate this hypothesis, total phenolic extracts were obtained from common raisins, local market-sourced. The acetone extract was tested for antibacterial activity against four prevalent bacterial pathogens (Staphylococcus aureus, Pseudomonas aeruginosa, Salmonella spp. and Escherichia coli). Antibiotic sensitivity and the Minimum Inhibitory Concentration (MIC) were determined for each bacterium. High performance liquid chromatography was used to identify compounds in the total phenolic extract. The raisin phenolic extract inhibited growth of all the tested bacteria; the greatest inhibitive effect (normalized to cefotaxime sodium control antibiotic) occurred against P. aeruginosa, followed by S. aureus > Salmonella spp.= E. coli. The phenolic extracts contained the bioactive compounds catechin, quercetin, and rutin. Thus, phytochemicals in raisin extract have antibacterial properties; this plant-based extract, or its bioactive constituents, may represent a promising natural preservative or antimicrobial agent for the food industry or anti-infective drug.

Keywords: Vitis vinifera raisin, extraction, phenolic compounds, antibacterial activity

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Authors: N. Behidj, K. Benyounes, T. Dahmane, A. Allem

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The aim of this study was to investigate the antimicrobial activity of flavonoids isolated from the aerial part of a medicinal plant which is Thymus inodorusby the middle agar diffusion method on following microorganisms. We have Staphylococcus aureus, Escherichia coli, Pseudomonas fluorescens, AspergillusNiger, Aspergillus fumigatus and Candida albicans. During this study, flavonoids extracted by stripping with steam are performed. The yields of flavonoids is 7.242% for the aqueous extract and 28.86% for butanol extract, 29.875% for the extract of ethyl acetate and 22.9% for the extract of di - ethyl. The evaluation of the antibacterial effect shows that the diameter of the zone of inhibition varies from one microorganism to another. The operation values obtained show that the bacterial strain P fluoresces, and 3 yeasts and molds; A. Niger, A. fumigatus and C. albicansare the most resistant. But it is noted that, S. aureus is shown more sensitive to crude extracts, the stock solution and the various dilutions. Finally for the minimum inhibitory concentration is estimated only with the crude extract of Thymus inodorus flavonoid.Indeed, these extracts inhibit the growth of Gram + bacteria at a concentration varying between 0.5% and 1%. While for bacteria to Gram -, it is limited to a concentration of 0.5%.

Keywords: antimicrobial activity, organic extracts, aqueous extracts, Thymus numidicus

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Authors: Methaq Algabr, Nabil Al-Hajj, Ameerh Jaber, Amtellah Alshotobi, Shaima'a Al-suryhi, Gadah Whaban, Nawal Alshehari

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Steam distillation of the essential oil of P. jaubertii was performed using a Clevenger apparatus. Essential oils were analyzed by gas chromatography-flame ionization detector (GC-FID) and gas chromatography coupled to chromatography–mass spectrometry (GC-MS). The major chemical components identified in P. jaubertii essential oil include carvotanacetone (63.975%), 1-methyl-1,2-propanedione (5.887%), 2,5-dimethoxy-para-cymene (3.303%) and ar-curcumene (3.276%). The antimicrobial activity of the essential oil of P. jaubertii was evaluated against all tested microorganisms. P. jaubertii essential oil inhibited all tested microorganisms except Escherichia coli with a minimum inhibitory concentration (MIC) of 5.0 μg/mL against Staphylococcus aureus.

Keywords: Pulicaria jaubertii, essential oil, antimicrobial, Carvotancetone

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Authors: Thilivhali Emmanuel Tshikalange, Darky Cheron Modishane, Frederick Tawi Tabit

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The fruit pulp extracts of twelve selected ethnobotanical wild edible fruits from Mutale local municipality in Venda (Limpopo Province, South Africa) were investigated for their antimicrobial, antioxidant and cytotoxicity activities. Methanol extracts were prepared and tested against six micro-organisms (Salmonella typhi, Streptococcus pyogenes, Bacillus cereus, Klebsiella pneumoniae, Prevotella intermedia and Candida albicans). The minimum inhibitory concentration (MIC) and minimum bactericidal concentration (MBC) were determined using the micro-dilution method, while for antioxidant activity the 2,2-diphenyl-1-picrylhydrazyl method was used. Of the 12 extracts tested, Adonsonia digitata, Berchemia discolor, Manilkara mochisia, Xanthocercis zambesiaca, Landolphia kirkii and Garcinia livingstonei showed antimicrobial activity, with MIC values ranging from 12.5 to 0.4 mg/ml. Gram negative bacteria were more resistant to the extracts in comparison to Gram positive bacteria. Antioxidant activity was only detected in Adonsonia digitata extract and the IC50 (substrate concentration to produce 50% reduction) was found to be 16.18µg/ml. The cytotoxicity of the extracts that showed antimicrobial and antioxidant activities was also determined. All plant extracts tested were non-toxic against human kidney cells (HEK293), with IC50 values of >400 µg/ml. The results presented in this study provide support to some traditional uses of wild edible fruits.

Keywords: antimicrobial, antioxidant, cytotoxicity, ethnobotanical, fruits

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Authors: R. M. Srivastava, Subbanna A.R.N.S, Md Abbas Ahmad, S. P.More, Shivashankar, B. Kalyanbabu

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The similar morphology associated with high genetic variability poses problems in phylogenetic studies of Helicoverpa armigera (Hubner). To identify genetic variation of North Western Himalayan population’s, partial (Mid to terminal region) cytochrome c oxidase subunit I (COX-1) gene was amplified and sequenced for three populations collected from Pantnagar, Almora, and Chinyalisaur. The alignment of sequences with other two populations, Nagpur representing central India population and Anhui, China representing complete COX-1 sequence revealed unanimity in middle region with eleven single nucleotide polymorphisms (SNPs) in Nagpur populations. However, the consensus is missing when approaching towards terminal region, which is associated with 15 each SNPs and pair base substitutions in Chinyalisaur populations. In minimum evolution tree, all the five populations were majorly separated into two clades, one comprising of only Nagpur population and the other with rest. Amongst, North Western populations, Chinyalisaur one is promising by farming a separate clade. The pairwise genetic distance ranges from 0.025 to 0.192 with the maximum between H. armigera populations of Nagpur and Chinyalisaur. This genetic isolation of populations can be attributed to a key role of topological barriers of weather and mountain ranges and temporal barriers due to cropping patterns.

Keywords: cytochrome c oxidase subunit I, northwestern Himalayan population, Helicoverpa armigera (Noctuidae: Lepidoptera), phylogenetic relationship, genetic variation

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Authors: Gabriel S. De Oliveira, Patricia P. Adriani, Christophe Moriseau, Bruce D. Hammock, Felipe S. Chambergo

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Epoxide hydrolases (EHs) are enzymes that are present in all living organisms and catalyze the hydrolysis of epoxides to the corresponding vicinal diols. EHs have high biotechnological interest for the drug design and chemistry transformation for industries. In this study, we describe the identification of substrates and inhibitors of epoxide hydrolase enzyme from the filamentous fungus Trichoderma reesei (TrEH), and these inhibitors showed the fungal growth inhibitory activity. We have used the cloned enzyme and expressed in E. coli to develop the screening in the library of fluorescent substrates with the objective of finding the best substrate to be used in the identification of good inhibitors for the enzyme TrEH. The substrate (3-phenyloxiranyl)-acetic acid cyano-(6-methoxy-naphthalen-2-yl)-methyl ester showed the highest specific activity and was chosen for the next steps of the study. The inhibitors screening was performed in the library with more than three thousand molecules and we could identify the 6 best inhibitors. The IC50 of these molecules were determined in nM and all the best inhibitors have urea or amide in their structure, because It has been recognized that these groups fit well in the hydrolase catalytic pocket of the epoxide hydrolases. Then the growth of T. reesei in PDA medium containing these TrEH inhibitors was tested, and fungal growth inhibition activity was demonstrated with more than 60% of inhibition of fungus growth in the assay with the TrEH inhibitor with the lowest IC50. Understanding how this EH enzyme from T. reesei responds to inhibitors may contribute for the study of fungal metabolism and drug design against pathogenic fungi.

Keywords: epoxide hydrolases, fungal growth inhibition, inhibitor, Trichoderma reesei

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Authors: Ya-Ting Chuang, Krystle Leung, Ya-Jen Chang, Rosemarie H. DeKruyff, Paul B. Savage, Richard Cruse, Christophe Benoit, Dirk Elewaut, Nicole Baumgarth, Dale T. Umetsu

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We examined characteristics of a Natural Killer T (NKT) cell subpopulation that developed during influenza infection in neonatal mice, and that suppressed the subsequent development of allergic asthma in a mouse model. This NKT cell subset expressed CD38 but not CD4, produced IFN-γ, but not IL-17, IL-4 or IL-13, and inhibited the development of airway hyperreactivity (AHR) through contact-dependent suppressive activity against helper CD4 T cells. The NKT subset expanded in the lungs of neonatal mice after infection with influenza, but also after treatment of neonatal mice with a Th1-biasing α-GalCer glycolipid analogue, Nu-α-GalCer. These results suggest that early/neonatal exposure to infection or to antigenic challenge can affect subsequent lung immunity by altering the profile of cells residing in the lung and that some subsets of NKT cells can have direct inhibitory activity against CD4+ T cells in allergic asthma. Importantly, our results also suggest a potential therapy for young children that might provide protection against the development of asthma.

Keywords: NKT subset, asthma, airway hyperreactivity, hygiene hypothesis, influenza

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Authors: Shubham Sharma, Swarna Jaiswal, Brendan Duffy, Amit Jaiswal

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The key features of any active packaging film are its biodegradability and antimicrobial properties. Biological macromolecules such as polyphenols (ferulic acid (FA) and tannic acids (TA)) are naturally found in plants such as grapes, berries, and tea. In this study, antimicrobial activity screening of several polyphenols was carried out by using minimal inhibitory concentration (MIC) and minimum bactericidal concentration (MBC) against two strains of gram-negative bacteria - Salmonella typhimurium, Escherichia coli, and two-gram positive strains - Staphylococcus aureus and Listeria monocytogenes. FA and TA had shown strong antibacterial activity at the low concentration against both gram-positive and gram-negative bacteria. The selected polyphenols FA and TA were incorporated at various concentrations (1%, 5%, and 10% w/w) in the poly(lactide) – poly (butylene adipate-co-terephthalate) (PLA-PBAT) composite film by using the solvent casting method. The effect of TA and FA incorporation in the packaging was characterized based on morphological, optical, color, mechanical, thermal, and antimicrobial properties. The thickness of the FA composite film was increased by 1.5 – 7.2%, while for TA composite film, it increased by 0.018 – 1.6%. FA and TA (10 wt%) composite film had shown approximately 65% - 66% increase in the UV barrier property. As the FA and TA concentration increases from 1% - 10% (w/w), the TS value increases by 1.98 and 1.80 times, respectively. The water contact angle of the film was observed to decrease significantly with the increase in the FA and TA content in the composite film. FA has shown more significant increase in antimicrobial activity than TA in the composite film against Listeria monocytogenes and E. coli. The FA and TA composite film has the potential for its application as an active food packaging.

Keywords: active packaging, biodegradable film, polyphenols, UV barrier, tensile strength

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Authors: Sanja O. Podunavac-Kuzmanović, Strahinja Z. Kovačević, Lidija R. Jevrić, Stela Jokić

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The complexes of transition metals with various organic ligands have been extensively studied as models of some important pharmaceutical molecules. It was found that biological properties of different substituted organic molecules are improved when they are complexed by different metals. Therefore, it is of great importance for the development of coordination chemistry to explore the assembly of functional organic ligands with metal ion and to investigate the relationship between the structure and property. In the present work, we have bioassayed the antibacterial potency of benzimidazoles and their metal salts (Cu or Zn) against yeast Sarcina lutea. In order to validate our in vitro study, we performed in silico studies using molecular docking software. The investigated compounds and their metal complexes (Cu, Zn) showed good to moderate inhibitory activity against Sarcina lutea. In silico docking studies of the synthesized compounds suggested that complexed benzimidazoles have a greater binding affinity and improved antibacterial activity in comparison with non-complexed ligands. These results are part of the CMST COST Action No. 1105 "Functional metal complexes that bind to biomolecules".

Keywords: organometallic complexes, benzimidazoles, chemometric design, Sarcina lutea

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Authors: Jiandong Ren, Lijun Zhao, Peng Chen

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Nafamostat (NA), a synthetic broad-spectrum serine protease inhibitor, has been routinely employed for the treatment of acute pancreatitis (AP) and other inflammatory-associated diseases in some East Asia countries. Although the potent inhibitory activity against inflammation-related proteases such as thrombin, trypsin, kallikrein, plasmin, coagulation factors and complement factors is generally considered to be responsible for the anti-inflammatory effects of NA, precise target and molecular mechanism underlying the anti-inflammatory activity in the treatment of AP remain largely unknown yet. As an intracellular inflammatory signaling platform, the NOD-like receptor protein 3 (NLRP3) inflammasome is recently identified to be involved in the development of AP. In present study, we have revealed that NA alleviated pancreatic injury in a caerulein-induced AP model by inhibiting the NLRP3 inflammasome activation in pancreas. Mechanistically, NA interacted with HDAC6, a cytoplasmic deacetylase implicated in the NLRP3 inflammasome pathway, and efficiently abrogated the function of HDAC6. This property enabled NA to influence HDAC6 dependent NF-κB transcriptional activity and thus block NF-κB-driven transcriptional priming of NLRP3 inflammasome. Moreover, NA exerted the potential to interfere HDAC6-mediated intracellular transport of NLRP3, thereby leading to the failure of NLRP3 inflammasome activation. Our current work has provided valuable insight into the molecular mechanism underlying the immunomodulatory effect of NA in treatment of AP, highlighting its promising application in prevention of NLRP3 inflammasome-associated inflammatory pathological damage.

Keywords: acute pancreatitis, HDAC6, nafamostat, NLRP3 inflammasome

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Authors: Zain Ul Abdin, Mirza Aizaz Asim, Rao Sohail Ahmad Khan, Luqman Amrao, Fiaz Hussain, Hasooba Hira, Saqi Kosar Abbas

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The success of Integrated vector management programmes mainly depends on the correct identification of insect vector species involved in vector borne diseases. Based on molecular data the most important insect species involved as vectors for Zoonotic diseases in Pakistan were identified. The precise and accurate identification of such type of organism is only possible through molecular based techniques like “DNA barcoding”. Morphological species identification in insects at any life stage, is very challenging, therefore, DNA barcoding was used as a tool for rapid and accurate species identification in a wide variety of taxa across the globe and parallel studies revealed that DNA barcoding data can be effectively used in resolving taxonomic ambiguities, detection of cryptic diversity, invasion biology, description of new species etc. A comprehensive survey was carried out for the collection of insects (both adult and immature stages) in district Faisalabad, Pakistan and their DNA was extracted and mitochondrial cytochrome oxidase subunit I (COI-59) barcode sequences was used for molecular identification of immature and adult life stage.This preliminary research work opens new frontiers for developing sustainable insect vectors management programmes for saving lives of mankind from fatal diseases.

Keywords: zoonotic diseases, cytochrome oxidase, and insect vectors, CO1

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Authors: Ibrahim M. Labouta, Gina N. Tageldin, Salwa M. Fahmy, Hayam M. Ashour, Mounir A. Khalil, Tamer M. Ibrahim, Nefertiti A. El-Nikhely

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Bruton’s tyrosine kinase (BTK) is a critical effector molecule in B cell antigen receptor (BCR) signaling transduction. It regulates B cell proliferation, development and survival. Since BTK is widely expressed in many B cell leukaemias and lymphomas, targeting BTK by small molecules inhibitors became an attractive idea as new treatment modalities for B cell mediated hematologic malignancies. Ibrutinib is the 1st generation BTK inhibitor, approved by FDA for treatment of relapsed mantle cell lymphoma (MCL) and chronic lymphocytic leukemia (CLL). It binds irreversibly to the unique cysteine (Cys481) within the ATP-binding pocket of BTK. Besides ibrutinib, many irreversible covalent BTK inhibitors comprising pyrimidine nucleus such as spebrutinib (phase IIb) showed high selectivity and potency when compared to it. In this study, the designed compounds were based on 5-cyano-2-methylsulfanyl pyrimidine core and decorated with electrophilic warheads which are essential for the optimal activity for targeted covalent inhibition (TCI). However, modifications at pyrimidine C4 or C6 were made by introduction of substituted amines which are provided to behave differently. The synthesized derivatives were evaluated for their anticancer activity in leukemia cell lines (e.g. THP-1). Results showed that, some derivatives exhibited antiproliferative activity with IC50 ranged from 5-50 μM, The in vitro enzymatic inhibitory assay for these compounds against BTK is still under investigation. Nevertheless, we could conclude from the initial biological screening that, the synthesized 4 or 6-subsitituted aminopyrimidines represent promising and novel antileukemic agents. Meanwhile, further studies are still needed to attribute this activity through targeting BTK enzyme and inhibition of BCR signaling pathway.

Keywords: BTK inhibitors, hematologic malignancies, structure based drug design (SBDD), targeted covalent inhibitors (TCI)

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Authors: Weiwei Cao, Xiaodong Xing

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In order to effectively resolve the microbial pollution and contamination, synthetic nano-antibacterial materials are widely used in daily life. Among them, nanodiamonds (NDs) have recently been demonstrated to hold promise as useful materials in biomedical applications due to their high specific surface area and biocompatibility. In this work, the copolymer, poly(4-vinylpyridine-co-2-hydroxyethyl methacrylate) was applied for the surface functionalization of NDs to produce the quaternized poly(4-vinylpyridine-co-2-hydroxyethyl methacrylate)-functionalized NDs (QNDs). Then, QNDs were used as a substrate for silver nanoparticles (AgNPs) to produce a QND@Ag hybrid. The composition and morphology of the resultant nanostructures were confirmed by Fourier transform infrared spectra (FT-IR), transmission electron microscope (TEM), X-ray diffraction (XRD), and thermogravimetric analysis (TGA). The mass fraction of AgNPs in the nanocomposites was about 35.7%. The antibacterial performances of the prepared nanocomposites were evaluated with Gram-negative Escherichia coli and Gram-positive Staphylococcus aureus by minimum inhibitory concentration (MIC), inhibition zone testing and time-kill study. As a result, due to the synergistic antibacterial activity of QND and AgNPs, this hybrid showed substantially higher antibacterial activity than QND and polyvinyl pyrrolidone (PVP)-stabilized AgNPs, and the AgNPs on QND@Ag were more stable than the Ag NPs on PVP, resulting in long-term antibacterial effects. More importantly, this hybrid showed excellent water solubility and low cytotoxicity, suggesting the great potential application in biomedical applications. The present work provided a simple strategy that successfully turned NDs into nanosized antibiotics with simultaneous superior stability and biocompatibility, which would broaden the applications of NDs and advance the development of novel antibacterial agents.

Keywords: cationic copolymer, nanodiamonds, silver nanoparticles, dual antibacterial activity, lower cytotoxicity

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Authors: Ferruh Taspinar, Gulce K. Seyyar, Gamze Kurt, Eda O. Okur, Emrah Afsar, Ismail Saracoglu, Betul Taspinar

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Alterations of physical activity can effect body composition (especially body fat ratio); however body mass index may not sufficient to indicate these minimal differences. The aim of this study was to evaluate the relationship between body composition and physical activity in university students. In this study, 132 university students (mean age; 21.21±1.51) were included. Tanita BC-418 and International Physical Activity Questionnaire (IPAQ) were used to evaluate participants. The correlation between the parameters was analysed via Spearman correlation analysis. Significance level in statistical analyses was accepted is 0.05. The results showed that there was no correlation between body mass index and physical activity (p>0.05). There was a positive correlation between body muscle ratio and physical activity, whereas a negative correlation between body fat ratio and physical activity (p<0.05). This study showed that body fat and muscle ratio affects the level of physical activity in healthy university students. Therefore, we thought that physical activity might reduce effects of the diseases caused by disturbed body composition. Further studies are required to support this idea.

Keywords: body composition, body mass index, physical activity, university student

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Authors: Wanthani Paengsri, Thanyarat Chuesaard, Napapha Promsawan

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Spilanthes acmella Murr. was extracted with methanol, yielding methanol crude extract 5.86 %w/w. This study aimed to examine the chemical composition and antioxidant activity of methanolic crude extract. The chemical composition of methanolic crude extract was analyzed by gas chromatography-mass spectrometry (GC-MS). The predominant components were found to be palmitic acid (40.08%), 2-hexadecanoyl glycerol (6.96%) and octadecanoic acid (4.06%). Antioxidant activity was determined using 2,2-diphenyl-1-picryl hydrazyl (DPPH) free radical, for evaluating free radicle scavenging activity. The methanolic extract at 150 µg/mL showed an antioxidant activity with high of radical scavenging activity (75.23%).

Keywords: antioxidant activity, GC-MS analysis, Spilanthes, Phak-Kratt Hauwaen

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Authors: Asad Ali, Asif Jamal

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The agriculture productivity losses due to microbial pathogens have been a serious issue in Pakistan and rest of the world. Present work was designed to isolate soil borne microorganisms having the antagonistic ability against notorious phytopathogens. From the initial collection of 23 bacterial isolates, two potent strains of Bacillus were screened on the basis of their comparative efficacy against devastating fungal pathogens. The strains AK-1 and AK-5 showed excellent inhibitory indexes against the majority of tested fungal strains. It was noted that both strains of Bacillus showed significant biocontrolling activity against Aspergillus flavus, Fusarium moniliforme, Colletotricum falcatum, Botrytis cinerea, Aspergillus niger, Fusarium oxysporum, Phythopthora capsici and Rhizopus oryzae. The strain AK-1 was efficient to suppress Aspergillus species and Rhizopus oryzae while AK-5 expressed significant antagonistic activity against Fusarium, Botrytis and Colletotricum species. On the basis of in vitro assay, it can be postulated that the Bacillus strains AK-1 and AK-5 can be used as bio-protective agent against various plant diseases. In addition, their applications as natural pesticides could be very helpful to prevent the adverse effects of chemical pesticides.

Keywords: bacillus species, biocontrol agent, biopesticides, phytopathogens

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Authors: Akkasit Jongjareonrak, Supansa Namchaiya

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Unripe green coffee cherry (UGCC) accounting about 5 % of total raw material weight receiving to the coffee bean production process and is, in general, sorting out and dump as waste. The UGCC is known to rich in phenolic compounds such as caffeoylquinic acids, feruloylquinic acids, chlorogenic acid (CGA), etc. CGA is one of the potent bioactive compounds using in the nutraceutical and functional food industry. Therefore, this study aimed at optimization the extraction condition of CGA from UGCC using Accelerated Solvent Extractor (ASE). The ethanol/water mixture at various ethanol concentrations (50, 60 and 70 % (v/v)) was used as an extraction solvent at elevated pressure (10.34 MPa) and temperatures (90, 120 and 150 °C). The recovery yield of UGCC crude extract, total phenolic content, CGA content and some bioactivities of UGCC extract were investigated. Using of ASE at lower temperature with higher ethanol concentration provided higher CGA content in the UGCC crude extract. The maximum CGA content was observed at the ethanol concentration of 70% ethanol and 90 °C. The further purification of UGCC crude extract gave a higher purity of CGA with a purified CGA yield of 4.28 % (w/w, of dried UGCC sample) containing 72.52 % CGA equivalent. The antioxidant activity and antimicrobial activity of purified CGA extract were determined. The purified CGA exhibited the 2,2-Diphenyl-1-picrylhydrazyl (DPPH) radical scavenging activity at 0.88 mg Trolox equivalent/mg purified CGA sample. The antibacterial activity against Escherichia coli was observed with the minimum inhibitory concentration (MIC) at 3.12 mg/ml and minimum bactericidal concentration (MBC) at 12.5 mg/ml. These results suggested that using of high concentration of ethanol and low temperature under elevated pressure of ASE condition could accelerate the extraction of CGA from UGCC. The purified CGA extract could be a promising alternative source of bioactive compound using for nutraceutical and functional food industry.

Keywords: bioactive, chlorogenic acid, coffee, extraction

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Authors: Shobha U. Jadhav, R. S. Saler

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Onion is most Important Vegetable crop grown throughout the world. Onion suffers from pest and fungal diseases but the fungicides cause pollution and disturb microbial balance of soil. Under integrated fungal disease management programme cost effective and eco- friendly component like plant extract are used to control plant pathogens. Alternaria porri, Fusarium oxysporium, Stemphylium vesicarium are soil borne pathogens of onion. Effect of three different plant extract (Datura metel, Pongamia pinnata, Ipomoea palmata) at five different concentration Viz, 10,25,50,75 and 100 percentage on these pathogens was studied by food poisoning techniquie. Detura metal gave 94.73% growth of Alternaria porri at 10% extract concentraton and 26.31% growth in 100% extract concentration. As compared to Fusarium oxysporium, and Stemphylium vesicarium, Alternaria porri give good inhibitory response. In Pongamia pinnata L. at 10% extract concentration 84.21% growth and at 100% extract concentration 36.84% growth of Stemphylium vesicarium was observed. Stemphylium vesicarium give good in inhibitory response as compared to Alternaria porri and Fusarium oxysporium. Ipomoea palmata in 10% extract concentration 92% growth and in 100% extract concentration 40% growth of Fusarium oxysporium was recorded. Fusarium oxysporium give good inhibitory response as compared to Alternaria porri and, Stemphylium vesicarium.

Keywords: pathogen, onion, plant extract, Allium cepa L.

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Authors: A. Monika, Manu Sharma, Hong Boo Lee, Richa Dhingra, Neelima Dhingra

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Nuclear factor-κappa B serve as a molecular lynchpin that links persistent infections and chronic inflammation to increased cancer risk. Inflammation has been recognized as a hallmark and cause of cancer. Natural products present a privileged source of inspiration for chemical probe and drug design. Herbal remedies were the first medicines used by humans due to the many pharmacologically active secondary metabolites produced by plants. Some of the metabolites like Lantadene (pentacyclic triterpenoids) from the weed Lantana camara has been known to inhibit cell division and showed anti-antitumor potential. The C-3 aromatic esters of lantadenes were synthesized, characterized and evaluated for cytotoxicity and inhibitory potential against Tumor necrosis factor alpha-induced activation of Nuclear factor-κappa B in lung cancer cell line A549. The 3-methoxybenzoyloxy substituted lead analogue inhibited kinase activity of the inhibitor of nuclear factor-kappa B kinase in a single-digit micromolar concentration. At the same time, the lead compound showed promising cytotoxicity against A549 lung cancer cells with IC50 ( half maximal inhibitory concentration) of 0.98l µM. Further, molecular docking of 3-methoxybenzoyloxy substituted analogue against Inhibitor of nuclear factor-kappa B kinase (Protein data bank ID: 3QA8) showed hydrogen bonding interaction involving oxygen atom of 3-methoxybenzoyloxy with the Arginine-31 and Glutamine-110. Encouraging results indicate the Lantadene’s potential to be developed as anticancer agents.

Keywords: anticancer, lantadenes, pentacyclic triterpenoids, weed

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Authors: Jia H. Wong, Jingli Zhang, Habsah Mohamad, Iswatun H. Abdullah Ripain, Muhammad Bilal, Amelia J. Lloyd, Abdul A. Mohamed Yusoff, Jafri M. Abdullah

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Epilepsy is one of the most common neurological diseases affecting more than 50 million of people worldwide. Epilepsy is a state of recurrent, spontaneous seizures with multiple syndromes and symptoms of different causes of brain dysfunction, prognosis, and treatments; characterized by transient, occasional and stereotyped interruptions of behavior whereby the excitatory-inhibitory activities within the central nervous system (CNS) are thrown out of balance due to various kinds of interferences. The goal of antiepileptic treatment is to enable patients to be free from seizures or to achieve control of seizures through surgical treatment and/or pharmacotherapy. Pharmacotherapy through AED plays an important role especially in countries with epilepsy treatment gap due to costs and availability of health facilities, skills and resources, yet there are about one-third of the people with epilepsy have drug-resistant seizures. Hence, this poses considerable challenges to the healthcare system and the effort in providing cost-effective treatment as well as the search for alternatives to treatment and management of epilepsy. Enhancement of γ-aminobutyric acid (GABA)-mediated inhibitory neurotransmission is one of the key mechanisms of actions of antiepileptic drugs. GABA type > a receptors (GABAAR) are ligand-gated ion channels that mediate rapid inhibitory neurotransmission upon the binding of GABA with a heteropentameric structure forming a central pore that is permeable to the influx of chloride ions in its activated state. The major isoform of GABAA receptors consists of two α1, two β2, and one γ2 subunit. It is the most abundantly expressed combinations in the brain and the most commonly researched through Xenopus laevis oocytes. With the advancing studies on ethnomedicine and traditional treatments using medicinal plants, increasing evidence reveal that spice and herb plants with medicinal properties play an important role in the treatment of ailments within communities across different cultures. Capsaicin is the primary natural capsaicinoid in hot peppers of plant genus Capsicum, consist of an aromatic ring, an amide linkage and a hydrophobic side chain. The study showed that capsaicins conferred neuroprotection in status epilepticus mouse models through anti-ictogenic, hypothermic, antioxidative, anti-inflammatory, and anti-apoptotic actions in a dose-dependent manner. In this study, five capsaicin derivatives were tested for their ability to increase the GABA-induced chloride current on α1β2γ2S of GABAAR expressed on Xenopus laevis oocytes using the method of two-microelectrode voltage clamp. Two of the capsaicin derivatives, IS5 (N-(4-hydroxy-3-methoxybenzyl)-3-methylbutyramide) and IS10 (N-(4-hydroxy-3-methoxybenzyl)-decanamide) at a concentration of 30µM were able to significantly increase the GABA-induced chloride current with p=0.002 and p=0.026 respectively. This study were able to show the enhancement effect of two capsaicin derivatives with moderate length of hydrocarbon chain on this receptor subtype, revealing the promising inhibitory activity of capsaicin derivatives through enhancement of GABA-induced chloride current and further investigations should be carried out to verify its antiepileptic effects in animal models.

Keywords: α1β2γ2 GABAA receptors, α1β2γ2S, antiepileptic, capsaicin derivatives, two-microelectrode voltage clamp, Xenopus laevis oocytes

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