Abstract: After cold pressing of pumpkin oil, the defatted oil cake (PUOC) was utilised as raw material for processing of bio-functional hydrolysates. In this study, the in vitro bioactivity of an alcalase (AH) and a pepsin hydrolysate (PH) prepared from the major pumpkin 12S globulin (cucurbitin) are compared. The hydrolysates were produced at optimum reaction conditions (temperature, pH) for the enzymes, during 60min. The bioactivity testing included antioxidant and angiotensin I converting enzyme inhibitory activity assays. The hydrolysates showed high potential as natural antioxidants and possibly antihypertensive agents in functional food or nutraceuticals. Additionally, preliminary studies have shown that both hydrolysates could exhibit modest α-amylase inhibitory activity, which indicates on their hypoglycemic potential.
Abstract: Potential synthesis of a series of 3-amino-4-arylazothiophene derivatives from reaction of 2-cyano-2-phenylthiocarbamoyl acetamide and the appropriate α-halogenated reagents, followed by coupling with different aryl diazonium salts (Japp-Klingemann reaction), and another series of 5-arylazo-thiazol-2-ylcarbamoyl-thiophene derivatives from base-catalyzed intramolecular condensation of 5-arylazo-2-(N-chloroacetyl)amino-thiazole with selected b-keto compounds (Thorpe-Ziegler reaction) was performed. The biological activity of the two series was studied in vitro. Their versatility for pharmaceutical purposes was reported, where they displayed remarkable activities against selected pathogenic microorganisms; Bacillus subtilis, Staphylococcus aureus (Gram positive bacteria), Escherichia coli, Pseudomonas aeruginosa (Gram negative bacteria), and Aspergillus flavus, Candida albicans (fungi) with various degrees related to their chemical structures.
Abstract: Gold nanoparticles (AuNPs) have gained increasing
interest in recent times. This is greatly due to their special features,
which include unusual optical and electronic properties, high stability
and biological compatibility, controllable morphology and size
dispersion, and easy surface functionalization. In typical synthesis,
AuNPs were produced by reduction of gold salt AuCl4 in an
appropriate solvent. A stabilizing agent was added to prevent the
particles from aggregating. The antibacterial activity of different
sizes of gold nanoparticles was investigated against Staphylococcus
aureus, Salmonella typhi and Pseudomonas pneumonia using the disk
diffusion method in a Müeller–Hinton Agar. The Au-NPs were
effective against all bacteria tested. That the Au-NPs were
successfully synthesized in suspension and were used to study the
antibacterial activity of the two medicinal plants against some
bacterial pathogens suggests that Au-NPs can be employed as an
effective bacteria inhibitor and may be an effective tool in medical
field. The study clearly showed that the Au-NPs exhibiting inhibition
towards the tested pathogenic bacteria in vitro could have the same
effects in vivo and thus may be useful in the medical field if well
researched into.
Abstract: The aim of this study was to determine the activity of superoxide dismutase (SOD), glutathione peroxidase (GPx), total antioxidant status (TAS) and accumulation of Hsp70 in porcine ovarian granulosa cells after deoxynivalenol (DON) and zearalenone (ZEA) exposure in vitro. Porcine ovarian granulosa cells were incubated with DON/ZEA administrations as follows: group A (10/10 ng/mL), group B (100/100 ng/mL), group C (1000/1000 ng/mL), and the control group without any additions for 24h. In this study mycotoxins developed stress reaction of porcine ovarian granulosa cells and increased accumulation of Hsp70 what resulted in increasing activities of SOD and GPx in groups with lower doses of mycotoxins. High dose of DON and ZEA had opposite effect on GPx activity than the lower doses. Slight increase in TAS of porcine granulosa cells was observed after mycotoxins exposure. These results contribute towards the understanding of cellular stress and its response.
Abstract: The main perspective of the present study aims at overcoming solubility problems by using the technique of solid dispersion. Repaglinide is a BCS Class II drug, having low aqueous solubility and therefore, low bioavailability. Solid dispersions of repaglinide with different carriers Polyvinyl Pyrrolidone (PVP) and Ethyl Cellulose (EC) in different ratios were prepared by suspending method and Dissolving methods. In vitro release studies revealed that the F7 formulation showed extended drug release. So, the dissolution profile of solid dispersion containing EC and PVP K30 (1: 3) was selected as the best formulation because of its extended drug release among all formulations. In conclusion, solid dispersions of Repaglinide in PVP have shown to be a promising approach to improve the bioavailability of Repaglinide.
Abstract: In this study, the in vitro anticholinesterase activity of
the volatile oils of both O. basilicum and O. africanum was
investigated and both samples showed significant activity. The major
constituents of the two oils were isolated using several column
chromatographies. Linalool, 1,8-cineol and eugenol were isolated
from the volatile oil of O. basilicum and camphor was isolated from
the volatile oil of O. africanum. The anticholinesterase activities of
the isolated compounds were also evaluated where 1,8-cineol showed
the highest inhibitory activity followed by camphor. To confirm these
activities, learning and memory enhancing effects were tested in
mice. Memory impairment was induced by scopolamine, a
cholinergic muscarinic receptor antagonist. Anti-amnesic effects of
both volatile oils and their terpenoids were investigated by the
passive avoidance task in mice. We also examined their effects on
brain acetylcholinesterase activity. Results showed that scopolamineinduced
cognitive dysfunction was significantly attenuated by
administration of the volatile oils and their terpenoids, eugenol and
camphor, in the passive avoidance task and inhibited brain
acetylcholinesterase activity. These results suggest that O. basilicum
and O. africanum volatile oils can be good candidates for further
studies on Alzheimer’s disease via their acetylcholinesterase
inhibitory actions.
Abstract: Aldehyde oxidase is molybdo-flavoenzyme involved in the oxidation of hundreds of endogenous and exogenous and N-heterocyclic compounds and environmental pollutants. Uncharged N-heterocyclic aromatic compounds such phenanthridine are commonly distributed pollutants in soil, air, sediments, surface water and groundwater, and in animal and plant tissues. Phenanthridine as uncharged N-heterocyclic aromatic compound was incubated with partially purified aldehyde oxidase from rainbow trout fish liver. Reversed-phase HLPC method was used to separate the oxidation products from phenanthridine and the metabolite was identified. The 6(5H)-phenanthridinone was identified the major metabolite by partially purified aldehyde oxidase from fish liver. Kinetic constant for the oxidation reactions were determined spectrophotometrically and showed that this substrate has a good affinity (Km = 78 ± 7.6µM) for hepatic aldehyde oxidase, will be a significant pathway. This study confirms that partially purified aldehyde oxidase from fish liver is indeed the enzyme responsible for the in vitro production 6(5H)-phenanthridinone metabolite as it is a major metabolite by mammalian aldehyde oxidase, coupled with a relatively high oxidation rate (0.77± 0.03 nmol/min/mg protein). In addition, the kinetic parameters of hepatic fish aldehyde oxidase towards the phenanthridine substrate indicate that in vitro biotransformation by hepatic fish aldehyde oxidase will be a significant pathway. This study confirms that partially purified aldehyde oxidase from fish liver is indeed the enzyme responsible for the in vitro production 6(5H)-phenanthridinone metabolite as it is a major metabolite by mammalian aldehyde oxidase.
Abstract: The aim of the present work was to test in vitro inhibition of food pathogens and spoilage bacteria by crude bacteriocins from autochthonous lactic acid bacteria. Thirty autochthonous lactic acid bacteria isolated previously, belonging to the genera: Lactobacillus, Carnobacterium, Lactococcus, Vagococcus, Streptococcus, and Pediococcus, have been screened by an agar spot test and a well diffusion assay against Gram-positive and Gram-negative harmful bacteria: Bacillus cereus, Bacillus subtilis ATCC 6633, Escherichia coli ATCC 8739, Salmonella typhimurium ATCC 14028, Staphylococcus aureus ATCC 6538, and Pseudomonas aeruginosa under conditions means to reduce lactic acid and hydrogen peroxide effect to select bacteria with high bacteriocinogenic potential. Furthermore, crude bacteriocins semiquantification and heat sensitivity to different temperatures (80, 95, 110°C, and 121°C) were performed. Another exploratory test concerning the response of St. aureus ATCC 6538 to the presence of crude bacteriocins was realized. It has been observed by the agar spot test that fifteen candidates were active toward Gram-positive targets strains. The secondary screening demonstrated an antagonistic activity oriented only against St. aureus ATCC 6538, leading to the selection of five isolates: Lm14, Lm21, Lm23, Lm24, and Lm25 with a larger inhibition zone compared to the others. The ANOVA statistical analysis reveals a small variation of repeatability: Lm21: 0.56%, Lm23: 0%, Lm25: 1.67%, Lm14: 1.88%, Lm24: 2.14%. Conversely, slight variation was reported in terms of inhibition diameters: 9.58± 0.40, 9.83± 0.46 and 10.16± 0.24 8.5 ± 0.40 10 mm for, Lm21, Lm23, Lm25, Lm14and Lm24, indicating that the observed potential showed a heterogeneous distribution (BMS = 0.383, WMS = 0.117). The repeatability coefficient calculated displayed 7.35%. As for the bacteriocins semiquantification, the five samples exhibited production amounts about 4.16 for Lm21, Lm23, Lm25 and 2.08 AU/ml for Lm14, Lm24. Concerning the sensitivity the crude bacteriocins were fully insensitive to heat inactivation, until 121°C, they preserved the same inhibition diameter. As to, kinetic of growth , the µmax showed reductions in pathogens load for Lm21, Lm23, Lm25, Lm14, Lm24 of about 42.92%, 84.12%, 88.55%, 54.95%, 29.97% in the second trails. Inversely, this pathogen growth after five hours displayed differences of 79.45%, 12.64%, 11.82%, 87.88%, 85.66% in the second trails, compared to the control. This study showed potential inhibition to the growth of this food pathogen, suggesting the possibility to improve the hygienic food quality.
Abstract: Alongside with antioxidant, pro-oxidant activity is also observed in phytochemical compounds. In the study, Ficus odorata, an endemic medicinal plant in the Philippines, was screened for the potential medical application of its pro-oxidant activity.
Phytochemical screening revealed the presence of terpenes, glycosides and phenolic acids. The crude extract was found to contain low gallic acid and quercetin equivalence. The TLC chromatogram of the crude extract showed that none of the 11 spots obtained has antioxidant activity nor correspond to gallic acid and quercetin standards. Experiments showed that the crude extract has stimulatory activity towards DPPH radicals, hydrogen peroxide, hydroxyl radicals, superoxide anions and nitric oxide. Moreover, the extract exhibited a low ferric reducing power.
The prooxidant activity was evident in the crude ethanolic leaf extract of F. odorata, which may provide a better understanding of the plant’s pharmacological importance in the prevention of diseases.
Abstract: The nanotechnology offers some exciting possibilities in cancer treatment, including the possibility of destroying tumors with minimal damage to healthy tissue and organs by targeted drug delivery systems. Considerable achievements in investigations aimed at the use of ZnO nanoparticles and nanocontainers in diagnostics and antitumor therapy were described. However, there are substantial obstacles to the purposes to be achieved by the use of zinc oxide nanosize materials in antitumor therapy. Among the serious problems are the techniques of obtaining ZnO nanosize materials. The article presents a new vector delivery system for the known antitumor drug, doxorubicin in the form of polymeric (PEO, starch-NaCMC) hydrogels, in which nanosize ZnO film of a certain thickness are deposited directly on the drug surface on glass substrate by DC-magnetron sputtering of a zinc target. Anticancer activity in vitro and in vivo of those nanosize zinc oxide composites is shown.
Abstract: This study was conducted to evaluate the response of almond genotypes to osmotic stress in vitro in order to screen drought tolerance. Explants subjected to polyethyleneglycol osmotic stress (0, 3.5, and 7.0% WV) on the MS medium. Concentrations of photosynthesis pigments, anthocyanins, and carothenoids were significantly reduced under osmotic stress. Under osmotic stress, leaf water content, cellular membrane stability and pigments concentrations were significantly higher in the leaves of drought tolerant genotypes. The results revealed that carotenoids and anthocyanins may act as photoprotectant compounds in almond leaves and involved in drought tolerance system of the plant.
Abstract: Two types of crushing were applied to grains of red sorghum: manual crushing using a mortar and pestle of kitchen and mechanical crushing using a hammer mill. The flours obtained at the end of these various crushing were filtered and subdivided in different fractions according to the diameters of the mesh of the sieves (0.16mm; 0.25mm; 0.315mm; 0.4mm, and 0.63mm…). Some physical, chemical and nutritional traits of these flours were evaluated using Association of Official Analytical Chemists (AOAC). In vitro digestibility of these flours was also studied with freezing of flour 1% like substrate and α-amylase from B. licheniformis (E.C.3.2.1.1; Megazyme, Wicklow, Ireland). The results revealed that the batches of flours which have the finest diameters as 0.16mm; 0.25mm are the richest one in nutrients and are also the most digestible. Also mechanical crushing is the best mean to obtain significant amount of flours. In conclusion, the type of crushing and the size of the particles have an impact on the final concentration of some nutrients of the flours obtained. Indeed, the finest particles (0.16mm – 0.25mm 0.315mm) obtained after sifting of the flours are more nutritive and have a better digestibility than others size. So the finest particles could be advised for management of cereals namely the sorghum for the production of the infantile foods.
Abstract: By hand pollination was conducted to evaluated different pollen sources and their affects on fruit set and quality of wax apple. The following parameters were recorded: fruit set, seed set, fruit characteristics. Results showed that fruit set percentage with seed were significantly high in ‘Long Red B’ when ‘Black’, ‘Thyto’ were used as pollen parents. Pollen of ‘Black’, ‘Thyto’ resulted in high fruit weight, fruit diameter, fruit length, bigger flesh thickness, better total soluble solids as compared with other pollens. The observation of pollen-growth in vitro revealed that pollen germination at 15% sucrose concentration are required for optimum pollen germination with the high pollen germination were found in ‘Black’, ‘Thyto’. From the result, we concluded that ‘Black’, ‘Thyto’ were proved to be good pollinizers in ‘Long Red B’. Therefore, artificial cross-pollination using ‘Black’, ‘Thyto’ as pollinizers were strongly recommended for ‘Long Red B’ cultivar in wax apple orchard.
Abstract: The purpose of this study was to prepare time and pH dependent release tablets of Ayurvedic Churna formulation and evaluate their advantages as colon targeted drug delivery system. The Vidangadi Churna was selected for this study which contains Embelin and Gallic acid. Embelin is used in Helminthiasis as therapeutic agent. Embelin is insoluble in water and unstable in gastric environment so it was formulated in time and pH dependent tablets coated with combination of two polymers Eudragit L100 and ethyl cellulose. The 150mg of core tablet of dried extract and lactose were prepared by wet granulation method. The compression coating was used in the polymer concentration of 150mg for both the layer as upper and lower coating tablet was investigated. The results showed that no release was found in 0.1 N HCl and pH 6.8 phosphate buffers for initial 5 hours and about 98.97% of the drug was released in pH 7.4 phosphate buffer in total 17 Hours. The in vitro release profiles of drug from the formulation could be best expressed first order kinetics as highest linearity (r2= 0.9943). The results of the present study have demonstrated that the time and pH dependent tablets system is a promising vehicle for preventing rapid hydrolysis in gastric environment and improving oral bioavailability of Embelin and Gallic acid for treatment of Helminthiasis.
Abstract: Floating tablets of Marichyadi Vati were developed with an aim to prolong its gastric residence time and increase the bioavailability of drug. Rapid gastrointestinal transit could result in incomplete drug release from the drug delivery system above the absorption zone leading to diminished efficacy of the administered dose. The tablets were prepared by wet granulation technique, using HPMC E50 LV act as Matrixing agent, Carbopol as floating enhancer, microcrystalline cellulose as binder, Sodium bi carbonate as effervescent agent with other excipients. The simplex lattice design was used for selection of variables for tablets formulation. Formulation was optimized on the basis of floating time and in vitro drug release. The results showed that the floating lag time for optimized formulation was found to be 61 second with about 97.32 % of total drug release within 3 hours. The vitro release profiles of drug from the formulation could be best expressed zero order with highest linearity r2 = 0.9943. It was concluded that the gastroretentive drug delivery system can be developed for Marichyadi Vati containing Piperine to increase the residence time of the drug in the stomach and thereby increasing bioavailability.
Abstract: Novel solid lipid nanoparticles (SLNs) were developed to improve oral bioavailability of oxyresveratrol (OXY). The SLNs were prepared by a high speed homogenization technique, at an effective speed and time, using Compritol® 888 ATO (5% w/w) as the solid lipid. The appropriate weight proportions (0.3% w/w) of OXY affected the physicochemical properties of blank SLNs. The effects of surfactant types on the properties of the formulations such as particle size and entrapment efficacy were also investigated. Conclusively, Tween 80 combined with soy lecithin was the most appropriate surfactant to stabilize OXY-loaded SLNs. The mean particle size of the optimized formulation was 134.40 ± 0.57 nm. In vitro drug release study, the selected S2 formulation showed a retarded release profile for OXY with no initial burst release compared to OXY suspension in the simulated gastrointestinal fluids. Therefore, these SLNs could provide a suitable system to develop for the oral OXY delivery.
Abstract: This study was designed for assessment of 3 types of Cysteine protease inhibitors (CPIs) fluromethylketone (FMK), vinyl sulfone (VS) and sodium nitro prussid (SNP), to define which of them is the best for curing S. mansoni infection in mice? In vitro, treated S. mansoni adult worms recorded a mortality rate after 1 hr of exposure to 500 ppm of FMK, VS and SNP as 75, 70 and 60%, respectively. FMK+PZQ treatment recorded the maximum reduction in worm burden (97.2% at 5 wk PI). VS treatment alone or combined with PZQ increases IgM, total IgG, IgG2 and IgG4 levels. In EM study, the completely implanted spines were reported in the degenerated tegument of adult worms in all groups treated with CPIs. VS+PZQ Treatment increased Igs levels but, its effect was different on worm reduction. So, it is not enough to eliminate the infection and FMK+PZQ considered the antischistosomicidal drug of choice.
Abstract: Chitosan (CH) material reinforced by bioactive glass (46S6) was fabricated. 46S6 containing 17% wt% CH was studied in vitro and in vivo. Physicochemical techniques, such as Fourier transform infrared spectroscopy (FT-IR), coupled plasma optical emission spectrometry (ICP-OES) analysis were used. The behavior of 46S6CH17 was studied by measuring the in situ pH in a SBF solution. The 46S6CH17 was implanted in the rat femoral condyl. In vitro 46S6CH17 gave an FTIR - spectrum in which three absorption bands with the maxima at 565, 603 and 1039cm-1 after 3 days of soaking in physiological solution. They are assigned to stretching vibrations of PO4^3- group in phosphate crystalline. Moreover, the pH measurement was decreased in the SBF solution. The stability of the calcium phosphate precipitation depended on the pH value. In vivo, a rise in the Ca and phosphate P ions concentrations in the implanted microenvironment was determined.
Abstract: The highest extractable concentration in the artificial sweat fluid was observed for Ba (120mg/kg; d.w.). The highest extractable concentration in the artificial gastric fluid was observed for Al (9030mg/kg; d.w.). Furthermore, the extractable concentrations of Ba (550mg/kg; d.w.) and Zn (400mg/kg: d.w.) in the bottom ash using artificial gastric fluid were elevated. The extractable concentrations of all heavy metals in the artificial gastric fluid were higher than those in the artificial sweat fluid. These results are reasonable in the light of the fact that the pH of the artificial gastric fluid was extremely acidic both before (pH 1.54) and after (pH 1.94) extraction, whereas the pH of the artificial sweat fluid was slightly alkaline before (pH 6.50) and after extraction (pH 8.51).
Abstract: Quercetin and (+)-catechin are metabolites present in Phyllanthus niruri plant, have potential in medicinal uses as anticancer and antioxidant agents. Studies on production of quercetin and (+)-catechin from P. niruri callus culture via in vitro technique were carried out and the results were compared to the intact plant. P. niruri explants were cultured on Murashige and Skoog (MS) solidified media supplemented with several phytohormone combinations for one month. The metabolites were extracted from P. niruri callus and intact plant by using carbon dioxide supercritical fluid extraction (SFE) with ethanol as modifier and solvent extraction techniques. The extracts were analyzed by means of HPLC method. Results showed that P. niruri callus culture was successfully established. The highest content of quercetin (1.72%) was found from P. niruri callus grown in media supplemented with 0.8mg/L kinetin and 0.2mg/L 2,4-dicholophenoxyacetic acid (2,4-D), which was 1.2 fold higher than intact plant. Meanwhile, the highest amounts of (+)-catechin (0.63%) was found from P. niruri callus grown in media with addition of 0.2mg/L 1-naphthalene acetic acid (NAA) and 0.8mg/L 2,4-D. The SFE condition in this study showed better extraction efficiency when higher contents of selected metabolites were found in all SFE extracts compared to the common solvent extracts.