Excellence in Research and Innovation for Humanity

International Science Index

Commenced in January 1999 Frequency: Monthly Edition: International Abstract Count: 50722

Pharmacological and Pharmaceutical Sciences

851
85741
The Cell Viability Study of Extracts of Bark, Flowers, Leaves and Seeds of Indian Dhak Tree, Flame of Forest
Abstract:
In pharmaceutical research and new drug development, medicinal plants have important roles. Similarly, Indian dhak tree belonging to family Fabaceae has been widely used in the traditional Indian medical system of ‘Ayurveda’ for the treatment of a variety of ailments. Hence the cell viability study was undertaken to evaluate and compare the activity of extracts of various parts like flower, bark, leaf, seed by conducting MTT assay method along with other pharmacognostical studies. The methanolic extracts of bark, flowers, leaves, and seeds were used for the study. The cell viability MTT assay was performed using the standard operating procedures. The extracts were dissolved in DMSO and serially diluted with complete medium to get the concentrations range of test concentration. DMSO concentration was kept < 0.1% in all the samples. HUVEC cells maintained in appropriate conditions were seeded in 96 well plates and treated with different concentrations of the test samples and incubated at 37°C, 5% CO₂ for 96 hours. MTT reagent was added to the wells and incubated for 4 hours; the dark blue formazan product formed by the cells was dissolved in DMSO under a safety cabinet and read at 550nm. Percentage inhibitions were calculated and plotted with the concentrations used to calculate the IC50 values. The bark, flower, leaves and seed extracts have shown the cytotoxicity activity and can be further studied for antiangiogenesis activity.
Digital Article Identifier (DAI):
850
85711
Achieving Appropriate Use of Antibiotics through Pharmacists’ Intervention at Practice Point: An Indian Study Report
Abstract:
Antibiotic resistance AR is a global issue, India started to redress the issues of antibiotic resistance late and it plans to have: active surveillance of microbial resistance and promote appropriate use of antibiotics. The present study attempted to achieve appropriate use of antibiotics through pharmacists’ intervention at practice point. In a quasi-experimental prospective cohort study, the cases with bacteremia from four hospitals were identified during 2015 and 2016 for intervention. The pharmacists centered intervention: active screening of each prescription and comparing with the selection of antibiotics with susceptibility of the bacteria. Wherever irrationality noticed, it was brought to the notice of the treating physician for making changes. There were two groups: intervention group and control group without intervention. The active screening and intervention in 915 patients has reduced therapeutic regimen time in patients with bacteremia. The intervention group showed the decreased duration of hospital stay 3.4 days from 5.1 days. Further, multivariate modeling of patients who were in control group showed that patients in the intervention group had a significant decrease in both duration of hospital stay and infection-related mortality. Unlike developed countries, pharmacists are not active partners in patient care in India. This unique attempt of pharmacist’ invention was planned in consultation with hospital authorities which proved beneficial in terms of reducing the duration of treatment, hospital stay, and infection-related mortality. This establishes the need for a collaborative decision making among the health workforce in patient care at least for promoting rational use of antibiotics, an attempt to combat resistance.
Digital Article Identifier (DAI):
849
85709
Role of Medicinal Plants in Treatment of Diseases and Drug Discovery in Azad Kashmir, Pakistan
Abstract:
The present study was conducted to study the role of medicinal plants used to cure different ailments in Azad Kashmir. Various ethno medicinal surveys were carried out during 2016 to enlist the uses of plants against various ailments by rural communities of the area. Information was obtained from 60 local people including 45 males (10 traditional health practitioners) and 15 females by semi structured interviews and group discussions. 65 plant species belonging to 45 families were reported. The dominant plant habit was herbaceous (56%) while decoction was the most common method of utilization (40%). The most cited turmoil was the gastrointestinal disorders. The data obtained were analyzed using ethno medicinal indices such as FL, UV, ICF, FC, and RFC. Results revealed that various species had numerous uses in curing of diseases. So conservation of biodiversity of these medicinal plants and traditional knowledge can play important role in improving the local health conditions of rural people and modern drug discovery and development.
Digital Article Identifier (DAI):
848
85414
Design, Development and Characterization of Pioglitazone Transdermal Drug Delivery System
Abstract:
The main aim of this research work was to design and development characterization of Pioglitazone transdermal drug delivery system by using various polymers such as Olibanum with different concentration by solvent evaporation technique. The prepared formulations were evaluated for different physicochemical characteristics like thickness, folding endurance, drug content, percentage moisture absorption, percentage moisture loss, percentage elongation break test and weight uniformity. The diffusion studies were performed by using modified Franz diffusion cells. The result of dissolution studies shows that formulation, F3 (Olibanum with 50 mg) showed maximum release of 99.95 % in 12hrs, whereas F1 (Olibanum and EC backing membrane) showed minimum release of 93.65% in 12 hr. Based on the drug release and physicochemical values obtained the formulation F3 is considered as an optimized formulation which shows higher percentage of drug release of 99.95 % in 12 hr. The developed transdermal patches increase the therapeutic efficacy and reduced toxic effect of pioglitazone.
Digital Article Identifier (DAI):
847
84939
Influence of ABCB1 2677G > T Single Nucleotide Polymorphism on Warfarin Maintenance Therapy among Patients with Prosthetic Heart Valve
Abstract:
The dose requirement of warfarin to achieve target INR range varies in patients with prosthetic heart valve. This variation in is affected by both genetic and non-genetic factors. Earlier studies have identified role of CYP2C9 and VKORC1 genetic polymorphisms on warfarin dose requirement. Warfarin being a substrate for drug transporter, P-glycoprotein coded by ABCB1 gene, may also be influenced by its genetic polymorphisms. This study was aimed to study the effect of single nucleotide polymorphism (SNP), ABCB1 2677G > T on warfarin maintenance dose requirement in patients with steady-state International Normalized Ratio (INR). The median dose requirement was significantly different between the genotype groups GG vs. GT (35 ± 20; 42.5 ± 18, p < 0.05), GG vs. TT (35 ± 20; 41.25 ± 25, p< 0.05). There was no significant difference between GT vs. TT. In conclusion, patients with variant allele require a higher weekly maintenance dose of warfarin compared to patients without variant allele.
Digital Article Identifier (DAI):
846
83531
Hexahydropyrimidine-2,4-Diones: Synthesis and Cytotoxic Activity
Abstract:
The discovery of new drugs in cancer chemotherapy is still a major topic because of severe side effects, selectivity problems and resistance development potential of existing drugs. In recent years, combined anticancer therapies or multi-acting drugs are clinically preferred over traditional cytotoxic treatment, with the aim of avoiding resistance and toxic side effects. Arrangement of multi-acting targets can be carried out either by combination of several drugs with different mechanisms or by usage of a single chemical compound capable of regulating several targets of a disease with multiple factors. In literature, several pyrimidine and piperazine derivatives have been involved in the structure of many compounds which have been used as chemotherapeutic agents along with wide clinical applications. The aim of this study is to combine pyrimidine and piperazine core structures to research and develop novel piperazinylpyrimidine derivatives with selective cytotoxicity over cancer cells. In this study, a group of novel 6-fluorophenyl-3-[2-(substitutedpiperazinyl)ethyl] hexahydropyrimidine-2,4-dione derivatives designed to observe the desired anticancer activity due to pyrimidine and piperazine based scaffolds. Target compounds were obtained by the reaction of appropriate piperazine derivatives and 6-(2/4-fluorophenyl)-3-(2-chloroethyl)hexahydropyrimidine-2,4-dione. The synthetic pathway of 6-(2/4-fluorophenyl)-3-(2-chloroethyl)hexahydropyrimidine-2,4-dione was started with Rodionov reaction using aldehyde, malonic acid and ammonium acetate in ethanol. Isolated β-fluorophenyl-β-amino acids were treated with 2-chloroethylisocyanate in the presence of an aqueous sodium hydroxide solution at room temperature to yield the sodium salts of the corresponding ureido acids. By addition of a mineral acid, ureido acids were precipitated. Later, these ureido acids were refluxed in thionyl chloride to give the 6-(2/4-fluorophenyl)-3-(2-chloroethyl)hexahydropyrimidine-2,4-di-one which were furthermore treated with secondary amines. Structures of purified compounds were characterized with IR, 1H-NMR, 13C-NMR, mass spectroscopies and elemental analysis. All of the compounds gave satisfactory analytical and spectroscopic data, which were in full accordance with their depicted structures. In IR spectra of the compounds, N-H group was seen at 3230-3213 cm⁻¹. C-H was seen at 3100-2820 cm⁻¹ and C=O vibrational peaks were observed approximately at 1725 and 1665 cm⁻¹ in accordance with literature. In the NMR spectra of target compounds, the methylene protons of piperazine give two separate multiplet peaks around 3.5 and 4.5 ppm representing the successful N-alkylation of the structure. The cytotoxic activity of the synthesized compounds was investigated on human bronchial epithelial (BEAS 2B), lung (A549), colon adenocarcinoma (COLO205) and breast (MCF7) cell lines, by means of sulphorhodamine B (SRB) assays in triplicate. IC₅₀ values of the screened derivatives were found in range of 11.8-78 µM. This project was supported by The Scientific and Technological Research Council of Turkey (TUBITAK, Project no: 215S157).
Digital Article Identifier (DAI):
845
82062
Formulation Development and Evaluation Chlorpheniramine Maleate Containing Nanoparticles Loaded Thermo Sensitive in situ Gel for Treatment of Allergic Rhinitis
Abstract:
The aim of the present study was to fabricate a thermo sensitive gel containing Chlorpheniramine maleate (CPM) loaded nanoparticles following intranasal administration for effective treatment of allergic rhinitis. Chitosan based nanoparticles were prepared by precipitation method followed by the addition of developed NPs within the Poloxamer 407 and carbopol 934P based mucoadhesive thermo-reversible gel. Developed formulations were evaluated for Particle size, PDI, % entrapment efficiency and % cumulative drug permeation. NP3 formulation was found to be optimized on the basis of minimum particle size (143.9 nm), maximum entrapment efficiency (80.10±0.414 %) and highest drug permeation (90.92±0.531 %). The optimized formulation NP3 was then formulated into thermo reversible in situ gel. This intensifies the contact between nasal mucosa and the drug, increases and facilitates the drug absorption which results in increased bioavailability. G4 formulation was selected as the optimize on the basis of gelation ability and mucoadhesive strength. Histology was carried out to examine the damage caused by the optimized G4 formulation. Results revealed no visual signs of tissue damage thus indicated safe nasal delivery of nanoparticulate in situ gel formulation G4. Thus, intranasal CPM NP-loaded in situ gel was found to be a promising formulation for the treatment of allergic rhinitis.
Digital Article Identifier (DAI):
844
81765
Evaluating the Hepato-Protective Activities of Combination of Aqueous Extract of Roots of Tinospora cordifolia and Rhizomes of Curcuma longa against Paracetamol Induced Hepatic Damage in Rats
Abstract:
Objective: To evaluate the hepato-protective activity of Tinospora cordiofolia (Tc) against paracetamol induced hepatic damage in rats. Methods: The plant stem (test drug) was procured locally, shade dried, powdered and extracted with water. Silymarin was used as standard hepatoprotective drugs and 2% gum acacia as a control (vehicle) against paracetamol (PCT) induced hepatotoxicity. Results and Discussion: The hepato-protective activity of aqueous stem extract was assessed by paracetamol induced hepatotoxicity preventive model in rats. Alteration in the levels of biochemical markers of hepatic damage like AST, ALT, ALP and lipid peroxides were tested in both paracetamol treated and untreated groups. Paracetamol (3g/kg) had enhanced the AST, ALT, ALP and the lipid peroxides in the serum. Treatment of silymarin and aqueous stem extract of Tc (200 and 400mg/kg) extract showed significant hepatoprotective activity by altering biochemical marker levels to the near normal. Preliminary phytochemical tests were done. Aqueous Tc extract showed presence of phenolic compound and flavonoids. Our findings suggested that Tc extract possessed hepatoprotective activity in a dose dependent manner. Conclusions: Tc was found to possess significant hepatoprotective property when treated with PCT. This was evident by decreasing the liver enzymes significantly when treated with PCT as compared to PCT only treated group (P < 0.05). Hence Tinospora cardiofolia could be a good, promising, preventive agent against PCT induced hepatotoxicity.
Digital Article Identifier (DAI):
843
81660
Biological Activities of Gentiana brachyphylla Vill. Herba from Turkey
Abstract:
Gentiana, a member of Gentianaceae, is represented by approximately 400 species in the world and 12 species in Turkey. Flavonoids, iridoids, triterpenoids and also xanthones are the major compounds of this genus, have been previously reported to have antiinflammatory, antimicrobial, antioxidant, hepatoprotective, hypotensive, hypoglycaemic, DNA repair and immunomodulatory properties. The methanolic extract of the aerial parts of Gentiana brachyphylla Vill. from Turkey was evaluated for its biological activities and its total phenolic content in the present study. According to the antioxidant activity results, G. brachyphylla methanolic extract showed very strong anti-DNA damage antioxidant activity with an inhibition of 81.82%. It showed weak ferric-reducing power with a EC50 value of 0.65 when compared to BHT (EC50 = 0.2). Also, at 0.5 mg/ml concentration, the methanolic extract inhibited ABTS radical cation activity with an inhibition of 20.13% when compared to Trolox (79.01%). Chelating ability of G. brachyphylla was 44.71% whereas EDTA showed 78.87% chelating activity at 0.2 mg/ml. Also G. brachyphylla showed weak 27.21% AChE, 20.23% BChE, strong 67.86% MAO-A and moderate 50.06% MAO-B, weak 19.14% COX-1, 29.11% COX-2 inhibitory activities at 0.25 mg/ml. The total phenolic content of G. brachyphylla was 156.23 ± 2.73 mg gallic acid equivalent/100 g extract.
Digital Article Identifier (DAI):
842
81657
Determination of Phenolic Contents and Antioxidant Activities of Chenopodium quinoa Willd. Seed Extracts
Abstract:
The genus Chenopodium belongs to Amaranthaceae, is represented by approximately 250 species in the world and 15 species and three subspecies in Turkey. Chenopodium species are traditionally used to treat chest and abdominal pain, shortness of breath, cough and neurological disorders. Chenopodium quinoa Willd. (Quinoa) is native to Andes region of South America (especially Peru and Bolivia) and cultivated in many countries include also Turkey in the world nowadays. The seeds of quinoa are rich in protein, and the phytochemical composition consists of antioxidant substances such as polyphenolic compounds, flavonoids, vitamins, and minerals; anticancer and neuroprotective compounds such as tocotrienols; anti-inflammatory compounds such as carotenoids and anthocyanins and also saponins and starch. Food products of quinoa such as quinoa cereal bar, pasta and cornflakes are used in the diet made during many disorders like obesity, cardiovascular disorder, hypertension and Celiac disease. Also quinoa seems to have antimicrobial, anti-inflammatory and cholesterol-lowering properties because of its bioactive compounds. In this present study, the aqueous ethanolic extracts of the seeds of three different coloured genotypes of quinoa were investigated for their antioxidant activities using 1,1-diphenyl-2-picrylhydrazyl (DPPH) radical scavenging activity, ferrous ion-chelating effect, ferric-reducing antioxidant power, ABTS radical cation decolorization assays and total phenolic contents using Folin-Ciocalteu assay. Among the three genotypes of quinoa; the aqueous ethanolic extract of the red genotype had the highest total phenolic content (83.54 ± 2.12 mg gallic acid/100 g extract) whereas the extract of the white genotype had the lowest total phenolic content (70.66 ± 0.25 mg gallic acid/100 g). According to the antioxidant activity results; the extracts showed moderate reducing power effect whereas weak ABTS radical cation decolorization and ferrous ion-chelating effect and also too weak DPPH radical scavenging activity when compared to the positive standards.
Digital Article Identifier (DAI):
841
81642
Optimization of Lercanidipine Nanocrystals Using Design of Experiments Approach
Abstract:
Lercanidipine hydrochloride is a calcium channel blockers used for treating angina pectoris and hypertension. Lercanidipine is a BCS Class II drug having poor aqueous solubility. Absolute bioavailability of Lercanidipine is very low and the main reason ascribed for this is poor aqueous solubility of the drug. Design and formulatation of nanocrystals by media milling method was main focus of this study. In this present study preliminary optimization was carried out with one factor at a time (OFAT) approach. For this different parameters like size of milling beads, amount of zirconium beads, types of stabilizer, concentrations of stabilizer, concentrations of drug, stirring speeds and milling time were optimized on the basis of particle size, polydispersity index and zeta potential. From the OFAT model different levels for above parameters selected for Plackett - Burman Design (PBD). Plackett-Burman design having 13 runs involving 6 independent variables was carried out at higher and lower level. Based on statistical analysis of PBD it was found that concentration of stabilizer, concentration of drug and stirring speed have significant impact on particle size, PDI, zeta potential value and saturation solubility. These experimental designs for preparation of nanocrystals were applied successfully which shows increase in aqueous solubility and dissolution rate of Lercanidipine hydrochloride.
Digital Article Identifier (DAI):
840
81639
Experimental Design for Formulation Optimization of Nanoparticle of Cilnidipine
Abstract:
Cilnidipine is practically insoluble in water which results in its insufficient oral bioavailability. The purpose of the present investigation was to formulate cilnidipine nanoparticles by nanoprecipitation method to increase the aqueous solubility and dissolution rate and hence bioavailability by utilizing various experimental statistical design modules. Experimental design were used to investigate specific effects of independent variables during preparation cilnidipine nanoparticles and corresponding responses in optimizing the formulation. Plackett Burman design for independent variables was successfully employed for optimization of nanoparticles of cilnidipine. The influence of independent variables studied were drug concentration, solvent to antisolvent ratio, polymer concentration, stabilizer concentration and stirring speed. The dependent variables namely average particle size, polydispersity index, zeta potential value and saturation solubility of the formulated nanoparticles of cilnidipine. The experiments were carried out according to 13 runs involving 5 independent variables (higher and lower levels) employing Plackett-Burman design. The cilnidipine nanoparticles were characterized by average particle size, polydispersity index value, zeta potential value and saturation solubility and it results were 149 nm, 0.314, 43.24 and 0.0379 mg/ml, respectively. The experimental results were good correlated with predicted data analysed by Plackett-Burman statistical method.
Digital Article Identifier (DAI):
839
81329
Absorbed Dose Estimation of ⁶⁸Ga-EDTMP in Human Organs
Abstract:
Bone metastases are observed in a wide range of cancers leading to intolerable pain. While, early detection can help the physicians in the decision of the type of treatment, various radiopharmaceuticals using phosphonates like 68Ga-EDTMP have been developed. In this work, due to the importance of absorbed dose, human absorbed dose of this new agent was calculated for the first time based on biodistribution data in Wild-type rats. 68Ga was obtained from 68Ge/68Ga generator with radionuclidic purity and radiochemical purity of higher than 99%. The radiolabeled complex was prepared in the optimized conditions. Radiochemical purity of the radiolabeled complex was checked by instant thin layer chromatography (ITLC) method using Whatman No. 2 paper and saline. The results indicated the radiochemical purity of higher than 99%. The radiolabelled complex was injected into the Wild-type rats and its biodistribution was studied up to 120 min. As expected, major accumulation was observed in the bone. Absorbed dose of each human organ was calculated based on biodistribution in the rats using RADAR method. Bone surface and bone marrow with 0.112 and 0.053 mSv/MBq, respectively, received the highest absorbed dose. According to these results, the radiolabeled complex is a suitable and safe option for PET bone imaging.
Digital Article Identifier (DAI):
838
81272
Patients' Quality of Life and Caregivers' Burden of Parkinson's Disease
Abstract:
Parkinson’s disease (PD) is a progressive neurodegenerative disorder with evolving layers of complexity. Both motor and non-motor symptoms of PD may affect patients’ quality of life (QoL). Life expectancy for an individual with Parkinson’s disease depends on the level of care the individual has access to, can have a direct impact on length of life. Therefore, improvement of the QoL is a significant part of therapeutic plans. Patients with PD, especially those who are in advanced stages, are in great need of assistance, mostly from their family members or caregivers in terms of medical, emotional, and social support. The role of a caregiver becomes increasingly important with the progression of PD, the severity of motor impairment and increasing age of the patient. The nature and symptoms associated with PD can place significant stresses on the caregivers’ burden. As the prevalence of PD is estimated to more than double by 2030, it is important to recognize and alleviate the burden experienced by caregivers. This study focused on the impact of the clinical features on the QoL of PD patients, and of their caregivers. This study included PD patients along with their caregivers and was undertaken at the Malaysian Parkinson's Disease Association from June 2016 to November 2016. Clinical features of PD patients were assessed using the Movement Disorder Society revised Unified Parkinson Disease Rating Scale (MDS-UPDRS); the Hoehn and Yahr Staging of Parkinson's Disease were used to assess the severity and Parkinson's disease activities of daily living scale were used to assess the disability of Parkinson’s disease patients. QoL of PD patients was measured using the Parkinson's Disease Questionnaire-39 (PDQ-39). The revised version of the Zarit Burden Interview assessed caregiver burden. At least one of the clinical features affected PD patients’ QoL, and at least one of the QoL domains affected the caregivers’ burden. Clinical features ‘Saliva and Drooling’, and ‘Dyskinesia’ explained 29% of variance in QoL of PD patients. The QoL domains ‘stigma’, along with ‘emotional wellbeing’ explained 48.6% of variance in caregivers’ burden. Clinical features such as saliva, drooling and dyskinesia affected the QoL of PD patients. The PD patients’ QoL domains such as ‘stigma’ and ‘emotional well-being’ influenced their caregivers’ burden.
Digital Article Identifier (DAI):
837
81137
Formulation and Evaluation of Dispersible Tablet of Furosemide for Pediatric Use
Abstract:
The objective of this work is to formulate a dry and dispersible form of furosemide in the context of pediatric dose adjustment. To achieve this, we have produced a set of formulas that will be tested in process and after compression. The formula with the best results will be improved to optimize the final shape of the product. Furosemide is the most widely used pediatric diuretic because of its toxicity. The manufacturing process was chosen by taking into account all the data relating to the active ingredient and the excipients used and complying with the specifications and requirements of dispersible tablets. The process used to prepare these tablets was wet granulation. Different excipients were used; lactose, maize starch, Magnésium Stearate and two super-disintegrants which incorporated in the formula by using one at a time or by simultaneously incorporating both while varying their incorporation in formula. The use of super-disintegrating into the formula allowed optimization of the disintegration time. The prepared tablets were evaluated for weight, content uniformity, hardness, disintegration time, friability and in vitro dissolution test.
Digital Article Identifier (DAI):
836
80531
Differential Effects of Parity, Stress and Fluoxetine Treatment on Locomotor Activity and Swimming Behavior in Rats
Abstract:
Peripartum period is a time where women are vulnerable to depression, and stress may further increase the risk of its occurrence. Use of selective serotonin reuptake inhibitors (SSRI) in the treatment of postpartum depression is a common practice. Comparison of antidepressant treatment, however, is rarely studied between gestated and nulliparous animals exposed to stress. This study was aimed to investigate the effect of parity and stress, as well as fluoxetine (an SSRI) treatment after stress exposure on the behavior of rats. Gestating and nulliparous Sprague Dawley rats were either subjected to chronic stressors or left undisturbed throughout the gestation period. After parturition, all stressors were stopped and some of the stressed rats were treated with fluoxetine (10mg/kg). Hence, the final groups formed were: 1. Non-stressed nulliparous rats, 2. Non-stressed dams, 3. Stressed nulliparous rats, 4. Stressed dams, 5. Fluoxetine-treated stressed nulliparous rats, and 6. Fluoxetine-treated stressed dams. Rats were tested in open field test (OFT), novel object recognition test (NOR) and forced swim test (FST) after weaning of pups. Gestational stress significantly reduced the locomotor activity of rats in OFT (p< 0.05), while fluoxetine significantly increased the activity in nulliparous rats (p< 0.001) but not the dams. While no differences were observed in NOR, stress and parity inhibited the rats from performing swimming behavior in FST. However, climbing and immobile behaviors in FST were found to have no significant differences, although there is a tendency of effect of treatment for immobility parameter (p=0.06) where fluoxetine-treated stressed dams were being the least immobile. In conclusion, the effects of parity and stress, as well as fluoxetine treatment, depended on the type of behavioral test performed.
Digital Article Identifier (DAI):
835
80502
Impact of Fluid Flow Patterns on Metastable Zone Width of Borax in Dual Radial Impeller Crystallizer at Different Impeller Spacings
Abstract:
Conducting crystallization in an agitated vessel requires a proper selection of mixing parameters that would result in a production of crystals of specific properties. In dual impeller systems, which are characterized by a more complex hydrodynamics due to the possible fluid flow interactions, revealing a clear link between mixing parameters and crystallization kinetics is still an open issue. The aim of this work is to establish this connection by investigating how fluid flow patterns, generated by two impellers mounted on the same shaft, reflect on metastable zone width of borax decahydrate, one of the most important parameters of the crystallization process. Investigation was carried out in a 15-dm3 bench scale batch cooling crystallizer with an aspect ratio (H/T) equal to 1.3. For this reason, two radial straight blade turbines (4-SBT) were used for agitation. Experiments were conducted at different impeller spacings at the state of complete suspension. During the process of an unseeded batch cooling crystallization, solution temperature and supersaturation were continuously monitored what enabled a determination of the metastable zone width. Hydrodynamic conditions in the vessel achieved at different impeller spacings investigated were analyzed in detail. This was done firstly by measuring the mixing time required to attain the desired level of homogeneity. Secondly, fluid flow patterns generated in a described dual impeller system were both photographed and simulated by VisiMix Turbulent software. Also, a comparison of these two visualization methods was performed. Experimentally obtained results showed that metastable zone width is definitely affected by the hydrodynamics in the crystallizer. This means that this crystallization parameter can be controlled not only by adjusting the saturation temperature or cooling rate, as is usually done, but also by choosing a suitable impeller spacing that will result in a formation of crystals of wanted size distribution.
Digital Article Identifier (DAI):
834
80319
Formulation and in vitro Evaluation of Transdermal Delivery of Articaine
Abstract:
The objective of this study is to formulate different topical preparations containing articaine and to investigate their permeation through goat skin. Initially, articaine and its hydrochloride salt were compared for in vitro permeation using Franz cell model. Goat skin samples were collected after euthanizing male goat kids purchased from the dairy goat farmers. Subcutaneous fat was removed and the skin was mounted on the donor chamber (orifice area 1.00 cm²) and drugs were applied onto the epidermis. Phosphate buffer saline (pH 7.4) was used to maintain sink condition in the receptor chamber (8 ml) of the Franz cell. Samples (0.4 ml) were collected at various intervals over 24 hours after each sampling equal volume of PBS was replaced in the receptor chamber. Articaine in the collected samples were quantified using LC/MS. The results suggested that articaine free base permeates better than its hydrochloride salt through goat skin. This study results support the fact that local anesthetics in its base form are lipophilic and thus penetrates faster through cell membranes than their salts. Later, articaine free base was formulated either using ethanol and octyl salicylate or dimethyl sulfoxide (DMSO) as penetration enhancers and was compared for in vitro permeation. The transdermal flux of articaine in the formulation containing DMSO was approximately 3.8 times higher than that of the formulation containing ethanol and octyl salicylate. Further studies to evaluate the local anesthetic efficacy of the topical formulation containing articaine for dermal anesthesia in animals have been planned.
Digital Article Identifier (DAI):
833
79952
Quality Control Parameters and Pharmacological Aspects of Less Known Medicinal Plant of India: Plumeria pudica Linn.
Abstract:
Plumeria pudica Linn. Family Apocynaceae commonly known as Nag Chmapa is grown wildly in many parts of India. The plant is medium size shrub, grown up to height of 5-10 feet, evergreen with white flowers. In traditional system of medicine, the plant is widely used in the treatment of worms, infection, inflammation, etc. So, far no any systematic and documented study was done to revealed quality control parameters and pharmacological aspect of the selected plant species, therefore, the attempt was made in present investigation to reveal the same. The parameters such as Ash value, FOM, LOD, SI, etc. were studied using various coarsely dried plant materials of the species. Analgesic, anti-inflammatory, anthelmentic and anti-microbial activity of various extract was investigated and reported in present work.
Digital Article Identifier (DAI):
832
79951
Traditional Herbal Medicine Used to Treat Infertility in Women by Traditional Practitioner of Malwa Region of Madhya Pradesh, India
Abstract:
Knowledge of use of traditional medicine is as old as human civilization in almost every system of medicine. Traditional practitioner viz., vaidhayas, ojha, hakim have their own herbal therapy in the treatment of infertility among women’s. Infertility is very common in developed and developing countries due to busy life style of women’s. The present study was initiated with an aim to identify medicinal plants resources from traditional practitioners of Malwa region of Madhya Pradesh to treat infertility. An ethnomedicinal study of Malwa region viz., Indore, Dewas, Ratlam, Ujjain, Dhar, Mandsour and Neemuch of Madhya Pradesh, India comprising fifty-seven study site was conducted during Jan-217 to June-2017. During the course of present investigation, the traditional use of medicinal plants for infertility in women was revealed by traditional practitioner. The botanical name, family, local name, part used, habit along with mode of their administration and dose duration were enumerated.
Digital Article Identifier (DAI):
831
79762
Cardiotrophin-1 and Leptin in Male Patients with Obstructive Sleep Apnea Syndrome
Abstract:
Elevated serum Cardiotrophin-1 (CT-1) and leptin levels are important risk factors for cardiovascular diseases (CVDs). Obstructive sleep apnea syndrome (OSAS) has been reported to increase the risk of CVDs, too. The aim of this study was to evaluate the concentrations of serum CT-1 and leptin in these patients and whether their possible association with the disease severity. Fifty newly diagnosed patients with OSAS and thirty nonapneic snoring subjects were participated in this study. The mean ages of patients and control groups were 47.40±13.30 and 43.23±10.50 years, respectively (P=0.128). Fasting serum triglyseride, total cholesterol, LDL and HDL cholesterol, also CT-1 and leptin levels were evaluated. A significant difference was found in the serum CT-1 and leptin levels between the patients and the controls:serum median CT-1 levels in patients and control groups, respectively, were 19.47 and 8.23 pg/mL (P < 0.001) and leptin levels were 2.07 and 1.29 ng/mL (P < 0.001). In severe patients group (n=39), serum median CT-1 level was found statistically significantly higher than the median level in mild/moderate patients (n=11) group. Patients CT-1 concentrations were not associated with lipoprotein levels and there was no correlation between patients’ leptin and lipid profile parameters. Two risk factors for CVDs, CT-1 and leptin, have significantly elevated and they were associated with OSAS. Furthermore, CT-1 was associated with the severity of disease. We recommend the use of increased serum CT-1 and leptin concentrations as markers of the presence and severity of OSAS.They can be used as early markers in male OSAS patients without known CVDs.
Digital Article Identifier (DAI):
830
79577
Chemical Composition, Antioxidant and Antimicrobial Activities of the Essential Oils of Different Pinus Species from Kosovo
Abstract:
Chemical profile, antioxidant and antimicrobial activity of total and fractionated essential oils (EOs) (F1 – hexane, F2 – hexane/diethyl ether, F3 – diethyl ether) derived from five Pinus species (Pinus heldreichii, P. peuce, P. mugo, Pinus nigra, P. sylvestris), were investigated. The hydrodistilled EOs and their chromatographic fractions (direct solid phase extraction, SPE) were analysed by GC-MS and 112 compounds separated and identified. The main constituents were α-pinene, β-pinene, D-limonene, β-caryophyllene, germacrene D, bornyl acetate and 3-carene. The antioxidant activities of total EOs were lower than those of the corresponding fractions, with F2 the strongest in all cases. EOs and fractions showed different degrees of antibacterial efficacy against different microbial pathogens (moderately strong antimicrobial activity against C. albicans and C. krusei ,while low or no activity against E. faecalis and E. coli strains). The detected inhibition zones and MICs for the EOs and fractions were in the range of 14 -35 mm and 0.125 - 1% (v/v), respectively. The components responsible for the antioxidant and antimicrobial activity were oxygenated monoterpenes and sesquiterpenes recovered in the polar EO fractions. These activities seem to be regulated by reciprocal interactions among the different subclasses of phytochemical species present in the EOs.
Digital Article Identifier (DAI):
829
79572
Evaluation of Antimicrobial Activity of Phenolic Compounds Extracted from Jordanian Juglans regia L.
Abstract:
In this study we have examined of antimicrobial activity for unripe Juglan Regia phenolic extracts against a wide range of pathogenic microorganisms. Walnut (Juglans regia L.) is a member of Juglandaceae family used as a remedy in folk medicine. Leaves, barks, fruits and husk (peel) reported to harbor distinctive medical effect. In our study, we examined the anti-microbial effect against a set of gram positive and negative bacteria and even we have tested them against eukaryotic candida strains in a concentration gradual manner. Ethyl acetate extract of J. regia had the best antibacterial activity when compared with ciprofloxacin. The Minimum inhibition concentration for S. aureus, P. aerogenosa and S. epidermidis MIC was 0.85 mg/mL.
Digital Article Identifier (DAI):
828
79491
Secondary Metabolites Identified from a Pseudoalteromonas rubra Bacterial Strain Isolated from a Fijian Marine Alga
Abstract:
The marine environment has continuously demonstrated to be a rich source of secondary metabolites and bioactive compounds that can address the many pharmaceutical problems facing mankind. The emergence of multidrug resistant pathogens has caused scientists to explore contemporary ways of combating these super bugs. A red-pigmented bacterial strain isolated from a marine alga collected in Fiji was identified to be Pseudoalteromonas rubra from 16s rRNA sequencing. This bacterial strain was cultured using a yeast-peptone media and incubated for five days. The ethyl acetate extract of this bacterium was subjected to chromatographic separation techniques such as vacuum liquid chromatography, flash chromatography, size exclusion chromatography and high-pressure liquid chromatography to yield the pure compound and a number of semi-pure fractions. The crude extract and subsequent purified fractions were analyzed by ultraviolet/visible spectroscopy and mass spectroscopy and was found to contain the compounds ivermectin, stenothricin, cyclo-L-pro-L-val, prodigiosin, mycophenolic acid, phenazine-1-carboxylic acid, eplerenone, staurosporine and pseudoalteromone A. The structure of the pure compound, pseudoalteromone A, was elucidated using NMR 1H, 13C, 1H-1H COSY, HSQC and HMBC spectroscopic data.
Digital Article Identifier (DAI):
827
79050
Antibiotic Potential of Bioactive Compounds from a Marine Streptomyces Isolated from South Pacific Sediments
Abstract:
Two bioactive compounds namely Vulgamycin (also known as enterocin A) and 5-deoxyenterocin were purified from a marine bacterial strain 1903. Strain 1903 was isolated from marine sediments collected from the Solomon Islands. Morphological features of strain 1903 showed that it belongs to the genus Streptomyces. The two secondary metabolites were extracted using EtOAc and purified by chromatographic methods using EtOAc and hexane solvents. Mass spectrum and NMR data of pure compounds were used to elucidate the chemical structures. In this study, results showed that both compounds were strongly active against Wild Type Staphylococcus aureus (WTSA) (MIC < 1 µg/mL) and in Brine shrimp assays (BSA) (MIC < 1 µg/mL). 5-deoxyenterocin was also active against Rifamycin resistant Staphylococcus aureus (RRSA) (MIC, 250 µg/mL) while vulgamycin showed bioactivity against Methicillin resistant Staphylococcus aureus (MRSA) (MIC 250 µg/mL). To the best of our knowledge, this is the first study that showed the bio-activity of 5-deoxyenterocin. This is also the first time that Vulgamycin has been reported to be active in a BSA. There has not been any mechanism of action studies for these two compounds against pathogens. This warrants further studies on their mechanism of action against microbial pathogens.
Digital Article Identifier (DAI):
826
78962
The Impact of Psychopathology Course on Students' Attitudes towards Mental Illness
Abstract:
Background: Negative attitudes towards the mentally ill are widespread and a course for concern as they have a detrimental impact on individuals affected by mental illness. A possible avenue for changing attitudes towards mental illness is through mental health literacy. In a college or university setting, an abnormal psychology course may be introduced in an attempt to change student’s attitudes towards the mentally ill. Objective: To determine if and how students’ attitudes towards the mentally ill change as a result of taking a course in abnormal psychology. Methods: Twenty nine (29) students were recruited from an abnormal psychology class at the University of Botswana. Attitude Scale for Mental Illness (ASMI) questionnaire was administered to participants at the beginning and end of the semester. SPSS was employed to analyze data. Pooled means were used to determine whether the student’s attitudes towards mental illness were negative or positive. A mean of 2.5 translated to negative attitude for both total attitude and attitudes in different domains of the scale. Paired sample t-test was then used to assess whether any changes noted in attitudes were statistically significant or not. Statistical significance was assumed at p < 0.05. Results: Students’ general attitude towards mental illness remained positive although the pooled mean value increased from 2.08 to 2.24. The change was not statistically significant. In relation to different sub scales, the values of the pooled means for all the sub scales showed an increase although the changes were not statistically significant except for the Stereotyping sub scale (p = 0.031). The stereotyping domain reflected a statistically significant change in student’s attitude from positive attitude to negative (X² = 2.06 to X² = 2.55). For the pessimistic prediction domain, students consistently showed a negative attitude (X² = 3.34 to X² = 3.55). The other 4 domains indicated that students had positive attitude toward mentally ill throughout. Discussion: Abnormal psychology students have a positive attitude towards the mentally ill generally. This could be attributed to the fact that all students in the abnormal psychology course are majoring in psychology and research has shown that interest in psychology can affect one’s attitude towards mental illness. The students continuously held the view that people with mental illness are unlikely to improve as evidenced by a high score for Pessimistic prediction domain for both pre and post-test. Students initially had no stereotyping attitude towards the mentally ill, but at the end of the course, they were of the opinion that people with mental illness can be defined in a certain behavioural pattern and mental ability. This results could be an indication that students have learnt well how to differentiate abnormal from normal behaviour not necessarily that students had developed a negative attitude. Conclusion: A course in abnormal psychology does have an impact on the students’ attitudes towards the mentally ill. The impact does not solely depend on knowledge of mental illness but also on several other factors such as contact with the mentally ill, interest in psychology, and teaching methods. However, it should be noted that sometimes improved knowledge in mental illness can be misunderstood for a negative attitude. For example, stereotyping attitudes may be a reflection of the ability to differentiate between abnormal and normal behaviour.
Digital Article Identifier (DAI):
825
78941
Comparison of Extracellular miRNA from Different Lymphocyte Cell Lines and Isolation Methods
Abstract:
The development of a panel of differential gene expression signatures has been of interest in the field of biomarker discovery for radiation exposure. In the absence of the availability of exposed human subjects, lymphocyte cell lines have often been used as a surrogate to human whole blood, when performing ex vivo irradiation studies. The extent of variation between different lymphocyte cell lines is currently unclear, especially with regard to the expression of extracellular miRNA. This study compares the expression profile of extracellular miRNA isolated from different lymphocyte cell lines. It also compares the profile of miRNA obtained when different exosome isolation kits are used. Lymphocyte cell lines were created using lymphocytes isolated from healthy adult males of similar racial descent (Chinese American and Chinese Singaporean) and immortalised with Epstein-Barr virus. The cell lines were cultured in exosome-free cell culture media for 72h and the cell culture supernatant was removed for exosome isolation. Two exosome isolation kits were used. Total exosome isolation reagent (TEIR, ThermoFisher) is a polyethylene glycol (PEG)-based exosome precipitation kit, while ExoSpin (ES, Cell Guidance Systems) is a PEG-based exosome precipitation kit that includes an additional size exclusion chromatography step. miRNA from the isolated exosomes were isolated using miRNEASY minikit (Qiagen) and analysed using nCounter miRNA assay (Nanostring). Principal component analysis (PCA) results suggested that the overall extracellular miRNA expression profile differed between the lymphocyte cell line originating from the Chinese American donor and the cell line originating from the Chinese Singaporean donor. As the gender, age and racial origins of both donors are similar, this may suggest that there are other genetic or epigenetic differences that account for the variation in extracellular miRNA gene expression in lymphocyte cell lines. However, statistical analysis showed that only 3 miRNA genes had a fold difference > 2 at p < 0.05, suggesting that the differences may not be of that great a significance as to impact overall conclusions drawn from different cell lines. Subsequent analysis using cell lines from other donors will give further insight into the reproducibility of results when difference cell lines are used. PCA results also suggested that the method of exosome isolation impacted the expression profile. 107 miRNA had a fold difference > 2 at p < 0.05. This suggests that the inclusion of an additional size exclusion chromatography step altered the subset of the extracellular vesicles that were isolated. In conclusion, these results suggest that extracellular miRNA can be isolated and analysed from exosomes derived from lymphocyte cell lines. However, care must be taken in the choice of cell line and method of exosome isolation used.
Digital Article Identifier (DAI):
824
78862
Establishing a Drug Discovery Platform to Progress Compounds into the Clinic
Authors:
Abstract:
The requirements for progressing a compound to clinical trials is well established and relies on the results from in-vitro and in-vivo animal tests to indicate that it is likely to be safe and efficacious when testing in humans. The typical data package required will include demonstrating compound safety, toxicity, bioavailability, pharmacodynamics (potential effects of the compound on body systems) and pharmacokinetics (how the compound is potentially absorbed, distributed, metabolised and eliminated after dosing in humans). If the desired criteria are met and the compound meets the clinical Candidate criteria and is deemed worthy of further development, a submission to regulatory bodies such as the US Food & Drug Administration for an exploratory Investigational New Drug Study can be made. The purpose of this study is to collect data to establish that the compound will not expose humans to unreasonable risks when used in limited, early-stage clinical studies in patients or normal volunteer subjects (Phase I). These studies are also designed to determine the metabolism and pharmacologic actions of the drug in humans, the side effects associated with increasing doses, and, if possible, to gain early evidence on their effectiveness. In order to reach the above goals, we have developed a pre-clinical high throughput Absorption, Distribution, Metabolism and Excretion–Toxicity (ADME–Toxicity) panel of assays to identify compounds that are likely to meet the Lead and Candidate compound acceptance criteria. This panel includes solubility studies in a range of biological fluids, cell viability studies in cancer and primary cell-lines, mitochondrial toxicity, off-target effects (across the kinase, protease, histone deacetylase, phosphodiesterase and GPCR protein families), CYP450 inhibition (5 different CYP450 enzymes), CYP450 induction, cardio-toxicity (hERG) and gene-toxicity. This panel of assays has been applied to multiple compound series developed in a number of projects delivering Lead and clinical Candidates and examples from these will be presented.
Digital Article Identifier (DAI):
823
78699
Preparation of Flurbiprofen Derivative for Enhanced Brain Penetration
Authors:
Abstract:
Nonsteroidal anti-inflammatory drugs (NSAIDs) are effective for relieving pain and reducing inflammation. They are nonselective inhibitors of two isoforms of COX, cyclooxygenase-1 (COX-1) and cyclooxygenase-2 (COX-2), and thereby inhibiting the production of hormone-like lipid compounds such as, prostaglandins and thromboxanes which cause inflammation, pain, fever, platelet aggregation, etc. In addition, recently there are many research articles reporting the neuroprotective effect of NSAIDs in neurodegenerative diseases, such as Alzheimer’s disease (AD) and Parkinson’s disease (PD). However, the clinical use of NSAIDs in these diseases is limited by low brain distribution. Therefore, in order to assist the in-depth investigation on the pharmaceutical mechanism of flurbiprofen in neuroprotection and to make flurbiprofen a more potent drug to prevent or alleviate neurodegenerative diseases, delivery of flurbiprofen to brain should be effective and sufficient amount of flurbiprofen must penetrate the BBB thus gaining access into the patient’s brain. We have recently developed several types of guanidine-rich molecular carriers with high molecular weights and good water solubility that readily cross the blood-brain barrier (BBB) and display efficient distributions in the mouse brain. The G8 (having eight guanidine groups) molecular carrier based on D-sorbitol was found to be very effective in delivering anticancer drugs to a mouse brain. In the present study, employing the same molecular carrier, we prepared the flurbiprofen conjugate and studied its BBB permeation by mouse tissue distribution study. Flurbiprofen was attached to a molecular carrier with a fluorescein probe and multiple terminal guanidiniums. The conjugate was found to internalize into live cells and readily cross the BBB to enter the mouse brain. Our novel synthetic flurbiprofen conjugate will hopefully delivery NSAIDs into brain, and is therefore applicable to the neurodegenerative diseases treatment or prevention.
Digital Article Identifier (DAI):
822
78563
In vitro Determination of Carbonic Anhydrase Inhibition of the Flowers of Vanda Orchid, Vanda Tessellata Roxb. (1795) by Modified Colorimetric Maren T.H. (1960) Method
Abstract:
The orchid, Vanda tessellata was chosen by the researchers because of the presence of the constituents in the family Orchidaceae such as alkaloids, flavonoids and glycosides that might give an inhibition activity of the carbonic anhydrase enzyme. This study aimed to determine the in vitro inhibition of carbonic anhydrase of Vanda tessellata flower extract. With the use of modified colorimetric Maren T.H. (1960) method, the time in seconds each test solution changed its color after the rate of CO2 hydration were recorded. Two solvents were used: the semi-polar, 95% ethanol and the non-polar, dichloromethane solvents. The percent inhibition activity of carbonic anhydrase of the different concentrations of solvents ethanol (1%, 25% and 50%) and dichloromethane (1% and 10%) test solutions were determined. Results showed that the ethanol-based extract of Vanda tessellata in different concentrations showed an inhibitory effect while the dichloromethane-based extract of Vanda tessellata showed no inhibitory effect of carbonic anhydrase activity. For ethanol extract, the concentration with the highest activity was 50% followed by 25% which changed its color from red to yellow with an average time of 13.11 seconds and 11.57 seconds but 1% with an average time of 7.56 seconds did not exhibit an effect. The researchers recommend the isolation of the specific active constituents of Vanda tessellata that is responsible for the inhibitory effect of carbonic anhydrase enzyme. It is also recommended to utilize different blood types to observe different reactions to the inhibition of the carbonic anhydrase.
Digital Article Identifier (DAI):