Search results for: drug%E2%80%93drug%20interactions

Authors: Noshaba Dilbar, Maria Jabbar

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Medicinal plants are considered to be the richest source of drug discovery. The main cause of medicinal properties of plants is the presence of bioactive compounds in them. Phytochemical screening is the valuable process that detects bioactive compounds(secondary metabolites) in plants. The present study was carried out to determine phytochemical profile and ethnobotanical importance of Capparidaceae species. ( Capparis spinosa and Dipterygium glaucum). The selection of plants was made on basis of traditional knowledge of their usage in ayurvedic medicines. Different type of solvents(ethanol, methanol, chloroform, benzene and petroleum ether) were used to make extracts of dry and fresh plants. Phytochemical screening was made by using various standard techniques. Results reveal the presence of large range of bioactive compounds i.e alakloids, saponins, flavonoids, terpenoids, glycosides, phenols and steroids. Methanol, petroleum ether and chloroform extracts showed high extractability of bioactive compounds. The results obtained ensure these plants a reliable source of pharmacological industry and can be used in making of various biological friendly drugs.

Keywords: bioactive compounds, Capparidaceae, phytochemical screening, secondary metabolites

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Authors: Danielle Page

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Foregoing studies, statistics, and medical evaluations have established a relationship between Posttraumatic stress disorder (PTSD) and criminal justice involvement in Vietnam veterans. War is highly trauma inducing and can leave combat veterans with mental disorders ranging from psychopathic thoughts to suicidal ideation. The majority of those suffering are unaware that they have PTSD, and as a coping mechanism, they often turn to self isolation. Beyond isolation, many veterans with symptomatic PTSD turn to aggression and substance abuse to cope with their internal agony. The most common crimes committed by veterans with PTSD fall into the assault and drug/alcohol abuse categories. Thus, a relationship is established between veteran populations and the criminal justice system. This dissertation aims to define the relationship between PTSD and criminal justice involvement in veterans, explore the mediating factors in this relationship, and analyze numerous court cases in this subject area. Further, it will examine the ways in which crime rates can be reduced for veterans with symptoms of PTSD. This ranges from the improvement of healthcare systems to the implementation of special courts to handle veteran cases.

Keywords: psychotraumatology, forensic psychology, PTSD, vietnam veterans

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Authors: Rachel F. Ajayi, Unathi Sidwaba, Usisipho Feleni, Samantha F. Douman, Ezo Nxusani, Lindsay Wilson, Candice Rassie, Oluwakemi Tovide, Priscilla G.L. Baker, Sibulelo L. Vilakazi, Robert Tshikhudo, Emmanuel I. Iwuoha

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Pyrazinamide (PZA) is among the first-line pro-drugs in the tuberculosis (TB) combination chemotherapy used to treat Mycobacterium tuberculosis. Numerous reports have suggested that hepatotoxicity due to pyrazinamide in patients is due to inappropriate dosing. It is therefore necessary to develop sensitive and reliable techniques for determining the PZA metabolic profile of diagnosed patients promptly and at point-of-care. This study reports the determination of PZA based on nanobiosensor systems developed from disuccinimidyl octanedioate modified Cytochrome P450-2E1 (CYP2E1) electrodeposited on gold substrates derivatised with (poly(8-anilino-1-napthalene sulphonic acid) PANSA/PVP-AgNPs nanocomposites. The rapid and sensitive amperometric PZA detection gave a dynamic linear range of 2 µM to 16 µM revealing a limit of detection of 0.044 µM and a sensitivity of 1.38 µA/µM. The Michaelis-Menten parameters; KM, KMapp and IMAX were also calculated and found to be 6.0 µM, 1.41 µM and 1.51 µA respectively indicating a nanobiosensor suitable for use in serum.

Keywords: tuberculosis, cytochrome P450-2E1, disuccinimidyl octanedioate, pyrazinamide

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Authors: Van Tran Thi Thuy, Cheol Won Lim, Dukjoon Kim

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A series of biodegradable copolymers based on polyaspartamide (PASPAM) were synthesized by grafting hydrophilic O-(2-aminoethyl)-O'-methylpoly(ethylene glycol) (MPEG), hydrophobic cholic acid (CA), and pH-sensitive hydrazine (Hyd) segments on a PASPAM backbone. The hydrazine group was effectively cleaved to release doxorubicin (DOX) conjugated on PASPAM in an acidic environment. The chemical structure of the polymer and the degree of substitution of each graft segment were analyzed using FT-IR and 1H-NMR spectroscopy. The size of the MPEG/Hyd/CA-g-PASPAM copolymer self-aggregates was examined by dynamic light scattering (DLS) and transmission electron microscope (TEM). The mean diameter of the self - aggregates increased from 125 to 200 nm at pH 7.4, as the degree of substitution of CA increased from 10 to 20 %. The release kinetics of DOX was strongly affected by the pH of the releasing medium. While less than 30% of the DOX-loaded was released in about 30 h at pH 7.4, more than 60% was released at pH 5.0 within the same time. The viability tests of human breast cancer cells (MCF-7) and human embryonic kidney cells (293T) show the potential application of MPEG/Hyd/CA-g-PASPAM copolymer self-aggregates in the controlled intracellular delivery for cancer treatments.

Keywords: pH-sensitive, drug delivery, polyaspartamide, self-assembly, nano-aggregates

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Authors: Ece A. Irmak, Amdulla O. Mekhrabov, M. Vedat Akdeniz

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There is a growing interest in the modeling and simulation of magnetic nanoalloys by various computational methods. Magnetic crystalline/amorphous nanoparticles (NP) are interesting materials from both the applied and fundamental points of view, as their properties differ from those of bulk materials and are essential for advanced applications such as high-performance permanent magnets, high-density magnetic recording media, drug carriers, sensors in biomedical technology, etc. As an important magnetic material, Fe-Ni based nanoalloys have promising applications in the chemical industry (catalysis, battery), aerospace and stealth industry (radar absorbing material, jet engine alloys), magnetic biomedical applications (drug delivery, magnetic resonance imaging, biosensor) and computer hardware industry (data storage). The physical and chemical properties of the nanoalloys depend not only on the particle or crystallite size but also on composition and atomic ordering. Therefore, computer modeling is an essential tool to predict structural, electronic, magnetic and optical behavior at atomistic levels and consequently reduce the time for designing and development of new materials with novel/enhanced properties. Although first-principles quantum mechanical methods provide the most accurate results, they require huge computational effort to solve the Schrodinger equation for only a few tens of atoms. On the other hand, molecular dynamics method with appropriate empirical or semi-empirical inter-atomic potentials can give accurate results for the static and dynamic properties of larger systems in a short span of time. In this study, structural evolutions, magnetic and electronic properties of Fe-Ni based nanoalloys have been studied by using molecular dynamics (MD) method in Large-scale Atomic/Molecular Massively Parallel Simulator (LAMMPS) and Density Functional Theory (DFT) in the Vienna Ab initio Simulation Package (VASP). The effects of particle size (in 2-10 nm particle size range) and temperature (300-1500 K) on stability and structural evolutions of amorphous and crystalline Fe-Ni bulk/nanoalloys have been investigated by combining molecular dynamic (MD) simulation method with Embedded Atom Model (EAM). EAM is applicable for the Fe-Ni based bimetallic systems because it considers both the pairwise interatomic interaction potentials and electron densities. Structural evolution of Fe-Ni bulk and nanoparticles (NPs) have been studied by calculation of radial distribution functions (RDF), interatomic distances, coordination number, core-to-surface concentration profiles as well as Voronoi analysis and surface energy dependences on temperature and particle size. Moreover, spin-polarized DFT calculations were performed by using a plane-wave basis set with generalized gradient approximation (GGA) exchange and correlation effects in the VASP-MedeA package to predict magnetic and electronic properties of the Fe-Ni based alloys in bulk and nanostructured phases. The result of theoretical modeling and simulations for the structural evolutions, magnetic and electronic properties of Fe-Ni based nanostructured alloys were compared with experimental and other theoretical results published in the literature.

Keywords: density functional theory, embedded atom model, Fe-Ni systems, molecular dynamics, nanoalloys

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Authors: Rakesh Kumar, Shashi Janeoo, Ankit Dhiman, Siddharth Chopra

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Arynes are versatile reactive intermediates that offer broad opportunities in green organic synthesis. Arynes are potential aryl group surrogates for the transition metal-free environment friendly arylation reactions. Regioselective arylations of quinolines were achieved by the reactions of quinoline N-oxides with aryne intermediates generated in situ from the Kobayashi precursors. Various 2-substituted quinolines provided 3-arylated-2-substituted quinolines under ambient conditions. Acridine N-oxides also reacted well and provided unusual 4-arylacridines. Various fluorine containing 2,3-diarylquinaolines prepared using this approach were evaluated for antibacterial activity and two compounds inhibited the drug-resistant strains of S-aureus with a good selectivity index. Further, the 2,3-diarylquinolines as the potential optoelectronic materials were prepared by the aryne chemistry approach and their optical and electronic properties for such applications are under study. The aryne intermediates provide an effective Green Chemistry tool to achieve versatile arylated heteroarenes for diverse applications.

Keywords: arynes, arylation, quinolines, acridines.

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Authors: Tita Nofianti, Tresna Lestari, Ade Y. Aprillia, Lilis Tuslinah, Ruswanto Ruswanto

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Nanoparticle technology gives a chance for drugs, especially natural based product, to give better activities than in its macromolecule form. The ginger torch is known to have activities as an antioxidant, antimicrobial, anticancer, etc. In this research, ginger torch flower extract was nanoparticlized using poloxamer 1, 3, and 5%. Nanoparticle was charaterized for its particle size, polydispersity index, zeta potential, entrapment efficiency, and morphological form by SEM (scanning electron microscope). The result shows that nanoparticle formulations have particle size 134.7-193.1 nm, polydispersity index is less than 0.5 for all formulations, zeta potential is -41.0 to (-24.3) mV, and entrapment efficiency is 89.93 to 97.99 against flavonoid content with a soft surface and spherical form of particles. Methanolic extract of ginger torch flower could enhance superoxide dismutase activity by 1,3183 U/mL in male rats. Nanoparticle formulation of ginger torch extract is expected to increase the capability of drug to enhance superoxide dismutase activity.

Keywords: superoxide dismutase, ginger torch flower, nanoparticle, poloxamer

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Authors: Shahnaz Mansouri, David Martin, Xiao Dong Chen, Meng Wai Woo

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Ultrafine hydrophobic and non-water-soluble drugs can increase the percentage of absorbed compared to their initial dosage. This paper provides a scalable new method of making ultrafine particles of substantially insoluble water compounds specifically, submicron particles of ethanol soluble and water insoluble pharmaceutical materials by steaming an ethanol droplet to prepare a suspension and then followed by immediate drying. This suspension is formed by adding evaporated water molecules as an anti-solvent to the solute of the samples and in early stage of precipitation continued to dry by evaporating both solvent and anti-solvent. This fine particle formation has produced fast dispersion powder in water. The new method is an extension of the antisolvent vapour precipitation technique which exposes a droplet to an antisolvent vapour with reference to the dissolved materials within the droplet. Ultrafine vitamin D3 and ibuprofen particles in the submicron ranges were produced. This work will form the basis for using spray dryers as high-throughput scalable micro-precipitators.

Keywords: single droplet drying, nano size particles, non-water-soluble drugs, precipitators

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Authors: Muhammad Mustafa Jafar, Syed Ashar Mahfooz, Muhammad Ejaz Saleem, Muhammad Asif Raza, Asghar Abbas, Rao Zahid Abbas, Muhammad Kasib Khan, Hafiz Muhammad Ishaq

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The Babesia gradually attained resistance against the synthetic medicines. To overcome the drug resistance, herbal therapy has gained more attention as compared to allopathic therapy. Peganumharmala (harmal) is a plant which has shown effective results against various protozoal diseases. Therefore, the present study was planned to monitor the efficacy of Peganumharmala (aqueous extract) against Babesiosis in cattle. For this purpose, a total of forty (n=40) infected animals were randomly divided into four equal groups (A, B, C, and D). Group A was treated with aqueous extract of Peganum harmala at 7.5 mg/kg, group B at 10 mg/kg and group C at 12.5 mg/kg of body weight. Group D served as a control group (normal). It was observed that there was a stabilization in hematological parameters (white and red blood cells, hemoglobin and Packed cell volume) in infected animals treated with Peganum harmala at different doses. Results of this study hence indicated that Peganum harmala extract at 12.5mg/kg BW is more effective against Babesiosis than lower doses.

Keywords: Babesiosis, cattle, control, Peganum harmala

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Authors: Phuriwat Laomethakorn, Siritron Samosorn, Ramida Watanapokasin

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Cancer metastasis is the major cause of cancer-related death. Therefore searching for a compound that could inhibit cancer metastasis is necessary. 13-Butoxyberberine bromide is a berberine derivative that has not been reported an anti-metastatic effect on skin cancer cells. This study aimed to investigate the anti-metastatic effect of 13-butoxyberberine bromide on skin cancer A431 cells. The effect of 13-butoxyberberine bromide on A431 cell viability was examined by MTT assay. Suppression of cell migration and invasion in A431 cells were determined by wound healing assay, transwell migration assay, and transwell invasion assay. Metastasis proteins were determined by western blotting. The results demonstrated that 13-butoxyberberine bromide decreased A431 cell viability in a dose-dependent manner. In addition, sub-toxic concentrations of 13-butoxyberberine bromide suppressed cell migration and invasion in A431 cells. In addition, 13-butoxyberberine bromide showed anti-metastatic effects by down-regulated MMP-2 and MMP-9 expression. These findings may be useful in the development of 13-butoxyberberine bromide as an anti-metastatic drug in the future.

Keywords: 13-butoxyberberine bromide, metastasis, skin cancer, MMP

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Authors: Peter Fedichev

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We studied fundamental aspects of aging to develop a mathematical model of gene regulatory network. We show that aging manifests itself as an inherent instability of gene network leading to exponential accumulation of regulatory errors with age. To validate our approach we studied age-dependent omic data such as transcriptomes, metabolomes etc. of different model organisms and humans. We build a computational platform based on our model to identify the targets and biomarkers of aging to design new drugs against aging and age-related diseases. As biomarkers of aging, we choose the rate of aging and the biological age since they completely determine the state of the organism. Since rate of aging rapidly changes in response to an external stress, this kind of biomarker can be useful as a tool for quantitative efficacy assessment of drugs, their combinations, dose optimization, chronic toxicity estimate, personalized therapies selection, clinical endpoints achievement (within clinical research), and death risk assessments. According to our model, we propose a method for targets identification for further interventions against aging and age-related diseases. Being a biotech company, we offer a complete pipeline to develop an anti-aging drug-candidate.

Keywords: aging, longevity, biomarkers, senescence

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Authors: Ihsan Burak Cam, Ferhan Balci-Torun, Ayhan Topuz, Esin Ari, Ismail Gokhan Deniz, Ilker Genc

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The seeds of Vaccaria hispanica have been used in food and pharmaceutical industry. It is an important product due to its superior starch granules, triterpenic saponins, and cyclopeptides suitable for drug delivery. V. hispanica naturally grows in different climatic regions and has genotypes that differ in terms of seed content and composition. Sixty-six V. hispanica seed specimens were collected based on the representation of the distribution in all regions of Turkey and the determination of possible genotypic differences between regions. The seeds, collected from each of the 66 locations, were grown in greenhouse conditions in Akdeniz University, Antalya. Saponin and cyclopeptide contents of the V. hispanica seeds were determined after harvest. Accelerated solvent extraction (ASE) was applied for the extraction of saponins and cyclopeptides. Cyclopeptide (segetalin A) and saponin content of V. hispanica seeds were found in the range of 0.165-0.654 g/100 g and 0.15-1.14 g/100 g, respectively. The results were found to be promising for the seeds from Turkey in terms of saponin content and quality. Acknowledgment: This study was supported by the Scientific and Research Council of Turkey (TUBITAK) (project no 112 O 136).

Keywords: Vaccaria hispanica, saponin, cyclopeptid, cow cockle seeds

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Authors: Ugur Cihat Sakarya

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This research focuses on psychedelic trance music events in Turkey in the context of altered states of consciousness (ASC). The fieldwork that was conducted from 2018 to 2019 is the main source of the research. Participant observation method was followed in 15 selected events. To direct the musical experiences of participants, performances were also presented as a Dj. Ten of these events are open-air festivals. Five of them are indoor parties. The observations made during fieldwork and suitable answers for inference from the interviews with participants, artists, DJs, and volunteers were selected, compiled, and presented. In the result, findings showed that these activities are perceived as temporary autonomous areas by the participants both in time and space and that these activities are suitable areas for expressing themselves as a group (psyfamily) against mainstream culture. It has been observed that the elements that complement the altered states of consciousness in these events are music, visual arts, drug use, and desire to experience spiritual experiences. It is thought that this first academic study -about this topic in Turkey- will open a door for future researches.

Keywords: consciousness, psychedelic, psytrance, rave, Turkey

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Authors: Watchareewan Thongsaard, Ratirat Sangpayap, Maneekarn Namsa-Aid

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Thunbergia laurifolia Linn. (TL) is a herbal medicine which has been used as an antidote for several poisonous agents including insecticides and as a component of a mixture of crude extracts to treat drug addicted patients. The aim of this study is to examine the level of dopamine in nucleus accumbens after chronic pre-administration of TL in ethanol addicted rats. Male Wistar rats weigh 200-250 g received TL methanol extract (200mg/kg, orally) 60 minutes before 20% ethanol (1 g/kg, i.p.) for 30 days. The nucleus accumbens was removed and tested for dopamine by HPLC-ECD. The level of dopamine was significantly increased by chronic ethanol administration, whereas the chronic TL extract administration did not cause a difference in dopamine level when compared to control. Moreover, the pre-treatment of TL extract before ethanol significantly reduced the dopamine level in nucleus accumbens to normal level when compared with chronic ethanol administration alone. These results suggested that the increase in dopamine level in the nucleus accumbens by chronic ethanol administration is the cause of ethanol addiction, and this effect is prevented by chronic TL pre-administration. Furthermore, chronic TL extract administration alone did not cause the changes in dopamine level in the nucleus accumbens, indicating that TL itself did not cause addiction.

Keywords: Thunbergia laurifolia Linn., alcohol addiction, dopamine, nucleus accumbens

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Authors: Afaf Bouchoucha, Karima Si Larbi, Mohamed Amine Bourouaia, Salah.Boulanouar, Safia.Djabbar

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The synthesis, characterization and comparative biological study of manganese (II) and copper (II) complexes with an heterocyclic ligand used in pharmaceutical field (Scheme 1), were reported. Two kinds of complexes were obtained with derivative sulfonamide, [M (L)₂ (H₂O)₂].H₂O and [M (L)₂ (Cl)₂]3H₂O. These complexes have been prepared and characterized by elemental analysis, FAB mass, ESR magnetic measurements, FTIR, UV-Visible spectra and conductivity. Their stability constants have been determined by potentiometric methods in a water-ethanol (90:10 v/v) mixture at a 0.2 mol l-1 ionic strength (NaCl) and at 25.0 ± 0.1 ºC using Sirko program. DFT calculations were done using B3LYP/6-31G(d) and B3LYP/LanL2DZ. The antimicrobial activity of ligand and complexes against the species Escherichia coli, P. aeruginosa, Klebsiella pneumoniae, S. aureus, Bacillus subtilisan, Candida albicans, Candida tropicalis, Saccharomyces, Aspergillus fumigatus and Aspergillus terreus has been carried out and compared using agar-diffusion method. Also, the toxicity study was evaluated on synchesis complexes using Mice of NMRI strain.

Keywords: hetterocyclic ligand, complex, stability constant, antimicrobial activity, DFT, acute and genotoxicity study

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Authors: K. Żak, S. Przetocka, R. Kitel, K. Guzik, B. Musielak, S. Malicki, G. Dubin, T. A. Holak

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Studies on tumor genesis revealed a number of factors that may potentially serve as molecular targets for immunotherapies. One of such promising targets are PD1 and PDL1 proteins. PD1 (Programmed cell death protein 1) is expressed by activated T cells and plays a critical role in modulation of the host's immune response. One of the PD1 ligands -PDL1- is expressed by macrophages, monocytes and cancer cells which exploit it to avoid immune attack. The notion of the mechanisms used by cancer cells to block the immune system response was utilized in the development of therapies blocking PD1-PDL1 interaction. Up to date, human PD1-PDL1 complex has not been crystallized and structure of the mouse-human complex does not provide a complete view of the molecular basis of PD1-PDL1 interactions. The purpose of this study is to obtain crystal structure of the human PD1-PDL1 complex which shall allow rational design of small molecule inhibitors of the interaction. In addition, the study presents results of binding small-molecules to PD1 and fragment docking towards PD1 protein which will facilitate the design and development of small–molecule inhibitors of PD1-PDL1 interaction.

Keywords: PD1, PDL1, cancer, small molecule, drug discovery

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Authors: Jeonghun Lee

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In this study, we investigated the relationship between stress and thyroid dysfunction in such patients who underwent thyroidectomy. This study included 101 patients who underwent thyroidectomy from January 2015 to June 2020 and experienced hypothyroidism. The included patients had good drug compliance with the same dosage of levothyroxine (LT4). The male-to-female ratio was 1:4.6, and the mean age was 45.4 years at surgery and 50.2 years at stressful events. Eighteen patients underwent lobectomies and, of these, 12 did not take LT4. The mean follow-up period was 49(8-93) months. Statistical analyses were performed using the paired t-test, Wilcoxon signed-rank test, and McNemer test using PROC MIXED with SAS 9.4. Forty-five patients (44.6%) had hypothyroidism with thyroid-stimulating hormone (TSH) >10 μIU/mL. There was distress in 81 patients and eustress in 10 patients. TSH levels increased during a mean 5.8 months (min 1, max 12) in 24 patients who specified the date of their life events. Even though each patient took the same dose of LT4, when the patients were under stress, both the free T4 and T3 decreased and TSH increased, regardless of whether the patient experienced distress or eustress (P <0.001). While adjusting for the effect of the free T4 and T3, TSH increased significantly in the patients after stress (P <0.001). For patients with thyroid cancer who are simultaneously experiencing life events, TSH may be used as a stress biomarker to enable the implementation of appropriate treatment and counseling strategies.

Keywords: endocrine, thyroid, thyroid function, biomarker, stress

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Authors: Shao-Hsuan Chien, Ju-Hui Fu

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Parkinson’s disease (PD) is a degenerative disorder of the central nervous system that is characterized by progressive loss of dopaminergic neurons in the substantia nigra pars compacta and motor impairment. Aggregation of α-synuclein in neuronal cells plays a key role in this disease. At present, therapeutics for PD provides moderate symptomatic benefit but is not able to delay the development of this disease. Current efforts for the treatment of PD are to identify new drugs that show slow or arrest progressive course of PD by interfering with a disease-specific pathogenetic process in PD patients. Maackiain is a bioactive compound isolated from the roots of the Chinese herb Sophora flavescens. The purpose of the present study was to assess the potential for maackiain to ameliorate PD in Caenorhabditis elegans models. Our data reveal that maackiain prevents α-synuclein accumulation in the transgenic Caenorhabditis elegans model and also improves dopaminergic neuron degeneration, food-sensing behavior, and life-span in 6-hydroxydopamine-induced Caenorhabditis elegans model, thus indicating its potential as a candidate antiparkinsonian drug.

Keywords: maackiain, Parkinson’s disease, dopaminergic neurons, α-Synuclein

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Authors: Flavia Laffleur, Andreas Bernkop-Schnürch

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Purpose: This study was aimed to investigate preactivated thiomers for their mucoadhesive potential. Methods: Accordingly, chitosan-thioglycolic-mercaptonicotinamide conjugates (chitosan-TGA-MNA) were synthesized by the oxidative S-S coupling of chitosan-thioglycolic acid (chitosan-TGA) with 6-mercaptonicotin amide (MNA). Unmodified chitosan, chitosan-TGA (thiomers) and chitosan-TGA-MNA conjugates were compressed into test discs to investigate cohesive properties, cytotoxicity assays and mucoadhesion studies. Results: Due to the immobilization of MNA, the chitosan-TGA-MNA conjugates exhibit comparatively higher swelling properties and cohesive properties corresponding unmodified chitosan. On the rotating cylinder, discs based on chitosan-TGA-MNA conjugates displayed 3.1-fold improved mucoadhesion time compared to thiolated polymers. Tensile study results were found in good agreement with rotating cylinder results. Moreover, preactivated thiomers showed higher stability. All polymers were found non-toxic over Caco-2 cells. Conclusion: On the basis of achieved results the pre activated thiomeric therapeutic agent seems to represent a promising generation of mucoadhesive polymers which are safe to use for a prolonged residence time to target the mucosa.

Keywords: biomedical application, drug delivery, polymer, thiomer

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Authors: U. L. Fulco, E. L. Albuquerque, José X. Lima Neto, L. R. Da Silva

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The binding of the nonsteroidal anti-inflammatory drug ibuprofen (IBU) to human serum albumin (HSA) is investigated using density functional theory (DFT) calculations within a fragmentation strategy. Crystallographic data for the IBU–HSA supramolecular complex shows that the ligand is confined to a large cavity at the subdomain IIIA and at the interface between the subdomains IIA and IIB, whose binding sites are FA3/FA4 and FA6, respectively. The interaction energy between the IBU molecule and each amino acid residue of these HSA binding pockets was calculated using the Molecular Fractionation with Conjugate Caps (MFCC) approach employing a dispersion corrected exchange–correlation functional. Our investigation shows that the total interaction energy of IBU bound to HSA at binding sites of the fatty acids FA3/FA4 (FA6) converges only for a pocket radius of at least 8.5 °A, mainly due to the action of residues Arg410, Lys414 and Ser489 (Lys351, Ser480 and Leu481) and residues in nonhydrophobic domains, namely Ile388, Phe395, Phe403, Leu407, Leu430, Val433, and Leu453 (Phe206, Ala210, Ala213, and Leu327), which is unusual. Our simulations are valuable for a better understanding of the binding mechanism of IBU to albumin and can lead to the rational design and the development of novel IBU-derived drugs with improved potency.

Keywords: ibuprofen, human serum albumin, density functional theory, binding energies

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Authors: M. A. Ahmed, N. Basha, I. V. Nsahlai

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This study determined the effectiveness of selected anthementics (Ivermectin 1% (IVM), Closantel 7.5% (CST) and a combination Abamectin 0.08% and Praziquantel 1.5% (CAP) currently being used in SA. Gender, initial egg per gram (EPG) and initial live weight aided in blocking animals into groups, each group was randomly treated with one of four drug treatments comprising: the untreated control (D0), IVM, CST, and CAP. Animals grazed throughout on infested pasture. Rectal faeces were collected on days 0, 7, 14, and 21 for determining EPG. Faeces were mixed per group and incubated to identify and determine the abundance of larval forms of Haemonchus, Trichostrongylus, Strongyloides, Namatodirus, and Cooperia species. Differences between treatments changed over time. On day7 IVM, CST, and CAP depressed EPG to 0.66, 0.37 and 0.80 of their respective starting values whilst EPG increased 1.39 times for D0. Thereafter, EPG increased consistently for all drugs; CST recorded the lowest values. Haemonchus, Trichostrongylus, Strongyloides, Namatodirus and Coperia species contributed respectively 60%, 30%, 6%, 3%, and 1% of the larval forms on day 0; and 78%, 8%, 11%, 1%, 2% on day 21. Larval forms increased for Haemonchus species but decreased for Trichostrongylus species over time. Closantel was the most effective dewormer. Haemonchus Spp. were least affected whilst Trichostrongylus Spp. were the most affect by all drugs.

Keywords: anthementics, faecal egg count, L3 larvae, sheep

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Authors: Abhishekkumar Ramasamy, Parameshwari

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Chitosan is the deacyelitated derivative of chitin, the second most abundant biopolymer just after cellulose. Without doubt, its biomedical usages have gained more importance among the vast variety of chitosan applications owing to its good biocompatibility and biodegradability. In recent years, particular interest has been devoted to chitosan hydrogels as a promising alternative in competition with conventional sutures or bioadhesives. Different parameters such as acid type and concentration, and degree of deacetylation (DD%) of chitosan, were altered to modify hydrogel properties including viscosity, pH, cohesive strength, and tissue bioadhesiveness. In the current work, we have investigated the effectiveness of chitosan hydrogel encapsulated with tanexamic acid to stop bleeding. Chitosan film was obtained with solubilization of chitosan powder in aqueous acidic media. In vivo experiments have been conducted on rat and rabbit models that provide a convenient way to evaluate the efficacy of prepared samples. The arteries vein was punctured on the hind limb of the rat and the gauze was been applied on the punchered area. Bioadhesive strength as well as irritant effects were discussed. Samples with higher degree of deacetylation, including Chs-16 and Chs-19 that were dissolved in lactic media showed best sealing effect.

Keywords: chitosan, biocomaptibility, biodegradability, bioadhersive, deacetylation

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Authors: Purnima Rawat, Divya Vohora, Sarika Gupta, Farhan J. Ahmad, Sushama Talegaonkar

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Nanoparticles (NPs) that target bone tissue were developed using PLGA–mPEG (poly(lactic-co-glycolic-acid)–polyethylene glycol) diblock copolymers by using pamidronate as a bone-targeting moieties. These NPs are expected to enable the transport of hydrophilic drugs. The NP was prepared by in situ polymerization method, and their in- vitro characteristics were evaluated using dynamic light scattering, transmission electron microscopy (TEM) and in phosphate-buffered solution. The bone targeting potential of the NP was also evaluated on in-vitro pre-osteoblast MCT3E1 cell line using ALP activity, degree of mineralization and RT-PCR assay. The average particle size of the NP was 101.6 ± 3.7nm, zeta potential values were negative (-25±0.34mV) of the formulations and the entrapment efficiency was 93± 3.1 % obtained. The moiety of the PLGA–mPEG–pamidronate NPs exhibited the best apatite mineral binding ability in-vitro MCT3E1 pre-osteoblast cell line. Our results suggested that the developed nanoparticles may use as a delivery system for Pamidronate in bone repair and regeneration, warranting further evaluation of the treatment of bone disease.

Keywords: nanoparticle, pamidronate, in-situ polymerization, osteoblast

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Authors: Sanjaykumar R. Patel, Parth R. Kayastha

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α-lactose monohydrate is widely used in the pharmaceutical industries as an inactive substance that acts as a vehicle or a medium for a drug or other active substance. It is a byproduct of dairy industries, and the recovery of lactose from whey not only boosts the improvement of the economics of whey utilization but also causes a reduction in pollution as lactose recovery can reduce the BOD of whey by more than 80%. In the present study, levels of process parameters were kept as initial lactose concentration (30-50% w/w), sonication amplitude (20-40%), sonication time (2-6 hours), and crystallization temperature (10-20 ^oC) for the recovery of lactose in ultrasound assisted cooling crystallization. In comparison with cooling crystallization, the use of ultrasound enhanced the lactose recovery by 39.17% (w/w). The parameters were optimized for the lactose recovery using Taguchi Method. The optimum conditions found were initial lactose concentration at level 3 (50% w/w), amplitude of sonication at level 2 (40%), the sonication time at level 3 (6 hours), and crystallization temperature at level 1 (10 °C). The maximum recovery was found to be 85.85% at the optimum conditions. Sonication time and the initial lactose concentration were found to be significant parameters for the lactose recovery.

Keywords: crystallization, lactose, Taguchi method, ultrasound

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Authors: Amine Mezni, Merfat Algethami, Ali Aldalbahi, Arwa Alrooqi, Abel Santos, Dusan Losic, Sarah Alharthi, Tariq Altalhi

Abstract:

In situ synthesis of carbon nanotubes featuring different diameters (10-200 nm), lengths (1 to 100 µm) and periodically nanostructured shape was performed in a custom designed chemical vapor deposition (CVD) system using nanoporous anodic alumina (NAA) under different conditions. The morphology of the resulting CNTs/NAA composites and free-standing CNTs were analyzed by transmission electron microscopy (TEM) and scanning electron microscopy (SEM). The results confirm that highly ordered arrays of CNTs with precise control of nanotube dimensions in the range 20-200 nm with tube length in the range < 1 µm to > 100 μm and with periodically shaped morphology can be fabricated using nanostructured NAA templates prepared by anodization. This technique allows us to obtain tubes open at one / both ends with a uniform diameter along the pore length without using any metal catalyst. Our finding suggests that this fabrication strategy for designing new CNTs membranes and structures can be significant for emerging applications as molecular separation/transport, optical biosensing, and drug delivery.

Keywords: carbon nanotubes, CVD approach, composites membrane, nanoporous anodic alumina

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Authors: Abdelhadi Adam Salih Denei

Abstract:

Silver nanoparticles (AgNPs) have been used in cancer therapy, and the area of nanomedicine has made unheard-of strides in recent years. A thorough summary of the development and assessment of AgNPs for their possible use in the fight against cancer is the goal of this review. Targeted delivery methods have been designed to optimise therapeutic efficacy by using AgNPs' distinct physicochemical features, such as their size, shape, and surface chemistry. Firstly, the study provides an overview of the several synthesis routes—both chemical and green—that are used to create AgNPs. Natural extracts and biomolecules are used in green synthesis techniques, which are becoming more and more popular since they are biocompatible and environmentally benign. It is next described how synthesis factors affect the physicochemical properties of AgNPs, emphasising how crucial it is to modify these parameters for particular therapeutic uses. An extensive analysis is conducted on the anticancer potential of AgNPs, emphasising their capacity to trigger apoptosis, impede angiogenesis, and alter cellular signalling pathways. The analysis also investigates the potential benefits of combining AgNPs with currently used cancer treatment techniques, including radiation and chemotherapy. AgNPs' safety profile for use in clinical settings is clarified by a comprehensive evaluation of their cytotoxicity and biocompatibility.

Keywords: silver nanoparticles, cancer, nanocarrier system, targeted delivery

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Authors: N. Nwachoko, E. B. Essien, E. O. Ayalogu

Abstract:

Owing to the outbreak of different diseases and microbial resistance to some available drugs, proper identification, and evaluation of plants have been encouraged. There have been claims worldwide by the traditional system that some plants possessed medicinal properties. Plants and their components have been said to be source of large amount of drugs which comprise of distinct groups such as antispasmodics, anticancer and antimicrobials. Researchers have reported that chemicals in plants are responsible for the medicinal uses of plants. Thus this study evaluated the protective effect of Aframomun chrysanthum seed aqueous extract in acetaminophen-induced liver toxicity in rats. A suspension of 750 mg/kg acetaminophen was administered once every 72 hours to induce toxicity in the rats. Oral administration of 500, 1000 and 2000 mg/kg body weight of the extract and 100 mg/kg of silymarin (reference drug) were administered for 10 days. Biochemical analysis showed significant (p < 0.05) increase in the activities of aspartate aminotransferase (AST), alanine aminotransferase (ALT)and alkaline phosphatase (ALP)as well as the concentrations of albumin (ALB) and total bilirubin (T.B.) levels in rats administered with acetaminophen only. The levels of these parameters were significantly (p < 0.05) decreased in the groups pretreated with the extract.

Keywords: Aframomun chrysanthum, silymarin, hepatoprotective, toxicity

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Authors: Hashaam Akhtar

Abstract:

IFNλR1 and IL10R2 collectively construct a heterodimer, which is an acknowledged functional receptor for all type III interferons (IFNs). Expression of IFNλR1 is highly tissue specific, which can help in making type III IFNs a drug of choice as comparable to its analogue, type I IFNs, for treating hepatitis C in the near future. Although, expression of IFNλR1 also varies with the concentration of type I IFNs, but in this study it was shown that the expression of IFNλR1 varies with the protein titers of IFN-α, IFN-λ3 and the newly discovered IFN-λ4. High dosage of IFN-α reduces the expression of IFNλR1 in HepG2 cells, which can affect the antiviral activity of type III IFNs in vivo. We premeditated an experimental strategy to differentiate monocytes into dendritic cells (DCs), type I and type II macrophages in vitro and quantified the expression of the IFNλR1 by qPCR. The exposure of newly discovered IFN-λ4 to macrophages and DCs also raised the expression of its own receptor, which shows that expression of IFN-λ4 protein in hepatitis C patient may augment type I treatment and help ease off viral titers. The results of this study may contribute in some understanding towards the mechanisms involved in the selective expression of IFNLR1 and exceptionalities associated with the receptor.

Keywords: IFNLR1, Interferon Lambda 4 (IFN-λ4), Mononuclear Phagocyte Cells (MPCs), expression

Procedia PDF Downloads 383

Authors: Hammed Tanimowo Aiyelabegan, Oluchukwu Franklin Aladi, Mutiu Adewumi Alabi, Raliat Abimbola Aladodo, Emmanuel Oladipupo Ajani, Abdulganiyu Giwa, Esther Owolabi

Abstract:

The study aimed to evaluate the inhibitory activities of ligands from Enantia chlorantha stem bark on α-amylase and α-glucosidase. In silico pharmacokinetic properties and docking scores were employed to analyse the inhibition using SwissADME and Autodock4.2, respectively. Results revealed that drug-likeness, pharmacokinetics and bioavailability radar of all the ligands except jatrorrhizine and acarbose falls within the radar according to the Lipinski rule of 5. The binding energies of the protein-ligand interactions also show that the ligand fits into the active site. The results obtained from this study show that the chemical constituents from Enantia chlorantha stem bark may bring about positive physiological changes in a patient suffering from diabetes mellitus. Further in vitro studies on diabetes cell lines and in vivo studies on the animal may validate these compounds for diabetes treatment. These phytoconstituents could help in the development of novel anti-diabetic molecules.

Keywords: diabetes mellitus, ?-amylase, ?-glucosidase, in silico, Enantia chlorantha stem bark

Procedia PDF Downloads 171

Authors: Sivakumar Singaravelu, Giriprasath Ramanathan, M. D. Raja, Uma Tirichurapalli Sivagnanam

Abstract:

The goal of the present study was to develop and evaluate composite film for tissue engineering application. The keratin was extracted from bovine horn and used for preparation of keratin (HK), physiologically clotted fibrin (PCF) and gelatin (G) blend films in different stoichiometric ratios (1:1:1, 1:1:2 and 1:1:3) by using solvent casting method. The composite films (HK-PCF-G) were characterized physiochemically using Fourier Transform Infrared Spectroscopy (FTIR), Differential Scanning Calorimetry (DSC), Thermogravimetric Analysis (TGA) and Scanning Electron Microscopy (SEM). The mechanical properties of the composite films were analyzed. The results of tensile strength show that ultimate strength and elongation were 10.72 Mpa and 4.83 MPA respectively for 1:1:3 ratio combination. The SEM image showed a slight smooth surface for 1:1:3 ratio combination compared to other films. In order to impart antibacterial activities, the composite films were loaded with Mupirocin (MP) to act against infection. The composite films acted as a suitable carrier to protect and release the drug in a controlled manner. This developed composite film would be a suitable alternative material for tissue engineering application.

Keywords: bovine horn, keratin, fibrin, gelatin, tensile strength

Procedia PDF Downloads 448