Search results for: common drug combinations
Commenced in January 2007
Frequency: Monthly
Edition: International
Paper Count: 7885

Search results for: common drug combinations

7135 Characteristics of Bio-hybrid Hydrogel Materials with Prolonged Release of the Model Active Substance as Potential Wound Dressings

Authors: Katarzyna Bialik-Wąs, Klaudia Pluta, Dagmara Malina, Małgorzata Miastkowska

Abstract:

In recent years, biocompatible hydrogels have been used more and more in medical applications, especially as modern dressings and drug delivery systems. The main goal of this research was the characteristics of bio-hybrid hydrogel materials incorporated with the nanocarrier-drug system, which enable the release in a gradual and prolonged manner, up to 7 days. Therefore, the use of such a combination will provide protection against mechanical damage and adequate hydration. The proposed bio-hybrid hydrogels are characterized by: transparency, biocompatibility, good mechanical strength, and the dual release system, which allows for gradual delivery of the active substance, even up to 7 days. Bio-hybrid hydrogels based on sodium alginate (SA), poly(vinyl alcohol) (PVA), glycerine, and Aloe vera solution (AV) were obtained through the chemical crosslinking method using poly(ethylene glycol) diacrylate as a crosslinking agent. Additionally, a nanocarrier-drug system was incorporated into SA/PVA/AV hydrogel matrix. Here, studies were focused on the release profiles of active substances from bio-hybrid hydrogels using the USP4 method (DZF II Flow-Through System, Erweka GmbH, Langen, Germany). The equipment incorporated seven in-line flow-through diffusion cells. The membrane was placed over support with an orifice of 1,5 cm in diameter (diffusional area, 1.766 cm²). All the cells were placed in a cell warmer connected with the Erweka heater DH 2000i and the Erweka piston pump HKP 720. The piston pump transports the receptor fluid via seven channels to the flow-through cells and automatically adapts the setting of the flow rate. All volumes were measured by gravimetric methods by filling the chambers with Milli-Q water and assuming a density of 1 g/ml. All the determinations were made in triplicate for each cell. The release study of the model active substance was carried out using a regenerated cellulose membrane Spectra/Por®Dialysis Membrane MWCO 6-8,000 Carl Roth® Company. These tests were conducted in buffer solutions – PBS at pH 7.4. A flow rate of receptor fluid of about 4 ml /1 min was selected. The experiments were carried out for 7 days at a temperature of 37°C. The released concentration of the model drug in the receptor solution was analyzed using UV-Vis spectroscopy (Perkin Elmer Company). Additionally, the following properties of the modified materials were studied: physicochemical, structural (FT-IR analysis), morphological (SEM analysis). Finally, the cytotoxicity tests using in vitro method were conducted. The obtained results exhibited that the dual release system allows for the gradual and prolonged delivery of the active substances, even up to 7 days.

Keywords: wound dressings, SA/PVA hydrogels, nanocarrier-drug system, USP4 method

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7134 Hepatoprotective Action of Emblica officinalis Linn. against Radiation and Lead Induced Changes in Swiss Albino Mice

Authors: R. K. Purohit

Abstract:

Ionizing radiation induces cellular damage through direct ionization of DNA and other cellular targets and indirectly via reactive oxygen species which may include effects from epigenetic changes. So there is a need of hour is to search for an ideal radioprotector which could minimize the deleterious and damaging effects caused by ionizing radiation. Radioprotectors are agents which reduce the radiation effects on cell when applied prior to exposure of radiation. The aim of this study was to access the efficacy of Emblica officinalis in reducing radiation and lead induced changes in mice liver. For the present experiment, healthy male Swiss albino mice (6-8 weeks) were selected and maintained under standard conditions of temperature and light. Fruit extract of Emblica was fed orally at the dose of 0.01 ml/animal/day. The animal were divided into seven groups according to the treatment i.e. lead acetate solution as drinking water (group-II) or exposed to 3.5 or 7.0 Gy gamma radiation (group-III) or combined treatment of radiation and lead acetate (group-IV). The animals of experimental groups were administered Emblica extract seven days prior to radiation or lead acetate treatment (group V, VI and VII) respectively. The animals from all the groups were sacrificed by cervical dislocation at each post-treatment intervals of 1, 2, 4, 7, 14 and 28 days. After sacrificing the animals pieces of liver were taken out and some of them were kept at -20°C for different biochemical parameters. The histopathological changes included cytoplasmic degranulation, vacuolation, hyperaemia, pycnotic and crenated nuclei. The changes observed in the control groups were compared with the respective experimental groups. An increase in the value of total proteins, glycogen, acid phosphtase, alkaline phosphatase activity and RNA was observed up to day-14 in the non drug treated group and day 7 in the Emblica treated groups, thereafter value declined up to day-28 without reaching to normal. The value of cholesterol and DNA showed a decreasing trend up to day -14 in non drug treated groups and day-7 in drug treated groups, thereafter value elevated up to day-28. The biochemical parameters were observed in the form of increase or decrease in the values. The changes were found dose dependent. After combined treatment of radiation and lead acetate synergistic effect were observed. The liver of Emblica treated animals exhibited less severe damage as compared to non-drug treated animals at all the corresponding intervals. An early and fast recovery was also noticed in Emblica pretreated animals. Thus, it appears that Emblica is potent enough to check lead and radiation induced heptic lesion in Swiss albino mice.

Keywords: radiation, lead , emblica, mice, liver

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7133 Prospects of Acellular Organ Scaffolds for Drug Discovery

Authors: Inna Kornienko, Svetlana Guryeva, Natalia Danilova, Elena Petersen

Abstract:

Drug toxicity often goes undetected until clinical trials, the most expensive and dangerous phase of drug development. Both human cell culture and animal studies have limitations that cannot be overcome by improvements in drug testing protocols. Tissue engineering is an emerging alternative approach to creating models of human malignant tumors for experimental oncology, personalized medicine, and drug discovery studies. This new generation of bioengineered tumors provides an opportunity to control and explore the role of every component of the model system including cell populations, supportive scaffolds, and signaling molecules. An area that could greatly benefit from these models is cancer research. Recent advances in tissue engineering demonstrated that decellularized tissue is an excellent scaffold for tissue engineering. Decellularization of donor organs such as heart, liver, and lung can provide an acellular, naturally occurring three-dimensional biologic scaffold material that can then be seeded with selected cell populations. Preliminary studies in animal models have provided encouraging results for the proof of concept. Decellularized Organs preserve organ microenvironment, which is critical for cancer metastasis. Utilizing 3D tumor models results greater proximity of cell culture morphological characteristics in a model to its in vivo counterpart, allows more accurate simulation of the processes within a functioning tumor and its pathogenesis. 3D models allow study of migration processes and cell proliferation with higher reliability as well. Moreover, cancer cells in a 3D model bear closer resemblance to living conditions in terms of gene expression, cell surface receptor expression, and signaling. 2D cell monolayers do not provide the geometrical and mechanical cues of tissues in vivo and are, therefore, not suitable to accurately predict the responses of living organisms. 3D models can provide several levels of complexity from simple monocultures of cancer cell lines in liquid environment comprised of oxygen and nutrient gradients and cell-cell interaction to more advanced models, which include co-culturing with other cell types, such as endothelial and immune cells. Following this reasoning, spheroids cultivated from one or multiple patient-derived cell lines can be utilized to seed the matrix rather than monolayer cells. This approach furthers the progress towards personalized medicine. As an initial step to create a new ex vivo tissue engineered model of a cancer tumor, optimized protocols have been designed to obtain organ-specific acellular matrices and evaluate their potential as tissue engineered scaffolds for cultures of normal and tumor cells. Decellularized biomatrix was prepared from animals’ kidneys, urethra, lungs, heart, and liver by two decellularization methods: perfusion in a bioreactor system and immersion-agitation on an orbital shaker with the use of various detergents (SDS, Triton X-100) in different concentrations and freezing. Acellular scaffolds and tissue engineered constructs have been characterized and compared using morphological methods. Models using decellularized matrix have certain advantages, such as maintaining native extracellular matrix properties and biomimetic microenvironment for cancer cells; compatibility with multiple cell types for cell culture and drug screening; utilization to culture patient-derived cells in vitro to evaluate different anticancer therapeutics for developing personalized medicines.

Keywords: 3D models, decellularization, drug discovery, drug toxicity, scaffolds, spheroids, tissue engineering

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7132 Fabrication of Biosensor Based on Layered Double Hydroxide/Polypyrrole/Carbon Paste Electrode for Determination of Anti-Hypertensive and Prostatic Hyperplasia Drug Terazosin

Authors: Amira M. Hassanein, Nehal A. Salahuddin, Atsunori Matsuda, Toshiaki Hattori, Mona N. Elfiky

Abstract:

New insights into the design of highly sensitive, carbon-based electrochemical sensors are presented in this work. This was achieved by exploring the interesting properties of conductive (Mg/Al) layered double hydroxide- Dodecyl Sulphate/Polypyrrole nanocomposites which were synthesized by in-situ polymerization of pyrrole during the assembly of (Mg/Al) layered double hydroxide, and by employing the anionic surfactant Dodecyl sulphate as a modifier. The morphology and surface area of the nanocomposites changed with the percentage of Pyrrole. Under optimal conditions, the modified carbon paste electrode successfully achieved detection limits of 0.057 and 0.134 nmol.L-1 of Terazosin hydrochloride in pharmaceutical formulation and spiked human serum fluid, respectively. Moreover, the sensors are highly stable, reusable, and free from interference by other commonly present excipients in drug formulations.

Keywords: layered double hydroxide, polypyrrole, terazosin hydrochloride, square-wave adsorptive anodic stripping voltammetry

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7131 Superoxide Dismutase Activity of Male Rats after Administration of Extract and Nanoparticle of Ginger Torch Flower

Authors: Tresna Lestari, Tita Nofianti, Ade Yeni Aprilia, Lilis Tuslinah, Ruswanto Ruswanto

Abstract:

Nanoparticle formulation is often used to improve drug absorptivity, thus increasing the sharpness of the action. Ginger torch flower extract was formulated into nanoparticle form using poloxamer 1, 3 and 5%. The nanoparticle was then characterized by its particle size, polydispersity index, zeta potential, entrapment efficiency and morphological form by SEM. The result shows that nanoparticle formulations have particle size 134.7-193.1 nm, polydispersity index less than 0.5 for all formulations, zeta potential -41.0 - (-24.3) mV and entrapment efficiency 89.93-97.99 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 the drug to enhance superoxide dismutase activity.

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

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7130 Effects of α-IFN –SingleWalled Carbon NanoTube and α-IFN-PLGA Encapsulated on Breast Cancer in Rats Induced by DMBA by Using CA15-3 Tumor Marker

Authors: Anoosh Eghdami

Abstract:

Background and aim: Conventional anticancer drugs display significant shortcomings which limit their use in cancer therapy. For this reason, important progress has been achieved in the field of nanotechnology to solve these problems and offer a promising and effective alternative for cancer treatment. Tumor markers may also be measured periodically during cancer therapy. Tumor markers may also be measured after treatment has ended to check for recurrence the return of cancer. The aim of this study was to evaluate the effect of nano drug delivery in induced breast cancer with DMBA by using CA15-3 tumor marker. Material and method: the rats were divided into five groups. The first group (control n=15) were fed only sesame oil as a gavage. In the second group n=15,10 mg DMBA was dissolved in 5ml of sesame oil and were fed as a gavage. In addition to DMBA treatment as the second group, in the 3,4and 5 groups after cancer creation, respectively affected by alpha interferon (α-IFN),alpha interferon conjugated with single walled carbon nano tube (α-IFN-SWNT) and encapsulated in poly lactic poly glycolic acid (α-IFN-PLGA). Tumor marker was measured in recent three groups. Results: The ANOVA test was used to determine the differences among the groups. Cancer inducing in rats (group 2) caused a significant increase in blood levels of CA15-3 (P<0.05). Administration of α-IFN, α-IFN –SWNT and α-IFN-PLGA in 3 groups of cancerous rats caused a significant decrease in blood levels of CA15-3 only the group that treated with α-IFN-PLGA (p<0.05). Conclusion: the results of this study indicate that nano drugs more effective than traditional drug in cancer treatment, although further work is needed to elucidate the safety and side effect of these compound in human.

Keywords: breast cancer, nano drug, tumor markers, CA15-3, α-IFN-PLGA, -IFN –SWNT

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7129 Combining Instance-Based and Reasoning-Based Approaches for Ontology Matching

Authors: Abderrahmane Khiat, Moussa Benaissa

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Due to the increasing number of sources of information available on the web and their distribution and heterogeneity, ontology alignment became a very important and inevitable problem to ensure semantic interoperability. Instance-based ontology alignment is based on the comparison of the extensions of concepts; and represents a very promising technique to find semantic correspondences between entities of different ontologies. In practice, two situations may arise: ontologies that share many common instances and ontologies that share few or do not share common instances. In this paper, we describe an approach to manage the latter case. This approach exploits the reasoning on ontologies in order to create a corpus of common instances. We show that it is theoretically powerful because it is based on description logics and very useful in practice. We present the experimental results obtained by running our approach on ontologies of OAEI 2012 benchmark test. The results show the performance of our approach.

Keywords: description logic inference, instance-based ontology alignment, semantic interoperability, semantic web

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7128 Active Surface Tracking Algorithm for All-Fiber Common-Path Fourier-Domain Optical Coherence Tomography

Authors: Bang Young Kim, Sang Hoon Park, Chul Gyu Song

Abstract:

A conventional optical coherence tomography (OCT) system has limited imaging depth, which is 1-2 mm, and suffers unwanted noise such as speckle noise. The motorized-stage-based OCT system, using a common-path Fourier-domain optical coherence tomography (CP-FD-OCT) configuration, provides enhanced imaging depth and less noise so that we can overcome these limitations. Using this OCT systems, OCT images were obtained from an onion, and their subsurface structure was observed. As a result, the images obtained using the developed motorized-stage-based system showed enhanced imaging depth than the conventional system, since it is real-time accurate depth tracking. Consequently, the developed CP-FD-OCT systems and algorithms have good potential for the further development of endoscopic OCT for microsurgery.

Keywords: common-path OCT, FD-OCT, OCT, tracking algorithm

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7127 A Survey on Compression Methods for Table Constraints

Authors: N. Gharbi

Abstract:

Constraint Satisfaction problems are mathematical problems that are often used to model many real-world problems for which we look if there exists a solution satisfying all its constraints. Table constraints are important for modeling parts of many problems since they list all combinations of allowed or forbidden values. However, they admit practical limitations because they are sometimes too large to be represented in a direct way. In this paper, we present a survey of the different categories of the proposed approaches to compress table constraints in order to reduce both space and time complexities.

Keywords: constraint programming, compression, data mining, table constraints

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7126 Formulation and Evaluation of Piroxicam Hydrotropic Starch Gel

Authors: Mohammed Ghazwani, Shyma Ali Alshahrani, Zahra Abdu Yousef, Taif Torki Asiri, Ghofran Abdur Rahman, Asma Ali Alshahrani, Umme Hani

Abstract:

Background and introduction: Piroxicam is a nonsteroidal anti-inflammatory drug characterized by low solubility-high permeability used to reduce pain, swelling, and joint stiffness from arthritis. Hydrotropes are a class of compounds that normally increase the aqueous solubility of insoluble solutes. Aim: The objective of the present research study was to formulate and optimize Piroxicam hydrotropic starch gel using sodium salicylate, sodium benzoate as hydrotropic salts, and potato starch for topical application. Materials and methods: The prepared Piroxicam hydrotropic starch gel was characterized for various physicochemical parameters like drug content estimation, pH, tube extrudability, and spreadability; all the prepared formulations were subjected to in-vitro diffusion studies for six hours in 100 ml phosphate buffer (pH 7.4) and determined gel strength. Results: All formulations were found to be white opaque in appearance and have good homogeneity. The pH of formulations was found to be between 6.9-7.9. Drug content ranged from 96.8%-99.4.5%. Spreadability plays an important role in patient compliance and helps in the uniform application of gel to the skin as gels should spread easily; F4 showed a spreadability of 2.4cm highest among all other formulations. In in vitro diffusion studies, extrudability and gel strength were good with F4 in comparison with other formulations; hence F4 was selected as the optimized formulation. Conclusion: Isolated potato starch was successfully employed to prepare the gel. Hydrotropic salt sodium salicylate increased the solubility of Piroxicam and resulted in a stable gel, whereas the gel prepared using sodium benzoate changed its color after one week of preparation from white to light yellowish. Hydrotropic potato starch gel proposed a suitable vehicle for the topical delivery of Piroxicam.

Keywords: Piroxicam, potato starch, hydrotropic salts, hydrotropic starch gel

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7125 Formulation and Characterization of Drug Loaded Niosomal Gel for Anti-Inflammatory Activity

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

Abstract:

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

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

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7124 Inhibition of Mixed Infection Caused by Human Immunodeficiency Virus and Herpes Virus by Fullerene Compound

Authors: Dmitry Nosik, Nickolay Nosik, Elli Kaplina, Olga Lobach, Marina Chataeva, Lev Rasnetsov

Abstract:

Background and aims: Human Immunodeficiency Virus (HIV) infection is very often associated with Herpes Simplex Virus (HSV) infection but HIV patients are treated with a cocktail of antiretroviral drugs which are toxic. The use of an antiviral drug which will be active against both viruses like ferrovir found in our previous studies is rather actual. Earlier we had shown that Fullerene poly-amino capronic acid (FPACA) was active in case of monoinfection of HIV-1 or HSV-1. The aim of the study was to analyze the efficiency of FPACA against mixed infection of HIV and HSV. Methods: The peripheral blood lymphocytes, CEM, MT-4 cells were simultaneously infected with HIV-1 and HSV-1. FPACA was added 1 hour before infection. Cells viability was detected by MTT assay, virus antigens detected by ELISA, syncytium formation detected by microscopy. The different multiplicity of HIV-1/HSV-1 ratio was used. Results: The double viral HIV-1/HSV-1 infection was more cytopathic comparing with monoinfections. In mixed infection by the HIV-1/HSV-1 concentration of HIV-1 antigens and syncytium formations increased by 1,7 to 2,3 times in different cells in comparison with the culture infected with HIV-1 alone. The concentration of HSV-1 increased by 1,5-1,7 times, respectively. Administration of FPACA (1 microg/ml) protected cells: HIV-1/HSV-1 (1:1) – 80,1%; HIV-1/HSV-1 (1:4) – 57,2%; HIV-1/HSV-1 (1:8) – 46,3 %; HIV-1/HSV-1 (1:16) – 17,0%. Virus’s antigen levels were also reduced. Syncytium formation was totally inhibited in all cases of mixed infection. Conclusion: FPACA showed antiviral activity in case of mixed viral infection induced by Human Immunodeficiency Virus and Herpes Simplex Virus. The effect of viral inhibition increased with the multiplicity of HIV-1 in the inoculum. The mechanism of FPACA action is connected with the blocking of the virus particles adsorption to the cells and it could be suggested that it can have an antiviral activity against some other viruses too. Now FPACA could be considered as a potential drug for treatment of HIV disease complicated with opportunistic herpes viral infection.

Keywords: antiviral drug, human immunodeficiency virus (hiv), herpes simplex virus (hsv), mixed viral infection

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7123 An Attack on the Lucas Based El-Gamal Cryptosystem in the Elliptic Curve Group Over Finite Field Using Greater Common Divisor

Authors: Lee Feng Koo, Tze Jin Wong, Pang Hung Yiu, Nik Mohd Asri Nik Long

Abstract:

Greater common divisor (GCD) attack is an attack that relies on the polynomial structure of the cryptosystem. This attack required two plaintexts differ from a fixed number and encrypted under same modulus. This paper reports a security reaction of Lucas Based El-Gamal Cryptosystem in the Elliptic Curve group over finite field under GCD attack. Lucas Based El-Gamal Cryptosystem in the Elliptic Curve group over finite field was exposed mathematically to the GCD attack using GCD and Dickson polynomial. The result shows that the cryptanalyst is able to get the plaintext without decryption by using GCD attack. Thus, the study concluded that it is highly perilous when two plaintexts have a slight difference from a fixed number in the same Elliptic curve group over finite field.

Keywords: decryption, encryption, elliptic curve, greater common divisor

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7122 Effect of Common Yoga Protocol on Reaction Time of Football Players

Authors: Vikram Singh

Abstract:

The objective of the study was to study the effectiveness of common yoga protocol on reaction time (simple visual reaction time-SVRT measured in milliseconds/seconds) of male football players in the age group of 15 to 21 years. The 40 boys were randomly assigned into two groups i.e. control and experimental. SVRT for both the groups were measured on day-1 and post intervention (common yoga protocol here) was measured after 45 days of training to the experimental group only. One way ANOVA (Univariate analysis) and Independent t-test using SPSS 23 statistical package was applied to get and analyze the results. There was a significant difference after 45 days of yoga protocol in simple visual reaction time of experimental group (p = .032), t (33.05) = 3.881, p = .000 (two-tailed). Null hypothesis (that there would be no post measurement differences in reaction times of control and experimental groups) was rejected. Where p<.05. Therefore alternate hypothesis was accepted.

Keywords: footballers, t-test, yoga protocol, reaction time

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7121 Capsaicin Derivatives Enhanced Activity of α1β2γ2S-Aminobutyric Acid Type a Receptor Expressed in Xenopus laevis Oocytes

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

Abstract:

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

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

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7120 Characteristics of Acute Poisoning in Emergency Departments: Multicenter Study in Korea

Authors: Hyuk-Hoon Kim, Young Gi Min

Abstract:

Background: Acute poisoning is the common cause of morbidity and mortality. Characteristics of acute poisoning differ between countries. While other countries operate the database system for poisoning, Korea has not collected the database for acute poisoning. Distribution of incidence of acute poisoning depending on the types of materials have also not studied in Korea. Our aims are to evaluate the etiologic and demographic characteristics of acute poisoning cases and to obtain up-to-date information on acute poisonings. Method: We retrospectively recorded cases of acute poisoning from eight emergency departments of second level or university hospitals from different cities in Gyeonggi province in Korea from April 2006 and March 2015. The distributions of incidence of acute poisoning depending on the types of materials are mapped by geographic information system. Result: A total of 3,449 poisoned cases were analyzed. Mean estimated age of patients was 39.56 ± 22.40 years. Mean male to female ratio of patients was 1:1.4. Mean proportion of intentional poisoning was 57.9%. Common materials are benzodiazepine (16.6%), carbon monoxide (10.5%), pesticide (8.1%) and zolpidem (7.1%) Common route of exposure is ingestion (79.5%) and followed by inhalation (16.5%). Common treatment methods are gastric lavage (20%) and activated charcoal (30%). Most cases had uneventful recovery; 61.4% were treated as outpatients and 0.1% of the poisoning resulted in death in ER. Conclusion: Even though the cases enrolled in our study is not the overall cases of acute poisoning in Korea, our study could be the basis of countermeasures for analysis and prevention of acute poisoning in Korea.

Keywords: acute poisoning, emergency department, epidemiology, Korea

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7119 Development and Validation of a Green Analytical Method for the Analysis of Daptomycin Injectable by Fourier-Transform Infrared Spectroscopy (FTIR)

Authors: Eliane G. Tótoli, Hérida Regina N. Salgado

Abstract:

Daptomycin is an important antimicrobial agent used in clinical practice nowadays, since it is very active against some Gram-positive bacteria that are particularly challenges for the medicine, such as methicillin-resistant Staphylococcus aureus (MRSA) and vancomycin-resistant Enterococci (VRE). The importance of environmental preservation has receiving special attention since last years. Considering the evident need to protect the natural environment and the introduction of strict quality requirements regarding analytical procedures used in pharmaceutical analysis, the industries must seek environmentally friendly alternatives in relation to the analytical methods and other processes that they follow in their routine. In view of these factors, green analytical chemistry is prevalent and encouraged nowadays. In this context, infrared spectroscopy stands out. This is a method that does not use organic solvents and, although it is formally accepted for the identification of individual compounds, also allows the quantitation of substances. Considering that there are few green analytical methods described in literature for the analysis of daptomycin, the aim of this work was the development and validation of a green analytical method for the quantification of this drug in lyophilized powder for injectable solution, by Fourier-transform infrared spectroscopy (FT-IR). Method: Translucent potassium bromide pellets containing predetermined amounts of the drug were prepared and subjected to spectrophotometric analysis in the mid-infrared region. After obtaining the infrared spectrum and with the assistance of the IR Solution software, quantitative analysis was carried out in the spectral region between 1575 and 1700 cm-1, related to a carbonyl band of the daptomycin molecule, and this band had its height analyzed in terms of absorbance. The method was validated according to ICH guidelines regarding linearity, precision (repeatability and intermediate precision), accuracy and robustness. Results and discussion: The method showed to be linear (r = 0.9999), precise (RSD% < 2.0), accurate and robust, over a concentration range from 0.2 to 0.6 mg/pellet. In addition, this technique does not use organic solvents, which is one great advantage over the most common analytical methods. This fact contributes to minimize the generation of organic solvent waste by the industry and thereby reduces the impact of its activities on the environment. Conclusion: The validated method proved to be adequate to quantify daptomycin in lyophilized powder for injectable solution and can be used for its routine analysis in quality control. In addition, the proposed method is environmentally friendly, which is in line with the global trend.

Keywords: daptomycin, Fourier-transform infrared spectroscopy, green analytical chemistry, quality control, spectrometry in IR region

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7118 Application of Observational Medical Outcomes Partnership-Common Data Model (OMOP-CDM) Database in Nursing Health Problems with Prostate Cancer-a Pilot Study

Authors: Hung Lin-Zin, Lai Mei-Yen

Abstract:

Prostate cancer is the most commonly diagnosed male cancer in the U.S. The prevalence is around 1 in 8. The etiology of prostate cancer is still unknown, but some predisposing factors, such as age, black race, family history, and obesity, may increase the risk of the disease. In 2020, a total of 7,178 Taiwanese people were nearly diagnosed with prostate cancer, accounting for 5.88% of all cancer cases, and the incidence rate ranked fifth among men. In that year, the total number of deaths from prostate cancer was 1,730, accounting for 3.45% of all cancer deaths, and the death rate ranked 6th among men, accounting for 94.34% of the cases of male reproductive organs. Looking for domestic and foreign literature on the use of OMOP (Observational Medical Outcomes Partnership, hereinafter referred to as OMOP) database analysis, there are currently nearly a hundred literature published related to nursing-related health problems and nursing measures built in the OMOP general data model database of medical institutions are extremely rare. The OMOP common data model construction analysis platform is a system developed by the FDA in 2007, using a common data model (common data model, CDM) to analyze and monitor healthcare data. It is important to build up relevant nursing information from the OMOP- CDM database to assist our daily practice. Therefore, we choose prostate cancer patients who are our popular care objects and use the OMOP- CDM database to explore the common associated health problems. With the assistance of OMOP-CDM database analysis, we can expect early diagnosis and prevention of prostate cancer patients' comorbidities to improve patient care.

Keywords: OMOP, nursing diagnosis, health problem, prostate cancer

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7117 Association of Glutathione S-transferase M1 and T1 Gene Polymorphisms with Vitiligo in Saudi Population

Authors: Ghaleb Bin Huraib, Fahad Al Harthi, Mohammad Mustafa, Abdulrahman Al-Asmari

Abstract:

Introduction: Vitiligo is an acquired pigmentary skin disorder with the regional disappearance of melanocytes. Vitiligo affects 0.1 to 2% of the global population, and the incidence varies substantially depending on ethnicity. Glutathione S-transferase (GST) is a multigene family of enzymes that detoxify oxidative stress products. The oxidative stress-related GSTM1/GSTT1 genes deletion may cause epidermal melanocytes destruction and the development of vitiligo. Hence, the present study aimed to investigate the association of GST gene polymorphisms with vitiligo in the Saudi population, if any. Materials and Methods: The present study includes 129 vitiligo cases and 130 age-matched healthy controls. The proportion of male and female patients with vitiligo is almost equal. The multiplex polymerase chain reaction (PCR) method was used for polymorphic analysis. Results: Increased odds of generalized vitiligo was observed with the null genotypes of GSTT1- gene (OR = 1.91, 95% CI = 1.07-3.42, p = 0.019). The possible genetic combinations of GSTM1/GSTT1 and their genotypic distribution showed the frequency of GSTM1+/GSTT1+ 62/130 (47.69%) and GSTM1-/GSTT1+ 52/130 (40.00%) were higher in controls than in cases 44/129 (34.11%), 43/129 (33.34%), respectively while GSTM1+/GSTT1- and GSTM1-/GSTT1- null genotypes were higher 22/129 (17.05%) and 20/129 (15.50%) in vitiligo patients as compared to controls 11/130 (8.46%), 5/130 (3.84%), respectively. The strength of association of different genetic combinations with cases have shown GSTM1+/GSTT1- (OR = 2.81, 95% CI = 1.24-6.40, p = 0.009) and GSTM1-/GSTT1- (OR = 5.63, 95% CI = 1.96 - 16.16, p = 0.0004) were significantly higher in vitiligo cases as compared to controls. We did not observe any significant association of age and gender of patients with GST gene polymorphisms. Conclusions: The GSTT1-, GSTM1+/GSTT1- and GSTM1-/GSTT1- null genotypes were significantly associated with vitiligo. These genetic polymorphisms may be the associative genetic risk factor for vitiligo among Saudis. It could be used as a genetic marker for screening vitiligo patients among Saudis. Further studies on GSTs gene polymorphism in larger sample sizes from different geographical areas and ethnicity are needed to strengthen the present findings.

Keywords: vitiligo, GSTM1, GSTT1, gene polymorphism, oxidative stress

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7116 Refractory Visceral Leishmaniasis Responding to Second-Line Therapy

Authors: Preet Shah, Om Shrivastav

Abstract:

Introduction : In India, Leishmania donovani is the only parasite causing Leishmaniasis. The parasite infects the reticuloendothelial system and is found in the bone marrow, spleen and liver. Treatment of choice is amphotericin-B with sodium stibogluconate being an alternative. Miltefosine is useful in refractory cases. In our case, Leishmaniasis occurred in a person residing in western India (which is quite rare) and it failed to respond to two different drugs (again an uncommon feature) before it finally responded to a third one. Description: A 50 year old lady, a resident of western India, with no history of recent travel, presented with an ulcer on the left side of the nose since 8 months. She was apparently alright 8 months back, when she noticed a small ulcerated lesion on the left ala of the nose which was immediately biopsied. The biopsy revealed amastigotes of Leishmania for which she was administered intra-lesional sodium stibogluconate for 1 month (4 doses every 8 days).Despite this, there was no regression of the ulcer and hence she presented to us for further management. On examination, her vital parameters were normal. Barring an ulcer on the left side of the nose, rest of the examination findings were unremarkable. Complete blood count was normal. Ultrasound abdomen showed hepatomegaly. PET-CT scan showed increased metabolic activity in left ala of nose, hepatosplenomegaly and increased metabolic activity in spleen and bone marrow. Bone marrow biopsy was done which showed hypercellular marrow with erythroid preponderance. Considering a diagnosis of leishmaniasis which had so far been unresponsive to sodium stibogluconate, she was started on liposomal amphotericin-B. At the time of admission, her creatinine level was normal, but it started rising with the administration of liposomal amphotericin-B, hence the dose was reduced. Despite this, creatinine levels did not improve, and she started developing hypokalemia and hypomagnesemia as side effects of the drug, hence further reductions in the dosage were made. Despite a total of 3 weeks of liposomal amphotericin-B, there was no improvement in the ulcer. As had so far failed to respond to sodium stibogluconate and liposomal amphotericin-B, it was decided to start her on miltefosine. She received the miltefosine for a total of 12 weeks. At the end of this duration, there was a marked regression of the cutaneous lesion. Conclusion: Refractoriness to amphotericin-B in leishmaniasis may be seen in up to 5 % cases. Here, an alternative drug such as miltefosine is useful and hence we decided to use it, to which she responded adequately. Furthermore, although leishmaniasis is common in the eastern part of India, it is a relatively unknown entity in the western part of the country with the occurrence being very rare. Because of these 2 reasons, we consider our case to be a unique one.

Keywords: amphotericin-b, leishmaniasis, miltefosine, tropical diseases

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7115 Effect of Risperidone and Haloperidol on Clinical Picture and Some Biochemical Parameters of Schizophrenic Libyan Patients

Authors: Mabruka S. Elashheb, Adullah Ali Bakush

Abstract:

Schizophrenia is referred to as a disorder, not a disease, because there has not been any clear, reliable, and specific etiological factor. Even if schizophrenia is not a very frequent disease, it is among the most burdensome and costly illnesses worldwide. Prevention of relapse is a major goal of maintenance treatment in patients with psychotic disorders. We performed a comparison of a newer, atypical antipsychotic drug, Risperidone, and an older, conventional neuroleptic drug, Haloperidol, in terms of the effect on the usual kidney and liver functions and negative and positive symptoms in patients with schizophrenia and schizoaffective disorder after three and five weeks of their treatments. It is apparent from the comparative data of Haloperidol and Risperidone treatments in schizophrenic patients that Resperidone had superior improvement of negative and positive symptoms of patients, no harmful effect on liver and kidney functions and greater efficacy and faster recovery from schizophrenic symptoms in patients. On the basis of our findings of the present study, we concluded that treatment with Risperidone is superior to Haloperidol in reducing the risk of relapse among outpatients with schizophrenic disorders.

Keywords: schizophrenia, Haloperidol, Risperidone, positive and negative symptom

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7114 Design and Development of Sustained Release Floating Tablet of Stavudine

Authors: Surajj Sarode, G. Vidya Sagar, G. P. Vadnere

Abstract:

The purpose of the present study was to prolong the gastric residence time of Stavudine by developing gastric floating drug delivery system (GFDDS). Moreover, to study influence of different polymers on its release rate using gas-forming agents, like sodium bicarbonate, citric acid. Floating tablets were prepared by wet granulation method using PVP K-30 as a binder and the other polymers include Pullulan Gum, HPMC K100M, six different formulations with the varying concentrations of polymers were prepared and the tablets were evaluated in terms of their pre-compression parameters like bulk density, tapped density, Haunsner ratio, angle of repose, compressibility index, post compression physical characteristics, in vitro release, buoyancy, floating lag time (FLT), total floating time (TFT) and swelling index. All the formulations showed good floating lag time i.e. less than 3 mins. The batch containing combination of Pullulan Gum and HPMC 100M (i.e. F-6) showed total floating lag time more than 12 h., the highest swelling index among all the prepared batches. The drug release was found to follow zero order kinetics.

Keywords: Suavudine, floating, total floating time (TFT), gastric residence

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7113 The Toxic Effects of Kynurenine Metabolites on SH-SY5Y Neuroblastoma Cells

Authors: Susan Hall, Gary D. Grant, Catherine McDermott, Devinder Arora

Abstract:

Introduction /Aim: The kynurenine pathway is thought to play an important role in the pathophysiology of numerous neurodegenerative diseases including depression, Alzheimer’s disease, and Parkinson’s disease. Numerous neuroactive compounds, including the neurotoxic 3-hydroxyanthranilic acid, 3-hydroxykynurenine and quinolinic acid and the neuroprotective kynurenic acid and picolinic acid, are produced through the metabolism of kynurenine and are thought to be the causative agents responsible for neurodegeneration. The toxicity of 3-hydroxykynurenine, 3-hydroxyanthranilic acid and quinolinic acid has been widely evaluated and demonstrated in primary cell cultures but to date only 3-hydroxykynurenine and 3-hydroxyanthranilic acid have been shown to cause toxicity in immortal tumour cells. The aim of this study was to evaluate the toxicity of kynurenine metabolites, both individually and in combination, on SH-SY5Y neuroblastoma cells after 24 and 72 h exposure in order to explore a cost-effective model to study their neurotoxic effects and potential protective agents. Methods: SH-SY5Y neuroblastoma cells were exposed to various concentrations of the neuroactive kynurenine metabolites, both individually and in combination, for 24 and 72 h, and viability was subsequently evaluated using the Resazurin (Alamar blue) proliferation assay. Furthermore, the effects of these compounds, alone and in combination, on specific death pathways including apoptosis, necrosis and free radical production was evaluated using various assays. Results: Consistent with literature, toxicity was shown with short-term 24-hour treatments at 1000 μM concentrations for both 3-hydroxykynurenine and 3-hydroxyanthranilic acid. Combinations of kynurenine metabolites showed modest toxicity towards SH-SY5Y neuroblastoma cells in a concentration-dependent manner. Specific cell death pathways, including apoptosis, necrosis and free radical production were shown to be increased after both 24 and 72 h exposure of SH-SY5Y neuroblastoma cells to 3-hydroxykynurenine and 3-hydroxyanthranilic acid and various combinations of neurotoxic kynurenine metabolites. Conclusion: It is well documented that neurotoxic kynurenine metabolites show toxicity towards primary human neurons in the nanomolar to low micromolar concentration range. Results show that the concentrations required to show significant cell death are in the range of 1000 µM for 3-hydroxykynurenine and 3-hydroxyanthranilic acid and toxicity of quinolinic acid towards SH-SY5Y was unable to be shown. This differs significantly from toxicities observed in primary human neurons. Combinations of the neurotoxic metabolites were shown to have modest toxicity towards these cells with increased toxicity and activation of cell death pathways observed after 72 h exposure. This study suggests that the 24 h model is unsuitable for use in neurotoxicity studies, however, the 72 h model better represents the observations of the studies using primary human neurons and may provide some benefit in providing a cost-effective model to assess possible protective agents against kynurenine metabolite toxicities.

Keywords: kynurenine metabolites, neurotoxicity, quinolinic acid, SH-SY5Y neuroblastoma

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7112 Role of Oxidative Stress and Nitric Oxide in the Protective Effects of Simvastatine against Isoniazid-Rifampicin-Induced Hepatotoxicity in Rats

Authors: Mabroka Omar Sherehe

Abstract:

Despite the great efficacy of isoniazid (INH) and rifampicine (RIF) combination in the treatment of tuberculosis, hepatotoxicity is the most common serious complication. The potential protective effect of simvastatin (sim) against combination-induced hepatotoxicity was investigated in the present study. The administration of INH-RIF combination (50mg/kg each for 14 days) resulted in a significant increased activities of serum alanine and aspartate aminotransferases, such effects were further supported by histopathological studies. INH-RIF combination produced a significant increase in liver lipid, decreased SOD and CAT, and a significant depletion of GSH level. Additionally, treatment with INH-RIF combination resulted in a significant increase in liver MPO activity. The lipid-lowering drug, Sim demonstrated in the current study an evident antioxidant action, such effect was mediated via decreasing the elevated MDA, MPO, and restoring liver CAT activity. Additionally, Sim restored liver NO level to near basal value Furthermore, one cannot rule out the lipid-lowering effect of Sim that would probably add to its beneficial hepatoprotective antioxidant activity, where Sim decreased the elevated cholesterol, TGs and LDL cholesterol level and increased the serum HDL cholesterol level.

Keywords: isoniazid, rifampicine, oxidative stress, nitric oxide

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7111 Phylogenetic Analysis of Klebsiella Species from Clinical Specimens from Nelson Mandela Academic Hospital in Mthatha, South Africa

Authors: Sandeep Vasaikar, Lary Obi

Abstract:

Rapid and discriminative genotyping methods are useful for determining the clonality of the isolates in nosocomial or household outbreaks. Multilocus sequence typing (MLST) is a nucleotide sequence-based approach for characterising bacterial isolates. The genetic diversity and the clinical relevance of the drug-resistant Klebsiella isolates from Mthatha are largely unknown. For this reason, prospective, experimental study of the molecular epidemiology of Klebsiella isolates from patients being treated in Mthatha over a three-year period was analysed. Methodology: PCR amplification and sequencing of the drug-resistance-associated genes, and multilocus sequence typing (MLST) using 7 housekeeping genes mdh, pgi, infB, FusAR, phoE, gapA and rpoB were conducted. A total of 32 isolates were analysed. Results: The percentages of multidrug-resistant (MDR), extensively drug-resistance (XDR) and pandrug-resistant (PDR) isolates were; MDR 65.6 % (21) and XDR and PDR with 0 % each. In this study, K. pneumoniae was 19/32 (59.4 %). MLST results showed 22 sequence types (STs) were identified, which were further separated by Maximum Parsimony into 10 clonal complexes and 12 singletons. The most dominant group was Klebsiella pneumoniae with 23/32 (71.8 %) isolates, Klebsiella oxytoca as a second group with 2/32 (6.25 %) isolates, and a single (3.1 %) K. varricola as a third group while 6 isolates were of unknown sequences. Conclusions/significance: A phylogenetic analysis of the concatenated sequences of the 7 housekeeping genes showed that strains of K. pneumoniae form a distinct lineage within the genus Klebsiella, with K. oxytoca and K. varricola its nearest phylogenetic neighbours. With the analysis of 7 genes were determined 1 K. variicola, which was mistakenly identified as K. pneumoniae by phenotypic methods. Two misidentifications of K. oxytoca were found when phenotypic methods were used. No significant differences were observed between ESBL blaCTX-M, blaTEM and blaSHV groups in the distribution of Sequence types (STs) or Clonal complexes (CCs).

Keywords: phylogenetic analysis, phylogeny, klebsiella phylogenetic, klebsiella

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7110 A Case Study on Parent-Child Relationship, Attachment Styles, and Romantic Relationship Quality of Illegitimate Emerging Adults

Authors: Pierre Nicole Patriarca

Abstract:

This study examined the attachment styles, parent-child relationship, and romantic relationship quality of five illegitimate emerging adults aged 18 to 23 years old. The researcher used self-report measures, inventory of parent and peer attachment, attachment style questionnaire, and network of relationship – relationship quality version in obtaining data. A semi-structured interview was also used to acquire qualitative data about the detailed perception and experiences on the attachment styles and parent-child relationship. Common themes of each variable were identified through thematic analysis. Results showed that four out of five participants depicted positive relationship to their fathers, while all of them reported to have positive relationship to their mothers. It was also found that four participants have preoccupied attachment style, while the other one has fearful attachment style. Common themes in describing their relationship with their mother include being close, influential to participants’ life, unbounded communication, favorable reason of trusting, and sometimes being inattentive. On the other hand, having distant relationship, limited communication about romantic relationship, uninfluential to participant’s life, and favorable reason of trusting were the common themes in describing relationship with father. Lastly, less trusting, being dependent, and emphasis on valuing intimacy were the common themes in describing their style of attachment.

Keywords: illegitimate, emerging adult, attachment, parent-child relationship, relationship quality

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7109 Prevalence and Factors Associated with Illicit Drug Use Among Undergraduate Students in the University of Lagos, Nigeria

Authors: Abonyi, Emmanuel Ebuka, Amina Jafaru O.

Abstract:

Background: Illicit substance use among students is a phenomenon that has been widely studied, but it remains of interest due to its high prevalence and potential consequences. It is a major mental health concern among university students which may result in behavioral and academic problems, psychiatric disorders, and infectious diseases. Thus, this study was done to ascertain the prevalence and factors associated with the use of illicit drugs among these groups of people. Methods: A cross-sectional and descriptive survey was conducted among undergraduate students of the University of Lagos for the duration of three(3) months (August to October 2021). A total number of 938 undergraduate students were selected from seventeen faculties in the university. Pretested questionnaires were administered, completed, and returned. The data were analyzed using descriptive statistics and multivariate regression analysis. Results: From the data collected, it was observed that out of 938 undergraduate students of the University of Lagos that completed and returned the questionnaires, 56.3% were female and 43.7% were male. No gender differences were observed in the prevalence of use of any of the illicit substances. The result showed that the majority of the students that participated in the research were females(56.6%); it was observed that there were a total of 541 2nd-year students(57.7%) and 397 final-year students(42.3). Students between the age brackets of 20- 24 years had the highest frequency of 648(69.1%) of illicit drug use and students in none health-related disciplines. The result also showed that the majority of the students reported that they use Marijuana (31.7%), while lifetime use of LSD (6.3%), Heroin(4.8%), Cocaine (4.7%), and Ecstasy(4.5), Ketamine (3.4%). Besides, the use of alcohol was below average(44.1%). Additionally, Marijuana was among the ones that were mostly taken by students having a higher percentage and most of these respondents had experienced relationship problems with their family and intentions (50.9%). From the responses obtained, major reasons students indulge in illicit drug use were; curiosity to experiment, relief of stress after rigorous academic activities, social media influence, and peer pressure. Most Undergraduate students are in their most hyperactive stage in life, which makes them vulnerable to always want to explore practically every adventure. Hence, individual factors and social media influence are identified as major contributors to the prevalence of illicit drug use among undergraduate students at the University of Lagos, Nigeria. Conclusion: Control programs are most needed among the students. They should be comprehensive and focused on students' psycho-education about substances and their related negative consequences, plus the promotion of students' life skills, and integration into the family – and peer-based preventive interventions.

Keywords: illicit drugs, addiction, undergraduate students, prevalence, substances

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7108 Manufacturing an Eminent Mucolytic Medicine Using an Efficient Synthesis Path

Authors: Farzaneh Ziaee, Mohammad Ziaee

Abstract:

N-acetyl-L-cysteine (NAC) is a well-known mucolytic agent, and recently its efficacy has been examined for the prevention and remediation of several diseases such as lung infections caused by Coronavirus. Also, it is administrated as the main antidote in paracetamol overdose and is effective for the treatment of idiopathic pulmonary fibrosis (IPF), chronic obstructive pulmonary disease (COPD). This medicine is used as an antioxidant to prevent diabetic kidney disease (nephropathy). In this study, a method for the acylation of amino acids is employed to manufacture this drug in a height yield. Regarding this patented path, NAC can be made in a single batch step at ambient pressure and temperature. Moreover, this study offers a technique to make peptide bonds which is of interest for pharmaceutical and medicinal industries. The separation process was undertaken using appropriate solvents to achieve an excellent purification level. The synthesized drug was characterized via proton nuclear magnetic resonance (1H NMR), high-performance liquid chromatography (HPLC), Fourier transform infrared spectroscopy (FT-IR), elemental analysis, and melting point.

Keywords: N-acetylcysteine, synthesis, mucolytic medication, lung anti-inflammatory, COVID-19, antioxidant, pharmaceutical supplement, characterization

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7107 U11 Functionalised Luminescent Gold Nanoclusters for Pancreatic Tumor Cells Labelling

Authors: Regina M. Chiechio, Rémi Leguevél, Helene Solhi, Marie Madeleine Gueguen, Stephanie Dutertre, Xavier, Jean-Pierre Bazureau, Olivier Mignen, Pascale Even-Hernandez, Paolo Musumeci, Maria Jose Lo Faro, Valerie Marchi

Abstract:

Thanks to their ultra-small size, high electron density, and low toxicity, gold nanoclusters (Au NCs) have unique photoelectrochemical and luminescence properties that make them very interesting for diagnosis bio-imaging and theranostics. These applications require control of their delivery and interaction with cells; for this reason, the surface chemistry of Au NCs is essential to determine their interaction with the targeted biological objects. Here we demonstrate their ability as markers of pancreatic tumor cells. By functionalizing the surface of the NCs with a recognition peptite (U11), the nanostructures are able to preferentially bind to pancreatic cancer cells via a receptor (uPAR) overexpressed by these cells. Furthermore, the NCs can mark even the nucleus without the need of fixing the cells. These nanostructures can therefore be used as a non-toxic, multivalent luminescent platform, capable of selectively recognizing tumor cells for bioimaging, drug delivery, and radiosensitization.

Keywords: gold nanoclusters, luminescence, biomarkers, pancreatic cancer, biomedical applications, bioimaging, fluorescent probes, drug delivery

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7106 Antimicrobial Activity of 2-Nitro-1-Propanol and Lauric Acid against Gram-Positive Bacteria

Authors: Robin Anderson, Elizabeth Latham, David Nisbet

Abstract:

Propagation and dissemination of antimicrobial resistant and pathogenic microbes from spoiled silages and composts represents a serious public health threat to humans and animals. In the present study, the antimicrobial activity of the short chain nitro-compound, 2-nitro-1-propanol (9 mM) as well as the medium chain fatty acid, lauric acid, and its glycerol monoester, monolaurin, (each at 25 and 17 µmol/mL, respectfully) were investigated against select pathogenic and multi-drug resistant antimicrobial resistant Gram-positive bacteria common to spoiled silages and composts. In an initial study, we found that growth rates of a multi-resistant Enterococcus faecalis (expressing resistance against erythromycin, quinupristin/dalfopristin and tetracycline) and Staphylococcus aureus strain 12600 (expressing resistance against erythromycin, linezolid, penicillin, quinupristin/dalfopristin and vancomycin) were more than 78% slower (P < 0.05) by 2-nitro-1-propanol treatment during culture (n = 3/treatment) in anaerobically prepared ½ strength Brain Heart Infusion broth at 37oC when compared to untreated controls (0.332 ± 0.04 and 0.108 ± 0.03 h-1, respectively). The growth rate of 2-nitro-1-propanol-treated Listeria monocytogenes was also decreased by 96% (P < 0.05) when compared to untreated controls cultured similarly (0.171 ± 0.01 h-1). Maximum optical densities measured at 600 nm were lower (P < 0.05) in 2-nitro-1-propanol-treated cultures (0.053 ± 0.01, 0.205 ± 0.02 and 0.041 ± 0.01, respectively) than in untreated controls (0.483 ± 0.02, 0.523 ± 0.01 and 0.427 ± 0.01, respectively) for E. faecalis, S. aureus and L. monocytogenes, respectively. When tested against mixed microbial populations during anaerobic 24 h incubation of spoiled silage, significant effects of treatment with 1 mg 2-nitro-1-propanol (approximately 9.5 µmol/g) or 5 mg lauric acid/g (approximately 25 µmol/g) on populations of wildtype Enterococcus and Listeria were not observed. Mixed populations treated with 5 mg monolaurin/g (approximately 17 µmol/g) had lower (P < 0.05) viable cell counts of wildtype enterococci than untreated controls after 6 h incubation (2.87 ± 1.03 versus 5.20 ± 0.25 log10 colony forming units/g, respectively) but otherwise significant effects of monolaurin were not observed. These results reveal differential susceptibility of multi-drug resistant enterococci and staphylococci as well as L. monocytogenes to the inhibitory activity of 2-nitro-1-propanol and the medium chain fatty acid, lauric acid and its glycerol monoester, monolaurin. Ultimately, these results may lead to improved treatment technologies to preserve the microbiological safety of silages and composts.

Keywords: 2-nitro-1-propanol, lauric acid, monolaurin, gram positive bacteria

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