Pharmacology Commons^™

Doxorubicin Modulates P-Glycoprotein Transcription Differently During Caco-2 Differentiation, Udomsak Udomnilobol, Suree Jianmongko

The Thai Journal of Pharmaceutical Sciences

P-glycoprotein (P-gp) is an efflux transporter protecting cells from various chemical threats. Upregulation of P-gp expression, mediated by reactive oxygen species (ROS), has been reported in doxorubicin-treated cells. However, during cell differentiation cellular redox status may vary. This study investigated the influence of cell differentiation on doxorubicin-mediated P-gp expression in Caco-2 cells, and its relation to cellular redox status. During 21-day culture, Caco-2 cells were divided into pre-, during-, and post-differentiation, based on total cell numbers, percentage of G0/G1 cells, and alkaline phosphatase activity. Our study demonstrated that Caco-2 cells were in a more reduced state on differentiation. At low …

Evaluation Of Acute Oral Toxicity Of Methanolic Fractions Of Sesbania Grandiflora Linn. Roots In Albino Mice, N. S. Vinay, S. Babitha, R. Nandeesh, S. Paramesh, E. Manjunath, J. P. Geetha, V. P. Veerapur, B. Swetha, H. V. Keerthi Prasanth

The Thai Journal of Pharmaceutical Sciences

Introduction: Although Sesbania grandiflora Linn. roots have valuable pharmacological effects, the comprehensive awareness about its toxicity potential has been lacking. Objectives: The objectives of the study were to assess the acute oral toxicity of methanolic fraction of S. grandiflora root (MFSGR). Materials and Methods: The female albino mice were divided into two groups (n = 5), one group served as normal control while the other treated with MFSGR (2000 mg/kg, p.o). Both the groups of mice were observed for 14 days for various parameters according to the Organization for Economic Cooperative and Development guidelines 425 TG. Results: Oral administration of …

Pharmacognostic And Chromatographic Evaluation Of Male And Female Flowers Of Coscinium Fenestratum For Berberine Content And Its Effect On Antioxidant Activity, T. S. Roopashree, Kuntal Das, N. Prashanth, K. Rakesh Kumar

The Thai Journal of Pharmaceutical Sciences

Coscinium fenestratum (CF) (Gaertn.) Colebr., [Family: Menispermaceae] is an endangered species of dioecious liana found in Western Ghats of India. The present investigation aimed with systematic analytical studies on the macroscopic, microscopic examination of male and female CF flowers, various solvent extractions, accompanied by phytochemical screening through chemical tests, identification of Berberine alkaloids, antioxidant activity, and Berberine quantification byhigh-performance thin-layer chromatography (HPTLC) process. Two different amounts of solvents (10 ml and 20 ml) with two different time intervals, that is, 15 min and 25 min, respectively, were used for extraction. Results revealed that both flowers had their own unique characters. …

Anthraquinones Extracted From Rubia Cordifolia Linn As Potential Ligands To Treat Alzheimer’S Disease, Pottella Srinivasulu, Janga Ramesh Babu, T.N.V. Ganesh Kumar, Padarthi Pavan Kumar, S. Vidyadhara

The Thai Journal of Pharmaceutical Sciences

Objective: The present investigation aims to predict the pharmacokinetic aspects and assessing the anti-Alzheimer’s activity using both molecular docking platform and ex vivo pharmacological studies on muscle contraction. Materials and Methods: 2-Methyl Anthraquinone (MAQ) and Quinizarine (QNZ) were isolated from Rubia cordifolia L., and evaluated for absorption, distribution, metabolism, excretion, and toxicity. Molecular docking was performed with the help of Mcule software on five drug targets acetylcholinesterase enzyme (AChE), cyclin-dependent kinase5 (CDK5), glycogen synthase kinase 3β (GSK3β), monoamine oxidase (MAO-B), and β-secretase enzyme (BACE). The pharmacological activity was screened by recording the muscle contractions of chick ileum. Results: The selected …

Current Perspectives On The Therapeutic Potential Of Mitragyna Speciosa And Its Derivatives On Animal Model, Norsyifa Harun, Illa Syafiqah Johari, Rima Atria Japarin, Farah Wahida Suhaimi, Zurina Hassan, Mohammed Shoaib

The Thai Journal of Pharmaceutical Sciences

The plant Mitragyna speciosa Korth. is receiving increased attention as a therapeutic substitution for opioid use disorder (OUD). The active alkaloids constituents of the plant, particularly mitragynine and 7-hydroxymitragynine, have been shown to modulate opioid receptors, acting as agonists at mu-opioid receptors. Given this pharmacology, several studies have examined the abuse and dependence potential of M. speciosa and its alkaloids in various animal models of dependence. In addition to action on opioid receptors, the Mitragyna alkaloids also appear to exert diverse activities at other receptors in the central nervous system which may explain the complex pharmacological profile of these alkaloids. …

Evidence For Intravenous Self-Administration Of Mitragynine In Fentanyl-Dependent Rats, Norsyifa Harun, Zurina Hassan, Surash Ramanathan, Mohammed Shoaib

The Thai Journal of Pharmaceutical Sciences

Introduction: Kratom (Mitragyna speciosa Korth) is currently used as an alternative for the self-treatment of pain and management of opioid dependence and withdrawal. Due to the opioid-like effect of the plant’s active alkaloid, mitragynine (MG), the evaluation of its ability to maintain self-administration in animal models of opioid dependence appears to be great significance. Objectives: Here, the ability of MG to cross-substitute to the reinforcing effects of the synthetic narcotic fentanyl is investigated. Methods: Rats with implanted catheters were allowed to self-administer fentanyl (2.0 μg/kg/infusion) on a fixed-ratio 1 of schedule of reinforcement. Results: A significant increase in lever pressing …

Synthesis And Anti-Inflammatory Effects Evaluation Of 1,3 Substituted Isatin Derivatives, Farshid Hassanzadeh, Elham Jafari, Nahal Khayambashi, Valiollah Hajhashemi

The Thai Journal of Pharmaceutical Sciences

Objectives: Inflammation is a pathophysiological response of the body to a variety of agents including infections and physical injury leading to local accumulation of plasma fluid and blood cells. Isatin as a promising heterocyclic molecule has shown interesting biological profile. In this study, some derivatives of isatin containing both Schiff and mannich base fragments were synthesized in a three-step procedure. Methods: Benzohydrazide derivatives were prepared by reaction of benzoat derivatives with hydrazine hydrate. The Schiff bases were formed by treatment isatin with the benzo hydrazide derivatives. The corresponding mannich bases have been synthesized by the reaction of the Schiff bases …

Present Clinical Trial Regulatory System And Strategies For Improvement In Thailand, Charunee Krisanaphan, Rungpetch Sakulbumrungsil

The Thai Journal of Pharmaceutical Sciences

The study aimed to identify gaps and to develop strategies for improving the clinical trial regulatory system in Thailand. Two-step cross-sectional survey was conducted. The first questionnaire addressed the present situation and the expected system sent by mail. The participants were from the lists of ethics committee (EC) members available online and others obtained from Food and Drug Administration (FDA). The second questionnaire determined the strategies and methods to improve the regulatory system. The participants were the attendees at the Thailand Toward Excellence in Clinical Trials meeting. The first questionnaire with response rate of 26.9% showed that the present situation …

In Vitro Antioxidants And Anticancer Activity Of Crude Extract Isolates From Euphorbiaceae In Northern Thailand, Siwalee Rattanapunya, Wiriyaporn Sumsakul, Akharasit Bunsongthae, Samart Jaitia

The Thai Journal of Pharmaceutical Sciences

The properties of Croton persimilis Müll.Arg. and Antidesma puncticulatum Miq.— interesting plant in the family Euphorbiaceae were investigated. The ethanol crude plant extracts were established for phytochemicals screening, antioxidants activities, anticancer in five important human cancer cell lines (MCF-7, MDA-MB-231, HeLa, HepG2, and NCI-H187), and cytotoxic activity in normal cell line (hTERT-HME1). The leaves extracts of C. persimilis Müll. Arg. contained flavonoids, saponins, terpenoids, and tannins. The total phenolic content properties were found in 43.40 ± 1.36 mg Gallic Acid Equivalents (GAE)/g crude extract. They also showed lowest antioxidant activity through 2, 2-diphenyl-1-picrylhydrazyl (DPPH) assay (IC50>1,000 μg/ml) and 2.4.2 …

Incidence Of Pneumocystis Carinii Pneumonia In Treatment-Naïve Hiv-Infected Adult Patients Receiving Primary Pneumocystis Carinii Pneumonia Chemoprophylaxis With 48-Week Antiretroviral Initiation, Piroon Khamlee, Peerawong Werarak, Chankit Puttilerpong

The Thai Journal of Pharmaceutical Sciences

Objective: The objective of the study was to determine the incidence of primary Pneumocystis carinii pneumonia (PCP) between patients who received and did not receive primary PCP chemoprophylaxis and investigate adverse drug reactions (ADRs) related to the chemoprophylaxis use. Method: A retrospective study was conducted in Siriraj Hospital, Thailand. Data were collected from HIV-infected adults, initiated with highly active antiretroviral therapy (HAART) with initial CD4+ <200 cells/mm3. Results: Overall, 217 patients had a median initial CD4+ of 83 cells/mm3 (interquartile range: 33.5–150.5) (range: 0–199), most of the initial HAART regimen was non-nucleoside reverse transcriptase inhibitors based containing tenofovir disoproxil fumarate (94.94%), and 104 patients (47.93%) received chemoprophylaxis. The incidence between patients who received and did not receive prophylaxis found no statistically significant difference (p = 0.133). Only one event was found in a severely immunocompromised patient who did not receive the prophylaxis. The absolute risk reduction of primary PCP incidence, and rate of ADRs was 0.89% (95% confidence interval, −0.84, 2.61) and 10.58% in patients who received the chemoprophylaxis, respectively. Conclusion: The initiation of HAART in HIV-infected patients who had the initial CD4+ cell count <200 cells/mm3 may impact on reducing the risk of developing primary PCP. Aside from the patients who received the prophylaxis, most of the adverse reactions were skin disorders.

Synthesis, Docking, And Molecular Dynamic Study Of Hydrazones Compounds To Search Potential Inhibitor For Breast Cancer Mcf-7, Jasril, Yuana Nurulita, Nur Afriana, Ihsan Ikhtiarudin, Neni Frimayanti

The Thai Journal of Pharmaceutical Sciences

Introduction: Hydrazones have been reported for various biological activities, such as anticancer. The presence of the azomethine group (-NHN=CH-) makes these compounds as one of the important classes in many synthetic products. Objective: The aim of this work is to explore the potential of halogenated hydrazones series as breast cancer inhibitors. Methods: In this study, some series of halogenated hydrazones have been synthesized through condensation reaction between halogenated benzaldehydes and phenylhydrazine under microwave irradiation. The structures of the halogenated hydrazoes were confirmed by ultraviolet, fourier-transform infrared, NMR, and gas chromatography-mass spectrometry spectroscopic data. The in silico studies i.e. docking and …

Comparative Studies On Biochemical And Pharmacological Profiles Of Unfractionated Heparins & Their Depolymerized Derivatives From Bovine, Ovine And Porcine Origins, Ahmed Kouta

Dissertations

Heparin and heparin related drugs have remained the anticoagulant of choice for medical and surgical indications. These drugs are comprised of poly-component sulfated chains of varying length and biophysical structure with direct and indirect pharmacological effects. Heparins produce their therapeutic effects by multiple mechanisms involving both the cellular and humoral targets. These drugs represent natural products which are isolated from mammalian tissue rich in mast cells. Currently used heparin and LMWHs are obtained from porcine mucosal tissue. Other animal sources including bovine and ovine tissues also provide additional sources for the manufacturing of heparins. While there may be microchemical and …

Influence Of 2,5-Dimethoxy-4-Iodoamphetamine (Doi) On Ethanol Preference And Consumption In C57bl/6 Male Mice, Alaina M. Jaster, Sam Gottlieb, Michael Miles, Javier González-Maeso

Graduate Research Posters

Substance use disorders (SUD) account for a large number of mental health diagnosis in the United States and around the world. Approximately 13.6 million adults 26 or older and 5.1 million young adults (ages 18-24) battled with a SUD in 2017. Alcohol Use Disorder (AUD) alone effects nearly 6% of the adult population within the United States. This creates a substantial burden on the individual, with alcohol being the third-leading cause of preventable death in the United States. Few treatments for AUD exist, with no new FDA-approved therapeutic treatments within the last 15 years. Additionally, the limited treatments we do …

Retrospective Review Of Pharmacogenetic Testing At An Academic Children's Hospital., Timothy A. Roberts, Jennifer A. Wagner, Tracy L. Sandritter, Benjamin T. Black, Andrea Gaedigk, Stephani L. Stancil

Manuscripts, Articles, Book Chapters and Other Papers

There is limited evidence to support pharmacogenetic (PGx) testing in children. We conducted a retrospective review of PGx testing among 452 patients at an academic children's hospital to determine the potential utility of PGx in diseases of childhood and to identify targets for future pediatric pharmacogenetic research. An actionable gene-drug pair associated with the 28 genes tested (Clinical Pharmacogenetics Implementation Consortium (CPIC) level A or B, Pharmacogenomics Knowledge Base (PharmGKB) level 1A or B, or US Food and Drug Administration (FDA) recommendation and a PharmGKB level) was present in 98.7% of patients. We identified 203 actionable gene-drug-diagnosis groups based on …

Structural Characterization And In Vitro Antiproliferative Activity Of Non-Specific Lipid Transfer Protein 1 (Nsltp1) From Fennel (Foeniculum Vulgare) Seeds, Mekdes Megeressa

Pharmaceutical Sciences (PhD) Dissertations

Non-specific lipid transfer proteins (nsLTPs) are cationic proteins involved in intracellular lipid shuttling, in growth and reproduction, as well as in defense against pathogenic microbes. Even though the primary and spatial structures of some nsLTPs from different plants indicate their similar features, they exhibit distinct lipid-binding specificities signifying their various biological roles that dictate further structural study. The present study determined the complete amino acid sequence, in silico 3D structure modeling, and in vitro antiproliferative activity of nsLTP1 from fennel (Foeniculum vulgare) seeds.

Fennel is a member of the family Umbelliferae (Apiaceae) native to southern Europe and the …

Amphiphilic Cell-Penetrating Peptides Containing Natural And Unnatural Amino Acids As Drug Delivery Tools And Antimicrobial Agents, David Salehi

Pharmaceutical Sciences (MS) Theses

Cell-penetrating peptides containing arginine as positively charged residues and tryptophan or diphenylalanine as hydrophobic residues were synthesized. The synthesis was accomplished through the Fmoc solid-phase peptide synthesis in the presence of HBTU and DIPEA. The side-chain protected linear peptides were cleaved from the resin and cyclized in the presence of DIC and HOAt in the solution phase overnight. MALDI-TOF mass spectrometry was used to characterize the peptides.

The cytotoxicity of the synthesized peptides was determined in CCRF-CEM (human, lymphoblast peripheral blood), and HEK-293 (human, embryonic epithelial kidney healthy) cells using the MTS assay. A concentration of 10 µM was found …

Melanogenesis, Its Regulatory Process, And Insights On Biomedical, Biotechnological, And Pharmacological Potentials Of Melanin As Antiviral Biochemical, Toluwase Hezekiah Fatoki, Omodele Ibraheem, Catherine Joke Adeseko, Boluwatife Lawrence Afolabi, Daniel Uwaremhevho Momodu, David Morakinyo Sanni, Jesupemi Mercy Enibukun, Ibukun Oladejo Ogunyemi, Akinwunmi Oluwaseun Adeoye, Harriet U. Ugboko, Amoge Chidinma Ogu, Abiodun Samuel Oyedele, Adejoju Omodolapo Adedara, Abiodun Joseph Jimoh, Oluwakemi Ruth Ogundana, Oritsetimeyin Eworitse Ebosa

Chemistry Student Research

Melanin is s most widely distributed pigment and is found in bacteria, fungi, plants, and animals. Melanogenesis is under complex regulatory control by multiple agents interacting through pathways activated by hormonal and receptor-dependent and -independent mechanisms. There are about 20 genes that are involved in the biochemical pathway of melanogenesis and its regulation, which include: tyrosinase, microphthalmia-associated transcription factor, melanocortin1 receptor, adenylate cyclase, protein kinase A. Human melanogenesis regulatory proteins such as MAPK1, CREB3, and CREBP, have binary interaction with the protein of herpesvirus, hepatitis C virus, Human immunodeficiency virus type 1, Simian virus 40, and Human adenovirus A and …

An Artificial Intelligence-Based, Personalized Smartphone App To Improve Childhood Immunization Coverage And Timelines Among Children In Pakistan: Protocol For A Randomized Controlled Trial, Abdul Momin Kazi, Saad Ahmed Qazi, Sadori Khawaja, Nazia Ahsan, Rao Moueed Ahmed, Muhammad Ayub Khan Mughal, Hussain Kalimuddin, Yasir Rauf, Mehreen Raza, Saima Jamal

Department of Paediatrics and Child Health

Background: The immunization uptake rates in Pakistan are much lower than desired. Major reasons include lack of awareness, parental forgetfulness regarding schedules, and misinformation regarding vaccines. In light of the COVID-19 pandemic and distancing measures, routine childhood immunization (RCI) coverage has been adversely affected, as caregivers avoid tertiary care hospitals or primary health centers. Innovative and cost-effective measures must be taken to understand and deal with the issue of low immunization rates. However, only a few smartphone-based interventions have been carried out in low- and middle-income countries (LMICs) to improve RCI.
Objective: The primary objectives of this study are to …

Effect Of Intrauterine Smoke Exposure On Microrna-15a Expression In Human Lung Development And Subsequent Asthma Risk., Sunita Sharma, Alvin T. Kho, Divya Chhabra, Kathleen Haley, Carrie A. Vyhlidal, R Gaedigk, J Steven Leeder, Kelan G. Tantisira, Benjamin Raby, Scott T. Weiss

Manuscripts, Articles, Book Chapters and Other Papers

Background: In utero smoke (IUS) exposure is associated with asthma susceptibility.

Objective: We sought to test the hypothesis that changes in miRNA expression by IUS exposure during human lung development is associated with asthma susceptibility.

Methods: Gene expression was profiled from 53 IUS unexposed and 51 IUS exposed human fetal lung tissues. We tested for the differential expression of miRNAs across post-conception age and by IUS using linear models with covariate adjustment. We tested the IUS-associated miRNAs for association with their gene expression targets using pair-wise inverse correlation. Using our mouse model, we investigated the persistence of the IUS-associated miRNA …

Acknowledgment Of Reviewers, Lily Chiu

Journal of Food and Drug Analysis

No abstract provided.