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Full-Text Articles in Pharmaceutics and Drug Design

Chemical Properties, Biological Activities And Poisoning Treatment Of Novichok: A Review, Tesia Aisyah Rahmania, Bantari Wisynu Kusuma Wardhani, Editha Renesteen, Yahdiana Harahap Aug 2021

Chemical Properties, Biological Activities And Poisoning Treatment Of Novichok: A Review, Tesia Aisyah Rahmania, Bantari Wisynu Kusuma Wardhani, Editha Renesteen, Yahdiana Harahap

Pharmaceutical Sciences and Research

Novichok is an organophosphate compound found as a nerve agent chemical weapon. However, the information about its chemical properties, biological activities, and molecular interactions in the body are still protected under the “top secret” security clearance. Novichok, with the codes A230, A232 and A234, is a compound whose structure has been successfully determined. The compound is synthesized from a precursor through a nucleophilic substitution reaction. Novichok agents are considered more potent than VX gas and can be applied in unitary and binary forms. This compound has ability for the binding with acetylcholinesterase (AChE) due to inability of acetylcholine metabolism. AChE …


The Effect Of Ethanol Extract Of Punica Granatum Linn. Leaves On Lipid Profiles Of Dyslipidemic Rat, Neng Fisheri Kurniati, Afrillia Nuryanti Garmana, Lia Nurul Sakinah Aug 2021

The Effect Of Ethanol Extract Of Punica Granatum Linn. Leaves On Lipid Profiles Of Dyslipidemic Rat, Neng Fisheri Kurniati, Afrillia Nuryanti Garmana, Lia Nurul Sakinah

Pharmaceutical Sciences and Research

It has been reported that peel of Punica granatum has antidyslipidemic activity. The aim of this research was to investigate the antidyslipidemic activity of Punica granatum leaf. The dried Punica granatum leaves were extracted with 96% ethanol. Rats were divided into several groups, which were normal, positive control, simvastatin at a dose of 10 mg/kg bw as reference group, and Punica granatum extract at a dose of 100 mg/kg. Before treatment, male Wistar rats were fed with high cholesterol chow for 3 months, and then plant extract was given for 4 weeks. Blood samples were collected at week 0, 12, …


Development Of A Combined Feedforward-Feedback Quality Control System For Extended-Release Granules Using A Quality By Design Approach, Yuxiang Zhao Aug 2021

Development Of A Combined Feedforward-Feedback Quality Control System For Extended-Release Granules Using A Quality By Design Approach, Yuxiang Zhao

Electronic Theses and Dissertations

Objectives

For a fluid bed film coating process to consistently deliver quality products, its control system needs to be robust against the variability of input materials and environmental disturbances. Presently, limited studies have been reported to understand the effects and interactions of the material attributes, environmental variables, and process parameters on the product in vitro drug dissolution. A control system can be developed with a proper understanding of the coating process, by adjusting the process parameters in feedback and feedforward manners to compensate for the undesired effect caused by disturbances, and ensure consistent product quality.

Methods

The control system was …


Uplc-Ms/Ms Analysis Of The Michaelis-Menten Kinetics Of Cyp3a-Mediated Midazolam 1′- And 4-Hydroxylation In Rat Brain Microsomes, Devaraj Venkatapura Chandrashekar, Barent Dubois, Reza Mehvar Aug 2021

Uplc-Ms/Ms Analysis Of The Michaelis-Menten Kinetics Of Cyp3a-Mediated Midazolam 1′- And 4-Hydroxylation In Rat Brain Microsomes, Devaraj Venkatapura Chandrashekar, Barent Dubois, Reza Mehvar

Pharmacy Faculty Articles and Research

Midazolam (MDZ) is a short-acting benzodiazepine with rapid onset of action, which is metabolized by CYP3A isoenzymes to two hydroxylated metabolites, 1′-hydroxymidazolam and 4-hydroxymidazolam. The drug is also commonly used as a marker of CYP3A activity in the liver microsomes. However, the kinetics of CYP3A-mediated hydroxylation of MDZ in the brain, which contains much lower CYP content than the liver, have not been reported. In this study, UPLC-MS/MS and metabolic incubation methods were developed and validated for simultaneous measurement of low concentrations of both hydroxylated metabolites of MDZ in brain microsomes. Different concentrations of MDZ (1–500 µM) were incubated with …


Design, Synthesis, And Evaluation Of A Novel Cytotoxic Peptide-Doxorubicin Conjugate Targeting Triple-Negative Breast Cancer, Elmira Ziaei Aug 2021

Design, Synthesis, And Evaluation Of A Novel Cytotoxic Peptide-Doxorubicin Conjugate Targeting Triple-Negative Breast Cancer, Elmira Ziaei

Pharmaceutical Sciences (PhD) Dissertations

The aim of this thesis was to design, synthesize, and characterize a novel peptide-doxorubicin conjugate, evaluate in vitro stability and cytotoxicity properties of the conjugate and study its mechanism for uptake into the triple-negative breast cancer (TNBC) cells. For the synthesis of the conjugate, first, doxorubicin (Dox) was conjugated to a highly efficient established cross-linker, MCC, to give an intermediate product, MCC-Dox. MCC-Dox was characterized using NMR spectroscopy, mass spectrometry, and RP-HPLC and purified for subsequent reaction. Second, the 11-mer peptide 18-4 (NH2-CWxEAAYQrFL-CONH2) with high proteolytic stability and specificity for breast cancer cells was reacted with …


Modulation Of Antibacterial Activity And Cytotoxicity In Amphipathic Cyclic Peptide [R4w4] Using Histidine Substitution, Ryan Stueber Aug 2021

Modulation Of Antibacterial Activity And Cytotoxicity In Amphipathic Cyclic Peptide [R4w4] Using Histidine Substitution, Ryan Stueber

Pharmaceutical Sciences (MS) Theses

Antibiotics have been the gold standard frontline defense against bacterial infections for decades. At the same time, these infecting bacteria have continued to evolve to resist developed antibiotics in an almost endless cycle. As such, we aim to take an alternative approach utilizing antimicrobial peptides (AMPs) as a means to end this cycle. [R4W4] is among known AMPs that demonstrated antimicrobial activity against methicillin-resistant staphylococcus aureus (MRSA) with a minimum inhibitory concentration (MIC) of 2.67 μg/mL. This peptide had notably effective antimicrobial activity, especially relative to linear (R4W4). However, it displayed a concerning level of cytotoxicity; eliciting a human embryonic …


Differential Effect Of Proinflammatory Cytokines On Corneal And Conjunctival Epithelial Cell Mucins And Glycocalyx, Kiumars Shamloo, Priya Mistry, Ashley Barbarino, Christopher Ross, Vishal Jhanji Jun 2021

Differential Effect Of Proinflammatory Cytokines On Corneal And Conjunctival Epithelial Cell Mucins And Glycocalyx, Kiumars Shamloo, Priya Mistry, Ashley Barbarino, Christopher Ross, Vishal Jhanji

Pharmacy Faculty Articles and Research

Purpose: Ocular surface mucins and glycocalyx are critical for providing ocular hydration as well lubrication and repelling pathogens or allergens. Elevated levels of tear proinflammatory cytokines in dry eye may have detrimental effect on mucins and glycocalyx. The present study tested the effect of proinflammatory cytokines IL-6, TNF-α, and IFN-γ on membrane-tethered mucins expression, glycocalyx, and viability of ocular surface epithelial cells.

Methods: Stratified cultures of human corneal and conjunctival epithelial cells were exposed to different concentrations of IL-6, TNF-α, and IFN-γ for 24 hours. The mucins gene and protein expressions were quantified by real-time polymerase chain reaction …


Engineering And Characterization Of Human Β-Defensin-3 And Its Analogues And Microcin J25 Peptides Against Mannheimia Haemolytica And Bovine Neutrophils, Harpreet Dhingra, Kamaljit Kaur, Baljit Singh Jun 2021

Engineering And Characterization Of Human Β-Defensin-3 And Its Analogues And Microcin J25 Peptides Against Mannheimia Haemolytica And Bovine Neutrophils, Harpreet Dhingra, Kamaljit Kaur, Baljit Singh

Pharmacy Faculty Articles and Research

Mannheimia haemolytica-induced bovine respiratory disease causes loss of millions of dollars to Canadian cattle industry. Current antimicrobials are proving to be ineffective and leave residues in meat. Antimicrobial peptides (AMPs) may be effective against M. haemolytica while minimizing the risk of drug residues. Cationic AMPs can kill bacteria through interactions with the anionic bacterial membrane. Human β-Defensin 3 (HBD3) and microcin J25 (MccJ25) are AMPs with potent activity against many Gram-negative bacteria. We tested the microbicidal activity of wild-type HBD3, three HBD3 peptide analogues (28 amino acid, 20AA, and 10AA) derived from the sequence of natural HBD3, and MccJ25 …


The Effects Of Dexmedetomidine On Preventing/Decreasing Severity Of Delirium When Given To Surgical Intensive Care Unit Patients: A Systematic Review Of Randomized Control Trials, Lindsey Hettish May 2021

The Effects Of Dexmedetomidine On Preventing/Decreasing Severity Of Delirium When Given To Surgical Intensive Care Unit Patients: A Systematic Review Of Randomized Control Trials, Lindsey Hettish

The Eleanor Mann School of Nursing Undergraduate Honors Theses

The purpose of this systematic review was to integrate research evidence from studies published from 2010 to 2020 on the relationship between administration of dexmedetomidine and severity/prevalence of postprocedural delirium in patients in the surgical intensive care unit. In this review, clinical trial studies were recovered by searching the MEDLINE Complete and PubMed databases and utilizing MeSH terminology search. The MeSH terms utilized to search for applicable articles on PubMed included: “intensive care units” or “critical care” or “critical care nursing”, and “delirium”, “dexmedetomidine”, and “surgical procedures, operative”. On MEDLINE Complete, the search terms utilized were “ICU or intensive care …


Identification Of Adverse Drug Reactions In Congestive Heart Failure Patients In A Tertiary Care Hospital, West Nusa Tenggara, Indonesia, Dita Marina Lupitaningrum, Putri Ramdaniah, Depi Yuliana Apr 2021

Identification Of Adverse Drug Reactions In Congestive Heart Failure Patients In A Tertiary Care Hospital, West Nusa Tenggara, Indonesia, Dita Marina Lupitaningrum, Putri Ramdaniah, Depi Yuliana

Pharmaceutical Sciences and Research

Congestive Heart Failure (CHF) is a progressive health problem with high mortality and morbidity and has the potential to develop adverse drug reactions (ADRs). This study was conducted to determine the prevalence of potential ADRs, the types of drugs that cause ADRs, the types of ADRs, and the risk factors that affect the ADRs in CHF patients. Data were collected using medical record of hospitalized patient at the West Nusa Tenggara (NTB) Provincial Hospital, Indonesia, in 2017 to 2019. The assessment of the causality and severity of ADRs used the Naranjo algorithm and the Hartwig and Siegel scale. This study …


Comprehensive In Silico Analysis Of Christinin Molecular Behaviour From Ziziphus Spina-Christi Leaves On Propionibacterium Acnes, Fitrianti Darusman, Taufik Muhammad Fakih Apr 2021

Comprehensive In Silico Analysis Of Christinin Molecular Behaviour From Ziziphus Spina-Christi Leaves On Propionibacterium Acnes, Fitrianti Darusman, Taufik Muhammad Fakih

Pharmaceutical Sciences and Research

The role of in silico studies in the discovery of new drugs is very important and interesting in the recent years, where the results can be used as confirmation of the results of in vitro tests carried out experimentally in the laboratory. One of the herbal ingredients is Ziziphus spina-christi leaves with effective antibacterial activity, such as for acne-causing bacteria, namely Propionibacterium acnes. This is because it contains main secondary metabolites with saponins as the major components which contain christinin as its active compound. There are four known types of christinin, namely christinin-A, christinin-B, christinin-C, and christinin-D. In this …


A Review: Composition Of Neonatal Meconium Microbiota And Its Role For Potential Probiotic, Devi Oktaviyani, Raden Zulfa 'Alawiyyah, Putri Nusaiba, Amarila Malik Apr 2021

A Review: Composition Of Neonatal Meconium Microbiota And Its Role For Potential Probiotic, Devi Oktaviyani, Raden Zulfa 'Alawiyyah, Putri Nusaiba, Amarila Malik

Pharmaceutical Sciences and Research

Early-life period (≤ 1 month after birth) is critical for determining long- and short-term health of neonates. Composition of neonates’ gut microbiota varies greatly between individuals whose development is influenced by various factors including differences in maternal diet and lifestyle during pregnancy, related to population and ethnicity. Balanced microbial composition can create symbiosis among commensal microbes, immunomodulatory compound production, and subsequent immune response regulation. Unbalanced microbiota composition, characterized by more pathogenic organism, less diversity, and less resistance to disease, is called dysbiosis. Probiotic bacteria are a bacteria group contributing to the balance of neonates’ gut microbiota. Probiotic bacterial strains, such …


Interpersonal Relationship And Its Effect On Treatment Compliance In Patients With Type-2 Diabetes Mellitus, Fransiskus Samuel Renaldi, Woro Riyadina, Muhammad Qamar, Rani Sauriasari Apr 2021

Interpersonal Relationship And Its Effect On Treatment Compliance In Patients With Type-2 Diabetes Mellitus, Fransiskus Samuel Renaldi, Woro Riyadina, Muhammad Qamar, Rani Sauriasari

Pharmaceutical Sciences and Research

Type-2 diabetes mellitus has become a chronic disease that can lead to serious complications and can only be prevented by compliant treatment of the patients. Compliance can be influenced by various factors, one of which is interpersonal factors. This study aimed to identify various interpersonal relationship problems between patients and healthcare workers that can affect their treatment compliance behavior. This study employed a qualitative design with phenomenological methods. This research was conducted in Central Bogor City in March-August 2020. The data were collected by conducting in-depth interviews with 20 type-2 diabetes mellitus patients who had been confirmed by the Community …


Drug Repurposing And Dosage Form Development Of Anti-Covid-19, Kevin Kwok Apr 2021

Drug Repurposing And Dosage Form Development Of Anti-Covid-19, Kevin Kwok

Pharmaceutical Sciences and Research

The COVID-19 pandemic has been occurring approximately for more than 1 year. This pandemic has been a health issue that hits all countries in the world caused by the transmission of SARS-CoV-2 virus from one individual to another. The symptoms showed from the infected are fever, shortness of breath, dry cough, headache, and sore throat, among others. The SARS-CoV-2 virus is transmitted through sneezing, coughing, talking, and touching infected objects. Along with this transmission, the SARS-CoV-2 virus will continue to mutate. This mutation becomes an obstacle as well as a challenge to find drugs that can overcome the SARS-CoV-2 virus …


Preliminary Characterization, Antioxidant And Antiproliferative Properties Of Polysaccharide From Caulerpa Taxifolia, Ariane Marie Bayro, Joanne Katherine Manlusoc, Renaliza Alonte, Catherine Caniel, Patrick Conde, Carlo Embralino Apr 2021

Preliminary Characterization, Antioxidant And Antiproliferative Properties Of Polysaccharide From Caulerpa Taxifolia, Ariane Marie Bayro, Joanne Katherine Manlusoc, Renaliza Alonte, Catherine Caniel, Patrick Conde, Carlo Embralino

Pharmaceutical Sciences and Research

Macroalgae are abundant sources of bioactive polysaccharides and prospective candidates for effective and non-toxic substances. This study aims to preliminary characterize and determine the in vitro antioxidant activity and cancer cell growth inhibitory activity against human lung adenocarcinoma cell (A549) of the polysaccharide from an invasive green alga, Caulerpa taxifolia. Crude polysaccharide (CP) was extracted from the dried algal sample of C. taxifolia by hot water extraction followed by absolute ethanol precipitation. CP was subjected to preliminary chemical characterization, including protein, carbohydrate, and sulfate content analysis by Kjeldahl titrimetry, acid hydrolysis, gravimetry, and ashing-acid water digestion ion chromatography, respectively. …


Suppression Of Human Coronavirus 229e Infection In Lung Fibroblast Cells Via Rna Interference, Hamidreza Montazeri Aliabadi, Jennifer Totonchy, Parvin Mahdipoor, Keykavous Parang, Hasan Uludağ Apr 2021

Suppression Of Human Coronavirus 229e Infection In Lung Fibroblast Cells Via Rna Interference, Hamidreza Montazeri Aliabadi, Jennifer Totonchy, Parvin Mahdipoor, Keykavous Parang, Hasan Uludağ

Pharmacy Faculty Articles and Research

Despite extensive efforts to repurpose approved drugs, discover new small molecules, and develop vaccines, COVID-19 pandemic is still claiming victims around the world. The current arsenal of antiviral compounds did not perform well in the past viral infections (e.g., SARS), which casts a shadow of doubt for use against the new SARS-CoV-2. Vaccines should offer the ultimate protection; however, there is limited information about the longevity of the generated immunity and the protection against possible mutations. This study uses Human Coronavirus 229E as a model coronavirus to test the hypothesis that effective delivery of virus-specific siRNAs to infected cells will …


Drug-Drug Interactions In Subjects Enrolled In Swog Trials Of Oral Chemotherapy, Lauren A. Marcath, Colin M. Finley, Siu Fun Wong, Daniel L. Hertz Mar 2021

Drug-Drug Interactions In Subjects Enrolled In Swog Trials Of Oral Chemotherapy, Lauren A. Marcath, Colin M. Finley, Siu Fun Wong, Daniel L. Hertz

Pharmacy Faculty Articles and Research

Background

Patients with cancer are at increased risk of drug-drug interactions (DDI), which can increase treatment toxicity or decrease efficacy. It is especially important to thoroughly screen DDI in oncology clinical trial subjects to ensure trial subject safety and data accuracy. This study determined the prevalence of potential DDI involving oral anti-cancer trial agents in subjects enrolled in two SWOG clinical trials.

Methods

Completed SWOG clinical trials of commercially available agents with possible DDI that had complete concomitant medication information available at enrollment were included. Screening for DDI was conducted through three methods: protocol-guided screening, Lexicomp® screening, and pharmacist determination …


Label‑Free Spectral Imaging To Study Drug Distribution And Metabolism In Single Living Cells, Qamar Alshammari, Rajasekharreddy Pala, Nir Katzir, Surya M. Nauli Feb 2021

Label‑Free Spectral Imaging To Study Drug Distribution And Metabolism In Single Living Cells, Qamar Alshammari, Rajasekharreddy Pala, Nir Katzir, Surya M. Nauli

Pharmacy Faculty Articles and Research

During drug development, evaluation of drug and its metabolite is an essential process to understand drug activity, stability, toxicity and distribution. Liquid chromatography (LC) coupled with mass spectrometry (MS) has become the standard analytical tool for screening and identifying drug metabolites. Unlike LC/MS approach requiring liquifying the biological samples, we showed that spectral imaging (or spectral microscopy) could provide high-resolution images of doxorubicin (dox) and its metabolite doxorubicinol (dox’ol) in single living cells. Using this new method, we performed measurements without destroying the biological samples. We calculated the rate constant of dox translocating from extracellular moiety into the cell and …


[(Wr)8Wkβa]-Doxorubicin Conjugate: A Delivery System To Overcome Multi-Drug Resistance Against Doxorubicin, Khalid Zoghebi, Hamidreza Montazeri Aliabadi, Rakesh Kumar Tiwari, Keykavous Parang Jan 2021

[(Wr)8Wkβa]-Doxorubicin Conjugate: A Delivery System To Overcome Multi-Drug Resistance Against Doxorubicin, Khalid Zoghebi, Hamidreza Montazeri Aliabadi, Rakesh Kumar Tiwari, Keykavous Parang

Pharmacy Faculty Articles and Research

Doxorubicin (Dox) is an anthracycline chemotherapeutic agent used to treat breast, leukemia, and lymphoma malignancies. However, cardiotoxicity and inherent acquired resistance are major drawbacks, limiting its clinical application. We have previously shown that cyclic peptide [WR]9 containing alternate tryptophan (W) and arginine (R) residues acts as an efficient molecular transporter. An amphiphilic cyclic peptide containing a lysine (K) residue and alternative W and R was conjugated through a free side chain amino group with Dox via a glutarate linker to afford [(WR)8WKβA]-Dox conjugate. Antiproliferative assays were performed in different cancer cell lines using the conjugate and the …


Amphiphilic Cell-Penetrating Peptides Containing Natural And Unnatural Amino Acids As Drug Delivery Tools And Antimicrobial Agents, David Salehi Jan 2021

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 …


Continuous Manufacturing Of Pharmaceuticals Using Novel Platforms, Sarah S. Aboelela Jan 2021

Continuous Manufacturing Of Pharmaceuticals Using Novel Platforms, Sarah S. Aboelela

Theses and Dissertations

Pharmaceuticals have been synonymously manufactured in a centralized, batch mode with less attention to process and formulation understanding. However, due to rising drug costs, shortages, and robustness issues, in addition to the alarming lack of flexibility and agility, regulatory agencies have pushed towards switching to continuous processes. They believed in continuous manufacturing, providing cleaner, flexible, and more efficient processes. Hence, it was foreseen to reduce development and manufacturing costs, time, and environmental impact and ensured drug product quality. Over the last two decades, continuous manufacturing quality, environmental, and economic advantages have been evident through many case studies and approved products …


Potential Of Jamu In Nanotechnology Perspective As An Alternative Treatment For Covid-19, Dhadhang Wahyu Kurniawan, Azis Ikhsanudin Dec 2020

Potential Of Jamu In Nanotechnology Perspective As An Alternative Treatment For Covid-19, Dhadhang Wahyu Kurniawan, Azis Ikhsanudin

Pharmaceutical Sciences and Research

The world seems to be recovering at this time, especially because of the 2019 global coronavirus disease pandemic (COVID-19) caused by the Coronavirus 2 virus (SARS-CoV-2). This virus is similar to other β-coronaviruses through several steps to enter and bind angiotensin-converting enzyme 2 (ACE2) as the main receptor. This binding, particularly in the respiratory epithelium and alveoli of the lungs, affects harmony in human host cells. No specific vaccines and antivirals are available to date as drug investigations are still ongoing. However, many Indonesians consume herbal medicine, especially 'empon-empon' containing the Zingiberaceae family, to protect their health from COVID-19. So …


Antioxidant And Antiaging Assays Of Ageratum Conyzoides (L.) Ethanolic Extract, Afifah B. Sutjiatmo, Novi Edriayani, Tira Endang Mulyasari, Faizal Hermanto, M. Fahrauk, Elin Y. Sukandar, Hanna Sari Widya Kusuma, Rizal Rizal, Wahyu Widowati Dec 2020

Antioxidant And Antiaging Assays Of Ageratum Conyzoides (L.) Ethanolic Extract, Afifah B. Sutjiatmo, Novi Edriayani, Tira Endang Mulyasari, Faizal Hermanto, M. Fahrauk, Elin Y. Sukandar, Hanna Sari Widya Kusuma, Rizal Rizal, Wahyu Widowati

Pharmaceutical Sciences and Research

The declining ability of tissues to repair or replace themselves and maintain their structure and normal function is called aging. Aging is caused by free radical that can induce the activation of elastase and collagenase. Ageratum conyzoides (L.) or known as Babadotan is a medicinal plant that has been reported to be a good source of antioxidants that also inhibit aging process. The purpose of this research is to evaluate the antioxidant and antiaging properties of Babadotan Ethanolic Extract (BEE). Franswoth method was used to determine the phytochemical assay of BEE. Measurement of 2,2-diphenyl 1-picrylhydrazyl (DPPH) scavenger was used for …


Evaluation Of Antipsychotic Activity Of Ethanolic Bark Extract Of Myrica Esculenta In Rats, Biswash Sapkota, Ankit Acharya, Bishal Dangi, Annegowda Hv Dec 2020

Evaluation Of Antipsychotic Activity Of Ethanolic Bark Extract Of Myrica Esculenta In Rats, Biswash Sapkota, Ankit Acharya, Bishal Dangi, Annegowda Hv

Pharmaceutical Sciences and Research

The antipsychotic properties of Myrica esculenta stem bark were evaluated. The stem bark was collected, shade dried, and pulverized. Extraction was carried out with 70% ethanol by occasional shaking. Preliminary phytochemical screening of the extract was investigated in this study. Antipsychotic activity was evaluated against apomorphine-induced stereotypy using cook’s pole climbing apparatus and haloperidol-induced catalepsy models. Bioamine determination of noradrenaline and dopamine was also performed. The extract contains phytochemicals, including glycosides, flavonoids, volatile oils, proteins, saponins, phenolics, and tannins. The result showed decreased apomorphine-induced stereotyped behavior. This study reported significant dose-dependent potentiation of haloperidol-induced catalepsy in rats and a longer …


The Anti-Proliferation Effect Of An Isolated Butanol Fraction Of Tampa Badak (Voacanga Foetida (Bl.) K. Schum) Leaves On Leukemia, Lung, And Cervical Cancer, Adriani Susanty, Dachriyanus Dachriyanus, Yanwirasti Yanwirasti, Fatma Sri Wahyuni, Andisyah Putri Sekar, Nur Alimin, Magdazaleni Magdazaleni, Sri Esky Sofia, Citra Kartika Dewi Dec 2020

The Anti-Proliferation Effect Of An Isolated Butanol Fraction Of Tampa Badak (Voacanga Foetida (Bl.) K. Schum) Leaves On Leukemia, Lung, And Cervical Cancer, Adriani Susanty, Dachriyanus Dachriyanus, Yanwirasti Yanwirasti, Fatma Sri Wahyuni, Andisyah Putri Sekar, Nur Alimin, Magdazaleni Magdazaleni, Sri Esky Sofia, Citra Kartika Dewi

Pharmaceutical Sciences and Research

Voacanga foetida (Bl.) K.Schum leaves are known to have cytotoxic activity against blood cancer cells. This study was aimed to determine the potential of an isolated butanol fraction of Voacanga foetida (Bl.) K.Schum leaves (Tb3 compound) in inhibiting the proliferation of several cancer cells, including leukemia (K562), lung cancer (A549), and cervical cancer (He-La) using the dye exclusion method. We found that the percentage of anti-proliferation of the Tb3 compound was increased in a dose-dependent manner, where it showed 83% (K562), 72.3% (He-La), and 70.7% (A549) inhibition at higher concentration. These values were relatively higher compared to doxorubicin as a …


Inhibitory And Anti-Biofilm Effects Of Orthoshipon Aristatus Against Candida Albicans, Ratika Rahmasari, Ananda Hanny Chairunissa, Marina Ika Irianti, Roshamur Cahyan Forestrania, Ayun Erwina Arifianti, Herman Suryadi, Juliann Nzembi Makau, Ibrahim Jantan, Berna Elya Dec 2020

Inhibitory And Anti-Biofilm Effects Of Orthoshipon Aristatus Against Candida Albicans, Ratika Rahmasari, Ananda Hanny Chairunissa, Marina Ika Irianti, Roshamur Cahyan Forestrania, Ayun Erwina Arifianti, Herman Suryadi, Juliann Nzembi Makau, Ibrahim Jantan, Berna Elya

Pharmaceutical Sciences and Research

There are increasing number of reports on Candida albicans developing resistance to available anti-fungal drugs. Thus, there is an urgent need to discover new agents for treatment of candidiasis. The alcoholic extracts of Orthoshipon aristatus have been shown to exhibit antifungal activity against C. albicans by using the agar diffusion and broth microdilution methods. However, the underlying mechanisms of anti-C. albicans effect of O. aristatus have not been well understood. This study was aimed to evaluate the cytotoxic and anti-biofilm effects of the n-hexane and ethanol extracts of purple and white varieties of O. aristatus leaves …


Fractionation Of Citronella Oil And Identification Of Compounds By Gas Chromatography-Mass Spectrometry, Yelfi Anwar, Victor S. Siringoringo Dec 2020

Fractionation Of Citronella Oil And Identification Of Compounds By Gas Chromatography-Mass Spectrometry, Yelfi Anwar, Victor S. Siringoringo

Pharmaceutical Sciences and Research

Citronella oil is one of the most important essential oils and is widely used in the pharmaceutical, cosmetic and food industries. However, the selling price of citronella oil is still low, so efforts are needed to increase its added value by isolating the active components such as citronellal, citronellol and geraniol. This study aims to isolate the active ingredients of citronella oil that have higher economic added value. Citronella oil was obtained by the process of distillation of Cymbopogon nardus (L.) Rendle leaves. The essential oil was then fractionated by a vacuum fractionation process. The essential oil fraction was identified …


Antifungal Activity Of Polyscias Scutellaria Fosberg Leaves Against Candida Albicans, Nada Marcha Putri, Jasmine Regita Putri, Berna Elya, Robiatul Adawiyah Dec 2020

Antifungal Activity Of Polyscias Scutellaria Fosberg Leaves Against Candida Albicans, Nada Marcha Putri, Jasmine Regita Putri, Berna Elya, Robiatul Adawiyah

Pharmaceutical Sciences and Research

Polyscias scutellaria Fosberg is one of the indigenous plants from Indonesia that widely used as folk medicines for several illnesses. The leaves of P. scutellaria were previously studied as an antimicrobial agent. Nonetheless, this theory of antifungal activity has never been scientifically verified. This study aimed to evaluate the antifungal activity of P. scutellaria against Candida albicans. The leaves of P. scutellaria were macerated using an ethanol solvent. Then, the extract was evaporated and dissolved by 1% DMSO into different concentrations (100 μg/mL, 200 μg/mL, 400 μg/mL, 800 μg/mL, 1600 μg/mL, 3200 μg/mL, and 6400 μg/mL). Fluconazole, as a …


Pharmacological Characterization Of Novel Serotonin Transporter Inhibitors Identified Through Computational Structure-Based Virtual Screening, Michael Wasko Dec 2020

Pharmacological Characterization Of Novel Serotonin Transporter Inhibitors Identified Through Computational Structure-Based Virtual Screening, Michael Wasko

Electronic Theses and Dissertations

Depression is a mental health disorder affecting greater than 350 million people worldwide with roughly 7% of the United States population diagnosed as of 2017. The selective serotonin reuptake inhibitors (SSRIs) have been the mainstay of pharmacotherapies for depression for the last 40 years. The SSRIs target the serotonin transporter (SERT), a monoamine transporter (MAT) responsible for terminating serotonergic neurotransmission. The SSRIs are not perfect therapeutics and suffer from delayed response times, inconsistent efficacy among patients, and often produce intolerable side effects. Therefore, a strong need exists to develop new antidepressants that are more efficacious and have fewer adverse effects. …


Anti-Muc4Β Antibodies As A Novel Therapeutic Modality For The Treatment Of Pancreatic Cancer, Catherine Orzechowski Dec 2020

Anti-Muc4Β Antibodies As A Novel Therapeutic Modality For The Treatment Of Pancreatic Cancer, Catherine Orzechowski

Theses & Dissertations

The deregulation of cell surface glycoproteins, such as mucins, is a hallmark of many tumors of epithelial origin. The transmembrane mucin MUC4, is differentially overexpressed in several malignancies, including pancreatic, breast, ovarian, lung, cervical, and head and neck cancers. Of all the aforementioned cancers, the role of MUC4 has been the most thoroughly in pancreatic cancer (PC), which is the 4th leading cause of cancer-related deaths in the United States. While MUC4 is undetectable in the normal or inflamed pancreas (pancreatitis), its expression progressively increases during PC progression and its higher expression correlates with poor survival. The role of MUC4 …