Pharmaceutics and Drug Design Commons^™

Structure-Activity Profiling Of Alkaloid Natural Product Pharmacophores Against A Schistosoma Serotonin Receptor, Jonathan S. Marchant, Wayne W. Harding, John D. Chan

Publications and Research

Serotonin (5-HT) is an important regulator of numerous aspects of flatworm biology, ranging from neuromuscularfunctionto sexualmaturationandegglaying. Intheparasiticblood flukeSchistosomamansoni,5-HTtargets several G-protein coupled receptors (GPCRs), one of which has been demonstrated to couple to cAMP and regulate parasite movement. This receptor, Sm.5HTRL, has been successfully co-expressed in mammalian cells alongside a luminescent cAMP-biosensor, enabling pharmacological profiling for candidate anti-schistosomal drugs. Here, we have utilized this assay to perform structure-activity investigations of 143 compounds containing previously identified alkaloid natural product pharmacophores (tryptamines, aporphines and protoberberines) shown to regulate Sm.5HTRL. These experiments mapped regions of the tryptamine pharmacophore amenable and intolerant to substitution, highlighting …

Evaluasi Kesesuaian Penulisan Resep Pada Kasus Ispa Non Pneumonia Di Poli Mtbs Puskesmas Kecamatan Cengkareng, Jakarta, Rani Sauriasari, Annisa Azka Hikmawati Aulia, Adisa Swastika

Pharmaceutical Sciences and Research

Acute respiratory infections (ARI) is one of the major health problems in Indonesia. There are three classifications of cases of ARI, consist of pneumonia, severe pneumonia and non pneumonia. This study aimed to find an overview of the use of antibiotics and the evaluation of suitability prescriptions performed in cases of non pneumonia Acute Respiratory Infections (ARI) in IMCI Polyclinic, Cengkareng District Community Health Centre (Puskesmas Cengkareng), West Jakarta. Evaluation for the prescription suitability was useful to find the percentage of the suitability of prescribing on the existing management. This activity was done using retrospective method with data of 100 …

Evaluasi Kesesuaian Dosis Pada Pasien Pediatri Bronkitis Akut Di Rumah Sakit Tentara Kartika Husada Kubu Raya, Variandini Aldhila Kharis, Rise Desnita, Hariyanto Ih

Pharmaceutical Sciences and Research

Selection and usage of rational drugs determine the success of expected therapeutic effect, especially for pediatrics. Acute bronchitis in pediatrics is one of the highest incidents of Acute Respiratory Infection (ARI) in Army Hospital Kartika Husada Kubu Raya. This study aimed to evaluate rationality of drug doses conformity in outpatient pediatric acute bronchitis in Army Hospital Kartika Husada Kubu Raya on 2015. This research was a descriptive observational research with cross-sectional design. The sample was taken with purposive sampling amounted to 36 prescriptions. Then the evaluation of drug doses conformity was counted according to the literature. The results showed that …

Pemodelan Molekul Turunan P-Metoksi Sinnamoil Hidrazida Sebagai Inhibitor Checkpoint Kinase 1 Dan Inhibitor Aromatase Secara In Silico, Galih Satrio Putra, Melanny Ika Sulistyowatya, Juni Ekowati, Tutuk Budiati

Pharmaceutical Sciences and Research

The development of anticancer drugs from ethyl p-methoxycinnamate (EPMC) derivatives has been done to compounds high activity in inducing cancer cells apoptosis and minimal side effects. p-Methoxycinnamoyl hydrazide derivates, modified from EPMC structure, were docked into the ligand-binding pocket of Check point kinase 1 enzymes (2YWP) and the aromatase enzyme (3S7S) using software Molegro Virtual Docker (MVD) Ver.5.5. We compared the Rerank score of native ligand with p-Methoxycinnamoyl hydrazide derivates. Rerank scores of compounds 4b and 4c (-99.98 Kcal/mol and -99.80 Kcal/mol) were lower than the native ligand A42 in inhibiting the enzyme checkpoint kinase 1. Rerank values of p-Methoxycinnamoyl …

L-Citrulline As Alternative Pharmacological Substance In Protecting Against Cardiovascular Disease, Andrea Laurentius, Gregorius Bhaskara Wikanendra, Tzeto Han Cong, Wawaimuli Arozal

Pharmaceutical Sciences and Research

Cardiovascular disease (CVD) has taken up to average 30% of death diagnoses in the world. Prevalent attempts of physicians to treat this disease came down to focus on using drugs with their specific mechanism of action. Since the method only cures the symptoms and need to be pharmacologically monitored, physicians and scientists have been struggling to find other treatment strategies. This problem led us to search for another substance dealing with CVD via preventive therapy, which does not require such close monitoring by physicians in its use. The answer relies on using L-citrulline as potential therapeutics in treating and preventing …

Recombinant Human Proteoglycan-4 Reduces Phagocytosis Of Urate Crystals And Downstream Nuclear Factor Kappa B And Inflammasome Activation And Production Of Cytokines And Chemokines In Human And Murine Macrophages, Marwa Qadri, Gregory D. Jay, Ling X. Zhang, Wendy Wong, Anthony M. Reginato, Changqi Sun, Tannin A. Schmidt

Pharmacy Faculty Articles and Research

Microbial biofilms are organized communities of cells that are associated with a wide spectrum of resistant and chronic infections that lead to the treatment failure. Accordingly, there is an urgent demand to create novel effective therapeutic drugs that can inhibit biofilm formation with new mechanisms of action to surmount the current escalating resistance. In this study, in silico hybrid model was utilized to develop three novel short linear peptides (4, 5, and 6) with potential biofilm inhibiting activities (scores > 1.0). The peptides were composed of cationic and hydrophobic residues. They were synthesized using solid-phase strategy. Synthesized peptides were purified and …

Astromimetics: The Dawn Of A New Era For (Bio)Materials Science?, Vuk Uskoković, Victoria M. Wu

Pharmacy Faculty Articles and Research

Composite, multifunctional fine particles are likely to be at the frontier of materials science in the foreseeable future. Here we present a submicron composite particle that mimics the stratified structure of the Earth by having a zero-valent iron core, a silicate/silicide mantle, and a thin carbonaceous crust resembling the biosphere and its biotic deposits. Particles were formulated in a stable colloidal form and made to interact with various types of healthy and cancer cells in vitro. A selective anticancer activity was observed, promising from the point of view of the intended use of the particles for tumor targeting across the …

Self-Assembling Bioaffinity Hydrogels For Localized Antibody Delivery, Wen Liu

Electronic Theses and Dissertations

The scope of illnesses that are being treated using monoclonal antibodies (mAbs) has been expanding from cancers to autoimmune diseases due to their high specificity to their molecular target. Because many of the new mAbs are aimed to modulate the immune system, an emerging concern is that patients with chronic illnesses are subjected to immune-related Adverse Events (irAEs). Loss of immunological tolerance to self-antigens or increased susceptibility to infections have been documented in some mAb treatments. Localized sustained release of mAb at disease sites might mitigate the risk of such toxicities. Antibody drugs are formulated typically for parenteral delivery because …

Evaluating Feasibility Of Blockchain Application For Dscsa Compliance, Tracie Scott, Armand L. Post, Johnny Quick, Sohail Rafiqi

SMU Data Science Review

Abstract. We evaluated the feasibility of using a blockchain technology to create a traceability solution for pharmaceutical drugs that would promote compliance with recent legislation. Counterfeit and other illegitimate pharmaceutical drugs threaten patient safety, drug efficacy, and patient trust. The purpose of the Drug Supply Chain Security Act (DSCSA) is to greatly reduce distribution of illegitimate drugs by requiring all pharmaceuticals to be serialized and traceable from the manufacturer through the supply chain to the dispenser. A software application to serialize and track pharmaceuticals must overcome numerous obstacles. In particular, the solution must provide a high degree of trust while …

Radical Social Ecology As Deep Pragmatism: A Call To The Abolition Of Systemic Dissonance And The Minimization Of Entropic Chaos, Arielle Brender

Student Theses 2015-Present

This paper aims to shed light on the dissonance caused by the superimposition of Dominant Human Systems on Natural Systems. I highlight the synthetic nature of Dominant Human Systems as egoic and linguistic phenomenon manufactured by a mere portion of the human population, which renders them inherently oppressive unto peoples and landscapes whose wisdom were barred from the design process. In pursuing a radical pragmatic approach to mending the simultaneous oppression and destruction of the human being and the earth, I highlight the necessity of minimizing entropic chaos caused by excess energy expenditure, an essential feature of systems that aim …

Designing A Calibration Set In Spectral Space For Efficient Development Of An Nir Method For Tablet Analysis, Md Anik Alam

Electronic Theses and Dissertations

Designing a calibration set is the first step in developing a spectroscopic calibration method for quantitative analysis of pharmaceutical tablets. This step is critical because successful model development depends on the suitability of the calibration data. For spectroscopic-based methods, traditional concentration based techniques for designing calibration sets are prone to have redundant information while simultaneously lacking necessary information for a successful calibration model. The traditional method also follows the same design approach for different spectroscopic techniques and different formulations, thereby lacks the optimizing capability to be technique and formulation specific.

A method for designing a calibration set in the Near …

Next Generation Of Translational Long-Acting Cabotegravir, Tian Zhou

Theses & Dissertations

Recent development of long-acting antiretroviral therapeutic regimens has opened a new chapter for HIV/AIDS management. Cabotegravir (CAB), as one of the very first long-acting antiretroviral regimens, has drawn tremendous attention. However, the remaining challenges include suboptimal dosing intervals, large injection volume, injection site reactions, lack of tissue penetration, etc. As one of the pioneers in this field, our lab was successful in harnessing mononuclear phagocytes as “Trojan horses” for antiretroviral drug delivery and transportation to viral reservoirs. We proposed this targeted delivery strategy could address the limitations of current CAB formulation. To this end, we developed folic acid decorated CAB …

Novel Determinants That Influence Azole Susceptibility In Candida Glabrata And Candida Albicans, Sarah Garland Whaley

Theses and Dissertations (ETD)

Despite the scientific and medical communities’ best efforts, the incidence of fungal infections in susceptible populations continues to rise. The most common cause of these opportunistic fungal infections is Candida. In fact, Candida is the fourth most common pathogen associated with nosocomial blood stream infections. Reported mortality rates for patients with candidemia vary, but have not decreased in the past fifteen years and are reported to be as high as 50%. Candida glabrata, second only to Candida albicans among Candida infections, expresses high rates of resistance to treatment with arguably the best class of currently available antifungals - …

Rheological Studies Of Injectable Thermoresponsive Biodegradable Hydrogels And Porcine Ocular Tissues, Chandana Reddy Damera

Theses and Dissertations (ETD)

This research has evaluated the rheological properties of two types of materials which include (i) semi-synthetic polymer-based injectable hydrogels [P(NIPAAm-co-DEX-Lactate HEMA) and P(NIPAAm-co-HA-AEMA)], and (ii) biological tissues (porcine ocular tissues).

A series of thermoresponsive and biodegradable in situ hydrogel based on N-isopropyacrylamide (NIPAAm) monomer and hydrolytically degradable oligolactate Dextran-lactate-HEMA or Hyaluronic acid (HA)-AEMA macromer were investigated as encapsulation matrices (scaffolds) for DPSCs/ADSCs and assess their applicability in dental/retinal tissue engineering. The rheological properties of the hydrogels were strongly dependent on the reaction conditions and composition of the hydrogels. Both the hydrogels exhibited linear viscoelasticity, and the values of storage moludus …

Optimasi Aktivitas Bakteriosin Yang Dihasilkan Oleh Bakteri Lactobacillus Plantarum Dari Minuman Ce Hun Tiau, Rafika Sari, Pratiwi Apridamayanti, Melly Octaviani

Pharmaceutical Sciences and Research

Bacteriocin is a protein compound with a small molecular weight that has an antibacterial activity. Bacteriocin has been widely applied as a natural food preservative, as it effectively prevents the growth of pathogenic bacteria in foods and beverages. The aim of this research was to know the activity of bacteriocin produced by lactic acid bacteria Lactobacillus plantarum from Ce hun tiau beverages against Escherichia coli and Staphylococcus aureuswith different pH and temperature treatments. In this study, Lactobacillus plantarum bacteria isolated from Ce hun tiau beverages were characterized by Gram staining test. Bacteriocin was extracted from Lactobacillus plantarum bacteria which had …

Aktivitas Mukolitik Kombinasi Ekstrak Etanol Daun Kemangi Dan Ekstrak Etanol Daun Sirih Merah, Neng Fisheri Kurniati, Deden Winda Suwandi, Safira Yuniati

Pharmaceutical Sciences and Research

A cough is a protective physiological mechanism that is useful for removing and clearing the respiratory tract from sputum and foreign particles that can cause infection. Treatments for cough disorders using medicinal plants were conducted because medicinal plants were widely known to have less side effects than synthetic drugs. Basil leaves (Ocimum sanctum L.) and red betel leaves (Piper crocatum Ruiz and Pav) have been used traditionally to treat a cough. The purpose of this study was to determine the mucolytic activity, and the effective concentration of the combination of basil and red betel leaves ethanol extract. The mucolytic activity …

Peran Tenaga Kefarmasian Dalam Penanggulangan Bencana Role Of Pharmacist In Disaster Management, Meutia Faradilla

Pharmaceutical Sciences and Research

Indonesia is a country that has high potency to be affected by disaster, either by natural or man-made disaster. After the 2004 tsunami, Indonesian government has improved its disaster prevention policy and program. In disaster management study, health management in disaster setting is aimed to assure the implementation of health service toward victims accordingly. As integrated part of the healthcare team in disaster management, pharmacists have to understand the importance of pharmaceutical care in pre-disaster, disaster, and post-disaster phase. This article aims to provide an overview on pharmacists’ role in disaster management from preparing and distributing medicine and medical devices …

Sensitivity Of Escherichia Coli Bacteria Towards Antibiotics In Patient With Diabetic Foot Ulcer, Rafika Sari, Pratiwi Apridamayanti, Indira Diah Puspita

Pharmaceutical Sciences and Research

Chronic complication of diabetes mellitus is diabetic foot ulcers. Diabetic foot ulcer can be defined as an open wound in the feet which will become infected as the result of high blood sugar levels that develops and become place of bacteria. One of the bacteria in diabetic foot ulcer is Escherichia coli. Imprecise use of antibiotics in the treatment of diabetic foot ulcers can cause antibiotic resistance to bacteria. This study aims to determine antibiotic sensitivity of Escherichia coli bacteria in diabetic foot ulcer Wagner grade III and IV. Samples of diabetic foot ulcer swab’s with Wagner grade III and …

Potency Of (Poly) Acrylic/Carboxymethyl Starch-Chitosan Biohydrogel For Curcumin Oral Delivery Matrix, Eka Ruriani, Djumali Mangunwidjaja, Nur Richana, Titi Candra Sunarti

Pharmaceutical Sciences and Research

Biohydrogel has gathered great interest in the pharmaceuticals field. This natural polymers were biodegradable, non-toxic, biocompatible, and its specific ability to response environment change can be considered for the controlled released matric of bioactive compound. In this study, the biohydrogel was synthesized by graft-copolymerization of acrylic acid onto carboxymethyl starch (CMS) and chitosan. The objective of this research was to determine the effect of CMS-chitosan ratio on the biohydrogel characteristic. The acrylic acid was grafted on to the backbone (3:1) using cerric ammonium nitrate as the inisiator.A standarded curcumin was applied to test the binding potency of matrix. A higher …

Evaluasi Rasionalitas Penggunaan Obat Antihipertensi Di Puskesmas Siantan Hilir Kota Pontianak Tahun 2015, Eka Kartika Untari, Alvani Renata Agilina, Ressi Susanti

Pharmaceutical Sciences and Research

Hypertension is widely known as cardiovascular disease. In addition to resulting heart failure, hypertension can result in kidney failure and cerebrovascular disease. This study was aimed to determine the percentage of treatment rationality of hypertensive patient treatment outpatient in Puskesmas Siantan Hilir Pontianak 2015 which includes the appropriate indication, appropriate drug, appropriate patient, and appropriate dose based on the guideline JNC 7. This study was cross-sectional study using medical records of outpatient hypertension patients in 2015. The total of sample analyzed in this research were 92 medical records of hypertension patients from 118 medical records. The percentage of using the …