Pharmaceutics and Drug Design Commons^™

Inhibition Of The Thioesterase Activity Of Human Fatty Acid Synthase By 1,4- And 9,10-Diones, Herman H. Odens

Faculty Works

Fatty acid synthase (FASN) is the enzyme that synthesizes fatty acids de novo in human cells. Although FASN is generally expressed at low levels in most normal tissues, its expression is highly upregulated in many cancers. Consistent with this notion, inhibition of FASN activity has demonstrated potential to halt proliferation and induce cell death in vitro and to block tumor growth in vivo. Consequently, FASN is widely recognized as a valuable therapeutic target. In this report, we describe a variety of 1,4-quinones and 9,10- anthraquinones, including several natural compounds and some newly synthesized compounds, that potently inhibit the thioesterase (TE) …

Potensi Pemanfaatan Nigella Sativa L. Sebagaiimunomodulator Dan Antiinflamasi, Farida Sulistiawati, Maksum Radji

Pharmaceutical Sciences and Research

Nigella sativa L. has long been used as an herbal medicine in some countries, particularly in the Middle East and in other Asian countries, including in Indonesia. One component is a protein compound extracted from black cumin oil residues, known to have efficacy to enhance the immune system and as an anti-inflammatory. As the compound will be degraded when administered orally, the research on its delivery systems, is interesting to be developed. This article will review about the prospects of their utilization and strategy formulation that preparation can be delivered orally.

Efek Ekstrak Etanol Daun Premna Cordifolia Terhadap Malondialdehida Tikus Yang Dipapar Asap Rokok, Asri Adyttia, Eka Kartika Untari, Sri Wahdaningsih

Pharmaceutical Sciences and Research

Free radical from cigarrete smoke cause lipid peroxidation that could be identified by increasing levels of Malondialdehida (MDA). Premna cordifolia leaves known having antioxidant activity in in vitro study. This study aimed to know the effect of P. cordifolia leaves extract on the levels of MDA after exposure to cigarette smoke. The simplicia extracted by maseration using 70% ethanol. Twenty four male wistar rats were divided into six groups, i.e. : control normal, negative control, positive control received cigarette smoke exposure and vitamin E (18mg/kg BW) and three groups received cigarette smoke exposure and P. cordifolia leaves extract with doses …

Uji Aktivitas Antioksidan Ekstrak Metanol Bunga Dan Daun Patikala (Etlingera Elatior (Jack) R.M.Sm) Menggunakan Metode Dpph, Virsa Handayani, Aktsar Roskiana Ahmad, Miswati Sudir

Pharmaceutical Sciences and Research

Patikala (Etlingera elatior (Jack) R.M.Sm) is a plant of the Zingiberaceae family. Patikala (E. elatior (Jack) R.M.Sm) have bioactive compounds are flavonoids that act as antioxidants. The purpose of this study was to measure free radical activity in the methanol extract of the fruit and leaves Patikala (E. elatior (Jack) R.M.Sm). Extraction of flowers and leaf samples by maceration method using methanol. Qualitative analysis of chemical compounds with certain eluent using Thin Layer Chromatography (TLC) to determine the group of active compounds in the extract. Antioxidant activity assay using the immersion method of DPPH (1,1-Diphenyl-2-picryl Hidrazil) measured absorption at a …

Aktivitas Penghentian Pendarahan Luar Ekstrak Etanol Daun Berenuk (Crescentia Cujete L) Secara In-Vivo, Anjar Mahardian Kusuma, Adri Nurrakhmat Sulistyo, Susanti Susanti, Sabikis Sabikis

Pharmaceutical Sciences and Research

Crescenti cujete L. or better known as calabash is a plant that thrives in Indonesia. Calabash has a great potential as an herbal remedy, but there is only some scientific research conducted on this plant, one of which is antibacterial against Bacillus subtilis and Escerichia coli on 2006 by Susanti. The method in this research was an experimental activities of the cessation external bleeding with 3 dose variation of calabash leaf extract 80%, 60%, and 40% by counting the bleeding time at base of the tail in mice. As a result, all groups of external bleeding cessation activities have better …

Uji Efek Antiinflamasi Fraksi Air Daun Mahkota Dewa (Phaleria Macrocarpa (Shecff.) Boerl.) Terhadap Tikus Putih (Rattus Norvegicus L.), Aprilita Rina Yanti Eff, Ema Dewanti, Melisha Adelina H

Pharmaceutical Sciences and Research

Inflammation occurs as the attempt of body to inactivate organisms that attack the body, removing irritants and regulate tissue repair. One of the medicinal plants used empirically as antiinflammation is the leaf of Mahkota Dewa (Phaleria macrocarpa (Schecff.) Boerl). This study investigated the effect of anti-inflammatory water fraction of leaf Mahkota Dewa using oedema induction method with caragenin in rat. Water fraction of Mahkota Dewa was given at the dose 0.5 g/kg BW ,1 g/kg BW and 2 g/kg BW. Sodium diclofenac was used as a positive control and CMC as negative control. The result showed water fractions of three …

Tablet Effervescent Ekstrak Belimbing Wuluh (Averrhoa Bilimbi L.) Dengan Variasi Kadar Pemanis Aspartam, Rosmala Dewi, Iskandarsyah Iskandarsyah, Devi Octarina

Pharmaceutical Sciences and Research

Averrhoa bilimbi is fruit that has many benefits but the usage is not optimal. That is why the aim of the research is to get formulation of effervescent granule and tablet containing dry Averrhoa bilimbi extract with modified concentration of aspartame as sweetening agent for commercial healthy drink. Granules and tablets were produced with dry method granulation with 40% of relative humidity (RH) and 25ºC of temperature. The three of formulation were qualified as effervescent granules and tablets. Favorite tests showed that no significant differences of appearances, tastes for three of effervescent granules and tablets.

Effect Of Twin Screw Granulator Process Parameters On Granule Attributes, Haosheng Xu, Ridade Sayin, James Litster

The Summer Undergraduate Research Fellowship (SURF) Symposium

Twin screw wet granulation has been considered as an efficient and effective technique of manufacturing granules (agglomerates made up of small particles) and has been widely applied in pharmaceutical industry. However, narrow granule size distributions are difficult to achieve. This study aims to elucidate the effect of process parameters such as liquid feed rate and screw configuration on the granule attributes through granule characterization. The methods used are sieve analysis (for size distribution), liquid distribution (determining the dye concentration in the granules) and density and porosity (percentage gas volume in the granule) analyses. A sieve shaker is used to divide …

Electrochemical Investigations Of Benzanthrone, Antonio Trevino, Kefa Karimu Onchoke

Undergraduate Research Conference

No abstract provided.

In Vitro Metabolic Stability Study Of New Cyclen Based Antimalarial Drug Leads Using Rp-Hplc And Lc-Ms/Ms, Apoorva V. Rudraraju, Mohammad F. Hossain, Anjuli Shrestha, Prince N.A. Amoyaw, Babu L. Tekwani, M. O. Faruk Khan

Pharmaceutical Science and Research

Metabolic stability of the new antimalarial drug leads is determined using Human Liver Microsome (HLM) and specific cytochrome P450 enzyme (CYP2C8) taking the clinically used antimalarial drug chloroquine as a positive control. Experiment is done using standard methods. All the assays were conducted in 0.5 M phosphate buffer at pH 7.4. In general the metabolic reaction was initiated by adding 1 mM NADPH and 0.5 mg of enzyme. Incubations were done with time frequency of 0 hr, 1 hr, and 2 hrs at 37°C and the reactions were terminated by adding acetonitrile in the equal amounts of the assay mixture …

Hydrodynamic Cfd Modeling Of A Pharmaceutical Reactor Vessel Provided With A Retreat-Blade Impeller Under Different Baffling Conditions, Christopher G. Foehner

Theses

In the pharmaceutical industry, glass-lined reactors and vessels are often utilized to carry out a variety of different unit operations. Within these systems, both the vessel and impellers are typically glass-lined in order to provide superior corrosion resistance, prevent product contamination, and enhance cleanability. This approach, in turn, often requires the use of different, and sometimes sub-optimal, baffling conditions, which affect the hydrodynamics of the vessels and the reactor performance.

Computational Fluid Dynamics (CFD) is a computational tool that employs numerical methods and algorithms to discretize and numerically solve partial differential equations (PDEs) representing mass, energy, and momentum conservation equations …

Assessment Of A Marine Polysaccharide For Use As Excipient In Pharmaceutical Hot-Melt Extrusion, Qing Ye

Theses

Pharmaceutical Hot Melt Extrusion (HME) is currently investigated by both industry and academia as a method for manufacturing solid oral dosages with improved bioavailability of poorly-water soluble active pharmaceutical ingredients (APIs) and control drug release of water-soluble APIs. Although HME is traditionally utilizing synthetic polymers to produce such dosages, biopolymers constantly gain ground by virtue of renewability, biocompatibility and in some cases biodegradability. In this work, the possibility of using Keltone, a marine polysaccharide derived from brown seaweed, as a polymeric excipient for pharmaceutical HME is explored. Keltone is insoluble in acidic pH and soluble in basic pH, therefore making …

Dispersion And Dissolution Kinetics Of Api Particles In Pharmaceutical Hot Melt Extrusion, Wang Zhan

Theses

Pharmaceutical Hot Melt Extrusion (HME) is essentially a special case of polymer compounding. The elementary steps involved in traditional plastics melt processing are handling of particulates, melting, dispersive and distributive mixing, devolatilization and stripping, and finally pressurization and pumping. However, for pharmaceutical HME, the dissolution of the API (Active Pharmaceutical Ingredient) is an additional and very important elementary step, along with the melting of the polymeric excipient that precedes it, and mixing which accelerates the dissolution process. A major concern in pharmaceutical HME is the thermal degradation of the API. To avoid overexposure of API to heat while ensuring complete …

Experimental Determination Of The Mixing Requirements For Solid Suspension In Pharmaceutical Stirred Tank Reactors, Anqi Zhou

Theses

Glass and glass-lined, stirred-tank reactors are of significant importance in the pharmaceutical and related industries. Because of fabrication issues, a retreat blade impeller (RBI) with a low impeller clearance off the tank bottom is commonly used in glass-lined reactors, typically combined with a single baffle (providing only partial baffling conditions) mounted from the top of the reactor. In addition, these reactors are often provided with a torispherical bottom. Other configurations are also used, including full baffling or no baffles at all, hemispherical bottoms, and different impeller types. Despite their common use, some of the most important mixing characteristics of this …

Design, Synthesis And Biological Evaluation Of Novel Compounds With Cns-Activity Targeting Cannabinoid And Biogenic Amine Receptors, Alexander M. Sherwood

LSU New Orleans Theses and Dissertations

This work seeks to contribute to the discipline of neuropharmacology by way of structure activity relationship from the standpoint of an organic chemist. More specifically, we sought to develop robust synthetic methodology able to efficiently produce an array of compounds for the purpose of systematic evaluation of their interaction with specific sights within the central nervous system (CNS) in order to better understand the mind and to develop drugs that may have beneficial effects on neurological function.

The focus of these studies has been toward the development of novel molecules, using a structure-activity relationship approach, that exhibit binding affinity at …

Nanotoxicity In Cells Of The Immune System, Jonathan J. Pelc

Science Scholars

Nanoparticles (NPs) provide a new medical approach to drug therapy. As with every new approach, safety precautions need to be taken, and the immediate and long-term effects for many NPs are still unclear. When administering a medical treatment into the human body, the first issue that needs to be addressed is host detection of the medicine and inflammation as a possible result of the treatment. If a new NP treatment causes inflammation before it releases its medicine, that treatment may be ineffective, even damaging to the patient. Small metallic and organic particles have been shown to elicit an inflammatory responses …

Development Of A Novel Vaccine Adjuvant System Utilizing An In Situ Implant System To Modified Release, Qiuye Zhang

Theses and Dissertations (ETD)

Pulsatile release formulations for single dose vaccines have been studied for many years because of the advantages that they may provide to vaccine administration with a single dose instead of prime and booster shots.

The aim of this work is to develop novel formulations based on an In Situ Implant (ISI) systems to provide a modified vaccine release and altered immune response, which could act as a booster administration. This type of system was selected because ISI systems are used for long acting administration of various drugs and ease of administration. A typical ISI system is comprised of hydrophilic organic …

Glioma: A Tale Of Corticosteroids, Thiopurines And Proposed Novel Antiglioma Small Molecules, Amira Ahmed

Theses and Dissertations (ETD)

Glioma is a brain tumor that arises from glial cells or glial progenitor cells, and represents 80% of malignant brain tumor incidence in the United States. Glioblastoma multiforme (GBM) is the most aggressive primary brain tumor malignancy with fewer than 8% of patients with GBM surviving for 3 years. Over the past 10 years, despite improvement in diagnosis and therapies for cancer, the survival rate for high-grade glioma patients remains unchanged. The main focus of this dissertation is to investigate two therapeutic agents that are related to increase tumor resistance or increase secondary tumor incidence, which might play a role …

Uji Aktivitas Antibakteri 1-[(Kuinazolin-4-On-2-Il)Metil]Piridin-1-Ium Bromida Dan 2-Bromometilkuinazolin-4-On, Hayun Hayun, Arif Arrahman, Herman Suryadi, Arry Yanuar

Pharmaceutical Sciences and Research

Antibacterial activity tests of quinazolin-4-one derivates: 1-[(6-nitroquinazolin-4one-2-yl)methyl]piridin-1-ium bromide (1), 1-[(6-aminoquinazolin-4-on-2-yl)methyl] piridin-1-um bromide (2), 2-bromomethylquinazolin-4-one (3) and 2-bromomethyl-6nitroquinazolin-4-one(4) with trimethoprim (5) as a positive standard were conducted. The antibacterial activity tests were carried out using disc diffusion method againts E.coli, S.aureus and S.thyposa, and determination of minimum inhibitory concentration (MIC). The results showed that compounds 1 and 2 are inactive as antibacterial, whereas compounds 3 and 4 are active.The activities to E.coli were ¼ times the activity of trimethoprim (MIC : 5 x 102 µg/ml compared to 1.25 x 102 µg/ml ). The activity to S. typhosa were ½-1 times the …

Respon Bioakumulator Eceng Gondok (Eichhornia Crassipes) Terhadap Logam Berat Pb Dan Cd Di Sungai Pegangsaan Dua, Sri Teguh Rahayu, Meutia Faradilla, Ester Yani Verawati, Muchrip Triana

Pharmaceutical Sciences and Research

Eichhornia crassipes is one of Indonesia’s wild plant that considered as weed. Its presence can disrupt ecosystems in the river. However, it is proven to absorb Pb and Fe. It is also believed that E.crassipes can absorb other metals such as Hg , Zn , Cu and Cd which were belong to the same group as Pb and Fe. In addition to heavy metal sequestration, Eichhornia crassipes can also absorb pesticide residues. This descriptive research was done to determine the bioaccumulator response to Pb and Cd in Pegangsaan Dua river using Inductively Coupled Plasma method. Bioaccumulator response of Eichhornia crassipes …