Pharmacology, Toxicology and Environmental Health Commons^™

Synthesis, Biochemical And Molecular Modelling Studies Of Antiproliferative Azetidinones Causing Microtubule Disruption And Mitotic Catastrophe, Niamh O'Boyle, Miriam Carr, Lisa M. Greene, Niall O. Keely, Andrew Js Knox, Thomas Mccabe, David G. Lloyd, Daniela M. Zisterer, Mary J. Meegan

Articles

The structure-activity relationships of antiproliferative β-lactams, focusing on modifications at the 4-position of the β-lactam ring, is described. Synthesis of this series of compounds was achieved utilizing the Staudinger and Reformatsky reactions. The antiproliferative activity was assessed in MCF-7 cells, where the 4-(4-ethoxy)phenyl substituted compound 26 displayed the most potent activity with an IC₅₀ value of 0.22 μM. The mechanism of action was demonstrated to be by inhibition of tubulin. Cell exposure to combretastatin A-4 and 26 led to arrest of MCF-7 cells in the G2/M phase of the cell cycle and induction of apoptosis. Additionally, mitotic catastrophe for …

Lead Identification Of Β-Lactam And Related Imine Inhibitors Of The Molecular Caperone Heat Shock Protein 90, Niamh O'Boyle, Andrew Js Knox, Trevor P. Price, D. Clive Williams, Daniela M. Zisterer, David G. Lloyd, Mary J. Meegan

Articles

Heat shock protein 90 is an emerging target for oncology therapeutics. Inhibitors of this molecular chaperone, which is responsible for the maintenance of a number of oncogenic proteins, have shown promise in clinical trials and represent a new and exciting area in the treatment of cancer. Heat shock protein 90 inhibitors have huge structural diversity, and here we present the identification of inhibitors based on β-lactam and imine templates. β-Lactam 5 and imines 12 and 18 exhibit binding to heat shock protein 90-α with IC₅₀ values of 5.6 μM, 14.5 μM and 22.1 μM respectively. The binding affinity displayed …

Synthesis And Cytotoxicity Study Of Magnetoliposomes Loaded Doxorubicin, Surachai Ngamratanapaiboon, Issara Sramala, Wichet Leelamanit

The Thai Journal of Pharmaceutical Sciences

The limitation of clinical use of doxorubicin is its side effects especially a cumulative dose-dependent cardiotoxicity. To overcome this, doxorubicin can be targeted to accumulate on the site of action and limit dispersion in healthy tissue. Magnetic li...

Effects Of Marmin Isolated From Aegle Marmelos Correa On L-Histidine Decarboxylase Enzyme In Rbl-2h3 Cells, Agung Endro Nugroho, Novrizal Abdi, Sugeng Riyanto, Kazutaka Maeyama, Zullies Ikawati

The Thai Journal of Pharmaceutical Sciences

Marmin or (7-(6’,7’-dihydroxygeranyl-oxy) coumarin is a compound isolated from Aegle marmelos Correa, in the study, we investigated the effects of marmin on the L-histidine decarboxylase (HDC), a rate-limiting histamine synthesizing enzyme, in rat ma...

Rapid Titrimetric And Spectrophotometric Assay Of Tramadol In Bulk Drug And In Formulation Using N-Bromosuccinimide And Methyl Orange As Reagents, K. B. Vinay, H. D., N. Rajendraprasad, M. S. Raghu, P. J. Ramesh, M. X. Cijo, K. Basavaiah

The Thai Journal of Pharmaceutical Sciences

Tramadol is a centrally acting analgesic used for prevention and treatment of moderate to severe pain. Two simple, rapid and sensitive methods by titrimetric and spectrophotometric techniques are described for the determination of tramadol hydrochloride ...

Allylmercaptocaptopril Attenuates Sodium Selenite Induced Experimental Cataractogenesis: An In Vitro And In Vivo Study, K. S. Lakshmi, Shrinivas Sharma

The Thai Journal of Pharmaceutical Sciences

The present study sought to assess the efficacy of the allylmercaptocaptopril เท preventing seleniteinduced cataractogenesis in an experimental setting. The first, in vitro phase of the study was performed on lenses from Wistar rats incubated for 24 ...

Design And Characterization Of Bioadhesive Ophthalmic Films Of Flurbiprofen, Rashi Saroot, Ritu Mehra Gilhotra

The Thai Journal of Pharmaceutical Sciences

An attempt has been made to formulate sustained release ophthalmic films of flurbiprofen along with bioadhesive polymers. Ocular films were prepared by using polymers; sodium alginate, chitosan and HPMC; alone and in different combinations. Glycerol was ...

Influence Of Surfactants On Crystal Form Of Mefenamic Acid, Kaival P., Kulkarni P.K., Mudit Dixit, Ashwini G. Kni

The Thai Journal of Pharmaceutical Sciences

Mefenamic acid is an anti inflammatory and poorly water-soluble drug. Since the drug powder can stick to any type of surface, and is not easy to handle in granulation and tabletting process, it is more desirable to recrystallize the mefenamic acid in suc...

Acute And Sub-Chronic Toxicity Studies Of A Standardized Extract Of Centella Asiatica Eca 233, Songpol Chivapat, Pranee Chavalittumrong, Mayuree H. Tantisira

The Thai Journal of Pharmaceutical Sciences

Acute toxicity study of Centella asiatica standardized extract ECa 233 was conducted by an oral administration of 10.0 g/kg extract into 10 male and 10 female mice. The extract at the given dose did not cause any toxic signs and death within the observat...

Hptlc-Densitometric Method Development And Validation For Simultaneous Determination Of Lamivudine, Nevirapine And Zidovudine In Fixed Dose Combinations, Gebremedhin Solomon, Ariaya Hymete, Abdel-Maaboud I. Mohamed, Adnan A. Bekhit

The Thai Journal of Pharmaceutical Sciences

In this study an HPTLC-densitometric method was developed for the simultaneous determination of lamivudine, nevirapine and zidovudine in pharmaceutical dosage forms which are used widely as first line HIV/AIDS treatment. Chromatographic separation of the...

Ion-Pair Titrimetric Assays Of Quetiapine Fumarate In Pharmaceuticals Using Sodium Tetraphenylboron And Sodium Lauryl Sulphate, N. Rajendraprasad, K. Basavaiah, Kanakapura B. Vinay

The Thai Journal of Pharmaceutical Sciences

Two simple, rapid, precise and accurate titrim etric methods employing sodium tetraphenylboron (STPB) and sodium lauryl sulphate (SLS) as titrants are described for the quantitative determination of quetiapine fumarate (QTF) in bulk drug and tablets. The...

Simultaneous Determination Of Ampicillin Sodium And Sulbactam Sodium In Binary Mixtures And Commercial Dosage Forms Using Chemometrics - Assisted Spectrophotometric Techniques, Zelalem M, Abdel-Maaboud I., Adnan A. Bekhit, Ariaya Hymete

The Thai Journal of Pharmaceutical Sciences

The binary mixture of ampicillin sodium and sulbactam sodium is officially analyzed by HPLC but can not be simultaneously determined by the normal spectrophotometric techniques since their absorption spectra have a strong degree of overlapping. The curre...

Minocycline And Magnesium In Combination Attenuates Oxidative Stress And Decreases Ischemic Neuronal Damage In Vivo, Pallab Bhattacharya, Anand Kr., Sudip Paul

The Thai Journal of Pharmaceutical Sciences

A neuroprotective strategy through a combination therapy is always being superior to any other singular therapeutic interventions, as these acts through a multifaceted approach within the brain during focal cerebral ischemia. Therefore, the development o...

Use Of Bromate - Bromide Mixture As A Reagent For The Determination Of Dothiepin Hydrochloride In Pharmaceuticals, Sameer A.M. Abdulrahman, Kanakapura Basavaiah

The Thai Journal of Pharmaceutical Sciences

The present study describes one titrimetric and two spectrophotometric methods for the determination of dothiepin hydrochloride (DOTH) in bulk drug and in tablets. The methods employed bromate-bromide mixture in acid medium as an oxidimetric as well as b...

Antioxidant Properties Of Squeezed Mangosteen Juice, Monrudee Sukma, Tanasait Ngawhirunpat, Praneet Opanasopit, Pongpun Siripong

The Thai Journal of Pharmaceutical Sciences

The aim of this study was to investigate antioxidant effects of squeezed mangosteen (Garcinia mangostana) juice as preferable diet for human consumption. Mangosteen juice was prepared from the aril part. Antioxidant properties were evaluated by total ant...

Author Index, Keyword Index, N/A

The Thai Journal of Pharmaceutical Sciences

No abstract provided.

Synthesis And Antihepatotoxic Activity Of Some New Xanthones Containing 1,4-Dioxane Ring System, Shah Alam Khan, Bahar Ahmed

The Thai Journal of Pharmaceutical Sciences

This study was aimed at the synthesis of few xanthone derivatives containing 1,4-dioxane ring system. The reaction of 3,4-dihydroxy xanthone derivatives (3a-c) with ethylene dibromide and epichlorohydrin under approriate reaction conditions afforded xant...

Effect Of Ocimum Sanctum Extract On Sodium Nitrite - Induced Experimental Amnesia In Mice, Manoj Dokania, Kamal Kishore, P.K. Sharma

The Thai Journal of Pharmaceutical Sciences

The present study investigated the antiamnesic effect of the extract of Ocimum sanctum (OS) on time induced amnesia and sodium nitrite-induced amnesia in mice by using two different rodent models of memory. The aqueous extract of OS was administered to m...

Identification Of Activities Involved In Cag/Ctg Repeat Instability, Nelson Lap Shun Chan

University of Kentucky Doctoral Dissertations

CAG/CTG repeat instability is associated with at least 14 neurological disorders, including Huntington’s disease and Myotonic dystrophy type 1. In vitro and in vivo studies have showed that CAG/CTG repeats form a stable hairpin that is believed to be the intermediate for repeat expansion and contraction.

Addition of extra DNA is essential for repeat expansion, so DNA synthesis is one of the keys for repeat expansion. In vivo studies reveal that 3’ CTG slippage with subsequent hairpin formation (henceforth called the 3’ CTG slippage hairpin) occurs during DNA synthesis. It is proposed that hairpin tolerance machinery is activated because prolonged …

Overuse Of Antibiotics In Children For Upper Respiratory Infections (Uris): A Dilemma, Malika Taufiq, Rukhsana Wamiq Zuberi

Department for Educational Development

No abstract provided.