This message contains My NCBI what's new results from the National Center for Biotechnology Information (NCBI) at the U.S. National Library of Medicine (NLM).
Do not reply directly to this message.
Sender's message:
Sent on Tuesday, 2011 Oct 11Search kinetoplastids OR kinetoplastid OR Kinetoplastida OR "trypanosoma brucei" OR leishmania OR brucei OR leishmaniasis OR "African trypanosomiasis"
Click here to view complete results in PubMed. (Results may change over time.)
To unsubscribe from these e-mail updates click here.
| PubMed Results |
| 1. | ChemMedChem. 2011 Oct 7. doi: 10.1002/cmdc.201100422. [Epub ahead of print]New Prodrugs of the Antiprotozoal Drug Pentamidine.Kotthaus J, Kotthaus J, Schade D, Schwering U, Hungeling H, Müller-Fielitz H, Raasch W, Clement B.SourcePharmaceutical Institute, Department of Pharmaceutical and Medicinal Chemistry, Christian-Albrechts-University of Kiel, Gutenbergstraße 76-78, 24118 Kiel (Germany). AbstractPentamidine is an effective antimicrobial agent that is approved for the treatment of African trypanosomiasis but suffers from poor oral bioavailability and central nervous system (CNS) penetration. This work deals with the development and systematic characterisation of new prodrugs of pentamidine. For this reason, numerous prodrugs that use different prodrug principles were synthesised and examined in vitro and in vivo. Another objective of the study was the determination of permeability of the different pentamidine prodrugs. While some of the prodrug principles applied in this study are known, such as the conversion of the amidine functions into amidoximes or the O-alkylation of amidoximes with a carboxymethyl residue, others were developed more recently and are described here for the first time. These newly developed methods aim to increase the affinity of the prodrug for the transporters and mediate an active uptake via carrier systems by conjugation of amidoximes with compounds that improve the overall solubility of the prodrug. The different principles chosen resulted in several pentamidine prodrugs with various advantages. The objective of this investigation was the systematic characterisation and evaluation of eight pentamidine prodrugs in order to identify the most appropriate strategy to improve the properties of the parent drug. For this reason, all prodrugs were examined with respect to their solubility, stability, enzymatic activation, distribution, CNS delivery, and oral bioavailability. The results of this work have allowed reliable conclusions to be drawn regarding the best prodrug principle for the antiprotozoal drug pentamidine. Copyright © 2011 WILEY-VCH Verlag GmbH & Co. KGaA, Weinheim. |
| Related citations | |
| 2. | Eur J Pharm Sci. 2011 Sep 29. [Epub ahead of print]Lipid nanoparticles containing oryzalin for the treatment of leishmaniasis.Lopes R, Eleutério CV, Gonçalves LM, Cruz ME, Almeida AJ.SourceResearch Institute for Medicines and Pharmaceutical Sciences (iMed.UL), Faculty of Pharmacy, University of Lisbon, Av. Prof. Gama Pinto, 1649-003 Lisboa, Portugal. AbstractOryzalin is a dinitroaniline drug that has attracted recent interest for the treatment of leishmaniasis. Its use as an antiparasitic therapeutic agent is limited by the low water solubility associated with an in vivo rapid clearance, leading to the administration of larger and possibly toxic doses in in vivo studies, and the use of solvents that may lead to undesirable side effects. In the present work oryzalin-containing lipid nanoparticles were produced by a emulsion-solvent evaporation technique using a composition suitable for parenteral administration, i.e., tripalmitin (solid lipid) and a complex mixture of three emulsifying agents (soya lecithin, Tween® 20 and sodium deoxycholate). Physicochemical characterization included the determination of mean particle size, polydispersity index, zeta potential, encapsulation efficiency and DSC studies. Final formulations revealed values of <140nm (PI<0.2) and zeta potential of ≈-35mV, as well as encapsulation efficiency >75%. The effects of various processing parameters, such as lipid and surfactant and composition and concentration, as well as the stability during the harsh procedures of autoclaving (121°C/15min) and freeze-drying were also evaluated. Formulations revealed to be stable throughout freeze-drying and moist-heath sterilization without significant variations on physicochemical properties and no significant oryzalin losses. The use of a complex surfactant mixture proved crucial for preserving formulation stability. Particularly, lecithin appears as a key component in the stabilization of tripalmitin-based oryzalin-containing lipid nanoparticles. Finally, cell viability studies demonstrated that the incorporation of oryzalin in nanoparticles decreases cytotoxicity, thus suggesting this strategy may improve tolerability and therapeutic index of dinitroanilines. Copyright © 2011. Published by Elsevier B.V. |
| Related citations | |
| 3. | BMC Res Notes. 2011 Oct 8;4(1):389. [Epub ahead of print]Visceral leishmaniasis in 26 HIV-negative adults.Lahlou H, Filali AB, Alami M, Amrani M, Berrady R, Rabhi S, Bono W.AbstractABSTRACT: BACKGROUND:Visceral leishmaniasis is a notifiable parasitic disease that had increased in incidence in our region on the past few years. It is common in children. In adults, it occurs more on a background of immunodeficiency, and frequently with incomplete clinical manifestations, making the diagnosis complicated. FINDINGS:The aim of our study is to reveal different features of visceral leishmaniasis in adults, through the analysis of its epidemiological, clinical and biological parameters, in a group of 26 patients. No one was infected with HIV or under immunosuppressive therapy Clinical presentation was generally conservative, but there was few differences in adults compared to children, concerning both the clinical symptoms and the laboratory parameters. Diagnosis was provided by direct examination of bone marrow smears in 24 cases (sensitivity 92%), and anti-leishmanial serology in the others. CONCLUSION:We should think to the diagnosis of VL even if the patient is not known immunocompromised, and even if the clinical is incomplete, to avoid a delay of care which can lead to serious complications. |
| Related citations | |
| 4. | J Egypt Soc Parasitol. 2011 Aug;41(2):485-96.Maternal brucellosis and human pregnancy.Mohammad KI, El Ghazaly MM, Zaalouk TK, Morsy AT.SourceDepartment of Obstetric and Gyncaecolgy, Al-Zahraa University Hospital, Cairo, Egypt. AbstractBrucellosis is a worldwide zoonotic gram-negative bacterium of worldwide distribution. Its role in causing miscarriage in animals is well documented. Data on its role in human abortion are very few. This paper was carried out on selected women with abortion or history of abortion to clarify the role of brucellosis in human abortion. A total of 129 women were selected from Al-Zahraa University Hospital and other obstetric and gynecological hospitals in the vicinity of Greater Cairo. The patients were subjected to clinical, gynecological, and serodiagnosis (STAT and ELISA) of brucellosis. Also, routine urine (Nuclepore technique) and stool (Kato thick smear) was done as well as skin tests and ELISA for common hepatic parasites. The results showed that 59 had brucellosis, 27 had toxoplasmosis, 15 had fascioliasis and 29 had other cause(s) of abortion. Meanwhile, none had visceral leishmaniasis or schistosomiasis mansoni. the signs and symptoms of all patients were hepatosplenomegaly (31.1%), lower back abdominal pain (23.13%), lassitude, headache (each, 21.7%), lymphadenopathy (20.1%), vomiting (17.1%), loss of appetite, myalgia or diarrhea or constipation (each, 15.42 %), weight loss (14.6%), chest pain (13.9%), night sweating or dizziness (11.65%), fever or right sided abdominal pain (each, 10.7%), chills (7.71%), urticaria or monoarthralgia (each, 3.85%). These signs and symptoms were confusing for specific clinical picture of brucellosis. Brucellosis patients were successfully treated with a combination of Rifampicin 600 mg. once daily and Septrin 800 mg twice daily for 6 weeks. Cure was achieved clinically and serologically. Patients with toxoplasmosis or fascioliasis were also treated with Fasinex and Mirazid respectively. Other parasites were also treated. |
| Related citations | |
No comments:
Post a Comment