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Godwin U Ebiloma, Teresa Díaz Ayuga, Emmanuel O Balogun, Lucía Abad Gil, Anne Donachie, Marcel Kaiser, Tomás Herraiz, Daniel K Inaoka, Tomoo Shiba, Shigeharu Harada, Kiyoshi Kita, Harry P de Koning, Christophe Dardonville
African trypanosomiasis is a neglected parasitic disease that is still of great public health relevance, and a severe impediment to agriculture in endemic areas. The pathogens possess certain unique metabolic features that can be exploited for the development of new drugs. Notably, they rely on an essential, mitochondrially-localized enzyme, Trypanosome Alternative Oxidase (TAO) for their energy metabolism, which is absent in the mammalian hosts and therefore an attractive target for the design of safe drugs...
February 26, 2018: European Journal of Medicinal Chemistry
Jacques-Robert Christen, Eliane Bourreau, Magalie Demar, Edward Lightburn, Pierre Couppié, Marine Ginouvès, Ghislaine Prévot, Jean-Pierre Gangneux, Hélène Savini, Frank de Laval, Vincent Pommier de Santi, Sébastien Briolant
BACKGROUND: New world cutaneous leishmaniasis (NWCL) can be found in French Guiana as well as in several other parts of Central and South America. Leishmania guyanensis accounts for nearly 90% of cases in French Guiana and is treated with pentamidine isethionate, given by either intramuscular or intravenous injection. The military population is particularly exposed due to repeated missions in the rainforest. The purpose of the present study was to identify the factors associated with pentamidine isethionate treatment failure in a series of service members with L...
February 23, 2018: Travel Medicine and Infectious Disease
Valeska Albuquerque Francesconi, Fabio Francesconi, Rajendranath Ramasawmy, Gustavo Adolfo Sierra Romero, Maria das Graças Costa Alecrim
BACKGROUND: The treatment of Leishmaniasis caused by Leishmania (Viannia) guyanensis is based on a weak strength of evidence from very few clinical trials and some case series reports. Current treatment guidelines recommend pentamidine isethionate or meglumine antimoniate (Glucantime) as the first-line choices. Both are parenteral drugs with a low therapeutic indexes leading to a high risk of undesired effects. Imidazole derivatives interfere with the production of leishmanial ergosterol, an essential component of their membrane structure...
February 26, 2018: PLoS Neglected Tropical Diseases
Róbson Ricardo Teixeira, Poliana Aparecida Rodrigues Gazolla, Adalberto Manoel da Silva, Maria Paula Gonçalves Borsodi, Bartira Rossi Bergmann, Rafaela Salgado Ferreira, Boniek Gontijo Vaz, Géssica Adriana Vasconcelos, Wallace Pacienza Lima
In this paper, it is described the synthesis and the evaluation of the leishmanicidal activity of twenty-six eugenol derivatives bearing 1,2,3-triazole functionalities. The evaluation of the compounds on promastigotes of Leishmania amazonensis (WHOM/BR/75/Josefa) showed that eugenol derivatives present leishmanicidal activities with varying degrees of effectiveness. The most active compound, namely 4-(3-(4-allyl-2-methoxyphenoxy)propyl)-1-(4-methylbenzyl)-1H-1,2,3-triazole (7k) (IC50 = 7.4 ± 0.8 μmol L-1), also targeted Leishmania parasites inside peritoneal macrophages (IC50 = 1...
February 3, 2018: European Journal of Medicinal Chemistry
Letícia de Almeida, Andressa Terumi Fujimura, Mayara Lucia Del Cistia, Bruno Fonseca-Santos, Kely Braga Imamura, Paul A M Michels, Marlus Chorilli, Márcia A S Graminha
The World Health Organization (WHO) estimates that more than one billion people suffer from neglected tropical diseases. Leishmaniasis is a widespread disease, affecting 12 million people around the world with about 1–2 million estimated new cases occurring every year. Although pentavalent antimonial drugs are the most frequently prescribed treatments for leishmaniasis, they produce severe side effects, including cardiotoxicity and hepatotoxicity. Other compounds, such as amphotericin B, pentamidine and miltefosine, are second choice drugs, but they also produce side effects that can endanger the patient's life...
February 2017: Journal of Biomedical Nanotechnology
Nida Ghouri, Khalid Mohammed Khan, Arshia, M Iqbal Choudhary, Shahnaz Perveen
BACKGROUND: Leishmaniasis is a protozoan parasitic vector-borne disease which is endemic in 88 tropical countries. Infected sand fly is the main cause of this disease while, there are several vectors, parasites, and reservoirs involved in the transmission of this disease. Leishmania donovani, L. infantum, and L. chagasi are. common disease causing species, spread through sandflies. It is considered to be a focal disease having scattered foci. Leishmaniasis is a disease with a broad clinical spectrum...
January 14, 2018: Medicinal Chemistry
Silvia Spoto, Sebastiano Costantino, Emanuele Valeriani, Marta Fogolari, Eleonora Cella, Giordano Dicuonzo, Massimo Ciccozzi, Silvia Angeletti
Adult-onset Still's disease (AOSD) due to visceral leishmaniasis (VL) has not been previously reported. This case report analyzes a single episode of AOSD probably due to a visceral leishmaniasis successfully treated with pentamidine isethionate and prednisone.
December 2017: Clinical Case Reports
Angela Scala, Anna Piperno, Nicola Micale, Placido G Mineo, Antonio Abbadessa, Roberta Risoluti, Germano Castelli, Federica Bruno, Fabrizio Vitale, Antonio Cascio, Giovanni Grassi
Pentamidine (Pent), an antiparasitic drug used for the treatment of visceral leishmaniasis, has been modified with terminal azide groups and conjugated to two different polymer backbones (PLGA-PEG [PP] copolymer and hyaluronic acid [HA]) armed with alkyne end-groups. The conjugation has been performed by Copper Catalyzed Azido Alkyne Cycloaddition (CuAAC) using CuSO4 /sodium ascorbate as metal source. The novel PP-Pent and HA-Pent bioconjugates are proposed, respectively, as non-targeted and targeted drug delivery systems against Leishmania infections...
December 8, 2017: Journal of Biomedical Materials Research. Part B, Applied Biomaterials
Yoshiyuki Ohara, Takanori Asakura, Soichiro Ueda, Yoshitake Yamada, Makoto Ishii, Tomoko Betsuyaku
No abstract text is available yet for this article.
December 1, 2017: QJM: Monthly Journal of the Association of Physicians
Jung-Ren Chen, Yu-Heng Lai, Jhih-Jie Tsai, Chung-Der Hsiao
Currently, drug screening relies on cell-based experiments or on animal models to confirm biological effects. The mammalian system is considered too time-consuming, expensive and complex to perform high-throughput drug screening. There is a gap between in vitro cell-based models and the in vivo mammalian models. The zebrafish is an ideal model that could link preclinical toxicity screening with the drug development pipeline. Taking advantage of a highly conservative genomic, rapid development, large number of offspring, low cost and easy manipulation, zebrafish has been considered an excellent animal model for disease-based drug screening...
November 27, 2017: Molecules: a Journal of Synthetic Chemistry and Natural Product Chemistry
Kah Tee Lim, Azimah Amanah, Nelson Jeng-Yeou Chear, Zuriati Zahari, Zafarina Zainuddin, Mohd Ilham Adenan
In our ongoing work searching for new trypanocidal lead compounds from Malaysian plants, two known piperidine alkaloids (+)-spectaline (1) and iso-6-spectaline (2) were isolated from the leaves of Senna spectabilis (sin. Cassia spectabilis). Analysis of the1 H and13 C NMR spectra showed that 1 and 2 presented analytical and spectroscopic data in full agreement with those published in the literature. All compounds were screened in vitro against Trypanosoma brucei rhodesiense in comparison to the standard drug pentamidine...
January 2018: Experimental Parasitology
Lyvia Lintzmaier Petiz, Amanda do Rocio Andrade Pires, Aurea Echevarria, Cláudio Eduardo Rodrigues-Santos, Maria Eliane Merlin Rocha, Alexandra Acco, Silvia Maria Suter Correia Cadena
Amidines are chemically characterized by the presence of two nitrogen atoms that bind to the same carbon atom in its structure. Several biological activities have been ascribed to these compounds. Pentamidine, an aromatic diamidine, is effective in the treatment against Pneumocystis carinii and leishmaniasis, but it can also have severe side effects. New amidine derivatives have been synthesized, among them N,N'-diphenyl-4-methoxy-benzamidine (methoxyamidine), which is effective against Leishmania amazonensis (LD50  = 20 μM) and Trypanosoma cruzi (LD50  = 59 nM)...
January 5, 2018: Chemico-biological Interactions
Abdelbasset A Farahat, Mohamed A Ismail, Arvind Kumar, Tanja Wenzler, Reto Brun, Ananya Paul, W David Wilson, David W Boykin
A novel series of indole and benzimidazole bichalcophene diamidine derivatives were prepared to study their antimicrobial activity against the tropical parasites causing African sleeping sickness and malaria. The dicyanoindoles needed to synthesize the target diamidines were obtained through Stille coupling reactions while the bis-cyanobenzimidazoles intermediates were made via condensation/cyclization reactions of different aldehydes with 4-cyano-1,2-diaminobenzene. Different amidine synthesis methodologies namely, lithium bis-trimethylsilylamide (LiN[Si(CH3)3]2) and Pinner methods were used to prepare the diamidines...
October 22, 2017: European Journal of Medicinal Chemistry
Lauve Rachel Tchokouaha Yamthe, Regina Appiah-Opong, Patrick Valere Tsouh Fokou, Nole Tsabang, Fabrice Fekam Boyom, Alexander Kwadwo Nyarko, Michael David Wilson
Leishmaniasis is a vector-borne neglected tropical disease caused by protozoan parasites of the Leishmania genus and transmitted by the female Phlebotomus and Lutzomyia sand flies. The currently prescribed therapies still rely on pentavalent antimonials, pentamidine, paromomycin, liposomal amphotericin B, and miltefosine. However, their low efficacy, long-course treatment regimen, high toxicity, adverse side effects, induction of parasite resistance and high cost require the need for better drugs given that antileishmanial vaccines may not be available in the near future...
October 29, 2017: Marine Drugs
Ermias Diro, Koert Ritmeijer, Marleen Boelaert, Fabiana Alves, Rezika Mohammed, Charles Abongomera, Raffaella Ravinetto, Maaike De Crop, Helina Fikre, Cherinet Adera, Harry van Loen, Achilleas Tsoumanis, Wim Adriaensen, Asrat Hailu, Johan van Griensven
Background: We have conducted a single-arm trial evaluating monthly pentamidine secondary prophylaxis (PSP) to prevent visceral leishmaniasis (VL) relapse in Ethiopian HIV-patients. Outcomes at 12 months of PSP have been previously reported, supporting PSP effectiveness and safety. However, remaining relapse-free after PSP discontinuation is vital. We now report outcomes and associated factors for a period of upto 2.5 years after initiating PSP, including one year follow-up after PSP discontinuation...
September 13, 2017: Clinical Infectious Diseases: An Official Publication of the Infectious Diseases Society of America
Iván A Aréchiga-Figueroa, Leticia G Marmolejo-Murillo, Meng Cui, Mayra Delgado-Ramírez, Marcel A G van der Heyden, José A Sánchez-Chapula, Aldo A Rodríguez-Menchaca
Inward rectifier potassium (Kir) channels are expressed in almost all mammalian tissues and contribute to a wide range of physiological processes. Kir4.1 channel expression is found in the brain, inner ear, eye, and kidney. Loss-of-function mutations in the pore-forming Kir4.1 subunit cause an autosomal recessive disorder characterized by epilepsy, ataxia, sensorineural deafness and tubulopathy (SeSAME/EST syndrome). Despite its importance in physiological and pathological conditions, pharmacological research of Kir4...
October 6, 2017: European Journal of Pharmacology
K F Urbancic, F Ierino, E Phillips, P F Mount, A Mahony, J A Trubiano
While trimethoprim-sulfamethoxazole is considered first-line therapy for Pneumocystis pneumonia prevention in renal transplant recipients, reported adverse drug reactions may limit use and increase reliance on costly and less effective alternatives, often aerosolized pentamidine. We report our experience implementing a protocolized approach to trimethoprim-sulfamethoxazole adverse drug reaction assessment and rechallenge to optimize prophylaxis in this patient cohort. We retrospectively reviewed 119 patients receiving Pneumocystis pneumonia prophylaxis prior to and after protocol implementation...
February 2018: American Journal of Transplantation
C Panozzo, A Laleve, D Tribouillard-Tanvier, J Ostojić, C H Sellem, G Friocourt, A Bourand-Plantefol, A Burg, A Delahodde, M Blondel, G Dujardin
Bcs1p is a chaperone that is required for the incorporation of the Rieske subunit within complex III of the mitochondrial respiratory chain. Mutations in the human gene BCS1L (BCS1-like) are the most frequent nuclear mutations resulting in complex III-related pathologies. In yeast, the mimicking of some pathogenic mutations causes a respiratory deficiency. We have screened chemical libraries and found that two antibiotics, pentamidine and clarithromycin, can compensate two bcs1 point mutations in yeast, one of which is the equivalent of a mutation found in a human patient...
December 2017: Biochimica et Biophysica Acta
Vanessa Ortega, Selma Giorgio, Eneida de Paula
Conventional chemotherapy for leishmaniasis includes considerably toxic drugs and reports of drug-resistance are not uncommon. Liposomal encapsulated drugs appear as an option for the treatment of leishmaniasis, providing greater efficacy for the active and reducing its side effects by promoting superior tissue absorption, favouring drug penetration into the macrophages, and retarding its clearance from the site of action. In this paper, a review on the advances achieved with liposome-based anti-leishmaniasis drug delivery systems is presented...
September 2017: Journal of Liposome Research
Genesis Palacios, Adriana Parodi, Yulieth A Upegui, Andres Montoya, Sergio Pulido, Iván D Vélez, Sara M Robledo
Current chemotherapeutic agents for leishmaniasis have several disadvantages interfering with the effective treatment and therefore more and better antileishmanial drugs are needed. Discovery of candidates for leishmaniasis treatment requires not only accurate and precise methodologies but also well-known biological system to measure infectivity of parasites and antileishmanial activity of the new compounds. Significant variation in the in vitro and in vivo infectivity and sensitivity to established and experimental drugs in Leishmania strains are reported...
November 2017: Parasitology
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