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https://www.readbyqxmd.com/read/28329730/synthesis-of-novel-quinoline-based-4-5-dihydro-1h-pyrazoles-as-potential-anticancer-antifungal-antibacterial-and-antiprotozoal-agents
#1
Jonathan Ramírez-Prada, Sara M Robledo, Iván D Vélez, María Del Pilar Crespo, Jairo Quiroga, Rodrigo Abonia, Alba Montoya, Laura Svetaz, Susana Zacchino, Braulio Insuasty
A new series of N-substituted 2-pyrazolines 9a-f, 10a-f, 11a-f, 12a-f and 13a-f were obtained from the cyclocondensation reaction of [(7-chloroquinolin-4-yl)amino]chalcones 8a-f with hydrazine hydrate and its derivatives. Fourteen of the synthesized compounds including the starting chalcones were selected by US National Cancer Institute (NCI) for testing their anticancer activity against 60 different human cancer cell lines, with the most important GI50 values ranging from 0.28 to 11.7 μM (0.13-6.05 μg/mL) and LC50 values ranging from 2...
March 16, 2017: European Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/28329481/cutaneous-leishmaniasis-mimicking-squamous-cell-carcinoma
#2
Tara Oetken, Bryan Hiscox, Ida Orengo, Theodore Rosen
A 41-year-old man from Cuero, Texas with a nonhealinglesion on his left cheek was referred to ourclinic for removal of a squamous cell carcinoma. Thepatient first noticed a "pimple" on his left cheek 3-4months prior to presentation. When the lesion beganto grow he presented to his primary care physician anda biopsy was taken, showing "atypical squamous cellproliferation." Mohs surgery was performed and thenodule was removed with no evidence of malignancyseen on histopathology. Upon review of the surgicalbiopsies by consulting pathologists, the diagnosis ofleishmaniasis was established and later confirmed bythe Center for Disease Control and Prevention (CDC)as Leishmania mexicana...
January 15, 2017: Dermatology Online Journal
https://www.readbyqxmd.com/read/28329329/increased-transmissibility-of-leishmania-donovani-from-the-mammalian-host-to-vector-sand-flies-after-multiple-exposures-to-sand-fly-bites
#3
Joanna G Valverde, Andrea Paun, Ehud Inbar, Audrey Romano, Michael Lewis, Kashinath Ghosh, David Sacks
Background: Patients with active visceral leishmaniasis are important reservoirs in the anthroponotic transmission cycle of Leishmania donovani. The role of the blood or skin as a source of infection to sand flies remains unclear, and the possible effect of multiple exposures to fly bites on transmissibility has not been addressed. Methods: L. donovani infected hamsters were exposed to xenodiagnoses with Lutzomyia longipalpis on the same or different sites on the abdomen on two consecutive days, or by artificial feeding on the skin or blood...
March 9, 2017: Journal of Infectious Diseases
https://www.readbyqxmd.com/read/28327804/efficacy-and-safety-of-amphotericin-b-deoxycholate-versus-n-methylglucamine-antimoniate-in-pediatric-visceral-leishmaniasis-an-open-label-randomized-and-controlled-pilot-trial-in-brazil
#4
Myrlena Mescouto Borges, Maria Cristina da Silva Pranchevicius, Elza Ferreira Noronha, Gustavo Adolfo Sierra Romero, César Omar Carranza-Tamayo
INTRODUCTION: Despite their high toxicity, antimonials and amphotericin B deoxycholate are commonly used for treating visceral leishmaniasis (VL). Few studies showing conflictive data about their efficacy and adverse events in pediatric population are available. This study aimed to evaluate efficacy and safety of amphotericin B deoxycholate vs. that of N-methylglucamine antimoniate in treating pediatric VL in Brazil. METHODS: This was a randomized, open-label, 2-arm and controlled pilot clinical trial...
January 2017: Revista da Sociedade Brasileira de Medicina Tropical
https://www.readbyqxmd.com/read/28327803/serodiagnosis-of-visceral-and-cutaneous-leishmaniasis-in-human-and-canine-populations-living-in-indigenous-reserves-in-the-brazilian-amazon-region
#5
Julia Teresa Ribeiro de Lima, Solange Maria Gennari, Herbert Sousa Soares, Antonio Humberto Hamad Minervino, Antonio Francisco Malheiros, Fernando Silveira Marques, Márcia Dalastra Laurenti, Rosangela Zacarias Machado, Arlei Marcili, Marcelo Bahia Labruna, Rodrigo Martins Soares
INTRODUCTION: Leishmaniasis is endemic to the Northern, Northeastern, Central-Western, and Southeastern regions of Brazil. We aimed to assess the epidemiological situation of leishmaniasis in humans and dogs in indigenous villages located in the States of Mato Grosso and Tocantins using a serological survey conducted in May 2011. METHODS: Serum samples were collected from 470 humans and 327 dogs living in villages of the Urubu Branco and Tapirapé Karajá indigenous reserves...
January 2017: Revista da Sociedade Brasileira de Medicina Tropical
https://www.readbyqxmd.com/read/28327802/in-vitro-and-in-vivo-antileishmanial-activity-of-artemisia-annua-l-leaf-powder-and-its-potential-usefulness-in-the-treatment-of-uncomplicated-cutaneous-leishmaniasis-in-humans
#6
Luz Estella Mesa, Daniel Vasquez, Pierre Lutgen, Iván Darío Vélez, Adriana María Restrepo, Isabel Ortiz, Sara María Robledo
INTRODUCTION: Cutaneous leishmaniasis (CL) is a tropical disease that affects millions of individuals worldwide. The current drugs for CL may be effective but have serious side effects; hence, alternatives are urgently needed. Although plant-derived materials are used for the treatment of various diseases in 80% of the global population, the validation of these products is essential. Gelatin capsules containing dried Artemisia annua leaf powder were recently developed as a new herbal formulation (totum) for the oral treatment of malaria and other parasitic diseases...
January 2017: Revista da Sociedade Brasileira de Medicina Tropical
https://www.readbyqxmd.com/read/28327794/seasonality-of-sand-flies-diptera-psychodidae-and-leishmania-dna-detection-in-vector-species-in-an-area-with-endemic-visceral-leishmaniasis
#7
Lara Saraiva, Camila Gonçalves Leite, Ana Cristina Vianna Mariano da Rocha Lima, Luiz Otávio Alves de Carvalho, Agnes Antônia Sampaio Pereira, Jerônimo Marteleto Nunes Rugani, Felipe Dutra Rego, Célia Maria Ferreira Gontijo, José Dilermando Andrade
BACKGROUND: Leishmaniases are a serious health problem in southeast Brazil, including the city of Belo Horizonte (BH), Minas Gerais state (MG), where there are high rates of incidence and mortality due to visceral leishmaniases. BH is divided into nine sanitary districts (SD) of which one, the Venda Nova SD, was selected for this study because it has high rates of positivity for canine leishmaniasis and high incidence of human leishmaniasis. OBJECTIVES: This study aimed to survey the sand fly fauna in Venda Nova SD from August 2011 to July 2013 and perform a descriptive analysis of the vector population...
April 2017: Memórias do Instituto Oswaldo Cruz
https://www.readbyqxmd.com/read/28327439/an-in-silico-functional-annotation-and-screening-of-potential-drug-targets-derived-from-leishmania-spp-hypothetical-proteins-identified-by-immunoproteomics
#8
Miguel A Chávez-Fumagalli, Mônica S Schneider, Daniela P Lage, Ricardo A Machado-de-Ávila, Eduardo A F Coelho
Leishmaniasis is a parasitic disease caused by the protozoan of the Leishmania genus. While no human vaccine is available, drugs such as pentavalent antimonials, pentamidine and amphotericin B are used for treat the patients. However, the high toxicity of these pharmaceutics, the emergence of parasite resistance and/or their high cost have showed to the urgent need of identify new targets to be employed in the improvement of the treatment against leishmaniasis. In a recent immunoproteomics approach performed in the Leishmania infantum species, 104 antigenic proteins were recognized by antibodies in sera of visceral leishmaniasis (VL) dogs...
March 19, 2017: Experimental Parasitology
https://www.readbyqxmd.com/read/28327413/domestic-dogs-as-reservoir-hosts-for-leishmania-donovani-in-the-southernmost-western-ghats-in-india
#9
P Jambulingam, N Pradeep Kumar, S Nandakumar, K P Paily, R Srinivasan
The peripheral blood samples from domestic dogs (n=47) and wild rats (n=25) in the Kani Tribe settlements, located southernmost part of the Western Ghats, Thiruvananthapuram district, Kerala, India were examined for Leishmania infection. This area is known for cases of leishmaniasis with cutaneous manifestations and sandfly abundance. The tribes domesticate dogs to protect them from untoward activities of wild animals. Leishmania donovani parasite DNA was detected only from 6.4% (n=3) of the blood samples collected from the domestic dogs by amplification of the diagnostic kinetoplast mini-circle DNA and PCR-RFLP analysis of the UTR region of heat shock protein 70 (hsp70) gene...
March 18, 2017: Acta Tropica
https://www.readbyqxmd.com/read/28324803/leishmania-donovani-resistant-to-ambisome-or-miltefosine-exacerbates-cd58-expression-on-nk-cells-and-promotes-trans-membrane-migration-in-association-with-cd2
#10
Pushkar Shivam, Sarita Kumari, Fauzia Jamal, Vikash Kumar, Manish Kumar, Sanjiva Bimal, Shyam Narayan, Vidya Nand Ravi Das, Krishna Pandey, Anil Kumar Gupta, Pradeep Das, Shubhankar Kumar Singh
Visceral leishmaniasis (VL) is a disease that is associated with compromised immunity and drug un-responsiveness as well as with the emergence of drug resistance in Leishmania donovani (Ld). Ld down-modulates cellular immunity by manipulating signaling agents, including a higher expression of the adhesion molecule CD58. The expression of CD58 and CD2 on natural killer (NK) cells facilitates intercellular adhesion and signaling. The influence of drug-resistant Ld on the expression of CD58 and CD2 was addressed in this study...
March 16, 2017: Cytokine
https://www.readbyqxmd.com/read/28322559/identification-of-novel-inhibitors-of-leishmania-donovani-%C3%AE-glutamylcysteine-synthetase-using-structure-based-virtual-screening-docking-molecular-dynamics-simulation-and-in-vitro-studies
#11
Pragati Agnihotri, Arjun Kumar Mishra, Shikha Mishra, Vijay Kumar Sirohi, Amogh A Sahasrabuddhe, J Venkatesh Pratap
Trypansomatids maintain their redox balance by the trypanothione based redox system, enzymes of which exhibit differences from mammalian homologues. γ-glutamylcysteine synthetase (Gcs) is an essential enzyme of this pathway performing the first and rate limiting step. L-buthionine-S,R-sulfoximine (BSO), a specific inhibitor of Gcs induces toxicity in hosts infected with T. brucei underlining for novel Gcs inhibitors. The present study reports identification of Ld Gcs inhibitors using computational approaches and their experimental validation...
March 21, 2017: Journal of Chemical Information and Modeling
https://www.readbyqxmd.com/read/28321221/leishmania-donovani-nucleoside-hydrolase-nh36-domains-induce-t-cell-cytokine-responses-in-human-visceral-leishmaniasis
#12
Micheli Luize Barbosa Santos, Dirlei Nico, Fabrícia Alvisi de Oliveira, Aline Silva Barreto, Iam Palatnik-de-Sousa, Eugenia Carrillo, Javier Moreno, Paula Mello de Luca, Alexandre Morrot, Daniela Santoro Rosa, Marcos Palatnik, Cristiane Bani-Corrêa, Roque Pacheco de Almeida, Clarisa Beatriz Palatnik-de-Sousa
Development of immunoprotection against visceral leishmaniasis (VL) focused on the identification of antigens capable of inducing a Th1 immune response. Alternatively, antigens targeting the CD8 and T-regulatory responses are also relevant in VL pathogenesis and worthy of being included in a preventive human vaccine. We assessed in active and cured patients and VL asymptomatic subjects the clinical signs and cytokine responses to the Leishmania donovani nucleoside hydrolase NH36 antigen and its N-(F1), central (F2) and C-terminal (F3) domains...
2017: Frontiers in Immunology
https://www.readbyqxmd.com/read/28321217/a-vaccine-therapy-for-canine-visceral-leishmaniasis-promoted-significant-improvement-of-clinical-and-immune-status-with-reduction-in-parasite-burden
#13
Bruno Mendes Roatt, Rodrigo Dian de Oliveira Aguiar-Soares, Levi Eduardo Soares Reis, Jamille Mirelle de Oliveira Cardoso, Fernando Augusto Siqueira Mathias, Rory Cristiane Fortes de Brito, Sydnei Magno da Silva, Nelder De Figueiredo Gontijo, Sidney de Almeida Ferreira, Jesus G Valenzuela, Rodrigo Corrêa-Oliveira, Rodolfo Cordeiro Giunchetti, Alexandre Barbosa Reis
Herein, we evaluated the treatment strategy employing a therapeutic heterologous vaccine composed of antigens of Leishmania braziliensis associated with MPL adjuvant (LBMPL vaccine) for visceral leishmaniasis (VL) in symptomatic dogs naturally infected by Leishmania infantum. Sixteen dogs received immunotherapy with MPL adjuvant (n = 6) or with a vaccine composed of antigens of L. braziliensis associated with MPL (LBMPL vaccine therapy, n = 10). Dogs were submitted to an immunotherapeutic scheme consisting of 3 series composed of 10 subcutaneous doses with 10-day interval between each series...
2017: Frontiers in Immunology
https://www.readbyqxmd.com/read/28321209/treatment-of-leishmania-leishmania-amazonensis-infected-mice-with-a-combination-of-a-palladacycle-complex-and-heat-killed-propionibacterium-acnes-triggers-protective-cellular-immune-responses
#14
Carolina S Paladi, Danielle A M da Silva, Priscila D Motta, Daniel M Garcia, Daniela Teixeira, Ieda M Longo-Maugéri, Simone Katz, Clara L Barbiéri
Palladacycle complex DPPE 1.2 was previously reported to inhibit the in vitro and in vivo infection by Leishmania (Leishmania) amazonensis. The aim of the present study was to compare the effect of DPPE 1.2, in association with heat-killed Propionibacterium acnes, on L. (L.) amazonensis infection in two mouse strains, BALB/c and C57BL/6, and to evaluate the immune responses of the treated animals. Foot lesions of L. (L.) amazonensis-infected mice were injected with DPPE 1.2 alone, or associated with P. acnes as an adjuvant...
2017: Frontiers in Microbiology
https://www.readbyqxmd.com/read/28320726/glucantime%C3%A2-causes-oxidative-stress-derived-dna-damage-in-balb-c-mice-infected-by-leishmania-leishmania-infantum
#15
Vanessa Ribeiro Moreira, Luís Cláudio Lima de Jesus, Rossy-Eric Pereira Soares, Luis Douglas Miranda Silva, Bruno Araújo Serra Pinto, Maria Norma Melo, Antonio Marcus de Andrade Paes, Silma Regina Ferreira Pereira
Leishmaniasis is a neglected tropical disease caused by over 20 species of the protozoan parasite Leishmania Regarding treatment, Glucantime® is the first-choice drug recommended by the World Health Organization for the treatment of all types of leishmaniasis. However, the mechanisms of action and toxicity of pentavalent antimonials, including genotoxic effetcs, remain unclear. Therefore, the mechanism by which Glucantime® causes DNA damage was investigated in BALB/c mice infected by Leishmania (Leishmania) infantum and treated with Glucantime® (20 mg/kg for 20 days)...
March 20, 2017: Antimicrobial Agents and Chemotherapy
https://www.readbyqxmd.com/read/28320721/a-library-of-seleno-compounds-and-leishmania-species-rising-evidences-towards-novel-agents
#16
Álvaro Martín-Montes, Daniel Plano, Rubén Martín-Escolano, Verónica Alcolea, Marta Díaz, Silvia Pérez-Silanes, Socorro Espuelas, Esther Moreno, Clotilde Marín, Ramón Gutiérrez-Sánchez, Carmen Sanmartín, Manuel Sánchez-Moreno
In vitro leishmanicidal activity of a series of forty-eight selenium derivatives, recently synthesized, was tested on Leishmania infantum and Leishmania braziliensis parasites, using promastigotes and intracellular amastigote forms. The cytotoxicity of the tested compounds on J774.2 macrophage cells was also measured in order to establish their selectivity. Six of the tested compounds (8, 10, 11, 15, 45 and 48) showed selectivity indexes higher than those of the reference drug Glucantime for both Leishmania species; in the case of L...
March 20, 2017: Antimicrobial Agents and Chemotherapy
https://www.readbyqxmd.com/read/28319176/insight-into-the-mechanism-of-action-of-temporin-sha-a-new-broad-spectrum-antiparasitic-and-antibacterial-agent
#17
Zahid Raja, Sonia André, Feten Abbassi, Vincent Humblot, Olivier Lequin, Tahar Bouceba, Isabelle Correia, Sandra Casale, Thierry Foulon, Denis Sereno, Bruno Oury, Ali Ladram
Antimicrobial peptides (AMPs) are promising drugs to kill resistant pathogens. In contrast to bacteria, protozoan parasites, such as Leishmania, were little studied. Therefore, the antiparasitic mechanism of AMPs is still unclear. In this study, we sought to get further insight into this mechanism by focusing our attention on temporin-SHa (SHa), a small broad-spectrum AMP previously shown to be active against Leishmania infantum. To improve activity, we designed analogs of SHa and compared the antibacterial and antiparasitic mechanisms...
2017: PloS One
https://www.readbyqxmd.com/read/28319012/the-expanding-world-of-human-leishmaniasis
#18
James A Cotton
New Leishmania isolates form a novel group of human parasites related to Leishmania enrietti, with cases in Ghana, Thailand, and Martinique; other relatives infect Australian and South American wildlife. These parasites apparently cause both cutaneous and visceral disease, and may have evolved a novel transmission mechanism exploiting blood-feeding midges.
March 16, 2017: Trends in Parasitology
https://www.readbyqxmd.com/read/28316425/molecular-characterization-of-leishmania-parasites-isolated-from-sandflies-species-of-a-zoonotic-cutaneous-leishmaniasis-in-musiyan-south-west-iran
#19
Farzaneh Kavarizadeh, Shahram Khademvatan, Babak Vazirianzadeh, Mohammad Hossein Feizhaddad, Mehdi Zarean
Cutaneous leishmaniasis (CL) is vector borne parasitic disease, considered as public health problem especially in border of Iran and Iraq, Dehloran County (Musian district). The aim of this study was molecular identification of Leishmania parasites in sandfly as vectors of Leishmaniasis. Totally 280 female sandflies were trapped by sticky traps from 7 rural areas of Musiyan in September-November 2012. All sandflies were identified using morphological characters of the head and abdominal terminalia. DNA was extracted from female sandflies and Leishmania was identified using PCR and sequencing...
March 2017: Journal of Parasitic Diseases: Official Organ of the Indian Society for Parasitology
https://www.readbyqxmd.com/read/28316420/lb-broth-lyophilized-rabbit-serum-llr-as-a-new-and-suitable-culture-medium-for-cultivation-of-promastigotes-of-leishmania-major
#20
Vahid Nasiri, Abdolhossein Dalimi, Fatemeh Ghaffarifar
Fetal calf serum is the major part and the most expensive ingredient of the Leishmania culture media. Here, the efficacy of the LB broth-lyophilized Rabbit serum medium (LLR) was evaluated in cultivation of Leishmaniamajor. Conventional Luria-Bertani (LB) broth medium was prepared and autoclaved for 15 min at 121 °C and then lyophilized Rabbit serum was added at the 1, 2.5, 5 and 10 % final concentrations. The efficacy of medium was evaluated by assessing the growth ability and replication pattern of the promastigotes of L...
March 2017: Journal of Parasitic Diseases: Official Organ of the Indian Society for Parasitology
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