Article
Pharmacology & Pharmacy
Atousa Hakamifard, Reza Radmehr, Fatemeh Sokhanvari, Fatemeh Sherkat, Amirali Hariri, Jaleh Varshosaz, Zabihollah Shahmoradi, Awat Feizi, Bahareh Abtahi-Naeini, Mahsa Pourmahdi-Boroujeni
Summary: This study aimed to investigate the effects of topical liposomal clarithromycin in combination with meglumine antimoniate on cutaneous leishmaniasis lesions. The results showed that the combination treatment significantly reduced the size of the lesions and had no significant adverse effects.
FRONTIERS IN PHARMACOLOGY
(2023)
Article
Immunology
Joao Paulo Araujo de Sousa, Julyanne Maria Saraiva de Sousa, Raiza Raianne Luz Rodrigues, Thais Amanda de Lima Nunes, Yasmim Alves Aires Machado, Alexandre Carvalho de Araujo, Ingrid Gracielle Martins da Silva, Karine Brenda Barros-Cordeiro, Sonia Nair Bao, Michel Mualem de Moraes Alves, Francisco Jaime Bezerra Mendonca-Junior, Klinger Antonio da Franca Rodrigues
Summary: Leishmaniasis, one of the most serious Neglected Tropical Diseases (NTDs), requires urgent therapeutic alternatives due to the problems with currently available drugs. This study found that a thiophene derivative, SB-200, showed promising anti-leishmanial activity and low toxicity in mice.
INTERNATIONAL IMMUNOPHARMACOLOGY
(2023)
Article
Parasitology
Iuliia K. Akulinina, Iza A. Berechikidze, Svetlana N. Larina, Tatyana Sakharova, Tatyana Yu Degtyarevskaya, Marco Romanelli
Summary: In vivo studies of monotherapy for zoonotic cutaneous leishmaniasis using doxycycline and comparison with meglumine antimoniate showed similar effectiveness by the 30th day, but with better outcomes in terms of weight gain and clinical recovery favoring doxycycline. By the 60th day of treatment, leishmania in the lesions were completely absent with doxycycline monotherapy, demonstrating its efficacy.
Article
Immunology
Marcelo R. Lyra, Liliane F. A. Oliveira, Armando O. Schubach, Raimunda N. R. Sampaio, Bruna C. Rodrigues, Marcia Hueb, Glaucia Cota, Rosiana E. Silva, Fabio Francesconi, Mauricio A. Pompilio, Adriana O. Franca, Valdir S. Amato, Regina M. Souza, Raquel V. C. Oliveira, Claudia M. Valete, Maria I. F. Pimentel
Summary: This study found that intralesional meglumine antimoniate (IL-MA) treatment for cutaneous leishmaniasis (CL) is noninferior to systemic MA (S-MA) and has less toxicity, making it a possible first-line therapy option.
CLINICAL INFECTIOUS DISEASES
(2023)
Review
Chemistry, Organic
Foroogh Mirzania, Javad Ghasemian Yadegari, Iraj Salimikia
Summary: This article reviews the research reports on naturally occurring diterpenoids extracted from plants with anti-leishmaniasis activity, providing an overview of the future of leishmaniasis drug discovery.
CURRENT ORGANIC CHEMISTRY
(2023)
Article
Chemistry, Medicinal
Nonkululeko H. Zuma, Janine Aucamp, Helena D. Janse van Rensburg, David D. N'Da
Summary: Leishmaniasis is a parasitic disease transmitted through vectors, primarily affecting populations in tropical and sub-tropical countries. The lack of a protective vaccine and limited availability of clinical drugs with high toxicity hinder the eradication and elimination of this disease. Multidrug resistant strains of the causative pathogens have further increased the need for new and effective antileishmanial drugs. In this study, nitrofurantoin, a clinical antibiotic, was chemically linked to a triazole scaffold using alkylene linkers of varying lengths, and the resulting hybrids showed promising in vitro antileishmanial activity against two strains of Leishmania parasites. Hybrid 13, containing a n-pentylene linker, exhibited micromolar activity against antimonial-resistant L. donovani, the causative agent of deadly visceral Leishmaniasis.
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
(2023)
Article
Infectious Diseases
Kaio Maciel De Santiago-Silva, Bruna Taciane da Silva Bortoleti, Laudicea do Nascimento Oliveira, Fernanda Lima de Azevedo Maia, Joyce Cristina Castro, Ivete Conchon Costa, Danielle Bidoia Lazarin, James L. Wardell, Solange M. S. Wardell, Magaly Girao Albuquerque, Camilo Henrique da Silva Lima, Wander Rogerio Pavanelli, Marcelle de Lima Ferreira Bispo, Raoni Schroeder B. Goncalves
Summary: Leishmaniasis is a neglected tropical disease with limited therapeutic options. In this study, new compounds were synthesized and evaluated for their biological activity against different forms of Leishmania parasites. Compound 4f showed the most promising results, exhibiting potent inhibitory effects on promastigotes and low toxicity to cells.
Article
Medicine, Research & Experimental
Guilherme S. Ramos, Virginia M. R. Vallejos, Marina S. Ladeira, Priscila G. Reis, Daniel M. Souza, Yuri A. Machado, Luiz O. Ladeira, Mauricio B. Pinheiro, Maria N. Melo, Ricardo T. Fujiwara, Frederic Frezard
Summary: The study found that fullerol has potential anti-leishmanial activity, especially when combined with liposomes, showing significant reduction in parasite load. This innovative approach provides a new potential method for treating VL.
BIOMEDICINE & PHARMACOTHERAPY
(2021)
Article
Immunology
Amrita Chakrabarti, Chintam Narayana, Nishant Joshi, Swati Garg, Lalit C. Garg, Anand Ranganathan, Ram Sagar, Soumya Pati, Shailja Singh
Summary: This study chemically synthesized a library of glycoside derivatives and evaluated their inhibitory efficacy against Leishmania donovani. The results showed that Gly2 had the highest inhibitory activity against promastigotes and strong binding affinity towards Gp63. In addition to its lethal effects on infectivity and multiplication, Gly2 also enhanced complement-mediated lysis and showed effectiveness against PKDL strain.
FRONTIERS IN CELLULAR AND INFECTION MICROBIOLOGY
(2022)
Article
Pharmacology & Pharmacy
Thayllan Teixeira Bezerra, Mayara Oliveira de Almeida, Nayane Maria de Amorim Lima, Naya Lucia de Castro Rodrigues, Viviane Gomes Pereira Ribeiro, Maria Jania Teixeira, Luigi Carbone, Giuseppe Mele, Diego Lomonaco, Selma Elaine Mazzetto
Summary: This study prepared green-based silver nanoparticles with cashew nutshell liquid and characterized their properties. The in vitro antileishmanial activity tests showed that cardol had high selectivity towards killing the parasite and should be further explored as a promising non-toxic treatment for cutaneous leishmaniasis.
INTERNATIONAL JOURNAL OF PHARMACEUTICS
(2022)
Article
Immunology
Lorena Bernardo, Jose Carlos Solana, Carmen Sanchez, Ana Torres, Eder Yaveth Reyes-Cruz, Eugenia Carrillo, Javier Moreno
Summary: Immunosuppressive treatment reduces the efficacy of pentavalent antimonials in patients by impeding parasite elimination and suppressing specific cellular immunity.
FRONTIERS IN IMMUNOLOGY
(2023)
Article
Instruments & Instrumentation
Lipika Ray, R. Karthik, Vikas Shrivastava, Sheelendra Pratap Singh, A. B. Pant, Neena Goyal, Kailash C. Gupta
Summary: A nanoformulation of AmB and Pip was developed, with controlled release properties and protection from acidic pH, showing enhanced drug bioavailability, non-nephrotoxic nature, and potential antileishmanial activity up to 96% inhibition of the parasite in vivo in the golden hamster-L. donovani model.
DRUG DELIVERY AND TRANSLATIONAL RESEARCH
(2021)
Article
Dermatology
Naghmeh Zabolinejad, Pouran Layegh, Zahra Abbasi Shaye, Maryam Salehi, Somayeh Ghanizadeh
Summary: This study evaluated the therapeutic effects of clarithromycin on leishmaniasis and found that oral clarithromycin had similar effects to systematic glucantime, suggesting it could be considered as a safe and effective treatment option.
JOURNAL OF DERMATOLOGICAL TREATMENT
(2022)
Article
Biochemistry & Molecular Biology
Mudassir Farooq, Faisal Usman, Sumera Zaib, Hamid Saeed Shah, Qazi Adnan Jamil, Fatima Akbar Sheikh, Ajmal Khan, Sameh Rabea, Soheir A. A. Hagras, Gaber El-Saber Batiha, Imtiaz Khan
Summary: Voriconazole-loaded transethosomes fabricated by TELs effectively improve drug solubility and skin permeation, enhancing efficacy. This transethosomal formulation can serve as an efficient drug delivery system through a topical route.
Article
Chemistry, Medicinal
Sonaly Lima Albino, Willian Charles da Silva Moura, Malu Maria Lucas dos Reis, Gleyton Leonel Silva Sousa, Pablo Rayff da Silva, Mayara Gabriele Carvalho de Oliveira, Tatiana Karla dos Santos Borges, Lucas Fraga Friaca Albuquerque, Sinara Monica Vitalino de Almeida, Maria do Carmo Alves de Lima, Selma Aparecida Souza Kuckelhaus, Igor Jose dos Santos Nascimento, Francisco Jaime Bezerra Mendonca Jr, Teresinha Goncalves da Silva, Ricardo Olimpio de Moura
Summary: The present study synthesized a new acridine derivative and characterized its chemical properties. Its potential as an antileishmanial agent was investigated through in vitro assays. The compound showed good antileishmanial activity and non-cytotoxicity to macrophages. It also exhibited a slight immunomodulatory activity and interacted with DNA, suggesting a potential molecular target.
Article
Parasitology
Yasmin Silva Rizk, Daiana de Jesus Hardoim, Kaique Bertrand Almeida Santos, Tania Zaverucha-do-Valle, Noemi Nosomi Taniwaki, Fernando Almeida-Souza, Carlos Alexandre Carollo, Marcos Andre Vannier-Santos, Carla Cardozo Pinto de Arruda, Katia da Silva Calabrese
Summary: Amentoflavone directly affects Leishmania parasites, leading to mitochondrial dysfunction and parasite death. Therefore, amentoflavone has the potential to be a promising candidate for the development of drugs against leishmaniasis.
PARASITOLOGY INTERNATIONAL
(2022)
Article
Chemistry, Medicinal
Joao Victor Silva-Silva, Carla J. Moragas-Tellis, Maria S. S. Chagas, Paulo Victor R. Souza, Davyson L. Moreira, Daiana J. Hardoim, Noemi N. Taniwaki, Vanessa F. A. Costa, Alvaro L. Bertho, Daniela Brondani, Eduardo Zapp, Aldo Sena de Oliveira, Katia S. Calabrese, Maria D. Behrens, Fernando Almeida-Souza
Summary: Carajurin, the main constituent of Arrabidaea chica, shows anti-Leishmania activity by affecting mitochondrial function and inducing reactive oxygen species production. The drug-likeness assessment of Carajurin also meets certain criteria of drug chemistry.
Article
Immunology
Juliane Siqueira Francisco, Marcia Andrea Barge Loucao Terra, Gabriel Couto Thurler Klein, Barbara Cristina Euzebio Pereira Dias de Oliveira, Marcelo Pelajo-Machado
Summary: This study revisits extramedullary hematopoiesis in the peripheral zone of murine hepatic schistosomal granulomas using new technical and conceptual approaches. The findings suggest that hematopoietic cells proliferate around trapped parasite eggs in the liver and around hepatic vessels. The microenvironment with acidic and sulfated glycoconjugates, reticular fibers, and the absence of fibronectin is identified as crucial for the attraction and maintenance of hematopoiesis. The study provides valuable insights into the pathology of schistosomiasis and the dynamics of hematopoiesis.
FRONTIERS IN IMMUNOLOGY
(2022)
Article
Microbiology
Estela Mariana Guimaraes Lourenco, Juliana Fortes Di Iorio, Fernanda da Silva, Felipe Leonardo Bley Fialho, Melquisedeque Mateus Monteiro, Adilson Beatriz, Renata Trentin Perdomo, Euzebio Guimaraes Barbosa, Jean Pierre Oses, Carla Cardozo Pinto de Arruda, Wagner Alves de Souza Judice, Jamal Rafique, Denis Pires de Lima
Summary: Leishmaniasis, a neglected tropical disease that affects more than 350 million people globally, currently lacks a vaccine and faces challenges in treatment. A multitarget drug strategy using flavonoid compounds shows promising prospects. In this study, 17 flavonoid analogues were synthesized using a scalable, easy-to-reproduce, and inexpensive method, all of which exhibited impressive inhibition against target enzymes highly expressed in the parasite. Compounds 3c, f12a, and f12b showed effectiveness against all tested isoforms and had low cytotoxicity. These results represent a pioneering advancement in understanding the mechanism of action of flavonoid derivatives against leishmaniasis and hold promise for the development of cysteine protease inhibitors for treatment.
Article
Chemistry, Medicinal
Diego B. Carvalho, Pedro A. N. Costa, Gisele B. Portapilla, Amarith R. das Neves, Cristiane Y. K. Shiguemoto, Bruno I. Pelizaro, Fernanda Silva, Eliane M. Piranda, Carla C. P. Arruda, Priscyla D. M. Gaspari, Iara A. Cardoso, Pedro H. Luccas, M. Cristina Nonato, Norberto P. Lopes, Sergio de Albuquerque, Adriano C. M. Baroni
Summary: Chagas disease and leishmaniasis are neglected diseases of high priority as a public health problem. In this study, a series of newly synthesized compounds showed promising antitrypanosomatid properties, indicating their potential as future treatments for these diseases.
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
(2023)
Editorial Material
Multidisciplinary Sciences
Kirk R. Johnson, Ian F. P. Owens
Article
Virology
Ieda Pereira Ribeiro, Lilian Goncalves do Nascimento, Luis Fernando Lopez Tort, Elisa Cavalcante Pereira, Lidiane Souza Raphael Menezes, Fabio Correia Malta, Barbara Cristina Euzebio Pereira Dias de Oliveira, Joao Paulo Rodrigues, Pedro Paulo de Abreu Manso, Marcelo Pelajo, Myrna Cristina Bonaldo, Paola Cristina Resende Silva, Marilda Mendonca Siqueira, Patricia Brasil, Tulio Machado Fumian
Summary: The study investigated the dynamic of SARS-CoV-2 viral excretion in rectal swab, saliva, and nasopharyngeal swab samples from symptomatic patients and asymptomatic contacts. It also evaluated the replication potential of SARS-CoV-2 in the gastrointestinal tract and the excretion of infectious SARS-CoV-2 from feces. The presence of replicating SARS-CoV-2 was found in a small percentage of rectal swab samples, while infectious SARS-CoV-2 was identified in only one sample. The study highlights the need for further research on fecal-oral transmission of SARS-CoV-2.
Article
Chemistry, Medicinal
Amarith R. das Neves, Diego B. Carvalho, Fernanda Silva, Rafael F. Rosalem, Bruno I. Pelizaro, Pamella F. Castilho, Kelly M. P. Oliveira, Nadla S. Cassemiro, Lucas R. Pessatto, Edgar J. Paredes-Gamero, Eliane M. Piranda, Denise B. Silva, Carla C. P. Arruda, Adriano C. M. Baroni
Summary: This study evaluated the in vivo intralesional treatment efficacy of five isoxazole derivatives and found that analogue 7 showed promising therapeutic effects and low toxicity. It could be a potential new drug candidate for CL caused by L. amazonensis.
ACS INFECTIOUS DISEASES
(2023)
Article
Biology
Sandra Alves de Araujo, Aldilene da Silva Lima, Claudia Quintino da Rocha, Henrique Previtalli-Silva, Daiana de Jesus Hardoim, Noemi Nosomi Taniwaki, Katia da Silva Calabrese, Fernando Almeida-Souza, Ana Lucia Abreu-Silva
Summary: This study verifies the antioxidant properties and efficacy against Chagas disease of the ethyl acetate fraction obtained from Terminalia catappa leaves. The ethyl acetate fraction showed the best inhibitory activity against the parasite responsible for Chagas disease and did not cause toxicity to host cells. Therefore, it can be considered an effective alternative for the treatment and control of Chagas disease.
Article
Chemistry, Medicinal
Estela M. G. Lourenco, Fernanda da Silva, Amarith R. das Neves, Iluska S. Bonfa, Alda Maria T. Ferreira, Adriana C. G. Menezes, Maria E. C. da Silva, Jessica T. dos Santos, Marco A. U. Martines, Renata T. Perdomo, Monica C. Toffoli-Kadri, Euzebio G. Barbosa, Sumbal Saba, Adilson Beatriz, Jamal Rafique, Carla C. P. de Arruda, Denis P. de Lima
Summary: Leishmaniases are neglected tropical diseases that have devastating health, social, and economic consequences. Current antileishmanial drugs are old, toxic, and unaffordable. A study synthesized 17 flavonoid derivatives and found that 11 of them showed high activity against the parasite and were safe for host cells.
ACS INFECTIOUS DISEASES
(2023)
Article
Pharmacology & Pharmacy
Steven Souza Paes, Joao Victor Silva-Silva, Paulo Wender Portal Gomes, Luely Oliveira da Silva, Ana Paula Lima da Costa, Manoel Leao Lopes Junior, Daiana de Jesus Hardoim, Carla J. Moragas-Tellis, Noemi Nosomi Taniwaki, Alvaro Luiz Bertho, Fabio Alberto de Molfetta, Fernando Almeida-Souza, Lourivaldo Silva Santos, Katia da Silva Calabrese
Summary: This study investigated the antileishmanial activity of (-)-5-demethoxygrandisin B, a compound isolated from Virola surinamensis, against Leishmania amazonensis. The results showed that the compound exhibited inhibitory effects on both the promastigote and intracellular amastigote forms of the parasite, possibly through its interaction with the TryR enzyme. The compound induced ultrastructural changes in the parasites and reduced the mitochondrial membrane potential.
Article
Multidisciplinary Sciences
Barbara Cristina Marcollino Bomfim, Jessyca Azevedo-Silva, Giulia Caminha, Joao Paulo Rodrigues Santos, Marcelo Pelajo-Machado, Jackline de Paula Ayres-Silva
Summary: Hematopoiesis is the process of blood cell generation and migration throughout different organs until reaching the bone marrow. The fetal liver plays a crucial role in hematopoiesis, with megakaryocytes undergoing proliferation and differentiation. This study aimed to characterize and quantify the glycan residues of fetal megakaryocytic cells in the mouse fetal liver at different gestational ages using lectins. The results showed the expression of various sugar residues and the occurrence of proliferation waves in megakaryocytes during liver development. Additionally, lectins proved to be a useful alternative to antibodies for displaying liver structures and megakaryocyte differentiation.
SCIENTIFIC REPORTS
(2023)
Article
Biochemistry & Molecular Biology
Edlainne Pinheiro Ferreira-Sena, Daiana de Jesus Hardoim, Flavia de Oliveira Cardoso, Luiz Ney d'Escoffier, Isabela Ferreira Soares, Joao Pedro Rangel da Silva Carvalho, Ricardo Almir Angnes, Stenio Perdigao Fragoso, Carlos Roberto Alves, Salvatore Giovanni De-Simone, Josue da Costa Lima-Junior, Alvaro Luiz Bertho, Tania Zaverucha-do-Valle, Franklin Souza da Silva, Katia da Silva Calabrese
Summary: Leishmaniasis is a complex and diverse disease that is considered a major public health problem. Despite the availability of treatment options, there are currently no vaccines for cutaneous leishmaniasis. This study focused on the prediction and characterization of antigenic epitopes that could interact with major histocompatibility complex class I in mice or humans. Through a combination of immunogenicity prediction and interaction assays, nine antigenic peptides were identified as strong candidates for the development of a peptide vaccine against leishmaniasis.
INTERNATIONAL JOURNAL OF MOLECULAR SCIENCES
(2023)