In vitro evaluation of alkaline lignins as antiparasitic agents and their use as an excipient in the release of benznidazole

Copyright © 2023. Published by Elsevier B.V.The Amazon rainforest is considered the largest tropical timber reserve in the world. The management of native forests in the Amazon is one of the most sensitive geopolitical issues today, given its national and international dimension. In this work, we obtained and characterized physicochemical lignins extracted from branches and leaves of Protium puncticulatum and Scleronema micranthum. In addition, we evaluated in vitro its potential as an antioxidant, cytotoxic agent against animal cells and antiparasitic against promastigotes of Leishmania amazonensis, trypomastigotes of T. cruzi and against Plasmodium falciparum parasites sensitive and resistant to chloroquine. The results showed that the lignins obtained are of the GSH type and have higher levels of guaiacyl units. However, they show structural differences as shown by spectroscopic analysis and radar charts. As for biological activities, they showed antioxidant potential and low cytotoxicity against animal cells. Antileishmanial/trypanocidal assays have shown that lignins can inhibit the growth of promastigotes and trypomastigotes in vitro. The lignins in this study showed low anti-Plasmodium falciparum activity against susceptible strains of Plasmodium falciparum and were able to inhibit the growth of the chloroquine-resistant strain. And were not able to inhibit the growth of Schistosoma mansoni parasites. Finally, lignins proved to be promising excipients in the release of benznidazole. These findings show the potential of these lignins not yet studied to promote different biological activities.publishersversionpublishe

ULTRASTRUCTURAL CHANGES IN Schistosoma mansoni MALE WORMS AFTER in vitro INCUBATION WITH THE ESSENTIAL OIL OF Mentha x villosa Huds

Introduction: The essential oil Mentha x villosa (MVEO) has a wide range of actions, including antibacterial, antifungal, antiprotozoal and schistosomicidal actions. The present study aimed to investigate the ultrastructural changes of MVEO on the tegument of adult Schistosoma mansoni. Materials and Methods: Different concentrations of MVEO were tested on S. mansoni adult worms in vitro. Ultrastructural changes on the tegument of these adult worms were evaluated using scanning electron microscopy (SEM) and transmission electron microscopy (TEM). Results: The MVEO caused the death of all worms at 500 μg mL-1 after 24 h. After 24h of 500 μg mL-1 MVEO treatment, bubble lesions were observed over the entire body of worms and they presented loss of tubercles in some regions of the ventral portion. In the evaluation by TEM, S. mansoni adult worms treated with MVEO, 500 μg mL-1, presented changes in the tegument and vacuoles in the syncytial matrix region. Glycogen granules close to the muscle fibers were visible. Conclusion: The ability of MVEO to cause extensive ultrastructural damage to S. mansoni adult worms correlates with its schistosomicidal effects and confirms earlier findings with S. mansoni

Insect/Bt-cotton interactions: Are immunological variables and hemocyte ultrastructure in Podisus nigrispinus (Hemiptera: Pentatomidae) affected?

Recent studies have shown that ingestion by the army worm Spodoptera frugiperda of Cry1Ac toxin from Bt cotton promotes histochemical and ultrastructural changes in the digestive cells of the predatory pentatomid bug Podisus nigrispinus. Therefore, mindful of the changes in the midgut of the predator, which represents the first line of defence in this insect, our aim was to test the hypothesis that the consumption of Bt cotton-fed S. frugiperda by P. nigrispinus might lead to alterations in components of the immune system of P. nigrispinus. The Cry1Ac toxin level in the leaves of Bt cotton, nitric oxide, phenoloxidase activity, and total proteins were quantified by ELISA. Total and differential hemocyte counts were evaluated, and hemocyte ultrastructure analysis was undertaken. We found that ingestion of the prey fed daily with approximately 23 ± 0.70 ng g-1 Cry1Ac by wet weight of leaves, and expressed by the Bt cotton, induces small ultrastructural changes in the predator's granulocytes and plasmatocytes. However, these changes did not affect the total number and differential and humoral variables analyzed for the bug's hemocytes. © 2013 Copyright Taylor and Francis Group, LLC

Ultrastructure of the antennal sensilla of Alabama argillacea (Hübner, 1823) (Lepidoptera: Erebidae)

Insects have several types of sensilla, the characterization of which has been fundamental to understanding the mechanisms of sensory perception in different species. This study aimed to describe the ultrastructure of the sensilla present on the antennae of Alabama argillacea (Hübner, 1823) (Lepidoptera: Erebidae), an important pest of cotton (Gossypium hirsutum L.) crops, as well as their possible variation between sexes. To do this, the antennae of males and females of A. argillacea were analyzed using scanning electron microscopy. Sensilla morphometry was assessed using photomicrographs, from which the lengths and basal and apical diameters of sensilla were measured using the ImageJ program. Seven types of sensilla were identified on the antennae of A. argillacea: sensilla trichodea, sensilla chaetica, sensilla auricillica, sensilla coeloconica, sensilla styloconica, sensilla basiconica, and sensilla Böhm bristles. Differences between the sensilla of males and females were found in their lengths and basal diameters in the distal and proximal regions. This suggests that sensilla functionality may not only vary from one species to another, but also between sexes within the same species. Thus, further transmission electron microscopy and single sensillum recording studies may provide more detailed information on the sensilla of A. argillacea and their functions. Keywords: Antenna, Cotton leafworm, Morphometry, Scanning electron microscop

Ultrastructural study of morphological changes in Schistosoma mansoni after in vitro exposure to the monoterpene rotundifolone

Submitted by Adagilson Silva ([email protected]) on 2017-06-21T18:45:16Z No. of bitstreams: 1 28327807 2017 mat-ult.oa.pdf: 1935700 bytes, checksum: 34f74a286f98660e097d361e8d522ca9 (MD5)Approved for entry into archive by Adagilson Silva ([email protected]) on 2017-06-21T19:22:48Z (GMT) No. of bitstreams: 1 28327807 2017 mat-ult.oa.pdf: 1935700 bytes, checksum: 34f74a286f98660e097d361e8d522ca9 (MD5)Made available in DSpace on 2017-06-21T19:22:49Z (GMT). No. of bitstreams: 1 28327807 2017 mat-ult.oa.pdf: 1935700 bytes, checksum: 34f74a286f98660e097d361e8d522ca9 (MD5) Previous issue date: 2017Fundação Oswaldo Cruz. Instituto Aggeu Magalhães. Departamento de Parasitologia, Laboratório de Biologia Celular e Molecular. Recife, PE, Brasil / Universidade Federal de Pernambuco. Laboratório de Imunopatologia Keizo Asami. Recife, PE, Brasil.Fundação Oswaldo Cruz. Instituto Aggeu Magalhães. Departamento de Parasitologia, Laboratório de Biologia Celular e Molecular. Recife, PE, Brasil / Universidade Federal de Pernambuco. Laboratório de Imunopatologia Keizo Asami. Recife, PE, Brasil.Universidade Federal da Paraíba. João Pessoa, PB, Brasil.Universidade Federal da Paraíba. João Pessoa, PB, Brasil.Fundação Oswaldo Cruz. Instituto Aggeu Magalhães. Departamento de Parasitologia, Laboratório de Biologia Celular e Molecular. Recife, PE, Brasil / Universidade Federal de Pernambuco. Laboratório de Imunopatologia Keizo Asami. Recife, PE, Brasil.Instituto Agronômico de Campinas. Centro de Pesquisa e Desenvolvimento de Recursos Genéticos Vegetais. Campinas, São Paulo, Brasil.Fundação Oswaldo Cruz. Instituto Aggeu Magalhães. Departamento de Parasitologia, Laboratório de Biologia Celular e Molecular. Recife, PE, Brasil / Universidade Federal de Pernambuco. Laboratório de Imunopatologia Keizo Asami. Recife, PE, Brasil.Fundação Oswaldo Cruz. Instituto Aggeu Magalhães. Departamento de Parasitologia, Laboratório de Biologia Celular e Molecular. Recife, PE, Brasil / Universidade Federal de Pernambuco. Laboratório de Imunopatologia Keizo Asami. Recife, PE, Brasil.Schistosomiasis, a parasitic disease caused by trematode flatworms of the genus Schistosoma, affects more than 200 million people worldwide, and its control is dependent on a single drug, praziquantel. Here, we report the in vitro effect of rotundifolone, a monoterpene isolated from Mentha x villosa (Lamiaceae), on Schistosoma mansoni adult worms

Ultrastructural study of morphological changes in Schistosoma mansoni after in vitro exposure to the monoterpene rotundifolone

ABSTRACT INTRODUCTION: Schistosomiasis, a parasitic disease caused by trematode flatworms of the genus Schistosoma, affects more than 200 million people worldwide, and its control is dependent on a single drug, praziquantel. Here, we report the in vitro effect of rotundifolone, a monoterpene isolated from Mentha x villosa (Lamiaceae), on Schistosoma mansoni adult worms. METHODS: The in vitro effect of rotundifolone on adult Schistosoma mansoni was evaluated by analysis of behavior and mortality and through a scanning electron microscopic analysis of ultrastructural changes in the tegument of the worms. RESULTS: At concentrations of 3.54 and 7.09μg/mL-1 rotundifolone, no worm mortality was observed at any of the sampling intervals. A minor reduction in movement of the tail, suckers, and gynecophoral canal membrane was observed after 96 h of exposure to 7.09μg/mL-1 rotundifolone. At 70.96μg/mL-1, a lack of movement was observed from 72h onwards and all worms were deemed dead; similar effects were observed at 48h with 177.4μg/mL-1, and at 24h with 354.8μg/mL-1 and 700.96μg/mL-1. Rotundifolone also caused death of all parasites and separation of coupled pairs into individual males and females after 24h at 354.8μg/mL-1. CONCLUSIONS: The main changes in the tegument induced by the different ROT treatments were: after 24h incubation, bubble lesions spread over the entire body and loss of tubercles occurred in some regions of the ventral region

Estudo ultraestrutural das alterações morfológicas de vermes machos de Schistosoma mansoni após exposição in vitro à alicina

Submitted by Ana Beatriz Oliveira ([email protected]) on 2019-01-22T12:42:12Z No. of bitstreams: 1 Ultrastructural study on the morphological changes to male worms of Schistosoma mansoni afer in vitro exposure to allicin.pdf: 1564268 bytes, checksum: 5261189754690c763da4eb7ce00e709e (MD5)Approved for entry into archive by Ana Beatriz Oliveira ([email protected]) on 2019-01-22T13:09:25Z (GMT) No. of bitstreams: 1 Ultrastructural study on the morphological changes to male worms of Schistosoma mansoni afer in vitro exposure to allicin.pdf: 1564268 bytes, checksum: 5261189754690c763da4eb7ce00e709e (MD5)Made available in DSpace on 2019-01-22T13:09:25Z (GMT). No. of bitstreams: 1 Ultrastructural study on the morphological changes to male worms of Schistosoma mansoni afer in vitro exposure to allicin.pdf: 1564268 bytes, checksum: 5261189754690c763da4eb7ce00e709e (MD5) Previous issue date: 2011Universidade Federal da Paraíba. Departamento de Fisiologia e Patologia. João Pessoa, PB, Brasil.Universidade Federal da Paraíba. Departamento de Ciências Farmacêuticas. João Pessoa, PB, Brasil.Universidade Federal da Paraíba. Departamento de Fisiologia e Patologia. João Pessoa, PB, Brasil.Universidade Federal da Paraíba. Departamento de Fisiologia e Patologia. João Pessoa, PB, Brasil.Universidade de Pernambuco. Departamento de Biologia Celular. Recife, PE, Brasil.Universidade Federal de Pernambuco. Laboratório de Microscopia Eletrônica. Laboratório de Imunopatologia Keizo Asami. Recife, PE, Brasil.Fundação Oswaldo Cruz. Instituto Aggeu Magalhães. Departamento de Parasitologia. Recife, PE, Brasil.Universidade Federal de Pernambuco. Laboratório de Microscopia Eletrônica. Laboratório de Imunopatologia Keizo Asami. Recife, PE, Brasil / Fundação Oswaldo Cruz. Instituto Aggeu Magalhães. Departamento de Parasitologia. Recife, PE, Brasil.Universidade de Pernambuco. Departamento de Biologia Celular. Recife, PE, Brasil / Universidade Federal de Pernambuco. Laboratório de Microscopia Eletrônica. Laboratório de Imunopatologia Keizo Asami. Recife, PE, Brasil / Fundação Oswaldo Cruz. Instituto Aggeu Magalhães. Departamento de Parasitologia. Recife, PE, Brasil.Universidade Federal da Paraíba. Departamento de Ciências Farmacêuticas. João Pessoa, PB, Brasil.INTRODUÇÃO: O alho apresenta uma ampla gama de ações, incluindo antibacteriana, antiviral, antifúngico, antiprotozoário e anti-helmíntico. Esta atividade antiparasitária tem sido atribuída à alicina, que é o principal constituinte do alho. O presente estudo teve como objetivo investigar a ação in vitro da alicina no tegumento de vermes adultos de Schistosoma mansoni utilizando a microscopia eletrônica de varredura. MÉTODOS: Camundongos Swiss Webster foram infectados com cercárias de S. mansoni (100 por camundongo) e sacrificados 50 dias depois para aquisição de vermes adultos. Estes vermes foram coletados por perfusão e colocados em meio RPMI 1.640 a 37°C antes de transferir para o meio RPMI contendo 0 (controle), 5, 10, 15 e 20mg/mL de alicina, onde eles foram incubados por 2h. Os vermes foram fixados em uma solução de glutaraldeído a 2,5%, lavados duas vezes, pós-fixados em tetróxido de ósmio, lavados duas vezes e então desidratados em séries crescentes de etanol. As amostras foram secadas, montadas em stubs, metalizadas em ouro e visualizadas utilizando o microscópio eletrônico de varredura. RESULTADOS: A concentração de 5mg/mL causou o enrugamento do tegumento; a concentração de 10mg/mL resultou em alterações nos tubérculos e perda ou modificações nos espinhos. Com 15 e 20mg/mL crescentes danos no tegumento pode ser visto, tais como formação de vesículas e presença de úlceras. CONCLUSÕES: Esses resultados demonstram os efeitos da alicina nos vermes adultos de S. mansoni e indicam que a maioria das alterações ocorrem numa concentração maior do que a normalmente indicada para o tratamento.INTRODUCTION: Garlic has a wide range of actions, including antibacterial, antiviral, antifungal, antiprotozoal and anthelmintic actions. This antiparasitic activity has been attributed to allicin, which is the main constituent of garlic. The present study aimed to investigate the in vitro activity of allicin on the tegument of adult Schistosoma mansoni worms using scanning electron microscopy. METHODS: Swiss Webster mice were infected with S. mansoni cercariae (100 per mouse) and sacrificed 50 days later to acquire the adult worms. These worms were collected by perfusion and placed in RPMI medium 1,640 at 37°C before transferring to RPMI media containing 0 (control), 5, 10, 15 and 20mg/mL of allicin, where they were incubated for 2h. The worms were fixed in 2.5% glutaraldehyde solution, washed twice, post-fixed in osmium tetroxide, washed twice and then dehydrated with ascending grades of ethanol. The samples were air-dried, mounted on stubs, gold coated in an ion sputtering unit and viewed using a scanning electron microscope. RESULTS: A concentration of 5mg/mL caused wrinkling in the tegument; a concentration of 10mg/mL resulted in changes to tubercles and loss or modification of spines. With 15 and 20mg/mL increasing damage to the tegument could be seen, such as vesicle formation and the presence of ulcers. CONCLUSIONS: These findings demonstrate the effect of allicin on adult S. mansoni worms and indicate that most of the changes occur at concentrations greater than that normally indicated for treatment

New 1,3-thiazole derivatives and their biological and ultrastructural effects on Trypanosoma cruzi

Submitted by Ana Maria Fiscina Sampaio ([email protected]) on 2016-12-13T14:26:25Z No. of bitstreams: 1 Gomes PATM New 1,3-thiazole derivatives....pdf: 2013088 bytes, checksum: 8ca722694d65ed4ac9b209d95a69248c (MD5)Approved for entry into archive by Ana Maria Fiscina Sampaio ([email protected]) on 2016-12-13T16:21:46Z (GMT) No. of bitstreams: 1 Gomes PATM New 1,3-thiazole derivatives....pdf: 2013088 bytes, checksum: 8ca722694d65ed4ac9b209d95a69248c (MD5)Made available in DSpace on 2016-12-13T16:21:46Z (GMT). No. of bitstreams: 1 Gomes PATM New 1,3-thiazole derivatives....pdf: 2013088 bytes, checksum: 8ca722694d65ed4ac9b209d95a69248c (MD5) Previous issue date: 2016CNPq; CAPES; PRONEX-FAPESB; PRONEM/FACEPE/CNPq.Universidade Federal de Pernambuco. Centro de Ciências da Saúde. Departamento de Ciências Farmacêuticas. Recife, PE, BrasilUniversidade Federal de Pernambuco. Centro de Ciências da Saúde. Departamento de Ciências Farmacêuticas. Recife, PE, BrasilUniversidade Federal de Pernambuco. Centro de Ciências da Saúde. Departamento de Ciências Farmacêuticas. Recife, PE, BrasilUniversidade de Pernambuco. Petrolina, PE, BrasilUniversidade Federal de Pernambuco. Centro de Ciências da Saúde. Departamento de Ciências Farmacêuticas. Recife, PE, BrasilUniversidade Federal de Pernambuco. Centro de Ciências da Saúde. Departamento de Ciências Farmacêuticas. Recife, PE, BrasilFundação Oswaldo Cruz. Centro de Pesquisas Gonçalo Moniz. Salvador, BA, BrasilFundação Oswaldo Cruz. Centro de Pesquisas Aggeu Magalhães. Recife, PE, BrasilFundação Oswaldo Cruz. Centro de Pesquisas Aggeu Magalhães. Recife, PE, BrasilFundação Oswaldo Cruz. Centro de Pesquisas Aggeu Magalhães. Recife, PE, BrasilFundação Oswaldo Cruz. Centro de Pesquisas Aggeu Magalhães. Recife, PE, BrasilMinistry of Education of Brazil. CAPES Foundation. Brasília, DF, Brasil / Universidade Federal de Minas Gerais. Departamento de Bioquímica e Imunologia. Belo Horizonte, MG, BrasilUniversidade Federal de Minas Gerais. Departamento de Bioquímica e Imunologia. Belo Horizonte, MG, BrasilUniversidade Federal de Pernambuco. Centro de Ciências da Saúde. Departamento de Ciências Farmacêuticas. Recife, PE, BrasilIn previous studies, the compound 3-(bromopropiophenone) thiosemicarbazone was described as a potent anti-Trypanosoma cruzi and cruzain inhibitor. In view to optimize this activity, 1,3-thiazole core was used as building-block strategy to access new lead generation of anti T. cruzi agents. In this way a series of thiazole derivatives were synthesized and most of these derivatives exhibited antiparasitic activity similar to benznidazole (Bzd). Among them, compounds (1c) and (1g) presented better selective index (SI) than Bzd. In addition, compounds showed inhibitory activity against the cruzain protease. As observed by electron microscopy, compound (1c) treatment caused irreversible and specific morphological changes on ultrastructure organization of T. cruzi, demonstrating that this class of compounds is killing parasites