Proteases de Leishmania: novos alvos para o desenvolvimento racional de fármacos

Leishmania causes tegumental and visceral diseases called leishmaniasis. Disease control is possible interrupting the transmission cycle, but HIV co-infection, chemotheraphy toxicity and lack of a vaccine are paramount difficulties. So, is necessary to study new Leishmania molecules and investigate the possibility to develop rational drugs using these molecules as targets. Leishmania express many peptidases during their life, and cysteine are the most abundant protease and many inhibitors were developed but failed to kill parasites. On the other hand, inhibitors of serine proteases killed promastigotes, indicating the possibility of these enzymes to be important targets in the development of anti-Leishmania drugs

Protease inhibitor activity of plant natural products as leishmanicine agents / Atividade de inibidores de proteases de produtos naturais contra agentes leishmanicidas

Objective: Investigate plant natural products with inhibitory activity of Leishmania proteases, because the inhibition of certain proteases induce the parasite death. Methods: Descriptive/exploratory study, integrative review type. The search was performed in the following databases: Scientific Electronic Library OnLine (SciELO), Medical Literature Analysis and Retrieval System Online (MEDLINE), Latin American and Caribbean Health Science Literature Database (LILACS) and PUBMED. The descriptors were used in combination, from the consultation in the Descriptors in Health Sciences (DECS) and Medical Subject Headings (MeSH), were: (Leishmania) AND (Protease Inhibitor) AND (Vegetable extracts); (Leishmania) AND (Protease Inhibitor) AND (Plant Extracts). Studies in English and Portuguese, published between 2000 and 2020, were included. Finally, the articles were categorized and analyzed. Results and discussion: This review included eight studies, published between 2000 and 2020. There were two publications in 2014, 2017 and 2019, in relation to the language, all eight studies were published in English. Five studies were carried out in India, two in Brazil and one in Iran. Seven of these were found in PUBMED database and one from MEDLINE, all were experimental, comprising in vitro research or using mice as animal models. Conclusions: It was noted that they use similar protocols for the isolation of protease inhibitor from plant species (affinity chromatography) and proteases from Leishmania sp. (cell lysis and protein precipitation and affinity chromatography). However, research involving Leishmania protease inhibitors are still scarce, requiring further studies on the subject, since the understanding of the functioning of these molecules has much to contribute to the development of new therapeutic targets

Antileishmanial effects of Crotalaria spectabilis Roth aqueous extracts on Leishmania amazonensis

Abstract Fifteen polar extracts from leaf, seed, pod, stem, flower and root of Crotalaria spectabilis were prepared using aqueous systems, based on the principles of green chemistry, and showed different protease inhibitor (PI) activities on trypsin, papain, pepsin and the extracellular L. amazonensis serine protease (LSPIII). The most pronounced inhibitory effect on LSPIII was observed in leaf (CS-P), root, stem, flower (CS-FPVPP) and pod (CS-VA) extracts. Crotalaria extracts exhibited low cytotoxicity on macrophages; however, they decreased the viability of L. amazonensis promastigotes and amastigotes, as observed in leaf (CS-AE, CS-P, CS-T and CS-PVPP), seed (CS-ST), flower and root (CS-RA) extracts. CS-P was chosen to study PI and secondary metabolites and a 10-12 kDa protein, analyzed by mass spectrometry, was identified as a serine PI homologous with papaya latex serine PI. Glycosylated flavonoids, such as quercetins, vitexin and tricin were the major secondary metabolites of CS-P. The presence of PIs in C. spectabilis is a new finding, especially in other organs than seeds since PIs have been reported only in seed legumes. Besides, this is the first report of antileishmanial activity of C. spectabilis extracts and the identification of serine polypeptide PI and glycosylated flavonoids from leaf

Canavalia ensiformis (L. ) DC ( Fabaceae )

Submitted by Angelo Silva ([email protected]) on 2016-07-20T12:52:00Z No. of bitstreams: 2 license.txt: 1748 bytes, checksum: 8a4605be74aa9ea9d79846c1fba20a33 (MD5) 5.pdf: 200521 bytes, checksum: 57c05d7f6584e5e09f7a6463dd751c7c (MD5)Approved for entry into archive by Michelle Lanzellote ([email protected]) on 2016-07-27T12:05:10Z (GMT) No. of bitstreams: 2 5.pdf: 200521 bytes, checksum: 57c05d7f6584e5e09f7a6463dd751c7c (MD5) license.txt: 1748 bytes, checksum: 8a4605be74aa9ea9d79846c1fba20a33 (MD5)Made available in DSpace on 2016-07-27T12:05:30Z (GMT). No. of bitstreams: 2 5.pdf: 200521 bytes, checksum: 57c05d7f6584e5e09f7a6463dd751c7c (MD5) license.txt: 1748 bytes, checksum: 8a4605be74aa9ea9d79846c1fba20a33 (MD5) Previous issue date: 2012Fundação Oswaldo Cruz. Instituto de Tecnologia em Fármacos. Laboratório de Química de Produtos Naturais. Rio de Janeiro, RJ, Brasil.A Canavalia ensiformis é uma leguminosa com ampla distribuição tropical. É bastante utilizada em agricultura como cobertura verde para enriquecer o solo de nutrientes. Devido ao seu elevado valor nutricional suas sementes são empregadas na alimentação do gado e suas folhas na alimentação humana. Ela é bastante resistente às variações das condições ambientais, insetos e microorganismos. Seus principais componentes biologicamente ativos são proteínas, peptídeos, enzimas ou derivados de aminoácidos e dentre os quais é importante chamar a atenção para concanavalina A, urease, canatoxina, jaburetox, serino-proteases e L-canavanina / L-canalina. Estes compostos apresentam importantes funções bioquímicas e suas atividades biológicas têm sido objeto de intensas investigações. Além disso, estes principais componentes purificados de sementes de C. ensiformis exercem importantes efeitos farmacológicos, auxiliando assim na compreensão da fisiologia dos organismos, como também no tratamento de diversas patologias.Canavalia ensiformis is a widely distributed tropical legume. It is extensively used in agriculture as a green cover for the nutritional enrichment of soils. Due to the high nutritional values the seeds are used to feed cattle and the leaves are food for humans. It is quite resistant to changes in environmental conditions, insects and microorganisms. The major compounds of C. ensiformis are biologically active proteins, peptides, enzymes or amino acid derivatives. Among these compounds it is important to mention concanavalin A, ureases, canatoxin, jaburetox, serine proteases, glycosidases and L-canavanina/L-canalina. These compounds play important biochemical roles in the plant and, their activities have been the subject of intense investigations. In addition, these major compounds extracted from seeds of C. ensiformis have important pharmacological effects, thereby aiding in the undestanding of physiology of organisms and in the treatment of various pathologies

Genus Crotalaria L. (Leguminoseae)

Submitted by Gilvan Almeida ([email protected]) on 2016-08-29T19:06:32Z No. of bitstreams: 2 license.txt: 1748 bytes, checksum: 8a4605be74aa9ea9d79846c1fba20a33 (MD5) 31.pdf: 311791 bytes, checksum: 6dbdb5c66ef81fc5a4f59deb066ff2b0 (MD5)Approved for entry into archive by Michelle Lanzellote ([email protected]) on 2016-09-19T19:53:19Z (GMT) No. of bitstreams: 2 license.txt: 1748 bytes, checksum: 8a4605be74aa9ea9d79846c1fba20a33 (MD5) 31.pdf: 311791 bytes, checksum: 6dbdb5c66ef81fc5a4f59deb066ff2b0 (MD5)Made available in DSpace on 2016-09-19T19:53:31Z (GMT). No. of bitstreams: 2 license.txt: 1748 bytes, checksum: 8a4605be74aa9ea9d79846c1fba20a33 (MD5) 31.pdf: 311791 bytes, checksum: 6dbdb5c66ef81fc5a4f59deb066ff2b0 (MD5) Previous issue date: 2010-09Fundação Oswaldo Cruz. Instituto de Tecnologia em Fármacos. Laboratório de Química de Produtos Naturais. Rio de Janeiro, RJ, Brasil.Fundação Oswaldo Cruz. Instituto de Tecnologia em Fármacos. Laboratório de Química de Produtos Naturais. Rio de Janeiro, RJ, Brasil.As leguminosas do gênero Crotalaria são nativas da Índia, com ampla adaptação às regiões tropicais do mundo. O nome Crotalaria refere-se ao chocalho das vagens secas, semelhante ao da cobra cascavel (Crotalus sp.). São arbustos de crescimento ereto e determinado e seu principal emprego é a adubação verde. Além disso, também podem ser usadas como plantas-armadilhas em solos infestados por nematóides e em regiões endêmicas da Dengue, na fixação do nitrogênio em sistemas de cultivo rotativo e na indústria de papel e fibras. Apesar da grande toxicidade de suas sementes, devido a presença de alcalóides pirrolizidínicos, inibidores de proteases e outros compostos, muitas moléculas têm sido isoladas e purificadas e seus potenciais de aplicação estudados. Diversos extratos de algumas espécies de Crotalaria foram ensaiados contra bactérias, insetos e parasitos e os resultados foram bastante promissores. Este trabalho tem como objetivo compilar estes resultados e discutir as possíveis aplicações biotecnológicas da Crotalaria.Legumes of the genus Crotalaria are native to India, with broad adaptation to tropical regions of the world. The name of Crotalaria refers to the rattle of dry pods, similar to the rattlesnake (Crotalus sp.). They are shrubs growing upright and determined, and its main job is the green manure. Furthermore, they can also be used as trap plants in soils infested with nematodes in endemic regions of Dengue in nitrogen fixation in crop rotation systems, industry and paper fibers and phytoremediation. Despite the high toxicity of its seeds due to presence of monocrotaline, protease inhibitors and other compounds, many molecules have been isolated and purified and its potential application has been studied. Extracts of some Crotalaria species were tested against bacteria, insects and parasites and the results were very promising. This paper aims to compile these results and discuss the possible biotechnological applications of Crotalaria

Bauhinia forficata Link (Fabaceae)

Submitted by Gilvan Almeida ([email protected]) on 2016-08-29T19:06:34Z No. of bitstreams: 2 license.txt: 1748 bytes, checksum: 8a4605be74aa9ea9d79846c1fba20a33 (MD5) 9.pdf: 268669 bytes, checksum: 409728fcaeb75814c914f78c124bb376 (MD5)Approved for entry into archive by Michelle Lanzellote ([email protected]) on 2016-09-19T13:01:44Z (GMT) No. of bitstreams: 2 license.txt: 1748 bytes, checksum: 8a4605be74aa9ea9d79846c1fba20a33 (MD5) 9.pdf: 268669 bytes, checksum: 409728fcaeb75814c914f78c124bb376 (MD5)Made available in DSpace on 2016-09-19T13:02:09Z (GMT). No. of bitstreams: 2 license.txt: 1748 bytes, checksum: 8a4605be74aa9ea9d79846c1fba20a33 (MD5) 9.pdf: 268669 bytes, checksum: 409728fcaeb75814c914f78c124bb376 (MD5) Previous issue date: 2015Fundação Oswaldo Cruz. Instituto de Tecnologia em Fármacos. Laboratório de Química de Produtos Naturais. Rio de Janeiro, RJ, Brasil.Fundação Oswaldo Cruz. Instituto de Tecnologia em Fármacos. Laboratório de Química de Produtos Naturais. Rio de Janeiro, RJ, Brasil.Bauhinia forficata é uma leguminosa nativa da Mata Atlântica vulgarmente conhecida como pata de vaca. Ela ocorre em quase todos os tipos de solos e sua madeira é usada na produção de papel, lenha e peças de carpintaria e, suas folhas como alimentação animal. É também empregada como cobertura vegetal, planta ornamental, mas sobre tudo, é uma planta medicinal. Seus principais componentes biologicamente ativos incluem compostos flavonóides que parecem ser os grandes responsáveis por suas propriedades farmacológicas, no entanto, terpenos, esteróides, ácidos aromáticos, quinonas, lactonas, alcalóides, inibidores de proteases, proteases e lectinas têm sido isolados e purificados a partir de diferentes órgãos de várias espécies do gênero Bauhinia. Estes novos compostos têm sido caracterizados e suas propriedades farmacológicas são objetos de intensas investigações. As folhas, as flores e as cascas do caule de B. forficata têm sido usadas na medicina popular para o tratamento de diferentes tipos de patologias, especialmente diabetes, dores e processos inflamatórios.Bauhinia forficata is a legume native from Atlantic Forest named as cowage. It occurs in almost all types of soils, its wood is used in the production of pulp and paper, wood and carpentry and its leaves employed as animal feed. It is also used in plant cover, as an ornamental plant, but, more importantly, as a medicinal plant. Among the most important biologically active ingredients include are flavonoid compounds that appear to be largely responsible for its pharmacological properties. However, terpenes, steroids, aromatic acids, quinones, lactones, alkaloids, lectins and protease inhibitors have also been isolated and purified from various organs of several species of the genus Bauhinia. These new compounds have been characterized and their pharmacological properties are the purpose of intense investigation. The leaves, seeds and stem from Bauhinia species have been used in folk medicine for the treatment of different kinds of diseases and conditions, especially diabetes, infection, pain and inflammatory processes

Mucuna pruriens (L) DC (Leguminosae)

Submitted by Gilvan Almeida ([email protected]) on 2016-08-29T19:06:32Z No. of bitstreams: 2 license.txt: 1748 bytes, checksum: 8a4605be74aa9ea9d79846c1fba20a33 (MD5) 32.pdf: 301143 bytes, checksum: 00af82537f86d7250ff4f6143261927d (MD5)Approved for entry into archive by Michelle Lanzellote ([email protected]) on 2016-09-19T14:39:06Z (GMT) No. of bitstreams: 2 license.txt: 1748 bytes, checksum: 8a4605be74aa9ea9d79846c1fba20a33 (MD5) 32.pdf: 301143 bytes, checksum: 00af82537f86d7250ff4f6143261927d (MD5)Made available in DSpace on 2016-09-19T14:39:18Z (GMT). No. of bitstreams: 2 license.txt: 1748 bytes, checksum: 8a4605be74aa9ea9d79846c1fba20a33 (MD5) 32.pdf: 301143 bytes, checksum: 00af82537f86d7250ff4f6143261927d (MD5) Previous issue date: 2010-09Fundação Oswaldo Cruz. Instituto de Tecnologia em Fármacos. Laboratório de Química de Produtos Naturais. Rio de Janeiro, RJ, Brasil.Fundação Oswaldo Cruz. Instituto de Tecnologia em Fármacos. Laboratório de Química de Produtos Naturais. Rio de Janeiro, RJ, Brasil.A Mucuna pruriens é uma leguminosa nativa da Índia e Antilhas e todos os seus órgãos possuem valiosas propriedades farmacológicas, tanto que é tradicionalmente usada como planta medicinal para o tratamento de várias enfermidades, que inclui desde doenças parasitárias até distúrbios fisiológicos. Seu principal componente é a L-DOPA e os extratos de sementescom altos teores desta substância são bastante empregados no tratamento da Doença de Parkinson. Além disso, são também ricos em alcalóides, cujas funções farmacológicas são objetos de intensas investigações. Este trabalho tem como objetivo compilar as informações a cerca das aplicações medicinais da Mucuna pruriens e discutir as possíveis aplicações farmacológicas desta planta.Mucuna pruriens is a legume native to India. All parts of the plant have valuable pharmacological properties and are traditionally used for various treatments ranging from parasitic diseases to neurolophysiological disorders. The major component is L-DOPA and seed extracts with high levels of this substance are extensively used in the treatment of Parkinson’s disease. Besides, the plant is also rich in alkaloids, whose pharmacological functions are the object of research. This paper aims to compile information about the medicinal applications of Mucuna pruriens and discusses the possible pharmacological applications of this plant in the treatment of parkinsonism, Diabetes, hypercholesterolemy, male sexual dysfunction among other diseases

NEOTROPICAL CARNIVORES: a data set on carnivore distribution in the Neotropics

Mammalian carnivores are considered a key group in maintaining ecological health and can indicate potential ecological integrity in landscapes where they occur. Carnivores also hold high conservation value and their habitat requirements can guide management and conservation plans. The order Carnivora has 84 species from 8 families in the Neotropical region: Canidae; Felidae; Mephitidae; Mustelidae; Otariidae; Phocidae; Procyonidae; and Ursidae. Herein, we include published and unpublished data on native terrestrial Neotropical carnivores (Canidae; Felidae; Mephitidae; Mustelidae; Procyonidae; and Ursidae). NEOTROPICAL CARNIVORES is a publicly available data set that includes 99,605 data entries from 35,511 unique georeferenced coordinates. Detection/non-detection and quantitative data were obtained from 1818 to 2018 by researchers, governmental agencies, non-governmental organizations, and private consultants. Data were collected using several methods including camera trapping, museum collections, roadkill, line transect, and opportunistic records. Literature (peer-reviewed and grey literature) from Portuguese, Spanish and English were incorporated in this compilation. Most of the data set consists of detection data entries (n = 79,343; 79.7%) but also includes non-detection data (n = 20,262; 20.3%). Of those, 43.3% also include count data (n = 43,151). The information available in NEOTROPICAL CARNIVORES will contribute to macroecological, ecological, and conservation questions in multiple spatio-temporal perspectives. As carnivores play key roles in trophic interactions, a better understanding of their distribution and habitat requirements are essential to establish conservation management plans and safeguard the future ecological health of Neotropical ecosystems. Our data paper, combined with other large-scale data sets, has great potential to clarify species distribution and related ecological processes within the Neotropics. There are no copyright restrictions and no restriction for using data from this data paper, as long as the data paper is cited as the source of the information used. We also request that users inform us of how they intend to use the data