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Quinones are natural products widely distributed in nature, which are involved in stages of several vital biological processes, with mostly having a variety of pharmacological properties. The main groups comprising most of these compounds are benzoquinones, naphthoquinones, anthraquinones, and phenanthraquinones. Quinone isolation has been a focus of study around the world in recent years; for this reason, this study approaches the junction of natural quinones identified by 13 C Nuclear Magnetic Resonance (NMR) spectroscopic analytical techniques. The methodology used to obtain the data collected articles from various databases on quinones from 2000 to 2022. As a result, 137 compounds were selected, among which 70 were characterized for the first time in the period investigated; moreover, the study also discusses the biosynthetic pathways of quinones and the pharmacological activities of the compounds found, giving an overview of the various applications of these compounds.

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BACKGROUND: Diabetes is a chronic metabolic disorder with a high global prevalence and one of the highest morbidity and mortality rates. Despite developments in synthetic medicine, the associated serious side effects with current antidiabetic drugs indicate an urgent need for novel effective treatments. Traditional medicinal plants offer great potential in the treatment of many diseases due to their bioactive phytochemicals and are a useful resource for developing safe and effective hypoglycemic agents. METHODS: The present review collates the most frequently used ethnomedicines for the management of diabetes mellitus in Trinidad and Tobago. Further, it provides scientific validation of the claimed antidiabetic effects of four selected ethnomedicines: Antigonon leptopus, Gomphrena globosa, Laportea aestuans and Stachytarpheta jamaicensis. A comprehensive literature search was conducted using various electronic scientific databases and search engines. Information was collected on the phytochemical and pharmacological aspects of these selected species to illustrate the antidiabetic activity and potential applications of these plants. CONCLUSION: The findings of the numerous in vitro and in vivo experiments from previously published literature indicate the four candidate plants as promising sources of antidiabetic lead compounds and provide useful information to stimulate extensive studies. Further investigations on the isolation, identification and clinical evaluation of the pharmacologically active constituents from these plants can lead to the discovery of new and effective antidiabetic agents.

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As plantas ornamentais foram selecionadas pelo homem a partir de caracteres atraentes e começaram a ser cultivadas por sua beleza. São utilizadas frequentemente em arquitetura e paisagismo de espaços externos, porém, pode possuir princípios ativos que as tornam tóxicas e que podem causar danos a saúde como irritações na pele e mucosas. No Brasil há descritas diversas plantas de uso ornamental e que são consideradas tóxicas, dentre elas podemos destacar popularmente hortênsia, comigo-ninguém-pode, espada-de- são-jorge e a coroa-de-cristo e na literatura o envenenamento humano por essas plantas tóxicas quase não é documentado o que despertou interesse nessa revisão. Logo, esse estudo possui objetivo de revisar as bases de dados em busca de informações de atividades biológicas, tóxicas, farmacológicas e de metabólitos bioativos das espécies Hydrangea macrophylla, Euphorbia milii, Dieffenbachia seguine e Dracaena trifasciata. Para o compilado de dados deste artigo de revisão, foram utilizados 51 artigos que reuniram as condições de elegibilidade buscadas. Os artigos foram lidos na integra e os dados agregados em tabela ou texto. Esta revisão observou que a maioria dos ensaios aplicados nessas espécies foram de caráter toxicológico e objetivavam a busca de veículos para controle de doenças ocasionadas por vetores. Os ensaios demonstraram potencial tóxico preliminar, justificando os efeitos relacionados à intoxicação ou aos danos á saúde como irritações na pele e mucosas.

Ornamental plants were selected by man from attractive characters and began to be cultivated for their beauty. They are often used in architecture and landscaping of outdoor spaces; however, they may have active ingredients that make them toxic and that can cause health damage such as skin and mucous membrane irritations. In Brazil there are described several plants of ornamental use and that are considered toxic, among them we can highlight hortênsia, comigo-ninguém-pode, espada-de-são-jorge e a coroa-de- cristo, and in the literature the human poisoning by these toxic plants is hardly documented which aroused interest in this review. Therefore, this study aims to review the databases in search of information on biological, toxic, pharmacological activities and bioactive metabolites of the species Hydrangea macrophylla, Euphorbia milii, Dieffenbachia seguine and Dracaena trifasciata. To compile data from this review article, 51 articles were used that met the sought eligibility conditions. The articles were read in full and the data aggregated in a table or text. This review noted that most of the tests applied to these species were toxicological in nature and aimed to search for vehicles to control diseases caused by vectors. The trials demonstrated preliminary toxic potential, justifying the effects related to intoxication or damage to health such as skin and mucous membrane irritations.

Las plantas ornamentales fueron seleccionadas por el hombre a partir de caracteres atractivos y empezaron a cultivarse por su belleza. A menudo se utilizan en la arquitectura y el paisajismo de espacios exteriores; sin embargo, pueden tener principios activos que las hacen tóxicas y que pueden causar daños a la salud, como irritaciones de la piel y de las mucosas. En Brasil están descritas varias plantas de uso ornamental y que son consideradas tóxicas, entre ellas se destacan hortênsia, comigo-ninguém-pode, espada-de-são-jorge e a coroa-de- cristo, y en la literatura el envenenamiento humano por estas plantas tóxicas está poco documentado lo que despertó el interés en esta revisión. Por lo tanto, este estudio tiene como objetivo revisar las bases de datos en busca de información sobre las actividades biológicas, tóxicas, farmacológicas y metabolitos bioactivos de las especies Hydrangea macrophylla, Euphorbia milii, Dieffenbachia seguine y Dracaena trifasciata. Para recopilar los datos de este artículo de revisión, se utilizaron 51 artículos que cumplían las condiciones de elegibilidad buscadas. Los artículos se leyeron en su totalidad y los datos se agregaron en una tabla o texto. En esta revisión se observó que la mayoría de los ensayos aplicados a estas especies eran de naturaleza toxicológica y tenían como objetivo la búsqueda de vehículos para el control de enfermedades causadas por vectores. Los ensayos demostraron potencial tóxico preliminar, justificando los efectos relacionados con intoxicación o daños a la salud, como irritaciones de piel y mucosas.

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Rice (Oryza L.) is an essential food for more than 50 percent of the world's population and is the world's second-largest grain crop. Pigmented rice comes in various colors, such as black, red, brown, and green. Anthocyanins, like cyanidin-3-O-glucoside and peonidin-3-O-glucoside, are the primary color pigments in colored rice, whereas proanthocyanidins and flavan-3-ol oligosaccharides, with catechins as the central synthesis unit, are found in brown rice. This review article's aim is to give information and a summary of rice activities, research methods, also mechanisms of action (Oryza L.). Intake of pigmented rice was already associated with a number of health benefits, including antioxidant activity, anticancer, antitumor, antidiabetic activity, and a reduced risk of cardiovascular disease. Rice contains several bioactive compounds, such as γ-oryzanol, phenolic acid, anthocyanins, proanthocyanidins, flavonoids, carotenoids, and phytosterols, which have been widely studied and shown to have several pharmacological activities. The use of current herbal compounds is rapidly increasing, including the practice of pharmacological disease prevention and treatment. Herbal remedies have entered the international market as a result of research into plant biopharmaceuticals and nutraceuticals. Through a variety of pharmacological activities, it is clear that Oryza L. is a popular herb. As a result, additional research on Oryza L. can be conducted to investigate more recent and comprehensive pharmacological effectiveness, to provide information and an overview of Rice (Oryza L.) activities, research methods, and mechanisms of action. Several natural substances are characterized by low water solubility, low stability, and sensitivity to light and oxygen, and the potential for poor absorption of the active substances requires modification of the formulation. To improve the effectiveness of pharmacologically active substances originating from natural ingredients, drug delivery systems that use lipid-based formulations can be considered innovations.

O arroz (Oryza L.) é um alimento essencial para mais de 50% da população mundial e é a segunda maior safra de grãos do mundo. O arroz pigmentado possui cores variadas, como preto, vermelho, marrom e verde. As antocianinas, como a cianidina-3-O-glicosídeo e a peonidina-3-O-glicosídeo, são os pigmentos de cor primária no arroz colorido, enquanto as proantocianidinas e os oligossacarídeos flavan-3-ol, com catequinas como unidade central de síntese, são encontrados no arroz marrom. O objetivo deste estudo de revisão é fornecer informações e um resumo das atividades do arroz, métodos de pesquisa e mecanismos de ação. A ingestão de arroz pigmentado já foi associada a vários benefícios à saúde, incluindo atividade antioxidante, anticancerígena, antitumoral, antidiabética e redução do risco de doenças cardiovasculares. O arroz contém vários compostos bioativos, como γ-orizanol, ácido fenólico, antocianinas, proantocianidinas, flavonoides, carotenóides e fitoesteróis, que têm sido amplamente estudados e têm mostrado diversas atividades farmacológicas. O uso de compostos fitoterápicos atuais está aumentando rapidamente, incluindo a prática de prevenção e tratamento farmacológico de doenças. Os remédios fitoterápicos entraram no mercado internacional como resultado da pesquisa de biofármacos e nutracêuticos vegetais. Através de uma variedade de atividades farmacológicas, fica claro que Oryza L. é uma erva popular. Como resultado, pesquisas adicionais sobre Oryza L. podem ser conduzidas para investigar a eficácia farmacológica mais recente e abrangente, fornecer informações e uma visão geral das atividades, métodos de pesquisa e mecanismos de ação do arroz (Oryza L.). Várias substâncias naturais são caracterizadas por baixa solubilidade em água, baixa estabilidade e sensibilidade à luz e ao oxigênio, e o potencial de má absorção das substâncias ativas requer modificação da formulação. Nesse sentido, alguns aspectos como a melhorara na eficácia de substâncias farmacologicamente ativas provenientes de ingredientes naturais e nos sistemas de liberação de fármacos que utilizam formulações à base de lipídios podem ser considerados como inovações.

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Background: A combination of pharmacological and biomedical assays was applied in this study to examine the bioactivity of Conus virgo crude venom in order to determine the potential pharmacological benefit of this venom, and its in vivo mechanism of action. Methods: Two doses (1/5 and 1/10 of LC50, 9.14 and 4.57 mg/kg) of the venom were used in pharmacological assays (central and peripheral analgesic, anti-inflammatory and antipyretic), while 1/2 of LC50 (22.85 mg/kg) was used in cytotoxic assays on experimental animals at different time intervals, and then compared with control and reference drug groups. Results: The tail immersion time was significantly increased in venom-treated mice compared with the control group. Also, a significant reduction in writhing movement was recorded after injection of both venom doses compared with the control group. In addition, only the high venom concentration has a mild anti-inflammatory effect at the late inflammation stage. The induced pyrexia was also decreased significantly after treatment with both venom doses. On the other hand, significant increases were observed in lipid peroxidation (after 4 hours) and reduced glutathione contents and glutathione peroxidase activity, while contents of lipid peroxidation and nitric oxide (after 24 hours) and catalase activity were depleted significantly after venom administration. Conclusion: These results indicated that the crude venom of Conus virgo probably contain bioactive components that have pharmacological activities with low cytotoxic effects. Therefore, it may comprise a potential lead compound for the development of drugs that would control pain and pyrexia.

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The genus Malachra L. belongs to the family Malvaceae. It includes herbs or subshrubs of nine accepted species with approximately thirty synonyms, and it has been widely used in community folk medicine to treat health problems including inflammation, nasal obstruction, leishmaniasis, malaria, childbirth, kidney disorders, fever, respiratory tract diseases, among others. From the genus Malachra L., flavonoids, steroids, triterpenes, anthocyanins, leucoanthocyanins, saponins, carbohydrates, phenols, glycosides, and alkaloids have been isolated and identified. Some pharmacological reports have indicated that the genus has antidiarrheal, antiepileptic, antiulcerogenic, antioxidant, anticonvulsant, antiviral, anticancer, antibacterial, anthelmintic, and hepatoprotective properties. However, there have been limited studies of bioactive molecules with pharmacological and biological activities associated with Malachra alceifolia Jacq., Malachra capitata (L.) L., Malachra fasciata Jacq., Malachra radiata (L.) L., Malachra ruderalis Gürke., Malachra rudis Benth., Malachra helodes Mart., Malachra urens Poit. ex Ledeb. & Alderstam., and Malachra officinalis Klotzsch. In this review, we consider the conservation of these species to save the ancestral knowledge of their traditional use in populations, and their pharmacological potential for future studies in search of alternatives for solutions to diseases in humans and animals and tools for the design and search of potential bioactive compounds against infectious and non-infectious agents.

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BACKGROUND: Passiflora L. is a genus belonging to the Passifloraceae family, with many species widely used in folk medicine and several pharmacological activities described in the scientific literature, being a major target for the development of new therapeutic products. Studies have identified several bioactive compounds in their composition as responsible for these activities, mainly C-glycoside flavonoids. OBJECTIVE: The aim of this study was to carry out a review of patents related to the genus and its application in several pharmacological activities, important for the development of new drugs and formulations. METHODS: The search was carried out in 5 specialized databases, INPI, EPO, WIPO, Latipat and Derwent, using the term 'Passiflora' combined with 'A61K and A61P', subclasses of section A of the International Patent Classification (IPC), which are destined to medical, dental or hygienic purposes, and therapeutic activity of chemical compounds or medicinal preparation, respectively. RESULTS: 1,198 patents citing the genus in the title or abstract have been found, 508 being duplicates. After exclusion and inclusion criteria, 23 patents written in English, Portuguese and Spanish were selected, which demonstrated biological assays in vivo with species of Passiflora as the only active constituent or incorporated in formulations with other compounds. CONCLUSION: The findings of this search showed growing interest in research and industrial areas in the pharmaceutical development with species of Passiflora, suggesting that the different bioactive compounds present in the genus can be considered as an important tool for the development of new effective and safe products with pharmacological potential.

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The pharmacological attributes of turmeric have been extensively described and frequently related to the action of curcuminoids. However, there is also scientific evidence of the contribution of turmeric oil. Since the oil does not contain curcuminoids in its composition, it is crucial to better understand the therapeutic role of other constituents in turmeric. The present review discusses the pharmacokinetics of turmeric oil, pointing to the potential application of its active molecules as therapeutic compounds. In addition, the bioactivities of turmeric oil and its safety in preclinical and clinical studies were revised. This literature-based research intends to provide an updated overview to promote further research on turmeric oil and its constituents.

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The genus Arrabidaea, consisting of ~170 species, belongs to the family Bignoniaceae, distributed around the Neotropics and temperate zone. The center of diversity of the family is in Brazil, where 56 genera and about 340 species exist. Most species of the genus Arrabidaea are traditionally utilized as diuretics and antiseptics, as well as for treating intestinal colic, diarrhea, kidney stones, rheumatoid arthritis, wounds, and enterocolitis. The genus is chemically diverse with different substance classes; most of them are triterpenes, phenolic acids, and flavonoids, and they exhibit valuable pharmacological properties, such as antitumor, antioxidant, leishmanicidal, trypanocidal, anti-inflammatory, and healing properties. This review presents information on the chemical constituents isolated from seven Arrabidaea species, and the pharmacological activities of the extracts, fractions and pure substances isolated since 1994, obtained from electronic databases. The various constituents present in the different species of this genus demonstrate a wide pharmacological potential for the development of new therapeutic agents, however its potential has been underestimated.

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Duguetia A. St. Hill (Annonaceae) is recognized as one of the major genera with approximately 100 species, 67 of which are found in Brazil (29 of those are endemic). They are arboreal species with edible fruits known as "pindaíba", "pindaíva" "pinha", and "envira" in Brazil. Many Duguetia species, in particular, have been used in traditional medicine to treat renal colic, stomachache, rheumatism, cough, toothache, muscle pain, fever, gastrointestinal pain, and breathing difficulties. In this study, we reviewed the chemical constituents and pharmacological properties of essential oils (EOs) from Duguetia species. A total of 12 species were found, along with their EO chemical constituents and bioactivities. Bicyclogermacrene, humulene epoxide II, spathulenol, germacrene D, caryophyllene oxide, viridiflorene, α-pinene, ß-caryophyllene, and ß-pinene were the main chemical constituents reported. The pharmacological effects of Duguetia species EOs included anti-inflammatory, antinociceptive, antibacterial, antifungal, antioxidant, anti-trypanosoma, cytotoxic and antitumor properties. This information adds to our understanding of the potential of the EOs of Duguetia species.

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Pregnanes and pregnane glycosides or their esters are well-studied secondary metabolites, many of them exhibit immunomodulator, anticancer, antidiabetic, antarthritic, antiulcer, anti-nociceptive, hypolipidemic, anti-inflammatory, and antibacterial properties. Pregnane glycosides are widely distributed in the families Apocyanaceae and Asclepiadaceae. Plant members of the genus Caralluma R.Br., Apocynaceae, are among the most studied species because of uses in traditional medicine or as food. They are a rich source of pregnane glycosides, as russelioside B. However, the bioactivity profile of this pregnane glycoside has not been reviewed until now. The present review aims to summarize the most important pharmacological and therapeutic applications of russelioside B with specific emphasis on the mechanism of actions associated with its administration in preclinical models. Russelioside B has many pharmacological effects including antidiabetic, anti-obesity, anti-nociceptive, antiulcer, anti-inflammatory, anti-arthritis effects, and antibiofilm, and wound healing activities. Despite its outstanding pharmacotherapeutic potential, russelioside B has never been tested in clinical trials. This review indicates that russelioside B is a potentially promising bioactive candidate, but further deeper mechanistic studies and clinical trials are needed in the future to elucidate its interaction with receptors of specific genes. Supplementary Information: The online version contains supplementary material available at 10.1007/s43450-022-00245-x.

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BACKGROUND: Tuberculosis is a chronic respiratory disease caused by Mycobacterium tuberculosis. The common treatment regimens of tuberculosis are lengthy with adverse side effects, low patient compliance, and antimicrobial resistance. Drug delivery systems (DDSs) can overcome these limitations. OBJECTIVE: This review aims to summarize the latest DDSs for the treatment of tuberculosis. In the first section, the main pharmacokinetic and pharmacodynamic challenges posed by the innate properties of the drugs are put forth. The second section elaborates on the use of DDS to overcome the disadvantages of the current treatment of tuberculosis. CONCLUSION: We reviewed research articles published in the last 10 years. DDSs can improve the physicochemical properties of anti-tuberculosis drugs, improving solubility, stability, and bioavailability, with better control of drug release and can target alveolar macrophages. However, more pre-clinical studies and robust bio-relevant analyses are needed for DDSs to become a feasible option to treat patients and attract investors.

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Background: A combination of pharmacological and biomedical assays was applied in this study to examine the bioactivity of Conus virgo crude venom in order to determine the potential pharmacological benefit of this venom, and its in vivo mechanism of action. Methods: Two doses (1/5 and 1/10 of LC50, 9.14 and 4.57 mg/kg) of the venom were used in pharmacological assays (central and peripheral analgesic, anti-inflammatory and antipyretic), while 1/2 of LC50 (22.85 mg/kg) was used in cytotoxic assays on experimental animals at different time intervals, and then compared with control and reference drug groups. Results: The tail immersion time was significantly increased in venom-treated mice compared with the control group. Also, a significant reduction in writhing movement was recorded after injection of both venom doses compared with the control group. In addition, only the high venom concentration has a mild anti-inflammatory effect at the late inflammation stage. The induced pyrexia was also decreased significantly after treatment with both venom doses. On the other hand, significant increases were observed in lipid peroxidation (after 4 hours) and reduced glutathione contents and glutathione peroxidase activity, while contents of lipid peroxidation and nitric oxide (after 24 hours) and catalase activity were depleted significantly after venom administration. Conclusion: These results indicated that the crude venom of Conus virgo probably contain bioactive components that have pharmacological activities with low cytotoxic effects. Therefore, it may comprise a potential lead compound for the development of drugs that would control pain and pyrexia.(AU)

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BACKGROUND: Medicinal plants present activities against neurodegenerative diseases with potential for the pharmaceutical industries. Therefore, the objective of this study was to investigate the current panorama of patents and articles of Brazilian medicinal plants with pharmacological activities in the Central Nervous System (CNS), regarding such aspects as the number of patents by countries, areas of knowledge, and technological maturity. METHODS: We carry out a technological exploration on the Questel Orbit® platform with the descriptors: Agave sisalana P., Amburana cearenses A., Dimorphandra mollis B., Jatropha curcas L., Poincianella pyramidalis T. and Prosopis juliflora (Sw.) DC. with pharmacological activity and scientific exploration in PubMed and Science Direct associated with the CNS in the title, abstract, and methodology. RESULTS: A total of 642 patents were identified between the years 1999-2019. India, China, and Brazil are highlighted, 6th place, out of a total of 48 countries. Of these, 30 patents were not in the National Institute of Industrial Property, and 10% are Brazilian in biotechnology and pharmaceutical products. Eleven articles were used in PubMed and Science Direct with scientific domains (anticancer, neuroprotection and anti-inflammatory). The Federal University of Bahia is highlighted, showing Technology Readiness Levels (TRL4), basic skills of pre-clinical research. CONCLUSION: Brazilian public universities have a significant role in the scientific, technological and innovative development of therapeutic assets for CNS.

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Piperine (PIP) is an alkaloid present in several species of piper, mainly Piper nigrum Linn. and P. longum, among other species. The present article provides a comprehensive review of PIP research in the last years concerning its chemical properties, synthesis, absorption, metabolism, bioavailability and toxicity. The reviewed PIP literature has shown many pharmacological properties, such as antidiabetic, antidiarrheal, antioxidant, antibacterial, and anti-parasitic activity of PIP. However, its low solubility and absorption make its application challenging. This review also includes advances in the development of nanosystems containing PIP, including liposomes, micelles, metal nanoparticles, nanofibers, polymeric nanoparticles, and solid-lipid nanoparticles. Finally, we discuss different in vitro and in vivo studies to evaluate the biological activity of this drug, as well as some methods for the synthesis of nanosystems and their physical characteristics.

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Fruit plants have been widely used by the population as a source of food, income and in the treatment of various diseases due to their nutritional and pharmacological properties. The aim of this study was to review information from the most current research about the phytochemical composition, biological and toxicological properties of four fruit species widely used by the world population in order to support the safe medicinal use of these species and encourage further studies on their therapeutic properties. The reviewed species are: Talisia esculenta, Brosimum gaudichaudii, Genipa americana, and Bromelia antiacantha. The review presents the botanical description of these species, their geographical distribution, forms of use in popular medicine, phytochemical studies and molecules isolated from different plant organs. The description of the pharmacological mechanism of action of secondary metabolites isolated from these species was detailed and toxicity studies related to them were reviewed. The present study demonstrates the significant concentration of phenolic compounds in these species and their anti-inflammatory, anti-tumor, photosensitizing properties, among others. Such species provide important molecules with pharmacological activity that serve as raw materials for the development of new drugs, making further studies necessary to elucidate mechanisms of action not yet understood and prove the safety for use in humans.

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Euterpe oleracea Mart. (EO), popularly known as açaí, belongs to the Arecaceae family and grows abundantly in Brazil. The fruit of this palm tree is widely used because of its anti-inflammatory and antioxidant properties. In this review, a search for literature and patent technological prospecting has been performed on the use of EO to treat and prevent diseases as well as to prepare pharmaceutical formulations. EO leaves, fruits, and oil stand out for their large number of pharmacological activities such as anti-inflammatory, antioxidant, antimicrobial, antinociceptive, anticancer, anti-atherogenic, and healing activities, protection against metabolic syndromes such as diabetes, hypertension, and hyperlipidemia, and protection of organs such as lung, kidney, liver, heart, and nervous system. While the phytochemical composition is intrinsically linked to identified biological activities, discoveries of the past decade concerning the use of this species have shown pharmacological alternatives mainly in the treatment and prevention of breast cancer and metabolic syndromes. Although studies and inventions on the use of EO though are believed to have been important in light of the pharmacological activities found, few clinical and toxicity tests have been performed. Nevertheless, with the increase of interest in EO, this species is believed to be only at the beginning of the breakthroughs in the development of promising products for the pharmaceutical industry.

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Abstract The aim of this study was to investigate in vitro antioxidant properties and in vivo protective effects of the methanol extract of the Hypericum triquetrifolium Turra (HT) seed against acute hepatotoxicity, myelotoxicity and hematotoxicity in rats induced by cyclophosphamide (CP). In order to investigate in vivo protective effects of the HT extract on rat tissues, the rats were divided into nine groups. The toxic effects of CP and the protective effects of HT extract on nucleated cells that are produced by bone marrow, serum alanine transaminase (ALT), alkaline phosphatase (ALP), lactate dehydrogenase (LDH) and oxidative stress index (OSI) levels were investigated biochemically. Additionally, liver tissue samples were examined for histopathological changes and apoptosis by Bcl-2, Bax and caspase-3 immunohistochemistry. The results of this study show that HT seed methanol extract has high total phenolic content (179.52 μg GAE/mg) and antioxidant activity (87.48% in 500 μg/mL concentration). CP administration caused hepatotoxicity, myelotoxicity and hematotoxicity in the rats. Whereas, the groups of rats that were injected with different concentrations of HT (25, 50 and 100 mg/kg) and CP (150 mg/kg) showed significant protective effects on bone marrow nucleated cells and important decreases on serum ALT, ALP, LDH and OSI levels were observed when compared with the CP injected group.

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The propolis produced by stingless bees of the tribe Meliponini is a viscous product that contains the resin collected from buds, leaves and plant exudates, mixed with salivary secretions, wax and soil. The species Scaptotrigona aff. postica (Latreille, 1807), (Hymenoptera, Apidae, Meliponinae) popularly known as “tubi” in Maranhão State, Brazil, does not mix soil to produce its propolis. The propolis from S. postica harvested in Barra do Corda, Maranhão State, is popularly used in the treatment of wounds and respiratory illnesses. The hydroalcoholic extract of this propolis, rich in flavone-6,8-di-C-glycosides (vicenin-2 and schaftoside), pyrrolizidine alkaloids derived from retronecine, catechin and caffeoylquinic acid derivatives exhibited antiviral activity against the herpes simplex and rubella viruses. The aim of this study was to increase knowledge about the chemical composition of the S. postica propolis by analyzing non-polar extracts obtained using hexane and chloroform as the solvents, by GC-EI-MS. A total of 15 constituents were identified comparing their respective mass spectral data with those available in the NIST data bases and those reported in the literature. The main constituents detected were the phenolic lipids, known as cardanols, 3-(4,7-heptadecadienyl) phenol (5), 3-(10-heptadecenyl) phenol (7), 3-heptadecylphenol (9) and 3-pentadecyl phenol or hydrocardanol (13), which predominated in the hexane extract, while the predominant constituents in the chloroform extract were 3-pentadecyl phenol or hydrocardanol (13) and 3-(8-pentadecenyl) phenol (12). The antioxidant, antitumoral, antifeedant, cytotoxic, anticarcinogenic, antiproliferative, antimicrobial, antileishmanial and larvicidal activities of the cardanols have been demonstrated in many studies.

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An N-methylated analog of a marine bacteria-derived natural proline-rich tetracyclopeptide was synthesized by coupling the deprotected dipeptide fragments Boc-l-prolyl-l-N-methylleucine-OH and l-prolyl-l-N-methylphenylalanine-OMe. A coupling reaction was accomplished utilizing N,N'-Dicyclohexylcarbodidimde (DCC) and 1-Ethyl-3-(3-dimethylaminopropyl) carbodiimide (EDC·HCl) as coupling agents and Triethylamine (TEA) or N-methylmorpholine (NMM) as the base in the presence of the racemization suppressing agent. This was followed by the cyclization of the linear tetrapeptide fragment under alkaline conditions. The structure of the synthesized cyclooligopeptide was confirmed using quantitative elemental analysis, FTIR (Fourier-transform infrared spectroscopy), ¹H NMR (Nuclear magnetic resonance spectroscopy), 13C NMR, and mass spectrometry. From the bioactivity results, it was clear that the newly synthesized proline-rich tetracyclopeptide exhibited better anthelmintic potential against Megascoplex konkanensis, Pontoscotex corethruses, and Eudrilus eugeniae at a concentration of 2 mg/mL as well as improved antifungal activity against pathogenic dermatophytes Trichophyton mentagrophytes and Microsporum audouinii at a concentration of 6 µg/mL, as compared to non-methylated tetracyclopeptide. Moreover, N-methylated tetracyclopeptide displayed significant activity against pathogenic Candida albicans.

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