ABSTRACT
Sesquiterpenoids are natural compounds composed of 15 carbon atoms， which can be divided into sesquiterpene alcohols， ketones， lactones， aldehydes， and carboxylic acids according to oxygen groups. These compounds are widely distributed in nature， and their physiological activities are diverse. For example， many sesquiterpenes with potential anticancer effects have been found for anti-tumor effects， including cytotoxicity， antioxidant， immune regulation， cell proliferation， and so on. In addition， some sesquiterpenoids have good application prospects in antibacterial， anti-inflammatory， and anti-cardiovascular diseases. Malignant tumors， inflammation， bacterial diseases， and cardiovascular diseases are the main diseases that cause human death， and natural products have unique advantages in the treatment of these diseases. Therefore， the development of new drugs that are easy to promote has become a new research hotspot. In this paper， the sesquiterpenes extracted from the natural components of Chinese herbs and plants with anti-tumor， anti-inflammatory， antibacterial， and anti-cardiovascular activities， such as Xanthium， Atractylodes， Convolvulus， Acanthium， Ligularia， Artemisia， Ligularia， Ligularia， Labiaceae Mint， Acanthophyllum， Turmeria， Ginger， and other Chinese herbs and plants， were discussed. The biological activities and related mechanisms of this compound were reviewed， which provided a reference for further research and clinical application of sesquiterpenes.
ABSTRACT
Abstract The present study evaluated the influence of carvacrol, terpinene-4-ol, and chlorhexidine on the physical-chemical properties of titanium surfaces, cell viability, proliferation, adhesion, and spreading of fibroblasts and osteoblasts in vitro. Titanium surfaces (Ti) were treated with Carvacrol (Cvc), Terpinen-4-ol (T4ol), Chlorhexidine (CHX), DMSO, and ultrapure water (Control group). Physical-chemical modifications were evaluated by surface wettability, the surface free energy (SFE) calculated from the contact angle values using the Owens-Wendt-Rabel-Kaeble (OWRK) equation, scanning electron microscopy (SEM) and energy dispersive spectrometry probe (EDS) system. Cells were seeded onto Ti-treated surfaces and incubated for 24 h and 72 h, then evaluated by Alamar blue assay and fluorescence microscopy. Surfaces treated with Cvc and T4ol showed the presence of Na, O, and Cl. All surfaces showed hydrophilic characteristics and SFE values between 5.5 mN/m and 3.4 mN/m. On the other hand, EDS peaks demonstrated the presence of O and Cl after CHX treatment. A reduction of cell viability and adhesion was noted on titanium surfaces treated with CHX after 24 and 72h. In conclusion, the results indicate that the decontamination with Cvc and T4ol on Ti surfaces does not alter the surface proprieties and allows an adequate interaction with cells involved in the re-osseointegration process such as fibroblasts and osteoblasts.
Resumo O presente estudo avaliou a influência do carvacrol, terpineno-4-ol e clorexidina nas propriedades físico-químicas de superfícies de titânio, viabilidade celular, proliferação, adesão e esplhamento de fibroblastos e osteoblastos in vitro. Superfícies de titânio (Ti) foram tratadas com Carvacrol (Cvc), Terpinen-4-ol (T4ol), Clorexidina (CHX), DMSO e água ultrapura (Grupo Controle). As modificações físico-químicas foram avaliadas pela molhabilidade da superfície, a energia livre de superfície (ELS) calculada a partir dos valores do ângulo de contato usando a equação de Owens-Wendt-Rabel-Kaeble (OWRK), microscopia eletrônica de varredura (MEV) e espectroscopia de raios X por energia dispersiva (EDS). As células foram semeadas em superfícies tratadas com Ti e incubadas por 24 h e 72 h, e avaliadas pelo ensaio Alamar blue e microscopia de fluorescência. As superfícies tratadas com Cvc e T4ol mostraram a presença de Na, O e Cl. Todas as superfícies apresentaram características hidrofílicas e valores de ELS entre 5,5 mN/m e 3,4 mN/m. Por outro lado, os picos de EDS demonstraram a presença de O e Cl após o tratamento com CHX. Uma redução da viabilidade celular e adesão foi observada em superfícies de titânio tratadas com CHX após 24 e 72h. Em conclusão, os resultados indicam que a descontaminação com Cvc e T4ol em superfícies de Ti não altera as propriedades da superfície e permite uma interação adequada com células envolvidas no processo de reosseointegração como fibroblastos e osteoblastos.
ABSTRACT
As an important model animal, fruit fly is characterized by outstanding genetic characteristics, relatively perfect nervous system, rapid reproduction, and low cost. Thus, it has been applied in the research on neuropsychiatric disorders in recent years, showing great potential in life science. The incidence of neuropsychiatric disorders has been on the rise, and the disorders have high disability rate and low case fatality rate. The global drug demand for such diseases is second only to cardiovascular and cerebrovascular diseases. At the moment, the demand of the drugs for the diseases have been rising, and it is an urgent task to develop related drugs. However, the research and development of the drugs are time-intensive and have a high failure rate. A suitable animal model can help shorten the time for drug screening and development, thereby reducing the cost and failure rate. This study reviews the application of fruit flies in several common neuropsychiatric disorders, which is expected to provide new ideas for the research and application of the model animals in traditional Chinese medicine.
Subject(s)
Animals , Medicine, Chinese Traditional , Drugs, Chinese Herbal/therapeutic use , Models, Animal , Cerebrovascular DisordersABSTRACT
Essential oils are volatile aromatic liquids derived from the secondary metabolism of plants, consisting of a complex mixture of different active compounds. Several medicinal plants are sources for the extraction of essential oils, being recognized as safe (GRAS) by the FDA (Food and Drug administration). The use of essential oils as possible food preservatives has been gaining ground in research due to their antioxidant and antibacterial activities, important characteristics in food preservation and also to the population's interest in consuming healthier products. Essential oils are a promising alternative for the food industry, as they act to control pathogenic and deteriorating bacteria. Compared to synthetic chemical preservatives, essential oils are generally safer, but have low stability, so encapsulation is a way to protect them from adversities. This review aims to demonstrate the effectiveness, stability and safety of essential oils and their use in food matrices.
Os óleos essenciais são líquidos aromáticos voláteis derivados do metabolismo secundário das plantas, sendo constituído por uma mistura complexa de diferentes compostos ativos. Diversas plantas medicinais são fontes de extração de óleos essenciais sendo reconhecidos como seguros (GRAS) pelo FDA (Food and Drug administration). A utilização de óleos essenciais como possíveis conservantes em alimentos vem ganhando espaço nas pesquisas devido a suas atividades antioxidantes e antibacterianas, características importantes na preservação de alimentos e também ao interesse da população em consumir produtos mais saudáveis. Os óleos essenciais são uma alternativa promissora para a indústria de alimentos, pois atuam no controle de bactérias patogênicas e deteriorantes. Em comparação com os conservantes químicos sintéticos, os óleos essenciais geralmente são mais seguros, porém apresentam baixa estabilidade, deste modo a encapsulação é uma forma de protegê-los de adversidades. Esta revisão tem como objetivo demonstrar a efetividade, estabilidade e a segurança dos óleos essenciais e seu uso em matrizes alimentares.
Los aceites esenciales son líquidos aromáticos volátiles derivados del metabolismo secundario de las plantas, constituidos por una mezcla compleja de diferentes compuestos activos. Varias plantas medicinales son fuentes para la extracción de aceites esenciales, siendo reconocidas como seguras (GRAS) por la FDA (Administración de Alimentos y Medicamentos). El uso de aceites esenciales como posibles conservantes de alimentos ha ido ganando terreno en las investigaciones debido a sus actividades antioxidantes y antibacterianas, características importantes en la conservación de alimentos y también al interés de la población por consumir productos más saludables. Los aceites esenciales son una alternativa prometedora para la industria alimentaria, ya que actúan para controlar las bacterias patógenas y deteriorantes. En comparación con los conservantes químicos sintéticos, los aceites esenciales son generalmente más seguros, pero tienen baja estabilidad, por lo que la encapsulación es una forma de protegerlos de las adversidades. Esta revisión tiene como objetivo demostrar la eficacia, estabilidad y seguridad de los aceites esenciales y su uso en matrices alimentarias.
ABSTRACT
Resumen Los organismos marinos poseen maravillosos colores que los hacen muy atractivos. Las características únicas de los compuestos sintetizados por especies de origen marino van más allá de su apariencia. Los pigmentos responsables de esos colores son capaces también de generar diversas actividades biológicas, como la capacidad antioxidante, la cual puede ocurrir a través de diversos mecanismos. Esto ha propiciado un aumento de su investigación, debido a su amplia aplicación en la biotecnología, farmacéutica, cosmética y alimentación de organismos vivos, expandiendo los estudios tanto in vitro como en ensayos in vivo. El objetivo de este trabajo fue compilar y describir diversos estudios recientes, enfocados en demostrar y elucidar los mecanismos de acción de los diferentes compuestos bioquímicos con actividad antioxidante, provenientes de algunos organismos marinos. Para ello, se utilizaron las bases de datos Scopus®, Web of Science™ y Microsoft Academic. Los pigmentos provenientes de organismos marinos representan una alternativa promisoria frente a los antioxidantes y aditivos sintéticos utilizados en la actualidad. El establecimiento y comprensión de los mecanismos de acción de los componentes pigmentados bioactivos, aislados de los organismos marinos, permitirá determinar con mayor precisión su posible aplicación en la industria.
Abstract Marine organisms have wonderful colors that make them very attractive. The unique characteristics of the compounds synthesized by species of marine origin go beyond their appearance. The pigments responsible for these colors are also capable of exerting biological activities, including the antioxidant capacity, which can be performed by different mechanisms. This has led to an increase in research attention due to their potential application in the pharmaceutical, cosmetics and food industries, and has expanded from in vitro studies to in vivo tests. The objective of this review is to compile and describe the studies aimed at establishing and elucidating the mechanisms of action of different biochemical compounds with antioxidant activities from marine species. In order to achieve that objective, the Scopus®, Web of Science™ and Microsoft Academic databases were used. Marine pigments represent a promising alternative to the antioxidants and synthetic additives used today. By establishing and understanding the mechanisms of action of the bioactive pigmented compounds isolated from marine organisms, it is possible to determine with greater precision their possible application in the industry.
ABSTRACT
he resistance against antimalarial drugs represents a global challenge in the fight and control of malaria. The Brazilian biodiversity can be an important tool for research and development of new medicinal products. In this context, toxinology is a multidisciplinary approach on the development of new drugs, including the isolation, purification, and evaluation of the pharmacological activities of natural toxins. The present study aimed to evaluate the cytotoxicity, as well as the antimalarial activity in silico and in vitro of four compounds isolated from Rhinella marina venom as potential oral drug prototypes. Methods: Four compounds were challenged against 35 target proteins from P. falciparum and screened to evaluate their physicochemical properties using docking assay in Brazilian Malaria Molecular Targets (BraMMT) software and in silico assay in OCTOPUS® software. The in vitro antimalarial activity of the compounds against the 3D7 Plasmodium falciparum clones were assessed using the SYBR Green I based assay (IC50). For the cytotoxic tests, the LD50 was determined in human pulmonary fibroblast cell line using the [3(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide] (MTT) assay. Results: All compounds presented a ligand-receptor interaction with ten Plasmodium falciparum-related protein targets, as well as antimalarial activity against chloroquine resistant strain (IC50 = 3.44 µM to 19.11 µM). Three of them (dehydrobufotenine, marinobufagin, and bufalin) showed adequate conditions for oral drug prototypes, with satisfactory prediction of absorption, permeability, and absence of toxicity. In the cell viability assay, only dehydrobufotenin was selective for the parasite. Conclusions: Dehydrobufotenin revealed to be a potential oral drug prototype presenting adequate antimalarial activity and absence of cytotoxicity, therefore should be subjected to further studies.(AU)
Subject(s)
Bufanolides/administration & dosage , Bufonidae , Biodiversity , Malaria/immunology , Antimalarials , In Vitro Techniques , Computer SimulationABSTRACT
ABSTRACT Objective: Developing anti-cancer drugs from natural products is receiving increasing interest worldwide due to limitations and side effects of anti-cancer drugs. The purpose of this study was to explore the anti-proliferative or cytopathic potential of natural compounds derived from plant sources as alternatives of synthetic compounds on human embryonic kidney carcinoma (HEK) cell line. Methods: In this study, aqueous and methanolic extracts were obtained from various plants, viz, Thapsia garganica, Citrus sinesis, Citrus limon and Vinca rosea. Extracts were serially diluted into 96-well microtitre plates and were screened for anti-proliferative potential against the HEK cell line via the neutral red dye uptake assay. Results: The findings revealed that methanolic extracts of T. garganica leaf and V. rosea leaf were the most effective as anti-proliferative or cytotoxic against the HEK cell line, with IC50 at 32-fold dilution of the extract. Conclusion: The extracts of T. garganic and V, rosea have been used as anti-proliferative drugs but after trial in experimental animals for being not toxic.
ABSTRACT
Rheumatoid arthritis (RA), the most common inflammatory arthropathy word wild, is a systemic autoimmune disease that mainly affects the synovium of joints with a high disability rate. Metabolic mis-regulation has emerged as a fundamental pathogenesis of RA linked to immune cell dysfunction, while targeting immunometabolism provides a new and effective approach to regulate the immune responses and thus alleviate the symptom of RA. Recently, natural active compounds from traditional Chinese medicines (TCMs) have potential therapeutic effects on RA and regulating immunometabolism. In this review, in addition to updating the connection between cellular metabolism and cell function in immune cells of RA, we summarized that the anti-inflammatory mechanisms of the potential natural compounds from TCM by targeting metabolic reprogramming of immune cells, and discusses them as a rich resource for providing the new potential paradigm for the treatment of RA.
ABSTRACT
Epilepsy is a chronic neurological disorder that causes uncontrolled seizures which can affect the bodyphysically and psychologically. When a person experiences seizure, it is very difficult for them to breathe andthey bite their tongue as a reflex. Glutamatergic and gamma-aminobutyric acid ergic (GABAergic) transmissionin the brain causes seizures. The immature brain is more prone to seizures than the adult brain. Gene SLC6A1produces GABA1 protein which helps in reuptake of GABA from the synapse. Presently in this study, proteinmodeling and molecular docking were performed on protein sequence sodium- and chloride-dependent GABAtransporter 1 that was retrieved from uniport. MODELLER 9.21 versions were used to develop a homologymodel. X-ray structure of Drosophila dopamine transporter in complex with cocaine (4XP4) from speciesDrosophila melanogaster was used as a template. Autodock4.2, a docking software, was used for moleculardocking studies. Against the modeled protein, 22 natural compounds were docked. According to the results,natural compounds like Morusin showed high binding energy against modeled protein than standard drugs.
ABSTRACT
Snake venoms are widely used as laboratory tools for studies of physiological, pharmacological and toxicological mechanisms. Venoms used here are rich sources of several classes of proteases that act on factors of the coagulation cascade, fibrinogenolysis and fibrinolysis, altering the hemostatic processes, and phospholipases A2 which are involved mainly in inflammatory and clotting processes. Natural products such as essential oils are made up of active ingredients with wide application in the food, pharmaceutical and cosmetic industries. Thus, this study evaluates the essential oils from Mentha viridis and Mentha pulegium on coagulation, fibrinogenolysis and degradation of azocasein, induced by Bothrops sp and Lachesis muta muta venoms. These oils were achieved by hydrodistillation and presented, respectively, as the main constituents linalool (40.70 %), carvone (13.52 %) and α-terpinene (8.56 %); pulegone (50.01 %), menthol (31.90 %) and menthone (16.56 %). The essential oils were previously incubated with Bothrops alternatus venom, for two different times, then plasma was added and time was recorded. The M. viridis oil presented greater anticlotting potential. Meanwhile, the M. pulegium oil presented anticlotting or proclotting activity dependent on the dose tested. The incubation time also influenced the effect of the oils on the coagulation time. At azocaseinolytic assay, the oil from M. pulegium reduced the activity for all evaluated venoms. The highest inhibition was of 39.99 %; on activity induced by B. jararacussu, M. viridis reduced the activity in 57.72 %. On B. moojeni, the major inhibition observed was of 74.67 %. The fibrinogenolysis induced by B. moojeni venom was totally inhibited by both oils in the evaluated proportions. The results show the presence in oils of protease inhibitors, considering serine and metalloproteases (acting on clotting factors or with hemorrhagic activity), as well as phospholipase A2 (enzymes involved in inflammation and clotting processes) inhibitors of wide application in medical and biotechnology areas.
Los venenos de serpientes son ampliamente utilizados como herramientas de laboratorio para estudios de mecanismos fisiológicos, farmacéuticos y toxicológicos. Los venenos son recursos ricos en diferentes clases de proteasas que actúan sobre los factores de la cascada de coagulación, fibrinogenólisis y fibrinólisis, alterando los procesos homeostáticos y las fosfolipasas A2, los cuales están involucrados en procesos inflamatorios y de coagulación. Los productos naturales como los aceites esenciales se componen de ingredientes activos de amplia aplicación en las industrias alimentaria, farmacéutica y cosmética. El presente estudio evalúa los aceites esenciales de Mentha viridis y Mentha pulegium sobre la coagulación, fibrinogenólisis y degradación de azocaseína, inducida por los venenos de Bothrops sp. y Lachesis muta muta. Los aceites esenciales fueron obtenidos por hidrodestilación y sus componentes principales fueron identificados respectivamente como el linalool (40.70 %), carvona (13.52 %) y α-terpineno (8.56 %); pulegone (50.01 %), mentol (31.9 %) y mentona (15.56 %). Los aceites esenciales fueron previamente incubados con veneno de Bothrops alternatus, durante dos tiempos diferentes, luego se agregó el plasma y fue registrado el tiempo. El aceite de M. viridis presentó el más grande potencial anticoagulante. Mientras tanto, el aceite de M. pulegium presentó actividad anticoagulante o procoagulante dependiendo de la dosis evaluada. El tiempo de incubación también influyó en el efecto de los aceites sobre el tiempo de coagulación. En el ensayo azocaseínolitico, el aceite de M. pulegium redujo la actividad para todos los venenos evaluados. La inhibición más alta inducida para el veneno de B. jararacussu fue de 39.99 %, para M. viridis la actividad fue reducida en 57.72 %, mientras que para B. moojeni, la mayor inhibición observada fue de 74.67 %. La fibrinogenólisis inducida por el veneno de B. moojeni fue totalmente inhibida por ambos aceites en las proporciones evaluadas. Los resultados muestran la presencia de inhibidores de proteasas en los aceites, como las serinas y metaloproteasas (actuando sobre los factores de coagulación o sobre la actividad hemorrágica), como también fosfolipasas A2 (enzimas involucradas en los procesos de inflamación y coagulación), los cuales son inhibidores de amplia aplicación en áreas médicas y biotecnológicas.
ABSTRACT
A leishmaniose, segundo a Organização Mundial de Saúde, é uma das mais negligenciadas doenças tropicais re-emergentes, sendo reportada em várias partes do globo. Diante das dificuldades encontradas com as drogas disponíveis no mercado atualmente, como a elevada toxicidade e, em alguns casos, resistência por parte do parasito, inúmeras pesquisas tem sido realizadas com o objetivo de encontrar novas alternativas para o tratamento da leishmaniose. Nesse contexto, chama-se a atenção para o foco em compostos oriundos de plantas, as quais podem apresentar moléculas que tragam bons resultados no futuro. O objetivo de presente trabalho foi o de realizar uma revisão bibliográfica sobre produtos naturais utilizados em pesquisas com Leishmania como potenciais agentes utilizados como forma de tratamento contra o referido parasita. Foram analisados artigos científicos publicados nos últimos 5 anos nas bases eletrônicas de dados indexados na base de dados da LILACS, PubMed e ScienceDirect, utilizando os descritores em português "plantas medicinais", "leishmania" e seus correspondentes em Inglês. Selecionaram-se 61 artigos de estudos científicos, oriundos de 17 países, a maioria realizada no Brasil e Índia. Com base nos mecanismos de ação propostos pelos autores dos trabalhos realizados com amastigotos de Leishmania, grande parte está associada com estresse oxidativo na célula e com alterações no ambiente do macrófago, criando espécies reativas que funcionam como microbicidas. É possível que um composto ativo de uma planta tenha mais de um alvo na célula, sendo capaz de interferir de diferentes maneiras, dependendo do tipo celular e dos alvos disponíveis. As vantagens da utilização da fitoterapia incluem o baixo custo, baixa incidência de efeitos colaterais e sua efetividade. Além disso, é importante que sejam consideradas as espécies vegetais disponíveis no local, visando à diminuição nos custos do fitoterápico.
According to the World Health Organization, Leishmaniasis is one of the most neglected re-emerging tropical diseases, being reported in several parts of the globe. In view of the difficulties encountered with drugs currently available on the market, such as high toxicity and, in some cases, resistance by the parasite, research has been carried out to find new alternatives for treating this disease. The objective of this study was to carry out a literature review on natural products used in Leishmania studies as potential treatment agents against that parasite. Scientific papers published in the past five years on the LILACS, PubMed and ScienceDirect electronic databases were analyzed using the following descriptors in English language and their correspondent in Portuguese: "medicinal plants" and "leishmania". A total of 61 articles from 17 countries were selected, mostly from Brazil and India. Based on the action mechanisms proposed by the authors of the studies performed with Leishmania amastigotes, a great part is associated with the oxidative stress in the cell and with changes in the macrophage environment, creating reactive species that act as microbicides. It is possible that an active compound from a given plant has more than one target in the cell, being able to interfere in different ways depending on the cell type and available targets. The advantages of using phytotherapy include low cost, low incidence of side effects, and high effectiveness. In addition, it is important to consider locally available plant species aimed at reducing costs.
Subject(s)
Plants, Medicinal , Therapeutics , LeishmaniasisABSTRACT
ABSTRACT Coffee rust is a fungal disease that has affected every coffee-producing region in the world. Given that the effectivity of the protectant and systemic fungicides applied routinely to control the spread of the causative agent of the disease (Hemileia vastatrix) has gradually diminished, besides are harmful to mammals and ecosystems, the objective of this work was to search for a mixture of harmless natural compounds with the potential to be applied in the field. So, a yeast strain producing a battery of long-chain carboxylic acids (CA) with fungicide properties was isolated from soil of coffee crop and identified as Pichia membranifaciens by ITS sequencing. Culture conditions of the yeast were optimized and the CA in the solution were characterized by Gas Chromatography-Mass Spectrometry (GC-MS) as ethyl formate (55.5 g L-1), octadecenoic acid (3.5 g L-1), propionic acid (7.2 g L-1), 3-(octadecanoyl)-propionic acid (7.2 g L-1) and methyl acetate (8.4 g L-1). Randomized field studies were conducted in three different locations in Chiapas, México. Five treatments were tested including three concentrations of the CA solution (389, 584 and 778 ppm) and copper oxychloride (5 000 ppm) as conventional control. The initial coffee rust incidence averages varied between sites: Maravillas (3-9%), Santo Domingo (10-16%) and Búcaro (16-22%). The treatments of CA solution proved to be effective at slowing down the progress of the rust disease even for the sites where initial incidence was high. Likewise, the CA solution reduced the viability of H. vastatrix spores, as assessed by fluorescence microscopy.
RESUMO A ferrugem do cafeeiro é uma doença que tem afetado as regiões produtoras de café no mundo. Considerando que os funguicidas protetores e sistemáticos que são aplicados rotinariamente para controlar a difusão do agente causador da doença (Hemileia vastatrix) são nocivos para os humanos, animais e ecossistemas, o objetivo deste trabalho é determinar um componente natural com potencial de uso. Uma cepa de levedura produzindo uma bateria de ácidos carboxílicos com ação funguicida foi isolada do solo e identificada como Pichia membranifaciens por sequenciamento ITS. Foram optimizadas as condições de cultura e os ácidos carboxílicos presentes na semi purificada sobrenadante (solução CA) foram caracterizados por cromatografia de gás espectometia de massa (GC-MS) como formato de etilo (55.5 g L-1), ácido octadecenóico (3.5 g L-1), ácido propiônico (7.2 g L-1), 3-(octadecanoil)-ácido propiônico 7.2 g L-1) e acetato de metilio (8.4 g L-1). Estudos do campo foram conduzidos em três locais na região de Chiapas, Mexico. Cinco tratamentos foram testados incluindo três concentrações da solução CA (389, 584 e 778 ppm) e o funguicida comercial contendo oxicloreto de cobre (500 ppm). As médias iniciais de incidência da ferrugem do cafeeiro variou em função do local: Maravilla (3-9%), Santo domingo (10-16%) e Búcaro (16-22%). A solução CA provou ser efetiva retardando o progresso da doença, mesmo nos locais onde a incidência inicial foi elevada. A solução CA reduziu a viabilidade dos esporos de H. Vastatrix, observado por meio de fluorescência.
ABSTRACT
The aim of this study was to identify the composition of the essential oil from leaves of Lippia sidoides (EOLS), a typical shrub commonly found in the dry northeast of Brazil, popularly known as “alecrim-pimenta”. Additionally, we investigated the nymphicidal, ovicidal, phagoinhibitory and excretion effects of EOLS, its major constituent thymol and its isomer carvacrol, on fourth instar nymphs and eggs of Rhodnius prolixus, the Chagas’ disease vector. The nymphicidal and ovicidal activity of thymol, carvacrol, and EOLS was assessed by tests using impregnated Petri dishes. The lethal concentration values (LC50) for EOLS, carvacrol, and thymol were 54.48, 32.98, and 9.38 mg/cm2, respectively. The ovicidal test showed that both carvacrol and thymol (50 mg/cm2) inhibited hatching (50% and 23.3%, respectively), while treatments with 10 mg/cm2 or 50 mg/cm2 EOLS did not affect the hatching rate at all (80% and 90%, respectively). We observed an anti-feeding effect in insects fed with blood containing natural products at the higher concentrations (100 µg/mL). Finally, excretion rate was affected by EOLS and carvacrol, but not by thymol. These findings offer novel insights into basic physiological processes that make the tested natural compounds interesting candidates for new types of insecticides.
Subject(s)
Animals , Rhodnius/parasitology , Cytotoxins/chemistry , Lippia , Biological AvailabilityABSTRACT
Traditional treatment of infectious diseases is based on compounds that aim to kill or inhibit bacterial growth. The bacterial resistance against antibiotics is a serious issue for public health. Today, new therapeutic targets other than the bacterial wall were deciphered. Quorum sensing or bacterial pheromones are molecules called auto-inducer secreted by bacteria to regulate some functions such as antibiotic resistance and biofilms formation. This therapeutic target is well-studied worldwide, nevertheless the scientific data are not updated and only recent researches started to look into its potential as a target to fight against infectious diseases. A major concern with this approach is the frequently observed development of resistance to antimicrobial compounds. Therefore, this paper aims to provide a current overview of the quorum sensing system in bacteria by revealing their implication in biofilms formation and the development of antibiotic resistance, and an update on their importance as a potential target for natural substances.
ABSTRACT
Leishmaniasis is considered as an emerging, uncontrolled disease and is endemic in 98 countries. Annually, about 2 million cases of cutaneous and 500 000 cases of visceral-type leishmaniasis are recorded and 60 000 persons died from the disease. In Mexico, cutaneous leishmaniasis is known as chiclero's ulcer and is reported in 22 states, it is considered as a health problem. For its treatment, pentavalent antimonial drugs are administered. These drugs cause severe side effects, are costly. Drug-resistant cases have been reported and have been developing for over 70 years. One alternative to the drugs that are currently available is to find active molecules in medicinal plants. Dihydrocorynantheine, corynantheine and corynantheidine are active against Leishmania major, while harmane, pleiocarpin, buchtienin, luteolin and quercetin are active against Leishmania donovani. In Mexico, about 20 medicinal plants have been evaluated against Leishmania mexicana, among which the most active are Tridax procumbens, Lonchocarpus xuul and Pentalinon andrieuxii. From these plants, active compounds with IC
ABSTRACT
Traditional treatment of infectious diseases is based on compounds that aim to kill or inhibit bacterial growth. The bacterial resistance against antibiotics is a serious issue for public health. Today, new therapeutic targets other than the bacterial wall were deciphered. Quorum sensing or bacterial pheromones are molecules called auto-inducer secreted by bacteria to regulate some functions such as antibiotic resistance and biofilms formation. This therapeutic target is well-studied worldwide, nevertheless the scientific data are not updated and only recent researches started to look into its potential as a target to fight against infectious diseases. A major concern with this approach is the frequently observed development of resistance to antimicrobial compounds. Therefore, this paper aims to provide a current overview of the quorum sensing system in bacteria by revealing their implication in biofilms formation and the development of antibiotic resistance, and an update on their importance as a potential target for natural substances.
ABSTRACT
Leishmaniasis is considered as an emerging, uncontrolled disease and is endemic in 98 countries. Annually, about 2 million cases of cutaneous and 500000 cases of visceral-type leishmaniasis are recorded and 60000 persons died from the disease. In Mexico, cutaneous leishmaniasis is known as chiclero's ulcer and is reported in 22 states, it is considered as a health problem. For its treatment, pentavalent antimonial drugs are administered. These drugs cause severe side effects, are costly. Drug-resistant cases have been reported and have been developing for over 70 years. One alternative to the drugs that are currently available is to find active molecules in medicinal plants. Dihydrocorynantheine, corynantheine and corynantheidine are active against Leishmania major, while harmane, pleiocarpin, buchtienin, luteolin and quercetin are active against Leishmania donovani. In Mexico, about 20 medicinal plants have been evaluated against Leishmania mexicana, among which the most active are Tridax procumbens, Lonchocarpus xuul and Pentalinon andrieuxii. From these plants, active compounds with IC ≤ 30 μg/mL or μM have been isolated, such as 3(S)-16,17-didehydrofalcarinol or Oxylipin, cholestra-4,20,24-trien-3-one or pentalinosterol, 24-methylcholest-4-24(28)-dien-3-one, cholest-4-en-3-one, 6,7-dihydroneridie-none, neridienone, cholest-5,20,24-trien-3β-ol, and isocordoin. Today, only pentalinonsterol has been synthesized and assayed in the visceral leishmaniasis experimental model using BALB/c mice infected with Leishmania donovani. Liposome formulation of this compound administered by intravenous route at 2.5 mg/kg showed a significant reduction of parasite load in mouse liver and spleen.
ABSTRACT
ABSTRACT Natural compounds are a gold mine for treating rheumatoid arthritis (RA). The etiology of this disease is linked to inflammation, where cytokines play an important role. Strategies have been drafted for targeting cytokines as a therapeutic option in patients with RA. Inhibiting cytokines with natural compounds has become a major focus for the development of drugs to treat RA. Here, a structure-based drug design approach was employed to identify novel leads to target the interleukin 6 receptor (IL-6R). A total of 48,531 compounds of natural origin were screened. Two of these compounds were shortlisted for molecular docking simulation and tested for inhibiting gp130 dimerization in human macrophages. The results show that Lead5 (CID5329098) significantly inhibited the release of gp130 in a dose-dependent manner, similar to the inhibitory effect of LMT-28 (p<0.005). This study provides an atomic scale outcome of a single natural compound that can be developed into a RA drug
Subject(s)
Arthritis, Rheumatoid/drug therapy , Cytokines , Receptors, Interleukin , Antirheumatic Agents/analysisABSTRACT
Drug-induced liver injury encompasses a spectrum of diseases ranging from mild biochemical abnormalities to acute liver failure; example of this scenery is hepatotoxicity caused by the first-line antituberculous drugs isoniazid, rifampin and pyrazinamide, which are basic for treatment of drug-sensible and drug-resistant tuberculosis. In the search for pharmacological alternatives to prevent liver damage, antitubercular drugs have been the subject of numerous studies and published reviews, a great majority of them carried out by Asian countries. At the same time, hepatoprotectors from plant source are now emerging as a possible alternative to counteract the toxic effects of these therapeutic agents. The present review aims to highlight the most recent studies on the subject, based information published in scientific databases such as Scopus and PubMed.
ABSTRACT
Drug-induced liver injury encompasses a spectrum of diseases ranging from mild biochemical abnormalities to acute liver failure; example of this scenery is hepatotoxicity caused by the first-line antituberculous drugs isoniazid, rifampin and pyrazinamide, which are basic for treatment of drug-sensible and drug-resistant tuberculosis. In the search for pharmacological alternatives to prevent liver damage, antitubercular drugs have been the subject of numerous studies and published reviews, a great majority of them carried out by Asian countries. At the same time, hepatoprotectors from plant source are now emerging as a possible alternative to counteract the toxic effects of these therapeutic agents. The present review aims to highlight the most recent studies on the subject, based information published in scientific databases such as Scopus and PubMed.