Indications for the use of cannabinoids / Indicação do uso de canabinoides

ABSTRACT BACKGROUND AND OBJECTIVES: The increasingly widespread use of cannabinoids in the management of acute and chronic pain generates an urgent need to study how cannabinoids act on CB1 and CB2 receptors and what their effects are on the organism. It is important to understand the difference in action between natural cannabinoids (cannabidiol, delta 9-tetrahydrocannabinol, cannabigerol, cannabinoil, terpenes) and synthetic ones, so that the appropriate choice is made in each case, and depending on the pathophysiology of pain, one or the other active is more indicated. CONTENTS: Studies collected in the Pubmed, Cochrane Library and Web of Science databases were analyzed. These studies focus were on natural cannabinoids (cannabidiol, delta 9-tetrahydrocannabinol, cannabigerol, cannabinoil, terpenes) and synthetic cannabinoids in the use for the treatment of chronic pain, their action on the endocannabinoid system through the activation of the CB1 and CB2 receptor and their effect after activating this receptor, aiming to compile which cannabinoid is more indicated in the treatment of pain pathology. CONCLUSION: The subject still requires much study and new articles are being published daily. The analysis of the studies must be carried out with criteria to evaluate their seriousness. The endocannabinoid system is closely linked to the treatment of chronic pain and some cannabinoids such as: cannabidiol, delta 9-tetrahydrocannabinol, cannabigerol, cannabinoil, as well as some terpenes are already considered important in the treatment of chronic pain inferring sparing effect of opioids, anticonvulsants, antidepressants among others.

RESUMO JUSTIFICATIVA E OBJETIVOS: O uso cada vez mais disseminado dos canabinoides no controle da dor aguda e crônica gera uma necessidade urgente do estudo de como os canabinoides agem nos receptores CB1 e CB2 e quais seus efeitos no organismo. É importante entender a diferença de ação entre os canabinoides naturais (canabidiol, delta 9-tetrahidrocanabinol, canabigerol, canabinol, terpenos) e os sintéticos, para que a escolha adequada seja realizada em cada caso, sendo que dependendo da fisiopatologia da dor é mais indicado um ou outro ativo. CONTEÚDO: Foram analisados estudos coletados na Pubmed, Cochrane Library e Web of Science. Os estudos se concentram em canabinoides naturais (canabidiol, delta 9-tetrahidrocanabinol, canabigerol, canabinoil, terpenos) e canabinoides sintéticos no uso para o tratamento da dor crônica, sua ação no sistema endocanabinoide através da ativação do receptor CB1 e CB2 e seu efeito após ativar esse receptor, visando compilar qual canabinoide é mais indicado no tratamento da patologia álgica. CONCLUSÃO: O assunto ainda requer muito estudo e diariamente novos artigos vem sendo publicados. A análise dos estudos deve ser realizada com critério para avaliar sua seriedade. O sistema endocanabinoide está intimamente ligado ao tratamento da dor crônica e alguns canabinoides como: canabidiol, delta 9-tetrahidrocanabinol, canabigerol, canabinoil, assim como alguns terpenos já são considerados importantes no tratamento da dor crônica inferindo efeito poupador de opioides, anticonvulsivantes, antidepressivos entre outros.

Perillyl alcohol modulates activation, permeability and integrity of human brain endothelial cells induced by Plasmodium falciparum

BACKGROUND Cerebral malaria (CM) is a severe immunovasculopathy caused for Plasmodium falciparum infection, which is characterised by the sequestration of parasitised red blood cells (pRBCs) in brain microvessels. Previous studies have shown that some terpenes, such as perillyl alcohol (POH), exhibit a marked efficacy in preventing cerebrovascular inflammation, breakdown of the brain-blood barrier (BBB) and brain leucocyte accumulation in experimental CM models. OBJECTIVE To analyse the effects of POH on the endothelium using human brain endothelial cell (HBEC) monolayers co-cultured with pRBCs. METHODOLOGY The loss of tight junction proteins (TJPs) and features of endothelial activation, such as ICAM-1 and VCAM-1 expression were evaluated by quantitative immunofluorescence. Microvesicle (MV) release by HBEC upon stimulation by P. falciparum was evaluated by flow cytometry. Finally, the capacity of POH to revert P. falciparum-induced HBEC monolayer permeability was examined by monitoring trans-endothelial electrical resistance (TEER). FINDINGS POH significantly prevented pRBCs-induced endothelial adhesion molecule (ICAM-1, VCAM-1) upregulation and MV release by HBEC, improved their trans-endothelial resistance, and restored their distribution of TJPs such as VE-cadherin, Occludin, and JAM-A. CONCLUSIONS POH is a potent monoterpene that is efficient in preventing P. falciparum-pRBCs-induced changes in HBEC, namely their activation, increased permeability and alterations of integrity, all parameters of relevance to CM pathogenesis.

Study of the interactions of di- and tri-terpenes from Stillingia loranthacea with the enzyme NSP16-NSP10 of SARS-CoV-2 / Estudo das interações de di- e tri-terpenos de Stillingia loranthacea com a enzima NSP16-NSP10 de SARS-CoV-2

Objective: This study aimed to evaluate the interactions of di- and tri-terpenes from Stillingia loranthacea with the enzyme NSP16-NSP10 of SARS-CoV-2, important for viral replication. Methods: The molecular docking technique was used to evaluate this interaction. Results: The analysis showed that the evaluated compounds obtained RMSD values of 0.888 to 1.944 Å and free energy of -6.1 to -9.4 kcal/mol, with the observation of hydrogen bonds, salt bridges, and pi-sulfur, pi-alkyl, and hydrophobic interactions. Conclusion: Thus, the results obtained show the potential of the compounds analyzed against the selected target. Since computer simulations are only an initial step in projects for the development of antiviral drugs, this study provides important data for future research.

Objetivo: avaliar as interações de di- e tri-terpenos de Stillingia loranthacea com a enzima NSP16-NSP10 de SARS-CoV-2, importante para a replicação viral. Métodos: A técnica de docking molecular foi utilizada para avaliar essa interação. Resultados: A análise mostrou que os compostos avaliados obtiveram valores de RMSD de 0,888 a 1,944 Å e energia livre de -6,1 a -9,4 kcal/mol, observando-se ligações de hidrogênio, pontes salinas e pi-enxofre, pi-alquil, e interações hidrofóbicas. Conclusão: Assim, os resultados obtidos mostram o potencial dos compostos analisados frente ao alvo selecionado. Como as simulações computacionais são apenas um passo inicial nos projetos de desenvolvimento de medicamentos antivirais, este estudo fornece dados importantes para pesquisas futuras.

Phytotoxicity of plant extracts of Vismia japurensis cultivated in vivo and in vitro / Fitotoxicidade de extratos de plantas de Vismia japurensis cultivadas in vivo e in vitro

Plants that produce secondary metabolites with allelopathic activity or phytotoxicity can be biotechnologically important, serving as sources of allelochemicals, and thus contributing to the agroindustrial sector. Vismia japurensis (Hypericaceae) is an Amazonian species that grows in clumps called vismiais, from which most other plants are absent. Accordingly, the objective of this study was to identify possible phytotoxicity effects of hexane and methanol extracts of Vismia japurensis leaves and branches in vivo and from seedlings grown in vitro on Lactuca sativa. In addition, fresh and dry leaves were assayed by the sandwich method in order to determine their ability to release allelochemicals. The hexanic extract from in vitro seedlings reduced germination by 10%, while the methanol extract produced a 16% reduction in germination speed. Root growth of Lactuca sativa was inhibited by 64.7% when subjected to hexane leaf extract, by 39.3% under the influence of hexane branch extract, and by 96.09% for in vitro seedling hexanic extract. When analysed by thin layer chromatography and 1H nuclear magnetic resonance, extracts showed evidence of terpenes, anthraquinones and flavonoids, with greater intensity of signals in the aromatic region of in vitro seedling hexanic extract. Clearly, Vismia japurensis has a high biotechnological potential in terms of the production of substances of low polarity with capacity to interfere in plant development.

Plantas que produzem metabólitos secundários com atividade alelopática ou fitotóxica podem ser biotecnologicamente importantes, servindo como fontes de aleloquímicos e, assim, contribuindo para o setor agroindustrial. Vismia japurensis (Hypericaceae) é uma espécie amazônica que cresce em grupos, formando vismiais. Assim, o objetivo deste estudo foi identificar possíveis efeitos fitotóxicos de extratos hexânicos e metanólicos de folhas e ramos de Vismia japurensis in vivo e de plântulas cultivadas in vitro sobre Lactuca sativa. Além disso, folhas frescas e secas foram analisadas pelo método sanduíche, a fim de determinar sua capacidade de liberação de aleloquímicos. O extrato hexânico de plântulas in vitro reduziu a germinação em 10% e o extrato metanólico promoveu uma redução de 16% na velocidade de germinação. O crescimento radicular de Lactuca sativa foi inibido em 64,7% quando submetido ao extrato hexânico das folhas, em 39,3% sob influência do extrato hexânico dos galhos e em 96,09% para o extrato de hexânico das plântulas in vitro. Quando analisados por cromatografia em camada delgada e ressonância magnética nuclear de 1H, os extratos mostraram evidências de terpenos, antraquinonas e flavonoides, com maior intensidade de sinais na região aromática do extrato hexânico das plântulas in vitro. Assim, Vismia japurensis possui elevado potencial biotecnológico em termos de produção de substâncias de baixa polaridade com capacidade de interferência no desenvolvimento de plantas.

Evaluation of copaiba oil as enhancer of ibuprofen skin permeation

Abstract The administration of medications on the skin through transcutaneous routes is a practice that has been used by mankind for millennia. Some studies have been reporting the use of terpenes and natural oils rich in terpenes as an enhancer of cutaneous penetration. Copaiba oil, due to its rich content of terpenes, presents itself as a great choice of penetration enhancer for drugs administered on the skin. In this study, we developed two cream formulations containing 5% of ibuprofen (IBU) and copaiba oil: IBCO5 and IBCO10 with 5% and 10% of copaiba oil respectively. Ex vivo cutaneous penetration/permeation studies of IBU were performed using pig ear skin as biological membrane in the Franz-type diffusion cells. The steady-state flux of IBU samples, IBCO5 (35.72 ± 6.35) and IBCO10 (29.78 ± 2.41) were significantly higher when compared with control without copaiba oil (10.32 ±1.52) and with a commercial product (14.44 ± 2.39). In the penetration analysis, the amount of IBU found in the samples IBCO5 and IBCO10 was markedly higher in the dermis than epidermis. Our results showed that copaiba oil possesses attracting properties in promoting skin penetration and permeation of IBU when added into cream formulations.

Phytotoxicity of plant extracts of Vismia japurensis cultivated in vivo and in vitro / Fitotoxicidade de extratos de plantas de Vismia japurensis cultivadas in vivo e in vitro

Plants that produce secondary metabolites with allelopathic activity or phytotoxicity can be biotechnologically important, serving as sources of allelochemicals, and thus contributing to the agroindustrial sector. Vismia japurensis (Hypericaceae) is an Amazonian species that grows in clumps called vismiais, from which most other plants are absent. Accordingly, the objective of this study was to identify possible phytotoxicity effects of hexane and methanol extracts of Vismia japurensis leaves and branches in vivo and from seedlings grown in vitro on Lactuca sativa. In addition, fresh and dry leaves were assayed by the sandwich method in order to determine their ability to release allelochemicals. The hexanic extract from in vitro seedlings reduced germination by 10%, while the methanol extract produced a 16% reduction in germination speed. Root growth of Lactuca sativa was inhibited by 64.7% when subjected to hexane leaf extract, by 39.3% under the influence of hexane branch extract, and by 96.09% for in vitro seedling hexanic extract. When analysed by thin layer chromatography and 1H nuclear magnetic resonance, extracts showed evidence of terpenes, anthraquinones and flavonoids, with greater intensity of signals in the aromatic region of in vitro seedling hexanic extract. Clearly, Vismia japurensis has a high biotechnological potential in terms of the production of substances of low polarity with capacity to interfere in plant development.

Plantas que produzem metabólitos secundários com atividade alelopática ou fitotóxica podem ser biotecnologicamente importantes, servindo como fontes de aleloquímicos e, assim, contribuindo para o setor agroindustrial. Vismia japurensis (Hypericaceae) é uma espécie amazônica que cresce em grupos, formando vismiais. Assim, o objetivo deste estudo foi identificar possíveis efeitos fitotóxicos de extratos hexânicos e metanólicos de folhas e ramos de Vismia japurensis in vivo e de plântulas cultivadas in vitro sobre Lactuca sativa. Além disso, folhas frescas e secas foram analisadas pelo método sanduíche, a fim de determinar sua capacidade de liberação de aleloquímicos. O extrato hexânico de plântulas in vitro reduziu a germinação em 10% e o extrato metanólico promoveu uma redução de 16% na velocidade de germinação. O crescimento radicular de Lactuca sativa foi inibido em 64,7% quando submetido ao extrato hexânico das folhas, em 39,3% sob influência do extrato hexânico dos galhos e em 96,09% para o extrato de hexânico das plântulas in vitro. Quando analisados por cromatografia em camada delgada e ressonância magnética nuclear de 1H, os extratos mostraram evidências de terpenos, antraquinonas e flavonoides, com maior intensidade de sinais na região aromática do extrato hexânico das plântulas in vitro. Assim, Vismia japurensis possui elevado potencial biotecnológico em termos de produção de substâncias de baixa polaridade com capacidade de interferência no desenvolvimento de plantas.

Phytotoxicity of plant extracts of Vismia japurensis cultivated in vivo and in vitro

Abstract Plants that produce secondary metabolites with allelopathic activity or phytotoxicity can be biotechnologically important, serving as sources of allelochemicals, and thus contributing to the agroindustrial sector. Vismia japurensis (Hypericaceae) is an Amazonian species that grows in clumps called vismiais, from which most other plants are absent. Accordingly, the objective of this study was to identify possible phytotoxicity effects of hexane and methanol extracts of Vismia japurensis leaves and branches in vivo and from seedlings grown in vitro on Lactuca sativa. In addition, fresh and dry leaves were assayed by the sandwich method in order to determine their ability to release allelochemicals. The hexanic extract from in vitro seedlings reduced germination by 10%, while the methanol extract produced a 16% reduction in germination speed. Root growth of Lactuca sativa was inhibited by 64.7% when subjected to hexane leaf extract, by 39.3% under the influence of hexane branch extract, and by 96.09% for in vitro seedling hexanic extract. When analysed by thin layer chromatography and 1H nuclear magnetic resonance, extracts showed evidence of terpenes, anthraquinones and flavonoids, with greater intensity of signals in the aromatic region of in vitro seedling hexanic extract. Clearly, Vismia japurensis has a high biotechnological potential in terms of the production of substances of low polarity with capacity to interfere in plant development.

Resumo Plantas que produzem metabólitos secundários com atividade alelopática ou fitotóxica podem ser biotecnologicamente importantes, servindo como fontes de aleloquímicos e, assim, contribuindo para o setor agroindustrial. Vismia japurensis (Hypericaceae) é uma espécie amazônica que cresce em grupos, formando vismiais. Assim, o objetivo deste estudo foi identificar possíveis efeitos fitotóxicos de extratos hexânicos e metanólicos de folhas e ramos de Vismia japurensis in vivo e de plântulas cultivadas in vitro sobre Lactuca sativa. Além disso, folhas frescas e secas foram analisadas pelo método sanduíche, a fim de determinar sua capacidade de liberação de aleloquímicos. O extrato hexânico de plântulas in vitro reduziu a germinação em 10% e o extrato metanólico promoveu uma redução de 16% na velocidade de germinação. O crescimento radicular de Lactuca sativa foi inibido em 64,7% quando submetido ao extrato hexânico das folhas, em 39,3% sob influência do extrato hexânico dos galhos e em 96,09% para o extrato de hexânico das plântulas in vitro. Quando analisados por cromatografia em camada delgada e ressonância magnética nuclear de 1H, os extratos mostraram evidências de terpenos, antraquinonas e flavonoides, com maior intensidade de sinais na região aromática do extrato hexânico das plântulas in vitro. Assim, Vismia japurensis possui elevado potencial biotecnológico em termos de produção de substâncias de baixa polaridade com capacidade de interferência no desenvolvimento de plantas.

Actividad antibacteriana de un extracto etanólico de propóleo peruano frente a Streptococcus mutans / Antibacterial activity of a Peruvian propolis ethanolic extract against Streptococcus mutans

Introducción: Los derivados del propóleo poseen propiedades antimicrobianas importantes y presentan un potencial uso para la prevención y tratamiento de la caries dental. Objetivo: Evaluar la actividad antibacteriana de un extracto etanólico de propóleo peruano frente a Streptococcus mutans. Métodos: Se obtuvo el extracto etanólico de propóleo por maceración en alcohol al 70 por ciento durante 15 días. El extracto etanólico de propóleo fue diluido con agua destilada para obtener concentraciones de 75 por ciento, 50 por ciento y 25 por ciento. La actividad antibacteriana se evaluó mediante la prueba de difusión en disco sobre medio agar cerebro-corazón inoculado con S. mutans ATCC® 25175™, se empleó clorhexidina (CHX) al 0,12 por ciento como control. Las placas de Petri fueron incubadas por 48 horas a 37 ºC en condiciones de microaerofilia. Posteriormente se realizó la medición de los halos de inhibición con un compás Vernier. Resultados: Todas las concentraciones del extracto etanólico de propóleo presentaron actividad antibacteriana frente al S. mutans (25 por ciento = 17,582 ± 2,578 mm; 50 por ciento = 16,906 ± 1,892 mm; 75 por ciento = 16,881 ± 2,013 mm; 100 por ciento = 17,201 ± 1,305 mm). Sin embargo, fueron menores que la CHX al 0,12 por ciento (24,543 ± 2,486 mm) (p < 0,05). Según la escala de Duraffourd, S. mutans fue sensible (+) y muy sensible (++) para todas las concentraciones del extracto etanólico de propóleo, mientras que para CHX al 0,12 % fue sumamente sensible (+++) (p < 0,05). Conclusiones: El extracto etanólico de propóleo peruano presenta actividad antibacteriana significativa considerada como sensible y muy sensible frente a S. mutans(AU)

Introduction: Due to their important antimicrobial properties, propolis by-products are potentially useful for the prevention and treatment of dental caries. Objective: Evaluate the antibacterial activity of a Peruvian propolis ethanolic extract against Streptococcus mutans. Methods: The propolis ethanolic extract was obtained by maceration in 70 percent alcohol for 15 days. The extract was diluted in distilled water to obtain concentrations of 75 percent , 50 percent and 25 percent . Antibacterial activity was evaluated by the disk diffusion test in brain heart agar medium inoculated with S. mutans ATCC® 25175™. Chlorhexidine (CHX) 0.12 percent was used as control. The Petri plates were incubated for 48 hours at 37ºC in microaerophilic conditions. The inhibition haloes were then measured with a Vernier caliper. Results: All the concentrations of the propolis ethanolic extract displayed antibacterial activity against S. mutans: 25 percent = 17.582 ± 2.578 mm; 50 percent = 16.906 ± 1.892 mm; 75 percent = 16.881 ± 2.013 mm; 100 percent = 17.201 ± 1.305 mm. However, values were lower than those of 0.12 percent CHX: 24.543 ± 2.486 mm (p < 0.05). According to the Duraffourd scale, S. mutans was sensitive (+) and very sensitive (++) to all propolis ethanolic extract concentrations, and highly sensitive to 0.12 percent chlorhexidine (+++) (p < 0.05). Conclusions: The Peruvian propolis ethanolic extract displays significant antibacterial activity against S. mutans. Such activity was evaluated as sensitive and very sensitive(AU)

Efeitos antifúngico e antiaflatoxigênico de timol e carvacrol em Aspergillus flavus / Antifungal and antiaflatoxigenic activities of thymol and carvacrol against Aspergillus flavus

O objetivo deste estudo foi avaliar os efeitos do timol e carvacrol contra Aspergillus flavus e a produção de aflatoxinas. Foram determinadas a concentração inibitória mínima (CIM), o espectro fungitóxico e a atividade inibidora de micotoxinas pelo timol e carvacrol. Os resultados mostraram que timol e carvacrol exibiram ação fungicida de acordo com a CIM de 2500 e 30 µg mL-1, respectivamente. Tanto o timol quanto o carvacrol inibiram significativamente o crescimento de A. flavus (p<0,05) a partir de 600 e 15 µg mL-1, respectivamente. A biomassa fúngica, estimada pela determinação da concentração de ergosterol, foi significativamente reduzida (p <0,05) em 2500 µg mL-1 de timol e 250 µg mL-1 de carvacrol. O timol e o carvacrol exibiram efeitos antiaflatoxigênicos em 600 e 125 µg mL-1, respectivamente. O timol e o carvacrol exibiram atividade antifúngica, mas não exibiram alta atividade antiaflatoxigênica. Carvacrol e timol podem ser considerados como potentes compostos naturais antifúngicos contra A. flavus.

The aim of this study was to evaluate the effects of thymol and carvacrol upon production of aflatoxins by Aspergillus flavus and upon its growth. Minimal inhibitory concentration (MIC), fungitoxic spectrum and mycotoxin inhibition were assessed. Results showed thymol and carvacrol exhibited fungicidal action, as determined by MIC values of 2500 and 30 µg mL-1, respectively. Both thymol and carvacrol significantly inhibited growth of A. flavus (p<0.05) at concentrations of 600 and 15 µg mL-1, respectively. Fungal biomass, as estimated by determination of ergosterol concentration, was significantly reduced (p<0.05) at thymol concentrations of 2500 µg mL-1 and at carvacrol concentrations of 250 µg mL-1. Thymol and carvacrol exhibited antiaflatoxigenic effects at concentrations of 600 and 125 µg mL-1, respectively. While both thymol and carvacrol showed possessing antifungal activities, neither were highly antiaflatoxigenic. Carvacrol and thymol might be considered for use as potential antifungal natural compounds against A. flavus.

Efficacy and residual effect of Illicium verum (star anise) and Pelargonium graveolens (rose geranium) essential oil on cat fleas Ctenocephalides felis felis / Eficácia e efeito residual dos óleos essenciais de Illicium verum (anis-estrelado) e Pelargonium graveolens (gerânio rosa) em pulgas de gato Ctenocephalides felis felis

Abstract The essential oils (EOs) of Illicium verum and Pelargonium graveolens were evaluated for lethality, inhibition of development and residual efficacy against the flea Ctenocephalides felis felis. Their chemical composition was characterized by means of gas chromatography with a flame ionization and mass spectrometry detection. Mortality at different immature stages and among adult fleas was measured through in vitro filter paper tests at different concentrations of EOs. The chemical characterization of I. verum volatile oil showed that E-anethole (79.96%) was the major constituent, while the major compounds in P. graveolens were citronellol (29.67%) and geraniol (14.85%). Insecticidal activity against both immature and adult flea stages were observed. The EO of I. verum had insecticidal activity for approximately 18 days, while the EO activity of P. graveolens lasted for 13 days. The pulicidal activity of I. verum remained above 70% for up to 9 days, while the activity of P. graveolens was 41.7% for up to 2 days. Essential oils, especially that of I. verum, showed insecticidal activity for flea control at different life cycle stages and have potential for the development of ectoparasiticides (biopesticides) for veterinary use.

Resumo Os óleos essenciais (OE) de Illicium verum e Pelargonium graveolens foram avaliados quanto à letalidade, inibição do desenvolvimento e eficácia residual contra a pulga Ctenocephalides felis felis. Sua composição química foi caracterizada por meio de cromatografia gasosa com detector de ionização de chama e espectrometria de massas. A mortalidade entre os diferentes estágios imaturos e pulgas adultas foi avaliada por meio de testes in vitro em papel filtro, contendo diferentes concentrações de OEs. A caracterização química do óleo volátil de I. verum mostrou que o E-anetol (79,96%) foi o constituinte majoritário, enquanto os principais compostos de P. graveolens foram citronelol (29,67%) e geraniol (14,85%). Foi observada atividade inseticida contra os estágios imaturos e adulto da pulga. O OE de I. verum teve atividade inseticida por aproximadamente 18 dias, enquanto o de P. graveolens durou 13 dias. A atividade pulicida de I. verum permaneceu acima de 70% até o 9º dia, enquanto a atividade de P. graveolens foi de 41,7% até o 2º dia. Os óleos essenciais, principalmente de I. verum, apresentam atividade inseticida para o controle de pulgas em diferentes estágios do ciclo de vida e têm potencial para o desenvolvimento de ectoparasiticidas (biopesticidas) de uso veterinário.

Insecticidal Activity of Lavandula dentata L. Essential Oil on Anticarsia gemmatalis (Hübner, 1818)

Abstract Anticarsia gemmatalis, commonly known as soybean caterpillar, causes important economic losses in soybean crops. Synthetic pesticides are the standard practice to control this insect. However, the indiscriminate use of these substances has increased the resistance of this pest. Thus, it is necessary to search for different control alternatives that are also more environmentally friendly. The objective of this work was to evaluate the chemical composition of Lavandula dentata L. essential oil (EO) and its activity on A. gemmatalis. The major compounds of essential oil were 1,8-cineole (31.5 wt.%), camphor (16.6 wt.%), and fenchone (15.9 wt.%). Bioassays were performed with third-instar caterpillars. EO concentrations of 0.1, 0.2, 0.3, 0.4, 0.5, 0.6, 0.7, 0.8, 0.9, and 1.0% v/v were diluted in Tween-80® 0.5% v/v and incorporated into the artificial diet given to caterpillars. Water, Tween-80® 0.5% v/v, and novaluron 0.075% w/v were added as negative and positive controls. For the aversion tests, soybean leaf discs were immersed in solutions with 0.4, 0.6, 0.8, and 1.0% v/v of EO, plus a negative control (water), and offered to caterpillars. In the bioassay, 100% mortality was observed from the concentration 0.6% v/v of the essential oil of L. dentata in 24 h; without statistical difference from 0.4 and 0.5% v/v. There was no important change in mortality between 24 and 72 h. In the aversion test, all EO treatments caused deterrence of caterpillars when compared to control, but without difference between EO concentrations. It was observed that L. dentata EO can be used as an alternative in the control of A. gemmatalis.

Thymol, menthol and eucalyptol as agents for microbiological control in the oral cavity: A scoping review / Timol, mentol y eucaliptol como agentes para el control microbiológico en cavidad bucal: una revisión exploratoria

SUMMARY Dental plaque is a complex environment that maintains a balance with certain microbial communities; however, this microhabitat can be disturbed by some endogenous species causing disease. An exploratory systematic review was carried out using the PubMed, Scopus, Lilacs, and Science Direct databases, identifying that the thymol, menthol, and eucalyptol compounds present varying antimicrobial activity, intra- and interspecies discordance, and a strong antimicrobial intensity on Aggregatibacter actinomycetemcomitans, Candida albicans, Candida dubliniensis, Enterococcus faecalis, Escherichia coli, Lactobacillus plantarum, and Streptococcus mutans, indicating that these phytochemicals can be considered broad-spectrum antimicrobial substances, with an effect on microorganisms linked to oral diseases.

RESUMEN La placa dental es un ambiente complejo que mantiene un equilibrio con determinadas comunidades microbianas; sin embargo, este micro hábitat puede ser perturbado por algunas especies endógenas causando enfermedad. Se realizó una revisión sistemática exploratoria empleando las bases de datos Pubmed, Scopus, Lilacs y Science Direct y se identificó que los compuestos timol, mentol y eucaliptol presentan actividad antimicrobiana variable, discordancias intra e inter-especie y una intensidad antimicrobiana fuerte sobre Aggregatibacter actinomycetemcomitans, Candida albicans, Candida dubliniensis, Enterococcus faecalis, Escherichia coli, Lactobacillusplantarum and Streptococcus mutans; indicando que estos fitoquímicos pueden ser consideradas como sustancias antimicrobianas de amplio espectro, con efecto sobre microorganismos relacionados con enfermedades bucales.

Bioactivity of Schinus molle L. and Schinus terebinthifolia Raddi. Essential Oils on Anticarsia gemmatalis (Hübner 1818)

Abstract Anticarsia gemmatalis is one of the main pests of the soybean crop, being controlled mainly with agrochemicals. The environmental and health risks, as well as the development of resistance by the pests, has led to the search for alternative control measures, aiming to use more eco-friendly procedures. The objective of this research was to evaluate the chemical composition and the bioactivity of Schinus molle and Schinus terebinthifolia essential oils (EOs) on A. gemmatalis. The major compound in both EOs was α-pinene (60.04 wt.% for S. molle and 38.49 wt.% for S. terebinthifolia). Bioassays were carried out with third instar larvae, with five replicates and each replicate with ten larvae, totaling 50 larvae per treatment. The oils were incorporated in the artificial diet (0.1, 0.5, 1.0, 1.5, and 2.0% v/v). The controls were: water, Tween-80® 0.5% v/v, and novaluron 0.075% v/v. According to the Probit method, the S. terebinthifolia EO presented a LC50 of 1.74% v/v (1.58-1.97% v/v); it was not possible to determine the LC50 for the S. molle EO. The mortality percentage after 24 and 48 h was 52% and 30% at 2.0% v/v for S. terebinthifolia and S. molle oil, respectively. After 72 h, the mortality rate for S. molle EO have not changed; for S. terebinthifolia EO it increased to 70%; the larvae treated with the chemical control (synthetic insecticide) had a mortality of 100%.

Analysis of Chemical Constituents in Bushao Tiaozhi Capsules by UPLC-Q-TOF-MS / 中国实验方剂学杂志

Objective:To analyze the main chemical constituents of traditional Chinese medicine compound Bushao Tiaozhi capsules by using UPLC-Q-TOF-MS technology. Method:The separation was eluted with Waters CORTECS UPLC C18 column（2.1 mm×150 mm，1.6 μm） in a gradient mode， with methanol-0.1% formic acid as the mobile phase. The column temperature was 40 ℃，the flow rate was 0.24 mL·min-1，and the injection volume was 1 μL. The mass spectrometry condition was X500R QTOF mass spectrometry，the positive and negative electrospray ionization （ESI） was adopted for determine the chromatographic effluent，and the main chromatographic peaks were assigned and distinguished by Q-TOF. Result:A total of 53 chemical constituents were identified by reference confirmation，literature comparison，and high mass spectrometry data analysis. The chemical constituent cluster was composed of 21 flavonoids，10 phenolics，5 monoterpene glycosides，7 diterpene lactones and 10 sesquiterpenes. Furthermore，all of the constituents were surveyed and classified according to their medicinal materials derivation. Among them，the 5 flavonoids components（mangiferin，isoquercitrin，typhaneoside，isorhamnetin 3-O-neohesperidoside，tiliroside）were identified in Microctis Folium for the first time. Conclusion:This study shows that UPLC-Q-TOF-MS technology provides a simple，rapid，and accurate method for the identification of chemical constituents in Bushao Tiaozhi capsules. The identified chemical components mostly cover the main constituents of each medicinal material in the formula，so as to provide a new technological method and theoretical foundation for further defining the pharmacological basis and mechanism of action and optimizing the quality control of Bushao Tiaozhi capsules.

Effects of co-administration of Ganoderma terpenoid extract with chloroquine on inflammatory markers and antioxidant status in Plasmodium berghei-infected mice / 中西医结合学报

OBJECTIVE@#To understand the protective effects of Ganoderma terpenoid extract (GTE) against Plasmodium berghei-malarial infection in mice, the present study was carried out to evaluate the effects of GTE in combination with chloroquine disulphate (CQ) on erythrocyte-selected inflammatory markers and antioxidant defense status in P. berghei-infected mice.@*METHODS@#P. berghei-infected mice were divided into six groups: infected control (IC) group, administered 1 mL Tween 20; GTE@*RESULTS@#Infected mice treated with a combination of GTE and CQ (GT@*CONCLUSION@#Data generated in this study showed that GTE enhanced the anti-plasmodial action of CQ in mice through its anti-inflammatory and antioxidant activities.

Research progress of natural non-alkaloids with analgesic activity / 中国中药杂志

Pain is a complex, unpleasant feeling and emotional experience associated with actual or potential tissue damage, and manifests itself in certain autonomous psychological and behavioral responses. The commonly used opioid and non-steroidal anti-inflammatory analgesics(NSAIDs) may cause adverse reactions to the kidney, liver, cardiovascular or gastrointestinal system and cause problems of drug abuse. Therefore, it is necessary to study new analgesic drugs with less side effects and significant analgesic effects. A variety of natural products derived from terrestrial plants, microorganisms, marine organisms and fungi have been an important source of clinical medicines and provide an inexhaustible resource for the development and innovation of modern medicines. Therefore, this paper mainly reviews the natural non-alkaloids with analgesic activity in order to provide reference for the research and development of analgesic drugs derived from natural products.

Essential oils as a source of bioactive molecules / Aceites esenciales como fuentes de moléculas bioactivas

SUMMARY Nature gives us a large number of compounds with interesting biological properties, within them we have essential oils, which are an important source of new bioactive molecules, which can replace synthetic chemicals, since they are friendly to the environment and they are less toxic. Currently there are more than 20.000 publications in which essential oils are related to some biological activity, according to the search made in different databases until January 2018. This confirms the wide utility of essential oils as the main source of bioactive metabolites, which can be used in different areas of our life.

RESUMEN La naturaleza nos proporciona una gran cantidad de compuestos con interesantes propiedades biológicas, dentro de los cuales tenemos los aceites esenciales, los cuales son una fuente importante de nuevas moléculas bioactivas, que pueden reemplazar a los químicos sintéticos, ya que son amigables con el medio ambiente y son menos tóxicos. Actualmente existen más de 20.000 publicaciones en las que los aceites esenciales están relacionados con alguna actividad biológica, según la búsqueda realizada en diferentes bases de datos hasta enero de 2018. Esto confirma la amplia utilidad de los aceites esenciales como principal fuente de metabolitos bioactivos, que pueden ser utilizados en diferentes áreas de nuestra vida.

Volatile chemical composition of essential oil from Bursera graveolens (Kunth) Triana & Planch and their fumigant and repellent activities

The objectives of this work were the study of the volatile chemical composition of essential oils (EO’s) from Bursera graveolens obtained in the locality of Malagana, municipality of Mahates, Bolívar, Colombia, as well as to evaluate their repellent and fumigant properties. EO’s were extracted by hydro-distillation and characterized by gas chromatography-mass spectrometry (GC-MS). The major compounds found in B. graveolens were limonene (42.2%), pulegone (20.9%), carvone (7.5%), caryophyllene (4.1%), and trans-carveol (3.8%). The repellent activity of EO’s was determined by the area preference method, where the EO of B. graveolens presented repellent activity against the Tribolium castaneum weevil at a concentration of 1 at 2% and 4 hours of exposure (88.1 and 88.6% respectively). B. graveolens essential oil was more effective in its fumigant activity with LC50 of 108.2 μg oil mL-1. Also, the fumigant and repellent activities of two individual compounds present in the oil were evaluated, that is, limonene (majority) and caryophyllene. The results indicated that B. graveolens essential oil could be a promising alternative to new natural repellents and biocides.

Research progress on active components of fungi transforming Chinese materia medica / 中草药

Active components of Chinese materia medica (CMM) are the material basis of its efficacy and the keys to realize modernization of CMM. How to improve the content of active ingredients of CMM has become a research hotspot, and microbial transformation is one of its key technologies. The practice has proved that the strains are different, the types of CMM are different, and the transformation effects are different. Therefore, the research on fungal transformation of CMM active ingredients such as terpenes, alkaloids, phenylpropanoids, quinones, steroids, organic acids, etc. is reviewed in this study.