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Bol. latinoam. Caribe plantas med. aromát ; 21(2): 207-214, mar. 2022. tab
Article in English | LILACS | ID: biblio-1395229


In this study, we investigated the main constituent, the predominant class and biological activity of the essential oil extracted from the leaves of Pimenta dioica and the pattern of the major constituent against larvae in the third stage of Aedes aegypti. For this reason, we extracted the oil by hydrodistillation, identified its components by gas chromatography coupled with mass spectrometry (GC/MS) and calculated the lethal concentration (LC50) of the larvicidal activity using the Reed-Muench method. The results show that the oil consists mainly of eugenol, in which the phenylpropanoid class predominated and the lethal concentration, LC50, was 38.86 µg mL-1at a confidence level of 2.25 µg mL-1, while the eugenol standard presented LC5079.75 µg mL-1at a confidence level of 2.10 µg mL-1. Given the facts, we conclude that the oil is more active than the standard and that it has the potential to replace chemical larvicides.

En este estudio, investigamos el constituyente principal, la clase predominante y la actividad biológica del aceite esencial extraído de las hojas de Pimenta dioica y el patrón del constituyente principal contra las larvas en la tercera etapa de Aedes aegypti. Por este motivo, extrajimos el aceite por hidrodestilación, identificamos sus componentes mediante cromatografía de gases acoplada a espectrometría de masas (GC/MS) y calculamos la concentración letal (CL50) de la actividad larvicida mediante el método Reed-Muench. Los resultados muestran que el aceite está constituido principalmente por eugenol, en el que predominó la clase fenilpropanoide y la concentración letal, CL50, fue de 38,86 µg.mL-1 a un nivel de confianza de 2,25 µg.mL-1, mientras que el estándar de eugenol presentó CL50 79,75 µg.mL -1 a un nivel de confianza de 2,10 µg.mL-1. Dados los hechos, concluimos que el aceite es más activo que el estándar y que tiene el potencial de reemplazar los larvicidas químicos.

Oils, Volatile/pharmacology , Oils, Volatile/chemistry , Aedes/drug effects , Pimenta/chemistry , Larvicides , Biological Assay , Biological Products , Eugenol/analysis , Plant Extracts/pharmacology , Plant Extracts/chemistry , Plant Leaves , Monoterpenes/analysis , Larva , Gas Chromatography-Mass Spectrometry
Bol. latinoam. Caribe plantas med. aromát ; 21(2): 156-175, mar. 2022. ilus, tab
Article in English | LILACS | ID: biblio-1393371


The purpose of this systematic review was to identify the available literature on the essential oil from species of genus Cordia. This study followed the Preferred Reporting Items for Systematic Reviews. The search was conducted on four databases: LILACS, PubMed, Science Direct, and Scopus until June 5th, 2020, with no time or language restrictions. Sixty out of the 1,333 initially gathered studies fit the inclusion criteria after the selection process. Nine species of Cordia were reported in the selected studies, out of which 79% of the evaluated studies reported essential oil from Cordia curassavica. The essential oil extraction methods identified were hydrodistillation and steam distillation. As for biological application, antimicrobial, anti-inflammatory, larvicidal and antioxidant activities were the most reported. The main compounds reported for essential oil were ß-caryophyllene, α-humulene, α-pinene, bicyclogermacrene, and sabinene. The information reported in this systematic review can contribute scientifically to the recognition of the importance of the genus Cordia.

El propósito de esta revisión sistemática fue identificar la literatura disponible sobre el aceite esencial de especies del género Cordia. Este estudio siguió los elementos de informe preferidos para revisiones sistemáticas. La búsqueda se realizó en cuatro bases de datos: LILACS, PubMed, Science Direct y Scopus hasta el 5 de junio de 2020, sin restricciones de tiempo ni de idioma. Sesenta de los 1.333 estudios reunidos inicialmente cumplieron los criterios de inclusión después del proceso de selección. Se informaron nueve especies de Cordia en los estudios seleccionados, de los cuales el 79% de los estudios evaluados informaron aceite esencial de Cordia curassavica. Los métodos de extracción de aceite esencial identificados fueron la hidrodestilación y la destilación al vapor. En cuanto a la aplicación biológica, las actividades antimicrobianas, antiinflamatorias, larvicidas y antioxidantes fueron las más reportadas. Los principales compuestos reportados para el aceite esencial fueron ß-cariofileno, α-humuleno, α-pineno, biciclogermacreno y sabineno. La información reportada en esta revisión sistemática puede contribuir científicamente al reconocimiento de la importancia del género Cordia.

Oils, Volatile/chemistry , Cordia/chemistry , Sesquiterpenes/analysis , Distillation , Monoterpenes/analysis
Article in Chinese | WPRIM | ID: wpr-935769


Objective: To investigate the effect and underlying mechanism of paeoniflorin on hippocampal neuron apoptosis induced by lead acetate. Methods: In September 2020, primary hippocampal neuronal cells were isolated and cultured from fetal rats, and identified using cellular immunofluorescent. MTT assay was used to measure the cell viability to determine the concentration and time of lead acetate-induced hippocampal neuron apoptosis. MTT was also used to evaluate the effect of paeoniflorin concentration on the apoptosis of hippocampal neurons induced by lead acetate. According to the results, different concentrations of paeoniflorin were selected to intervene hippocampal neuron cells, after 24 h, lead acetate was added to the cells, meanwhile, blank and model groups were set up, the content of reactive oxygen species (ROS) , superoxide dismutase (SOD) , lactate dehydrogenase (LDH) , malondialdehyde (MDA) and Caspase-3 were measured. Extracellular signal regulated kinase (ERK) , phosphorylated ERK (p-ERK) , p38 mitogen -activated protein kinases (p38MAPK) , phosphorylated p38MAPK (p-p38MAPK) , c-Jun N-terminal kinase (JNK) and phosphorylated JNK (p-JNK) protein expression in hippocampal neuronal cells were determined by Western blotting. Results: The isolated and cultured hippocampal neurons were identified by immunofluorescence chemical staining and then treated with lead acetate, MTT results showed that lead acetate had the best toxicity effect when treated for 24 h at a concentration of 25 μmol/L. Paeoniflorin showed no cytotoxic effect on hippocampal neuronal cells when the concentrations below 80 μmol/L. Compared with the model group, the activity of hippocampal neuronal cells was significantly increased after treating with 20, 40 or 80 μmol/L paeoniflorin (P<0.05) . Compared with the blank group, the ROS activity, LDH release level, MDA content and caspase-3 content were significantly increased (P<0.01) , and the SOD activity was significantly decreased (P< 0.01) in the hippocampal neuronal cells of the model group. Compared with the model group, the ROS activity, LDH release level, MDA content and caspase-3 content were obviously decreased (P<0.05) , SOD activity was significantly increased (P <0.01) after hippocampal neuronal cells were treated with 40 or 80 μmol/L paeoniflorin. Relative to the model group, the ratio of p-ERK/ERK were significantly up-regulated (P<0.01) , while the ratios of p-p38MAPK/p38MAPK and p-JNK/JNK were significantly down-regulated after hippocampal neuronal cells were treated with 40 or 80 μmol/L paeoniflorin (P<0.05) . Conclusion: Paeoniflorin may down-regulate the expression of p-p38MAPK and p-JNK protein, up-regulate the expression of p-ERK protein, and inhibit the apoptosis of hippocampal neurons induced by lead acetate through the MAPK signaling pathway.

Acetates/pharmacology , Animals , Apoptosis , Caspase 3/metabolism , Extracellular Signal-Regulated MAP Kinases/metabolism , Glucosides , Hippocampus/metabolism , JNK Mitogen-Activated Protein Kinases/pharmacology , Lead , Monoterpenes , Neurons/metabolism , Rats , Reactive Oxygen Species/metabolism , Superoxide Dismutase/metabolism , p38 Mitogen-Activated Protein Kinases/metabolism
Article in Chinese | WPRIM | ID: wpr-928026


This study aims to establish a rapid and sensitive UPLC-MS/MS method for simultaneously determining the content of strychnine and paeoniflorin in plasma and brain tissue of rats, and compare the pharmacokinetic behavior and brain tissue distribution of paeoniflorin combined with normal and toxic doses of strychnine in rats after percutaneous administration. Compared with those in the toxic-dose strychnine group, the AUC_(0-t), AUC_(0-∞), and C_(max) of strychnine decreased by 51.51%, 45.68%, and 46.03%, respectively(P<0.01), and the corresponding values of paeoniflorin increased by 91.41%, 102.31%, and 169.32%, respectively(P<0.01), in the compatibility group. Compared with the normal-dose strychnine group, the compatibility group showed insignificantly decreased C_(max), AUC_(0-t), and AUC_(0-∞) of strychnine, increased C_(max) and T_(max) of paeoniflorin(P<0.01), 66.88% increase in AUC_(0-t), and 70.55% increase in AUC_(0-∞) of paeoniflorin. In addition, the brain tissue concentration of strychnine decreased and that of paeoniflorin increased after compatibility. The combination of paeoniflorin with normal dose and toxic dose of strychnine can inhibit the percutaneous absorption of strychnine, and greatly promote the percutaneous penetration of paeoniflorin, whereas the interaction mechanism remains to be explored. The UPLC-MS/MS method established in this study is easy to operate and has good precision. It is suitable for in vivo study of pharmacokinetic behavior and brain tissue distribution of paeoniflorin and strychnine after percutaneous administration in rats, which provides reference for the safe and rational clinical use of strychnine and the combined use of drugs, and lays a solid foundation for the development of external preparations containing Strychni Semen.

Administration, Cutaneous , Animals , Brain , Bridged-Ring Compounds/pharmacology , Chromatography, Liquid/methods , Glucosides , Monoterpenes , Rats , Rats, Sprague-Dawley , Strychnine , Tandem Mass Spectrometry/methods , Tissue Distribution
Article in Chinese | WPRIM | ID: wpr-928007


Monoterpenes are widely used in cosmetics, food, medicine, agriculture and other fields. With the development of synthetic biology, it is considered as a potential way to create microbial cell factories to produce monoterpenes. Engineering Saccharomyces cerevisiae to produce monoterpenes has been a research hotspot in synthetic biology. In S. cerevisiae, the production of geranyl pyrophosphate(GPP) and farnesyl pyrophosphate(FPP) is catalyzed by a bifunctional enzyme farnesyl pyrophosphate synthetase(encoded by ERG20 gene) which is inclined to synthesize FPP essential for yeast growth. Therefore, reasonable control of FPP synthesis is the basis for efficient monoterpene synthesis in yeast cell factories. In order to achieve dynamic control from GPP to FPP biosynthesis in S. cerevisiae, we obtained a novel chassis strain HP001-pERG1-ERG20 by replacing the ERG20 promoter of the chassis strain HP001 with the promoter of cyclosqualene cyclase(ERG1) gene. Further, we reconstructed the metabolic pathway by using GPP and neryl diphosphate(NPP), cis-GPP as substrates in HP001-pERG1-ERG20. The yield of GPP-derived linalool increased by 42.5% to 7.6 mg·L~(-1), and that of NPP-derived nerol increased by 1 436.4% to 8.3 mg·L~(-1). This study provides a basis for the production of monoterpenes by microbial fermentation.

Fermentation , Geranyltranstransferase/genetics , Monoterpenes/metabolism , Saccharomyces cerevisiae/metabolism , Saccharomyces cerevisiae Proteins/metabolism
Chinese Journal of Biotechnology ; (12): 427-442, 2022.
Article in Chinese | WPRIM | ID: wpr-927720


Monoterpenoids that belong to the terpenoids family are usually volatile and have strong aroma. Some monoterpenoids also have antioxidant, antibacterial and anti-inflammatory activities, which make them important raw materials for medicine, food and cosmetics industry. In recent years, the heterologous synthesis of monoterpenoids by microorganisms has attracted extensive attention. However, its large-scale application is greatly hampered by the low yield and high production cost. Nowadays, the rapid development of synthetic biology provides new approaches for enhancing the production of monoterpenoids by microorganisms. Different kinds of recombinant strains can be obtained via engineering of microbial cells to produce a variety of monoterpenoids with different properties. This paper summarized the latest strategies and progress in the application of synthetic biology to produce monoterpenoids by microorganisms, including the design and modification of biosynthetic pathway, as well as the design and optimization of high-yield monoterpenoids producing chassis cells.

Biosynthetic Pathways , Metabolic Engineering , Monoterpenes/metabolism , Synthetic Biology , Terpenes
Bol. latinoam. Caribe plantas med. aromát ; 20(6): 649-659, nov. 2021. ilus, tab
Article in English | LILACS | ID: biblio-1369974


The objective was to evaluate the production and composition of lavender essential oil, simultaneously at open field and greenhouse, in spring-summer season, under different types of fertilization. Each cultivation system was considered an experiment (field and greenhouse), and in both, the experimental design used was randomized blocks, with five treatments, being fertilization with nutrient source -100% mineral (100%M), 100% organic (100%O), 100% organomineral (100%OM), 50% organomineral (50%OM), and without fertilization (control), and three repetitions. Better performance and productivity of Lavandula dentatais related to respectively 100% OM and 50% OM fertilization in the field and greenhouse. The essential oil content does not differ between cultivation systems and kind of fertilizers, and the majorities compounds were 1.8-cineol, fenchone and camphor.

El objetivo fue evaluar la producción y composición del aceite esencial de lavanda a campo abierto e invernadero simultáneamente, en la temporada primavera-verano, bajo diferentes tipos de fertilización. Cada sistema de cultivo fue considerado un experimento (campo e invernadero), y en ambos, el diseño experimental utilizado fue bloques al azar, con cinco tratamientos, siendo la fertilización con fuente de nutrientes 100% mineral (100% M), 100% orgánico (100% O), 100% organomineral (100% MO), 50% organomineral (50% MO), y sin fertilización (control), y tres repeticiones. Un mejor rendimiento y productividad de Lavandula dentata está relacionado con una fertilización de 100%OM y 50% OM en el campo y en invernadero, respectivamente. El contenido de aceite esencial no difiere entre sistemas de cultivo y tipo de fertilizante, y los compuestos mayoritarios fueron 1.8-cineol, fenchone y alcanfor.

Plant Oils/metabolism , Plant Oils/chemistry , Oils, Volatile/metabolism , Oils, Volatile/chemistry , Lavandula/chemistry , Agricultural Cultivation , Nutrients , Monoterpenes/analysis , Greenhouses , Fertilization
Arq. bras. med. vet. zootec. (Online) ; 73(1): 82-90, Jan.-Feb. 2021. tab, graf
Article in English | LILACS, VETINDEX | ID: biblio-1153042


Essential oils (EO) such as carvacrol represent a wide range of mainly volatile aromatic plant compounds which hold antioxidant, antibacterial and antifungal potential, in addition to other properties of interest to animal health, such as the ability to modulate the microbiome. Current horse care commonly involves an intensive management system with an excessive use of concentrated feed, which can lead to severe digestive and metabolic disorders. Studies with EO in horses are limited, but the use of carvacrol essential oil (CEO) can promote benefits in microbial fermentation. The objective was to investigate the effect of different quantities of CEO on the apparent total digestibility of nutrients, microbial profile in the feces and postprandial blood glucose and insulin response when added to the equine diet. Eight Mini-Horse geldings were used (42±6 months; 135±15 kg BW) and fed with a proportion of 60% concentrate and 40% grass hay. The treatments were: 0, 100, 200 and 300 ppm of CEO. The addition of CEO up to 300 ppm did not influence the apparent digestibility of nutrients or the postprandial plasma glucose and insulin response. The use of CEO maintained the fermentative digestive health of horses fed with concentrate diets.(AU)

Os óleos essenciais (EO), como o carvacrol, são descritos por representarem ampla gama de compostos principalmente voláteis de plantas aromáticas, com potencial antioxidante, antibacteriano, antifúngico, entre outras propriedades de interesse para a saúde animal, como a modulação do microbioma. Atualmente, os cavalos são submetidos a manejo intensivo, com uso excessivo de ração concentrada, o que pode causar graves distúrbios digestivos e metabólicos. Em cavalos, estudos com EO são limitados, mas o uso de óleo essencial de carvacrol (CEO) poderia promover benefícios na fermentação microbiana. O objetivo da presente pesquisa foi investigar o efeito de diferentes quantidades de óleo essencial de carvacrol, adicionadas à dieta de equinos, sobre a digestibilidade aparente total de nutrientes, o perfil microbiano por meio das fezes e a resposta sanguínea pós-prandial de glicose e insulina. Foram utilizados oito cavalos castrados, da raça Mini-Horse (42±6 meses), 135±15kg PV, alimentados na proporção de 60% concentrado e 40% feno de capim. Os tratamentos foram: 0, 100, 200 e 300ppm de CEO. A adição de CEO até 300ppm não influencia a digestibilidade aparente dos nutrientes e a resposta de glicose e insulina plasmática pós-prandial. O uso de EO demonstra manter a saúde digestiva fermentativa quando os cavalos são alimentados com dieta rica em concentrado.(AU)

Animals , Oils, Volatile/therapeutic use , Digestion/drug effects , Glucose , Horses/blood , Insulin/blood , Dietary Supplements/analysis , Monoterpenes
Article in Chinese | WPRIM | ID: wpr-921798


Huangqin Decoction(HQD) is a classic prescription for treating dysentery in the Treatise on Cold Damage and now is mainly used for the treatment of ulcerative colitis(UC). Since there are no requirements on specific Paeonia species, both Paeoniae Radix Alba(white peony root, WPR) and Paeoniae Radix Rubra(red peony root, RPR) are clinically used in HQD now. Although the two types of peony roots are close in origin and similar in primary components, the medicinal properties and efficacies are different. Furthermore, the systematic comparative analysis on the efficacy differences in treating UC of HQD with the roots of multi-originated peony has been seldom reported. This study compared and evaluated the pharmacological effects of HQD prepared from the roots of multi-originated peony, including WPR, RPR-l(derived from P. lactiflora), and RPR-v(derived from P. veitchii) based on the mouse model of UC induced by dextran sodium sulfate(DSS) by animal behaviors, pathological section(colon), and cytokine expression(IL-1β and IL-6), aiming to provide evidence for the identification of the original resource of peony root in HQD. The results indicated that all HQD samples prepared from WPR, RPR-l, and RPR-v could improve the symptoms of UC. Compared with the HQD-WPR, HQD-RPR-l and HQD-RPR-v were significantly different in weight loss, colon length, and disease activity index(DAI) score, but there was no significant difference between HQD-RPR-l and HQD-RPR-v. Moreover, HQD-RPR-v exhibited the most significant improvement in the pathological morphology of colonic tissue and mucosal defects. According to the previous comparative analysis of chemical profiling and content distribution of HQD prepared from the roots of multi-originated peony, RPR-v in HQD was potent in protecting against UC, which was presumedly attributed to a large number of monoterpene glycosides and galloyl glucoses. This study provided a scientific basis for the determination of peony root in HQD and its clinical medication.

Animals , Colitis, Ulcerative/drug therapy , Dextran Sulfate , Disease Models, Animal , Drugs, Chinese Herbal/therapeutic use , Mice , Monoterpenes , Paeonia/chemistry , Plant Roots/chemistry
Article in Chinese | WPRIM | ID: wpr-921731


Paeoniae Radix Alba is the dried root of Paeonia lactiflora, which was first recorded in the Shennong's Classic of Materia Medica and listed as the top grade. It is a common blood-tonifying herb, and its chemical components are mainly monoterpenes and their glycosides, triterpenes, flavonoids and so on. Modern research has demonstrated that Paeoniae Radix Alba has the activities of anti-inflammation, pain easing, liver protection, and anti-oxidation, and thus it is widely used in clinical practice and has broad development prospects. In this paper, the research progress on the chemical composition, pharmacological effects, and quality control of Paeoniae Radix Alba were summarized. On this basis, the Q-markers of Paeoniae Radix Alba were predicted from the aspects of mass transfer and traceability, chemical composition specificity, and availability and measurability of chemical components, which will provide a scientific basis for the quality evaluation of Paeoniae Radix Alba.

Drugs, Chinese Herbal , Medicine, Chinese Traditional , Monoterpenes , Paeonia , Plant Extracts
Article in Chinese | WPRIM | ID: wpr-921639


Five monoterpenoid compounds(1-5) were isolated and purified from the acetone fraction of the aqueous extract of Zingiberis Rhizoma Recens by MCI, Sephadex LH-20, silica gel, semi-preparative HPLC, and TLC. Their structures were identified with multiple spectroscopical methods including 1 D-NMR, 2 D-NMR, and MS. The five compounds were identified as(2E,6Z)-8-hydroxy-2,6-dimethylocta-2,6-dien-1-yl-(E)-3-(4-hydroxy-3-methoxyphenyl) acrylate(1),(2E,6E)-8-hydroxy-3,7-dimethylocta-2,6-die-noic acid(2),(E)-1,8-dihydroxy-3,7-dimethyl-2-octenoic acid(3), linalyl-β-D-glucopyranoside(4), and β-D-glucopyranoside-(2E)-3,7-dimethyl-2,6-octadien-1-yl(5), respectively.Compound 1 was a new monoterpene ester, and compounds 4-5 were isolated from this plant for the first time.

Chromatography, High Pressure Liquid , Esters , Monoterpenes , Rhizome
Article in Chinese | WPRIM | ID: wpr-888120


The study aims to investigate the effect of the compatibility of paeonol and paeoniflorin(hereinafter referred to as the compatibility) on the expression of myocardial proteins in rats with myocardial ischemia injury and explore the underlying mechanism of the compatibility against myocardial ischemia injury. First, the acute myocardial infarction rat model was established by ligation of the anterior descending branch of the left coronary artery. The model rats were given(ig) paeonol and paeoniflorin. Then protein samples were collected from rat cardiac tissue and quantified by tandem mass tags(TMT) to explore the differential proteins after drug intervention. The experimental results showed that differential proteins mainly involved phagocytosis engulfment, extracellular space, and antigen binding, as well as Kyoto encyclopedia of genes and genomes(KEGG) pathways of complement and coagulation cascades, syste-mic lupus erythematosus, and ribosome. In this study, the target proteins and related signaling pathways identified by differential proteomics may be the biological basis of the compatibility against myocardial ischemia injury in rats.

Acetophenones , Animals , Glucosides , Monoterpenes , Myocardial Ischemia/genetics , Myocardial Reperfusion Injury , Proteomics , Rats , Rats, Sprague-Dawley
Article in Chinese | WPRIM | ID: wpr-879015


The volatile oil from Mastiche and Olibanum medicinal materials was extracted by steam distillation, and the chemical components of the volatile oil were analyzed by GC-MS technology. The differences of the volatile oil components were compared and study on the Helicobacter pylori in vitro antimicrobial activitiy was conducted. The results showed that the yields of the volatile oil from Mastiche and Olibanum were 11.93% and 2.40%, respectively. A total of 46 compounds(91.31%) were identified from the volatile oil from Mastiche annd 35 compounds(92.49%) from Olibanum. The classification and comparison study of the components showed that the content of monoterpenes in the volatile oil from Mastiche was the highest(40.69%), followed by alcohols(28.48%); while the content of alcohols in the volatile oil from Olibanum was the highest(35.81%), followed by esters(24.92%). There were significant differences in the components of volatile oil from Mastiche and Olibanum, which might be one of the reasons for the difference in efficacy and application. In vitro bacteriostatic experiments showed that the minimum inhibitory concentration(MIC) of the volatile oil from Mastiche against H. pylori was 1 mg·mL~(-1), and the MIC of the volatile oil from Olibanum against H. pylori was more than 1 mg·mL~(-1). In combination with the results of the oil yield experiment, Mastiche had the advantage of inhibiting H. pylori activity. The research results provide scientific basis for the rational application of Mastiche and Olibanum.

Anti-Bacterial Agents/pharmacology , Frankincense , Gas Chromatography-Mass Spectrometry , Helicobacter pylori , Monoterpenes/analysis , Oils, Volatile/pharmacology
Article in Chinese | WPRIM | ID: wpr-878981


To compare the effect of hot or warm property of Chinese medicine(CM) on the skin toxicity of essential oils(EOs) as penetration enhancer in vitro and in vivo, and explore the mechanism. EOs were extracted from WIM of Bichengqie(Litseae Fructus), Dingxiang(Flos Syzygii Aromatici), Huajiao(Pericarpium Zanthoxyli Bungeani), and Xiaohuixiang(Fructus Foeniculi) with warm property, and Ganjiang(Rhizoma Zingiberis), Gaoliangjiang(Rhizoma Alpiniae Officinari), Hujiao(Fructus Piperis), and Wuzhuyu(Fructus Evodiae Rutaecarpae) with hot property, respectively. Then the in vitro toxicity was evaluated by human keratinocyte cytotoxicity. In vivo skin irritation potency was also evaluated through pathological observation after topical administration. The components, especially those located in stratum corneum, were analyzed by GC-MS. The main components, namely monoterpenes and sesquiterpenes, of EOs extracted from CM with hot property,were detected for the interaction with keratino-lipid ceramide 3 by molecular simulation technology; and the interaction energy value was calculated based on the optimal conformation. It was found that the skin cell toxicity of EOs from CM with hot property was significantly higher than that of EOs from CM with warm property. However, there was no significant difference between them by in vivo skin irritation evaluation. Whether from CM with hot property or warm property, EOs showed a significant reduced toxicity compared with azone. Sesquiterpenes(33.56%±19.38%) were found to be one of the main components in EOs from CM with hot property, while almost no sesquiterpenes was found in EOs from CM with warm property. After topical administration of EOs from CM with hot property, sesquiterpenes were demonstrated to be prone to locate in stratum corneum. The results of molecular simulation also revealed that the interaction between sesquiterpenes and ceramide 3 was significantly stronger than that of monoterpenes(P<0.01). In conclusion, the location of sesquiterpenes in stratum corneum resulted in the significant difference between in vitro skin cell toxicity and in vivo skin irritation potency. The EOs from CM with hot property shall be taken into account for further development of potent penetration enhancer.

Humans , Monoterpenes/metabolism , Oils, Volatile/toxicity , Sesquiterpenes/metabolism , Skin/metabolism , Skin Absorption
Article in English | WPRIM | ID: wpr-922765


Guided by cell-based anti-anaphylactic assay, eighteen cage-like monoterpenoid glycosides (1-18) were obtained from the bioactive fraction of P. lactiflora extract. Among these, compounds 1, 5, 6, 11, 12, 15, and 17 significantly reduced the release rate of β-HEX and HIS without or with less cytotoxicity. Furthermore, the most potent inhibitor benzoylpaeoniflorin (5) was selected as the prioritized compound for the study of action of mechanism, and its anti-anaphylactic activity was medicated by dual-inhibiting HDC and MAPK signal pathway. Moreover, molecular docking simulation explained that benzoylpaeoniflorin (5) blocked the conversion of L-histidine to HIS by occupying the HDC active site. Finally, in vivo on PCA using BALB/c mice, benzoylpaeoniflorin (5) suppressed the IgE-mediated PCA reaction in antigen-challenged mice. These findings indicated that cage-like monoterpenoid glycosides, especially benzoylpaeoniflorin (5), mainly contribute to the anti-anaphylactic activity of P. lactiflora by dual-inhibiting HDC and MAPK signal pathway. Therefore, benzoylpaeoniflorin (5) may be considered as a novel drug candidate for the treatment of anaphylactic diseases.

Animals , Glucosides , Mice , Mice, Inbred BALB C , Molecular Docking Simulation , Monoterpenes , Paeonia , Plant Roots
Acta cir. bras ; 36(11): e361106, 2021. tab, graf
Article in English | LILACS, VETINDEX | ID: biblio-1360062


ABSTRACT Purpose: To delve into the influence of paeoniflorin (PA) on abating primary biliary cholangitis (PBC)-induced liver fibrosis and its causative role. Methods: Our team allocated the mice to control group, PA group, PBC group and PBC+PA group. We recorded the weight change of mice in each group. We used Masson staining for determining liver fibrosis, immunofluorescence staining for measuring tumor necrosis factor-α (TNF-α) expression, quantitative real-time polymerase chain reaction (qRT-PCR) for assaying related gene expression, as well as Western blot for testing related protein expression. Results: The weight of PBC model mice declined. Twenty-four weeks after modeling, the positive rate of anti-mitochondrial antibody-M2 (AMA-M2) in PBC mice reached 100%. Alkaline phosphatase (ALP), alanine aminotransferase (ALT), aspartate aminotransferase (AST), hydroxyproline (HYP), laminin (LN), procollagen type III (PC III), and malondialdehyde (MDA) contents saliently waxed (p<0.01). Meanwhile, superoxide dismutase (SOD) and glutathione peroxidase (GSH-px) activity patently waned (p<0.01). Liver fibrosis levels were flagrantly higher (p<0.01), and TNF-α, NOD-like receptor protein 3 (NLRP3), caspase-1, interleukin-18 (IL-18), and interleukin-1β (IL-1β) protein or gene expression were manifestly up-regulated (p<0.01). PA could restore the weight of PBC mice, strikingly restrain the positive expression of AMA-M2, and down-regulate serum ALP, ALT, AST, HYP, LN, PC III, MDA in PBC mice (p<0.01). PA could also significantly up-regulate SOD and GSH-px levels (p<0.01), down-regulate IL-1β, IL-18, caspase-1, NLRP3, and TNF-α protein or gene expression in PBC mice (p<0.01) and inhibit liver fibrosis levels (p<0.01). Conclusions: PA can reduce PBC-induced liver fibrosis in mice and may function by curbing the formation of NLRP3.

Animals , Mice , Monoterpenes/pharmacology , NLR Family, Pyrin Domain-Containing 3 Protein/metabolism , Glucosides/pharmacology , Liver Cirrhosis/prevention & control , Liver Cirrhosis/drug therapy , Aspartate Aminotransferases , Liver/pathology
Article in English | LILACS | ID: biblio-1284447


This paper described the chemical compositions and antimicrobial activity of the essential oils from the leaves and stem of Amomum rubidumLamxay & N. S. Lý, collected from Bidoup Nui Ba National Park, Lam Dong, Vietnam. The essential oils were obtained by hydrodisitllation method while antimicrobial activity was evaluetd by microdilution broth susceptibility assay. The main constituents of the leaf essential oil were identified as 1,8-cineole (37.7%), δ-3-carene (19.5%) and limonene (16.3%) while δ-3-carene (21.9%), limonene (17.8%) and ß-phellandrene (14.6%) dominated in the stem essentialoil. The leaf and stem essential oils displayed stronger inhibition of Pseudomonas aeruginosa with MIC of 25 µg/mLand 50 µg/mL respectively. The stem essential oil was active against Candida albicans (MIC, 50 µg/mL) while both essential oils inhibited the growth of Fusarium oxysporum (MIC 50 µg/mL). This is the first report on chemical constituents and antimicrobial activity of the essential oils of A. rubidum.

Este artículo describe la composición química y la actividad antimicrobiana de aceites esenciales de las hojas y el tallo de Amomum rubidum Lamxay & N. S. Lý recolectados del Parque Nacional Bidoup Nui Ba, Lam Dong, Vietnam. Los aceites esenciales se obtuvieron mediante el método de hidrodisitilación, mientras que la actividad antimicrobiana se evaluó mediante un ensayo de susceptibilidad de caldo de microdilución. Los principales componentes del aceite esencial de la hoja se identificaron como 1,8-cineol (37,7%), δ-3-careno (19,5%) y limoneno (16,3%), mientras que δ-3-careno (21,9%), limoneno (17,8 %) y ß-felandreno (14,6%) dominaron en el aceite esencial del tallo. Los aceites esenciales de hoja y tallo mostraron una inhibición más fuerte de Pseudomonas aeruginosa con un MIC de 25 µg/mL y 50 µg/mL, respectivamente. El aceite esencial del tallo fue activo contra Candida albicans (MIC, 50 µg/mL) mientras que ambos aceites esenciales inhibieron el crecimiento de Fusarium oxysporum (MIC 50 µg/mL). Este es el primer informe sobre los componentes químicos y la actividad antimicrobiana de los aceites esenciales de A. rubidum.

Oils, Volatile/pharmacology , Amomum/chemistry , Anti-Infective Agents/pharmacology , Pseudomonas aeruginosa/drug effects , Candida albicans/drug effects , Oils, Volatile/chemistry , Microbial Sensitivity Tests , Distillation , Chromatography, Gas , Plant Stems , Plant Leaves , Monoterpenes/analysis , Fusarium/drug effects , Anti-Infective Agents/chemistry
Bol. latinoam. Caribe plantas med. aromát ; 20(1): 61-70, 2021. tab, ilus
Article in English | LILACS | ID: biblio-1284444


Identification of the chemical compositionof essential oils is very important for ensuring the quality of finished herbal products. The objective of the study was to analyze the chemical components present in the essential oils of five Beilschmiediaspecies (i.e. B. kunstleri, B. maingayi, B. penangiana, B. madang, and B. glabra) by multivariate data analysis using principal component analysis (PCA) and hierarchical clustering analysis (HCA) methods. The essential oils were obtained by hydrodistillation and fully characterized by gas chromatography (GC) and gas chromatography-mass spectrometry (GC-MS). A total of 108 chemical components were successfully identified from the essential oils of five Beilschmiediaspecies. The essential oils were characterized by high proportions of ß-caryophyllene (B.kunstleri), δ-cadinene (B. penangianaand B. madang), and ß-eudesmol (B. maingayiand B. glabra). Principal component analysis (PCA) and hierarchical cluster analysis (HCA) revealed that chemical similarity was highest for all samples, except for B. madang. The multivariate data analysis may be used for the identification and characterization of essential oils from different Beilschmiediaspecies that are to be used as raw materials of traditional herbal products.

La identificación de la composición química de los aceites esenciales es muy importante para garantizar la calidad de los productos herbales terminados. El objetivo del estudio fue analizar los componentes químicos presentes en los aceites esenciales de cinco especies de Beilschmiedia (B. kunstleri, B. maingayi, B. penangiana, B. madangy B. glabra) mediante análisis de datos multivariados utilizando los métodos de análisis de componente principal (PCA) y análisis de agrupamiento jerárquico (HCA). Los aceites esenciales se obtuvieron por hidrodestilación y se caracterizaron completamente por cromatografía de gases (GC) y cromatografía de gases-espectrometría de masas (GC-MS). Se identificaron con éxito un total de 108 componentes químicos a partir de los aceites esenciales de las cinco especies de Beilschmiedia. Los aceites esenciales se caracterizaron por altas proporciones de ß-cariofileno (B. kunstleri), δ-cadineno (B. penangianay B. madang) y ß-eudesmol (B. maingayiy B. glabra). El análisis de componentes principales (PCA) y el análisis de conglomerados jerárquicos (HCA) revelaron que la similitud química fue más alta para todas las muestras, excepto para B. madang. El análisis de datos multivariados puede usarse para la identificación y caracterización de aceites esenciales de diferentes especies de Beilschmiedia que se utilizan como materias primas de productos herbales tradicionales.

Oils, Volatile/chemistry , Lauraceae/chemistry , Sesquiterpenes/analysis , Cluster Analysis , Distillation , Multivariate Analysis , Chromatography, Gas/methods , Principal Component Analysis , Monoterpenes/analysis
Rev. Ciênc. Méd. Biol. (Impr.) ; 19(2): 258-264, set 24, 2020. tab
Article in English | LILACS | ID: biblio-1358136


Introduction: bacterial infections are a public health problem. Besides, the emergence of strains resistant to antimicrobials has contributed to the search for new alternatives, such for the terpenes with antimicrobial potential. Objectives: the objective of this study was to determine the possible interaction of isolated monoterpenes (-)-Carveol, Geraniol, Citronellol, α-terpineol, R-(-) Carvone, (-)-Menthol, Linalool, D-Dihydrocarvone, and (-)-Terpine-4-ol with conventional antimicrobials (Chloramphenicol, Minocycline, Amoxicillin and Ciprofloxacin) when they are evaluated on Staphylococcus aureus, Staphylococcus epidermidis, Bacillus subtilis, Escherichia coli and Pseudomonas aeruginosa strains. Methodology: the minimum inhibitory concentrations of these test drugs were determined using the microdilution method. The Checkerboard method was used to assess the interactions, by determining the fractional inhibitory concentration index (FIC index). Results: aamong the monoterpenes, only Carveol, Citronellol, and Geraniol presented antimicrobial activity (MIC < 1024 µg/mL). They presented synergistic effects against Pseudomonas aeruginosa ATCC-9027 (FIC index ≤ 0.5) when in combination with Minocycline. Conclusion: this study contributes to the development of new approaches to control bacterial resistance and to the possibility of discovering new drugs.

Introdução: as infecções bacterianas são um problema de saúde pública. Além disso, o surgimento de cepas resistentes aos antimicrobianos tem contribuído para a busca de novas alternativas, como a pesquisa de terpenos com potencial antimicrobiano. Objetivos: o objetivo deste estudo foi determinar a possível interação de monoterpenos isolados (-) - Carveol, Geraniol, Citronelol, α-terpineol, R - (-) Carvona, (-)-Mentol, Linalol, D-Diidrocarvona e (-)-Terpina-4-ol com antimicrobianos convencionais (cloranfenicol, minociclina, amoxicilina e ciprofloxacina) quando avaliados em Staphylococcus aureus, Staphylococcus epidermidis, Bacillus subtilis, Escherichia coli e Pseudomonas aeruginosa. Metodologia: as concentrações inibitórias mínimas destas drogas foram determinadas usando o método de microdiluição. O método checkerboard foi utilizado para avaliar as interações, determinando o índice de concentração inibitória fracionária (índice FIC). Resultados: entre os monoterpenos, apenas Carveol, Citronelol e Geraniol apresentaram atividade antimicrobiana (CIM < 1024 µg/mL). Eles apresentaram efeitos sinérgicos contra Pseudomonas aeruginosa ATCC-9027 (índice FIC ≤ 0,5) quando em combinação com Minociclina. Conclusão: este estudo contribui para o desenvolvimento de novas abordagens para o controle da resistência bacteriana e para a possibilidade de descoberta de novas drogas.

Pseudomonas aeruginosa , Staphylococcus aureus , Staphylococcus epidermidis , Bacillus subtilis , Complementary Therapies , Monoterpenes , Escherichia coli , Gram-Negative Bacteria , Gram-Positive Bacteria , Anti-Infective Agents