La Huamanripa (Senecio tephrosioides Turcz) como alternativa saludable para afecciones respiratorias durante la pandemia COVID-19 / Huamanripa (Senecio tephrosioides Turcz) as a healthy alternative for respiratory conditions during the COVID-19 pandemic / Huamanripa (Senecio tephrosioides Turcz) como alternativa saudável para problemas respiratórios durante a pandemia de COVID-19

Desde tiempo histórico las plantas medicinales se han empleado como ingrediente principal para preparación de diferentes recetas. Motivo que se investigó sobre la Huamanripa como alternativa saludable para afecciones respiratorias durante la pandemia COVID-19 en Barranca. Objetivo. El objetivo fue determinar la eficiencia de la Huamanripa como alternativa saludable para las afecciones respiratorias en la pandemia. Materiales y Método. La metodología se basa en investigación descriptiva con enfoque cuantitativo prospectivo, por lo que se cuestionó sobre la preparación, frecuencia de consumo y para que enfermedades se consumen. Obtenidos los datos se procesaron mediante estadísticas básicas y regresión. Resultados. Se determinó que la Huamanripa lo usan para tratamiento casero medicinal y consume con frecuencia 4 a 5 veces por semana para afecciones respiratorias y COVID-19, consumo de Huamanripa por mes con 23 % de la población, porcentaje de alivio de afecciones respiratorias con 84 %, correlación entre el consumo de Huamanripa y porcentaje de alivio r = 0.99 y en análisis de varianza del consumo de Huamanripa y el porcentaje de alivio no hubo significancia. Conclusiones. Concluye que la Huamanripa es una alternativa eficiente y se puede complementar con otros tratamientos para las afecciones respiratorias y síntomas de COVID-19; ya sea por sus propiedades como aceites especiales y terpenos que tienen efectos antimicrobiana, antiinflamatoria, aliviante, lo cual favorece a la salud.

Since historical times, medicinal plants have been used as the main ingredient for the preparation of different recipes. For this reason, Huamanripa was investigated as a healthy alternative for respiratory diseases during the COVID-19 pandemic in Barranca. Objective. The objective was to determine the efficiency of Huamanripa as a healthy alternative for respiratory diseases during the pandemic. Materials and Method. The methodology is based on descriptive research with a prospective quantitative approach, so that the preparation, frequency of consumption and the diseases for which it is consumed were questioned. Data were obtained and processed by means of basic statistics and regression. Results. It was determined that Huamanripa is used for medicinal home treatment and consumed 4 to 5 times a week for respiratory diseases and COVID-19, consumption of Huamanripa per month with 23% of the population, percentage of relief of respiratory diseases with 84%, correlation between consumption of Huamanripa and percentage of relief r = 0.99 and in variance analysis of Huamanripa consumption and percentage of relief there was no significance. Conclusions. It is concluded that Huamanripa is an efficient alternative and can be complemented with other treatments for respiratory conditions and symptoms of COVID-19; either by its properties such as special oils and terpenes that have antimicrobial, anti-inflammatory, relieving effects, which favors health.

Desde tempos históricos as plantas medicinais têm sido utilizadas como ingrediente principal para a preparação de diferentes receitas. Por esta razão, Huamanripa foi investigado como uma alternativa saudável para doenças respiratórias durante a pandemia da COVID-19 em Barranca. Objetivo. O objetivo era determinar a eficiência de Huamanripa como uma alternativa saudável para as doenças respiratórias durante a pandemia. Materiais e Método. A metodologia é baseada em pesquisa descritiva com uma abordagem quantitativa prospectiva, de modo que foram feitas perguntas sobre a preparação, a freqüência do consumo e para quais doenças é consumida. Os dados foram obtidos e processados utilizando estatísticas básicas e regressão. Resultados. Foi determinado que Huamanripa é usado para tratamento medicinal domiciliar e consumido 4 a 5 vezes por semana para doenças respiratórias e COVID-19, consumo de Huamanripa por mês com 23% da população, porcentagem de alívio de doenças respiratórias com 84%, correlação entre consumo de Huamanripa e porcentagem de alívio r = 0,99 e na análise de variância do consumo de Huamanripa e da porcentagem de alívio não houve significância. Conclusões. Conclui que Huamanripa é uma alternativa eficiente e pode ser complementada com outros tratamentos para condições respiratórias e sintomas da COVID-19; seja por suas propriedades como óleos especiais e terpenos que têm efeitos antimicrobianos, anti-inflamatórios, aliviadores, o que favorece a saúde.

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.

Antibacterial and hemolytic activity of extracts and compounds obtained from epicarps and seeds of Garcinia madruno(Kunth) Hammel / Actividad antimicrobiana y hemolítica de extractos y compuestos obtenidos del epicarpio y las semillas de Garcinia madruno (Kunth) Hammel

This paper describes the evaluation of the antimicrobial and hemolytic activity of the hexane, dichloromethane, ethyl acetate and methanol extracts from seeds and epicarps of Garcinia madruno; as well garcinol, morelloflavone and volkensiflavone isolated from the same species. In the preliminary test of bacterial susceptibility, hexane extracts from seeds and epicarps and the three compounds tested only displayed inhibitory growth effect against Gram-positive bacteria. The minimum inhibitory concentrations of extract and compounds ranging from 86.6 to 1253.4 µg/mL. The hemolytic activity was assessed; however, except for the methanol extract from seeds, none of the samples studied induced hemolysis. Thus, our results suggest that extracts and compounds from G. madruno have the potential to be used in the control of pathologies associated to Gram-positive bacteria. This is the first report of the antimicrobial and hemolytic activity of extracts of different polarity obtained from seeds and epicarps of this edible species.

El presente artículo describe la evaluación de la actividad antimicrobiana y hemolítica de los extractos de hexano, diclorometano, acetato de etilo y metanol, obtenidos de la semilla y el epicarpio de Garcinia madruno; así como de garcinol, morelloflavona y volkensiflavona; aislados de la misma especie. En el ensayo de susceptibilidad bacteriana, tanto el extracto de hexano obtenido a partir de la semilla y el epicarpio, y los tres compuestos aislados, únicamente mostraron actividad inhibitoria del crecimiento contra bacterias Gram-positivas. La concentración mínima inhibitoria presentó valores entre 86.6 y 1253.4 µg/mL. También se estableció la actividad hemolítica; sin embargo, con excepción del extracto metanólico obtenido a partir de las semillas, ninguna de las muestras evaluadas indujo hemólisis. Por lo tanto, los resultados sugieren que los extractos y compuestos de G. madruno tienen el potencial de ser usados en el control de bacterias Gram-positivas asociadas a diversas patologías. Este es el primer reporte de actividad antimicrobiana y hemolítica de extractos de diferente polaridad obtenidos de las semillas y epicarpios de esta especie comestible.

Estudio comparativo de la actividad anti-fúngica de extractos secuenciales de Fuchsia lycioides contra Candida sp / comparative study of the antifungal activity of sequencial extracts of Fuchsia lycioides against Candida sp

The genus Fuchsia is generally used in herbal preparations to treat conditions caused by microorganisms. Based on the popular use of this type of plants, the objective of this study was to obtain sequential extracts of increasing polarity from the branches of Fuchsia lycioides by maceration at room temperature and by the Soxhlet method at 60ºC, to later evaluate the antifungal capacity of the extracts against different clinical isolates of the Candida genus. The ethyl acetate extract exhibited strong anti-fungal activity, selectively inhibiting C. albicans strains with MIC and CMF values of 10 and 15 µg/mL, respectively; comparable with the drug itraconazole®. The analysis of the extract by GC-MS showed a high concentration of terpenoids (mainly phytol) and phenylpropanoids (mainly cinnamic acid), possibly responsible for the antifungal activity of the ethyl acetate extract of F. lycioides.

El género Fuchsia se usa generalmente en preparaciones de hierbas para tratar afecciones provocadas por microorganismos. En base al uso popular de este tipo de plantas, el objetivo de este estudio fue obtener los extractos secuenciales de polaridad creciente de las ramas de Fuchsia lycioides por maceración a temperatura ambiente y por el método Soxhlet a 60ºC, para luego evaluar la capacidad antifúngica de los extractos frente a diferentes aislados clínicos del genero Candida. El extracto de acetato de etilo exhibió una fuerte actividad antifúngica inhibiendo en forma selectiva las cepas de C. albicans con valores de CMI y de CMF de 10 y 15 µg/mL, respectivamente; comparables con el fármaco itraconazol®. El análisis del extracto por CG-EM mostró una alta concentración de terpenoides (principalmente fitol) y fenilpropanoides (principalmente ácido cinámico), posibles responsables de la actividad antifúngica del extracto de acetato de etilo de F. lycioides.

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.

Plant Pharmacophylogeny: Review and Future Directions / 中国结合医学杂志

Medicinal plants have provided numerous medicinal active ingredients for thousands of years and these ingredients have been used in Chinese medicine (CM) and traditional pharmacologies worldwide. Recently, the exploitation and utilisation of medicinal plant resources has increased significantly. The results of the studies have led to the identification of many active components, such as steroidal alkaloids, saponins, terpenoids, and glycosides, in various medicinal plants with different evolutionary levels. Moreover, research on the chemical classification, molecular phylogeny, and pharmacological activity of medicinal plants is increasing in popularity. Pharmacophylogeny is an interdisciplinary topic that studies the correlation between plant phylogeny, chemical composition, and curative effects (pharmacological activity and the traditional curative effect) of medicinal plants. In addition, it provides the basic tools to enable research and development of CM resources. This literature review, based on the genetic relationship between phytogroup and species, highlights the formation process, research content, applications, and future directions of pharmacophylogeny.

Research progress of Curcuma kwangsiensis root tubers and analysis of liver protection and anti-tumor mechanisms based on Q-markers / 中国中药杂志

Curcuma kwangsiensis root tuber is a widely used genuine medicinal material in Guangxi, with the main active components of terpenoids and curcumins. It has the effects of promoting blood circulation to relieve pain, moving Qi to relieve depression, clearing heart and cooling blood, promoting gallbladder function and anti-icterus. Modern research has proved its functions in liver protection, anti-tumor, anti-oxidation, blood lipid reduction and immunosuppression. Considering the research progress of C. kwangsiensis root tubers and the core concept of quality marker(Q-marker), we predicted the Q-markers of C. kwangsiensis root tubers from plant phylogeny, chemical component specificity, traditional pharmacodynamic properties, new pharmacodynamic uses, chemical component measurability, processing methods, compatibility, and components migrating to blood. Curcumin, curcumol, curcumadiol, curcumenol, curdione, germacrone, and β-elemene may be the possible Q-markers. Based on the predicted Q-markers, the mechanisms of the liver-protecting and anti-tumor activities of C. kwangsiensis root tubers were analyzed. AKT1, IL6, EGFR, and STAT3 were identified as the key targets, and neuroactive ligand-receptor interaction signaling pathway, nitrogen metabolism pathway, cancer pathway, and hepatitis B pathway were the major involved pathways. This review provides a basis for the quality evaluation and product development of C. kwangsiensis root tubers and gives insights into the research on Chinese medicinal materials.

Microbial synthesis of monoterpenoids: a review / 生物工程学报

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.

A novel approach to Cestrum intermedium (mata-boi): anatomical and physical-chemical characterization, in vitro biological activities, and metabolites of a Brazilian native species

Abstract The Brazilian native species Cestrum intermedium, known as mata-boi, induces hepatotoxicity and death when ingested by cattle. While most studies on this species focus on toxicological features, our study is the first to describe the anatomy and in vitro biological activities of Cestrum intermedium. We investigated adult leaves and stems by histochemistry, described their anatomy, performed physical-chemical analysis, determined in vitro antioxidant and antimicrobial activities, and identified secondary metabolites. A few noteworthy anatomical features were the anomocytic stomata on the abaxial surface and the absence of trichomes, in addition to the circular shaped petiole with two projections on the adaxial surface. Histochemical analysis showed chemical markers such as alkaloids, usually reported as toxic, and terpenoids. Potassium nitrate (ATR-FTIR) and lupeol palmitate (NMR) were detected on the crude stem extract. Thermogravimetric and physical-chemical analysis provided fingerprint parameters for the species. Minimal Inhibitory Concentration (MIC) assay revealed that Staphylococcus aureus, Staphylococcus epidermidis, and Candida albicans were weakly inhibited by extract samples. Chloroform and ethyl acetate fractions presented high phenolic content, which resulted in in vitro antioxidant activity. These novel features expand the knowledge about this species, considering that previous studies mainly focused on its toxicity. Our study also provided characteristics that may help in avoiding misidentification between Cestrum members, especially when taxonomic keys cannot be employed, as in the absence of flowers and fruits.

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.

Actividad antibacteriana del extracto etanólico de Plantago major frente a Streptococcus mutans / Antibacterial activity of Plantago major ethanolic extract against Streptococcus mutans

Introducción: Las propiedades antibacterianas de Plantago major frente a microorganismos orales no se ha estudiado ampliamente. Objetivo: Identificar los metabolitos secundarios presentes en el extracto etanólico de Plantago major y determinar su actividad antibacteriana frente a Streptococcus mutans. Métodos: Se prepararon concentraciones del 25 por ciento, 50 por ciento, 75 por ciento y 100 por ciento de extracto etanólico (EE) de Plantago major. Se cargaron seis discos de papel con 10 µL, 15 µL, 20 µL y 25 µL de cada concentración, haciendo un total de 96 discos. Los discos fueron colocados en placas Petri con agar cerebro-corazón inoculadas con Streptococcus mutans, se empleó clorhexidina al 0,12 por ciento como control positivo. Se calcularon seis repeticiones para cada concentración. Las placas fueron incubadas a 37 °C por 48 horas. La medición de los halos de inhibición se realizó con un compás digital. El análisis estadístico se realizó mediante la prueba ANOVA de un factor seguido por la prueba post hoc de Tukey. Resultados: El análisis químico del extracto etanólico de Plantago major identificó la presencia de terpenos, diterpenos, saponinas, terpenoidales y aceites esenciales. Las concentraciones del 25 por ciento y 50 por ciento no mostraron efecto antibacteriano, los volúmenes mayores de 20 µL de la concentración del 75 por ciento y todas los del 100 por ciento fueron efectivos para inhibir el crecimiento de Streptococcus mutans con halos de inhibición de 8,36 mm a 14,64 mm. La clorhexidina al 0,12 por ciento inhibió el crecimiento de Streptococcus mutans con halos de inhibición de 17,77 mm en promedio, presentando diferencias significativas con todas las concentraciones del extracto etanólico de Plantago major (P < 0,05). Conclusiones: El extracto etanólico de Plantago major presentó derivados de los terpenos y saponinas, y mostró actividad antibacteriana frente a Streptococcus mutans en volúmenes y concentraciones mayores a 20 µL/75 por ciento(AU)

Introduction: The antibacterial properties of Plantago major against oral microorganisms have not been widely studied. Objective: Identify the secondary metabolites present in an ethanolic extract of Plantago major and determine their antibacterial activity against Streptococcus mutans. Methods: The Plantago major ethanolic extract (EE) was prepared at concentrations of 25 percent, 50 percent, 75 percent and 100 percent. Six paper discs were loaded with 10 µl, 15 µl, 20 µl and 25 µl of each concentration, for a total 96 discs, which were then placed on Petri plates with brain heart agar inoculated with Streptococcus mutans. The positive control was 0.12 percent chlorhexidine. Six replicates were estimated for each concentration. The plates were incubated at 37ºC for 48 hours. Inhibition haloes were measured with a digital caliper. Statistical analysis was based on one-factor ANOVA testing followed by Tukey's post hoc test. Results: Chemical analysis of the Plantago major ethanolic extract identified the presence of terpenes, diterpenes, saponins, terpenoids and essential oils. The 25 percent and 50 percent concentrations did not display an antibacterial effect, whereas volumes above 20 µl of the 75 percent concentration and all 100 percent volumes were effective to inhibit Streptococcus mutans growth with inhibition haloes of 8.36 mm to 14.64 mm. 0.12 percent chlorhexidine inhibited Streptococcus mutans with inhibition haloes of 17.77 mm on average, presenting significant differences with all the concentrations of the Plantago major ethanolic extract (p < 0.05). Conclusions: The Plantago major ethanolic extract was found to contain terpene and saponin derivatives, and displayed antibacterial activity against Streptococcus mutans at volumes and concentrations above 20 µl / 75 percent(AU)

Structural elucidation, mechanism of action, antibacterial proficiency and synergistic forte of purified Euphorbia hirta whole plant extract against multi-drug resistant otitis media infection / Elucidación estructural, mecanismo de acción, competencia antibacteriana y fuerza sinérgica del extracto de planta entera de Euphorbia hirta purificado contra la infección por otitis media resistente a múltiples fármacos

This study investigated the antibacterial potential of Euphorbia hirtawhole plant extracts, honey and conventional antibiotics and their synergistic effects against selected multidrug resistant and typed bacterial strains associated with otitis media. E. hirtawhole plant extract was purified using column chromatography technique. The antibacterial assays of extracts were done using standard microbiological procedures. Protein, sodium and potassium ion leakage of the synergistic mixtures was determined using flame-photometry. At 100 mg/ml, acetone extracts presented highest inhibition against S. aureus (NCTC 6571) with 32 ± 0.83 mm zone of inhibition. The fractional inhibitory concentration indices displayed higher synergism in combination of plant extract, honey and ciprofloxacin against P. mirabilisat 0.02 compared to drug combination synergy standard (≤ 0.5). This work revealed augmentation of ciprofloxacin potency when combined with purified E. hirta acetone extract and honey and implies their high potential in the treatment of multidrug resistant infectionof otitis media.

Este estudio investigó el potencial antibacteriano de extractos de plantas enteras de Euphorbia hirta, miel y antibióticos convencionales y sus efectos sinérgicos contra cepas bacterianas seleccionadas multirresistentes y tipificadas asociadas con la otitis media. El extracto de la planta entera de E. hirtase purificó usando la técnica de cromatografía en columna. Los ensayos antibacterianos de extractos se realizaron utilizando procedimientos microbiológicos estándar. La fuga de iones de proteínas, sodio y potasio de las mezclas sinérgicas se determinó mediante fotometría de llama. A 100 mg/ml, los extractos de acetona presentaron la mayor inhibición contra S. aureus (NCTC 6571) con una zona de inhibición de 32 ± 0,83 mm. Los índices de concentración inhibitoria fraccional mostraron un mayor sinergismo en combinación de extracto de planta, miel y ciprofloxacina contra P. mirabilisa 0,02 en comparación con el estándar de sinergia de combinación de fármacos (≤ 0,5). Este trabajo reveló un aumento de la potencia de la ciprofloxacina cuando se combina con extracto de acetona purificado de E. hirtay miel e implica sualto potencial en el tratamiento de infecciones de otitis media resistentes a múltiples fármacos.

Chemical composition, antioxidant, antimicrobial activity, toxicity, genetic analysis and popular use of Eugenia luschnathiana (O. Berg) Klotzsch ex B. D. Jacks: a literature review / Composición química, actividad antioxidante, antimicrobiana, toxicidad, análisis genético y uso popular de Eugenia luschnathiana (O. Berg) Klotzsch ex B. D Jack: una revisión de la literatura

This review describes the geographical distribution, botanical data, popular use, chemical composition, pharmacological activities and genetic aspects related to Eugenia luschnathiana, a native Brazilian plant popularly known as "bay pitomba". E. luschnathiana leaves are characterized morphologically by the presence of a petiole, an attenuated base, acuminated apex, elliptical shape, and parallel venation. The major chemical compounds found in E. luschnathiana are sesquiterpenes. Literature reports showed that E. luschnathiana extracts have antioxidant properties and antimicrobial activity against Gram-negative and Gram-positive bacteria. The extractsfrom the leaf, fruit and stem, and a concentrated residual solution of its essential oil, displayed negligible toxicity. Lastly, a cytogenetic analysis indicated that some markers can be used for the study of genetic diversity, population structure, and genetic improvements. The information available on E. luschnathiana supports the hypothesis that this plant may be a source of compounds with promising pharmacological activity.

Esta revisión describe la distribución geográfica, datos botánicos, uso popular, composición química, actividad farmacológica y el análisis genético de Eugenia luschnathiana, una planta originaria del Brasil conocida popularmente como "pitomba da baía". Las hojas de E. luschnathiana se caracterizan por la presencia de pecíolo, base atenuada, ápice acuminado, forma elíptica y venación paralela. Su composición química presenta mayormente sesquiterpenos. Los informes en la literatura muestran que los extractos de E. luschnathiana presentan propiedades antioxidantes y actividad antimicrobiana contra las bacterias Gram-negativas y Gram-positivas. Los extractos de la hoja, fruto y tallo, y una solución residual concentrada del aceite esencial, presentaron baja toxicidad. Por último, un análisis citogenético indicó que algunos marcadores pueden utilizarse para estudios de diversidad genética, estructura poblacional y mejoramiento genético. Las informaciones disponibles acerca de E. luschnathiana proponen la hipótesis de que esta planta puede ser una fuente de compuestos con actividad farmacológica prometedora.

New sources of botanical acaricides from species of Croton with potential use in the integrated management of Tetranychus urticae / Nuevas fuentes de acaricidas botánicos de especies de Croton con uso potencial en el manejo integrado de Tetranychus urticae

Essential oils from the leaves and stems of Croton adenocalyx, C. grewioides, C. heliotropiifoliusand C. blanchetianus obtained through hydrodistillation were analyzed by GC-MS. We then investigated the lethal and sublethal effects of the Croton oils and 15 major constituents against Tetranychus urticae. ß-Caryophyllene was the major component in the leaf and stem oils from C. heliotropiifolius and C. adenocalyx. Spathulenol and (E)-anethole were the major constituents identified in the leaf and stem oils of C. blanchetianus and C. grewioides, respectively. The oil with the greatest lethal and sublethal effects was those from C. adenocalyx. Among the constituents ß-caryophyllene and spatulenol were the most toxic to the mite, where as eugenol and methyl eugenol were the most repellent. The toxicity and repellency of the Croton oils, particularly the oils from C. adenocalyx, demonstrate that these oils constitute a promising alternative to synthetic acaricides for use in the control of T. urticae.

Los aceites esenciales de las hojas y tallos de Croton adenocalyx, C. growioides, C. heliotropiifolius y C. blanchetianus obtenidos mediante hidrodestilación fueron analizados a través de GC-MS. Se investigaron los efectos letales y subletales de los aceites de Croton y 15 componentes principales contra Tetranychus urticae. El ß-cariofileno fue el componente principal en los aceites de hojas y tallos de C. heliotropiifolius y C. adenocalyx. El espatulenol y el (E)-anetol fueron los principales componentes identificados en los aceites de hojas y tallos de C. blanchetianus y C. growioides, respectivamente. El aceite con los mayores efectos letales y subletales fue el de C. adenocalyx. Entre los componentes, el ß-cariofileno y el espatulenol fueron los más tóxicos para el ácaro, mientras que el eugenol y el metil eugenol fueron los más repelentes. La toxicidad y la repelencia de los aceites de Croton, particularmente los aceites de C. adenocalyx, demuestran que estos aceites constituyen una alternativa prometedora respecto a los acaricidas sintéticos para uso en el control de T. urticae.

Terpenoids from leaves of Chinese hawthorn / 中国中药杂志

Fifteen compounds were isolated from the 70% EtOH extract of leaves of Chinese hawthorn(Crataegus pinnatifida var. major) by various purification steps, and their structures were determined as 2α,3α,12β,19α,-tetrahydroxyursan-13β,28-olide(1),euscaphic acid(2), tormentic acid(3), ursolic acid(4), pomolic acid(5), corosolic acid(6), maslinic acid(7), linalyl rutinoside(8),(Z)-3-hexenyl β-D-glucoside(9),(3S, 6S)-cis-linalool-3,7-oxide-β-D-glucopyranoside(10), pisumionoside(11), icariside B6(12), byzantionoside B(13),(6R,7E,9R)-9-Hydroxy-4,7-megastigmadien-3-one 9-O-β-D-glucopyranoside(14) and(6S,7E,9R)-6,9-dihydroxy-4,7-megastigmadien-3-one 9-O-β-D-glucopyranoside(15) mainly based on the mass spectrum(MS) and nuclear magnetic resonance(NMR) spectroscopic techniques, of which compound 1 was a new pentacyclic triterpene, and compounds 2, 5, 6, 8, 10, 13 and 15 were isolated form this plant for the first time.

Advances in metabolic engineering of Saccharomyces cerevisiae for terpenoids biosynthesis / 生物工程学报

Terpenoids are a group of structurally diverse compounds with good biological activities and versatile functions such as anti-cancer and immunity-enhancing effects, and are widely used in food, healthcare and medical industries. Facilitated by the increasing understandings on the natural biosynthetic pathways of terpenoids in recent years, Saccharomyces cerevisiae has been engineered into high-yield strains for production of a variety of terpenoids, some of which have reached or become close to the level required by industrial production. In this connection, synthetic biology driven biotechnological production of terpenoids has become a promising alternative to chemical synthesis and traditional extraction approaches. This article summarizes the recent process in engineering S. cerevisiae for terpenoids biosynthesis, highlighting the effect of synthetic biology strategies by taking a couple of typical terpenoids as examples.

Synthetic biology of plants-derived medicinal natural products / 生物工程学报

Medicinal natural products derived from plants are usually of low content and difficult to extract and isolate. Moreover, these compounds are structurally complex, making it difficult to obtain them by environmental unfriendly chemical synthesis. Biosynthesis of medicinal natural products through synthetic biology is a novel, environment-friendly and sustainable approach. Taking terpenoids (ginsenosides, paclitaxel, artemisinin, tanshinones), alkaloids (vincristine and morphine), and flavonoids (breviscapine) as examples, this review summarizes the advances of the biosynthetic pathways and synthetic biology strategies of plant-derived medicinal natural products. Moreover, we introduce the key technologies and methods of synthetic biology used in the research of medicinal natural products, and provide future prospects in this area.

Strictosidine synthase, an indispensable enzyme involved in the biosynthesis of terpenoid indole and β-carboline alkaloids / 中国天然药物

Terpenoid indole (TIAs) and β-carboline alkaloids (BCAs), such as suppressant reserpine, vasodilatory yohimbine, and antimalarial quinine, are natural compounds derived from strictosidine. These compounds can exert powerful pharmacological effects but be obtained from limited source in nature. the whole biosynthetic pathway of TIAs and BCAs, The Pictet-Spengler reaction catalyzed by strictosidine synthase (STR; EC: 4.3.3.2) is the rate-limiting step. Therefore, it is necessary to investigate their biosynthesis pathways, especially the role of STR, and related findings will support the biosynthetic generation of natural and unnatural compounds. This review summarizes the latest studies concerning the function of STR in TIA and BCA biosynthesis, and illustrates the compounds derived from strictosidine. The substrate specificity of STR based on its structure is also summarized. Proteins that contain six-bladed four-stranded β-propeller folds in many organisms, other than plants, are listed. The presence of these folds may lead to similar functions among organisms. The expression of STR gene can greatly influence the production of many compounds. STR is mainly applied to product various valuable drugs in plant cell suspension culture and biosynthesis in other carriers.

Chemical constituents of Psidium guajava and their antitumor and antifungal activities / 中国中药杂志

Twenty-six compounds, including sixteen meroterpenoids(1-16), a triterpenoid(17), four terpenoid derivatives(18-21), and five aromatic compounds(22-26), were isolated from the leaves of Psidium guajava. Their structures were identified by spectroscopic analyses including NMR and MS. Compounds 21-26 were obtained from plants of Psidium for the first time. Based on the structure,(R)-2-ethylhexyl 2H-1,2,3-triazole-4-carboxylate(24 a), an α-glucosidase inhibitor recently isolated from Paramignya trimera, should be revised as compound 24. Meroterpenoids 1-16 were evaluated for their antitumor and antifungal activities. Meroterpenoids psiguajadial D(4), guapsidial A(5), 4,5-diepipsidial A(7), guadial A(14), and guadial B(15) showed cytotoxicities against five human tumor cell lines(HL-60, A-549, SMMC-7721, MCF-7, and SW-480), among which 5 was the most effective with an IC_(50) of 3.21-9.94 μmol·L~(-1).

Research advances in methods of cyclezation mechanism of sesquiterpenes / 中国中药杂志

Terpenes are the largest group of natural products and contain the widest assortment of structural types. Terpene cyclization is also the most complex reaction found in nature. For a long time, terpenoids with diverse structures have attracted natural product chemists to explore their biosynthesis mechanism. Such a large number of terpene skeletons are catalyzed by enzymes called terpene synthase. Sesquiterpene synthase is a kind of terpene synthase, which can catalyze the cyclization of linear precursor farnesyl pyrophosphate(FPP) to sesquiterpene skeletons. Sesquiterpene synthase cyclize a single precursor FPP into many sesquiterpene skeletons. With the continuous discovery of sesquiterpene synthase, the cyclization mechanism of sesquiterpene synthase has been studied deeply. In recent years, with the development and improvement of isotope labeling of substrate FPP and structural analysis of sesquiterpene synthase, the structure and cyclization mechanism of sesquiterpene synthase have been studied more systematically and accurately. In this review, we reviewed the progress of the research methods on the mechanism of sesquiterpene cyclization by substrate isotope labeling and protein structure, as well as the summary and prospect of sesquiterpene synthase research.