Total phenolic, monomeric anthocyanin content and antioxidant activity of Berberis commutata Eichler fruits / Contenido fenólico total, antocianinas monoméricas y actividad antioxidante de los frutos de Berberis commutata Eichler

Background: Berberis commutata Eichler is a berry that grows in the Peruvian Andes and has been consumed in the Andes of South America since ancient times. The edible fruits have an intense purple color and are rich in anthocyanins and phenolic compounds that are available from February until May each year. The color of the fruits is a soft purple dye for natural fibers, and many birds use them as food. Objective: This study quantified the total phenolic, monomeric anthocyanin content and antioxidant activity of Berberis commutata Eichler berries. Methods: The total phenolic content was determined by the Folin-Ciocalteu colorimetric assay. Monomeric anthocyanin content was determined by the method is pH differential, and the antioxidant activity was measured using the Brand-Williams method. Results: The total phenolic content was 7,490 ± 0.85 mg GAE/100g, and the monomeric anthocyanin content was 70 ± 0.03 mg/100g. The antioxidant activity of the berries showed a tendency to increase with B. commutata extract concentration; an EC50 of 0.91 mg/mL was calculated, indicating a high antioxidant power. Conclusion: Our results showed that B. commutata E. has both high total phenolic content and monomeric anthocyanins comparable to other superfruits and high antioxidant activity, which means that it is possible to use this berberis species as a functional food.

Introducción: Berberis commutata Eichleres una baya que crece en los Andes peruanos. Los frutos comestibles tienen un intenso color púrpura rico en antocianinas y componentes fenólicos que están disponibles desde febrero hasta mayo de cada año. El color de sus frutos se utiliza como un suave colorante púrpura para las fibras naturales y muchas aves los utilizan como alimento. Sin embargo, desde la antigüedad los frutos de esta especie han sido consumidas en los Andes de Sudamérica. Objetivo: Este estudio cuantificó el contenido fenólico total, antocianinas monoméricas y la actividad antioxidante usando el método del radical DPPH de las bayas de Berberis commutata Eichler. Método: El contenido fenólico total se midió a través del ensayo colorimétrico de Folin-Ciocalteu, el contenido de antocianinas monoméricas se determinó mediante el método del pH diferencial y la actividad antioxidante se midió con el método de Brand-Williams. Resultados: El contenido fenólico total fue de 7,490 ± 0.85 mg GAE/100g y el contenido de antocianinas monoméricas fue de 70 ± 0.03 mg/100g. La actividad antioxidante de las bayas mostró una tendencia a aumentar con la concentración del extracto de B. commutata, se calculó un EC50 de 0.91 mg/mL que indica un alto poder antioxidante. Conclusión: Nuestros resultados mostraron que B. commutata E. tiene tanto un alto contenido fenólico total, así como antocianinas monoméricas comparables con otras superfrutas y una elevada actividad antioxidante, lo que significa que es posible utilizar esta especie de berberis como alimento funcional.

Inhibitory effects of baicalein against herpes simplex virus type 1

Herpes simplex virus type 1 (HSV-1) is a ubiquitous and widespread human pathogen, which gives rise to a range of diseases, including cold sores, corneal blindness, and encephalitis. Currently, the use of nucleoside analogs, such as acyclovir and penciclovir, in treating HSV-1 infection often presents limitation due to their side effects and low efficacy for drug-resistance strains. Therefore, new anti-herpetic drugs and strategies should be urgently developed. Here, we reported that baicalein, a naturally derived compound widely used in Asian countries, strongly inhibited HSV-1 replication in several models. Baicalein was effective against the replication of both HSV-1/F and HSV-1/Blue (an acyclovir-resistant strain)

Comparative Study on Dpph Free Radical Scavenging Activity of 25 Kinds of Traditional Chinese Medicinal Plants

Aims: To determine and compare the antioxidant activity of water and ethanol extract of 25 kinds of traditional chinese medicinal plants. Results: The ethanol extract of 4 kinds of medicinal herbs had the strongest scavenging activity. They were Magnolia officinalis, Rheum officinale, Psoralea corylifolia and Radix Bupleuri. In addtion, Rheum laciniatum, Chrysanthemum morifolium, Magnolia officinalis and Salvia miltiorrhiza had the strongest scavenging activity of their water extract. On the basis of the above comparison, we evaluated EC50 and total phenolic content of their ethanol extract. The EC50 of Magnolia officinalis, Rheum officinale, Psoralea corylifolia and Radix Bupleuri were 2.75mg·mL-1, 11.82mg·mL-1, 25.22mg·mL-1and 42.67mg·mL-1. The total phenlic content of them were 4.80μg·L-1 , 1.19μg·L-1, 1.07μg·L-1 and 0.75μg·L-1, respectively. Conclusion: The results showed the correlation between the antioxidant activity and the total phenol content. Furthermore, the reaction time of the DPPH test affected the free radical scavenging, which reflected the difference of the extract component would impact the test method.

Establishment and application of a drug screening model targeting somatostatin receptor 2 / 中国药理学通报

Aim To establish a cell model to detect the activity of somatostatin (SST) by targeting somatostatin receptor 2 (SSTR2), and to provide a simple and stable evaluation method for the drug screening of SSTR2 agonists and somatostatin analogues (SSTA). Methods The target gene of SSTR2 was integrated into the pEGFP-N3 vector, and the recombinant plasmid was constructed and transfected into HEK293 cells. After G418 screening, positive clone was selected and the stable cell lines were obtained by expanding culture. The stable cell lines were identified by fluorescence cell imaging, Western blot and qPCR. A calcium flow detection system was established to optimize cell number, fluorescence dye concentration and incubation time. Finally, the screening model was used to detect the different batches of the marketed somatostatin preparation Stilamin. Results SSTR2 stable cell lines were successfully constructed, and the receptors were mainly distributed on the cell membrane. The optimal conditions for calcium flow detection were determined as follows; 30 000 cells/Well, Fluo-4/AM indicator concentration was 3 p,mol • L -1 ~5 u,mol • L-1 , incubation time was 45 min. Under this condition, EC50 value of Stilamin in different batches was stable. Conclusions SSTR2 overexpressed stable cell lines are successfully constructed and calcium flow detection method is optimized to provide a simple and stable model for the screening of somatostatin receptor agonists.

Surrogate potency assays:Comparison of binding profiles complements dose response curves for unambiguous assessment of relative potencies / 药物分析学报

Surface plasmon resonance (SPR) systems are widely used for detailed characterization of antibody ac-tivities including antigen and Fc-receptor binding. During the later stages of development, where the focus is to ensure that established critical quality attributes (CQAs) are maintained during cell culture, purification and formulation processes, analysis is simplified, and relative potencies are often de-termined. Here, simulation of binding data revealed that relative potency values, determined via parallel line analysis (PLA) and half maximal effective concentration (EC50) analysis accurately reflect changes in active concentration only if binding kinetics remain unchanged. Changes in the association rate constant shifted dose response curves, and therefore relative potencies, in the same way as changes in analyte concentration do. However, for interactions characterized by stable binding, changes in the dissociation rate constant did not result in any shift, suggesting that this type of change may go unnoticed in the dose response curve. Thus, EC50 and PLA analyses of dose response curves obtained with an anti-TNF-αan-tibody were complemented with the Biacore functionality for sensorgram comparison analysis, whereby changes in antigen and Fc-receptor binding profiles could be detected. Next, analysis of temperature stressed TNF-α antibody revealed that calibration free concentration analysis (CFCA) data correlated perfectly with relative potency values. Together, these results demonstrate that combinations of SPR based dose response curves, sensorgram comparison and CFCA can be used to strengthen the confidence in relative potency assessments, and suggest that SPR can potentially be used as a surrogate potency assay in the quality control of biotherapeutic medicines.

Effects of different doses of dexmedetomidine on etomidate in inhibiting the EC50 of laryngeal mask placement / 中国生化药物杂志

Objective To investigatethe EC50 of different doses of dexmedetomidine on etomidate inhibited responses tolaryngeal maskinsertion in patients.Methods 88 with breast cancerfrom surgical department in Zhuji Hospital of Traditional Chinese Medical from August 2014 to August 2015were selected and randomly divided into the control group(groupA)and the experiment group(group B1,group B2 and group B3)with 22 casesin each group,respectively,intravenous pump 0.9％sodium chloride solution and DEX(dose followed by 0.3,0.6,0.9μg/kg).The next sequential intravenous infusion of etomidateafter 10 min.The EC50 and the 95％confidence interval of etomidate were determined by sequential method in each group of patients,the changes of vital signs and adverse reactionsin patients were monitored.Results Four groups of patients with LMA EC50 and 95％confidence interval of etomidate respectively:0.78(0.723～0.835)μg/mL in group A,0.66(0.612～0.711)μg/mL in group B1,0.58(0.532～0.627)μg/mL in group B2,0.46(0.416～0.521)μg/mL in group B3.Four groups of patients with laryngeal mask insertion immediately before MAP and HR were lower than the baseline value,the difference was statistically significant(P<0.05),but the LMA elevated after one min.The control group of four patients with respiratory depression,three cases of patients with bradycardia in group B3,two cases of patients with hypotension were improved after symptomatic treatment.Conclusion In a certain range,increasing the dose of dexmedetomidine reduces the effective concentration of etomidate,which inhibits the laryngeal mask placement reaction.

Antiplasmodial Activity of Leaf Extracts of Zanthoxylum chalybeum Engl.

Background: Medicinal herbs have long been used in the treatment of malaria in the endemic tropical and subtropical regions of the world, especially in sub-Saharan Africa where malaria has remained as a top killer disease to children under five years and expectant mothers. Among the herbs commonly used in Uganda to treat malaria is Zanthoxylum chalybeum (ZC) root-bark and to a lesser extent its leaves. However, the continued use of the root-bark has led to plant extinction due to the destructive method of harvesting the herb as opposed to the leaves. Aim: The study investigated the antiplasmodial activity of the crude ether and methanol leaf extracts of ZC with chloroquine diphosphate as a positive control. Materials and Methods: The in vitro Micro-Test (MARK III) kit was used to determine the antiplasmodial activity of Z. chalybeum Engl. ether and methanol extracts. The effective concentration that caused a 50% P. falciparum schizonts suppression (EC50) values were determined. The antiplasmodial activities of the ether and methanol extracts were expressed as 50% effective concentration (EC50) that was determined from doseresponse curve by non-linear regression analysis (curve-fit) using GraphPad Prism (version 6) software at 95% confidence intervals. Results: The results showed that ether extract of ZC had EC50 value of 13.39 (95% CI: 10.82 – 16.59) μg/ml and methanol extract had EC50 value of 8.10 (95% CI: 5.89 – 11.12) μg/ml. The chloroquine diphosphate, standard had EC50 value of 25.33 (95% CI: 17.07 – 37.60) μg/ml. Conclusion: The ether and methanol extracts of Z. chalybeum Engl. contains compounds that caused Plasmodium falciparum schizonts suppression at a lower concentration, hence the continued use of the herb by the traditional herbalist and local communities in Uganda, in the treatment of malaria.

Antioxidant and antimicrobial properties of Litsea elliptica Blume and Litsea resinosa Blume (Lauraceae)

<p><b>OBJECTIVE</b>To investigate antioxidant and antimicrobial activities of two plant species, Litsea elliptica (L. elliptica) and Litsea resinosa (L. resinosa).</p><p><b>METHODS</b>In vitro method-2,2-diphenyl-1-picrylhydrazyl radical scavenging assay was conducted for antioxidant activity determination while antimicrobial assay consisted of agar well diffusion assay and mycelial radial growth assay.</p><p><b>RESULTS</b>Methanol extracts of root and stem of L. elliptica and L. resinosa exhibited the highest antioxidant activity with EC50 of 23.99, 41.69, 11.22 and 35.48 mg/L respectively. All methanol extracts of L. resinosa as well as root extracts from L. elliptica showed significant scavenging activity. Hexane extract from stem of L. resinosa presented the largest inhibition zone in Gram-negative bacteria Pseudomonas aeruginosa and Escherichia coli while chloroform extract from inner bark of L. resinosa showed major inhibition towards Gram-positive bacteria Bacillus subtilis. Essential oils from the root of both species showed significant antifungal activities which are 80.11% and 66.85% respectively.</p><p><b>CONCLUSIONS</b>Overall, methanol extracts from root and stem of both species showed antioxidant activity comparable to standard butylated hydroxytoluene. Extracts from L. resinosa demonstrated stronger antimicrobial properties compared to that from L. elliptica.</p>

Antioxidant and antimicrobial properties of Litsea elliptica Blume and Litsea resinosa Blume (Lauraceae)

Objective: To investigate antioxidant and antimicrobial activities of two plant species, Litsea elliptica (L. elliptica) and Litsea resinosa (L. resinosa). Methods: In vitro method -2,2-diphenyl-1-picrylhydrazyl radical scavenging assay was conducted for antioxidant activity determination while antimicrobial assay consisted of agar well diffusion assay and mycelial radial growth assay. Results:Methanol extracts of root and stem of L. elliptica and L. resinosa exhibited the highest antioxidant activity with EC50 of 23.99, 41.69, 11.22 and 35.48 mg/L respectively. All methanol extracts of L. resinosa as well as root extracts from L. elliptica showed significant scavenging activity. Hexane extract from stem of L. resinosa presented the largest inhibition zone in Gram-negative bacteria Pseudomonas aeruginosa and Escherichia coli while chloroform extract from inner bark of L. resinosa showed major inhibition towards Gram-positive bacteria Bacillus subtilis. Essential oils from the root of both species showed significant antifungal activities which are 80.11%and 66.85%respectively. Conclusions:Overall, methanol extracts from root and stem of both species showed antioxidant activity comparable to standard butylated hydroxytoluene. Extracts from L. resinosa demonstrated stronger antimicrobial properties compared to that from L. elliptica.

Quantitative stuucture-activity relationships t predict in vitro teac and ec500 of synthetic anilines / Relacionescuantiitativas actividad-estructura para predeci la teac y la eec50 de anilinas sintéticas / Relaçõs quantitaativas atividade - estrutura para a predição a teaceaec50 da anilinas sintéticas

Quantitative Structure-Activity Relationships (QSAR) are useful in understanding how chemical structure relates to the biological activity of natural or synthetic compounds and for designing newer and better compounds. In the present study, 22 N-arylmethyl substituted anilines were treated with ABTS (2,2'-azinobis- (3-ethylbenzothiazoline-6-sulfonic-acid)) and DPPH (2,2-diphenyl-1-picrylhy-dracyl) radicals in order to evaluate their TEAC (mmol trolox/mmol antioxidant, Trolox Equivalent Antioxidant Capacity) and EC50 (mmol antioxidant/mmol initial DPPH, Antioxidant Equivalent Concentration to decrease the initial DPPH concentration by 50 %) values, respectively. Different QSARs were developed based on these data, using theoretical descriptors derived from geometry-optimized molecular structures. A model with electronic energy (EE), total charge weighted partial positively charged surface area (PPSA-2), and exact polarizability (αzz) as descriptors showed satisfactory predictive TEAC performance according to internal and external validation procedures. It can be useful in predicting data and setting a testing priority for those compounds not yet synthesized or for which experimental data are not available.

Las relaciones cuantitativas actividad-estructura (QSAR) son útiles para entender la forma en que la estructura química de sustancias sintéticas y naturales se relaciona con la actividad biológica, y para el diseño de nuevos y mejores compuestos. En el presente estudio fueron evaluadas las capacidades de 22 anilinas N-arylmetil sustituidas para la captura de los radicales ABTS (ácido 2,2'-azino-bis(3-etilbenzo-tiazolino-6-sulfónico) y DPPH (2,2-difenil-1-picrilhidracilo), relacionadas con los valores de TEAC (mmol trolox/mmol antioxidante, capacidad antioxidante equivalente al Trolox) y EC50 (concentración equivalente de antioxidante para disminui r la concentración inicial de DPPH enun 50%), respectivamente. Las TEAC, las EC50 y los descriptores teóricos derivados de las estructuras moleculares optimizadas fueron utilizados para elaborar las diferentes QSAR. Los modelos TEAC con descriptores como EE (energía electrónica), PPSA-2 (carga total pesada con el área superficial cargada positivamente) y αzz (polarizabilidad exacta) mostraron una capacidad de predicción satisfactoria por procedimientos de validación interna y externa, por lo que pueden ser útiles para la predicción de actividades de compuestos que aún no han sido sintetizados o con datos experimentales no disponibles.

Relaçãos quantitativa atividade - estrutura tem sido empregado para estabelecer se a estrutura química está relacionada com a atividade biológica dos químicos naturais e sintéticos e para o desenho de novos e melhores compostos. No presente estudo foram avaliadas as capacidades de 22 anilinas N-arylmetil sustituidas para a captura dos radicais de ABTS (ácido-2,2'-azino-bis(3-etilo-benzo-tiazolino-6-sulfônic o) e DPPH (2,2-difenilo-1-picrilhidracilo), relacionadas com os valores de TEAC (mmol trolox/mmol antioxidante, capacidade antioxidante equivalente ao Trolox) yEC50 (concentração equivalente de antioxidante para a diminuição da concentração inicial de DPPH para um 50 %) respectivamente. As TEAC, as EC50 eos descritores teóricos derivados das estruturas moleculares otimizadas foram empregados para elaborar as diferentes QSARs. Os modelos TEAC com descritores como EE (Energia Eletrônica), PPSA-2 (carga total pesada com a área superficial carregada positivamente) y αzz (polarizabilidade exata) mostraram uma satisfatória capacidade de predição pelos procedimentos de validação interna e externa, e por tanto podem ser úteis para a predição da capacidade antioxidante de compostos que ainda no tem sido sintetizados com dados experimentais não disponíveis.

The Interaction between Remifentanil and Propofol during Total Intravenous Anesthesia and the Adequate Effect Site Concentration / 대한마취과학회지

BACKGROUND: This study was performed to evaluate the interaction between remifentanil and propofol by comparing median-effect concentration (EC50) of single and co-administration, and to find adequate combination doses for general anesthesia for gastrectomy. METHODS: Thirty-six ASA physical status 1 or 2 patients scheduled for gastrectomy were randomly assigned to the remifentanil, propofol, or combination group.To obtain the dose-effect curve of remifentanil or propofol only, the effect site concentration of each drug was escalated until bispectral index (BIS) was reached 40 by a target-controlled infusion (TCI) during the steady operational period.For the combination group, 0.25, 0.5, 1, 2, and 2.5 timed EC50 of each drug were co-administered.The heart rate, mean arterial pressure and BIS were measured during the study period.The interaction between remifentanil and propofol was analyzed with using isobologram. RESULTS: The EC50 of remifentanil for hypnosis (BIS 40) was 1.96 ng/ml, and that of propofol was 1.35microgram/ml.In the combination group, the EC50 of remifentanil was 0.81 ng/ml and that of propofol was 0.56microgram/ml.EC90 of remifentanil and propofol alone were 13.43 ng/ml and 4.88microgram/ml. For EC90 of the combination group, remifentanil 3.54 ng/ml and propofol 2.50 microgram/ml were required.The distance from the theoretical additive line in the isobologram was larger in the higher doses (EC50 < EC75 < EC90). CONCLUSIONS: This study shows that remifentanil and propofol reveal synergism by isobolographic analysis during intravenous anesthesia.

The Effect of Cigarette Smoking on Propofol EC50 of Airway Obstruction during Target Controlled Infusion of Propofol / 대한마취과학회지

BACKGROUND: Airway obstruction is a main cause of respiratory complications during sedation. The aim of this study was to identify the effect of smoking on the target plasma concentration of propofol (EC50) of airway obstruction during target controlled infusion (TCI) of propofol. METHODS: Thirty healthy male adults scheduled for lower extremity surgery under regional anesthesia were randomly allocated to one of five target plasma concentrations (CP) of propofol: 1.0, 2.0, 3.0, 4.0, 5.0microgram/ml (n = 6 for each concentration). After performing regional anesthesia, oxygen was supplied and ETCO2 was measured. All patients received propofol TCI with the assigned CP. The occurrence of airway obstruction was observed until 5 minutes after effect site concentration (CE) reached CP. When hypoxemia, apnea or total airway obstruction was observed, ventilation was assisted with 100% oxygen. The CP, smoking history, snoring history, age, body mass index, Mallampati's classification and thyromental distance were regarded as independent variables. The relationship of airway obstruction and the variables was analyzed with logistic regression with Wald-forward method. By the equation of the probability of airway obstruction 'P = 1/(1 + e-z)', we estimated the propofol EC50 of airway obstruction in smokers and nonsmokers. RESULTS: The result of logistic regression was as following: z (airway obstruction) = -5.557 + 2.128 x CP [microgram/ml] + 3.625 x smoking (CP: P = 0.007, smoking: P = 0.047). The propofol EC50 of airway obstruction of non-smokers and smokers was 2.6 (1.5-9.4)microgram/ml and 0.9 (-9.3)microgram/ml, respectively. CONCLUSIONS: The propofol EC50 of airway obstruction of smokers was lower than that of nonsmokers.