Chemical composition, antioxidant and antimicrobial activities of essential oil from the aerial parts of Chuquiraga arcuataHarling grown in the highlands of Ecuador / Composición química, actividades antioxidantes y antimicrobianas del aceite esencial de las partes aéreas de Chuquiraga arcuataHarling cultivado en las tierras altas del Ecuador

Thechemical composition, antioxidant and antimicrobial activities of the essential oil from aerial parts (leaves and flowers) of Chuquiraga arcuataHarling grown in the Ecuadorian Andes were studied. One hundred and twenty-six compounds were identified in the essential oil. Monoterpene hydrocarbons (45.8%) and oxygenated monoterpenes (44.1%) had the major percentages. The most abundant compounds were camphor (21.6%), myrcene (19.5%), and 1,8-cineole (13.4%). Antioxidant activity was examined using DPPH, ABTS,and FRAP assays. The essential oil had a moderate scavenging effect and reduction of ferric ion capacity through FRAP assay. Antimicrobial activity of the essential oil was observed against four pathogenic bacteria and a fungus. The essential oil exhibited activity against all microorganism strains under test, particularly against Candida albicansand Staphylococcus aureuswith MICs of 2.43-12.10 µg/mL.

Se estudió la composición química, actividades antioxidantes y antimicrobianas del aceite esencial procedente de las partes aérea (hojas y flores) de Chuquiraga arcuataHarling cultivadas en los Andes ecuatorianos. Se identificaron 126 compuestos en el aceite esencial. Los hidrocarburos monoterpénicos (45,8%) y los monoterpenos oxigenados (44,1%) tuvieron el mayor porcentaje. Los compuestos más abundantes fueron alcanfor (21,6%), mirceno (19,5%) y 1,8-cineol (13,4%). La actividadantioxidante se examinó mediante ensayos DPPH, ABTS y FRAP. El aceite esencial tuvo un efecto eliminador moderado y una reducción de la capacidad de iones férricos mediante el ensayo FRAP. Se observó actividad antimicrobiana del aceite esencial contra cuatro bacterias y un hongo patógenos. El aceite esencial mostró actividad contra todas las cepas de microorganismos bajo prueba, particularmente contra Candida albicansy Staphylococcus aureuscon CMI de 2,43-12,10 µg/mL.

Promoción de actividades físicas para adultos mayores: Una estrategia educativa para estudiantes de Gerontología

En la actualidad, existe una tendencia progresiva al envejecimiento de la población. El propósito de esta investigación consistió exponer una estrategia educativa para los estudiantes del 5.º nivel de Gerontología que contribuya a la promoción de la actividad física en el adulto mayor. La investigación se enmarcó en una metodología mixta y un diseño descriptivo de corte transversal. Se emplearon métodos científicos que en el orden teórico se encuentran análisis-síntesis, inductivo-deductivo y el sistémico estructural, y como métodos empíricos la revisión documental, la observación, la encuesta y entrevistas, las cuales fueron aplicadas a una muestra de 38 sujetos y revelan la importancia de la actividad física como estrategia que permite alcanzar un envejecimiento activo y con calidad de vida en la tercera edad. Según estos resultados, la aplicación de una estrategia educativa estructurada en tres etapas y dos fases contribuye a la autogestión del aprendizaje de los estudiantes, donde el contexto profesional se convierte en un auténtico espacio de formación.

Atualmente, há uma tendência progressiva de envelhecimento da população. O objetivo desta pesquisa foi apresentar uma estratégia educacional para estudantes do 5º nível de Gerontologia que contribua para a promoção da atividade física em idosos. A pesquisa foi enquadrada em uma metodologia mista e um desenho descritivo transversal. Foram utilizados os métodos científicos teórico, indutivo-dedutivo e sistêmico-estrutural, e os métodos empíricos foram revisão documental, observação, inquérito e entrevistas, que foram aplicados a uma amostra de 38 sujeitos e revelam a importância da atividade física como estratégia para alcançar o envelhecimento ativo e a qualidade de vida dos idosos. De acordo com esses resultados, a aplicação de uma estratégia educacional estruturada em três etapas e duas fases contribui para o autogerenciamento da aprendizagem dos alunos, em que o contexto profissional se torna um autêntico espaço de treinamento.

Currently, there is a progressive trend towards population aging. The purpose of this research was to present an educational strategy for students of the 5th level of Gerontology that contributes to the promotion of physical activity in older adults. The research was framed in a mixed methodology and a cross-sectional descriptive design. Scientific methods were used that in the theoretical order include analysis-synthesis, inductive-deductive and structural systemic and as empirical methods documentary review, observation, survey and interviews, applied to a sample of 38 subjects. The study revealed the importance of physical activity as a strategy that allows achieving active aging with quality of life. According to these results, the application of an educational strategy, structured in three stages and two phases, contributes to the self-management of student learning, where the professional context becomes an authentic training space.

¿Cómo y Cuánto se Mueven los Adultos que sufrieron un Evento Coronario un Año después de haber entrado a un Programa de Rehabilitación Cardiaca? / How and How Much Do Adults Who Suffered a Coronary Event Move One Year After Entering a Cardiac Rehabilitation Program?

Introducción. Establecer un estilo de vida activo y saludable es uno de los objetivos más importantes y desafiantes de la rehabilitación cardíaca. Comprender el comportamiento de los patrones de actividad física (AF) en adultos que han sufrido un evento coronario y que han participado en un programa de Rehabilitación Cardíaca (RC) es necesario para evaluar su impacto y proponer estrategias oportunas en esta área. Objetivo. Evaluar el cumplimiento de la recomendación global de AF 1 año después de ingresar a un programa de RC para enfermedad arterial coronaria. Métodos. Se aplicó el Cuestionario Internacional de Actividad Física a adultos con enfermedad coronaria tratada a los 6 y 12 meses de su ingreso a un programa de Rehabilitación Cardíaca en 6 hospitales de Chile, entre mayo de 2019 y febrero de 2020 en el contexto del estudio aleatorizado. Se realizó un ensayo clínico multicéntrico de no inferioridad (Hybrid Cardiac Rehabilitation Trial, HYCARET). Resultados. 117 participantes (74 hombres, edad 59,34 ±9,52 años, 83,4±27,2% de adherencia a la RC) físicamente activos al final de un programa de RC fueron evaluados a los 6 y 12 meses desde el ingreso para determinar su adherencia a la AF. La tasa de seguimiento fue del 94,01% a los 6 meses (6m) y del 78,63% a los 12 meses (12m). El 90% de los participantes seguían físicamente activos a los 6 meses y el 92,39% seguían activos a los 12 meses después del evento coronario. Un 5,98% fueron clasificados como inactivos a los 6 m pero estaban físicamente activos al año. En contraste, sólo el 0,85% se volvió inactivo a los 6 meses y permaneció inactivo hasta 1 año, mientras que el 4,27% se reportó como activo a los 6 meses, pero terminó estando inactivo al año. La AF relacionada con las tareas del hogar es responsable del 40% y más del gasto calórico total de los adultos después de un evento coronario en todo momento. El gasto calórico relacionado con actividades recreativas y transporte disminuyó a los 6 y 12 meses, mientras que el gasto calórico asociado con el trabajo y las actividades domésticas aumentó a los 6 y 12 meses después de completar un programa de RC. Conclusión. Los adultos que completan un programa de RC continúan activos 6 y 12 meses después de un evento coronario. Sin embargo, las actividades que generan mayor gasto calórico varían con el tiempo. Este hallazgo resalta la importancia de fomentar la actividad física como parte del tiempo de ocio y recreación en los adultos, ya que se sabe que su beneficio es mayor.

Background. Establishing a healthy, active lifestyle is one of the most important and challenging goals of cardiac rehabilitation. Understanding the behavior of physical activity (PA) patterns in adults who have suffered a coronary event and who have participated in a Cardiac Rehabilitation (CR) program is necessary to evaluate its impact and propose timely strategies in this area. Objetive. To evaluate compliance with the global PA recommendation 1 year after entering a CR program for coronary artery disease. Methods. The International Physical Activity Questionnaire was applied to adults with coronary heart disease treated 6 and 12 months after admission to a Cardiac Rehabilitation program in 6 hospitals in Chile, between May 2019 and February 2020 in the context of the randomized study. A multicenter non-inferiority clinical trial (Hybrid Cardiac Rehabilitation Trial, HYCARET) was conducted. Results. 117 participants (74 men, age 59.34 ± 9.52 years, 83.4 ± 27.2% adherence to CR) physically active at the end of a CR program were evaluated at 6 and 12 months from entry. to determine their adherence to PA. The follow-up rate was 94.01% at 6 months (6m) and 78.63% at 12 months (12m). 90% of participants were still physically active at 6 months and 92.39% were still active at 12 months after the coronary event. 5.98% were classified as inactive at 6 m but were physically active at one year. In contrast, only 0.85% became inactive at 6 months and remained inactive for up to 1 year, while 4.27% reported themselves as active at 6 months but ended up being inactive at one year. Housework-related PA is responsible for 40% and more of adults' total caloric expenditure after a coronary event at all times. Caloric expenditure related to recreational activities and transportation decreased at 6 and 12 months, while caloric expenditure associated with work and home activities increased at 6 and 12 months after completing a CR program. Conclusion. Adults who complete a CR program remain active 6 and 12 months after a coronary event. However, the activities that generate the greatest caloric expenditure vary over time. This finding highlights the importance of promoting physical activity as part of leisure and recreation time in adults, since it is known that its benefit is greater.

Modulación por Passiflora edulis de triglicéridos y colesterol intracelulares en líneas celulares de cáncer colorrectal SW480 y sus derivadas metastásicas (SW620) / Modulation by Passiflora edulis of intracellular triglycerides and cholesterol in SW480 col orectal cancer cell lines and their metastatic derivatives (SW620)

Cancer cells modify lipid metabolism to proliferate, Passiflora edulis ( P. edulis ) fruit juice (ZuFru) has antitumor activity, but whether a mechanism is through modulation of cell lipids is unknown. T o establish if ZuFru modifies cholesterol and triglycerides in SW480 and SW620. ZuFru composition was studied by phytochemical march; antiproliferative activity by sulforhodamine B, cholesterol , and triglycerides by Folch method. Z ufru contains anthocyanins, flavonoids, alkaloids , and tannins. Cell lines showed differences in their growth rate ( p =0.049). At 39.6 µg/m L of ZuFru, cell viability was decreased: SW480 (45.6%) and SW620 (45.1%). In SW480, cholesterol (44.6%) and triglycerides (46.5%) decreased; In SW620, cholesterol decreased 14.8% and triglycerides increased 7%, with significant differences for both lines. A ntiproliferative activity of ZuFru could be associated with the inhibition of intracellular biosynthesis of cholesterol and triglycerides in SW480. Action mechanisms need to be further investigated.

Las células cancerosas modifican el metabolismo lipídico para proliferar; el zumo de fruta (ZuFru) de Passiflora edulis ( P. edulis ) tiene activida d antitumoral, sin embargo, se desconoce si se involucran los lípidos celulares. E stablecer si ZuFru modifica colesterol y triglicéridos en células SW480 y SW620. C omposición del ZuFru, actividad antiproliferativa, colesterol y triglicéridos. Se encontraro n antocianinas, flavonoides, alcaloides y taninos. Las líneas celulares mostraron diferencias en su tasa de crecimiento ( p =0 . 049); ZuFru 39,6 µg/ml se disminuyó la viabilidad celular; SW480 (45,6%) y SW620 (45,1%); en SW480 colesterol (44,6%) y triglicérid os (46,5%) en SW620, colesterol (14,8%) y los triglicéridos aumentaron 7%, con diferencias significativas para ambas líneas. La actividad antiproliferativa del ZuFru podría estar asociada a la inhibición de la biosíntesis intracelular de colesterol y de tr iglicéridos en SW480, pero no en SW620. Estos mecanismos de acción deben ser fuertemente investigados.

Effect of refining and pressing temperature on chemical attributes of canola oil produced in Chile

The consumption of vegetable oils is common in our daily diet. Rapeseed oil (canola oil) is the third most consumed edible oil in the world, followed by palm and soybean oils in terms of production. Rapeseed oil has a low proportion of saturated fatty acids, while it is rich in unsaturated fatty acids, as well as in healthy compounds such as phenols, tocopherols, phytosterols, carotenoids, and fat-soluble vitamins. However, processing technologies affect the content and functional activities of bioactive compounds in the oil. Aim: To assess any potential effect of hot or cold pressing and a refining process on the nutritional value and the profile of several bioactive compounds in canola oils produced in Chile. Methods: Canola oils were characterized regarding their fatty acid profile, phytosterol and tocopherol composition, total phenol content, and antioxidant activity, according to the mode of extraction (cold or hot pressed) and before and after bWeing subjected to a refining process. Results: Fatty acid profiles were not significantly different in any of the analyzed canola oils. Refining but not temperature extraction led to a sharp decrease of phytosterols and tocopherols. Hot pressing significantly increased the amount of total phenols (3.1 times) and the antioxidant activity measured by ORAC (3.1 times) and DPPH (8.3 times) compared to the cold extraction. However, phenolic concentration and antioxidant capacity decreased after refining. Conclusions: Refining processes should be adjusted to reduce the loss of bioactive compounds in the oil.

El consumo de aceites vegetales es habitual en nuestra dieta diaria. El aceite de colza (aceite de canola) es el tercer aceite comestible más consumido en el mundo, seguido por los aceites de palma y soja en términos de producción. El aceite de colza tiene una baja proporción de ácidos grasos saturados, mientras que es rico en ácidos grasos insaturados, así como en compuestos liposolubles saludables como fenoles, tocoferoles, fitoesteroles, carotenoides y vitaminas. Sin embargo, las tecnologías de procesamiento afectan el contenido y las actividades funcionales de los compuestos bioactivos en el aceite. Objetivo: Evaluar cualquier efecto potencial del prensado en caliente o en frío y un proceso de refinación sobre el valor nutricional y el perfil de varios compuestos bioactivos en los aceites de canola producidos en Chile. Métodos: Los aceites de canola se caracterizaron en cuanto a su perfil de ácidos grasos, composición de fitoesteroles y tocoferoles, contenido de fenoles totales y actividad antioxidante, según el modo de extracción (prensado en frío o en caliente) y antes y después de ser sometidos a un proceso de refinación. Resultados: Los perfiles de ácidos grasos no fueron significativamente diferentes en ninguno de los aceites de canola analizados. La refinación, pero no la extracción en caliente, condujo a una fuerte disminución de los fitoesteroles y tocoferoles. El prensado en caliente aumentó significativamente la cantidad de fenoles totales (3,1 veces) y la actividad antioxidante medida por ORAC (3,1 veces) y DPPH (8,3 veces) en comparación con la extracción en frío. Sin embargo, la concentración de fenoles y la capacidad antioxidante disminuyeron después del refinado. Conclusión: Los procesos de refinación deben ajustarse para reducir la pérdida de compuestos bioactivos en el aceite.

Antimicrobial and antioxidant activity of Panax ginseng and Hedysarum neglectum root crop extracts / Atividade antimicrobiana e antioxidante de extratos de raízes de Panax ginseng e Hedysarum neglectum

In order to ensure the timely and uninterrupted supply of medicinal plant raw materials, the methods of cultivation of plant cell cultures, namely, the production of plant root cultures, are relevant. In this paper, the geroprotective potential of Hedysarum neglectum Ledeb and Panax ginseng C. A. Mey root cultures is studied. They were cultured under in vitro conditions by transforming the rhizome (H. neglectum) and seed seedlings (P. ginseng) with Agrobacterium rhizogenes 15834 Swiss. To identify the geroprotective potential, the antimicrobial disc-diffusion method and the antioxidant activity were analyzed by titration of KMnO4 extracts of plant root cultures. The qualitative and quantitative composition was analyzed using high-performance liquid chromatography, thin-layer chromatography, and gas chromatography with mass spectrometry. In the course of the work, the presence of antimicrobial and antioxidant activity of plant root culture extracts was established. Biologically active substances contained in extracts of Hedysarum neglectum Ledeb root crops and Panax ginseng C. A. Mey are characterized by geroprotective potential, so they can act as a source of natural antioxidants in the functional nutrition of the geroprotective orientation.

Para garantir o abastecimento em tempo e ininterrupto de matérias-primas de plantas medicinais, são relevantes os métodos de cultivo de culturas de células vegetais, nomeadamente a produção de culturas de raízes vegetais. Neste trabalho, foi estudado o potencial geroprotetor de culturas de raízes de Hedysarum neglectum Ledeb e Panax ginseng C. A. Mey. Eles foram cultivados em condições in vitro pela transformação do rizoma (H. neglectum) e mudas de sementes (P. ginseng) com Agrobacterium rhizogenes 15834 Swiss. Para identificar o potencial geroprotetor, o método antimicrobiano de difusão em disco e a atividade antioxidante foram analisados por titulação de extratos de KMnO4 de raízes de plantas. A composição qualitativa e quantitativa foi analisada por cromatografia líquida de alta eficiência, cromatografia em camada delgada e cromatografia gasosa com espectrometria de massa. No decorrer do trabalho, foi constatada a presença de atividade antimicrobiana e antioxidante dos extratos de raízes de plantas. Substâncias biologicamente ativas contidas em extratos de raízes de H. neglectum Ledeb e P. ginseng C. A. Mey são caracterizadas pelo potencial geroprotetor, podendo atuar como fonte de antioxidantes naturais na nutrição funcional da orientação geroprotetora.

The antagonistic activity of the synbiotic containing Lactobacillus acidophilus and pineapple residue FOS against pathogenic bacteria / A atividade antagônica do simbiótico contendo Lactobacillus acidophilus e resíduo de abacaxi FOS contra bactérias patogênicas

Fructooligosaccharide is used widely in many foods and pharmaceutical industries and produced by using different ways such as extracting it from plants or producing it by using plants and microorganisms' enzymes. In a previous study, we extracted Fructosyltransferase (Ftase) enzyme from pineapple residue and produced FOS. In this study, we measured the antagonistic activity of two synbiotics, the first synbiotic containing Lactobacillus acidophilus and the produced FOS, the second synbiotic containing Lactobacillus acidophilus and standard FOS, against pathogenic bacteria (P. aeruginosa, E. coli, S. aureus and B cereus). The results showed that the antagonistic activity of both synbiotic types was very close, as there were no significant differences between them except in the antagonistic activity against S. aureus, there was a significant difference between the synbiotic containing the standard FOS, which was the highest in its antagonistic activity compared to the synbiotic containing the produced FOS in this study. The activity of the fructooligosaccharide (FOS) extracted from pineapple residue was evident in enhancing the activity of the probiotic bacteria (L. acidophilus), which had a major role in the production of acids and compounds that inhibited the pathogenic bacteria. The diameters of inhibition areas in the current study ranged between 19.33-28 mm, and E. coli was more susceptible to inhibition, followed by S. aureus, P. aeruginosa, and B. cereus, respectively.

O fruto-oligossacarídeo (FOS) é amplamente utilizado em muitos alimentos e indústrias farmacêuticas, e é produzido por meio de diferentes maneiras, como extraí-lo de plantas ou produzi-lo usando enzimas de plantas e microrganismos. Em um estudo anterior, extraímos a enzima frutosiltransferase (Ftase) do resíduo de abacaxi e produzimos FOS. Neste estudo, medimos a atividade antagônica de dois simbióticos: o primeiro simbiótico contendo Lactobacillus acidophilus e o FOS produzido, e o segundo simbiótico contendo Lactobacillus acidophilus e o FOS padrão, contra bactérias patogênicas (P. aeruginosa, E. coli, S. aureus e B. cereus). Os resultados mostraram que a atividade antagônica de ambos os tipos simbióticos foi muito próxima, pois não houve diferenças significativas entre eles, exceto na atividade antagônica contra S. aureus, em que houve uma diferença significativa entre o simbiótico contendo o FOS padrão, que foi o mais alto em sua atividade antagônica, em comparação com o simbiótico contendo o FOS produzido neste estudo. A atividade do fruto-oligossacarídeo (FOS) extraído do resíduo de abacaxi ficou evidente no aumento da atividade da bactéria probiótica (L. acidophilus), que teve papel importante na produção de ácidos e compostos inibidores das bactérias patogênicas. Os diâmetros das áreas de inibição no estudo atual variaram entre 19,33 e 28 mm, e E. coli foi mais suscetível à inibição, seguida por S. aureus, P. aeruginosa e B. cereus, respectivamente.

Elemene Antitumor Drugs Development Based on "Molecular Compatibility Theory" and Clinical Application: A Retrospective and Prospective Outlook / 中国结合医学杂志

Elemene, derived from Curcuma wenyujin, one of the "8 famous genuine medicinal materials of Zhejiang province," exhibits remarkable antitumor activity. It has gained wide recognition in clinical practice for effectiveness on tumors. Dr. XIE Tian, introduced the innovative concept of "molecular compatibility theory" by combining Chinese medicine principles, specifically the "monarch, minister, assistant, and envoy" theory, with modern biomedical technology. This groundbreaking approach, along with a systematic analysis of Chinese medicine and modern biomedical knowledge, led to the development of elemene nanoliposome formulations. These novel formulations offer numerous advantages, including low toxicity, well-defined composition, synergistic effects on multiple targets, and excellent biocompatibility. Following the principles of the "molecular compatibility theory", further exploration of cancer treatment strategies and methods based on elemene was undertaken. This comprehensive review consolidates the current understanding of elemene's potential antitumor mechanisms, recent clinical investigations, advancements in drug delivery systems, and structural modifications. The ultimate goal of this review is to establish a solid theoretical foundation for researchers, empowering them to develop more effective antitumor drugs based on the principles of "molecular compatibility theory".

Monotropein Induced Apoptosis and Suppressed Cell Cycle Progression in Colorectal Cancer Cells / 中国结合医学杂志

OBJECTIVE@#To determine whether monotropein has an anticancer effect and explore its potential mechanisms against colorectal cancer (CRC) through network pharmacology and molecular docking combined with experimental verification.@*METHODS@#Network pharmacology and molecular docking were used to predict potential targets of monotropein against CRC. Cell counting kit assay, plate monoclonal assay and microscopic observation were used to investigate the antiproliferative effects of monotropein on CRC cells HCT116, HT29 and LoVo. Flow cytometry and scratch assay were used to analyze apoptosis and cell cycle, as well as cell migration, respectively in HCT116, HT29, and LoVo cells. Western blotting was used to detect the expression of proteins related to apoptosis, cell cycle, and cell migration, and the expression of proteins key to the Akt pathway.@*RESULTS@#The Gene Ontology and Reactome enrichment analyses indicated that the anticancer potential of monotropein against CRC might be involved in multiple cancer-related signaling pathways. Among these pathways, RAC-beta serine/threonine-protein kinase (Akt1, Akt2), cyclin-dependent kinase 6 (CDK6), matrix metalloproteinase-9 (MMP9), epidermal growth factor receptor (EGFR), cell division control protein 42 homolog (CDC42) were shown as the potential anticancer targets of monotropein against CRC. Molecular docking suggested that monotropein may interact with the 6 targets (Akt1, Akt2, CDK6, MMP9, EGFR, CDC42). Subsequently, cell activity of HCT116, HT29 and LoVo cell lines were significantly suppressed by monotropein (P<0.05). Furthermore, our research revealed that monotropein induced cell apoptosis by inhibiting Bcl-2 and increasing Bax, induced G1-S cycle arrest in colorectal cancer by decreasing the expressions of CyclinD1, CDK4 and CDK6, inhibited cell migration by suppressing the expressions of CDC42 and MMP9 (P<0.05), and might play an anticancer role through Akt signaling pathway.@*CONCLUSION@#Monotropein exerts its antitumor effects primarily by arresting the cell cycle, causing cell apoptosis, and inhibiting cell migration. This indicates a high potential for developing novel medication for treating CRC.

Effect of Diffuse Glioma with Precentral Gyrus Invasion on Interhemispheric Brain Activation： A Task-based FMRI Study / 中山大学学报(医学科学版)

ObjectivesTo explore the effect of diffuse glioma with precentral-gyrus invasion on fMRI activation maps by grasping T-fMRI. MethodsA total of 56 diffuse glioma patients were divided into precentral-gyrus invasion （PGI： n=21） and precentral-gyrus non-invasion （PGNI： n=35） groups. Three statistical thresholds （P value： 10-4， P1； 10-6， P2； 10-8， P3） were set to obtain the activation maps accordingly （V1， V2 and V3）. The interhemispheric and bilateral precentral gyrus activation volumes ratios （IAVR and PAVR） were calculated， respectively. The activation volumes ［△V1=V1-V2； △V2=V2-V3； △Vn （ipsilateral）/△Vn’ （contralateral）， n=1， 2］ within two statistical thresholds and the corresponding interhemispheric ratio was further compared. In addition， the associations of tumor characteristics with IAVR and PAVR were analyzed. ResultsCompared with PGNI， PGI showed significantly decreased IAVR at p1， and the same trends of PAVR in PGI at P1 and P2 （P＜0.05）. However， neither IAVR nor PAVR showed significant differences at P3. PGI showed significantly lower ratios of △V1/△V1’ than PGNI （P=0.02）， except for △V2/△V2’. Additionally， within PGI， PAVR was negatively correlated with tumor volume （P=0.043）， and the distance from the tumor to the hand-knob was positively correlated with the IAVR and PAVR （P＜0.05）. ConclusionDiffuse glioma invading eloquent areas tended to affect interhemispheric asymmetry of activation at relatively lower statistical thresholds than diffuse glioma without invasion， rather than stricter statistical thresholds. Multiple ranges of statistical thresholds were recommended to analyze T-fMRI.

The effect of mini basketball on upper limb strength performance in children aged 4-6 years: a Meta analysis / 中国学校卫生

Objective@#To systematically evaluate the effect of mini basketball on children s upper limb strength in China, and to provide basis for the development of kindergarten mini basketball and the improvement of children s upper limb strength performance.@*Methods@#CNKI, Wanfang Data, VIP, PubMed, and Web of Science databases were searched from the establishment of the database to July 26, 2023. The PICOST model was used for literature screening, and 13 literature with a total of 20 studies were finally included. The Cochrane System Evaluation Criteria was used for literature quality evaluation. Review Manager 5.4 and Stata 17 were used for statistical analysis and publication bias test.@*Results@#A total of 939 children were included in 20 studies, including 470 in the experimental group and 469 in the control group. Meta analysis showed that mini basketball had an extremely significant effect on the improvement of children s upper limb strength ( SMD=0.83, 95%CI=0.53-1.13, Z=5.40, P < 0.01 ). The results of subgroup analysis showed that there was no significant gender difference in the improvement of children s upper limb strength by mini basketball ( P >0.05), mini basketball exercise with an intervention time of less than or equal to 30 minutes ( SMD=0.49, 95%CI=0.29-0.70, Z=4.70, P <0.01) and an exercise cycle of more than 12 weeks ( SMD=1.25, 95%CI=0.54-1.96, Z= 3.45 , P<0.01) can achieve a better intervention effect on the upper limb strength of children. Meta regression results showed that the exercise intervention time was the main source of heterogeneity ( t=2.71, 95%CI= 1.38-22.93, P <0.05). Egger s test showed that the publication bias of the included studies was not statistically significant ( t=0.78, P >0.05).@*Conclusions@#Mini basketball training can improve the upper limb strength of children, but there is no significant gender difference. The upper limb strength is affected by the restriction of intervention time and exercise cycle. Schools can appropriately add small basketball in physical education classes to improve children s upper limb strength.

Development and verification of a detection method for activity of neutralizing antibody in ELISA antibody positive serum of rats immunized with recombinant human interleukin-1 receptor antagonist / 中国生物制品学杂志

@#Objective To develop and verify a method for detecting the activity of neutralizing antibodies in ELISA antibody positive serum of rats immunized with recombinant human interleukin-1 receptor antagonist(rhIL-1Ra). Methods The SD rats were subcutaneously immunized with 3,20 and 100 mg/kg rhIL-1Ra injection respectively,10 rats in each group,half male and half female,twice a day at an interval of at least 4 h between each dose for 13 consecutive weeks. The blood samples were collected from the jugular vein of rats during the administration period and the recovery period. The serum samples were isolated and detected for the antibody titers by ELISA,and the samples positive for rhIL-1Ra antibody were purified by Protein A chromatographic column. Based on,D10G4·1 cells biological activity assay,a method for the detection of neutralizing antibody activity was developed and verified for the specificity,sensitivity and precision. The neutralizing antibody activity of rhIL-1Ra antibody positive serum determined by ELISA was detected by using the developed method.Results With the increase of doses,the serum antibody titers of rats in various dose groups gradually increased,and there were still antibodies in the recovery period,and the titer was still high. Rabbit anti-rhIL-1Ra monoclonal antibody showed obvious neutralizing effect on rIL-1Ra,while rabbit anti-rIFN-2b monoclonal antibody had no dose-effect relationship with rIL-1Ra. The sensitivity of the method was 171. 93 μg/mL;The CVs of precision verification were not more than 20%. The positive antibody sera detected by ELISA all had neutralizing effect on rhIL-1Ra injection,which was consistent with the results detected by ELISA. Conclusion The method developed in this study has good specificity and high sensitivity in the detection of serum neutralizing antibody activity in rats immunized with rhIL-1Ra,which can be used to detect the serum neutralizing antibody activity of animals with rhIL-1Ra repeated administration.

Study on the antifungal activity and mechanism of Huangqin decoction against Trichophyton mentagrophytes / 中国药房

OBJECTIVE To study the antifungal activity of Huangqin decoction （HQD） against Trichophyton mentagrophytes and explore its mechanism. METHODS Minimal inhibitory concentration （MIC）， minimal fungicidal concentration （MFC）， mycelial length， spore germination rate， biomass and mycelium ultrastructure observation were performed to evaluate the antifungal activity of HQD against T. mentagrophytes. The effects of HQD on the cell wall of T. mentagrophytes were detected through sorbitol protection experiment. By measuring the content of ergosterol and the activities of squalene epoxide （SE） and lanosterol 14α-demethylase （CYP51）， the activity of HQD on the cell membrane of T. mentagrophytes was investigated. The effects of HQD on T. mentagrophytes mitochondria were investigated by determining the activities of malate dehydrogenase （MDH）， succinate dehydrogenase （SDH）， and ATPases （including sodium potassium ATPase， calcium magnesium ATPase， and total ATPase）. RESULTS HQD exhibited significant antifungal activity against T. mentagrophytes with MIC of 3.13 mg/mL and MFC of 25 mg/mL. After intervention with HQD， the mycelial length of T. mentagrophytes was significantly shortened （P＜0.05）； spore germination rate， biomass， the content of ergosterol in the cell membrane， the activities of SE and CYP51 in the cell membrane and MDH， SDH and ATPase in mitochondria were all decreased significantly （P＜0.05）； cell structure had been ；damaged to a certain extent， but the integrity of the cell wall had not been affected. CONCLUSIONS HQD shows significant antifungal activity against T. mentagrophytes， the mechanism of which may be associated with reducing the 0791- content of ergosterol in the cell membrane and the activities of SE， CYP51， and mitochondria-related enzymes.

Biological Activities of Sesquiterpenoids： A Review / 中国实验方剂学杂志

Sesquiterpenoids are natural compounds composed of 15 carbon atoms， which can be divided into sesquiterpene alcohols， ketones， lactones， aldehydes， and carboxylic acids according to oxygen groups. These compounds are widely distributed in nature， and their physiological activities are diverse. For example， many sesquiterpenes with potential anticancer effects have been found for anti-tumor effects， including cytotoxicity， antioxidant， immune regulation， cell proliferation， and so on. In addition， some sesquiterpenoids have good application prospects in antibacterial， anti-inflammatory， and anti-cardiovascular diseases. Malignant tumors， inflammation， bacterial diseases， and cardiovascular diseases are the main diseases that cause human death， and natural products have unique advantages in the treatment of these diseases. Therefore， the development of new drugs that are easy to promote has become a new research hotspot. In this paper， the sesquiterpenes extracted from the natural components of Chinese herbs and plants with anti-tumor， anti-inflammatory， antibacterial， and anti-cardiovascular activities， such as Xanthium， Atractylodes， Convolvulus， Acanthium， Ligularia， Artemisia， Ligularia， Ligularia， Labiaceae Mint， Acanthophyllum， Turmeria， Ginger， and other Chinese herbs and plants， were discussed. The biological activities and related mechanisms of this compound were reviewed， which provided a reference for further research and clinical application of sesquiterpenes.

Development and verification of a rapid detection method for adalimumab biological activity based on U937-NF-κB-Luc cell line / 中国生物制品学杂志

@#Objective To develop and verify a rapid detection method for the biological activity of adalimumab based on U937-NF-κB-Luc cell line. Methods Using U937-NF-κB-Luc cell line as the detection cells,a method for detecting the biological activity of adalimumab was developed based on luciferase luminescence principle. The method was optimized for the concentration of tumor necrosis factor-α(TNF-α)(160 ng/mL as initial concentration,2 times serial dilution,10dilutions),the initial concentration of antibody(2 000 ng/mL,2 times serial dilution,20 dilutions),the dilution multiple of antibody(1. 5,2,3,4 times),the inoculation amount(8 × 103,2 × 104,4 × 104,6 × 104cells/well)and the incubation time(0. 5,1,2,3 h),and verified for the specificity,accuracy,precision and linear range. The relative potency of five batches of adalimumab was detected by using the optimized method and TNF-α neutralization activity method based on L929cells respectively. Results The dose-response curve of adalimumab international standard showed a typical S-type,and the data complied with the four-parameter equation y =(A-D)/[1 +(x/C)B]+ D,R2> 0. 99. The optimum concentration of TNF-α was 5 ng/mL,the initial concentration of antibody was 800 ng/mL,the dilution ratio for adalimumab was 1∶2,the inoculation amount was 2 × 104cells/well,and the induction time was 2 h. Three therapeutic monoclonal antibodies of TNF-α target,such as adalimumab,obtained good dose-response curves,while therapeutic monoclonal antibodies of other non-TNF-α targets did not show this curve. The linear regression equation of the logarithmic value of theoretical potency and the logarithmic value of the corresponding measured potency had a slope of 1. 037,and the relative bias was within the range of ± 12%. The geometric coefficient of variation(GCV)of the relative titer measured value of each sample was less than20%. The theoretical potency ranged from 64% to 156%,showing a good linear relationship with the measured values,and the fitting linear regression equation was y = 1. 037 4 x-0. 023 7,R2= 0. 998 4. There was no significant difference in the relative potency measured results of five batches of adalimumab by the two methods(t = 1. 198,P = 0. 265 1). Conclusion The developed detection method for adalimumab biological activity based on U937-NF-κB-Luc cell line has good specificity,accuracy and precision with short time consumption(3 h),which can be used as a rapid evaluation method for the biological activity of adalimumab.

Synthesis and antibacterial activities of phosphonate derivatives containing aminothiazoloxime fragment / 药学学报

Based on the principle of molecular hybridization, fifteen compounds were designed and synthesized through the combination of aminothiazoloxime and phosphonate fragment. The results showed that these compounds had better inhibitory effects on the tested bacteria. In particular, the activities of compounds Ⅲf and Ⅲi against S. aureus, E. coli, methicillin-resistant S. aureus (MRSA) and fluoroquinolone-resistant E. coli (FREC) were the most significant, the minimal inhibitory concentration (MIC) of Ⅲf was 1, 8, 4, 16 μg·mL-1 respectively, and the MIC of Ⅲi was 4, 4, 16, 8 μg·mL-1 respectively, which were slightly lower than that of the control drug oxacillin, and their anti-E. coli, MRSA and FREC activities were superior to that of the control drug oxacillin. Their activities to S. aureus were close to that of oxacillin, and to E. coli, MRSA and FREC were superior to that of oxacillin, which is worthy of further study.

Synthesis and antibacterial activity evaluation of octapeptin derivatives / 药学学报

Octapeptin has strong antibacterial activity against Gram-negative bacteria such as Escherichia coli, Klebsiella pneumoniae and Acinetobacter baumannii, while it also has activity against some Gram-positive bacteria. This study used natural octapeptin A3 and B3 as lead compounds for structural modification. Twenty-one peptide derivatives (including A3 and B3) containing eight amino acid residues were prepared by solid-phase synthesis, and evaluated for antibacterial activity and renal cytotoxicity. Among them, three compounds 6, 7 and 17 exhibited broad-spectrum antibacterial activity and significantly enhanced the activity for Gram-positive bacteria while maintaining the activity of Gram-negative bacteria. Several compounds improved the activity for Pseudomonas aeruginosa. Compound 7 was active against all test strains and had relatively low renal cytotoxicity. The results provide a basis for the further development of novel polypeptide antibiotics.

A new pyrazine from Hypecoum erectum L / 药学学报

Four pyrazines were isolated from the n-butanol fraction of Hypecoum erectum L. by using various chromatographic methods, including MCI gel, ODS, silica gel and semi-preparative HPLC. The structures of the isolated compounds were identified as hyperectpyrazin A (1), 1′S-(6-methylpyrazin-2-yl)-ethane-1′,2′-diol (2), 2-hydroxymethyl-6-methylpyrazin (3) and pyrazine-2-carboxylic acid (4) by spectroscopy methods (1D NMR, 2D NMR, UV, IR, MS, etc.). The absolute configuration of compound 2 was determined by using the Mo2(OAc)4 induced CD analysis for the first time. Compound 1 was a new compound, compounds 2-4 were isolated from H. erectum for the first time. Compounds 1-4 were evaluated for their inhibition against acetylcholinesterase and nitric oxide generation induced by lipopolysaccharide-RAW264.7 macrophage cells. At a concentration of 50 μmol·L-1, compounds 2 and 4 displayed inhibitory effects on acetylcholinesterase with the inhibition rates of 44.40% and 43.99%, respectively.

An unprecedented pair of Z/E isomeric pyridinium compound from the aqueous extract of Aspongopus chinensis Dallas / 药学学报

A novel pair of Z/E isomeric compounds with unprecedented carbon skeleton were isolated from an aqueous extract of Aspongopus chinensis Dallas by macroporous resin, silica gel, and semi-preparative high performance liquid chromatography (HPLC). Their structures were identified by nuclear magnetic resonance (NMR), Infrared spectroscopy (IR), Mass spectroscopy (MS) and other spectroscopic methods as (Z)-3-(but-1″-en-1″-yl)-1-(2ʹ-hydroxyethyl)-4-propylpyridin-1-ium, namely aspongopyridine A, and (E)-3-(but-1″-en-1″-yl)-1-(2ʹ-hydroxyethyl)-4-propylpyridin-1-ium, namely aspongopyridine B, respectively. Besides, the anti-inflammatory, anti-tumor, acetylcholinesterase inhibition and butyrylcholinesterase inhibition activities of the compounds 1 and 2 were evaluated. The results showed that compounds 1 and 2 have no anti-inflammatory, anti-tumor, and butyrylcholinesterase inhibition activities instead of weak acetylcholinesterase inhibition activity.

Advances in antitumor research of bifunctional small molecule inhibitors targeting heat shock protein 90 / 药学学报

The heat shock protein 90 (Hsp90) protein family is a cluster of highly conserved molecules that play an important role in maintaining cellular homeostasis. Hsp90 and its co-chaperones regulate a variety of pathways and cellular functions, such as cell growth, cell cycle control and apoptosis. Hsp90 is closely associated with the occurrence and development of tumors and other diseases, making it an attractive target for cancer therapeutics. Inhibition of Hsp90 expression can affect multiple oncogenic pathways simultaneously. Most Hsp90 small molecule inhibitors are in clinical trials due to their low efficacy, toxicity or drug resistance, but they have obvious synergistic anti-tumor effect when used with histone deacetylase (HDAC) inhibitors, tubulin inhibitors or topoisomerase II (Topo II) inhibitors. To address this issue, the design of Hsp90 dual-target inhibitors can improve efficacy and reduce drug resistance, making it an effective tumor treatment strategy. In this paper, the domain and biological function of Hsp90 are briefly introduced, and the design, discovery and structure-activity relationship of Hsp90 dual inhibitors are discussed, in order to provide reference for the discovery of novel Hsp90 dual inhibitors and clinical drug research from the perspective of medicinal chemistry.