Protopanaxadiol-type ginsenoside hydrolases and their application in the preparation of ginsenoside Compound K: a review / 生物工程学报

Ginsenoside Compound K (CK) has anti-cancer and anti-inflammatory pharmacological activities. It has not been isolated from natural ginseng and is mainly prepared by deglycosylation of protopanaxadiol. Compared with the traditional physicochemical preparation methods, the preparation of CK by hydrolysis with protopanaxadiol-type (PPD-type) ginsenoside hydrolases has the advantages of high specificity, environmental-friendliness, high efficiency and high stability. In this review, the PPD-type ginsenoside hydrolases were classified into three categories based on the differences in the glycosyl-linked carbon atoms of the hydrolase action. It was found that most of the hydrolases that could prepare CK were PPD-type ginsenoside hydrolase type Ⅲ. In addition, the applications of hydrolases in the preparation of CK were summarized and evaluated to facilitate large-scale preparation of CK and its development in the food and pharmaceutical industries.

Quantification of Panax notoginseng saponins metabolites in rat plasma with in vivo gut microbiota-mediated biotransformation by HPLC-MS/MS / 中国天然药物

Panax notoginseng saponins (PNS) are the major components of Panax notoginseng, with multiple pharmacological activities but poor oral bioavailability. PNS could be metabolized by gut microbiota in vitro, while the exact role of gut microbiota of PNS metabolism in vivo remains poorly understood. In this study, pseudo germ-free rat models were constructed by using broad-spectrum antibiotics to validate the gut microbiota-mediated transformation of PNS in vivo. Moreover, a high performance liquid chromatography-electrospray ionization tandem mass spectrometry (HPLC-ESI-MS/MS) was developed for quantitative analysis of four metabolites of PNS, including ginsenoside F1 (GF1), ginsenoside Rh2 (GRh2), ginsenoside compound K (GCK) and protopanaxatriol (PPT). The results showed that the four metabolites could be detected in the control rat plasma, while they could not be determined in pseudo germ-free rat plasma. The results implied that PNS could not be biotransformed effectively when gut microbiota was disrupted. In conclusion, gut microbiota plays an important role in biotransformation of PNS into metabolites in vivo.

Study on transformation rules of terrestrosin D in course of Tribuli Fructus stir-frying based on simulated processing technology / 中国中药杂志

The contents of terrestrosin D and hecogenin from Tribuli Fructus were determined before and after stir-frying. The results showed that the content of terrestrosin D was decreased significantly,and the content of hecogenin was increased significantly after such processing. In order to verify the inference that terrestrosin D was converted to hecogenin by stir-frying,the quantitative variation rules of terrestrosin D and hecogenin were studied by simulated processing technology,and the simulated processing product of terrestrosin D was qualitatively characterized by ultra performance liquid chromatography/time of flight mass spectrometry( UPLC-TOF/MS) to clarify its transformation process during stir-frying. The results showed that the content of terrestrosin D was decreased significantly at first and then a platform stage appeared with the prolongation of processing time at a certain temperature. Raising the stir-frying temperature could further decrease the content of terrestrosin D and delay the time that the platform stage appeared. When the processing was simulated at higher temperatures( 220 ℃ and 240 ℃),the content of hecogenin was increased gradually with the increase of processing temperature and the prolongation of processing time. In the process of stir-frying,the deglycosylation reaction of terrestrosin D to hecogenin was not completed in one step. The deglycosylation reaction occurred first at the end of the sugar chain,and then other glycosyl units in the sugar chain were sequentially removed from the outside to the inside to finally form the hecogenin. This study provides a basis for further revealing the detoxification mechanism of stir-fried Tribuli Fructus.

Effect of telomerase activation on biological behaviors of neural stem cells in rats with hypoxic-ischemic insults / 中国当代儿科杂志

<p><b>OBJECTIVE</b>To investigate the effect of telomerase activation on biological behaviors of neural stem cells after hypoxic-ischemic insults.</p><p><b>METHODS</b>The neural stem cells passaged in vitro were divided into four groups: control, oxygen-glucose deprivation (OGD), OGD+cycloastragenol (CAG) high concentration (final concentration of 25 μM), and OGD+CAG low concentration (final concentration of 10 μM). The latter three groups were subjected to OGD. Telomerase reverse transcriptase (TERT) expression level was evaluated by Western blot. Telomerase activity was detected by telomerase repeat amplification protocol (TRAP). Cell number and neural sphere diameter were measured under a microscope. The activity of lactate dehydrogenase (LDH) was examined by chemiluminescence. Cell proliferation rate and apoptosis were detected by flow cytometry.</p><p><b>RESULTS</b>After OGD insults, obvious injury of neural stem cells was observed, including less cell number, smaller neural sphere, more dead cells, lower proliferation rate and decreased survival rate. In CAG-treated groups, there were higher TERT expression level and telomerase activity compared with the control group (P<0.05). In comparison with the OGD group, CAG treatment attenuated cell loss (P<0.05) and neural sphere diameter decrease (P<0.05), promoted cell proliferation (P<0.05), and increased cell survival rate (P<0.05). Low and high concentrations of CAG had similar effects on proliferation and survival of neural stem cells (P>0.05). In the normal cultural condition, CAG treatment also enhanced TERT expression (P<0.05) and increased cell numbers (P<0.05) and neural sphere diameter (P<0.05) compared with the control group.</p><p><b>CONCLUSIONS</b>Telomerase activation can promote the proliferation and improve survival of neural stem cells under the state of hypoxic-ischemic insults, suggesting telomerase activators might be potential agents for the therapy of hypoxic-ischemic brain injury.</p>

Intervenção nas situações de crise psíquica: dificuldades e sugestões de uma equipe de atenção pré-hospitalar / Intervention in situations of psychic crisis: challenges and suggestions of a prehospital care staff / Intervención en situaciones de crisis psíquica: problemas y sugerencias de un equipo de atención prehospitalaria

Pesquisa descritiva, qualitativa, que objetivou conhecer como os profissionais de atenção pré-hospitalar percebem as intervenções nas pessoas em crise psíquica. O estudo foi realizado, no estado de Santa Catarina, com quatro equipes das Unidades de Suporte Básico do Serviço de Atendimento Móvel de Urgência, mediante entrevista, no período de abril a junho de 2011. Utilizou-se como método de análise o Discurso do Sujeito Coletivo. Dos resultados emergiram dois temas: Percepção das dificuldades no atendimento à pessoa em crise psíquica e Sugestões na busca por um atendimento mais próximo do desejado à pessoa em crise psíquica. As dificuldades apontadas se relacionam à falta de capacitação e de um local para encaminhamento e sugerem treinamento e sistematização do atendimento. Conclui-se que se faz necessário investir em processo de formação pautado em novas estratégias de cuidado norteadas pelos princípios do SUS e no paradigma psicossocial, além de rediscutir a estratégia de protocolos como sistemas norteadores e não padronizadores.

A qualitative and descriptive research, aimed at knowing how the pre-hospital care professionals perceive the interventions towards people in mental crisis. The study was developed in Santa Catarina with four teams of basic life support units of the Department of Mobile Emergency Care, during April to June 2011. The Collective Subject Discourse was used as the method of analysis. Two themes emerged: Awareness of the difficulties in meeting a person in mental crisis and Suggestions in the search for a closer attention to the person in mental crisis. The difficulties mentioned were related to the lack of training and a local to forward the patients, suggesting a better training and systematization of care. We conclude that it is necessary to invest in the educational process, based on new care strategies guided by the principles of SUS and of the psychosocial paradigm, and revisit the strategy of protocols as guidelines and not as standardizing systems.

Investigación descriptivo-cualitativa, que objetivó conocer como los profesionales de la atención pre-hospitalaria perciben las intervenciones en personas con crisis mental. El estudió fue realizado en Santa Catarina con cuatro equipos de las Unidades de Soporte Vital Básico, mediante entrevista realizada de abril a junio de 2011. El Discurso del Sujeto Colectivo fue utilizado como método de análisis; surgiendo dos temas: Percepción de las dificultades en la atención a la persona en crisis mental y Sugerencias en la búsqueda de una mejor atención a la persona en crisis mental. Las dificultades mencionadas se relacionan con la falta de capacitación y lugar para la atención, sugiriendo un mejor entrenamiento y sistematización de la atención. Se resalta la necesidad de invertir en el proceso de formación basado en nuevas estrategias de atención guiadas por los principios del SUS y el paradigma psicosocial, y revisar la estrategia de protocolos como nortes no estandarizados.

Evaluación Antiinflamatoria in vivo de sapogeninas de residuos de quinua real (Chenopodium quinoa Willd) / In vivo anti-inflammatory evaluation of sapogenins from residues of real quinoa (Chenopodium quinoa Willd)

Bolivia es el primer exportador de quinua (Chenopodium quinoa Willd) a nivel mundial, para su exportación la quinua sufre un proceso de beneficiado que separa el epispermo saponinas tienen una parte apolar o sapogeninas de naturaleza triterpénica, como el ácido oleanólico, al cual se le atribuye muchas propiedades farmacológicas, entre ellas propiedades antiinflamatorias. En el presente trabajo se contribuye al estudio farmacológico de sapogeninas de quinua mediante la evaluación de la actividad antiinflamatoria in vivo del extracto de sapogeninas totales y de las sapogeninas aisladas. Para esto, se realizó un estudio de los residuos de quinua obtenidos por diversas empresas beneficiadoras de quinua determinándose que el año 2010 se generaron 1000 TM de este residuo y que su producción fue incrementándose. A partir de estos residuos, se obtuvo un extracto hidro-alcohólico que presenta un 56% p/p de saponinas, el cual fue sometido a una hidrolisis ácida generando un extracto de sapogeninas totales con un rendimiento de 79 %p/p. A partir de este extracto, se aislaron cuatro compuestos: ácido oleanólico (Tm1), oleanato de metilo (Tm2), hederagenina (Tm3) y ácido fitolaccagénico (Tm4). La evaluación antiinflamatoria del extracto y compuestos aislados, se realizó en dos modelos de experimentación animal: modelo de edema de oreja inducido por aceite de crotón (TPA) y modelo de edema de pata inducido por carregenina. Así, la aplicación de 14 mg/oreja del extracto de sapogeninas inhibió un 68% del edema auricular inducido por TPA, mientras que la aplicación de 1mg/ oreja de los compuestos aislados mostró los siguientes resultados: 30% de inhibición para el ácido oleanólico y 24% para el oleanato de metilo, por lo que puede decir que presento una actividad antiinflamatoria significativa (p <0,05) frente al grupo control; sin embargo la hederagenina y el ácido fitolaccagenico inhibieron solo el 15% y 12 % del edema lo cual no representa una actividad antiinflamatoria significativa frente al grupo control. Por otra parte, en el modelo por vía oral la aplicación 636mg/kg po del extracto de sapogeninas totales dio una inhibición del 55,2% de la inflamación y la aplicación de 100mg/ kg po de los compuestos aislados inhibió un 84,2% (Ácido oleanóico), 84,64%(ácido fitolaccagénico), 57,6% (oleanato de metilo) y 70,3 (hederagenina),por lo que podemos decir que los compuestos aislados y el extracto de sapogeninas totales presentan una inhibición significativa frente al grupo control desde las 3 h hasta las 7 h después de la aplicación de la carragenina. Finalmente, se estableció un método de control químico del extracto de sapogeninas totales, por cromatografía liquida de alta resolución HPLC, a partir del cual se determinó el porcentaje de cada compuesto en el extracto dando los siguientes resultados: Tm1 (20,8%) Tm2 (8%), Tm3 (26%) y Tm4 (24%). Por lo que podemos decir que tanto el extracto de sapogeninas totales como las sapogeninas aisladas presentan una actividad antiinflamatoria significativa en los modelos evaluados, en particular el extracto de sapogeninas totales presenta una mejor actividad en el modelo por vía tópica, mientras que los compuestos aislados presentaron mejor actividad en el modelo por vía oral. (AU)

Revisión química y homeopática de la Calendula officinalis / Chemistry and homeopathic Calendula officinalis Review

La caléndula es una planta originaria de Europa cuyas propiedades curativas seaprovechan desde épocas remotas, por lo que actualmente es cultivada en todoel mundo. Extractos y ungüentos elaborados con este vegetal han mostrado susvirtudes para cicatrizar heridas y atender afecciones de la piel, y este saber empíricoha sido comprobado a través de diversos estudios científicos, como los que serevisan a lo largo del presente artículo. En Homeopatía, su tintura se emplea como antiséptica, analgésica y cicatrizantede la piel y la mucosa bucal, mientras que sus dinamizaciones se prescriben aindividuos nerviosos, irritables, con marcada tendencia a los sobresaltos y muysensibles a los estímulos sensoriales. Además de esto, Caléndula officinalis tienela capacidad de ayudar en el tratamiento de problemas crónicos y agudos relacionadoscon lesiones externas o en diferentes sistemas, como las vías urinarias, lossistemas respiratorio y digestivo, y los órganos reproductivos femeninos.

Calendula is a plant native to Europe whose healing properties are used sinceancient times, so it is now cultivated worldwide. Extracts and ointments made fromthis plant have shown their strengths to heal wounds and treat skin conditions, andthis empirical knowledge has been proven through scientific studies, such as thosereviewed throughout this article. In Homeopathy, the tincture is used as antiseptic, analgesic and healingof the skin and oral mucosa, while their dynamizations are prescribed to irritable,with a marked tendency to shocks and very sensitive to sensory stimuli people.In addition, Calendula officinalis has the ability to help in the treatment of chronicand acute problems related to external injuries or different systems, like urinary,respiratory and digestive systems, and female reproductive organs.

Study on pharmacokinetics of 20 (S) -protopanaxadiol lipid cubic nanoparticles / 中国中药杂志

<p><b>OBJECTIVE</b>To establish a high-performance liquid chromatographic/tandem mass spectrometry (HPLC-MS/MS) method for determining 20(S)-protopanaxadiol (PPD) in rat plasma, in order to analyze pharmacokinetic characteristics of PPD and PPD cubic nanoparticles.</p><p><b>METHOD</b>Sprague-Dawley rats were administered orally with PPD and PPD cubic nanoparticles, respectively. Their blood samples were obtained from fossa orbitalis at regular time points. The mobile phase was 0.05% formic acidac etonitrile-0.05% formic acidac water (95:5). Electrospray ionization (ESI) was adopted for the quadrupole tandem mass spectrum. SCAN mode was used for the quantitative analysis, with m/z 460. 4/425.3 and m/z 622.9/318.3 (Rh2, interior label) as secondary fragment ions. The concentration of PPD in plasma was analyzed. The concentration-time curve was mapped. The data were calculated by DAS program.</p><p><b>RESULT</b>The linearity of the PPD plasma concentration determination method ranged between 10-1 407 microg x L(-1), with the limit of quantification of 2.5 microg x L(-1). Both of the inter-day and intra-day precisions (RSD) were less than 13.25%, and the accuracy (relative error) was between +/- 8.50%.</p><p><b>CONCLUSION</b>The method was so highly specific and sensitive with less plasma that it is suitable for pharmacokinetic studies. The prepared 20(S)-protopanaxadiol lipid cubic nanoparticles can enhance its absorption in vivo. Its relative bioavailability is 166% of the raw material.</p>

Bioactivity of five components of Chinese herbal formula Jiangzhi granules against hepatocellular steatosis / 中西医结合学报

<p><b>OBJECTIVE</b>This study aims to evaluate the bioactivity of five components of the traditional Chinese medicine complex prescription Jiangzhi granules against hepatocellular steatosis.</p><p><b>METHODS</b>The five major components, including protopanaxadiol, tanshinone IIA, emodin, chlorogenic acid, and nuciferine, were extracted from Jiangzhi granules. Their cytotoxicity was assessed to determine the safe dose of each component for HepG2 cells. HepG2 cellular steatosis was induced using 1 mmol/L of free fatty acids (FFAs) for 24 h, and then treated with each component at high, intermediate, and low doses (500, 50, and 5 μmol/L), respectively for another 24 h. The effects on HepG2 steatosis were observed directly under optical phase microscopy, or through oil red O staining and Nile red assays. In addition, the levels of reactive oxygen species (ROS) in the steatotic HepG2 cells with and without high-dose protopanaxadiol treatment were measured using fluorescent dye 2',7'-dichlorodihydrofluorescein diacetate staining.</p><p><b>RESULTS</b>No obvious cytotoxicity was observed in the HepG2 cells incubated with each of the five components at up to 500 μmol/L. At 24 h after incubation with FFAs, the HepG2 cells swelled and many lipid droplets accumulated. The lipid content was attenuated after 24 h of incubation with protopanaxadiol, tanshinone IIA, and emodin at 500 or 50 μmol/L (P < 0.05), especially with 500 μmol/L protopanaxadiol (P < 0.01). In addition, the ROS level was elevated in steatotic cells, but decreased after intervention with 500 μmol/L protopanaxadiol (P < 0.05).</p><p><b>CONCLUSION</b>Protopanaxadiol, tanshinone IIA, and emodin alleviate hepatocellular steatosis in a dose-dependent manner, and oxidative stress regulation may partially contribute to the effects of protopanaxadiol.</p>

Effects of administration of IH901, a ginsenoside intestinal metabolite, on muscular and pulmonary antioxidant functions after eccentric exercise

This study was conducted to investigate whether administration of IH901, a ginseng intestinal metabolite, ameliorates exercise-induced oxidative stress while preserving antioxidant defense capability in rat skeletal muscles and lung. Eight adult male Sprague-Dawley rats per group were randomly assigned to the resting control, exercise control, resting with IH901 (25, 50, and 100 mg/kg) consumption (R/IH901), or exercise with IH901 (25, 50, and 100 mg/kg) consumption (E/IH901) group. The trained groups ran 35 min 2 days/week for 8 weeks. To analyze the IH901-training interaction, serum biochemical analysis, lipid peroxidation, citrate synthase, protein oxidation, antioxidant and superoxide dismutase in skeletal muscles and lung tissue were measured. Compared to the exercise control group, animals that consumed IH901 had significantly increased exercise endurance times (p < 0.05) and decreased plasma creatine kinase and lactate dehydrogenase levels (p < 0.05), while those in the E/IH901 groups had increased citrate synthase and anti-oxidant enzymes and decreased lipid peroxidation and protein oxidation (p < 0.05). In conclusion, IH901 consumption in aging rats after eccentric exercise has beneficial effects on anti-inflammatory and anti-oxidant activities through down-regulation of pro-inflammatory mediators, lipid peroxidation, and protein oxidation and up-regulation of anti-oxidant enzymes.

Screening of pregnane X receptor activation from ginsenosides / 药学学报

In order to study effects of ginseng on the metabolism of drug belong to CYP3A4 substrate, screening of pregnane X receptor activation from ginsenosides was performed by reporter assay. Based on PXR-CYP3A stable translation cell lines, 13 ginsenosides were screened for pregnane X receptor activation by reporter assays, and RIF as the positive control. The effect of ginsenosides Rg1 onCYP3A4 mRNA expression was also investigated by RT-PCR. The PXR-CYP3A stable translation cell lines had good response to RIF, and the EC50 is 2.51 micro mol x L(-1). When the condition of final concentration was 10 micromol x L(-1), ginsenoside F2 and protopanaxatriol had moderate inductive effects on PXR. Panaxotriol, Rg2, pseudoginsenoside F11, Rg1, ginsenoside and Rb3 had inhibitory effects on PXR. Ginsenoside Rf1, Rg3, Rh2 and protopanaxdiol had no obvious effects on PXR. Rg1 down-regulated CYP3A4 mRNA expression in a concentration-dependent manner. Activation of pregnane X receptor by ginsenosides may influence the metabolism of drug belong to CYP3A4 substrate, and cause ginseng-drug interactions.

Polybasic research on the biopharmaceutical characteristics of 20 (S)-protopanaxadiol / 药学学报

In this study, the biopharmaceutical properties of 20 (S)-protopanaxadiol (PPD) were studied. Firstly, the equilibrium solubility and apparent oil/water partition coefficient of PPD were used to predict the absorption in vivo. Meanwhile the membrane permeability and absorption window were studied by Caco-2 cell model and single-pass intestinal perfusion model. Furthermore, the bioavailability and metabolism were combined to study the absorption properties and metabolic properties in vivo. All of them were used to provide theoretical and practical foundation for designing PPD preparation. The results showed that PPD is poorly water-soluble, and the equilibrium solubility in water is only 35.24 mg x L(-1). The oil-water partition coefficient is 46.21 (logP = 1.66). By Caco-2 cell model, the results showed PPD uptake in general, and it also has efflux. By in situ intestinal perfusion model, the results showed that the absorption of PPD in the intestine is good, and the effective permeability coefficient were duodenum > jejunum > ileum > colon. The oral bioavailability of PPD was 29.39%. It was not well. Metabolic studies showed PPD in vivo presented a wide spread metabolism. So the main factors that restricted oral bioavailability of PPD were the poor solubility and first-pass effect.

Chemical constituents from roots and rhizomes of Panax ginseng cultivated in Jilin province / 中国中药杂志

The chemical constituents of the roots and rhizomes of Panax ginseng were systematically investigated by various column chromatographic methods including Amberlite XAD-4 macroporous adsorptive resins and silica gel as well as high-performance liquid chromatography, and their chemical structures were identified by physico-chemical properties and spectral analyses. Twenty-eight compounds were isolated from the 70% ethanolic-aqueous extract and identified as koryoginsenoside R1 (1), ginsenoside Rg1 (2), ginsenoside Rf (3), notoginsenoside R2 (4), ginsenoside Rg2 (5), notoginsenoside Fe (6), ginsenjilinol (7), ginsenoside Re5 (8), noto-ginsenoside N (9), notoginsenoside R1 (10), ginsenoside Re2 (11), ginsenoside Re1 (12), ginsenoside Re (13), ginsenoside Rs2 (14), ginsenoside Ro methyl ester (15), ginsenoside Rd (16), ginsenoside Re3 (17), ginsenoside Re4 (18), 20-gluco-ginsenoside Rf (19), ginsenoside Ro (20), ginsenoside Rc (21), quinquenoside-R1 (22), ginsenoside Ra2 (23), ginsenoside Rb1 (24), ginsenoside Ra1 (25), ginsenoside Ra3 (26), ginsenoside Rb2 (27), and notoginsenoside R4 (28). All isolated compounds are 20 (S) -protopanaxadiol or protopanaxatriol type triterpenoid saponins. Compound 1 was isolated from the roots and rhizomes of P. ginseng cultivated in Jilin province for the first time and compound 6 was isolated from the roots and rhizomes of P. ginseng for the first time. The 1H-NMR data of compounds 6, 14 and 19 were assigned for the first time.

Inhibitory Effects of Ginsenoside Metabolites, Compound K and Protopanaxatriol, on GABAC Receptor-Mediated Ion Currents

Ginsenosides, one of the active ingredients of Panax ginseng, show various pharmacological and physiological effects, and they are converted into compound K (CK) or protopanaxatriol (M4) by intestinal microorganisms. CK is a metabolite derived from protopanaxadiol (PD) ginsenosides, whereas M4 is a metabolite derived from protopanaxatriol (PT) ginsenosides. The gamma-aminobutyric acid receptorC (GABAC) is primarily expressed in retinal bipolar cells and several regions of the brain. However, little is known of the effects of ginsenoside metabolites on GABAC receptor channel activity. In the present study, we examined the effects of CK and M4 on the activity of human recombinant GABAC receptor (rho1) channels expressed in Xenopus oocytes by using a 2-electrode voltage clamp technique. In oocytes expressing GABAC receptor cRNA, we found that CK or M4 alone had no effect in oocytes. However, co-application of either CK or M4 with GABA inhibited the GABA-induced inward peak current (IGABA). Interestingly, pre-application of M4 inhibited IGABA more potently than CK in a dose-dependent and reversible manner. The half-inhibitory concentration (IC50) values of CK and M4 were 52.1+/-2.3 and 45.7+/-3.9 microM, respectively. Inhibition of IGABA by CK and M4 was voltage-independent and non-competitive. This study implies that ginsenoside metabolites may regulate GABAC receptor channel activity in the brain, including in the eyes.

Biotransformation in vivo/vitro and bioactive properties of rare ginsenoside IH901 / 生物工程学报

Recent metabolomics research revealed a new ginseng ginsenoside IH901 that is synthesized by intestinal microbial transformation in oral administration of ginseng. IH901 shows various biological activities, including anti-tumor, anti-inflammatory, anti-diabetic, and anti-aging. In recent years, great effort has been made to prepare IH901 by microbial and enzymatic transformation in a large scale. In this paper, we reviewed the biotransformation pathways both in vivo and in vitro and bioactive properties of rare ginsenoside IH901.

Effects of Protopanaxatriol-Ginsenoside Metabolites on Rat N-Methyl-D-Aspartic Acid Receptor-Mediated Ion Currents

Ginsenosides are low molecular weight glycosides found in ginseng that exhibit neuroprotective effects through inhibition of N-methyl-D-aspartic acid (NMDA) receptor channel activity. Ginsenosides, like other natural compounds, are metabolized by gastric juices and intestinal microorganisms to produce ginsenoside metabolites. However, little is known about how ginsenoside metabolites regulate NMDA receptor channel activity. In the present study, we investigated the effects of ginsenoside metabolites, such as compound K (CK), protopanaxadiol (PPD), and protopanaxatriol (PPT), on oocytes that heterologously express the rat NMDA receptor. NMDA receptor-mediated ion current (INMDA) was measured using the 2-electrode voltage clamp technique. In oocytes injected with cRNAs encoding NMDA receptor subunits, PPT, but not CK or PPD, reversibly inhibited INMDA in a concentration-dependent manner. The IC50 for PPT on INMDA was 48.1+/-4.6 microM, was non-competitive with NMDA, and was independent of the membrane holding potential. These results demonstrate the possibility that PPT interacts with the NMDA receptor, although not at the NMDA binding site, and that the inhibitory effects of PPT on INMDA could be related to ginseng-mediated neuroprotection.

EVALUACIÓN DEL EFECTO SANITIZANTE DE UN EXTRACTO BIODEGRADABLE OBTENIDO DE LA ESPECIE Solanum marginatum, DE USO ETNOBOTÁNICO EN BOYACÁ / EVALUATION OF THE SANITIZER EFFECT OF A BIODEGRADABLE EXTRACT OF ETHNOBOTANICAL USE IN BOYACÁ, OBTAINED FROM THE Solanum marginatum SPECIES

Las plantas del género Solanum, dentro del que se encuentra el "lulo de perro" (Solanum marginatum), especie considerada una maleza, contienen saponinas, las cuales tienen propiedades de emulsionar la grasa, similares al jabón. Esta característica fue aprovechada para evaluar el poder sanitizante del extracto alcohólico del fruto, en calidad de limpiador biodegradable, de gran utilidad en la industria. El potencial sanitizante del limpiador preparado se evaluó según el procedimiento descrito por Carrascal, Páez y Burbano (1998), y se encontró como condiciones óptimas de efectividad antimicrobial: una concentración del 10% y un tiempo de contacto de 6 minutos sobre microorganismos bacilos gram negativos, que presentan un máximo de inhibición de 99,58%. Al comparar la efectividad del producto obtenido contra la de dos conocidos sanitizantes comerciales (Mat-98® y Germigel®), se encontró una respuesta similar. Por hidrólisis del crudo de saponina se liberaron las sapogeninas presentes, los cristales obtenidos se analizaron por espectroscopía infrarroja y se les determinó el punto de fusión, coincidiendo los resultados con la Hecogenina.

Plants of the genus Solanum, within which the "Lulo perro" (Solanum marginatum) is found and is considered as a weed species, contain saponins which have fat emulsifying properties similar to soap. This feature was used to evaluate the sanitizing power of the alcoholic extract of the fruit as a biodegradable cleaner which is very useful for industrial purposes. The sanitizing potential of the cleaner preparation was assessed using the procedure described by Carrascal, Páez y Burbano (1998), and it was found to have optimum antimicrobial effectiveness conditions: a 10% concentration and a 6 minute contact time over gram negative bacilli microorganisms which represent a maximum inhibition of 99 58%. When comparing the effectiveness of the product against two well-known commercial sanitizers. (Mat-98® and Germigel®), a similar response was found. Using crude hydrolysis of saponin, present sapogenins were released, the crystals obtained were analyzed using infrared spectroscopy, and melting point was determined. These results coincided with the Hecogenin.

Pharmacokinetics of ginsenosides Rg1 and its metabolites in rats / 药学学报

To study the pharmacokinetics of ginsenosides Rg1 and its metabolites after iv and oral administration in Wistar rats, the LC-MS/MS method was selected to determine ginsenosides Rg1 and its metabolites in plasma and their pharmacokinetic parameters were calculated. After oral administration of ginsenosides Rg1 to rats, ginsenosides Rg1, Rh1, F1 and protopanaxatriol (Ppt) could be detected in plasma. Their Tmax were 0.92, 3.64, 5.17, and 7.30 h, respectively; MRT were 2.68, 5.06, 6.65, and 5.33 h, respectively; AUC(o-t), were 2 363.5, 4 185.5, 3 774.3, and 396.2 ng x mL(-1) x h, respectively. After iv administration of ginsenosides Rg1 to rats, ginsenosides Rg1, Rh1 and FI could be detected in plasma. Their T1/2betaS were 3.12, 5.87, and 6.87 h, respectively; MRTs were 1.92, 5.99, and 7.13 h, respectively; AUCo-tS were 1 454.7, 597.5, and 805.6 ng x mL(-1) x h, respectively. So, it can be concluded that after oral administration, the amounts of metabolites were higher than the prototype in vivo, and the distribution and elimination of the metabolites were relatively slow. After iv administration, the amount of prototype were higher than that of the metabolites in vivo, and the distribution and elimination of the metabolites were relatively slow.

Preparation and study in vitro of 20 (S)-protopanaxadiol pharmacosomes / 中国中药杂志

To prepare and evaluate in vitro the 20 (S) -Protopanaxadiol (Ppd) pharmacosome. The Ppd pharmacosome was successfully prepared by thin film-dispersion and its stability in vitro was studied. The particle size of pharmacosome was evaluated by dynamic scattering (DLS) and the encapsulation efficiency was determined by using centrifugal ultra-filtration. The encapsulation efficiency of Ppd pharmacosome was (80.84 +/- 0.53)% with the diameter of 100. 1 nm; While the encapsulation efficiency of Ppd pharmacosome that added Brij 78 added was (72.76 +/- 0.63)% with the diameter of 117. 3 nm. In addition, the effect of some factors on the encapsulation efficiency and the particles size, such as temperature, alcohol, pH and artificial gastrointestinal fluids, were investigated respectively. The selected formulation and technology are simple and practical to prepare Ppd pharmacosome and preparation properties are more stable.

Inhibitory effect of ginseng saponin IH901 on proliferation and metastasis of ECV304 cell line and its molecular mechanism / 药学学报

This study aims to investigate the inhibitory effect on proliferation and metastasis of 20-O-(beta-D-glucopyranosyl)-20(S)-protopanaxadiol (IH901) on ECV304 cell line. MTT assay was used to examine the effect of cell proliferation inhibition and the adhesive ability of ECV304 cells to artificial basement membrane. Morphology of cell apoptosis was observed with phase contrast microscope. Apoptosis rate and cell cycle were detected by flow cytometry (FCM). Cell migration was measured by wound healing assay. ELISA kit was used to detect VEGF and bFGF. Caspases were detected by Western blotting. Results indicated that ginseng saponin IH901 can downregulate the expression of growth promoting protein VEGF and bFGF, and upregulate pro apoptosis protein cleaved caspase-9 and cleaved caspase-3. The increase in the apoptotic sub-G1 fraction is in a dose-dependent manner, and cell cycle arrests in the G0/G1 phase was detected by FCM. Morphological examination of IH901-treated samples showed cells with chromatin condensation, cell shrinkage, and all typical characteristics of apoptotic cells. Therefore, IH901 dramatically suppresses cell proliferation and adhesion and migration of ECV304 cell line.