RESUMEN
Metabolic oligosaccharide engineering (MOE) is a classical chemical approach to perturb, profile and perceive glycans in physiological systems, but probes upon bioorthogonal reaction require accessibility and the background signal readout makes it challenging to achieve glycan quantification. Here we develop SeMOE, a selenium-based metabolic oligosaccharide engineering strategy that concisely combines elemental analysis and MOE,enabling the mass spectrometric imaging of glycome. We also demonstrate that the new-to-nature SeMOE probes allow for detection, quantitative measurement and visualization of glycans in diverse biological contexts. We also show that chemical reporters on conventional MOE can be integrated into a bifunctional SeMOE probe to provide multimodality signal readouts. SeMOE thus provides a convenient and simplified method to explore the glyco-world.
Asunto(s)
Selenio , Polisacáridos/metabolismo , Oligosacáridos/metabolismo , Ingeniería Metabólica , Espectrometría de MasasRESUMEN
In this study, the crude polysaccharides was extracted from Shengfupian and purified by Sevag deproteinization. Then, the purified neutral polysaccharide fragment was obtained by the DEAE-52 cellulose chromatography column and Sephadex G-100 co-lumn. The structure of polysaccharides was characterized by ultraviolet spectroscopy, infrared spectroscopy, ion chromatography, and gel permeation chromatography. To investigate the anti-inflammatory activity of Shengfupian polysaccharides, LPS was used to induce inflammation in RAW264.7 cells. The expression of the CD86 antibody on surface of M1 cells, the function of macrophages, and the content of NO and IL-6 in the supernatant were examined. An immunodepression model of H22 tumor-bearing mice was established, and the immunomodulatory activity of Shengfupian polysaccharides was evaluated based on the tumor inhibition rate, immune organ index and function, and serum cytokine levels. Research indicated that Shengfupian polysaccharides(80 251 Da) was composed of arabinose, galactose, glucose, and fructose with molar ratio of 0.004â¶0.018â¶0.913â¶0.065. It was smooth and lumpy under the scanning electron microscope. In the concentration range of 25-200 µg·mL~(-1), Shengfupian polysaccharides exhibited little or no toxicity to RAW264.7 cells and could inhibit the polarization of cells to the M1 type and reduce the content of NO and IL-6 in the cell supernatant. It could suppress the phagocytosis of cells at the concentration of 25 µg·mL~(-1), while enhancing the phagocytosis of RAW264.7 cells within the concentration range of 100-200 µg·mL~(-1). The 200 mg·kg~(-1) Shengfupian polysaccharides could alleviate the spleen injury caused by cyclophosphamide, increase the levels of IL-1ß and IL-6, and decrease the level of TNF-α in the serum of mice. In conclusion, Shengfupian polysaccharides has anti-inflammatory effect and weak immunomodulatory effect, which may the material basis of Aconm Lateralis Radix Praeparaia for dispelling cold and relieving pain.
Asunto(s)
Citocinas , Interleucina-6 , Animales , Ratones , Interleucina-6/genética , Citocinas/metabolismo , Polisacáridos/farmacología , Polisacáridos/química , Células RAW 264.7 , Antiinflamatorios/farmacología , Antiinflamatorios/química , Espectrofotometría InfrarrojaRESUMEN
Polysaccharides from Bergenia emeiensis (PBE) showed a robust antioxidant ability on scavenging free radicals in vitro. However, the further antioxidant potential in cell level and in vivo was still unknown. Therefore, in this present study, the protective effect of PBE on human cervical carcinoma cell (Hela) cells and Caenorhabditis elegans against oxidative stress was evaluated. The results showed PBE could reduce the reactive oxygen species (ROS) level in Hela cells and promote the mitochondrial membrane potential. Then, the cell apoptosis was reduced. Moreover, PBE could enhance the survival of C. elegans under thermal stress to 13.44%, and significantly reduce the ROS level, which was connected with the overexpression of sod-3 and the increased nuclear localization of daf-16 transcription factor. Therefore, PBE exhibited a strong antioxidant capacity in the cellular level and for a whole organism. Thus, polysaccharides from B. emeiensis have natural potential to be a safe antioxidant.
Asunto(s)
Antioxidantes/farmacología , Extractos Vegetales/farmacología , Polisacáridos/farmacología , Saxifragaceae/química , Animales , Antioxidantes/química , Apoptosis/efectos de los fármacos , Caenorhabditis elegans/efectos de los fármacos , Caenorhabditis elegans/metabolismo , Supervivencia Celular/efectos de los fármacos , Regulación de la Expresión Génica , Estrés Oxidativo/efectos de los fármacos , Extractos Vegetales/química , Extractos Vegetales/aislamiento & purificación , Polisacáridos/química , Polisacáridos/aislamiento & purificación , Especies Reactivas de Oxígeno/metabolismo , Factores de Transcripción/metabolismoRESUMEN
Bergeniaemeiensis is a traditional herb in Chinese folk medicine. Most related studies are focused on the bioactivity of bergenin, neglecting other bioactive compounds. In our previous work, polysaccharides were identified in B. emeiensis rhizome. To evaluate the extraction process and the antioxidant ability of these polysaccharides, a response surface method and antioxidant assays were applied. The results showed that the yield of polysaccharides was highly affected by extraction time, followed by temperature and solvent-to-sample ratio. Under the optimal conditions (43 °C, 30 min and 21 mL/g), the yield was 158.34 ± 0.98 mg/g. After removing other impurities, the purity of the polysaccharides from B. emeiensis (PBE) was 95.97 ± 0.92%. The infrared spectrum showed that PBE had a typical polysaccharide structure. Further investigations exhibited the PBE could scavenge well DPPH and ABTS free radicals and chelate Fe2+, showing an excellent antioxidant capacity. In addition, PBE also enhanced the cell viability of HEK 239T and Hep G2 cells under acrylamide-exposure conditions, exhibiting great protection against the damage induced by acrylamide. Therefore, PBE can be considered a potential natural antioxidant candidate for use in the pharmaceutical industry as a health product.
RESUMEN
Rosa banksiae Ait. (R. banksiae) is a traditional Chinese folk medicine and an ornamental plant. Most previous studies have focused on cultivation and utilization while there are few research papers on the pharmacological activity of R. banksiae. This study aimed to get a better understanding of R. banksiae by extracting polyphenols with fractionated extraction technology. The results showed that ethyl acetate phase (EAP) contained the most polyphenols, while water phase (WP) had the least. HPLC analysis indicated that rutin and luteolin-4'-O-glucoside existed in the EAP and butanol phase (BP), but quercetin was only detected in the EAP. Six phenolic compositions were not detected in WB. The antioxidant and anti-tumor abilities of the EAP and BP were excellent. The results revealed that R. banksiae possessed a great antioxidant capacity and was rich in polyphenols, thus indicating R. banksiae was suitable for being a natural antioxidant and an abundant source of polyphenols.
Asunto(s)
Antineoplásicos/farmacología , Antioxidantes/análisis , Antioxidantes/farmacología , Flores/química , Extractos Vegetales/farmacología , Polifenoles/análisis , Rosa/química , Acetatos/química , Butanoles/química , Cromatografía Líquida de Alta Presión , Glucósidos/análisis , Células HeLa , Humanos , Luteolina/análisis , Fenoles/análisis , Extractos Vegetales/química , Quercetina/análisis , Rutina/análisis , Solventes/química , Agua/químicaRESUMEN
In this study, an efficient strategy developed by integrating UPLC-Q/TOF-MS, network pharmacology, and molecular simulation, was proposed and applied for rapidly screening bioactive candidates from ginger. A UPLC-Q/TOF MS-guided isolation targeting non-volatile pungent compounds resulted in the isolation and identification of 19 compounds in the rhizome of Zingiber officinale, including six new compounds (1-6). Based on target prediction and Gene Ontology (GO), the primary biological function of compounds was predicted to be associated with cancer and the key target was VEGFR2 (vascular endothelial growth factor receptor 2). Moreover, cytotoxic activity assays demonstrated that the isolated compounds had potential anti-proliferative effects on MDA-MB-231, A549 and HCT116 cells. In particular, compounds 7 and 8 exhibited the highest cytotoxicity against HCT116 compared with the other cell lines, with IC50 values ranging from 4.70 to 7.40 µM. In addition, VEGFR2 inhibition of compounds 7 and 8 was validated based on enzyme activity assays and their interaction mechanisms were illuminated through molecular simulations. These experimental data are consistent with the calculated results, indicating the veracity of the proposed method. In conclusion, the integrated strategy is a quick and efficient way to explore bioactive compounds as well as research the possible targets, providing us with a good possibility of screening new lead compounds from natural sources.
Asunto(s)
Antineoplásicos Fitogénicos/farmacología , Extractos Vegetales/farmacología , Zingiber officinale/química , Antineoplásicos Fitogénicos/química , Sitios de Unión , Línea Celular Tumoral , Proliferación Celular , Fraccionamiento Químico , Regulación de la Expresión Génica/efectos de los fármacos , Humanos , Estructura Molecular , Extractos Vegetales/química , Receptor 2 de Factores de Crecimiento Endotelial Vascular/genética , Receptor 2 de Factores de Crecimiento Endotelial Vascular/metabolismoRESUMEN
Ginger, a popular functional food, has been widely used throughout the world for centuries. However, its metabolic behaviors remain unclear, which entails an obstacle to further understanding of its functional components. In this study, the metabolic profiles of ginger in rats were systemically investigated by UPLC-Q/TOF-MS. The results included the characterization of 92 components of ginger based on the summarized fragmentation patterns and self-building chemical database. Furthermore, four representative compounds were selected to explore the typical metabolic pathways of ginger. Consequently, 141 ginger-related xenobiotics were characterized, following the metabolic spots of the pungent phytochemicals were summarized. These findings indicated that the in vivo effective components of ginger were mainly derived from [6]-gingerol and [6]-shogaol. Meanwhile, hydrogenation, demethylation, glucuronidation, sulfation, and thiolation were their major metabolic reactions. These results expand our knowledge about the metabolism of ginger, which will be important for discovering its functional components and the further mechanism research.
Asunto(s)
Agentes Aversivos/química , Alimentos Funcionales/análisis , Extractos Vegetales/química , Zingiber officinale/química , Animales , Agentes Aversivos/metabolismo , Catecoles/análisis , Catecoles/metabolismo , Cromatografía Líquida de Alta Presión , Alcoholes Grasos/análisis , Alcoholes Grasos/metabolismo , Zingiber officinale/metabolismo , Masculino , Metaboloma , Extractos Vegetales/metabolismo , Ratas , Ratas Sprague-Dawley , Espectrometría de Masas en Tándem , Xenobióticos/química , Xenobióticos/metabolismoRESUMEN
The Dioscorea hypoglauca rhizome and D. spongiosa rhizome in "China Pharmacopoeia" are often used as Bixie in clinically, with the function of removing dampness, clearing away turbidness and dispelling wind to remove pain, and has been widely used in stranguria marked by chyluria, joint stiffness and rheumatic arthralgia. It has obvious curative effect and broad application prospect. However, in recent years the progress of research is slow for its miscellaneous sources, chaotic varieties and lack of relevant quality assessment. The previous research on Bixie is mainly reflected in the chemical compositions, mainly including steroids, diarylheptanoids and lignans and so on. Among them, steroidal saponins are the main components and the main effective substances for their pharmacological activities. Recent studies have shown that Bixie and its main components have significant effects in anti-trioxypurine, anti-inflammation, analgesia and anti-osteoporosis, and have made great progress, providing an experimental basis for the research and development of clinical drugs. But the specific substance and specific mechanism of its pharmacological action are not clear, and need further exploration. By consulting the relevant literature at home and abroad, the author has summarized the chemical constituents, quality evaluation, pharmacological action of Bixie, hoping to provide a reference for further research, development and utilization of Bixie.
Asunto(s)
Dioscorea/química , Medicamentos Herbarios Chinos/farmacología , Rizoma/química , Analgésicos/farmacología , Antiinflamatorios/farmacología , Conservadores de la Densidad Ósea/farmacología , China , Dioscorea/clasificación , Lignanos/farmacología , Fitosteroles/farmacología , Saponinas/farmacologíaRESUMEN
A photo-medical capsule that emits blue light for Helicobacter pylori treatment was described in this paper. The system consists of modules for pH sensing and measuring, light-emitting diode driver circuit, radio communication and microcontroller, and power management. The system can differentiate locations by monitoring the pH values of the gastrointestinal tract, and turn on and off the blue light according to the preset range of pH values. Our experimental tests show that the capsule can operate in the effective light therapy mode for more than 32 minutes and the wireless communication module can reliably transmit the measured pH value to a receiver located outside the body.
Asunto(s)
Infecciones por Helicobacter/terapia , Helicobacter pylori/efectos de la radiación , Luz , Fototerapia/métodos , Electrodos , Diseño de Equipo , Tracto Gastrointestinal/fisiología , Humanos , Concentración de Iones de Hidrógeno , Fototerapia/instrumentación , Tecnología InalámbricaRESUMEN
Aquatic ecological carrying capacity is an effective method for analyzing sustainable development in regional water management. In this paper, an integrated approach is employed for assessing the aquatic ecological carrying capacity of Wujin District in the Tai Lake Basin, China. An indicator system is established considering social and economic development as well as ecological resilience perspectives. While calculating the ecological index, the normalized difference vegetation index (NDVI) is extracted from Moderate Resolution Imaging Spectroradiometer (MODIS) time-series images, followed by spatial and temporal analysis of vegetation cover. Finally, multi-index assessment of aquatic ecological carrying capacity is carried out for the period 2000 to 2008, including both static and dynamic variables. The results reveal that aquatic ecological carrying capacity presents a slight upward trend in the past decade and the intensity of human activities still exceeded the aquatic ecological carrying capacity in 2008. In terms of human activities, population has decreased, GDP has quadrupled, and fertilizer application and industrial wastewater discharge have declined greatly in the past decade. The indicators representing aquatic ecosystem conditions have the lowest scores, which are primarily attributed to the water eutrophication problem. Yet the terrestrial ecosystem is assessed to be in better condition since topographic backgrounds and landscape diversity are at higher levels. Based on the work carried out, it is suggested that pollutant emission be controlled to improve water quality and agricultural development around Ge Lake (the largest lake in Wujin District) be reduced.