RESUMEN
Chemical constituents from the ethanol extract of Picrorhiza scrophulariiflora were isolated and purified by column chromatography. Their structures were identified by HR-MS, 1D and 2D-NMR, and their cytotoxicity was assessed by CCK-8 assay. Four compounds were isolated and identified as follows: 2ß-D-glucosyloxy-3ß,16α,20ß-trihydroxy-9-methyl-19-norlanosterol-5,25-diene-22-one(1), 2ß-D-glucosyloxy-3ß,16α,20ß-trihydroxy-9-methyl-19-norlanosta-5,24-diene-22-one(2), 25-acetoxy-2ß-glucosyloxy-3ß,16α,20ß-trihydroxy-9-methyl-19-norlanosta-5-ene-22-one(3) and 25-acetoxy-2ß-glucosyloxy-3ß,16α,20ß-trihydroxy-9-methyl-19-norlanosta-5,23-(E)-diene-22-one(4). Compound 1 represents a new cucurbitane glycoside. The half inhibitory concentrations of the 4 compounds exceeded 100 µmol·L~(-1) against four tumor cell lines, indicating no significant cytotoxicity.
Asunto(s)
Glicósidos , Picrorhiza , Glicósidos/química , Glicósidos/aislamiento & purificación , Humanos , Línea Celular Tumoral , Picrorhiza/química , Estructura Molecular , Espectroscopía de Resonancia Magnética , Medicamentos Herbarios Chinos/química , TriterpenosRESUMEN
To characterize the chemical constituents of Huanbei Zhike Prescription by ultra-high performance liquid chromatography-time of flight mass spectrometry( UPLC-Q-TOF-MS/MS). A Thermo Syncronls C18 column( 2. 1 mm×100 mm,1. 7 µm) was used with methanol( A)-0. 1% formic acid solution( B) as the mobile phase for gradient elution. The injection volume was 2 µL; the column temperature was 40 â; the flow rate was 0. 3 m L·min-1; and electrospray ionization( ESI) source was used to collect data in positive and negative ion modes. The ion scanning range was m/z 50-1 200,with capillary voltage of 3 000 V,ion source temperature of100 â,atomization gas flow rate of 50 L·h-1,desolvent gas flow rate of 800 L·h-1,desolvent temperature of 400 â,cone hole voltage of 40 V,with argon as the collision gas and the collision energy was 20-35 V. The excimer ion peak information was analyzed by Waters UNIFI data processing software. The molecular formula with error within 1×10-5 was compared with the data in database to identify the compounds. The secondary fragment ion information of the target compound was selected,and then compared with the retention time and fragmentation patterns provided by the database and the existing literature to further confirm the compositions and structures of the compounds. A total of 68 main compounds in Huanbei Zhike Prescription were identified,including 38 flavonoids,10 organic acids,6 terpenoids and 10 nitrogen-containing compounds,of which 12 compounds were verified by the control substances. This method is rapid and accurate,which provides a new strategy for the qualitative analysis of the chemical constituents of Huanbei Zhike Prescription,and lays a foundation for the further study and quality control of the compound pharmacodynamic substance.
Asunto(s)
Medicamentos Herbarios Chinos/química , Cromatografía Líquida de Alta Presión , Flavonoides/análisis , Espectrometría de Masas en Tándem , Terpenos/análisisRESUMEN
OBJECTIVE: To explore the protective effect of baicalin against rotenone-induced injury on PC12 cells, and the po-tential mechanism of action action was also explored. METHOD: PC12 cells were injured by rotenone and were treated with different concentrations (0.1, 1, 10 µmol x L(-1)) of baicalin at the same time. Cell viability was analyzed by MTT, and morphology was observed by phase-contrast microscopy. The cell apoptosis was detected by flow cytometry by Annexin V-FITC/PI staining. The intracellular ROS level was determined by fluorescence microscope with DCF-DA staining. The expression of Bcl-2, Bax and Caspase-3 was analyzed by Western blot. RESULT: The viability of PC12 cells exposure to rotenone for 24 hour was gradually decreased with dose escalating and 1.5 µmol x L was adopted to do the following experiment. Baicalin increased cell viability, improved cell morphology and decreased intracellular ROS level. Moreover, FACS indicated baicalin attenuated the apoptosis induced by rotenone significantly. Western blot showed that Bcl-2, Bax and Caspase-3 expression in rotenone-induced PC12 cells was reversed by baicalin. CONCLUSION: This study has demonstrated that baicalin protects PC12 cells against rotenone-induced apoptosis, at least in part, by scavenging excessive ROS and inhibiting the mitochondrion-dependent apoptotic pathway.
Asunto(s)
Citoprotección/efectos de los fármacos , Flavonoides/farmacología , Rotenona/farmacología , Animales , Apoptosis/efectos de los fármacos , Caspasa 3/metabolismo , Supervivencia Celular/efectos de los fármacos , Regulación de la Expresión Génica/efectos de los fármacos , Espacio Intracelular/efectos de los fármacos , Espacio Intracelular/metabolismo , Células PC12 , Proteínas Proto-Oncogénicas c-bcl-2/metabolismo , Ratas , Especies Reactivas de Oxígeno/metabolismo , Proteína X Asociada a bcl-2/metabolismoRESUMEN
<p><b>OBJECTIVE</b>Parkinson's disease (PD) is featured with motor disorder and nonmotor manifestations including psychological symptoms, autonomic nervous system dysfunction, and paresthesia, which results in great inconvenience to the patients' life. The apolipoprotein (Apo) superfamily, as a group of potentially modifiable biomarkers in clinical practice, is of increasing significance in the diagnosis, evaluation, and prognosis of PD. The present review summarized the current understanding and emerging findings of the relationship between Apo superfamily and PD.</p><p><b>DATA SOURCES</b>All literatures were identified by systematically searching PubMed, Embase, and Cochrane electronic databases with terms "Parkinson disease," "apolipoprotein," and their synonyms until May 2017.</p><p><b>STUDY SELECTION</b>We have thoroughly examined titles and abstracts of all the literatures that met our search strategy and the full text if the research is identified or not so definite. Reference lists of retrieved articles were also scrutinized for additional relevant studies.</p><p><b>RESULTS</b>The levels of plasma ApoA1 are inversely correlated with the risk of PD and the lower levels of ApoA1 trend toward association with poorer motor performance. Higher ApoD expression in neurons represents more puissant protection against PD, which is critical in delaying the neurodegeneration process of PD. It is suggested that APOE alleles are related to development and progression of cognitive decline and age of PD onset, but conclusions are not completely identical, which may be attributed to different ApoE isoforms. APOJ gene expressions are upregulated in PD patients and it is possible that high ApoJ level is an indicator of PD dementia and correlates with specific phenotypic variations in PD.</p><p><b>CONCLUSIONS</b>The Apo superfamily has been proved to be closely involved in the initiation, progression, and prognosis of PD. Apos and their genes are of great value in predicting the susceptibility of PD and hopeful to become the target of medical intervention to prevent the onset of PD or slow down the progress. Therefore, further large-scale studies are warranted to elucidate the precise mechanisms of Apos in PD.</p>
RESUMEN
<p><b>OBJECTIVE</b>To provide a comprehensive and latest overview of susceptibility-weighted imaging (SWI) in the application of thrombolysis in acute ischemic stroke, and to update the decision-making effect and clinical value of SWI on identifying stroke patients suitable for thrombolytic therapy and possible benefits and risks followed.</p><p><b>DATA SOURCES</b>Literatures referred to this review were collected from PubMed, Medline, and EMBASE published till May 2017, using the search terms including susceptibility-weighted imaging, gradient-echo, T2*, thrombolysis, recombinant tissue plasminogen activator (rt-PA), thrombolytic therapy, and stroke.</p><p><b>STUDY SELECTION</b>Papers in English or with available English abstracts were considered, with no limitation of study design. References were also identified from the bibliographies of identified articles and the authors' files.</p><p><b>RESULTS</b>SWI is of guiding significance for thrombolytic therapy in stroke patients, it can predict the location and length of thrombus and ischemic penumbra. It is worthy of noting that susceptibility vessel sign (SVS) on SWI can be used to predict recanalization after thrombolytic therapy and whether it is better to implement endovascular thrombolectomy in combination or alone. SWI is sensitive in detecting cerebral microbleed (CMB), and CMB might not be a contraindication for thrombolytic therapy, yet CMBs in multiple foci could possibly be related to intracranial hemorrhage (ICH) after thrombolysis. SVS and CMB on SWI sequence are of instructive value in performing antiplatelet therapy after thrombolytic therapy. Cerebral venous change on SWI is related to lower recanalization rate and poor outcome after thrombolysis.</p><p><b>CONCLUSIONS</b>It seems that SWI can be applied to guide individualized thrombolytic therapies and assist clinicians in making better decisions by weighing benefits and risks. However, there still exist controversies about the relationship between signs on SWI and thrombolytic therapy.</p>