9 research outputs found

    Pharmacokinetics and Biodistribution of Aurantiamide and Aurantiamide Acetate in Rats after Oral Administration of Portulaca oleracea L. Extracts

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    Aurantiamide and aurantiamide acetate are the main active constituents of purslane (Portulaca oleracea L.), an edible plant with various biological activities. In this study, we developed a validated UHPLC-MS/MS method to quantitate the concentrations of aurantiamide and aurantiamide acetate in the plasma and various organ tissues of rat as the basis to study their pharmacological profile and distribution in vivo. Aurantiamide and aurantiamide acetate were rapidly absorbed following oral administration, both achieving a <i>C</i><sub>max</sub> at around 0.2 h. The extent of their metabolisms also varied among different organ tissues, resulting in about 90% reduction in concentrations 4 h after their administration, thus leaving no long-term accumulation in the tissues. This is the first study to examine the pharmacokinetic and biodistribution of aurantiamide and aurantiamide acetate in rat, and our work may serve as the first step toward the investigation of the underlying mechanisms associated with the biological activity of purslane

    SPECT/CT imaging of chemotherapy-induced tumor apoptosis using <sup>99m</sup>Tc-labeled dendrimer-entrapped gold nanoparticles

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    <p>Non-invasive imaging of apoptosis in tumors induced by chemotherapy is of great value in the evaluation of therapeutic efficiency. In this study, we report the synthesis, characterization, and utilization of radionuclide technetium-99m (<sup>99m</sup>Tc)-labeled dendrimer-entrapped gold nanoparticles (Au DENPs) for targeted SPECT/CT imaging of chemotherapy-induced tumor apoptosis. Generation five poly(amidoamine) (PAMAM) dendrimers (G5.NH<sub>2</sub>) were sequentially conjugated with 1,4,7,10-tetraazacyclododecane-1,4,7,10-tetraacetic acid (DOTA), polyethylene glycol (PEG) modified duramycin, PEG monomethyl ether, and fluorescein isothiocyanate (FI) to form the multifunctional dendrimers, which were then utilized as templates to entrap gold nanoparticles. Followed by acetylation of the remaining dendrimer surface amines and radiolabeling of <sup>99m</sup>Tc, the SPECT/CT dual mode nanoprobe of tumor apoptosis was constructed. The developed multifunctional Au DENPs before and after <sup>99m</sup>Tc radiolabeling were well characterized. The results demonstrate that the multifunctional Au DENPs display favorable colloidal stability under different conditions, own good cytocompatibility in the given concentration range, and can be effectively labeled by <sup>99m</sup>Tc with high radiochemical stability. Furthermore, the multifunctional nanoprobe enables the targeted SPECT/CT imaging of apoptotic cancer cells <i>in vitro</i> and tumor apoptosis after doxorubicin (DOX) treatment in the established subcutaneous tumor model <i>in vivo</i>. The designed duramycin-functionalized Au DENPs might have the potential to be employed as a nanoplatform for the detection of apoptosis and early tumor response to chemotherapy.</p

    Pharmacokinetics and Biodistribution of Aurantiamide and Aurantiamide Acetate in Rats after Oral Administration of Portulaca oleracea L. Extracts

    No full text
    Aurantiamide and aurantiamide acetate are the main active constituents of purslane (Portulaca oleracea L.), an edible plant with various biological activities. In this study, we developed a validated UHPLC-MS/MS method to quantitate the concentrations of aurantiamide and aurantiamide acetate in the plasma and various organ tissues of rat as the basis to study their pharmacological profile and distribution in vivo. Aurantiamide and aurantiamide acetate were rapidly absorbed following oral administration, both achieving a <i>C</i><sub>max</sub> at around 0.2 h. The extent of their metabolisms also varied among different organ tissues, resulting in about 90% reduction in concentrations 4 h after their administration, thus leaving no long-term accumulation in the tissues. This is the first study to examine the pharmacokinetic and biodistribution of aurantiamide and aurantiamide acetate in rat, and our work may serve as the first step toward the investigation of the underlying mechanisms associated with the biological activity of purslane

    Data_Sheet_1_Effect of ambient temperature and other environmental factors on stroke emergency department visits in Beijing: A distributed lag non-linear model.pdf

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    BackgroundMost studies have focused on the relationship between ambient temperature and stroke mortality, but studies on the relationship between ambient temperature and stroke occurrence are still limited and inconsistent.ObjectiveThis study aimed to analyze the effect of ambient temperature and other environmental factors on emergency stroke visits in Beijing.MethodsOur study utilized stroke visit data from the Beijing Red Cross Emergency Medical Center during 2017–2018, and applied a generalized additive model (GAM) as well as a distributed lag non-linear model (DLNM), respectively, regarding the direct, lagged, and cumulative effects of ambient temperature alone and with correction for other environmental factors on stroke occurrence.ResultsWith a total of 26,984 emergency stroke patients in 2017–2018, both cold and hot effects were observed and weakened after correction for other environmental factors. Compared to the reference temperature, in the multi-factor model, extreme cold (−10°C) reached a maximum relative risk (RR) of 1.20 [95% Confidence Interval (CI): 1.09, 1.32] at lag 14 days, and extreme hot (30°C) had a maximum RR of 1.07 (95% CI: 1.04, 1.11) at lag 6 days. The cumulative effect of extreme cold reached a maximum of 2.02 (95% CI: 1.11, 3.67) at lag 0–14 days, whereas the cumulative effect of extreme hot temperature is greatest at lag 0–10 days, but no statistically significant effect was found. In addition, ischemic stroke patients, the elderly, and males were more susceptible to the effects of cold temperature.ConclusionsThere is a non-linear relationship between ambient temperature and stroke occurrence, with cold temperature having a greater and longer-lasting impact than hot temperature.</p
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