38 research outputs found

    Design, synthesis and biological evaluation of isochroman-4-one hybrids bearing piperazine moiety as antihypertensive agent candidates

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    7,8 Dihydroxy 3 methyl isochromanone 4 XJP is a polyphenolic natural product with moderate antihypertensive activity. T o obtain new agents with stronger potency and safer profile , we employed XJP and naftopidil as the lead compound s t o design and synth esize a novel class of hybrids as antihypertensive candidates, In the present study, a series of hybrids ( 6a r ) of XJP bearing arylpiperazine moiety, which is identified as the pharmacophore of naftopidil, were designed and synthesized as novel α 1 adrenergic receptor antagonists. The biological evaluation showed that target compounds 6c , 6e , 6f , 6g , 6h , 6m and 6q possessed potent in vitro vasodilation potency and α 1 adrenergic receptor antagonistic activity . Furthermore, the most potent compound 6e significantly reduced the systolic and diastolic blood pressure in spontaneously hypertensive rats (SHRs),which was comparable to that of naftopidil, and it had no observable effects on the basal heart rate, suggesting that 6e deserves to be further investigated as a potential clinical candidate for the treatment of hypertension

    Antitumor Research of the Active Ingredients from Traditional Chinese Medical Plant Polygonum Cuspidatum

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    In recent years, the utilization of Chinese native medicine and other plant extracts in the treatment of diseases has attracted extensive attention, especially in the area of malignant tumors. However, lots of herbal remedies active ingredients have not been found or have been discovered but not effectively developed and applied. Therefore, screening new Chinese medicine active components and determining their antitumor effects have become a new breakthrough in the prevention and treatment of tumor disease. In the past years, a large number of studies have demonstrated that Polygonum cuspidatum and its active components like resveratrol showed excellent antitumor activities, including our own antitumor studies about resveratrol in colorectal cancer. The purpose of this review is to summarize the research progress of Chinese herb Polygonum cuspidatum and its active components in tumor diseases and provide theoretical basis for further scientific experiments and clinical applications

    Analysis of the Influence Mechanism of Consumers’ Trading Behavior on Reusable Mobile Phones

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    The aim of this study is to investigate the decision-making mechanism of reusable mobile phone trading behaviors by using the extended theory of planned behavior. In this study, based on the survey data of 964 residents in Beijing, China and structural equation modeling method, the main factors that affect consumers’ reusable mobile phone trading behavior and their degree of influence were analyzed, followed by discussion on decision-making mechanisms. The findings show that consumers’ behavioral selection has been significantly related to four intrinsic subjective factors and fifteen external objective factors, and the combined effect of the latter ones is nearly triple of that of the former ones. Moreover, the observed variables of environmental awareness, information leakage sensitivity, trading convenience and consumer trading returns are the four most significant factors. The impact of active trading behavior is not significant. However, this may be because that there were no great trading rewards, lack of trading awareness and regulations. Finally, the study put forward relevant policy recommendations for improving the comprehensive management of recycling reusable mobile phones, and provides a theoretical reference for improving the recycling rate of reusable mobile phones
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