Meiho University Institutional Repository:Item 987654321/2799
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    题名: Dicentrine Analogue-Induced G2/M Arrest and
    作者: Lin, Huei-Fang;Huang, Huey-Lan;Liao, Jyh-Fei;Shen, Chien-Chang;Huang, Ray-Ling
    关键词: future study.Lindera megaphyllal" Lauraceael" D‑dicentrinel" dicentrine analoguesl" cytotoxicityl" apoptosisl" topoisomerase II inhibitorl
    日期: 2015-08-26
    上传时间: 2015-08-26T02:59:48Z (UTC)
    摘要: Lindera megaphylla has been traditionally used as
    an antineoplastic and wound healing remedy.We
    previously demonstrated the antitumor effects of
    D-dicentrine, a natural aporphine alkaloid from
    the root of L. megaphylla. To generate analogues,
    series of phenanthrene alkaloids from D-dicentrine
    were synthesized by degradation with ethyl
    chloroformate in pyridine, base hydrolysis, and Nalkylation.
    In this study, we demonstrated that
    one of the synthesized D-dicentrine analogues
    (here after designated as analogue 1) exhibited
    more potent cytotoxic effects than D-dicentrine
    in colon adenocarcinoma, hepatoma, leukemia,
    and epidermoid carcinoma cells. We performed
    cell cycle and apoptotic analysis by flow cytometry,
    an apoptotic DNA detection ELISA assay, and
    topoisomerase II activity by the kinetoplast DNA
    concatenation assay for studying their cytotoxic
    mechanisms. We found that both D-dicentrine
    and analogue 1 induced apoptosis and G2/M arrest
    histonebound
    DNA fragments. Moreover, we found thatanalogue 1 was 28-fold more potent than D-dicentrinefor inhibition of topoisomerase II activityby the kinetoplast DNA concatenation assay. Ourfindings indicate that D-dicentrine analogue 1 isvery promising as a potential antitumor agent forfuture study.apoptotic cells induced by analogue 1 was 4.5-fold higher than that induced by D-dicentrine asevident from measuring the amount of histoneboundhistoneboundDNA fragments. Moreover, we found thatanalogue 1 was 28-fold more potent than D-dicentrinefor inhibition of topoisomerase II activityby the kinetoplast DNA concatenation assay. Ourfindings indicate that D-dicentrine analogue 1 isvery promising as a potential antitumor agent for
    显示于类别:[生物科技系] 期刊論文

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