An improved synthesis of piperlongumine and the preliminary imaging evaluation on tumor targeting

An improved synthesis of piperlongumine and the preliminary imaging evaluation on tumor targeting
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胡椒长明的合成改进及肿瘤靶向影像学初步评价

DOI:
10.1007/s10967-020-07117-5
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发表时间:
2020-03
影响因子:
1.6
通讯作者:
Chuan Zhang
Chuan Zhang
中科院分区:
化学4区
文献类型:
--
作者:
Kun He;Honglei Xu;Tingfang Wang;Xiao Li;Bingjie Guo;Danni Li;Yi Li;Chuan Zhang

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Piperlongumine is a natural product that exhibited anti-cancer effect for various tumor types. For in vivo metabolism, I-125 labeled piperlongumine (125I-PL) was expelled by kidney soon post injection, so tumor targeting was achieved at 30 min post injection;125I-PL reached a 2.33 ± 0.51 ratio of tumor/liver in SMMC-7721 (HCC tumor cells line) subcutaneous tumor BALB/c nude mice, but a negative uptake was observed in MHCC97h subcutaneous tumor mice. Therefore, piperlongumine was conveniently synthesized via amidation approach, and the fast clearance and tumor targeting were manifested for the first time.
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