有机锡化合物抗肿瘤生物活性研究

彭; 俊苏怀德

有机锡化合物抗肿瘤生物活性研究

彭,
俊苏怀德

STUDIES ON THE ANTUMOR ACTIVITY OF ORGANOTIN COMPOUNDS

J Peng,
HD Su

摘要

摘要: 有机锡(IV)化合物能明显地抑制大鼠脑组织中PKC活性和肿瘤细胞增殖，且两者之间存在着相关性。抗肿瘤活性的构效关系是：(1)有机基团R决定整个化合物的生物活性，Ph>Et>n-Bu；(2)卤素的电负性影响化合物活性的大小。抗肿瘤活性可能通过snR₂²⁺实现。并能部分地阻断HL-60细胞周期中的G_I期向S期的移行。SnPh₂F₂，SnPh₂(CysOS)H₂O和SnPh₂Cl2·phen(CH₃)₂对PKC的IC₅₀值分别为25，15和20 umol·L^-1，对HL-60细胞的IC₅₀值分别为0．5，4．0和0．3umol·L^-1。但它们无诱导分化HL-60和K562细胞的作用。

Abstract: Organotin compounds were found to obviously inhibit the activity of phospholipid/Ca²⁺-dependent protein kinase(PKC)in rat brain tissue and the proliferation of tumor cell lines in vitro．The results showed that a correlation exists between the effects on PKC and anti-proliferative and antitumor activities．The structure-activity relationship was shown to be as follows：(1)R，the organic group determines the biological activity；(2)electronegativity of the halogen can affect the activity．The organotin compounds inhibit tumor cells by itsSnR₂²⁺，and inhibit G₁→s phases of HL-60 cell cycle．The IC₅₀ ofSnPh₂F₂，SnPh₂(CysOS)·H₂O andSnPh₂CI₂·phen(CH₃)₂are respectively 25，15 and 20 umol·L^-1 on PKC，0．5，4．0 and 0.3 umol.L^-1 on HL-60 cells，2．7，9 and 1.5 umol·L^-1 on BEL-7402 cells，2．2，15 and 5.0 umol·L^-1 on KB cells．But no induction of differentiation of leukemic cell lines HL-60 and K562 Was observed．

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