PROSTAGLANDIN D-2, A POTENTIAL ANTI-NEOPLASTIC AGENT
PROSTAGLANDIN D-2, A POTENTIAL ANTI-NEOPLASTIC AGENT
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DOI：
10.1016/0006-291x(82)91063-4
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发表时间：
1982-01-01
影响因子：
3.1
通讯作者：
HAYAISHI, O
中科院分区：
文献类型：
--
作者：
FUKUSHIMA, M;KATO, T;HAYAISHI, O
用L1210小鼠白血病细胞系和几种人白血病细胞系检测了各种野牡丹素的细胞毒作用，发现前列腺素D_2（PGD_2）最有活性。超过3.6 μ M，PGD 2对L1210细胞生长产生剂量依赖性抑制。在14.3 μ M时，生长被完全抑制;在培养过程中活细胞的数量显著减少。显微镜下，剩余细胞显示退行性变化，细胞质中有许多空泡。PGD 2对L1210细胞生长的IC 50 [50%生长抑制浓度]值为6.9 μ M（2.4 μ g/ml）;在该浓度下，培养24小时的细胞中的DNA合成也降低至对照细胞中水平的1/2。在几种人白血病细胞系（NALL-1、RPMI-8226、RPMI-8402和Sk-Ly-16）中也发现了类似浓度的PGD 2的生长抑制作用。在测试的其它洋地黄素中，PGA 2显示出相当的生长抑制活性，而PGE 2显示出较小但显著的生长抑制活性; PGB 2、PGF 2 α、PGF 3 α、PGF 2而PGI 2在14.3 μ M时对细胞增殖没有这种作用。提示PGD 2具有潜在的抗肿瘤活性。
Cytotoxic actions of various prostaglandins were examined on L1210 mouse leukemia and several human leukemia cell lines; prostaglandin D2 (PGD2 was found most active. PGD2 exerted a dose dependent inhibition of L1210 cell growth over 3.6 .mu.M. At 14.3 .mu.M growth was completely inhibited; the number of viable cells remarkably decreased during culture. Microscopically the remaining cells showed degenerative changes with many vacuoles in their cytoplasm. The IC50 [50% growth inhibitory concentration] value of PGD2 on L1210 cell growth was 6.9 .mu.M (2.4 .mu.g/ml); at this concentration the DNA synthesis in 24 h cultured cells was also decreased to 1/2 the level in the control cells. Such growth inhibition by PGD2 was also found at similar concentrations with several human leukemia cell lines (NALL-1, RPMI-8226, RPMI-8402 and Sk-Ly-16). Among other prostaglandins tested, PGA2 showed a comparable, and PGE2, a less but significant, growth inhibitory activity; PGB2, PGF2.alpha. and PGI2 had no such effects on cell proliferation at 14.3 .mu.M. A potential antineoplastic activity of PGD2 was suggested.