摘要
采用国内合成的８－氯腺苷经体内、外实验研究，结果表明，用１００ｍｇ·ｋｇ￣（－１）·ｄ￣（－１）×７剂量，可使小鼠肝癌实体瘤Ｈ＿２２抑制率达７１．７％±１３．３％腹腔注射（ｉｐ）和６６．１％±４．４６％静脉注射（ｉｖ），使白血病Ｌ１２１０荷瘤小鼠的生命延长率达１２４．Ｏ％±２２．１％（ｉｐ）和１０４．２％±２０．１％（ｉｖ）。体外实验显示，８－氯腺苷对人白血病细胞系ＨＬ－６０和Ｋ＿５６２以及人胃癌细胞系ＭＧＣ８Ｏ－３均有明显抑制生长作用，其ＩＣ＿５０值分别为：１．８μｍｏｌ／Ｌ、４．２μｍｏｌ／Ｌ和１．５６μｍｏｌ／Ｌ。该药采用腹腔一次注射测定小鼠的ＬＤ＿５０为：１０２５．０±５２．４ｍｇ／ｋｇ；大鼠的ＬＤ＿５０为：７９３．４±７０．７ｍｇ／ｋｇ，表明其急性毒性很低。
Abstract 8-chloroadenosine showed
marked activity against mice solid tumor hepatoma 22(H_22) and
asciticleukemia L-1210.At 100mg. Kg￣(-1)./d×7,the inhibition rate
of H_22 was 71.7±13.3%(P<0.01)and 66.1 ±4.46%(P<0.
01),i.p.and.v.,respectively;at the same dose,the life-prolonging rate
ofmice bearing L-1210 was 124.O±22.1%(P<0.01)and 104.2±
20.1%(P<0.01),i.p.and i.v.,respectively.8-chloroadenosine also showed
activity against 3 human cancer cell lines in vitro.The IC_50
valueswere determined by measuring cell growth using trypan blue dye
exclusion.The resutls showed thatHL-60 and K_562, and human gastric
cancer cell line MGc8O-3 had IC_50 values of 1.8μmol/L,4.2μmol/L
and 1.56μmol/L, respectively.The toxicity of 8-chloroadenosine was
low, with LD_50 of1025.0±52.4mg/kg for mice and 793.4±70.7mg/kg for
rats by single i.p. injection.
出处
《中华肿瘤杂志》
CAS
CSCD
北大核心
1995年第1期5-8,共4页
Chinese Journal of Oncology
基金
国家"八五"科技攻关和自然科学基金
