论文部分内容阅读
目的：为了在体外培养的肿瘤细胞中证实一组有生物活性载体：磺胺（ＳＵ）、９－氨基吖啶（ＡＣＤ）、异烟肼（ＩＮＨ）的植物生长调节剂４－氯（Ｍ）、２，４－二氯（Ｄ）或２，４，５－三氯（Ｔ）的萘氧乙酸、２，３，５－三氯苯甲酸（ＴＢ）、α－萘乙酸（ＮＡＡ）的衍生物对小鼠艾氏腹水癌细胞ＤＮＡ多聚酶（ＤＰ）的抑制作用，并筛选出抑酶力最强的化合物。方法：参照Ｋ．Ｏｎｏ法分离、纯化并检测ＤＰ活性。ＭＴＴ法测定对体外培养肿瘤细胞的ＩＣ５０。结果：１１个植物生长调节剂中５个化合物在１００μｇ／ｍｌ浓度下对ＤＰ粗酶抑制作用大于５０％，抑制率分别是Ａ８４０３（２，４－Ｄ－ＡＣＤ）７８．５±５．５％，Ａ８８４５（２，４，５－Ｔ－ＳＭＺ）７５．８±１６．０％，Ａ８６０１（ＮＡＡ－ＳＮ）７４．５±６．０％，Ａ８８７４（２，４，５－Ｔ－ＩＮＨ）７３．４±２．９％，Ａ８８７３（４Ｍ－ＩＮＨ）７１．０±１２．１％。其中Ａ８４０３（９－２，４－二氯苯氧乙酸氨基吖啶，２，４－Ｄ－ＡＣＤ）抑制ＤＰ能力最强。对ＤＰα的ＩＣ５０为３．４１４２μｇ／ｍｌ，对ＤＰβ的ＩＣ５０为３．７５２３μｇ／ｍｌ。Ａ８４０３对体外培养的低分化鼻咽癌ＣＮＥ－２细胞及ＨｅＬａ?
OBJECTIVE: To identify a group of plant growth regulators 4-chloro (M) with biologically active carriers: sulfa (SU), 9-aminoacridine (ACD) and isoniazid (INH) Naphthyloxyacetic acid, 2,3,5-trichlorobenzoic acid (TB), derivatives of α-naphthaleneacetic acid (NAA) of 2,4-dichloro (D) On Ehrlich ascites tumor cells DNA polymerase (DP) inhibition, and screening out the strongest inhibitory enzyme compounds. Method: Refer to K. Ono method to separate, purify and detect DP activity. The IC50 of tumor cells cultured in vitro was determined by MTT assay. Results: Five compounds from 11 plant growth regulators inhibited DP crude enzyme by more than 50% at the concentration of 100μg / ml, the inhibitory rates were 78.4 ± 5.5% for A8403 (2,4-D-ACD) , A8845 (2,4,5-T-SMZ) 75.8 ± 16.0%, A8601 (NAA-SN) 74.5 ± 6.0%, A8874 (2,4,5-T-INH) .4 ± 2.9%, A8873 (4M-INH) 71.0 ± 12.1%. Among them, A8403 (9-2,4-dichlorophenoxyacetophenone, 2,4-D-ACD) has the strongest inhibitory effect on DP. The IC50 for DP [alpha] is 3.4142 [mu] g / ml and the IC50 for DP [beta] is 3.7523 [mu] g / ml. A8403 on cultured poorly differentiated nasopharyngeal carcinoma CNE-2 cells and HeLa?