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宝鸡文理学院 化学化工学院, 陕西省植物化学重点实验室,陕西 宝鸡,721013
纸质出版日期:2016-12-10,
收稿日期:2016-7-3,
修回日期:2016-10-9,
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王欢, 王姣, 李宗孝等. ITC研究达卡巴嗪与DNA反应动力学[J]. 发光学报, 2016,37(12): 1560-1565
WANG Huan, WANG Jiao, LI Zong-xiao etc. Interaction Dynamics Between Dacarbazine and DNA[J]. Chinese Journal of Luminescence, 2016,37(12): 1560-1565
王欢, 王姣, 李宗孝等. ITC研究达卡巴嗪与DNA反应动力学[J]. 发光学报, 2016,37(12): 1560-1565 DOI: 10.3788/fgxb20163712.1560.
WANG Huan, WANG Jiao, LI Zong-xiao etc. Interaction Dynamics Between Dacarbazine and DNA[J]. Chinese Journal of Luminescence, 2016,37(12): 1560-1565 DOI: 10.3788/fgxb20163712.1560.
利用等温滴定量热(ITC)、光谱、粘度测量等方法,研究了小牛胸腺DNA与抗癌药物达卡巴嗪的相互作用。结果表明:达卡巴嗪与DNA作用后,吸收光谱会出现增色、蓝移和粘度减小等现象。采用ITC法得到了结合常数以及结合位点数,发现达卡巴嗪与DNA以非经典嵌插式及表面作用两种方式结合。对于嵌插式,
H
1
<
0,
S
1
>
0,
K
1
=5.6310
4
,结合位点数0.10;对于药物分子仅与DNA表面发生作用而并未嵌入到DNA分子的疏水部分的结合方式,
H
2
>
0,
S
2
>
0,
K
2
=1.0010
3
,结合位点数9.99。同时发现紫外法得到的结合常数是
K
a
=6.7010
4
,与ITC的嵌插式吻合。
The interaction between calf thymus DNA and anti-cancer drug dacarbazine was investigated using isothermal titration calorimetry(ITC)
spectroscopy
viscosity and other methods. The hyperchromic effect and blue shift in the absorption spectra as well as viscosity decline are observed clearly after the interaction between dacarbazine and DNA. Furthermore
the binding constant and number of binding sites are also recorded by ITC
presenting that the interactions of the dacarbazine with DNA can be categorized for two modes:a non-classical intercalation type and surface binding effect. In former
H
1
<
0
S
1
>
0
K
1
=5.6310
4
the binding site is 0.10. In latter
only surficial interaction during the combination of the drug molecule with DNA occurs
not embedding into the hydrophobic part of the DNA molecule
due to
H
2
>
0
S
2
>
0
K
2
=1.0010
3
and the binding site of 9.99. Meanwhile
UV method is also employed to find the binding constant of
K
a
=6.7010
4
which is consistence with ITC observation.
DNA达卡巴嗪光谱法作用机理等温滴定量热
DNAdacarbazinespectroscopyinteraction mechanismisothermal titration calorimetry
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