Evaluation of Anticancer Activity of Water‐Soluble Curcumin through the Induction of Apoptosis by p53 and p21 Modulation,ChemistrySelect

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Evaluation of Anticancer Activity of Water‐Soluble Curcumin through the Induction of Apoptosis by p53 and p21 Modulation
ChemistrySelect ( IF 1.9 ) Pub Date : 2018-03-15 , DOI: 10.1002/slct.201800217
Govindharasu Banuppriya ₁ , Ganeshan Shakambari ₂ , Rajendran Sribalan ₁ , Perumal Varalakshmi ₂ , Vediappen Padmini ₁

Affiliation

Amide containing water soluble curcumin derivatives were synthesized and studied for their anti‐cancer activity. The synthesized water soluble compounds were cytotoxic when tested in vitro on HeLa cell and induced a p53 mediated apoptosis as evidenced by immunoblot analysis. Further DNA binding studies were also carried out to investigate the interaction between these synthesized curcumin compounds and HS‐DNA. The binding constant values (0.8167_X10⁴ M⁻¹of 5a, 0.5443 _X10³ M⁻¹ of 5b) suggested a good binding propensity to DNA. Physical properties such as stability, solubility, and log p values were investigated for the synthesized compounds.

中文翻译：

通过调节p53和p21诱导细胞凋亡评估水溶性姜黄素的抗癌活性

合成了含酰胺的水溶性姜黄素衍生物，并研究了其抗癌活性。合成的水溶性化合物在HeLa细胞上进行体外测试时具有细胞毒性，并通过免疫印迹分析证明可诱导p53介导的细胞凋亡。还进行了进一步的DNA结合研究，以研究这些合成的姜黄素化合物与HS-DNA之间的相互作用。结合常数的值（0.8167 _X 10 ⁴中号^-1 5a的，0.5443 _X 10 ³中号^-1 5b的）建议了良好的结合特性以将DNA。研究了合成化合物的物理性质，如稳定性，溶解度和log p值。

更新日期：2018-03-15

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