Cytotoxicity Evaluation of Dimethoxy and Trimethoxy Indanonic Spiroisoxazolines Against Cancerous Liver Cells

Current Chemical Biology Pub Date : 2020-02-29 DOI:10.2174/2212796813666190926112807

A. Abolhasani, F. Heidari, S. Noori, S. Mousavi, H. Abolhasani

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引用次数: 5

Abstract

3'-(3,4-dimethoxyphenyl)-4'-(4-(methylsulfonyl)phenyl)-4'H-spiro [indene-2,5'-isoxazol]-1(3H)-one and 4'-(4-(methylsulfonyl)phenyl)-3'-(3,4,5-trimethoxyphenyl)- 4'H-spiro[indene-2,5'-isoxazol]-1(3H)-one compounds containing indanonic spiroisoxazoline core are widely known for their antiproliferative activities and investigation of tubulin binding modes. To evaluate the cytotoxicity effect of Dimethoxy and Trimethoxy Indanonic Spiroisoxazolines against HepG2 cancerous liver cell line and to perform a comparison with other known anti-liver cancer drugs. The evaluation of cytotoxicity of dimethoxy and trimethoxy indanonic spiroisoxazoline compounds, Oxaliplatin, Doxorubicin, 5-fluorouracil and Cisplatin against HepG2 (hepatocellular liver carcinoma) cell line has been performed using MTT assay and analyzed by GraphPad PRISM software (version 8.0.2). Potent cytotoxicity effects against HepG2 cell line, comparable to Cisplatin (IC50= 0.047±0.0045 µM), Oxaliplatin (IC50= 0.0051µM), Doxorubicin (IC50= 0.0014µM) and 5- fluorouracil (IC50= 0.0089 µM), were shown by both dimethoxy (IC50= 0.059±0.012 µM) and trimethoxy (IC50= 0.086±0.019 µM) indanonic spiroisoxazoline compounds. In vitro biological evaluations revealed that dimethoxy and trimethoxy indanonic spiroisoxazoline compounds are good candidates for the development of new anti-liver cancer agents.

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二甲氧基和三甲氧基吲哚酮螺异恶唑啉对肝癌细胞的细胞毒性评价

3'-(3,4-二甲氧基苯基)-4'-(4-(甲基磺酰基)苯基)-4'- h -spiro[茚-2,5'-异恶唑]-1(3H)- 1和4'-(4-(甲基磺酰基)苯基)-3'-(3,4,5-三甲氧基苯基)-4'- h -spiro[茚-2,5'-异恶唑]-1(3H)- 1含有吲哚酮螺的化合物因其抗增殖活性和对微管蛋白结合模式的研究而广为人知。目的评价二甲氧基和三甲氧基吲哚酮螺异恶唑啉对HepG2肝癌细胞株的细胞毒性作用，并与其他已知抗肝癌药物进行比较。采用MTT法评价二甲氧基和三甲氧基茚二酮螺异恶唑啉化合物、奥沙利铂、阿霉素、5-氟尿嘧啶和顺铂对HepG2(肝细胞肝癌)细胞株的细胞毒性，并采用GraphPad PRISM软件(8.0.2版)进行分析。二甲氧基(IC50= 0.059±0.012µM)和三甲氧基(IC50= 0.086±0.019µM)茚二酮螺异恶唑啉化合物对HepG2细胞株的细胞毒作用与顺铂(IC50=0.047±0.0045µM)、奥沙利铂(IC50= 0.0051µM)、阿霉素(IC50= 0.0014µM)和5-氟尿嘧啶(IC50= 0.0089µM)相当。体外生物学评价表明，二甲氧基和三甲氧基吲哚醌螺异恶唑啉类化合物是开发新型抗肝癌药物的良好候选者。

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来源期刊

Current Chemical Biology Medicine-Biochemistry (medical)

CiteScore

1.40

自引率

0.00%

发文量

期刊介绍： Current Chemical Biology aims to publish full-length and mini reviews on exciting new developments at the chemistry-biology interface, covering topics relating to Chemical Synthesis, Science at Chemistry-Biology Interface and Chemical Mechanisms of Biological Systems. Current Chemical Biology covers the following areas: Chemical Synthesis (Syntheses of biologically important macromolecules including proteins, polypeptides, oligonucleotides, oligosaccharides etc.; Asymmetric synthesis; Combinatorial synthesis; Diversity-oriented synthesis; Template-directed synthesis; Biomimetic synthesis; Solid phase biomolecular synthesis; Synthesis of small biomolecules: amino acids, peptides, lipids, carbohydrates and nucleosides; and Natural product synthesis).