Synthesis of (-)-epigallocatechin-3-gallate derivative containing a triazole ring and combined with cisplatin/paclitaxel inhibits NSCLC cancer cells by decreasing phosphorylation of the EGFR. Issue 9 (September 2020)

• Record Type: Journal Article
• Authors: Zi, Cheng-Ting; Sun, Pei-Yuan; Zhang, Ning; Tang, Han; Yang, Hao-Nang; Wang, Qi; Wang, Yu-Na; Wang, Jing; Wang, Xuan-Jun; Sheng, Jun
• Is Part Of: Journal of chemical research. Volume 44:Issue 9/10(2020)
• Page Start: 586
• Page End: 591
• Publication Date: 2020-09
• Subjects: combination -- (-)-epigallocatechin-3-gallate derivative -- wild type of epidermal growth factor receptor -- non-small-cell lung cancer -- synthesis; Chemistry -- Research -- Periodicals; Chemistry -- Periodicals; 540.5
• DOI: 10.1177/1747519820910390
• Languages: English
• ISSNs: 1747-5198

Abstract

Non-small-cell lung cancer is one of the principal causes of cancer-related death around the world. Chemotherapy is commonly used to treat wild type of epidermal growth factor receptor non-small-cell lung cancer. (-)-Epigallocatechin-3-gallate is the most abundant and active catechin. However, (-)-epigallocatechin-3-gallate has limited clinical application due to its poor stability and absorption. Herein, we report that a glycosylated azide undergoes a click reaction with the terminal alkyne of (-)-epigallocatechin-3-gallate to yield a triazole-linked glucose-(-)-epigallocatechin-3-gallate derivative and have evaluated its in vitro anticancer activity against human non-small-cell lung cancer cells using the 3-(4, 5-dimethylthiazol-2-yl)-2, 5-diphenyltetrazolium bromide assay. The product inhibits human non-small-cell lung cancer cell lines with wild type of epidermal growth factor receptor and in combination with cisplatin/ paclitaxel results in more pronounced proliferation inhibition than when used alone. Stability investigations indicates that the conjugated glucose residue can improve the stability of the (-)-epigallocatechin-3-gallate scaffold. Our studies suggest that the combination of the glucose-(-)-epigallocatechin-3-gallate derivative and chemotherapeutic drugs may provide a novel strategy for the treatment of non-small-cell lung cancer.