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Molecular mechanism and pharmacokinetics of flavonoids in the treatment of resistant EGF receptor‐mutated non‐small‐cell lung cancer: A narrative review
Author(s) -
Wang Xuewen,
Chen Bing,
Xu Dafen,
Li Zhijun,
Liu Hao,
Huang Zhengjun,
Huang Kangping,
Lin Xinhua,
Yao Hong
Publication year - 2021
Publication title -
british journal of pharmacology
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 2.432
H-Index - 211
eISSN - 1476-5381
pISSN - 0007-1188
DOI - 10.1111/bph.15360
Subject(s) - lung cancer , pharmacology , t790m , atp binding cassette transporter , efflux , mechanism (biology) , cancer research , epidermal growth factor receptor , cancer , pharmacokinetics , drug resistance , mutation , biology , medicine , oncology , transporter , gene , genetics , gefitinib , philosophy , epistemology
Here, we review the molecular mechanism and pharmacokinetics of flavonoids in the treatment of resistant EGF receptor (EGFR)‐mutated non‐small‐cell lung cancer (NSCLC) and particularly the possible mechanism(s) of delicaflavone, a biflavonoid extracted from S elaginella doederleinii Hieron . EGFR TK inhibitors (EGFR‐TKI) are ubiquitously used in the treatment of NSCLC bearing EGFR mutations. However, patients treated with EGFR‐TKI inevitably and continuously develop resistance. In laboratory studies, flavonoids, as potential adjuvants for cancer chemotherapy, exhibited anti‐cancer properties such as inhibition of chemoresistance by interference with ABC transporters‐induced drug efflux, curbing of c‐MET amplification, or reversal of T790M mutation‐mediated resistance. The current review aims at summarizing the association between the anti‐cancer potentials of flavonoids and their possible regulatory roles in certain types of mutation that could trigger EGFR‐TKI resistance in NSCLC. Potential practical applications of these phytochemicals, as well as the relevant pharmacokinetics, are also discussed.