TY - JOUR
T1 - Glucose-modification of cisplatin to facilitate cellular uptake, mitigate toxicity to normal cells, and improve anti-cancer effect in cancer cells
AU - Quan, Li
AU - Lin, Zuantao
AU - Lin, Yuebin
AU - Wei, Yanchun
AU - Lei, Liu
AU - Li, Yaxi
AU - Tan, Gongjun
AU - Xiao, Min
AU - Wu, Tianfu
N1 - Funding Information:
This work was supported by grants from the start-up fund of Huaiyin Institute of Technology , the Natural Science Foundation of Jiangsu Provincial Department of Education ( 17KJB530001 ), the Natural Science Foundation of China ( 51803068 and 31470926 ), Jiangsu Government Overseas Studies Scholarship ( JS-2017-201 ), the International Cooperation in Science and Technology Research projects ( HAC201615 ), and Jiangsu Qing Lan project . Appendix A
Publisher Copyright:
© 2019 Elsevier B.V.
Copyright:
Copyright 2020 Elsevier B.V., All rights reserved.
PY - 2020/3/5
Y1 - 2020/3/5
N2 - Cisplatin has been considered an effective anticancer drug clinically. However, drug resistance and side effects of toxicity on normal cells greatly diminish the anti-cancer outcome of cisplatin. In this study, glucose modification was conducted to improve cisplatin anti-cancer efficacy. Firstly, cisplatin was oxidized to c,c,t-[Pt(NH3)2Cl2(OH)2] and then a carboxyl group was introduced to obtain c,c,t-[Pt(NH3)2Cl2(OOCCH2CH2COOH)2] (Pt(IV)–COOH), and finally glucose was grafted onto Pt(IV)–COOH. The glucose modification of cisplatin opens the glucose transport channels (GTC) on the cell membrane for Pt drug. The opening of GTC increases the uptake of Pt drug for cells. This simple and effective modification strategy may not only mitigate toxicity to normal cells, but also increase the anti-cancer effect of Pt drugs.
AB - Cisplatin has been considered an effective anticancer drug clinically. However, drug resistance and side effects of toxicity on normal cells greatly diminish the anti-cancer outcome of cisplatin. In this study, glucose modification was conducted to improve cisplatin anti-cancer efficacy. Firstly, cisplatin was oxidized to c,c,t-[Pt(NH3)2Cl2(OH)2] and then a carboxyl group was introduced to obtain c,c,t-[Pt(NH3)2Cl2(OOCCH2CH2COOH)2] (Pt(IV)–COOH), and finally glucose was grafted onto Pt(IV)–COOH. The glucose modification of cisplatin opens the glucose transport channels (GTC) on the cell membrane for Pt drug. The opening of GTC increases the uptake of Pt drug for cells. This simple and effective modification strategy may not only mitigate toxicity to normal cells, but also increase the anti-cancer effect of Pt drugs.
KW - Anti-cancer efficacy
KW - Cisplatin
KW - Glucose transport channel
KW - Glucose-modification
KW - Platinum(Ⅳ)
UR - http://www.scopus.com/inward/record.url?scp=85076215292&partnerID=8YFLogxK
UR - http://www.scopus.com/inward/citedby.url?scp=85076215292&partnerID=8YFLogxK
U2 - 10.1016/j.molstruc.2019.127361
DO - 10.1016/j.molstruc.2019.127361
M3 - Article
AN - SCOPUS:85076215292
SN - 0022-2860
VL - 1203
JO - Journal of Molecular Structure
JF - Journal of Molecular Structure
M1 - 127361
ER -