• 专利标题:   Preparing graphene quantum dot of targeting tumor cell nucleus useful for preparing antitumor drug, comprises e.g. reacting hydrazine with nitric acid to obtain trinitropyrene, freezing and drying trinitropyrene, and resuspending.
  • 专利号:   CN108125982-A
  • 发明人:   QI L, LIN D, PAN T, YANG M, CHENG R, CHEN L, YAO Q, ZHANG L, DAI L
  • 专利权人:   UNIV WENZHOU MEDICAL
  • 国际专利分类:   A61K033/44, A61K047/64, C01B032/184, A61P035/00
  • 专利详细信息:   CN108125982-A 08 Jun 2018 A61K-033/44 201852 Pages: 8 Chinese
  • 申请详细信息:   CN108125982-A CN11294970 08 Dec 2017
  • 优先权号:   CN11294970

▎ 摘  要

NOVELTY - Preparing graphene quantum dot of targeting tumor cell nucleus comprises e.g. (1) using hydrazine as raw material, reacting hydrazine with nitric acid under high temperature to obtain trinitropyrene, and freezing and drying the trinitropyrene; resuspending the trinitropyrene with aqueous ammonia water, carrying ultrasonic reaction, adding the reacted mixture to the reaction kettle, carrying hydrothermal reaction to obtain aminated graphene quantum dots, dialyzing the aminated graphene quantum dots in dialysis bag by deionized water, freezing and drying; and (2) activating the carboxy terminus of the FITC-RGDS polypeptide by using carbodiimide/N-hydroxysuccinimide at room temperature, covalently linking the FITC-RGDS polypeptide and the aminated graphene quantum dot obtained in the step (1) through amide reaction, where tumor-targeted graphene quantum dots prepared in this step (2) are graphene quantum dots covalently linked to the RGDS polypeptide. USE - The graphene quantum dot of targeting tumor cell nucleus is useful for preparing antitumor drug ( where the antitumor drug comprises graphene quantum dot of targeting tumor cell nucleus mentioned above)(claimed), and killing effect on tumor cells. ADVANTAGE - The graphene quantum dot of targeting tumor cell nucleus: has specific function of targeting tumors and nuclei. DETAILED DESCRIPTION - Preparing graphene quantum dot of targeting tumor cell nucleus comprises (1) using hydrazine as raw material, reacting hydrazine with nitric acid under high temperature to obtain trinitropyrene, and freezing and drying the trinitropyrene; resuspending the trinitropyrene with aqueous ammonia water, carrying ultrasonic reaction, adding the reacted mixture to the reaction kettle, carrying hydrothermal reaction to obtain aminated graphene quantum dots, dialyzing the aminated graphene quantum dots in dialysis bag by deionized water, freezing and drying; where the molecular weight cut off of the dialysis bag is less than or equal to 3500; (2) activating the carboxy terminus of the FITC-RGDS polypeptide by using carbodiimide/N-hydroxysuccinimide at room temperature, covalently linking the FITC-RGDS polypeptide and the aminated graphene quantum dot obtained in the step (1) through amide reaction, where tumor-targeted graphene quantum dots prepared in this step (2) are graphene quantum dots covalently linked to the RGDS polypeptide; and (3) using carbodiimide/N-hydroxysuccinimide to activate the carboxy terminal of TAT polypeptide at room temperature, covalently binding to the remaining primary amino group at the edge of the tumor-targeting graphene quantum dot prepared in step (2), constructing graphene quantum dots with targeted tumor nucleus, where the graphene quantum dots targeting the tumor cell nucleus are covalently linked to the graphene quantum dots by the RGDS polypeptide and the TAT polypeptide. An INDEPENDENT CLAIM is also included for the graphene quantum dot of targeting tumor cell nucleus prepared by above mentioned method.