▎ 摘　　要

NOVELTY - Graphene base that targets major groove of DNA and inhibits topoisomerase comprises a nano-scale graphene planar structure with size of 1-10 nm and thickness of 0.34-3.4 nm. USE - The graphene base targeting the major groove of DNA is useful in pharmaceutical composition and for preparing an inhibitor and/or a medicine or a composition for treating and/or preventing disease, reversing drug resistance of drug-resistant cells and/or inhibiting metastasis of cancer cells. The graphene base is useful in preparation of a reversal agent for reversing tumor multidrug resistance and/or an inhibitor for inhibiting cancer cell metastasis. The tumor multidrug resistance includes one or more of breast cancer resistance to adriamycin, colon cancer resistance to paclitaxel and cervical cancer resistance to cisplatin. The disease is cancer, diseases associated with excessive topoisomerase I and/or topoisomerase II activity, or their combination. The graphene base is also useful in fluorescent probe for labeling of isolated DNA or labeling of DNA or nucleus in living cells. The cancer is colon cancer, breast cancer, gastriccancer, lung cancer, colorectal cancer, pancreatic cancer, ovarian cancer, prostate cancer, kidney cancer, liver cancer, brain cancer, melanoma, multiple myeloma, chronic myelogenous leukemia, blood tumor and lymphatic tumor. The cell is human breast cancer cell MCF-7, human osteosarcoma cell MG-63, human pancreatic cancer cell PANC-1, human liver cancer cell HepG2, human lung cancer cell A549, mouse breast cancer cell 4T1, gastric cancer cell Hgc-27, human colon cancer cell HCT-8, malignant melanoma cell A375, human cervical cancer cell Hela or their combination (all claimed). ADVANTAGE - The graphene base has a simple structure, is easy to synthesize, has precise targeting function of the nuclear DNA major groove and high-efficiency inhibitory activity on topoisomerase I and II, especially in the absence of small molecular drug components and no grafted special targeting molecules and exhibits high anticancer activity than chemotherapeutic drugs. DETAILED DESCRIPTION - INDEPENDENT CLAIMS are included for the following: (1) method for preparing the graphene base targeting the major groove of DNA and inhibiting topoisomerase involves (a) performing one-step reaction by in the presence of a catalyst, reacting a precursor in one step in an alcohol solvent to form the graphene base, where the precursor is julolidine and the catalyst is an organic acid and/or its anhydride, and/or a phosphorus-containing compound; (2) use of the graphene base targeting the major groove of DNA and inhibiting topoisomerase, (i) to prepare an inhibitor for inhibiting topoisomerase, and/or (ii) to prepare a medicine or a composition for treating and/or preventing cancer; and (3) fluorescent probe comprising the graphene base.