title: The syntheses and characterizations of vanadium complexes with 1,2-dihydroxyanthraquinone and the structure-effect relationship in their in vitro anticancer activities.
abstract: [V(V)O2(O2C14H6O2)(C5N2H12)](C5N2H13)(CH3OH) (1) and {Na[V(V)O(O2C14H6O2)2][(CH3)2NCHO]}n (2) have been synthesized by the reaction of V2O5 and NaVO3 with aromatic 1,2-diol (1,2-dihydroxyanthraquinone), and their molecular and crystal structures have been determined by X-ray diffraction. MTT assay tests of the V(V)O2L(A)L(B) and V(V)OL2 complexes against cancer cells have revealed that, when L is catechol, VOL2 showed broad-spectrum, high anticancer activities which were proportional to their concentration; however when L is naphthol or alizarin, VOL2 displayed little effect towards the cancer cells; moreover, complex 1 in the coordination model of V(V)O2L(A)L(B) showed specifically higher inhibition (88.65%) against HCT-8 than the clinical anticancer drug Fu-5 (69.97%). The results revealed that both the V(V) and the ligands cannot influence the inhibition against cancer cells individually. The mechanism of the broad-spectrum anticancer activities of VOL2 when L is catechol ligand might originate from the redox activities of V(V)/V(IV) which regulate the concentration of ROS (reactive oxygen species). N-Methylpiperazine formed as a by-product in complex 1 was confirmed by (1)H NMR and its formation mechanism catalyzed by V2O5 has been deduced.
authors.affiliation: Department of Chemistry, Capital Normal University, Beijing, 100037, China.
authors.forename: Shizhen
authors.initials: S
authors.lastname: Du
authors.forename: Jun
authors.initials: J
authors.lastname: Feng
authors.forename: Xiaoming
authors.initials: X
authors.lastname: Lu
authors.forename: Guo
authors.initials: G
authors.lastname: Wang
mesh_terms: D000880:Anthraquinones / Q000737:chemistry*; D000970:Antineoplastic Agents / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D045744:Cell Line, Tumor; D049109:Cell Proliferation / Q000187:drug effects; D002470:Cell Survival / Q000187:drug effects; D004305:Dose-Response Relationship, Drug; D004354:Drug Screening Assays, Antitumor; D005472:Fluorouracil / Q000494:pharmacology; D006801:Humans; D008958:Models, Molecular; D015394:Molecular Structure; D009942:Organometallic Compounds / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D013329:Structure-Activity Relationship; D014639:Vanadium / Q000737:chemistry*
chemical_list: D000880:Anthraquinones; D000970:Antineoplastic Agents; D009942:Organometallic Compounds; D014639:Vanadium; C010078:alizarin; D005472:Fluorouracil