Synthesis of platinum(II) and palladium(II) complexes with 9,9-dihexyl-4,5-diazafluorene and their in vivo antitumour activity against Hep3B xenografted mice.
Two complexes dichloro(9,9-dihexyl-4,5-diazafluorene)platinum(II) (Pt-DHF) and dichloro(9,9-dihexyl-4,5-diazafluorene)palladium(II) (Pd-DHF) were synthesized and their in vivo antitumour activity was investigated using an athymic nude mice model xenografted with human Hep3B carcinoma cells. Pt-DHF- and Pd-DHF-treated groups showed significant tumour growth inhibition (with about 9-fold and 3-fold tumour growth retardation) when compared with the vehicle control group. The liver toxicology effects on the animals of the two compounds were investigated. Pt-DHF and Pd-DHF-treated groups had a lower alanine transaminase and aspartate transaminase values than those of the vehicle treated group as the animals from the vehicle control group had very heavy hepatoma burden. We assume that both complexes could be further investigated as effective antitumour agents and it is worthwhile to study their underlying working mechanism.
Institute of Molecular Functional Materials, Department of Chemistry and Partner State Key Laboratory of Environmental and Biological Analysis, Hong Kong Baptist University, Hong Kong, PR China; Chengdu Institute of Organic Chemistry, Chinese Academy of Sciences, Chengdu, 610041, PR China; HKBU Institute of Research and Continuing Education, Shenzhen Virtual University Park, Shenzhen, 518057, PR China.
Q-W
QW
Wang
State Key Laboratory of Chirosciences, Department of Applied Biology and Chemical Technology, The Hong Kong Polytechnic University, Hong Kong, PR China. Electronic address: tcstacey@polyu.edu.hk.
P-L
PL
Lam
Department of Medicine and Therapeutics, The Chinese University of Hong Kong, Hong Kong, PR China.
R S-M
RS
Wong
Faculty of Health Sciences, University of Macau, Macau, PR China.
G Y-M
GY
Cheng
State Key Laboratory of Chirosciences, Department of Applied Biology and Chemical Technology, The Hong Kong Polytechnic University, Hong Kong, PR China.
K-H
KH
Lam
Clinical Division, School of Chinese Medicine, Hong Kong Baptist University, Hong Kong, PR China. Electronic address: bzxiang@hkbu.edu.hk.
Z-X
ZX
Bian
Institute of Molecular Functional Materials, Department of Chemistry and Partner State Key Laboratory of Environmental and Biological Analysis, Hong Kong Baptist University, Hong Kong, PR China; HKBU Institute of Research and Continuing Education, Shenzhen Virtual University Park, Shenzhen, 518057, PR China. Electronic address: clamho@hkbu.edu.hk.
C-L
CL
Ho
Department of Applied Physics and Chemistry, University of Taipei, Taipei, 100, Taiwan.
Y-H
YH
Feng
Centre of Biotechnology, Department of Life Sciences and Biotechnology, University of Ferrara, Ferrara, Italy.
R
R
Gambari
Department of Applied Physics and Chemistry, University of Taipei, Taipei, 100, Taiwan. Electronic address: yhlo@utaipei.edu.tw.
Y-H
YH
Lo
Institute of Molecular Functional Materials, Department of Chemistry and Partner State Key Laboratory of Environmental and Biological Analysis, Hong Kong Baptist University, Hong Kong, PR China; State Key Laboratory of Chirosciences, Department of Applied Biology and Chemical Technology, The Hong Kong Polytechnic University, Hong Kong, PR China; HKBU Institute of Research and Continuing Education, Shenzhen Virtual University Park, Shenzhen, 518057, PR China. Electronic address: rwywong@hkbu.edu.hk.
W-Y
WY
Wong
State Key Laboratory of Chirosciences, Department of Applied Biology and Chemical Technology, The Hong Kong Polytechnic University, Hong Kong, PR China; Department of Medicine and Therapeutics, The Chinese University of Hong Kong, Hong Kong, PR China; Clinical Division, School of Chinese Medicine, Hong Kong Baptist University, Hong Kong, PR China. Electronic address: chchui@hkbu.edu.hk.
C-H
CH
Chui
D000818:Animals; D000970:Antineoplastic Agents / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology / Q000627:therapeutic use; D006528:Carcinoma, Hepatocellular / Q000188:drug therapy; D045744:Cell Line, Tumor; D049109:Cell Proliferation / Q000187:drug effects; D056831:Coordination Complexes / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D004195:Disease Models, Animal; D004789:Enzyme Activation / Q000187:drug effects; D064593:Heterografts; D006801:Humans; D008099:Liver / Q000187:drug effects; D008113:Liver Neoplasms / Q000188:drug therapy; D051379:Mice; D009944:Organoplatinum Compounds / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology* / Q000627:therapeutic use; D010165:Palladium / Q000737:chemistry* / Q000494:pharmacology / Q000627:therapeutic use; D010984:Platinum / Q000737:chemistry* / Q000494:pharmacology / Q000627:therapeutic use
D000970:Antineoplastic Agents; D056831:Coordination Complexes; D009944:Organoplatinum Compounds; C000615818:dichloro(9,9-dihexyl-4,5-diazafluorene)palladium(II); C000615817:dichloro(9,9-dihexyl-4,5-diazafluorene)platinum(II); D010984:Platinum; D010165:Palladium
Antitumour; In vivo; Palladium-diazafluorene complex; Platinum-diazafluorene complex