PMID- 34555601
OWN - NLM
STAT- MEDLINE
DCOM- 20220222
LR  - 20220222
IS  - 1873-3344 (Electronic)
IS  - 0162-0134 (Linking)
VI  - 225
DP  - 2021 Dec
TI  - Systematic evaluation of the antitumor activity of three ruthenium polypyridyl 
      complexes.
PG  - 111616
LID - S0162-0134(21)00263-4 [pii]
LID - 10.1016/j.jinorgbio.2021.111616 [doi]
AB  - Ruthenium-containing complexes have emerged as good alternative to the currently 
      used platinum-containing drugs for malignant tumor therapy. In this work, 
      cytotoxic effects of recently synthesized ruthenium polypyridyl complexes 
      [Ru(bpy)(2)(CFPIP)](ClO(4))(2) (bpy = 2,2'-bipyridine, 
      CFPIP = (E)-2-(4-fluorostyryl)-1H-imidazo[4,5-f][1,10]phenanthroline, Ru(II)-1), 
      [Ru(phen)(2)(CFPIP)](ClO(4))(2) (phen = 1,10-phenanthroline, Ru(II)-2) and 
      [Ru(dmb)(2)(CFPIP)](ClO(4))(2) (dmb = 4,4'-dimethyl-2,2'-bipyridine, Ru(II)-3) 
      toward different tumor cells were investigated in vitro and compared with 
      cisplatin, the most widely used chemotherapeutic drug against hepatocellular 
      carcinoma (HepG-2). The results demonstrate that target complexes show excellent 
      cytotoxicity against HepG-2 cells with low IC(50) value of 21.4 +/- 1.5, 18.0 +/- 2.1 
      and 22.3 +/- 1.7 muM, respectively. It was important noting that target Ru(II) 
      complexes exhibited better antitumor activity than cisplatin 
      (IC50 = 28.5 +/- 2.4 muM) against HepG-2 cells, and has no obvious toxicity to 
      normal cell LO2. DNA binding results suggest that Ru(II)-1, Ru(II)-2 and Ru(II)-3 
      interact with CT DNA (calf thymus DNA) through intercalative mode. Complexes 
      exerted its antitumor activity through increasing anti-migration and inducing 
      cell cycle arrest at the S phase. In addition, the apoptosis was tested by AO 
      (acridine orange)/EB (ethidium bromide) staining and flow cytometry. 
      Mitochondrial membrane potential (MMP), reactive oxygen species (ROS), and 
      colocalization tests were also evaluated by ImageXpress Micro XLS system. 
      Overall, the results show that the ruthenium polypyridyl complexes induce 
      apoptosis in HepG-2 cells through ROS-mediated mitochondria dysfunction pathway.
CI  - Copyright (c) 2021 Elsevier Inc. All rights reserved.
FAU - Jiang, Guang-Bin
AU  - Jiang GB
AD  - Guangxi Key Laboratory of Electrochemical and Magnetochemical Function Materials, 
      College of Chemistry and Bioengineering, Guilin University of Technology, Guilin 
      541004, China. Electronic address: jianggb@glut.edu.cn.
FAU - Zhang, Wen-Yao
AU  - Zhang WY
AD  - School of Pharmacy, Guangdong Pharmaceutical University, Guangzhou 510006, PR 
      China.
FAU - He, Miao
AU  - He M
AD  - School of Pharmacy, Guangdong Pharmaceutical University, Guangzhou 510006, PR 
      China.
FAU - Gu, Yi-Ying
AU  - Gu YY
AD  - School of Pharmacy, Guangdong Pharmaceutical University, Guangzhou 510006, PR 
      China.
FAU - Bai, Lan
AU  - Bai L
AD  - School of Pharmacy, Guangdong Pharmaceutical University, Guangzhou 510006, PR 
      China.
FAU - Wang, Yang-Jie
AU  - Wang YJ
AD  - School of Pharmacy, Guangdong Pharmaceutical University, Guangzhou 510006, PR 
      China.
FAU - Yi, Qiao-Yan
AU  - Yi QY
AD  - School of Pharmacy, Guangdong Pharmaceutical University, Guangzhou 510006, PR 
      China.
FAU - Du, Fan
AU  - Du F
AD  - School of Pharmacy, Guangdong Pharmaceutical University, Guangzhou 510006, PR 
      China.
LA  - eng
PT  - Journal Article
PT  - Research Support, Non-U.S. Gov't
DEP - 20210920
PL  - United States
TA  - J Inorg Biochem
JT  - Journal of inorganic biochemistry
JID - 7905788
RN  - 0 (Antineoplastic Agents)
RN  - 0 (Coordination Complexes)
RN  - 0 (Pyridines)
RN  - 0 (Reactive Oxygen Species)
RN  - 7UI0TKC3U5 (Ruthenium)
RN  - 9007-49-2 (DNA)
RN  - 91080-16-9 (calf thymus DNA)
SB  - IM
MH  - Animals
MH  - Antineoplastic Agents/chemical synthesis/metabolism/*pharmacology
MH  - Apoptosis/drug effects
MH  - Cattle
MH  - Cell Line, Tumor
MH  - Cell Movement/drug effects
MH  - Cell Proliferation/drug effects
MH  - Coordination Complexes/chemical synthesis/metabolism/*pharmacology
MH  - DNA/metabolism
MH  - Drug Screening Assays, Antitumor
MH  - Humans
MH  - Membrane Potential, Mitochondrial/drug effects
MH  - Mitochondria/drug effects
MH  - Pyridines/chemical synthesis/metabolism/*pharmacology
MH  - Reactive Oxygen Species/metabolism
MH  - Ruthenium/chemistry
MH  - S Phase Cell Cycle Checkpoints/drug effects
OTO - NOTNLM
OT  - Antitumor activity
OT  - Apoptosis
OT  - Cell cycle arrest
OT  - Mitochondria
OT  - Ruthenium(II) complexes
EDAT- 2021/09/24 06:00
MHDA- 2022/02/23 06:00
CRDT- 2021/09/23 20:19
PHST- 2021/07/09 00:00 [received]
PHST- 2021/08/20 00:00 [revised]
PHST- 2021/09/14 00:00 [accepted]
PHST- 2021/09/24 06:00 [pubmed]
PHST- 2022/02/23 06:00 [medline]
PHST- 2021/09/23 20:19 [entrez]
AID - S0162-0134(21)00263-4 [pii]
AID - 10.1016/j.jinorgbio.2021.111616 [doi]
PST - ppublish
SO  - J Inorg Biochem. 2021 Dec;225:111616. doi: 10.1016/j.jinorgbio.2021.111616. Epub 
      2021 Sep 20.