PMID- 3474661
OWN - NLM
STAT- MEDLINE
DCOM- 19870826
LR  - 20220330
IS  - 0027-8424 (Print)
IS  - 1091-6490 (Electronic)
IS  - 0027-8424 (Linking)
VI  - 84
IP  - 15
DP  - 1987 Aug
TI  - Dequalinium, a topical antimicrobial agent, displays anticarcinoma activity based 
      on selective mitochondrial accumulation.
PG  - 5444-8
AB  - Positively charged lipophilic compounds, such as rhodamine 123, localize in 
      mitochondria and are selectively accumulated and retained by carcinoma cells. It 
      has been suggested that this phenotype may be exploited for selective killing of 
      carcinoma cells by lipophilic cations. Here we report that doubly positively 
      charged dequalinium, which has been used for 30 years as an antimicrobial agent 
      in over-the-counter mouthwashes, lozenges, ointments, and paints, exhibits 
      significant anticarcinoma activity. Dequalinium is more effective than seven of 
      eight established anticancer drugs in prolonging the survival of mice with 
      intraperitoneally implanted mouse bladder carcinoma MB49. Dequalinium also 
      inhibits the growth of subcutaneously implanted human colon carcinoma CX-1 in 
      nude mice and recurrent rat colon carcinoma W163 in rats. Lipophilic cationic 
      compounds, such as dequalinium, could comprise a unique class of anticarcinoma 
      agents.
FAU - Weiss, M J
AU  - Weiss MJ
FAU - Wong, J R
AU  - Wong JR
FAU - Ha, C S
AU  - Ha CS
FAU - Bleday, R
AU  - Bleday R
FAU - Salem, R R
AU  - Salem RR
FAU - Steele, G D Jr
AU  - Steele GD Jr
FAU - Chen, L B
AU  - Chen LB
LA  - eng
GR  - CA19589/CA/NCI NIH HHS/United States
PT  - Journal Article
PT  - Research Support, U.S. Gov't, P.H.S.
PL  - United States
TA  - Proc Natl Acad Sci U S A
JT  - Proceedings of the National Academy of Sciences of the United States of America
JID - 7505876
RN  - 0 (Antibiotics, Antineoplastic)
RN  - 0 (Quinolinium Compounds)
RN  - 0 (Rhodamines)
RN  - 1N3CZ14C5O (Rhodamine 123)
RN  - E7QC7V26B8 (Dequalinium)
SB  - IM
MH  - Animals
MH  - Antibiotics, Antineoplastic/*therapeutic use
MH  - Dequalinium/*therapeutic use
MH  - Male
MH  - Mice
MH  - Mice, Inbred Strains
MH  - Microscopy, Fluorescence
MH  - Mitochondria/*metabolism
MH  - Neoplasm Transplantation
MH  - Phenotype
MH  - Quinolinium Compounds/*therapeutic use
MH  - Rhodamine 123
MH  - Rhodamines/metabolism
MH  - Urinary Bladder Neoplasms/*drug therapy
PMC - PMC298874
EDAT- 1987/08/01 00:00
MHDA- 2001/03/28 10:01
PMCR- 1988/02/01
CRDT- 1987/08/01 00:00
PHST- 1987/08/01 00:00 [pubmed]
PHST- 2001/03/28 10:01 [medline]
PHST- 1987/08/01 00:00 [entrez]
PHST- 1988/02/01 00:00 [pmc-release]
AID - 10.1073/pnas.84.15.5444 [doi]
PST - ppublish
SO  - Proc Natl Acad Sci U S A. 1987 Aug;84(15):5444-8. doi: 10.1073/pnas.84.15.5444.