PMID- 8564263
OWN - NLM
STAT- MEDLINE
DCOM- 19960305
LR  - 20190512
IS  - 0007-1188 (Print)
IS  - 0007-1188 (Linking)
VI  - 116
IP  - 4
DP  - 1995 Oct
TI  - The effect of a synthetic 7-thiaprostaglandin E1 derivative, TEI-6122, on 
      monocyte chemoattractant protein-1 induced chemotaxis in THP-1 cells.
PG  - 2298-302
AB  - 1 The ability of various prostaglandins (PGs) to inhibit monocyte chemotaxis 
      induced by monocyte chemoattractant protein-1 (MCP-1) was investigated with a 
      human monocytic leukaemia cell line, THP-1. Moreover, to investigate the 
      mechanism of the inhibitory action of PGs the involvement of either intracellular 
      adenosine 3': 5'-cyclic monosphosphate (cyclic AMP) accumulation or intracellular 
      Ca2+ mobilization was studied. 2 TEI-6122, a synthetic 7-thia-PGE1 derivative, 
      inhibited chemotaxis of THP-1 cells induced by MCP-1 with an IC50 of 1.5 pM. Its 
      inhibitory activity was 1000 fold more than that of PGE1 and PGE2 (IC50 = 2.8 nM 
      and 0.9 nM, respectively), which were more potent than other PGs such as PGA1, 
      PGA2, PGF2 alpha and PGI2 (IC50 > or = 1 microM). 3 With respect to the effect on 
      intracellular cyclic AMP accumulation in THP-1 cells, TEI-6122 was as potent as 
      PGE1 and PGE2, which were approximately 100 to 1000 fold more potent than the 
      other PGs such as PGA1, PGA2 and PGI2. The minimum concentration of TEI-6122 
      required to increase intracellular cyclic AMP accumulation in THP-1 cells was 1 
      nM. 4 TEI-6122 and PGE1 (4 microM) transiently increased intracellular calcium 
      levels in THP-1 cells. When added prior to MCP-1, both PGs partially suppressed 
      the increased in Ca2+ caused by this cytokine. There were no significant 
      differences between the activity of TEI-6122 and PGE1 in either respect. 5 It is 
      concluded that TEI-6122, a synthetic 7-thia-PGE1 derivative is a much more potent 
      inhibitor of MCP-1-induced THP-1 cell chemotaxis than PGEI and PGE2 which are the 
      best inhibitors among the natural PGs tested, while neither intracellular cyclic 
      AMP accumulation nor effects on Ca2+ mobilization account for the extremely 
      potent inhibitory activity of TEI-6122. Thus, either a novel PGE2 receptor 
      (EPreceptor) or a novel intracellular signal transduction system may be involved 
      in the extremely potent chemotaxis inhibitory activity of TEI-6122.
FAU - Tanaka, H
AU  - Tanaka H
AD  - Pharmaceutical Discovery Research Laboratories, Teijin Institute for Biomedical 
      Research, Tokyo, Japan.
FAU - Minoshima, T
AU  - Minoshima T
FAU - Endo, N
AU  - Endo N
LA  - eng
PT  - Journal Article
PL  - England
TA  - Br J Pharmacol
JT  - British journal of pharmacology
JID - 7502536
RN  - 0 (Chemokine CCL2)
RN  - 0 (Fibrinolytic Agents)
RN  - 83058-69-9 (TFC 612)
RN  - E0399OZS9N (Cyclic AMP)
RN  - F5TD010360 (Alprostadil)
RN  - SY7Q814VUP (Calcium)
SB  - IM
MH  - Alprostadil/*analogs & derivatives/pharmacology
MH  - Calcium/metabolism
MH  - Chemokine CCL2/*antagonists & inhibitors/pharmacology
MH  - Chemotaxis, Leukocyte/*drug effects
MH  - Cyclic AMP/metabolism
MH  - Fibrinolytic Agents/*pharmacology
MH  - Humans
MH  - Kinetics
MH  - Leukemia, Monocytic, Acute/metabolism/physiopathology
MH  - Tumor Cells, Cultured
PMC - PMC1908987
EDAT- 1995/10/01 00:00
MHDA- 1995/10/01 00:01
PMCR- 1996/10/01
CRDT- 1995/10/01 00:00
PHST- 1995/10/01 00:00 [pubmed]
PHST- 1995/10/01 00:01 [medline]
PHST- 1995/10/01 00:00 [entrez]
PHST- 1996/10/01 00:00 [pmc-release]
AID - 10.1111/j.1476-5381.1995.tb15068.x [doi]
PST - ppublish
SO  - Br J Pharmacol. 1995 Oct;116(4):2298-302. doi: 
      10.1111/j.1476-5381.1995.tb15068.x.