Document Detail

Effect of tacrolimus derivatives on immunosuppression.
MedLine Citation:
PMID:  19407973     Owner:  NLM     Status:  MEDLINE    
In this study, the effects of the FK506-mPEG on immune cell activity, skin grafting rejection, and Freund's complete adjuvant arthritis were investigated. The proliferation of T cells was inhibited with increase with the FK506 and FK506-mPEG concentrations. FK506 and FK506-mPEG at concentrations between 0.01 nM and 1000 nM had very similar effects on the proliferation of the T cells. On the other hand, in the case of the proliferation of T cells by calcium ionophore A23187 (1 microM), when the FK506-mPEG concentration was increased from 0.01 to 1000 mM, the proliferation was decreased from 90.8 to 40.3%. This was 1.8-fold higher than that of paramethoxyamphetamine (PMA). The inhibitory effect of FK506-mPEG on mast cell proliferation was higher than that of FK506. When B cells were cultured for 7 days in basal medium with no pokeweed mitogen (PWM), the IgG production was 156.2 ng/mL. On the other hand, in the case of the same treatment with 0.25% of PWM, it was 876.4 ng/mL. This is about 5.6-fold higher than with no PWM. These results show that FK506-mPEG may be practically applicable as a prodrug for the immunosuppressant FK506.
Dubok Choi; Hoon Cho
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Publication Detail:
Type:  Journal Article; Research Support, Non-U.S. Gov't     Date:  2009-04-29
Journal Detail:
Title:  Archives of pharmacal research     Volume:  32     ISSN:  0253-6269     ISO Abbreviation:  Arch. Pharm. Res.     Publication Date:  2009 Apr 
Date Detail:
Created Date:  2009-05-01     Completed Date:  2009-05-14     Revised Date:  -    
Medline Journal Info:
Nlm Unique ID:  8000036     Medline TA:  Arch Pharm Res     Country:  Korea (South)    
Other Details:
Languages:  eng     Pagination:  549-57     Citation Subset:  IM    
Department of Environmental Health, Cho-dang University, Chonnam, 534-800, Korea.
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MeSH Terms
Antibody Formation / drug effects
Arthritis, Experimental / chemically induced,  immunology,  prevention & control
B-Lymphocytes / drug effects,  immunology
Cell Line, Tumor
Cell Proliferation / drug effects
Dose-Response Relationship, Drug
Drug Stability
Freund's Adjuvant
Graft Rejection / etiology,  immunology,  prevention & control
Graft Survival / drug effects
Histamine Release / drug effects
Immunosuppressive Agents / pharmacology*
Mast Cells / drug effects,  immunology
Mice, Inbred BALB C
Mice, Inbred C3H
Mice, Inbred DBA
Polyethylene Glycols / pharmacology*
Prodrugs / pharmacology*
Skin Transplantation / adverse effects
T-Lymphocytes / drug effects,  immunology
Tacrolimus / analogs & derivatives,  pharmacology*
Time Factors
Reg. No./Substance:
0/Immunosuppressive Agents; 0/Polyethylene Glycols; 0/Prodrugs; 109581-93-3/Tacrolimus; 9007-81-2/Freund's Adjuvant

From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine

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