Anti-inflammatory and immunosuppressive properties of the bis-benzylisoquinolines: in vitro comparisons of tetrandrine and berbamine.
Tetrandrine and berbamine are two naturally occurring analogues with a bis-benzylisoquinoline structure. Comparative in vitro studies show that tetrandrine has significantly greater suppressive effects on adherence, locomotion and 3H-deoxyglucose uptake of neutrophils, as well as the mitogen-induced lymphocyte responses and mixed lymphocyte reactions. Also, tetrandrine displayed anti-oxidant activity while berbamine did not. By contrast, berbamine demonstrated a significantly greater capacity for inhibition of NK cell cytotoxicity. These results show that tetrandrine is superior to berbamine in most aspects of anti-inflammatory and immunosuppressive activity. Since these two alkaloids differ by only one substitution in the side chain of one of the benzene rings, these findings may provide further insight into structure-activity relationships and clues to the synthesis and development of active analogues of this promising class of drugs for the treatment of chronic inflammatory diseases.
Li
S Y
SY
Department of Child Health, University of Queensland, Mater Children's Hospital, South Brisbane, Australia.
Ling
L H
LH
Teh
B S
BS
Seow
W K
WK
Thong
Y H
YH
D000470:Alkaloids / Q000494:pharmacology*; D000894:Anti-Inflammatory Agents, Non-Steroidal / Q000138:chemical synthesis; D000970:Antineoplastic Agents / Q000494:pharmacology*; D000975:Antioxidants; D044182:Benzylisoquinolines; D002465:Cell Movement; D003847:Deoxyglucose / Q000378:metabolism; D006801:Humans; D007104:Immune Adherence Reaction; D007166:Immunosuppressive Agents / Q000138:chemical synthesis; D066298:In Vitro Techniques; D007694:Killer Cells, Natural / Q000187:drug effects; D008213:Lymphocyte Activation / Q000187:drug effects; D008214:Lymphocytes / Q000187:drug effects; D008934:Mitogens / Q000494:pharmacology; D009504:Neutrophils / Q000187:drug effects
D000470:Alkaloids; D000894:Anti-Inflammatory Agents, Non-Steroidal; D000970:Antineoplastic Agents; D000975:Antioxidants; D044182:Benzylisoquinolines; D007166:Immunosuppressive Agents; D008934:Mitogens; C009438:tetrandrine; D003847:Deoxyglucose; C027870:berbamine