Biological activity of the functional epitope of ciguatoxin fragment AB on the neuroblastoma sodium channel in tissue culture.
It is well established that the targeted receptor for ciguatoxin (CTX) in mammalian tissues is the sodium channel, affecting the influx of sodium into cells and altering the action potential and function of the cell. Since the syntheses of fragments of CTX has become available, our focus has been on the receptor functions of the west sphere AB and east sphere JKLM fragments using the neuroblastoma cell assay, guinea pig atrium assay, and the membrane immunobead assay (MIA). The data presented here suggest that the west sphere AB of the ciguatoxin molecule is the active portion and is responsible for the activation of the sodium channels.
Hokama
Y
Y
Department of Pathology, John A. Burns School of Medicine, University of Hawaii at Manoa, Honolulu, Hawaii 96822, USA. yoshitsu@hawaii.edu
Chun
K E
KE
Campora
C E
CE
Higa
N
N
Suma
C
C
Hamajima
A
A
Isobe
M
M
D000818:Animals; D045744:Cell Line, Tumor; D002922:Ciguatoxins / Q000037:antagonists & inhibitors / Q000737:chemistry / Q000494:pharmacology*; D000939:Epitopes; D006168:Guinea Pigs; D006325:Heart Atria / Q000187:drug effects / Q000503:physiopathology; D008297:Male; D051379:Mice; D009200:Myocardial Contraction / Q000187:drug effects / Q000502:physiology; D009447:Neuroblastoma / Q000378:metabolism / Q000473:pathology; D009474:Neurons / Q000187:drug effects* / Q000378:metabolism / Q000473:pathology; D017747:Seafood / Q000032:analysis; D015222:Sodium Channels / Q000187:drug effects* / Q000378:metabolism; D013329:Structure-Activity Relationship; D013552:Swine
D000939:Epitopes; D015222:Sodium Channels; D002922:Ciguatoxins