title: Influence of cucumariosides upon intracellular [Ca2+]i and lysosomal activity of macrophages.
abstract: Biological effects of the triterpene glycosides, cucumariosides A(2)-2 and A(7)-1 from the edible sea cucumber Cucumaria japonica and their aglycones were investigated using embryos of the sea urchin Strongylocentrotus nudus and the BALB/C line mouse peritoneal macrophages. Cucumariosides were highly cytotoxic in a sea urchin embryo development test with EC(50) values of 0.3 and 1.98 microg/mL, respectively. The aglycone was completely lacking in cytotoxicity. In subtoxic concentrations (0.001-0.1 microg/mL), cucumarioside A(2)-2 showed more then 2-fold stimulation of lysosomal activity and induced a rapid short-term increase in cytosolic Ca(2+) content in mouse macrophages. The maximal stimulatory effect was detected after 1-2 h of cultivation of cells with this glycoside. Cucumarioside A(7)-1 demonstrated more weak effects and even slightly inhibited lysosomal activity, while the aglycone was completely ineffective. At the toxic concentration (1 microg/mL), cucumarioside A(2)-2 induced the sharp irreversable increase of intracellular Ca(2+) concentration. We suggested that cucumariosides, especially A(2)-2, may act as Ca(2+) agonists due to their membranolytic properties.
authors: Pacific Institute of Bioorganic Chemistry, Far Eastern Branch of RAS, Vladivostok 690022, Russia. agafonova@piboc.dvo.ru
authors: Irina G
authors: IG
authors: Agafonova
authors: Dmitry L
authors: DL
authors: Aminin
authors: Sergey A
authors: SA
authors: Avilov
authors: Valentin A
authors: VA
authors: Stonik
mesh_terms: D000818:Animals; D002118:Calcium / Q000378:metabolism*; D002455:Cell Division / Q000187:drug effects; D004625:Embryo, Nonmammalian / Q000166:cytology / Q000187:drug effects; D006027:Glycosides; D008247:Lysosomes / Q000187:drug effects* / Q000378:metabolism; D017737:Macrophages, Peritoneal / Q000187:drug effects* / Q000378:metabolism / Q000648:ultrastructure; D051379:Mice; D008807:Mice, Inbred BALB C; D012617:Sea Urchins / Q000196:embryology; D015398:Signal Transduction / Q000187:drug effects; D014315:Triterpenes / Q000494:pharmacology*
chemical_list: D006027:Glycosides; D014315:Triterpenes; C033504:cucumarioside; D002118:Calcium