ABSTRACT
The structural basis for the intracellular delivery of OSW-1 is investigated using fluorescent derivatives of OSW-1 and its closely related congeners. Despite the large differences in activity, all the fluorescent probes are found to translocate across the plasma membrane to the ER and Golgi apparatus. This observation suggests that the glycosylated cholestane moiety plays an important role in the cell internalization and intracellular localization property of OSW-1.
Subject(s)
Cholestenones/chemistry , Cholestenones/metabolism , Fluorescent Dyes/chemistry , Fluorescent Dyes/metabolism , Intracellular Space/metabolism , Saponins/chemistry , Saponins/metabolism , Biological Transport , HeLa Cells , HumansABSTRACT
A novel fluorescent photoaffinity probe of OSW-1 was prepared in two steps from a naturally occurring inactive congener by a sequential site-selective acylation strategy using Me2SnCl2. It displayed highly potent anticancer activity and a similar intracellular localization property to that of a fluorescently-tagged OSW-1, thereby demonstrating its potential utility in live cell studies.
Subject(s)
Antineoplastic Agents/chemical synthesis , Cholestenones/chemical synthesis , Fluorescent Dyes/chemical synthesis , Photoaffinity Labels/chemical synthesis , Saponins/chemical synthesis , Acylation , Antineoplastic Agents/pharmacokinetics , Antineoplastic Agents/pharmacology , Cell Proliferation/drug effects , Cholestenones/pharmacokinetics , Cholestenones/pharmacology , Fluorescent Dyes/pharmacokinetics , Fluorescent Dyes/pharmacology , HeLa Cells , Humans , Neoplasms/drug therapy , Photoaffinity Labels/pharmacokinetics , Photoaffinity Labels/pharmacology , Saponins/pharmacokinetics , Saponins/pharmacologyABSTRACT
Correction for 'Synthesis of a fluorescent photoaffinity probe of OSW-1 by site-selective acylation of an inactive congener and biological evaluation' by K. Sakurai et al., Chem. Commun., 2017, DOI: .
ABSTRACT
In a Muscovy duck breeding-growing farm in Aomori prefecture, most of ducklings hatched during spring in 1994 died within two-week-old. The mortality was nearly 100%. In most cases, birds died without clinical signs and some with leg weakness. By serological and virological tests, the outbreak was identified as a goose parvovirus infection. In pathological test, however, no typical manifestations of goose parvovirus infections (hepatitis and intranuclear inclusion bodies in hepatic cells) were detected.
