Abstract
For further structure-activity relationship (SAR) research of OSW saponins, a cholestane glycoside, namely 3beta, 16beta, 26-trihydroxycholest-5-en-22-one 16-O-(2-O-4-methoxybenzoyl-beta-D-xylopyranosyl)-(1-->3)-2-O-acetyl-alpha-L-arabinopyranoside (1) together with two 1-->4-linked disaccharide analogues (2 and 3) were synthesized. Their cytotoxic activities were evaluated by the standard MTT assay. Compound 1 showed potent cytotoxicity against five types of human tumor cells, with IC50 ranging between 1.3 and 73 nM.
Copyright (c) 2010 Elsevier Ltd. All rights reserved.
Publication types
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Research Support, Non-U.S. Gov't
MeSH terms
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Antineoplastic Agents
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Antineoplastic Agents, Phytogenic / chemical synthesis
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Antineoplastic Agents, Phytogenic / chemistry*
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Antineoplastic Agents, Phytogenic / pharmacology*
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Cell Line, Tumor
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Cell Survival / drug effects
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Cholestanes / chemical synthesis
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Cholestanes / chemistry*
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Cholestanes / pharmacology*
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Cholestenones / chemical synthesis
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Cholestenones / chemistry*
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Cholestenones / pharmacology*
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Cytotoxins / chemical synthesis
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Cytotoxins / chemistry
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Cytotoxins / pharmacology
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Drug Screening Assays, Antitumor
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Glycosides / chemical synthesis
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Glycosides / chemistry*
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Glycosides / pharmacology*
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Humans
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Models, Molecular
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Neoplasms / drug therapy
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Ornithogalum / chemistry
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Saponins / chemical synthesis
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Saponins / chemistry*
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Saponins / pharmacology*
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Structure-Activity Relationship
Substances
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Antineoplastic Agents
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Antineoplastic Agents, Phytogenic
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Cholestanes
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Cholestenones
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Cytotoxins
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Glycosides
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Saponins
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OSW 1