Abstract
The glycoglycerolipid, monogalactosyl diacylglycerol (MGDG), containing two alpha-linolenic acids (C18:3), was isolated from bitter melon as a potent and selective inhibitor of mammalian DNA polymerase (pol) species such as pols alpha, gamma, delta, and epsilon with IC(50) values of 17.6-37.2muM. This MGDG also suppressed the growth of six human cancer cell lines, although normal human cell lines were not affected. This compound (i.e., MGDG-C18:3-C18:3) was a stronger inhibitor than both MGDG-C18:1-C18:0 and MGDG-C18:0-C18:0. In this study, we discussed the structure-function relationship in the selective inhibition of mammalian replicative pols and human cancer cell proliferation by MGDGs.
Publication types
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Research Support, Non-U.S. Gov't
MeSH terms
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Animals
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Antineoplastic Agents, Phytogenic / chemistry
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Antineoplastic Agents, Phytogenic / isolation & purification
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Antineoplastic Agents, Phytogenic / pharmacology*
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Cattle
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Cell Line, Tumor
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Cucurbitaceae / chemistry
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DNA-Directed DNA Polymerase / drug effects*
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Enzyme Inhibitors / chemistry
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Enzyme Inhibitors / isolation & purification
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Enzyme Inhibitors / pharmacology*
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Galactolipids / chemistry
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Galactolipids / isolation & purification
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Galactolipids / pharmacology*
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Humans
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In Vitro Techniques
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Neoplasms / enzymology*
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Nucleic Acid Synthesis Inhibitors
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Plant Extracts / chemistry
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Plant Extracts / isolation & purification
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Plant Extracts / pharmacology*
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Structure-Activity Relationship
Substances
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Antineoplastic Agents, Phytogenic
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Enzyme Inhibitors
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Galactolipids
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Nucleic Acid Synthesis Inhibitors
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Plant Extracts
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monogalactosyldiacylglycerol
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DNA-Directed DNA Polymerase