Abstract
Pseurotin A was isolated from a culture of marine Bacillus sp. FS8D and showed to be active against the proliferation of four different glioma cells with IC50 values of 0.51-29.3 μM. It has been found that pseurotin A downregulated the expression of tumour glycolytic enzymes pyruvate kinase M2 (PKM2) and lactate dehydrogenase 5 (LDH5) and upregulated the expression of pyruvate dehydrogenase beta (PDHB), adenosine triphosphate synthase beta (ATPB) and cytochrome C (Cyto-C), the important regulators for tricarboxylic acid cycle and oxidative phosphorylation. The data suggested that targeting multiple metabolic enzymes might be one of the antiglioma mechanisms of pseurotin A.
Keywords:
Bacillus sp. FS8D; antiglioma activity; pseurotin A; tumour metabolic enzymes.
MeSH terms
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Animals
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Antineoplastic Agents / pharmacology*
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Bacillus / chemistry*
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Bacillus / metabolism
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Carrier Proteins / genetics
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Carrier Proteins / metabolism
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Cell Proliferation / drug effects
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Cytochromes c / metabolism
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Down-Regulation / drug effects
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Enzymes / genetics
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Enzymes / metabolism*
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Glioma / drug therapy*
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Glioma / metabolism
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Glycolysis
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Humans
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Inhibitory Concentration 50
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Isoenzymes / genetics
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Isoenzymes / metabolism
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L-Lactate Dehydrogenase / genetics
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L-Lactate Dehydrogenase / metabolism
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Lactate Dehydrogenase 5
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Membrane Proteins / genetics
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Membrane Proteins / metabolism
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Mitochondrial Proton-Translocating ATPases / metabolism
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Pyrrolidinones / isolation & purification
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Pyrrolidinones / pharmacology*
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Thyroid Hormone-Binding Proteins
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Thyroid Hormones / genetics
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Thyroid Hormones / metabolism
Substances
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Antineoplastic Agents
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Carrier Proteins
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Enzymes
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Isoenzymes
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Membrane Proteins
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Pyrrolidinones
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Thyroid Hormones
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pseurotin
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Cytochromes c
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L-Lactate Dehydrogenase
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Lactate Dehydrogenase 5
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ATP synthase beta subunit, rat
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Mitochondrial Proton-Translocating ATPases