Hypocholesterolemic action of 1-ethoxysilatrane

Mehta, Priya; Ramasarma, T.; Kurup, C. K. Ramakrishna

doi:10.1016/0005-2760(87)90316-x

Cited by 6 publications

(7 citation statements)

References 9 publications

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“…Silatranes were extensively studied after the discovery of specific biological activity of 1-arylsilatrane by Voronkov et al 27 Some reviews are reported on synthetic methods and bioactivity of silatranes [256][257][258][259][260][261][262][263][264] and biochemical roles of Si in animals and birds 265 which suggests the interactions of silatrane structure with biological membranes of feeding minks, sheep, pigs, dairy cattle and chickens. 6.4.1 Pilotropic activity.…”

Section: Application To Biological Systemsmentioning

confidence: 99%

Silatranes: a review on their synthesis, structure, reactivity and applications

2011

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This critical review summarizes progress of the rapidly developing and very active field of silatrane chemistry. The first part of the review deals with general synthetic approaches used to synthesize different silatranes. The most interesting feature of silatranes, i.e., variation of Si-N bond length on the basis of the axial substituent of Si, and other structural features, are described in the second part with special emphasis on crystallographic and theoretical studies. It is followed by a discussion on the reactivity of various silatranes. Silatranes have now gained acceptance for a wide variety of applications which are summarized in the last section of review. Some of them have extensive interest due to their medical use to heal wounds or stimulate hair-growth (pilotropic activity), biological properties, pharmacological properties e.g. antitumor, anticancer, antibacterial, anti-inflammatory, fungicidal activity, stimulating effect in animal production and seed germination effects. The review focuses on the extended potential of silatranes in sol-gel processes, mesoporous zeotypes, atomic force microscopy, commercial products such as adhesion promoters, polymer formation and rubber compositions. This critical review will be helpful for general researchers, experts, advanced undergraduates and newcomers working on silatrane chemistry as this review presents greater emphasis on synthesis and characterization, structural properties, reactivity and applications of silatranes in the field of biology, material science, sol-gel chemistry, pharmaceutics, agriculture and medicine (311 references).

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Section: Application To Biological Systemsmentioning

confidence: 99%

Silatranes: a review on their synthesis, structure, reactivity and applications

2011

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“…) tion (7) to form silatrane glycol 2 quantitatively. We recently determined that this reaction could be easily scaled to kilogram quantities (using 1 kg in a 12 L reactor).…”

Section: Synthesis Of Silatrane Glycolmentioning

confidence: 99%

“…Reaction (7) makes it possible to synthesize silatrane directly from silica in one step. If the ethylene glycol ligand can be exchanged easily with other ligands, this may o †er a novel, simple and low-cost route to other silatranes.…”

Section: Synthesis Of Silatrane Glycolmentioning

confidence: 99%

Simple, low-cost synthetic route to potentially polymerizable silatranes

Cheng¹,

Laine²

1999

New J. Chem.

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“…A number of compounds given to rats are known to decrease the concentration in serum and biogenesis in the liver, of cholesterol. Some examples are ~x-p-chlorophenoxyisobutyrate (CPIB, also known as clofibrate) [6,7], ubiquinone [8,9], diethylhexyl phthalate [10], 1-ethoxysilatrane [11,12]. The affected site in all these cases appears to be HMGCoA reductase in the endoplasmic reticulum from which microsomes are derived.…”

Section: Introductionmentioning

confidence: 98%

“…We describe here the preparation of a soluble 58-kDa enzyme by starting with heavy microsomes with limited protease activity. We chose for detailed studies the compound, 1-ethoxysilatrane, shown in our laboratory to be a potent hypocholesterolemic agent, whose administration to rats resulted in decrease in concentration in serum [11] and of biogenesis in the liver [12] of cholesterol. Treatment with this compound resulted in decrease in the activity, but not the concentration of the protein, of HMGCoA reductase in microsomes isolated from the liver [12].…”

Section: Introductionmentioning

confidence: 99%

Preparation of a soluble 58kDa-3-hydroxy-3-methylglutaryl CoA reductase from liver microsomes and its inhibition by ethoxysilatrane, a hypocholesterolemic compound

et al. 1992

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On repeated thawing at room temperature of frozen preparations of heavy microsomes from rat livers, HMGCoA reductase activity was solubilized due to limited proteolysis. This soluble enzyme was partially purified by fractionation with ammonium sulfate and filtration on Sephacryl S-200 column. The active enzyme was coeluted with a major 92 kDa-protein and was identified as a 58 kDa-protein after separation by SDS-PAGE and immunoblotting. Ethoxysilatrane, a hypocholesterolemic compound, which decreased the liver-microsomal activity of HMGCoA reductase on intra-peritonial treatment of animals, showed little effect on the enzyme activity with isolated microsomes or the 50 kDa-soluble enzyme when added in the assay. But it was able to inhibit the activity of the soluble 58 kDa-enzyme in a concentration-dependent, reversible manner. Cholesterol and an oxycholesterol were without effect whereas chlorophenoxyisobutyrate and ubiquinone showed small inhibition under these conditions. The extra region that links the active site domain (50 kDa protein) to the membrane, present in the 58 kDa-protein appears to be involved in mediating the inhibition by silatrane.

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Hypocholesterolemic action of 1-ethoxysilatrane

Cited by 6 publications

References 9 publications

Silatranes: a review on their synthesis, structure, reactivity and applications

Silatranes: a review on their synthesis, structure, reactivity and applications

Simple, low-cost synthetic route to potentially polymerizable silatranes

Preparation of a soluble 58kDa-3-hydroxy-3-methylglutaryl CoA reductase from liver microsomes and its inhibition by ethoxysilatrane, a hypocholesterolemic compound

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