- Preparation of ORMOSIL nanoparticles conjugated with vitamin D3 analogues and their biological evaluation
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Dye-doped, 90 nm diameter, multifunctional organically modified silica (ORMOSIL) nanoparticles were prepared by condensation of vinyltriethoxysilane within surfactant-stabilized microemulsions and conjugated with several vitamin D3 derivatives. For this, vitamin D analogues possessing at least one hydroxyl group derivatized as vinylcarbonate have been synthesized. These analogues were conjugated to ORMOSIL nanoparticles through the carbonate function, forming carbamate derivatives of vitamin D nanoparticles. The interaction between these nanoparticles and human serum albumin, which is one of the serum transporters of the insoluble vitamin D3, was investigated by surface plasmon resonance. The results obtained revealed that this approach allows obtaining water-soluble vitamin D3 derivatives, which maintain their full protein binding ability.
- González-García, Tania,Fernández, Susana,Lubian, Elisa,Mancin, Fabrizio,Ferrero, Miguel
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- Preparation method of 25-hydroxyvitamin D3, 1alpha, 25-dihydroxyvitamin D3 and isotope internal standard compound thereof
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The invention discloses a preparation method of 25-hydroxyvitamin D3 and 1alpha, 25-dihydroxyvitamin D3 and an isotope internal standard compound thereof. The preparation method comprises the following steps: a compound III is subjected to SO2 conjugate protection, O3 oxidation, NaBH4 reduction, iodination ring opening, conjugate addition with acrylate, and reaction with a methyl Grignard reagentor isotope labeled methyl Grignard reagent, a silicon protecting group is removed under the action of TBAF, and a product is obtained through ultraviolet irradiation configuration inversion under thecatalysis of 9-acetyl anthracene. The method is good in reaction selectivity, high in total yield, simple and convenient to operate and short in isotope introduction step, and the isotope utilizationrate is greatly increased.
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- 1α,25-Dihydroxyvitamin D3-3β-bromoacetate, a potential cancer therapeutic agent: Synthesis and molecular mechanism of action
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Synthesis of 1α,25-dihydroxyvitamin D3-3β- bromoacetate (1,25(OH)2D3-3-BE), a potential anti-cancer agent is presented. We also report that mechanism of action of 1,25(OH) 2D3-3-BE may involve reducti
- Ray, Rahul,Lambert, James R.
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p. 2537 - 2540
(2011/06/11)
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