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Proposal of novel inhibitors for vitamin-D receptor: Molecular docking, molecular mechanics and ab initio molecular orbital simulations.
Biophys Chem
March 2021
Department of Computer Science and Engineering, Toyohashi University of Technology, Tempaku-cho, Toyohashi, Aichi 441-8580, Japan. Electronic address:
The specific binding of active vitamin-D to the vitamin-D receptor (VDR) is closely related to the onset of immunological diseases. To inhibit the binding, various compounds have been developed as potent inhibitors against VDR. Among them, a compound NS-54c, which was developed based on the first VDR antagonist TEI-9647 (25-dehydro-1α-hydroxyvitamin D-26,23-lactone), was revealed to posse almost 1000-fold improved antagonistic activity over the original TEI-9647.
View Article and Find Full Text PDFThe effects of eggshell calcium (Biomin H ) and its combinations with alfacalcidol (1α-hydroxyvitamin D3) and menaquinone-7 (vitamin K2) on ovariectomy-induced bone loss in a rat model of osteoporosis.
J Anim Physiol Anim Nutr (Berl)
March 2021
Centre of Experimental Medicine, Institute of Experimental Pharmacology and Toxicology, Slovak Academy of Sciences, Bratislava, Slovakia.
The purpose of this study was to investigate the impact of eggshell calcium (Biomin H dietary supplement) and its combinations with alfacalcidol (1α-hydroxyvitamin D ) and menaquinone-7 (vitamin K ) on ovariectomy-induced bone loss in rats. Adult female rats (n = 48) were divided into 6 groups of 8 individuals each: sham-operated rats (SHAM); ovariectomized (OVX) rats untreated; OVX rats treated with Biomin H (BIO); OVX rats simultaneously receiving Biomin H , vitamin D (BIO + D ); OVX rats simultaneously treated with Biomin H , vitamin K (BIO + K ) and OVX rats treated with Biomin H , vitamin D , vitamin K (BIO + D + K ) during 8 weeks. Biochemical parameters, bone mineral density (BMD), bone mineral content (BMC) and femoral bone microstructure were determined.
View Article and Find Full Text PDFEffects of Vitamin D Analogs Alfacalcidol and Calcitriol on Cell Proliferation and Migration of HEC1A Endometrial Adenocarcinoma Cells.
Nutr Cancer
August 2021
Department of Medical Pharmacology, Faculty of Medicine, University of Mersin, Mersin, Turkey.
Endometrial carcinoma is the most diagnosed among infiltrating tumor of the female genital tract. Vitamin D has antiproliferative and immunomodulatory properties besides its classical effect on calcium and phosphate. We aimed to demonstrate whether alfacalcidol and calcitriol have any effect on proliferation and migration.
View Article and Find Full Text PDFStrategies and limitations associated with in vitro characterization of vitamin D receptor activators.
Biochem Pharmacol
September 2018
Department of Pharmaceutical Sciences, Leslie Dan Faculty of Pharmacy, University of Toronto, Toronto, Ontario, Canada. Electronic address:
In vitro cell-based assays are common screening tools used for the identification of new VDR ligands. For 25-hydroxyvitamin D [25(OH)D] and 1α-hydroxyvitamin D [1α(OH)D], protein expressions of CYP2R1 and CYP27B1, respectively, that form the active 1α,25-dihydroxyvitamin D [1,25(OH)D] ligand were detected in human embryonic kidney (HEK293) cells expressing the GAL4-hVDR, the human brain microvessel endothelial (hCMEC/D3) and adenocarcinoma colonic (Caco-2) cells. The impact of bioactivation enzymes was shown upon the addition of ketoconazole (10 μM KTZ), a pan-CYP inhibitor, which reduced the apparent potency of 25(OH)D and increased the EC from 272 to 608 nM in HEK293 cells.
View Article and Find Full Text PDFBiochemical Characterization of the Cytochrome P450 CYP107CB2 from Bacillus lehensis G1.
Protein J
April 2018
Faculty of Health and Life Sciences, Management and Science University, 40100, Shah Alam, Selangor, Malaysia.
The bioconversion of vitamin D3 catalyzed by cytochrome P450 (CYP) requires 25-hydroxylation and subsequent 1α-hydroxylation to produce the hormonal activated 1α,25-dihydroxyvitamin D3. Vitamin D3 25-hydroxylase catalyses the first step in the vitamin D3 biosynthetic pathway, essential in the de novo activation of vitamin D3. A CYP known as CYP107CB2 has been identified as a novel vitamin D hydroxylase in Bacillus lehensis G1.
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