739898

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Phosphate overload directly induces systemic inflammation and malnutrition as well as vascular calcification in uremia.

Shunsuke Yamada et al.

American journal of physiology. Renal physiology, 306(12), F1418-F1428 (2014-05-09)

Hyperphosphatemia contributes to increased cardiovascular mortality through vascular calcification (VC) in patients with chronic kidney disease (CKD). Malnutrition and inflammation are also closely linked to an increased risk of cardiovascular death in CKD. However, the effects of Pi overload on

1,25-Dihydroxy vitamin D3 downregulates pro-inflammatory cytokine response in pulmonary tuberculosis.

M Harishankar et al.

International immunopharmacology, 23(1), 148-152 (2014-09-10)

1,25-Dihydroxy vitamin D3 [1,25(OH)2D3] is a potent immunomodulator and regulates various immune responses to Mycobacterium tuberculosis (Mtb). The present study aimed to understand the effect of 1,25(OH)2D3 on pro-inflammatory cytokine response to Mtb antigen. Peripheral blood mononuclear cells from 42

Inhibition of Mouse Breast Tumor-Initiating Cells by Calcitriol and Dietary Vitamin D.

Youngtae Jeong et al.

Molecular cancer therapeutics, 14(8), 1951-1961 (2015-05-03)

The anticancer actions of vitamin D and its hormonally active form, calcitriol, have been extensively documented in clinical and preclinical studies. However, the mechanisms underlying these actions have not been completely elucidated. Here, we examined the effect of dietary vitamin

Kruppel-like factors in an endothelial and vascular smooth muscle cell coculture model: impact of a diabetic environment and vitamin D.

Tali Zitman-Gal et al.

In vitro cellular & developmental biology. Animal, 51(5), 470-478 (2015-03-07)

Endothelial cells (EC) and vascular smooth muscle cells (VSMC) are involved in the development of local and diffuse vasculopathies by participating in inflammatory processes that can lead to uncontrolled vascular complications. Our aim was to study the possible interactions of

Identification of differentiation-stage specific markers that define the ex vivo osteoblastic phenotype.

Natalie A Twine et al.

Bone, 67, 23-32 (2014-07-02)

The phenotype of osteoblastic (OB) cells in culture is currently defined using a limited number of markers of low sensitivity and specificity. For the clinical use of human skeletal (stromal, mesenchymal) stem cells (hMSC) in therapy, there is also a

Differential antitumor effects of vitamin D analogues on colorectal carcinoma in culture.

J M Wierzbicka et al.

International journal of oncology, 47(3), 1084-1096 (2015-08-12)

Colorectal cancer (CRC) is an emerging global problem with the rapid increase in its incidence being associated with an unhealthy lifestyle. Epidemiological studies have shown that decreased levels of vitamin D3 significantly increases the risk of CRC. Furthermore, negative effects

A new class of vitamin D analogues that induce structural rearrangement of the ligand-binding pocket of the receptor.

Yuka Inaba et al.

Journal of medicinal chemistry, 52(5), 1438-1449 (2009-02-06)

To identify novel vitamin D receptor (VDR) ligands that induce a novel architecture within the ligand-binding pocket (LBP), we have investigated eight 22-butyl-1alpha,24-dihydroxyvitamin D(3) derivatives (3-10), all having a butyl group as the branched alkyl side chain. We found that

'Novel alkyl side chain sulfone 1alpha,25-dihydroxyvitamin D3 analogs: a comparison of in vitro antiproliferative activities and in vivo calcemic activities'.

Aimee R Usera et al.

Bioorganic & medicinal chemistry, 17(15), 5627-5631 (2009-07-07)

The replacement of a t-butyl group with a trifluoromethyl group has profound effects on the biological profile of 1alpha,25-dihydroxyvitamin D(3) sulfone analogs. Investigation of whether the improved biological activities are due to steric and electronic factors of the trifluoromethyl group

Porphyromonas gulae 41-kDa fimbriae induced osteoclast differentiation and cytokine production.

Haruka Sasaki et al.

The Journal of veterinary medical science, 77(3), 265-271 (2014-11-26)

Porphyromonas gulae is considered to be associated with canine periodontitis. We have previously reported that the P. gulae American Type Culture Collection (ATCC) 51700 comprised 41-kDa fimbriae. The purpose of the present study was to demonstrate the roles of 41-kDa

Inhibitory effects of French pine bark extract, Pycnogenol®, on alveolar bone resorption and on the osteoclast differentiation.

Hideki Sugimoto et al.

Phytotherapy research : PTR, 29(2), 251-259 (2014-10-23)

Pycnogenol(®) (PYC) is a standardized bark extract from French maritime pine (Pinus pinaster Aiton). We examined the inhibitory effects of PYC on alveolar bone resorption, which is a characteristic feature of periodontitis, induced by Porphyromonas gingivalis (P. gingivalis) and osteoclast differentiation.

Evaluation of vitamin D3 A-ring analogues as Hedgehog pathway inhibitors.

Upasana Banerjee et al.

Bioorganic & medicinal chemistry letters, 22(3), 1330-1334 (2012-01-10)

A structure-activity relationship study focusing on the A-ring of vitamin D3 (VD3) was undertaken to elucidate its role in inhibiting the Hedgehog pathway and in mediating anti-cancer effects. Analogues resulting from simple functional group substitution at 3' position of VD3

Increased CYP24A1 expression is associated with BRAF(V600E) mutation and advanced stages in papillary thyroid carcinoma.

Minjing Zou et al.

Clinical endocrinology, 81(1), 109-116 (2014-01-03)

1α, 25(OH)2 D3 (calcitriol), the active form of vitamin D, has been shown to exert antiproliferative effects in many cancers. Overexpression of CYP24A1, the primary vitamin D-inactivating enzyme, is also observed in a variety of human cancers, thus potentially neutralizing

Synthesis and biological properties of 2-methylene-19-nor-25-dehydro-1alpha-hydroxyvitamin D(3)-26,23-lactones--weak agonists.

Grazia Chiellini et al.

Bioorganic & medicinal chemistry, 16(18), 8563-8573 (2008-08-30)

In a continuing effort to explore the 2-methylene-1alpha-hydroxy-19-norvitamin D(3) class of pharmacologically important vitamin D compounds, two novel 2-methylene-19-nor-25-dehydro-1alpha-hydroxyvitamin D(3)-26,23-lactones, GC-3 and HLV, were synthesized and biologically tested. Based on reports of similarly structured molecules, it was hypothesized that these

Vitamin D and estrogen synergy in Vdr-expressing CD4(+) T cells is essential to induce Helios(+)FoxP3(+) T cells and prevent autoimmune demyelinating disease.

Justin A Spanier et al.

Journal of neuroimmunology, 286, 48-58 (2015-08-25)

Multiple sclerosis (MS) is a neurodegenerative disease resulting from an autoimmune attack on the axon-myelin unit. A female MS bias becomes evident after puberty and female incidence has tripled in the last half-century, implicating a female sex hormone interacting with

The active form of vitamin D, calcitriol, induces a complex dual upregulation of endothelin and nitric oxide in cultured endothelial cells.

Patricia Martínez-Miguel et al.

American journal of physiology. Endocrinology and metabolism, 307(12), E1085-E1096 (2014-10-23)

Despite the presence of vitamin D receptor (VDR) in endothelial cells, the effect of vitamin D on endothelial function is unknown. An unbalanced production of vasoactive endothelial factors such as nitric oxide (NO) or endothelin-1 (ET-1) results in endothelial dysfunction

Vitamin D deficiency promotes nonalcoholic steatohepatitis through impaired enterohepatic circulation in animal model.

Ming Kong et al.

American journal of physiology. Gastrointestinal and liver physiology, 307(9), G883-G893 (2014-09-13)

Vitamin D deficiency (VDD) or insufficiency is recognized for its association with nonalcoholic steatohepatitis (NASH), whereas the underlying mechanism remains unknown. Using animal models, we found that vitamin D deficiency promoted the high-fat diet (HFD)-initiated simple steatosis into typical NASH

Convergent synthesis of double point modified analogs of 1α, 25-dihydroxyvitamin D2 for biological evaluation

Nadkarni S, et al.

The Journal of Steroid Biochemistry and Molecular Biology, 164, 45-49 (2016)

PLGA nanoparticles as a platform for vitamin D-based cancer therapy.

Maria J Ramalho et al.

Beilstein journal of nanotechnology, 6, 1306-1318 (2015-07-23)

Poly(lactic-co-glycolic acid) (PLGA) nanoparticles were studied as drug delivery vehicles for calcitriol, the active form of vitamin D3. In vitro effects of calcitriol encapsulated in PLGA nanoparticles were evaluated with respect to free calcitriol on human pancreatic cell lines, S2-013

13,13-Dimethyl-des-C,D analogues of (20S)-1α,25-dihydroxy-2-methylene-19-norvitamin D₃ (2MD): total synthesis, docking to the VDR, and biological evaluation.

Katarzyna Plonska-Ocypa et al.

Bioorganic & medicinal chemistry, 19(23), 7205-7220 (2011-10-25)

As a continuation of our studies focused on the vitamin D compounds lacking the C,D-hydrindane system, 13,13-dimethyl-des-C,D analogues of (20S)-1α,25-dihydroxy-2-methylene-19-norvitamin D(3) (2, 2MD) were prepared by total synthesis. The known cyclohexanone 30, a precursor of the desired A-ring phosphine oxide

Removal of the 26-methyl group from 19-nor-1α,25-dihydroxyvitamin D₃ markedly reduces in vivo calcemic activity without altering in vitro VDR binding, HL-60 cell differentiation, and transcription.

Pawel Grzywacz et al.

Journal of medicinal chemistry, 53(24), 8642-8649 (2010-11-26)

Twelve new analogues of 19-nor-1α,25-dihydroxyvitamin D₃ (5-16) were prepared by convergent syntheses, employing the Wittig-Horner reaction. The necessary Grundmann type ketones (45-48), possessing fixed configurations of the hydroxyl group at C-25, were obtained by a multistep procedure from commercial vitamin

Association of vitamin D3 with alveolar bone regeneration in dogs.

Hsiang-Hsi Hong et al.

Journal of cellular and molecular medicine, 19(6), 1208-1217 (2015-03-11)

Designed sockets prepared on the mandibles of nine Beagle dogs were divided into three groups: Calcitriol +Alloplast, Alloplast and Empty. Five of the nine dogs received Vit.D3 and calcium supplement (Vit.D/Ca group), while the other four dogs without supplements were

Rotenoids and flavonoids with anti-invasion of HT1080, anti-proliferation of U937, and differentiation-inducing activity in HL-60 from Erycibe expansa.

Hisashi Matsuda et al.

Bioorganic & medicinal chemistry, 15(3), 1539-1546 (2006-12-13)

Principal rotenoids (deguelin, tephrosin, rotenone, and 12a-hydroxyrotenone) (3-30microM) isolated from the stems of Erycibe expansa significantly inhibited invasion of human fibrosarcoma HT1080 cells through Matrigel-coated filters and release of proMMPs-2 and 9. In addition, deguelin and tephrosin showed differentiation-inducing activity

Suppression of murine experimental autoimmune encephalomyelitis development by 1,25-dihydroxyvitamin D3 with autophagy modulation.

Chao Zhen et al.

Journal of neuroimmunology, 280, 1-7 (2015-03-17)

Multiple sclerosis (MS) has been associated with a history of sub-optimal exposure to ultraviolet light, implicating vitamin D3 as a possible protective agent. We evaluated whether 1,25(OH)2D3 attenuates the progression of experimental autoimmune encephalomyelitis (EAE), and explored its potential mechanisms.

Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).

Zhichao Liu et al.

PLoS computational biology, 7(12), e1002310-e1002310 (2011-12-24)

Drug-induced liver injury (DILI) is a significant concern in drug development due to the poor concordance between preclinical and clinical findings of liver toxicity. We hypothesized that the DILI types (hepatotoxic side effects) seen in the clinic can be translated

Local administration of calcitriol positively influences bone remodeling and maturation during restoration of mandibular bone defects in rats.

Hongrui Liu et al.

Materials science & engineering. C, Materials for biological applications, 49, 14-24 (2015-02-18)

The aim of this study was to investigate the influence of calcitriol on osteoinduction following local administration into mandibular bone defects. Calcitriol-loaded absorbable collagen membrane scaffolds were prepared using the polydopamine coating method and characterized by scanning electron microscopy. Composite

Hologram QSAR model for the prediction of human oral bioavailability.

Tiago L Moda et al.

Bioorganic & medicinal chemistry, 15(24), 7738-7745 (2007-09-18)

A drug intended for use in humans should have an ideal balance of pharmacokinetics and safety, as well as potency and selectivity. Unfavorable pharmacokinetics can negatively affect the clinical development of many otherwise promising drug candidates. A variety of in

Noninvasive Optical Imaging of UV-Induced Squamous Cell Carcinoma in Murine Skin: Studies of Early Tumor Development and Vitamin D Enhancement of Protoporphyrin IX Production.

Kishore R Rollakanti et al.

Photochemistry and photobiology, 91(6), 1469-1478 (2015-08-01)

Better noninvasive techniques are needed to monitor protoporphyrin IX (PpIX) levels before and during photodynamic therapy (PDT) of squamous cell carcinoma (SCC) of the skin. Our aim was to evaluate (1) multispectral fluorescent imaging of ultraviolet light (UV)-induced cancer and

Calcitriol promotes augmented dopamine release in the lesioned striatum of 6-hydroxydopamine treated rats.

Wayne A Cass et al.

Neurochemical research, 39(8), 1467-1476 (2014-05-27)

Current therapies for Parkinson's disease (PD) offer symptomatic relief but do not provide a cure or slow the disease process. Treatments that could halt progression of the disease or help restore function to damaged neurons would be of substantial benefit.

Calcitriol May Down-Regulate mRNA Over-Expression of Toll-Like Receptor-2 and -4, LL-37 and Proinflammatory Cytokines in Cultured Human Keratinocytes.

Mi Sook Jeong et al.

Annals of dermatology, 26(3), 296-302 (2014-06-27)

Although vitamin D analogs have been used in the topical treatment of psoriasis, their mechanisms of action are not well understand. Calcitriol, the hormonally active vitamin D3 metabolite, has been demonstrated to exert immunomodulatory effects in the skin by down-regulating

In vivo dual targeting of the oncogenic Ether-à-go-go-1 potassium channel by calcitriol and astemizole results in enhanced antineoplastic effects in breast tumors.

Janice García-Quiroz et al.

BMC cancer, 14, 745-745 (2014-10-05)

The oncogenic ether-à-go-go-1 potassium channel (EAG1) activity and expression are necessary for cell cycle progression and tumorigenesis. The active vitamin D metabolite, calcitriol, and astemizole, a promising antineoplastic drug, target EAG1 by inhibiting its expression and blocking ion currents, respectively.

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