Quercetin-6-C-β-d-glucopyranoside isolated from Ulmus wallichiana planchon is more potent than quercetin in inhibiting osteoclastogenesis and mitigating ovariectomy-induced bone loss in rats

Siddiqui, Jawed A.; Sharan, Kunal; Swarnkar, Gaurav; Rawat, Preeti; Kumar, M. N. V. Ravi; Manickavasagam, Lakshmi; Maurya, Rakesh; Pierroz, Dominique D.; Chattopadhyay, Naibedya

doi:10.1097/gme.0b013e3181e84e67

Cited by 39 publications

(45 citation statements)

References 33 publications

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“…Kaempferol is a flavanoid associated with good skeletal health [43,44]. It has been demonstrated to overcome the deleterious effect on bone density in oestrogen deficiency [43], to exhibit an antiosteoclastogenic effect [45,46] and to promote osteoblast differentiation [42].…”

Section: Nanotechnology For Osteoporosismentioning

confidence: 99%

Nanotechnology towards prevention of anaemia and osteoporosis: from concept to market

Shukla

Dasgupta

Ranjan

et al. 2017

Biotechnology & Biotechnological Equipment

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The application of nanotechnology in medicine, diagnostics, therapeutics, drug delivery, etc. in order to overcome the limitations faced by these fields has already been established. Anaemia and osteoporosis are two of the most widely prevalent iron and calcium deficiency diseases among women. Conventional drugs for both have their inherent limitations which can be overcome by nanotechnology. Nanonization of drugs has been established as a very efficient way to enhance the bioavailability and absorption of the drug in the gastrointestinal tract. In addition to this, encapsulation of drugs in solid lipid nanoparticles is also employed to increase the stability of the drug in the gastrointestinal tract and to facilitate its controlled release. Nanotechnology is also applied in bone tissue engineering to prepare bone grafts for bone injury. Nanotechnology-based bone grafts have shown to possess enhanced mechanical properties and better biocompatibility and osteoconduction than the conventional bone grafts. This review article highlights the research trends and challenges of nanotechnology based drugs to combat iron deficiency anaemia and osteoporosis. This review outlines the recent research trends in nano-drugs and touches on issues concerning the market, industries and patents pertaining to drugs for anaemia and osteoporosis. To provide the safety and risk factors of nanomaterials, we have briefly highlighted the toxicological aspects of nanomaterials used in drugs.

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Section: Nanotechnology For Osteoporosismentioning

confidence: 99%

Nanotechnology towards prevention of anaemia and osteoporosis: from concept to market

Shukla

Dasgupta

Ranjan

et al. 2017

Biotechnology & Biotechnological Equipment

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“…5A and B), whereas PPARg agonist Pio significantly enhanced body weight 6 days onwards without altering feed intake GTDF, QCG, and DHQ were isolated from the stem bark of Ulmus wallichiana Planchon (19,(48)(49)(50). QR was prepared from stems of Cissus quadrangularis (51).…”

Section: Gtdf Fails To Improve Diabetic Phenotype In Bks-db/db Micementioning

confidence: 99%

Orally Active Osteoanabolic Agent GTDF Binds to Adiponectin Receptors, With a Preference for AdipoR1, Induces Adiponectin-Associated Signaling, and Improves Metabolic Health in a Rodent Model of Diabetes

et al. 2014

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Adiponectin is an adipocytokine that signals through plasma membrane–bound adiponectin receptors 1 and 2 (AdipoR1 and -2). Plasma adiponectin depletion is associated with type 2 diabetes, obesity, and cardiovascular diseases. Adiponectin therapy, however, is yet unavailable owing to its large size, complex multimerization, and functional differences of the multimers. We report discovery and characterization of 6-C-β-d-glucopyranosyl-(2S,3S)-(+)-5,7,3′,4′-tetrahydroxydihydroflavonol (GTDF) as an orally active adiponectin mimetic. GTDF interacted with both AdipoRs, with a preference for AdipoR1. It induced adiponectin-associated signaling and enhanced glucose uptake and fatty acid oxidation in vitro, which were augmented or abolished by AdipoR1 overexpression or silencing, respectively. GTDF improved metabolic health, characterized by elevated glucose clearance, β-cell survival, reduced steatohepatitis, browning of white adipose tissue, and improved lipid profile in an AdipoR1-expressing but not an AdipoR1-depleted strain of diabetic mice. The discovery of GTDF as an adiponectin mimetic provides a promising therapeutic tool for the treatment of metabolic diseases.

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“…Interestingly, a quercetin-like varient, quercetin-6-C-β-D-glucopyranoside isolated from Ulmus wallichiana planchon has been demonstrated to possess enhanced anti-osteoclastogenic activity and to mitigate ovariectomy-induced bone loss in rats (17).…”

Section: Introductionmentioning

confidence: 99%

Quercetin, a potent suppressor of NF-κB and Smad activation in osteoblasts

Weitzmann¹

2011

Int J Mol Med

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Abstract. Osteoclasts, the bone resorbing cells of the body, form when osteoclast precursors are exposed to the key osteoclastogenic cytokine receptor activator of NF-κB ligand (RANKL), a process requiring induction of NF-κB signaling. Quercetin is a ubiquitous plant-derived flavonoid with well documented antiinflammatory properties, in part, a consequence of its capacity to downmodulate the NF-κB signal transduction pathway. Consistent with this mechanism of action quercetin is reported to suppress osteoclastogenesis in vitro and prevent bone loss in ovariectomized mice in vivo. By contrast, the effect of quercetin on osteoblasts, the cells responsible for bone formation, is contradictory with conflicting reports of inhibition as well as stimulation. Given our previous reports that NF-κB antagonists promote osteoblast differentiation and activity, we compared the effects of quercetin on osteoclast and osteoblast differentiation and on NF-κB signal transduction in vitro. As expected, quercetin potently suppressed osteoclastogenesis and NF-κB activation induced by RANKL in osteoclast precursors. However, the same doses of quercetin had no effect on osteoblast mineralization, and failed to significantly alleviate the inhibitory effect of NF-κB-induced by TNFα, even though quercetin potently suppressed NF-κB activation in these cells. This apparent contradiction was explained by the fact that addition to its anti-NF-κB activity, quercetin also potently antagonized both TGFβ and BMP-2-induced Smad activation in osteoblast precursors. Taken together our data suggest that multiple competing actions of quercetin mediate both stimulatory and inhibitory actions on osteoblasts with the final physiological effect likely a function of the net balance between these stimulatory and inhibitory effects.

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Quercetin-6-C-β-d-glucopyranoside isolated from Ulmus wallichiana planchon is more potent than quercetin in inhibiting osteoclastogenesis and mitigating ovariectomy-induced bone loss in rats

Abstract: QCG improves bone biomechanical quality more effectively than Q through positive modifications of bone mineral density and bone microarchitecture without a hyperplastic effect on the uterus.

Cited by 39 publications

References 33 publications

Nanotechnology towards prevention of anaemia and osteoporosis: from concept to market

Nanotechnology towards prevention of anaemia and osteoporosis: from concept to market

Orally Active Osteoanabolic Agent GTDF Binds to Adiponectin Receptors, With a Preference for AdipoR1, Induces Adiponectin-Associated Signaling, and Improves Metabolic Health in a Rodent Model of Diabetes

Quercetin, a potent suppressor of NF-κB and Smad activation in osteoblasts

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