A phosphorylated phloretin derivative. Synthesis and  effect on intestinal Na<sup>+</sup>-dependent phosphate absorption

Peerce, Brian E.; Clarke, Rebecca

doi:10.1152/ajpgi.00308.2001

Cited by 13 publications

(5 citation statements)

References 34 publications

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“…In severe renal failure and end‐stage renal disease, one possible therapeutic target to control hyperphosphatemia is the development of compounds that inhibit intestinal sodium‐dependent Pi cotransporters (12–15). Inhibiting intestinal Pi absorption by inhibition of type IIb transporter by FGF23 would be a desirable method to control serum Pi levels in patients with chronic renal disease (CRF) or undergoing dialysis.…”

Section: Discussionmentioning

confidence: 99%

Inhibition of Intestinal Sodium‐dependent Inorganic Phosphate Transport by Fibroblast Growth Factor 23

et al. 2005

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The mechanisms by which fibroblast growth factor 23 (FGF23) alters inorganic phosphate (Pi) homeostasis is not entirely clear. In the present study, we examined the effect of FGF23 on intestinal sodium-dependent Pi transport in mice. Injection of FGF23(R179Q) markedly reduced serum Pi and 1,25(OH)2D3 levels in normal mice. Those animals show the reduction of intestinal sodium-dependent Pi transport activity and the amount of type IIb sodium-dependent Pi cotransporter (type IIb NaPi) protein in the brush border membrane vesicles. In vitamin D receptor null mice (VDR-/-), FGF23(R179Q) had no effect on intestinal sodium-dependent Pi transport activity and type IIb NaPi protein levels. The present study suggests that FGF23(R179Q) reduces intestinal sodium-dependent Pi transport activity and type IIb NaPi protein levels by a mechanism that is dependent on VDR.

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Section: Discussionmentioning

confidence: 99%

Inhibition of Intestinal Sodium‐dependent Inorganic Phosphate Transport by Fibroblast Growth Factor 23

et al. 2005

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“…Phosphonoformate (PFA, a phosphonocarboxylate) has a K i value of 0.37 mM in rat small intestine BBMVs, which indicates a low affinity of NPT2b for PFA as compared to P i [ 115 ]. 2′-Phosphophloretin (2′-PP), a derivative of the plant chalcone phloretin, more strongly inhibits Na + -dependent P i uptake, with K i values of 38 ± 7 nM in rabbit intestinal BBMVs and 42 ± 8 nM in rat intestinal BBMVs [ 116 ]. Pentavalent arsenate can be transported by NPT2b and also acts as a competitive inhibitor of NPT2b (K i = 51 µM for rat Npt2b in Xenopus oocytes) [ 115 ].…”

Section: Disorders Of Phosphate Homeostasismentioning

confidence: 99%

Importance of Dietary Phosphorus for Bone Metabolism and Healthy Aging

Serna

Bergwitz

2020

Nutrients

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Inorganic phosphate (Pi) plays a critical function in many tissues of the body: for example, as part of the hydroxyapatite in the skeleton and as a substrate for ATP synthesis. Pi is the main source of dietary phosphorus. Reduced bioavailability of Pi or excessive losses in the urine causes rickets and osteomalacia. While critical for health in normal amounts, dietary phosphorus is plentiful in the Western diet and is often added to foods as a preservative. This abundance of phosphorus may reduce longevity due to metabolic changes and tissue calcifications. In this review, we examine how dietary phosphorus is absorbed in the gut, current knowledge about Pi sensing, and endocrine regulation of Pi levels. Moreover, we also examine the roles of Pi in different tissues, the consequences of low and high dietary phosphorus in these tissues, and the implications for healthy aging.

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“…When given to hemodialysis patients, oral nicotinamide reduced hyperphosphatemia (128), although treatment was associated with significant gastrointestinal side effects that may limit its clinical usefulness. Phosphophloretin, a phosphorylated form of the plant chalcone phloretin, has been shown to be a competitive inhibitor of renal (100) and intestinal sodium-dependent phosphate transport in rabbits (98), rats (98), and humans (99) and to reduce serum phosphate levels in normal (98) and uremic rats (101). Finally, JTP-59557, a triazole derivative, is a noncompetitive inhibitor of phosphate transport across the rat small intestine in vivo, which is probably due to an action on NaPi-IIb (82).…”

Section: Intestinal Phosphate Transport In Crfmentioning

confidence: 99%

Phosphate homeostasis and the renal-gastrointestinal axis

Marks¹,

Debnam²,

Unwin

2010

American Journal of Physiology-Renal Physiology

180

154

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Transport of phosphate across intestinal and renal epithelia is essential for normal phosphate balance, yet we know less about the mechanisms and regulation of intestinal phosphate absorption than we do about phosphate handling by the kidney. Recent studies have provided strong evidence that the sodium-phosphate cotransporter NaPi-IIb is responsible for sodium-dependent phosphate absorption by the small intestine, and it might be that this protein can link changes in dietary phosphate to altered renal phosphate excretion to maintain phosphate balance. Evidence is also emerging that specific regions of the small intestine adapt differently to acute or chronic changes in dietary phosphate load and that phosphatonins inhibit both renal and intestinal phosphate transport. This review summarizes our current understanding of the mechanisms and control of intestinal phosphate absorption and how it may be related to renal phosphate reabsorption; it also considers the ways in which the gut could be targeted to prevent, or limit, hyperphosphatemia in chronic and end-stage renal failure.

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A phosphorylated phloretin derivative. Synthesis and effect on intestinal Na⁺-dependent phosphate absorption

Abstract: Peerce, Brian E., and Rebecca Clarke. A phosphorylated phloretin derivative. Synthesis and effect on intestinal Na ϩ -dependent phosphate absorption.

Cited by 13 publications

References 34 publications

Inhibition of Intestinal Sodium‐dependent Inorganic Phosphate Transport by Fibroblast Growth Factor 23

Inhibition of Intestinal Sodium‐dependent Inorganic Phosphate Transport by Fibroblast Growth Factor 23

Importance of Dietary Phosphorus for Bone Metabolism and Healthy Aging

Phosphate homeostasis and the renal-gastrointestinal axis

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A phosphorylated phloretin derivative. Synthesis and effect on intestinal Na+-dependent phosphate absorption

Abstract: Peerce, Brian E., and Rebecca Clarke. A phosphorylated phloretin derivative. Synthesis and effect on intestinal Na ϩ -dependent phosphate absorption.

Cited by 13 publications

References 34 publications

Inhibition of Intestinal Sodium‐dependent Inorganic Phosphate Transport by Fibroblast Growth Factor 23

Inhibition of Intestinal Sodium‐dependent Inorganic Phosphate Transport by Fibroblast Growth Factor 23

Importance of Dietary Phosphorus for Bone Metabolism and Healthy Aging

Phosphate homeostasis and the renal-gastrointestinal axis

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Product

Resources

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A phosphorylated phloretin derivative. Synthesis and effect on intestinal Na⁺-dependent phosphate absorption