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Phloridzin AND Beta cells

Katsutoshi Miyagawa, Tatsuya Kondo, Rieko Goto, Rina Matsuyama, Kaoru Ono, Sayaka Kitano, Shuji Kawasaki, Motoyuki Igata, Junji Kawashima, Takeshi Matsumura, Hiroyuki Motoshima, Eiichi Araki
BACKGROUND: Dipeptidyl peptidase-4 (DPP-4) inhibitors modulate incretin hormones and exert anti-diabetic effects in type 2 diabetes mellitus. Treatment with angiotensin II type 1 receptor blockers (ARB) is a proven successful intervention for hypertension with type 2 diabetes. The present study investigated the combined effects of the DPP-4 inhibitor vildagliptin and the ARB valsartan in a mouse model of type 2 diabetes. METHODS: C57BL/6 J mice fed with high-fat diet (HFD) or db/db mice were treated with placebo, phloridzin (PHZ), vildagliptin alone (ViL), valsartan alone (VaL) or ViL with VaL (ViLVaL) for 8 weeks...
2013: Cardiovascular Diabetology
Eitan M Akirav, Maria-Teresa Baquero, Lynn W Opare-Addo, Michael Akirav, Eva Galvan, Jake A Kushner, David L Rimm, Kevan C Herold
OBJECTIVE: β-Cell and islet endothelial cell destruction occurs during the progression of type 1 diabetes, but, paradoxically, β-cell proliferation is increased during this period. Altered glucose tolerance may affect β-cell mass and its association with endothelial cells. Our objective was to study the effects of glucose and inflammation on islet vascularity and on β function, mass, and insulin in immunologically tolerant anti-CD3 monoclonal antibody (mAb)-treated and prediabetic NOD mice...
March 2011: Diabetes
Junzhi Wang, Mi Hwa Chung, Bingjie Xue, Hong Ma, Chaomei Ma, Masao Hattori
Phloridzin, a phloretin 2'-beta-D-glucoside, belongs to dihydrochalcones and mainly exists in the fruits of Malus pumila Mill., Lithocarpus polystachyus REHD and the root skins, stems, tender leaves and fruits of Malus hupehensis. It has many pharmacological activities, such as regulating blood sugar level and blood pressure, protecting heart, scavenging of oxygen free radicals and antioxidant injuries. Thus, market demand of products containing phloridzin is increasing year by year. Our research results demonstrated that phloridzin is provided with a double directional adjusting function of estrogenic and antiestrogenic activities...
2010: Biological & Pharmaceutical Bulletin
Sachin A Paranjape, Owen Chan, Wanling Zhu, Adam M Horblitt, Ewan C McNay, James A Cresswell, Jonathan S Bogan, Rory J McCrimmon, Robert S Sherwin
OBJECTIVE: Insulin released by the beta-cell is thought to act locally to regulate glucagon secretion. The possibility that insulin might also act centrally to modulate islet glucagon secretion has received little attention. RESEARCH DESIGN AND METHODS: Initially the counterregulatory response to identical hypoglycemia was compared during intravenous insulin and phloridzin infusion in awake chronically catheterized nondiabetic rats. To explore whether the disparate glucagon responses seen were in part due to changes in ventromedial hypothalamus (VMH) exposure to insulin, bilateral guide cannulas were inserted to the level of the VMH and 8 days later rats received a VMH microinjection of either 1) anti-insulin affibody, 2) control affibody, 3) artificial extracellular fluid, 4) insulin (50 microU), 5) insulin receptor antagonist (S961), or 6) anti-insulin affibody plus a gamma-aminobutyric acid A (GABA(A)) receptor agonist muscimol, prior to a hypoglycemic clamp or under baseline conditions...
June 2010: Diabetes
Jordi Altirriba, Albert Barbera, Héctor Del Zotto, Belen Nadal, Sandra Piquer, Alex Sánchez-Pla, Juan J Gagliardino, Ramon Gomis
BACKGROUND: Sodium tungstate is known to be an effective anti-diabetic agent, able to increase beta cell mass in animal models of diabetes, although the molecular mechanisms of this treatment and the genes that control pancreas plasticity are yet to be identified. Using a transcriptomics approach, the aim of the study is to unravel the molecular mechanisms which participate in the recovery of exocrine and endocrine function of streptozotocin (STZ) diabetic rats treated with tungstate, determining the hyperglycemia contribution and the direct effect of tungstate...
2009: BMC Genomics
Eun-Gyoung Hong, Dae Young Jung, Hwi Jin Ko, Zhiyou Zhang, Zhexi Ma, John Y Jun, Jae Hyeong Kim, Andrew D Sumner, Thomas C Vary, Thomas W Gardner, Sarah K Bronson, Jason K Kim
Although insulin resistance has been traditionally associated with type 2 diabetes, recent evidence in humans and animal models indicates that insulin resistance may also develop in type 1 diabetes. A point mutation of insulin 2 gene in Ins2(Akita) mice leads to pancreatic beta-cell apoptosis and hyperglycemia, and these mice are commonly used to investigate type 1 diabetes and complications. Since insulin resistance plays an important role in diabetic complications, we performed hyperinsulinemic-euglycemic clamps in awake Ins2(Akita) and wild-type mice to measure insulin action and glucose metabolism in vivo...
December 2007: American Journal of Physiology. Endocrinology and Metabolism
Melanie Kern, Gudrun Pahlke, Yufanyi Ngiewih, Doris Marko
Glycogen synthase kinase-3beta (GSK3beta) is one of the key elements of the Wnt pathway involved in the regulation of beta-catenin homeostasis. The inhibition of GSK3beta kinase activity might lead to the onset of beta-catenin/TCF/LEF-mediated gene transcription, representing a potentially mitogenic stimulus. Apple polyphenols have been shown to mediate several biological effects that might be of interest with respect to chemoprevention. The objective of the study was to elucidate whether apple polyphenols also modulate key elements of the Wnt pathway, an effect that might limit the usefulness of these compounds for the prevention of carcinogenesis...
September 20, 2006: Journal of Agricultural and Food Chemistry
Takashi Mizuma, Norihiko Fuseda, Masahiro Hayashi
Glycosidase activity influences the intestinal absorption of glycosides. Our previous study in rats suggested that disaccharide conjugates might be prototypes for pre-prodrugs aiming at the Na(+)/glucose co-transporter-mediated transport of prodrugs (drug glucoside) as a novel absorption pathway. One of the crucial factors is the formation of a glucoside drug from the disaccharide conjugate. Since there is a large species difference in metabolism, it is necessary to examine the cells and/or enzymes derived from human tissue to confirm this concept...
May 2005: Journal of Pharmacy and Pharmacology
Katalin Ugocsai, Andreas Varga, Péter Molnár, Sándor Antus, Joseph Molnár
The effects of various flavonoids and carotenoids on Rhodamine 123 accumulation in multidrug-resistant Colo 320 human colon cancer cells expressing MDR1/LRP were studied. The Colo 205 cell line was used as a drug-sensitive control. Rotenon, Catechin, Neohesperidin, Naringin, Robinin, Phloridzin, Robinetin, Dihydrobinetin, Dihydrofisetin, Kampferol, Dihidroquercetin, Sakuranin and Sakuranetin were tested on Colo 320 cells: only Rotenon was found to be effective as regards multidrug resistance (MDR) reversal, while a majority of the flavonoids, such as Catechin, Neohesperidin, Naringin, Robinin, Phloridzin, Dihydrobinetin and Sakuranetin, had only marginal effects on Rhodamine 123 accumulation...
March 2005: In Vivo
Akira Ikari
Exposure of cells or organs to sublethal stress induces the expression of some heat-shock proteins (Hsp), including Hsp70. In porcine renal LLC-PK(1) cells, heat stress (HS) elevates Hsp70 expression and Na(+)-dependent glucose transport. We examined whether Na(+)-dependent glucose transporter (SGLT1) interacts with Hsp70 to elevate SGLT1 activity and whether SGLT1 activation is involved in the recovery from HS injury. HS (42 degrees C for 3 h) elevated SGLT1 activity and expression of SGLT1 in the apical membrane fraction...
December 2004: Yakugaku Zasshi: Journal of the Pharmaceutical Society of Japan
Hong Zhao, Shoshana Yakar, Oksana Gavrilova, Hui Sun, Yang Zhang, Hyunsook Kim, Jennifer Setser, William Jou, Derek LeRoith
The chronic hyperglycemia that occurs in type 2 diabetes may cause deterioration of beta-cell function and insulin resistance in peripheral tissues. Mice that express a dominant-negative IGF-1 receptor, specifically in skeletal muscle (MKR mice), exhibit severe insulin resistance, hyperinsulinemia, dyslipidemia, and hyper-glycemia. To determine the role of hyperglycemia in the worsening of the diabetes state in these animals, MKR mice were treated with phloridzin (PHZ), which inhibits intestinal glucose uptake and renal glucose reabsorption...
November 2004: Diabetes
Kyla M Smith, Amy M L Ng, Sylvia Y M Yao, Kathy A Labedz, Edward E Knaus, Leonard I Wiebe, Carol E Cass, Stephen A Baldwin, Xing-Zhen Chen, Edward Karpinski, James D Young
Human concentrative nucleoside transporter 1 (hCNT1) mediates active transport of nucleosides and anticancer and antiviral nucleoside drugs across cell membranes by coupling influx to the movement of Na(+) down its electrochemical gradient. The two-microelectrode voltage-clamp technique was used to measure steady-state and presteady-state currents of recombinant hCNT1 produced in Xenopus oocytes. Transport was electrogenic, phloridzin sensitive and specific for pyrimidine nucleosides and adenosine. Nucleoside analogues that induced inwardly directed Na(+) currents included the anticancer drugs 5-fluorouridine, 5-fluoro-2'-deoxyuridine, cladribine and cytarabine, the antiviral drugs zidovudine and zalcitabine, and the novel thymidine mimics 1-(2-deoxy-beta-d-ribofuranosyl)-2,4-difluoro-5-methylbenzene and 1-(2-deoxy-beta-d-ribofuranosyl)-2,4-difluoro-5-iodobenzene...
August 1, 2004: Journal of Physiology
Akira Ikari, Mika Nakano, Mihoko Ishibashi, Kazuya Kawano, Yasunobu Suketa, Hitoshi Harada, Kuniaki Takagi
Exposure of cells or organs to sublethal physical or chemical stresses induces disruption of cellular structures and functions. Here, we examined whether Na(+)-glucose cotransporter (SGLT1) is involved in the recovery from heat shock (HS) injury in porcine renal epithelial LLC-PK(1) cells. Recovery from HS (42 degrees C for 3 h, then 37 degrees C for 12 h) increased SGLT1 activity, assessed by [14C]alpha-methyl glucopyranoside uptake, and a maximal transport rate (V(max)) from 2.4 to 5.9 nmol/mg protein/30 min, but did not alter an apparent affinity constant (K(m))...
December 7, 2003: Biochimica et Biophysica Acta
Thomas Walle, U Kristina Walle
Phloridzin, a glucoside of the flavonoid-like polyphenol phloretin, has long been known to be a specific nontransportable inhibitor of the sodium-dependent glucose transporter SGLT1. The objective of this study was to determine whether efflux by multidrug resistance-associated protein (MRP) transporters might have masked the absorption by SGLT1 in previous studies. Various cells used as transport models were incubated with phloridzin (50 microM) in the absence and presence of 50 microM 3-[[3-[2-(7-chloroquinolin-2-yl)vinyl]phenyl]-(2-dimethylcarbamoylethylsulfanyl)methylsulfanyl] propionic acid (MK-571), a highly selective MRP1/MRP2 inhibitor, and the cellular uptake of phloridzin was measured by high performance liquid chromatography...
November 2003: Drug Metabolism and Disposition: the Biological Fate of Chemicals
Thomas Pulinilkunnil, Ashraf Abrahani, Jospy Varghese, Nathan Chan, Irvin Tang, Sanjoy Ghosh, Jerze Kulpa, Michael Allard, Roger Brownsey, Brian Rodrigues
During diabetes, impaired glucose transport and utilization by the heart switches energy production to exclusive beta-oxidation of fatty acid (FA). In the current study, we examined the contribution of cardiac lipoprotein lipase (LPL) towards providing FA to the diabetic heart. Streptozotocin (STZ) caused an augmentation of LPL activity at the coronary lumen, an effect duplicated by diazoxide (DZ). With DZ, the amplification of LPL at the coronary luminal surface was determined to be exceptionally rapid. Interestingly, unlike DZ, the capability of hearts from STZ animals to maintain this amplified LPL activity was sustained in vitro...
September 2003: Journal of Molecular and Cellular Cardiology
R A Walgren, J T Lin, R K Kinne, T Walle
Although it has been suggested that the intestinal glucose transporter may actively absorb dietary flavonoid glucosides, there is a lack of direct evidence for their transport by this system. In fact, our previous studies with the human Caco-2 cell model of intestinal absorption demonstrated that a major dietary flavonoid, quercetin 4'-beta-glucoside, is effluxed by apically expressed multidrug resistance-associated protein-2, potentially masking evidence for active absorption. The objective of this study was to test the hypothesis that quercetin 4'-beta-glucoside is a substrate for the intestinal sodium-dependent D-glucose cotransporter SGLT1...
September 2000: Journal of Pharmacology and Experimental Therapeutics
X J Yang, L M Kow, T Funabashi, C V Mobbs
Glucose-responsive neurons in the ventromedial hypothalamus (VMH) are stimulated when glucose increases from 5 to 20 mmol/l and are thought to play an essential role in regulating metabolism. The present studies examined the role of glucose metabolism in the mechanism by which glucose-responsive neurons sense glucose. The pancreatic, but not hepatic, form of glucokinase was expressed in the VMH, but not cerebral cortex, of adult rats. In brain slice preparations, the transition from 5 to 20 mmol/l glucose stimulated approximately 17% of the neurons (as determined by single-cell extracellular recording) from VMH but none in cortex...
September 1999: Diabetes
A Saint-Pol, P Codogno, S E Moore
In hepatocellular carcinoma HepG2 cells, free polymannose-type oligosaccharides appearing in the cytosol during the biosynthesis and quality control of glycoproteins are rapidly translocated into lysosomes by an as yet poorly defined process (Saint-Pol, A., Bauvy, C., Codogno, P., and Moore, S. E. H. (1997) J. Cell Biol. 136, 45-59). Here, we demonstrate an ATP-dependent association of [2-3H]mannose-labeled Man5GlcNAc with isolated rat liver lysosomes. This association was only observed in the presence of swainsonine, a mannosidase inhibitor, which was required for the protection of sedimentable, but not nonsedimentable, Man5GlcNAc from degradation, indicating that oligosaccharides were transported into lysosomes...
May 7, 1999: Journal of Biological Chemistry
J P Buts, B Duranton, N De Keyser, E M Sokal, A S Maernhout, F Raul, S Marandi
The mechanism(s) by which insulin enhance prematurely the activity of brush border membrane (BBM) hydrolases in rat immature intestine is unknown. Therefore, we have compared the responses of four BBM enzymes [sucrase-isomaltase (SI), maltase, lactase-phloridzine hydrolase (LPH), and aminopeptidase] with exogenous insulin, the analog B-Asp10, IGF-I, and antireceptor MAb [insulin-receptor (IR) MAb] given to preweaning pups. Low doses of insulin caused a precocious induction of SI and of SI mRNA and stimulated maltase activity without effect on LPH nor on aminopeptidase activities...
May 1998: Pediatric Research
Walsh, Wood, Perry, Thomas
Although urea transport is receiving increased attention in mammalian systems, very little is known about urea transport in fish tissues. This study examined mechanisms of urea transport in red blood cells and hepatocytes from the lesser spotted dogfish (Scyliorhinus canicula), Atlantic stingray (Dasyatis sabina), turbot (Scopthalmus maximus), redfish (Scianops ocellatus), gulf toadfish (Opsanus beta) and oyster toadfish (Opsanus tau). Urea appeared to be passively distributed in both tissues (i.e. there was no difference between plasma and tissue urea concentrations)...
August 1994: Journal of Experimental Biology
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