Absorption of monosaccharides is mainly mediated by Na+-D-glucose cotransporter SGLT1 and the facititative transporters GLUT2 and GLUT5. SGLT1 and GLUT2 are relevant for absorption of D-glucose and D-galactose while GLUT5 is relevant for D-fructose absorption. SGLT1 and GLUT5 are constantly localized in the brush border membrane (BBM) of enterocytes, whereas GLUT2 is localized in the basolateral membrane (BLM) or the BBM plus BLM at low and high luminal D-glucose concentrations, respectively. At high luminal D-glucose, the abundance SGLT1 in the BBM is increased. Hence, D-glucose absorption at low luminal glucose is mediated via SGLT1 in the BBM and GLUT2 in the BLM whereas high-capacity D-glucose absorption at high luminal glucose is mediated by SGLT1 plus GLUT2 in the BBM and GLUT2 in the BLM. The review describes functions and regulations of SGLT1, GLUT2, and GLUT5 in the small intestine including diurnal variations and carbohydrate-dependent regulations. Also, the roles of SGLT1 and GLUT2 for secretion of enterohormones are discussed. Furthermore, diseases are described that are caused by malfunctions of small intestinal monosaccharide transporters, such as glucose-galactose malabsorption, Fanconi syndrome, and fructose intolerance. Moreover, it is reported how diabetes, small intestinal inflammation, parental nutrition, bariatric surgery, and metformin treatment affect expression of monosaccharide transporters in the small intestine. Finally, food components that decrease D-glucose absorption and drugs in development that inhibit or downregulate SGLT1 in the small intestine are compiled. Models for regulations and combined functions of glucose transporters, and for interplay between D-fructose transport and metabolism, are discussed.

/pdf/glucose-transporters-in-the-small-intestine-in-health-and-bt55c0vkbv.pdf

Glucose transporters in the small intestine in health and disease

Anti-diabetic drugs recent approaches and advancements

Background: A critical factor for maintenance of glucose balance is the renal recovery of glucose from the glomerular filtrate mediated primarily by sodium glucose co-transporter 2 (SGLT2). This capacity can be modulated by SGLT2 inhibitors thereby providing a unique insulin independent method of treatment of diabetes. Objective/method: A discussion of the evolution of SGLT inhibitors as inferred from patents published from 2005 to 2009 is prefaced by a brief review of the role of SGLT in glucose transport and the clinical findings illustrating the therapeutic potential of SGLT inhibitors as anti-diabetic agents. These compounds comprise O, C and N-glycosides generated by attachment of an appropriate lipophilic aglycone component to a suitable glucose analogue. Conclusion: The realization that the in vivo potency of O-glucosides was markedly less than that of C-glucosides necessitated a shift in medicinal chemistry focus of the pharmaceutical companies pursuing SGLT2 inhibitors. Particular emphasis is pla...

Evolution of sodium glucose co-transporter 2 inhibitors as anti-diabetic agents.

Compounds of Formula (A) and (B) are described herein and the uses thereof for the treatment of diseases, conditions and/or disorders mediated by sodium-glucose transporter inhibitors (in particular, SGLT2 inhibitors).

Dioxa-bicyclo[3.2.1]octane-2,3,4-triol derivatives

Structural modification aimed for improving solubility of lead compounds in early phase drug discovery

Provided is a novel C-phenyl glycitol compound that may serve as a prophylactic or therapeutic agent for diabetes by inhibiting both SGLT1 activity and SGLT2 activity, thereby exhibiting a glucose absorption suppression action and a urine glucose excretion action. A C-phenyl glycitol compound represented by Formula (I) below or a pharmaceutically acceptable salt thereof or a hydrate thereof wherein R1 and R2 are the same or different and represent a hydrogen atom, a hydroxyl group, a C1-6 alkyl group, a C1-6 alkoxy group or a halogen atom, R3 is a hydrogen atom, a C1-6 alkyl group, a C1-6 alkoxy group or a halogen atom, Y is a C1-6 alkylene group, -O-(CH2)n- (n is an integer of 1 to 4) or a C2-6 alkenylene group, provided that when Z is NHC(= NH)NH2 or -NHCON(RB)RC, n is not 1, Z is -CONHRA, -NHC(=NH)NH2 or -NHCON(RB)RC, Formula (A) or Formula (B).

C-phenyl glycitol compound for the treatment of diabetes

A C-phenyl 1-thioglucitol compound represented by the formula (I), a pharmaceutically acceptable salt thereof, or a hydrate of the compound or the pharmaceutically acceptable salt. (I) wherein X represents a hydrogen atom or a C1-6 alkyl group; Y represents a C1-6 alkylene group or ~O-(CH2)n- (n represents an integer ranging from 1 to 5); and Z represents ~CONHRA or ~NHCONHRB (provided that, when Z represents ~NHCONHRB, n is not 1), where RA represents a C1-6 alkyl group substituted by 1 to 3 groups independently selected from a hydroxyl group and ~CONH2; and RB represents a hydrogen atom or a C1-6 alkyl group substituted by 1 to 3 groups independently selected from a hydroxyl group and ~CONH2. The compound, the salt or the solvate can inhibit the SGLT1 activity to prevent the absorption of glucose or the like, or can inhibit both the SGLT1 activity and the SGLT2 activity to prevent the absorption of glucose or the like and excrete a urine sugar, and is therefore useful as a prophylactic or therapeutic agent for diabetes.

C-phenyl 1-thioglucitol compound

Design and synthesis of 1H-pyrazolo[3,4-c]pyridine derivatives as a novel structural class of potent GPR119 agonists.

Disclosed is a 1-phenyl 1-thio-D-glucitol compound having the formula (I) or the like, a pharmaceutically acceptable salt thereof, a hydrate of the compound or the pharmaceutically acceptable salt, or a pharmaceutical agent comprising the compound, the pharmaceutically acceptable salt or the hydrate as an active ingredient, which can inhibit both the activities of SGLT1 and SGLT2 and has both of an effect of inhibiting the absorption of glucose through a digestive tract and an urinary glucose excretion effect, and therefore is useful as a new type of prophylactic or therapeutic agent for diabetes, a diabetes-related disease or a diabetic complication.

1-phenyl 1-thio-d-glucitol derivative

The object is to provide a novel phenyl 5-thioglucoside compound which can control IGT (impaired glucose tolerance) by inhibiting the SGLT1 activity and inhibiting the absorption of glucose through a digestive tract. Provided is a phenyl 5-thioglucoside compound represented by the formula (I), a pharmaceutically acceptable salt thereof, or a hydrate of the compound or the salt. (I) wherein R1 and R2 independently represent a hydrogen atom, a hydroxyl group, a C1-6 alkyl group, a C1-6 alkoxy group or a halogen atom; Z represents –NHSO2-phenyl, -NHSO2NH2 or –Y-Q; Y represents a single bond, a C1-6 alkylene group or an alkenylene group; and Q represents –NHC(=NH)NH2, -NHCON(RA)RB, -CONH(RC) or a 4- to 6-membered heterocycloalkyl group substituted by at least one member selected from a C1-6 alkyl group and an oxo group (the heterocycloalkyl group may be fused with a phenyl group).

Phenyl 5-thio glycoside compound

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