Deglycosylation of individual flavonoids and flavonoid containing plant extracts by purified human intestinal lactase-phlorizin hydrolase (LPH)

Schwanck, B; Behrendt, Michael E.; Hy, Naim; Blaschek, W.

doi:10.1055/s-0031-1282218

Cited by 4 publications

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“…Phlorizin can be effectively hydrolyzed by lactase phlorizin hydrolase (LPH), an enzyme that is expressed in the brush border membrane of the small intestine. It is a glycoprotein with two catalytic sites: one is responsible for hydrolyzing lactose, the main carbohydrate in milk (important for infants and young children), and the other exhibits a broad activity against various flavonoids and glycosyl-N-acylsphingosines [63][64][65]. LPH is, for example, responsible for the hydrolysis of phlorizin, quercetin-4′-O-glucoside, kaempferol-3-O-glucoside, apigenin-7-O-glucoside, luteolin-3′-7-O-diglucoside, genistein-7-O-glucoside, and daidzein-7-O-glucoside [61,62,64,65].…”

Section: Natural Products As Sglt Inhibitorsmentioning

confidence: 99%

“…It is a glycoprotein with two catalytic sites: one is responsible for hydrolyzing lactose, the main carbohydrate in milk (important for infants and young children), and the other exhibits a broad activity against various flavonoids and glycosyl-N-acylsphingosines [63][64][65]. LPH is, for example, responsible for the hydrolysis of phlorizin, quercetin-4′-O-glucoside, kaempferol-3-O-glucoside, apigenin-7-O-glucoside, luteolin-3′-7-O-diglucoside, genistein-7-O-glucoside, and daidzein-7-O-glucoside [61,62,64,65]. Phloretin, the resultant aglycon of hydrolysis of phlorizin by LPH, is thought to be taken up by enterocytes in the small intestine, to inhibit GLUT2 expressed in their basolateral membrane, and, thus, to cause a delay in glucose absorption and to lower blood glucose levels [63,66].…”

Section: Natural Products As Sglt Inhibitorsmentioning

confidence: 99%

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Natural Products as Lead Compounds for Sodium Glucose Cotransporter (SGLT) Inhibitors

Blaschek

2017

Planta Med

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Glucose homeostasis is maintained by antagonistic hormones such as insulin and glucagon as well as by regulation of glucose absorption, gluconeogenesis, biosynthesis and mobilization of glycogen, glucose consumption in all tissues and glomerular filtration, and reabsorption of glucose in the kidneys. Glucose enters or leaves cells mainly with the help of two membrane integrated transporters belonging either to the family of facilitative glucose transporters (GLUTs) or to the family of sodium glucose cotransporters (SGLTs). The intestinal glucose absorption by endothelial cells is managed by SGLT1, the transfer from them to the blood by GLUT2. In the kidney SGLT2 and SGLT1 are responsible for reabsorption of filtered glucose from the primary urine, and GLUT2 and GLUT1 enable the transport of glucose from epithelial cells back into the blood stream.The flavonoid phlorizin was isolated from the bark of apple trees and shown to cause glucosuria. Phlorizin is an inhibitor of SGLT1 and SGLT2. With phlorizin as lead compound, specific inhibitors of SGLT2 were developed in the last decade and some of them have been approved for treatment mainly of type 2 diabetes. Inhibition of SGLT2 eliminates excess glucose via the urine. In recent times, the dual SGLT1/SGLT2 inhibitory activity of phlorizin has served as a model for the development and testing of new drugs exhibiting both activities.Besides phlorizin, also some other flavonoids and especially flavonoid enriched plant extracts have been investigated for their potency to reduce postprandial blood glucose levels which can be helpful in the prevention and supplementary treatment especially of type 2 diabetes.

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Section: Natural Products As Sglt Inhibitorsmentioning

confidence: 99%

Section: Natural Products As Sglt Inhibitorsmentioning

confidence: 99%

Natural Products as Lead Compounds for Sodium Glucose Cotransporter (SGLT) Inhibitors

Blaschek

2017

Planta Med

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New insights on bioactivities and biosynthesis of flavonoid glycosides

Yang

Liu

Yang

et al. 2018

Trends in Food Science & Technology

181

107

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Metabolism and health effects of phyto-estrogens

Nie

Xing

et al. 2015

Critical Reviews in Food Science and Nutrition

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Phyto-estrogens are plant-derived compounds that can exert various estrogenic and anti-estrogenic effects, and are usually used as a natural alternative to estrogen replacement due to their health benefits, including a lowered risk of osteoporosis, heart disease, breast cancer, and menopausal symptoms. Phyto-estrogens are also considered as endocrine disruptors due to their structure similar to human female hormone 17-β oestradiol. However, the issue of whether phyto-estrogens are beneficial or harmful to human health remains unknown, as this may depend on the dose, form, level and duration of administration of phyto-estrogens, and influence by genetics, metabolism, gut physiology, age, diet, and the health status of individuals. Clarification on this issue is necessary for the sake of their two-side effects on human health and rapidly increasing global consumption of phyto-estrogens. This review mainly includes the metabolism of phyto-estrogens and weighs the evidence for and against the purported health benefits and adverse effects of phyto-estrogens.

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Deglycosylation of individual flavonoids and flavonoid containing plant extracts by purified human intestinal lactase-phlorizin hydrolase (LPH)

Cited by 4 publications

References 0 publications

Natural Products as Lead Compounds for Sodium Glucose Cotransporter (SGLT) Inhibitors

Natural Products as Lead Compounds for Sodium Glucose Cotransporter (SGLT) Inhibitors

New insights on bioactivities and biosynthesis of flavonoid glycosides

Metabolism and health effects of phyto-estrogens

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