Inhibitory sacharidáz

Acarbose

• Bay g 5421, Glucobay®, Precose®, Prandase®; Bayer
• Pseudotetrasaccharide
• Inhibits intestinal alpha-glucosidase reversibly at the brush border of intestinal mucosa
• Disaccharides to monosaccharides is prevented
• Uptake of monosaccharides is retarded
• Postprandial insulin and glucose levels are reduced
• In vitro, acarbose (4 µM) strongly inhibited the activities of alpha-amylase and sucrase (98 and 63%, respectively)
• At higher concentration (200 µM)
• Also inhibited isomaltase activity (28%)
• Negligible effects on trehalase and lactase activities
• Gradual dose increments prevent GI side effects
• Dose-dependent reduction of weight gain
• To weight-reduced women limited weight regain
• One year, double-blind, randomized, placebo-controlled study in type 2 diabetes subjects
• Acarbose lost 0.5 kg
• Placebo group gained 0.3 kg [12]
• Acarbose (150 mg/day) to women with polycystic ovary syndrome
• Significantly reduced body weight and BMI [12]

Berry polyphenols

• Anthocyanins
• Ellagitannins
• Reduce postprandial hyperglycemia
• Directly induce secretion of insulin from pancreatic cells
• Inhibition of alpha-glucosidase and alpha-amylase
• Also exerts inhibitory activity on pancreatic lipase [12]

Ellagitannin-rich extracts

• Raspberry
• Strawberry
• Cloudberry
• Arctic bramble
• Seem to be the most effective at inhibiting lipase
• Some published data extract-induced fecal lipid excretion
• Associated with reductions in weight gain
• Changes in TG metabolism [12]
• Other studies report no significant correlations
• Compensatory increases in lipase secretion
• Similar to those seen in studies on condensed tannins in rats [12]

Cyclocarya paliurus (Batal.) Iljinskaja

• Tree found in the highlands of southern China
• Cyclocarioside A, II and III
• Triterpenoid saponins
• From the leaves of C. paliurus
• Insulin-like activity in adipocytes, in vivo and in vitro [12]
• Inhibitory activity toward pancreatic lipase
• C. paliurus extract (250 mg/kg) to mice
• Suppressed the expected increase in plasma triacylgycerol levels
• Probably due to lipase inhibition
• Alpha-glucosidase inhibitory activity
• At the dose of 5 µg/mL [12]
• C. paliurus extract (250 mg/kg) to micesuppressed
• The expected increase of blood glucose level following sucrose administration [12]

Deoxynojirimycin (DNJ)

• Polyhydroxylated alkaloid
• From mulberry trees
• Competitive inhibitor of small-intestinal brush-border alpha-glucosidase
• Functional foods and food additives
• Diabetic rats - DNJ (20 mg/kg) prevents weight gain
• Synthetic derivatives
• Potent alpha-glucosidase inhibitors
• Competitive inhibitors
• BAY o 1248 (emiglitate)
• 0.1 to 5 µg/mL inhibit
• Sucrase (up to 97%)
• Glucoamylase (up to 96%)
• BAY m 1099 (miglitol)
• Inhibited weight gain in animals fed a diet high in starch
• Did not have any effect on animals fed with glucose [12]

Green tea

• Widely consumed and for centuries
• Long-term consumption of green tea and its extract (GTE) associated with weight loss
• Mainly through a thermogenic mechanism
• Derived from an oxidation-free process
• High levels of catechins are retained [12]
• Full fermentation processes used to produce black tea
• Significantly reduce catechins levels
• Main active ingredients in GTE:
• Catechins epigallocatechin gallate (EGCG; Teavigo®)
• Epigallocatechin (EGC)
• Epicatechin gallate (ECG)
• Epicatechin (EC) [12]
• Inhibition of adipocyte division and maturation
• Reduce glucose and fat absorption by inhibiting GI enzymes involved in nutrient digestion
• Green tea extract AR25 (Exolise®; standardized at 25% catechins)
• Effectively inhibited gastric and pancreatic lipase activities
• Tea polyphenols
• Inhibit alpha-amylase and alpha-glucosidase in vitro [12]
• Green tea catechins reduced alpha-amylase and sucrase activities in rat intestine
• Streptozotocin-induced diabetic rats
• Green tea extracts to the diet (0.01% and 0.2% of diet) significantly reduced
• Maltase (both doses)
• Saccharase
• Lactase (higher dose) [12]
• Green tea extract (3% of diet) to rats fed a high fat diet
• Decreased body weight gain and visceral fat accumulation
• Increase in fecal lipids
• Administration of AR25 for 3 months human obese
• Decreased body weight and waist circumference [12]

Phaseolus vulgaris L (kidney bean)

• Purified, non-toxic (P. vulgaris contains toxic substances) extract
• Large amounts of phaseolamine
• Phase 2®; previously sold as Phaseolamin 2250®
• 1 g of the product blocking 2250 starch calories, DEcarb®
• A glycoprotein that inhibits alpha-amylase
• Non competitive
• US, several different preparations are commercially available
• Phaseolamine binds to alpha-amylase 1:1
• Complex inhibiting the enzyme
• Rats intragastric phaseolamine
• Reduces post-prandial and basal plasma glucose levels [12]
• Phaseolamine
• Reduces food intake
• Consequently body weight [12]
• P. vulgaris extract
• Seems to stimulate CCK release
• Interfere with central mechanisms that regulate food intake and food palatability
• Large doses of phaseolamine
• Impairs the growth rate of rats
• Normoglycemic and diabetic individuals
• Earlier reduction of postprandial glucose levels
• 57% lower glucose absorption [12]
• 1.5 g of phaseolamine to healthy participants
• Blocked the absorption of 66% of carbohydrates from standard meal
• Double-blind, placebo-controlled clinical trial 30 days
• 4% loss of body weight compared to 0.47% placebo group
• 10% reduction in body fat in the experimental group [12]
• Randomized, double-blinded, placebo-controlled studies on normal and overweight on high carbohydrate diet
• 1 month 445 to 1000 mg/day P. vulgaris extract
• Significant reduction in both total body mass and BMI compared to control and changes in body composition [12]

Salix matsudana

• Chinese willow
• One ingredient of Rev Hardcore® and Methyl Ripped®
• Leaves have been used in traditional Chinese medicine
• Polyphenol extracts have anti-obesity actions
• Polyphenol fractions to DIO mice
• Reduced adiposity and body weight
• In vitro analysis S. matsudana extract
• Inhibited the enzyme alpha-amylase
• Polyphenol fractions presence
• Completely inhibited the intestinal absorption of palmitic acid
• Inhibition of carbohydrate and lipid absorption
• Acceleration of fat mobilization
• Enhancement of NA-induced lipolysis in adipocytes [12]
• Have been shown to have anti-obesity actions
• In vitro
• In rodents
• Research in humans, especially on the long term effects, is lacking [12]

Extracts of black, green, and mulberry teas

• Extracts of black, green, and mulberry teas
• Interfere with carbohydrate and TG absorption
• Ability to inhibit
• Alpha-amylase
• Beta-glucosidase
• Sodium-glucose transporters
• Pancreatic lipase
• Green (0.1 g), black (0.1 g), and mulberry (1.0 g) tea leaves
• Contained cca
• 5 mg DNJ-type compounds
• 100 mg epicatechin gallate
• 300 mg epigallocatechin gallate
• 100 mg theaflavin
• To humans reduced carbohydrate (derived from starch) absorption by 25% [12]