ABSTRACT
Absorption and metabolism of a natural compound, 6-O-caffeoylsophorose (CS) from acylated anthocyanins in a red vinegar fermented with purple sweet potato, were clarified. The absorption of CS and conjugated CS in blood from orally administrated Sprague-Dawley rats at a dose of 400 mg/kg was investigated by electrochemical detection-high performance liquid chromatography. As a result, CS was successfully detected in rat plasma (AUC(0-6h), 108.6 ± 8.1 nmol h/mL) and was found to be an intact absorbable polyphenol. In addition, half of the absorbed CS was detected as its conjugates (AUC(0-6h), 50.7 ± 5.7 nmol h/mL) as well as caffeic and ferulic acids from CS. By a time-of-flight-mass spectrometric analysis of CS-administered plasma sample, glucuronide and methylated conjugates of CS were identified, in addition to glucuronide, methylated, or sulfate conjugates of caffeic and ferulic acids. Consequently, CS was absorbed in intact form into rat blood and partly degraded to caffeic and ferulic acids or metabolized by glucuronidation, methylation, or sulfatation.
Subject(s)
Chromatography, High Pressure Liquid/methods , Disaccharides/blood , Disaccharides/metabolism , Spectrometry, Mass, Electrospray Ionization/methods , Absorption , Animals , Male , Rats , Rats, Sprague-DawleyABSTRACT
BACKGROUND: A new fermented tea produced by tea-rolling processing of loquat (Eriobotrya japonica) leaf with green tea leaf (denoted as LG tea) showed a potent antihyperglycaemic effect in maltose-loaded rats. The aim of this study, therefore, was to identify alpha-glucosidase inhibitors in the antihyperglycaemic tea product. RESULTS: LG tea had a threefold higher maltase-inhibitory activity (IC(50) 0.065 mg dried extract mL(-1)) than either the constituent loquat leaf or green tea alone. In addition, LG tea favourably inhibited maltase action rather than sucrase action. As a result of bio-guided high-performance liquid chromatography separations of LG tea, theasinensin A, theasinensin B, strictinin and 1,6-digalloylglucose were newly identified as maltase inhibitors with IC(50) values of 142, 225, 398 and 337 micromol L(-1) respectively, along with previously identified catechins and theaflavins. CONCLUSION: Judging from the magnitude of the alpha-glucosidase-inhibitory contribution of each isolated compound to the overall inhibition of LG tea, catechins were the main candidates responsible for alpha-glucosidase or maltase inhibition in LG tea, followed by theaflavins, theasinensins, strictinin and 1,6-digalloylglucose.
Subject(s)
Camellia sinensis/chemistry , Enzyme Inhibitors/isolation & purification , Enzyme Inhibitors/pharmacology , Eriobotrya/chemistry , Fermentation , Glycoside Hydrolase Inhibitors , Plant Leaves/chemistry , Tea/chemistry , Benzopyrans/chemistry , Benzopyrans/isolation & purification , Benzopyrans/pharmacology , Catechin/analogs & derivatives , Catechin/chemistry , Catechin/isolation & purification , Catechin/pharmacology , Chromatography, High Pressure Liquid , Enzyme Inhibitors/chemistry , Food Handling/methods , Hyperglycemia/prevention & control , Magnetic Resonance Spectroscopy , Molecular Structure , Phenols/chemistry , Phenols/isolation & purification , Phenols/pharmacology , Spectrometry, Mass, Electrospray IonizationABSTRACT
BACKGROUND: In the field of food science, much interest has been focused on the development of alternative medicinal foods with the ability to regulate excess blood glucose level (BGL) rise. The authors have successfully developed a new fermented tea product (LG tea) by co-fermentation of loquat (Eriobotrya japonica) leaf and summer-harvested green tea leaf. The objective of this study was to examine the acute suppression effect of LG tea on BGL rise in disaccharide-loaded Sprague-Dawley (SD) rats and to evaluate its possible usage as an antidiabetic functional food material. RESULTS: As a result of single oral administration of hot water extract of LG tea (50 mg kg(-1)) to maltose-loaded SD rats, BGL at 30 min was significantly decreased by 23.8% (P < 0.01) compared with the control. A corresponding reduction in serum insulin secretion was also observed. The ED(50) value of LG tea (50.7 mg kg(-1)) was estimated to be about 16-fold higher than that of the therapeutic drug acarbose (3.1 mg kg(-1)). CONCLUSION: No significant change in BGL was observed when sucrose or glucose was administered, suggesting that the suppression effect of LG tea was achieved by maltase inhibition, not by sucrase inhibition or glucose transport inhibition at the intestinal membrane.
