Effects of nutrient restriction and melatonin supplementation from mid-to-late gestation on maternal and fetal small intestinal carbohydrase activities in sheep.

The objective of this experiment was to evaluate the effects of nutrient restriction and melatonin supplementation during mid-to-late gestation on maternal and fetal small intestinal carbohydrase activities in sheep. Ewes were randomly assigned to one of 4 dietary treatments arranged in a 2 × 2 factorial design. Ewes were fed to provide 100% (adequate; ADQ) or 60% (restricted; RES) of nutrient recommendations, and diets were supplemented with either no melatonin (control; CON) or 5 mg melatonin/d (melatonin; MEL). This resulted in 4 treatment groups: CON-ADQ (n = 7), CON-RES (n = 8), MEL-ADQ (n = 8), MEL-RES (n = 8). Treatments began on day 50 of gestation, and ewes were euthanized on day 130 for tissue collection. The maternal and fetal small intestine were collected and assayed for small intestinal carbohydrase activities. Data were analyzed using the GLM procedure of SAS with fetal sex, melatonin, nutrition, and the melatonin by nutrition interaction included in the model statement. There were no melatonin by nutrition interactions for maternal or fetal small intestinal protein concentration or carbohydrase activities (P ≥ 0.11). Dietary melatonin supplementation decreased (P = 0.03) maternal small intestinal protein concentration by 22.7% and increased (P = 0.03) maternal small intestinal glucoamylase, isomaltase, and maltase activity per gram protein by 45.5%, 41.3%, and 40.6%, respectively. Nutrient restriction from mid-to-late gestation did not influence (P ≥ 0.46) maternal small intestinal protein concentration, or maltase, isomaltase, and lactase activity. Maternal glucoamylase activity per gram intestine increased (P = 0.05) with nutrient restriction by 49.1%. Melatonin supplementation and maternal nutrient restriction did not influence (P ≥ 0.15) fetal small intestinal protein concentration, or glucoamylase, isomaltase, and lactase activity. Maternal nutrient restriction from mid-to-late gestation decreased (P = 0.05) fetal maltase activity per gram intestine by 20.5% but did not influence fetal maltase activity per gram protein. These data indicate that some maternal and fetal carbohydrases are influenced by nutrient restriction and melatonin supplementation in sheep. More information is needed to understand how nutritional and hormonal factors regulate digestive enzyme activity in ruminants to design improved maternal nutrition programs to optimize fetal growth and development while maintaining maternal productivity.

The Ability to Dissipate Heat Is Likely to Be a More Important Limitation on Lactation in Striped Hamsters with Greater Reproductive Efforts under Warmer Conditions.

The limitations on energy availability and outputs have been implied to have a profound effect on the evolution of many morphological and behavioral traits. It has been suggested that the reproductive performance of mammals is frequently constrained by intrinsic physiological factors, such as the capacity of the mammary glands to produce milk (the peripheral limitation [PL] hypothesis) or that of the body to dissipate heat (the heat dissipation limitation [HDL] hypothesis). Research on a variety of small mammals, however, has so far failed to provide unequivocal support for one hypothesis over the other. We tested the PL and HDL hypotheses in female striped hamsters (Cricetulus barabensis) with artificially manipulated litter sizes of two (three or four pups removed from natural litter size), five, eight (two or three pups added to natural litter size), and 12 (five to seven pups added to natural litter size) pups at ambient temperatures of 21° and 30°C. Energy intake and milk output of mothers, litter size, and litter mass were measured throughout lactation. Several markers indicating digestive enzyme activity and the gene expression of hypothalamic neuropeptides related to food intake were also measured. Food consumption and milk output increased with increasing litter size but reached a ceiling at 12 pups, causing 12-pup litters to have significantly lower litter mass and pup body mass than litters composed of fewer pups. Litter mass and maternal metabolic rate, milk output, maltase, sucrase, and aminopeptidase activity in the small intestine, and gene expression of hypothalamic orexigenic peptides were significantly lower at 30°C than at 21°C, and these differences were considerably more pronounced in 12-pup litters. These results suggest that PL and HDL can operate simultaneously but that the HDL hypothesis is probably more valid at warmer temperatures. Our results suggest that increased environmental temperatures in future climates may limit reproductive output through heat dissipation limits.

Comparison of CYP Induction by Coleus forskohlii Extract and Recovery in the Small Intestine and Liver of Mice.

We examined CYP induction and recovery at various doses of Coleus forskohlii extract (CFE) to assess potential drug interactions by a mechanism involving intestinal CYP. Mice were administered diets with various doses of CFE up to 0.5% (equivalent to 700-800 mg/kg body weight) for 2 weeks, then CFE was withdrawn for 3 d. Changes in CYP activities and mRNA expression in the small intestine and liver were then evaluated. CFE induced CYP in the small intestine at a higher dose compared to the liver; CYP3A was induced at 0.5% and 0.005% CFE in the small intestine and liver, respectively. There was no sex difference in CFE dose for CYP induction. CYP induction quickly reverted after withdrawal of CFE, especially for CYP3A, in the small intestine; whereas, a gradual recovery was observed in the liver. In conclusion, CFE induced CYP in the small intestine and liver; however, a higher dose of CFE was needed for the small intestine. Moreover, the induction was soon recovered, suggesting actual interactions of CFE with prescription drugs are unlikely to occur through CYP in the small intestine.

Bioactivity-based analysis and chemical characterization of hypoglycemic and antioxidant components from Artemisia argyi.

Diabetes is one of the metabolic disorders in the world. It is the prime reason of mortality and morbidity owing to hyperglycemia which is link with numerus obstacles. Artemisia argyi is commonly used as an ingredient in healthy foods as well as an herbal medicine in Asian countries. The present research aims to evaluate the hypoglycemic effects of A. argyi and reveal its the potentially active constituents. The chemical composition was identified by HPLC-DAD-Q-TOF-MS, and fractionation was performed by extraction. The fractions were assessed by the blood glucose level, oral glucose tolerance and small intestinal α-glucosidase inhibitory tests, and an analysis of the total phenolic content (TPC), antioxidant and α-glucosidase inhibitory activities. In our efforts to characterize the compounds responsible for hypoglycemic effect, bioactivity-guided fraction of the MeOH extract and chemical investigation of its active EtOAc fraction led to the successful identification of caffeoylquinic acids, which were elucidated by molecular docking, using the crystal structure of S. cerevisiae isomaltase (PD code: 3AXI). In summary, this bio-guided search revealed that caffeoylquinic acids from A. argyi as potential active constituents displayed with hypoglycemic activity, which provided a basis for further study of pharmacological activity.

Effects of cottonseed meal on growth performance, small intestinal morphology, digestive enzyme activities, and serum biochemical parameters of geese.

Cottonseed meal (CSM), an oil industry by-product, is an attractive alternative protein source in poultry diets. To investigate the effects of CSM on growth performance, small intestinal morphology, digestive enzyme activities, and serum biochemical parameters of geese, a total of 300 healthy, 28-day-old, male Jiangnan geese were randomly divided into 5 treatments, with 6 pens of 10 geese each. Five isonitrogenous and isocaloric experimental diets were formulated to produce diets in which 0% (control), 25% (CSM25), 50% (CSM50), 75% (CSM75), and 100% (CSM100) of protein from soybean meal was replaced by CSM (corresponding to 0, 6.73, 13.46, 20.18, and 26.91% CSM in the feed, respectively). At 28, 42, and 70 d, BW and feed intake for each pen were measured. Blood, small intestine, and chyme samples were collected at 70 d. The results showed that dietary 13.46% CSM or more decreased BW at 42 d and ADG from 28 to 42 d but increased the feed/gain ratio (F/G) from 28 to 42 d (P < 0.05). From 42 to 70 d, geese in the CSM groups had higher ADFI and ADG than those of the control group (P < 0.05). Geese in the CSM75 and CSM100 groups had a higher ADG from 28 to 70 d and BW at 70 d and a lower F/G from 42 to 70 d than those of the control group (P < 0.05). Dietary 6.73% CSM also improved ADFI from 28 to 70 d (P < 0.05). Compared to the control, geese in the CSM groups had decreased pepsin and lipase activities, and those in the CSM25, CSM50, and CSM75 groups had increased villus height in the jejunum at 70 d (P < 0.05). All groups had similar concentrations of total protein, blood urea nitrogen, uric acid, cholesterol, triglyceride, calcium, and phosphorus in serum (P > 0.05). In conclusion, excessive use of CSM (>6.73%) decreased growth performance at an early age (28 to 42 d) in geese, whereas 6.73 to 26.91% CSM in feed improved growth performance from 28 to 70 d.

Sea Buckthorn Oil as a Valuable Source of Bioaccessible Xanthophylls.

Sea buckthorn oil, derived from the fruits of the shrub, also termed seaberry or sandthorn, is without doubt a strikingly rich source of carotenoids, in particular zeaxanthin and ß-carotene. In the present study, sea buckthorn oil and an oil-in-water emulsion were subjected to a simulated gastro-intestinal in vitro digestion, with the main focus on xanthophyll bioaccessibility. Zeaxanthin mono- and di-esters were the predominant carotenoids in sea buckthorn oil, with zeaxanthin dipalmitate as the major compound (38.0%). A typical fatty acid profile was found, with palmitic (49.4%), palmitoleic (28.0%), and oleic (11.7%) acids as the dominant fatty acids. Taking into account the high amount of carotenoid esters present in sea buckthorn oil, the use of cholesterol esterase was included in the in vitro digestion protocol. Total carotenoid bioaccessibility was higher for the oil-in-water emulsion (22.5%) compared to sea buckthorn oil (18.0%) and even higher upon the addition of cholesterol esterase (28.0% and 21.2%, respectively). In the case of sea buckthorn oil, of all the free carotenoids, zeaxanthin had the highest bioaccessibility (61.5%), followed by lutein (48.9%), making sea buckthorn oil a potential attractive source of bioaccessible xanthophylls.

Effects of dietary leucine and phenylalanine on gastrointestinal development and small intestinal enzyme activities in milk-fed holstein dairy calves.

This study was investigated the effects of dietary supplementation of leucine and phenylalanine on the development of the gastrointestinal tract and the intestinal digestive enzyme activity in male Holstein dairy calves. Twenty calves with a body weight of 38 ± 3 kg at 1 day of age were randomly divided into four groups: a control group, a leucine group (1.435 g·l-1), a phenylalanine group (0.725 g·l-1), and a mixed amino acid group (1.435 g·l-1 leucine plus 0.725 g·l-1 phenylalanine). The supplementation of leucine decreased the short-circuit current (Isc) of the rumen and duodenum (P<0.01); phenylalanine did not show any influence on the Isc of rumen and duodenum (P>0.05), and also counteracted the Isc reduction caused by leucine. Leucine increased the trypsin activity at the 20% relative site of the small intestine (P<0.05). There was no difference in the activity of α-amylase and of lactase in the small intestinal chyme among four treatments (P>0.05). The trypsin activity in the anterior segment of the small intestine was higher than other segments, whereas the α-amylase activity in the posterior segment of the small intestine was higher than other segments. Leucine can reduce Isc of the rumen and duodenum, improve the development of the gastrointestinal tract, and enhance trypsin activity; phenylalanine could inhibit the effect of leucine in promoting intestinal development.

In vitro hypoglycemic potential of spices: Cinnamon and Cumi.

Present study evaluates the anti-hyperglycemic potential of two Indian spices Cinnamomum zeylanicum(CZ) and Cumin cyminum(CC) (whole powder and aqueous extracts) using in vitro techniques like glucose adsorption assay, amylolysis kinetics and ex vivo assays like amylase, Sucrase and α-glucosidase assay. CZ displayed higher glucose adsorption and glucose diffusion retardation than CC, as shown by glucose adsorption and amylolysis kinetics assay. CZ showed lower inhibition of α-amylase and sucrase where as CC has no effect on both the enzymes. In case of α-glucosidase, CC had better inhibition than CZ. Further research is needed to understand the mechanism through which both the spices act to regulate the hyperglycemia.

Dietary pectin and mango pulp effects on small intestinal enzyme activity levels and macronutrient digestion in grower pigs.

The effects of refined pectin and mango pulp on macronutrient digestion and small intestinal enzyme activity were studied in grower pigs. Diets based on wheat starch with and without apple pectin or dried mango fruit pulp were fed to 30 grower pigs for 21 days. Pigs were euthanized two hours postprandially, and their gastrointestinal contents recovered. Starch and protein digestion as well as α-amylase activity were all increased in pigs fed pectin. In contrast, fat digestion, lipase and protease (trypsin) activities were all significantly reduced in these pigs. Pigs fed the mango fruit pulp diet had intermediate effects compared with pigs fed refined pectin and control diets. The data suggests that pectin has a significant effect on digestive enzyme activity and subsequent influence on macronutrient digestion. The fact that pectin caused either an increase (α-amylase) or decrease (lipase, protease) in enzyme activity in digesta, which either did (starch, lipid) or did not (protein) associate with residual nutrient differences illustrates the complexity of small intestinal responses to added fibre in diets.

The impact of sesquiterpenes ß-caryophyllene oxide and trans-nerolidol on xenobiotic-metabolizing enzymes in mice in vivo.

1. Sesquiterpenes, constituents of plant essential oil, are popular bioactive compounds due to the positive effect on human health, but their potential toxicity and possible herb-drug interactions are often omitted. In our in vivo study, we followed up the effect of p.o. administration of two sesquiterpenes ß-caryophyllene oxide (CAO) and trans-nerolidol (NER) on various xenobiotic-metabolizing enzymes in mice liver and small intestine. 2. To spot the early effect of studied compounds, enzymatic activity and mRNA levels were assessed 6 and 24 h after single dose. 3. CAO and NER markedly increased cytochromes P450 (CYP2B, 3A, 2C) activity and mRNA levels in both tissues. Liver also showed elevated activity of aldo-ketoreductase 1C and carbonyl reductase after treatment. Contrary, sesquiterpenes decreased NAD(P)H:quinone oxidoreductase 1 activity in small intestine. Among conjugation enzymes, only liver sulfotransferase activity was increased by sesquiterpenes. 4. Our results document that single dose of sesquiterpenes modulate activities and expression of several xenobiotic-metabolizing enzymes.

Autodigestion by migrated trypsin is a major factor in small intestinal ischemia-reperfusion injury.

BACKGROUND: The pathophysiological role of pancreatic digestive hydrolases in intestinal ischemia-reperfusion (I/R) injury is still not clear. Here, we studied whether ischemia-induced injury to the small intestine can be explained by the autodigestion hypothesis. MATERIALS AND METHODS: Mesenteric I/R was induced in rats by superior mesenteric artery occlusion (90 min) and reopening (120 min). Thirty minutes before superior mesenteric artery occlusion, aprotinin (14.7 mg/kg), orlistat (5 mg/kg), and their combination or α1-proteinase inhibitor (60 mg/kg) were injected into the lumen of the small intestine. Systemic and vital parameters, intestinal microcirculation, and mucosal barrier function were monitored during the observation phase; markers of small intestinal injury, as well as trypsin-, chymotrypsin-, elastase-, and lipase-like activities in intestinal effluates were assessed at the end. RESULTS: The pattern of small intestinal injury correlated inversely with the local alterations in microvascular tissue perfusion and corresponded with the intestinal distribution of trypsin-like activity. Aprotinin almost completely inhibited trypsin-like activity (P < 0.05) and significantly reduced intestinal tissue injury. Combined with orlistat, it also increased the postischemic blood pressure (P < 0.05) but not the intestinal barrier function. Macroscopic as well as the histologic alterations were decreased by α1-proteinase inhibitor, which significantly improved postischemic blood pressure (P < 0.05). CONCLUSIONS: The I/R-induced pattern of small intestinal injury is likely to result from both local differences in tissue ischemia and the digestive activity of migrated pancreatic trypsin. Therefore, administration of aprotinin and orlistat into ischemic small intestines may be a therapeutic option in patients with a poor diagnosis.

Inhibition of Human and Rat Sucrase and Maltase Activities To Assess Antiglycemic Potential: Optimization of the Assay Using Acarbose and Polyphenols.

We optimized the assays used to measure inhibition of rat and human α-glucosidases (sucrase and maltase activities), intestinal enzymes which catalyze the final steps of carbohydrate digestion. Cell-free extracts from fully differentiated intestinal Caco-2/TC7 monolayers were shown to be a suitable source of sucrase-isomaltase, with the same sequence as human small intestine, and were compared to a rat intestinal extract. The kinetic conditions of the assay were optimized, including comparison of enzymatic and chromatographic methods to detect the monosaccharide products. Human sucrase activity was more susceptible than the rat enzyme to inhibition by acarbose (IC50 (concentration required for 50% inhibition) = 2.5 ± 0.5 and 12.3 ± 0.6 µM, respectively), by a polyphenol-rich green tea extract, and by pure (-)-epigallocatechin gallate (EGCG) (IC50 = 657 ± 150 and 950 ± 86 µM respectively). In contrast, the reverse was observed when assessing maltase activity (e.g. , EGCG: IC50 = 677 ± 241 and 14.0 ± 2.0 µM for human and rat maltase, respectively). 5-Caffeoylquinic acid did not significantly inhibit maltase and was only a very weak inhibitor of sucrase. The data show that for sucrase and maltase activities, inhibition patterns of rat and human enzymes are generally qualitatively similar but can be quantitatively different.

Modulatory Effect of an Isolated Triglyceride from Fenugreek Seed Oil on of α-Amylase, Lipase and ACE Activities, Liver-Kidney Functions and Metabolic Disorders of Diabetic Rats.

This study was designed to examine physicochemical characteristics, chemical compositions and biological activities of fenugreek seed oil (FSO) and its pure triglyceride (TG). One fenugreek TG was purified using a bioassay-guided fractionation and administrated to surviving diabetic rats. The free fatty acids percentage as well as, the peroxide, the saponification and the iodine values were 2%, 12 mequiv. O2/kg of oil, 189 (mg KOH/g) and 110 (g/100 g of oil), respectively. Linolenic acid (C18:3 26.14%), Linoleic acid (C18:2 41.13%) and Oleic acid (C18:1 17.07%) were the dominant fatty acids in the FSO. ß-sitosterol was the major sterol (85.3%) in the FSO. LnLnO (17.1%), LLL (16.6%), OLL and OOLn (8.4%), were the abundant triglycerides. The hexane extract of fenugreek seed (exhibiting the powerful inhibitory activity against alpha-amylase) was purified using a bioassay-guided fractionation affording one fenugreek TG: (11Z)-11- eicosenoic acid 2, 3- bis[((9Z, 12Z, 15Z)-1-oxo-9, 12, 15-octadecatrien-1-yl)oxy] propyl ester. In diabetic rats, the administration of the fenugreek TG inhibited α-amylase activity in small intestine by 36% as compared to untreated diabetic rats. Moreover, fenugreek TG increased insulin sensibility which leads to decrease in blood glucose level by 43%. In addition, this study demonstrated that administration of pure fenugreek TG to diabetic rats ameliorated the glycogen rate in liver and muscle. In addition, the administration of fenugreek TG reverted back the activity of angiotensin converting enzyme respectively in kidney and plasma by 33 and 29%. Interestingly, the fenugreek TG inhibited lipase activity in small intestine by 33% which leads to the regulation of lipid profile. Moreover, the fenugreek TG protected liver-kidney function evidenced by histological study. In conclusion, our finding demonstrates that the administration of fenugreek TG to diabetic rats can make it a potential candidate for industrial application as a pharmacological agent for the treatment of hyperglycemia.

Effect of increasing the proportion of dietary concentrate on gastrointestinal tract measurements and brush border enzyme activity in Holstein steers.

The aim of this study was to determine the time course for adaptation of the reticulo-rumen, omasum, abomasum, and small intestine in response to an abrupt increase in the proportion of grain in the diet. Adaptive responses include tissue and digesta mass, small intestinal length, and brush border enzyme activity in the duodenum, proximal jejunum, and ileum. Twenty-five Holstein steers (213 ± 23 kg; 5 to 7 mo of age) were blocked by body weight, and within block were randomly assigned to 1 of 5 treatments: the control diet (CTRL; 92% chopped grass hay and 8% mineral and vitamin supplement on a dry matter basis) or a moderate grain diet (MGD; 50% chopped grass hay, 42% rolled barley grain, and 8% mineral and vitamin supplement) that was fed for 3 (MGD3), 7 (MGD7), 14 (MGD14), or 21 d (MGD21). Dry matter intake was limited to 2.25% of body weight to ensure that changes in dry matter intake did not confound the results. On the last day of the dietary exposure, steers were slaughtered 2 h after feeding. Reticulo-rumen tissue mass and ruminal epithelium mass in the ventral sac of the rumen were not affected by the MGD. Wet reticulo-ruminal digesta mass decreased from CTRL to MGD7 and then increased, but reticulo-ruminal digesta dry matter mass did not differ between treatments. Omasal mass, omasal tissue mass, and omasum digesta mass decreased linearly with the number of days fed MGD, but abomasal tissue mass tended to increase linearly. Duodenal tissue mass tended to increase linearly, and ileal length increased linearly with the number of days fed MGD. Lactase activity in the proximal jejunum increased linearly and maltase activity in duodenum tended to increase linearly with days fed MGD. Aminopeptidase N activity in the proximal jejunum increased cubically with days fed MGD, and dipeptidylpeptidase IV activity in ileum tended to decrease from CTRL to MGD14 and then tended to increase. Adaptation to a diet with a greater proportion of concentrate involves changes in the mass and length of regions of the gastrointestinal tract and brush border enzyme activity. These changes take place gradually over at least 3 wk.

In vitro digestibility of highly concentrated methylcellulose O/W emulsions: rheological and structural changes.

The changes in structure during the digestion of highly concentrated methyl cellulose (MC) O/W emulsions and of hydrated MC were investigated. The effect of human saliva and in vitro stomach digestion was attributed to a dilution effect, rather than to pH or pepsin activity. After in vitro intestine incubation, a decrease in viscoelasticity and an increase in fat globule size were observed. The fat released after the digestion of the MC emulsion was 49.8% of the initial fat, indicating the existence of a big physical impediment. In comparison with an O/W whey protein emulsion with fat content equal to the fat released during the MC emulsion digestion, a 12% reduction in free fatty acid formation was found, which indicates that the decrease in fat bioaccessibility in the MC emulsion should be attributed not only to a physical effect against fat release but also to a further impediment related to the fat digestion process. Fat released quantification informs about the physical retention of fat in the emulsion matrix structure. Enzymes may not act if fat is not released and solubilized. Free fatty acid quantification is the real indicator of fat digestion, but contrary to the total fat released, it is affected by a wide variety of enzymatic factors, which should be considered for the correct comparison of systems of different properties, for example systems where the amount of fat release during the digestion may be different or initially unknown.

Hydrophobic substituents increase the potency of salacinol, a potent α-glucosidase inhibitor from Ayurvedic traditional medicine 'Salacia'.

Using an in silico method, seven analogs bearing hydrophobic substituents (8a: Me, 8b: Et, 8c: n-Pent, 8d: n-Hept, 8e: n-Tridec, 8f: isoBu and 8g: neoPent) at the 3'-O-position in salacinol (1), a highly potent natural α-glucosidase inhibitor from Ayurvedic traditional medicine 'Salacia', were designed and synthesized. In order to verify the computational SAR assessments, their α-glucosidase inhibitory activities were evaluated in vitro. All analogs (8a-8g) exhibited an equal or considerably higher level of inhibitory activity against rat small intestinal α-glucosidases compared with the original sulfonate (1), and were as potent as or higher in potency than the clinically used anti-diabetics, voglibose, acarbose or miglitol. Their activities against human maltase exhibited good relationships to the results obtained with enzymes of rat origin. Among the designed compounds, the one with a 3'-O-neopentyl moiety (8g) was most potent, with an approximately ten fold increase in activity against human maltase compared to 1.

Sulfate conjugation of daphnetin by the human cytosolic sulfotransferases.

ETHNOPHARMACOLOGICAL RELEVANCE: In Turkey, daphnetin-containing Daphne oleoides is used as a folk medicine for treating rheumatic pain and lumbago. A daphnetin-containing traditional Chinese medicine tablet, named Zushima-Pian, is available in China for treating rheumatoid arthritis. The present study aimed to investigate the metabolism of daphnetin through sulfation in cultured human cells and to identify the human cytosolic sulfotransferase(s) (SULT(s)) that is(are) capable of mediating the sulfation of daphnetin. MATERIALS AND METHODS: Cultured HepG2 human hepatoma cells and Caco-2 human colon carcinoma cells were labeled with [(35)S]sulfate in the presence of different concentrations of daphnetin. Thirteen known human SULTs, previously expressed and purified, as well as cytosols of human kidney, liver, lung, and small intestine, were examined for daphnetin-sulfating activity using an established sulfotransferase assay. RESULTS: [(35)S]sulfated daphnetin was found to be generated and released by HepG2 cells and Caco-2 cells labeled with [(35)S] sulfate in the presence of daphnetin. Among the 13 known human SULTs, SULT1A1, SULT1A2, SULT1A3, SULT1B1, and SULT1C4 displayed significant sulfating activity toward daphnetin. Of the four human organ samples later tested, small intestine and liver cytosols displayed considerably higher daphnetin-sulfating activity than those of lung and kidney. CONCLUSION: The results derived from the present study showed unequivocally that daphnetin could be sulfated in cultured human cells and by purified human SULT enzymes as well as human organ cytosols. The information obtained provided a basis for further studies on the metabolism of daphnetin through sulfation in vivo.

Pomegranate peel extract decreases small intestine lipid peroxidation by enhancing activities of major antioxidant enzymes.

BACKGROUND: Pomegranate peel extract (PPE) contains several compounds with antioxidative properties. PPE added to foods may interact with endogenous antioxidants and promote health. However, little is known about the biochemical mechanisms by which PPE exerts their actions on tissues of biological systems in vivo. The purpose of this study was to determine the effects of PPE on activities of antioxidant enzymes. Mice were used to investigate the effects of PPE on plasma levels of malondialdehyde (MDA), tissue MDA content and activities of superoxide dismutase 1 (SOD1), SOD2 and glutathione peroxidase (GPX) in the small intestine, liver and skeletal muscle - different tissues involved in the digestion, absorption and metabolism of dietary nutrients. Control mice were fed a standard diet, whereas treated mice were fed for 40 days with the standard diet containing 5% or 10% PPE. RESULTS: Mice fed the 10% PPE diet exhibited lower plasma MDA concentrations, reduced content of MDA in the small intestine and liver and higher levels of SOD1 and GPX activities in the small intestine compared to mice fed the control diet. CONCLUSIONS: These findings demonstrate that intake of PPE in diet attenuates small intestine lipid peroxidation and strengthens the first line of small intestine antioxidant defense by enhancing enzymatic antioxidative pathways. PPE is worthy of further study as a therapeutic approach to prevent peroxidative stress-induced gut pathogenesis. © 2015 Society of Chemical Industry.

Enzymatic Formation of Novel Ginsenoside Rg1-α-Glucosides by Rat Intestinal Homogenates.

The variation of linkage positions in ginsenosides leads to diverse pharmacological efficiencies. The hydrolysis and transglycosylation properties of glycosyl hydrolase family enzymes have a great impact on the synthesis of novel and structurally diversified compounds. In this study, six ginsenoside Rg1-α-glucosides were found to be synthesized from the reaction mixture of maltose as a donor and ginsenoside Rg1 as a sugar acceptor in the presence of rat small intestinal homogenates, which exhibit high α-glucosidase activities. The individual compounds were purified and were identified by spectroscopy (HPLC-MS, (1)H-NMR, and (13)C-NMR) as 6-O-[α-D-glcp-(1→4)-ß-D-glcp]-20-O-(ß-D-glcp)-20(S)-protopanaxatriol, 6-O-ß-D-glcp-20-O-[α-D-glcp-(1→6)-(ß-D-glcp)]-20(S)-protopanaxatriol, 6-O-ß-D-glcp-20-O-[α-D-glcp-(1→4)-(ß-D-glcp)]-20(S)-protopanaxatriol, 6-O-[α-D-glcp-(1→6)-ß-D-glcp]-20-O-(ß-glcp)-20(S)-protopanaxatriol, 6-O-[α-D-glcp-(1→3)-ß-D-glcp]-20-O-(ß-D-glcp)-20(S)-protopanaxatriol, and 6-O-ß-D-glcp-20-O-[α-D-glcp-(1→3)-(ß-D-glcp)]-20(S)-protopanaxatriol. Among these six, 6-O-ß-D-glcp-20-O-α-D-glcp-(1→6)-(ß-D-glcp)-20(S)-protopanaxatriol and 6-O-α-D-glcp-(1→6)-ß-D-glcp-20-O-(ß-D-glcp)-20(S)-protopanaxatriol are considered to be novel compounds of alpha-ginsenosidal saponins which pharmacological activities should be further characterized. This is the first report on the enzymatic elaboration of ginsenoside Rg1 derivatives using rat intestinal homogenates. To the best of our knowledge, it is also the first to reveal the sixth and 20th positions of an unusual α-D-glucopyranosyl-(1→6)-ß-D-glucopyranosyl sugar chain with 20(S)-protopanaxatriol saponins in Panax ginseng Mayer.

Cranberry extract-enriched diets increase NAD(P)H:quinone oxidoreductase and catalase activities in obese but not in nonobese mice.

Consumption of antioxidant-enriched diets is 1 method of addressing obesity, which is associated with chronic oxidative stress and changes in the activity/expression of various enzymes. In this study, we hypothesized that the modulation of antioxidant enzymes and redox status through a cranberry extract (CBE)-enriched diet would differ between obese and nonobese mice. The CBE used in this study was obtained from the American cranberry (Vaccinium macrocarpon, Ericaceae), a popular constituent of dietary supplements that is a particularly rich source of (poly)phenols and has strong antioxidant properties. The present study was designed to test and compare the in vivo effects of 28-day consumption of a CBE-enriched diet (2%) on the antioxidant status of nonobese mice and mice with monosodium glutamate-induced obesity. Plasma, erythrocytes, liver, and small intestine were studied concurrently to obtain more complex information. The specific activities, protein, and messenger RNA expression levels of antioxidant enzymes as well as the levels of malondialdehyde and thiol (SH) groups were analyzed. Cranberry extract treatment increased the SH group content in plasma and the glutathione S-transferase activity in the erythrocytes of the obese and nonobese mice. In addition, in the obese animals, the CBE treatment reduced the malondialdehyde content in erythrocytes and increased NAD(P)H: quinone oxidoreductase (liver) and catalase (erythrocytes and small intestine) activities. The elevation of hepatic NAD(P)H: quinone oxidoreductase activity was accompanied by an increase in the corresponding messenger RNA levels. The effects of CBE on the activity of antioxidant enzymes and redox status were more pronounced in the obese mice compared with the nonobese mice.