Recent studies have documented the importance of postprandial hyperglycaemia in the incidence of chronic diseases, including type 2 diabetes. Inhibition of digestive enzymes, including membrane-bound brush-border α-glucosidases, leads to slowed carbohydrate digestion and absorption, and reduced postprandial glycemia. Nuts are widely eaten around the world and have the potential to inhibit α-glucosidases through their content of polyphenols and other bioactive compounds. According to our recent systematic review(1), no study has investigated the inhibitory effects of nut extracts on human α-glucosidase activities. Almost all studies in this area have been conducted on yeast α-glucosidase, with only a few using rat α-glucosidase. While there is no sequence homology between yeast and human α-glucosidase, there is 74% to 78% sequence homology between rat and human α-glucosidases(1). The lack of studies on the effect of bioactive compounds from nuts on human α-glucosidases, along with the growing attention to nuts as an important component of a healthy diet with the potential to reduce the risk of chronic diseases(2), highlights the need for research to evaluate the inhibitory effect of nut extracts on human α-glucosidases. The aim of the current study is to explore the inhibitory effect of extracts from nuts on human carbohydrate digestive enzymes. Walnuts and almonds were ground and defatted with hexane, extracted in 80% (v/v) acetone, and further purified using solid-phase extraction to obtain phenolic-rich extracts. The Folin–Ciocalteu assay was used to approximate the polyphenol content of the samples. Following our recently published detailed protocol(3), cell-free extracts from human intestinal Caco-2/TC7 cells were used as a source of α-glucosidase in enzyme inhibition assays, with sucrose, maltose and isomaltose as substrates and appropriate controls. The assay products were quantified using high-performance anion exchange chromatography with pulsed amperometric detection (HPAEC-PAD). Glucose production in the presence of various concentrations of phenol-rich nut extracts was compared using a one-way ANOVA and half-maximal inhibitory concentration (IC50) values were calculated. The Folin–Ciocalteu data demonstrate that walnut extracts comprise a relatively high polyphenol content, with 18.1 ± 0.23 mg (epigallocatechin gallate [EGCG] equivalent) per gram of fresh weight, while almond extracts contain 0.87 ± 0.03 mg EGCG equivalent/g of fresh weight. The walnut phenolic-rich extract dose-dependently inhibited human intestinal sucrase and maltase activities (both p<0.01), with IC50 values of 1.67 mg/mL and 2.84 mg/mL, respectively. We demonstrate that phenolic-rich walnut extracts can inhibit human α-glucosidases in vitro and therefore walnuts may contribute to slowing carbohydrate digestion in humans. As such, we plan to assess the effects of walnuts on postprandial glycaemia in vivo.

We previously reported that the addition of a specified mulberry fruit extract (MFE) to rice consistently reduces post-prandial glycaemic (PPG) and post-prandial insulinemic (PPI) responses. This research tested whether this effect generalises to a broad range of rice types, reflecting the wide variation in rice characteristics known to influence glycaemic responses. In a randomised, balanced, partial factorial crossover design, Sona Masoori (SM), Bora Saul (BS), Gobindobogh (Gb) and Banskati (Bn) rices were tested with and without 0·37 g MFE. Healthy, normal-weight Indian adults (N 120) each consumed four of the eight possible boiled rice meals, all containing about 50 g available carbohydrate. The primary outcome was the effect of MFE on PPG, expressed as the percentage change in the positive, incremental AUC over 2 h. The mean effect of MFE on PPG for all rice types combined was −11·4 % (P < 0·003). The reduction in PPG was in a qualitatively similar range for all rice types (–9·8 to −15·1 %), and this was statistically significant for Bn. MFE also reduced the corresponding PPI response to all rice types combined by a mean of 10·1 % (P < 0·001; range −6·1 to −13·4 %), and the reduction in PPI was statistically significant for SM, Gb and BS. In conclusion, addition of 0·37 g MFE modestly reduced PPG and PPI responses to rices in general, and the effects were statistically significant for specific rice types.

Studies were conducted to test if dicamba reduces haloxyfop herbicidal activity and to determine if this interaction by auxin-type herbicides or bentazon was caused by preventing the haloxyfop-induced inhibition of acetyl-CoA carboxylase (ACCase). Addition of dicamba at concentrations of 2.17 or 4.34 mM reduced haloxyfop activity on tall fescue shoots. Haloxyfop at 14 to 20 μM inhibited the activity of ACCase in cell-free extracts from tall fescue by nearly 50%. Dicamba did not prevent the inhibitory effect of haloxyfop on ACCase activity in these cell-free enzyme preparations. Dicamba alone at concentrations as high as 3.2 mM had no significant effect on the in vitro activity of the enzyme. Bentazon concentrations up to 10 mM did not prevent haloxyfop inhibition of ACCase activity. Bentazon alone or mixed with haloxyfop significantly inhibited ACCase activity at bentazon concentrations starting at 1 mM with near 40% inhibition at 10 mM. of the numerous possible explanations for the interference of dicamba or bentazon with haloxyfop action, interaction directly at the enzyme level appears to have been eliminated.

Tomato and pepper differ in their whole-plant tolerance to sulfonylurea (SU) herbicides rimsulfuron and halosulfuron despite both being members of the Solanaceae family. This study examined whether tomato's tolerance to SU herbicides rimsulfuron and halosulfuron was due to insensitivity of the target enzyme acetolactate synthase (ALS). Rimsulfuron and halosulfuron inhibited ALS from both tomato and pepper leaves. Enzyme inhibition and kinetic analyses showed that extractable ALS from tomato was more sensitive to rimsulfuron and halosulfuron than ALS from pepper. ALS from both species were inhibited with a mixed inhibition pattern. Thus, results indicate that enzyme insensitivity is not the reason why tomato is more tolerant than pepper to these herbicides. Tomato tolerance to rimsulfuron at the whole-plant level was reduced in the presence of terbufos, a known inhibitor of cytochrome P450 enzymes. Rimsulfuron applied at 0.018 and 0.035 kg ha−1 with 1.1 kg ha−1 of terbufos reduced tomato shoot weight 69 and 66%, respectively, compared with a 4 and 29% reduction when rimsulfuron was applied alone. The reduction of tomato tolerance to rimsulfuron by terbufos suggests that the sensitivity differences between these species may reflect their differences in SU herbicide metabolism.

Several seed production fields of the Italian ryegrass cultivar ‘Tetrone’ were destroyed in 1988 by 280 to 350 g ai ha−1 racemic fenoxaprop applied for wild oat control. Because similar rates of fenoxaprop had possessed adequate safety when applied to ‘Oregon common’ Italian ryegrass, suspicion arose that the cultivars differed in tolerance. Seedlings of 21 commonly grown cultivars were screened in the greenhouse at the three-leaf growth stage to determine their fresh weight GR50 for fenoxaprop. The GR50 values for the two most tolerant cultivars, ‘Marshall’ and ‘Torero’, were more than threefold greater than the two most sensitive cultivars, ‘Futaharu’ and ‘Ace’. Cultivars could be separated into sensitive, intermediate, and tolerant groups, but the distribution of the GR50 values appeared to be continuous rather than discrete. Tolerance increased with growth stage, and the average GR50 for tillered plants was 80% higher than that for the two-leaf stage and 41% higher than that for the four-leaf stage seedlings. Cultivars differed slightly in the specific activity of acetyl–coenzyme A carboxylase (ACCase) (EC 6.4.1.2) and in the I50 values for the inhibition by fenoxaprop, but the only clear relationship between these biochemical factors and whole-plant tolerance was a threefold increase in ACCase activity at the tillered stage over that present in the younger seedlings.

In 1996 a common sunflower population near Howard, SD, was suspected to be cross-resistant to imazethapyr and chlorimuron. Whole-plant acetolactate synthase (ALS) assays confirmed ALS-inhibitor resistance in the Howard biotype. The I 50 values (inhibition of 50% of the enzyme activity) indicated that the resistant population required 39 and 9 times more imazethapyr and chlorimuron, respectively, to obtain the same level of enzyme inhibition compared with the sensitive biotype. Herbicide dose response data supported the whole-plant enzyme assay data; control (> 90%) was not achieved with less than a four-times application rate of chlorimuron. Control with imazethapyr was not achieved even with a 16-times rate. Chlorimuron and imazethapyr controlled 70 and 95% of the population, respectively, when a four-times rate of each herbicide was applied separately. Differences in 14C-herbicide absorption were observed, suggesting that there may be physical or chemical differences in leaf surface composition between the resistant and sensitive biotypes. Although translocation of 14C-herbicide was less in the resistant biotype than in the sensitive biotype, the differences were not enough to explain chlorimuron and imazethapyr selectivity between the two biotypes. Overall results suggested that the differences in the common sunflower populations were attributed to an altered site of action on the ALS enzyme.

In liver, through the reaction catalysed by alanine aminotransferase (ALT), alanine becomes an effective precursor for gluconeogenesis. In the present study amino-oxyacetate (AOA) was used to evaluate its effect on liver ALT activity of the carnivorous fish Sparus aurata. Moreover, the derived metabolic effects on metabolites and other key enzymes of glycolysis, gluconeogenesis and the pentose phosphate pathway were also studied. A dose-effect-dependent inhibition of AOA on hepatic cytosolic and mitochondrial ALT activity was observed in vitro. In vivo, AOA behaved as an inhibitor of hepatic cytosolic ALT activity. A long-term exposure to AOA increased pyruvate kinase activity in the liver irrespective of the composition of the diet supplied to fish. 1H NMR studies showed that inclusion of AOA to the diet decreased the hepatic levels of alanine, glutamate and glycogen. Moreover, 2H NMR analysis indicated a higher renewal rate for alanine in the liver of fish fed with a high-carbohydrate/low-protein diet, while AOA decreased alanine 2H-enrichment irrespective of the diet. The present study indicates that AOA-dependent inhibition of the cytosolic ALT activity could help to increase the use of dietary carbohydrate nutrients.

This article reviews the current knowledge regarding the hepatic cytochrome P450 system, with particular reference to its effect on psychotherapeutic medication. The metabolic processes – by which drugs are broken down in the liver by cytochrome P450 enzymes – are affected by genetic variation between individuals, inhibition and induction of these enzymes by other drugs, disease and age. Genetic influences and enzyme inhibition/induction are discussed in particular detail in this article.