Nine terpenylated coumarins, namely 7-(E)-3′,7′-dimethyl-6′-oxo-2′,7′-octadienyloxy-coumarin (1), schinilenol (2), schinindiol (3), collinin (4), ...7-(E)-7′-hydroxy-3′,7′-dimethy-locta-2′,5′-dienyloxy-coumarin (5), 8-methoxyanisocoumarin (6), 7-(6′R-hydroxy-3′,7′-dimethyl-2′E,7′-octadienyloxy)coumarin (7), (E)-4-methyl-6-(coumarin-7′-yloxy)hex-4-enal (8), and aurapten (9), along with a 4-quinolone alkaloid (10) and integrifoliodiol (11), were isolated from the leaves of Zanthoxylum schinifolium. Of the isolates, compounds 4 and 7 potentially inhibited NO production in lipopolysaccharide (LPS)-stimulated macrophage RAW264.7 cells, with IC₅₀ values of 5.9 ± 0.8 and 18.2 ± 1.8 μM, respectively. Furthermore, compounds 4 and 7 dose-dependently reduced the LPS-induced iNOS expression. Moreover, pre-incubation of cells with 4 and 7 significantly suppressed LPS-induced COX-2 protein expression. In addition, compounds 4, 7, 8, and 10 showed strong α-glucosidase inhibitory effects, with IC₅₀ values of 92.1 ± 0.7, 90.6 ± 0.9, 78.2 ± 0.2, and 82.4 ± 0.8 μM, respectively. Compounds 1, 5, and 11 displayed moderate effects with IC₅₀ values of 161.6 ± 0.3, 164.4 ± 1.1, and 155.4 ± 0.9 μM, while acarbose, a positive control, possessed an IC₅₀ value of 121.5 ± 1.0 μM. This is the first investigation on the α-glucosidase inhibitory effect of components from Zanthoxylum schinifolium. Further studies should be made on active compounds.
Enterobacter sakazakii can cause fatal invasive infection of neonates associated with the presence of this organism in powdered infant milk formula. A new chromogenic medium (Druggan–Forsythe–Iversen ...agar, DFI) is described for the selective detection of this emergent pathogen. The medium is based on the α-glucosidase reaction which is detected using 5-bromo-4-chloro-3-indolyl-α,
d-glucopyranoside (XαGlc).
Ent. sakazakii hydrolyses this substrate to an indigo pigment, producing blue-green colonies on this medium. DFI was compared with the current method of detection on violet red bile glucose agar (VRBGA) followed by pigment production on tryptone soy agar (TSA) after 48–72 h at 25 °C and subsequent biochemical profile determination using Biomerieux API20E. Ninety-five clinical and food strains of
Ent. sakazakii were detected on the DFI chromogenic medium 2 days sooner than the alternative method. The characteristics of 148 strains representing 17 genera of non-
Ent. sakazakii Enterobacteriaceae were compared using the two methods. Only 16/18
Escherichia vulneris strains, 2/3 strains of
Pantoea spp. and 1/8
Citrobacter koseri strains gave false positive results on DFI agar.
Eight α-glucosidase positive strains were identified as
Pantoea using their API20E biochemical profile, but had higher percentage identification as
Ent. sakazakii using ID32E. Therefore the DFI medium enables the detection of
Ent. sakazakii within mixed cultures of Enterobacteriaceae, whereas the organism could be missed when using VRBGA since the latter is a general Enterobacteriaceae selective medium. In addition, the common use of API20E to check yellow pigmented colonies on TSA may lead to false negative results and consequently the acceptance of a batch of infant formula milk (IFM) that contains
Ent. sakazakii.
Objectives To evaluate sperm quality, levels of markers of epididymal and accessory gland function, and T in semen from men grouped according to their body mass index (BMI). Design Blind prospective ...study. Setting Andrology and reproduction laboratory in Cordoba, Argentina (2006–2007). Patient(s) Seven hundred ninety-four men. Intervention(s) N one. Main Outcome Measure(s) In semen samples, sperm quality (volume, density, motility, morphology, viability, hypoosmotic swell test, and nuclear maturity) and levels of neutral alpha-glucosidase, fructose, citric acid and T. Result(s) Multivariate analysis showed a negative association between BMI and motility, rapid motility and neutral alpha-glucosidase levels, and a positive association between BMI and seminal fructose levels. No associations were found among BMI and sperm concentration, the other parameters evaluated, or seminal T levels. Conclusion(s) Results found in our study support a deleterious effect of obesity on seminal quality, probably by alterations in the function of the epididymis (i.e., in epididymal maturation).
This study aimed at investigating the effect of dietary zinc on performance, jejunal brush border membrane enzyme activities and mRNA levels of enzymes and two zinc transporters in piglets. A total ...of 126 piglets were weaned at 26 ±1 days of age and randomly allocated into three groups fed with diets 50, 150 and 2500 mg zinc/kg. Performance was recorded and at weekly intervals, eight piglets per group were killed. The activities of isolated brush border membrane enzymes including lactase, maltase, sucrase, aminopeptidase-N and intestinal alkaline phosphatase (IAP), and the relative transcript abundance of aminopeptidase-N (APN), sucrase–isomaltase (SUC), IAP and the two zinc transporters SLC39A4 (ZIP4) and SLC30A1 (ZnT1) were investigated in the jejunum. Feeding pharmacological zinc levels increased weight gain (p < 0.001) during the first week, but performance was lower (p < 0.05) in the third week. Organ zinc concentrations were increased by high dietary zinc level. The activity of IAP was higher (p < 0.05) with the highest dietary zinc level, no effects were determined for other enzymes. Dietary zinc level had no effect on transcript abundance of digestive enzymes. The mRNA levels decreased (p < 0.001) for ZIP4, and increased for ZnT1 (p < 0.05) with pharmacological zinc levels. In conclusion, pharmacological zinc levels improved performance in the short-term. Intestinal mRNA level of zinc transporters changed with high zinc supply, but this did not prevent zinc accumulation in tissues, suggesting hampered homoeostatic regulation. This might cause impaired performance during longer supply.
Pompe disease, a severe and often fatal neuromuscular disorder, is caused by a deficiency of the lysosomal enzyme acid alpha-glucosidase (GAA). The disease is characterized by the accumulation of ...excess glycogen in the heart, skeletal muscle, and CNS. Currently approved enzyme replacement therapy or experimental adeno-associated virus (AAV)-mediated gene therapy has little effect on CNS correction. Here we demonstrate that a newly developed AAV-PHP.B vector can robustly transduce both the CNS and skeletal muscles in GAA-knockout (GAAKO) mice. A single intravenous injection of an AAV-PHP.B vector expressing human GAA under the control of cytomegalovirus (CMV) enhancer-chicken β-actin (CB) promoter into 2-week-old GAAKO mice resulted in widespread GAA expression in the affected tissues. Glycogen contents were reduced to wild-type levels in the brain and heart, and they were significantly decreased in skeletal muscle by the AAV treatment. The histological assay showed no visible glycogen in any region of the brain and spinal cord of AAV-treated mice. In this study, we describe a set of behavioral tests that can detect early neurological deficits linked to extensive lysosomal glycogen accumulation in the CNS of untreated GAAKO mice. Furthermore, we demonstrate that the therapy can help prevent the development of these abnormalities.
Kaempferia galanga rhizome (KGR) is a stemless, sweet-smelling, enduring, and rhizomatous monocotyledonous plant of the ginger family also called sand ginger or kencur. lt possesses many ...pharmacological effects and the goal of this study is to use several solvent solutions to determine the antioxidant and anti-diabetic potential of KGR. By observing KGR's alpha-glucosidase and alpha-amylase inhibitory activity, the in vitro diabetic activity was assessed. The in vitro cancer preventive action was evaluated by doing the 2,2-diphenyl-1-picrylhydrazyl test. The outcomes of the study showed increase in dose-dependent percentage of inhibition in α-amylase and α-glucosidase activity for both extract and standard ranging from 100 to 500 μg/ml. The current review proposes that the concentrate of KGR could be utilized for the treatment of diabetes mellitus as well with respect to dealing with the oxidative stress-related diseases.
We investigated the structural effects of metabolite analogs derived from a naturally-occurring zwitterionic metabolite, glycine betaine, on the activity of several hydrolases. The initial velocities ...of the hydrolases were enhanced by the addition of the solutes into the buffer solution. Based on a detailed study using α-glucosidases, the acceleration efficiency of the enzymatic activity was strongly induced by solutes possessing bulky and aliphatic ammonium cations, indicating that enhancement of activity by the solutes depended on their chemical structures. Kinetic analysis revealed that the acceleration of the hydrolysis reaction was related to both the decrement of
K
m and increment of
V
max values. Furthermore, the addition of the metabolite analogs enhanced not only the rate constant but also the thermostability, salt tolerance, and substrate specificity of α-glucosidase simultaneously through the reduction of conformational perturbation of the enzyme.
► Coumestrol shows the most potent α-glucosidase inhibition of all soy bean leaf extracts. ► Coumestrol starts to accumulate in soybean leaves from 84days after sowing. ► A new α-glucosidase ...inhibitor, Glyceollin V was isolated from soybean leaves.
The leaves of soybean (Glycine max) were extracted into four different polar solvents: ethylacetate, butanol, ethanol and water. The ethylacetate extract (EE) showed the lowest IC50 value against α-glucosidase (70.1μg/ml). To investigate the compounds responsible for this effect, activity guided fractionation of soybean leaves by chromatography yielded seven phenolic compounds which were identified as formononetin (1), afromosin (2), coumestrol (3), isotrifoliol (4), phaseol (5), glyceofuran (6) and a new compound, glyceollin V (7). Importantly, coumestrol 3 was not only the most potent component with IC50=6.0μM, but also the most abundant polyphenol in soybean leaves. There was shown to be an increasing inhibition across the developmental stage of the plant, which correlated strongly with an increase in compound 3 in the leaves. In fact, we have shown it can comprise up to 65% of the polyphenols in the leaves by HPLC analysis.
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