3 research outputs found
Anti-α-glucosidase and Anti-dipeptidyl Peptidase-IV Activities of Extracts and Purified Compounds from Vitis thunbergii var. <i>taiwaniana</i>
Ethanol extracts (Et) from the stem
(S) and leaf (L) of Vitis thunbergii var. <i>taiwaniana</i> (VTT) were used to investigate
yeast α-glucosidase and porcine
kidney dipeptidyl peptidase-IV (DPP-IV) inhibitory activities. Both
VTT-Et showed complete α-glucosidase inhibition at 0.1 mg/mL;
VTT-S-Et and VTT-L-Et showed 26 and 11% DPP-IV inhibition, respectively,
at 0.5 mg/mL. The VTT-Et interventions (20 and 50 mg/kg) resulted
in improvements in impaired glucose tolerance of diet-induced obese
rats. (+)-Hopeaphenol, (+)-vitisin A, and (−)-vitisin B were
isolated from the ethyl acetate fractions of S-Et and showed yeast
α-glucosidase inhibition (IC<sub>50</sub> = 18.30, 1.22, and
1.02 μM) and porcine kidney DPP-IV inhibition (IC<sub>50</sub> = 401, 90.75, and 15.3 μM) compared to acarbose (6.39 mM)
and sitagliptin (47.35 nM), respectively. Both (+)-vitisin A and (−)-vitisin
B showed mixed noncompetitive inhibition against yeast α-glucosidase
and porcine kidney DPP-IV, respectively. These results proposed that
VTT extracts might through inhibitions against α-glucosidase
and DPP-IV improve the impaired glucose tolerance in diet-induced
obese rats
135-Day Interventions of Yam Dioscorin and the Dipeptide Asn-Trp (NW) To Reduce Weight Gains and Improve Impaired Glucose Tolerances in High-Fat Diet-Induced C57BL/6 Mice
The
C57BL/6J mice were fed a 135-day normal diet or a high-fat
diet (HFD) without, or concurrent with, a single yam dioscorin (80
mg/kg) or dipeptide NW (40 mg/kg) intervention every day. The final
body weights (g) of mice were 26.1 ± 1.4, 34.97 ± 2.1, 31.75
± 2.6, and 31.66 ± 3.1, respectively, for normal diet-fed,
HFD-fed, dioscorin-intervened, and NW-intervened group. The mice in
both intervened groups showed similar less weight gains and had significant
differences (<i>P</i> < 0.05) compared to those in the
HFD group under the same cumulative HFD intakes. The blood biochemical
index of mice with dioscorin interventions showed significantly lower
contents in total cholesterol and low-density lipoprotein, and NW
interventions showed significantly lower total triglyceride contents
compared to those of the HFD group (<i>P</i> < 0.05).
Both intervened mice exhibited similar reductions in total visceral
lipid contents and have significant differences compared to those
of the HFD group (<i>P</i> < 0.05). The dioscorin intervention
was better than NW interventions in lowering blood glucose levels
by oral glucose tolerance tests and both showed significant differences
(<i>P</i> < 0.05) compared to those in the HFD group.
Yam dioscorin or dipeptide NW will potentially be used for preventive
functional foods of less body weight gains and impaired glucose tolerance
controls, which require further clinical trial investigations
Data_Sheet_1_Design of Diarylheptanoid Derivatives as Dual Inhibitors Against Class IIa Histone Deacetylase and β-amyloid Aggregation.PDF
<p>Alzheimer’s disease (AD) is a progressive neurodegenerative disorder with multiple etiologies. Beta-amyloid (Aβ) self-aggregation and overexpression of class IIa histone deacetylases (HDACs) are strongly implicated with AD pathogenesis. In this study, a series of novel diarylheptanoid derivatives were designed, synthesized and evaluated for use as dual Aβ self-aggregation and class IIa HDAC inhibitors. Among these compounds, 4j, 5c, and 5e displayed effective inhibitions for Aβ self-aggregation, HDAC5 activity and HDAC7 activity with IC<sub>50</sub> values of <10 μM. The compounds contain three common features: (1) a catechol or pyrogallol moiety, (2) a carbonyl linker and (3) an aromatic ring that can function as an HDAC cap and create hydrophobic interactions with Aβ<sub>1-42</sub>. Furthermore, compounds 4j, 5c, and 5e showed no significant cytotoxicity to human neuroblastoma SH-SY5Y cells and also exhibited neuroprotective effect against H<sub>2</sub>O<sub>2</sub>-induced toxicity. Overall, these promising in vitro data highlighted compounds 4j, 5c, and 5e as lead compounds that are worthy for further investigation.</p