• Journal of Life Science
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• v.33 no.10
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• pp.783-790
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• 2023

Modern people have an increased incidence of metabolic diseases due to changed eating habits, and diabetes is considered the most significant metabolic disease. Given that existing diabetes treatments are accompanied by side effects, the aim of this study was to identify traditional natural products that have anti-diabetic activity. The potential anti-diabetic and antioxidant activities of natural products were examined using 2,2-diphenyl-1-picrylhydrazyl (DPPH) free radical scavenging assay, α-glucosidase assay, and protein tyrosine phosphatase 1B (PTP1B) inhibition assay. Methanol extracts of Ulmus davidiana var. japonica, Acer tegmentosum branches, Nelumbo nucifera seeds, and Carthamus tinctorius seeds were found to have high anti-diabetic activity and further fractionated with solvents using ethyl acetate and butanol. Consequently, the ethyl acetate fraction of C. tinctorius seeds (MG-11-E) with high α-glucosidase and PTP1B inhibitory activity was selected. MG-11-E was subjected to preparative thin layer chromatography, and fraction #6 showed high α-glucosidase and PTP1B inhibitory activity. Fraction #6 was analyzed and fractionated via high performance liquid chromatography with 50% methanol as the mobile phase, and anti-diabetic activity was observed in the sample that eluted after 4 min as a single peak. The α-glucosidase inhibitory activity exhibited by this sample seemed to be greater than the PTP1B inhibitory activity; thus, it was concluded that a greater anti-diabetic therapeutic effect may be achieved by combining this agent with natural products that inhibit PTP1B activity.

• Journal of Applied Biological Chemistry
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• v.64 no.1
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• pp.89-96
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• 2021

The aim of this study is to examine the effect of Caulerpa okamurae ethanol extract (COE) on glucose metabolism and insulin sensitivity as one of the drug targets for treatment of type2 diabetes. COE significantly inhibited protein tyrosine phosphatase (PTP1B) and dipeptidyl peptidase-IV (DPP-IV) enzyme activities in vitro assay. Also, COE significantly enhanced the glucose uptake and the expression of insulin receptor substrate-1 (IRS-1) and glucose transporter4 (GLUT4) proteins in 3T3-L1 adipocytes or zebrafish larvae compared with control. In dexamethasone-induced resistance model of L6 myotubes, the protein expression of insulin signaling and glucose uptake was effectively increased by the treatment of COE. In contrast, the elevated phosphorylation of IRS-1 Ser307 was normally suppressed by treatment of COE. However, COE had no effect on insulin secretion in pancreatic beta cells. Thus, our results suggest that COE improves the glucose metabolism and insulin sensitivity through the regulation of insulin signaling and GLUT4 protein in insulin's target cells and zebrafish larvae.

• Molecules and Cells
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• v.41 no.3
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• pp.244-255
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• 2018

Low-grade pro-inflammatory state and leptin resistance are important underlying mechanisms that contribute to obesity-associated hypertension. We tested the hypothesis that Astragaloside IV (As IV), known to counteract obesity and hypertension, could prevent obesity-associated hypertension by inhibiting pro-inflammatory reaction and leptin resistance. High-fat diet (HFD) induced obese rats were randomly assigned to three groups: the HFD control group (HF con group), As IV group, and the As IV + ${\alpha}$-bungaratoxin (${\alpha}-BGT$) group (As IV+${\alpha}-BGT$ group). As IV ($20mg{\cdot}Kg^{-1}{\cdot}d^{-1}$) was administrated to rats for 6 weeks via daily oral gavage. Body weight and blood pressure were continuously measured, and NE levels in the plasma and renal cortex was evaluated to reflect the sympathetic activity. The expressions of leptin receptor (LepRb) mRNA, phosphorylated signal transducer and activator of transcription-3 (p-STAT3), phosphorylated phosphatidylinositol 3-kinase (p-PI3K), suppressor of cytokine signaling 3 (SOCS3) mRNA, and protein-tyrosine phosphatase 1B (PTP1B) mRNA, pro-opiomelanocortin (POMC) mRNA and neuropeptide Y (NPY) mRNA were measured by Western blot or qRT-PCR to evaluate the hypothalamic leptin sensitivity. Additionally, we measured the protein or mRNA levels of ${\alpha}7nAChR$, inhibitor of nuclear factor ${\kappa}B$ kinase subunit ${\beta}/nuclear$ factor ${\kappa}B$ ($IKK{\beta}/NF-KB$) and pro-inflammatory cytokines ($IL-1{\beta}$ and $TNF-{\alpha}$) in hypothalamus and adipose tissue to reflect the anti-inflammatory effects of As IV through upregulating expression of ${\alpha}7nAChR$. We found that As IV prevented body weight gain and adipose accumulation, and also improved metabolic disorders in HFD rats. Furthermore, As IV decreased BP and HR, as well as NE levels in blood and renal tissue. In the hypothalamus, As IV alleviated leptin resistance as evidenced by the increased p-STAT3, LepRb mRNA and POMC mRNA, and decreased p-PI3K, SOCS3 mRNA, and PTP1B mRNA. The effects of As IV on leptin sensitivity were related in part to the up-regulated ${\alpha}7nAchR$ and suppressed $IKK{\beta}/NF-KB$ signaling and pro-inflammatory cytokines in the hypothalamus and adipose tissue, since co-administration of ${\alpha}7nAChR$ selective antagonist ${\alpha}-BGT$ could weaken the improved effect of As IV on central leptin resistance. Our study suggested that As IV could efficiently prevent obesityassociated hypertension through inhibiting inflammatory reaction and improving leptin resistance; furthermore, these effects of As IV was partly related to the increased ${\alpha}7nAchR$ expression.

• Herbal Formula Science
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• v.30 no.4
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• pp.249-257
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• 2022

Objectives : Aquilaria crassna is a traditional herbal medicine, which is used to treat allergies, diabetes, neurological diseases. Recently, Aquilaria crassna extracts have been reported in anti-bacterial and anti-inflammatory activities. In this study, various solvents fraction of Aquilaria crassna were investigated on various physiological activities. Methods : According to the polarity, the solvents fraction of Aquilaria crassna were confirmed through TLC, and the activities of the extracts were confirmed in anti-diabetes, anti-obesity, whitening, anti-gout, and anti-inflammation. Results : TLC results showed that ACM and ACM/E have similar patterns and most of the components were transferred to ACM/E. Treatment with ACM and ACM/E fraction were significantly decreased the generation of NO in lipopolysaccharide (LPS)-stimulated macrophage cells. Analysis of biological activities such as α-glucosidase, protein tyrosine phosphatase (PTP1B), tyrosinase, xanthine oxidase (XO) and pancreatic lipase inhibition, showed that ACM and ACM/E have more inhibitory effects than other fractions. Conclusions : Therefore, the results of the present study clearly demonstrate that Aquilaria crassna and its constituents might be beneficial in the prevention or treatment of immune-regulating effects.