• Archives of Pharmacal Research
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• 제28권2호
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• pp.142-150
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• 2005

The synthesis and structure-activity relationships of a novel series of substituted quercetins that activates peroxisome proliferator-activated receptor gamma ($PPAR{\gamma}$) are reported. The $PPAR{\gamma}$ agonistic activity of the most potent compound in this series is comparable to that of the thiazolidinedione-based antidiabetic drugs currently in clinical use.

• 대한약학회:학술대회논문집
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• 대한약학회 2000년도 춘계총회 및 학술대회
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• pp.160.3-161
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• 2000

• 약학회지
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• 제39권5호
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• pp.541-547
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• 1995

In order to investigate the usability of PALMIWON as antidiabetic immuno-modulating prescription for Insulin-dependent diabetes, we studies the effects of PALMIWON on immune cell and ${\beta}-cell$. U937 was used as the model of immune cell and RINm5F as the model of ${\beta}-cell$. The effects of PALMIWON was measured by cell viability in terms of MIT assay. As a result, PALMIWON and the compositional drugs showed the different effects m immune cell and ${\beta}-cell$. Cell viability of U937 was significantly decreased wheras that of RINm5F was no significantly difference between drug treated group and control, or significantly less reduction compared with U937. It implies that PALMIWON is useful as immunotherapeutic agents in the prevention and therapy of type 1 diabetes.

• Journal of Microbiology and Biotechnology
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• 제29권5호
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• pp.713-720
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• 2019

Acanthamoeba castellanii belonging to the T4 genotype may cause a fatal brain infection known as granulomatous amoebic encephalitis, and the vision-threatening eye infection Acanthamoeba keratitis. The aim of this study was to evaluate the antiamoebic effects of three clinically available antidiabetic drugs, Glimepiride, Vildagliptin and Repaglinide, against A. castellanii belonging to the T4 genotype. Furthermore, we attempted to conjugate these drugs with silver nanoparticles (AgNPs) to enhance their antiamoebic effects. Amoebicidal, encystation, excystation, and host cell cytotoxicity assays were performed to unravel any antiacanthamoebic effects. Vildagliptin conjugated silver nanoparticles (Vgt-AgNPs) characterized by spectroscopic techniques and atomic force microscopy were synthesized. All three drugs showed antiamoebic effects against A. castellanii and significantly blocked the encystation. These drugs also showed significant cysticidal effects and reduced host cell cytotoxicity caused by A. castellanii. Moreover, Vildagliptin-coated silver nanoparticles were successfully synthesized and are shown to enhance its antiacanthamoebic potency at significantly reduced concentration. The repurposed application of the tested antidiabetic drugs and their nanoparticles against free-living amoeba such as Acanthamoeba castellanii described here is a novel outcome that holds tremendous potential for future applications against devastating infection.

• Natural Product Sciences
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• 제27권2호
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• pp.99-114
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• 2021

Type 2 diabetes mellitus (T2DM) and its complications are important noncommunicable diseases with high mortality rates. Protein tyrosine phosphatase 1B (PTP1B) and aldose reductase inhibitors are recently approached and advanced for T2DM and its complications therapy. Matricaria chamomilla L. is acknowledged as a worldwide medicinal herb that has many beneficial health effects as well as antidiabetic effects. Our research was designed to determine the most potential antidiabetic phytochemicals from M. chamomilla employing in silico study. 142 phytochemicals were obtained from the databases. The first screening employed iGEMdock and Swiss ADME, involving 93 phytochemicals. Finally, 30 best phytochemicals were docked. Molecular docking and visualization analysis were performed using Avogadro, AutoDock 4.2., and Biovia Discovery Studio 2016. Molecular docking results demonstrate that ligand-protein interaction's binding affinities were -5.16 to -7.54 kcal/mol and -5.30 to -12.10 kcal/mol for PTP1B and aldose reductase protein targets respectively. In silico results demonstrate that M. chamomilla has potential antidiabetic phytochemical compounds for T2DM and its complications. We recommended anthecotulide, quercetin, chlorogenic acid, luteolin, and catechin as antidiabetic agents due to their binding affinities against both PTP1B and aldose reductase protein. Those phytochemicals' significant efficacy and potential as antidiabetic must be investigated in further advanced research.

• Bulletin of the Korean Chemical Society
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• 제33권11호
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• pp.3772-3776
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• 2012

Mitogen-activated protein kinase phosphatase 4 (MKP4) has proved to be a promising target for the development of therapeutics for the treatment of diabetes and the other metabolic diseases. Here, we report an example for a successful application of the structure-based virtual screening to identify three novel inhibitors of MKP4. These inhibitors have desirable physicochemical properties as a drug candidate and reveal a moderate potency with $IC_{50}$ values ranging from 4.9 to $32.3{\mu}M$. Therefore, they deserve consideration for further development by structure-activity relationship studies to optimize the inhibitory and antidiabetic activities. Structural features relevant to the stabilization of the newly identified inhibitors in the active site of MKP4 are discussed in detail.

• Bulletin of the Korean Chemical Society
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• 제33권7호
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• pp.2365-2368
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• 2012

The $11{\beta}$-hydroxysteroid dehydrogenase type 1 ($11{\beta}$-HSD1) enzyme is involved in modulation of glucocorticoid activity within target tissues. This enzyme may contribute to obesity and/or metabolic disease through its action in adipose or liver tissue. Inhibition of $11{\beta}$-HSD1 has major therapeutic potential for glucocorticoid-associated diseases, including obesity, diabetes (wound healing), and muscle atrophy. To develop such therapeutics, we performed a pharmacophore-based virtual screening (VS) for identification of novel $11{\beta}$-HSD1 inhibitors and found that the VS hit compounds show potent inhibition of $11{\beta}$-HSD1 enzyme activity. Further, we present a binding model for active compounds. The proposed pharmacophore may serve as a useful guideline for future design of new chemical entities as $11{\beta}$-HSD1-targeted antidiabetic agents.

• 생약학회지
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• 제44권1호
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• pp.75-82
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• 2013

Previous studies have shown that Aloe QDM complex, which is consisted of chromium (Cr), aloesin (ALS) and processed Aloe vera gel (PAG), exert antidiabetic activity in a high fat diet-induced mouse model of type 2 diabetes. In this study we examined the mechanism of the antidiabetic activity of the Aloe QDM complex. Rat myoblast cell line L6 cells were cultured in the presence of Cr, ALS, and PAG alone and in combinations, and then the capability of the cells to uptake glucose was examined using radiolabeled glucose. All of the 3 agents, Cr, ALS and PAG, exerted glucose uptake-enhancing activity in L6 cells. The most potent capability to uptake glucose was observed when L6 cells were cultured with the Aloe QDM complex. The activity of the Aloe QDM complex to enhance glucose uptake was prominent in conditions where existing insulin concentrations are low. We also examined the effects of the Aloe QDM complex on the plasma membrane expression of GLUT4 in L6 cells. The Aloe QDM complex increased the content of GLUT4 in the plasma membrane, while decreasing the content of GLUT4 in the light microsome. Taken together, these results show that the antidiabetic activity of the Aloe QDM complex is at least in part due to the stimulation of glucose uptake into the muscle cells, and this activity of the Aloe QDM complex is mediated through the enhancement of the translocation of GLUT4 into the plasma membrane.

• Fisheries and Aquatic Sciences
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• 제26권1호
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• pp.1-23
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• 2023

Marine bioactive substances (MBS), such as phlorotannins, collagens, peptides, sterols, and polysaccharides, are increasing attention as therapeutic agents for several diseases due to their pharmacological effects. Previous studies have demonstrated the biological activities of MBS including antibacterial, anticoagulant, antidiabetic, antimicrobial, anti-inflammatory activities. Among numerous human diseases, periodontitis is one of the high-prevalence inflammatory diseases in the world. To treat periodontitis, several surgeries (bone grafting, flap surgery, and soft tissue graft) are usually used. However, the surgery for patients with chronic periodontitis induces several side effects, including additional inflammatory responses at the operated site, chronic wound healing, and secondary surgery. Therefore, this review assessed the most recent trends in MBS using Google Scholar, PubMed, and Web of Science search engines to develop marine-derived therapeutic agents for periodontitis. Further, we summarized the current applications and therapeutic potential of MBS to serve as a reference for developing novel technologies applied to MBS against periodontitis treatment.

• 한국간호교육학회지
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• 제19권2호
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• pp.127-136
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• 2013

Purpose: The aim of the study was to evaluate the effect of self-monitoring of blood glucose (SMBG)-based Diabetes Self-Management Education (DSME) on glycemic control in type 2 diabetes. Methods: This study was designed to compare changes in glycemic control over 12months in SMBG-based DSME group (n=65) versus control group (n=65). Data were obtained from medical records type 2 diabetic patients treated with oral antidiabetic agents and above HbA1c 7.0% from June 2006 to August 2008. All participants completed DSME defined as informational intervention of lifestyle habits and reinforcement of educational Monthly News letter delivered by the diabetes nurse educator. SMBG-based DSME group requested to measure blood glucose 7 times a day for a week and to record their diary and received counseling with a focus on diet and lifestyle during the education. Assessments were conducted baseline, 3, 6 and 12 months. HbA1c was used as an index of glycemic control. Results: 12 months later, the level of HbA1c was reduced by $1.28{\pm}1.68%$ in experimental group and $0.49{\pm}1.05%$ in the control group. We found a significant effect of $Time^*$ Group interaction (p=.013). Conclusion: SMBG-based DSME for patients with type 2 diabetes with oral antidiabetic agents was effective in improving glycemic control and maintaining long-term glycemic control.