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AMP-activated protein kinase
 
Cellular Energy Sensor & Drug Targets for Meabolic Diseases and Cancer

AMP-activated protein kinase (AMPK) recognizes the cellular energy level under various conditions and regulates energy homeostasis. Thus, AMPK plays a central role in the regulation of energy homeostasis by activating ATP-generating pathways and inhibiting ATP-consuming  pathways. 

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In response to cellular energy level, AMPK inhibits anabolic pathways such as fatty acid synthesis and gluconeogenesis whereas it stimulates glucose uptake, fatty acid oxidation, mitochondrial biogenesis. 

As a result, AMPK is considered a novel drug target for diabetes and obesity.

AMPK also regulates autophagy, which plays a central role in a various cellular processes.

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Exercise shows beneficial effects for preventing obesity, diabetes, cancer, aging through regulation of energy metabolic pathways. AMP-activated protein kinase (AMPK) mediates the beneficial effects of exercise and is known to be a target for drug development for obesity and diabetes.

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It is a critical work to understand cellular energy metabolisms and identify novel cellular mediator that mediates the beneficial effects of exercise.

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Discovery of small molecules that regulate a cellular mediator can lead to development of anti-obesity, anti-diabetes, anti-cancer drugs.

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Administration of cryptotanshinon (cry) into fat animals , which activates AMPK,  reduced the body weight ~30 %, showing excellent anti-obesity effect. 

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Cryptotanshinon (cry) also significantly reduced the blood glucose level in three different diabetes animal models.

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Cryptotanshinon (cry) effectively reduced the tumor volume in xenograft model. This compound has potential as a drug candidate for treatment of obesity, diabetes, and cancer.

Functional Materials for Cosmetics

Discovery of materials with whitening effect, anti-aging effect, hair growth effect is another task in the laboratory. These materials can be developed into cosmetics.

whitening effect

Anti-aging effect

anti-oxidant 

effect

hair growth effect

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Whitening effect of CES201

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Functional Materials for Cosmetics

AMPK plays a significant role in skin development and hair growth. We are developing AMPK-activating materials (CES201, CES301), which can regulate melanogenesis, skin aging, and hair growth.  Based on the knowledge obtained, discovery of materials with whitening effect, anti-aging effect, hair growth effect is another task in the laboratory. These materials can be developed into cosmetics.

whitening effect

Anti-aging effect

anti-oxidant 

effect

hair growth effect

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Whitening effect of CES201

Melanocyte-stimulating hormone (a-MSH) induced melanin synthesis ~2 fold in melanomas. CES201 treatment resulted in a significant suppression of melanin synthesis. As a positive control, arbutin was used. This result shows that this compound has skin whitening effect and can be used as a functional material for cosmetics.

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Hair growth-promoting effect of CES301 in vitro

Dermal papilia cells were treated with CES 301 and various growth factors including IGF-1, KGF, VEGF, HGF were highly induced. These data highlights the potential of CES301 as hair growth-promoting agent.

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Hair growth-promoting effect of CES301 in vivo

5 week-old mice were shaved at the back and then treated with a diet containing CES301 for 2 weeks. Compared to the positive control, minoxidil, a medication used for the treatment pattern hair loss. CES301 show potent hair-growth effects 

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Anti-aging effects of CES201

Treatment of keratinocytes (skin cells) with H2O2 induced population of aging cells, but CES201 significantly blocked these effects, suggesting the potential of CES201 as anti-aging agent.

Areas of Expertise
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