Functional Actives


- Anti-obesity


Obesity has now reached pandemic proportions leading to a collection of morbidities referred to as metabolic syndrome, including insulin resistance, Type 2 diabetes, and cardiovascular diseases. Currently, more than one billion adults worldwide are overweight and at least 300 million of them are clinically obese (WHO, 2009). Therefore, prevention and treatment of obesity is one of the most important health-care challenges of our time.


Whilst bariatric surgery often results in weight loss, its associated cost is prohibitive for widespread application. In addition, the current options for medical treatment of obesity, such as Orlistat and Sibutramine, are limited due to side effects. Orlistat (Xenical) and Sibutramine (Reductil) are an anorectic or appetite suppressants. Both drugs have side-effects, including increased blood pressure, dry mouth, constipation, headache, and insomnia. Because of dissatisfaction with the high costs and potentially hazardous side-effects, the importance of natural products is sharply increasing as a potential source of anti-obesity agents. At present, a wealth of information has indicated that numerous bioactive components from nature may be useful for the treatment of obesity. A good example of such is polyphenols. These show strong anti-obesity activity and include apigenin, genistein, isorhamnetin, and the catechins.


To date, main targets or strategies for the development of anti-obesity agents have been largely classified into five categories based on their distinct mechanisms: (1) decreased lipid absorption, (2) decreased energy intake, (3) increased energy expenditure, (4) decreased pre-adipocyte differentiation and proliferation, and (5) decreased lipogenesis and increased lipolysis.



Mechanism scheme

The largest class of health problems is caused by obesity, due in part to an excess of fat cells. The obesity epidemic has focused on adipose tissue and the development of fat cells (i.e. adipocytes), which is known as adipogenesis. A thorough understanding of the differentiation process could provide important information in regards to the potential management of adipocyte cell number in order to control certain diseases. Indeed, a detailed study of differentiation, expansion and endocrine function of adipocytes is necessary for planning therapies against obesity and its metabolic complications. (Figure 1)


Figure 1. Adipose tissue



White adipose tissue (WAT) or white fat is one of the two types of adipose tissue found in mammals. The other kind of adipose tissue is brown adipose tissue. WAT is a remarkable endocrine organ that secretes a number of hormones, known as adipokines, involved in the regulation of metabolic functions. Brown adipose tissue (BAT) or brown fat is especially abundant in newborns and in hibernating mammals. Its primary function is to generate heat through mitochondrial uncoupling of lipid oxidation. (Figure 2)


Figure 2. Adipocyte differentiation and function in energy

Adipose tissue growth involves the formation of new adipocyte from precursor cells. The undifferentiated preadipocyte then differentiate into muture adipocyte, leading to a further increase in adipocyte size. The inhibition of adipocyte differentiation is one of the main targets for slimming. Adipocyte differentiation is the sequential cascade of transcriptional events that control adipogenesis. (Figure 1)



Figure 3. The transcriptional control of adipogenesis

The central players are peroxisome proliferator-activated receptor γ (PPARγ) and CCAAT/enhancer binding protein α (C/EBPα), both of which are required to coordinate the expression of adipogenic genes (e.g., aP2, SCD, pyruvate carboxylate). A number of studies have demonstrated that natural compounds, such as EGCG, genistein, berberine, conjugated linoleic acid, resveratrol, capsaicin, and procyanidins, inhibited adipogenesis via suppression of PPAR and CEBP expression. (Figure 3)



Publications

·Isorhamnetin represses adipogenesis in 3T3-L1 cells. Obesity. 2009, 17(2), 226-232.

·The study on anti-obesity activity of the wild plants of Jeju Island. Journal of the Society of Cosmetic Scientists of Korea. 2007, 33(3), 175-179.



Patents

·Korean application No.: 10-2012-0116851/Filing Date: 19. Oct. 2012.


·Korean application No.: 10-2009-0035960/Filing Date: 24. Apr. 2009.


·Registration No.: 10-1213693-0000; Registration Date: 12. Dec. 2012.



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