A series of SynLeptin peptides, particularly, SynLeptin-2 shows remarkable anti-obesity activities which were verified in animal experiments using mice and rabbits.

The SynLeptin-2 peptide decreases food intake by appetite inhibitory action, which can be reversed by appetite stimulant AGRP.

 

The core technology of Yonsei University is to provide promising anti-obesity agents, a series of ‘SynLeptin’ peptides. The SynLeptin peptides exhibits anti-obesity activities by distinctly various actions suchc as reducing fat mass, decreasing food intake, increasisng fat oxidation, increasing energy expenditure and body temperature and increasing appetite suppressor.

Obesity is a pathologic disorder caused by excess fat accumulation in various tissues. Excess food-intake of high fat content, lack of exercise, and genetic, environmental and psychological factors are the causes of obesity. Obsesity is considered as a direct or indirect cause of diabetes mellitus, cardiovascular diseases and short life expectation. A multitue of approaches and researches have been made to prevent and treat obesity but have finally failed to effectively treat obesity. Although many patients make various efforts such as diet-control, rigorous exercise and chemotherapy to prevent and treat obesity, they tend to return to obese state when they stop those efforts.

SynLeptin of Yonsei University has been developed on the basis of findings that the Tat polypeptide derived from HIV (Human Immunodeficiency Virus) and various peptides derived from Tat have excellent anti-obesity activity. Among Tat-derived peptides, two peptides originated from Tat that are called SynLeptin-1 and SynLeptin-2, respectively, are very effective in reducing the fat mass in vivo. SynLeptin-1 comprisese 71 amino acid residues of Tat and SynLeptin-2, 86 amino acid residues of Tat.  The rabbits subcutanesouly administered with the two peptides were observed to be decreaseed in body weight. Among two peptides, SynLeptin-2 has been analzyed to exhibit more prominent inhibition action to fat mass than SynLeptin-1. The representative analysis results of SynLeptin-2 for anti-obesity activities are as follows: The SynLeptin-2 peptide was prepared in the fusion form with GST (glutathione-S-transferase).

The subcutaneous injection of GST-SynLeptin-2 exhibited an average of 10.73 g reduction in body weight compared with control mice as determined on day 100 post-treatment.

The SynLeptin-2 peptide decreases food intake by appetite inhibitory action, which can be reversed by appetite stimulant AGRP.

The pharmacokinetics of SynLeptin-2 has been studied by our laboratory (see Shin BS, et al. (2007) Pharmacokinetics of GST-TatdMt, a recombinant fusion protein possessing potent anti-obesity activity, in mice. Arch Pharm Res. 30(9):1162-7). The absolute bioavailability of SynLeptin-2 was 42.8% and 60.5% after p.o. and i.p. administration, respectively. Given the cell-penetrating potential, SynLeptin-2 may be absorbed into the systemic circulation to a relatively high extent after extravascular administration such as subcutaneous administration.

 

Preclinical

 

PCT (WO 2002/085938)

Korea 10-465589  (Granted);    U.S.A 2007-0073040  (Pending);  

Europe EP1385881  (Pending);   Japan JP03801565  (Granted);

Russia RU2280468 (Granted);    China CN1520422  (Pending);

India 01681/DELNP/2003 (Pending);  Canada CA244602 (Pending).

 

 

 

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