Abstract
KTTKS is a matrikine that originates from the proteolytic hydrolysis of collagen. This peptide stimulates ECM production and types I and III collagen expression in vitro. A more stable form of KTTKS is pal-KTTKS, known as Matrixyl® or palmitoyl pentapeptide-3. A series of novel pentapeptides, analogues of KTTKS with the general formula X-KTTKS-OH(NH2), where X = acetyl, lipoyl, palmitoyl residues, was designed and synthesized. Their effect on amidolytic activity of urokinase, thrombin, trypsin, plasmin, t-PA, and kallikrein were tested. Cytotoxic tests on fibroblasts, as well as collagen and DNA biosynthesis tests for selected peptides, were also carried out. The test results showed that the most active plasmin inhibitors were palmitoyl peptides, whether in acid or amide form. No biological effects of lysine modification to arginine in the synthesized peptides were found. None of the synthesized peptides was not cytotoxic on fibroblasts, and three of them showed cell growth. These three compounds showed no concentration-activity relationship in the collagen and DNA biosynthesis assays.
Highlights
Aging is a natural process connected with decreased metabolic activity in cells and poor regenerative abilities of the human body [1,2]
Urokinase activation in SC was confirmed in tests in vitro, in which a urokinase precursor became active after incubation with the insoluble component of homogenate SC. These results show that the urokinase-type plasminogen activator is activated in SC after breaking the barrier, which may activate the plasminogen/plasmin system in the epidermis [36]
Thirty new and two previously known (KTTKS-OH and Pal-KTTKS-OH) peptides were obtained with satisfactory yields, ranging from 42 to 68%, by solid phase peptide synthesis
Summary
Aging is a natural process connected with decreased metabolic activity in cells and poor regenerative abilities of the human body [1,2]. There are numerous products on the market, collectively referred to as “cosmeceuticals”, whose aim is to remedy skin aging processes such as dry skin or the appearance of wrinkles. The first anti-aging (anti-wrinkle) cosmeceuticals, introduced in the early 1990s, were fruit acids, which improve skin appearance through peeling and moisturizing. The generations of anti-wrinkle products were retinol and its derivatives, used in the treatment of acne lesions. They smoothen wrinkles and help remove skin discolorations.
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