Untitled

Abstract

The healing effect of human epidermal growth factor (hEGF) on open wounds was studied in rats. No improvement in wound healing was found by topical application of EGF alone to open wound sites. We found an ointment containing EGF and a protease inhibitor, nafamostat mesilate or gabexate mesilate, or gelatin accelerated the healing rate of open wounds. Significant increases in the dry weight of the wound site granulation tissue, uronic acid (as an index of acid mucopolysaccharide) and hydroxyproline (as an index of collagen) were observed by treatment with EGF ointment containing nafamostat compared with the controls. The effects of the protease inhibitor on wound healing were dose dependent. Nafamostat was more efficient than gabexate or gelatin on wound healing. The degradation of 125I-EGF in wound tissue homogenate was significantly decreased in the presence of a protease inhibitor, such as nafamostat or gabexate, or gelatin. These findings indicate that the stabilization of EGF at the wound site is an important factor in permitting the expression of its healing effects and suggest that the ointment containing EGF and a stabilizing agent would be a suitable dosage form for acceleration of wound repair.

Topical application of epidermal growth factor accelerates wound healing by myofibroblast proliferation and collagen synthesis in rat

“…In particular, the topical application of EGF has been shown to accelerate the healing rate of open wounds [18]. The present study also demonstrated that a topical treatment with a rhEGF ointment significantly reduced the wound closure time (at least 2 days) in a full thickness wound model compared with that of the animals treated with the ointment base only.…”

“…There have been many studies aimed at developing a topical formulation with the sustained and stable pharmacological properties of recombinant human EGF (rhEGF) [14,18]. The wound healing properties of a topical rhEGF treatment have been reported in split- or partial-thickness skin wound in pigs and guinea pigs, respectively [2,15].…”

Experimental NMR and MS study of benzoylguanidines. Investigation ofE/Zisomerism

“…Arylthioureas have attracted great attention owing to their diverse biological activities as antiviral agents, herbicides, pesticides, plant growth regulators and chelating agents . Guanidinium‐based molecules also showed several biological activities such as cardiovascular dilators, antihistaminics, anti‐inflammatory agents, antidiabetics, antibacterial, antifungal, antiprotozoal, antiparasitic and antiviral . Lamy et al .…”

Synthesis of Guanidines in Solution

“…The tripeptide sequence RGD (Arg-Gly-Asp) is a common cell-recognition motif responsible for the binding of the integrin receptors [4]. Guanidinium-based molecules are extensively utilised as cardiovascular drugs [8], antihistaminines [9], antiinflammatory agents [10,11], antidiabetic drugs [12], antibacterial and antifungal drugs [13], antiprotozal and other antiparasitic drugs [14] and antiviral drugs [15]. Nonpeptide cyclic cyanoguanidines are HIV-1 protease inhibitors [6], while carboxylic guanidino analogs show activity as influenza neuroaminidase inhibitors [7].…”