Pharmacological effects and pharmacokinetic properties of a dual-function peptide 5rolGLP-HV
Pharmacology study published in Applied Biochemistry and Biotechnology (2016)
Abstract
In order to better understand the therapeutic mechanism of dual-function peptide 5rolGLP-HV in treatment of treat diabetes and its complication of thrombosis, the pharmacological effects and pharmacokinetic properties of 5rolGLP-HV were conducted in this study. 5rolGLP-HV was orally administered to diabetic mice, and the hypoglycemic mechanism was investigated. Thrombotic mice were applied to study the thrombus dissolving ability of 5rolGLP-HV. The concentration of rolGLP and rHV in rat plasma following single oral dose or intravenous injection of 5rolGLP-HV was measured. Treatment with 5rolGLP-HV decreased insulin resistance (2.96 ± 1.43 vs. 9.35 ± 1.51, p < 0.05) of diabetic mice. 5rolGLP-HV shortened the length of thrombus in thrombosis mice (2.92 ± 0.74 vs. 5.92 ± 1.16 cm, p < 0.01) and extended the thrombin time (15.35 ± 1.22 vs. 8.67 ± 0.89 s, p < 0.01) of normal mice. Meanwhile, 5rolGLP-HV restored the damage of pancreatic, liver, kidney, and adipose tissues induced in the diabetic mice. 5rolGLP-HV exhibited a fast absorption and slow elimination phase after digested into rolGLP-1 and rHV in vivo. These results suggested that 5rolGLP-HV had an ideal therapeutic potential in the prevention of β cell dysfunction in type 2 diabetes and delay of the thrombus.
Abstract sourced from PubMed (NCBI) for the cited record. See the original publication for the authoritative version.
Resumen
Engineered dual-function fusion peptide 5rolGLP-HV combining GLP-1 (glycemic) and hirudin variant (antithrombotic) activities. Demonstrates both hypoglycemic and anticoagulant effects in rodents.
Por qué esto importa para la hirudoterapia
This study examined the pharmacological effects and pharmacokinetic properties of 5rolGLP-HV, a dual-function peptide combining a GLP-1 analog (rolGLP) with recombinant hirudin (rHV), orally administered to diabetic and thrombotic mice. The peptide decreased insulin resistance, shortened thrombus length, extended thrombin time, and restored pancreatic, liver, kidney, and adipose tissue damage in diabetic mice, while exhibiting rapid absorption and slow elimination after in vivo digestion into rolGLP-1 and rHV. The findings matter to ASH's domain because they demonstrate antithrombotic activity of a hirudin-containing fusion peptide alongside metabolic benefits. Caveat: this is a preclinical animal study (mice and rats) with no human data, and the engineered fusion peptide is distinct from traditional hirudotherapy or the native leech secretome.
Citación
Pharmacological effects and pharmacokinetic properties of a dual-function peptide 5rolGLP-HV.
Ni Z et al. · Applied biochemistry and biotechnology, 2016
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Añadido a la biblioteca ASH: May 27, 2026 · Última actualización del sitio: June 18, 2026