Orlando, Zoya and Lengers, Isabelle and Melzig, Matthias F. and Buschauer, Armin and Hensel, Andreas and Jose, Joachim (2015) Autodisplay of Human Hyaluronidase Hyal-1 on Escherichia coli and Identification of Plant-Derived Enzyme Inhibitors. MOLECULES, 20 (9). pp. 15449-15468. ISSN 1420-3049,
Full text not available from this repository. (Request a copy)Abstract
Hyaluronan (HA) is the main component of the extracellular matrix (ECM). Depending on its chain size, it is generally accepted to exert diverse effects. High molecular weight HA is anti-angiogenic, immunosuppressive and anti-inflammatory, while lower fragments are angiogenic and inflammatory. Human hyaluronidase Hyal-1 (Hyal-1) is one of the main enzymes in the metabolism of HA. This makes Hyal-1 an interesting target. Not only for functional and mechanistic studies, but also for drug development. In this work, Hyal-1 was expressed on the surface of E. coli, by applying Autodisplay, to overcome formation of inactive inclusion bodies. With the cells displaying Hyal-1 an activity assay was performed using stains-all dye. Subsequently, the inhibitory effects of four saponins and 14 plant extracts on the activity of surface displayed Hyal-1 were evaluated. The determined IC50 values were 177 mu M for glycyrrhizic acid, 108 mu M for gypsophila saponin 2, 371 mu M for SA1657 and 296 mu M for SA1641. Malvae sylvestris flos, Equiseti herba and Ononidis radix extracts showed IC50 values between 1.4 and 1.7 mg/mL. In summary, Autodisplay enabled the expression of functional human target protein Hyal-1 in E. coli and facilitated an accelerated testing of potential inhibitors.
| Item Type: | Article |
|---|---|
| Uncontrolled Keywords: | SURFACE DISPLAY; ANGIOGENIC OLIGOSACCHARIDES; R LIPOPOLYSACCHARIDES; RECOMBINANT PROTEINS; EXPRESSION SYSTEM; AUTOTRANSPORTER; CANCER; ACID; IMMUNOCHEMISTRY; PURIFICATION; Autodisplay; Hyal-1; hyaluronan; natural inhibitors |
| Subjects: | 500 Science > 540 Chemistry & allied sciences |
| Divisions: | Chemistry and Pharmacy > Institute of Pharmacy > Pharmaceutical/Medicinal Chemistry II (Prof. Buschauer) |
| Depositing User: | Dr. Gernot Deinzer |
| Date Deposited: | 11 Jun 2019 12:13 |
| Last Modified: | 11 Jun 2019 12:13 |
| URI: | https://pred.uni-regensburg.de/id/eprint/4875 |
Actions (login required)
 |
View Item |
