Pharmacological profile of a novel H2S-releasing aspirin

Anna Sparatore; Elena Perrino; Valerio Tazzari; Daniela Giustarini; Ranieri Rossi; Giuseppe Rossoni; Kati Erdman; Henning Schröder; Piero Del Soldato

doi:10.1016/j.freeradbiomed.2008.11.013

Pharmacological profile of a novel H₂S-releasing aspirin

Anna Sparatore, Elena Perrino, Valerio Tazzari, Daniela Giustarini, Ranieri Rossi, Giuseppe Rossoni, Kati Erdman, Henning Schröder, Piero Del Soldato

Pharmaceutics

Research output: Contribution to journal › Article › peer-review

123 Scopus citations

Abstract

The pharmacological profile of a new, safe, and effective hydrogen sulfide (H₂S)-releasing derivative of aspirin (ACS14) is described. We report the synthesis of ACS14, and of its deacetylated metabolite (ACS21), the preliminary pharmacokinetics, and its in vivo metabolism, with the H₂S plasma levels after intravenous administration in the rat. ACS14 maintains the thromboxane-suppressing activity of the parent compound, but seems to spare the gastric mucosa, by affecting redox imbalance through increased H₂S/glutathione formation, heme oxygenase-1 promoter activity, and isoprostane suppression.

Original language	English (US)
Pages (from-to)	586-592
Number of pages	7
Journal	Free Radical Biology and Medicine
Volume	46
Issue number	5
DOIs	https://doi.org/10.1016/j.freeradbiomed.2008.11.013
State	Published - Mar 1 2009

Keywords

Aspirin
Dithiolethione
Free radicals
Glutathione
Heme oxygenase-1
Hydrogen sulfide
Thromboxane

Publisher link

10.1016/j.freeradbiomed.2008.11.013

Find It

Find It at U of M Libraries

Cite this

@article{1bfee9de1cf24891a5002d43d4fdb0ad,

title = "Pharmacological profile of a novel H2S-releasing aspirin",

abstract = "The pharmacological profile of a new, safe, and effective hydrogen sulfide (H2S)-releasing derivative of aspirin (ACS14) is described. We report the synthesis of ACS14, and of its deacetylated metabolite (ACS21), the preliminary pharmacokinetics, and its in vivo metabolism, with the H2S plasma levels after intravenous administration in the rat. ACS14 maintains the thromboxane-suppressing activity of the parent compound, but seems to spare the gastric mucosa, by affecting redox imbalance through increased H2S/glutathione formation, heme oxygenase-1 promoter activity, and isoprostane suppression.",

keywords = "Aspirin, Dithiolethione, Free radicals, Glutathione, Heme oxygenase-1, Hydrogen sulfide, Thromboxane",

author = "Anna Sparatore and Elena Perrino and Valerio Tazzari and Daniela Giustarini and Ranieri Rossi and Giuseppe Rossoni and Kati Erdman and Henning Schr{\"o}der and Soldato, {Piero Del}",

year = "2009",

month = mar,

day = "1",

doi = "10.1016/j.freeradbiomed.2008.11.013",

language = "English (US)",

volume = "46",

pages = "586--592",

journal = "Free Radical Biology and Medicine",

issn = "0891-5849",

publisher = "Elsevier Inc.",

number = "5",

}

TY - JOUR

T1 - Pharmacological profile of a novel H2S-releasing aspirin

AU - Sparatore, Anna

AU - Perrino, Elena

AU - Tazzari, Valerio

AU - Giustarini, Daniela

AU - Rossi, Ranieri

AU - Rossoni, Giuseppe

AU - Erdman, Kati

AU - Schröder, Henning

AU - Soldato, Piero Del

PY - 2009/3/1

Y1 - 2009/3/1

N2 - The pharmacological profile of a new, safe, and effective hydrogen sulfide (H2S)-releasing derivative of aspirin (ACS14) is described. We report the synthesis of ACS14, and of its deacetylated metabolite (ACS21), the preliminary pharmacokinetics, and its in vivo metabolism, with the H2S plasma levels after intravenous administration in the rat. ACS14 maintains the thromboxane-suppressing activity of the parent compound, but seems to spare the gastric mucosa, by affecting redox imbalance through increased H2S/glutathione formation, heme oxygenase-1 promoter activity, and isoprostane suppression.

AB - The pharmacological profile of a new, safe, and effective hydrogen sulfide (H2S)-releasing derivative of aspirin (ACS14) is described. We report the synthesis of ACS14, and of its deacetylated metabolite (ACS21), the preliminary pharmacokinetics, and its in vivo metabolism, with the H2S plasma levels after intravenous administration in the rat. ACS14 maintains the thromboxane-suppressing activity of the parent compound, but seems to spare the gastric mucosa, by affecting redox imbalance through increased H2S/glutathione formation, heme oxygenase-1 promoter activity, and isoprostane suppression.

KW - Aspirin

KW - Dithiolethione

KW - Free radicals

KW - Glutathione

KW - Heme oxygenase-1

KW - Hydrogen sulfide

KW - Thromboxane

UR - http://www.scopus.com/inward/record.url?scp=59249087703&partnerID=8YFLogxK

UR - http://www.scopus.com/inward/citedby.url?scp=59249087703&partnerID=8YFLogxK

U2 - 10.1016/j.freeradbiomed.2008.11.013

DO - 10.1016/j.freeradbiomed.2008.11.013

M3 - Article

C2 - 19100325

AN - SCOPUS:59249087703

SN - 0891-5849

VL - 46

SP - 586

EP - 592

JO - Free Radical Biology and Medicine

JF - Free Radical Biology and Medicine

IS - 5

ER -