Drug synergism: studies of combination of RK-52 and curcumin against rhodesain of Trypanosoma brucei rhodesiense

Publication type:
Journal article
Metadata:
Autoren
  • Roberta Ettari
  • Santo Previti
  • Carla Di Chio
  • Santina Maiorana
  • Alessandro Allegra
  • Tanja Schirmeister
  • Maria Zappala
Autoren-URL
https://www.webofscience.com/api/gateway?GWVersion=2&SrcApp=fis-test-1&SrcAuth=WosAPI&KeyUT=WOS:000535281200030&DestLinkType=FullRecord&DestApp=WOS_CPL
DOI
10.1021/acsmedchemlett.9b00635
Externe Identifier
  • Clarivate Analytics Document Solution ID: LQ8XJ
  • PubMed Identifier: 32435388
ISSN
1948-5875
Ausgabe der Veröffentlichung
5
Zeitschrift
ACS MEDICINAL CHEMISTRY LETTERS
Schlüsselwörter
  • Rhodesain
  • Trypanosoma
  • drug combination studies
  • curcumin
  • synthetic inhibitor
  • synergism
Paginierung
806 - 810
Datum der Veröffentlichung
2020
Status
Published
Titel
Drug Synergism: Studies of Combination of RK-52 and Curcumin against Rhodesain of <i>Trypanosoma brucei rhodesiense</i>
Sub types
  • Article
Ausgabe der Zeitschrift
11

Data source: Web of Science (Lite)

Other metadata sources:
Autoren
  • Roberta Ettari
  • Santo Previti
  • Carla Di Chio
  • Santina Maiorana
  • Alessandro Allegra
  • Tanja Schirmeister
  • Maria Zappalà
DOI
10.1021/acsmedchemlett.9b00635
eISSN
1948-5875
ISSN
1948-5875
Ausgabe der Veröffentlichung
5
Zeitschrift
ACS Medicinal Chemistry Letters
Sprache
en
Online publication date
2020
Paginierung
806 - 810
Datum der Veröffentlichung
2020
Status
Published
Herausgeber
American Chemical Society (ACS)
Herausgeber URL
http://dx.doi.org/10.1021/acsmedchemlett.9b00635
Datum der Datenerfassung
2023
Titel
Drug Synergism: Studies of Combination of RK-52 and Curcumin against Rhodesain of <i>Trypanosoma brucei rhodesiense</i>
Ausgabe der Zeitschrift
11

Data source: Crossref

Abstract
Rhodesain is an enzyme essential for the life of <i>Trypanosoma brucei rhodesiense,</i> a parasite causing a rapid-onset form of Human African Trypanosomiasis. <b>RK-52</b> is a synthetic inhibitor of rhodesain, characterized by an impressive <i>k</i> <sub>second</sub> value (<i>k</i> <sub>second</sub> = 67000 × 10<sup>3</sup> M<sup>-1</sup> min<sup>-1</sup>) and by a picomolar affinity toward the trypanosomal protease (<i>K</i> <sub>i</sub> = 38 pM). Differently, curcumin, the golden multitarget nutraceutical obtained from <i>Curcuma longa</i> L., was proven to inhibit rhodesain noncompetitively with an IC<sub>50</sub> of 7.75 μM. In the present study, we carried out studies of a combination of RK-52 and curcumin toward rhodesain, by applying the Chou and Talalay approach, which led us to obtain a combination index <1 for the most relevant f<sub>a</sub> values, which means a potent synergistic effect for the reduction of rhodesain activity from 40% to 99%.
Addresses
  • Department of Chemical, Biological, Pharmaceutical and Environmental Sciences, University of Messina, Viale Annunziata, 98168 Messina, Italy.
Autoren
  • Roberta Ettari
  • Santo Previti
  • Carla Di Chio
  • Santina Maiorana
  • Alessandro Allegra
  • Tanja Schirmeister
  • Maria Zappalà
DOI
10.1021/acsmedchemlett.9b00635
eISSN
1948-5875
Externe Identifier
  • PubMed Identifier: 32435388
  • PubMed Central ID: PMC7236278
Funding acknowledgements
  • Ministero dell?Istruzione, dell?Universit? e della Ricerca:
Open access
false
ISSN
1948-5875
Ausgabe der Veröffentlichung
5
Zeitschrift
ACS medicinal chemistry letters
Sprache
eng
Medium
Electronic-eCollection
Online publication date
2020
Paginierung
806 - 810
Datum der Veröffentlichung
2020
Status
Published
Publisher licence
CC BY
Datum der Datenerfassung
2020
Titel
Drug Synergism: Studies of Combination of RK-52 and Curcumin against Rhodesain of <i>Trypanosoma brucei rhodesiense</i>.
Sub types
  • rapid-communication
  • Journal Article
Ausgabe der Zeitschrift
11

Files

https://pubs.acs.org/doi/pdf/10.1021/acsmedchemlett.9b00635 https://europepmc.org/articles/PMC7236278?pdf=render

Data source: Europe PubMed Central

Abstract
Rhodesain is an enzyme essential for the life of Trypanosoma brucei rhodesiense, a parasite causing a rapid-onset form of Human African Trypanosomiasis. RK-52 is a synthetic inhibitor of rhodesain, characterized by an impressive k second value (k second = 67000 × 103 M-1 min-1) and by a picomolar affinity toward the trypanosomal protease (K i = 38 pM). Differently, curcumin, the golden multitarget nutraceutical obtained from Curcuma longa L., was proven to inhibit rhodesain noncompetitively with an IC50 of 7.75 μM. In the present study, we carried out studies of a combination of RK-52 and curcumin toward rhodesain, by applying the Chou and Talalay approach, which led us to obtain a combination index <1 for the most relevant fa values, which means a potent synergistic effect for the reduction of rhodesain activity from 40% to 99%.
Date of acceptance
2020
Autoren
  • Roberta Ettari
  • Santo Previti
  • Carla Di Chio
  • Santina Maiorana
  • Alessandro Allegra
  • Tanja Schirmeister
  • Maria Zappalà
Autoren-URL
https://www.ncbi.nlm.nih.gov/pubmed/32435388
DOI
10.1021/acsmedchemlett.9b00635
Externe Identifier
  • PubMed Central ID: PMC7236278
ISSN
1948-5875
Ausgabe der Veröffentlichung
5
Zeitschrift
ACS Med Chem Lett
Sprache
eng
Country
United States
Paginierung
806 - 810
Datum der Veröffentlichung
2020
Status
Published online
Titel
Drug Synergism: Studies of Combination of RK-52 and Curcumin against Rhodesain of Trypanosoma brucei rhodesiense.
Sub types
  • Journal Article
Ausgabe der Zeitschrift
11

Data source: PubMed

Autoren
  • Roberta Ettari
  • Santo Previti
  • Carla Di Chio
  • Santina Maiorana
  • Alessandro Allegra
  • Tanja Schirmeister
  • Maria Zappalà
Zeitschrift
ACS Medicinal Chemistry Letters
Datum der Veröffentlichung
2020
Herausgeber
ACS Publications
Datum der Datenerfassung
2021
Titel
Drug synergism: studies of combination of RK-52 and curcumin against rhodesain of Trypanosoma brucei rhodesiense
Sub types
  • article

Data source: Manual

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