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Garcinol from Garcinia indica inhibits HIV-1 reverse transcriptase-associated ribonuclease H

DOI zum Zitieren der Version auf EPub Bayreuth: https://doi.org/10.15495/EPub_UBT_00005785
URN to cite this document: urn:nbn:de:bvb:703-epub-5785-5

Title data

Corona, Angela ; Seibt, Sebastian ; Schaller, David ; Schobert, Rainer ; Volkamer, Andrea ; Biersack, Bernhard ; Tramontano, Enzo:
Garcinol from Garcinia indica inhibits HIV-1 reverse transcriptase-associated ribonuclease H.
In: Archiv der Pharmazie. Vol. 354 (2021) Issue 9 . - No. 2100123.
ISSN 1521-4184
DOI der Verlagsversion: https://doi.org/10.1002/ardp.202100123

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Abstract

The bioactive components of Garcinia indica, garcinol (camboginol), and isogarcinol (cambogin), are suitable drug candidates for the treatment of various human diseases. HIV-1-RNase H assay was used to study the RNase H inhibition by garcinol and isogarcinol. Docking of garcinol into the active site of the enzyme was carried out to rationalize the difference in activities between the two compounds. Garcinol showed higher HIV-1-RNase H inhibition than the known inhibitor RDS1759 and retained full potency against the RNase H of a drug-resistant HIV-1 reverse transcriptase form. Isogarcinol was distinctly less active than garcinol, indicating the importance of the enolizable β-diketone moiety of garcinol for anti-RNase H activity. Docking calculations confirmed these findings and suggested this moiety to be involved in the chelation of metal ions of the active site. On the basis of its HIV-1 reverse transcriptase-associated RNase H inhibitory activity, garcinol is worth being further explored concerning its potential as a cost-effective treatment for HIV patients.

Further data

Item Type: Article in a journal
Keywords: antiviral drugs; garcinol; Garcinia indica; HIV; RNase H
DDC Subjects: 500 Science > 540 Chemistry
Institutions of the University: Faculties > Faculty of Biology, Chemistry and Earth Sciences > Department of Chemistry > Chair Organic Chemistry I > Chair Organic Chemistry I - Univ.-Prof. Dr. Rainer Schobert
Faculties
Faculties > Faculty of Biology, Chemistry and Earth Sciences
Faculties > Faculty of Biology, Chemistry and Earth Sciences > Department of Chemistry
Faculties > Faculty of Biology, Chemistry and Earth Sciences > Department of Chemistry > Chair Organic Chemistry I
Language: English
Originates at UBT: Yes
URN: urn:nbn:de:bvb:703-epub-5785-5
Date Deposited: 20 Sep 2021 08:53
Last Modified: 20 Sep 2021 08:53
URI: https://epub.uni-bayreuth.de/id/eprint/5785

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