Rosmarinic Acid Present in Lepechinia floribunda and Lepechinia meyenii as a Potent Inhibitor of the Adenylyl Cyclase gNC1 from Giardia lamblia

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Abstract
Giardiasis is a parasitosis caused by Giardia lamblia with significant epidemiological and clinical importance due to its high prevalence and pathogenicity. The lack of optimal therapies for treating this parasite makes the development of new effective chemical entities an urgent need. In the search for new inhibitors of the adenylyl cyclase gNC1 obtained from G. lamblia, 14 extracts from Argentinian native plants were screened. Lepechinia floribunda and L. meyenii extracts exhibited the highest gNC1 inhibitory activity, with IC50 values of 9 and 31 µg/mL, respectively. In silico studies showed rosmarinic acid, a hydroxycinnamic acid present in both mentioned species, to be a promising anti-gNC1 compound. This result was confirmed experimentally, with rosmarinic acid showing an IC50 value of 10.1 µM. Theoretical and experimental findings elucidate the molecular-level mechanism of rosmarinic acid, pinpointing the key interactions stabilizing the compound–enzyme complex and the binding site. These results strongly support that rosmarinic acid is a promising scaffold for developing novel compounds with inhibitory activity against gNC1, which could serve as potential therapeutic agents to treat giardiasis.
Funding Information
  • Agencia Nacional de Promoción Científica y Tecnológica (PICT 2015-1769, PICT-2018-03259, PICT 2017-1381, PICT 2019-2019-00721, PICT-2020-SERIES-01627, PICT-2021-CAT-II-00045, PIP-2017-2019, PIP-2021-2023)
  • Consejo Nacional de Investigaciones Científicas y Técnicas (PICT 2015-1769, PICT-2018-03259, PICT 2017-1381, PICT 2019-2019-00721, PICT-2020-SERIES-01627, PICT-2021-CAT-II-00045, PIP-2017-2019, PIP-2021-2023)

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