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Bioorganic and Medicinal Chemistry 2014-Jan

Discovery of the rapanone and suberonone mixture as a motif for leishmanicidal and antifungal applications.

Samo registrirani uporabniki lahko prevajajo članke
Prijava / prijava
Povezava se shrani v odložišče
Raphaella Correia da Costa
Dandara Braga Santana
Renata Mendonça Araújo
José Elias de Paula
Patrícia Coelho do Nascimento
Norberto Peporine Lopes
Raimundo Braz-Filho
Laila Salmen Espindola

Ključne besede

Povzetek

Leishmaniasis and fungal infections are significant diseases impacting worldwide public health. Treatments have developed greatly over time, however, there is a necessity to discover less toxic drugs, which have greater efficacy and are more economically accessible. This work conducted a screening of Cerrado species extracts: Connarus suberosus Planch. (Connaraceae), Neea theifera Oerst. (Nyctaginaceae) and Myrcia linearifolia Cambess. (Myrtaceae) against Leishmania (Leishmania) amazonensis, dermatophytes and yeasts. Leishmanicidal and antifungal tests were conducted using MTT colorimetric assay and CLSI methodology, respectively. Connarus suberosus extracts presented the most promising results against the aforementioned microorganisms, which has not been described in the literature. The root bark EtOAc extract was selected for chemical fractionation resulting in a mixture of rapanone (1) and a previously unreported compound named as suberonone (2); a mixture of β-sitosterol (3) and stigmasterol (4); oleic acid (5); geranilgeraniol (6); and two derivatives obtained from 1 and 2 mixture. The rapanone and suberonone mixture demonstrated a MIC of 15.62 μg/mL against Candida albicans ATCC 10231.

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