We describe the
in vitro activity of two natural isomeric
ent-beyerene diterpenes, several derivatives and synthetic intermediates. Beyerenols
1 and
2 showed EC
50 of 4.6?±?9.4 and 5.3?±?9.4?μg/mL against amastigotes of
L. (V) brazilensis, with SI of 5.1 and 7.7, respectively. Beyerenol
1 was synthesized from stevioside.
In vivo experiments with bereyenols showed cure in 50% of hamsters infected with
L. (V) brazilensis topically applied as Cream I (beyerenol
1, 0.81%, w/w) and Cream III (beyerenol
2, 1.96%, w/w). These results suggest that beyerenols are potential candidates for cutaneous leishmaniasis chemotherapy by topical application.
In vitro assays of amastigotes of
L. (V) brazilensis showed EC
50 of 1.1?±?0.1 and 1.3?±?0.04?μg/mL, with SI of 3.1 and 3.5 for hydrazone intermediates
10 and
11, respectively.
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