Therapeutic switching: from antidermatophytic essential oils to new leishmanicidal products

Abstract

This study examined whether the antidermatophytic activity of essential oils (EOs) can be used as an indicator for the discovery of active natural products against Leishmania amazonensis. The aerial parts of seven plants were hydrodistilled. Using broth microdilution techniques, the obtained EOs were tested against three strains of dermatophytes (Trichophyton mentagrophytes, Microsporum gypseum and Microsporum canis). To compare the EOs antifungal and antiparasitic effects, the EOs activities against axenic amastigotes of L. amazonensis were concurrently evaluated. For the most promising EOs, their antileishmanial activities against parasites infecting peritoneal macrophages of BALB/c mice were measured. The most interesting antifungal candidates were the EOs from Cymbopogon citratus, Otacanthus azureus and Protium heptaphyllum, whereas O. azureus, Piper hispidum and P. heptaphyllum EOs exhibited the lowest 50% inhibitory concentration (IC50) values against axenic amastigotes, thus revealing a certain correspondence between both activities. The P. hispidum EO was identified as the most promising product in the results from the infected macrophages model (IC50: 4.7 µg/mL, safety index: 8). The most abundant compounds found in this EO were sesquiterpenes, notably curzerene and furanodiene. Eventually, the evaluation of the antidermatophytic activity of EOs appears to be an efficient method for identifying new potential drugs for the treatment of L. amazonensis.

Evaluation of Chemical Composition and Antileishmanial and Antituberculosis Activities of Essential Oils of Piper Species

“…The essential oil of the aerial parts of Piper auritum had CC 50 values of 106.4 ± 3.4 µg/mL against peritoneal macrophages from BALB/c mice [32]. Piper hispidum had a CC 50 value of 35.5 µg/mL against peritoneal macrophages from BALB/c mice and CC 50 > 100 against Vero cells [33]. The present study found higher values, which may be due to differences in the chemical composition of the oils and due to different assay conditions used.…”

“…Studies carried out with the essential oil of Piper hispidum identified an IC 50 of 3.4 µg/mL against amastigote forms of Leishmania amazonensis [33]. The leishmanicidal activity of the essential oils is due to the presence of terpenoids, which have demonstrated antiparasitic activity against a range of species of Leishmania [34].…”

Piper Species: A Comprehensive Review on Their Phytochemistry, Biological Activities and Applications

“…Promising antiplasmodial activity was reported for extracts from P. capense [268], P. cumanense [170] and P. nigrum [272], with IC 50 values of 2 µg/mL, 7 μg/mL and 12.5 μg/mL, respectively. In contrast, antitrypanosomal and antileishmanial potentialities were prominent in the EO from P. aduncum [45] with IC 50 values of 2.8 μg/mL, 12.1 μg/mL and 9 μg/mL in cell-derived and metacyclic trypomastigotes, as well as intracellular amastigotes, and P. malacophyllum with 17 μg/mL against trypomastigotes [273] of T. cruzi ; while oil from P. demeraranum with IC 50 value of 15 µg/mL [93] and P. hispidum with 4.7 µg/mL value [274] against Leishmania amazonensis .…”

Linalool, a Piper aduncum essential oil component, has selective activity against Trypanosoma cruzi trypomastigote forms at 4°C

“…Piper auritum EO inhibits the proliferation of promastigotes of Leishmania major , L. mexicana , L. braziliensis and L. donovani , with IC 50 values (for 72 h treatments) between 12.8 and 63.3 µg/mL ( Monzote et al 2010) . Also P. hispidum EO showed promising results (high antileishmanial activity with low cytotoxicity, and a safety index of eight) when treating L. amazonensis -infected macrophages ( Houël et al 2015) . The EO of P. cubeba was not active against L. amazonensis , but was effective against T. cruzi , with IC 50 values of 45.5 and 87.9 µg/mL, for trypomastigote and amastigote forms, respectively ( Esperandim et al 2013) .…”