Leishmania mexicana is one of the pathogens causing cutaneous leishmaniasis which is associated with patient morbidity. In our researches for new safe and effective treatments, thirty-seven essential oils (EOs) extracted from Vietnamese plants were screened in vitro for the first time on Leishmania mexicana mexicana (Lmm) promastigotes at the maximum concentration of 50 nL/mL. Active EOs were also analyzed for cytotoxicity on mammalian cell lines (WI38, J774) and their selectivity indices (SI) were calculated. Their composition was determined by GC-MS and GC-FID. Our results indicated that EOs extracted from Cinnamomum cassia, Zingiber zerumbet, Elsholtzia ciliata and Amomum aromaticum, possessed a moderate anti-leishmanial activity, with IC50 values of 2.92 ± 0.08, 3.34 ± 0.34, 8.49 ± 0.32 and 9.25 ± 0.64 nL/mL respectively. However, they also showed cytotoxicity with SI < 10. The most promising EO was extracted from Ocimum gratissimum, displaying an IC50 of 4.85 ± 1.65 nL/mL and SI > 10. It contained 86.5% eugenol, which was demonstrated to be effective on Lmm with IC50 of 2.57 ± 0.57 nL/mL and not toxic on mammalian cells, explaining the observed activity.
Twelve new terpenoids (1–12) were
isolated from the stems of Fissistigma polyanthoides, an anti-inflammatory medicinal plant traditionally used in Vietnam.
Most of them (1–9) possess a sesquiterpenoid
backbone (e.g., guaiane, germacrane, and cadinane) connected to a
2′-O-trans-cinnamoyl)-β-d-glucopyranose moiety, which is rare in Nature. Among them,
compounds 4 (5/8-fused ring) and 6 (spiran
[4,5] ring) represent uncommonly rearranged sesquiterpenoids. Compounds 10–12 are a novel monoterpene and two
megastigmane derivatives, respectively. The individual structures
were elucidated by combining NMR and MS data, and their configuration
was established in NOESY and ECD experiments. Compounds 1–9 were also examined for their potential to
interact with nuclear factor-kappa B activator protein 1 (NF-κB/AP-1)
signaling by using the myelomonocytic reporter cell line THP-1Blue-CD14.
Compounds 1–5 showed dose-dependent
inhibitory effects [IC50 13.7 μM (1)
to 49.0 μM (5)] on lipopolysaccharide-stimulated
cells. However, compounds 1 to 4 also negatively
affected cell viability in the same concentration range, while compound 5 was less potently cytotoxic.
Human African trypanosomiasis (HAT), known as sleeping sickness and caused by Trypanosoma brucei, is threatening low-income populations in sub-Saharan African countries with 61 million people at risk of infection. In order to discover new natural products against HAT, thirty-seven Vietnamese essential oils (EOs) were screened for their activity in vitro on Trypanosoma brucei brucei (Tbb) and cytotoxicity on mammalian cells (WI38, J774). Based on the selectivity indices (SIs), the more active and selective EOs were analyzed by gas chromatography. The anti-trypanosomal activity and cytotoxicity of some major compounds (isolated or commercial) were also determined. Our results showed for the first time the selective anti-trypanosomal effect of four EOs, extracted from three Zingiberaceae species (Curcuma longa, Curcuma zedoaria, and Zingiber officinale) and one Lauraceae species (Litsea cubeba) with IC50 values of 3.17 ± 0.72, 2.51 ± 1.08, 3.10 ± 0.08, and 2.67 ± 1.12 nL/mL respectively and SI > 10. Identified compounds accounted for more than 85% for each of them. Among the five major components of Curcuma longa EO, curlone is the most promising anti-trypanosomal candidate with an IC50 of 1.38 ± 0.45 µg/mL and SIs of 31.7 and 18.2 compared to WI38 and J774 respectively.
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