In vitro antileishmanial and cytotoxicity activities of essential oils from Haplophyllum tuberculatum A. Juss leaves, stems and aerial parts.

BMC Complement Altern Med. 2018 Feb 14;18(1):60. doi: 10.1186/s12906-018-2128-6. Hamdi A1,2, Bero J3, Beaufay C3, Flamini G4, Marzouk Z5, Vander Heyden Y6, Quetin-Leclercq J3. Author information 1 Department of Analytical Chemistry, Applied Chemometrics and Molecular Modelling (FABI), Center for Pharmaceutical Research (CePhaR), Vrije Universiteit Brussel (VUB), Laarbeeklaan 103, 1090, Brussels, Belgium. hamdiessia@gmail.com. 2 Laboratoire de Développement Chimique Galénique et Pharmacologique des Médicaments. Faculté de Pharmacie, Université de Monastir, 5000, Monastir, Tunisia. hamdiessia@gmail.com. 3 Pharmacognosy Research Group (GNOS), Louvain Drug Research Institute (LDRI), Université catholique de Louvain (UCL), B1.72.03 Av. E. Mounier 72, B-1200, Bruxelles, Belgium. 4 Dipartimento di Scienze Farmaceutiche, Sede Chimica Bioorganica e Biofarmacia, Università di Pisa, Via Bonanno 33, 56126, Pisa, Italy. 5 Laboratoire de Développement Chimique Galénique et Pharmacologique des Médicaments. Faculté de Pharmacie, Université de Monastir, 5000, Monastir, Tunisia. 6 Department of Analytical Chemistry, Applied Chemometrics and Molecular Modelling (FABI), Center for Pharmaceutical Research (CePhaR), Vrije Universiteit Brussel (VUB), Laarbeeklaan 103, 1090, Brussels, Belgium. Yvan.Vander.Heyden@vub.be. Abstract BACKGROUND: Plants used for traditional medicine produce diverse and complex secondary metabolites exhibiting various medicinal properties. The medicinal plant Haplophyllum tuberculatum is used by native people against malaria and parasitic infections. METHODS: In this study and in order to contribute for the search of new natural drugs for leishmaniasis, the essential oils of H. tuberculatum leaves, stems and aerial parts (leaves+stems) collected in two different periods, 2013 and 2015, and their components by GC/FID and GC/MS analyses were investigated. Those collected in 2013 were also re-analyzed two years later. The extracted oils were screened in vitro for anti-leishmanial activity on Leishmania mexicana mexicana (L.m.m.) promastigotes and cytotoxicity on the Chinese Hamster Ovary (CHO) cell line. Limonene (1.5 - 8%), its isomers (R- (+)-limonene and S-(-)-limonene), linalool and octanol were also tested. RESULTS: Results showed that the chemical composition varied according to the year of collection. Though major compounds remain almost the same, qualitative and quantitative variations in the composition of the EOs can be observed between the two years of collection, with some minor compounds identified only in one type of samples. Variation in the composition were also observed in the re-analyzed volatile oils, showing stability concerns. The essential oils and R-(+)-limonene showed moderate anti-leishmanial activity. Their IC50 range from 6.48 to 50.28 μg/ml. Cytotoxicity assays for theses volatile extracts, R- (+)-limonene and S- (-)-limonene on CHO cells showed relatively potent cytotoxicity with a selectivity index <10. Their CC50 range from 27.79 to 82.56 μg/ml. CONCLUSIONS: The findings of the present study demonstrated that H. tuberculatum might not be considered as a natural source for production of new anti-leishmanial agents without further analyzing its eventual in vivo toxicity as well as that of major pure compounds. KEYWORDS: Anti-leishmanial; Cytotoxicity; Essential oils; Haplophyllum tuberculatum; Limonene PMID: 29444667 PMCID: PMC5813356 DOI: 10.1186/s12906-018-2128-6 [Indexed for MEDLINE] Free PMC Article