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Title: (R)-(−)-Aloesaponol III 8-Methyl Ether from Eremurus persicus: A Novel Compound against Leishmaniosis
Authors: Rossi, Daniela
Ahmed, Karzan
Gaggeri, Raffaella
Della Volpe, Serena
Maggi, Lauretta
Mazzeo, Giuseppe
Longhi, Giovanna
Abbate, Sergio
Corana, Federica
Martino, Emanuela
Machado, Marisa
Varandas, Raquel
Sousa, Maria
Collina, Simona
Keywords: Leishmaniosis
Drug identification
Eremurus persicus
Plant extract
(R)-aloesaponol III-8 methyl ether
Issue Date: 2017
Publisher: MDPI
Abstract: Leishmaniosis is a neglected tropical disease which affects several millions of people worldwide. The current drug therapies are expensive and often lack efficacy, mainly due to the development of parasite resistance. Hence, there is an urgent need for new drugs effective against Leishmania infections. As a part of our ongoing study on the phytochemical characterization and biological investigation of plants used in the traditional medicine of western and central Asia, in the present study, we focused on Eremurus persicus root extract in order to evaluate its potential in the treatment of leishmaniosis. As a result of our study, aloesaponol III 8-methyl ether (ASME) was isolated for the first time from Eremurus persicus root extract, its chemical structure elucidated by means of IR and NMR experiments and the (R) configuration assigned by optical activity measurements: chiroptical aspects were investigated with vibrational circular dichroism (VCD) and electronic circular dichroism (ECD) spectroscopies and DFT (density functional theory) quantum mechanical calculations. Concerning biological investigations, our results clearly proved that (R)-ASME inhibits Leishmania infantum promastigotes viability (IC50 73 µg/mL), inducing morphological alterations and mitochondrial potential deregulation. Moreover, it is not toxic on macrophages at the concentration tested, thus representing a promising molecule against Leishmania infections.
Peer review: yes
DOI: 10.3390/molecules22040519
ISSN: 1420-3049
Appears in Collections:I&D CNC - Artigos em Revistas Internacionais
FFUC- Artigos em Revistas Internacionais

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