Alkaloid profile and cholinesterase inhibition activity of five species of Amaryllidaceae family collected from Mérida state-Venezuela

Rojas-Vera, Janne; Buitrago-Díaz, Alexis A.; Possamai, Letícia M.; Timmers, Luís Fernando Saraiva Macedo; Tallini, Luciana R.

doi:10.1016/j.sajb.2020.03.001

Cited by 25 publications

(28 citation statements)

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“…Notably, lower toxicity against Vero cells was observed with extract 56 obtained from bulbs in comparison to extract 82 from the same plant and site but processed from aerial parts. In relation to that, Rojas-Vera and co-workers found that the quantity of lycorine-type alkaloids was higher in bulbs from C. erubescens (collected in Venezuela) while non-identified alkaloids were higher in leaves [ 35 ]. It has been described that lycorine extracted from Narcissus species had an IC 50 = 0.7 µM against T. cruzi but was not parasite-specific [ 23 ], which may suggest the presence of other alkaloids in extract 56 that are responsible for its registered anti-parasitic capacity.…”

Section: Discussionmentioning

confidence: 99%

Amaryllidaceae plants: a potential natural resource for the treatment of Chagas disease

et al. 2021

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Background Chagas disease is a neglected zoonosis caused by the parasite Trypanosoma cruzi. It affects over six million people, mostly in Latin America. Drugs available to treat T. cruzi infection have associated toxicity and questionable efficacy at the chronic stage. Hence, the discovery of more effective and safer drugs is an unmet medical need. For this, natural products represent a pool of unique chemical diversity that can serve as excellent templates for the synthesis of active molecules. Methods A collection of 79 extracts of Amaryllidaceae plants were screened against T. cruzi. Active extracts against the parasite were progressed through two cell toxicity assays based on Vero and HepG2 cells to determine their selectivity profile and discard those toxic to host cells. Anti-T. cruzi-specific extracts were further qualified by an anti-amastigote stage assay. Results Two extracts, respectively from Crinum erubescens and Rhodophiala andicola, were identified as highly active and specific against T. cruzi and its mammalian replicative form. Conclusions The results retrieved in this study encourage further exploration of the chemical content of these extracts in search of new anti-T. cruzi drug development starting points. Graphic abstract

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Section: Discussionmentioning

confidence: 99%

Amaryllidaceae plants: a potential natural resource for the treatment of Chagas disease

et al. 2021

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“…Later, different research groups have described some variations in the concentration of ATCI, DTNB or AChE. For example, Tallini et al (2018) and Rojas-Vera et al (2021) apply an AChE working solution with concentration of 6.24 U/ml. Bozkurt et al (2021) use solutions with concentrations of 0.2 mM for DTNB and 0.24 mM for ATCI while Zhan et al (2017) use 3 mM and 15 mM for DTNB and ATCI, respectively.…”

Section: Microplate Assaymentioning

confidence: 99%

“…GC-MS is the most applied approach to identify Amaryllidaceae alkaloids and to determine their relative percentage in the alkaloid mixtures (Cortes et al 2015, Bozkurt et al 2017. In the recent years, in silico approaches have been frequently used for both, searching for AChE inhibitors within the studied extracts and to better explain their activity (Moraga-Nicola ´s et al 2018; Moreno et al 2020;Ortiz et al 2018;Rojas-Vera et al 2021;Shawky et al 2019;Sibanyoni et al 2020, etc. ).…”

Section: Extracts From Amaryllidaceae Plants With Ache Inhibitory Activitymentioning

confidence: 99%

“…Similarly, 1-O-acetylcaranine, galanthine, 1-Oacetyllycorine, sternbergine, 2-methoxypratosine, cantabricine, galanthamine, N-demethylgalanthamine, N-formylnorgalanthamine, 6-epimesembranol, mesembrine, and pancratinine C identified in Phaedranassa species (Moreno et al 2021) and vittatine, crinine and crinamine, originating from Phaedranassa brevifolia Meerow were subjected to molecular docking (Acosta et al 2021). In another docking study of buphanisine, lycorine and sanguinine, detected in the leaf extract of Crinum amabile, the X-ray complexes between hAChE and donepezil and paraoxon (PDB codes: 4EY7 and 5HF5) were used in AutoDock software (Rojas-Vera et al 2021). In general, the corresponding estimated binding free energies in the above mentioned reports were lower than those for galanthamine.…”

Section: Docking Studies On Other Amaryllidaceae Alkaloidsmentioning

confidence: 99%

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The Amaryllidaceae alkaloids: an untapped source of acetylcholinesterase inhibitors

et al. 2021

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The AChE inhibitory activity of alkaloid extracts and compounds has been in the focus of research on the plants of Amaryllidoideae subfamily since the approval of galanthamine in 2001 by FDA for treatment of mild to moderate Alzheimer's disease. A small fraction of the huge biodiversity of the plants producing Amaryllidaceae alkaloids has been studied as a source of AChE inhibitors. Less than 20% of the known Amaryllidaceae alkaloids have been tested in vitro for their ability to inhibit AChE. Galanthamine, lycorine and haemanthamine are scaffolds for semi-synthesis of potent AChE inhibitors. In the last years, galanthamine has been studied in silico for drug optimization and synthesis of potent dual-binding AChE inhibitors. In silico studies of other Amaryllidaceae alkaloids have also provoked the interest of researchers in the last years. The aim of this article is to provide a comprehensive review on studies of the AChE inhibitory activity of extracts and compounds from the plants of Amaryllidoideae subfamily covering the literature from the last two decades.

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“…Due to its high cost and low yield, this molecule is still obtained from Amaryllidaceae species such as Galanthus nivalis, Leucojum aestivum, Lycoris radiata, and different species of Narcissus by pharmaceutical companies [23]. In recent years, the search for new bioactive structures obtained from Amaryllidadeae species has increased, and the anti-cholinesterase potential of different Crinum species has been reported for C. amabile, C. bulbispermum, C. erubescens, C. jagus, C. moorei and C. zeylanicum collected in South America [24][25][26][27].…”

Section: Introductionmentioning

confidence: 99%

Alkaloid Profiling and Cholinesterase Inhibitory Potential of Crinum × amabile Donn. (Amaryllidaceae) Collected in Ecuador

Tallini

Carrasco

León

et al. 2021

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Natural products are one of the main sources for developing new drugs. The alkaloids obtained from the plant family Amaryllidaceae have interesting structures and biological activities, such as acetylcholinesterase inhibition potential, which is one of the mechanisms used for the palliative treatment of Alzheimer’s disease symptoms. Herein we report the alkaloidal profile of bulbs and leaves extracts of Crinum × amabile collected in Ecuador and their in vitro inhibitory activity on acetylcholinesterase (AChE) and butyrylcholinesterase (BuChE) enzymes. Using Gas Chromatography coupled to Mass Spectrometry (GC-MS), we identified 12 Amaryllidaceae alkaloids out of 19 compounds detected in this species. The extracts from bulbs and leaves showed great inhibitory activity against AChE and BuChE, highlighting the potential of Amaryllidaceae family in the search of bioactive molecules.

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Alkaloid profile and cholinesterase inhibition activity of five species of Amaryllidaceae family collected from Mérida state-Venezuela

Cited by 25 publications

References 45 publications

Amaryllidaceae plants: a potential natural resource for the treatment of Chagas disease

Amaryllidaceae plants: a potential natural resource for the treatment of Chagas disease

The Amaryllidaceae alkaloids: an untapped source of acetylcholinesterase inhibitors

Alkaloid Profiling and Cholinesterase Inhibitory Potential of Crinum × amabile Donn. (Amaryllidaceae) Collected in Ecuador

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