Ortiz JE

References (6)

Title : Inhibitory effect of galantamine and donepezil combination against cholinesterase: An in silico and in vitro study - Adarvez-Feresin_2024_Arch.Pharm.(Weinheim)__e2300581
Author(s) : Adarvez-Feresin CW , Ortiz JE , Pineiro MD , Parravicini O , Enriz RD , Garro AD , Feresin GE
Ref : Arch Pharm (Weinheim) , :e2300581 , 2024
Abstract : This study aimed to evaluate the in silico and in vitro inhibitory effect of the combined use of galantamine (GAL) and donepezil (DON) against acetylcholinesterase and butyrylcholinesterase (BuChE) enzymes. In silico and in vitro cholinesterase analysis were carried out for GAL and DON alone and combined. Molecular modeling studies were carried out (docking analysis, molecular dynamics simulation, and quantum theory of atoms in molecules). Cholinesterase's inhibitory activities by modified Ellman's method and the drug combination effect using the Chou-Talalay method were assayed. GAL/DON combination showed the co-occupancy of the ligands in both enzymes through in silico studies. Regarding in vitro BuChE inhibition analyses, three of five combinations showed an interaction between GAL and DON at the threshold of additive affect (0.9 < CI < 1.1), with a tendency toward a synergistic effect for higher concentrations. This is the first report showing the efficacy of the GAL/DON combinations inhibiting BuChE, showing the importance of analyzing the behavior of different ligands when co-occupancy into the active site is possible. These combinations might be a possible therapy to improved efficacy, reduced doses, minor side effects, and high levels of the neurotransmitter in the synaptic space for Alzheimer's disease.
ESTHER : Adarvez-Feresin_2024_Arch.Pharm.(Weinheim)__e2300581
PubMedSearch : Adarvez-Feresin_2024_Arch.Pharm.(Weinheim)__e2300581
PubMedID: 38229212

Title : Antiparasitic Activity of Hippeastrum Species and Synergistic Interaction between Montanine and Benznidazole against Trypanosoma cruzi - Pineiro_2023_Microorganisms_11_
Author(s) : Pineiro M , Ortiz JE , Spina Zapata RM , Barrera PA , Sosa MA , Roitman G , Bastida J , Feresin GE
Ref : Microorganisms , 11 : , 2023
Abstract : BACKGROUND: Hippeastrum species have a wide range of biological properties. In Argentina, this genus comprises ten widely distributed species. PURPOSE: To evaluate the antiparasitic and anticholinesterase activities and chemical profiles of seven Argentinean Hippeastrum species and determine the synergism between the major isolated alkaloid-montanine-and benznidazole in anti-Trypanosoma cruzi activity. METHODS: The antiparasitic activity was evaluated through antiproliferative and viability assays against T. cruzi epimastigotes. Synergism assays were performed using the Chou-Talalay method. AChE and BuChE inhibitory activities were also assessed. The alkaloid composition was obtained using GC-MS analysis. RESULTS: All extracts showed strong growth inhibition of T. cruzi epimastigote proliferation. The extracts from H. aglaiae, H. aulicum, and H. hybrid stand out for their potent and total growth inhibition, which was comparable to benznidazole. The H. reticulatum extract showed strong Acetylcholinesterase (AChE) inhibitory activities, while five species showed moderate Butyrylcholinesterase (BuChE) inhibition. Fifteen alkaloids were identified by means of GC-MS. Regarding the synergism assessment, the highest synergistic effect was obtained from the combination of montanine and benznidazole. CONCLUSION: Hippeastrum species bulb extracts from Argentina were shown to be a good source of antiparasitic alkaloids and cholinesterase inhibitors. The synergism between montanine and benznidazole emerges as a potential combination for future studies to treat Chagas disease.
ESTHER : Pineiro_2023_Microorganisms_11_
PubMedSearch : Pineiro_2023_Microorganisms_11_
PubMedID: 36677436

Title : Alkaloids Analysis of Habranthus cardenasianus (Amaryllidaceae), Anti-Cholinesterase Activity and Biomass Production by Propagation Strategies - Zaragoza-Puchol_2021_Molecules_26_
Author(s) : Zaragoza-Puchol D , Ortiz JE , Orden AA , Sanchez M , Palermo J , Tapia A , Bastida J , Feresin GE
Ref : Molecules , 26 : , 2021
Abstract : Plants in the Amaryllidaceae family synthesize a diversity of bioactive alkaloids. Some of these plant species are not abundant and have a low natural multiplication rate. The aims of this work were the alkaloids analysis of a Habranthus cardenasianus bulbs extract, the evaluation of its inhibitory activity against cholinesterases, and to test several propagation strategies for biomass production. Eleven compounds were characterized by GC-MS in the alkaloid extract, which showed a relatively high proportion of tazettine. The known alkaloids tazettine, haemanthamine, and the epimer mixture haemanthidine/6-epi-haemanthidine were isolated and identified by spectroscopic methods. Inhibitory cholinesterases activity was not detected. Three forms of propagation were performed: bulb propagation from seed, cut-induced bulb division, and micropropagated bulbs. Finally, different imbibition and post-collection times were evaluated in seed germination assays. The best propagation method was cut-induced bulb division with longitudinal cuts into quarters (T1) while the best conditions for seed germination were 0-day of post-collection and two days of imbibition. The alkaloids analyses of the H. cardenasianus bulbs showed that they are a source of anti-tumoral alkaloids, especially pretazettine (tazettine) and T1 is a sustainable strategy for its propagation and domestication to produce bioactive alkaloids.
ESTHER : Zaragoza-Puchol_2021_Molecules_26_
PubMedSearch : Zaragoza-Puchol_2021_Molecules_26_
PubMedID: 33401696

Title : Cholinesterase-inhibitory effect and in silico analysis of alkaloids from bulbs of Hieronymiella species - Ortiz_2018_Phytomedicine_39_66
Author(s) : Ortiz JE , Garro A , Pigni NB , Aguero MB , Roitman G , Slanis A , Enriz RD , Feresin GE , Bastida J , Tapia A
Ref : Phytomedicine , 39 :66 , 2018
Abstract : BACKGROUND: In Argentina, the Amaryllidaceae family (59 species) comprises a wide variety of genera, only a few species have been investigated as a potential source of cholinesterases inhibitors to treat Alzheimer disease (AD). PURPOSE: To study the acetylcholinesterase (AChE) and butyrylcholinesterase (BChE) inhibitory activities of the basic dichloromethane extracts (E) from Hieronymiella aurea, H. caletensis, H. clidanthoides, H. marginata, and H. speciosa species, as well as the isolated compounds from these plant extracts. STUDY DESIGN AND METHODS: AChE and BChE inhibitory activities were evaluated with the Ellman's spectrophotometric method. The alkaloids composition from the E was obtained by gas chromatography-mass spectrometry (GC-MS). The E were successively chromatographed on a silica gel column and permeated on Sephadex LH-20 column to afford the main alkaloids identified by means of spectroscopic data. Additionally, an in silico study was carried out. RESULTS: Nine known alkaloids were isolated from the E of five Hieronymiella species. Galanthamine was identified in all the species by GC-MS standing out H. caletensis with a relative abundance of 9.79% of the total ion current. Strong AChE (IC50=1.84 - 15.40microg/ml) and moderate BChE (IC50=23.74 - 136.40microg/ml) inhibitory activities were displayed by the extracts. Among the isolated alkaloids, only sanguinine and chlidanthine (galanthamine-type alkaloids) demonstrated inhibitory activity toward both enzymes. The QTAIM study suggests that sanguinine has the strongest affinity towards AChE, attributed to an additional interaction with Ser200 as well as stronger molecular interactions Glu199 and His440.These results allowed us to differentiate the molecular behavior in the active site among alkaloids possessing different in vitro inhibitory activities. CONCLUSION: Hieronymiella species growing in Argentina represent a rich and widespread source of galanthamine and others AChE and BChE inhibitors alkaloids. Additionally, the new trend towards the use of natural extracts as pharmaceuticals rather than pure drugs opens a pathway for the development of a phytomedicine derived from extracts of Hieronymiella spp.
ESTHER : Ortiz_2018_Phytomedicine_39_66
PubMedSearch : Ortiz_2018_Phytomedicine_39_66
PubMedID: 29433685

Title : Alkaloids from Hippeastrum argentinum and Their Cholinesterase-Inhibitory Activities: An in Vitro and in Silico Study - Ortiz_2016_J.Nat.Prod_79_1241
Author(s) : Ortiz JE , Pigni NB , Andujar SA , Roitman G , Suvire FD , Enriz RD , Tapia A , Bastida J , Feresin GE
Ref : Journal of Natural Products , 79 :1241 , 2016
Abstract : Two new alkaloids, 4-O-methylnangustine (1) and 7-hydroxyclivonine (2) (montanine and homolycorine types, respectively), and four known alkaloids were isolated from the bulbs of Hippeastrum argentinum, and their cholinesterase-inhibitory activities were evaluated. These compounds were identified using GC-MS, and their structures were defined by physical data analysis. Compound 2 showed weak butyrylcholinesterase (BuChE)-inhibitory activity, with a half-maximal inhibitory concentration (IC50) value of 67.3 +/- 0.09 muM. To better understand the experimental results, a molecular modeling study was also performed. The combination of a docking study, molecular dynamics simulations, and quantum theory of atoms in molecules calculations provides new insight into the molecular interactions of compound 2 with BuChE, which were compared to those of galantamine.
ESTHER : Ortiz_2016_J.Nat.Prod_79_1241
PubMedSearch : Ortiz_2016_J.Nat.Prod_79_1241
PubMedID: 27096334

Title : Wild Argentinian Amaryllidaceae, a New Renewable Source of the Acetylcholinesterase Inhibitor Galanthamine and Other Alkaloids - Ortiz_2012_Molecules_17_13473
Author(s) : Ortiz JE , Berkov S , Pigni NB , Theoduloz C , Roitman G , Tapia A , Bastida J , Feresin GE
Ref : Molecules , 17 :13473 , 2012
Abstract : The Amaryllidaceae family is well known for its pharmacologically active alkaloids An important approach to treat Alzheimer&'s disease involves the inhibition of the enzyme acetylcholinesterase AChE Galanthamine an Amaryllidaceae alkaloid is an effective selective reversible and competitive AchE inhibitor This work was aimed at studying the alkaloid composition of four wild Argentinian Amarillydaceae species for the first time as well as analyzing their inhibitory activity on acetylcholinesterase Alkaloid content was characterized by means of GC-MS analysis Chloroform basic extracts from Habranthus jamesonii Phycella herbertiana Rhodophiala mendocina and Zephyranthes filifolia collected in the Argentinian Andean region all contained galanthamine and showed a strong AChE inhibitory activity IC(50 between 1.2 and 2 181;g/mL To our knowledge no previous reports on alkaloid profiles and AChEIs activity of wild Argentinian Amarillydaceae species have been publisihed The demand for renewable sources of industrial products like galanthamine and the need to protect plant biodiversity creates an opportunity for Argentinian farmers to produce such crops.
ESTHER : Ortiz_2012_Molecules_17_13473
PubMedSearch : Ortiz_2012_Molecules_17_13473
PubMedID: 23149565