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

Plants ◽  
2021 ◽  
Vol 10 (12) ◽  
pp. 2686
Author(s):  
Luciana R. Tallini ◽  
Angelo Carrasco ◽  
Karen Acosta León ◽  
Diego Vinueza ◽  
Jaume Bastida ◽  
...  
Keyword(s):  
Inhibitory Activity ◽  
Biological Activities ◽  
New Drugs ◽  
Bioactive Molecules ◽  
Acetylcholinesterase Inhibition ◽  
Plant Family ◽  
Disease Symptoms ◽  
Amaryllidaceae Alkaloids ◽  
Inhibitory Potential

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.

scholarly journals Chemical Profiling and Cholinesterase Inhibitory Activity of Five Phaedranassa Herb. (Amaryllidaceae) Species from Ecuador

Molecules ◽  
2020 ◽  
Vol 25 (9) ◽  
pp. 2092 ◽  
Author(s):  
Raúl Moreno ◽  
Luciana R. Tallini ◽  
Cristina Salazar ◽  
Edison H. Osorio ◽  
Evelin Montero ◽  
...  
Keyword(s):  
Inhibitory Activity ◽  
Potential Role ◽  
Biological Activities ◽  
New Drugs ◽  
Inhibitory Effects ◽  
Chemical Profiling ◽  
Cholinesterase Inhibitory Activity ◽  
Insight Into

It is estimated that 50 million people in the world live with dementia, 60–70% of whom suffer from Alzheimer’s disease (AD). Different factors are involved in the development of AD, including a reduction in the cholinergic neurotransmission level. The Amaryllidaceae plant family contains an exclusive, large, and still understudied alkaloid group characterized by a singular skeleton arrangement and a broad spectrum of biological activities. The chemistry and biodiversity of Ecuadorian representatives of the Phaedranassa genus (Amaryllidaceae) have not been widely studied. In this work, five Ecuadorian Phaedranassa species were examined in vitro for their activity towards the enzymes acetyl- (AChE) and butyrylcholinesterase (BuChE), and the alkaloid profile of bulb extracts was analyzed by GC-MS. The species Phaedranassa cuencana and Phaedranassa dubia showed the most AChE and BuChE inhibitory activity, respectively. To obtain insight into the potential role of the identified alkaloids in these inhibitory effects, docking experiments were carried out, and cantabricine showed in silico inhibitory activity against both cholinesterase structures. Our results show that Amaryllidaceae species from Ecuador are a potential source of new drugs for the palliative treatment of AD.

Synthesis, Molecular Docking and Pharmacological Investigation of Heterocyclic Amine Derivatives as Potential Anticancer Agents

2021 ◽  
Author(s):  
Ahmed Sadiq Sheikh ◽  
Humaira Nadeem ◽  
Mahboob Alam ◽  
Muhammad Tariq Khan ◽  
Ameer Khusro ◽  
...  
Keyword(s):  
Molecular Docking ◽  
Carbonic Anhydrase ◽  
Anticancer Agents ◽  
Inhibitory Activity ◽  
Chemotherapeutic Agents ◽  
New Drugs ◽  
Heterocyclic Amine ◽  
Life Threatening ◽  
Inhibitory Potential

Abstract Cancer is life threatening disease that causes great damage to health worldwide. Studies shown that hypoxia is the major contributor to tumor and cancer development due to overexpression of carbonic anhydrase. To encounter such cells abnormalities, demanding new drugs or novel analogs of currently in use. Therefore, the search for new pharmacoactive moieties with considerable effective activity against such tumors and cancers is needed. The implication of heterocyclic amine and acetamide derivatives well known as chemotherapeutic agents. Heterocyclic amine morpholine was taken as principal products and its new derivatives were synthesized after being designed computationally via molecular docking. A series of some of its new synthetic analogs i.e heterocyclic amine derivatives 1(a-o) were successfully synthesized and screened for their anticancer and carbonic anhydrase inhibitory potential. Most of the compounds showed good results possessing reasonable carbonic anhydrase inhibitory activity particularly compounds 1c, 1d, 1h and 1i showed very reasonable carbonic anhydrase inhibitory activity whereas compound 1h showed maximum inhibition comparable to acetazolamide. Similarly, four of the synthesized compounds showed good anticancer activity particularly compound 1b, 1c, 1h, and 1i showed reasonable, whereas compound 1h have better IC50 value comparable to cisplatin when evaluated via in vitro MTT assay.

scholarly journals Effect of Germination on Alfalfa and Buckwheat: Phytochemical Profiling by UHPLC-ESI-QTOF-MS/MS, Bioactive Compounds, and In-Vitro Studies of Their Diabetes and Obesity-Related Functions

Antioxidants ◽  
2021 ◽  
Vol 10 (10) ◽  
pp. 1613
Author(s):  
Simon-Okomo Aloo ◽  
Fred-Kwame Ofosu ◽  
Deog-Hwan Oh
Keyword(s):  
Inhibitory Activity ◽  
Biological Activities ◽  
Radical Scavenging Activity ◽  
Radical Scavenging ◽  
Alfalfa Seed ◽  
Edible Seeds ◽  
Alfalfa Sprouts ◽  
Inhibitory Potential ◽  
Alfalfa Sprout

Germination can be used to enhance nutritional value and health functions of edible seeds. Sprouts are considered healthier than raw seeds because they are richer in the basic nutritional components (carbohydrates, protein, vitamins, and minerals) and also contain more bioactive components responsible for various biological activities. The effect of sprouting on the antioxidant, antidiabetic, antiobesity activities, and metabolite profiles of alfalfa and buckwheat seeds was investigated in this study. DPPH radical scavenging activity was highest in buckwheat sprouts followed by alfalfa sprout, buckwheat seed, and alfalfa seed, respectively. ABTS radical scavenging potential showed a similar trend as DPPH with buckwheat sprouts exerting the best scavenging capacity. Alfalfa sprout and buckwheat seed exhibited the highest percentage inhibitory activity of α-glucosidase (96.6 and 96.5%, respectively). Alfalfa sprouts demonstrated the strongest inhibitory activity against pancreatic lipase (57.12%) while alfalfa seed showed the highest advanced glycation end products (AGEs) formation inhibitory potential (28.7%). Moreover, thirty-three (33) metabolites were characterized in the seed and sprout samples. Sprouts demonstrated a higher level of metabolites compared to raw seeds. Hence, depending on the type of seed and the target activity, sprouting is a good technique to alter the secondary metabolites and functional properties of edible seeds.

scholarly journals The toxic effect of Vu-Defr, a defensin from Vigna unguiculata seeds, on Leishmania amazonensis is associated with reactive oxygen species production, mitochondrial dysfunction, and plasma membrane perturbation

2018 ◽  
Vol 64 (7) ◽  
pp. 455-464 ◽  
Author(s):  
Géssika Silva Souza ◽  
Lais Pessanha de Carvalho ◽  
Edésio José Tenório de Melo ◽  
Valdirene Moreira Gomes ◽  
André de Oliveira Carvalho
Keyword(s):  
Reactive Oxygen Species ◽  
Mitochondrial Membrane ◽  
Biological Activities ◽  
Reactive Oxygen ◽  
Leishmania Amazonensis ◽  
New Drugs ◽  
Oxygen Species ◽  
Membrane Perturbation ◽  
Plant Defensins

Plant defensins are plant antimicrobial peptides that present diverse biological activities in vitro, including the elimination of Leishmania amazonensis. Plant defensins are considered promising candidates for the development of new drugs. This protozoan genus has great epidemiological importance and the mechanism behind the protozoan death by defensins is unknown, thus, we chose L. amazonensis for this study. The aim of the work was to analyze the possible toxic mechanisms of Vu-Defr against L. amazonensis. For analyses, the antimicrobial assay was repeated as previously described, and after 24 h, an aliquot of the culture was tested for viability, membrane perturbation, mitochondrial membrane potential, reactive oxygen species (ROS) and nitric oxide (NO) inductions. The results of these analyses indicated that after interaction with L. amazonensis, the Vu-Defr causes elimination of promastigotes from culture, membrane perturbation, mitochondrial membrane collapse, and ROS induction. Our analysis demonstrated that NO is not produced after Vu-Defr and L. amazonensis interaction. In conclusion, our work strives to help to fill the gap relating to effects caused by plant defensins on protozoan and thus better understand the mechanism of action of this peptide against L. amazonensis.

scholarly journals Synthesis and AChE Inhibitory Activity of Novel Thiazolylhydrazone Derivatives

Molecules ◽  
2019 ◽  
Vol 24 (13) ◽  
pp. 2392 ◽  
Author(s):  
Derya Osmaniye ◽  
Begüm Nurpelin Sağlık ◽  
Ulviye Acar Çevik ◽  
Serkan Levent ◽  
Betül Kaya Çavuşoğlu ◽  
...  
Keyword(s):  
Alzheimer’S Disease ◽  
Alzheimer's Disease ◽  
Inhibitory Activity ◽  
New Drugs ◽  
Brain Diseases ◽  
Structure Identification ◽  
Ache Inhibitor ◽  
In Vitro Tests ◽  
Active Inhibitor

Alzheimer’s disease (AD) is the most common of the degenerative brain diseases and is described together with the impairment of cognitive function. Patients with AD lose the capability to code new memories, and life conditions are extremely difficult. The development of new drugs in this area continues at a great pace. A novel series of thiazole-piperazine hybrids, aimed against Alzheimer’s disease (AD), have been synthesized. The structure identification of synthesized compounds was elucidated by 1HNMR, 13C-NMR, and LCMSMS spectroscopic methods. The inhibitory potential of the synthesized compounds on cholinesterase enzymes was investigated. The compounds 3a, 3c and 3i showed significant inhibitory activity on the acetylcholinesterase (AChE) enzyme. On the other hand, none of the compounds showed significant inhibitory activity on the butyrylcholinesterase (BChE) enzyme. In addition to enzyme inhibition studies, enzyme kinetic studies were performed to observe the effects of the most active inhibitor compounds on the substrate–enzyme relationship. In addition to in vitro tests, docking studies also indicated that compound 3c potentially acts as a dual binding site AChE inhibitor.

scholarly journals Metabolite Profiling of Aquilaria malaccensis Leaf Extract Using Liquid Chromatography-Q-TOF-Mass Spectrometry and Investigation of Its Potential Antilipoxygenase Activity In-Vitro

Processes ◽  
2020 ◽  
Vol 8 (2) ◽  
pp. 202 ◽  
Author(s):  
Manar A. Eissa ◽  
Yumi Z. H-Y. Hashim ◽  
Dina M. El-Kersh ◽  
Saripah S. S. Abd-Azziz ◽  
Hamzah Mohd. Salleh ◽  
...  
Keyword(s):  
Biological Activities ◽  
Chemical Constituents ◽  
Oral Epithelial Cells ◽  
Aquilaria Malaccensis ◽  
Ic50 Value ◽  
Mucosal Cells ◽  
Anti Inflammatory ◽  
Agarwood Resin ◽  
Inhibitory Potential

The Aquilaria malaccensis species of the genus Aquilaria is an abundant source of agarwood resin and many bioactive phytochemicals. Recent data regarding the chemical constituents and biological activities of Aquilaria leaves led us to attempt to qualitatively profile the metabolites of Aquilaria malaccensis leaves from a healthy, noninoculated tree through phytochemical screening, GC-MS, and LC/Q-TOF-MS. The present work is also the first to report the antilipoxygenase activity of A. malaccensis leaves from healthy noninoculated tree and investigate its toxicity on oral mucosal cells. A total of 53 compounds were tentatively identified in the extract, some of which have been described in literature as exhibiting anti-inflammatory activity. A number of compounds were identified for the first time in the extract of A. malaccensis leaf, including quercetin, quercetin-O-hexoside, kaempferol-O-dirhamnoside, isorhamnetin-O-hexoside, syringetin-O-hexoside, myricetin, tetrahydroxyflavanone, hesperetin, sissotrin, and lupeol. The antilipoxygenase assay was used to determine the lipoxygenase (LOX) inhibitory potential of the extract, while a WST-1 assay was conducted to investigate the effect of the extract on oral epithelial cells (OEC). The extract implied moderate anti-LOX activity with IC50 value of 71.6 µg/mL. Meanwhile, the cell viability of OEC ranged between 92.55% (10 µg/mL)–76.06% ± (100 µg/mL) upon treatment, indicating some potential toxicity risks. The results attained encourage future studies of the isolation of bioactive compounds from Aquilaria malaccensis leaves, as well as further investigation on the anti-inflammatory mechanisms and toxicity associated with their use.

scholarly journals GC-MS Investigation of Amaryllidaceae Alkaloids in Galanthus xvalentinei nothosubsp. subplicatus

2013 ◽  
Vol 8 (3) ◽  
pp. 1934578X1300800
Author(s):  
Buket Bozkurt Sarikaya ◽  
Strahil Berkov ◽  
Jaume Bastida ◽  
Gulen Irem Kaya ◽  
Mustafa Ali Onur ◽  
...  
Keyword(s):  
Inhibitory Activity ◽  
Anticholinesterase Activity ◽  
Amaryllidaceae Alkaloids ◽  
Acetylcholinesterase Inhibitory Activity ◽  
Aerial Parts ◽  
Ms Analysis ◽  
Ellman’S Method ◽  
First Time

A GC-MS analysis of alkaloids in the aerial parts and bulbs of Galanthus x valentinei nothosubsp. subplicatus was performed for the first time. Totally, twenty-six alkaloids were identified, of which tazettine and galanthindole were the major ones. Acetylcholinesterase inhibitory activity of the alkaloidal extracts was determined using modified in vitro Ellman's method. Significant anticholinesterase activity was observed in the tested samples (bulbs: IC50 = 21.3 μg/mL, aerial parts: IC50 = 16.3 μg/mL).

scholarly journals In vitro and in vivo activities of flavonoids – apigenin, baicalin, chrysin, scutellarin – in regulation of hypertension – a review for their possible effects in pregnancy-induced hypertension

2019 ◽  
Vol 65 (1) ◽  
pp. 55-70 ◽  
Author(s):  
Marcin Ożarowski ◽  
Radosław Kujawski ◽  
Przemysław Ł. Mikołajczak ◽  
Karolina Wielgus ◽  
Andrzej Klejewski ◽  
...  
Keyword(s):  
Ex Vivo ◽  
Biological Activities ◽  
Wide Spectrum ◽  
Chemical Compounds ◽  
New Drugs ◽  
Future Application ◽  
Mediators Of Inflammation ◽  
And Function

Summary Flavonoids and their conjugates are the most important group of natural chemical compounds in drug discovery and development. The search for pharmacological activity and new mechanisms of activity of these chemical compounds, which may inhibit mediators of inflammation and influence the structure and function of endothelial cells, can be an interesting pharmacological strategy for the prevention and adjunctive treatments of hypertension, especially induced by pregnancy. Because cardiovascular diseases have multi-factorial pathogenesis these natural chemical compounds with wide spectrum of biological activities are the most interesting source of new drugs. Extracts from one of the most popular plant used in Traditional Chinese Medicine, Scutellaria baicalensis Georgi could be a very interesting source of flavonoids because of its exact content in quercetin, apigenin, chrysin and scutellarin as well as in baicalin. These flavonoids exert vasoprotective properties and many activities such as: anti-oxidative via several pathways, anti-in-flammatory, anti-ischaemic, cardioprotective and anti-hypertensive. However, there is lack of summaries of results of studies in context of potential and future application of flavonoids with determined composition and activity. Our review aims to provide a literature survey of in vitro, in vivo and ex vivo pharmacological studies of selected flavonoids (apigenin, chrysin and scutellarin, baicalin) in various models of hypertension carried out in 2008–2018.

scholarly journals Antioxidant, Antidiabetic, and Anticholinesterase Activities and Phytochemical Profile of Azorella glabra Wedd

Plants ◽  
2019 ◽  
Vol 8 (8) ◽  
pp. 265 ◽  
Author(s):  
Immacolata Faraone ◽  
Dilip K. Rai ◽  
Daniela Russo ◽  
Lucia Chiummiento ◽  
Eloy Fernandez ◽  
...  
Keyword(s):  
Biological Activities ◽  
Radical Scavenging Activity ◽  
Radical Scavenging ◽  
Reducing Power ◽  
Ethanol Extract ◽  
Flowering Plant ◽  
Acetylcholinesterase Inhibition ◽  
Neutral Radical ◽  
Phytochemical Profile

Oxidative stress is involved in different diseases, such as diabetes and neurodegenerative diseases. The genus Azorella includes about 70 species of flowering plant species; most of them are commonly used as food and in particular as a tea infusion in the Andean region of South America in folk medicine to treat various chronic diseases. Azorella glabra Wedd. aerial parts were firstly analyzed for their in vitro antioxidant activity using different complementary assays. In particular, radical scavenging activity was tested against biological neutral radical DPPH; ferric reducing power and lipid peroxidation inhibitory capacity (FRAP and Beta-Carotene Bleaching tests) were also determined. The Relative Antioxidant Capacity Index (RACI) was used to compare data obtained by different assays. Then, the inhibitory ability of samples was investigated against α-amylase and α-glucosidase enzymes involved in diabetes and against acetylcholinesterase and butyrylcholinesterase enzymes considered as strategy for the treatment of Parkinson’s or Alzheimer’s diseases. Moreover, the phytochemical profile of the sample showing the highest RACI (1.35) and interesting enzymatic activities (IC50 of 163.54 ± 9.72 and 215.29 ± 17.10 μg/mL in α-glucosidase and acetylcholinesterase inhibition, respectively) was subjected to characterization and quantification of its phenolic composition using LC-MS/MS analysis. In fact, the ethyl acetate fraction derived from ethanol extract by liquid/liquid extraction showed 29 compounds, most of them are cinnamic acid derivatives, flavonoid derivatives, and a terpene. To the best of our knowledge, this is the first report about the evaluation of significant biological activities and phytochemical profile of A. glabra, an important source of health-promoting phytochemicals.

scholarly journals Propolis: A Complex Natural Product with a Plethora of Biological Activities That Can Be Explored for Drug Development

2015 ◽  
Vol 2015 ◽  
pp. 1-29 ◽  
Author(s):  
Ricardo Silva-Carvalho ◽  
Fátima Baltazar ◽  
Cristina Almeida-Aguiar
Keyword(s):  
Chemical Composition ◽  
Biological Activities ◽  
Clinical Effectiveness ◽  
Biological Properties ◽  
New Drugs ◽  
Published Data ◽  
Alternative Source ◽  
Scientific Attention

The health industry has always used natural products as a rich, promising, and alternative source of drugs that are used in the health system. Propolis, a natural resinous product known for centuries, is a complex product obtained by honey bees from substances collected from parts of different plants, buds, and exudates in different geographic areas. Propolis has been attracting scientific attention since it has many biological and pharmacological properties, which are related to its chemical composition. Severalin vitroandin vivostudies have been performed to characterize and understand the diverse bioactivities of propolis and its isolated compounds, as well as to evaluate and validate its potential. Yet, there is a lack of information concerning clinical effectiveness. The goal of this review is to discuss the potential of propolis for the development of new drugs by presenting published data concerning the chemical composition and the biological properties of this natural compound from different geographic origins.

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