scholarly journals Chemical Constituents and Biologic Activities of Sage Species: A Comparison between Salvia officinalis L., S. glutinosa L. and S. transsylvanica (Schur ex Griseb. & Schenk) Schur

Antioxidants ◽  
2020 ◽  
Vol 9 (6) ◽  
pp. 480 ◽  
Author(s):  
Andrei Mocan ◽  
Mihai Babotă ◽  
Anca Pop ◽  
Ionel Fizeșan ◽  
Alina Diuzheva ◽  
...  
Keyword(s):  
Chemical Constituents ◽  
Hplc Method ◽  
In Vitro Assays ◽  
Cytotoxic Effects ◽  
Starting Point ◽  
Health Related ◽  
Salvia Officinalis L ◽  
First Time ◽  
Rutin And Quercetin

Even though Salvia genus is one of the most known and studied taxa of Lamiaceae family, the knowledge regarding the chemical composition and health-related benefits of some locally used Salvia species (mostly endemic) is still scarce. In this regard, the present work aims to evaluate the chemical profile and potential bioactivities of 70% (v/v) ethanolic extracts obtained from the less-studied S. transsylvanica and S. glutinosa in comparison with S. officinalis. HPLC-PDA analysis revealed the presence of rutin and catechin as the main compounds in the extracts of the three studied species (using the employed HPLC method), whereas the presence of naringenin was highlighted only in S. glutinosa extract. Chlorogenic acid, rutin and quercetin were identified and quantified for the first time in S. transsylvanica extracts. The in vitro antioxidant capacity of each extract was tested through complementary methods (phosphomolybdenum assay, DPPH, ABTS, CUPRAC and FRAP assays), and correlated with the presence of phenolics (especially flavonoids) in high amounts. The neuroprotective and antidiabetic abilities of S. officinalis (the most active as AChE, BChE and α-glucosidase inhibitor), S. glutinosa (the most active as α-amylase inhibitor) and S. transsylvanica were also studied. For each extract it was determined the antimicrobial, antifungal and cytotoxic effects using in vitro assays. The obtained results confirm the potential of S. transsylvanica and S. glutinosa as promising sources of bioactive compounds and as a starting point for further analyses.

scholarly journals Simple Thalidomide Analogs in Melanoma: Synthesis and Biological Activity

2021 ◽  
Vol 11 (13) ◽  
pp. 5823
Author(s):  
Alexia Barbarossa ◽  
Alessia Catalano ◽  
Jessica Ceramella ◽  
Alessia Carocci ◽  
Domenico Iacopetta ◽  
...  
Keyword(s):  
Anticancer Agent ◽  
Ring System ◽  
In Vitro Assays ◽  
Tubulin Polymerization ◽  
Cytotoxic Effects ◽  
Ongoing Research ◽  
Drug Candidates ◽  
Small Series ◽  
Clinical Interest

Thalidomide is an old well-known drug that is still of clinical interest, despite its teratogenic activities, due to its antiangiogenic and immunomodulatory properties. Therefore, efforts to design safer and effective thalidomide analogs are continually ongoing. Research studies on thalidomide analogs have revealed that the phthalimide ring system is an essential pharmacophoric fragment; thus, many phthalimidic compounds have been synthesized and evaluated as anticancer drug candidates. In this study, a panel of selected in vitro assays, performed on a small series of phthalimide derivatives, allowed us to characterize compound 2k as a good anticancer agent, acting on A2058 melanoma cell line, which causes cell death by apoptosis due to its capability to inhibit tubulin polymerization. The obtained data were confirmed by in silico assays. No cytotoxic effects on normal cells have been detected for this compound that proves to be a valid candidate for further investigations to achieve new insights on possible mechanism of action of this class of compounds as anticancer drugs.

scholarly journals Ozonized Water in Microbial Control: Analysis of the Stability, In Vitro Biocidal Potential, and Cytotoxicity

Biology ◽  
2021 ◽  
Vol 10 (6) ◽  
pp. 525
Author(s):  
Laerte Marlon Conceição dos Santos ◽  
Eduardo Santos da Silva ◽  
Fabricia Oliveira Oliveira ◽  
Leticia de Alencar Pereira Rodrigues ◽  
Paulo Roberto Freitas Neves ◽  
...  
Keyword(s):  
Microbial Control ◽  
Fibroblast Cell ◽  
In Vitro Assays ◽  
Control Analysis ◽  
Cytotoxic Effects ◽  
Cell Wall Lysis ◽  
Osmotic Stability ◽  
Human Ear ◽  
The Stability

O3 dissolved in water (or ozonized water) has been considered a potent antimicrobial agent, and this study aimed to test this through microbiological and in vitro assays. The stability of O3 was accessed following modifications of the physicochemical parameters of water, such as the temperature and pH, with or without buffering. Three concentrations of O3 (0.4, 0.6, and 0.8 ppm) dissolved in water were tested against different microorganisms, and an analysis of the cytotoxic effects was also conducted using the human ear fibroblast cell line (Hfib). Under the physicochemical conditions of 4 °C and pH 5, O3 remained the most stable and concentrated compared to pH 7 and water at 25 °C. Exposure to ozonized water resulted in high mortality rates for Escherichia coli, Pseudomonas aeruginosa, Staphylococcus aureus, Enterococcus faecalis, and Candida albicans. Scanning electron micrograph images indicate that the effects on osmotic stability due to cell wall lysis might be one of the killing mechanisms of ozonized water. The biocidal agent was biocompatible and presented no cytotoxic effect against Hfib cells. Therefore, due to its cytocompatibility and biocidal action, ozonized water can be considered a viable alternative for microbial control, being possible, for example, its use in disinfection processes.

Identification of Positive Allosteric Modulators of Glycine Receptors from a High-Throughput Screen Using a Fluorescent Membrane Potential Assay

2016 ◽  
Vol 21 (10) ◽  
pp. 1042-1053 ◽  
Author(s):  
Clara Stead ◽  
Adam Brown ◽  
Cathryn Adams ◽  
Sarah J. Nickolls ◽  
Gareth Young ◽  
...  
Keyword(s):  
Membrane Potential ◽  
High Throughput ◽  
Glycine Receptor ◽  
Functional Characterization ◽  
In Vitro Assays ◽  
Allosteric Modulators ◽  
Inhibitory Neurotransmission ◽  
Starting Point ◽  
Positive Allosteric Modulators

Glycine receptor 3 (GlyRα3) is a ligand-gated ion channel of the cys-loop family that plays a key role in mediating inhibitory neurotransmission and regulation of pain signaling in the dorsal horn. Potentiation of GlyRα3 function is therefore of interest as a putative analgesic mechanism with which to target new therapeutics. However, to date, positive allosteric modulators (PAMs) of this receptor with sufficient selectivity to enable target validation studies have not been described. To address this lack of pharmacological tools, we developed a suite of in vitro assays comprising a high-throughput fluorescent membrane potential screen and a medium-throughput electrophysiology assay using IonFlux HT together with conventional manual patch clamp. Using these assays, we conducted a primary screening campaign and report the structures of hit compounds identified as GlyR PAMs. Our functional characterization data reveal a hit compound with high efficacy relative to current known potentiators and selectivity over GABAAR, another major class of inhibitory neurotransmission receptors of importance to pain. These small-molecule GlyR PAMs have high potential both as early tool compounds to enable pharmacological studies of GlyR inhibitory neurotransmission and as a starting point for the development of potent, selective GlyRα3 PAMs as novel analgesics.

scholarly journals Pharmacologic Activities¬ of 3’-Hydroxypterostilbene: Cytotoxic, Anti-Oxidant, Anti-Adipogenic, Anti-Inflammatory, Histone Deacetylase and Sirtuin 1 Inhibitory Activity

2015 ◽  
Vol 18 (4) ◽  
pp. 713 ◽  
Author(s):  
Jody K Takemoto ◽  
Connie M. Remsberg ◽  
Neal M. Davies
Keyword(s):  
Histone Deacetylase ◽  
Inhibitory Activity ◽  
Sirtuin 1 ◽  
In Vitro Assays ◽  
Naturally Occurring ◽  
Anti Oxidant ◽  
Anti Inflammatory ◽  
First Time ◽  
Stilbene Compounds

Purpose: Delineate the selected pharmacodynamics of a naturally occurring stilbene 3’-Hydroxypterostilbene. Objective: Characterize for the first time the pharmacodynamics bioactivity in several in-vitro assays with relevant roles in heart disease, inflammation, cancer, and diabetes etiology and pathophysiology. Methods: 3’-Hydroxypterostilbene was studied in in-vitro assays to identify possible bioactivity. Results: 3’-Hydroxypterostilbene demonstrated anti-oxidant, anti-inflammatory, cytotoxic, anti-adipogenic, histone deacetylase, and sirtuin-1 inhibitory activity. Conclusions: The importance of understanding individual stilbene pharmacologic activities were delineated.  Small changes in chemical structure of stilbene compounds result in significant pharmacodynamic differences. This article is open to POST-PUBLICATION REVIEW. Registered readers (see “For Readers”) may comment by clicking on ABSTRACT on the issue’s contents page.

scholarly journals Nimesulide Based Novel Glycolamide Esters: Their Design, Synthesis, and Pharmacological Evaluation

2013 ◽  
Vol 2013 ◽  
pp. 1-8 ◽  
Author(s):  
Kavitha Kankanala ◽  
Vangala Ranga Reddy ◽  
Yumnam Priyadarshini Devi ◽  
Lakshmi Narasu Mangamoori ◽  
Khagga Mukkanti ◽  
...  
Keyword(s):  
Cancer Cell Line ◽  
Human Colon ◽  
Colon Cancer Cell Line ◽  
Cytotoxic Activities ◽  
Step Method ◽  
Human Colon Cancer ◽  
Cytotoxic Effects ◽  
Design Synthesis ◽  
First Time

The nimesulide based novel glycolamide esters were designed and synthesized for the first timeviaa three-step method starting from nimesulide. Structures of the synthesized compounds were confirmed by spectroscopic analysis. All the synthesized compounds were examined for their cytotoxic effectsin vitro,some of which showed significant cytotoxic activities against HCT-15 human colon cancer cell line.

scholarly journals Berberine Derivatives as Pseudomonas aeruginosa MexXY-OprM Inhibitors: Activity and In Silico Insights

Molecules ◽  
2021 ◽  
Vol 26 (21) ◽  
pp. 6644
Author(s):  
Giorgia Giorgini ◽  
Gianmarco Mangiaterra ◽  
Nicholas Cedraro ◽  
Emiliano Laudadio ◽  
Giulia Sabbatini ◽  
...  
Keyword(s):  
Pseudomonas Aeruginosa ◽  
In Silico ◽  
Rational Design ◽  
Specific Binding ◽  
In Silico Analysis ◽  
In Vitro Assays ◽  
Binding Modes ◽  
Starting Point ◽  
Berberine Derivatives

The natural alkaloid berberine has been demonstrated to inhibit the Pseudomonas aeruginosa multidrug efflux system MexXY-OprM, which is responsible for tobramycin extrusion by binding the inner membrane transporter MexY. To find a structure with improved inhibitory activity, we compared by molecular dynamics investigations the binding affinity of berberine and three aromatic substituents towards the three polymorphic sequences of MexY found in P. aeruginosa (PAO1, PA7, and PA14). The synergy of the combinations of berberine or berberine derivatives/tobramycin against the same strains was then evaluated by checkerboard and time-kill assays. The in silico analysis evidenced different binding modes depending on both the structure of the berberine derivative and the specific MexY polymorphism. In vitro assays showed an evident MIC reduction (32-fold and 16-fold, respectively) and a 2–3 log greater killing effect after 2 h of exposure to the combinations of 13-(2-methylbenzyl)- and 13-(4-methylbenzyl)-berberine with tobramycin against the tobramycin-resistant strain PA7, a milder synergy (a 4-fold MIC reduction) against PAO1 and PA14, and no synergy against the ΔmexXY strain K1525, confirming the MexY-specific binding and the computational results. These berberine derivatives could thus be considered new hit compounds to select more effective berberine substitutions and their common path of interaction with MexY as the starting point for the rational design of novel MexXY-OprM inhibitors.

scholarly journals Antiproliferative Activity and Apoptotic Efficiency of Syzygium cumini Bark Methanolic Extract against EAC Cells In Vivo

2020 ◽  
Vol 20 ◽  
Author(s):  
Mst. Ayesha Siddika ◽  
Plabon K. Das ◽  
Saharia Y. Asha ◽  
Suraiya Aktar ◽  
Abu Rahyan M. Tareq ◽  
...  
Keyword(s):  
Anticancer Activity ◽  
Antiproliferative Activity ◽  
Methanolic Extract ◽  
Chemical Constituents ◽  
Antioxidant Properties ◽  
In Vitro Assays ◽  
Syzygium Cumini ◽  
Anticancer Activities ◽  
Eac Cells

Background: Syzygium cumini, one of the evidence-based traditional medicinal plant used in the treatment of various ailments. Objectives: Herein, the antioxidant property and anticancer property of Syzygium cumini against Ehrlich Ascites Carcinoma (EAC) were examined in search of effective chemotherapeutics. Methods: In vitro assays, phytochemical and chromatographic analysis were used to determine antioxidant properties and chemical constituents of Syzygium cummini bark methanolic extract (SCBME). Functional assays were used to measure the anticancer activity of SCBME. Fluorescence microscopy and RT-PCR were used to examine morphological and molecular changes of EAC cells followed by SCBME treatment. Results: Phytochemical and GC–MS analysis confirmed the presence of compounds with antioxidant and anticancer activities. Accordingly, we have noted a strong antioxidant activity of SCBME with an IC50 value of 10μg/ml. Importantly, SCBME exerted a dose-dependent anticancer activity with significant inhibition of EAC cell growth (71.08 ± 3.53%; p<0.001), reduction of tumour burden (69.50%; p<0.01) and increase of life span (73.13%; p<0.001) of EACbearing mice at 75mg/kg/day. Besides, SCBME restored the blood toxicity towards normal in EAC-bearing mice (p<0.05). SCBME treated EAC cells showed apoptotic features under a fluorescence microscope and fragment DNA in DNA laddering assay. Moreover, up-regulation of the tumour suppressor p53 and pro-apoptotic Bax and down-regulation of NF-κB and anti-apoptotic Bcl-2 genes, implied induction of apoptosis followed by SCBME treatment. Conclusion: The antiproliferative activity of SCBME against EAC cells is likely due to apoptosis, mediated by regulation of p53 and NF-κB signalling. Thus, SCBME can be considered as a useful resource in cancer chemotherapy.

scholarly journals Mangiferin Rich Products from Aphloia theiformis (Vahl) Benn Leaves: Extraction, Fractionation, Phytochemical Characterization, and Antioxidant Properties

Molecules ◽  
2020 ◽  
Vol 25 (9) ◽  
pp. 2081
Author(s):  
Dovilė Grauzdytė ◽  
Audrius Pukalskas ◽  
Chaker El Kalamouni ◽  
Petras Rimantas Venskutonis
Keyword(s):  
Antioxidant Capacity ◽  
Antioxidant Properties ◽  
Natural Antioxidants ◽  
Liquid Extraction ◽  
In Vitro Assays ◽  
Synthetic Antioxidant ◽  
Liquid Liquid Extraction ◽  
Extraction Solvents ◽  
First Time

Aphloia theiformis is traditionally used in Mauritius, Madagascar, and Reunion Island for treating several diseases. In this study, various extraction solvents and schemes were applied for the recovery of antioxidant rich fractions from the leaves of A. theiformis. The products were evaluated for their antioxidant capacity using well known in vitro assays. Major compounds were characterized by UPLC–QTOF–MS. Hydrophilic extracts of A. theiformis demonstrated strong antioxidant properties, which are comparable with the synthetic antioxidant Trolox. UPLC analysis confirmed mangiferin as the main secondary metabolite of A. theiformis. Tormentic and hydroxytormentic acids as well as their isomers were also abundant in A. theiformis extracts and fractions, while their amounts were determined for the first time. The most potential extract was further separated into the fractions by liquid-liquid extraction and by precipitation at low temperature. Antioxidant capacity and composition of secondary metabolites of derived fractions were determined. Some of the fractions possessed remarkable antioxidant capacity, comparable to pure mangiferin. The results obtained reveal high potential of A. theiformis for recovery of natural antioxidants and other bioactive phytochemicals, particularly mangiferin.

scholarly journals Chemical Constituents From the Aerial Part of Tiliacora triandra (Colebr.) Diels and Their α-Glucosidase and α-Amylase Inhibitory Activity

2020 ◽  
Vol 15 (1) ◽  
pp. 1934578X1989959
Author(s):  
Emmanuel Ayobami Makinde ◽  
Chitchamai Ovatlarnporn ◽  
Chonlatid Sontimuang ◽  
Gaëtan Herbette ◽  
Opeyemi Joshua Olatunji
Keyword(s):  
Inhibitory Activity ◽  
Chemical Constituents ◽  
Ethyl Linoleate ◽  
Resonance Spectroscopy ◽  
Ionization Mass ◽  
Pheophorbide A ◽  
Aerial Parts ◽  
Fatty Acid Derivatives ◽  
First Time

Two new fatty acid derivatives identified as 5,7-dihydroxy-6-oxoheptadecanoic acid (1) and ethyl-5,7-dihydroxy-6-oxooctadecanoate (2) together with four known compounds, ethyl linolenate (3), ethyl linoleate (4), ethyl pheophorbide A (5), and pheophorbide A (6), were isolated from the aerial parts of Tiliacora triandra. All the compounds were isolated from T. triandra for the first time. The structures of the compounds were elucidated using high-resolution electrospray ionization mass spectrometry, 1-dimensional and 2-dimensional nuclear magnetic resonance spectroscopy, and comparison with literature data. All the isolated compounds were evaluated for their in vitro inhibitory activity against α-glucosidase and α-amylase. Compounds 1-6 exhibited α-glucosidase inhibitory activity with half-maximal inhibitory concentration values (IC50) values in the range of 11.58-424.06 μM, while only compound 1 displayed inhibitory activity against α-amylase at an IC50 value of 26.27 μM.

Naucleactonin D, an Indole Alkaloid and other Chemical Constituents from Roots and Fruits of Mitragyna inermis

2012 ◽  
Vol 67 (11) ◽  
pp. 1159-1165 ◽  
Author(s):  
Erik V. Donfack ◽  
Bruno N. Lenta ◽  
Michel D. T. Kongue ◽  
Yannick F. Fongang ◽  
Silvère Ngouela ◽  
...  
Keyword(s):  
Chemical Constituents ◽  
Indole Alkaloid ◽  
Artemia Salina ◽  
Published Data ◽  
Phytochemical Investigation ◽  
Brine Shrimps ◽  
First Time ◽  
C Nmr ◽  
Mitragyna Inermis

Phytochemical investigation of the roots and fruits of Mitragyna inermis (Rubiaceae) resulted in the isolation of a new indole alkaloid, named naucleactonin D (1), together with fourteen known compounds: nauclefiline (2), naucleficine (3), nauclefidine (4), angustoline (5), angustine (6), barbinervic acid (7), quinovic acid 3-O-a-L-rhamnopyranoside (8), betulinic acid (9), a mixture of ursolic (10) and oleanolic acid (11), a mixture of stigmasterol and b-sitosterol, b-sitosterol 3-O- b-D-glucopyranoside, and strictosamide (12) as the major compound. The structures of the isolated compounds were elucidated by detailed spectroscopic analysis and by comparison with published data. No 13C NMR data for 2 and 3 exist in the literature and compounds 2, 3, 5, 7, and 12 are reported for the first time from the genus Mitragyna. The crude extract and isolated compounds were tested in vitro for their preliminary cytotoxicity against brine shrimps (Artemia salina).

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