Neuroprotectıve Potential of the Tubers of Corydalis triternata Zucc. Growing in Turkey

2020 ◽  
Vol 42 (4) ◽  
pp. 515-515
Author(s):  
Mehtap K l c Mehtap K l c ◽  
Erdal Kaya Erdal Kaya ◽  
Ayhan Ibrahim Aysal Ayhan Ibrahim Aysal ◽  
Bilge Sener Bilge Sener
Keyword(s):  
Metabolite Profile ◽  
Positive Control ◽  
Anticholinesterase Activity ◽  
Ex Situ ◽  
In Vitro Tests ◽  
Drug Candidates ◽  
Ic50 Value ◽  
Ic50 Values ◽  
Tof Ms

The continuing research for the determination of bioactive secondary metabolites from Turkish geophytes as therapeutic agents for dementia is mainly based on the need for drug candidates affected to brain areas. In this study, the in vitro anticholinesterase activity of the alkaloidal fractions of the tubers of Corydalis triternata Zucc. was investigated for their neuroprotective potential. Furthermore, the content of the active alkaloid fractions of the tubers was determined by LC-Q-TOF-MS. The tubers of Corydalis triternata Zucc. were collected from Hatay province of Turkey. The plant species were also preserved as ex-situ in Yalova-Turkey. The alkaloidal extract was prepared from the tubers. The anticholinesterase activities of the extracts and fractions were tested by modification of the Ellman’s method. The optimization of LC-MS conditions was used in ESI in the positive ion mode. The in vitro tests were highlighted that the alkaloidal extract of the tubers exhibited the highest activity against AChE and BuChE with IC50 values of 17.56 and#177; 1.0 g/mL and 326.23 and#177; 2.6 g /mL (galanthamine 6.8 and#177; 0.5 g /mL and 344.4 and#177; 8.2 g /mL as positive control), respectively. The fractions CK-3 and 4 were showed the highest inhibitory activity against AChE with the IC50 value (6.88 and#177; 0.3 g mL and 7.26 and#177; 0.3 g /mL), the fractions CK-5,6,7 and 8 have indicated potent inhibitory activities by compared with galanthamine, which was used as positive control with IC50 value 6.8 and#177; 0.5 g /mL. Among the fractions obtained from the alkaloidal extract, protoberberine-type alkaloids were exerted the most promising activity against both cholinesterases. The present study was described for the first time the in vitro anticholinesterase activity of Corydalis triternata Zucc. as neuroprotective potential and their metabolite profile by LC-Q-TOF-MS. Besides, the anticholinesterase assays on alkaloidal extract and its fractions showed that protoberberine-type alkaloids were determined the most potent inhibitor against AChE and BuChE.

scholarly journals Olive Mill Wastewater Polyphenol-Enriched Fractions by Integrated Membrane Process: A Promising Source of Antioxidant, Hypolipidemic and Hypoglycaemic Compounds

Antioxidants ◽  
2020 ◽  
Vol 9 (7) ◽  
pp. 602 ◽  
Author(s):  
Rosa Tundis ◽  
Carmela Conidi ◽  
Monica R. Loizzo ◽  
Vincenzo Sicari ◽  
Alfredo Cassano
Keyword(s):  
High Performance ◽  
Olive Mill Wastewater ◽  
In Vitro Tests ◽  
Ic50 Value ◽  
Bleaching Test ◽  
Ic50 Values ◽  
Olive Waste ◽  
Promising Source ◽  
Olive Mill

The valorisation of food wastes is a challenging opportunity for the green, sustainable, and competitive development of industry. The recovery of phenols contributes to the sustainability of olive waste sector, reducing its environmental impact and promoting the development of innovative formulations of interest for pharmaceutical, nutraceutical, and cosmeceutical applications. In this work, olive mill wastewater was treated through a combination of microfiltration (MF), nanofiltration (NF), and reverse osmosis (RO) in a sequential design to produce polyphenol-enriched fractions that have been investigated for their chemical profile using ultra-high-performance liquid chromatography (UHPLC), and their potential antioxidant, hypolipidemic, and hypoglycaemic activities. RO retentate exhibited the highest content of hydroxytyrosol, tyrosol, oleuropein, verbascoside, vanillic acid, and luteolin. In particular, a content of hydroxytyrosol of 1522.2 mg/L, about five times higher than the MF feed, was found. RO retentate was the most active extract in all in vitro tests. Interestingly, this fraction showed a 2,2′-azino-bis(3-ethylbenzothiazoline-6-sulfonic) acid (ABTS) radicals scavenging activity with an IC50 value of 6.9 μg/mL and a potential inhibition of lipid peroxidation evaluated by the β-carotene bleaching test with IC50 values of 25.1 μg/mL after 30 min of incubation. Moreover, RO retentate inhibited α-amylase and α-glucosidase with IC50 values of 65.3 and 66.2 μg/mL, respectively.

scholarly journals Bioguided Isolation of Cyclopenin Analogues as Potential SARS-CoV-2 Mpro Inhibitors from Penicillium citrinum TDPEF34

Biomolecules ◽  
2021 ◽  
Vol 11 (9) ◽  
pp. 1366
Author(s):  
Bathini Thissera ◽  
Ahmed M. Sayed ◽  
Marwa H. A. Hassan ◽  
Sayed F. Abdelwahab ◽  
Ngozi Amaeze ◽  
...  
Keyword(s):  
Hydrophobic Interactions ◽  
Structural Information ◽  
Positive Control ◽  
Penicillium Citrinum ◽  
Moderate Activity ◽  
Enzyme Active Site ◽  
Drug Candidates ◽  
Ic50 Values

SARS-CoV-2 virus mutations might increase its virulence, and thus the severity and duration of the ongoing pandemic. Global drug discovery campaigns have successfully developed several vaccines to reduce the number of infections by the virus. However, finding a small molecule pharmaceutical that is effective in inhibiting SARS-CoV-2 remains a challenge. Natural products are the origin of many currently used pharmaceuticals and, for this reason, a library of in-house fungal extracts were screened to assess their potential to inhibit the main viral protease Mpro in vitro. The extract of Penicillium citrinum, TDPEF34, showed potential inhibition and was further analysed to identify potential Mpro inhibitors. Following bio-guided isolation, a series of benzodiazepine alkaloids cyclopenins with good-to-moderate activity against SARS-CoV-2 Mpro were identified. The mode of enzyme inhibition of these compounds was predicted by docking and molecular dynamic simulation. Compounds 1 (isolated as two conformers of S- and R-isomers), 2, and 4 were found to have promising in vitro inhibitory activity towards Mpro, with an IC50 values range of 0.36–0.89 µM comparable to the positive control GC376. The in silico investigation revealed compounds to achieve stable binding with the enzyme active site through multiple H-bonding and hydrophobic interactions. Additionally, the isolated compounds showed very good drug-likeness and ADMET properties. Our findings could be utilized in further in vitro and in vivo investigations to produce anti-SARS-CoV-2 drug candidates. These findings also provide critical structural information that could be used in the future for designing potent Mpro inhibitors.

scholarly journals Evaluation of the Antileishmanial Properties of Ixora brachiata Roxb on Leishmania major and Leishmania infantum by Colorimetric MTT Assay

2019 ◽  
Vol 7 (4) ◽  
pp. 126-129
Author(s):  
Kaveh Eskandari ◽  
Shahram Khademvatan ◽  
Batool Sadeghi Nejad ◽  
Sedigheh Yusef Naanaie ◽  
Kobra kohansal
Keyword(s):  
Leishmania Infantum ◽  
Leishmania Major ◽  
Positive Control ◽  
Root Extract ◽  
Diphenyltetrazolium Bromide ◽  
Ic50 Value ◽  
Ic50 Values ◽  
Parasitic Activity ◽  
Different Doses

Background: Leishmaniasis is a major global health problem which affects millions of people, especially in the developing countries. The incidence of leishmaniasis has increased and there is no vaccination for Leishmania infections and standard drugs for treatment of the disease have many side effects; therefore, it is necessary to find new effective alternatives. Objectives: The purpose of this study was to evaluate the in vitro antileishmanial activity of Ixora brachiata root extract against Leishmania major and Leishmania infantum promastigotes. Materials and Methods: Different doses of the selected plant extract was tested against L. major and L. infantum promastigotes using colorimetric MTT [3-(4, 5-methylthiazol-2-yl)-2, 5-diphenyltetrazolium bromide] assay. Glucantime was used as the positive control. Results: Anti-parasitic activity was revealed for I. brachiata root on L. major and L. infantum with 50% inhibitory concentration (IC50) values of 0.91 and 2.63 µg/mL, respectively compared to the standard drugs, glucantime, which had an IC50 value of 40.2 µg/mL for L. major and 18.5 µg/ mL for L. infantum after 72 hours. Conclusion: The results of this study created a new background on the development of drug against leishmania parasite.

Inhibition of Protein Tyrosine Phosphatase 1B by Lutein Derivatives isolated from Mexican Oregano (Lippia graveolens)

2018 ◽  
Vol 17 (3) ◽  
pp. 134-139
Author(s):  
R.M. Perez-Gutierrez
Keyword(s):  
Protein Tyrosine Phosphatase ◽  
Inhibitory Activity ◽  
Spectroscopic Data ◽  
Methanol Extract ◽  
Tyrosine Phosphatase ◽  
Positive Control ◽  
Protein Tyrosine Phosphatase 1B ◽  
Protein Tyrosine ◽  
Ic50 Value ◽  
Ic50 Values

Methanol extract from Lippia graveolens (Mexican oregano) was studied in order to identify inhibitory bioactives for protein tyrosine phosphatase 1B (PTP1B). Known flavone as lutein (1), and another flavone glycoside such as lutein-7-o-glucoside (2), 6-hydroxy-lutein-7-ohexoside (3) and lutein-7-o-ramnoide (4) were isolated from methanol extract of aerial parts of the Lippia graveolens. All isolates were identified based on extensive spectroscopic data analysis, including UV, IR, NMR, MS and compared with spectroscopic data previously reported. These flavones were evaluated for PTP1B inhibitory activity. Among them, compounds 1 and 3 displayed potential inhibitory activity against PTP1B with IC50 values of 7.01 ± 1.25 μg/ml and 18.4 μg/ml, respectively. In addition, compound 2 and 4 showed moderate inhibitory activity with an IC50 value of 23.8 ± 6.21 and 67.8 ± 5.80 μg/ml respectively. Among the four compounds, luteolin was found to be the most potent PTP1B inhibitor compared to the positive control ursolic acid, with an IC50 value of 8.12 ± 1.06 μg/ml. These results indicate that flavonoids constituents contained in Lippia graveolens can be considered as a natural source for the treatment of type 2 diabetes.

Synthesis and Structure−Activity Relationship Studies of N-monosubstituted Aroylthioureas as Urease Inhibitors

2020 ◽  
Vol 16 ◽  
Author(s):  
Wei-Wei Ni ◽  
Hai-Lian Fang ◽  
Ya-Xi Ye ◽  
Wei-Yi Li ◽  
Li Liu ◽  
...  
Keyword(s):  
Regression Analysis ◽  
Mammalian Cells ◽  
Intact Cell ◽  
Linear Regression Analysis ◽  
Positive Control ◽  
Acetohydroxamic Acid ◽  
Urease Inhibitors ◽  
Ic50 Value ◽  
Ic50 Values ◽  
Low Cytotoxicity

Background: Thiourea is a classical urease inhibitor usually as a positive control, and many N,N`-disubstituted thioureas have been determined as urease inhibitors. However, due to steric hindrance, N,N`-disubstituted thiourea motif could not bind urease as thiourea. On the contrary, N-monosubstituted thioureas with a tiny thiourea motif could theoretically bind into the active pocket as thiourea. Objective: A series of N-monosubstituted aroylthioureas were designed and synthesized for evaluation as urease inhibitors. Methods: Urease inhibition was determined by the indophenol method and IC50 values were calculated using computerized linear regression analysis of quantal log dose-probit functions. The kinetic parameters were estimated viasurface plasmon resonance (SPR) and by nonlinear regression analysis based on the mixed type inhibition model derived from Michaelis-Menten kinetics. Results: Compounds b2, b11and b19 reversibly inhibited urease with a mixed mechanism, and showed excellent potency against both cell-free urease and urease in intact cell, with IC50 values being 90-to 450-fold and 5-to 50-fold lower than the positive control acetohydroxamic acid, respectively. The most potent compound b11 showed IC50 value of 0.060 ±0.004μM against cell-free urease, which bound to urea binding site with a very low KDvalue (0.420±0.003nM) and a very long residence time (6.7 min). Compound b11was also demonstrated having very low cytotoxicity to mammalian cells. Conclusion: These results revealed that N-monosubstituted aroylthioureas clearly bind the active site of urease as expected, and represent a new class of urease inhibitors for the development of potential therapeutics against infections caused by ure-ase-containing pathogens.

scholarly journals The Repurposed Drugs Suramin and Quinacrine Cooperatively Inhibit SARS-CoV-2 3CLpro In Vitro

Viruses ◽  
2021 ◽  
Vol 13 (5) ◽  
pp. 873
Author(s):  
Raphael J. Eberle ◽  
Danilo S. Olivier ◽  
Marcos S. Amaral ◽  
Ian Gering ◽  
Dieter Willbold ◽  
...  
Keyword(s):  
Binding Mode ◽  
Drug Candidates ◽  
Main Protease ◽  
Ic50 Values ◽  
Repurposed Drugs ◽  
Antiparasitic Drugs ◽  
Inhibitory Potential ◽  
Dynamics Simulations ◽  
Micromolar Range

Since the first report of a new pneumonia disease in December 2019 (Wuhan, China) the WHO reported more than 148 million confirmed cases and 3.1 million losses globally up to now. The causative agent of COVID-19 (SARS-CoV-2) has spread worldwide, resulting in a pandemic of unprecedented magnitude. To date, several clinically safe and efficient vaccines (e.g., Pfizer-BioNTech, Moderna, Johnson & Johnson, and AstraZeneca COVID-19 vaccines) as well as drugs for emergency use have been approved. However, increasing numbers of SARS-Cov-2 variants make it imminent to identify an alternative way to treat SARS-CoV-2 infections. A well-known strategy to identify molecules with inhibitory potential against SARS-CoV-2 proteins is repurposing clinically developed drugs, e.g., antiparasitic drugs. The results described in this study demonstrated the inhibitory potential of quinacrine and suramin against SARS-CoV-2 main protease (3CLpro). Quinacrine and suramin molecules presented a competitive and noncompetitive inhibition mode, respectively, with IC50 values in the low micromolar range. Surface plasmon resonance (SPR) experiments demonstrated that quinacrine and suramin alone possessed a moderate or weak affinity with SARS-CoV-2 3CLpro but suramin binding increased quinacrine interaction by around a factor of eight. Using docking and molecular dynamics simulations, we identified a possible binding mode and the amino acids involved in these interactions. Our results suggested that suramin, in combination with quinacrine, showed promising synergistic efficacy to inhibit SARS-CoV-2 3CLpro. We suppose that the identification of effective, synergistic drug combinations could lead to the design of better treatments for the COVID-19 disease and repurposable drug candidates offer fast therapeutic breakthroughs, mainly in a pandemic moment.

scholarly journals Control of bovine tick [Rhipicephalus (Boophilus) microplus] with Brunfelsia uniflora leaf extract

2019 ◽  
pp. 903-910
Author(s):  
Elaine Yae Yamashita Sugauara ◽  
ElisângelaYumi Sugauara ◽  
Rosangela Rumi Sugauara ◽  
Wanessa de Campos Bortolucci ◽  
Herika Line Marko de Oliveira ◽  
...  
Keyword(s):  
Ethyl Ester ◽  
Leaf Extract ◽  
Acid Ethyl Ester ◽  
Acaricidal Activity ◽  
Boophilus Microplus ◽  
Ex Situ ◽  
In Vitro Tests ◽  
Free Living ◽  
Crude Leaf Extract

Bovine tick has caused losses in livestock production profitability in Brazil. However, tick control has caused resistance of these ectoparasites against utilized acaricides. Alternative tick controls have been utilizing plants as sources of effective botanical acaricides. Brunfelsia uniflora is a Brazilian plant with antimicrobial and antioxidant activity; however, there are no reports on its acaricidal activity. Therefore, this study aimed to evaluate the chemical composition of B. uniflora leaf ethanolic extract and its efficiency to control bovine tick in vitro and free-living stage ex situ. The crude leaf extract was analyzed by gas chromatographer coupled to mass spectrometer (GC-MS) with identification of 17 compounds. The major compounds were phytol (22.96%), 9,12,15-octadecatrienoic acid, ethyl ester (Z,Z,Z) (21.18%), hexadecanoic acid, ethyl ester (12.74%) and vitamin E (8.77%). The crude extract presented acaricidal activity in vitro against ingurgitated adult females, larvae and eggs of bovine tick. The LC99.9 for larvae was 103.21 mg mL-1 in in vitro tests and was 100% efficient for ex situ larva test (free-living stage). B. uniflora leaf extract is an alternative for the control of the bovine tick cycle, mainly in the free-living stage (non-parasitic stage) under field conditions.

scholarly journals Antibacterial Effect of Silver Nanoparticles on Klebsiella spp

2020 ◽  
Vol 1 (2) ◽  
pp. 8-15
Author(s):  
Gislanne Stéphanne Estevam da Silva ◽  
Rivaldo Leon Bezerra Cabral ◽  
Nathalie de Sena Pereira ◽  
José Heriberto Oliveira do Nascimento ◽  
Dany G kramer
Keyword(s):  
Silver Nanoparticles ◽  
Bacterial Resistance ◽  
Brain Heart Infusion ◽  
Trisodium Citrate ◽  
Antimicrobial Activities ◽  
Positive Control ◽  
Negative Control ◽  
In Vitro Tests ◽  
Klebsiella Spp

Silver nanoparticles (AgNP) can be incorporated into medical devices, such as tissues, to circumvent bacterial resistance such as Klebsiella spp, which can lead to skin and mucosal infections. Thus, the aim of the present study was to synthesize silver nanoparticles for later incorporation into cotton fabrics and in vitro tests against Klebsiella spp. The AgNP colloidal solution was synthesized (AgNO3 - 0.1 mM, 100 mM trisodium citrate, polyvinylpyrrolidone - 0.24 g, H2OH2) and then impregnated into the cotton fabric pretreated with poly diallyl dimethylammonium chloride (PDDA) of 100/500 tissue, shaken for 30 minutes). The material produced was analyzed by the FTIR; DLS and reflectance spectroscopy. The tests of the antimicrobial activities were by the microdilution technique against Klebsiella spp, in tubes containing Brain Heart Infusion (BHI), with the solution of silver (1); Tissue containing AgNP - 4 mm (2); Negative control (3) and positive control - ceftriaxone (4). Regarding MIC, the inhibitory activity occurred of the dilutions between 1/2 and 1/16. The AgNP particles had an average size of 24.75 nm. As synthesized AgNPs demonstrate the excellent antimicrobial activity against Klebsiella spp, with special emphasis on applications in nanotechnology and nanomedicine, targeting multiresistant antibiotic bacteria.

scholarly journals Study on α-glucosidase inhibitory activity of 40 kinds of vegetables, tubers, and fruits in An Giang

2021 ◽  
Vol 63 (4) ◽  
pp. 42-46
Author(s):  
Thi-My-Linh Lam ◽  
◽  
Minh-Tuan Le ◽  
Manh-Ha Bui ◽  
◽  
...  
Keyword(s):  
Glycine Max ◽  
Inhibitory Activity ◽  
Positive Control ◽  
Syzygium Cumini ◽  
Inhibition Rate ◽  
Ic50 Value ◽  
Areca Catechu ◽  
Ic50 Values

A study on the α-glucosidase inhibitory activity of 40 kinds of vegetables, tubers, and fruits found in the An Giang province was conducted. The results indicated that all 40 extracted samples displayed α-glucosidase inhibitory activity at a concentration of 250 μg ml-1, 36 extracted samples showed an inhibition rate greater than 50% at 250 μg ml-1, 25 extracted samples had over 50% at 100 μg ml-1, 17 extracted samples possessed more than 50% at 50 μg ml-1, 7 extracted samples sampled showed over 50% at 25 μg ml-1, 5 extracted samples were greater than 50% at 10 μg ml-1, and 1 extracted sample was greater than 50% at 1 μg ml-1. Among the 40 samples, those taken from the seeds of Areca catechu, the fruits of Cassia grandis, the fruits of Syzygium cumini, the seeds of Glycine max,andthe stems of Enydra fluctuansexhibited the strongest α-glucosidase inhibitory activity in methanol, with IC50 values of 0.15, 2.54, 4.05, 5.17 and 8.68 μg ml-1, respectively, which were stronger than the positive control acarbose with an IC50 value of 214.5 μg ml-1

scholarly journals Differential Interactome Based Drug Repositioning Unraveled Abacavir, Exemestane, Nortriptyline Hydrochloride, and Tolcapone as Potential Therapeutics for Colorectal Cancers

2021 ◽  
Vol 1 ◽  
Author(s):  
Hande Beklen ◽  
Sema Arslan ◽  
Gizem Gulfidan ◽  
Beste Turanli ◽  
Pemra Ozbek ◽  
...  
Keyword(s):  
Drug Repositioning ◽  
Positive Control ◽  
Drug Candidates ◽  
Novel Biomarkers ◽  
Critical Requirement ◽  
Nortriptyline Hydrochloride ◽  
In Silico Molecular Docking ◽  
Prognostic Power ◽  
Potential Therapeutics

There is a critical requirement for alternative strategies to provide the better treatment in colorectal cancer (CRC). Hence, our goal was to propose novel biomarkers as well as drug candidates for its treatment through differential interactome based drug repositioning. Differentially interacting proteins and their modules were identified, and their prognostic power were estimated through survival analyses. Drug repositioning was carried out for significant target proteins, and candidate drugs were analyzed via in silico molecular docking prior to in vitro cell viability assays in CRC cell lines. Six modules (mAPEX1, mCCT7, mHSD17B10, mMYC, mPSMB5, mRAN) were highlighted considering their prognostic performance. Drug repositioning resulted in eight drugs (abacavir, ribociclib, exemestane, voriconazole, nortriptyline hydrochloride, theophylline, bromocriptine mesylate, and tolcapone). Moreover, significant in vitro inhibition profiles were obtained in abacavir, nortriptyline hydrochloride, exemestane, tolcapone, and theophylline (positive control). Our findings may provide new and complementary strategies for the treatment of CRC.

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