Synthesis of 1,2,3,triazole modified analogues of hydrochlorothiazide via click chemistry approach and in-vitro α-glucosidase enzyme inhibition studies

2021 ◽  
Author(s):  
Hina Siddiqui ◽  
M. A. A. Baheej ◽  
Saeed Ullah ◽  
Fazila Rizvi ◽  
Shazia Iqbal ◽  
...  
Keyword(s):  
Click Chemistry ◽  
Enzyme Inhibition ◽  
Inhibition Studies

Mycobacterial DNA GyrB Inhibitors: Ligand Based Pharmacophore Modelling and In Vitro Enzyme Inhibition Studies

2014 ◽  
Vol 14 (17) ◽  
pp. 1990-2005 ◽  
Author(s):  
Shalini Saxena ◽  
Janupally Renuka ◽  
Variam Jeankumar ◽  
Perumal Yogeeswari ◽  
Dharmarajan Sriram
Keyword(s):  
Enzyme Inhibition ◽  
Pharmacophore Modelling ◽  
Inhibition Studies

scholarly journals Phytochemical Composition and Enzyme Inhibition Studies of Buxus papillosa C.K. Schneid

Processes ◽  
2020 ◽  
Vol 8 (7) ◽  
pp. 757
Author(s):  
Hammad Saleem ◽  
Thet Thet Htar ◽  
Rakesh Naidu ◽  
Gokhan Zengin ◽  
Marcello Locatelli ◽  
...  
Keyword(s):  
Enzyme Inhibition ◽  
Skin Diseases ◽  
Research Work ◽  
Tentative Identification ◽  
Chemical Profiling ◽  
Phytochemical Composition ◽  
In Vitro Bioassays ◽  
Inhibition Studies ◽  
Wide Usage

The current research work is an endeavor to study the chemical profiling and enzyme-inhibition potential of different polarity solvent (n-hexane, dichloromethane—DCM and methanol—MeOH) extracts from the aerial and stem parts of Buxus papillosa C.K. Schneid. All the extracts were analyzed for HPLC-PDA phenolic quantification, while both (aerial and stem) DCM extracts were studied for UHPLC-MS phytochemical composition. The inhibitory activity against the clinically important enzymes having crucial role in different pathologies like skin diseases (tyrosinase), inflammatory problems (lipoxygenase—LOX) and diabetes mellitus (α-amylase) were studied using standard in vitro bioassays. The DCM extracts upon UHPLC-MS analysis conducted in both negative and positive ionization modes has led to the tentative identification of 52 important secondary metabolites. Most of these belonged to the alkaloid, flavonoid, phenolic and triterpenoid classes. The HPLC-PDA polyphenolic quantification identified the presence of 10 phenolic compounds. Catechin was present in significant amounts in aerial-MeOH (7.62 ± 0.45 μg/g extract) and aerial-DCM (2.39 ± 0.51-μg/g extract) extracts. Similarly, higher amounts of epicatechin (2.76 ± 0.32-μg/g extract) and p-hydroxybenzoic acid (1.06 ± 0.21 μg/g extract) were quantified in aerial-DCM and stem-MeOH extracts, respectively. Likewise, all the extracts exhibited moderate inhibition against all the tested enzymes. These findings explain the wide usage of this plant in folklore medicine and suggest that it could be further studied as an origin of novel bioactive phytocompounds and for the designing of new pharmaceuticals.

404 ‘In vitro’ enzyme inhibition studies with some imides related to aminoglutethimide

1983 ◽  
Vol 19 ◽  
pp. 135
Author(s):  
M.J. Daly ◽  
P.J. Nicholls ◽  
H.J. Smith ◽  
M.G. Rowlands ◽  
M.A. Bunnett
Keyword(s):  
Enzyme Inhibition ◽  
Inhibition Studies

scholarly journals Antidiabetic and In Vitro Enzyme Inhibition Studies of Methanol Extract of Ocimum tenuiflorum Linn Leaves and Its Fractions

2020 ◽  
Vol 31 (1) ◽  
pp. 141-158
Author(s):  
Leila Mousavi ◽  
◽  
Rabeta Mohd Salleh ◽  
Vikneswaran Murugaiyah ◽  
◽  
...  
Keyword(s):  
Enzyme Inhibition ◽  
Methanol Extract ◽  
Ocimum Tenuiflorum ◽  
Inhibition Studies

scholarly journals Anti-glycation and antioxidant properties of Abutilon indicum plant leaves

2021 ◽  
Vol 3 (1) ◽  
pp. 001-005
Author(s):  
Dinesha Ramadas ◽  
Santhosh Kumar Nune ◽  
Chikkanna D ◽  
Maheshwara KV ◽  
Vedamurthy Joshi
Keyword(s):  
Glucose Uptake ◽  
Enzyme Inhibition ◽  
Antioxidant Properties ◽  
Yeast Cells ◽  
Alpha Amylase ◽  
Phytochemical Analysis ◽  
Plant Leaves ◽  
Inhibition Studies ◽  
Abutilon Indicum

The study was done to investigate the in vitro anti-diabetic activity of Ethanol-water extract of Abutilon indicum plant leaves. The phytochemicals present in the extract was analyzed by using standard methods. In vitro antioxidant study was done using DPPH radical scavenging activity. The In vitro anti-diabetic studies were done by alpha amylase enzyme, alpha glucosidases enzyme inhibition studies and Glucose uptake in Yeast cells studies. The phytochemical analysis showed that the extract rich with proteins, polyphenols, flavonoids, alkaloids, tannins, polysaccharides. The in vitro antiglycation potential of extract was confirmed through alpha amylase enzyme, alpha glucosidases enzyme inhibition studies and Glucose uptake in Yeast cells studies. The results of the present study showed the significant antioxidant and antidiabetic activity. The potential pharmacological activity of Abutilon indicum might be the presence of phytochemicals.

scholarly journals Anti-glycation and antioxidant properties of Abutilon indicum plant leaves

2021 ◽  
Vol 2 (2) ◽  
pp. 269-273
Author(s):  
Dinesha Ramadas ◽  
Santhosh Kumar Nune ◽  
Chikkanna D ◽  
Maheshwara KV ◽  
Vedamurthy Joshi
Keyword(s):  
Glucose Uptake ◽  
Enzyme Inhibition ◽  
Antioxidant Properties ◽  
Yeast Cells ◽  
Alpha Amylase ◽  
Phytochemical Analysis ◽  
Plant Leaves ◽  
Inhibition Studies ◽  
Abutilon Indicum

The study was done to investigate the in vitro anti-diabetic activity of Ethanol-water extract of Abutilon indicum plant leaves. The phytochemicals present in the extract was analyzed by using standard methods. In vitro antioxidant study was done using DPPH radical scavenging activity. The In vitro anti-diabetic studies were done by alpha amylase enzyme, alpha glucosidases enzyme inhibition studies and Glucose uptake in Yeast cells studies. The phytochemical analysis showed that the extract rich with proteins, polyphenols, flavonoids, alkaloids, tannins, polysaccharides. The in vitro antiglycation potential of extract was confirmed through alpha amylase enzyme, alpha glucosidases enzyme inhibition studies and Glucose uptake in Yeast cells studies. The results of the present study showed the significant antioxidant and antidiabetic activity. The potential pharmacological activity of Abutilon indicum might be the presence of phytochemicals.

Evaluation of Snake Venom’s PhospholipaseA2 Enzyme Inhibition Activity of Cyphostemma adenocoule

2020 ◽  
Vol 14 (3) ◽  
pp. 196-202
Author(s):  
Atul Kaushik ◽  
Teamrat S. Tesfai ◽  
Daniel K. Barkh ◽  
Furtuna K. Ghebremeskel ◽  
Habtom G. Zerihun ◽  
...  
Keyword(s):  
Enzyme Inhibition ◽  
Snake Venom ◽  
Ethanol Extract ◽  
Egg Yolk ◽  
Chloroform Extract ◽  
Inhibition Activity ◽  
Traditional Use ◽  
Snake Bites ◽  
Ethanol Extracts

Background: A snake bite is fundamentally an injury often resulting in puncture wounds meted out by the animal's fangs and occasionally resulting in envenomation. Rate of snake bites around 5,400,000 bites per year leads to over 2,500,000 envenomings and around 125,000 fatal cases annually. Snake venom enzymes are rich in metalloproteinases, phospholipaseA2, proteinases, acetylcholinesterases and hyaluronidases. Objective: Cyphostemma adenocoule is traditionally being used for the treatment of snake bites in Eritrea. The present research was aimed at evaluating the snake venom enzyme inhibition activity of C. adenocoule against puff adder venom and developing a base for the traditional use of the plant against snakebites in Eritrea. Methods: The anti-venom activity of C. adenocoule was assessed in-vitro through phospholipaseA2 enzyme inhibition assay using egg yolk as a cell. The ethanol and chloroform extracts of C. adenocoule showed in vitro anti phospholipase A2 activity, whereas the water extracts of the plant showed no activity. Results: Among the extracts of C. adenocoule, the highest percentage of inhibition was obtained from chloroform extract (95.55% at 100mg/ml). The extract showed prominent activity at different concentrations (34.7% at10mg/ml, 48.8% at 20mg/ml, 54.8% at 40mg/ml, 60.9% at 60mg/ml, 80.5% at 80mg /ml). The ethanol extract also showed certain activity at various concentrations (25.22% at10mg/ml, 14.78% at 20mg/ml, 2.6% at40mg/ml). The activity of the chloroform extracts increases as concentration increases, whereas the activity of the ethanol extracts decreases as concentration increases. The aqueous extract of C. adenocoule did not show any activity at all concentrations. Conclusion: In this study, the chloroform and ethanol extracts of the plant inhibited the enzyme of interest and thus proved the efficacy of anti-snake venom activity of the plant.

Coumaronochromone as antibacterial and carbonic anhydrase inhibitors from Aerva persica (Burm.f.) Merr.: experimental and first-principles approaches

2020 ◽  
Vol 0 (0) ◽  
Author(s):  
Muhammad Imran ◽  
Ahmad Irfan ◽  
Mohammed A. Assiri ◽  
Sajjad H. Sumrra ◽  
Muhammad Saleem ◽  
...  
Keyword(s):  
Carbonic Anhydrase ◽  
First Principles ◽  
Molecular Electrostatic Potential ◽  
Chemical Constituents ◽  
Bacterial Strains ◽  
Hirshfeld Analysis ◽  
Carbonic Anhydrase Inhibition ◽  
Inhibition Studies ◽  
Lowest Unoccupied Molecular Orbitals

AbstractThe Aerva plants are exceptionally rich in phytochemicals and possess therapeutics potential. Phytochemical screening shows that Aerva persica (Burm.f.) Merr. contains highest contents i.e., total phenolics, flavonoids, flavonols, tannins, alkaloids, carbohydrates, anthraquinones and glycosides. In-vitro antibacterial and enzymatic (carbonic anhydrase) inhibition studies on methanol extracts of A. persica indicated the presence of biological active constituents within chloroform soluble portions. Investigation in the pure constituents on the chloroform portions of A. persica accomplished by column chromatography, NMR and MS analysis. The bioguided isolation yields four chemical constituents of coumaronochromone family, namely aervin (1-4). These pure chemical entities (1-4) showed significant antibacterial activity in the range of 60.05–79.21 µg/ml against various bacterial strains using ampicillin and ciprofloxacin as standard drugs. The compounds 1-4 showed promising carbonic anhydrase inhibition with IC50 values of 19.01, 18.24, 18.65 and 12.92 µM, respectively, using standard inhibitor acetazolamide. First-principles calculations revealed comprehensive intramolecular charge transfer in the studied compounds 1-4. The spatial distribution of highest occupied and lowest unoccupied molecular orbitals, ionization potential, molecular electrostatic potential and Hirshfeld analysis revealed that these coumaronochromone compounds would be proficient biological active compounds. These pure constituents may be used as a new pharmacophore to treat leaukomia, epilepsy, glaucoma and cystic fibrosis.

scholarly journals The Physical Adsorption of Gelatinized Starch with Tannic Acid Decreases the Inhibitory Activity of the Polyphenol against α-Amylase

Foods ◽  
2021 ◽  
Vol 10 (6) ◽  
pp. 1233
Author(s):  
Yueyi Wang ◽  
Shuangshuang Li ◽  
Fangting Bai ◽  
Junwei Cao ◽  
Lijun Sun
Keyword(s):  
Enzyme Inhibition ◽  
Tannic Acid ◽  
Inhibitory Activity ◽  
Adsorption Property ◽  
Physical Adsorption ◽  
Enzyme Active Site ◽  
Opposite Trend ◽  
Gelatinized Starch ◽  
The Difference

The effects of mixing orders of tannic acid (TA), starch, and α-amylase on the enzyme inhibition of TA were studied, including mixing TA with α-amylase before starch addition (order 1), mixing TA with pre-gelatinized starch before α-amylase addition (order 2) and co-gelatinizing TA with starch before α-amylase addition (order 3). It was found that the enzyme inhibition was always highest for order 1 because TA could bind with the enzyme active site thoroughly before digestion occurred. Both order 2 and 3 reduced α-amylase inhibition through decreasing binding of TA with the enzyme, which resulted from the non-covalent physical adsorption of TA with gelatinized starch. Interestingly, at low TA concentration, α-amylase inhibition for order 2 was higher than order 3, while at high TA concentration, the inhibition was shown with the opposite trend, which arose from the difference in the adsorption property between the pre-gelatinized and co-gelatinized starch at the corresponding TA concentrations. Moreover, both the crystalline structures and apparent morphology of starch were not significantly altered by TA addition for order 2 and 3. Conclusively, although a polyphenol has an acceptable inhibitory activity in vitro, the actual effect may not reach the expected one when taking processing procedures into account.

scholarly journals Alkynyl N-BODIPYs as Reactive Intermediates for the Development of Dyes for Biophotonics

2020 ◽  
Vol 3 (1) ◽  
pp. 15
Author(s):  
César Ray ◽  
Andrés García-Sampedro ◽  
Christopher Schad ◽  
Edurne Avellanal-Zaballa ◽  
Florencio Moreno ◽  
...  
Keyword(s):  
Pancreatic Cancer ◽  
Photodynamic Therapy ◽  
Click Chemistry ◽  
Cancer Cells ◽  
Reactive Intermediates ◽  
New Approach ◽  
Pancreatic Cancer Cells ◽  
Bio Imaging

A new approach for the rapid multi-functionalization of BODIPY dyes towards biophotonics is reported. It is based on novel N-BODIPYs, through reactive intermediates with alkynyl groups to be further derivatized by click chemistry. This approach has been exemplified by the development of new dyes for cell bio-imaging, which have proven to successfully internalize into pancreatic cancer cells and accumulate in the mitochondria. The in vitro suitability for photodynamic therapy (PDT) was also analyzed and confirmed our compounds to be promising PDT candidates for the treatment of pancreatic cancer.

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