scholarly journals IN VITRO STUDIES ON THE ANTIDIABETIC ACTIVITY OF 2-THIOHYDANTOIN USING α-amylase AND α-GLUCOSIDASE

2019 ◽  
pp. 155-157 ◽  
Author(s):  
UMA S ◽  
DEVIKA PT
Keyword(s):  
Therapeutic Approach ◽  
Enzyme Assay ◽  
Inhibitory Concentration ◽  
Glucose Production ◽  
Inhibitory Effect ◽  
In Vitro Studies ◽  
Antidiabetic Activity

Objective: The aim of the present study was to investigate the inhibitory effect of 2-thiohydantoin on the enzymes α-amylase and α-glucosidase in vitro as an antidiabetic therapeutic approach to reduce gastrointestinal glucose production. Methods: Antidiabetic activity of the compound, 2-thiohydantoin was measured using the enzymes α-amylase and α-glucosidase. Results: Half-maximal inhibitory concentration of the antidiabetic α-amylase was found to be 410.35 μg/ml and α-glucosidase was found to be 356.33 μg/ml, respectively. Conclusion: The result obtained in the in vitro enzyme assay suggests the antidiabetic activity of 2-thiohydantoin.

scholarly journals In-Vitro Antidiabetic Effect of Ziziphus mucronata Leave Extracts

2021 ◽  
Vol 11 (6-S) ◽  
pp. 9-13
Author(s):  
Olaitan Kabir Abolaji ◽  
A.N. Ukwuani-Kwaja ◽  
I Sani ◽  
M.N. Sylvester
Keyword(s):  
Glucose Production ◽  
Inhibitory Effect ◽  
Alpha Amylase ◽  
Antidiabetic Activity ◽  
Anthraquinone Glycosides ◽  
Enzymes Inhibition ◽  
Ziziphus Mucronata ◽  
Dose Dependent Increase ◽  
Dose Dependent

Background: Diabetes is a metabolic disorder characterized by hyperglycemia due to the body’s inability to produce insulin or inaction of the produced insulin or a combination of both. One antidiabetic therapeutic approach is to reduce gastrointestinal glucose production and absorption through the inhibition of carbohydrate digesting enzymes such as alpha-amylase as well as through the inhibition of hemoglobin glycosylation. Objective: This study sets out to evaluate the in vitro antidiabetic activity of Ziziphus mucronata extracts for their effect on alpha-amylase and glycosylation of hemoglobin. Methods: Successive gradient maceration of Z. mucronata leaves were carried out using Hexane, Acetone, Methanol and separately with water to obtain four (4) extracts labelled HE, AE, ME, and WE respectively. These were subjected to in vitro studies for their inhibitory effect on alpha-amylase and hemoglobin glycosylation, Standard laboratory methods were used to screen for phytochemicals of the most potent extract. Results: The result showed that AE, ME and WE extract exhibited a dose-dependent increase in percentage inhibition of both alpha-amylase and hemoglobin glycosylation. However, on a stricking note, the AE showed a more potent data result with percentage (%) potency of 71.02 at 1mg/ml, the lowest glucose concentration (of 25mg/ml) at 0.242nm as well as the highest hemoglobin glycosylation inhibitory mean concentration of 3.663nm after 72 hours. The AE of Z. mucronata (the most potent) revealed the presence of alkaloids, anthraquinone, glycosides, flavonoids, phenols, saponin, tanins and terpenoids. Conclusion: Thus, the Acetone extract is more likely to give a lead antidiabetic drug molecule of drug when further explored; which somewhat justify the folkloric claims of Z. mucronata leave as an antidiabetic. Keywords: Heamoglabin glycosylation, Alpha-amylase enzymes, Inhibition, Glucose.

scholarly journals In Vitro Effects of Doxycycline on Replication of Feline Coronavirus

Pathogens ◽  
2021 ◽  
Vol 10 (3) ◽  
pp. 312
Author(s):  
Magdalena Dunowska ◽  
Sayani Ghosh
Keyword(s):  
Inhibitory Concentration ◽  
Infectious Virus ◽  
Treatment Options ◽  
Inhibitory Effect ◽  
Virus Titration ◽  
Reverse Transcription Quantitative Pcr ◽  
In Vitro Effects ◽  
Dose Dependent ◽  
Feline Coronavirus

Feline infectious peritonitis (FIP) is a sporadic fatal disease of cats caused by a virulent variant of feline coronavirus (FCoV), referred to as FIP virus (FIPV). Treatment options are limited, and most of the affected cats die or are euthanized. Anecdotally, doxycycline has been used to treat FIP-affected cats, but there are currently no data to support or discourage such treatment. The aim of this study was to establish whether doxycycline inhibits replication of FIPV in vitro. The virus was cultured in Crandell-Rees feline kidney cells with various concentrations of doxycycline (0 to 50 µg/mL). The level of FIPV in cultures was determined by virus titration and FCoV-specific reverse-transcription quantitative PCR. Cell viability was also monitored. There was no difference in the level of infectious virus or viral RNA between doxycycline-treated and untreated cultures at 3, 12- and 18-hours post-infection. However, at 24 h, the growth of FIPV was inhibited by approximately two logs in cultures with >10 µg/mL doxycycline. This inhibition was dose-dependent, with inhibitory concentration 50% (IC50) 4.1 µg/mL and IC90 5.4 µg/mL. Our data suggest that doxycycline has some inhibitory effect on FIPV replication in vitro, which supports future clinical trials of its use for the treatment of FIP-affected cats.

scholarly journals In Vitro α-Glucosidase and α-Amylase Inhibitory Activities of Free and Bound Phenolic Extracts from the Bran and Kernel Fractions of Five Sorghum Grain Genotypes

Foods ◽  
2020 ◽  
Vol 9 (9) ◽  
pp. 1301
Author(s):  
Yun Xiong ◽  
Ken Ng ◽  
Pangzhen Zhang ◽  
Robyn Dorothy Warner ◽  
Shuibao Shen ◽  
...  
Keyword(s):  
Digestive System ◽  
Inhibitory Concentration ◽  
Inhibitory Effect ◽  
Inhibitory Effects ◽  
Phenolic Contents ◽  
Inhibitory Activities ◽  
Sorghum Grain ◽  
Global Health Challenge ◽  
Phenolic Extracts

Diabetes is a global health challenge. Currently, an effective treatment for diabetes is to reduce the postprandial hyperglycaemia by inhibiting the carbohydrate hydrolysing enzymes in the digestive system. In this study, we investigated the in vitro α-glucosidase and α-amylase inhibitory effects of free and bound phenolic extracts, from the bran and kernel fractions of five sorghum grain genotypes. The results showed that the inhibitory effect of sorghum phenolic extracts depended on the phenolic concentration and composition. Sorghum with higher phenolic contents generally had higher inhibitory activity. Among the tested extracts, the brown sorghum (IS131C)-bran-free extract (BR-bran-free, half-maximal inhibitory concentration (IC50) = 18 ± 11 mg sorghum/mL) showed the strongest inhibition against α-glucosidase which was comparable to that of acarbose (IC50 = 1.39 ± 0.23 mg acarbose/mL). The red sorghum (Mr-Buster)-kernel-bound extract (RM-kernel-bound, IC50 = 160 ± 12 mg sorghum/mL) was the most potent in inhibiting α-amylase but was much weaker compared to acarbose (IC50 = 0.50 ± 0.03 mg acarbose/mL).

scholarly journals Nisin and ε-poly-L-lysine as natural antimicrobials towards spoilage-associated Lactobacillus plantarum

2021 ◽  
Vol 51 (2) ◽  
Author(s):  
Fernanda Cristina Kandalski Bortolotto ◽  
Maria Helena da Rosa Farfan ◽  
Nathalia Cristina Kleinke Jede ◽  
Gabriela Maia Danielski ◽  
Renata Ernlund Freitas de Macedo
Keyword(s):  
Lactic Acid ◽  
Lactic Acid Bacteria ◽  
Inhibitory Concentration ◽  
Inhibitory Effect ◽  
Minimal Bactericidal Concentration ◽  
Natural Antimicrobials ◽  
Food Preservatives ◽  
Spoilage Bacteria ◽  
Mass Spectrometry Identification

ABSTRACT: Sausages are highly susceptible to microbial spoilage. Lactic acid bacteria (LAB) is the main group of spoilage bacteria in vacuum packed cooked sausages. To control microbial growth natural antimicrobials have been used as food preservatives. The aim of this study was to identify strains of lactic acid bacteria isolated from spoiled commercial Calabresa sausages and use them in an in vitro challenge with the natural antimicrobials, nisin (NI) and ε-poly-L-lysine (ε-PL). Mass spectrometry identification of LAB isolated from sausages using MALDI-TOF revealed a predominance of L. plantarum in the LAB population. RAPD-PCR of L. plantarum strains showed four different genetic profiles. Minimal inhibitory concentration (MIC) and minimal bactericidal concentration (MBC) of NI and ε-PL, alone and in combination, against a pool of different profiles L. plantarum were determined. MIC of NI and ε-PL were 0.468 mg/ L and 75 mg/ L; respectively, whereas MBC of NI and ε-PL were 12.48 mg/L and 150 mg/L, respectively. The combined effect of NI and ε-PL was determined using concentrations at 1/4 and 1/8 of individual MICs. Synergistic effect was confirmed at both concentrations showing a fractional inhibitory concentration index of 0.5 and 0.2, respectively. The combination of NI and ε-PL at a small concentration of 0.05 mg/L and 9.375 mg/L, respectively, showed inhibitory effect towards spoilage L. plantarum Results show the potential of the combined use of NI and ε-PL to control sausage spoilage-associated with lactobacilli.

scholarly journals Psoromic Acid, a Lichen-Derived Molecule, Inhibits the Replication of HSV-1 and HSV-2, and Inactivates HSV-1 DNA Polymerase: Shedding Light on Antiherpetic Properties

Molecules ◽  
2019 ◽  
Vol 24 (16) ◽  
pp. 2912 ◽  
Author(s):  
Sherif T. S. Hassan ◽  
Miroslava Šudomová ◽  
Kateřina Berchová-Bímová ◽  
Karel Šmejkal ◽  
Javier Echeverría
Keyword(s):  
Dna Polymerase ◽  
Active Sites ◽  
Inhibitory Action ◽  
Inhibitory Concentration ◽  
Competitive Inhibition ◽  
Inhibitory Effect ◽  
Standard Drug ◽  
Key Enzyme ◽  
Hsv 1

Psoromic acid (PA), a bioactive lichen-derived compound, was investigated for its inhibitory properties against herpes simplex virus type 1 (HSV-1) and type 2 (HSV-2), along with the inhibitory effect on HSV-1 DNA polymerase, which is a key enzyme that plays an essential role in HSV-1 replication cycle. PA was found to notably inhibit HSV-1 replication (50% inhibitory concentration (IC50): 1.9 μM; selectivity index (SI): 163.2) compared with the standard drug acyclovir (ACV) (IC50: 2.6 μM; SI: 119.2). The combination of PA with ACV has led to potent inhibitory activity against HSV-1 replication (IC50: 1.1 µM; SI: 281.8) compared with that of ACV. Moreover, PA displayed equivalent inhibitory action against HSV-2 replication (50% effective concentration (EC50): 2.7 μM; SI: 114.8) compared with that of ACV (EC50: 2.8 μM; SI: 110.7). The inhibition potency of PA in combination with ACV against HSV-2 replication was also detected (EC50: 1.8 µM; SI: 172.2). Further, PA was observed to effectively inhibit HSV-1 DNA polymerase (as a non-nucleoside inhibitor) with respect to dTTP incorporation in a competitive inhibition mode (half maximal inhibitory concentration (IC50): 0.7 μM; inhibition constant (Ki): 0.3 μM) compared with reference drugs aphidicolin (IC50: 0.8 μM; Ki: 0.4 μM) and ACV triphosphate (ACV-TP) (IC50: 0.9 μM; Ki: 0.5 μM). It is noteworthy that the mechanism by which PA-induced anti-HSV-1 activity was related to its inhibitory action against HSV-1 DNA polymerase. Furthermore, the outcomes of in vitro experiments were authenticated using molecular docking analyses, as the molecular interactions of PA with the active sites of HSV-1 DNA polymerase and HSV-2 protease (an essential enzyme required for HSV-2 replication) were revealed. Since this is a first report on the above-mentioned properties, we can conclude that PA might be a future drug for the treatment of HSV infections as well as a promising lead molecule for further anti-HSV drug design.

scholarly journals Screening and Application of Chitin Synthase Inhibitors

Processes ◽  
2020 ◽  
Vol 8 (9) ◽  
pp. 1029
Author(s):  
Xiaozai Shi ◽  
Shuo Qiu ◽  
Yingling Bao ◽  
Hanchi Chen ◽  
Yuele Lu ◽  
...  
Keyword(s):  
Antifungal Activity ◽  
Inhibitory Concentration ◽  
Inhibitory Effect ◽  
Chitin Synthase ◽  
Fungal Cell ◽  
Ic50 Value ◽  
Further Development ◽  
Fungicide Target ◽  
Better Than

Chitin is an important part of the fungal cell wall, but is not found in plants and mammals, so chitin synthase (CHS) can be a green fungicide target. In this paper, 35 maleimide compounds were designed and synthesized as CHS inhibitors. All the screened compounds showed different degrees of CHS inhibitory activity and antifungal activity in vitro. In particular, the half–inhibitory concentration (IC50) value of compound 20 on CHS was 0.12 mM, and the inhibitory effect was better than that of the control polyoxin B (IC50 = 0.19 mM). At the same time, this compound also showed good antifungal activity and has further development value.

scholarly journals The Inhibitory Effect of Clindamycin onLactobacillus in vitro

2001 ◽  
Vol 9 (4) ◽  
pp. 239-244 ◽  
Author(s):  
Alla Aroutcheva ◽  
Jose A. Simoes ◽  
Susan Shott ◽  
Sebastian Faro
Keyword(s):  
Minimum Inhibitory Concentration ◽  
Inhibitory Concentration ◽  
Inhibitory Effect ◽  
Bacteriostatic Effect ◽  
The Mean ◽  
High Concentrations ◽  
Effect On Growth

Objective:To evaluate thein vitroeffect of varying concentrations of clindamycin onLactobacillusspp.Methods: Concentrations of clindamycin ranging from 1.95–20 000 mg/ml were studied for their effect on the growth of six strains ofLactobacillus.Results:Clindamycin concentrations between 1.95–31.25 mg/ml had no statistically significant effect on growth of lactobacilli (p> 0.05). Concentrations 125 and 250 mg/ml had a bacteriostatic effect. The mean minimum inhibitory concentration (MIC) for studiedLactobacillusstrains was determined as 1000 mg/ml.Conclusion:High concentrations of clindamycin achieved in the vagina by intravaginal application might be inhibitory forLactobacillus.

scholarly journals Assessment of In Vitro Antidiabetic Potential of Purified Anthocyanin Extract from Floral Petals of Wild Balsam Species

2020 ◽  
Vol 10 (3) ◽  
pp. 31-35
Author(s):  
R ARATHY ◽  
K MURUGAN ◽  
KV DINESH BABU ◽  
GS MANOJ
Keyword(s):  
International Diabetes Federation ◽  
Inhibitory Effect ◽  
Alpha Amylase ◽  
Herbal Remedies ◽  
Antidiabetic Activity ◽  
Public Health Issue ◽  
Impatiens Balsamina ◽  
Alpha Glucosidase

Diabetes is a notorious and growing clinical and public health issue. The International Diabetes Federation assumes that 592 million had diabetes by 2035 and that by 2040 the number will increase to 642 million. Cardiovascular corollary accounts for four million deaths annually attributable to diabetes. Evidence reveals that certain glucose-lowering phytochemicals can improve vascular outcomes with type 2 diabetes, which, together with better understanding of using multiple therapies concurrently, offers opportunities for beneficial personalization of medication regimens. Anthocyanins are coloured pigments and are natural antioxidants. Keeping this in focus, this study was undertaken to evaluate the in vitro antidiabetic activity in the petals of wild Impatiens balsamina L. The anthocyanin was extracted from floral petals of wild balsam species and purified to homogeneity using chromatographic techniques. Evaluation of in vitro antidiabetic properties of anthocyanin extract revealed a dose-dependent increase in the inhibitory effect on the alpha-glucosidase (200 μg/ml) and alpha-amylase enzymes (500 μg/ml) and was comparable with the standard acarbose drug (189 μg/ml and 50 μg/ml). These results indicated that anthocyanin could be used as a source of functional food and nutraceuticals. This information from wild species will be useful in finding more potent antidiabetic principle from the natural resources for the clinical development of antidiabetic therapeutics. Future studies are planned to substantiate the antidiabetic power of anthocyanin using in vivo animal models. Keywords: Alpha amylase, alpha glucosidase, diabetes, herbal remedies, Impatiens balsamina L.

scholarly journals Synergistic effect of 5-fluorodeoxyuridine and quinazoline antifolates on murine leukemia self-cultured in vitro.

1997 ◽  
Vol 44 (4) ◽  
pp. 735-742
Author(s):  
M Balińska ◽  
I Szablewska ◽  
D Janiszewska ◽  
A Brzezińska ◽  
K Pawełczak
Keyword(s):  
Synergistic Effect ◽  
Inhibitory Concentration ◽  
Inhibitory Effect ◽  
Leukemia Cells ◽  
Parental Line ◽  
Prior Use ◽  
Thymidylate Synthesis ◽  
Combined Drugs ◽  
Murine Leukemia

The effect of thymidylate synthase inhibitors, fluorodeoxyuridine (FdUrd) and its two sulphonamide derivatives was examined in the culture of murine leukemia cells -- 5178Y (parental subline) and its fluorodeoxyuridine resistant subline 5178Y/F. A synergistic effect of the antimetabolites on cell survival was observed on exposure of the culture of either line to a slightly inhibitory concentration of FdUrd (1 nM) in combination with 2-desamino-2-methyl-10-propargyl-5,8-dideaza-pteroylsulphogluta mate or 2-desamino-2-methyl-10-propargyl-5,8-dideaza-pteroylsulphoglyci ne. This effect was accompanied by a marked reduction, in both cell lines of intracellular concentration of 5,10-methylenetetrahydro-pteroyl-polyglutamate, although its concentration in the resistant subline was 3 times as high as in the parental line. The inhibitory effect of combined drugs on the cellular pool of folates in 5178Y line depended also on the sequence of drug addition, whereas in the FdUrd resistant line this sequence was without any effect. The results obtained strongly suggest that under certain conditions inhibition of thymidylate synthesis by antifolates is intensified by a prior use of FdUrd.

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