scholarly journals Targeting the Secreted Aspartic Proteinase (SAP-1) Associated with Virulence in C. albicans by C. cassia Bio-compounds: A Computational Approach

2020 ◽  
pp. 75-86
Author(s):  
Abigail Ranasinghe ◽  
A. S. Smiline Girija ◽  
J. Vijayashree Priyadharsini
Keyword(s):  
3D Structure ◽  
Data Bank ◽  
Inhibitory Effect ◽  
Computational Approach ◽  
Diffusion Method ◽  
Discovery Studio ◽  
Medicinal Value ◽  
Ligand Interactions ◽  
Vitro Analysis

Evaluation of the drug ligand interactions between the C. cassia bio-compounds with the SAP-1 in C. albicans to explore the inhibitory medicinal potential of C. cassia bio-compounds by a computational approach is performed in the present investigation. Antimicrobial assay was done using agar well diffusion method with the crude aqueous and ethanolic extracts of the dried barks of C. cassia against C. albicans. 2D & 3D structures of the active bio-compounds of C. cassia were optimized and the 3D structure of SAP-1 was retrieved from the PDB data bank. In-silico inhibitory potential of the selected C. cassia biocompounds against SAP-1 was done by Auto Dock 2.0 and was visualized with Accelrys discovery studio visualizing tool with the assessment of the molecular properties of the ligands against SAP-1 by molinspiration calculations and further assessment for their drug likeliness. In-vitro analysis showed a promising anti-fungal activity of C. cassia extracts against C. albicans. Cinnamoyl E-acetate and Eugenyl acetate seem to possess promising inhibitory effect to target SAP-1 with a least binding energy of –5.33 and -5.21 Kcal/mol with four hydrogen bonds respectively. Molinspiration assessments showed zero violations for all the C. cassia compounds with the TPSA scores of <140 Å towards the best oral bioavailability. The findings of the study emphasize that cinnamaldehyde, cinnamoyal acetate and eugenol from C. cassia seem to possess a promising inhibitory effect against SAP-1 of C. albicans suggesting the medicinal value of the spice against SAP-1.

Preliminary in Vitro Investigations on The Inhibitory Activity of The Original Dietary Supplement Oxidal® on Pathogenic Bacterial Strains

2020 ◽  
Vol 11 ◽  
pp. 37-43
Author(s):  
Prof. Teodora P. Popova ◽  
Toshka Petrova ◽  
Ignat Ignatov ◽  
Stoil Karadzhov
Keyword(s):  
Dietary Supplement ◽  
Broad Spectrum ◽  
Pathogenic Bacteria ◽  
Antimicrobial Agents ◽  
Clinical Effectiveness ◽  
Inhibitory Effect ◽  
Diffusion Method ◽  
Bacterial Strains ◽  
Microbial Strains

The antimicrobial action of the dietary supplement Oxidal® was tested using the classic Bauer and Kirby agar-gel diffusion method. Clinical and reference strains of Staphylococcus aureus and Escherichia coli were used in the studies. The tested dietary supplement showed a well-pronounced inhibitory effect against the microbial strains commensurable with that of the broad-spectrum chemotherapeutic agent Enrofloxacin and showed even higher activity than the broad spectrum antibiotic Thiamphenicol. The proven inhibitory effect of the tested dietary supplement against the examined pathogenic bacteria is in accordance with the established clinical effectiveness standards for antimicrobial agents.

scholarly journals Development of mouthwash with Rosmarinus officinalis extract

2014 ◽  
Vol 50 (4) ◽  
pp. 851-858 ◽  
Author(s):  
Isabela Moreira Baumgratz de Paula ◽  
Flávia Costa Moraes ◽  
Orlando Vieira de Souza ◽  
Célia Hitomi Yamamoto
Keyword(s):  
Sodium Fluoride ◽  
Inhibitory Activity ◽  
Raw Materials ◽  
Ethanol Extract ◽  
Inhibitory Effect ◽  
Rosmarinus Officinalis ◽  
Hexane Fraction ◽  
Diffusion Method ◽  
Oral Infections

Rosmarinus officinalis, which belongs to the Lamiaceaefamily, is a species of medicinal flora with therapeutic properties. In order to exploit the benefits of these properties, a mouthwash formulation was developed, with careful selection of raw materials to meet pharmacotechnical requirements. Extracts of the plant were incorporated into a mouthwash, which was shown to have inhibitory action in vitro against the micro-organisms commonly found in periodontics. Controls for assessing the quality of the drugs were carried out, quantifying phenols and flavonoids as chemical markers. Mouthwash solutions were formulated containing 0.1, 5 and 10% ethanol extract of R. officinalis; and 0.05, 5 and 10% of the hexane fraction of R. officinalis. In order to evaluate synergism, ethanol extract and hexane fraction were also added to formulations containing 0.05% sodium fluoride and 0.12% chlorhexidine digluconate. These formulations were assessed for inhibitory effect against the specific microorganisms involved in the process of bacterial plaque formation, S. mutans(ATCC25175) and C. albicans(ATCC 10231), frequently found in cases of oral infections. The agar diffusion method was used to evaluate the inhibitory activity of extracts and formulations. All mouthwash solutions displayed inhibitory activity having higher sensitivity to S. mutansfor the 5% ethanol extract+0.05% sodium fluoride, and greater sensitivity to C. albicansfor the 10% hexane fraction. Results were characterized by the appearance of a growth inhibition halo, justifying the utilization and association of extracts of R. officinalis.

scholarly journals Antimicrobial properties of antibiotic-loaded implants

2020 ◽  
Vol 102-B (6_Supple_A) ◽  
pp. 158-162
Author(s):  
Quentin Griseti ◽  
Christophe Jacquet ◽  
Pierre Sautet ◽  
Matthew P. Abdel ◽  
Sébastien Parratte ◽  
...  
Keyword(s):  
Titanium Alloy ◽  
Antimicrobial Properties ◽  
Porous Metal ◽  
Porous Titanium ◽  
Inhibitory Effect ◽  
Control Group ◽  
Local Antibiotics ◽  
Significant Difference ◽  
Vitro Analysis

Aims The aim of this study was to compare the ability of tantalum, 3D porous titanium, antibiotic-loaded bone cement, and smooth titanium alloy to inhibit staphylococci in an in vitro environment, based on the evaluation of the zone of inhibition (ZOI). The hypothesis was that there would be no significant difference in the inhibition of methicillin-sensitive or methicillin-resistant Staphylococcus aureus (MSSA/MRSA) between the two groups. Methods A total of 30 beads made of three different materials (tantalum/3D porous titanium and smooth titanium alloy) were bathed for one hour in a solution of 1 g vancomycin in 20 ml of sterile water for injection (bath concentration: 50 mg/mL). Ten 1 cm3 cylinders of antibiotic-loaded cement were also created by mixing standard surgical cement with 1 g of vancomycin in standardized sterile moulds. The cylinders were then placed on agar plates inoculated with MSSA and MRSA. The ZOIs were measured each day and the cylinders were transferred onto a new inoculated plate. Results For MSSA and MRSA, no inhibitory effect was found in the control group, and antibiotic-loaded smooth titanium alloy beads showed a short inhibitory effect until day 2. For MSSA, both tantalum and 3D porous titanium beads showed significantly larger mean ZOIs than cement beads (all p < 0.01) each day until day 7 for tantalum and until day 3 for 3D porous titanium. After six days, antibiotic-loaded cement had significantly larger mean ZOIs than the 3D porous titanium (p = 0.027), but no significant difference was found with tantalum (p = 0.082). For MRSA, both tantalum and 3D porous titanium beads had significantly larger mean ZOIs than antibiotic-loaded cement each day until day 6 for tantalum (all p < 0.01) and until day 3 for 3D porous titanium (all p < 0.04). Antibiotic-loaded cement had significantly larger mean ZOIs than tantalum and 3D porous titanium from day 7 to 9 (all p < 0.042). Conclusion These results show that porous metal implants can deliver local antibiotics over slightly varying time frames based on in vitro analysis. Cite this article: Bone Joint J 2020;102-B(6 Supple A):158–162.

scholarly journals Evaluation of three plant species to control black scurf disease of Irish potato (Solanum tuberosum Linn.)

2020 ◽  
Vol 12 (1) ◽  
pp. 90-99
Author(s):  
Matthew O. ADEBOLA ◽  
Tunde S. BELLO ◽  
Esther A. SERIKI ◽  
Mariam B. AREMU
Keyword(s):  
Solanum Tuberosum ◽  
Mycelial Growth ◽  
Pathogenic Fungus ◽  
Inhibitory Effect ◽  
Black Scurf ◽  
Irish Potato ◽  
Diffusion Method ◽  
Leaf Extracts

Irish potato (Solanum tuberosum) is an important worldwide food crop and one of the most popular in Nigeria. Its abundance and successful yield have been immensely affected by black scurf disease caused by Rhizoctonia solani. Harnessing a cost-effective management of this pathogenic fungus, three botanical species Acalypha wilkesiana, Moringa oleifera and Carica papaya leaves, each at concentrations of 0 mg ml-1 (control), 25 mg ml-1, 50 mg ml-1 and 75 mg ml-1 were evaluated in vitro. The plant leaf extracts were prepared using methanol and were evaluated for their toxicity using agar well diffusion method. The fungus was isolated from spoilt Irish potato with black scurf symptoms. The results showed the presence of some phytochemicals in leaf extract of each of the plants tested. The three leaves extract independently inhibited mycelial growth of R. solani. The potency of all the plant extracts increased with the increase in concentration. The highest concentration (75 mg ml-1) of M. oleifera and C. papaya evaluated, gave the highest inhibitory effect of 0.81 mm and 1.63 mm respectively, which were not significantly different (p> 0.05), but was obviously different from A. wilkesiana (2.81 mm). Furthermore, M. oleifera extract gave the highest percentage of mycelial growth inhibition of the fungus in all grades of the concentrations evaluated, whereas A. wilkesiana showed the least. The leaves of the three species are therefore recommended for in vivo control of this fungus, owing to their proven efficacy and to their cheap availability.

scholarly journals MOLECULAR DOCKING STUDY ON 1H-(3,4d) PYRAZOLO-PYRIMIDINES AS CYCLIN DEPENDANT KINASE (CDK2) INHIBITORS

2016 ◽  
Vol 9 (1) ◽  
pp. 94
Author(s):  
Manisha S. Phoujdar ◽  
Gourishankar R. Aland
Keyword(s):  
Data Bank ◽  
Docking Study ◽  
Docking Studies ◽  
Van Der Waals Interactions ◽  
Binding Modes ◽  
Molecular Docking Study ◽  
Discovery Studio ◽  
Receptor Assays

Objective: CDK2 inhibitors are implicated in several carcinomas viz. Carcinoma of lung, bladder, sarcomas and retinoblastoma. Pyrazolopyrimidines, being purine bioisosters inhibit more than one type of kinase. In this study, we are studying some novel derivatives of 1H-pyrazolo [3,4d] pyrimidines not reported earlier. The objective of the present study is an attempt towards design and development of 1H-[3,4-] pyrazolo-pyrimidines as CDK2 inhibitors through rational drug design.Methods: The present study has been done on CDK2 structure, PDB ID, 3WBL, co-crystallized with ligand PDY from RCSB protein data bank. A series of seventeen 1H-Pyrazolo [3,4-d] pyrimidines feasible for synthesis was docked on the said CDK2 receptor using Auto Dock 4 version, 1.5.6. Outputs were exported to discovery studio 3.5 client for visual inspection of the binding modes and interactions of the compounds with amino acid residues in the active sites.Results: The results of docking studies revealed that the present series of 1H-Pyrazolo[3,4-d] pyrimidines is showing significant binding through hydrogen bonding, hydrophobic, pi and Van der waals interactions, similar to the ligand PDY. Some conserved H-bond interactions comparable to bioisosters and compounds presently under human trials were noted. Ki values predicted in silico also suggest that the series will show promising CDK2 inhibitory activity.Conclusion: The series designed and docked can be further developed by synthesis and in vitro and in vivo activity. The receptor inhibitory activity can also be checked by specific receptor assays.

Rapid and efficient synthesis of newer heterocyclic 2-azetidinone and 5-benzylidine-4-oxo-thiazolidine compounds and their pharmacological studies

2019 ◽  
Author(s):  
Chem Int
Keyword(s):  
Inhibitory Effect ◽  
Diffusion Method ◽  
Spectroscopic Techniques ◽  
Antimicrobial Compounds ◽  
Efficient Synthesis ◽  
Proteus Vulgaris ◽  
Bacterial Strains ◽  
Pharmacological Studies ◽  
In Vitro Antibacterial Activity

A straightforward rapid and efficient protocol for the synthesis of 2-azetidinone (D1-10) and 5-benzylidine-4-oxo-thiazolidine (F1-10) has been designed and synthesized in order to find newer antimicrobial compounds. The structure of entitle compounds have been evaluated on the basis of various spectroscopic techniques FTIR, 1H-NMR, 13C-NMR as well as elemental microanalysis. The title compounds were screened for their preliminary in vitro antibacterial activity against a panel of selected pathogenic bacterial strains, Staphylococcus aureus (MTCC 96), Escherichia coli (MTCC 443), Proteus vulgaris (MTCC 426) and Pseudomonas aeruginosa (MTCC 424) using cup-plate agar diffusion method at 40 μg/ml concentration. Out of synthesized compounds, compound nos. D4, D5, D7, D8, D9 and D10 have shown outstanding inhibitory effect against all pathogens and consider as the best bioactive desired antibacterial analogue of the series as compare to standard drugs ampicilline and chloramphenicol.

scholarly journals In vitro antibacterial activity of Terminalia chebula leaf gall extracts against some human pathogenic strains

2012 ◽  
Vol 1 (8) ◽  
pp. 217-220 ◽  
Author(s):  
BE Ravi Shankara ◽  
YL Ramachandra ◽  
S Sundara Rajan ◽  
J Preetham ◽  
PS Sujan Ganapathy
Keyword(s):  
Antibacterial Activity ◽  
Aqueous Extract ◽  
Ethanol Extract ◽  
Pharmaceutical Journal ◽  
Inhibitory Effect ◽  
Diffusion Method ◽  
Terminalia Chebula ◽  
Bacterial Strains ◽  
South Indian

The leaf galls of Terminalia chebula is used widely as Karkatasringi in south Indian markets. Karkatashringi is an important crude drug employed in various indigenous systems of medicine against several diseases and the drug has diverse medicinal properties. The present study was carried out to understand the antimicrobial activity of various extracts. The antibacterial activity of T. chebula (leaf gall) was evaluated against ten bacterial strains including Gram-positive and Gram-negative bacteria using the agar-well diffusion method. Among the two extracts tested, the ethanol extract presented the best results against all the bacteria while aqueous extract showed moderate inhibition of the microbial growth. Each extract is unique against different microorganisms; Staphylococcus aureus was more susceptible to both extract among the tested organisms, whereas Serratia marcescens and Proteus mirabilis were less susceptible for ethanol and aqueous extract respectively. The inhibitory effect of the extracts was compared with standard antibiotic Ciprofloxacin.DOI: http://dx.doi.org/10.3329/icpj.v1i8.11254 International Current Pharmaceutical Journal 2012, 1(8): 217-220 

scholarly journals Suppression of inflammatory mediators by aqueous leaf extract of Crotalaria verrucosa: in vivo and in vitro analysis

2020 ◽  
Vol 9 (12) ◽  
pp. 1897
Author(s):  
Mohammad Mustakim Billah ◽  
Abir Huzaifa ◽  
M. Abdul Kader Khan ◽  
Nusrat Jahan Vabna ◽  
Kashfia Nawrin ◽  
...  
Keyword(s):  
Leaf Extract ◽  
Protein Denaturation ◽  
Inflammatory Activity ◽  
Medicinal Value ◽  
Aqueous Leaf Extract ◽  
Anti Inflammatory ◽  
Vitro Analysis ◽  
In Vitro Analysis

Background: Crotalaria verrucosa is a traditional plant frequently prescribed by the tribes for its medicinal value against inflammation. The present study was designed to investigate the scientific basis for medicinal value in inflammation by in vivo and in vitro analysis.Methods: Anti-inflammatory activity of the plant’s leaf was evaluated by two in vivo methods - carrageenan induced rat paw edema and xylene induced mice ear edema. Moreover, in vitro analysis was performed through heat induced hemolysis and heat induced protein denaturation methods.Results: The inflammation produced by carrageenan and xylene were effectively suppressed by the aqueous leaf extract of C. verrucosa (CVAQ) at 600 mg/kg body weight which was comparable to the standards. In heat induced hemolysis test the extract was able to inhibit the lysis up to 70% at 500 µg/ml whereas in heat induced protein denaturation test it reduces the percentage till 69% at the same concentration.Conclusions: The findings suggested that CVAQ possess moderate to high anti-inflammatory activity when applied in low to high concentrated doses. However, the study can only conclude from this basic evaluation that the extract needs to be further investigated for identifying the potential compound which contributed to such medicinal value of the plant.

scholarly journals The influence of plant essential oils on in vitro growth of Pectobacterium and Dickeya spp. bacteria

2021 ◽  
Vol 20 (6) ◽  
pp. 19-29
Author(s):  
Małgorzata Schollenberger ◽  
Agnieszka Gadomska-Gajadhur ◽  
Ewa Mirzwa-Mróz ◽  
Damian Kret ◽  
Ewa Skutnik ◽  
...  
Keyword(s):  
Essential Oils ◽  
Soft Rot ◽  
Inhibitory Effect ◽  
Diffusion Method ◽  
Juniperus Virginiana ◽  
Bacterial Strains ◽  
Disk Diffusion Method ◽  
First Report ◽  
Plant Essential Oils

 The activity of essential oils from Eucalyptus globulus, Pinus silvestris, Lavandula angustifolia, Juniperus virginiana, Rosmarinus officinalis and Citrus paradise against the soft-rot pathogens Pectobacterium carotovorum subsp. carotovorum, Pectobacterium atrosepticum, Pectobacterium parmentieri and Dickeya solani was determined in vitro. The antibacterial activity of the essential oils will be evaluated using the disk-diffusion method by Kirby-Bauer [Bauer et al. 1966]. It was found that all the presented essential oils varied in antimicrobial activity against the four bacterial strains. No differences in the influence of streptomycin on inhibition of growth of the four bacterial strains were observed. Among six tested plants, essential oils from P. sylvestris had the strongest inhibitory effect on the growth of soft rot bacteria from Pectobacterium genus. This paper constitute the first report on the activity of the essential oils obtained from J. virginiana against soft rot bacteria. They are also the first report on the activity of the essential oils obtained from E. globulus, P. silvestris, L. angustifolia and C. paradisi against P. atrosepticum, P. parmentieri and D. solani as well as on the activity of the R. officinalis essential oils against P. atrosepticum and P. parmentieri.

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