scholarly journals Synthesis of the Polyhydroquinoline Derivative 4-(2-Chloro-Phenyl)-2,7,7-Trimethyl5-oxo-1,4,5,6,7,8-Hexahydroquinoline-3-Carboxylic Acid Ethyl Ester: Antimicrobial and Enzyme Modulator

2021 ◽  
Author(s):  
Gustavo Henrique Andrade Machado ◽  
Marcus Vinícius Cardoso Trento ◽  
Juliana Junqueira Pinelli ◽  
Roberta Hilsdorf Piccoli ◽  
Sérgio Scherrer Thomasi ◽  
...  
Keyword(s):  
Multicomponent Reactions ◽  
Acid Ethyl Ester ◽  
Biological Properties ◽  
Dilution Method ◽  
Clotting Time ◽  
Phospholipase Activity ◽  
Thrombolytic Activity ◽  
Serial Dilution Method ◽  
Pharmacological Potential ◽  
Bothrops Moojeni

Abstract Multicomponent reactions are extremely relevant in green chemistry. They offer better conditions than traditional synthesis and are, therefore, used for many organic modifications. Recently, the synthesis of polyhydroquinolines has received much attention for its high pharmacological potential. In the present study, a polyhydroquinoline derivative was synthesized without the use of catalysts or solvents. The results of nuclear magnetic resonance and infrared spectroscopy demonstrated that the molecule was successfully synthesized. The molecule presents significant results of antimicrobial activity for the bacteria tested in the serial dilution method. It also increased the clotting time by 25.66 seconds for the highest dose and 12.66 seconds for the other doses tested. Prior incubation with the dose of 125 mg reduced the thrombolytic activity to 73%. The 125, 100, and 50 mg doses previously incubated with Bothrops moojeni venom inhibited approximately 30% of the phospholipase activity. The molecule was also able to reduce the cytotoxicity induced by proteases significantly. In conclusion, the molecule presents several biological properties, which highlights its pharmaceutical potential.

Synthesis, Characterization and Antimicrobial Evaluation of Some N-Substituted Benzimidazole Derivatives

2020 ◽  
Vol 17 (1) ◽  
pp. 87-91 ◽  
Author(s):  
Anuj Kumar ◽  
Yogesh Kumar ◽  
Jagdish K. Sahu ◽  
Sushil Kumar
Keyword(s):  
Antimicrobial Agents ◽  
New Technologies ◽  
Biological Properties ◽  
Benzimidazole Derivatives ◽  
Dilution Method ◽  
Moderate Activity ◽  
Significant Activity ◽  
Microbial Diseases ◽  
Serial Dilution Method ◽  
Antibacterial And Antifungal

Background: Due to the appearance of communicable microbial diseases and the toxicity related with presently used several antimicrobials such as β-lactam antibiotics, tetracyclines, quinolones, macrolides, glycopeptides (vancomycin) etc, demand for new antimicrobial agents has become a great concern in new technologies to improve efficacy and safety. Methods: In search of new antimicrobial agents with higher potency, some N-substituted benzimidazole derivatives (4, 5a-5h & 6) were obtained by chloroacetylation of benzimidazole followed by reaction with different amines, which were characterized by spectroscopic methods. All the target compounds were evaluated for their antibacterial and antifungal activity against microorganisms using two-fold serial dilution method. Results: Among the compounds evaluated, compounds 4 and 5d exhibited potent activity against Bacillus thuringiensis and Candida albicans while showed moderate activity against Escherischia coli when compared to amoxicillin and fluconazole. Compound 5a showed significant activity against tested microorganisms. Conclusion: From the current study, it may be concluded that synthesized compounds are fulfilling in terms of their structural distinctiveness and marked biological properties. These compounds might be encouraged to initiate a new class of antimicrobial agents.

The Structure and Antibacterial Activity of Taurine and its Magnesium Complex

2011 ◽  
Vol 366 ◽  
pp. 404-407
Author(s):  
Li Hua Wang
Keyword(s):  
Escherichia Coli ◽  
Antibacterial Activity ◽  
Bacillus Subtilis ◽  
Single Crystal ◽  
Dilution Method ◽  
Monoclinic Space Group ◽  
X Ray Diffraction ◽  
X Ray ◽  
Antibacterial Assay ◽  
Serial Dilution Method

The block single-crystals of taurine were obtained, and its structure was determined by single-crystal X-ray diffraction. The single-crystal X-ray analysis of taurine reveals that the crystal belongs monoclinic, space group P2(1)/c with a = 0.52824(10) nm, b = 1.1647(8) nm, c = 0.79236(13) nm, ß = 94.0850(10). The magnesium complex with taurine has been synthesized in ethanol. The antibacterial assay of the Mg (II) complex was measureed using a modified version of the 2-fold serial dilution method. The results show that the complex shows considerable antibacterial activity against escherichia coli, bacillus subtilis and staphylococcus white.

scholarly journals ANTIBIOTICS RESISTANCE OF CORYNEBACTERIUM NON DIPHTHERIAE STRAINS

2017 ◽  
pp. 3-8
Author(s):  
G. G. Kharseeva ◽  
N. A. Voronina ◽  
T. D. Gasretova ◽  
O. I. Sylka ◽  
S. Yu. Tyukavkina
Keyword(s):  
Serial Dilution ◽  
Urogenital Tract ◽  
Antibiotics Resistance ◽  
Dilution Method ◽  
Frequency Of Occurrence ◽  
Serial Dilution Method ◽  
Resistant Strains

Aim. Study the frequency of occurrence of antibiotics resistant strains of various species of Corynebacterium non diptheriae. Materials and methods. C.pseudodiphtheriticum, C.pseudotuberculosis, C.xerosis, C.amycolatum, C.striatum, C.ulcerans strains isolated from patients with pathologies of respiratory and urogenital tract, as well as individuals taking prophylaxis examination were used. Sensitivity to antibacterial preparations was determined by the serial dilution method. Results. The highest number of Corynebacterium non diptheriae strains displayed resistance to benzylpenicillin (54.8%) and lincomycin (50.7%), and lowest - to cefotaxime, cefazolin (6.8%) and vancomycin (13.7%). The highest number of antibiotics resistant strains were detected among members of C.pseudotuberculosis {100%), C.xerosis (96.0%) and C. pseudodiphtheriticum (81.0%) species. Polyresistant strains were detected most frequently among C.xerosis, C.amycolatum and C.striatum species. Strains of Corynebacterium non diptheriae most frequently displayed resistance to 1 or 2 antibacterial preparations (24.7%), less frequently - to 3 (20.5%), 4 (13.7%), 5 (4.1%) and 6 (1.4%) preparations. Conclusion. The amount of antibiotics resistant strains of Corynebacterium non diptheriae is large (89.0%) and non-similar in various species.

scholarly journals Screening of Punica granatum extract for antimicrobial activity against oral micro organisms

2020 ◽  
Vol 6 (2) ◽  
pp. 73-77
Author(s):  
Meera Avadhani ◽  
◽  
Meena Anand Kukkamalla ◽  
Kishore G Bhat ◽  
◽  
...  
Keyword(s):  
Research Work ◽  
Fusobacterium Nucleatum ◽  
Punica Granatum ◽  
Dilution Method ◽  
Dental Patients ◽  
Mueller Hinton ◽  
Mueller Hinton Agar ◽  
Serial Dilution Method ◽  
Micro Organisms ◽  
Dental Infections

Background and Objectives: A lot of research work in both dental and medical fields support the curative properties of pomegranate. Accordingly, it was decided to prepare a pomegranate mouthwash and evaluate it among Dental patients diagnosed with Chronic Gingivitis. The objective of the present invitro study is to assess the Minimum Inhibitory Concentration (MIC) of the commercially available pomegranate extract powder against few oral pathogenic microorganisms. Methodology: Serial dilution method using thioglycolate broth medium was used for anerobes like Streptococcus mutans, Fusobacterium nucleatum, Aggregatibacter actinomycetomcomitans, Prevotella intermedia and Mueller hinton agar mediated growth was used for aerobe like Staphylococcus aureus. Following which microdilution assay was performed and accordingly evaluated the MIC. Based on this report, the test rinse was prepared and further evaluated using the same methodology for both aerobes and anerobes. Results and Inference: It was observed from the MIC report for both aerobes and anerobes that at a concentration of 0.2% the formulated mouth rinse was effective against all the chosen organisms. The results of the study infer that products like mouthwash, dental gels etc made from this concentration could be possibly used for the control of dental infections.

scholarly journals Potential Anticancer Properties and Mechanisms of Action of Formononetin

2019 ◽  
Vol 2019 ◽  
pp. 1-11 ◽  
Author(s):  
Dongjun Jiang ◽  
Azhar Rasul ◽  
Rabia Batool ◽  
Iqra Sarfraz ◽  
Ghulam Hussain ◽  
...  
Keyword(s):  
Trifolium Pratense ◽  
Antioxidant Properties ◽  
Cancer Therapeutics ◽  
Biological Properties ◽  
Anticancer Properties ◽  
Biological Potential ◽  
Pharmacological Potential ◽  
Reported Data ◽  
Pharmacologically Active ◽  
Promising Source

Nature, a vast reservoir of pharmacologically active molecules, has been most promising source of drug leads for the cure of various pathological conditions. Formononetin is one of the bioactive isoflavones isolated from different plants mainly from Trifolium pratense, Glycine max, Sophora flavescens, Pycnanthus angolensis, and Astragalus membranaceus. Formononetin has been well-documented for its anti-inflammatory, anticancer, and antioxidant properties. Recently anticancer activity of formononetin is widely studied. This review aims to highlight the pharmacological potential of formononetin, thus providing an insight of its status in cancer therapeutics. Formononetin fights progression of cancer via inducing apoptosis, arresting cell cycle, and halting metastasis via targeting various pathways which are generally modulated in several cancers. Although reported data acclaims various biological properties of formononetin, further experimentation on mechanism of its action, medicinal chemistry studies, and preclinical investigations are surely needed to figure out full array of its pharmacological and biological potential.

scholarly journals Evaluation of anticoagulant and thrombolytic activity of Berberis orthobotrys in animal model

2018 ◽  
Vol 13 (2) ◽  
pp. 196 ◽  
Author(s):  
. Alamgeer ◽  
Mahpara Tarar ◽  
Umme Habiba Hasan ◽  
Muhammad Saleem
Keyword(s):  
Bleeding Time ◽  
Methanol Extract ◽  
Activated Partial Thromboplastin Time ◽  
Coumaric Acid ◽  
Clotting Time ◽  
Aqueous Methanol ◽  
Thrombolytic Activity ◽  
Coagulation Parameters ◽  
Hplc Profile ◽  
Pharmacological Basis

<p class="Abstract">Fundamental to this research was the evaluation of anticoagulant and thrombolytic potential of Berberis orthobotrys using clotting time, prothrombin time and activated partial thromboplastin time performed at 2.5, 5, 10% concentration. Aqueous-methanol extract significantly (p&lt;0.05) increased the coagulation parameters both in human blood as well as in rabbit blood and exhibited the more salient effect on prolongation of these coagulation parameters at 10% concentration. Aqueous methanol extract (25, 50 and 100 mg/kg) produced the preferential increase in bleeding time and clotting time nevertheless the effect was more perceptible after 90 min at 100 mg/kg. Moreover, the crude extract presented a substantial increase in coagulation parameters after 7 days of administration in rabbits with more pronounced effects at the highest dose. HPLC profile of aqueous methanol extract revealed the presence of quercetin, p-coumaric acid, gallic acid, vanillic acid, 4-hydroxy-3-methoxy benzoic acid. Thus, the present study provides the pharmacological basis for its medical use in cardiovascular and other thrombotic disorders.</p>

Procoagulant activity of erythrocytes and platelets through phosphatidylserine exposure and microparticles release in patients with nephrotic syndrome

2012 ◽  
Vol 107 (04) ◽  
pp. 681-689 ◽  
Author(s):  
Chunyan Gao ◽  
Rui Xie ◽  
Chengyuan Yu ◽  
Qin Wang ◽  
Fangfang Shi ◽  
...  
Keyword(s):  
Nephrotic Syndrome ◽  
Cell Injury ◽  
Anticoagulant Activity ◽  
Minimal Change Nephrotic Syndrome ◽  
Significant Inhibition ◽  
Minimal Change ◽  
Procoagulant Activity ◽  
Clotting Time ◽  
Thrombolytic Activity ◽  
Inhibition Effect

SummaryRecent studies showed that an imbalance of prothrombotic and antithrombotic factors and impaired thrombolytic activity contribute to the thrombophilia of the nephrotic syndrome (NS). However, it is not clear whether blood cell injury and/or activation is involved in hypercoagulability in NS patients. Our objectives were to study the increase in microparticle (MP) release and phosphatidylserine (PS) exposure on the outer membrane of MP-origin cells in NS patients, and to evaluate their procoagulant activity (PCA). The subjects were patients with membranous nephropathy (MN), minimal change nephrotic syndrome (MCNS) and healthy controls. Analyses of MPs and PS exposure were performed using a flow cytometer. PCA was determined by clotting time and purified coagulation complex assays. We found that lactadherin+ MPs, which derived from red blood cells (RBC), platelet and endothelial cell, increased in NS patients. Moreover, PS exposure on RBCs and platelets in each NS group, especially in MN, are higher than that in controls. MP shedding and PS exposure of RBCs/platelets were highly procoagulant in NS patients. However, blockade of PS with lactadherin inhibited over 90% of PCA while an anti-tissue factor antibody had no significant inhibition effect. Our results demonstrate that the thrombophilic susceptibility of NS may be partly ascribed to MP release and PS exposure of RBCs, platelets and endothelial cells. Lactadherin is a sensitive probe for PS that has high anticoagulant activity.

scholarly journals Dry season and diurnal surveys of phylloplane fungi of Hevea brasiliensis in Nigeria

2014 ◽  
Vol 23 (1) ◽  
pp. 143-147
Author(s):  
J. A. Okhuoya ◽  
C. O. Ahweyevu
Keyword(s):  
Hevea Brasiliensis ◽  
Fungal Spores ◽  
Dry Season ◽  
Dilution Method ◽  
Fungal Population ◽  
Peak Period ◽  
Mature Leaves ◽  
Phylloplane Fungi ◽  
Young Leaves ◽  
Serial Dilution Method

Monthly and diurnal variation of phylloplane fungi of rubber (<i>Hevea brasiliensis</i>) leaves were studied over a period of four months in the dry season, using two culturing methods. Composite fungal population was the highest in April and the lowest in February. Serial dilution method recorded the higher number of fungal spores than ballistospore method. Mature leaves were found to have more fungal spores than premature and young leaves. Spore concentration on the leaves showed diurnal periodicity, with peak period of spores between 12-18 hr. Rubber leaves outside the plantation, had more spores on their surfaces than those shaded by the plantation canopy. The factors responsible for these observations were discussed.

scholarly journals DETEKSICEMARAN BAKTERIOLOGIS DAN LOGAM BERAT DAGING LANGKITANG (Faunus ater)

2020 ◽  
Vol 6 (1) ◽  
pp. 14-20
Author(s):  
yosmed Hidayat ◽  
◽  
Erismar Amri
Keyword(s):  
Heavy Metal ◽  
Microbial Contamination ◽  
Atomic Absorption Spectrophotometry ◽  
Most Probable Number ◽  
Dilution Method ◽  
Probable Number ◽  
Absorption Spectrophotometry ◽  
Bacteriological Testing ◽  
Lead Metal ◽  
Serial Dilution Method

This study aims to determine the level of bacteriological contamination and heavy metal lead (Pb) in langkitang (Faunus ater) meat. The sample were taken randomly as 15 samples from traders. Examination of microbial contamination in meat used a serial dilution method Most Probable Number (MPN) consisting of the presumptive test, confirmed test, and completed test. Measurement of Lead Heavy Metal (Pb) content used Atomic Absorption Spectrophotometry (AAS). The result of bacteriological testing of the MPN/ 100 ml sample showed that the tested Langkitang meat contained contaminating bacteria for each sample tested, and Lead metal was also detected, some of which had values that exceeded the threshold. Based on the results of the analysis, the langkitang meat has a microbial and lead metal contamination content that exceeds the health threshold so that it takes proper processing before the meat is consumed

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