Agar Cup Plate Method Research Articles

Design, Synthesis, Antimicrobial Evaluation of Novel 2-Oxo-4-Substituted Aryl-Azetidine Benzotriazole Derivatives.

A series of compounds was synthesized and characterized to explore new antimicrobial agents. These compounds were evaluated by using the agar cup plate method. The most active compound exhibited a zone of inhibition 18±0.09 mm and 19±0.09 mm against E. Coli and S. aureus, respectively. To gain insights into the intermolecular interactions, molecular docking studies were performed at the active site of the glucosamine fructose 6 phosphate synthase (GlcN 6 p) enzyme (PDB Id: 1XFF). The results of the molecular docking studies are in agreement with the pharmacological evaluation with potent compounds, exhibiting docking scores of -11.2. However, deformability, B-factor and covariance computations showed a result that the most active compound favored molecular connections with the protein. Therefore, our research is important for the development of antimicrobial agents.

Formulation and evaluation of herbal cream using ethanolic extract of Emblica officinalis for antibacterial activity

Skin infections occur commonly and after present therapeutic challenges to practioners due to the growing concerns regarding multidrug resistant bacterial, viral and fungal strain. The aim of present study was to formulate topical cream using Ethanolic leaves extract Emblica officinalis and evaluate In­­- vitro study the antibacterial activity of the ethanolic extracts of dried leaves of Emblica officinalis was determined by using the Agar cup plate method versus different bacteria such as Staphylococcus aureus, Bacillus subtilis, Escherichia coli and Pseudomonas aeruginosa etc. By blending the ethanolic extract of Emblica officinalis (10 % w/w) into aqueous cream we formulated herbal cream. Formulation of herbal cream evaluation their physio-chemical properties, in vitro drug release and in vitro Antibacterial Activity against Staphylococcus aureus, Bacillus cereus, Escherichia coli, Pseudomonas aeruginosa. The herbal cream formulation A5 show better release and effective against bacterial strain

Phytochemical Extraction and Activity against Salmonella Typhi of Selaginella Bryopteris

Selaginella Bryopteris is widely known medicinal plant in India. It has many medicinal use such as anti-bacterial, antifungal and anti-cancer activity. The present study is performed to determine the activity of Selaginella Bryopteris belongs to family Selaginellaceae against Salmonella Typhi (Non-pathogenic strain). The activity is done by using methanolic extract of Selaginella Bryopteris against standard strain, Salmonella Typhi (Non-pathogenic strain). The testing is done by agar cup plate method. The zone of inhibition of methanolic extract of Selaginella Bryopteris is compared with methanol blank as a standard. The 50mg/ml methanolic extract of Selaginella Bryopteris shows maximum inhibition (7mm) whereas the blank methanol does not show any kind of inhibition.

Synthesis, Biological Evaluation and In-silico Studies of 3-((4-(6-(Substitutedphenyl)-2-Mercaptopyrimidin-4-Yl) Phenyl) Imino)- 1-((Dimethylamino) Methyl) Indolin-2-One

A novel isatin and pyrimidine prototype derivatives 3-((4-(6-(substitutedphenyl)-2-mercaptopyrimidin-4-yl)phenyl)imino)- 1-((dimethylamino)methyl)indolin-2-one were synthesized and designed from the intermediate chalcones. The produced components were characterized, anti-tubercular and antimicrobial screening was done by agar dilution and agar-cup plate methods, respectively. From the studies, it was revealed that derivatives 5e, 5h and 5i showed increased potency. Further in-silico studies were carried out by molecular docking with the interaction of target components 5a-5j within the Mycobacterium tuberculosis enoyl-acp reductase enzyme (1ZID), drug likeness, and pharmacokinetic parameters were measured by osiris property explorer and molinspiration online toolkit respectively.

Formulation of mucoadhesive mouth paint for oral infections

Oral mucoadhesive mouth paint preparation was designed and prepared for the treatment of oral candidiasis, where prolonged drug release at the infected area is essential. Fluconazole, a recent triazole derivative having antifungal activity is chosen as the desired drug in this study to formulate mucoadhesive mouth paint. Oral candidiasis is a common infection in debilated patients, AIDS patients and in persons who administer immunosuppressive drugs. Mouth paints containing 1% fluconazole with hydrophilic polymer HPMC was prepared and compared with mouth paint prepared without the addition of hydrophilic polymer. The prepared mouth paint formulation was subjected to various evaluation parameters like pH determination, drug content, rheological behavior, mucoadhesive studies, spreadability and IR spectral analysis. In vitro drug release studies were carried out at salivary pH 6.4 using cellophane membrane as barrier. Stability studies were carried out at different temperature conditions like ambient temp (R. T.), 8 ± 1oC, 45 ± 2oC at 75% ± 5% R. H. (accelerated temperature) 3 months and analyzed at different time intervals for drug content, physical appearance, pH, mucoadhesive strength and spreadability and the prepared formulation was found to be stable. Antimicrobial studies were carried out to ascertain the antifungal activity of prepared mucoadhesive formulation against the pure drug. The test organism Candida albicans was a clinical isolate obtained from a diseased patient suffering from oral Candidiasis. In vitro antifungal activity was evaluated using standard Agar cup-plate method by zone inhibitions studies. Formulations, containing HPMC showed good zone inhibition. In vivo oral mucosal skin irritancy tests were carried out using mucoadhesive formulation on lab experimental animals (Rabbits and Guinea-pigs) and on healthy human volunteers. No edema, erythema, inflammation or redness in the mucosal cavity of both animals and human volunteers were observed.

Preliminary physico – phytochemical and phytocognostical evaluation of the leaves parts and evaluation of herbal ointment using leaves of Achyranthes aspera L. Leaf extract

Herbal plants are huge sources of neutraceuticals, prevent the different disease or maintain healthy life. Plant produces primary metabolites for their basic survival and secondary metabolites for their ecological, taxonomical and biochemical differentiation and diversity. Achyranthes aspera L. (Family Amaranthaceae) are broadly used in traditional system of medicine throughout different part of India, South Andaman Island, Pacific Island, Baluchistan, Tropical Asia, America, and Australia. It has great medicinal importance like to stomach tonic, diuretic, laxative, anthelmintic, anti hyperlipidemic, expectorant, anti-inflammatory, anti-bacterial, anti-fungal, hypoglycemic, anti-asthmatic and anti-allergic etc. The study of diseases and their treatment are important part of our ancient time worldwide. The knowledge of medicinal plants must have been accumulated in the course of many centuries. Herbal medicine prepare different part of plant are used. Herbal drug is design as the alternative formulation for the external use in the form of ointment. For the clinical use the herbal ointment apply externally on human body. The main aims of this research are Preliminary physico–phytochemical & phytocognostical evaluation of the leaves parts and preparation of herbal ointment from the Achyranthes aspera. Achyranthes aspera L. plants used as antibacterial activity. Under this research work, it is design as herbal ointment with the help of Ethanolic extract of Achyranthes aspera and determines the anti-bacterial capacity on it. In vitro study the antibacterial activity of the Ethanolic extracts of dried leaves of Achyranthes aspera L. are determine by using the Agar cup plate method versus different bacteria such as Staphylococcus aureus, Bacillus subtilis, Escherichia coli and Pseudomonas aeruginosa etc. By blending the Ethanolic extract of Achyranthes aspera L. (10 % w/w) into aqueous cream we formulated herbal ointment. The emulsifying agent and simple ointment bases are added in above herbal ointment for increase the antibacterial effectiveness during in vitro evaluation. The current study deals with the characterization of morphological features, determination of physical constant such as the total cash value, water soluble ash value were 11.25%, 5.25% respectively. Loss of weight drying was 12.9%, foaming index>100, swelling index were1.5cm, the percent yield for petroleum ether 5.25%, chloroform 6.34%, ethanol 7.65%, and aqueous 8.35%, and determination of formulation and evaluation of herbal ointment using Achyranthes aspera L. leave extract.

Secondary Metabolite Variation and Bioactivities of Two Marine Aspergillus Strains in Static Co-Culture Investigated by Molecular Network Analysis and Multiple Database Mining Based on LC-PDA-MS/MS.

Co-culture is known as an efficient way to explore the metabolic potential of fungal strains for new antibiotics and other therapeutic agents that could counter emerging health issues. To study the effect of co-culture on the secondary metabolites and bioactivities of two marine strains, Aspergillus terreus C23-3 and Aspergillus. unguis DLEP2008001, they were co-cultured in live or inactivated forms successively or simultaneously. The mycelial morphology and high-performance thin layer chromatography (HPTLC) including bioautography of the fermentation extracts were recorded. Furthermore, the agar cup-plate method was used to compare the antimicrobial activity of the extracts. Based on the above, liquid chromatography-photodiode array-tandem mass spectrometry (LC-PDA-MS/MS) together with Global Natural Products Social molecular networking (GNPS) and multiple natural products database mining were used to further analyze their secondary metabolite variations. The comprehensive results showed the following trends: (1) The strain first inoculated will strongly inhibit the growth and metabolism of the latter inoculated one; (2) Autoclaved A. unguis exerted a strong inducing effect on later inoculated A. terreus, while the autoclaved A. terreus showed high stability of its metabolites and still potently suppressed the growth and metabolism of A. unguis; (3) When the two strains are inoculated simultaneously, they both grow and produce metabolites; however, the A. terreus seemed to be more strongly induced by live A. unguis and this inducing effect surpassed that of the autoclaved A. unguis. Under some of the conditions, the extracts showed higher antimicrobial activity than the axenic cultures. Totally, A. unguis was negative in response but potent in stimulating its rival while A. terreus had the opposite effect. Fifteen MS detectable and/or UV active peaks showed different yields in co-cultures vs. the corresponding axenic culture. GNPS analysis assisted by multiple natural products databases mining (PubChem, Dictionary of Natural Products, NPASS, etc.) gave reasonable annotations for some of these peaks, including antimicrobial compounds such as unguisin A, lovastatin, and nidulin. However, some of the peaks were correlated with antagonistic properties and remain as possible novel compounds without mass or UV matching hits from any database. It is intriguing that the two strains both synthesize chemical ‘weapons’ for antagonism, and that these are upregulated when needed in competitive co-culture environment. At the same time, compounds not useful in this antagonistic setting are downregulated in their expression. Some of the natural products produced during antagonism are unknown chlorinated metabolites and deserve further study for their antimicrobial properties. In summary, this study disclosed the different responses of two Aspergillus strains in co-culture, revealed their metabolic variation, and displayed new opportunities for antibiotic discovery.

Lysinibacillus Isolate MK212927: A Natural Producer of Allylamine Antifungal 'Terbinafine'.

Resistance to antifungal agents represents a major clinical challenge, leading to high morbidity and mortality rates, especially in immunocompromised patients. In this study, we screened soil bacterial isolates for the capability of producing metabolites with antifungal activities via the cross-streak and agar cup-plate methods. One isolate, coded S6, showed observable antifungal activity against Candida (C.) albicans ATCC 10231 and Aspergillus (A.) niger clinical isolate. This strain was identified using a combined approach of phenotypic and molecular techniques as Lysinibacillus sp. MK212927. The purified metabolite displayed fungicidal activity, reserved its activity in a relatively wide range of temperatures (up to 60 °C) and pH values (6–7.8) and was stable in the presence of various enzymes and detergents. As compared to fluconazole, miconazole and Lamisil, the minimum inhibitory concentration of the metabolite that showed 90% inhibition of the growth (MIC90) was equivalent to that of Lamisil, half of miconazole and one fourth of fluconazole. Using different spectroscopic techniques such as FTIR, UV spectroscopy, 1D NMR and 2D NMR techniques, the purified metabolite was identified as terbinafine, an allylamine antifungal agent. It is deemed necessary to note that this is the first report of terbinafine production by Lysinibacillus sp. MK212927, a fast-growing microbial source, with relatively high yield and that is subject to potential optimization for industrial production capabilities.

Formulation and evaluation of herbal ointment using leaves of Thuja orientalis l. Leaf extract

The study of diseases and their treatment are important part of our ancient time worldwide. The knowledge of medicinal plants must have been accumulated in the course of many centuries. Herbal plants are huge sources of neutraceuticals, prevent the different disease or maintain healthy life. Plant produces primary metabolites for their basic survival and secondary metabolites for their ecological, taxonomical and biochemical differentiation and diversity. Herbal medicine prepare different part of plant are used. Herbal drug is design as the alternative formulation for the external use in the form of ointment. For the clinical use the herbal ointment apply externally on human body. The main aims of this research are preparation of herbal ointment from the Thuja orientalis L.Plants used as antibacterial activity. Under this research work, it is design as herbal ointment with the help of Ethanolic extract of Thuja orientalis L. and determines the anti bacterial capacity on it. In vitro study the antibacterial activity of the Ethanolic extracts of dried leaves of Thuja orientalis L. are determine by using the Agar cup plate method versus different bacteria such as Staphylococcus aureus, Bacillus subtilis, Escherichia coli and Pseudomonas aeruginosa etc. By blending the Ethanolic extract of Thuja orientalis L.(10 % w/w) into aqueous cream we formulated herbal ointment. The emulsifying agent and simple ointment bases are added in above herbal ointment for increase the antibacterial effectiveness during in vitro evaluation. Thuja orientalis L. (Family Cupressaceae) are broadly used in traditional system of medicine throughout different part of India, China, Russia, Korea, Japan, India, Florida and Iran. It is used in the treatment of diarrhea, cough, cold, bronchitis, and upper part repertory infection. The current study deals with the determination of formulation and evaluation of herbal ointment using Thuja orientalis leave extract.

In vitro characterization of antimicrobial activity of an endophytic bacterium Enterobacter cloacae (MG001451) isolated from Ocimum sanctum

Enterobacter cloacae (MG001451) isolated from surface-sterilized parts of Ocimum sanctum showed potent antimicrobial activities against six bacterial human pathogens (Staphylococcus aureus, Escherichia coli, Bacillus subtilis, Klebsiella pneumonia, Salmonella enterica, Pseudomonas aeruginosa), one bacterial phytopathogen (Xanthomonas oryzae) and two fungal phytopathogens (Pythium debaryanum and Rhizoctonia solani). The antibacterial activities were studied through Disc diffusion, Bacteriocin Like Inhibition Studies BLIS and Agar cup plate method and confirmed through Thin Layer Chromatography (TLC)-Bioautography. The Minimum Inhibitory Concentration (MIC) value of the extract of E. cloacae against the bacterial test organisms ranged from 0.39–12.5 mg/ml. Lower MIC and Minimum Microbicidal Concentration (MMC) values were found against Bacillus subtilis followed by Staphylococcus aureus. The isolate E. cloacae also inhibited the growth of Rhizoctonia solani and Pythium debaryanum, while studied through, dual culture and well plate assay method. Higher inhibition % was reported against Rhizoctonia solani(73.75 ± 2.5%) than Pythium debaryanum (60.24 ± 2.08%). Secondary metabolites like alkaloids, phenols, polychlorinated biphenyls, aromatic hydrocarbons, esters, etc. were identified in the extract through Gas Chromatography coupled Mass Spectrometry (GC-MS), which could be responsible for antimicrobial activities as observed during the investigation.

PHOTO EFFECT AND BIO-AUTOGRAPHIC STUDIES OF INTRACELLULAR ORANGE FLUORESCENT PIGMENT PRODUCED BY Bacillus endophyticus

Present study has focused on the effect of chemical (solvents) and physical (photo) conditions on pigment production and its bioactivity of intracellular orange fluorescent pigment (IOFP) extracted from soil bacterium Bacillus endophyticus. Standardization of pigment and its colour stability was confirmed by using different solvents (70% & 100% ethanol, hexane, heptane, ethyl acetate, acetone, petroleum ether, chloroform, methanol and distilled water), photo conditions (Dark, U.V light and White light) on pigment production and its bio-activeness by antibacterial activity using agar cup plate method against gram-positive (Staphylococcus aureus, streptococcus pyogenes and Listeria monocytogenes) and gram-negative (Salmonella typhi, Vibrio cholera, Shigella Flexneri and E.coli) human pathogens and purification of pigment by TLC coupled with bio-autographic studies. Acetone is proved to be the best solvent for extraction and the pigment was stable in all solvents without changing its colour except heptane. When compared to control (dark incubation) antibacterial activity of IOFP produced in U.V and W. Light was effective against all tested pathogens with slight differences in their antibacterial activity. TLC bio-autographic studies reveal that the separated pure band shows clear zone of inhibition under red back ground of live cells stating that, the compound is active against human bacterial pathogens. Hence this study concludes that, the production and biological activity of the IOFP was independent of light incubation, and TLC guided bio-autographic approach offers a rapid detection technique that avoids the testing of purified fraction once again.

Antibacterial Performance of a Streptomyces spectabilis Strain Producing Metacycloprodigiosin.

After separation of bacterial colonies on solid plates, purification, and screening through the agar cup-plate method, an antibiotic-resistant bacterial isolate was obtained, and named strain L20190601, the 16S rRNA gene sequence data of strain L20190601 to GenBank, NCBI have provided GenBank accession number MW931615. 16S rRNA gene sequencing revealed that this isolate was highly similar to a number of Streptomyces species. Among them, the homology with S. spectabilis was the highest, reaching 99.9, together with curved hyphal morphology and biochemical tests, allowed us to identify strain L20190601 as S. spectabilis. The red pigment produced by S. spectabilis strain L20190601 was structurally identified. An acid-base color reaction assay showed that when this pigment was dissolved in a solution at pH 3.0 and 9.0, the color of the solution was red and yellow, respectively. In addition, the analysis of absorption spectra revealed that at pH 8.0 and 3.0, the maximum absorption peaks were at 466 and 531nm, respectively. These results are consistent with the spectral absorption characteristics of metacycloprodigiosin reported in the literature. Moreover, the retention time of purified pigments was identical to those of standard metacycloprodigiosin solutions. Mass spectrometry analysis revealed that the molecular weight of the red compound was 392.2 [M + H]+. Finally, metacycloprodigiosin was found to be effective against eight clinically common pathogens: Staphylococcus aureus, Bacillus subtilis, Escherichia coli, Streptococcus pyogenes, Pseudomonas aeruginosa, Bacillus typhi, Candida albicans, and Trichophyton rubrum. In summary, metacycloprodigiosin exhibited strong antibacterial activity and a broad antibacterial spectrum, and thus is a promising compound for the development of a new type of antibacterial drug.

Formulation and evaluation of herbal ointment using leaves of Acacia nilotica (L.) Delile extract

Diseases have co-existed with life, the study of diseases and their treatment is important part of our ancient plant worldwide. Herbal plants are wonderful origin of traditional & modern medicine, useful for primary health care system. Herbal medicine prepare various part of plant are used. Instead off an herbal drug is design as the alternative formulation for the external use in the form of ointment. For the medicinal use the herbal ointment apply externally on human body. The main aims of this research are preparation of herbal ointment from the Acacia nilotica (L.) Delile plants the antibacterial activity. Under this research work, it is design as herbal ointment with the help of ethanolic extract of Acacia nilotica (L.) Delile determines the anti-bacterial capacity on it. In vitro study the antibacterial activity of the ethanolic extracts of dried leaves of Acacia nilotica (L.) Delile are determine by using the Agar cup plate method versus different bacteria such as Staphylococcus aureus, Bacillus subtilis, Escherichia coli and Pseudomonas aeruginosa etc. By blending the ethanolic extract of Acacia nilotica (L.) Delile (10 % w/w) into aqueous cream we formulated herbal ointment. The emulsifying agent and simple ointment bases are added in above herbal ointment for increase the antibacterial effectiveness during in vitro evaluation. Acacia nilotica (Family Leguminosae) are broadly used in traditional system of medicine throughout different part of India, Africa & America. It is used in the treatment of diarrhea, dysentery, cough, tuberculosis and leprosy. The current study deals with the determination of formulation and evaluation of herbal ointment using Acacia nilotica (L.) leave extract.

Formulation and evaluation of herbal ointment using Emblica officinalis extract

Herbal medicine prepare various part of plant are used like flower, leaves, seeds, root etc. Instead off an herbal drug is design as the alternative formulation for the external use in the form of ointment. For the medicinal use the herbal ointment apply externally on human body. The main aims of this research are preparation of herbal ointment from the Emblica officinalis plants the antibacterial activity. Under this research work, it is design as herbal ointment with the help of methanolic extract of Emblica officinalis and determines the anti-bacterial capacity on it. In vitro study the antibacterial activity of the methanolic extracts of dried leaves of Emblica officinalis are determine by using the Agar cup plate method versus different bacteria such as Staphylococcus aureus, Bacillus subtilis, Escherichia coli and Pseudomonas aeruginosa etc. By blending the methanolic extract of Emblica officinalis (10 % w/w) into aqueous cream we formulated herbal ointment. The emulsifying agent and simple ointment bases are added in above herbal ointment for increase the antibacterial effectiveness during in vitro evaluation. The herbal ointment is also better in comparison to a commercial brand of Gentamicin ointment. Emblica officinalis (Family Euphorbiaceae) are broadly used in traditional system of medicine throughout different part of India. It is used in the treatment of cold, anemia, dysentery, fever, gravel, sores. It is very important to standardize the plant part pharmacognostically for its utilization in different formulation. The current study deals with the determination of formulation and evaluation of herbal ointment using Emblica officinalis extract.

Synthesis, Characterization and in vitro Antimicrobial Evaluation of Pyrazole Based Oxothiazolidine Hybrids

In this work, pyrazole based oxothiazolidine hybrids, 4-{4-[2-(1-phenyl-3-(substituted)phenyl-1H-pyrazol-4-yl)-4-oxo-thiazolidin-3-yl]-phenyl}-morpholin-3-one (11a-l) were synthesized using molecular hybridization approach through Vilsmeier-Haack reaction. The titled compounds 11a-l were characterized by elemental analysis, IR, 1H NMR and mass spectral studies. The antibacterial activity of 11a-l was evaluated in vitro by agar cup plate method against B. cocous, B. subtillis, E. coli and P. vulgaris. The antifungal activity of compounds 11a-l was evaluated in vitro by agar based disk diffusion method against A. niger. The results of antibacterial and antifungal evaluation were reported in terms of zone of inhibition measured in mm. The synthesized compounds 11a-l exhibited moderate to good antibacterial and antifungal potential. Compound 4-{4-[2-(1-phenyl-3-(2-methoxyphenyl)phenyl-1H-pyrazol-4-yl)-4-oxo-thiazolidin-3-yl]-phenyl}-morpholin-3-one (11h) emerged as a most potent antimicrobial agent displaying zone of inhibition 21, 20, 21, 24 and 20 mm against B. cocous, B. subtillis, E. coli, P. vulgaris and A. niger, respectively.

Molecular Docking-Guided Ungual Drug-Delivery Design for Amelioration of Onychomycosis.

The present work envisaged an adherent luliconazole-loaded bilayer nail lacquer (BNL) with significant transungual activity. The locally applied sustained-release BNL formulation was designed for an improved retention, payload, and final dermatokinetic disposition. A primary step in the fabrication of a BNL included overcoming of physical barriers like α-keratin (also α-keratin), a protein present in human nails, and then allowing the drug molecule to permeate at the site of action. Although luliconazole is an established antifungal agent, has limited clinical exploitation for its use in treating onychomycosis. An in silico study elucidating its interaction with lanosterol-14-α demethylase, an enzyme which is the key region of drug action mechanism, was highly supportive of its imminent clinical potential. Optimization of prepared BNL formulations via response surface modeling (Box–Behnken Design-Expert 10.0.6) logically ascertained the effect of selected independent variables and showcased its effect via dependent responses. Surface morphology of the prepared BNL films was well corroborated for the presence of two distinct polymeric layers through scanning electron microscopy imaging. Nail permeation studies revealed a cumulative drug release of 71.25 ± 0.11% through bovine hooves up to 24 h. Luliconazole while exposing antifungal activity against clinical isolates of Trichophyton rubrum in agar cup-plate method disclosed a 38 mm diameter zone of inhibition. Further, the optimized BNL exhibited a bioadhesive force of 1.9 ± 0.11 N, which assured its retention on the nail surface for prolonged duration of time. In Conclusion, it is deduced that the conventional treatment modalities for onychomycosis require circumvention of certain pharmacotechnical caveats. Therefore, in the present study, a multipronged BNL system was proposed, which negates the need of frequent drug application, improvises cosmetic appearance, yields fruitful therapeutic outcomes, and has a clinical supremacy over the available therapeutics.

Synthesis, antimicrobial activity, pharmacophore modeling and molecular docking studies of new pyrazole-dimedone hybrid architectures

BackgroundDesign and synthesis of pyrazole-dimedone derivatives were described by one-pot multicomponent reaction as new antimicrobial agents. These new molecular framework were synthesized in high yields with a broad substrate scope under benign conditions mediated by diethylamine (NHEt2). The molecular structures of the synthesized compounds were assigned based on different spectroscopic techniques (1H-NMR, 13C-NMR, IR, MS, and CHN).ResultsThe synthesized compounds were evaluated for their antibacterial and antifungal activities against S. aureus ATCC 29213, E. faecalis ATCC29212, B. subtilis ATCC 10400, and C. albicans ATCC 2091 using agar Cup plate method. Compound 4b exhibited the best activity against B. subtilis and E. faecalis with MIC = 16 µg/L. Compounds 4e and 4l exhibited the best activity against S. aureus with MIC = 16 µg/L. Compound 4k exhibited the best activity against B. subtilis with MIC = 8 µg/L. Compounds 4o was the most active compounds against C. albicans with MIC = 4 µg/L.ConclusionIn-silico predictions were utilized to investigate the structure activity relationship of all the newly synthesized antimicrobial compounds. In this regard, a ligand-based pharmacophore model was developed highlighting the key features required for general antimicrobial activity. While the molecular docking was carried out to predict the most probable inhibition and binding mechanisms of these antibacterial and antifungal agents using the MOE docking suite against few reported target proteins.

Investigation on solution-to-gel characteristic of thermosensitive and mucoadhesive biopolymers for the development of moxifloxacin-loaded sustained release periodontal in situ gels.

The objectives of present research were to develop and characterize thermosensitive and mucoadhesive polymer-based sustained release moxifloxacin in situ gels for the treatment of periodontal diseases. Poloxamer- and chitosan-based in situ gels are in liquid form at room temperature and transform into gel once administered into periodontal pocket due to raise in temperature to 37°C. Besides solution-to-gel characteristic of polymers, their mucoadhesive nature aids the gel to adhere to mucosa in periodontal pocket for prolonged time and releases the drug in sustained manner. These formulations were prepared using cold method and evaluated for pH, solution-gel temperature, syringeability and viscosity. In vitro drug release studies were conducted using dialysis membrane at 37°C and 50rpm. Antimicrobial studies carried out against Aggregatibacter actinomycetemcomitans (A.A.) and Streptococcus mutans (S. Mutans) using agar cup-plate method. The prepared formulations were clear and pH was at 7.01-7.40. The viscosity of formulations was found to be satisfactory. Among the all, formulations comprising of 21% poloxamer 407 and 2% poloxamer 188 (P5) and in combination with 0.5% HPMC (P6) as well as 2% chitosan and 70% β-glycerophosphate (C6) demonstrated an ideal gelation temperature (33-37°C) and sustained the drug release for 8h. Formulations P6 and C6 showed promising antimicrobial efficacy with zone of inhibition of 27mm for A.A. and 55mm for S. Mutans. The developed sustained release in situ gel formulations could enhance patient's compliance by reducing the dosing frequency and also act as an alternative treatment to curb periodontitis.

Design, synthesis, molecular docking studies and anti-microbial activity of novel 1,2,3,4-tetrahydrocarbazole derivatives

The heterocyclic compounds naming tetrahydrocarbazoles having the significant biological properties. The newly substituted tetrahydrocarbazole derivatives were prepared from substituted phenylhydrazine and cyclohexanone in glacial acetic acid under reflux. These intermediates on reaction with substituted aromatic acid chlorides in alkaline media finally converted to N-Substituted tetrahydrocarbazoles. Fifteen compounds are synthesized and characterized by their melting point (MP), IR, NMR, MS and elemental analysis. All the compounds were subjected to molecular docking studies for Gln-6-p enzyme (1XFF) inhibition. The results of in silico molecular docking showed that all the derivates have significant binding energies, good affinity with active pocket and it may be reflected as a good inhibitor of GlcN-6-P synthase. The anti-microbial activity was assessed by agar cup plate method and the result showed 8 compounds having the better anti-microbial response against the bacterial and fungal strains. In conclusion, the study helps to give the greater scope of developing these tetrahydrocarbazoles derivatives which help to promote the effective anti-bacterial agents.Padmavathi and Tajne, International Current Pharmaceutical Journal, August 2016, 5(9): 73-78http://www.icpjonline.com/documents/Vol5Issue9/01.pdf

Large Scale Screening of Ethnomedicinal Plants for Identification of Potential Antibacterial Compounds.

The global burden of bacterial infections is very high and has been exacerbated by increasing resistance to multiple antibiotics. Antibiotic resistance leads to failed treatment of infections, which can ultimately lead to death. To overcome antibiotic resistance, it is necessary to identify new antibacterial agents. In this study, a total of 662 plant extracts (diverse parts) from 222 plant species (82 families, 177 genera) were screened for antibacterial activity using the agar cup plate method. The aqueous and methanolic extracts were prepared from diverse plant parts and screened against eight bacterial (two Gram-positive and six Gram-negative) species, most of which are involved in common infections with multiple antibiotic resistance. The methanolic extracts of several plants were shown to have zones of inhibition ≥ 12 mm against both Gram-positive and Gram-negative bacteria. The minimum inhibitory concentration was calculated only with methanolic extracts of selected plants, those showed zone of inhibition ≥ 12 mm against both Gram-positive and Gram-negative bacteria. Several extracts had minimum inhibitory concentration ≤ 1 mg/mL. Specifically Adhatoda vasica, Ageratum conyzoides, Alangium salvifolium, Alpinia galanga, Andrographis paniculata, Anogeissus latifolia, Annona squamosa, A. reticulate, Azadirachta indica, Buchanania lanzan, Cassia fistula, Celastrus paniculatus, Centella asiatica, Clausena excavate, Cleome viscosa, Cleistanthus collinus, Clerodendrum indicum, Croton roxburghii, Diospyros melanoxylon, Eleutherine bulbosa, Erycibe paniculata, Eryngium foetidum, Garcinia cowa, Helicteres isora, Hemidesmus indicus, Holarrhena antidysenterica, Lannea coromandelica, Millettia extensa, Mimusops elengi, Nyctanthes arbor-tristis, Oroxylum indicum, Paederia foetida, Pterospermum acerifolium, Punica granatum, Semecarpus anacardium, Spondias pinnata, Terminalia alata and Vitex negundo were shown to have significant antimicrobial activity. The species listed here were shown to have anti-infective activity against both Gram-positive and Gram-negative bacteria. These results may serve as a guide for selecting plant species that could yield the highest probability of finding promising compounds responsible for the antibacterial activities against a broad spectrum of bacterial species. Further investigation of the phytochemicals from these plants will help to identify the lead compounds for drug discovery.