Mohd. Akram

Antimicrobial Activity of Five Herbal Extracts Against Multi Drug Resistant (MDR) Strains of Bacteria and Fungus of Clinical Origin

Antimicrobial activities of the crude ethanolic extracts of five plants were screened against multidrug resistant (MDR) strains of Escherichia coli, Klebsiella pneumoniae and Candida albicans. ATCC strains of Streptococcus mutans, Staphylococcus aureus, Enterococcus faecalis, Streptococcus bovis, Pseudimonas aeruginosa, Salmonella typhimurium, Escherichia coli, Klebsiella pneumoniae and Candida albicans were also tested. The strains that showed resistance against the maximum number of antibiotics tested were selected for an antibacterial assay. The MDR strains were sensitive to the antimicrobial activity of Acacia nilotica, Syzygium aromaticum and Cinnamum zeylanicum, whereas they exhibited strong resistance to the extracts of Terminalia arjuna and Eucalyptus globulus. Community-acquired infections showed higher sensitivity than the nosocomial infections against these extracts. The most potent antimicrobial plant was A. nilotica (MIC range 9.75-313µg/ml), whereas other crude plant extracts studied in this report were found to exhibit higher MIC values than A. nilotica against community acquired as well as nosocomial infection. This study concludes that A. nilotica, C. zeylanicum and S. aromaticum can be used against multidrug resistant microbes causing nosocomial and community acquired infections.

Studies of mixed micelle formation between cationic gemini and cationic conventional surfactants

Mixed micellization of dimeric cationic surfactants tetramethylene-1,4-bis(hexadecyldimethylammonium bromide)(16-4-16), hexamethylene-1,6-bis(hexadecyldimethylammonium bromide) (16-6-16) with monomeric cationic surfactants hexadecyltrimethylammonium bromide (CTAB), cetylpyridinium bromide (CPB), cetylpyridinium chloride (CPC), and tetradecyltrimethylammonium bromide (TTAB) have been studied by conductivity and steady-state fluorescence quenching techniques. The behavior of mixed systems, their compositions, and activities of the components have been analyzed in the light of Rubinghs regular solution theory. The results indicate synergism in the binary mixtures. Ideal and experimental critical micelle concentrations (i.e., cmc(*) and cmc) show nonideality, which is confirmed by beta values and activity coefficients. The micelle aggregation numbers (N(agg)), evaluated using steady-state fluorescence quenching at a total concentration of 2 mM for CTAB/16-4-16 or 16-6-16 and 5 mM for TTAB/16-4-16 or 16-6-16 systems, indicate that the contribution of conventional surfactants was always more than that of the geminis. The micropolarity, dielectric constant and binding constants (K(sv)) of mixed systems have also been evaluated from the ratios of respective peak intensities (I(1)/I(3) or I(0)/I(1)).

Effect of gemini (alkanediyl-α,ω-bis(dimethylcetylammonium bromide)) (16-s-16, s = 4, 5, 6) surfactants on the interaction of ninhydrin with chromium-glycylphenylalanine

The effect of gemini (alkanediyl-α,ω-bis(dimethylcetylammonium bromide)) (16-s-16, s=4, 5, 6) surfactants on the interaction of ninhydrin with chromium(III) complex of glycylphenylalanine ([Cr(III)-Gly-Phe]2+) has been investigated using UV-visible spectrophotometer at different temperatures. The order of reaction with respect to [Cr(III)-Gly-Phe]2+ is unity while it is fractional with respect to ninhydrin. Whereas, the values of rate constant (kψ) increase and leveling-off regions, like conventional single chain cetyltrimethylammonium bromide (CTAB) surfactant, were observed with geminis, later produces a third region of increasing kψ at higher gemini surfactant concentrations. This unusual third-region effect of the gemini micelles is assigned to changes in their micellar morphologies. The results obtained in micellar media were treated in terms of pseudo-phase model. The values of thermodynamic parameters (Ea, ΔH# and ΔS#) and binding constants (KA and KNin) have been evaluated.

Interaction between dipeptide (glycyl-phenylalanine) and ninhydrin: role of CTAB and gemini (16-s-16, s=4, 5, 6) surfactant micelles.

The kinetics of interaction of dipeptide glycylphenylalanine (Gly-Phe) with ninhydrin have been studied by following the reaction spectrophotometrically at 70 °C and a particular pH 5.0 in the absence and presence of conventional cetyltrimethylammonium bromide (CTAB) and gemini (alkanediyl-α,ω-bis(dimethylhexadecylammonium bromide)) surfactants. The rate shows first- and fractional-order dependence on [Gly-Phe] and [ninhydrin], respectively. The surfactants were found to catalyse the reaction. Furthermore, whereas the typical rate constant (kΨ) increase and leveling-off regions are observed with geminis, just like as seen with conventional surfactants, the former produced a third region of increasing kΨ at higher concentrations. A kinetic rate law consistent with experimental results has been derived on the basis of the proposed mechanism.

Conductometric study of antidepressant drug–cationic surfactant mixed micelles in aqueous solution

Conductivity measurements have been carried out on aqueous solutions of two antidepressant drugs (nortriptyline hydrochloride and clomipramine hydrochloride) with four cationic surfactants (monomeric: cetyltrimethylammonium bromide, tetradecylammonium bromide; dimeric: 1,5-pentanediyl-alpha-omega-bis(hexadecyldimethylammonium bromide), 1,4-butanediyl-alpha,omega-bis(hexadecyldimethylammonium bromide) as well as with sodium chloride. Counterions from NaCl adsorb to the charged headgroup of the drug molecules and reduce the repulsion, hence cmc decreases. cmc values decreased with the addition of surfactants indicating mixed micelle formation. Experimental mole fraction of surfactants in micelle (X1) and their ideal values (X1 id) also support this explanation. Interaction parameter, beta, and excess free energy of micellization are negative suggesting synergism in mixed state. Activity coefficients are less than unity which means non-ideal mixing.

Micellar properties of a phenothiazine drug in presence of additives

In this study micellar properties of a phenothiazine drug, promazine hydrochloride, at different concentrations of NaCl and cationic surfactants (conventional as well as gemini surfactants) are presented. The parameters studied are cmc (critical micelle concentration), X1 (mole fraction of surfactant in micelles), f1, f2 (activity coefficients) and ΔGex (excess free energy). Cl− ions (from NaCl) get adsorbed on the micellar head groups and, by decreasing the repulsion among them, lower the cmc. Surfactants form mixed micelles with the drug and the values of X1, X1id (mole fraction of the surfactant in micelles in ideal state), interaction parameter β, f1 and f2 all suggest non-ideal but synergistic nature. The ΔGex values are negative indicating that the mixed state is more stable than the pure micelle state.

Tigecycline : A Critical Update

Abstract Tigecycline is the first Food and Drug Administration (FDA) approved glycylcycline antibiotic. It has shown remarkable in vitro activity against a wide variety of Gram-positive, Gram-negative and anaerobic bacteria including many multidrug resistant (MDR) strains. However, it has minimal activity against Pseudomonas aeruginosa and Proteus spp. To date, little resistance to tigecycline has been reported. Clinical trials studying complicated skin and skin-structure infections (cSSSIs) demonstrated that tigecycline has equivalent efficacy and safety compared with the combination of van-comycin and aztreonam. For complicated intra-abdominal infections (cIAIs), tigecycline was found to be as effective as imipenem/cilastatin. Adverse events related to tigecycline therapy, i.e. nausea and vomiting, were tolerable. Currently available data suggest that tigecycline may play an important role in the future as a monotherapy alternative to older broad-spectrum antibiotics, such as advanced generation cephalosporins, carbapenems, fluoroquinolones, piperacillin/tazobactam, and Gram-positive directed agents (e.g. daptomycin, linezolid and quinupristin/dalfopristin) for which resistance is being increasingly reported from all parts of the world.

Bio-physicochemical analysis of ethylene oxide-linked diester-functionalized green cationic gemini surfactants

A novel series of oxy-diester-functionalized gemini surfactants (Cm-E2O-Cm) was synthesized and the physicochemical parameters were evaluated by surface tension and steady-state fluorescence measurements. Negative values of Gibbs free energy change of adsorption and micellization indicate that adsorption and micellization of Cm-E2O-Cm gemini surfactants are spontaneous. These surfactants have lower Krafft points and thus better solubility. Besides, they exhibit excellent foam and micro-emulsion stability. Interestingly, these geminis show low cytotoxicity, as revealed by HC50 analysis. FT-IR spectra after alkaline treatment confirm their cleavable nature. Moreover, a fascinating feature of these geminis is their considerably high biodegradability. Thus, a comprehensive study of the synthesized gemini surfactants has been carried out that may be significant for potential applications in various fields, more specifically in biomedicine and cosmetics, where efficiency and safety are strictly connected.

Mixing Behavior of Conventional and Gemini Cationic Surfactants

Micellization behavior of cationic monomeric surfactants, hexadecyltrimethylammonium bromide (CTAB), cetylpyridinium bromide (CPB), cetylpyridinium chloride (CPC), tetradecyltrimethylammonium bromide (TTAB), and dimeric (gemini) cationic surfactant pentamethylene‐1, 5‐bis(hexadecyldimethylammonium bromide) with formula C16H33(CH3)2N+(CH2)5N+(CH3)2C16H33 · 2Br−, abbreviated as 16‐5‐16, in mixed states (binary) have been studied by conductivity. The micellar compositions, activities of the components, and their mutual interactions have been estimated from Rubinghs theory. The mixtures show nonideal behavior with favorable interactions.

Micellar and salt effects on the rate of the condensation between ninhydrin and [Cr(his)(H2O)3]2+

Abstract The rates of reaction between ninhydrin and [Cr(his)(H 2 O) 3 ] 2+ (his, histidine) have been determined in water and in micelles formed by the surfactants cetyltrimethylammonium bromide (CTAB; cationic), sodium dodecyl sulphate (SDS; anionic) and octylphenoxy polyethoxy ethanol (Triton X-100, TX-100; non-ionic) in the presence and absence of various salts at 80°C and pH 5.0. SDS micelles show no effect on the reaction rate but increase in the total concentration of CTAB from 0.0 to 20.0×10 −3 mol dm −3 results in an increase in the pseudo-first-order rate constant ( k ψ ) by a factor of ca. 3. The micellar catalysis is explained in terms of the pseudophase model of the micelles. CTAB micelles decrease the activation enthalpy and make the activation entropy less negative. At constant concentration of CTAB, the rate constant decreases with increase in concentration of added anions (bromide, chloride, sulphate and nitrate). The kinetic data have been used to calculate the micellar binding constants K S for [Cr(his)(H 2 O) 3 ] 2+ and K N for ninhydrin and the respective values are 28 and 73 mol −1 dm 3 at 80°C.