A new antibacterial pyridinoside from a Streptomyces species

A new compound, 8-propionate-2-β-(D+)-glucosyl-9,10-pyranopyridine, was isolated from the chloroform extract of a Streptomyces species. The structure of the compound was confirmed by spectroscopic techniques including UV, IR, HR-ESI-MS, 1H-NMR, 13C-NMR, 1H-1H COSY and HMBC (long range coupling) spectra. The compound showed significant antibacterial activity against Gram-positive bacteria. The minimum inhibitory concentrations (MIC) of the isolated compound against Bacillus megaterium, Streptococcus β-haemolyticus, Bacillus subtilis, Escherichia coli, Salmonella typhi and Shigella dysenteriae were found to be 0.16, 0.08, 0.08, 0.04, 0.08 and 0.08 μM, respectively.Colegio de Farmacéuticos de la Provincia de Buenos Aire

Analogues of Disulfides from Allium stipitatum demonstrate potent anti-tubercular activities through drug efflux pump and Biofilm inhibition

Disulfides from Allium stipitatum, commonly known as Persian shallot, were previously reported to possess antibacterial properties. Analogues of these compounds, produced by S-methylthiolation of appropriate thiols using S-methyl methanethiosulfonate, exhibited antimicrobial activity, with one compound inhibiting the growth of Mycobacterium tuberculosis at 17 µM (4 mg L-1) and other compounds inhibiting Escherichia coli and multi-drug-resistant (MDR) Staphylococcus aureus at concentrations ranging between 32-138 µM (8-32 mg L-1). These compounds also displayed moderate inhibitory effects on Klebsiella and Proteus species. Whole-cell phenotypic bioassays such as the spot-culture growth inhibition assay (SPOTi), drug efflux inhibition, biofilm inhibition and cytotoxicity assays were used to evaluate these compounds. Of particular note was their ability to inhibit mycobacterial drug efflux and biofilm formation, while maintaining a high selectivity towards M. tuberculosis H37Rv. These results suggest that methyl disulfides are novel scaffolds which could lead to the development of new drugs against tuberculosis (TB)

Studies on the physiochemical characteristics of Tremella extra-cellular polysaccharides

EThOS - Electronic Theses Online ServiceGBUnited Kingdo

Additive effect of lipid lowering drug (Simvastatin) in combination with antidiabetic drug (Glibenclamide) on alloxan induced diabetic rats with long term dyslipidemia

High blood glucose level, elevated level of liver enzyme, necrosis and shrinkage of islets of Langerhans has been implicated in the pathogenesis of type 2 diabetes. High blood glucose cause oxidative stress, production of free radical as well as elevated SGPT and SGOT level. Both glibenclamide and simvastatin in fixed dose used as antihyperglycemic antidyslipidemic and antioxidative agents for type 2 diabetes treatment. This study therefore aimed to evaluate the antihyperglycemic, antidyslipidemic and antioxidative effect of fixed dose combination of glibenclamide (0.6 mg/70 kg body weight) and simvastatin (5 mg/70 kg body weight) on long term alloxan induced diabetic rats with cardiovascular disease using various diagnostic kits as a parameter of phamacotherapeutic and pharmacological effect. The study was carried out using 96 Swiss Albino male rats weighing about 200-220 g. Combination therapy induced a significant decrease in blood glucose level in alloxan induced diabetic rats, from 33.75 ± 1.65 to 5.80 ± 0.07 mmol/l 2 h after last dose administration, after 4 weeks treatment. In case of dyslipidemic effect, combination therapy reduced total cholesterol (45 %), triglyceride (36 %) and low density lipoprotein-cholesterol (32 %) levels significantly and increased high density lipoprotein-cholesterol level (57 %) in comparison with their respective diabetic control groups. Results of this study showed that combination therapy effectively decreased SGPT (ALAT) (55 %) and SGOT (ASAT) (51 %) in comparison with diabetic control group. It was also observed that catalase and superoxide dismutase enzyme activity was increased by 58 and 91 % respectively in comparison with diabetic control group after 4 weeks treatment with combination of both drugs. In conclusion, these findings of combination therapy (glibenclamide and simvastatin) on alloxan induced diabetes in rats are significantly better than monotherapy using single drug. The results of the present study suggest that, combination of the fixed dose of glibenclamide and simvastatin might be efficacious in patients with diabetic dyslipidemia and increased oxidative stress. Furthermore, this combination therapy offer dosage convenience to the patients and by virtue of its dual mode of action might be a useful addition to the therapeutic armamentarium for patients with diabetic dyslipidemia and oxidative stress.10 page(s

Bioactive acetophenones from Plectranthus venteri

In a project to investigate the chemistry of South African Plectranthus species, from the dichloromethane extract of the aerial parts of Plectranthus venteri, we isolated two known natural product acetophenones, namely 2-hydroxy-3,4,5,6-tetramethoxy-acetophenone (1) and 2-hydroxy-4,5,6-trimethoxy-acetophenone (2). Structures were assigned using NMR spectroscopy and HRTOFESIMS. Compound 1 was previously synthesised as a precursor to the polymethoxylated flavone nobiletin. The acetophenones exhibited remarkable inhibitory activities against the transfer of the IncW plasmid R7K in a bacterial plasmid transfer inhibition assay

Antibacterial and antifungal activities of the constituents of flemingia paniculata

A salicylic acid derivative (1), a cinnamaldehyde (2), and six isoflavones (3-8) from the stem bark of Flemingia paniculata. Wall. (Leguminosae) were tested for antibacterial (both Gram-positive and Gram-negative) and antifungal activities. All the compounds showed significant activities against the test organisms having MIC values in the range of 1.57-200 μ g/mL. The highest potency (MIC = 1.57 μ g/mL) was exhibited by 3 against Staphylococcus aureus