Posted by admin on Jun 30, 2016 in |
Antimicrobial peptides (AMP) showed a broad spectrum of cytotoxic activity against cancer cells, which could provide a new class of anticancer drugs. In this study, we have evaluated the cytotoxic and apoptotic activity of magainin II, an AMP compared with 5-Fluorouracil (5-FU) in colo320 DM cancer cells, and magainin II cytotoxicity was assessed on vero cell line by MTT. The cells cultured in the presence or absence of magainin II and 5-FU. The magainin II inhibited cell viability in dose dependent manner was quantified by MTT assay. The IC50 of magainin II was found to be 89.3nM and at this concentration the cytotoxicity was not observed in vero cell line. The cytotoxicity of the magainin II was further confirmed by lactate dehydrogenase (LDH) assay and neutral red uptake assay (NRU). Apoptosis induction was verified by DNA fragmentation analysis. The morphological changes in colo 320 DM cells was measured by DAPI and acridine orange/ethidium bromide staining, showed nuclear condensation, and this substantiates the apoptotic action of magainin II. The cell...
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Posted by admin on Jun 30, 2016 in |
Lactobacillus plantarum culture supernatants (LAPS) have antimicrobial, pro‐healing and anesthetic properties, so our medical team applied whole cultures and LAPS in chronic wounds with encouraging results. Metabolites responsible for LAPS properties and its action mechanism were previously determined. Objective: to design methods and culture media to increase the production of LAPS metabolites and optimize it´s therapeutic effectiveness. Modifications in MRS broth composition were made and L. plantarum was cultivated in the resulting different media with different physicochemical conditions to obtain modified supernatants (LAPSm). Antimicrobial and anti-biofilm activity (crystal violet) of LAPSm on strains typically isolated from chronic wounds (Pseudomonas aeruginosa, Staphylococcus aureus, Staphylococcus epidermidis and Serratiamarcescens), was tested. Concentration of barbiturates in LAPSm was quantified by GCMS and its relative anesthetic potency in healthy volunteers was evaluated. DNAase and auto inducers type 2biological activity in LAPSm were quantified. In addition, a safety assessment of LAPSm application on healthy skin of 200 volunteers was performed. LAPSm obtained from media with high concentrations of yeast extract possessed the greatest anesthetic power....
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Posted by admin on Jun 30, 2016 in |
Azetidin-2-one analogues are reported to exhibit various pharmacological activities like cholesterol absorption inhibitory activity, human tryptase, thrombin and chymase inhibitory activity, vasopressin V1a antagonist activity, antidiabetic, anti-inflammatory, antiparkinsonian and anti-HIV activity in addition to antimicrobial.1-6 In the present study, Isoniazid (INH), the established antitubercular drug was selected as the lead for the design and development of antitubercular agents with minimal toxic effects. A novel series of amino azetidinones were designed from corresponding azetidin-2-ones using various in silico methods. Docking studies were performed at Mtb enoyl acp reductase (4DRE) and the derivatives exhibited best docking scores were prepared from corresponding azetidin-2-ones by treating with various molecules containing amino groups in the presence of TEA. Azetidin-2-ones in turn were obtained from a series of INH Schiff bases by reaction with chloro acetyl chloride. Structures of the newly synthesized compounds were assigned on the basis of elemental analysis, IR, 1H NMR, 13CNMR and mass spectral studies. The newly synthesized compounds were screened for their in vitro antitubercular activity using Alamar blue assay...
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Posted by admin on May 31, 2016 in |
Objective: The present work is aimed to screen phytochemicals, in vitro antimicrobial and antioxidant activity of the non polar and polar extracts of Acacia sinuata. Methods: Leaves of Acacia sinuata– were collected, dried and powdered. The powdered material is subjected to soxhlet extraction using various polar to non polar solvents and allowed for evaporation. The crude extracts thus obtained were used for further screening of phytochemicals, in vitro antimicrobial activity and antioxidant activities. Results: Phytochemical evaluation of Acacia sinuata proved that most of the secondary metabolites are extracted in polar solvents than non polar solvent like hexane. All the extracts of the Acacia sinuata possess significant amount of phenols and flavonoids and they also showed antimicrobial and antioxidant activity. Out of all the extracts of Acacia sinuata, methanol extracts showed better antibacterial, antifungal activity and antioxidant activity. Conclusion: The present work concluded that the methanol extract of Acacia sinuata was useful to develop new plant based dugs against various pathogenic bacteria as well as fungal...
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Posted by admin on May 31, 2016 in |
Diazonium salt of 2-(p-aminophenyl)-1,8-naphthyridine (I) was coupled with active methylene compounds to afford the hydrazono-1,8-napthyridinyl (III-V) and azo(VI) derivatives. Hydrazono ethyl acetoacetate (III) and ethyl cyanoacetate (IV) derivatives on treatment with hydrazine and substituted hydrazine’s were later reacted with hydroxylamine HCl in the presence of ethanol followed by cyclization to afford pyrazolinone (IIIa-e) & (IVa-e) and isoxazolinones (VII&IX). Hydrazono acetyl acetone (V) and azo dibenzoyl methane (VI) derivatives on treatment with hydrazine and substituted hydrazines, hydroxylamine HCl and with urea in the presence of ethanol followed by cylization resulted in the formation of pyrazoles (Va-e) & (VIa-e), isoxazole (IX&XI) and substituted pyrimidine-2-ones (X&XII). All the newly synthesized compounds were screened for their in-vitro antibacterial activity & antifungal activity by Agar cup-plate method and Serial dilution methods. In Agar cup plate method the Compounds IIId, IVd, VId showed Impressive antibacterial and antifungal activity. In Serial dilution method the compounds Vd & VId showed excellent antibacterial activity against B.Subtilis with an MIC of 7.8 µg/ml where as the compounds IVd, Vd...
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