Biological and Sensing Applications of a Few 1,3,4-Oxadiazole Based Donor-Acceptor Systems.

1,3,4-Oxadiazole pharmacophore is still considered a viable biologically active scaffold for the synthesis of more effectual and broad-spectrum antimicrobial agents. Therefore, the present study is based on five 1,3,4-oxadiazole target structures, viz., CAROT, CAROP, CARON (D-A-D-A systems) and NOPON and BOPOB (D-A-D-A-D systems) bearing various bioactive heterocyclic moieties relevant to potential biological activities. Three of the compounds, CARON, NOPON and BOPOB were assessed in-vitro for their efficacy as antimicrobial agents against gram positive (Staphylococcus aureus and Bacillus cereus) and gram negative (Escherichia coli and Klebsiella pneumonia) bacteria; and two fungi, Aspergillus niger and Candida albicans; also, as an anti-tuberculosis agent against Mycobacterium tuberculosis. Most of the tested compounds displayed promising antimicrobial activity, especially CARON which was then analyzed for the minimum inhibitory concentration (MIC) studies. Similarly, NOPON portrayed the highest anti-TB activity among the studied compounds. Consequently, to justify the detected anti-TB activity of these compounds and to recognize the binding mode and important interactions between the compounds and the ligand binding site of the potential target, these compounds were docked into the active binding site of cytochrome P450 CYP121 enzyme of Mycobacterium tuberculosis, 3G5H. The docking results were in good agreement with the result of in-vitro studies. In addition, all the five compounds were tested for their cell viability and have been investigated for cell labeling applications. To conclude, one of the target compounds, CAROT was used for the selective recognition of cyanide ion by 'turn-off' fluorescent sensing technique. The entire sensing activity was examined by spectrofluorometric method and MALDI spectral studies. The limit of detection obtained was 0.14 µM.

Multi-functional bioactive secondary metabolites derived from endophytic fungi of marine algal origin.

Endophytic fungi from marine macroalgae are endowed with various pharmacologically active metabolites. This study mined, identified and screened endophytic fungi (EF) isolated from marine algae from the west coast of South India for screening anticancer, antioxidant and antimicrobial secondary metabolite producers. Five EF isolated from sampled marine algae were identified using morphology and ITS based identification as Grammothele fuligo, Rigidoporus vinctus, Cystobasidium minutum, Candida railenensis and Pichia kudriavzevii. After culturing 20 days on PDA medium, the ethyl acetate extracts of Cystobasidium minutum showed potent antimicrobial activity against P. aeruginosa with an IC50 value of 458.7 ± 1.021 µg/mL whereas Pichia kudriavzevii extracts showed promising antioxidant activity (IC50 value of 65.78 ± 1.082 µg/mL, 38.74 ± 1.040 µg/mL and 32.01 ± 1.018 µg/mL for DPPH assay, ABTS assay and FRAP assay respectively) and high cytotoxic activity against MG63 cell line (IC50 = 145.1 ± 1.086 µg/mL, no activity against U87 cells). The phytochemical screening of the extracts unveiled the existence of diverse groups of secondary metabolites. Further, Gas Chromatography Mass Spectroscopy (GC-MS) analysis of the extract revealed the presence of compounds that are known to be antibacterial, antioxidant and cytotoxic. These results indicate that marine derived endophytes could be potent sources for multi-functional bioactive compounds and may find prospective application in pharmaceutical industry.

Degradation-Dependent Controlled Delivery of Doxorubicin by Glyoxal Cross-Linked Magnetic and Porous Chitosan Microspheres.

Glyoxal cross-linked porous magnetic chitosan microspheres, GMS (∼170 µm size), with a tunable degradation profile were synthesized by a water-in-oil emulsion technique to accomplish controlled delivery of doxorubicin (DOX), a chemotherapeutic drug, to ensure prolonged chemotherapeutic effects. The GMS exhibit superparamagnetism with saturation magnetization, M s = 7.2 emu g-1. The in vitro swelling and degradation results demonstrate that a swelling plateau of GMS is reached at 24 h, while degradation can be modulated to begin at 96-120 h by formulating the cross-linked network using glyoxal. MTT assay, live/dead staining, and F-actin staining (actin/DAPI) validated the cytocompatibility of GMS, which further assured good drug loading capacity (35.8%). The release mechanism has two stages, initiated by diffusion-inspired release of DOX through the swollen polymer network (72 h), which is followed by a disintegration-tuned release profile (>96 h) conferring GMS a potential candidate for DOX delivery.

Radio frequency plasma assisted surface modification of Fe3O4 nanoparticles using polyaniline/polypyrrole for bioimaging and magnetic hyperthermia applications.

Surface modification of superparamagnetic Fe3O4 nanoparticles using polymers (polyaniline/polypyrrole) was done by radio frequency (r.f.) plasma polymerization technique and characterized by XRD, TEM, TG/DTA and VSM. Surface-passivated Fe3O4 nanoparticles with polymers were having spherical/rod-shaped structures with superparamagnetic properties. Broad visible photoluminescence emission bands were observed at 445 and 580 nm for polyaniline-coated Fe3O4 and at 488 nm for polypyrrole-coated Fe3O4. These samples exhibit good fluorescence emissions with L929 cellular assay and were non-toxic. Magnetic hyperthermia response of Fe3O4 and polymer (polyaniline/polypyrrole)-coated Fe3O4 was evaluated and all the samples exhibit hyperthermia activity in the range of 42-45 °C. Specific loss power (SLP) values of polyaniline and polypyrrole-coated Fe3O4 nanoparticles (5 and 10 mg/ml) exhibit a controlled heat generation with an increase in the magnetic field.

Correlation of Oxygenation and Radiographic Assessment of Lung Edema (RALE) Score to Lung Ultrasound Score (LUS) in Acute Respiratory Distress Syndrome (ARDS) Patients in the Intensive Care Unit.

BACKGROUND: Lung ultrasound score (LUS) as well as radiographic assessment of lung edema (RALE) score as calculated from chest radiography (CXR) have been applied to assess Acute Respiratory Distress Syndrome (ARDS) severity. CXRs, which are frequently performed in ARDS patients, pose a greater risk of radiation exposure to patients and health care staff. AIMS AND OBJECTIVES: The aim of the study was to evaluate if LUS had a better correlation to oxygenation (PaO2/FiO2) compared with the RALE score in ARDS patients. We also aimed to analyse if there was a correlation between RALE score and LUS. We wanted to determine the LUS and RALE score cut-off, which could predict a prolonged length of intensive care unit (ICU) stay (≥10 days) and survival. METHODS: Thirty-seven patients aged above 18 years with ARDS as per Berlin definition and admitted to the ICU were included in the study. It was a retrospective study done over a period of 11 months. On the day of admission to ICU, the global and basal LUS, global and basal RALE score, and PaO2 /FiO2 were recorded. Outcome and days of ICU stay were noted. RESULTS: Global LUS score and PaO2/FiO2 showed the best negative correlation (r = -0.491), which was significant (p = 0.002), followed by global RALE score and PaO2/FiO2 (r = -0.422, p = 0.009). Basal LUS and PaO2/FiO2 also had moderate negative correlation (r = -0.334, p = 0.043) followed by basal RALE score and PaO2/FiO2 (r = -0.34, p = 0.039). Global RALE score and global LUS did not show a significant correlation. Similarly, there was no significant correlation between basal RALE score and basal LUS. Global and basal LUS as well as global and basal RALE score were not beneficial in predicting either a prolonged length of ICU stay or survival as the area under curve was low. CONCLUSION: In ARDS patients, global LUS had the best correlation to oxygenation (PaO2/FiO2), followed by global RALE score. Basal LUS and basal RALE score also had moderate correlation to oxygenation. However, there was no significant correlation between global LUS and global RALE score as well as between basal LUS and basal RALE score. Global and basal LUS as well as global and basal RALE scores were not able to predict a prolonged ICU stay or survival in ARDS patients.