Marine fungi are a promising source for bioactive compounds [1]. The fungal strain 222 has been isolated from wood collected at the coast of the Greifswalder Bodden, Baltic Sea, Germany and produces structurally new naphthalenone derivatives, balticols A to F. They possess antiviral activities [2]. Since other naphthalene compounds are known for their anti-inflammatory activities we investigated whether the balticols have an influence on inflammatory immune cells. Balticols (1 and 10µg/ml) were added to rat mononuclear cells (F344-MNC) which were cultured alone or together with H9c2-cardiomyocytes. The latter represents a model of inflammation similar as observed after myocardial infarction. MNC's were collected after 48h and analyzed for T-, B-, NK-, TH-cells and CTL's by flow cytometry. Dexamethasone (Dexa, 10–9 mol/l) served as positive control. None of the balticols except balticol E changed the number of control MNC's. The proportion of T-cells was decreased by balticol B and D, but ICAM-1+T-cells increased. Balticol D decreased TH- and increased B-cells as Dexa which additionally decreased CTL's. None of the substances influenced NK cells. After co-culture with cardiomyocytes TH-cells were decreased while CTL's and ICAM-1+T-cells increased. Balticol D partly anticipated the decrease of TH. Balticol E decreased T-cells, especially TH-cells, but stimulated ICAM-1+T-cells. Dexa anticipated the increase of CTL's, had no influence on the proportion of TH-cells and diminished ICAM-1+T-cells. In summary, balticols B, D and E influence unstimulated MNC's. Unambiguous anti-inflammatory effects were detected using Dexa and balticol E which exerts its effect due reduction of T-cells. arabic 14 English 83
B. Haertel, Muftah A. Shushni, Ulrike Lindequist(1-2010)

Because of the evolving resistance of microorganisms against existing antibiotics, there is an increasing need for new ones, not only in human, but also in veterinary medicine. The dichloromethane extract of a fungal strain of the genus Lophiostoma, isolated from driftwood collected from the coast of the Baltic Sea, displayed antibacterial activity against some fish pathogenic bacteria. Ergosterol epoxide (1), cerebroside C (2) and oxasetin (3) were isolated from the extract and structurally elucidated on the basis of spectroscopic data and chemical evidence. Compound 3 exhibited in vitro activity against Vibrio anguillarum, Flexibacter maritimus and Pseudomonas anguilliseptica with minimal inhibitory concentrations of 12.5, 12.5 and 6.25 microg/mL, respectively. Molecular docking studies were performed to understand the interaction of compound 3 with different macromolecular targets. Analysis of in silico results, together with experimental findings, validates the antimicrobial activity associated with compound 3. These results may be exploited in lead optimization and development of potent antibacterial agents. arabic 23 English 137
Muftah A Shushni, Faizul Azam, Ulrike Lindequist, (9-2013)

Paracetamol is one of the most widely used drug as antipyretic and analgesic for mild to moderate pain. Currently, paracetamol is the first-line choice for pain management and antipyresis. Ion channels are pore-forming proteins that allow the flow of ions across membranes and involved in many cellular processes; drugs acting on ion channels have long been used for the treatment of many diseases. Objective: To estimate the effect of voltage gated ion channel blockers on analgesic activity of Paracetamol and explore the interaction between ion channel blockers and paracetamol on pain behaviour. Materials and Methods: Male albino mice were used. The central antinociceptive activity was determined by hot plate test and formalin test (Phase I; neuropathic pain). Antiinflammatory activity was determined by formalin test (Phase II). Intraperitoneal injection was adopted. Five groups of mice were used. Group 1; control group (1% T80), group 2; treated with (200mg/kg) paracetamol, group 3; treated with different drugs of ion channel blockers, group 4; received standard drugs, Aspirin (200mg/kg) for formalin test (phase II) or tramadol (5mg/kg) for hot plate test and formalin test (phase I), group 5; received combined treatment of ion channel blockers and paracetamol. Results: Pain produced by noxious stimuli (heat and formalin) was significantly reduced by acute administration of paracetamol. Inflammation pain produced by formalin injection was significantly decreased by acute administration of paracetamol. Acute administration of nifedipine showed significant decrease in nociception and inflammation pain. Combined treatment of nifedipine and paracetamol produced antinociceptive and anti-inflammatory activity but less than the additive effect. Verapamil has no analgesic effect in the two models, and did not change the affect of paracetamol analgesic activity when administered together. Phenytoin produces significant decrease in nociceptive pain using hot plate but not in formalin test (Phase I), and produce significant decrease in inflammatory pain (Phase II). The combined treatment of phenytoin and paracetamol showed analgesic activity less than the additive effect. 4-Aminopyridine produces significant antinociceptive and anti-inflammatory activity. The combined administration of 4-aminopyridine and paracetamol showed analgesic activity, which is less than the additive effect using formalin test, while paracetamol analgesic activity is potentiated by 4-aminopyridine using hot plate test. Conclusion: Paracetamol has antinociception and anti-inflammatory activity on pain model used (Hot plate test and Formalin test). Ion channel blockers produce antinociception and anti-inflammatory activity. Verapamil has no effect on nociception or inflammation pain and no effect on paracetamol analgesic activity. Nifedipine, phenytoin and 4-aminopyridine interact with paracetamol producing less additive analgesic effect, except 4-aminopyridine in thermal stimuli (Hot plate) is more sensitive compared to chemical stimuli (formalin test – phase I), where potentiates paracetamol action.
هناء مدحت الزقلعي (2014)