Gene/Protein Disease Symptom Drug Enzyme Compound
Pivot Concepts:   Target Concepts:
Query: UNIPROT:P00750 (PLA)
 16,800 document(s) hit in 31,850,051 MEDLINE articles (0.00 seconds)

A methoxylated fatty acid that inhibits phospholipase A(2) (PLA(2); EC 3.1.1.4) was purified from the brown seaweed Ishige okamurae. Approximately 8.1 mg of the inhibitory compound, 7-methoxy-9-methylhexadeca-4,8-dienoic acid, was isolated from 1 kg of I. okamurae powder. Recombinant PLA(2) derived from the pathogenic bacterium Vibrio mimicus was used as the target enzyme. The methoxylated fatty acid compound competitively inhibited PLA(2) with a Ki value of 3.9 microg/mL. The concentrations required for 50% inhibition of PLA(2), oedema and erythema were 1.0 microg/mL, 3.6 mg/mL and 4.6 mg/mL, respectively. The compound strongly inhibited PLA(2) activity in vitro and had potent antiinflammatory activity in vivo.
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PMID:A methoxylated fatty acid isolated from the brown seaweed Ishige okamurae inhibits bacterial phospholipase A2. 1857 Feb 68

The effect of the vesicating agent sulfur mustard (SM) has been investigated in vitro using murine peritoneal macrophages. The rationale for this study was three-fold: (1) the first symptoms after exposure to SM are mucous and cutaneous erythema, itching and oedema suggesting that inflammatory cells may represent an early target of SM toxicity; (2) it has been proposed that macrophages and their secretory products may participate in the degradation of the dermal-epidermal junction; and (3) macrophages are important components of the immune system and any alteration of their metabolism may be relevant in clarifying the immune impairments caused by SM. Cell viability, measured by LDH release and lysozyme production, was reduced in a concentration-dependent manner following exposure to SM at 10 mum or higher. A reduction of superoxide anion and hydrogen peroxide production was observed on exposure to concentrations greater than 10 and 1 mum, respectively. Cell-associated plasminogen activator activity was significanty increased (130% of the control) following exposure to 10 mum and a decrease occurred with exposures to 100 mum or more. The release of arachidonic acid equivalents was not significantly affected by SM treatment. These results demonstrate the cytotoxic effects of SM towards macrophages in culture. While activated macrophages may be present in the dermis after in vivo exposure to SM, no evidence was found of a direct stimulatory effect of SM on the production of macrophage inflammatory products.
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PMID:Effects of sulfur mustard on selected biochemical parameters of murine peritoneal macrophages in culture. 2069 97