Respiratory nitrate reductase from the denitrifying bacterium Pseudomonas stutzeri is an iron-sulfur enzyme containing the molybdenum cofactor. Hydrolysis of native nitrate reductase with aqueous sulfuric acid revealed 0.92 mol of 5′-GMP per mol of enzyme. The pterin present in the molybdenum c...
[Fe–S] clusters are essential cofactors in all domains of life. They play many biological roles due to their unique abilities for electron transfer and conformational control. Yet, producing and analyzing Fe–S proteins can be difficult and even misleading if not done anaerobically. Due to uniq...
Molybdoenzymes are complex enzymes in which the molybdenum cofactor (Moco) is deeply buried in the enzyme. Most molybdoenzymes contain a specific chaperone for the insertion of Moco. For the formate dehydrogenase FdsGBA from Rhodobacter capsulatus the two chaperones FdsC and FdsD were identified...
The pterin cofactor in formate dehydrogenase isolated from Methanobacterium formicium is identified as molybdopterin guanine dinucleotide. The pterin, stabilized as the alkylated, dicarboxamidomethyl derivative, is shown to have absorption and chromatographic properties identical to those of the...
Several arvanil analogs were synthesized where the end n-pentyl chain was branched and carried substituents at the terminal end of the chain. A high yielding total synthesis of these analogs was developed from methyl hex-5-ynoate, which was converted to the synthon 6 in a facile five step sequen...
Activation of cannabinoid receptors causes inhibition of spasticity, in a mouse model of multiple sclerosis, and of persistent pain, in the rat formalin test. The endocannabinoid anandamide inhibits spasticity and persistent pain. It not only binds to cannabinoid receptors but is also a full ago...
The effects of arvanil (N-arachidonoyl-vanillyl-amine), a structural hybrid between capsaicin and anandamide, on ion currents in a mouse neuroblastoma and rat glioma hybrid cell line, NG108-15, were examined with the aid of the whole-cell voltage-clamp technique. Arvanil (0.2–50 μM) caused an ...
In this study we analysed the regulation of gene expression by arvanil and anandamide in human peripheral blood mononuclear cells (PBMCs) to clarify their immunosuppressive properties. PBMCs were activated, leading to CD36 down regulation, that was normalized by arvanil and anandamide. We used m...
The present study was designed to examine whether arvanil (N-arachidonoyl-vanillyl-amide), an endocannabinoid/vanilloid structural “hybrid”, might provide symptom relief in the rat model of Huntington's disease (HD) generated by bilateral intrastriatal application of 3-nitropropionic acid...
This study examined the immunomodulatory effect of arvanil, a synthetic capsaicin–anandamide hybrid. Arvanil inhibits lymphocyte proliferation and IFN-γ production. The phenotype of activated CD4 + T cells treated with arvanil shows a down-regulation of T cell activation markers such as CD25, ...
Cardio-respiratory effects of an intravenous injection of arvanil, a structural “hybrid” between capsaicin and anandamide, were investigated in 40 urethane-chloralose anaesthetized and spontaneously breathing rats. In the group of rats the response to arvanil was checked to establish the appro...
Arvanil is a metabolically stable hybrid between anandamide and capsaicin. The present study was designed to test the role of the vagal pathway in post-arvanil respiratory and blood pressure responses. Respiratory and pressure changes evoked by an intravenous injection of arvanil were investigat...
BackgroundRecent evidence reveals therapeutic potential for cannabinoids to reduce seizure frequency, severity and duration. Animal models are useful tools to determine the potential antiseizure or antiepileptic effects of cannabinoids. The objective of this study was evaluation of the effect of...
Various graft copolymers were obtained by ring-opening of succinic groups in styrene-isoprene block copolymers, modified with maleic anhydride, using reagents containing nucleophilic groups. Comblike hydrophilic graft copolymers were prepared using polyethylene glycol-550-monomethyl ether or pol...
Preliminary studies on the biosynthesis of tolytoxin (1) in the terrestrial blue-green alga Scytonema mirabile BY-8-1 are reported. Incorporation experiments with [1,2-13C] acetate, [1-13C,18O]acetate, [1,2-13C]glycine, [2-13C,15N]glycine and [methyl- 13C]methionine indicate that the carbon chai...
In a search for a mannopyranose analogue which inhibits α-mannosidases but not α-fucosidases, α-homonojirimycin was prepared; the syntheses of 6-epi-α-homonojirimycin and of 2,6-dideoxy-2,6-imino-L-glycero-D-talo-heptonic acid (a highly substituted pipecolic acid) are also reported.
Homoazasugars have the distinction as a class of natural products in that most of them have been synthesised before they were isolated. Syntheses of α-1 and β-homomannojirimycin 2 rely on the stereoselective and chemoselective sodium cyanoborohydride reduction of a [2.2.2] bicyclic imino lacto...
A thermally induced intramolecular 1,3-dipolar cycloaddition of an azidoester and subsequent sodium cyanoborohydride reduction of the resulting bicyclic vinylogous urethane to give a bicyclic aminolactone allows access to an eight carbon homologue of α-homomannojirimycin which is a weak fucosid...
C-2 and C-6 of a heptonolactone are joined together by nitrogen to afford α-homomannojirimycin (HMJ) and 6-epi-α-homomannojirimycin; the inhibition of some α-mannosidases and α-fucosidases by these iminoheptitols is reported.
A novel Schiff base derivative containing 1, 2, 4-triazole nucleus (TMPIMP) was synthesized from 4- [1,2,4] triazol-1-ylmethyl-phenylamine and salicylaldehyde in the presence of glacial acetic acid in an ethanolic medium. The synthesized compound was characterized by 1H-NMR, IR and UV spectral a...
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