An antibody to Clostridium pasteurianum rubredoxin was found in goat serum after multiple injections of the protein. This antibody was purified by adsorption and elution from a Sepharose-rubredoxin column. The purified antibody formed a precipitating complex with C. pasteurianum rubredoxin and a...
The transcripts of the rubredoxin gene from C. pasteurianum have been shown to have a size of approx. 230 bases by Northern blotting techniques. The transcription start has been located within 41 bases upstream of the initiator codon. The data demonstrate that the rubredoxin gene is monocistroni...
New derivatives of 2-(1-amino-1-phenylmethyl)-1,3,4-oxadiazole and 1,2,4-triazin-6-one were synthesised in the reactions of optically active α-aminocarboxylic acid hydrazides and triethyl orthoesters in xylene. The electronic and steric effects of substituents at the α position influencing the...
Novel sophisticated derivatizing agents for the efficient enantioselective separation and mass spectrometric detection of d- and l-amino acids have been developed. Two new axially chiral reagents derived from 6,6′-dimethyl-2,2′-biphenyldiamine were synthesized. Their chiral separation and dete...
3-(3-Phenoxybenzyl)amino-β-carboline 2h showed extremely-high activity; the IC50 value was 0.074 μM. To verify 2h-induced cell death types, we observed the chromatin condensation, the DNA fragmentation and activated caspase-3 using Hoechst 33342, agarose electrophoresis and western blot, and s...
Within the framework of a more general study aimed at the enantiomeric resolution of non-UV-absorbing chiral amino acids via derivatization with chiral isothiocyanates, we have examined the applicability of two such derivatizing agents, (S)-1-(1-naphthyl)ethyl isothiocyanate (SNEIT) and (S)-1-ph...
Tubulin-interacting agents, like vinca alkaloid and taxanes, play a fundamental role in cancer chemotherapy, making cellular microtubules (MT), one of the few validated anticancer targets. Cancer resistance to classical MT inhibitors has motivated the development of novel molecules with increase...
A series of 15 mostly new dialkoxyphosphoryl alkyl and aralkyl isothiocyanates were synthesized using two alternative strategies, and their in vitro antiproliferative activity against several cancer cell lines (including drug resistant) is here demonstrated. The IC50 values measured for the new ...
Chiral derivatization with an enantiomerically pure reagent is an economical and effective way to separate the enantiomers of optically active drugs on achiral HPLC columns. This paper describes the preparation and analytical testing of two novel chiral derivatizing agents (CDAs) deriving from t...
ABSTRACTThe anticancer effects of Isothiocyanates and their synthetic derivates (ITCs) are very extensive. The anticancer mechanisms and the researches of ITCs are reviewed in this paper. The mechanisms may be combination and modification of drug-metabolizing enzymes, influence on the cell cycle...
Organic isothiocyanates (ITCs) are a very important group of biologically active compounds. They do not occur as a free form in nature, but they are liberated from glucosinolates in plant tissues by enzymatic degradation. In this group are compounds with very different structural features, rangi...
We have investigated the effect of inhaled HOE 140, a novel bradykinin B2 receptor antagonist, against bradykinin- and vagal stimulation-induced airway microvascular leakage and bronchoconstriction in anesthetized guinea-pigs. Lung resistance was measured for 6 min after challenge, followed by m...
The role of the amino acids contained in the sequence of HOE 140 (H-DArg1-Arg2-Pro3-Hyp4-Gly5-Thi6-Ser7-DTic8-Oic9-Arg10-OH), a potent and selective bradykinin B2 receptor peptide antagonist, has been investigated by the replacement of each original residue (one by one) with Ala. The resulting s...
The type of antagonism exhibited by the potent bradykinin B2 receptor antagonist, Hoe 140, on the rat uterus was investigated using various approaches. In the isolated rat uterus the concentration-response curve of bradykinin was shifted to the right and the maximum effect was reduced after pret...
The effect of Hoe 140, a bradykinin B2 receptor antagonist, on vasodilator responses to bradykinin was investigated in the mesenteric vascular bed of the cat under constant flow conditions. Injections of bradykinin into the mesenteric vascular bed induced dose-related decreases in perfusion pres...
1.1. This study examines the effect of Hoe 140, a bradykinin (BK) 2 receptor antagonist, indomethacin and prednisolone on chronic adjuvant arthritis of the knee in rats. We also evaluated the influence of Hoe 140 on BK-forming enzymes in the synovial and paw tissues.2.2. Adjuvant arthritis was i...
Bradykinin is a potent inflammatory mediator which may be involved in various airway diseases. A selective and potent antagonist of the bradykinin B2 receptor has recently been discovered (HOE 140: d-Arg-[Hyp3,Thi5,d-Tic7,Oic8]bradykinin). The purpose of this study was to evaluate the potency of...
Des-Arg10-Hoe 140 is a potent and selective …
The effects of bradykinin and the bradykinin B2 receptor antagonists d-Arg-[Hyp3,Thi5,8,d-Phe7]-bradykinin (NPC 349) and d-Arg-[Hyp3,Thi5,d-Tic7,Oic8]-bradykinin (Hoe 140) were examined in the electrically-stimulated rat vas deferens. Cumulative additions of bradykinin (1–3000 nM) produced two ...
Bradykinin is a mediator of vasogenic brain edema formation. Recent reports suggest that bradykinin interacts with nitric oxide synthase (NOS) system in the central nervous system (CNS). However, role of bradykinin in spinal cord injury (SCI) induced alterations in the blood-spinal cord barrier ...
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