Transport of 5-(dimethyltriazeno)imidazole4-carboxamide (NSC 45388) and the 3,3-bis(2-chloroethyl) derivative (NSC 82196) was studied in vitro in Ll210 cells and in drug-resistant sublines. Uptake of both compounds was temperature sensitive and apparently nonsaturable. Accumulated NSC 45388 could be removed from the cells by brief suspension in buffer at 37°.In contrast, accumulated NSC 82 196...

Heat shock factor 1 (HSF1), a transcription factor activated by various stressors, regulates proliferation and apoptosis by inducing expression of target genes, such as heat shock proteins and Bcl-2 (B-cell lymphoma 2) interacting cell death suppressor (BIS). HSF1 also directly interacts with BIS, although it is still unclear whether this interaction is critical in the regulation of glioblastom...

BACKGROUND Propofol and remifentanil are usually co-administered and have shown synergistic effect for anesthesia. However, the synergistic effect of the two drugs on hypnosis measured by bispectral index (BIS) was controversial in previous studies. The aim of this study was to identify the interaction of propofol and remifentanil on BIS and the optimal dose combinations for hypnosis under 66% ...

Background: Ensuring adequate depth of anesthesia during surgery is essential for anesthesiologists to prevent the occurrence of unwanted alertness during surgery or failure to return to consciousness. Since the purpose of using anesthetics is to affect the central nervous system, brain signal processing such as electroencephalography (EEG) can be used to predict different levels of anesthesia....

in this paper, new (2e, 2'e)-3, 3'-(((3- hydroxypropane-1, 2-diyl) bis (oxy)) bis (2, 1-phenylene)) bis (1-phenylprop-2-en-1-one) (2a) was prepared in good yield by condensation reaction of acetophenone with bisaldehyde (1a) in ethanolic naoh solutions at room temperature. the (2e, 2'e)-3, 3'-(((3- hydroxypropane-1, 2-diyl) bis (oxy)) bis (2, 1-phenylene)) bis (1-phenylprop-...

BACKGROUND The relationship between measures of drug effect such as bispectral index (BIS) and end-tidal (ET) levels of anaesthetic agents is described by the 'effect site equilibrium half-time', t(1/2)(ke0). There are limited data available on sevoflurane t(1/2)(ke0) during routine anaesthesia and surgery. Preliminary observations suggested t(1/2)(ke0) for the degree of hypnosis as estimated b...

Methylglyoxal bis(guanylhydrazone) {1,1'-[(methylethanediylidene)-dinitrilo]diguanidine} is a very potent inhibitor of putrescine-activated S-adenosylmethionine decarboxylases from many different mammalian tissues, including sublines of mouse L1210 leukaemia that are resistant to the drug as well as sublines that are sensitive. The inhibition of purified rat ventral prostate S-adenosylmethionin...

The enzyme trypanothione reductase (TR), together with its substrate, the glutathione-spermidine conjugate trypanothione, plays an essential role in protecting parasitic trypanosomatids against oxidative stress and is a target for drug design. Here we show that a naturally occurring spermine derivative, the antihypertensive agent kukoamine A [N1N12-bis(dihydrocaffeoyl)-spermine] inhibits TR as ...