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Pharmacokinetic studies on 1-(2-chloroethyl)-3-isobutyl-3-(beta-maltosyl)-1-nitrosourea (TA-077). II. Hydrolysis by tissue homogenates and drug uptake by tumor cells in vitro.

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1-(2-Chloroethyl)-3-isobutyl-3-(beta-maltosyl)-1-nitrosourea (TA-077) was hydrolyzed to its glucosyl metabolite TA-G by homogenates of guinea pig organs, rabbit VX-2 carcinoma and rat Yoshida sarcoma. The rate of TA-G formation by the kidney was the highest among the tissues examined and that by the

Sucrase-isomaltase expression and enterocytic ultrastructure of human colorectal tumors.

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We report the relative frequency of sucrase-isomaltase (SI) antigen expression in human colonic adenocarcinoma (22/57), in peritumoral mucosa taken next to the tumor (31/41) or distant from it (29/42) as well as in 21/23 polyps. Our results are based on indirect immunofluorescence with a monoclonal

Nephrotoxicity of cis-diamminedichloroplatinum with or without ifosfamide in cancer treatment.

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cis-Diamminedichloroplatinum (DDP) and ifosfamide (IPP) are effective cytostatic agents with a considerable nephrotoxicity. Because of the known synergism of both drugs in animals the combination has been studied in man with disseminated testicular cancer. Nature and extent of nephrotoxicity of DDP

Comparison of tumor growth inhibitory and toxic effects of a new fluorouracil--nitrosourea derivative (B-3839).

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The toxic effect and anti-tumor activity of B-3839, a new molecular combination of pyrimidine antimetabolite 5-fluorouracil (5-FU) with the alkylating agent N-Chloroethyl-N-nitrosourea (BCNU), was compared to that of BCNU and 5-FU given alone and in physical combination. The tumor inhibitory effect

Octreotide alleviates obesity by reducing intestinal glucose absorption and inhibiting low-grade inflammation.

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OBJECTIVE To investigate the role of octreotide, a somatostatin (SST) analog with anti-inflammatory effects, on the digestive and absorptive functions of jejunum in rats fed a high-fat diet, as well as its therapeutic prospects for diet-induced obesity. METHODS Rats were divided into three groups

Effect of non-steroidal anti-inflammatory drugs and the pro-carcinogen 1,2 dimethylhydrazine on the rat intestinal membrane structure and function.

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The present study was designed to evaluate the effects of three non-steroidal anti-inflammatory drugs (NSAIDs) with varying cycloxygenase selectivities on the small intestinal biochemical composition, function and histology during 1, 2-dimethylhydrazine (DMH) administration. Sprague Dawley male rats

Synthesis, enzymatic activity, and X-ray crystallography of an unusual class of amino acids.

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The synthesis of two novel amino acids, nitrogen analogues of the naturally occurring glycosidase inhibitor, salacinol, containing a carboxylate inner salt are described, along with the crystal structure of one of these analogues in the active site of Drosophila melanogaster Golgi mannosidase II

Similarity of hydrolyzing activity of human and rat small intestinal disaccharidases.

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BACKGROUND The purpose of this study was to clarify whether it is possible to extrapolate results from studies of the hydrolyzing activity of disaccharidases from rats to humans. METHODS We measured disaccharidase activity in humans and rats using identical preparation and assay methods, and

Modulation of 5-fluorouracil in mice using uridine diphosphoglucose.

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Uridine diphosphoglucose (UDPG) is a precursor of uridine that can be used as a rescuing agent from 5-fluorouracil (5FU) toxicity. Four doses of UDPG (2000 mg/kg i.p. or p.o. at 2, 6, 24, and 30 h after 5FU bolus) allowed the escalation of a weekly bolus of 5FU from 100 mg/kg (5FU100) to 150 mg/kg

Pharmacokinetic studies on 1-(2-chloroethyl)-3-isobutyl-3-(beta-maltosyl)-1-nitrosourea (TA-077). I. Blood and tissue concentrations of a new nitrosourea antitumor agent TA-077 and its metabolite TA-G after intravenous injection of TA-077 in various experimental animals.

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1-(2-Chloroethyl)-3-isobutyl-3-(beta-maltosyl)-1-nitrosourea (TA-077) is a new masked antitumor agent, which is hydrolyzed by maltase to give rise to a more cell-permeable and, hence, more cytotoxic metabolite, TA-G. TA-077 was intravenously administered to mice, rats, guinea pigs, rabbits and dogs

Pharmacokinetic studies on 1-(2-chloroethyl)-3-isobutyl-3-(beta-maltosyl)-1-nitrosourea (TA-077). III. Pharmacokinetics of a new nitrosourea antitumor agent TA-077 in humans (a phase I study).

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A new nitrosourea antitumor agent TA-077, 1-(2-chloroethyl)-3-isobutyl-3-(beta-maltosyl)-1-nitrosourea, was intravenously administered to 15 cancer patients at doses ranging from 7 to 100 N (1 N = 30 mg/m2) in a phase I clinical trial. Time courses of blood concentrations of TA-077 and its active

Enzymatically modified isoquercitrin, alpha-oligoglucosyl quercetin 3-O-glucoside, is absorbed more easily than other quercetin glycosides or aglycone after oral administration in rats.

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Quercetin, a flavonol contained in various vegetables and herbal medicines, has various biological activities including anti-cancer, anti-allergic and anti-oxidative activities. However, low oral bioavailability of quercetin due to insolubility in water has limited its use as a food additive or

Beneficial effects of cyclosporine and rapamycin in small bowel ischemic injury.

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Gut ischemia has been implicated in the pathogenesis of necrotizing enterocolitis. Cyclosporine A and rapamycin, both potent novel immunosuppressants which act on signal transduction pathways in CD4+ T-cells, could potentially modulate immune/inflammatory cellular reactions involved in tissue

Impact of weaning and an antioxidant blend on intestinal barrier function and antioxidant status in pigs.

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The objective of this experiment was to investigate the influence of weaning stress and an antioxidant blend on gut health and free radical metabolism in postweaning pigs. A total of 96 pigs from 12 litters were randomly divided by litter to 3 groups with 4 litters each. The control group and the

Antioxidants from black and green tea: from dietary modulation of oxidative stress to pharmacological mechanisms.

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The consumption of tea (Camellia sinensis) has been correlated with a low incidence of chronic pathologies, such as cardiovascular disease and cancer, in which oxidative stress plays a critical role. Tea catechins and theaflavins are, respectively, the bioactive phytochemicals responsible for the

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