Skeletonizing en bloc esophagectomy for cancer.

Objective: To evaluate the long-term outcome of patients with esophageal cancer after resection of the extraesophageal component of the neoplastic process en bloc with the esophageal tube.

Summary Background Data: Opinions are conflicting about the addition of extended resection of locoregional lymph nodes and soft tissue to removal of the esophageal tube.

Methods: Esophagectomy performed en bloc with locoregional lymph nodes and resulting in a real skeletonization of the nonresectable anatomical structures adjacent to the esophagus was attempted in 324 patients.

Dynamic contrast enhanced magnetic resonance imaging subtraction in evaluating osteosarcoma response to chemotherapy.

Purpose: To evaluate the results of a new technique of dynamic contrast enhanced Magnetic Resonance (MR) imaging subtraction in the assessment of osteosarcoma response to chemotherapy.

Methods: 24 patients with high grade osteosarcoma, treated with preoperative neo-adjuvant chemotherapy, underwent MR at high field strength (1.5 T).

[Pulse inversion ultrasonography with ultrasonography contrast media (levovist) in the evaluation of hepatic metastasis].

Purpose: To evaluate if Pulse Inversion Harmonic Imaging with contrast agent injection (Levovist) is able to determine an increase of echogenicity in normal hepatic parenchyma, and to compare its capability to detect metastatic focal lesions with that of standard US and spiral CT. To define and standardize the technical and methodological aspects of this new technique.

Material And Methods: A selected group of 72 patients (42 males and 30 females) with clinical and instrumental suspect of hepatic metastatic lesions was included in the prospective study.

Human stomach has a recordable mechanical activity at a rate of about three cycles/minute.

Objective: To discover whether the human stomach contracts every 20 seconds or not.

Design: Manometric study.

Setting: Teaching hospital, Belgium.

Denervated stomach as an esophageal substitute recovers intraluminal acidity with time.

Objective: To determine whether the denervated stomach as an esophageal substitute recovers normal intraluminal acidity with time.

Summary Background Data: Bilateral truncal vagotomy to the stomach as an esophageal substitute reduces both gastric acid production and antral motility, but a spontaneous motor recovery process takes place over years.

Methods: Intraluminal gastric pH and bile were monitored during a 24-hour period 1 to 195 months after transthoracic elevation of the stomach as esophageal replacement in 91 and 76 patients, respectively.

[Cine magnetic resonance with dobutamine following a myocardial infarct].

Purpose: Dobutamine cine MRI is a new diagnostic imaging technique in the pretreatment (revascularization) assessment of myocardial infarction patients. We report the results of a comparative study of the diagnostic yield of dobutamine cine MRI with that of stress echocardiography in the assessment of viable myocardium. We also propose a new method for analysis of cine MR images, employing digital subtraction, aimed at decreasing subjectivity in the quantitative assessment of myocardial wall thickening.

Human stomach has a recordable mechanical activity at a rate of about three cycles/minute.

Objective: To discover whether the human stomach contracts every 20 seconds or not.

Design: Manometric study.

Setting: Teaching hospital, Belgium.

[Hepatic arterial vascular anatomy and its variants].

Purpose: We investigated the frequency of anatomical variants of the hepatic artery, which can influence interventional angiographic procedures.

Material And Methods: We reviewed 150 consecutive angiograms performed for the treatment of primary (112) or metastatic (38) liver tumors and evaluated the frequency of anatomical variants of the hepatic artery based on the classification proposed by Michels in 1955, which describes 10 variants. The so-called typical anatomy, which is in fact only found in 55% of cases, is indicated as type I.

Coronally advanced flap for the treatment of buccal gingival recessions with and without enamel matrix derivative. A split-mouth study.

Background: The coronally advanced flap (CAF) is a predictable method for achieving root coverage in buccal gingival recessions. The use of enamel matrix derivative (EMD) has already been tested in treating intrabony defects. No clinical comparative study has been published evaluating the CAF in combination with EMD in treating buccal gingival recessions.

Pyrazolo[4,3-e]1,2,4-triazolo[1,5-c]pyrimidine derivatives as highly potent and selective human A(3) adenosine receptor antagonists: influence of the chain at the N(8) pyrazole nitrogen.

An enlarged series of pyrazolotriazolopyrimidines previously reported, in preliminary form (Baraldi et al. J. Med.

[Antineoplastic perfusion with percutaneous stop-flow control in the treatment of advanced pelvic malignant neoplasms].

Purpose: The object of our study was to apply percutaneous stop-flow technique to advanced pelvic cancer in order to evaluate its feasibility, standardize the procedure and obtain preliminary results.

Material And Methods: April to December 1997 we submitted ten patients with advanced pelvic cancer to percutaneous stop-flow technique. Seven patients had a pelvic recurrence from carcinoma of the rectum, two patients had inoperable recto-sigmoid cancer, and another one had a local recurrence of ovarian cancer.

[2,1-c][1,4]benzodiazepine (PBD)-distamycin hybrid inhibits DNA binding to transcription factor Sp1.

We designed and synthesized the hybrid 6, prepared combining the minor groove binders distamycin A and pyrrolo [2,1-c][1,4] benzodiazepine (PBD) 4, related to the natural occurring anthramycin (2) and DC-81 (3). In this paper, the effects of the compound 6 on molecular interactions between DNA and transcription factor Sp1 were studied. The results obtained demonstrate that PBD-distamycin hybrid is a powerful inhibitor of Sp1/DNA interactions.

In vivo lipid peroxidation and platelet activation in cystic fibrosis.

F(2)-isoprostanes are bioactive peroxidation products of arachidonic acid whose urinary excretion provides an index of lipid peroxidation in vivo. We tested the hypothesis that formation of F(2)-isoprostanes is altered in patients with cystic fibrosis and contributes to platelet activation and pulmonary dysfunction in this setting. The urinary excretion of immunoreactive 8-iso-prostaglandin F(2alpha) (PGF(2alpha)) was significantly (p = 0.

Synthesis and biological effects of a new series of 2-amino-3-benzoylthiophenes as allosteric enhancers of A1-adenosine receptor.

New derivatives of PD 81,723, an allosteric enhancer of agonist binding to the A1-adenosine receptor, have been synthesized and evaluated in an intact cell assay. Compounds 3a, 3o and 3p appeared to be more potent than PD 81,723 and at a concentration of 0.1 microM caused significant reductions of cAMP content of CHO cells expressing the human A1-adenosine receptor.

Synthesis and antitumor activity of new benzoheterocyclic derivatives of distamycin A.

The design, synthesis, and in vivo and in vitro antileukemic activity of a novel series of compounds (13-22 and 34), in which different benzoheterocyclic rings, bearing a nitrogen mustard or a benzoyl nitrogen mustard or an alpha-bromoacryloyl group as alkylating moieties, are tethered to a distamycin frame, are reported, and structure-activity relationships are discussed. The new derivatives were prepared by coupling nitrogen mustard-substituted, benzoyl nitrogen mustard-substituted, or alpha-bromoacryloyl-substituted benzoheterocyclic carboxylic acids 23-32 with desformyldistamycin (33) or in one case with its two-pyrrole analogue 35. With very few exceptions, the activities of compounds bearing the same alkylating moiety are slightly affected by the kind of the heteroatom present on the benzoheterocyclic ring.

Synthesis of hybrid distamycin-cysteine labeled with 99mTc: a model for a novel class of cancer imaging agents.

The synthesis of a hybrid constituted by distamycin A and cysteine labeled with the gamma-emitting radionuclide 99mTc to afford the conjugate complex 5 is reported. This new radiopharmaceutical is of potential interest as tumor imaging agent in diagnostic nuclear medicine. The preparation of the hybrid distamycin A-cysteine 4 has been achieved by coupling deformyldistamycin A and Boc-Dmt-OH.

Roux-en-Y jejunal loop and bile reflux.

Background: The current opinion is that the reflux of jejunal juice over the whole length of a long Roux-en-Y jejunal loop is very uncommon. We aimed to challenge this concept by monitoring the presence of bile in the organ proximal to a 60-cm loop during a 24-hour period with use of the Bilitec device, an optoelectronic instrument capable of measuring absorbance of a beam of light, the wavelength of which is close to the absorbance peak of bilirubin.

Patients And Methods: Forty-one patients, 8 of whom had been cholecystectomized, were investigated after total gastrectomy (group I, n = 17), distal gastrectomy (group II, n = 7), or duodenal switch (group III, n = 17).

[(3)H]MRE 3008F20: a novel antagonist radioligand for the pharmacological and biochemical characterization of human A(3) adenosine receptors.

The lack of a radiolabeled selective A(3) adenosine receptor antagonist is a major drawback for an adequate characterization of this receptor subtype. This paper describes the pharmacological and biochemical characterization of the tritiated form of a new potent A(3) adenosine receptor antagonist, the pyrazolo triazolo pyrimidine derivative [(3)H]5N-(4-methoxyphenylcarbamoyl)amino-8-propyl-2-(2-furyl )pyrazolo [4,3-e] -1,2,4- triazolo[1,5-c]pyrimidine ([(3)H]MRE 3008F20). [(3)H]MRE 3008F20 bound specifically to the human adenosine A(3) receptor expressed in CHO cells (hA(3)CHO), and saturation analysis revealed a single high affinity binding site, K(D) = 0.

Synthesis of conformationally constrained analogues of KN62, a potent antagonist of the P2X7-receptor.

Conformationally constrained analogues of KN62 containing 1,2,3,4-tetrahydro-7-hydroxyisoquinoline-3-carboxylic acid with S configuration in position 3 were synthesized and their antagonist activities were tested on human macrophage cells. While KN62 is a potent antagonist of the P2X7 receptor, these analogues were inactive as antagonists and only one compound showed appreciable activity as P2X7 antagonist, which was 30 times weaker than that reported for KN62.

DNA sequence-recognizing properties of minor groove alkylating agents. Effects of the replacement of N-methylpyrrole by an N-methylimidazole on tallimustine and its own homologue.

The linkage of an heterocycle, like N-methylimidazole, to minor DNA groove binders containing two or three pyrroles lead to a new class of oligopeptides with reduced antitumor activity both in vitro and in vivo if compared to tallimustine (CAS 115308-98-0) and its tetrapyrrole homologue 9. In the present paper is reported the correlation between the cytoxicity of tallimustine and its derivatives 9-11 with their ability to inhibit polymerase chain reaction (PCR) amplification of oestrogen receptor and Ha-ras gene sequences, containing A + T rich and G + C rich regions, respectively. Tallimustine and its tetrapyrrole homologue 9 were found to have higher sequence selectivity for the human oestrogen receptor (ER) gene with respect to the relative imidazole-containing analogues.

A(3) adenosine receptor ligands: history and perspectives.

Adenosine regulates many physiological functions through specific cell membrane receptors. On the basis of pharmacological studies and molecular cloning, four different adenosine receptors have been identified and classified as A(1), A(2A), A(2B), and A(3). These adenosine receptors are members of the G-protein-coupled receptor family.

Synthesis and preliminary biological evaluation of [3H]-MRE 3008-F20: the first high affinity radioligand antagonist for the human A3 adenosine receptors.

The synthesis and the preliminary biological evaluation of the first high affinity radioligand antagonist for the human A3 adenosine receptor, named [3H]-MRE 3008-F20 are reported. [3H]-MRE 3008-20 bound human A3 receptors expressed in CHO cells with K(D) and Bmax value of 0.82 +/- 0.

1H-pyrazolo[2,3-d][1,2,4]triazine-3,7-diones as a new class of human leukocyte elastase inhibitors.

A novel series of 1H-2-phenyl-substituted-pyrazolo[2,3-d][1,2,4]triazine-3,7-diones (3a-g) as potential inhibitors of Human Leukocyte Elastase (HLE) are reported, the acyl-pyrazole being probably involved in the inhibition mechanism of the serino-protease enzymes. The most potent inhibitor both in vivo and in vitro was 2-o-methoxyphenyl-5-methyl-6-nitro-pyrazolo[2,3-d][1,2,4]triazine-3,7-di one (3e), which significantly suppressed the HLE-induced pulmonary injury in rats when administered orally (100 mg/kg, 3 h prior to HLE administration.