Dimeric L-dopa derivatives as potential prodrugs.

A series of dimeric derivatives (+)-1, and (+)-2, and (+)-3a-d of L-Dopa diacetyl esters was synthesized and evaluated as potential L-Dopa prodrugs with improved physicochemical properties. All the new compounds showed chemical stability in aqueous buffer solutions (pH 1.3 and 7.

A new simple laparoscopic-extracorporeal technique for the repair of a Morgagni diaphragmatic hernia.

We used a new technique to treat a right-sided Morgagni hernia in a symptomatic adult with a transverse colon that was herniated in the chest. Three trocars were required. The herniated viscera were easily reduced in the abdomen, and the diaphragmatic border that was mobilized from the liver showed the elliptical diaphragmatic defect (9 x 5 cm); however, the hernial sac was not resected.

Purpurin-18 in combination with light leads to apoptosis or necrosis in HL60 leukemia cells.

Photodynamic therapy (PDT), a cancer treatment using a photosensitizer and visible light, has been shown to induce apoptosis or necrosis. We report here that Purpurin-18 (Pu18) in combination with light induces rapid apoptotic cell death in the human leukemia cell line (HL60) at low doses and necrosis at higher concentrations. Cells treated with Pu18 and light under apoptotic conditions exhibited DNA laddering and an increase in both cellular content of subdiploid DNA and externalization of phosphatidylserine (PS), indicating DNA fragmentation and loss of membrane phospholipid asymmetry.

Clinical utility of CEA, CA 19-9, and CA 72-4 in the follow-up of patients with resectable gastric cancer.

Background: The aim of this longitudinal study was to evaluate the effectiveness of the serum tumor markers CEA, CA 19-9, and CA 72-4 in the early diagnosis of recurrence of gastric cancer.

Methods: One hundred and thirty-three patients who had undergone potentially curative surgery were considered. Serum samples were obtained preoperatively, 1 week after surgery, and at every follow-up examination.

[Evolution of the technique and indications of mini-invasive surgery of cholelithiasis].

Background: A review of the experience with laparoscopic cholecystectomy to evaluate the impact of the efficacy, safety, and complications on the learning curve.

Study Design: Retrospective study.

Methods: Between 1993 and 1998, 415 patients, 123 males and 292 females, median age 52.

[Difficulties in defining and diagnosing gastroesophageal reflux: practical implications in surgery].

Today, it is difficult to set a correct definition and diagnosis of gastroesophageal reflux disease. The attempt to define it on the basis of "typical" symptoms, like heartburn and regurgitation, or "atypical" symptoms, like chronic cough, asthma, hoarseness and thoracic pain, or on the basis of endoscopic esophagitis presents notable difficulties. Moreover, the problem of a correct definition is tightly tied up to the ability to set a correct and early diagnosis.

Collecting duct is a site of sodium retention in PAN nephrosis: a rationale for amiloride therapy.

Micropuncture studies of the distal nephron and measurements of Na,K-ATPase activity in microdissected collecting tubules have suggested that renal retention of sodium in puromycin aminonucleoside (PAN) nephrotic rats originates in the collecting duct. The present study demonstrated this hypothesis by in vitro microperfusion and showed that amiloride was able to restore sodium balance. Indeed, isolated perfused cortical collecting ducts from PAN-treated rats exhibited an abnormally high transepithelial sodium reabsorption that was abolished by amiloride, and in vivo administration of amiloride fully prevented decreased urinary sodium excretion and positive sodium balance in nephrotic rats.

Oesophageal perforation after sclerotherapy. Description of a case.

Surgery is considered mandatory for major oesophageal perforations but the operative risk in cirrhotic patients is very high. The best treatment of these perforations is unknown as these have been always analyzed together with all other kinds of oesophageal perforations. A case is reported of spontaneous healing of severe postsclerosal perforation in an aged cirrhotic patient treated conservatively who otherwise should have been treated surgically.

The care of elderly, terminally ill oncological patients in caregiving sanitary residences.

A panoramic survey is outlined regarding the care system of terminally ill oncologic patients with particular regard to the elderly. National and international experiences are considered offering a caregiving service out of hospital, in small dwelling centers being able to relieve the sufferings of the last days of life. The caregiving sanitary residences and hospices are inserted in a network of services for the elderly oncological patients, representing an adequate answer for the problems.

[Migration of the catheter of a totally implantable venous system. A rare mechanical complication].

Catheter migration, represents a rare, mechanical complication following the use of totally implantable venous devices. A case, in which the catheter was inserted into the right internal jugular vein by percutaneous route, without radiological control, is described. Following the chemotherapy infusion drugs, the patient developed a catheter displacement and subcutaneous extravasation.

Sleep related O2 desaturation in COPD patients with normoxaemia and mild hypoxyaemia.

It is unknown whether daytime features predict oxygenation during sleep in COPD patients with normoxaemia or mild hypoxaemia. In this study our purpose was to evaluate by a pulse oxymeter, nocturnal desaturation in 33 COPD with PaO2 > 60 mmHg and to examine some daytime parameters as possible predictors of nocturnal hypoxaemia. A significant nocturnal desaturation has been defined by spending > or = 30% of total sleep-time with a TSTSaO2 < 90% > 30.

Synthesis of L-(+)-3-(3-hydroxy-4-pivaloyloxybenzyl)-2,5-diketomorpholine as potential prodrug of L-dopa.

The synthesis and in vitro chemical and enzymatic stability of L-(+)-3-(3-hydroxy-4-pivaloyloxybenzyl)-2,5-diketomorpholine (9) as L-Dopa prodrug are described. Prodrug 9 possesses a good lipophilicity (log P = 2.153 +/- 0.

Medical treatment of brain metastases from solid tumours.

Brain metastases (BrM) are estimated to occur in 20% to 40% of cancer patients, and two-thirds of them become symptomatic during their lifetime. Although every solid tumour may spread to the brain, the risk of developing BrM is higher in lung cancer, breast cancer and melanoma patients. Several findings suggest that the incidence of BrM is rising as a result of advances in imaging procedures and improvements in therapy, which leaves more cancer patients at risk as survival increases.

Surgical treatment of gastrointestinal carcinomas in octogenarians: risk factors for complications and long-term outcome.

Background: The aims of this retrospective study were to determine the factors predictive of morbidity and mortality, and to evaluate the probability of long-term survival in octogenarians with carcinomas of the gastrointestinal tract.

Patients And Methods: Out of a total of 194 patients, aged 80 years or over, with histologically diagnosed carcinoma of the stomach or colon-rectum, observed between 1987 and 1995, 167 underwent surgery and were included in this study. The relationship between a series of clinico-pathological variables and morbidity/mortality rates was investigated by univariate and multivariate analysis.

[Characterization and prognostic value of colorectal adenomas with molecular genetic markers].

Aim: The study analyses the expression of DNA-ploidy, ki-67, PCNA and p-53 and their role as potential markers of the development of colorectal adenomas.

Methods: 34 adenomas of the large intestine were analysed using endoscopic exeresis in 15 males and 13 females with a mean age of 64 years (range 42-80). Flow cytometric analysis was carried out to calculate the DNA-index and immunohistochemical tests were used to evaluate ki-67, PCNA and p-53.

Hypercapnia in obstructive sleep apnoea syndrome.

Background: The reports on the prevalence of hypercapnia in Obstructive Sleep Apnoea Syndrome (OSAS) are conflicting. We studied the prevalence of hypercapnia in a population of OSAS patients referred to a Department of Respiratory Medicine and the mechanism of the respiratory failure in OSAS associated with Obesity Hypoventilation Syndrome (OHS) or with Chronic Obstructive Pulmonary Disease (COPD) (Overlap syndrome).

Methods: We studied 219 consecutive OSAS patients during a period of 3 years.

[Trends in stomach carcinoma. A statistical analysis of 1204 cases].

The authors report a retrospective analysis of their experience of gastric cancer. One thousand two hundred and four patients, observed between 1977 and 1994, of whom 1,094 underwent surgery, were studied. Data analysis was performed, dividing this period as follows: 1977-1982, 1983-1988, 1989-1994.

Cellular adaptation of the mouse cortical thick ascending limb of Henle's loop (CTAL) to dietary magnesium restriction: enhanced transepithelial Mg2+ and Ca2+ transport.

Mice aged 4 or 8 weeks were fed with a low-Mg2+ diet for 1, 2, 3 or 4 days. After 1 day of diet, the urinary excretion of Mg2+ and Ca2+ was strongly reduced in both animal groups (4 and 8 weeks), accompanied by a significant fall in plasma Mg2+ concentration and an increase in urinary volume. This profile persisted after 2, 3 or 4 days of dietary Mg2+ restriction.

Binding and preliminary evaluation of 5-hydroxy- and 10-hydroxy-2,3, 12,12a-tetrahydro-1H-[1]benzoxepino[2,3,4-ij]isoquinolines as dopamine receptor ligands.

The N-methyl, N-ethyl, and N-n-propyl derivatives of 5-hydoxy- and 10-hydroxy-2,3,12,12a-tetrahydro-1H-[1]benzoxepino[2,3, 4-ij]isoquinolines were prepared as monophenolic ligands for the dopamine receptor and evaluated for their affinity at D(1)-like and D(2)-like subtypes. All compounds showed very low D(1) affinities. This could be ascribed to the absence of a catechol nucleus or of the beta-phenyldopamine pharmacophore.

P53 accumulation is a prognostic factor in intestinal-type gastric carcinoma but not in the diffuse type.

Background: The prognostic value of p53 nuclear accumulation in gastric cancer is still unclear, as shown by the discordant results still reported in the literature. In this study, we evaluated the correlation between p53 accumulation and long-term survival of patients resected for intestinal and diffuse-type gastric cancer.

Methods: Eighty-three patients with carcinoma of the intestinal type and 53 patients with carcinoma of the diffuse type were included in the study.

psi(SO2NH) transition state isosteres of peptides. Synthesis and bioactivity of sulfonamido pseudopeptides related to carnosine.

This paper reports the synthesis of tauryl dipeptides related to carnosine. In particular H-Tau-His-OH (5), H-Tau-His(pi-Me)-OH (6) and H-Tau-His(tau-Me)-OH (9) are described. The enzyme carnosinase has been isolated from pig kidney and after purification has been used to test the stability and the inhibitory activity of the three new analogues.

[The topical therapy of ulcerative colitis. A multicenter study with beclomethasone dipropionate foam].

Background And Aims: The use of steroids was recently extended to the various forms of ulcerative rectocolitis by the introduction of topical formulations, above all steroids with an hepatic "first pass" devoid of systemic interference. The aim of this study was to evaluate the efficacy and tolerability of Beclomethasone dipropionate (BDP) in a rectal foam formulation, in the treatment of patients suffering from ulcerative colitis.

Methods: The experimental protocol took the form of a 28-day open prospective trial using BDP rectal foam in patients suffering from ulcerative colitis.