Novel tricyclic poly(ADP-ribose) polymerase-1 inhibitors with potent anticancer chemopotentiating activity: design,synthesis, and X-ray cocrystal structure

A series of novel compounds have been designed that are potent inhibitors of poly(ADP-ribose) polymerase-1 (PARP-1), and the activity and physical properties have been characterized. The new structural classes, 3,4,5,6-tetrahydro-1H-azepino[5,4,3-cd]indol-6-ones and 3,4-dihydropyrrolo[4,3,2-de]isoquinolin-5-(1H)-ones, have conformationally locked benzamide cores that specifically interact with the PARP-1 protein. The compounds have been evaluated with in vitro cellular assays that measure the ability of the PARP-1 inhibitors to enhance the effect of cytotoxic agents against cancer cell lines.     

Criteria for judging the improvement in subclinical rheumatic valvitis

Recent technical improvements in cross-sectional echocardiography have made it possible to detect even mild organic regurgitation of the mitral and aortic valves in patients with acute rheumatic fever. To determine the prevalence and prognosis of subclinical valvitis, we have analyzed 104 patients with acute rheumatic fever referred to our institution. Of 53 patients who had no murmur, 22 of them with polyarthritis, 29 with chorea, and 2 with polyarthritis and chorea, 23 (43.4%) had subclinical valvitis. Isolated mitral regurgitation was the most common valvar lesion, seen in 82.6% of the patients. Isolated aortic regurgitation was detected in 4.4% of the cases, and combined mitral and aortic regurgitation in the remaining 13%. During follow-up, the degree of mitral regurgitation improved in 59.1%, decreased in 18.2%, and increased or remained unchanged in 22.7% according to the length of colour jet. According to criterions of velocity, mitral regurgitation improved in 86.4% of the patients, and increased or unchanged in the remaining 13.6%. Mitral regurgitation disappeared completely in 6 of the patients (27.3%) as judged according to both the length of colour jet and the velocity of regurgitation. Aortic regurgitation improved in all the patients with this problem, disappearing completely in two of the four. Based on this experience, we suggest that not only the disappearance of regurgitation, but also improvements in the echocardiographic diagnostic criterions of regurgitation, such as the length of the colour jet less than 1 cm, or velocity less than 2.5 m/s, or indicative of regurgitation that is either intermittent or of short duration, should also be considered as criterions indicating improvement in valvar regurgitation in patients with subclinical rheumatic valvitis.     

Emergency endovascular management of pulmonary artery aneurysms in Behçet's disease: report of two cases and a review of the literature

his report describes two patients with a known history of Beh?et's disease in whom massive hemoptysis developed from rupture of pulmonary artery aneurysms. The high recurrence rate of complications related to pulmonary artery aneurysms and even the aneurysms themselves due to inadequacy of medical therapy and the disadvantages of surgical treatment make these aneurysms candidates for endovascular management. The pulmonary artery aneurysms reported here were successfully treated with endovascular embolization using n-butyl cyanoacrylate. Pulmonary artery aneurysm embolization in Beh?et's disease has been reviewed in the light of relevant literature.     

Ghosal haemato-diaphyseal dysplasia: A new disorder

We describe two siblings, products of a first cousin marriage, with diaphyseal dysplasia, severe anaemia, leukopenia, and thrombocytopenia. Radiologically, both had wide medullary cavities with discrete cortical hyperosthosis. Bone marrow was hypocellular. These, and six similar cases in the literature [6], suggest that they represent a form of diaphyseal dysplasia differing from Camurati-Engelmann disease by their radiological appearance, associated haematological abnormalities and autosomal recessive inheritance.     

Comparison of the factors that influence obesity prevalence in three district municipalities of the same city with different socioeconomical status: a survey analysis in an urban Turkish population

BACKGROUND: To evaluate the obesity status, factors and comorbidities related to it in three district municipalities (DM) that compose city center of Bursa with inhabitants of different socioeconomic status. METHODS: A total of 1632 inhabitants >/=18 years of age were interviewed. The number of sample in each DM was obtained proportional to their populations by stratified sampling method. Among 1632, a total of 1543 subjects were included by random sampling and a questionnaire was filled in including demographic, social and behavioral features. RESULTS: The participants living in DM with the highest socioeconomical status (SES) score and level of education had the lowest body mass index (BMI) and body fat percentage (%BF) compared to other DMs. The lowest obesity prevalence (30.8% vs. 36.4% and 39.3%) in that DM was possibly due to younger age, lower female ratio, more active professional, higher percentage of smoking, more consumption of vegetables, olive or corn oil, and less carbohydrate. For the evaluation of the factors that may influence obesity risk, we investigated the effects of these factors in men and women separately with logistic regression model. Sedentary life style and dyslipidemia (DL) in men, being unemployed, having lower level of education and having hypertension (HT) in women and familial obesity in both gender were found to be related to increased obesity risk. CONCLUSIONS: The prevalence of obesity in Bursa is increasing although inhabitants are taking some precautions parallel to their socioeconomical and educational levels. Obesity is becoming a more alarming public health problem in Bursa and Turkey like in most other parts of the world, which forces us to invent new prevention policies. Besides, the results of our study highlight the fact that especially female education requires more attention for decreasing obesity prevalence in coming generations.     

In Vivo Study to Assess the Viability and Mass Effect of Fascia Injection in Comparison with Block Fascia Graft

Recently, fat injection has gained favor among plastic surgeons for soft tissue augmentation. However, fat injections lose 50% of their volume after 1 year. The profession is in need of an injectable bulking material that gives a long-lasting improvement. Using 30 male rats, this study investigated the stability of the size and structure of the injected fascia autograft and compared it with surgically transplanted fascia. The fascia graft was harvested from the back of the rat, big, and divided into two equal pieces. The first piece was minced into a paste and injected subcutaneously on the anterior surface of the right ear. The other piece was transplanted subcutaneously on the anterior surface of the left ear. The grafts were observed for any sign of resorption over 1 to 6 months.Grossly, injection and transplantation sites were palpable at the end of the observation periods. Microscopic examination showed that injected fascia maintains its histomorphologic structure.These findings indicate that the injected fascia graft is well tolerated, and the size of the graft remained stable. According to this study, fascia injection can result in bulking material that gives a long-lasting improvement, and can be a viable alternative to other methods.     

Staged Abdominal Repair for Treatment of Moderate to Severe Secondary Peritonitis

The aim of this study was to evaluate the effects of planned relaparotomy and to assess factors that may contribute to mortality in patients with moderate to severe secondary peritonitis. A total of 36 consecutive patients with an Acute Physiologic and Clinical Health Evaluation (APACHE) II score of >10 were enrolled the study for a 2-year period. The mean age of the patients was 56 years (17-92 years), and 23% of them were male. One-third of them had postoperative peritonitis; 152 scheduled operations were done, and the overall mortality rate was 36%. For patients whose septic source was in the upper gastrointestinal system, control of the source was more difficult (p = 0.004). Overall, 28 complications developed in 61% of the patients. Initial and second-day APACHE II scores were 14.5 (11-27) and 12.0 (9-25), respectively. The initial APACHE II score of survivors was lower than that of nonsurvivors [p = 0.0001, 95% confidence interval (CI) -9.5, -3.6]. Second-day APACHE II scores were not different (p = 0.19; 95% CI -3.79, 0.80). Striking end or lateral duodenal leaks were clearly associated with high mortality. It is found that the initial APACHE II score, the success of controlling the source, the occurrence of complications, and the type of illness are independent factors that may affect mortality. We concluded that staged abdominal repair should be used with caution in the treatment of lateral or end duodenal leaks. It is a good alternative to conventional laparotomy for moderate to severe forms of secondary peritonitis from other sources.The preliminary data of this study were presented at the Turkish Surgical Congress in Antalya, Turkey in 2002.