Anilide formation from thioacids and perfluoroaryl azides.

A metal-free method for fast and clean anilide formation from perfluoroaryl azide and thioacid is presented. The reaction proved highly efficient, displaying fast kinetics, high yield, and good chemoselectivity. The transformation was compatible with various solvents and tolerant to a wide variety of functional groups, and it showed high performance in polar protic/aprotic media, including aqueous buffer systems.

[Case of prostate cancer associated with bisphosphonate-related osteonecrosis of the jaw followed by retropharyngeal abscess].

A 67-year-old man with castration-resistant prostate cancer associated with multiple bone metastases had been treated with zoledronic acid and docetaxel. Although there was no evidence of damage around the right lower jaw bone, the patient complained of pain in May 2011, which worsened during the next 2 weeks and was followed by difficulty with breathing. Computed tomographic (CT) findings of the cervical area showed swelling of the cervical tissue with air and tightening of the trachea, suggesting cellulitis caused by gas gangrene. He was intubated and treated with antibiotics. On the 12th hospital day, CT scan revealed a pharyngeal abscess and we performed a drainage operation. On the 20th hospital day, bone of the intraoral lower jaw was exposed, revealing that the infection was caused by osteonecrosis. Additional CT findings showed the abscess extending to the mediastinum and multiple liver metastases. Although antibiotic therapy was continued, the patient died of liver failure on the 61st day.

[A case of ductal adenocarcinoma of prostate associated with retroperitoneal multiple cysts].

A 61-year-old man came to our hospital with a complaint of lower abdominal pain. Computed tomography (CT) and magnetic resonance imaging (MRI) around his abdominal area showed large multiple cysts in the pelvis suggesting a malignant tumor. He showed high levels of serum carbohydrate antigen 19- 9 (CA19-9) and carcinoembryonic antigen (CEA). The complete diagnostic studies, including upper gastrointestinal endoscopy and colonoscopy examinations, failed to demonstrate the presence of alimentary primary tumors. With the diagnosis of cystic tumor in the pelvis, the operation was performed. The cysts adhered firmly to the surrounding organs including bladder and peritonium, which could not be resected completely. A histopathological diagnosis was papillary adenocarcinoma positive for prostate specific antigen (PSA). Because the level of serum PSA was 9.39 ng/ml, prostate biopsy was performed and ductal adenocarcinoma of prostate was revealed. After the operation, the levels of serum CA19-9 and CEA decreased to a normal level. Androgen deprivation therapy (ADT) was started, and the level of PSA was normalized one month later. Ductal adenocarcinoma forming cysts is rare. We reviewed 15 cases reported in the Japanese literature.

[A case of prostate cancer diagnosed by lymphadenectomy].

A 65-year-old man was referred to our hospital because of an elevated value of prostate specific antigen (PSA) (10.9 ng/ml). An eight-core prostate biopsy was negative. One year later, serum PSA increased to 55. 8 ng/ml and pelvic magnetic resonance imaging (MRI) showed a left external iliac lymph node enlargement. A ten-core prostate biopsy was negative. Six months later, the serum PSA increased to 88.1 ng/ml, but an seventeen-core prostate biopsy was negative again. A positron emission tomographycomputed tomography scan showed nothing other than increased uptake localized to the left enlarged external iliac lymph node. Pelvic lymphadenectomy was performed and histological examination, including immunohistological staining with PSA, confirmed lymph node metastasis from prostate cancer. Androgen deprivation therapy was started and 2 month later, serum PSA declined to below 1.0 ng/ml.

[A case of skin cancer diagnosed 21 days after renal transplantation].

The patient was a 67-year-old man who was started on peritoneal dialysis for treatment of diabetic nephropathy in March 2010. He received an ABO-compatible living-donor kidney transplant from his wife in October 2010. The immunosuppressive regimen consisted of tacrolimus, mycophenolate mofetil, steroid and basiliximab. Before the operation, a bump on his forehead/temple region that was increasing in size for years was noted. The bump had a scaly surface and the top of the bump was sloughed on postoperative day 14. Histological examination suggested malignancy. On postoperative day 21, a skin biopsy was performed by dermatologists and squamous cell carcinoma was confirmed. On postoperative day 36, wide excision and transposition flap procedures were performed by the plastic surgeon. At 15 months after transplantation, the kidney graft was functioning well with a serum creatinine level of 0.84 mg/dl and there was no sign of recurrence of the squamous cell carcinoma.

[A case of myxofibrosarcoma of the bladder].

A 43-year-old woman presented to our hospital with the chief complaints of gross hematuria and dysuria. Cystoscopy and magnetic resonance imaging showed a tumor on the dome of the bladder and large blood clots. Computed tomography demonstrated no findings of distant metastasis. Following transurethral resection of the tumor, the tumor was histologically diagnosed as myxofibrosarcoma with muscular invasion, and partial cystectomy was performed in September 2009. There has been no evidence of recurrence or metastasis for 24 months postoperatively. In addition, the Japanese literature on myxofibrosarcoma of the bladder was reviewed and discussed.

[Two cases of urolithiasis induced by topiramate].

Topiramate is an antiepileptic medicine that has been used adjunctively in the treatment of refractory seizures in Japan since 2007. Topiramate has been shown to inhibit specific carbonic anhydrase activity in the kidney and may induce a distal type of renal tubular acidosis. Case 1 : A 22-year-old male was referred to our hospital after complaining of left flank pain. He developed a seizure disorder and had been using topiramate for 4 months. Drip infusion pyelography showed a left ureteral stone. Case 2 : A 7-year-old boy presented with gross hematuria. He developed West syndrome and had been using topiramate for 6 months. A computed tomographic scan showed a right kidney stone.

[Early initiation of antiplatelet therapy after urological surgery : a prospective study].

In recent times, the number of patients receiving antiplatelet drugs for the prevention of cardiovascular and cerebrovascular diseases has been increasing. We examined the possibility of early initiation of antiplatelet therapy after urological operations. Between April 2008 and February 2009, 62 patients who received antiplatelet drugs and underwent urological surgeries (open surgery, transurethral surgery and laparoscopic surgery) and prostate biopsies were examined. Of the 62 patients, 59 were randomized into 2 groups ; 32 patients receiving antiplatelet treatment initiation within 24 hours (early group) and 29 patients receiving this treatment more than 24 hours (late group) after the urological operation. The end point of this study was the re-cessation of antiplatelet therapy because of the development of postoperative complications (hematuria, blood loss, etc.) and cardiovascular and cerebrovascular events within 1 month. There was no significant difference in the urological events observed between these groups, including 2 of the 32 (6.3%) patients in the early group and 3 of the 27 (11.1%) in the late group. Cardiovascular and cerebrovascular diseases were not noted in any of the patients within 1 month. In conclusion, we think that it is possible to initiate antiplatelet therapy within 24 hours after urological operations and prostate biopsies in the absence of active blood loss. Early initiation may prevent the risk of cardiovascular and cerebrovascular disease in the future.

[A case of urethrovaginal fistula caused by a foreign body in the vagina].

A 25-year-old woman had a urethrovaginal fistula caused by a foreign body in her vagina. The patient had sought an appointment with a gynecologist for removal of the foreign body in her vagina. However, one day before the scheduled appointment, she developed acute urinary retention and visited the emergency room of our hospital. A urinary catheter inserted into the urethra was found to come out through the vagina. The foreign body, a bottle cap made of polypropylene and measuring 48 x 28 mm in size, was removed. A cystourethroscopic examination confirmed the presence of the urethrovaginal fistula. Repeat cystourethroscopy performed after one month of conservative management showed a persistent urethrovaginal fistula, which had, in fact, increased in size as compared with that at the initial examination. Surgery was undertaken for repair of the fistula ; fistula closure was successfully accomplished by suture in three layers : urethral wall, subcutaneous tissue, and the vaginal wall. This is the second report of a urethrovaginal fistula caused by a foreign body in the vagina.

[A case report: retroperitoneoscopic nephrectomy for a giant hydronephrosis of a horseshoe kidney].

A 30-year-old female was referred to our hospital complaining of left flank pain. She was diagnosed with a giant hydronephrosis in a horseshoe kidney. We performed a retroperitoneoscopic nephrectomy on the non-functioning moiety of the horseshoe kidney. After the placement of a ureteral catheter, she underwent a retroperitoneal nephrectomy. The feeding vessels consisted of four arteries and four veins. The thin isthmus of the horseshoe kidney was divided using scissors, without the need for electrocautery, and hemostasis was achieved using monopolar shears. Laparoscopic nephrectomy on a horseshoe kidney is a difficult surgery given the aberrant vessels and isthmus, so it tends to be avoided for reasons of safety. However, if appropriate preoperative imaging is carried out and the procedure is conducted in a careful manner, it can be made a safe and minimally invasive operation.

[Primary signet-ring cell carcinoma of the urinary bladder: a case report].

We report a case of signet-ring cell carcinoma of the urinary bladder. A 60-year-old man was hospitalized because of total macrohematuria. Cystoscopic examination revealed a non-papillary sessile tumor on the posterior wall of the urinary bladder. The pathological diagnosis was stage pT1 signet ring cell carcinoma. Upper gastrointestinal endoscopy and computed tomographic scanning revealed no involvement of other organs. Radical cystectomy and creation of an ileal neobladder were performed. The histopathological stage was pT3aN0M0. Adjuvant chemotherapy (TS-1) was performed and the patient is currently free from disease at eight months after the surgery. This disease is usually diagnosed at an advanced stage and has a poor prognosis. To our knowledge, this is the first case report on the creation of an ileal neobladder for the treatment of primary signet-ring cell carcinoma of the urinary bladder.

[Scrotal hematoma associated with idiopathic thrombocytosis: a case report].

We report a case of acute scrotal hematoma associated with idiopathic thrombocytosis. A 75-year-old man visited our hospital for the treatment of a left scrotal mass that had been increasing in size; the mass had developed after the puncture of left testicular hydrocele. The patient was diagnosed with acute scrotal hematoma on the basis of ultrasonography findings. The patient underwent an emergency operation for the removal of the hematoma. On 2 days after the surgery we noticed an increase in the size of the hematoma. The patient had a 4-year clinical history of idiopathic thrombocytosis for which he had not received any treatment. Although the platelet count was slightly high at the time of the operation, complete hemostasis did not occur because of the existence of platelet dysfunction. The second hematoma was treated conservatively. To our knowledge, this is the first case report on the acute scrotal hematoma associated with idiopathic thrombocytosis.

[Subtotal cystectomy and ileal substitution cystoplasty for complicated vesicovaginal fistula: a case report].

A 68-year old female underwent laparoscopic vaginal hysterectomy for uterine wall perforation, following the removal of an intrauterine contraceptive device (IUD). The patient entered our hospital complaining of persistent genital bleeding, lower abdominal pain and urinary incontinence. She was diagnosed with a vesicovaginal fistula. The diameter of the fistula was over 3 cm and extended from the trigone to the internal urethral orifice, complicating the right distal ureteral obstruction. Therefore, curative surgery required a subtotal cystectomy and substitution cystoplasty due to severe urothelial changes, hydronephrosis and poor bladder compliance. An ileal neobladder (modified Studer's method) was successfully created and the postopertive course was uneventful. Although minor urinary incontinence persists, she can void through the urethra which has improved her quality of life.

[Vesicosigmoidal fistula caused by diverculitis: report of cases and literature review in Japan].

BACKGROUND: In Japan, patients suffering vesicosigmoidal fistula caused by diverculitis is increasing. Our aim is to report our seven cases and the literature review related with this disease. METHODS: A retrospective record review of seven patients in our hospital who were diagnosed and treated for vesicosigmoidal fistulas over a 12-year period from 1994 was performed. Data collection focused on symptoms, diagnostic studies, and methods of management. RESULTS: All of the patients were male whose ages ranged from 41 to 82 years, with a mean age of 60.7 years. All of the patients presented with some of the common presenting symptoms of pneumaturia, fecaluria, irritation, abdominal pain, recurrent urinary tract infection, macroscopic hematuria. In all cases, abnormal cystoscopic findings were observed. Onestage colectomy with partial cystectomy was underwent in all cases. CONCLUSION: Many of the patients suffering from vesicosigmoidal fistula caused by diverticulitis have urological symptoms. So the above mentioned examinations are required when the outpatients complained of pneumaturia, fecaluria, irritative voiding symptoms, reccurent urinary tract infection. After diagnosed, surgical treatment is the most standard therapy and when the appropriate operative method is selected, postoperative prognosis is favorable.

Selenazoles (selenium compounds) facilitate survival of cultured rat pheochromocytoma PC12 cells after serum-deprivation and stimulate their neuronal differentiation via activation of Akt and mitogen-activated protein kinase, respectively.

The activation of extracellular receptor kinase (ERK) is one of the checkpoints to assess the activation of the classical Ras/mitogen-activated protein kinase (MAPK) cascade. Therefore, we tested more than 100 selenium-containing compounds for their ability to activate the MAPK signal pathway. Among them, we found that three selenazoles, 5-chloroacetyl-2-piperidino-1,3-selenazole (CS1), 5-chloroacetyl-2-morpholino-1,3-selenazole (CS2), and 5-chloroacetyl-2-dimethylamino-1,3-selenazole (CS3), induced the phosphorylation of ERK. These compounds also enhanced the phosphorylation of Akt, a signal transducing protein kinase for cell survival; and this phosphorylation was followed by suppression of cell death, thus suggesting that they had anti-apoptotic effects. Moreover, CSs 1-3 induced neurite outgrowth and facilitated the expression of neurofilament-M of PC12 cells, demonstrating that they induced neuronal differentiation of these cells. On the other hand, the CS-induced phosphorylation of MAPK was enhanced by buthionine sulfoximine (BSO), an activator of protein tyrosine phosphatases (PTPs), but inhibited by N-acetyl-l-cysteine (NAC), an inhibitor of receptor tyrosine kinase. These results imply that activation of some receptor tyrosine kinase(s) is involved in the mechanism of action of CSs 1-3. The activation of MAPK by CSs 1-3 was suppressed by U0126, a MEK inhibitor, but not by K252a, an inhibitor of TrkA; AG1478, an antagonist of epidermal growth factor receptor (EGFR); or by pertussis toxin. These results demonstrate that the CS-induced phosphorylation of Akt and MAP kinase (receptor tyrosine kinase(s)-MEK1/2-ERK1/2) cascades was responsible for suppression of apoptosis and facilitation of neuronal differentiation of PC12 cells, respectively. Our results suggest that CSs 1-3 are promising candidates as neuroprotective and/or neurotrophic agents for the treatment of various neurodegenerative neurological disorders.

Bis-(2-amino-5-selenazoyl) ketone as a superoxide anion-scavenger.

We investigated the superoxide anion scavenging effects of 2-amino-1,3- selenazoles and bis-(2-amino-5-selenazoyl) ketones using a highly sensitive quantitative chemiluminescence method. At 166 microM, the 2-amino-1,3-selenazoles and bis-(2-amino-5-selenazoyl) ketones scavenged in the range of 10.0 to 80.0% of O(2)(-). Bis[2-dimethylamino-5-(1,3-selenazolyl)] ketone exhibited the strongest superoxide anion-scavenging activity among the six kinds of 2-amino-1,3-selenazoles and three kinds of bis-(2-amino-5-selenazoyl) ketones. The 50% inhibitory concentration (IC(50)) of bis[2-dimethylamino-5-(1,3-selenazolyl)] ketone was determined to be 37.1 microM. Thus, bis[2-dimethylamino-5-(1,3-selenazolyl)] ketone acted in vitro as effective and potentially useful O(2)(-) scavenger.

Lysophosphatidylethanolamine in Grifola frondosa as a neurotrophic activator via activation of MAPK.

We found that Grifola frondosa extracts induced the activation of mitogen-activated protein kinase (MAPK) in cultured PC12 cells, a line of rat pheochromocytoma cells. The active substance was isolated by a few chromatographic steps, including high-performance liquid chromatography, and was identified to be lysophosphatidylethanolamine (LPE) from various structural analyses. LPE from G. frondosa (GLPE) was confirmed to induce the activation of MAPK of cultured PC12 cells and was found to suppress cell condensation and DNA ladder generation evoked by serum deprivation, suggesting that the GLPE had antiapoptotic effects. Moreover, GLPE caused morphological changes in and upregulation of neurofilament M expression of PC12 cells, demonstrating that the GLPE could induce neuronal differentiation of these cells. The activation of MAPK by GLPE was suppressed by AG1478, an antagonist of epidermal growth factor receptor (EGFR), and by U0126, an inhibitor of MAPK kinase (MEK1/2), but not by K252a, an inhibitor of TrkA, or by pertussis toxin. These results demonstrate that GLPE induced the MAPK cascade [EGFR-MEK1/2-extracellular signal-regulated protein kinases (ERK1/2)] of PC12 cells, the activation of which induced neuronal differentiation and suppressed serum deprivation-induced apoptosis. This study has clarified for the first time the involvement of the MAPK signal cascade in LPE actions.

Superoxide anion-scavenging effect of 2-amino-1,3-selenazoles.

We investigated the superoxide anion scavenging effects of thirteen 2-amino-1,3-selenazoles using a highly sensitive quantitative chemiluminescence method. At 166 microM, the 2-amino-1,3-selenazoles scavenged in the range of 14.3 to 96.7% of O2-. 2-Piperidino-1,3-selenazole and 4-phenyl-2-piperidino-1,3-selenazole exhibited the strongest superoxide anion-scavenging activity among the 2-amino-1,3-selenazoles. The 50% inhibitory concentrations (IC50) of 2-piperidino-1,3-selenazole and 4-phenyl-2-piperidino-1,3-selenazole were determined to be 4.03 microM and 92.6 microM, respectively. Thus, these compounds acted in vitro as effective O2- scavengers.

Selenoureas and thioureas are effective superoxide radical scavengers in vitro.

Oxygen radicals, such as superoxide radicals, embellishing DNA, protein, lipids, etc., and carrying out the obstacle of the function of a cell is known. It depends for the oxidant level in the living body on the balance of a generation system and an elimination system of oxygen radicals, and research which controls an oxidant level in the living body is briskly done by taking in the substance which eliminates an oxygen radical. We investigated scavenging effects of superoxide radicals by selenoureas and thioureas using a highly sensitive and quantitative chemiluminescence method. At 330 nM, five selenoureas and five thioureas scavenged fractions of superoxide radicals (O2-) ranging from 8.4% to 87.6%. Among five N,N-unsubstituted selenoureas and N,N-unsubstituted thioureas 1-selenocarbamoylpiperidine and 1-thiocarbamoylpyrrolidine were the most effective scavengers. A possibility that selenoureas could use it as a new superoxide anion-scavenging substance from the result of this research became clear.

Selenocarbamates are effective superoxide anion scavengers in vitro.

We investigated the superoxide anion-scavenging effects of six selenocarbamates and four thiocarbamates, using a highly sensitive quantitative chemiluminescence method. At 333 nM, six selenocarbamates and four thiocarbamates scavenged in the range of 2.9-68.7% of O(2)*-. Se-methyl N-phenylselenocarbamate and Se-methyl N-(4-methylphenyl)selenocarbamate exhibited the strongest superoxide anion-scavenging activity among the Se-selenocarbamates. In contrast, the corresponding S-thiocarbamates had moderate inhibitory effect. The 50% inhibitory concentrations (IC(50)) of Se-methyl-N-phenylselenocarbamate and Se-methyl-N-(4-methylphenyl)selenocarbamate were determined to be 140 nM and 162 nM, respectively. Thus, these compounds acted in vitro as effective and potentially useful O(2)*- scavengers.