Multi-substituted N-phenyl-2, 2-dichloroacetamide analogues as anti-cancer drugs: design, synthesis and biological evaluation / 药学学报

Our earlier research has shown that mono-substituted N-phenyl-2, 2-dichloroacetamide exhibited much higher anti-cancer activity than the lead compound sodium dichloroacetate (DCA). In this paper, a variety of multi-substituted N-phenyl-2, 2-dichloroacetamides were synthesized and biologically evaluated. The results showed that 3, 5-disubstituted N-phenyl-2, 2-dichloroacetamide analogues had satisfactory potency. Among them, N-(3, 5-diiodophenyl)-2, 2-dichloroacetamide had an IC50 of 2.84 micromol x L(-1) against non-small cell lung cancer cell line A549 and could induce cancer cell apoptosis.

Continuous intravenous infusion of fentanyl for pain due to stomatitis, pharyngitis, and esophagitis after hematopoietic stem cell transplantation

<b>Purpose</b>: The effectiveness of continuous intravenous infusion of fentanyl for pain due to stomatitis, pharyngitis, and esophagitis after hematopoietic stem cell transplantation (HSCT) was investigated. <b>Methods</b>: Subjects included 15 HSCT patients with pain due to mucosal damage. Continuous intravenous infusion of fentanyl was commenced at a dose of 12.5 μg/hour. Pain was controlled through an increase or decrease in volume as needed. Grade of oral mucosal damage, pain scale, and QOL index such as the number of tooth brushing or gargles were measured at the start of administration of fentanyl and at the time of maximum dosage. <b>Results</b>: The median time to start of fentanyl administration was day 7 after transplantation. The median duration of administration was 12 days. The median maximum dosage of fentanyl was 980 (range, 243.8∼3,010) μg/day, and it was reached at a median of day 5 after administration of fentanyl was started. Compared to that observed at the start of fentanyl administration, the grade of oral mucosal damage was significantly increased at the time of maximum administration. However, pain scale was significantly decreased and QOL index was maintained. <b>Conclusion</b>: Continuous intravenous infusion of fentanyl suppressed the increase of pain when mucosal damage increased, maintained QOL, and possibly contributed to selfcare. Palliat Care Res 2011; 6(2):246-252

Treatment of hepatic cysts with dehydrated alcohol sclerosing agent guided by CT / 介入放射学杂志

Objective To evaluate the clinical effects of CT guided percutaneous aspiration and sclerotherapy in treatment of hepatic cysts.Methods Sixty three patients with single(n=41)and muttiple(n= 22)hepatic cysts were undertaken CT guided pereutaneous aspiration and sclerotherapy with injection of absolute alcohol.Results Sixty three patients underwent follow-up for 3-15 months after the operation showing effective indexes as grade 0 for 4(6.39%),gradeⅠfor 8(12.69%),gradeⅡfor 23(36.51%)and gradeⅢfor 28(44.44%)cases.The total effective rate reached 93.61%.No serious complications occurred. Conclusion Sclerosing therapy with absolute alcohol is safe,economic,simple and effective for treating hepatic cysts.(J Intervent Radiol,2007,16:850-852)

Percutaneous radiofrequency ablation for liver cancer located under the diaphragm / 介入放射学杂志

Objective To evaluate the feasibility and safety in the treatment of liver cancer located under the diaphragm with cool-tip radiofrequency ablation(RFA)percutaneously under CT guidance.Methods 20 patients with total 25 lesions were treated by CT-guided RFA with cool-tip electrode involving the induced necroses.The postoperative efficacy was evaluated by enhanced CT or MRI.Results 72% lesions were completely necrotized(18/25),28% lesions were majorly necrotized(7/25).No severe complications occurred. Conclusion CT-RFA with cool-tip electrode is effective and safe in treating liver cancer located under the diaphragm.

Usefulness of CT Angiography in Patients with Intracranial Occlusive Vascular Disease of the Circle of Willis: Comparison with Conventional Angiography

PURPOSE: To assess the usefulness of CT angiography(CTA) compared with compared with conventional angiography(CA) in the evaluation of intracranial occlusive vascular disease. MATERIALS AND METHODS: We evaluated 26 patients with clinically suspected intracranial occlusive vascular disease studied with both CTA and CA. Incases where there was no vascular lesion on CA, we used CTA to retrospectively review the detection rate and size of individual vessels, and compared the findings with those obtained by CA. In cases of occlusive vascular lesion, we evaluated the degree of stenosis on CTA and compared this with the CA findings. We also measured the time taken to use both modalities. RESULTS: Sixteen patients had no vascular lesion and ten patients had occlusive vascularlesions. Compared with CA, CTA detected 97%(124/128) of normal intracranial arteies ; their diameter measured on CTA was slightly smaller than that on CA. On CTA, the degree of stenosis was correctly estimated in eight lesions, underestimated in one and overestimated in one. Examination time ranged between 15 and 20 minutes with CTA and between 40 and 60 minutes with CA. CONCLUSION: Compared with CA, CTA shows good correlation in the delineation of intracranial normal and occlusive vessels around the Circle of Willis. CTA may be an additional tool for the evaluation of the Circle of Willis in patients with suspected intracranial occlusive vascular disease. CTA may, additionally, be used as a follow-up method in patients with acute cerebral infarctions after thrombolytic therapy.

Electron Microscopic Study on Mitochondria and Cytochrome Oxidase Activity Following Acute Carbon Monoxide Exposure in Rat Myocardium

The problem of carbon monoxide intoxication has been increasing since 1950s and it is still regarded as one of the most serious public health problem in Korea. If the patients survives the acute episode, elimination of carbon monoxide occurs in the rate of a halt-time of 3 to 4 hours. Nevertheless, there may remain after effect. Therefore, the present study was desinged to elucidate the change of myocardial tissue caused by acute carbon monoxide poisoning were evaluated by electrton microscopic observation of the severity of the mitochondrial swelling and cytochrome oxidase activity, which was demonstrated by histochemical staining with diaminobenzidine(DAB). Male Sprague-Dawley rats were exposed to the carbon monoxide of 1500 ppm for 150 minutes. They were divided into two groups ; one group were treated with hyperbaric oxygenation 15 minutes after carbon monoxide exposure, the other were not treated. Rats were sacrified 6 hours, 12 hours, 1 day, 3 days, 7days, 14 days, and 21 days after carbon monoxide exposure. The specimens were collected from the apex of the heart. In the group without hyperbaric oxygenation, mitochondrial swelling subsided 21 days after carbon monoxide exposure accompained by restoration of cytochrome oxidase activity. On the other hand, with hyperbaric oxygenation, healing process was shortened. Cytochrome oxidase activity was restored 7 days after carbon monoxide exposure.