PURPOSE: Idoxifene is currently entering phase II clinical trials for the treatment of advanced breast cancer. The radiolabeled idoxifene using 123I provides an opportunity for clinical pharmacology with single photon emission computed tomography (SPECT). The purpose of this study was to prepare radiolabeled idoxifene using 123I and to determine its cell uptake of breast cancer cell line. MATERIALS AND METHODS: With a view to evaluating new anticancer drugs, we are investigating the novel antiestrogen pyrrolidino- 4-iodotamoxifen (idoxifene). [123I]Idoxifene has been prepared in no-carrier-added form using a tributyl stannylated precursor which has been synthesized by means of (2-chloroethoxy)benzene with (+/-)-2- phenylbutanoic acid on the basis of previously reported standard methods. The biodistribution and dynamic behavior of the compound were investigated using the comparative breast cancer cell line, MCF-7 (estrogen receptor-positive) and MDA-MB-468 (non-estrogen receptor). RESULTS AND CONCLUSION: Acylation of (2-chloroethoxy)benzene with (+/-)-2-phenylbutanoic acid gave the versatile ketone (81%) which reacted with 1,4-diiodobenzene to give triphenylethylene as a mixture of E and Z geometric isomers, which were separated by the recrystallization in ethanol. The E-isomer was treated with pyrrolidine to give idoxifene (67%). In order to incorporate radioactive iodine into the 4-position, the 4-stannylated precursor was prepared (30%). The yield of radioiodination was 90-92% with a high radiochemical purity greater than 98%. The ratio of tumor uptake of the breast cancer cell line between MCF-7 and MDA-MB-468 was about 1.7.
Acylation ; Breast Neoplasms* ; Breast* ; Cell Line ; Estrogen Receptor Modulators ; Ethanol ; Iodine ; Pharmacology, Clinical ; Tomography, Emission-Computed, Single-Photon

No abstract available.
Atrial Natriuretic Factor* ; Humans* ; Lymph Nodes* ; Polymerase Chain Reaction*

A Morel-Lavallée lesion is a posttraumatic, closed internal degloving injury caused by shearing force abruptly separating the skin and superficial fascia from the deep fascia and creating a potential space. Blood, lymphatic fluid, and debris collect and fill the space. The most commonly affected sites are the thigh, knee, hip, and pelvic area, but the lesion can occur anywhere in the body. Among various treatments, surgical procedure is a good option if the lesion is chronic and a thick peripheral capsule has developed. We report an uncommon case of a chronic Morel-Lavallée lesion in the sacrococcygeal area, a rarely reported location, with an associated coccygeal fracture and dislocation.
Coccyx ; Dislocations ; Fascia ; Hip ; Knee ; Skin ; Subcutaneous Tissue ; Thigh

BACKGROUND AND OBJECTIVES: ovastatin, a HMG-CoA reductase inhibitor, is known to show antiproliferative effects on VSMC after vessel injury, but a large amount of the drug is needed orally for this purpose. This study investigated the effects of lovastatin given locally to injured carotid arteries of rats on reducing neointimal hyperplasia. MATERIALS AND METHOD: Lovastatin was given perivascularly to balloon-injured carotid arteries of 21 rats in 1 microM to the low-dose group, and 30 microM to the high-dose group. The control group was treated with pluronic gel only. Two weeks later, the lumen area, neointimal areas and the number of actively proliferating cells were obtained and compared. RESULTS: eointimal area was 0.113+/-0.032 mm2, 0.065+/-0.017 mm2, 0.072+/-0.017 mm2 in the control, low-dose and high-dose groups respectively. The area was significantly smaller in the treatment groups (p<0.05), but no significant difference was observed between the treatment groups. The number of actively proliferating cells per mm2 of neointimal area were 714.5+/-227.4, 688.4+/-333.7, and 1526.3+/-744.0 in the groups respectively, and the number was significantly high in the high-dose group (p<0.05). CONCLUSION: Local administration of lovastatin is effective in reducing neointimal hyperplasia after vascular injury, but extremely high doses are not needed locally for this purpose.
Animals ; Carotid Arteries* ; Carotid Artery Injuries* ; Hyperplasia* ; Lovastatin* ; Oxidoreductases ; Rats* ; Vascular System Injuries

BACKGROUND AND OBJECTIVES: Heart rate variability(HRV) reflects the autonomic integration of heart. There were many reports that HRV in patients with myocardial infarction or heart failure is an independent prognostic factor to predict fatal arrhythmia and sudden cardiac death. But, the role of HRV is still controversial in stable angina patients without history of myocardial infarction. In this study, we tried to compare HRV indices between stable angina patients and normal subjects. MATERIALS AND METHODS: Twenty-one stable anginal patients without history of myocardial infarction (mean age : 57 +/- 2 years) and twenty-one relatively healthy persons without history of coronary heart disease (mean age : 53 +/- 2 years) were included in the study and underwent 24-hour ambulatory ECG monitoring. In patients group, all underwent coronary angiography after 24-hour ambulatory ECG monitoring. HRV was analyzed over the whole 24 hours, using time and frequency domain parameters, according to time phases and coronary angiographic severity. RESULTS: There were no significant differences in age, sex and cardiovascular risk factors, except hypertension (p=.001) between two groups. HRV indices such as rMSSD, pNN50, LF, HF, LFnorm and HFnorm were significantly decreased (p<0.05) in patients group. But the angiographic severity of coronary arteries did not show any significant effect on the HRV indices in patients group. CONCLUSIONS: We observed significantly reduced HRV indices in patients with stable angina without history of myocardial infarction.
Angina, Stable* ; Arrhythmias, Cardiac ; Coronary Angiography ; Coronary Disease ; Coronary Vessels ; Death, Sudden, Cardiac ; Electrocardiography ; Heart Failure ; Heart Rate* ; Heart* ; Humans ; Hypertension ; Myocardial Infarction* ; Risk Factors

To identify the long-term survival rate and prognostic factors of AMI in Korea, total 404 patients who presented between Jan 1984 and mar 1989 at Seoul National University Hospotal were followed for and average of 24.9+/-18.2 months(range 1 to 69 months). 50 patients(12.4%) died during the in-hospital period and 25 patients(6.2%) died after discharge. Among the survivors reinfarction developled in 11 patients(3.3%). Overall survival rates were 0.87, 0.85, 0.83, 0.81, 0.79, 0.77 and event-free survival rates were 0.87, 0.84, 0.83, 0.79, 0.77, 0.72 at 1, 6, 12, 24, 36, 48 months respectively. During the in-hospital period sex, age, peak creatine kinase level, Killip class, Q wave in ECG, heart failure, and AV block in anterior infarction were of prognostic value. After discharge age, exercise duration on pre-discharge treadmill test, cardiac index, ejection fraction, and presence of heart failure were significant prognostic factors. Pre-discharge coronary angiographies were performed in 217 cases. There was no statistically significant difference in survival rate between multiple vessel disease and single vessel disease. But the more the number of involved vessels was, the higher the incidence of reinfarction was. In the group with jeopardy score less than 8, event-free survival rate was signigicantly higher. Overall survival rate was higher and reinfarction rate was lower in the group, but both were not statistically significant. On discriminant analysis of in-hospital prognostic factors, Killip class, heart failure and age were independent prognostic factors, but other factors had no additional prognostic value.
Atrioventricular Block ; Coronary Angiography ; Creatine Kinase ; Disease-Free Survival ; Electrocardiography ; Exercise Test ; Heart Failure ; Humans ; Incidence ; Infarction ; Korea ; Myocardial Infarction* ; Seoul ; Survival Rate* ; Survivors

BACKGROUND AND OBJECTIVES: Pulmonary embolism (PE) is a disease with high mortality if left untreated. But, confirmative diagnosis is difficult because many diagnostic modalities are nonspecific. Pulmonary angiography, which is considered as the gold standard diagnostic tool, is invasive, costly, time-consuming, and not always available in small centers. Echocardiography is a non-invasive and available in the emergency room without significant time delay. We investigated the role of echocardiography as a screening test in patients with suspected PE. MATERIALS AND METHODS: (A) Retrospective study: We analyzed the recorded videotapes of transthoracic echocardiography in fifty patients with confirmed PE from Jan 1995 to Aug 1999. From the frequent echocardiographic findings of those patients, positive criteria were defined as followed ( 2 among 1-5 or only 6). (1) RV or pulmonary artery dilatation (RVEDA/LVEDA 0.6) (2) RV hypokinesis (3) paradoxical septal wall motion (4) pulmonary hypertension (5) TR (moderate degree or more) (6) Visible thrombus. Although the degree of TR was less than moderate, if the degree of pulmonary hypertension was more than moderate, we considered as PE. (B) Prospective study: From Nov 1999 to June 2000, patients with suspected pulmonary embolism underwent a transthoracic echocardiography and perfusion-ventilation lung scan or chest CT. We assessed echocardiographic findings, sensitivity and specificity of the previously defined echocardiographic positive criteria for PE. RESULTS: (A) Retrospective study: The sensitivity of echocardiography for PE was 74%. (B) Prospective study: The number of enrolled patients was thirty-four. In twenty patients the diagnosis was PE. The sensitivity of echocardiography was 75% but the specificity was 14%. CONCLUSION: Echocardiography may be used as a good screening test in patients who are clinically suspicious of pulmonary embolism.
Angiography ; Diagnosis ; Dilatation ; Echocardiography* ; Emergency Service, Hospital ; Humans ; Hypertension, Pulmonary ; Lung ; Mass Screening* ; Mortality ; Prospective Studies ; Pulmonary Artery ; Pulmonary Embolism* ; Retrospective Studies ; Sensitivity and Specificity ; Thrombosis ; Tomography, X-Ray Computed ; Videotape Recording

BACKGROUND AND OBJECTIVES: Pulmonary embolism (PE) is a disease with high mortality if left untreated. But, confirmative diagnosis is difficult because many diagnostic modalities are nonspecific. Pulmonary angiography, which is considered as the gold standard diagnostic tool, is invasive, costly, time-consuming, and not always available in small centers. Echocardiography is a non-invasive and available in the emergency room without significant time delay. We investigated the role of echocardiography as a screening test in patients with suspected PE. MATERIALS AND METHODS: (A) Retrospective study: We analyzed the recorded videotapes of transthoracic echocardiography in fifty patients with confirmed PE from Jan 1995 to Aug 1999. From the frequent echocardiographic findings of those patients, positive criteria were defined as followed ( 2 among 1-5 or only 6). (1) RV or pulmonary artery dilatation (RVEDA/LVEDA 0.6) (2) RV hypokinesis (3) paradoxical septal wall motion (4) pulmonary hypertension (5) TR (moderate degree or more) (6) Visible thrombus. Although the degree of TR was less than moderate, if the degree of pulmonary hypertension was more than moderate, we considered as PE. (B) Prospective study: From Nov 1999 to June 2000, patients with suspected pulmonary embolism underwent a transthoracic echocardiography and perfusion-ventilation lung scan or chest CT. We assessed echocardiographic findings, sensitivity and specificity of the previously defined echocardiographic positive criteria for PE. RESULTS: (A) Retrospective study: The sensitivity of echocardiography for PE was 74%. (B) Prospective study: The number of enrolled patients was thirty-four. In twenty patients the diagnosis was PE. The sensitivity of echocardiography was 75% but the specificity was 14%. CONCLUSION: Echocardiography may be used as a good screening test in patients who are clinically suspicious of pulmonary embolism.
Angiography ; Diagnosis ; Dilatation ; Echocardiography* ; Emergency Service, Hospital ; Humans ; Hypertension, Pulmonary ; Lung ; Mass Screening* ; Mortality ; Prospective Studies ; Pulmonary Artery ; Pulmonary Embolism* ; Retrospective Studies ; Sensitivity and Specificity ; Thrombosis ; Tomography, X-Ray Computed ; Videotape Recording

BACKGROUND: Left ventricular contrast echocardiography has been used to evaluate congenital cardiac anomaly, valvular regurgitation, left ventricular wall motion and myocardial perfusion. The contrast agent capable of crossing the pulmonary capillary must be small, stable and echoreflective. METHODS: To make a transpulmonary contrast agent, a mixture of 8 mL of fluorocarbon (C3F8) gas, 5% human serum albumin and 5% dextrose solution was sonicated for 80 seconds. We measured the microbubble size and number of the contrast agent by Coulter counter and hemocytometer. We injected the contrast agent intravenously into the 8 mongrel dogs with systemic arterial blood pressure and heart rate monitoring. The dosage of the contrast agent was various from 0.01 mL/Kg to 0.1 mL/Kg. Echocardiographic examination was done while the contrast agent was injected. Arterial blood gas analysis was done repeatedly before and after contrast agent injection. RESULTS: The microbubble size of the contrast agent was 60.8+/-9.3 fL, and its number was 1.0 x 10 8 /mL. Left ventricular opacification was observed in all cases by intravenous injection of the contrast agent. The minimal dose for the complete opacification of the left ventricle by visual estimation was 0.05 mL/Kg. Hemodynamic variables did not change between pre and post injection of the contrast agent. CONCLUSION: Fluorocarbon based contrast agent could be used intravenously to opacify the left ventricle and it causes no hemodynamic chage in mongrel dogs.
Animals ; Arterial Pressure ; Blood Gas Analysis ; Capillaries ; Dogs ; Echocardiography* ; Glucose ; Heart Rate ; Heart Ventricles ; Hemodynamics* ; Humans ; Injections, Intravenous* ; Microbubbles ; Perfusion ; Serum Albumin

BACKGROUND AND OBJECTIVES: This study was performed to investigate the antiproliferative effect of lovastatin on vascular smooth muscle cell, especially to determine whether lovastatin induces apoptosis in vascular smooth muscle cell and the products of mevalonate pathway can reverse the antiproliferative effect of lovastatin. METHODS AND MATERIALS: Lovastatin only and lovastatin with one of the products of mevalonate pathway such as isopentenyl adenine, farnesol, mevalonate, cholesterol were added respectively in cultured rat vascular smooth muscle cells stimulated with 10% fetal calf serum. DNA synthesis was measured by tritiated-thymidine incorporation. Cell number was determined by hemocytometric counting. Cells were Giemsa-stained to evaluate morphological changes of apoptosis. Extracted DNA from the cells treated with lovastatin was assessed by gel electrophoresis. RESULTS: 1)Lovastatin inhibited DNA synthesis and cell proliferation in a dose-dependent manner. 2)The inhibitory effects of lovastatin could be reversed almost completely by mevalonate, partially by farnesol. 3)Lovastatin-treated vascular smooth muscle cells showed typical morphological changes of apoptosis. 4)A distinct ladder of DNA bands was visualized by gel electrophoresis of the DNA from the cells treated with lovastatin. CONCLUSION: Mevalonate metabolism is essential for vascular smooth muscle cell proliferation. The antiproliferative effect of lovastatin may result from the induction of apoptosis in vascular smooth muscle cells.
Adenine ; Animals ; Apoptosis ; Cell Count ; Cell Proliferation ; Cholesterol ; DNA ; Electrophoresis ; Farnesol ; Lovastatin* ; Metabolism ; Mevalonic Acid ; Muscle, Smooth, Vascular* ; Rats