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: 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

OBJECTIVES: Due to the heterogeneous receptor distribution and changes of receptor status over time, the biochemical measurement of estrogen receptor status of biopsy specimens is not sufficient to diagnose breast cancer. As a result, I-123 labeled estradiols have been applied for the diagnosis. The purpose of this study was to develop a suitable radioligand for imaging estrogen receptor-positive human breast tumors. METHODS: Among the various estradiol derivatives, 17alpha-[123I]iodovinyl estradiol ([123I]IVE) has been prepared from 17alpha-ethynyl estradiol. Labeling of E-17alpha-[123I]iodovinyl estradiol (E-[123I]IVE) was carried out using peracetic acid with [123I]NaI and Z-[123I]IVE labelling was archived using chloamine- T/HCl solution with [123I]NaI. Labeling yield was determined by silica thin-layer chromatography (TLC) and radiochemical purity was measured by high performance liquid chromatography (HPLC). The biodistribution of E-[123I]IVE was measured in immature female rats at 60 min, 120 min and 300 min after injection. RESULTS: The labeling yield of two isomers was 92% and 94% (E-[123I]IVE and Z-[123I]IVE, respectively). The radiochemical purity was more than 98% after purification. The highest uptake was observed at 120 min in uterus (3.11% ID/g for E-[123I]IVE). CONCLUSION: These results suggest the possibility of using E-[123I]IVE as an imaging agent for the evaluation of the presence of estrogen receptor in patients with breast cancer.
Animals ; Biopsy ; Breast Neoplasms ; Chromatography, Liquid ; Chromatography, Thin Layer ; Diagnosis ; Estradiol* ; Estrogens ; Female ; Humans ; Peracetic Acid ; Rats ; Silicon Dioxide ; Uterus

BACKGROUND AND OBJECTIVES: Many western studies have shown that primary percutaneous transluminal coronary angioplasty (PTCA) may have better clinical result over thrombolytic therapy in patients with acute myocardial infarction. There are, however, few reports about the role of primary PTCA in Korea. We reviewed the cases of primary PTCA and thrombolysis with delayed PTCA in Samsung Medical Center to compare the clinical outcomes of two treatment modalities. MATERIALS AND METHOD: This study was a non-randomized and retrospective trial. From August 1995 to March 1998, 80 AMI patients within 12 hours of symptom onset underwent primary PTCA (n=26) or thrombolytic therapy (n=54) in Samsung Medical Center. Patients who had thrombolysis were performed coronary angiography fourth to fifth hospital day routinely. Risk factors and time to treatment (pain-to-needle time and door- to-needle time) were reviewed from patient record. Angiographic data including TIMI flow were obtained from angiography data base and angiographic film. We compared the 30-day and 8-month event rate of death, re-infarction, re-PTCA, and CABG between two groups. RESULTS: Baseline characteristics (sex, age, blood pressure, heart rate, AMI location, ejection fraction of left ventricle) were similar between two groups. There was no statistically significant difference in pain-to-needle time and door-to-needle time between two groups. The 30-day mortality rate was similar between two groups (primary group 3.8%, thrombolysis 5.6%, p=1.0). The 30-day event rate also showed no difference between two groups (primary PTCA 7.7%, thrombolysis 11.1%, p=1.0) and there was similar tendency in 8-month event rate (primary PTCA 19.2%, thrombolysis 14.8%, p=0.62). However, the admission duration of primary PTCA group was shorter than that of thrombolysis (8.7 vs 12 days, p=0.03). CONCLUSION: Primary PTCA have similar clinical outcome except shorter hospital admission duration when compared to thrombolysis with routine elective coronary angiography and delayed PTCA in AMI patients without cardiogenic shock.
Angiography ; Angioplasty, Balloon, Coronary ; Blood Pressure ; Coronary Angiography ; Heart Rate ; Humans ; Korea ; Mortality ; Myocardial Infarction* ; Retrospective Studies ; Risk Factors ; Shock, Cardiogenic ; Thrombolytic Therapy ; Time-to-Treatment

Coronary arteriovenous malformation (AVM) is a rare congenital coronary anomaly. We report a 60 year-old woman with variant angina and coronary AVM. She presented with recurrent chest pain at rest but there were no significant cardiovascular risk factors. Baseline coronary angiography showed the AVM which originated from first diagonal branch. Acetylcholine (Ach) provocation test was performed at left anterior descending artery (LAD) to induce coronary spasm. Ach 50 microgram injection induced severe diffuse spasm at LAD with typical chest pain. We confirmed that this patient has variant angina with AV malformation.
Acetylcholine ; Arteries ; Arteriovenous Malformations* ; Chest Pain ; Coronary Angiography ; Female ; Humans ; Middle Aged ; Risk Factors ; Spasm

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: Neurocardiogenic syncope is believed to be caused by a transient imbalance of autonomic nervous system. Actually, there were significant differences in heart rate variability (HRV) indices during head-up tilt test between patients with neurocardiogenic syncope and normal controls. But there was no definite evidence for it during daily activity. So, we tried to evaluate HRV during daily activity with 24-hour ambulatory electrocardiography monitoring. MATERIALS AND METHODS: 27 patients with neurocardiogenic syncope or presyncope (mean age 45+/-3) and 25 normal volunteers (mean age 47+/-2) comparable for age and sex underwent 24-hour ambulatory electrocardiography. Head-up tilt test was used to diagnose neurocardiogenic syncope or presyncope in patients group. HRV was analysed over the whole 24 hours, using time and frequency domain parameters. Student's t-test was applied. ResultsThere were no significant differences in HRV measures between two groups, over 24-hour period and day-time and night-time period. But the hourly HRV measures showed a transient decrease of LF, LFnorm and LF/HF ratio in patients group compared to normal control group. CONCLUSIONS: These results indicate that patients with neurocardiogenic syncope or presyncope suffer from temporarily decreased sympathetic tone with normal parasympathetic tone. So, transient additive change of autonomic nervous tone may cause syncope or presyncope in these patients. (Korean Circulation J 2000;30 (6):716-723)
Autonomic Nervous System ; Electrocardiography, Ambulatory ; Healthy Volunteers ; Heart Rate* ; Heart* ; Humans ; Syncope* ; Syncope, Vasovagal*

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