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The total synthesis of two decahydroquinoline poison frog alkaloids ent- cis - 195A and cis - 211A were achieved in 16 steps (38% overall yield) and 19 steps (31% overall yield), respectively, starting from known compound 1 . Both alkaloids were synthesized from the common key intermediate 11 in a divergent fashion, and the absolute stereochemistry of natural cis - 211A was determined to be 2 R , 4a R , 5 R , 6 S , and 8a S . Interestingly, the absolute configuration of the parent decahydroquinoline nuclei of cis - 211A was the mirror image of that of cis - 195A , although both alkaloids were isolated from the same poison frog species, Oophaga ( Dendrobates ) pumilio , from Panama.

The expansionable human hepatoma cell lines have potential for use in a bio-artificial liver (BAL) system for liver disease due to the shortage of donation. However, at present, bioartificial livers are incomplete and the functions need to be improved or at least maintained for a longer period. In the present study, the authors aimed to establish a novel hepatoma cell line for a longer-term or permanent artificial liver. For this purpose, bcl-2, an anti-apoptosis gene, was introduced into hepatoma HepG2 cells. Over-expression of Bcl-2 significantly inhibited apoptosis. After 15 d of serum-deprived culture, the viability of HepG2-Bcl2 was 51% while that of mock transfectant (HepG2-mock) was decreased to 14%. In the presence of hygromycin B, HepG2-mock were dead by day 6, while the HepG2-Bcl2 viability at day 9 was 65%. Over-expression of Bcl-2 prolonged the period of the stationary phase in the growth curve and did not affect the growth rate during the exponential phase. To test the liver function, albumin production was measured. After 10 d of culture, the albumin concentration in the culture supernatant of HepG2-Bcl2 was 30 ng ml(-1), while that of HepG2-mock was 23 ng ml(-1). The cytochrome P-450 activity per culture of 3-methyl-cholanthrene-treated HepG2-Bcl2 was double that of treated HepG2-mock. Introduction of Bcl-2 was effective for the generation of a novel hepatoma cell line for artificial livers.

We report early detection of bile leakage into the thoracic cavity by hepatobiliary scintigraphy in a rare case of spontaneous withdrawal of the catheter for percutaneous transhepatic cholangiographic drainage (PTCD). An 81-year-old man with inoperable carcinoma of the common bile duct was readmitted with a 38 degrees C fever and suspected bile leakage from the hepatic biliary tree following withdrawal of the catheter for PTCD. While plain X-ray immediately after readmission revealed no abnormality in the chest or abdomen, hepatobiliary scintigraphy revealed not only bile leakage into the right thoracic cavity but also the site of laceration. We conclude that hepatobiliary scintigraphy is a simple, non-invasive procedure useful in the early detection and localization of bile leakage following spontaneous withdrawal of the catheter for PTCD.

Twenty-two patients with completed stroke were studied to evaluate the clinical usefulness of three-dimensional (3D) surface display in brain imaging with Tc-99m HM-PAO. Perfusion defects were seen by standard 3D surface display in all 13 patients, with low density areas (LDA) extending to the cerebral cortex on X-ray computed tomography. In nine patients with LDA limited around the basal ganglia, perfusion defects were not identified by standard display alone, but six were found to have such defects by 3D surface display minus the covering upper structure. This study indicates that standard 3D surface display is useful in stereoscopically evaluating cortical defects without searching through a large number of single photon emission computed tomographic (SPECT) images. Moreover, 3D surface display minus the upper structure is effective to demonstrate defects within the brain.

A patient with secondary myelofibrosis associated with prostatic cancer gained hematologic remission after hormone therapy. Before treatment, a bone scan with Tc-99m MDP showed diffuse, increased uptake in the axial skeleton without visualization of the appendicular skeleton; a bone marrow scan with In-111 chloride revealed decreased uptake in the central marrow. Following hormone therapy, a bone scan showed an almost normal distribution with visualization of the appendicular skeleton and bone marrow scan indicating improved uptake of the central marrow. Radionuclide bone and bone marrow imaging was thus useful not only in diagnosing secondary myelofibrosis but also in evaluating the effects of therapy.

A multi-center clinical trial was performed to evaluate the clinical usefulness of 123I-orthoiodohippurate (123I-OIH) in patients with renal and urinary disorders. 123I-OIH was evaluated to be "safe" in all 259 cases it was injected. 123I-OIH was useful in all 248 cases analyzed for the overall clinical usefulness evaluated by the investigators. The clinical significance of the drug was also evaluated in terms of renal blood flow function, renal parenchymal function, urinary function and the ability to differentiate between renal and urinary disorders. In the comparison with 123I-OIH (90 cases), 123I-OIH was superior as evaluated by the investigators and the Committee both. In the comparison with 99mTc-DTPA (113 cases), 123I-OIH was evaluated as superior by the investigators, but no significant difference was found by the Committee. In image qualities, 123I-OIH was evaluated as superior to 131I-OIH and equal to 99mTc-DTPA by the Committee. In overall efficiency, 123I-OIH was evaluated as being more valuable than 131I-OIH in 92% of the 90 cases and more valuable than 99mTc-DTPA in 50% of the 113 cases. 123I-OIH was evaluated as being less valuable than 131I-OIH in no cases and less valuable than 99mTc-DTPA in 7% of the 113 cases. These results suggest that 123I-OIH is superior to 131I-OIH and equal or superior to 99mTc-DTPA as a radiopharmaceutical for gamma camera-renography.

The safety, clinical usefulness and the optimal dose of 123I-orthoiodohippurate (123I-OIH) were evaluated in patients with mild renal disorders. 123I-OIH was administered intravenously to 45 patients, and 39 of those patients were analyzed for the clinical usefulness. The numbers of cases analyzed were 10 for 9.25 MBq (0.25 mCi), 18.5 MBq (0.5 mCi) and 74 MBq (2.0 mCi) and 9 for 37 MBq (1.0 mCi). Neither adverse reaction nor abnormal laboratory findings due to 123I-OIH administration were observed in the 45 patients. The clinical usefulness of the drug was evaluated in terms of individual renal function, regional renal functions, renal blood flow, parenchymal function and urinary function, and ability to differentiate between the renal and urinary functions, and the overall clinical usefulness. In the evaluation by the investigators, there were no significant differences in each of these parameters among any of the doses administered. In the evaluation by the Committee, however, the usefulness with 74 MBq superior to those with 9.25 MBq and 18.5 MBq, while there was no significant differences between those with 37.5 MBq and 74 MBq. The qualities of the blood flow phase images, functional phase images, functional images, and the statistical noises of the individual and the regional kidney renograms were also evaluated by the Committee. The image qualities and the statistical noises with 37 MBq were superior to those with 9.25 MBq and 18.5 MBq except for the functional image quality, and there were no significant differences between those with 37 MBq and 74 MBq other than the regional renograms and the functional images, which were superior with 74 MBq.(ABSTRACT TRUNCATED AT 250 WORDS)

One of our co-workers was sensitized with a 1% DNCB solution in acetone. Biopsies were obtained from skin lesions 1, 2, 4, 8, 12, 24, 30, 36 and 48 hours after a challenge with 0.1% DNCB solution. In the upper dermis, a rapid decrease of tissue fibrinolytic activity was found which disappeared after 30 hours. In the lower dermis, biphasic changes were observed. Tissue fibrinolytic activity increased one hour and 12-36 hours after challenge, whereas at 48 hours, when erythema was most intensive, it decreased in comparison to the normal activity. Erythema and histological changes of the epidermis and the dermis appeared after approximately 12 hours. As for lymphocytes, T-cells were seen at first. Furthermore, B-cells were noted after approximately 30 hours when marked infiltration began to appear.

Forty-one patients with or without adrenocortical disorders were studied to evaluate the clinical usefulness of SPECT in adrenal imaging with I-131 Adosterol. In the SPECT images from this study, all glands with either normally functioning or hyperfunctioning adrenal cortices could be detected, while those glands with hypofunctioning adrenal cortices could not be detected. Particularly in transaxial and sagittal slices, the adrenal gland was identified posteriorly and was clearly distinguished from the gallbladder. In preliminary results using SPECT by a standard method, uptake in 68 detectable glands ranged from 1.7% to 4.9% in four glands with Cushing's syndrome, from 1.1% to 1.3% in seven glands with primary aldosteronism, and were distributed below 1.0% in the remaining glands with normally functioning adrenal cortices. These data show that it is possible to evaluate the adrenocortical functioning status simply by analyzing the SPECT images of the adrenal.