Anti-tumor activities of decursinol angelate and decursin from<Emphasis Type="Italic">Angelica gigas</Emphasis>

The in vivo anti-tumor activities of decursinol angelate (1) and decursin (2) isolated from the roots of Angelica gigas were investigated. These two compounds, when administered consecutively for 9 days at 50 and 100 mg/kg i.p. in mice, caused a significant increase in the life span and a significant decrease in the tumor weight and volume of mice inoculated with Sarcoma-180 tumor cells. These results suggest that decursinol angelate (1) and decursin (2) from A. gigas have anti-tumor activities.     

Antibacterial compounds from the leaves of<Emphasis Type="Italic">Acanthopanax senticosus</Emphasis>

Chiisanogenin (1), hyperin (2) and chiisanoside (3) were isolated from the leaves of Acanthopanax senticosus, and were tested for their inhibitory activities against 6 strains of bacteria. Among them, chiisanogenin (1) revealed broad but moderate antibacterial activities against G (+) and G (-) bacteria, the minimum inhibitory concentration (MIC) being in the range of 50-100 microg/ml.     

Ginsenoside RB<Subscript>1</Subscript> the anti-ulcer constituent from the head of<Emphasis Type="Italic">Panax ginseng</Emphasis>

We previously reported that the butanol (BuOH) fraction of the head of Panax ginseng exhibited gastroprotective activity in peptic and chronic ulcer models. In order to identify the active constituent, an activity-guided isolation of the BuOH faction was conducted with a HCl x ethanol-induced gastric lesion model. The BuOH fraction was passed through a silica-gel column using a chloroform-methanol gradient solvent system, and six fractions (frs. 1-6) were obtained. The active fr. 5 was further separated by silica-gel column, to yield 6 subfractions (subfrs. a-f). Subfr. d was composed of ginsenosides Re, Rc and Rb1. The most active constituent was ginsenoside Rb1 (GRb1), a protopanaxadiol glycoside, which was investigated for its anti-ulcer effect. Gastric injury induced by HCl x ethanol, indomethacin and pyloric ligation (Shay ulcer) was apparently reduced with oral GRb1 doses of 150 and 300 mg/kg. GRb1 at these dosage significantly increased the amount of mucus secretion in an ethanol-induced model. The anti-ulcer effects were consistent with the result of histological examination. These results suggest that the major active constituent in the head of Panax ginseng is GRb1, and that anti-ulcer effect is produced through an increase in mucus secretion.     

Synthesis and PGE<Subscript>2</Subscript> inhibitory activity of vinylated and allylated chrysin analogues

Vinylated and allylated chrysin analogues were prepared as congeners of prenylated flavonoids and evaluated their anti-inflammatory activity. 8-Substituted chrysin analogues were prepared from 2'-hydroxy-3'-iodo-4',6'-dimethoxyacetophenone in 3 steps. 3-Allylated chrysin analogues were prepared from chrysin in 3 steps. Synthesized chrysin analogues (4, 5 and 8) showed moderate inhibitory activities of PGE2 production from LPS-induced RAW 264.7 cells.     

Surface damage on open box posterior-stabilized polyethylene tibial inserts

Twenty retrieved Scorpio posterior-stabilized implants were available for analysis. The mean implantation time was 22 months (range, 2 days-42 months). Favorable types and amounts of surface damage were seen on the tibiofemoral and backsides of these modular PE liners that had been packaged in an inert environment and then sterilized by gamma irradiation. Delamination represented only 0.1% of the total surface damage. Off-axis loading (varus malalignment) was associated with tibial component loosening but there was no evidence of peripheral damage of PE caused by edge loading. With this open-box design, hyperextension marks on the anterior aspect of the posterior-stabilized post from femoral component impingement occurred in 11 of 20 cases and was related to sagittal component positioning: excess tibial slope or increased tibial slope combined with a flexed femoral component. Unique coarse abrasions occurred in 16 of 20 cases and were the result of cement extrusion into the open box, especially with varus malalignment. These observations provide guidance for optimizing the surgical technique and the design of posterior-stabilized total knee components.     

Hepatic arteries in potential donors for living related liver transplantation: evaluation with multi-detector row CT angiography

PURPOSE: To assess the accuracy of multi-detector row computed tomographic (CT) angiography in the evaluation of hepatic arterial anatomy in living related liver transplantation (LRLT) donors. MATERIALS AND METHODS: During a 10-month period, 62 potential LRLT donors were evaluated with CT and conventional angiography. Multi-detector row CT was performed after intravenous injection of 150 mL of contrast material at 3 mL/sec. CT angiograms of the hepatic arteries were generated by a radiologist who used volume rendering and maximum intensity projection techniques without knowledge of results of conventional angiography. Two reviewers reviewed CT and conventional angiograms retrospectively in consensus. The results of the two examinations were then compared. RESULTS: CT examinations were technically adequate in 56 (90%) donors. Respiratory motion artifact compromised detailed hepatic artery analysis in six donors (10%). Second-order branches of right hepatic arteries were visualized in 58 donors (94%), and second-order branches of left hepatic arteries were visualized in 51 (82%). A total of 27 hepatic arterial anatomic variations were detected in 22 donors at conventional angiography. CT angiography accurately depicted 25 (93%) anatomic variations in 20 donors (91%). CT angiography did not depict an accessory right hepatic artery in two donors. The number and origins of dominant arteries supplying segment IV were accurately identified at CT angiography in 51 donors (82%). Hepatic arterial anatomy depicted at CT angiography was identical to that at conventional angiography in 50 donors (81%). CONCLUSION: Multi-detector row CT angiography is useful but limited in its ability to depict the dominant artery supplying segment IV and small accessory hepatic arteries.     

Case report: magnetic resonance imaging of vaginal malignant melanoma

We report two cases of vaginal melanoma with magnetic resonance imaging findings. The first melanoma was a bilobular polypoid mass with melanotic and amelanotic components, which arose from the lateral wall of the vaginal canal. The melanotic melanoma showed high signal intensity (SI) on T1-weighted images and low SI on T2-weighted images, which was not suppressed by a fat-saturated sequence. Another melanoma showed a pale brown polypoid mass in the vagina, which revealed intermediate SI on T1-weighted images and high SI on T2-weighted images. On fat-suppressed images, both tumors were more clearly demonstrated with high SI.     

Peroxisome proliferator-activated receptor (PPAR)-alpha activation prevents diabetes in OLETF rats: comparison with PPAR-gamma activation

Lipid accumulation in nonadipose tissues is closely related to the development of type 2 diabetes in obese subjects. We examined the potential preventive effect of peroxisome proliferator-activated receptor (PPAR)-alpha and PPAR-gamma stimulation on the development of diabetes in obese diabetes-prone OLETF rats. Chronic administration of a PPAR-alpha agonist (0.5% [wt/wt] fenofibrate) or a PPAR-gamma agonist (3 mg x kg(-1) x day(-1) rosiglitazone) completely prevented the development of glycosuria. Pancreatic islets from untreated OLETF rats underwent sequential hypertrophy and atrophy, which was completely prevented by chronic fenofibrate treatment. In contrast, rosiglitazone treatment did not affect islet hypertrophy at earlier stages but prevented beta-cell atrophy at later stages. Fenofibrate treatment decreased body weight and visceral fat, whereas rosiglitazone treatment increased body weight. Despite the opposite effects on adiposity, both drugs were equally effective in improving insulin actions in skeletal muscle. Furthermore, both drugs significantly decreased the triglyceride content in the soleus muscle and pancreatic islets. The present study demonstrates that the PPAR-alpha agonist fenofibrate prevents the development of diabetes in OLETF rats by reducing adiposity, improving peripheral insulin action, and exerting beneficial effects on pancreatic beta-cells.     

Apoptosis and modulation of cell cycle control by synthetic derivatives of ursodeoxycholic acid and chenodeoxycholic acid in human prostate cancer cells

The effects of synthetic derivatives of ursodeoxycholic acid (UDCA), HS-1183, and chenodeoxycholic acid (CDCA), HS-1199 and HS-1200, on the proliferation of human prostate carcinoma PC-3 cells were investigated. Whereas CDCA and UDCA had no effects on the growth of cells in a concentration range we have tested, HS-1199 and HS-1200 completely inhibited the cell proliferation, and HS-1183 showed a weak inhibitory activity. This proliferation-inhibitory effect of the synthetic bile acid derivatives was due to the induction of apoptosis, which was confirmed by observing DNA fragmentation, chromatin condensation and cleavage of PARP. Flow cytometric analysis also revealed that the synthetic bile acid derivatives arrested the cell cycle progression at the G1 phase, which effects were associated with inhibition of phosphorylation of pRB and enhanced binding of pRB and E2F-1. They also suppressed Cdk2 and cyclin E-dependent kinase activities without changes of their expressions. Furthermore, the synthetic bile acids increased the levels of Cdk inhibitor, p21WAF1/CIP1, expression and activated the reporter construct of p21WAF1/CIP1 promoter in p53-independent manner, and p21WAF1/CIP1 proteins induced by the synthetic bile acid derivatives were associated with Cdk2 and proliferating cell nuclear antigen. These distinctive features suggest that it is possible to create the new drugs useful for cancer therapy from the synthetic bile acid derivatives as lead compounds.