Cysteine, histidine and glycine exhibit anti-inflammatory effects in human coronary arterial endothelial cells.

The activation of nuclear factor-kappa B (NF-κB) in vascular endothelial cells may be involved in vascular pathogeneses such as vasculitis or atherosclerosis. Recently, it has been reported that some amino acids exhibit anti-inflammatory effects. We investigated the inhibitory effects of a panel of amino acids on cytokine production or expression of adhesion molecules that are involved in inflammatory diseases in various cell types. The activation of NF-κB was determined in human coronary arterial endothelial cells (HCAECs) because NF-κB modulates the production of many cytokines and the expression of adhesion molecules. We examined the inhibitory effects of the amino acids cysteine, histidine and glycine on the induction of NF-κB activation, expression of CD62E (E-selectin) and the production of interleukin (IL)-6 in HCAECs stimulated with tumour necrosis factor (TNF)-α. Cysteine, histidine and glycine significantly reduced NF-κB activation and inhibitor κBα (IκBα) degradation in HCAECs stimulated with TNF-α. Additionally, all the amino acids inhibited the expression of E-selectin and the production of IL-6 in HCAECs, and the effects of cysteine were the most significant. Our results show that glycine, histidine and cysteine can inhibit NF-κB activation, IκBα degradation, CD62E expression and IL-6 production in HCAECs, suggesting that these amino acids may exhibit anti-inflammatory effects during endothelial inflammation.

Pacovatinins A-C, new labdane diterpenoids from the seeds of Renealmia exaltata.

Three new labdane diterpenoids, pacovatinins A-C (1-3), were isolated from seeds of the Brazilian medicinal plant Renealmia exaltata ("Pacová-catinga"), and their structures including absolute configurations were elucidated by spectroscopic data and a modified Mosher method.

Porwenins A and B, new clerodane diterpenoids from Portulaca okinawensis.

Two new clerodane-type diterpenes, porwenins A (1) and B (2), were isolated from Portulaca okinawensis, and the structures were elucidated by spectroscopic data.

Acutifolins A-F, a new flavan-derived constituent and five new flavans from Brosimum acutifolium.

Acutifolin A (1), a novel constituent with a bicyclo[3.3.1]non-3-ene-2,9-dione ring, acutifolins B-F (2-6), five new flavans, and three known flavans were isolated from the bark of Brosimum acutifolium, a Brazilian folk medicine ("Mururé"). Their structures were elucidated by spectroscopic methods, including 2D NMR.

Echinophyllins C-F, new nitrogen-containing clerodane diterpenoids from Echinodorus macrophyllus.

Four new nitrogen-containing clerodane diterpenoids, echinophyllins C-F (1-4), were isolated from the leaves of the Brazilian medicinal plant Echinodorus macrophyllus ("Chapéu-de-couro"), and their structures and relative stereochemistry were elucidated from their spectroscopic data. Compounds 1-4 possess an alpha,beta-unsaturated gamma-lactam ring consisting of a clerodane diterpene unit and an amine moiety.

Chapecoderins A-C, new labdane-derived diterpenoids from Echinodorus macrophyllus.

A new seco-labdane-type diterpenoid, chapecoderin A (1), and two new rearranged labdane-type diterpenoids, chapecoderins B (2) and C (3), were isolated from the leaves of the Brazilian medicinal plant Echinodorus macrophyllus ("Chapéu-de-couro"), and their structures and relative stereochemistry were elucidated by spectroscopic data. Chapecoderins A-C (1-3) possess in common an alpha,beta-unsaturated gamma-lactone ring in the side chain.

Analysis of major components and bisphenol A in commercial Bis-GMA and Bis-GMA-based resins using high performance liquid chromatography.

The purpose of this study was to examine the quality of commercially available Bis-GMA because concerns about Bis-GMA and Bis-GMA-based resins have been recently expressed in dentistry. Four major components and bisphenol A, which is a compound of recent controversy, were quantitatively analyzed using high performance liquid chromatography (HPLC) in three commercial Bis-GMA and six Bis-GMA-based composite resins. The contents of genuine Bis-GMA, Iso-bis-GMA, Bis-GMA-H, and Bis-GMA-M as well as the total content of the four monomers were 45.7-57.5%, 19.9-26.2%, 1.8-5.0%, 0.6-15.0% and 83.7-85.6% in the commercial Bis-GMAs, or 3.8-9.1%, 1.7-4.3%, 0.1-0.5%, 0.1-2.0% and 5.8-14.0% in composite resins, respectively. There were some differences in the composition of the major components between domestic and foreign materials. Bisphenol A contents in the unpolymerized composite resins were 1.5-10.2 micrograms/g resin.

Microanalysis of a selective potent anti-Helicobacter pylori compound in a Brazilian medicinal plant, Myroxylon peruiferum and the activity of analogues.

A selective potent anti-Helicobacter pylori isoflavone was isolated from a Brazilian Medicinal Plant, Myroxylon peruiferum. The isolation bioassay-guided and the characterization of an active anti-H. pylori constituent was performed using the methanol extract of plant of minute amount. The active compound was identified as cabreuvin (1), an isoflavone derivative. The structure-activity relationships of several related compounds were also investigated.

Analysis of major components contained in Bis-GMA monomer.

The major components contained in commercial Bis-GMA monomer were isolated by thin layer chromatography (TLC) and identified by NMR and high resolution mass spectroscopy. In addition to the two major components already known (Bis-GMA and Iso-bis-GMA), an unknown hydrophilic third major component was isolated and identified as 2,2-[4-(2-hydroxy-3- methacryloyloxy-1-propoxy)-4'-(2,3-dihydroxy-1-propoxy)]dipheny lpropane. This compound was designated as BIS-GMA-H, because it has a structure of Bis-GMA with one of which methacrylic ester bond hydrolyzed.

2-aminopropionitrile polymer. I. The hydrolyzate of the basic fraction.

The basic fraction of a 2-aminopropionitrile polymer was subjected to acid hydrolysis and was analyzed by means of GC-MS, after trimethylsilylation. The fundamental polymer structural units were alanine, 2,2'-iminodipropionic acid, N-(1-cyanoethyl)alanine, N-ethylalanine, glycine, cyanoglycine, and 5-amino-4-carboxyimidazole residues. The last three units may be derived from hydrogen cyanide. Oligomeric combinations of these units were also detected in the hydrolyzate, due to partial hydrolysis of the polymer.

A double blind comparative study of tegafur (FT) and UFT (a combination of Tegafur and uracil) in advanced breast cancer.

A double blind study to compare the efficacy of oral UFT (400 mg Tegafur (FT) plus 896 mg uracil/day) with that of oral FT (800 mg/day) on advanced breast cancer was performed between November, 1986, and November, 1989. Sixty patients were registered for the trial and fifty-six cases were evaluated (28 for UFT and 28 for FT). The primary end points in the study were response rate and time to relapse. There were no significant differences in patients' characteristics in either group. The objective response rates were 39% (11/28; 95% confidence interval (C.I.), 22-59%) in UFT and 21% (6/28; 95% C.I., 8-41%) in FT, without statistical significance (P = 0.25). For time to relapse, a trend was seen in favor of UFT, but this effect did not achieve statistical significance (P = 0.09). Both subjective and objective adverse effects were similar between the two treatments. The overall survivals were similar in both parts of the study. The size of the trial was too small for a definite conclusion to be drawn although, for both response rate and time to relapse, a trend was seen in favor of UFT. A large scale randomized study will be necessary to compare the drugs in the management of patients with advanced breast cancer.

Stromelysin-3 mRNA expression and malignancy: comparison with clinicopathological features and type IV collagenase mRNA expression in breast tumors.

mRNA expression of stromelysin-3 (ST3) and 72K type IV collagenase (cIVase) in 4 human breast cancer cell lines and 55 resected breast tumors were examined using Northern blot analysis. In 4 cell lines ST3 was not expressed at all, while cIVase gene expression was detected in 3 of them. The ST3 expression was found more specifically in malignant tumors (39/40, 97.5%) than in benign ones (4/15, 26.7%), although cIVase was expressed in all tumor specimens. The quantitative analysis showed that ST3 expression in malignancies was significantly greater than that in benign tumors (P = 0.0007), while cIVase expression was not (P = 0.1381). ST3 gene expression was also closely related to the presence of lymph node metastasis (P = 0.047), while cIVase was not (P = 0.1091). These results suggest, therefore, that ST3 is expressed more specifically by stromal cells surrounding cancer cells than cIVase. Since ST3 mRNA expression was independent of the EGFR, ER and erbB2 protein expression, ST3 may be a new potent prognostic guide for breast carcinomas, which can detect highly malignant subpopulations.

[A case of complete remission in brain metastasis from lung adenocarcinoma with EAP (etoposide, adriamycin, cisplatin)].

A 61-year-old male patient who developed brain metastasis 6 months after the lung resection for adenocarcinoma was treated with the 3 courses of EAP (Etoposide 150 mg/body/course, ADR 40 mg/body/course, CDDP 100 mg/body/course). Although our doses were lesser than Preusser's, symptoms soon subsided, and brain CT revealed a complete disappearance of metastases 16 days after the beginning of the first EAP course. During 5 months of CR, the patient had enjoyed his common daily life, the relapse, however, occurred. Since brain metastasis is life threatening, such an effective regimen like EAP should be made further studies to it.

Growth fractions of breast cancer in relation to epidermal growth factor receptor and estrogen receptor.

Growth fractions detected by a monoclonal antibody, Ki-67, were examined in 40 human breast cancer tissues and the results compared with the immunocytochemical reactivities of epidermal growth factor receptor (EGFR) and estrogen receptor (ER). The proportion of proliferating cells displaying Ki-67 positive staining was significantly higher in the EGFR positive tumors than in the EGFR negative tumors (p less than 0.01). The average percentage of Ki-67 positive cells in the EGFR positive tumors was 19.9 per cent, whereas that in the EGFR negative tumors was 8.0 per cent. By contrast, an inverse relationship between the proportion of proliferating cells and ER positive cells detected by anti-ER monoclonal antibody was observed. This data indicated the difference in growth fractions with relation to the EGFR and ER status of breast cancer.

[A calcified mucinous adenocarcinoma of the stomach--case report].

The paper discusses the case of a 44-year-old woman with an epigastric discomfort at Hiroshima University Hospital. A barium study of the stomach showed rigidity and a giant fold. A subsequent abdominal roentgenogram and CT disclosed calcification throughout the stomach wall. Thus, is hopes of effecting a cure, a total gastrectomy, a partial resection of transverse colon, a splenectomy and a pancreatic tail resection were performed. A surgical specimen macroscopically presented an inelastic and thickened wall of the entire stomach, and deposits of whitish calcium were visible within the gastric wall. The pathological diagnosis indicated a mucinous adenocarcinoma, se, INF alpha, v2, ly3, n4 (No. 221), with calcification of this mucinous adenocarcinoma in the stomach.

[Studies on the constituents of Leucoseptrum stellipillum].

Flavonoids, triterpenoids, and steroids were isolated from the leaves of Leucoseptrum stellipillum (MIQ). Kitamura et Murata and identified as apigenin, luteolin, chrysoeriol, ursolic acid, pomolic acid, tormentic acid, beta-sitosterol, and beta-sitosterol glucoside by comparison of their spectral data with those of authentic specimens. Among these compounds, the triterpenoids showed significant antibacterial activities against Streptococcus mutans.