In vivo evaluation of a new sealant material on a rat lung air leak model.

The ability of an albumin-based hydrogel sealant (ABHS) to prevent air leakage through the suture line after pulmonary surgery was evaluated by comparison with that of a fibrin glue (FG). As an air-leak model, a rat lung was used in which a standard incision was made and the burst pressure for ABHS and FG was measured. The average burst pressures at time 0 for the FG and ABHS groups were 30.8+/-15.2 and 77.5 +/-19.1 mmHg, respectively. At Day 3, the value of ABHS (76.3 +/- 15.8 mmHg) was still significantly higher (P<0.05) than that of FG (60.0 +/- 21.9 mmHg). At Day 7, no statistical difference was observed between the FG group(71.2 +/- 18.6 mmHg) and the ABHS group(88.8 +/- 11.7 mmHg). Histological examination of the incision at Day 14 revealed that neither sealant was not visible at the incision site, and there was no evidence of adverse tissue reaction. It was concluded that ABHS had good sealing properties and is an alternative to FG for air leakage treatment in pulmonary surgery.

Ardisiphenols A-C, novel antioxidants from the fruits of Ardisia colorata.

Novel alk(en)ylphenols, named ardisiphenols A--C (1--3) were isolated from the fruits of Ardisia colorata, together with known alk(en)ylresorcinols (4--6). Their structures were determined by the NMR and MS/MS analyses. All compounds showed scavenging activities towards 1,1-diphenyl-2-picrylhydrazyl (DPPH) radical and cytotoxicities against murine breast cancer cell line, FM3A.

[Characteristics of Papaver somniferum L. cv. ikkanshu cultivated in Izu].

The seeds of Papaver somniferum L. cv. Ikkanshu were sown in November (Autumn sowing: AS) and March (Spring sowing: SS) in a field at Izu Experimental Station for Medicinal Plants of National Institute of Health Sciencs, and both AS and SS plants were cultivated to investigate their growth, opium yield and alkaloid content in the opium. Growing periods from the sowing to the opium harvest were approximately six months for AS plants and three months for SS plants. Sizes of plants and capsules in AS were bigger than those in SS, reflecting their growth period. Opium yields per an are in AS and SS were 212.09 g and 142.03 g, respectively. The opium was able to be collected four times in the AS plants though the SS plants ceased to exude opium after the second incision. Therefore higher yield of opium in AS plants seems to be attributed to an amount of opium in the third and fourth incision. Average morphine content in the total opium was 15.61% in AS plants and 15.04% in SS plants, and the estimated amounts of morphine per an are in AS and SS plants were 33.16 g and 21.38 g, respectively.

[Anti-dermaptophyte activity of phenolic compounds in "mokusaku-eki"].

"Mokusaku-eki," a kind of pyroligneous acid, is a dark brown color solution obtained from the charcoal burner of such Quercus spp. woods as a by-product. This is used as a folk medicine in water eczema. The n-hexane fraction of this solution contained several phenolic compounds such as 4-ethyl-2-methoxyphenol (3) and 2,6-dimethoxyphenol (4), which could not be found in the fresh woods. Among these compounds, 3 has the highest anti-dermaptophyte activity against Trichophyton mentagrophytes at minimum inhibitory concentration (MIC) 150 micrograms/ml.

Gene expression of insulin signal-transduction pathway intermediates is lower in rats fed a beef tallow diet than in rats fed a safflower oil diet.

To elucidate the effects of dietary fatty acid composition on the insulin signaling pathway, we measured the gene expression of the earliest steps in the insulin action pathway in skeletal muscle of rats fed a safflower oil diet or a beef tallow diet. Rats were meal-fed an isoenergetic diet based on either safflower oil or beef tallow for 8 weeks. Both diets provided 45%, 35%, and 20% of energy as fat, carbohydrate, and protein, respectively. Insulin resistance, assessed from the diurnal rhythm of plasma glucose and insulin and the oral glucose tolerance test (OGTT), developed in rats fed a beef tallow diet. Body fat content was greater in rats fed a beef tallow diet versus a safflower oil diet. The level of insulin receptor mRNA, relative expression of the insulin receptor mRNA isoforms, and receptor protein were not affected by the composition of dietary fatty acids. The abundance of insulin receptor substrate-1 (IRS-1) and phosphatidylinositol (PI) 3-kinase mRNA and protein was significantly lower in rats fed a beef tallow diet versus a safflower oil diet. We conclude that long-term feeding of a high-fat diet with saturated fatty acids induces decrease in IRS-1 and PI 3-kinase mRNA and protein levels, causing insulin resistance in skeletal muscle.

Isolation of camelliaside C from "tea seed cake" and inhibitory effects of its derivatives on arachidonate 5-lipoxygenase.

A new flavonol glycoside, camelliaside C, was isolated from "tea seed cake" prepared from the defatted seeds of Camellia sinensis O. Kuntze. The structure was determined as kaempferol 3-O-beta-D-galactopyranosyl-(1-->2)-beta-D-glucopyranoside by spectroscopic methods (FAB-MS, UV, IR, 1H- and 13C-NMR) and the enzymatic transformation of camelliaside C to astragalin. Camelliaside C showed an inhibitory effect on the arachidonate 5-lipoxygenase of RBL-1 cells (IC50:1.4 x 10(-4)M) as did camelliaside A and B isolated from the same product.

[A new lupin alkaloid, (-)-leontalbinine N-oxide, in Sophora flavescens var. angustifolia seeds and its synthesis by biomimetic transformation from (+)-matrine N-oxide].

The possibility of the biomimetic transformation of (+)-matrine N-oxide, a main alkaloid in Sophora flavescens var. angustifolia, under various oxidative conditions was examined by the use of several metallic ions. When (+)-matrine N-oxide was warmed with FeSO4, or Fe(COOH)2 in MeOH-H2O at 40 degrees C, (-)-7, 11-didehydromatrine [(-)-leontalbinine], a minor alkaloid in the same plant, was obtained along with (+)-matrine. This selective formation of (-)-leontalbinine seems to be specific to the reaction of (+)-matrine N-oxide with ferrous reagents. In addition, the structure of the newly isolated minor lupin alkaloid from the seeds of S. flavescens. was determined as (-)-leontalbinine N-oxide from its spectral comparison with the authentic sample.

Two flavonol glycosides from seeds of Camellia sinensis.

Two novel flavonol triglycosides, camelliaside A and B, have been isolated from seeds of Camellia sinensis. The structures were determined to be kaempferol 3-O-[2-O-beta-D- galactopyranosyl-6-O-alpha-L-rhamnopyranosyl]-beta-D-glucopyranoside and kaempferol 3-O-[2-O-beta- D-xylopyranosyl-6-O-alpha-L-rhamnopyranosyl]-beta-D-glucopyranoside on the basis of spectroscopic, chemical and enzymatic studies. These types of interglycosidic linkages, Gal(1----2)[Rha(1----6)]Glc and Xyl(1----2)[Rha(1----6)]Glc, have not been reported previously in flavone and flavonol glycosides.

Synthesis of entadamide A and entadamide B isolated from Entada phaseoloides and their inhibitory effects on 5-lipoxygenase.

Two new sulfur-containing amides, entadamide A (1) and entadamide B (2), isolated from the seeds of Entada phaseoloides, were synthesized by the addition reaction of methanethiol to propiolic acid (5) followed by condensation with ethanolamine by the use of dicyclohexylcarbadiimide. These compounds inhibited the 5-lipoxygenase activity of RBL-1 cells at 10(-4) g/ml. This finding suggests that entadamides A and B may be examples of a new type of antiinflammatory drug.

[A case of rectal carcinoma that disappeared following preoperative chemotherapy with an FT-207 suppository--confirmed by a thorough histologic examination of the resected specimen].

Presented is the case of a patient, a 56-year-old female, who had complained of bloody stool and constipation. A barium enema and endoscopic examination revealed a tumor (Type 2) with a crater surrounded by a thick embankment, extending from the anterior wall to the left wall of the lower rectum. Biopsy specimens of the tumor disclosed a well-differentiated adenocarcinoma. A FT-207 suppository (1500 mg/day) was administered preoperatively for 50 days (total dose 75 g). On February 16, 1987, the patient underwent an abdominoperineal excision. The resected specimen took on the appearance of a chronic ulcer with an irregular depression, measuring 2.0 x 3.0 cm in size, in the lower rectum. The histology of the lesion also indicated a chronic ulcer, the base of which consisted of fibrosis covered with regenerative mucosa. No cancer cells or nests were demonstrated even serial tissue sections. As far as the rectal carcinoma is concerned, there has been no reported case of its disappearance by preoperative chemotherapy. The above results suggest that preoperative adjuvant chemotherapy can be quite effective against an advanced rectal carcinoma.