Bile acids and bile alcohols are termed cholanoids. Biles of evolutionarily primtive vertebrates such as fishes, amphibians, and reptiles contain bile alcohols and higher bile acids in place of C24 bile acids in mammals. These higher cholanoids have the C24 bile acid type of nuclear structure and all or part of the side chain of cholesterol. The chemical structure, the natural distribution, and the biosynthetic pathways of bile alcohols and higher bile acids were studied. The results indicate that these compounds are evolutional precursors of the C24 bile acids found in mammalian species and the mechanism of the conversion of cholesterol to the C24 bile acids in mammals is a recapitulation of the evolution of cholanoid molecules.
The highly differentiated gastric parietal cell has a characteristic morphology and plays a specialized role in the hydrochloric acid secretion into the stomach lumen. The major enzyme in this system is an ATP-driven proton pump, the H+/K+-ATPase, which is responsible for proton translocation across the apical plasma membrane. The primary structures of the catalytic α and glycosylated β subunits, and their transmembrane topology are similar to those of the corresponding subunits of Na+/K+-ATPase, suggesting that the reaction mechanism of both ATPases would be essentially the same if not identical. Most of the positions of introns in the H+/K+-ATPase subunit genes are essentially the same as those in the corresponding Na+/K+-ATPase subunit gene. These findings suggest that the α and β subunit genes, respectively, of the two ATPases were derived from the common ancestors. We found that a DNA sequence motif, (G/C) PuPu (G/C) NGAT (A/T) PuPy, was located in the upstream regions of both α and β subunit genes from human and rat. This motif may be a binding site for a positive transcriptional regulator that functions specifically in the parietal cells. cDNA cloning and in situ hybridization demonstrated that novel zinc finger proteins (GATA-GT1 and GATA-GT2) are present in the gastric parietal cells. These proteins bind to the (G/C) PuPu (G/C) NGAT (A/T) PuPy motif. Furthermore, they activate the transcription of the reporter gene with the 5'-upstream region of the α or β subunit gene. These results suggest that gastric GATA DNA-binding proteins play important roles in transcriptional activation of H+/K+-ATPase genes in the parietal cells.
A series of 2, 3, 4, 5-tetrahydro-1, 5-benzothiazepine and related compounds were prepared, and the intracellular Ca2+ inhibitory effects were examined using methoxamine-or caffeine-induced contraction of isolated rabbit arteries. Structure-activity relationship studies of these compounds are discussed and the results suggest that novel 5-[3-[2-(3, 4-dimethoxyphenyl) ethyl] aminopropionyl]-2, 3, 4, 5-tetrahydro-1, 5-benzothiazepine fumarate (20d) showed the most potent inhibitory action on the intracellular Ca2+ release.
Crude drugs derived from Adiantum species are used as febrifuge, antidote, diuretic, tonic, etc. Some commercial samples of these drugs are composed of finely cut ultimate pinnules only, which have false indusia and spores. In this paper, in order to establish a classification method based on the characteristics of the ultimate pinnules and their attachments, the morphological study using stereoscope and scanning electron microscope, and X-ray microanalysis using an electron probe microanalyzer were carried out on the false indusia and spores, and the ultimate pinnules, respectively, of 19 Adiantum species. The results showed that examined all species could be distinguished from each other by the following characteristics : in the false indusium, the shape and the presence or absence of hairs ; in the spore, the shape, the ornamentation, the ratio of the laesura, and the equatorial diameter ; in the X-ray images of the ultimate pinnule, the distributional patterns of silicon and calcium. The distributional patterns of silicon were due to the presence of spicular cells, hairs and papillae, and calcium was present as crystals of calcium oxalate. The average content of silicon in the ultimate pinnules of Adiantum species was 1.99%.
The constituents of monoterpene in Paeoniae Radix were analyzed by means of high performance liquid chromatography (HPLC) using hitherto elucidated eight monoterpene glycosides, paeoniflorin 1, oxypaeoniflorin 2, benzoylpaeoniflorin 3, benzoyloxypaeoniflorin 4, galloylpaeniflorin 5, galloyloxypaeoniflorin 6, albiflorin 7 and lactiflorin 8 and a monoterpene paeoniflorigenone 9. In sixty seven kinds of Paeoniae Radix collected in Japan, China, and South and North Korea those monoterpene constituents 1-9 were found to exist in the amounts of ranging 0.12-9.61% 1, 0.06-10.8% 2, 0.02-0.79% 3, 0.24-0.47% 4, 0.25-2.53% 5, 0.05-2.86% 6, 0.09-2.76% 7, 0.35-0.64% 8 and 0.01-0.49% 9 respectively.In addition, these results obtained by the quantitative analysis were discussed from the viewpoint of the external figures and processing methods.
Four flavonoid compouds, avicularin (1), hyperin (2), quercitrin (3), taxillusin (4), were isolated from leaves of Taxillus kaempferi, and three catechin compouds, (+)-catechin (6), procyanidin B-1 (7), procyanidin B-3 (8), showing a reddish purple color on the reaction with Ehrlich reagent, were also isolated from the stems. Each of these seven isolated compounds was identified by comparing the spectral data with those of the references. Compound 8 was examined to substantiate the stereochemical configurations of conformer, a and b in the detailed 1H-nuclear magnetic resonance (1H-NMR) spectrum using the nuclear Overhauser effect (NOE) difference spectroscopy and spin decoupling experiment in the acetone-d6 solution.
The relation between constituents and effects on hemorheology with processing of root of Rehmannia glutinosa was investigated. With the processing to dried or steamed root from crude root, the content of stachyose, which was the highest component in crude root, was decreased and the content of manninotriose was increased. Iridoid glycoside, catalpol, was gradually decreased with the processing. From these results, the content of carbohydrates and catalpol made it possible to estimate the quality of Rehmanniae Radix by processings. On the other hand, the change of pharmacological activities with the processing was investigated. The 50% ethanolic extract (BJ-ext) from steamed root of R. glutinosa increased erythrocyte deformability and erythrocyte ATP contents, inhibited polybrene-induced erythrocyte aggregation, and promoted an activity of fibrinolytic system. The extracts from crude or dried root had weak or no effect. The crude or dried root and steamed root of R. glutinosa showed the different pharmacological activities, and the quality of Rehamanniae Radix by processings may be estimated by investigation of correlation between the changes of constituents and improvable effects of hemorheology.
Effects of the mixture (SK-204) consisting of dried shiitake mushroom (Lentinus edodes) treated with wet-heating and fructo-oligosaccharides (7 : 3) on the experimental models of pulmonary thrombosis induced by lactic acidosis in rats were evaluated. Chronic oral administration (10 weeks) of SK-204 significantly prevented the thrombus formation on this thrombosis model. However, decreases in the numbers of platelet and fibrinogen level by lactate were not changed by SK-204. These results suggest that SK-204 have an anti-thrombotic action, which is due to neither the inhibition of platelet aggregation nor coagulation, but probably due to the promotion of fibrinolysis and thrombolysis.