近赤外分光法(Near-infrared spectroscopy)を用いた歯科装具の脳血流動態に及ぼす影響

広島大学(Hiroshima University)博士(歯学)Doctor of Philosophy in Dental Sciencedoctora

Pharmacology of sinomenine, an anti-rheumatic alkaloid from Sinomenium acutum

The root and stem decoctions of Sinomenium acutum Rehd. et Wils. (formerly Sinomenium diversifolius Diels, one type of Fang-chi (Chinese)) have been used as a folk remedy for neuralgia and rheumatoid arthritis in many areas of the Far East. In Japan and China various viny plants have been identified as Fang-chi (Boi in Japanese) since antiquity. This uncertain nomenclature has made it difficult to evaluate the efficacy of the Fang-chi described in the classic literature. Among traditional Fang-chi plants only Sinomeniumacutum has been demonstrated to contain the alkaloid sinomenine, which is now known to be effective in neuralgia and rheumatic diseases. Sinomenine is a unique plant alkaloid, as it potently releases histamine in association with degranulation of tissue mast cells in mammalian tissues. This action occurs preferentially in the skin and joint capsules. The released histamine is responsible for the dominant pharmacological actions of sinomenine, such as vasodilatation, increased vascular permeability, acceleration of the thoracic and peripheral lymph flow, contraction of plain muscles, increased peristalsis of the intestines, and stimulation of gastric acid secretion. At toxic doses of sinomenine, convulsive central excitation was observed in most laboratory animals. Clinical side effects encountered with high doses of injected sinomenine or of decocted Sinomenium acutum were: injection site flare, pruritus in the head and upper part of the body, edema around the lips and eyelids, and temporary cephalalgia. Most of these side effects were reduced by classical antihistamines (H1-receptor antagonists). Daily subcutaneous injections of sinomenine for more than one week produced an analgesic effect in mice. Granulation tissue growth and adjuvant arthritis induced in rats were both inhibited by daily injections of a small dose of sinomenine hydrochloride or histamine dihydrochloride. These inhibitory effects were mediated through histamine H2-receptors probably on fibroblasts (for granulation tissue growth) and on T-cells (for adjuvant arthritis), since these effects were clearly inhibited by the H2-antagonist burimamide but not by the H1-antagonist mepyramine. The anti-rheumatic effect on Sinomenium acutum are probably genuine and can probably be attributed to the histamine-releasing properties of sinomenine.</p

Dogs refractory to compound 48/80 and sinomenine

Five (21 per cent) out of 24 mongrel dogs were found to be refractory to compound 48/80 and also to sinomenine (cross-tolerance). These nonreactor dogs responded normally to PVP and tween 20 and showed normal sensitivity to histamine. The incidence was similar in both sexes. Mechanisms of this type refractoriness were discussed.</p

Dual action of antihistamines on histamine release

1. Quantitative examinations were made on the effect of benadryl and neoantergan on the histamine release in vitro from chopped skin of dogs and in vivo from rat skin. For estimation of the in vitro histamine release by biological method, a chemical procedure for separating the diffused-out histamine from mixed antihistamines was carried out. 2. Both antihistamines caused a fairly marked release of histamine from chopped skin tissues in comparatively higher concentrations. This action was synergistic with histamine-releasing effect of sinomenine and anaphylatoxin. 3. In lower concentrations, however, both antihistamines inhibited the in vitro histamine-releasing effect of sinomenine and anaphylatoxin. 4. Administration of a comparatively large amount of benadryl markedly depleted the skin histamine of a rat in vivo but smaller amount clearly suppressed the histamine depletion by subsequently administered sinomenine. 5. Based on the evidence of such dual action of antihistamines, some considerations were made on the site of action of these agents.</p

The Action of Antihistamines on the Lymph Formation and Its Effect on the Action of Some Lymphagogues

Increase of capillary permeability is the chief symptomatic reaction of various pathologic states, especially that of localized inflammation, and this is the characteristic pharmacological properties of histamine at a far smaller concentration than that of any other chemical substances (Lewis, 1927; Crammer and Hele, 1944). There are numerous observations as to the diminishing effect of antihistamines on the flare and wheal caused by histamine and the inhibition by antihistamines of localized accumulation of intravenously injected dyes, such as trypan blue, referable to intradermal injection of histamine (for refs. cf. Loew, 1947; Fe£nberg et al., 1950). As for the inhibition of capillary permeability by antihistamines, some maintain that this action is limited to the case where such permeability has been increased by histamine (Wells, Morris and Dragstedt, 1946; Netter, 1947; Rigdon, 1949), but no single and decisive conclusion can yet be given.</p

Enriched standard conjugate priors and the right invariant prior for Wishart distributions

We investigate Bayesian predictive distributions for Wishart distributions under the Kullback--Leibler divergence. We consider a recently introduced class of prior distributions, called the family of enriched standard conjugate prior distributions and compare the Bayesian predictive distributions based on these prior distributions. We study the performance of the Bayesian predictive distribution based on the reference prior distribution in the family. We show that there exists a prior distribution in the family that dominates the reference prior distribution

Formation of an inactive substrate-Cu-Enzyme complex of xanthine oxidase

In the previous papers, it has been shown that the substrate inhibition of xanthine oxidase (xanthine: O2 oxidoreductase, EC 1. 2. 3. 2) induced by excess purines requires a small amount of exogenous metallic ions. Among these ions, Cu&#178;+ was the most typical one. At any stage of enzyme reaction, the inhibition began immediately on addition of a small amount of Cu&#178;+ such as 6.6 X 10-7 M. Since the depressed activity was not restored by the addition of chelating agents such as histamine and EDTA, it was suggested that the substrate, Cu&#178;+ and enzyme form a stable inactive enzyme complex, from which chelating agent can no longer remove Cu. The present communication describes the further investigations concerned with the formation of the substrate-enzyme complex in the presence of Cu&#178;+ and with the catalytic nature of this complex on other substrate and acceptor systems.</p

Anti-inflammatory effect of antiplasmin agents,&#949; -aminocaproic acid and trans-4-aminomethyl-cyclohexane carboxylic acid, in rats

1. Both EACA and AMCHA clearly showed an anti-inflammatory effect, by intravenous, intramuscular, or oral route, against inflammatory edema produced in rats by intracutaneous injection of rabbit's anti-rat serum, carrageenin, histamine, serotonin, or bradykinin, as tested by the punch method. 2. The two compounds also showed inhibitory action against the cotton pellet granuloma when used in a larger dose. 3. There was virtually no difference between the two compounds in their anti-inflammatory activity, in spite of the fact that antiplasmin activity of AMCHA is evidently greater than that of EACA. In addition, there was no increase in fibrinolysis at the site of antiserum inflammation in rats. Therefore, it would be difficult to presume that the anti-inflammatory action of these compounds is due to their antiplasmin activity. 4. Salicylates, pyrazolidine derivatives, and non-steroidal antiinflammatory agents like flufenamic acid inhibited degranulation of isolated rat mast cells induced by compound 48/80 and also inhibited ATP-32Pi exchange reaction in rat liver mitochondria, but such actions were not observed in EACA or AMCHA. 5. Anti-inflammatory effect of EACA and AMCHA did not decrease after adrenalectomy but did become weak in hypophysectomized rats. EACA did not increase blood sugar level in normal rats so that its antiinflammatory action is not due to hyperglycemia, and the effect of hypophysectomy may not be correlated to carbohydrate metabolism. 6. Anti- inflammatory effect of EACA and AMCHA appeared more rapidly after intramuscular or oral administration than by intravenous injection but the effect was not fortified after their in vitro incubation with tissues of stomach, intestine, or liver.</p