Chemical Investigation and Pharmacological Action of Urushiol

Extracts was obtained from the sap flowing from the stump of Rhus Verniciflua Stokes by using alcohoI and ether as solvents. Urushiol was obtained by distilling this obtained extract fractionally. The following materials are separated from urushiol through the means of Aluminium column chromatography by which mixture solvent (ethylether, ethyl alcohol and chlorform) was used: a) Triolefinic component(A fraction), which has 3 double bonds. b) Diolefinic component(B fraction), which has 2 double bonds. c) Monoolefinic component(C fraction), which has 1 double bond. d) Hydrourushiolr D fraction), which is fully saturated. These materials were chemically confirmed, and B fraction was converted to Mehtyl ether to compare with free hydroxyl group in B fraction. The following experiments were done in order to study the relationship between the above said chemical structures and physiological means. These experiments were done under the consideration that the nucleous of urushiol, which is used as Anthelmintics among the country people, is homologue to with of Hexylresorci nol. These experiments were on anthelmintic and general pharmacological actions of urushiol. And the tissue reaction phenomena intensity and toxicity of each fraction of urushiol were comparatively experimented. The intensity of tissue reaction phenomena increased in proportion the increase of the double bonds of the side chain of urushiol, but its toxicity decreased on urushiol. Hydroxyl radical in the nucleous of urushiol influenced a little on the intensity of action, not on the physiological actions. Accordingly the effective factor is the side chain and the double bonds in the side chain

In Vitro Reactivation of Acetylcholinesterase Inhibited by Paration and PAP

Cholinesterase in human blood cells and plasm'" are inhibited in varying degrees by organophosphorus: insecticides and nerve agents through phosphorylation The phosphorylated enzymes can often be reactivated by nucleophilic compounds such as oximes and hydroxamic acids provided conversion of inhibited enzyme to a nonreactive form(aging) has not occured In this work. the effects of organophosphorus insecticides (Parathion and PAP) on membrane-bound acetylcholinesterase from human erythrocyte ghosts were studied by using automatic recording spectrophotometer according to the method of Ellman et aL Also, the influence of the oxime upon reactivation was studied. 1. There was a concenturation dependent inhibition f acetylcholinesterase by parathion and PAP. The inhibition of acetylcholinesterase by PAP was shown to be more rapid and complete than that by para thion. 2. Decreasing the concenturation of 2-PAM below 정 x lO M resulted in incomplete reactivation. At therapeutical concenturation of 2-PAM, 82.6% of the enzyme activity was restored in parathion-inhibited 'enzyme , and 64.0% in PAP inhibited enzyme. 3. In vitro reactivation by 2-PAM of PAP inhibited cholinesterase was shown to be more difficult than that of paration-inhibited cholinesterase 4. Maximal reactivation of inhibited acetylcholinesterase was noted 30 minutes after addiction of 2 -PAM and thereafter the degree of reactivation decTeased. 5. No spontaneous reactivation was noticed during rthe time of the experiment It was concluded that the rate and ease of inhibition and reactivation are dependent on the bulk of the side chain(leaving group) , and the phosphorylated oximes may act as anticholinesterase

The effect of ouabain on Ca++-troponin interaction

The possible mechanism of inotropic action of cardiac glycosides(CG) have been sought with respects to the cellular and intracellular mobi1izatiop of calcium. But calcium, which plays a triggering role in excitation-contraction coupling, acts upon the contractile protein, esp. troponin. eventually stimulates ATPase activity of actomyosin and induces the muscular contraction. Although many investigations were devoted to search for the possible effects of CG on the contractile protein, no conclusive evidence for a direct interference of CG with the physicochemical or enzymatic properties of the actomyosin is available. Present study was made to observe the effect of ouabain on the Catt-troponin interaction in the superprecipitation of actomyosion. The results are summarized as follows. 1. The initiation of the superprecipitation of natural actomyosin was delayed by adding EGTA before the superprecipitation reaction. This delayed initiation by EGT A was not affected by ouabain. 2. The addition of EGT A during the superprecipitation caused the superprecipitation curve to be declined nearly to the level before the reaction. This clearing effect of EGT A on superprecipitation was reversed by ouabain. which also accelerated curve to reach the maximum more rapidly. 3. Above effect of ouabain showed the doseresponse manner. 4. Di git onin did not show such effect as ouabain did. 5. Above effect of ouabain on the action of EGT A during the reaction also obtained from the Perry myosin B superprecipitation in the presence of troponin and tropomyosin. 6. It is suggested that ouabain affects the troponincalcium interaction and alters the binding property of calcium to the troponin

The effect of Acanthopanax glucoside on central nervous system. The effect on Conditioned Avoidance Behavior.

Acanthopanax spinosus Miq. is one of Arailaceae family plants which has been known as tonics in orient. We obtained glucoside fraction from methanol extract of Acanthopanax and observe its effect on conditioned avoidance response and emotional change in rats. Acanthopanax glucoside depressed the condi tioned responses but glucoside did not affect the learning. Acanthopanax glucoside decreased the number of fecal balls during conditioned avoidance responce. It is suggested that Acanthopanax glucoside may depress the fearfulness derived from noxious stimuli or unfamiliar enviroment

The Effect of d-amphetamine on the content of 5-hydroxytryptamine, 5-hydroxyindole 3-acetic acid and the activity of monoamine oxidase of rat brain

Amphetamine causes a variety of CNS stimulating effects and various behavioral changes in men and animals, which were first described by Piness (1930) and Alles et al. (1933). It is well known that amphetamine induces psychosis closely mimicking paran< lid schizophrenia, and has been used as a research tool for the etiologic role of Schizophrenia. Many investigators have generally believed that .amphetarnine was a prototype activator of catecholamine mechanisms in the CNS, but more recent findings strongly suggest that 5-hydroxytryptamine(5HT) is involved in, at least, some of the effects of d. amphetarnine. Also, d-arnphetamine has been known to be a reversible inhibitor of monoamine oxidase (MAO) 'with a preference for MAO type A in vitro. This present study was set up to determine if, and 'to what extent, the turnover of 5-HT is influenced >by d-amphetamine administration. 5-HT and its major metabolite, 5-hydroxyindole.:: J-acetic acid (5-HIAA) were determined fluorometri- cally at various times after the intraperitioneal inje. ction of d-amphetamine (2mg/kg) by the combined method of Curzon and Green (1970), and Shellenberger et al. ('71). Monoamine oxidase activity of whole brain towards the substrate kynuriamine was .measured by the modified method of Kraml('65). Following results were obtained: 1. 5-HT level showed a maximal increase (126. 6% of control) at 15 min post-injection and increase lasted for 30 min, and thereafter 5-HT decreased till 24 hr post- injection, and returned to nearly control level at 48 hr after injection. 2. 5-HIAA level began to decrease at 30 min postinjection, reaching lowest levels at approximately the 1 hr-4 hr post-iniection (78% of control), and returned to control level at 24 hr after injection, and thereafter the level increased to HI. 7% of control at 48 hr post-injection. 3. MAO activity showed the lowest level at 15 min post-iniection (86. 9% of control), and thereafter slightly low activity persisted (90. 3%~97. 1% of control), till 2 hr post-injection, MAO activity began to increase at 4 hr. post-injection, reaching the highest level at 24 hr post-injection (142.7% of control). 4. 5-HIAA/5-HT ratio began to decrease at 15 min post-injection, and decrease lasted for 2 hrs. Thereafter, the ratio showed to increase, reaching the highest value at 24 hr after injection (141.1% of control). We strongly suggest that 5-hydroxytryptamine turnover is influenced by d-amphetamine administration through the effect on the activity of monoamine oxidase

The Effect of Panax Ginseng Saponin on Central Nervous System in Rat -The Psychopharmacological effect of Ginseng-

The effect of Panax Ginseng saponin on central nervous system was reported by many authors. But there was no consistent opinion on central action of Ginseng. We studied the effects of Panax Ginseng saponin fraction on central nervous system through general behavior observation. open-field exploratory behavior and conditioned avoidance behavior. The results are as follow: 1) The general behavior of rat in home cage was not influenced by 2.5mg/kg of Ginseng saponin fraction. but 10mg/kg of Ginseng suppressed the general activity of rat. 2) Open-field exploratory behavior of rat was greatly increased by injection of 2.5mg/kg and 5.0 mg/Kg of Ginseng saponin fraction compared with control group. 3) ChlorpromazineCl. 25mg/g) suppressed the conditioned avoidance behavior of rat. On the other hand. Ginseng saponin fraction stimulated conditioned avoidance behavior of rat. 4) These results suggest that Panax Ginseng saponin fraction has the protective adaptogenic action

Studies on the cardiotonic effect of Aconiti tuber

The positive inotropic and the hemodynamic effects of Aconiti tuber butanol fraction were studied in excised rat auricle and in intact anesthetized rabbit. In contrast with digitalis cardiac glycoside, Aconiti tuber butanol fraction showed strong positive inotropic effect on rat auricle, which was not influenced by varying concentrations of potassium in Krebs solution. High calcium concentrations in the nutrient medium reduced the positive inotropic effect of Aco.. niti tuber butanol fraction, while low calcium shoo wed to increase the positive inotropic action. This synergistic effect of calcium with Aconiti tuber butanol fraction was similar to that of digitalis glyco.. side with calcium in a digitalis susceptible cardiac muscle preparation. In the hemodynamics of anesthetized rabbit heart rate, left ventricular diastolic pressure and systemic arterial pressure were slightly reduced by Aconiti tuber butanol fraction. Cardiac output seemed to be increased by Aconiti, but it was variable and insignificant