Decreased body temperature dependent appearance of behavioral despair in the forced swimming test in mice.

Effects of body temperature on the immobile response and brain glucose metabolism were examined in the forced swimming test in mice. The first experiment was performed to study behavior, after initial periods of vigorous activity, a characteristic immobile posture occurred when the water was 25 and 35 degrees C. However, several minutes after forced swimming at 25 degrees C, significantly decreased spontaneous motility occurred in a time-dependent manner, but no changes was observed at 35 degrees C. Our interpretation was that mechanisms of acquisition and retention of the forced swim-induced immobile response differed. Body temperature was also significantly decreased at 25 degrees C but not at 35 degrees C in the forced swimming test. This lowering of body temperature almost paralleled the immobile response. The second experiment was a biochemical study in which the uptake of [(14)C] 2-deoxy-d-glucose into the brain significantly decreased after forced swimming at 25 degrees C but did not change in the forced swim loaded mice when the water was 35 degrees C. These results suggested two types of immobile mechanisms in the forced swimming test: (1) an early phase acquisition of the immobile response which might be related to adaptive response and (2) a late phase to retain the immobile response which might be related to the decrease in brain glucose metabolism.

Inhibitory effects of dehydrocorydaline isolated from Corydalis Tuber against type I-IV allergic models.

An alkaloidal component, dehydrocorydaline (DHC) isolated from Corydalis Tuber (tuber of Corydalis turtschaninovii forma yanhusuo), has been screened for activity against types I-IV allergic reactions. In a type I allergic models, DHC at a dose of 0.5 mmol/kg, p.o. inhibited 48 h homologous passive cutaneous anaphylaxis (PCA) in rats, which is related to IgE. DHC also exhibited an inhibitory effect on antigen-induced histamine release from peritoneal mast cells. In a type II allergic model, DHC did not inhibit reversed cutaneous anaphylaxis (RCA) in rats. In a type III allergic model, DHC showed weak inhibition on direct passive arthus reaction (DPAR) in rats. Furthermore, in a type IV allergic model, DHC had inhibitory effects on the induction phase and effector phase in picryl chloride-induced contact dermatitis (PC-CD). These results indicated that DHC not only inhibits antibody-mediated allergic reactions but also influences cell-mediated allergia reactions, and the inhibitory effect of Corydalis Tuber on allergic reactions may be partially attributed to DHC.

Studies on rehmanniae radix. I. Effect of 50% ethanolic extract from steamed and dried rehmanniae radix on hemorheology in arthritic and thrombosic rats.

Effects of 50% ethanolic extract (JR-ext) from Chinese Rehmanniae Radix (the steamed and dried root of Rehmannia glutinosa, "Jyuku-Jio" in Japanese) on the hemorheology of inflammatory, thrombosic and intact animals were examined in the in vivo models. JR-ext (200 mg/kg, p.o.) inhibited the reduction of fibrinolytic activity and erythrocyte deformability, the decrease in erythrocyte counts and the increase in connective tissue of the thoracic artery in a chronic inflammatory model, adjuvant-induced arthritis. However, JR-ext was ineffective on the development of edema in the arthritic rats and on acute and chronic inflammation. JR-ext inhibited the reduction of erythrocyte deformability, but not the decrease of coagulative factors in a thrombosic model, endotoxin-induced disseminated intravascular coagulation (DIC). JR-ext also showed a promoting effect on erythrocyte deformability and fibrinolytic activity in intact rats. These results suggest that orally administered JR-ext can prevent an inducement of impediment in the peripheral microcirculation of various chronic diseases through the improvement of hemorheology.

Anti-inflammatory activities of methanolic extract and alkaloidal components from Corydalis tuber.

A methanolic extract (CM-ext) from Corydalis tuber (Corydalis turtschaninovii Besser forma yanhusuo Y. H. Chou et C. C. Hsu) has been screened for activity in experimental models of inflammation. CM-ext (200 or 500 mg/kg, p.o.) inhibited an increase in vascular permeability in mice induced by acetic acid, and reduced acute paw edema in rats induced by compound 48/80 or carrageenin. CM-ext suppressed the development of adjuvant-induced edema in arthritic rats. CM-ext and its alkaloidal components, dehydrocorydaline, d-glaucine and l-tetrahydrocoptisine inhibited compound 48/80-induced histamine release from peritoneal mast cells of rats. Since these substances from C. tuber were found to be effective in both the acute and chronic phases of inflammation, the crude drug C. tuber can be considered to exert anti-inflammatory activity.

[Pharmacological studies on leaf of Arctostaphylos uva-ursi (L.) Spreng. IV. Effect of 50% methanolic extract from Arctostaphylos uva-ursi (L.) Spreng. (bearberry leaf) on melanin synthesis].

Effects of 50% methanolic extract (U-ext) from the leaf of Arctostaphylos uva-ursi (L.) Spreng. (bearberry leaf) on melanin synthesis were investigated in vitro. The U-ext and arbutin isolated from the bearberry leaf had an inhibitory effect on tyrosinase activity. Furthermore, the U-ext inhibited the production of melanin from dopa by tyrosinase and from dopachrome by autoxidation. These results suggest that the bearberry leaf was found to be an effective inhibitor of the production of melanin.

Effects of protopine on blood platelet aggregation. III. Effect of protopine on the metabolic system of arachidonic acid in platelets.

The mode of action of protopine on blood platelet aggregation was investigated in the metabolic system of arachidonic acid and in liberation of platelet activating factor using in vitro experimental models. Protopine inhibited the releases of arachidonic acid and platelet activating factor from platelet membrane phospholipids. Protopine also inhibited the conversion of prostaglandin G2 to thromboxane A2, as well as carboxyheptyl imidazole, a thromboxane synthetase inhibitor. These results indicated that protopine functions both as a phospholipase inhibitor and a thromboxane synthetase inhibitor. It is expected that protopine can be applied for treatment of thrombosis as an antiplatelet drug.

Effects of protopine on blood platelet aggregation. II. Effect on metabolic system of adenosine 3',5'-cyclic monophosphate in platelets.

The mode of action of protopine on rabbit platelet aggregation was investigated in the metabolic system of adenosine 3',5'-cyclic monophosphate (cyclic AMP) in vitro experimental models. The inhibitory activity of protopine on adenosine 5'-diphosphate induced platelet aggregation was increased in the presence of prostaglandin I2 or papaverine in platelets. Protopine elevated content of the basal cyclic AMP accumulation in platelets and enhanced activity of crude adenylate cyclase prepared from platelets, but was ineffective on cyclic AMP phosphodiesterase. It is concluded that protopine has an inhibitory activity on platelet aggregation, activates adenylate cyclase and increases cyclic AMP content in platelets, in addition to other inhibitory actions in the metabolic system of cyclic AMP.

[Phagocytic activity of leaves of Epimedium species on mouse reticuloendotherial system].

Effects of a 70% methanolic extract (E-S) from the dried leaves of Epimedium sagittatum on a phagocytic activity of reticuloendothelial system were studied by the carbon clearance method in mice. The clearance-rate of carbon significantly increased 1 h after the oral administration of E-S (200 or 500 mg/kg, one time/d for 5d). E-S activated the phagocytosis of carbon by Kupffer cells in the liver. Icariin and epimedin C isolated from E-S also activated the phagocytosis. These results suggest that E-S promotes the phagocytic activity of the reticuloendothelial system in mice and has a stimulatory effect on macrophage.

Studies of Panax japonicus fibrinolysis.

The effects of a 70% methanol extract (PMe) obtained from the rhizomes of Panax japonicus C. A. Meyer on experimental thrombosis and fibrinolysis were investigated in vivo and in vitro. PMe showed a promotive effect on the activation of the fibrinolytic system as determined by the euglobulin lysis time (ELT) assay but was inactive to the inhibitory effect against endotoxin-induced disseminated intravascular coagulation (DIC) in rats. PMe and its major components, chikusetsusaponin III, IV, and V, strongly promoted the action of urokinase in fibrin plate. These results suggested that PMe promotes the fibrinolysis and its effective components are chikusetsusaponin III, IV, and V.