Hematological studies on black cumin oil from the seeds of Nigella sativa L.

The methanol soluble portion of black cumin oil, which is prepared by compression of seeds of Nigella sativa L., showed inhibitory effects on arachidonic acid (AA)-induced platelet aggregation and blood coagulation. By bioactive assay of AA-induced platelet aggregation, the methanol soluble part was purified to isolate a new compound 2-(2-methoxypropyl)-5-methyl-1,4-benzenediol (1) and two known compounds, thymol (2), carvacrol (3), having very strong inhibitory activity. Further, we then examined the isolated compounds (1-3) and eight related compounds by the screening test for AA-induced platelet aggregation. Compounds possessing aromatic hydroxyl and acetoxyl group had more potent activity than aspirin, which is well known as a remedy for thrombosis.

New furostanol glycosides, chinenoside IV and V, from Allium chinense.

Further studies on water-soluble components in the bulbs of Allium chinense G. Don have led to the isolation of two new furostanol saponins, chinenoside IV (1) and V (2). On the basis of chemical evidence and spectral analyses [1H-, 13C-NMR (DEPT), 1H-1H COSY (COSY45 and p-type), 1H-1H relay-COSY, 1H-13C COSY, HMBC, and FAB-MS], the structure of 1 was established as 26-O-beta-glucopyranosyl-3 beta,26-dihydroxy-23-hydroxymethyl-25(R)- 5 alpha-furost-20(22)-en-6-one 3-O-beta-xylopyranosyl(1-->4)-[alpha- arabinopyranosyl(1-->6)]-beta-glucopyranoside and that of 2 to be 26-O-beta-glucopyranosyl-3 beta, 26-dihydroxy-23-hydroxymethyl-25-(R)-5 alpha-furost-20(22)-en-6-one 3-O-alpha-arabinopyranosyl (1-->6)-beta- glucopyranoside, respectively.

PC-2, linear homoglucan with alpha-linkages, peripherally enhances the hippocampal long-term potentiation.

PURPOSE: To investigate central effectiveness of PC-2, a glucan from lichen Parmelia caperata with alpha(1-3)(1-4) linkages in the ratio 3:2, with regard to the long-term potentiation (LTP) of evoked potential. METHODS: The extent of LTP, induced by high-frequency stimulation of medial perforant pathway, was evaluated as fractional increase in population spike amplitude in dentate gyrus in anesthetized rats. RESULTS: Oral and intravenous application of PC-2 resulted in significant enhancement of LTP elicited by a weak, but not by a strong, tetanic stimulation. No influence of PC-2 on basal evoked synaptic potential was found. Bilateral adrenalectomy profoundly suppressed the positive impact of the glucan on the formation of LTP, but showed no effect upon the magnitude and time-course of population spike enhancement in vehicle-treated subjects. Two related alpha-glucans with different chemical structures did not show any effect comparable to that of PC-2. CONCLUSIONS: Peripheral application of PC-2 significantly enhances LTP in dentate gyrus in rats. Results indicate that the effect of PC-2 might be peripherally mediated and that the specific higher structure of PC-2 is crucial for its biological activity.

[Two new steroidal saponins from Allium sativum and their inhibitory effects on blood coagulability].

Six compunds were isolated from the fresh bulbs of Allium sativum L (garlic). Their structures were elucidated as proto-iso-eruboside-B (I), eruboside-B (II), iso-eruboside-B (III), sativioside C (IV), adenosine (V) and tryptophan (VI). I and III are new steroidal saponins. This paper deals with the structural determination of I and III and their effects on platelet aggregation, blood coagulation and fibrinolysis in vitro.

[Two new steroidal saponins from Allium macrostemon].

Two new steroidal saponins, macrostemonoside A and D, were isolated from the bulbs of Allium macrostemon Bung (Chinese name as Xie bai), a Traditional Chinese Medicine used for the treatment of myocardial infarction. Their structures were established as tigogenin-3-O-beta-D-glucopyranosyl(1-->2) [beta-D-glucopyranosyl(1-->3)1]-beta-D-glucopyranosyl(1-->4)-beta-D- galactopyranoside (1) and tigogenin-3-O-beta-D-glucopyranosyl(1-->2)[beta-D-glucopyranosyl (1-->3)(6-O-acetyl-beta-D-glucopyranosyl)] (1-->4)-beta-D-galactopyranoside (2) by spectral and chemical evidences. 1 showed remarkable inhibitory effect on rabbit platelet aggregation induced by ADP in vitro (IC50 = 0.065 mmol).

Hematological studies on naturally occurring substances. VI. Effects of an animal crude drug "chan su" (bufonis venenum) on blood coagulation, platelet aggregation, fibrinolysis system and cytotoxicity.

During the screening test of the animal crude drug "Chan su" (Chinese name, toad-cake), the venom of Bufo bufo gargorizans CANTOR (Bufonidae), on blood coagulation, platelet aggregation, fibrinolysis system and cytotoxicity, the ethyl acetate extract showed promotive action on platelet aggregation and remarkable cytotoxic activity on HeLa-S3 cells. Nine kinds of bufadienolides were isolated from the ethyl acetate extract by bioactivity-guided fractionation and were identified by chemical and spectral analysis.

Structures of two new fibrinolytic saponins from the seed of Luffa cylindrica Roem.

Two new fibrinolytic saponins, lucyosides N and P, were isolated from the seeds of Luffa cylindrica Roem. (Cucurbitaceae). On the basis of chemical and spectral evidence, lucyoside N was characterized as 3-O-beta-D-galactopyranosyl-(1----2)-beta-D-glucuronopyranosyl-28- O-beta-D-xylopyranosyl-(1----4)-[beta-D-glucopyranosyl-(1----3)]-alpha-L -rhamnopyranosyl-(1----2)-alpha-arabinopyranosyl quillaic acid. Lucyoside P was characterized as a gypsogenin glycoside with the same sugar moiety as lucyoside N.

Inhibitory effect of a lichen polysaccharide sulfate, GE-3-S, on the replication of human immunodeficiency virus (HIV) in vitro.

A sulfate (GE-3-S) prepared by chlorosulfonic acid treatment of GE-3, a partially acetylated beta(1----6) glucan of the lichen Umbilicaria esculenta, inhibited the cytopathic effect of human immunodeficiency virus (HIV) and suppressed the HIV-antigen expression in Molt-4 (clone 8) cells. GE-3-S also suppressed the giant cell formation of HIV-infected Molt-4 cells, and inhibited HIV-induced plaque formation by 50% at the dose of 19.5 micrograms/ml and completely at 250 micrograms/ml in MT4 cells. GE-3-S had no direct effect on the reverse transcriptase of HIV.

Hematological studies on naturally occurring substances. II. Effects of animal crude drugs on blood coagulation and fibrinolysis systems.

The effects of 112 extracts prepared from 37 kinds of animal crude drugs and a dog's filaria were investigated on the blood coagulation and fibrinolysis systems in vitro. The plasma recalcification time method was employed for the assay of blood coagulation and fibrinolytic activity was tested by the fibrin plate method. It was found that the water extracts of Bombyx Batryticatus, Carpio Fel and Holotrichiae Vermiculus showed potent inhibitory effects on blood coagulation. The methanol extracts of Phocae Thstis et Penis, Scorpion and Tabanus were promotive effect, on the other hand. As regards the fibrinolysis system, the water extracts of Agkistrodon, Lumbricus, Hirudo, Scolopendra and Scorpion and the methanol extract of Hirudo showed a remarkable activity.

A new 5'-nucleotidase inhibitor, nucleoticidin. II. Physico-chemical properties and structure elucidation.

A novel 5'-nucleotidase inhibitor, named nucleoticidin, was isolated from a fermentation broth of Pseudomonas sp. The molecular weight was estimated by gel filtration to be over 1,000,000. Nucleoticidin is composed of D-glucose and D-mannose at a molar ratio of 1.7 to 1.0. Combined analyses using chemical and physico-chemical methods, such as gas liquid chromatography and mass fragmentography, revealed that nucleoticidin has a structural unit with mannosyl residues at the terminal of a (1----4) linked D-glucosyl main chain with beta-configuration.

A case of idiopathic fatty liver detectable only by ultrasonography.

A 40-year-old man was diagnosed as fatty liver according to our ultrasonographical criteria for fatty liver, i.e., liver-kidney contrast in the ultrasound mass screening of the liver, biliary tract and pancreas. He lacked any signs or symptoms, nor any known causes of fatty liver, i.e., obesity, diabetes, hyperlipidemia, ingestion of alcohol or drugs. Liver biopsy of this patient revealed fatty change of about 50% of the hepatic lobules. It has been difficult to suspect the presence of latent fatty liver which lacked both the abnormality in the liver function test and hepatomegaly, and even impossible when it lacked any risk factors. In the future as the ultrasonography becomes more generally used as a primary screening examination, "idiopathic latent fatty liver", like this patient, will be more frequently found and this, in turn, will contribute to the progress of the epidemiology and etiology of fatty liver.

Ultrasonographical diagnosis of fatty liver: significance of the liver-kidney contrast.

In order to investigate the reliability of ultrasonography in the diagnosis of fatty liver, retrospective evaluation was made of abdominal echograms in 45 patients with various diffuse liver diseases who underwent liver biopsy within 2 weeks after the ultrasound study. Instead of the well-recognized but subjective diagnostic criterion, i.e. the bright liver pattern, liver-kidney contrast is proposed as a new criterion. The liver-kidney contrast is based on the brightness of the liver in comparison to the renal parenchyma where fatty change seldom occurs. Combination of this liver-kidney contrast with two other well-known ultrasonographical findings of fatty liver, vascular blurring and deep attenuation, enables us to grade fatty change semiquantitatively. When fatty change of over 30% in the hepatic lobule was adopted as the definition of fatty liver, the satisfaction of both liver-kidney contrast and vascular blurring presented an ultrasound diagnostic criterion for fatty liver, with sensitivity of 83%, specificity of 100%, and an accuracy of 96%.

Computed tomography in the diagnosis of fatty liver: total lipid content and computed tomography number.

Fifty-three histologically proved cases of various diffuse liver disease were studied for their computed tomography numbers (CTN). The machine used was Ohio Nuclear's Delta Scanner 50FS type and CTN was expressed by the Hounsfield unit (H). Mean CTN in each group was as follows: 66.6 +/- 2.6 H in normal control (N), 63.3 +/- 6.0 H in chronic hepatitis (CH). 61.8 +/- 7.0 H in liver cirrhosis (LC), and 44.4 +/- 10.6 H in fatty infiltration (FI). There were no significant differences among them except FI group. As N group were all above 60 H and CH and LC groups were all above 50 H, CTN below 60 H suggests chronic liver disease or fatty infiltration and CTN below 50 H strongly suggests fatty infiltration. In eleven cases where total lipid content of the liver could be be biochemically determined by the sulfo-phospho-vanillin reagent, a relation of total lipid content to CTN was studied. As a result, a significant correlation existed between them (r = -0.89; p less than 0.001). If the diagnostic criterion of fatty liver was set at total lipid content above 100 mg/g wet liver, CT criterion was estimated at CTN below 48 H from the regression formula.