The antipruritogenic effect of the 70% ethanol extract obtained from Kochiae Fructus (fruits of Kochia scoparia) and its active components were investigated on a compound 48/80-induced pruritogenic model in male ddY strain mice. The extract (200, 500 mg/kg, p.o.) inhibited the scratching behavior as a pruritogenic indicator. Oleanolic acid oligoglycoside, momordin Ic, isolated from the extract also exhibited the inhibition. These results suggest that Kochiae Fructus could be used as an antipruritogenic agent and its inhibitory effect may be partially attributed to momordin Ic.
We studied the effects of nifedipine (NF) on UV-induced photohemolysis of erythrocytes in vitro. A suspension in physiologic saline of erythrocytes separated from the venous blood sample freshly obtained from a dog was prepared and used. NF is a photolabile agent, and this drug was extremely sensitive to the long wavelength (365 nm) of UV light. The most abundant photodegradation product was a nitroso-derivative which changed into a lactam-derivative in the dog erythrocyte suspension with or without irradiation. NF itself showed protective effects against photohemolysis of erythrocytes caused by 365 nm of UV light as well as hypotonic hemolysis. But NF enhanced the degree of photohemolysis under oxygen condition. The photohemolysis enhanced by NF was reduced by thiobarbituric acid, indicating an oxidative stress by a radical intermediate of NF to photohemolysis. On the other hand, the nitroso-derivative reacted with erythrocyte hemoglobin spectroscopically to change into the lactam-derivative. It is considered that NF is a phototoxic agent to cause photohemolysis by producing a radical intermediate with oxygen and unknown species of hemoglobin degraded with the nitroso-derivative of nifedipine photoproduct.
From the stems of Myrica gale var. tomentosa (Myricaceae), a new triterpenoid, myricalactone (1) was isolated together with serratenedione, serratenediol, myricolal and so on. The structure of 1 was determined as 19β-hydroxy-1, 3-dioxo-oleane-11, 13(18)-dien-28-oic acid 28, 19-lactone on the basis of chemical and spectrometric evidence including an X-ray crystallographic analysis of methyl ether of 1.
The structure of recombinant human serum albumin derived from Pichia pastoris (rHSA) was analyzed in detail. Complete amino acid analysis was performed by the phenyl isothiocyanate precolumn labeling method. The amino terminal sequence was determined by the Edman degradation. The carboxyl terminal amino acid was determined by digestion with carboxypeptidase, and the carboxyl terminal peptide fragment was analyzed by electrospray mass spectrometry. The peptide fragments of rHSA digested with Lysylendopeptidase, Endoproteinase Glu-C, or Endoproteinase Asp-N were analyzed by electrospray mass spectrometry. The complete amino acid composition, the terminal sequences and the complete amino acid sequence of rHSA agreed with the primary structure deduced from its cDNA. The elution pattern of reduced and carboxymethylated rHSA digested with Lysylendopeptidase and the elution pattern of intact rHSA digested with pepsin were respectively similar to those of plasmaderived human serum albumin (pHSA). The pattern of CD spectrum of rHSA was identical in both shape and magnitude to that of pHSA. 1H-NMR spectra of rHSA and pHSA in deuterium oxide showed the same signal patterns in the observed region (δ10.5-0.5 ppm). Cross peaks assigned to the α proton-β proton of Asp-1 (δ 4.2/2.8 ppm) and the δ proton-ε proton of lysine residues (δ 2.8-3.2/1.4-2.0) showed the same cross peak patterns and chemical shifts in two-dimensional phase sensitive double-quantum filtered 1H-1H correlation spectra of rHSA and pHSA.
In the present study, we investigated the hypolipidemic effect of F-1394, a potent and selective inhibitor of acyl-CoA : cholesterol acyltransferase (ACAT), in dogs fed with a high-fat diet consisting of regular foods, 5% cholesterol and 16% fat. The serum cholesterol levels in dogs reached the steady-state 1 week after the start of feeding of a high-fat diet and were about 2-fold greater than those in normolipidemic dogs. Graded administration of the doses of F-1394 (1-30 mg/kg/d) to the dogs fed with a high-fat diet prevented the elevation of serum cholesterol levels. In the hyperlipidemic dogs fed with a high-fat diet for 14 d before the start of the administration of F-1394, the oral administration of F-1394 at a dose of 1, 3 or 10 mg/kg/d for 21 d reduced the serum cholesterol levels in a dose-dependent manner. The estimated ID50 value was 7.2±0.3 mg/kg/dp.o. (12.1±0.5 mol/kg/dp.o.). F-1394 did not affect the body weight and no diarrhea was observed by the administration of F-1394. F-1394 at a dose of 10 mg/kg/d or more also significantly inhibited the increase of serum triglyceride levels 3 h after the feeding of high-fat diet. These results suggest that F-1394 inhibits the ACAT activity in the canine small intestine and, subsequently, the inhibition of ACAT activity contributes much to the prevention of cholesterol absorption via the gut, resulting in a decrease in serum cholesterol levels in the dogs fed with high-fat diet. Furthermore, F-1394 may also have an inhibitory effect on the triglyceride absorption via the gut, and the therapeutical use for postprandial hypertriglyceridemia is expected.
The cholecystokinin (CCK) plasma concentration of a basal level in a normal rat was at a hardly detectable level (a few pg/ml) even using the highly sensitive chemiluminescent enzyme immunoassay. In this paper, we prepared an anti-CCK F(ab')2 fragment which was made by pepsin digestion from the anti-CCK antiserum. The anti-CCK F (ab')2 fragment was immobilized to the Sepharose 4B gel activated BrCN and packed to column. We have extracted and concentrated CCK in the rat plasma using this column and the CCK assayed by the chemiluminescent enzyme immunoassay (CL-EIA) of CCK. The immunoaffinity column extraction system was more accurate and precise than a reversed phase gel extraction system. The mean recovery of CCK from the rat pooled plasma using the immuno-affinity column was 62.2% (n=12) by the proposed CL-EIA. The mean±S.E. (n=3) of the CCK concentration in the fasted rat plasma is 3.54±0.10 pg/ml. The plasma CCK concentrations of normal rats and those of camostat administrated rats, could be measured by the proposed CL-EIA using the immuno-affinity column as a pretreatment.
Experimentally measured water vapor sorption isotherms (SIe) of alkaliprocessed collagen fibers C-20 and C-30 were compared with the theoretical isotherms (SIt) to elucidate the change of the microporous structure caused by the alkali-treatment during 20 and 30 d. The amino acid compositions of the collagen fibers were analyzed, then SIts were calculated from multiplying the degree of hydrophilicity of the sorption site. The amounts of sorbed water of SIe were greater than those of SIt in the range of the water activity higher than 13%. The great difference was observed at C-20 rather than C-30. The difference between SIe and SIt was attributed to the large amount of sorbed water in the micropores. This result confirms that the change of collagen fiber during alkali process is explained by the microporous structure, not by the stability of the triple-helix structure.