Biological & pharmaceutical bulletin
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The cathartic effect of isobarbaloin, a stereoisomer of barbaloin (compound principally responsible for the cathartic activity of Aloe), was examined in male rats by oral administration. Individual differences in sensitivity in the laxative activity of isobarbaloin and barbaloin was not found. ⋯ Also, isobarbaloin administered orally was demonstrated to decompose to aloe-emodin-9-anthrone (active metabolite of barbaloin) as well as to barbaloin. Therefore, it is considered that the mechanism underlying the cathartic effect of isobarbaloin is the same as that of barbaloin.
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A sensitive and rapid colorimetry for determination of methemoglobin (MetHb) in hemolysate of the test blood was devised by measurement of absorbance at 563 nm, the isosbestic point of spectra of cyanomethemoglobin and oxyhemoglobin, at pH 6.8. MetHb was determined as the difference in absorption caused by cyanide in the absence of potassium ferricyanide divided by the difference in absorption caused by cyanide in the presence of the ferricyanide. ⋯ Results obtained by the method were in satisfactory agreement with theoretical results for mixture of MetHb, COHb, and oxyhemoglobin. The method was compared with two other methods using 55 forensic blood samples containing various amounts of MetHb and COHb, and proved to be suitable for practical samples.
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We investigated here the effect of Hachimi-jio-gan (HJ), a Japanese and Chinese herbal medicine, on immunoglobulin A (IgA) producing cells in Peyer's patch. The oral administration of HJ (0.1, 0.2, 1.0 g/kg for 2 d) enhanced the IgA producing cells almost 2-fold compared with the control group on days 4 and 5 after the administration. Furthermore, HJ augmented antigen-specific IgA (anti-SRBC IgA) production. ⋯ To characterize its active ingredients, HJ was fractionated by ethanol precipitation. The crude polysaccharide fraction (EP fraction) showed the ability to augment IgA production, but low molecular weight fraction (ES fraction) did not. These results suggest that the crude polysaccharide fraction might be responsible for the augmentation of IgA production by HJ.
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Pharmacokinetics of metyrapone and metyrapol enantiomers was studied in the rat to determine the stereoselective reductive metabolism of metyrapone. The HPLC method using a chiral column was developed for the stereoselective analysis of metyrapol enantiomers in rat plasma. The AUC ratio of (-)- and (+)-metyrapol appeared in rat plasma after i.v. administration of metyrapone was about 3:1. ⋯ The inhibition of steroid 11 beta-hydroxylase by metyrapone, racemic metyrapol, (-)-metyrapol or (+)-metyrapol was analyzed in rat adrenal homogenates. Metyrapol was equally as potent as metyrapone in the inhibition of steroid 11 beta-hydroxylase and each enantiomer of metyrapol showed similar inhibitory activity on the rat adrenal steroid 11 beta-hydroxylase. These results indicate there is an insignificant difference in the inhibitory effects on steroid 11 beta-hydroxylase of metyrapol enantiomers, and that the inhibitory effects of metyrapol may be involved in the pharmacological activity of metyrapone in vivo.
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Orally administered barbaloin (100 mg/kg) did not induce any diarrhea in male Wistar rats, in spite of severe diarrhea with sennoside B (40 mg/kg). Also, in gnotobiote rats mono-associated with Peptostreptococcus intermedius, a human intestinal anaerobe capable of reducing sennidins to rhein anthrone, barbaloin did not induce diarrhea; the faecal water content (71.9%) 8 h after the administration of barbaloin was not increased, compared with that (73.9%) just before the treatment. ⋯ At this time, barbaloin was transformed to aloe-emodin anthrone in the feces from the gnotobiote rats mono-associated with the strain BAR, but not in feces from the conventional rats or the gnotobiote rats mono-associated with P. intermedius. These facts indicate that barbaloin is inactive as a laxative itself but is activated to aloe-emodin anthrone, a genuine purgative component, by Eubacterium sp. strain BAR.