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At least 595 records · Page 33Linked to original sources

Changes in biliary and fecal bile acids in mice after treatments with diosgenin and beta-sitosterol.

Diosgenin and beta-sitosterol (1% in diet) were administered to CRJ:CD-1 male mice for 15 days, in order to examine the changes in bile acid metabolism. There were some differences between diosgenin and beta-sitosterol in their effects on diet intake, liver weight, and plasma cholesterol level. However, both phytosterols caused no statistically significant changes in body weight gain, decreased cholesterol absorption to about one-third that observed in control mice, decreased liver cholesterol level, increased fecal excretion of cholesterol, and decreased fecal excretion of bile acids. Most of the increase in fecal excretion of cholesterol occurred 2 days after the start of feeding of phytosterols and gradually declined thereafter, but the levels on day 15 were nevertheless higher than those in the control mice. The fecal excretion of bile acids decreased progressively after the treatment with phytosterols. The decrease of bile acid derived from chenodeoxycholic acid was more predominant than the decrease of those derived from cholic acid, resulting in an increase of the cholic acid/chenodeoxycholic acid ratio. The biliary cholesterol, phospholipid, and bile acid mole % ratios and the lithogenic index were not changed, but the percentages of cholic acid and its related bile acids (the cholic acid group) to the total bile acids increased and those of the chenodeoxycholic acid group decreased after the treatments. The pool size of bile acids decreased in the mice given diosgenin but not in those given beta-sitosterol. Distribution of bile acids between the gallbladder and intestine was not altered by either phytosterol.(ABSTRACT TRUNCATED AT 250 WORDS)

Animals↗

How vitamin C, clofibrate and diosgenin control cholesterol metabolism in male guinea-pigs.

Following daily administration of cholesterol-enriched scorbutogenic diet to male guinea-pigs for 24 days, elevation of tissue cholesterol level occurred with concurrent pronounced depletion of tissue ascorbic acid. When these hypercholesterolemic guinea-pigs received clofibrate or diosgenin with or without daily supplementary vitamin C for 10 days, alterations in the bodyweight, plasma and hepatic ascorbic acid and clofibrate and diosgenin separately caused reduction in bodyweight and also in tissue ascorbic acid and cholesterol levels. In contrast, bodyweight and tissue ascorbic acid concentrations were increased by vitamin C alone or in combination with clofibrate or diosgenin. The cholesterol lowering actions of clofibrate and diosgenin were enhanced by daily supplementary vitamin C in hypercholesterolemic guinea-pigs. It is concluded that vitamin C plays an important role in the control of cholesterol metabolism in hypercholesterolemic guinea-pigs receiving clofibrate or diosgenin.

Animals↗

[Pharmacology of calenduloside B, a new triterpene glycoside from the roots of Calendula officinalis].

Calendulozide B--trioside of oleanolic acid, isolated from rhizomes of Calendula officinalis, Fam. Compositae, used perorally in doses of 5, 10, 20 and 50 mg/kg exerted an antiulcerous action in 3 experimental ulcer models of different genesis (caffein-arsenic, butadion and induced by ligation of pylorus) and also displayed a certain antiphlogistic and sedative action. It did not have any effect on the cardiovascular system, the tone of intestinal smooth muscles, diuretic renal function and electrolytes excretion with urine or on the biligenic function of the liver. The drug is devoid of locally irritation properties, manifests a relatively low hemolytic activity (15000 after Kofler) and an insignificant toxicity both with its one-time and chronic administration.

Animals↗

[Effect of triterpene glycosides on the stability of bilayer lipid membranes, containing different sterols].

Low concentrations of triterpene glycosides: holothurin A, stichoposide A and cauloside C sharply change the stability of bilayer lipid-sterine membranes. The glycosides activity decreases in the line: holothurin A, stichoposide A, cauloside C. The effective doses of glycosides are to a great extent determined by structural peculiarities of sterines which compose the films. A correlation was observed between the effect of triterpene glycosides on the stability of model bilayer membranes and their physiological activity. The model lipid-sterine membranes can be used in the primary screening of triterpene glycosides to estimate their physiological activity.

Drug Stability↗

[Pharmacological studies on a prescription containing Bupleuri Radix (IV). Effects of saikosaponin on the anti-inflammatory action of glucocorticoid].

Effects of saikosaponin d extracted from Bupleuri Radix on the antigranulomatous action of glucocorticoid were investigated in rats by the cotton pellet method. Saikosaponin d (0.1 mg/kg/day x 4 days) and dexamethasone (0.1 mg/kg/day x 4 days) reduced the weight of cotton-induced granuloma to 89.58% and 88.54% of the control, respectively. These antigranulomatous actions failed to show a significant difference from the control. However, the combined administration of saikosaponin d and dexamethasone produced a significant antigranulomatous action, namely, the decrease in the weight of granuloma to 62.5% of the control. While the combination of saikosaponin d and dexamethasone showed an inhibitory trend against the increase in serum triglyceride as induced by dexamethasone, the cholesterol level was elevated by the combination. The body weight was significantly reduced by the combined administration as compared with the group treated with dexamethasone alone, but no apparent difference existed in the adrenal and thymus weights between them.

Animals↗

[Comparative study of anti-tumor activity of the monoglucosides protopanaxadiol and betulafolientriol].

Antitumor and cytotoxic activity of monoglucosides such as 3-0-panaxadiol (1), 12-0-panaxadiol (2) and 20-0-panaxadiol (3) and 3-0-betulafolientriol (4), 12-0-betulafolientriol (5) and 20-0-betulafolientriol (6) was studied. It was found that in concentrations of 10 to 50 micrograms/ml the above monosides induced marked impairment of the selective permeability of the tumor cells and the inhibition of the labeled precursor inclusion into the macromolecule biosynthesis. Administration of the monosides in a single dose of 100 mg/kg 24 hours after the inoculation of the Ehrlich tumor cells resulted in prolongation of the mean life-span of the mice by 144 per cent (1), 153 per cent (2), 144 per cent (3), 125 per cent (4), 133 per cent (5) and 178 per cent (6). A significant reduction of the tumor mass was observed at the early stages of the tumor development and later the tumor progress intensively resumed. The tests for the effect of the monoside-activated macrophages on the growth of the tumor cells showed that production of the growth factors by the macrophages was stable and had a negative action on the efficacy of the chemotherapy with the monoglucosides.

Animals↗

Comparison between the effects of crude saikosaponin and 16, 16-dimethyl prostaglandin E2 on tannic acid-induced gastric mucosal damage in rats.

Hung, C.R., T.S. Wu and T.Y. Chang. The comparison between the effects of ethanol-extracted saikosaponin (SS) and 16, 16-dimethyl prostaglandin E2 (dmPGE2) on gastric acid back diffusion and mucosal damage induced by 100 mg/kg of acidified tannic acid (tannic acid dissolved in 100 mm HCl + 54 mM NaCl solution) was studied in the vagotomized rat. Crude saikosaponin (500 mg/kg) given by intragastric irrigation (I.G.) produced a significant inhibition (p < 0.05), while dmPGE2 (100 micrograms/kg) provoked a significant increase (p < 0.05) in acid back diffusion induced by acid solution. When graded doses of SS (100-1000 mg/kg) were added to acidified tannic acid solution and instilled to the stomach, a dose-dependent inhibition in acidified tannic acid-induced mucosal ulceration and acid back diffusion was achieved. The decrease in the H+ concentration and the increase in the Na+ concentration in the final samples induced by acidified tannic acid were also significantly (p < 0.05) inhibited by the same doses of SS. However, neither intraduodenal (I.D.) nor intravenous (i.v.) administration of SS was effective in inhibiting these ulcerogenic parameters. When dmPGE2 (3-100 micrograms/kg) was given concomitantly with acidified tannic acid solution, the acid back diffusion as well as mucosal ulceration provoked by acidified tannic acid were not significantly improved. The volume of luminal contents but not electrolyte concentrations in the final sample was considerably increased by adding dmPGE2 to the acidified tannic acid solution. The failure of I.D. or i.v. of dmPGE2 in inhibiting tannic acid-induced acid back diffusion and mucosal ulceration was also observed in other series of experiments.(ABSTRACT TRUNCATED AT 250 WORDS)

16,16-Dimethylprostaglandin E2↗

[Isolation and identification of two new saponins from Bupleurum smithii Wolff].

Two new saikosaponins of oleanane type were isolated from the roots of Bupleurum smithii Wolff, collected in Minhe County, Qinghai, namely saikosaponin k (VIb) and saikosaponin 1 (VIII). Their structures were elucidated on the basis of spectral analysis of UV, IR, 1HNMR, 13CNMR and FAB-MS. Saikosaponin k (VIb) was identified as 3 beta, 16 beta, 23,28-tetrahydroxyoleana-11,13(18)-dien-3-O-beta-D-xylopyranosyl-(1-->2)-beta- D-glucopyranosyl-(1-->3)-beta-D-fucopyranoside, and saikosaponin 1 (VIII) as 3 beta, 16 alpha, 23,28,30-pentahydroxyoleana-11,13(18)-dien-3-O-beta-D- glucopyranosyl-(1-->3)-beta-D-fucopyranoside, respectively.

Drugs, Chinese Herbal↗

[Action of triterpene glycosides of the dammarane series and their aglycones on lipid membranes].

The action of the dammarane triterpene glycosides Rb1 and Rg1 and their aglycones 20(S) protopanaxatriole and 20(S) protopanaxadiole from Korean ginseng on permeability of bilayer lipid membranes formed of monolayers was studied. RgI, protopanaxatriole and protopanaxadiole in concentrations of 3, 0.5 and 30 micrograms/ml respectively formed single ionic channels in the water phase on the membrane side containing cholesterol. The channel conductivity was 5 to 30 pSm in 1 M KCl. The ionic channels were more selective with respect to K+ as compared to Cl-. Rb1 was also able to increase the conductivity of the lipid membranes. However, no jumps in the current characteristics of the single channels were detected. All the substances in high concentrations on one side of the membrane independently of the cholesterol content induced fluctuation of the high amplitude current (from several tens of pSm to several hundreds of nSm).

Drugs, Chinese Herbal↗

[Action of triterpene glycosides of the dammarane series and their aglycones on the K+ and H+ ion currents in erythrocytes, induced by the ionophore A23187 and divalent ions].

The influence of the dammarane triterpene glycosides Rb1, Rb2, Rg1 and Rf and their aglycones 20(S) protopanaxatriol and 20(S) protopanaxadiol on fluctuation of the K+ and H+ flows in erythrocytes induced by ionophore A23187 and Ca2+ was studied. It was shown that glycoside Rb1 (10 to 50 micrograms/ml) and 20(S) protopanaxatriol (30 micrograms/ml) had a property of inducing fluctuation of the K+ and H+ flows in erythrocytes. In case of Rb1 the system entirely reversed to the initial state whereas in case of the protopanaxatriol use after the fluctuation the system did not reverse to the initial state. Glycosides Rb2 (10 to 30 micrograms/ml), Rg1 (5 to 20 micrograms/ml) and Rf (10 to 100 micrograms/ml) and 20(S) protopanaxadiol (30 micrograms/ml) in the concentrations used did not initiate the fluctuations. The above substances increased the extracellular concentration of K+ and pH without the system reversion to the initial state.

Animals↗