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At least 397 records · Page 22Linked to original sources
PubMed1986

Pharmacological effects of oral saikosaponin a may differ depending on conditions of the gastrointestinal tract.

Saikosaponin a and its 8 derivatives, structural isomers and their monoglycosides and aglycones, which were formed in the gastrointestinal tract with their fecal contents depending on food intake, showed different effects on protein synthesis by rat hepatocytes in primary culture. Saikosaponin a and its monoglycoside and aglycone were detectable in plasma of rats when saikosaponin a was orally administered. Pharmacological effects of saikosaponin a when orally administered may differ depending on conditions of the gastrointestinal tract.

Animals↗
PubMed1995

Ginsenosides of the protopanaxatriol group cause endothelium-dependent relaxation in the rat aorta.

The vasoactive effects of several ginsenosides, purified from Panax ginseng, were tested in the rat aorta. Ginsenosides from the protopanaxatriol group and its purified ginsenosides Rg1 and Re cause endothelium dependent relaxation which is associated with the formation of cyclic GMP. Both responses to these protopanaxatriol-containing ginsenosides are inhibited by methylene blue, an inhibitor of soluble guanylate cyclase and of nitric oxide synthase. In contrast, ginsenosides from the protopanaxadiol group and its purified ginsenosides Rb1 and Re do not affect vascular tone or production of cyclic GMP in the rat aorta. These findings demonstrate that ginsenosides from the protopanaxatriol group but not from the protopanaxadiol group enhance the release of nitric oxide from endothelial cells and may contribute to the beneficial effect of ginseng on the cardiovascular system.

Animals↗
PubMed1980

Configurational assignments to spirostan-3-ols by mass spectrometry.

A study of the degree of water elimination from ions derived from spirostan-3-ols by electron bombardment has shown that the loss is greatest from those ions produced by the 5 beta-spirostan-3 alpha-ols, less from the 5 beta-spirostan-3 beta-ols and the 5 alpha-spirostan-3 alpha-ols, which give losses of the same order of magnitude; and least from the 5 alpha-spirostan-3 beta-ols. The extent of water elimination can be used to help characterise spirostan-3-ols isolated from plant materials.

Chemical Phenomena↗
PubMed1995

Cell type-oriented differential modulatory actions of saikosaponin-d on growth responses and DNA fragmentation of lymphocytes triggered by receptor-mediated and receptor-bypassed pathways.

We examined the immunoregulatory action of saikosaponin-d (SSd), which was isolated from the root of Bupleurum talcatum L. and had a steroid-like structure, on murine thymocytes, and compared the action with that on spleen cells. Constitutive DNA synthesis or the growth response stimulated with anti-CD3mAb of thymocytes were down-regulated by 3 micrograms/ml SSd, whereas with spleen cells these were up-regulated by the same concentration of SSd. On the other hand, 3 micrograms/ml of SSd greatly up-regulated the growth response and interleukin 2 (IL-2)/interleukin 4 (IL-4) production induced through a receptor-bypassed pathway by calcium ionophore A23187 plus phorbol 12-myristate 13-acetate (PMA) in thymocytes, whereas it only slightly up-regulated them in spleen cells. Moreover, the same concentration of SSd inhibited DNA fragmentation in thymocytes induced by A23187 or PMA. These results suggest a unique cell type-dependent immuno-modulatory action of SSd.

Animals↗
PubMed1985

Effect of saikosaponin derivatives upon the immune response against T-dependent and T-independent antigens in mice.

Effect of water soluble extracts and purified derivatives from the root of the plant Bupletum falcatum L. upon the immune response of BALB/c mice was investigated using heterologous erythrocytes and bacterial lipopolysaccharide. This Chinese Medicine is famous for its reputed anti-inflammatory, anti-tumor and other biological activities, and has been widely used alone or in a complexed form since ancient times in Oriental Countries. The effect on immune responsiveness of this drug was judged by the measurement of antibody secreting cells causing localized hemolysis in agar gel. The purified derivatives, Saikosaponin (SS) a and d, suppressed anti-SRBC plaque-forming cells (PFC), but the other derivatives, b1 and b2 and c, did not. Moreover, derivatives a and d also enhanced anti-LPS PFC. From experiments establishing minimum effective doses for anti-SRBC PFC in mice, one mg/kg was optimum for BALB/c mice. The effect of the drug on antibody formation against heterologous erythrocytes was nonspecific because treated mice had greatly depressed PFC responses against both sheep and rabbit erythrocytes. The phenotypic effect of this drug as judged by PFC against T-dependent or T-independent antigen was not identified. However, it was suggested that the purified derivatives SSa and d stimulated both T- and B-cells. The possible mechanism of effect against immunocompotent cells is discussed.

Animals↗
PubMed1988

An investigation of the immune suppression induced by some saikosaponin derivatives.

The relationship between lymphocyte activation by purified plant glycoside and the suppression of antibodies against sheep erythrocytes was investigated by an adoptive cell transfer system. Glycosides are one of the main components of Shôsaikotô--famous hematopoietic remedies of oriental medicine. In earlier reports, BALB/c mice treated with these drugs, suppressed the plaque-forming cell (PFC) response to T-dependent antigens. In contrast, the PFC response was enhanced for T-independent antigens. In this communication, an experiment was designed to determine the nature of the suppressive factor(s) produced in treated mice. Mice were orally or intraperitoneally administered 1 mg/kg of five types of purified SS derivatives every other day on five consecutive occasions. Spleen cells and serum were prepared from SS-treated mice and were then passively transferred to recipient mice. On the spleen cells (and not any of the sera) from drug-treated hosts effectively suppressed the PFC in recipients. The spleen cells of treated mice were further divided into adherent and non-adherent cells; each cell type was transferred into recipient animals. The observed suppressive activity was clearly detected in the non-adherent cell population. A subsequent analysis of the lymphocyte subpopulation revealed that Lyt.1.1 negative and Lyt.2.2 positive cells were responsible for this suppression. It was concluded that some SS derivatives elevate the activities of the major immunocyte population, with suppressor cell activity predominating.

Animals↗
PubMed1989

Activation of murine peritoneal macrophages by saikosaponin a, saikosaponin d and saikogenin d.

Macrophage activation by saikosaponins and saikogenins was investigated and compared with that by other saponins and macrophage stimulants. Saikosaponins a and d induced a marked cell accumulation in the peritoneal cavity when administered intraperitoneally. Among saikosaponins and saikogenins tested, saikosaponin d significantly activated peritoneal macrophages in terms of enhancement of phagocytic activity, increased level of cellular lysosomal enzyme (acid phosphatase), induction of cytostatic activity and expression of Ia antigen on the cell surface. The activities of saikosaponin d were much stronger than those of typical saponins ginsenoside Rg1 and glycyrrhizin and almost comparable with or somewhat weaker than those of lipopolysaccharide, a streptococcal preparation OK-432 and formalin-killed Propionibacterium acnes, indicating that saikosaponin d is a potent macrophage activator.

Animals↗
PubMed1990

Protective effect of saikosaponin A, saikosaponin D and saikogenin D against Pseudomonas aeruginosa infection in mice.

Effects of saikosaponins and their genins on nonspecific resistance against Pseudomonas aeruginosa and Listeria monocytogenes infections were investigated. When mice were administered intraperitoneally (i.p.) saikosaponins one day before i.p. infection with P. aeruginosa, saikosaponins a and d induced a marked enhancement of nonspecific resistance at a dose of 10 micrograms/mouse. Also, saikogenin D, a secondary metabolite of saikosaponin d, showed an enhancing effect. The most effective condition for enhancing the nonspecific resistance was i.p. administration of saikosaponin d one day before i.p. or intravenous (i.v.) infection with P. aeruginosa, when mice were treated i.p., i.v., or subcutaneously with saikosaponin d 1, 4 or 7 days previously. Effect of saikosaponin d was weaker than that of formalin-killed bacilli of Propionibacterium acnes and lipopolysaccharide. On the other hand, effect of saikosaponin d on enhancement of nonspecific resistance against L. monocytogenes was not seen. Effector cells participating in the enhanced protection induced by saikosaponin d may be macrophages, since macrophages were a major component in peritoneal cells obtained from mice administered i.p. saikosaponin d 1 day earlier and intracellular bactericidal activity of peritoneal macrophages against P. aeruginosa increased.

Animals↗
PubMed1991

Effects of saikosaponin-d on the functions and morphology of macrophages.

The effects of saikosaponin-d, isolated from Bupleurum Radix, on phagocytosis and spreading of mouse peritoneal macrophages were investigated. Macrophages from saikosaponin-d-treated mice showed a significant increase in spreading activity followed by an increase in phagocytic activity. An intense distribution of microfilaments and microtubules was also observed in these macrophages by immunofluorescence microscopy.

Animals↗
PubMed1991

Effect of saikosaponin on the immune responses in mice.

The in vivo effects of saikosaponin, isolated from Bupleurum radix, on the immune responses are still poorly understood. We have already shown that saikosaponin-d increases phagocytic activities of murine peritoneal macrophages such as spreading activity, phagocytosis, lysosomal enzyme activity and intracellular killing activity of living yeast. This work extends these observations by showing that treatment with saikosaponin also increased the antibody response in plaque-forming cell numbers after in vivo immunization with sheep red blood cells (SRBC) and an augmentation of spleen cell proliferation responses to stimulation with T- or B-cell mitogens both before and after immunization. Furthermore, after SRBC immunization, the macrophages from mice treated with saikosaponin-d revealed significant increases in spreading activity and lysosomal enzyme activity. The chemiluminescences of the macrophages from mice treated with saikosaponin-d stimulated by opsonized zymosan and PMA were enhanced and interleukin-1 production by the cells was increased in a dose-dependent manner. These results demonstrate that saikosaponin-d may stimulate in vivo immunological lymphocyte functions, partly by activating some macrophage functions.

Animals↗
PubMed1986

Inhibitory effects of ursolic and oleanolic acid on skin tumor promotion by 12-O-tetradecanoylphorbol-13-acetate.

Ursolic acid (UA) and oleanolic acid (OA), which had been isolated from Glechoma hederacea as inhibitors of Epstein-Barr virus (EBV) activation induced by 12-O-tetradecanoylphorbol-13-acetate (TPA), were tested against inhibitory effect on tumor promotion by TPA in vivo. They inhibited effectively the tumor promotion in mouse skin and the activities were comparable to that of a known inhibitor of tumor promotion, retinoic acid (RA). Interestingly, UA was more effective on a single application before initial TPA-treatment than on a continuous application before each TPA-treatment, while OA and RA were ineffective in the same treatment. These data suggest that the role of UA for inhibitory action on tumor promotion differs slightly from those of RA and OA.

Animals↗
PubMed1986

Search for possible antitumor promoters by inhibition of 12-O-tetradecanoylphorbol-13-acetate-induced Epstein-Barr virus activation; ursolic acid and oleanolic acid from an anti-inflammatory Chinese medicinal plant, Glechoma hederaceae L.

From an anti-inflammatory Chinese medicinal plant, Glechoma hederaceae L., two triterpene carboxylic acids, ursolic acid (UA) and oleanolic acid (OA) have been isolated as inhibitors of 12-O-tetradecanoylphorbol-13-acetate (TPA) induced Epstein-Barr virus (EBV) activation in Raji cells. Both acids significantly inhibited the activation at a 1000-fold molar ratio to TPA, and also teleocidin B-4. The dose responses of the acids were very similar to those of the antitumor promoters, retinoic acid (RA) and glycyrrhetinic acid (GA). However, a characteristic property that UA and OA possess, far higher cell viability to the Raji cells than RA to the Raji cells, has been pointed out. Furthermore, enhancement of the inhibitory activity was found in 3-keto derivatives of UA and OA, while either loss of oxygen functionality at C-3 position of UA or oxidation at C-3 of GA led to reduction of the activity. Binding assay suggested that the inhibitory activity should be exhibited by some event caused after binding of TPA to the receptor in the cells.

Biological Assay↗
PubMed1988

Inhibitory effects of 12-O-tetradecanoylphorbol-13-acetate and teleocidin B induced Epstein-Barr virus by saponin and its related compounds.

The inhibitory effects of triterpene glycosides and monoterpene glycosides on 12-O-tetradecanoylphorbol-13-acetate (TPA) and teleocidin B in the Epstein-Barr virus (EBV) activation in Raji cells were studied. Concomitant treatment of Raji cells with TPA or Teleocidin B and these glycosides showed the inhibition of EBV activation. We herein report in vitro structure-activity studies using a biological test system on a variety of triterpene glycosides having 1 sugar chain (monodesmoside), 2 sugar chain (bisdesmoside) and an acyl side-chain. Among these glycosides, triterpene 3-O-glycosides and acylated saponin exhibited an effective inhibition of EBV activation; therefore, the sugar chain at C-3 of the triterpene and/or the acyl side-chain were determined to be essential to the inhibitory activities in this test system. The data suggested that these triterpenoid glycosides which were originally used as herbal drugs and folk remedies in many areas of the world, were in fact inhibitory compounds, thus explaining the EBV activation in the in vitro test system.

Antineoplastic Agents↗
PubMed1995

Central administration of saikosaponin-d increases corticotropin-releasing factor mRNA levels in the rat hypothalamus.

Saiko agents, Chinese herbal drugs, stimulate corticotropin-releasing factor (CRF) release from the hypothalamus, adrenocorticotropin (ACTH) secretion and proopiomelanocortin (the precursor for ACTH) gene expression in the anterior pituitary. In the present study, the effect of intracerebroventricular injection of saikosaponin (SS)-a and -d, two of the main components of saiko agents, on hypothalamic CRF gene expression was examined in pentobarbital-anesthetized rats. Administration of SS-d, 0.2-2.0 micrograms/kg body wt, increased plasma ACTH levels, proopiomelanocortin mRNA levels in the anterior pituitary and the CRF mRNA level in the hypothalamus in a dose-dependent manner, whereas SS-a failed to have an affect on these levels. These findings indicate that SS-d stimulates both CRF gene expression and CRF release, which in turn increases ACTH release and proopiomelanocortin gene expression in the anterior pituitary. Therefore, SS-d is believed to have an important role both in saiko agent-induced CRF release and CRF gene expression in the hypothalamus.

Adrenocorticotropic Hormone↗
PubMed1987

Isolation and partial purification of Lantana (Lantana camara L.) toxins.

A partially purified toxin fraction and lantadene A were obtained from Lantana camara L. leaves by batch extraction, column chromatography and fractional crystallization. Toxicity was tested in guinea pigs. The total number of chemical entities in the partially purified toxin preparation was 7, the 2 major ones being lantadene A and lantadene B. Lantadene A was nontoxic in itself. Likewise, another fraction containing lantadene A, lantadene B and 3 more components with higher polarity was found to be nontoxic. The toxic component(s) are different from lantadene A/B but appear to resemble them very closely.

Administration, Oral↗
PubMed1984

Antihepatotoxic actions of papyriogenins and papyriosides, triterpenoids of Tetrapanax papyriferum leaves.

Antihepatotoxic actions of the papyriogenins and papyriosides from Tetrapanax papyriferum leaves were examined utilizing carbon tetrachloride (CCl4)- and galactosamine (GalN)-induced cytotoxicity in primary cultured rat hepatocytes. Remarkable antihepatotoxic effects were observed with papyriogenin B, papyriogenin A, propapyriogenin A2, papyriogenin C, 11-dehydropropapyriogenin A2, 16-epi-saikogenin C and propapyriogenin A1 in the CCl4-induced cytotoxicity assay, and papyriogenin A, propapyriogenin A1 and propapyriogenin A2 were active in preventing GalN-induced cytotoxicity although these triterpenoids were rather cytotoxic at a higher dose in the latter assay. Structure-activity relationship is discussed.

Alanine Transaminase↗
PubMed1988

Effect of prolonged administration of sublethal concentrations of aridanin isolated from Tetrapleura tetraptera and bayluscide on the glycogen and protein content of Biomphalaria glabrata.

The effect of chronic application of sublethal concentrations of aridanin isolated from Tetrapleura tetraptera (0.25-0.125 ppm) and of bayluscide (0.05-0.025 ppm) on the glycogen and protein content of Biomphalaria glabrata was determined. Aridanin and bayluscide produced significant reductions in the glycogen content of B. glabrata, but a significant decrease in the protein content of the snails was not apparent until after 4 weeks of continuous exposure. The results indicate that the molluscicides may exert their primary molluscicidal action on the carbohydrate metabolism of the snail.

Animals↗