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Collected Abstracts: Chai Hu/Radix Bupleurum

Immunology 1999 Jul;97(3):540-547

B-cell proliferation activity of pectic polysaccharide from a medicinal herb, the roots of Bupleurum falcatum L. and its structural requirement.

Sakurai MH, Matsumoto T, Kiyohara H, Yamada H

Oriental Medicine Research Center, The Kitasato Institute, Tokyo, Japan.

[Record supplied by publisher]

Pectic polysaccharide fraction (BR-2) containing pharmacologically active pectic polysaccharide, bupleuran 2IIc, which was prepared from a medicinal herb, the roots of Bupleurum falcatum L., was administered orally to C3H/HeJ mice for 7 consecutive days. Proliferative responses of spleen cells were enhanced in the presence of the purified pectic polysaccharide, bupleuran 2IIc, but another B-cell mitogen, lipopolysaccharide (LPS) did not give a similar effect. In vitro studies using spleen cells showed that bupleuran 2IIc also stimulated lymphocytes, depleted of adherent cells or T cells. Bupleuran 2IIc treatment increased subpopulation of CD25+ and surface immunoglobulin M-positive (sIgM+) lymphocytes. Non-specific immunoglobulin secretion of spleen cells treated with bupleuran 2IIc was increased according to the culture time, and coexistence of interleukin-6 (IL-6) enhanced the secretion more than that of bupleuran 2IIc alone. These results suggest that bupleuran 2IIc proliferates B cells in the absence of macrophages, and the resulting activated B cells are then induced into antibody-forming cells in the presence of IL-6. Among the structural region of bupleuran 2IIc, ramified region (PG-1), which consists of rhamnogalacturonan core rich in neutral sugar chain, showed the potent mitogenic activity suggesting it to be an active site. Mitogenic activity of bupleuran 2IIc was reduced in the presence of antipolysaccharide antibody (antibupleuran 2IIc/PG-1-IgG), which recognizes the ramified region of bupleuran 2IIc as the antigenic epitope. Mitogenic activity of bupleuran 2IIc was also reduced by the addition of beta-d-GlcpA-(1-->6)-beta-d-Galp-(1-->6)-d-Galp or beta-d-GlcpA-(1-->6)-d-Galp, which are a part of the epitopes of antibupleuran 2IIc/PG-1-IgG. These results suggest that the epitopes in bupleuran 2IIc act as active sites of the polysaccharide during mitogenic activity.

Carbohydr Res 1998 Oct;311(4):219-29

Characterization of antigenic epitopes in anti-ulcer pectic polysaccharides from Bupleurum falcatum L. using several carbohydrases.

Sakurai MH, Kiyohara H, Matsumoto T, Tsumuraya Y, Hashimoto Y, Yamada H

Oriental Medicine Research Center, Kitasato Institute, Tokyo, Japan.

A polyclonal antibody (anti-bupleuran 2IIc/PG-1-IgG) against the "ramified" region (PG-1) of an anti-ulcer pectic polysaccharide was prepared and its antigenic epitopes were analyzed by using several carbohydrases. Enzymatic removal of arabinosyl residues from PG-1 by endo-(1-->5)-alpha-L-arabinanase (from Aspergillus niger) did not reduce the binding ability of anti-bupleuran 2IIc/PG-1-IgG to PG-1. When the endo-(1-->5)-alpha-L-arabinanase-resistant fraction (EA-1) was digested with rhamnogalacturonase A (rRGase A from A. aculeatus), a high-molecular-mass fragment fraction (RA-1) and an oligosaccharide fraction (RA-3) were obtained. RA-3 contained at least four kinds of oligosaccharides liberated from the rhamnogalacturonan core. This partial removal of the rhamnogalacturonan core in EA-1 also did not reduce the binding of the antibody to the polysaccharide. Further digestion of RA-1 with exo-(1-->3)-beta-D-galactanase (from Irpex lacteus), gave a high-molecular-mass fragment (EXG-1) and a trace of oligosaccharides (EXG-3). Methylation and FABMS analyses indicated that EXG-3 contained mono- and di-galactosyl oligosaccharides possessing terminal GlcA or GlcA4Me. Removal of the EXG-3 fraction from RA-1 by exo-(1-->3)-beta-D-galactanase significantly reduced the ability of the binding of the antibody to the polysaccharide. When PG-1 was digested with endo-(1-->6)-beta-D-galactanase (from Trichoderma viride) or beta-D-glucuronidase (from A. niger), the reactivities of both enzyme-resistant fractions to the antibody were decreased in comparison with that of PG-1. Both radish arabinogalactan (containing GlcA4Me) and beta-D-GlcpA-(1-->6)-beta-D-Galp-(1-->6)-D-Galp were shown to inhibit the reactivity of PG-1 to the antibody by competitive ELISA. These results suggest that 6-linked galactosyl chains containing terminal GlcA or GlcA4Me attached to (1-->3)-beta-D-galactosyl chains, are important sugar residues in the antigenic epitopes of the "ramified" region of bupleuran 2IIc.

Life Sci 1998;63(13):1147-56

In vivo and in vitro antiinflammatory activity of saikosaponins.

Bermejo Benito P, Abad Martinez MJ, Silvan Sen AM, Sanz Gomez A, Fernandez Matellano L, Sanchez Contreras S, Diaz Lanza AM

Department of Pharmacology, Faculty of Pharmacy, University Complutense, Madrid, Spain.

Buddlejasaponin I and saikosaponin 1 and 2, biologically active compounds from Scrophularia scorodonia and Bupleurum rigidum respectively, exert potent in vivo antiinflammatory effects on mouse ear edema induced by phorbol myristate acetate (PMA). The effects of these compounds on swelling and other inflammatory parameters are described. In screening for in vitro effects of saikosaponins on cellular systems generating cyclooxygenase (COX) and lipoxygenase (LOX) metabolites, we observed that most saikosaponins showed a significant effect. The action is more marked on LOX metabolite LTC4. Our data support the inhibition of arachidonic acid metabolism as one of the biochemical mechanisms that might be the rationale for the putative antiphlogistic activity of these saikosaponins.

Planta Med 1998 Jun;64(5):404-7

Anti-inflammatory activity of unusual lupane saponins from Bupleurum fruticescens.

Just MJ, Recio MC, Giner RM, Cuellar MJ, Manez S, Bilia AR, Rios JL

Department de Farmacologia, Universitat de Valencia, Burjassot, Spain.

Extracts from Bupleurum fruticescens were examined for oral and topical anti-inflammatory activities. The BuOH extract proved to be active against carrageenan and tetradecanoylphorbol acetate acute edemas and allowed the isolation of three saponins identified by spectroscopic techniques as 3 beta-O-(O-alpha-L-rhamnopyranosyl-(1-->4)-O-[beta-D-glucopyranosyl- (1-->6)]-O-beta-D-glucopyranosyl)lup-20(29)-ene-23,28-dioic acid (fruticesaponin A), 3 beta-O-(O-alpha-L-rhamnopyranosyl-(1-->4)-O-beta-D-glucopyranosyl) lup-20(29)-ene-23,28-dioic acid 28-O-beta-D-glucopyranosyl ester (fruticesaponin B), and 3 beta-O-(O-alpha-L-rhamnopyranosyl-(1-->4)-O-[beta-D-glucopyranosyl- (1-->6)]-O-beta-D-glucopyranosyl)-lup-20(29)-ene-23,28-dioic acid 28-O-beta-D-glucopyranosyl ester (fruticesaponin C). These compounds were studied against carrageenan, tetradecanoylphorbol acetate, arachidonic acid and ethyl phenylpropiolate acute edemas. Fruticesaponin B, a bidesmosidic saponin with an unbranched saccharide moiety was the most active in all the tests applied.

Planta Med 1998 Apr;64(3):220-4

Inhibitory effect of bupleuri radix saponins on adhesion of some solid tumor cells and relation to hemolytic action: screening of 232 herbal drugs for anti-cell adhesion.

Ahn BZ, Yoon YD, Lee YH, Kim BH, Sok DE

College of Pharmacy, Chungnam National University, Taejon, Korea.

Anti-cell adhesive activity and hemolytic action of herbal drugs were investigated. Among 232 herbal drugs tested, six showed a remarkable anti-cell adhesive activity, and the extract from the roots of Bupleurum falcatum (Umbelliferae), the semen of Psorala corylifolia (Leguminosae), and the semen of Areca catechu (Palmae) showed an anti-cell adhesive action at non-cytotoxic concentrations. Saikosaponins-a, d and e, isolated from the roots of Bupleurum falcatum, exhibited a potent anti-cell adhesive activity and a strong hemolytic action. In a structure-activity relationship for both activities, it seems that a sugar moiety and an ether linkage between C-13 and C-28 are required for good bioactivities. In addition, saikosaponin d with a beta-hydroxy group at C-16 was more potent than saikosaponin a possessing an alpha-hydroxy group. Taken together, it is suggested that the mechanism for anti-cell adhesive activity of saikosaponin may resemble that for their hemolytic action.

Biol Pharm Bull 1997 Jul;20(7):759-64

Wide range of molecular weight distribution of mitogenic substance(s) in the hot water extract of a Chinese herbal medicine, Bupleurum chinense.

Izumi S, Ohno N, Kawakita T, Nomoto K, Yadomae T

Laboratory of Immunopharmacology of Microbial Products, School of Pharmacy, Tokyo University of Pharmacy and Life Science, Japan.

In this study, we examined the contribution of lignin-like materials in lower molecular weight (MW) fractions from the hot water extract of Bupleuri Radix (Bupleurum chinense) (HWE-BR) for their immunopharmacological activities. Mitogenic activity was detected in all the fractions of MW ranges: lower than 1.0 kDa, 1.0-3.5 kDa, 3.5-10 kDa, and 10-50 kDa. After NaClO2 treatment of these subfractions, UV spectra, ESR spectra, mitogenic activities on murine B-cells, and the activity of inducing nitric oxide in RAW 264.7 cells were significantly reduced, suggesting that lignin-like polyphenolic substance(s) of various MW might take part in these activities. The intensity of ESR spectra and mitogenic activities were stronger in higher MW subfractions, thus the content of stable radical species and/or the degrees of polymerization would be important for their immunopharmacological activities.

Biol Pharm Bull 1997 Jan;20(1):97-100

Analysis of mitogenic substances in Bupleurum chinense by ESR spectroscopy.

Ohtsu S, Izumi S, Iwanaga S, Ohno N, Yadomae T

Laboratory of Immunopharmacology of Microbial Products, School of Pharmacy, Tokyo University of Pharmacy and Life Sciences, Hachioji, Japan.

The polyphenolic substance(s) in the hot water extract of Bupleurum chinense (PSF) showed strong mitogenic activity. In this paper, we analyzed PSF by using ESR spectroscopy, and found that i) PSF showed a strong ESR signal on g = 2.005 which was similar to the commercially available lignin; ii) Sho-saiko-to, which contains an extract of B. chinense, also showed similar signals on ESR; iii) Powdered B. chinense also showed similar signals on g = 2.005. Peroxidase activity, essential for producing polyphenolic substances, was detected in the cold water extract of B. chinense. In addition, the signal intensity of the ESR spectrum of B. chinense was increased after boiling. The data of the ESR spectra of the model reactions using lignin, arginine, proline and maltose also strongly suggested that a certain chemical modification proceeded during the hot water extraction to increase the percentage of the stable free radical. These facts strongly suggested that the mitogenic substance in B. chinense is a polyphenolic substance extracted by hot water, and the structure was modified during the extraction to increase the stable free radical components.

Planta Med 1996 Aug;62(4):341-6

Detection and tissue distribution of anti-ulcer pectic polysaccharides from Bupleurum falcatum by polyclonal antibody.

Sakurai MH, Matsumoto T, Kiyohara H, Yamada H

Oriental Medicine Research Center, Kitasato Institute, Tokyo, Japan.

Anti-sera against the "ramified" region (PG-1) of an anti-ulcer polysaccharide (bupleuran 2IIc), which was purified from the roots of Bupleurum falcatum L, were obtained by immunization of rabbits, and a polyclonal anti-bupleuran 2IIc/PG-1-antibody of the IgG class was purified by Protein G and "ramified" region (PG-1) immobilized affinity chromatographies. The antigenic specificity of anti-bupleuran 2IIc/PG-1-IgG was examined by a two-site sandwich ELISA which was developed as an improved method for microanalysis of bupleuran 2IIc using a biotinylated antibody. Another pectin from B. falcatum and anti-complementary pectins from Angelica acutilaba and Glycyrrhiza uralensis also showed significant reactivity to anti-bupleuran 2IIc/PG-1-IgG, although these reactivities were lower than that of bupleuran 2IIc. Other polysaccharides tested such as apple pectin, araban, yeast mannan, pullulan, etc., had negligible reactivity. The KDO-containing region and oligogalacturonides, which were obtained by endo-alpha-(1-->4)-polygalacturonase digestion of bupleuran 2IIc, were also not significantly recognized by anti-bupleuran 2IIc/PG-1-IgG. When bupleuran 2IIc was administered to the mice i.v., the polysaccharide disappeared from the circulation within 24 h and was mainly detected in the liver by the two-site sandwich ELISA. However the clearance of bupleuran 2IIc from the circulation was delayed by pretreatment with iota-carrageenan. When the crude polysaccharide fraction (BR-2), containing mainly bupleurans 2IIb and 2IIc from B.falcatum, was administrated orally to the mice, the polysaccharides were detected in the liver and Peyer's patch.

Ceska Slov Farm 1995 Oct;44(5):246-51

[Phytotherapeutic aspects of diseases of the cardiovascular system. 5. Saponins and possibilities of their use in prevention and therapy].

[Article in Czech]

Purmova J, Opletal L

Katedra farmaceuticke botaniky a ekologie farmaceuticke fakulty Univerzity Karlovy, Hradec Kralove.

The summarizing paper deals with the structure and biological effects of saponins generally and in relation with the treatment and prevention of diseases of the heart and circulatory system. In this field, mainly the saponins from the plants of the genera Panax, Gynostemma or Bupleurum are of use. Also soya saponins and saponins of the genera Astragalus, Salvia, Boussigaultia and Litchi can be employed. Saponins exert a positive effect on the function of the heart direct, or they help treat related diseases. For instance, they inhibit the formation of lipid peroxides in the cardiac muscle or in the liver, they influence the function of enzymes contained in them, they decrease blood coagulation, cholesterol and sugar levels in blood, they stimulate the immunity system. They act either direct, blocking the transfer of Ca2+ ions or modulating the function of Na(+)-K(+)-ATPase, or they help resorb other active principles. It can be concluded that saponins are a prospective group of drugs of natural origin for the prevention and treatment of diseases of the heart and circulatory system.

Publication Types:

  • Review
  • Review, tutorial
J Tradit Chin Med 1995 Jun;15(2):96-8

Treatment of primary thrombocytopenic purpura by modified minor decoction of bupleurum.

Duan Y, Zhao X, Xu X, Yang J, Li Z

Department of Traditional Chinese Medicine, People's Hospital of Langfang City, Hebei Province.

Publication Types:

  • Clinical trial
Immunopharmacology 1995 Apr;29(3):207-13

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.

Kato M, Pu MY, Isobe K, Hattori T, Yanagita N, Nakashima I

Department of Immunology, Nagoya University School of Medicine, Japan.

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.

J Pharm Pharmacol 1995 Feb;47(2):152-6

Regulation of immune complexes binding of macrophages by pectic polysaccharide from Bupleurum falcatum L.: pharmacological evidence for the requirement of intracellular calcium/calmodulin on Fc receptor up-regulation by bupleuran 2IIb.

Matsumoto T, Yamada H

Oriental Medicine Research Center, Kitasato Institute, Tokyo, Japan.

The pectic polysaccharide, bupleuran 2IIb, up-regulates Fc-receptor (FcR) expression on peritoneal macrophages in a dose-dependent manner. The intracellular signal transduction by bupleuran 2IIb leading to the expression of FcR was studied. Neither the protein kinase C (PKC) inhibitor, 1-(5-isoquinolinylsulphonyl)-2-methylpiperazine dihydrochloride, nor the structurally distinct PKC antagonist, calphostin C, inhibited bupleuran 2IIb-induced up-regulation of FcR, whereas two direct activators of PKC, L-alpha-1-oleoyl-2-acetyl-sn-3-glycerol and N-(6-phenylhexyl)-5-chloro-1-naphthalenesulphonamide were unable to up-regulate the expression of FcR. The protein kinase A (PKA) inhibitor, N-[2-(methylamino)ethyl]-5-isoquinolinesulphonamide dihydrochloride also did not inhibit bupleuran 2IIb-induced up-regulation of FcR. Fluorescence image analysis using the calcium-sensitive dye, Fura-2, demonstrated that bupleuran 2IIb induced a rapid increase in intracellular levels of calcium (Ca2+). When macrophages were treated with calcium antagonist, 8-(diethylamino)-octyl-3,4,5-trimethoxybenzoate hydrochloride, bupleuran 2IIb-induced up-regulation of FcR was inhibited in a dose-dependent manner. The bupleuran 2IIb-induced up-regulation of FcR was also blocked by two structurally distinct calmodulin antagonists, trifluoperazine and N-(6-aminohexyl)-5-chloro-1-naphthalenesulphonamide hydrochloride. Furthermore, elevation of intracellular Ca2+ using the calcium ionophore, A23187, led to up-regulation of the FcR expression in a dose-dependent manner. These results suggest that bupleuran 2IIb induces the up-regulation of FcR on macrophages by a mechanism dependent on an increase in intracellular Ca2+ followed by activation of the calmodulin, but not by a PKC or PKA pathway.

Cell Immunol 1994 Nov;159(1):15-25

Characterization of the immunoregulatory action of saikosaponin-d.

Kato M, Pu MY, Isobe K, Iwamoto T, Nagase F, Lwin T, Zhang YH, Hattori T, Yanagita N, Nakashima I

Department of Immunology, Nagoya University School of Medicine, Japan.

The immunoregulatory action of saikosaponin-d (SSd), which was isolated from the root of Bupleurum falcatum L. and has a steroid-like structure, was examined on splenic T lymphocytes of C57BL/6 mice. SSd displayed a definite action in vitro to bidirectionally control the growth response of T lymphocytes stimulated by concanavalin A, anti-CD3 monoclonal antibody, and calcium ionophore A23187 plus phorbol 12-myristate 13-acetate. Low concentrations (1-3 micrograms/ml) of SSd upregulated the responses to suboptimum stimuli of agonists, particularly during the relatively late stage of the responses, whereas it downregulated the responses to supraoptimal stimuli. Under appropriate experimental conditions, SSd promoted interleukin-2 (IL-2) production and IL-2 receptor expression. It also accelerated c-fos gene transcription, but it did not modulate the level of tyrosine phosphorylation of cellular proteins. We concluded from these results that SSd uniquely modulates T lymphocyte function and that at least one target of the action of SSd is located at or before the step of c-fos gene transcription and after T-cell receptor/CD3-mediated protein tyrosine kinase activation.

Int J Immunopharmacol 1993 Aug;15(6):683-93

The pectic polysaccharide from Bupleurum falcatum L. enhances immune-complexes binding to peritoneal macrophages through Fc receptor expression.

Matsumoto T, Cyong JC, Kiyohara H, Matsui H, Abe A, Hirano M, Danbara H, Yamada H

Oriental Medicine Research Center, Kitasato Institute, Tokyo, Japan.

Binding of glucose oxidase-anti-glucose oxidase complexes (GAG), a model of immune complexes, to macrophages was enhanced by treatment with an acidic pectic polysaccharide, bupleuran 2IIb, from Bupleurum falcatum L. GAG binding to macrophages by bupleuran 2IIb increased in a dose-dependent fashion, and was abolished when the Pronase-treated macrophages were incubated with bupleuran 2IIb. The GAG binding enhancing activity of bupleuran 2IIb was reduced by periodate oxidation but not Pronase digestion of bupleuran 2IIb. When bupleuran 2IIb was digested with endo-polygalacturonase, the resulting enzyme resistant carbohydrate portion showed potent activity. Scatchard analysis indicated enhanced expression of the Fc receptor (FcR) on the surface by the action of bupleuran 2IIb. The enhancement of GAG binding by bupleuran 2IIb was inhibited by the presence of actinomycin D or cycloheximide. Bupleuran-2IIb-stimulated cells showed enhanced expression of both FcRI and FcRII mRNA, which were measured as PCR products. These results suggested that the endo-polygalacturonase resistant carbohydrate portion of bupleuran 2IIb is important for the expression of the activity, and that the activity of bupleuran 2IIb on GAG binding was mediated by receptors for polysaccharide on the cells. The up-regulation of the Fc receptor by bupleuran 2IIb was also suggested to mediate by de novo synthesis of the receptor protein.

J Pharm Pharmacol 1993 Jun;45(6):535-9

Role of polymorphonuclear leucocytes and oxygen-derived free radicals in the formation of gastric lesions induced by HCl/ethanol, and a possible mechanism of protection by anti-ulcer polysaccharide.

Matsumoto T, Moriguchi R, Yamada H

Oriental Medicine Research Center, Kitasato Institute, Tokyo, Japan.

This study examined the role of oxygen-derived free radicals in the pathogenesis of gastric mucosal lesions induced by HCl/ethanol. Superoxide dismutase, and catalase, and their combination reduced gastric lesion formation in mice. Gastric lesions were also reduced in mice treated with cyclophosphamide or anti-neutrophils, but not in mice treated with allopurinol or desulphated-carrageenan. Cobra venom factor did not reduce lesion formation. These results suggested that oxygen-free radicals may contribute to the formation of gastric mucosal lesions induced by HCl/ethanol, and that oxygen radicals were generated from neutrophils but not from xanthine oxidase. Anti-ulcer pectic polysaccharide, bupleuran 2IIc, which was recently isolated from the roots of Bupleurum falcatum L., showed potent inhibition of HCl/ethanol-induced gastric lesions in mice. Bupleuran 2IIc seemed to scavenge hydroxyl radical effectively. It was suggested that this anti-ulcer polysaccharide may provide protection to the gastric mucosa by scavenging oxygen-free radicals.

Planta Med 1991 Dec;57(6):555-9

Purification of anti-ulcer polysaccharides from the roots of Bupleurum falcatum.

Yamada H, Sun XB, Matsumoto T, Ra KS, Hirano M, Kiyohara H

Oriental Medicine Research Center, Kitasato Institute, Tokyo, Japan.

A water-soluble crude polysaccharide fraction (BR-1) prepared from the root of Bupleurum falcatum L. (Japanese name = Saiko) prevented HCl/ethanol induced ulcerogenesis in mice significantly. BR-1 was fractionated into four polysaccharide fractions (BR-2, BR-3, BR-4, and BR-5) by the addition of cetyltrimethylammonium bromide, and the strongly acidic polysaccharide fraction BR-2 showed the most potent inhibition of gastric lesion formation. When BR-2 was further fractionated by anion-exchange chromatography, the most potent anti-ulcer activity was observed in the pectin-like polysaccharide, bupleuran 2IIc. Bupleuran 2IIc was homogeneous as determined by electrophoresis and gel filtration. Bupleuran 2IIc was composed mainly of galacturonic acid with small proportions of arabinose, rhamnose, and galactose, and its average relative molecular mass was estimated to be 63,000 d. BR-2 lost most of its activity after treatment with periodate or digestion with endo-polygalacturonase indicating that the polygalacturonan region and/or the molecular mass may contribute to activity.

Planta Med 1991 Dec;57(6):511-4

The effects of saikosaponin on macrophage functions and lymphocyte proliferation.

Ushio Y, Abe H

Research Institute of Oriental Medicine, Kinki University, Osaka, Japan.

The effects of saikosaponin-d (ssd), isolated from Bupleurum radix, on phagocytic functions of mouse peritoneal macrophages were investigated after treatment in vitro. The macrophages treated with ssd showed a significant increase in PMA-induced chemiluminescence. An increase in phagocytosis was detected after treatment with saikosaponin-b2 (0.1 microM) for 24 h in vitro, while a suppression of phagocytosis was observed following treatment with saikosaponins (0.5 microM). Treatment with ssd markedly increased the random migration of resident peritoneal macrophages, but did not affect the migration towards FMLP. We further investigated the effect of ssd on proliferative responses of spleen cells and found that ssd, which itself has no mitogenic activity, decreased spleen cell proliferative response to T-cell mitogen, but increased the response to B-cell mitogen.

Carbohydr Res 1991 Oct 14;219:173-92

Partial structure of an anti-ulcer pectic polysaccharide from the roots of Bupleurum falcatum L.

Yamada H, Hirano M, Kiyohara H

Oriental Medicine Research Center of the Kitasato Institute, Tokyo, Japan.

Methylation analysis of a pectic polysaccharide (Bupleuran 2IIc) with anti-ulcer activity, isolated from the roots of Bupleurum falcatum L., revealed (1----4)-linked alpha-GalA together with small proportions of 2,4- and 3,4-linked GalA, and variously linked neutral sugars. Digestion of Bupleuran 2IIc with endo-alpha-(1----4)-polygalacturonase gave mainly galacturono-oligosaccharides (PG-4) and small proportions of enzyme-resistant regions (PG-1-3). PG-1 contained the sequence----4)GalA- (1----2)-Rha-(1----4)-GalA-(1----, and partial acid hydrolysis gave GalA-(1----4)-Rha, GlcA-(1----4)-Rha, and several di- and oligosaccharides consisting variously of Xyl, Glc, Gal, and Man. PG-2 and PG-3 each contained Rha, Fuc, Ara, Xyl, Man, Gal, Glc, GalA, GlcA, 2-Me-Fuc, 2-Me-Xyl, apiose (Api), aceric acid (AceA), and 3-deoxy-D-manno-2-octulosonic acid (Kdo). PG-4 contained (1----4)-linked alpha-galacturono-di-to-penta- saccharides and GalA. The galacturono-tetra- and -penta-saccharides had one and three methyl-esterified GalA units, respectively, and some of the galacturono-oligosaccharides contained 2,4- or 2,3-linked GalA.

J Pharm Pharmacol 1991 Oct;43(10):699-704

Effects of a polysaccharide fraction from the roots of Bupleurum falcatum L. on experimental gastric ulcer models in rats and mice.

Sun XB, Matsumoto T, Yamada H

Oriental Medicine Research Center, Kitasato Institute, Tokyo, Japan.

Effects of an acidic polysaccharide fraction, BR-2, from the roots of Bupleurum falcatum L., on HCl-ethanol, ethanol and water immersion stress-induced gastric lesions in mice and pylorus-ligated ulcers in rats have been studied. Oral administration of BR-2 at doses of 50 to 200 mg kg-1 inhibited the formation of the gastric lesions induced by necrotizing agents such as HCl-ethanol and ethanol, in a dose dependent manner. This protective effect was observed after oral, intraperitoneal, and subcutaneous administration of BR-2 (25-100 mg kg-1). BR-2 also inhibited the formation of gastric ulcers which were induced by water immersion stress or pylorus-ligation. Prostaglandin E2 in gastric juice from rats and in gastric mucosa from mice was not influenced by oral administration of BR-2. The protective action of BR-2 against HCl-ethanol-induced gastric lesions was not abolished by pretreatment with indomethacin (20 mg kg-1, i.p.). The amount of alcian blue binding to mucosa also increased after administration of BR-2 (100 mg kg-1, p.o.); however, the amount of hexosamine and N-acetylneuraminic acid in mucosa did not change significantly.

Prostaglandins Leukot Essent Fatty Acids 1991 Sep;44(1):51-6

Inhibition of platelet activation and endothelial cell injury by flavan-3-ol and saikosaponin compounds.

Chang WC, Hsu FL

Department of Pharmacology, College of Medicine, National Cheng Kung University, Taiwan, Republic of China.

The effects of flavan-3-ol and saikosaponin compounds on platelet aggregation, platelet thromboxane biosynthesis and H2O2-induced endothelial cell injury were studied. Seven flavan-3-ol compounds isolated from Camellia sinensis L. var sinensis O. Kuntze (Theaceae) and three saikosaponin compounds isolated from Bupleurum falcatum L. (Umbelliferae) were used. Among the 10 compounds tested, only epigallocatechin and saikosaponin a significantly inhibited human platelet aggregation induced by ADP, and the potency of inhibition was comparable with aspirin. Both of epigallocatechin and saikosaponin a dose-dependently inhibited the platelet thromboxane formation from exogenous and endogenous arachidonic acid. In the prevention of H2O2-induced endothelial cell injury in culture, only gallocatechin-3-0-gallate and epicatechin-3-0-gallate were effective. The inhibitory effect of epigallocatechin and saikosaponin a on platelet activation and the cytoprotective effect of gallocatechin-3-0-gallate and epicatechin-3-0-gallate on H2O2-induced endothelial cell injury could give evidence of explaining the possible role of flavan-3-ol and saikosaponin compounds in maintaining vascular homeostasis.

Nippon Yakurigaku Zasshi 1991 Jan;97(1):13-21

[Studies on antinephritic effects of plant components in rats (1). Effects of saikosaponins original-type anti-GBM nephritis in rats and its mechanisms].

[Article in Japanese]

Hattori T, Ito M, Suzuki Y

Department of Pharmacology, Faculty of Pharmacy, Meijo University, Nagoya, Japan.

This study was designed to clarify the anti-nephritic effects of the saikosaponins that are contained in Bupleurum falcatum L. crude saikosaponin at 1.0 mg and 5.0 mg/kg, i.p. prevented urinary protein excretion and elevation of serum cholesterol content on the 10th day after the injection of anti-GBM serum. Moreover, crude saikosaponin at 1.0 mg and 5.0 mg/kg, i.p. significantly inhibited histopathological changes such as hypercellularity and adhesion. On the other hand, saikosaponin a (5.0 mg/kg, i.p.) and d (1.0 mg and 5.0 mg/kg, i.p.) also prevented urinary protein excretion, elevation of serum cholesterol content, and histopathological changes. In the second study, to clarify the anti-nephritic mechanisms of saikosaponins on this model, we investigated the effect of saikosaponins on platelet aggregation, release of corticosterone and reactive oxygen species scavengers activity. Crude saikosaponin and saikosaponin d significantly inhibited the increase in platelet aggregation, and saikosaponin d enhanced the serum and intra-adrenal corticosterone levels. Crude saikosaponin and saikosaponin a inhibited the decrease in activity of scavengers (SOD, catalase, glutathione peroxidase). These results indicate that saikosaponins were effective on this model, and anti-nephritic mechanisms of saikosaponins were party due to anti-platelet, corticosterone releasing and enhancing action on the activity of reactive oxygen species scavengers.

Int J Immunopharmacol 1991;13(5):501-8

Effect of saikosaponin on the immune responses in mice.

Ushio Y, Oda Y, Abe H

Research Institute of Oriental Medicine, Kinki University, Osaka, Japan.

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.

Int J Immunopharmacol 1991;13(5):493-9

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

Ushio Y, Abe H

Research Institute of Oriental Medicine, Kinki University, Osaka, Japan.

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.

Am J Chin Med 1990;18(3-4):105-12

The pharmacological and pathological studies on Taiwan folk medicine (III): The effects of bupleurum kaoi and cultivated bupleurum falcatum var. komarowi.

Lin CC, Chiu HF, Yen MH, Wu CC, Chen MF

School of Pharmacy, Kaohsiung Medical College, Taiwan, Republic of China.

The protective effects of water extract from roots of Bupleurum kaoi Liu, Chao et Chuang and Bupleurum flacatum L. var. Komarowi Koso-Polj on CCl4-induced hepatoxicity have been investigated. Both B. kaoi (p less than 0.05) and B. falcatum var. komarowi (p less than 0.01) possessed more marked anti-hepatotoxic pharmacological effects than Bupleurum chinense DC., the typical strain widely used in Taiwan. The pathological improvement from treatment by means of the three drugs to alleviate CCl4-induced hepatic toxicity was estimated using morphological changes of hepatocytes, reduction of inflammatory cells infiltration and liver function tests.

Chem Pharm Bull (Tokyo) 1989 Oct;37(10):2736-40

Corticosterone secretion-inducing activity of saikosaponin metabolites formed in the alimentary tract.

Nose M, Amagaya S, Ogihara Y

The corticosterone secretion-inducing activities of saikosaponin a, saikosaponin c and saikosaponin d, isolated from the root of Bupleurum falcatum L., and 27 metabolites formed in the murine alimentary tract were studied in mice. Serum corticosterone was determined by high-performance liquid chromatography (HPLC). Intraperitoneal administration of saikosaponin a and its intestinal metabolite, prosaikogenin F, showed corticosterone secretion-inducing activity at a dose of 0.1 mmol/kg, and maximally increased it at a dose of 0.4 mmol/kg. On the other hand, the genuine sapogenin, saikogenin F, was inactive. Saikosaponin b1 and saikosaponin g, gastric metabolites of saikosaponin a, and their intestinal metabolites, prosaikogenin A, prosaikogenin H, saikogenin A and saikogenin H, were also inactive. Serum corticosterone was increased by the administration of saikosaponin d and its intestinal metabolite, prosaikogenin G, at a dose of 0.04 mmol/kg, and it reached the maximal level at the dose of 0.1 mmol/kg. Saikogenin G also showed a slight activity. A gastric metabolite of saikosaponin d, saikosaponin b2, and its intestinal metabolites, prosaikogenin D and saikogenin D, were inactive. In the experiments on saikosaponin c and its metabolites, saikosaponin c was inactive but its intestinal metabolites, especially prosaikogenin E-2, showed activity almost equal to that of saikosaponin a. Saikosaponin h and saikosaponin i, gastric metabolites of saikosaponin c, were also inactive, but their prosaikogenins showed slight activities. When these compounds were orally administered, their corticosterone secretion-inducing activities were similar to those obtained in the intraperitoneal experiment. These results suggest that a proper polar balance between the sugar moiety and the aglycone is important for the corticosterone secretion-inducing activity of saikosaponins and their metabolites.


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