Research Publications on "Sho-saiko-to" (1990-2001)

 

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<5>

Authors

  Li C.  Homma M.  Oka K.

Institution

  Department of Clinical Pharmacology, School of Pharmacy, Tokyo University of

  Pharmacy and Life Science, Japan.

Title

  Characteristics of delayed excretion of flavonoids in human urine after

  administration of Shosaiko-to, a herbal medicine.

Source

  Biological & Pharmaceutical Bulletin.  21(12):1251-7, 1998 Dec.

Abstract

  There has been little explanation of herbal medicines by modern medical

  sciences, including pharmacokinetics, whereas physicians follow empirical

  indications written in classical literature. Recent reports of herb-induced

  adverse reactions compelled us to proceed the investigation of a herbal

  medicine Shosaiko-to (TJ-9) from a pharmacokinetic point of

  view. To five healthy volunteers, a single 5 g dose of TJ-9, consisting of 7

  herbs, was administered. We conducted HPLC analysis of the timed-urine

  specimens to disclose the type and amount of compounds excreted. Excretion

  rate-time curves were analyzed individually. Four flavonoids, liquiritigenin,

  baicalein, wogonin and oroxylin A, were found both in the urine and TJ-9. The

  glycosides in TJ-9 were absorbed after microflora hydrolysis. Davidigenin,

  which was not found in TJ-9, was an intestinal metabolite of liquiritigenin.

  Also, two flavanones, S-dihydrowogonin and S-dihydrooroxylin A, were

  identified as the metabolites of wogonin and oroxylin A, respectively.

  Excretion rate-time curves of the flavonoids were divided into three types of

  structure-dependent absorption, i.e. (1) the fast absorption of herbal-origin

  aglycons, (2) the moderately-delayed absorption of aglycons derived from

  herbal glycosides, and (3) markedly-delayed absorption after the molecular

  transformation of herbal compounds. Individual excretion profiles seemed to

  depend on microflora activities. Two types of flavanones, S-dihydrowogonin

  and S-dihydrooroxylin A, were found in a half of the volunteers, suggesting

  there might be two kinds of volunteers, namely, rapid and poor metabolizers

  of flavonoids.

 

<6>

Authors

  Nakahata N.  Kutsuwa M.  Kyo R.  Kubo M.  Hayashi K.  Ohizumi Y.

Institution

  Department of Pharmaceutical Molecular Biology, Faculty of Pharmaceutical

  Sciences, Tohoku University, Sendai, Japan.

Title

  Analysis of inhibitory effects of scutellariae radix and baicalein on

  prostaglandin E2 production in rat C6 glioma cells.

Source

  American Journal of Chinese Medicine.  26(3-4):311-23, 1998.

Abstract

  Inhibitory mechanism of the water extract of Scutellariae Radix on

  prostaglandin E2 (PGE2) release was examined in C6 rat glioma cells.

  Scutellariae Radix reduced a Ca2+ ionophore A23187-induced PGE2 release by

  inhibition of arachidonic acid (AA) liberation. Sho-saiko-to

  and San'o-shashin-to, which contain Scutellariae Radix, also inhibited PGE2

  release. A23187 caused phosphorylation of mitrogen-activated protein kinase

  (MAPK), resulting in activation of cytosolic phospholipase A2 (cPLA2).

  Scutellariae Radix and baicalein inhibited the phosphorylation of MAPK.

  Baicalein, but not baicalin, inhibited A23187-induced PGE2 release. These

  results suggest that baicalein in Scutellariae Radix reduces AA liberation

  through the inhibition of the MAPK-cPLA2 pathway.

 

<7>

Authors

  Kyo R.  Nakahata N.  Sakakibara I.  Kubo M.  Ohizumi Y.

Institution

  Department of Pharmaceutical Molecular Biology, Faculty of Pharmaceutical

  Sciences, Tohoku University, Aramaki, Sendai, Japan.

Title

  Effects of Sho-saiko-to, San'o-shashin-to and Scutellariae

  Radix on intracellular Ca2+ mobilization in C6 rat glioma cells.

Source

  Biological & Pharmaceutical Bulletin.  21(10):1067-71, 1998 Oct.

Abstract

  Glial cells are able to support neurons physically and functionally. The

  present study was undertaken to determine the effects of Kampo medicines on

  glial cell function, especially Ca2+ mobilization. C6 rat glioma cells

  expressed H1-histamine, muscarinic cholinergic and adrenergic

  alpha1-receptors, stimulation of which resulted in phosphoinositide

  hydrolysis and increase in intracellular Ca2+ concentrations ([Ca2+]i). The

  water extracts of Sho-saiko-to and San'o-shashin-to, Kampo

  medicines which contain Scutellariae Radix (Ogon, the root of Scutellaria

  baicalensis GFORGI), inhibited histamine (100 microM)-induced increase in

  [Ca2+]i in a concentration-dependent manner. The water extract of

  Scutellariae Radix potently decreased [Ca2+]i in a concentration-dependent

  manner. Sho-saiko-to, San'o-shashin-to and Scutellariae

  Radix significantly inhibited histamine-induced accumulation of total

  [3H]inositol phosphates, consistent with their inhibition of the increase in

  [Ca2+1]i. These results suggest that Sho-saiko-to,

  San'o-shashin-to and Scutellariae Radix inhibit Ca2+ mobilization mediated

  via an inhibition of phospholipase C. The inhibitory effect may be important

  in interpreting the pharmacological actions of above Kampo medicines.

 

<8>

Authors

  Kayano K.  Sakaida I.  Uchida K.  Okita K.

Institution

  First Department of Internal Medicine, Yamaguchi University, School of

  Medicine, Ube City, Japan.

Title

  Inhibitory effects of the herbal medicine Sho-saiko-to

  (TJ-9) on cell proliferation and procollagen gene expressions in cultured rat

  hepatic stellate cells.

Source

  Journal of Hepatology.  29(4):642-9, 1998 Oct.

Abstract

  BACKGROUND/AIMS: It is of extreme importance to prevent liver fibrosis and

  subsequent progression to liver cirrhosis. The aim of our study was to

  elucidate in vitro whether Sho-saiko-to exerted inhibitory

  effects on hepatic stellate cells. METHODS: Hepatic stellate cells were

  isolated from male Wistar rats. Water-soluble ingredients of

  Sho-saiko-to were obtained at concentrations of 10, 100,

  250, 500 and 1000 microg/ml. Morphological transformation was observed under

  a phase-contrast microscope. Flow cytometric analysis was performed on day 4

  after culture to evaluate the potential to proliferate of the stellate cells

  by analyzing cell cycles. Northern blot analysis was carried out on day 3

  after culture to determine the expressions of type I and type III procollagen

  mRNAs. RESULTS: (i) Sho-saiko-to 500 and 1000 microg/ml

  inhibited morphological transformation of the stellate cells to

  myofibroblast-like cells. (ii) Sho-saiko-to 500 and 1000

  microg/ml significantly (p<0.0001) accumulated the cells in the G0/G1 phase

  (118.8+/-0.7%, 119.2+/-0.5%, respectively as compared with control) and

  significantly (p<0.0001) decreased cell numbers subsequently in G2/M phase

  (47.5+/-8.1%, 48.9+/-2.0%, respectively). (iii) Sho-saiko-to

  500 and 1000 microg/ml also significantly (p<0.05 or p<0.0001) suppressed

  procollagen mRNA expression of type I to 51.5+/-6.4%, 34.9+/-3.7%,

  respectively, and type III to 51.3+/-12.3%, 46.7+/-11.4%, respectively.

  CONCLUSIONS: We have clarified the inhibitory effects of

  Sho-saiko-to on hepatic stellate cells in vitro.

  Sho-saiko-to could be a potent inhibitor in the pathogenesis

  of liver fibrosis.

 

<9>

Authors

  Matsumoto T.  Shibata T.

Institution

  Department of Otolaryngology, Izumiotsu Municipal Hospital, Osaka, Japan.

Title

  The ex vivo effect of the herbal medicine sho-saiko-to on

  histamine release from rat mast cells.

Source

  European Archives of Oto-Rhino-Laryngology.  255(7):359-64, 1998.

Abstract

  A traditional Japanese herbal medicine, Shosaiko-to (SST),

  has been used orally to treat several chronic diseases. Since these have

  included allergic rhinitis and bronchial asthma, we investigated the effect

  of SST on histamine release and the intracellular Ca2+ response in mast cells

  ex vivo. A single dose of 1.0 g/kg SST was administered orally to immunized

  rats 2-12 h before death. Mast cells were then separated from peritoneal

  lavages and stimulated with antigen. SST at 3 h after oral administration

  most significantly inhibited histamine release. This inhibitory effect was

  dose-dependent and was weaker than that of tranilast. In contrast, SST at 3 h

  had no effect on the antigen-induced Ca2+ response of the mast cells and

  failed to inhibit compound 48/80-induced histamine release. Our findings show

  that SST indeed has an active anti-allergic effect. We suggest that SST

  inhibits IgE receptor-associated protein phosphorylation in the histamine

  release pathway.

 

<10>

Authors

  Kato M.  Liu W.  Yi H.  Asai N.  Hayakawa A.  Kozaki K.  Takahashi M.

  Nakashima I.

Institution

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

Title

  The herbal medicine Sho-saiko-to inhibits growth and

  metastasis of malignant melanoma primarily developed in ret-transgenic mice.

Source

  Journal of Investigative Dermatology.  111(4):640-4, 1998 Oct.

Abstract

  Sho-saiko-to is the most popular herbal medicine in Japan.

  We investigated the anti-tumor and anti-metastatic effects of

  Sho-saiko-to and its chemically defined ingredients on the

  primary skin melanoma that developed in a metallothionein-I (MT)/ret

  transgenic mouse line and on a melanoma cell line (Mel-ret), which was

  derived from a primary tumor developed in a MT/ret transgenic mouse. In

  vitro, Sho-saiko-to suppressed the growth of Mel-ret cells

  more strongly than any single ingredient of Sho-saiko-to,

  although baicalin as one of several ingredients tested also suppressed it

  significantly. In vivo, Sho-saiko-to (i) significantly (p <

  0.02) prolonged the onset of tumor development (1.5 mo), (ii) definitely

  retarded the transition to malignancy, (iii) significantly decreased the

  incidence of distant metastasis to brain (p < 0.002), kidney (p < 0.05), and

  liver (p < 0.05) at the malignant stage, and (iv) significantly (p < 0.02)

  prolonged life span (2.6 mo). Moreover, Sho-saiko-to and

  baicalin down-regulated the matrix metalloproteinase-2 and -9 expression

  levels, and upregulated their inhibitor expression level in both the primary

  tumors and Mel-ret cells. In conclusion, Sho-saiko-to

  displayed anti-tumor and anti-metastatic effects on melanoma with regulation

  of the balance of matrix metalloproteinase and tissue inhibitor of the matrix

  metalloproteinase levels.

 

<11>

Authors

  Li C.  Homma M.  Oka K.

Institution

  Department of Clinical Pharmacology, School of Pharmacy, Tokyo University of

  Pharmacy and Life Science, Japan.

Title

  Chiral resolution of four major flavanones in post-administrative urine of

  Chinese herbal medicines by HPLC on macroporous silica gel coated with

  cellulose tris(3,5-dimethylphenylcarbamate).

Source

  Biomedical Chromatography.  12(4):199-202, 1998 Jul-Aug.

Abstract

  Direct chiral resolution of four major flavanones recovered from

  post-administrative urine of the traditional Chinese medicines Daisaiko-to

  and Shosaiko-to was achieved by high-performance liquid

  chromatography (HPLC) on macroporous silica gel coated with cellulose

  tris(3,5-dimethylphenylcarbamate), Chiralcel OD. Chromatographic conditions

  were optimized so as to attain satisfactory enantiomeric resolution of the

  polysubstituted flavanones. Urinary liquiritigenin and naringenin were

  considerable mixtures of R and S-enantiomers, while S-enantiomers of

  dihydrowogonin and dihydrooroxylin A were predominantly excreted. Our chiral

  HPLC techniques can be applied to pharmacokinetical evaluation of the chiral

  flavanone enantiomers following oral administration of the herbal medicines.

 

<12>

Authors

  Liu W.  Kato M.  Akhand AA.  Hayakawa A.  Takemura M.  Yoshida S.  Suzuki H.

  Nakashima I.

Institution

  Department of Immunology, Nagoya University School of Medicine, Nagoya

  466-8550, Japan.

Title

  The herbal medicine sho-saiko-to inhibits the growth of

  malignant melanoma cells by upregulating Fas-mediated apoptosis and arresting

  cell cycle through downregulation of cyclin dependent kinases.

Source

  International Journal of Oncology.  12(6):1321-6, 1998 Jun.

Abstract

  The anti-tumor effect and its mechanism of the herbal medicine

  sho-saiko-to were investigated on a murine malignant

  melanoma cell line (Mel-ret). Sho-saiko-to induced apoptotic

  cell death of Mel-ret cells with a definite increase of cell surface Fas

  antigen and Fas ligand (FasL). Sho-saiko-to arrested Mel-ret

  cells in G1 phase by decreasing the expression of cyclin-dependent kinase

  (cdk) 4 and its homologue cdk6. Kinase activities of cdk4 and cdk6 were

  identified to be downregulated by sho-saiko-to. Ingredient

  analysis revealed that baicalin is likely the main active constituent in the

  upregulation of Fas antigen and Fas ligand, while glycyrrhizin is the main

  constituent in the inhibition of cdks.

 

<13>

Authors

  Li C.  Homma M.  Ohkura N.  Oka K.

Institution

  Department of Clinical Pharmacology, School of Pharmacy, Tokyo University of

  Pharmacy and Life Science, Japan.

Title

  Stereochemistry and putative origins of flavanones found in

  post-administration urine of the traditional Chinese remedies

  shosaiko-to and daisaiko-to.

Source

  Chemical & Pharmaceutical Bulletin.  46(5):807-11, 1998 May.

Abstract

  Optically active flavanones, dihydrowogonin and dihydrooroxylin A, were found

  in the urine of healthy volunteers who orally received the traditional

  Chinese remedies Shosaiko-to and Daisaiko-to on separate

  occasions. These remedies, which consisted of dried extracts of Scutellariae

  Radix and other herbs, contained the metabolic precursors of the flavanones,

  but not the flavanones themselves, in stoichiometrically sufficient amounts.

  Structures and stereochemistry of the flavanones were elucidated by UV,

  circular dichroism (CD), electron impact (EI)-MS and 1H-NMR analyses, showing

  that the biotransformations from the corresponding flavones, wogonin and

  oroxylin A, were stereoselective with a preference for the S-enantiomers. The

  putative origins of the flavanones were confirmed in terms of

  pharmacokinetics. Renal excretion-time data of the flavanones and the

  flavones suggested that the stereoselective transformations might have

  occurred in the intestinal tract as a result of microfloral metabolism before

  absorption.

 

<14>

Authors

  Kojima K.  Mizukami H.  Tazawa T.  Nose M.  Inoue M.  Ogihara Y.

Institution

  Faculty of Pharmaceutical Sciences, Nagoya City University, Nagoya, Japan.

Title

  Long-term administration of "sho-saiko-to" increases

  cytochrome P-450 mRNA level in mouse liver.

Source

  Biological & Pharmaceutical Bulletin.  21(4):426-8, 1998 Apr.

Abstract

  Simplified differential display of mRNA was applied to isolate and identify

  genes transcriptionally regulated in mouse liver by

  sho-saiko-to administration. A cDNA fragment up-regulated by

  sho-saiko-to was isolated and characterized. cDNA sequencing

  and subsequent database analysis revealed that the fragment showed

  significant sequence similarity with mouse testosterone 16-alpha-hydroxylase

  (cytochrome P-450[16alpha]) cDNA. The increased level of mRNA expression of

  cytochrome P-450(16alpha) in association with sho-saiko-to

  administration suggests the molecular mechanism of the chemopreventive effect

  of sho-saiko-to. This result indicates the usefulness of the

  mRNA differential display technique to investigate the molecular mechanism of

  Kampo medicine.

 

<15>

Authors

  Nishimura N.  Naora K.  Hirano H.  Iwamoto K.

Institution

  Department of Pharmacy, Shimane Medical University Hospital, Izumo, Japan.

Title

  Effects of Sho-saiko-to on the pharmacokinetics and

  pharmacodynamics of tolbutamide in rats.

Source

  Journal of Pharmacy & Pharmacology.  50(2):231-6, 1998 Feb.

Abstract

  Although Sho-saiko-to (Xiao Chai Hu Tang), a major Chinese

  traditional medicine, is frequently prescribed with other synthetic or

  biotechnological drugs for the treatment of various chronic diseases, there

  is a dearth of information about interactions between

  sho-saiko-to and co-administered drugs. This paper reports

  the effects of Sho-saiko-to on the pharmacokinetics and

  glucose responses of a sulphonylurea hypoglycaemic agent, tolbutamide, after

  their oral administration in rats. After oral administration of tolbutamide

  (50 mg kg(-1)) with or without Sho-saiko-to extract powder

  (300 mg kg(-1)) to male Sprague-Dawley rats cannulated in the jugular vein,

  plasma tolbutamide and glucose levels were periodically measured.

  Co-administration of Sho-saiko-to tended to elevate the

  plasma tolbutamide concentration in the absorption phase. A two-compartment

  lag-time model was found to describe the plasma tolbutamide

  concentration-time data. The maximum concentration of tolbutamide was

  significantly increased and time to reach the maximum concentration was

  reduced to about 70% by co-administration with Sho-saiko-to.

  There was no significant change in area under the curve or in the elimination

  half-life of tolbutamide. The extent of the lowering effect of tolbutamide on

  plasma glucose levels was increased up to 0.75 h and decreased after 5 h

  after co-administration of Sho-saiko-to. In conclusion,

  these studies suggest that sho-saiko-to slightly hastens the

  gastrointestinal absorption of tolbutamide. Furthermore, it is considered

  that elevation of the gastrointestinal absorption rate by

  Sho-saiko-to might potentiate the hypoglycaemic effect of

  this sulphonylurea in the early period after oral administration.

 

<16>

Authors

  Sakaida I.  Matsumura Y.  Akiyama S.  Hayashi K.  Ishige A.  Okita K.

Institution

  First Department of Internal Medicine, School of Medicine, Yamaguchi

  University, Japan.

Title

  Herbal medicine Sho-saiko-to (TJ-9) prevents liver fibrosis

  and enzyme-altered lesions in rat liver cirrhosis induced by a

  choline-deficient L-amino acid-defined diet.

Source

  Journal of Hepatology.  28(2):298-306, 1998 Feb.

Abstract

  BACKGROUND/AIM: A herbal medicine, Sho-saiko-to (TJ-9), has

  recently been orally administered to patients with chronic liver disease in

  Japan and has been reported to inhibit the development of hepatocellular

  carcinoma. The aim of this study was to investigate whether TJ-9 has an

  inhibitory effect on the development of preneoplastic lesions and liver

  fibrosis in rats. METHODS: The effects of the TJ-9 were examined using the

  choline-deficient L-amino acid-defined (CDAA) diet-induced liver fibrosis

  model in 16-week-old male Wistar rats. RESULTS: TJ-9 (1% w/w) prevented

  fibrosis, as indicated by reduced hydroxyproline content in the liver and

  inhibition of the increase in a serum marker of fibrosis (hyaluronic acid),

  without reducing the increase in serum alanine aminotransferase and aspartate

  aminotransferase. TJ-9 also reduced the expression of type III procollagen

  alpha 1 mRNA in the liver, as well as the proliferation of myofibroblast-like

  cells (activated stellate cells, activated Ito cells). Furthermore, TJ-9

  reduced the number of preneoplastic lesions, detected as enzyme-altered

  (glutathione S-transferase placental form-positive) lesions, in the liver.

  CONCLUSIONS: These results indicate that the herbal medicine

  Sho-saiko-to (TJ-9) prevents fibrosis as well as

  preneoplastic lesions, not by inhibiting hepatocyte cell death but by

  inhibiting the activation of stellate cells, which are considered to be the

  main collagen-producing cells, leading to a reduction in the development of

  preneoplastic lesions.

 

<17>

Authors

  Miyamura M.  Ono M.  Kyotani S.  Nishioka Y.

Institution

  Department of Pharmacy, Kochi Medical School Hospital, Kohasu, Japan.

Title

  Effects of sho-saiko-to extract on fibrosis and regeneration

  of the liver in rats.

Source

  Journal of Pharmacy & Pharmacology.  50(1):97-105, 1998 Jan.

Abstract

  Sho-saiko-to, one of the most widely used Chinese herbal

  preparations, has long been used for the treatment of chronic liver diseases.

  We have investigated its effect in retarding the process of liver fibrosis

  and accelerating liver regeneration, especially its effect on Ito cells that

  are thought to be deeply involved with liver fibrosis.

  Sho-saiko-to extract and its active constituents were orally

  administered to rats with dimethylnitrosamine-induced liver-injury. After

  treatment with sho-saiko-to extract hepatic function

  improved, histopathological results confirmed repair of liver tissue, and

  retinoid levels increased. On the other hand, when active constituents of

  sho-saiko-to extract were administered alone, liver retinoid

  levels remained low, implying that interaction among active constituents of

  the extract was suppressing Ito cell activation. When

  sho-saiko-to extract was administered to 70% hepatectomized

  normal and liver-injured rats, liver weight, the number of S-phase-cells and

  retinoid levels increased with time. However, these changes were different

  for normal and liver-injured rats, suggesting that the site of action of

  sho-saiko-to extract in regenerating liver is different for

  normal and liver-injured rats. These results show that

  sho-saiko-to extract was useful for suppressing the

  activation of Ito cells.

 

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