• 생약학회지
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• 제30권2호
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• pp.111-114
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• 1999

Inhibitory effect of water and ethyl acetate extract of 60 kinds of herbal medicines was investigated on ${\beta}-glucuronidase$. Among water extract of them, Galla Rhois had the most potent ${\beta}-glucuronidase-inhibitory\;activity$. Termaliae Fructus, Amomi Tsa-ko Fructus and Arecae Semen were also potent inhibitors. Among ethyl acetate extract of them, Galla Rhois had the most potent ${\beta}-glucuronidase-inhibitory\;activity$. Nelumbinis Semen. Ephedrae Radix and Termaliae Fructus were also potent inhibitors. The extract of Galla Rhois had potent hepatoprotective effect on $CCl_4-induced$ hepatotoxicity of rats. These results suggest that the ${\beta}-glucuronidase$ seems to be closely related to the liver injury, which could be prevented by the inhibitor of ${\beta}-glucuronidase$.

• 한국식품영양학회지
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• 제25권3호
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• pp.620-628
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• 2012

We examined the effects of biological activity Phellinus linteus mycelium culture with cassiae semen extract. Firstly, the optimal temperature, initial pH and culture period for mycelial growth in a liquid culture of P. linteus were determined, and they were $30^{\circ}C$, pH 5.0 and 8 days respectively. The five herbal materials were examined against several health functional efficacies, and, as a result, Cassiae semen was chosen, with its superior inhibitory effects in ${\beta}$-glucuronidase inhibitory activity, electron donating activity, ACE inhibitory, and ${\alpha}$-glucosidase inhibitory activities(95.3%, 80.9%, 96.1 and 24.2%, respectively). P. linteus fruit body was investigated on ${\beta}$-glucuronidase inhibitory activity, electron donating activity, ACE inhibitory, and ${\alpha}$-glucosidase inhibitory activities, and they were 54.7%, 81.9%, 30.0% and 20.1%, respectively. Accordingly, C. semen was used in the following experiment, to give an additive functional effect on the P. linteus. As the amount of C. semen in the cultural media increased, mycelial weight and ${\beta}$-glucan contents also increased, but final pH was not influenced. In addition, the ${\beta}$-glucuronidase inhibitory activity, electron donating activity, and ${\alpha}$-glucosidase inhibitory activity increased. P. linteus mycelium culture showed higher activities in the other three tests above, except for electron donating activity, when C. semen was added to the medium before cultivation.

• Natural Product Sciences
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• 제7권3호
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• pp.63-67
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• 2001

${\beta}-Glucuronidase-inhibitory$ and hepatoprotective effects of Chungpesagan-tang, which has been used for liver diseases and stroke, on $CCl_4-induced$ hepatotoxicity of rats was investigated. Chungpesagan-tang potently inhibited ${\beta}-glucuronidases$. Serum AST, ALT and LDH levels of the $CCl_4$ group orally treated with Chungpesagan-tang (100 mg/kg) were lowered to 47, 28 and 58% of the $CCl_4-treated$ group, respectively. Among the ingredients of Chungpesagan-tang, Puerariae Radix, Scutellariae Radix and Rhei Rhizoma potently inhibited the ${\beta}-glucuronidase$ and protected $CCl_4-induced$ liver injury. The hepatoprotective activity of Puerariae Radix was affected by ingredients of Chungpesagan-tang: Scutellariae Radix had the synergistic activity, but Angelicae Tenussimae Radix exhibited the antagonistic activity. These results suggest that the ${\beta}-glucuronidase$ inhibitor of herbal medicines may protect $CCl_4-induced$ liver injury and puerarin should be a natural prodrug for the hepatoprotective effect.

• Toxicological Research
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• 제14권2호
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• pp.163-169
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• 1998

Fluoride (F), over a narrow concentration range, increases bone formation. Aluminum (Ai) too is biphasic in its action on bone, being mitogenic at very low levels and inhibitory at higher levels. Both F and Al are present in finished drinking water where the chemical interaction of these two agents is well characterized. F and AI, given individually, accumulate preferentially in bone. In addition. in vivo studies have shown that F causes the co-accumulation of Al in bone. Thus, it was necessary to determine the interactive effect of these two agents on bone mitogenesis. Calvaria were obtained from neonatal CD-1 mice and cultured with various concentrations of F (0.05~19 ppm) as NaF, Al (2 ppb~2 ppm) as $AlCl_3$ , or F and Al for 3 days at $37^{\circ}C$ on a rotating roller drum. Alkaline phosphatase activity in calvaria and $\beta$-glucuronidase activity in culture medium were determined as a measures of bone turnover. Alkaline phosphatase activity in calvaria was significantly increased by F (0.05~2 ppm) treatment and $\beta$-glucuronidase activity was slightly increased in the culture medium of calvaria treated with 0.3 ppm Al. The combination of 19 ppm F and 0.3 ppm Al increased alkaline phosphatase activity in calvaria, but did not affect $\beta$-glucuronidase activity, suggesting the interactive effect of fluoride and aluminum on bone turnover.

• Food Science and Biotechnology
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• 제17권5호
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• pp.1110-1114
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• 2008

$\beta$-Glucuronidases of intestinal bacteria are capable of retoxifying compounds that have been detoxified by liver glucuronidation, which is one of the most important detoxication processes in the liver. Therefore, this enzyme is known to accelerate colon cancer invasion and metastasis. Two bromophenols, 2,4,6-tribromophenol (I) and 2,4-dibromophenol (II), were purified from the red alga Grateloupia elliptica. $IC_{50}$ values of bromophenol I and II against Escherichia coli $\beta$-glucuronidase were 5.4 and 8.5 mg/mL, respectively. Hence, bromophenols of G. elliptica, a potent $\beta$-glucuronidase inhibitor, can be used as a novel pharmaceutical agent for the prevention and treatment of colon cancer.

• Journal of Microbiology and Biotechnology
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• 제31권11호
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• pp.1576-1582
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• 2021

Bacterial β-glucuronidase in the intestine is involved in the conversion of 7-ethyl-10-hydroxycamptochecin glucuronide (derived from irinotecan) to 7-ethyl-10-hydroxycamptothecin, which causes intestinal bleeding and diarrhea (side effects of anti-cancer drugs). Twelve compounds (1-12) from Polygala tenuifolia were evaluated in terms of β-glucuronidase inhibition in vitro. 4-O-Benzoyl-3'-O-(O-methylsinapoyl) sucrose (C3) was highly inhibitory at low concentrations. C3 (an uncompetitive inhibitor) exhibited a k_i value of 13.4 μM; inhibitory activity increased as the substrate concentration rose. Molecular simulation revealed that C3 bound principally to the Gln158-Tyr160 enzyme loop. Thus, C3 will serve as a lead compound for development of new β-glucuronidase inhibitors.

• Journal of Microbiology
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• 제39권3호
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• pp.154-161
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• 2001

In recent years, colon cancer has been reported to be one of the most important causes of cancer morbidity and mortality in Korea. Epidemiological and experimental studies suggest that lactic acid bacteria (LAB) used to ferment dairy products inhibits colon carcinogenesis. The present study was designed to determine whether the colon cancer inhibitory effect of LAB (Bifidobacterium longum Hy8001; Bif and Lactobacillus acidophilus HY2l04; Lac) of Korean origin, is associated with intestinal microflora composition and certain enzyme activity in rats treated with azoxymethane (AOM). At five weeks of age, SD rats were divided at random into four (AOM alone, Bif, Lac, and Bif+Lac) groups. Oral administration of lactic acid bacteria cultures were performed daily until the termination of the study. Two weeks later all animals were given a subcutaneous injection of AOM dissolved in normal saline at a dose of 15 mg/kg of body weight once weekly for 2 weeks. Every two weeks for 10 weeks, five of the rats in each group were randomly chosen for fecal specimen collection. The fecal specimens were used for assay of $\beta$-glucuronidase and nitroreductase, and analysis of intestinal microflora composition. The activity of $\beta$-glucuronidase which plays an important role in the production of the carcinogenic metabolite of azoxymethane was remarkably increased in the AOM alone group after AOM injection and maintained the high level during the experiment. However, LAB inhibited the AOM-induced increase in $\beta$-glucuronidase activity. Nitroreductase activity decreased by 30-40% in LAB treated groups in comparison with that of the AOM alone group. The results of the present study suggest that LAB inhibits colon carcinogenesis by modulating the metabolic activity of intestinal micro-flora and improving the composition of intestinal microflora.

• 생약학회지
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• 제30권3호
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• pp.269-274
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• 1999

To analyze scientifically the prescription principle of polyprescriptions (Gamchotang, Daewhanggamchotang, Jakyakgamchotang, Gamchogungangtang and Gilkyungtang) containing Glycyrrhizae Radix, the transforming rate of glycyrrhizin in these polyprescriptions to 18 ${\beta}-glycyrrhetinic$ acid and their inhibitory effect on ${\beta}-glucuronidase$, hyaluronidase, phosphodiesterase and trypsin were investigated. When Glycyrrhizae Radix containing polyprescriptions were extracted with water, the contents of glycyrrhizin in water extract of Glycyrrhizae Radix with Rhei Rhizoma or with Zingiberis Rhizoma were higher than that of Glycyrrhizae Radix only, but that in water extract of Glycyrrhizae Radix with Platicodi Radix was lower than that of Glycyrrhizae Radix only. By human intestinal bacteria, glycyrrhizin was metabolized to 18 ${\beta}-glycyrrhetinic$ acid. These metabolism of glycyrrhizin in polyprescriptions containing Glycyrrhizae Radix was inhibited by Rhei Rhizoma, Paeoniae Radix and Platicodi Radix, but was not affected by Zingiberis Rhizoma. The inhibitory activity of Glycyrrhizae Radix on hyaluronidase and ${\beta}-glucuronidase$, was synergistic with Rhei Rhizoma or Zingiberis Rhizoma, but was antagonistic by Platicodi Radix.

• Archives of Pharmacal Research
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• 제28권3호
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• pp.325-329
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• 2005

The hepatoprotective activity of lactic acid bacteria (Lactobacillus brevis HY7401, Lactobacillus acidophilus CSG and Bifidobacterium longum HY8001), which inhibited $\beta$-glucuronidase productivity of intestinal microflora, on t-BHP- or CCl$_4$-induced hepatotoxicity of mice were evaluated. These oral administration of lactic acid bacteria lowered $\beta$-glucuronidase production of intestinal microflora as well as Escherichia coli HGU-3. When lactic acid bacteria at a dose of 0.5 or 2 g (wet weight)/kg was orally administered on CCl$_4$-induced liver injury in mice, these bacteria significantly inhibited the increase of plasma alanine transferase and aspartate transferase activities by $17-57\%$ and $57-66\%$ of the $CCI_4$ control group, respectively. These lactic acid bacteria also showed the potent hepatoprotective effect against t-BHP-induced liver injury in mice. The inhibitory effects of these lactic acid bacteria were more potent than that of dimethyl diphenyl bicarboxylate (DDB), which have been used as a commercial hepatoprotective agent. Among these lactic acid bacteria, L. acidophilus CSG exhibited the most potent hepatoprotective effect. Based on these findings, we insist that an inhibitor of $\beta$-glucuronidase production in intestine, such as lactic acid bacteria, may be hepatoprotective.

• 한국응용약물학회:학술대회논문집
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• 한국응용약물학회 1994년도 춘계학술대회 and 제3회 신약개발 연구발표회
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• pp.242-242
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• 1994

Cortex mori (Morus alba L.), the root bark of mulberry tree, has been used as an antiphlogistic, diuretic, and expectorant in herbal medicine. The purpose of this study was to determine whether Cortex mori could inhibit the ovalbumin (OA) -induced late asthmatic reaction in guinea pigs. Guinea pigs were sensitized by two exposures to an aerosol of OA(1.0%) and then challenged with aerosolized antigen(2.0%), The animals were pretreated by three inhalations of the aerosoled Cortex mori either before antigen sensitization or cahllenge. Bronchoalveolar lavage fluid(BALF) and peripheral blood were collected at 17 hours after OA challenge. The cell populations in BALF and peripheral blood were examined to determine the changes of the relative proportions of eosinophils,neutrophils and mononuclear cells etc. Beta-glucuronidase activity in BALF was measured to evaluate the alveolar macrophage activation. OA-induced histamine release from guinea pig peritoneal fluid cells was measured by radioisotope enzymatic asssay. Results were as follows. The number of eosinophils, neutriphils and lymphocytes recovered in BALF were significantly increased in the 17h following aerosol challenge with OA. Among them, eosinophil and neutriphils were decreased remarkably in group that had been preinhalated with Cortex mori. The number of lymphocytes in BALF were not decreased in group pretreated with CM before sensitization but decreased in Group pretreated with CM before challenge. After OA challenge, the number of eosinophils in peripheral blood were markedly increased, but Cortex mori inhibited significantly the OA-induced eosinophilia. Beta-glucuronidase activity in the supernatants of BALF were significantly increased in the 17h following aerosol challenge with OA, however, pretreatment of Cortex mori had no influence on Beta-glucuronidase activity, suggesting that Cortex mori had no inhibitory effect on OA-induced alveolar macrophage activation. Cortex mori inhibited the OA-induced histamine release from guinea pig peritoneal fluid cells. From the above results, it is suggested that Cortex mori contains some substances with an activity to inhibit the the OA-induced late phase reaction of the bronchial asthma in guinea pigs.