• 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 ${\beta}-glucuronidase$.

• Natural Product Sciences
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• 제5권1호
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• pp.48-53
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• 1999

There are epidemiological evidences that the population with high fecal ${\beta}-glucuronidase$ activity has greater risk of colon cancer than the population with low fecal ${\beta}-glucuronidase$. This relationship was investigated by using the mouse-dimethylhydrazine colon carcinogenesis model and the extract of antler which was a ${\beta}-glucuronidase$ inhibitor. Mice with low fecal ${\beta}-glucuronidase$ activity induced by administration of water and Folch's fraction of antler had significantly fewer aberrant crypts after injections of 1,2-dimethylhydrazine (DMH) than mice treated with DMH alone. The result supports the hypothesis that the inhibitor of ${\beta}-glucuronidase$ such as antler extract can protect an animal against the induction of colon cancer.

• Archives of Pharmacal Research
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• 제18권2호
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• pp.79-83
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• 1995

There is epidemilogical evidence that the population with high fecal ${\beta}-glucuronidase$activity has greater risk of colon cancer than the population with low facal ${\beta}-glucuronidase$. This relationship was investigated by using the mouse-dimethylhydrazine colon carcinogenesis model and the fraction of Glucidum which is a .${\beta}-glucuronidase$inhibitor. Mice with low facal ${\beta}-glucuronidase$activity induced by consumption of the ether fraction of G lucidum had significantly fewer aberrant crypts(AC) after injections of 1, 2-dimethylhydeazine (DMH) than mice treated with DMH alone. The result supports the hypothesis that the inhibitor such as the ether fraction of G lucidum can protect an animal against the induction of colon cancer.

• 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.

• 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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• 제14권3호
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• pp.349-356
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• 1998

We identified S9940, a novel microbial metabolite from Streptomyces spp., to inhibit the release of neurotransmitter from PC12 cells. S9940 is an inhibitor of trifiated norepinephrine ([$^{3}H$]-NE) release in high $K^+$ buffer solution containing ionomycin, indicating that S9940 inhibits neurotransmitter release after the influx of $Ca^{2+}$ ions. We also examined the effect of S9940 on $\beta-glucuronidase$ release from guinea pig neurophils and the effect on the neurite extension of PC12 cells and rat hippocampal neurons. As a result, S9940 inhibited $\beta-glucuronidase$ release: when treated with $5{\mu}g/ml$ of S9940, which prevented [$^{3}H$]-NE release, the inhibition of neurite extension for both PC12 cells and rat hippocampal neurons was observed.

• 한국균학회지
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• 제50권1호
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• pp.31-40
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• 2022

비병원성 야생효모로부터 대장에서의 독성물질 활성화에 관여하여 대장암을 유발시키는 효소 중의 하나인 β-glucuronidase를 저해하는 물질을 생산하기 위하여 대전광역시 월평공원으로부터 분리 동정한 야생효모들 중 비병원성 야생효모들을 선별하여 배양 상등액과 무세포 추출물을 각각 제조한 후 β-glucuronidase 저해활성을 측정하였다. 133균주의 비병원성 야생효모들 중 C. oleophila WP5-19-1의 무세포추출물이 49.0%의 가장 높은 저해활성을 보여 우수 균주로 최종 선발하였다. β-Glucuronidase 저해물질 최적 생산 조건은 C. oleophila WP5-19-1를 초기 pH를 6.0으로 조정한 dextrose 5% 함유한 potato dextrose 배지에 접종하여 30℃에서 24시간 배양하였을 때였고 이때 IC₅₀값; 8.4 mg으로 가장 높은 저해활성을 보였다. C. oleophila WP5-19-1의 β-glucuronidase 저해물질을 한외여과와 Sephadex G-50으로 gel 여과를 실시하여 부분 정제하였고 이들은 30-60℃, pH 6.0-9.0에서 80% 이상의 잔존 저해활성을 보여 안정하였다. 또한 철, 구리, 아연과 같은 중금속 이온들은 저해활성을 활성화시켰다.

• Preventive Nutrition and Food Science
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• 제2권1호
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• pp.55-60
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• 1997

A lysosomal and matrix degrading enzyme $\beta$-glucuronidase activity was measured in BALS/c mice fed high and low Ca in combination with the i.p. adminstration of calcium-regulating hormones including parathyoid hormone(PTH), calcitonin(CT) and cholecalciferol(Vit D). After feeding experimental diets for five weeks, mice were sacrificed by cervical dislocation and the enzyme was fluometrically measured at 440nm. $\beta$-Glucuronidase activity was inhibited by high calcium in the diet. in addition, vitamin D also inhibited the enzyme activity in the serum regardless of the level of dietary calcium. In contrast, PTH has shown to stimulate the enzyme at all the levels of dietary calcium. Calcitonin, and inhibitor of PTH action for bone resorption, revealed to curb PTH effect in this enzyme, whereas CT stimulated the action of vitamin D in the serum. The above results led us to conclude that osteoclastic bone resorption and senile osteoporosis may be reduced by adequate dietary calcium and vitamin D.

• 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.

• 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.