• 제목/요약/키워드: inhibitory effects

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Inhibitory Effects of Quinoline Isolated from Ruta chalepensis and Its Structurally Related Derivatives against α-Amylase or α-Glucosidase

  • Park, Jun-Hwan;Lee, Hoi-Seon
    • Journal of Applied Biological Chemistry
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    • 제58권1호
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    • pp.5-8
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    • 2015
  • This study was to isolate an active component of the chloroform fraction from the methanol extract of Ruta chalepensis leaves and to measure inhibitory effects against ${\alpha}$-glucosidase or ${\alpha}$-amylase. The inhibitory compound of R. chalepensis leaves was isolated using chromatographic methods and identified as quinoline. Quinoline and its structurally related derivatives were tested for their inhibitory activities by evaluating the $IC_{50}$ values against ${\alpha}$-amylase or ${\alpha}$-glucosidase and were compared with that of acarbose. Based on the $IC_{50}$ values, quinazoline exhibited the greatest inhibitory activity ($20.5{\mu}g/mL$), followed by acarbose ($66.5{\mu}g/mL$), and quinoline ($80.3{\mu}g/mL$) against ${\alpha}$-glucosidase. In case of ${\alpha}$-amylase, quinazoline had potent inhibitory activity, followed by quinoline ($179.5{\mu}g/mL$) and acarbose ($180.6{\mu}g/mL$). These results indicate that R. chalepensis extract, quinoline, and quinazoline could be useful for inhibiting ${\alpha}$-glucosidase or ${\alpha}$-amylase.

전도산(顚倒散)의 추출용매에 따른 항염 및 항산화 비교 연구 (The Comparative Study of Anti-inflammation and Anti-oxidation in Accodance with Extraction Solvents of Jeondo-san)

  • 서형식
    • 한방안이비인후피부과학회지
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    • 제23권2호
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    • pp.69-80
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    • 2010
  • Objective : The purpose of this study was to compare anti-Inflammation and anti-oxidation of Jeondo-San(JDS) extracted with two kinds of solvents, ethanol and water. Methods : Two kinds of JDS extractions were prepared 20, 50, $100\;{\mu}g/mg$. The Cytotoxicity was measured by MTT assay in Raw 264.7 cell. The anti-inflammation effects were measured by inhibitory efficacy on $PGE_2$, NO, TNF-$\alpha$, COX-2 and iNOS in Raw 264.7 cell. The anti-oxidation effects were measured by ROS inhibitory efficacy, intracellular GSH synthesis and DPPH Radical scavenging in HaCaT cell. Results : 1. All of JDS extraction groups had no cytotoxicity in Raw 264.7 cell. 2. All of JDS extraction groups showed significantly inhibitory effect on production of $PGE_2$. Inhibitory efficacy increased in accodance with concentration. 3. All of JDS extraction groups showed significantly inhibitory effect on production of NO. Inhibitory efficacy increased in accodance with concentration. 4. All of JDS extraction groups did not show significantly inhibitory effect on production of TNF-$\alpha$. 5. $100\;{\mu}g/ml$ JDS extracted with ethanol and $50\;{\mu}g/ml$, $100\;{\mu}g/ml$ JDS extracted with water showed inhibitory effect on iNOS expression. 6. All of JDS extraction groups showed significantly inhibitory effect on production of ROS. Inhibitory efficacy increased in accodance with concentration. Ethanol extractions were better than water extractions. 7. $100\;{\mu}g/ml$ JDS extracted with ethanol only produced GSH of $32{\pm}5.2%$. 8. All of JDS extraction groups showed significantly scavenging effect of DPPH radicals. Inhibitory efficacy increased in accodance with concentration. Ethanol extractions were better than water extractions. Conclusion : Two kinds of JDS extractions have not cytotoxicity and inhibit production of NO. JDS extracted with water was effective in anti-inflammation, JDS extracted with ethanol was effective in anti-oxidation.

β-Glucuronidase 저해 활성이 우수한 결명자를 첨가한 상황 균사체 배양액의 생리활성 (Biological Activities of Phellinus linteus Mycelium Culture with Cassiae Semen Extract on β-Glucuronidase Inhibitory Activity)

  • 오은희;박정미;김상희;송인규;한남수;윤향식
    • 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.

Inhibitory Effects of Curcuminoids on $17{\beta}$-hydroxysteroid Dehydrogenase Type 1 Activity in Animal Livers

  • Lee, Sung-Eun;Park, Byeoung-Soo;Kim, Hye Jin;Lee, Eun-Woo;Yum, Jong Hwa
    • 대한의생명과학회지
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    • 제19권2호
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    • pp.147-152
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    • 2013
  • 17-${\beta}$-hydroxysteroid dehydrogenase type 1 ($17{\beta}$-HSD type 1) mediates the reaction of $17{\beta}$-estradiol (E2) production from estrone (E1). Inhibitory effects of curcuminoids on $17{\beta}$-HSD type 1 activity were investigated to find a lead compound for treating estrogen-dependent diseases including breast cancer. Among curcuminoids, demethoxycurcumin showed potent inhibitory effect ($IC_{50}=2.7{\mu}M$) on mouse $17{\beta}$-HSD type 1. Curcuminoids also displayed their inhibitory effects on the production of $17{\alpha}$-estradiol which is a carcinogenic metabolite produced by the enzyme. Bisdemethoxycurcumin ($IC_{50}=1.3{\mu}M$) showed potent inhibitory effect on the $17{\alpha}$-estradiol production by chicken $17{\beta}$-HSD type 1. Curcuminoids did not inhibit ERE transcriptional activity with and without E2. Taken together, curcuminoids can be used for treating and preventing E2-dependent diseases via inhibition on $17{\beta}$-HSD type 1 activity.

Antibacterial Activity of Water Soluble Components of Elfvingia applanata Alone and in Combinations with Quinolones

  • Kim, Young-So;Eo, Seong-Kug;Oh, Ki-Wan;Lee, Chong-Kil;Lee, Young-Nam;Han, Seong-Sun
    • Mycobiology
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    • 제29권1호
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    • pp.11-14
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    • 2001
  • A preparation of water soluble components(EA) was made from carpophores of Elfvingia applanata(Pers.) Karst and its in vitro antibacterial activity on a number of bacterial species was examined by macrobroth dilution assay. Among 16 species of bacteria tested, the most potent antibacterial activity was observed against Staphylococcus epiderrnidis and Proteus vulgaris, of which MICs were 1.25 mg/ml. To investigate the antibacterial effects in combinations of EA with quinolone antibiotics, such as ciprofloxacin, enoxacin, lomefloxacin, norfloxacin, and ofloxacin, the fractional inhibitory concentrations(FICs) and the fractional inhibitory concentration indices(FICIs) for four bacterial strains were determined by macrobroth dilution checkerboard assay. Combinations of EA and quinolones exhibited either additive or indifferent effects of antibacterial activity in most instances. However, both synergistic and antagonistic effects were not observed in any cases.

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새삼, 실새삼 및 갯실새삼 추출물이 Clone M-3 세포주의 Melanin 생합성 및 Tyrosinase 활성에 미치는 영향과 세포독성 및 항산화효과 (Inhibitory Effects on Melanin Biosynthesis and Tyrosinase Activity; Cytotoxicity in Clone M-3 and Antioxidant Activity by Cuscuta japonica, C. australis, and C, chinensis Extracts)

  • 장수진;석귀덕
    • 약학회지
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    • 제50권6호
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    • pp.421-428
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    • 2006
  • Water extracts, ethanol extracts, and juice of Cusuta japonica, C, australis, and C. chinensis were prepared, and their cytotoxicity, antioxidant activity and inhibitory effects on tyrosinase activitiy and melanin biosynthesis were estimated by using melanoma Clone M-3. From this study; the following conclusions were attained. Extracts of Cuscuta japonica, C. australis, and C. chinensis showed noticeable cytotoxicity except ethanol extracts from the stem of C. australis. A maximual cytotoxicity was observed with tile ethanol extract from the seed of C, australis (87.39%). While the ethanol extract from the seed of C. japonica (91.88%) showed the most pronounced inhibitory effect on melanin biosynthesis, the water extract from the stem of C. japonica (1.05%) possessed very little inhibitory effect. The most inhibitory effect on tyrosinase activity was observed with the water extract from the stem of C. australis (76.67%). Howeverr the water extract from the stem of C. japonica showed a very poor effect on the inhibition of tyrosinase activity All the preparations, except extracts from the seed of C. australis were able to remove reactive oxygen species (ROS) in a dose-dependent manner. The juice of C. japonica demonstrated the strongest activity (59.02%).

Agarwood Inhibits Histamine Release from Rat Mast Cells and Reduces Scratching Behavior in Mice -Effect of Agarwood on Histamine Release and Scratching Behavior-

  • Inoue, Eiji;Shimizu, Yasuharu;Masui, Ryo;Tsubonoya, Tomoe;Hayakawa, Tomomi;Sudoh, Keiichi
    • 대한약침학회지
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    • 제19권3호
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    • pp.239-245
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    • 2016
  • Objectives: This study was conducted to clarify the effects of agarwood on histamine release from mast cells in rats and on the scratching behaviors in mice. Methods: Histamine release from rat mast cells induced by compound 48/80 or concanavalin A (Con A) and compound 48/80-induced scratching behavior in mice were examined to investigate the effects of agarwood. The hyaluronidase activity and the 3',5'-cyclic adenosine monophosphate (cAMP) levels in mast cells were examined to investigate the mechanisms for the inhibition of histamine release. The correlation between the inhibitory effects of agarwood on histamine release and the content of its typical ingredients, a 2-(2-phenylethyl)chromone derivatives, was analyzed using thin-layer chromatography. Results: Agarwood showed an inhibitory effect on mast-cell histamine release induced by compound 48/80 or Con A without any effect on hyaluronidase activity; this effect involves an increase in the cAMP levels in mast cells. Oral administration of agarwood showed an inhibitory effect on compound 48/80-induced scratching behavior in mice. The inhibitory effects of agarwood on histamine release were quite different, depending on the area where the agarwood was produced, its quality, and its market price. No correlation was found between the inhibitory effects of agarwood on histamine release and the typical ingredients of agarwood, which are 2-(2-phenylethyl)chromone derivatives. Conclusion: These results show that agarwood inhibits histamine release from mast cells partially through an increase in the cAMP levels in cells. We suggest that some active ingredients of agarwood must be effective on oral intake and that agarwood can be used to treat patients with a number of conditions, including urticaria, atopic dermatitis, and bronchial asthma, in which an increase in histamine release occurs. Differences in the pharmacological effects of this crude drug among markets may provide important information for the quality control of this herbal medicine.

인진사령산이 흰쥐 간손상(肝損傷)에 미치는 영향(影響) (Effects of Injinsaryung-san on Experimental Liver Damage in Rats)

  • 표임정;이장훈;우홍정;김병운
    • 대한한의학회지
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    • 제16권2호
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    • pp.281-298
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    • 1995
  • The following results were made by observation GOT, GPT, ALP, total cholesterol and higlyceride in serum to research the effects of medicines which are Injinsaryungsan(Sample- A) and another medicine(Sample-B) of which Injin(Artemisiae Capillaris Herba)was increased in quantity on liver damaged by $CCl_4$ and d-galactosamine in rats. 1. The high concentrated extracts of Sample A group and Sample- B group showed significant inhibltory effects on the increase of serum GPT, ALP, LDH, total cholesterol and triglyceride levels induced by $CCl_4$ and d-galactosamine. 2. The high concentrated extracts of sample A group and Sample B group showed more significant inhibitory effects(P〈0.001) than the low ones' effects(P〈0.01) on the increase of serum triglyceride level induced by $CCl_4$ 3. Sample-A group showed significant inhibitory effects on the increase of serum GOT, GPT. ALP, total cholesterol and triglyceride levels, but no significance on the increase of serum LDH level induced by d-galactosamine. 4. Sample-B group showed very significant inhibitory effects on the increase of serum GOP, GPT, ALP, LDH, total cholesterol and triglyceride levels induced by d-galactosamine. 5. As compared with Sample-A group, Sample-B group of which Injin was increased in quantity showed more significant inhibitory effects on all items of this experiment induced by $CCl_4$ and d-galactosamine. As mentioned above. it seemed that both Injinsaryungsan and another medicine of which Injin was increased in quantity had effects protecting liver and anti-fatty liver induced by $CCl_4$ and d-galactosamine in rats. Specially Sample-B group had very significant effects on liver damage as compared with Sample-B group. Therefore it seems that more researches on variation according to the increase of Injin dose must be continued for curing liver diseases.

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알로에(蘆회), 녹차(綠茶), 꿀(蜂蜜)의 미백효과에 관한 연구 (The Study on Depigmentation Effects of Aloe, Camellia sinensis and Mel)

  • 한은정;이길영;김혜정;김윤범
    • 한방안이비인후피부과학회지
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    • 제16권3호
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    • pp.145-163
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    • 2003
  • Objectives : This study was performed to investigate the depigmentation effects of Aloe, Camellia sinensis and Mel. Methods : Inhibition of tyrosinase activity, melanin production & melanoma cell viability in cultured B16 melanoma cells, UV screen and cytoprotective effects on PC12 cells injured by hydrogen peroxide were measured. Results : Aloe has some inhibitory effects on tyrosinase activity, on the other hand Camellia sinensis and Mel do not have. They did not show any inhibitory effects on melanin production in melanoma cells and cytoprotective effects on PC12 cells injured by hydrogen peroxide. Aloe and Camellia sinensis have some inhibitory effects on UV screen. Conclusions : This study shows that Aloe and Camellia sinensis which were generally used for external application have some depigmentation effects. Following this, We should use them for whitening agents and the depigmentation effects of the other natural subjects which were generally used for external application should be examined.

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Effects of cholane compounds on the development of morphine tolerance

  • Kim, Hack-Seang;Lee, Young-Eun;Oh, Ki-Wan;Lee, Myung-Koo
    • Archives of Pharmacal Research
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    • 제13권1호
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    • pp.38-42
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    • 1990
  • The present study was undertaken to determine the inhibitory effects of cholane compounds, unsodeoxycholic acid (UDCA) and chenodeoxycholic acid (CDCA) on the development of morphine-induced tolerance and physical dependence, and also to determine the hepatic glutathione contents. UDCA and CDCA inhibited the development of morphine-induced tolerance and physical dependence significantly. UDCA inhibited the hepatic glutathione decrease induced by morphine multiple injections, while this effect was not observed in CDCA treated mice. It was throught that the inhibitory effects of hepatic glutathione decrease in morphine-treated mice by UDCA and CDCA showed a tendency of inhibitory effects of development of morphine tolerance and dependence.

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