• International Journal of Industrial Entomology and Biomaterials
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• 제15권2호
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• pp.161-164
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• 2007

While searching for ${\alpha}$-glucosidase inhibitors, the active compound was found in a methanol extract of Burthus martensi Kirsch. The separation of the active compound was performed using various chromatography methods and the physico-chemical properties of the purified compound were characterized. The compound showed very potent inhibitory activity against ${\alpha}-glucosidase$ with an $IC_{50}$ value of $5.3\;{\mu}g/ml$. Lineweaver-Burk plot indicated that its inhibition of ${\alpha}-glucosidase$ was competitive.

• 대한화장품학회지
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• 제27권1호
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• pp.99-109
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• 2001

Novel glucoconjugates phenolic moiety, 3-(methoxycarbonyl)-4-(hydroxyphenyl)-$\beta$-D-glucopyranoside(4), 3-(methoxyacetyl)-4-(hydroxyphenyl)-$\beta$-D-glucopyranoside(7), 4-(hydroxyphenyl)-$\beta$-D-ribofuranoside(11), were synthesized. In order to investigate their depigmentation effect, inhibitory activity against mushroom tyrosinase and inhibitory activity of melanin synthesis in B16 melanoma cell were evaluated in vitro. Compound 11 showed 92.0$\mu\textrm{g}$/㎖ of tyrosinase inhibitory activity whereas compound 4 and 7 showed very low activity not less than 300$\mu\textrm{g}$/㎖. Inhibitory activities of melanin synthesis in B16 melanoma cell of compound 4, 7, and 11 were 8.7, 15.1, and 36.0%, respectively, at the concentration of 100$\mu\textrm{g}$/㎖. Inhibitory activity of compound 11 was much higher than that of arbutin at the same concentration.

• 한국식품과학회지
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• 제34권3호
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• pp.493-497
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• 2002

한국산 인삼 5년근을 60% acetone으로 추출하여 Sepadex LH-20 gel column chromatography, MCI-CHP 20 gel column chromatography, Bondapak $C_{18}$, column chromatography을 이용하여 TLC와 HPLC로 순도를 검증한 후 3 종의 polyphenol 화합물을 분리하였다. Compound I과 II는 Sepadex LH-20 gel column chromatography에서 증류수상에서 용출되었고 compound Ⅲ는 40% methanol 상에서 용출됨을 보아 compound II와 compound III는 흡착성이 강한 polyphenol 화합물이라 추정되었다. 혈압강하에 관여하는 효소인 angiotensin converting enzyme(ACE)의 저해효과는 compound II가 157 ppm에서 31.86%로 3 가지 분획물 중 가장 우수하였으며 compound I과 III는 높은 활성을 보이지 않았다. 통풍예방에 관여하는 xanthine oxidase 저해효과는 compound I, II에서 666 ppm에서 100%저해효과를 나타내었으나 compound III는 저해효과가 낮았다. Melanin을 형성하는 tyrosinase 저해효과를 실함한 결과 compound III는 400 ppm에서 28.6%의 저해효과를 나타내었고 Compound I과 II의 저해효과는 낮았다.

• 약학회지
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• 제43권1호
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• pp.28-32
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• 1999

Four derivatives of kojic acid were synthesized and their inhibitory activities against tyrosinase were evaluated. The C-2 hydroxymethyl and C-7 hydroxyl of kojic acid were replaced by carboxylate and amine, respectively. These derivatives were coupled to L-phenylalanine, producing two amide compounds. The carboxylate derivative (3), its amide compound (5), and the amine derivative (7) were weak inhibitors. The amide compound (9) where amine derivative (7) coupled to L-phenylalanine showed strong inhibitory activity ($IC_{50}=24.6{\;}{\mu}M$) comparable to kojic acid.

• Natural Product Sciences
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• 제10권6호
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• pp.315-320
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• 2004

Alpha-viniferin was previously isolated as a cyclooxygenase (COX)-2 inhibitor from Carex humilis (Cyperaceae) and is an oligomeric stilbene compound with benzofuran (BF) moieties in its chemical structure. In the present study, a chemically synthetic BF compound, named as 3,3-dimethyl-2,3,4,6,7,8,9,10,11,12,13,14,15,16,17,18-hexadecahydro-1H-benzo[b] cyclopentadeca[d]furan-1-one, was discovered to inhibit bacterial lipo polysaccharide (LPS)-induced prostaglandin $E_2$ $(PGE_2)$ production in macrophages RAW 264.7. The BF compound exhibited a selectively preferred inhibitory effect on COX-2 activity over COX-1 activity. Furthermore, BF compound inhibited LPS-induced COX-2 expression at transcription level. As a down-regulatory mechanism of COX-2 expression shown by BF compound, suppression of nuclear factor $(NF)-{\kappa}B$ activation has been demonstrated. BF compound inhibited LPS-induced $NF-{\kappa}B$ transcriptional activity and nuclear translocation of $NF-{\kappa}B$ p65, in parallel, but did not affect LPS-induced degradation of inhibitory ${\kappa}B{\alpha}$ protein $(I{\kappa}B{\alpha})$. Taken together, anti-inflammatory effect of BF compound on $PGE_2$ production was ascribed by its down-regulatory action on LPS-induced COX-2 synthesis in addition to inhibitory action on enzyme activity of COX-2.

• Biomolecules & Therapeutics
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• 제6권4호
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• pp.364-370
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• 1998

Glycosidase inhibitors from urine of Bombyx mori were isolated and their inhibitory activities on glycosidases were evaluated. Six compounds were isolated by using several ion exchange columns, and their chemical structures were identified by the physicochemical and spectral data. Compound IV, V and Ⅵ were identified as 1-deoxynojirimycin, fagomine and 1,4-dideoxy-1,4-imino-D-arabinitol, respectively. Among six compounds isolated,1-deoxynojirimycin(IV) was the most potent inhibitor on $\alpha$-glucosidase and $\beta$-galactosidase of rat intestine, and its inhibitory activities for trehalase and almond $\beta$-glucosidase were relatively weak. Compound V and Ⅵl retained a little inhibitory potency toward $\alpha$-glucosidase and $\beta$-galactosidase. Compound II and III, however, have been found to have no effect on all glycosidases tested in this study.

• 대한수의학회지
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• 제5권1호
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• pp.43-57
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• 1965

It has been-reported that rabbit serum exhibit an inhibitory action on avian infectious bronchitis virus in embryonating chicken embryo. In this thesis, the biological, serological, physical and chemical properties of normal rabbit serum on the effect of the virus propagation were studied. Throughout the studies, the following experimental results 'were obtained and summarized here. 1. An inhibitory action of rabbit serum on avian infectious bronchitis vrius is due to the normal serum constituents. 2. The nature of the neutralization between normal rabbit serum and the virus is similar to that of the specific antiserum and the virus. 3. Rabbit serum, heat inactivated at $56^{\circ}C$, for 30 minutes, showed its average $log_{10}El,D_{50}Nl$ of 3.7. 4. The inhibitory compound present in the normal rabbit serum is inactivated by means of 5 per cent trypsin, 0.01 M potassium periodate, and absorbed to zymosan. 5. The inhibitory compound was not affected by 0.05 M trichloroacetic acid and 0.005M $KH_2PO_4$. 6. The higher the temperature of heat inactivation of rabbit serum caused the lesser the neutralizing effect on the virus. Heating the serum at $66^{\circ}C$, for 30 minutes brought about a complete loss of the neutralizing index of the serum. 7. No ions, as a cofactor, was incorporated to the inhibitory action of rabbit serum on the virus. 8. The inhibitory compound amays be found in a fraction of serum globulin.

• Journal of Microbiology and Biotechnology
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• 제31권7호
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• pp.1022-1027
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• 2021

Three compounds were isolated from marine-derived Streptomyces sp. CNQ-031, and their inhibitory activities against monoamine oxidases (MAOs), acetylcholinesterase (AChE), butyrylcholinesterase (BChE), and β-secretase (BACE-1) were evaluated. Compound 1 (5,7-dihydroxy-2-isopropyl-4H-chromen-4-one) was a potent and selective inhibitor of MAO-A, with a 50% inhibitory concentration (IC₅₀) of 2.70 µM and a selectivity index (SI) of 10.0 versus MAO-B. Compound 2 [5,7-dihydroxy-2-(1-methylpropyl)-4H-chromen-4-one] was a potent and low-selective inhibitor of MAO-B, with an IC₅₀ of 3.42 µM and an SI value of 2.02 versus MAO-A. Compound 3 (1-methoxyphenazine) did not inhibit MAO-A or MAO-B. All three compounds showed little inhibitory activity against AChE, BChE, and BACE-1. The K_i value of compound 1 for MAO-A was 0.94 ± 0.28 µM, and the K_i values of compound 2 for MAO-A and MAO-B were 3.57 ± 0.60 and 1.89 ± 0.014 µM, respectively, with competitive inhibition. The 1-methylpropyl group in compound 2 increased the MAO-B inhibitory activity compared with the isopropyl group in compound 1. Inhibition of MAO-A and MAO-B by compounds 1 and 2 was recovered by dialysis experiments. These results suggest that compounds 1 and 2 are reversible, competitive inhibitors of MAOs and can be considered potential therapies for neurological disorders such as depression and Alzheimer's disease.

• 대한화장품학회지
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• 제24권3호
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• pp.45-50
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• 1998

13 develop an active agent for skin whitening, we examined the inhibitory effects of 285 plant extracts on tyrosinase activity and found some plant extracts have an ability to inhibit tyrosinase activity. Of these plant extracts, ramulus mori extracts showed the highest inhibiting activity on enzyme activity. From these results, we selected ramulus mori as a new active agent for skin whitening. $IC_{50}$/ of this extracts on tyrosinase activity is 12.48$\mu\textrm{g}$/m1. Also, ramulus mori extracts showed inhibitory activity on melanin synthesis in B-16 melanoma cells. We isolated active compound from ramulus mori extracts using various column chromatography and recrystalization and identified its chemical structure using Mass spectroscopy, IR and NMR analysis. So, it is identified as Mulberrin, a maior compound of ramutus mori and turned out that it has potent ability on tyrosinase inhibition. $IC_{50}$/ of this compound for tyrosinase activity is 0.5$\mu\textrm{g}$/ml. Also, this compound showed potent inhibitory activity on melanin synthesis in B-16 melanoma cells. This extracts was turned out to be safe in many safety tests.

• International Journal of Industrial Entomology and Biomaterials
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• 제16권2호
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• pp.57-59
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• 2008

While searching for pancreatic lipase inhibitors, the active compound was found in a methanol extract of Apis mellifera venome. The active compound was isolated by Diaion HP-20 column chromatography, thin layer chromatography and HPLC. The active compound is stable to the extreme pH and heat. There is no loss of activity both in acidic and alkaline solution in the pH range of 2 to 11 by heating for 15 minutes at $90^{\circ}C$. The rf value of the compound was 0.51 at TLC with butanol : methanol: water (4:1:2) solvent system. The molecular weight of the compound was determined to be 293 by EI-MS.