• Title/Summary/Keyword: inhibitory

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Relationship Between Tyrosinase Inhibitory Action and Oxidation-Reduction Potential of Cosmetic Whitening Ingredients and Phenol Derivatives

  • Sakuma, Katsuya;Ogawa, Masayuki;Sugibayashi, Kenji;Yamada, Koh-ichi;Yamamoto, Katsumi
    • Archives of Pharmacal Research
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    • v.22 no.4
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    • pp.335-339
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    • 1999
  • The oxidation-reduction potentials of cosmetic raw materials, showing tyrosinase inhibitory action, and phenolic compounds structurally similar to L-tyrosine were determined by cylcic voltammetry. The voltammograms obtained could be classified ito 4 patterns (patterns 1-4). Patterns 1, characterized by oxidation and reduction peaks as a pair, was observed with catechol, hydroquinone or phenol, and pattern 2 exhibiting another oxidation peak in addition to oxidation and reduction peaks as a pair was found with arbutin, kojic acid, resorcinol, methyl p-hydroxybenzoate and L-tyrosine as the substrate of tyrosinase. Pattern 3 with an independent oxidation peak only was expressed by L-ascorbic acid, and pattern 4 with a reduction peak only at high potentials, by hinokitiol. The tyrosinase inhibitory activity of these compounds was also evaluated using the 50% inhibitory concentration ($IC_{50}$) and the inhibition constant (Ki) as parameters. Hinokitiol, classified as patterns 4, showed the highest inhibitory activity (lowest $IC_{50}$ and Ki). Hydroquinone showing the second highest activity belonged to pattern 1, which also included compounds exhibiting pattern 2 was relatively low with Ki values being in the order of 10-4 M. Although there was no consistent relationship between oxidation-reduction potentials and tyrosinase inhibitory action, the voltammetry data can be used as an additional index to establish the relationship between the structure and the tyrosine inhibitory activity.

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Isolation and identification of angiotensin I-converting enzyme inhibitory peptides derived from thermolysin-injected beef M. longissimus

  • Choe, Juhui;Seol, Kuk-Hwan;Kim, Hyun-Jin;Hwang, Jin-Taek;Lee, Mooha;Jo, Cheorun
    • Asian-Australasian Journal of Animal Sciences
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    • v.32 no.3
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    • pp.430-436
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    • 2019
  • Objective: This study identified angiotensin I-converting enzyme (ACE) inhibitory peptides in beef M. longissimus injected with thermolysin (80 ppm) and stored for 3 days at $5^{\circ}C$. Methods: Crude peptides (molecular weight <3 kDa) were obtained from the thermolysin hydrolysate and separated into seven fractions. Fraction V showing the highest ACE inhibitory activity was further fractionated, yielding subfractions V-15, V-m1, and V-m2, and selected for superior ACE inhibitory activity. Finally, twelve peptides were identified from the three peak fractions and the ACE inhibitory activity ($IC_{50}$) of each peptide was evaluated. Results: The Leu-Ser-Trp, Phe-Gly-Tyr, and Tyr-Arg-Gln peptides exhibited the strongest ACE inhibitory activity ($IC_{50}$ values of 0.89, 2.69, and 3.09 mM, respectively) and had higher concentrations (6.63, 10.60, and 29.91 pg/g; p<0.05) relative to the other peptides tested. Conclusion: These results suggest that the thermolysin injection process is beneficial to the generation of bioactive peptides with strong ACE inhibitory activity.

Angiotensin I Converting Enzyme Inhibitory Activity of Krill (Euphausia superba) Hydrolysate

  • Kim Dong-Soo;Park Douck-Choun;Do Jeong-Ryong
    • Fisheries and Aquatic Sciences
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    • v.5 no.1
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    • pp.21-27
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    • 2002
  • Angiotensin I converting enzyme inhibitory activities of shelled krill (Euphausia superba) hydrolysates by autolysis and by hydrolysis with commercial proteases were analyzed. Among the proteases, Alcalase was the most effective protease for the hydrolysis of krill considering the degree of hydrolysis $(87.5\%)$ and the ACE inhibitory activity $(60\%)$. Four hour hydrolysis suggested as the most suitable and economic. In order to establish the optimum hydrolysis condition of krill, degree of hydrolysis and ACE inhibitory activity as affected by Alcalase concentration and water amount added were statistically analyzed by response surface methodology (RSM). The optimum hydrolysis condition was $2.0\%$ Alcalase hydrolysis in 2 volumes (v/w) of water at $55\% for 4 hr. The hydrolysate prepared from the optimum hydrolysis condition was fractionated by molecular weight. The lower molecular weight fraction showed the higher ACE inhibitory activity. $IC_{50}$ of the fraction under 500 Da was 0.57mg protein/mL.

Antimutagenic Effects of the Juice and Boiling Water Extract of houttuynia cordata Thunb (어성초즙 및 추출물의 항돌연변이 효과)

  • 최영현;김은영;박건영;이숙희;이원호
    • Journal of the Korean Society of Food Science and Nutrition
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    • v.23 no.6
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    • pp.916-921
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    • 1994
  • The inhibitory effects of the juice and boiling water extract of Houttuyina cordata Thunb., which has been known as a traditional folk antitumor agent, on the genotxicity induced by mutagens were investigated . For this purpose, Salmonella typhimurium TA98 and TA100, and the transheterozygous (mwh/+) third larvae of Drosophila melanogaster were used. The juice of fresh H. cordata 9JHC) and boiling H. cordata extract (BHC) showed antimutagenicities toared alfatoxin B₁ in S. typhimurium TA 98 and TA100. The JHC's inhibitory effect increased by 76% to 98% as the adding concentrations increased, and the BHC had a 86-97% inhibitory effect. however, in the case of N-methyl-N'-nitro-N nitrosoguanidine (MNNG), the JHC's inhibitory effect was 52-60% irrespectively of its concentrations and the BHC had a low inhibitory effect. The JHC and BHC slightly reduced the somatic chromosomal mutagenicity by MNNG in the wing hair spot test system (mwh/+) of D. melanogaster, which suggests that they can inhibit gene mutation , deletion and mitotic chromosomal recomgination.

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Purification of Rotavirus Infection-Inhibitory Protein from Bifidobacterium breve K-110

  • Bae, Eun-Ah;Han, Myung-Joo;Song, Mi-Jeong;Kim, Dong-Hyun
    • Journal of Microbiology and Biotechnology
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    • v.12 no.4
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    • pp.553-556
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    • 2002
  • The inhibitory activity of fifty Bifidobacteria toward the infectivity of a rotavirus, which is the predominant cause of sporadic diarrhea in infants and young children, was investigated, and Bifidobacterium breve K-110 was found to have the most potent inhibitory activity. Accordingly, the rotavirus infection-inhibitory protein was purified, and its molecular weight was determined to be 76 kDa by SDS-PAGE. It was heat-labile and its 50% inhibitory concentration ($IC_{50}$) was 0.045 $\mu g/ml$.

Inhibitory Effect of a Drug Metabolizing Enzyme CYP3A4 on Spices (향신료의 약물대사효소 CYP3A4 저해효과)

  • Cha, Bae-Cheon
    • Korean Journal of Pharmacognosy
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    • v.34 no.1 s.132
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    • pp.86-90
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    • 2003
  • For the determination of inhibiting cytochrome P450(CYP)3A4 activity, an improvement HPLC method was established by using a new internal standard and solvent system. Moreover, CYP3A4 amount for a optimum reaction of enzyme was determined by a comparative study with a variety concentration of enzyme. Using a established method, inhibitory effect of CYP3A4 that is drug metabolizing enzyme Investigated on EtOAc extracts of 5-class spices. As a result of experiment, EtOAc extract of white pepper (Piper nigrum L.) showed strong inhibitory activity. On a continuous experiment, the fraction 2, 4 and 5 of while pepper extract showed remarkable inhibitory activity. Pipeline, a main constituent of pepper was not included in these fraction. It is suggested that major compounds for the inhibitory activity of white pepper may be other ingredient that is not piperine.

The Inhibitory Activity on Monoamine Oxidase of the Fruit of Morus alba (상심자의 모노아민산화효소 저해활성)

  • Hwang, keum-Hee;Song, Im
    • Korean Journal of Pharmacognosy
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    • v.34 no.2 s.133
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    • pp.185-189
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    • 2003
  • We examined the inhibitory activities against monoamine oxidase (MAO) of Morus alba in vitro and in vivo methods. Methanolic extract of M. alba showed significantly inhibitory activities on MAO-A and MAO-B that were prepared from rat brain and liver in vitro. The inhibitory activities were measured by serotonin and benzylamine as substrates, respectively. MAO-A and MAO-B activities were potently inhibited by ethylacetate extracts of M. alba in vitro tests. Those activities in vivo tests have different tendency each other. MAO-A activity was increased by the oral administration of methanolic extract of M. Alba, while, MAO-B activity was decreased. Consequently, we can suggest that M. alba may have the effects on the inhibitory activities against MAO both in vitro and in vivo.

Suppression Effect of Curcuma longa Rhizome-Derived Components against Nitric Oxide Synthase

  • Lee, Hoi-Seon
    • Journal of Applied Biological Chemistry
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    • v.52 no.4
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    • pp.212-215
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    • 2009
  • The inhibitory effects of Curcuma longa rhizome-derived materials against nitric oxide (NO) production were assessed. The inhibitory effect (57%) on NO production was evidenced by the methanol extract of C. longa at $1\;{\mu}g/mL$. In the fractionation of the methanol extract, the ethyl acetate fraction evidenced an inhibitory effect greater than 62.1% at $1\;{\mu}g/mL$. The active constituent was identified as curcumin. Curcumin exerted potent inhibitory effects of 78.7 and 65.7% at concentrations of 1 and $0.5\;{\mu}g/mL$, respectively. Furthermore, the inhibitory effect of ar-turmerone was measured as 31.3 and 15.8% at 1 and $0.5\;{\mu}g/mL$, respectively. The iNOS expression-suppressive effects of curcumin were assessed via western blot analysis. Our results suggest that curcumin and ar-turmerone may prove useful in the development of new types of NO inhibitors.

Screening of Korean Marine Plants Extracts for Inhibitory Activity on Protein Tyrosine Phosphatase 1B

  • Lee, Hee-Jung;Kim, You-Ah;Lee, Jung-Im;Lee, Burm-Jong;Seo, Young-Wan
    • Journal of Applied Biological Chemistry
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    • v.50 no.2
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    • pp.74-77
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    • 2007
  • Crude extracts of 69 marine organisms (27 salt marsh plants and 42 seaweeds) were screened for the inhibitory activity against the protein tyrosine phosphatase 1B (PTP1) in vitro. The most active extracts were methanol extracts from Derbesia marina (80.6% in inhibitory activity) and Symphycladia latiscula (85.6%) at the concentration of $15{\mu}g/mL$. Methanol extracts of Codium adhaerens and Hisikia fuziformis were moderately inhibitory with 71.2 and 69.1% inhibition, respectively. It was peculiar that only the extracts from seaweeds show inhibitory activity where those from salt marsh plants do not show any significant effect.

Synthesis and de-pigmentation effect of phenolic glucoconjugates

  • Kim, Ki-Ho;Kim, Ki-Soo;Lee, Jae-Soeb;Ko, Kang-Il;Lee, Soo-Hee
    • Journal of the Society of Cosmetic Scientists of Korea
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    • v.27 no.1
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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.

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