• Title/Summary/Keyword: inhibitory compound

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Antioxidant and Tyrosinase Inhibitory Activity of Extract Rumex japonicus HOUTT Root and Its Fractions (양제근 추출물 및 분획의 항산화 활성과 Tyrosinase 저해 활성)

  • Yang, Sun A;Seo, Go Eun;Pyo, Byoung Sik;Kim, Sun Min;Choi, Cheol Hee
    • Korean Journal of Medicinal Crop Science
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    • v.25 no.1
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    • pp.10-15
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    • 2017
  • Background: We investigated the antioxidative and tyrosinase inhibitory activities of 70% ethanol extract, and its fractions, of the root of Rumex japonicus HOUTT. Methods and Results: The total phenolic compound contents of the 70% ethanol extract and ethyl acetate fraction were 168.99 mg/g and 651.78 mg/g, respectively. The antioxidant activity was compared through the DPPH radical and nitric oxide (NO) scavenging assays. The ethyl acetate fraction showed the highest DPPH radical and NO scavenging abilities, which confirmed the antioxidant activity. Specifically, the ethyl acetate fraction showed a higher DPPH radical scavenging ability than ascorbic acid. These results were related to the total phenolic compound content of the ethyl acetate fraction. Moreover, in the tyrosinase inhibition assay, the ethyl acetate fraction exhibited stronger inhibitory activity than arbutin, which was used as the positive control. The cell viability of L929 cells was analyzed by MTT assay after treatment with 70% ethanol extract and all fractions; no changes in viability were observed, which demonstrated the nontoxic nature of the extract and fractions. Conclusions: These results suggested that the extract from the root of R. japonicus and its ethyl acetate fraction could be a novel resource for the development of a cosmetic with antioxidant and tyrosinase inhibitory activity.

Inhibitory Effects of Ginseng Extracts on Histamine-release from Rat's Mast Cell (인삼추출물의 랫트 비만세포 히스타민 유리 억제 효과)

  • Park, Kwang-Hyun;Kim, Young-Seon;Jeong, Jae-Hun
    • Korean Journal of Plant Resources
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    • v.24 no.1
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    • pp.98-104
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    • 2011
  • We investigated inhibitory effects of ginseng extracts against compound 48/80-induced responses in rat peritoneal mast cells. Initially, we optimized extraction condition with various temperature and time for recovery of high saponin contents in extracts. Using a primary rat peritoneal mast cells, we examined whether ginseng extracts inhibit compound 48/80-induced histamine release form rat mast cells. High red ginseng-spercific saponin containing extracts were recovered at $85^{\circ}C$ for 48 hr, and had no cytotoxicity with relatively high dose of extracts on rat peritoneal mast cells(<0.5 mg/ml). For examine of ameliorate effects of mast cells responses by ginseng extract, we pre-treated the extracts or saline to mast cells and treated compound 48/80. In results, compound 48/80 treatment was increased histamine release (approximately 30%) from mast cells than normal group, whereas ginseng treatment was completely inhibited histamine release. These results suggested that ginseng extracts inhibits the compound 48/80-induced mast cell activation, and ginseng extracts is a candidate for effective therapeutic tools of allergic diseases.

Phenolic and Furan Type Compounds Isolated from Gastrodia elata and their Anti-Platelet Effects

  • Pyo Mi Kyung;Jin Jing Ling;Koo Yean Kyoung;Yun-Choi Hye Sook
    • Archives of Pharmacal Research
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    • v.27 no.4
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    • pp.381-385
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    • 2004
  • Nine phenolic ($1\~9$) and two furan type (10, 11) compounds, were isolated from the methanolic extract of the tuber of Gastrodia elata Blume (Orchidaceae) in the course of continuing search for platelet anit-aggregating plant components. Compound 1 was identified as 4,4'-dihy-droxybenzyl sulfone, a novel compound for the best of our knowledge. Compound 10, 5-hydroxymethyl-2-furancarboxaldehyde, was isolated for the first time from this plant. Compound 1 ($IC_{50};\;83{\mu}M$) was about four times more inhibitory to U46619 induced aggregation than ASA ($IC_{50};\340{\mu}M$). Compound 9, 4,4'-dihydroxy-dibenzylether, ($IC_{50};\;5{\mu}M$, $3{\mu}M\;and\;33{\mu}M$, respectively) was $10\~}80$ fold more potent than ASA ($IC_{50};\;420\;{\mu}M,\;53\;{\mu}M\;and\;340\;{\mu}M$ respectively) to collagen, epinephrine and U46619 induced aggregation, although it is less active than ASA to AA induced aggregation.

Characteristics of the Purple Pigment Compound in Halophytic Plant, Suaeda japonica (내염성 식물 칠면초 (Suaeda japonica )가 갖는 자색 색소의 특징)

  • Chung, Sang-Ho
    • Proceedings of the Korea Contents Association Conference
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    • 2013.05a
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    • pp.361-362
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    • 2013
  • As one of the steps toward understanding how the plant is well adapted to strongly saline habitats, the purple pigment compound that is accumulated in Suaeda japonica was extracted and characterized. The extracted pigment compound exhibited typical characteristics of betacyanin that were represented by water solubility, pH- and temperature-dependent color changes, sensitivity to light, UV-Vis spectra, and gel electrophoretic migration pattern. LC-MS of the extracted pigment compound showed the presence of two major protonated molecular ions ($[M+H]^+$) at m/z 651.1 and m/z 827.1. According to the DPPH assay, it was found to have an antioxidant activity that is linearly increased in proportion to the reaction time for up to 30 min, and the activity was comparable to that of control BHA at 9.0 mg/ml. The cytotoxic activity against several tumor cell lines was also examined following the MTT assay. The significant growth inhibitory effect was observed on two tumor cell lines, SW-156 (human kidney carcinoma) and HEC-1B (human endometrial adenocarcinoma). Probably, the pigment compound may function as an osmolyte to uphold halotolerant physiological processes in saline environment.

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Inhibitory Effect of Allergic Reaction by Gunggwihyangso-San (궁귀향소산(芎歸香蘇散)의 항Allergy 및 항염증 효과)

  • Kwon, Ki-Won;Shin, Sang-Woo;Park, Jong-Hyun
    • Journal of Physiology & Pathology in Korean Medicine
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    • v.22 no.3
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    • pp.585-592
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    • 2008
  • The present study was conducted to investigate the anti-allergic activity of Gunggwihyangso-San(GHS). We investigated the anti-allergic effects of GHS in RBL-2H3 basophilic leukemia cells by compound 48/80, a mast cell degranulator and compound 48/80 induced anaphylactic shock in mice. Gunggwihyangso-San significantly inhibited ${\beta}$-hexosaminidase and histamine release from compound 48/80 stimulated RBL-2H3 cells. In addition, GHS effectively inhibited anaphylactic shock in mice by 50% at a dose 80 mg/mouse versus PBS treated control after the I.p injection(8 mg/kg) of compound 48/80. The in vitro anti-inflammatory activities of GHS in LPS-stimulated RAW 264.7 cells were investigated. GHS inhibited NO production in LPS-stimulated RAW 264.7 cells and effectively dowregulated the expression of iNOS mRNA and iNOS protein expression in LPS-stimulated RAW 264.7 cells. These result provide evidences that GHS may be beneficial in the treatment of allergic inflammtory disease.

Isolation and Characterization of α-Glucosidase Inhibitor Produced by Bacillus sp. SKU31-1 Strain (Bacillus sp. SKU31-1가 생산하는 α-Glucosidase 저해제 분리 및 특성 조사)

  • Kim, Shin-Duk
    • Korean Journal of Microbiology
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    • v.50 no.4
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    • pp.381-383
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    • 2014
  • In the course of screening for ${\alpha}$-glucosidase inhibitor produced by microorganism, the active compound was isolated from the culture filtrate of Bacillus sp. SKU31-1 using a series of chromatography procedures. The structure of the active compound was elucidated as 5-amino-1-hydroxymethyl-1, 2, 3, 4-cyclohexanetetrol on the basis of spectroscopic evidence obtained and comparison with data from the literature. The active compound showed potent inhibitory activity against ${\alpha}$-glucosidase with an $IC_{50}$ value of $1.9{\mu}M$ for maltose and 4.9 mM for sucrose. A Lineweaver-Burk plot indicated that its inhibition of ${\alpha}$-glucosidase was competitive, with a $K_i$ value of 0.15 mM.

Features and Functions of Purple Pigment Compound in Halophytic Plant Suaeda japonica : Antioxidant/Anticancer Activities and Osmolyte Function in Halotolerance

  • Chung, Sang Ho
    • Korean Journal of Plant Resources
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    • v.31 no.4
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    • pp.342-354
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    • 2018
  • Suaeda japonica is a halophytic plant that lives in mudflat at intertidal zone of western and southern coastal areas of Korea. The seawater-living plants showed a purple color during their whole life. In contrast, freshwater-living plants displayed a green color in leaves. When seawater-living plants were transferred to potting soil, the purple color was gradually changed to green in the leaves. The extracted purple pigment compound exhibited typical characteristics of betacyanin that were represented by water solubility, pH- and temperature-dependent color changes, sensitivity to light, UV-Vis spectra, and gel electrophoretic migration pattern. The LC-MS analysis of the extracted pigment compound showed the presence of two major protonated molecular ions ($[M+H]^+$) at m/z 651.1 and m/z 827.1. Antioxidant activity of the pigment compound was determined using stable free radical DPPH assay. It was found to have an antioxidant activity that is linearly increased in proportion to the reaction time for up to 30 min, and the activity was comparable to that of control BHA at 9.0 mg/ml. The anticancer activity against several tumor cell lines was also examined following the MTT assay. The significant growth inhibitory effect was observed on two tumor cell lines, SW-156 (human kidney carcinoma) and HEC-1B (human endometrial adenocarcinoma). Probably, the pigment compound may function as an osmolyte to uphold halotolerant physiological processes in saline environment.

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
    • Biomedical Science Letters
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    • v.19 no.2
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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.

The Constituents Isolated from Peucedanum japonicum Thunb. and their Cyclooxygenase (COX) Inhibitory Activity

  • Zheng, Mingshan;Jin, Wenyi;Son, Kun-Ho;Chang, Hyeun-Wook;Kim, Hyun-Pyo;Bae, Ki-Hwan;Kang, Sam-Sik
    • Korean Journal of Medicinal Crop Science
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    • v.13 no.2
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    • pp.75-79
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    • 2005
  • Five coumarins, psoralen (1), scopoletin (2), isoimperatorin (4), (+)-marmesin (5) and xanthotoxin (6), three chromones, cimifugin (3), hamaudol (7) and sec-O-glucosylhamaudol (10), one sterol, daucosterol (8) and one aliphatic alcohol, galactitol (9) were isolated from the root of Peucedanum japonicum. Their chemical structures were identified by the physicochemical and spectroscopic data by comparing literature values. Among them, compounds 9 and 10 were isolated for the first time from this plant. The anti-inflammatory effects of isolated compounds were examined on cyclooxygenase (COX), compounds 1, 2 and 7 showed inhibitory activity on COX-1 with $IC_{50}$ values of 0.88, 0.27 and 0.30 mM, respectively. In the test for COX-2 activity, only compound 7 showed significant inhibitory activity with the $IC_{50}$ value of 0.57 mM. The other compounds exhibited weak inhibitory or no inhibitory activity.

Inhibitory Activitv of (1,3-Dioxolan-2-yl and Dioxan-2-yl)methylaminium Derivatives against Acetylcholinesterase (Acetylcholinesterase에 대한 (1,3-Dioxolan-2-yl 및 Dioxan-2-yl)methylaminium유도체의 저해 작용)

  • Phi, Taek-San;Kim, Yun-Bae;Kim, Jee-Cheon;Cho, Young;Sok, Dai-Eun;Cha, Seung-Hee;Seo, Won-Jun
    • YAKHAK HOEJI
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    • v.38 no.5
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    • pp.511-515
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    • 1994
  • We examined the inhibitory activity of (1,3-dioxolan-2-yl and 1,3-dioxan-2-yl)methylaminium derivatives(A; 1-8) against acetylcholinesterase. Derivatives of six-membered 1,3-dioxane exhibited more potent inhibitory effect than corresponding 5-membered 1,3-dioxolanes. The presence of methyl group at C4 position of dioxane ring was effective to increase the inhibitory potency of heterocyclic analogues. The activity of N-phenacyl-aminiums was greater than that of N,N,N-trimethyl-aminiums. In general, the terminal methyl group on 1,3-dioxane ring and the phenacyl group in ammonium compound A were assumed to be important factors to enhance the inhibitory action.

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