• Title/Summary/Keyword: hyaluronidase inhibitor

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Hyaluronidase Inhibitor from Uncariae Ramulus et Uncus (조구등의 Hyaluronidase 저해물질)

  • Jeong, Sei-Joon;Ko, Yong-Seok;Ahn, Nyeon-Hyung;Kim, Youn-Chul
    • Korean Journal of Pharmacognosy
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    • v.29 no.3
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    • pp.169-172
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    • 1998
  • Hyaluronidase is one of the mucopolysaccharide-splitting enzyme and is related to the permeability of the vascular system and inflammation. An anti-hyaluronidase assay guided fractionation of the methanolic extract of Uncariae Ramulus et Uncus has furnished a pentacyclic triterpene, ursolic acid (compound I). Compound I exhibited hyaluronidase inhibitory activity with $IC_{50}$ value of 0.15 mM, and disodium cromoglycate showed the inhibitory activity with $IC_{50}$ value of 1.78 mM as a positive control.

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Screening of Hyaluronidase Inhibitory Activity Using a Microplate Assay (Microplate방법을 이용한 Hyaluronidase 저해 활성 검색)

  • Jeong, Sei-Joon;Kim, Na-Young;Ahn, Nyeon-Hyoung;Kim, Youn-Chul
    • Korean Journal of Pharmacognosy
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    • v.28 no.3
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    • pp.131-137
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    • 1997
  • The aqueous and methanolic extracts of 110 crude drugs were screened for hyaluronidase inhibitory activity using a microplate assay. Among them, MeOH extract of 15 crude drugs inhibited more than 80% of hyauluronidase activity at the concentration of 5mg/ml. The active principles of Anemarrhenae Rhizoma, Rhei Rhizoma, Ephedrae Herba, Pteropi Faeces and Ginseng Radix alba were transferred into organic solvents.

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Isolation of Hyaluronidase Inhibitory Component from the Roots of Astraglus membranaceus Bunge (Astragali Radix)

  • Lee, Yun-Mi;Choi, Soo-Im;Lee, Jae-Won;Jung, Sun-Mi;Park, Sang-Min;Heo, Tae-Ryeon
    • Food Science and Biotechnology
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    • v.14 no.2
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    • pp.263-267
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    • 2005
  • In order to isolate hyaluronidase (HAase) inhibitor from Astragali radix (AR), dried roots were extracted with ethanol, prior to sequential fractionations with n-hexane, chloroform, ethyl acetate, n-butanol, and aqueous fractions. The n-butanol soluble fraction was found to exhibit the most pronounced inhibitory effect (68%) on HAase, and the active components were separated using various chromatographic methods, including column chromatography and preparative HPLC. The active component was isolated from the n-butanol soluble fraction of AR and was structurally identified as calycosin-7-O-${\beta}$-D-glucopyranoside by LC-MS, IR, $^1H$ NMR, and $^{13}C$ NMR analysis. The $IC_{50}$ of calycosin-7-O-${\beta}$-D-glucopyranoside's HAase activity was found to be 3.7 mg/mL.

Hyaluronidase Inhibitor 개발에 관한 연구

  • 김진웅
    • Proceedings of the Korean Society of Applied Pharmacology
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    • 1993.04a
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    • pp.128-128
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    • 1993
  • 총 40종 생약의 hyaluronidase에 대한 저해 효과를 검색한 결과, 백지, 오수유, 향부자, 섬백리향, 배풍등, 황금, 황련, 진피, 소리쟁이, 반디나물 등 10종 생약에서 저해 활성을 관찰할 수 있었다. 또한 권백의 n-BuOH 분획에서 2개의 biflavonoid 성분인 amentoflavone, isocryptomerin을 분리하였으며, chloroform 분획에서 cryptomerin B를 분리하였다. 이들 화합물의 화학구조는 각종 기기분석 data를 이용하여 결정하였으며, 이들 화합물중 cryptomerin B는 Selaginellaceae에서 처음으로 분리 보고되는 화합물이다. 현재 이들 화합물의 생리 활성에 대하여 검사중이다.

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Inhibitory Effect of Astragali Radix on Matrix Degradation in Human Articular Cartilage

  • CHOI SOOIM;PARK SO-RA;HEO TAE-RYEON
    • Journal of Microbiology and Biotechnology
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    • v.15 no.6
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    • pp.1258-1266
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    • 2005
  • The present study was carried out in order to assess the protective effects of calycosin-7-O-$\beta$-D-glucopyranoside, isolated from Astragali radix (AR), on hyaluronidase (HAase) and the recombinant human interleukin-$1\beta$ (IL-$1\beta$)-induced matrix degradation in human articular cartilage and chondrocytes. We isolated the active component from the n-butanol soluble fraction of AR (ARBu) as the HAase inhibitor and structurally identified as calycosin-7-O-$\beta$-D-glucopyranoside by LC-MS, IR, ${1}^H$ NMR, and ${13}^C$ NMR analyses. The $IC_{50}$ of this component on HAase was found to be 3.7 mg/ml by in vitro agarose plate assay. The protective effect of ARBu on the matrix gene expression of immortalized chondrocyte cell line C28/I2 treated with HAase was investigated using a reverse transcription polymerase chain reaction (RT-PCR), and its effect on HAase and IL-$1\beta$-induced matrix degradation in human articular cartilage was determined by a staining method and calculating the amount of degraded glycosaminoglycan (GAG) from the cultured media. Pretreatment with calycosin-7-O-$\beta$-D-glucopyranoside effectively protected human chondrocytes and articular cartilage from matrix degradation. Therefore, calycosin-7-O-$\beta$-D-glucopyranoside from AR appears to be a potential natural ant-inflammatory or antii-osteoarthritis agent and can be effectively used to protect from proteoglycan (PG) degradation.

Screening of Hyaluronidase Inhibitor in Korean Medicinal Plants (천연물로부터 히알루로니다아제 저해제 검색)

  • Hwang, Seon Gu;Yang, Anna;Kim, Soo Jung;Kim, Min Kee;Kim, Sung Soo;Oh, Hyun Jung;Lee, Jung Dae;Lee, Eun Ju;Nam, Kung-Woo;Han, Man-Deuk
    • Journal of Life Science
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    • v.24 no.5
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    • pp.498-504
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    • 2014
  • Mammalian hyaluronidases (HAase, EC 3.2.1.35) are a family of enzymes that hydrolyse N-acetyl-D-glucosamine (1-4) glycosidic bonds in hyaluronic acid, which is found in skin, cartilage, and the vitreous body. Although HAase is generally present in an inactive form within subcellular lysosomes, it is released in an active form in some types of inflammation and tissue injuries, thereby contributing to the inflammatory response. The HAase inhibitory activity of 500 methanolic extracts of 500 species from medicinal plants was screened using a Morgan microplate assay. The viscosity of the hyaluronic acid was measured with an Ubbelohde viscometer. Three MeOH extracts inhibited more than 50% of HAase activity at a concentration of 2 mg/ml. HAase inhibitory rates (%) of three species of medicinal plant extracts, Styrax japonica, Deutzia coreana, and Osmanthus insularis were 57.28%, 53.50%, and 53.19%, respectively. The rate of HAase inhibition of the extracts was dose dependent. In the HAase inhibitory assay using the Ubbelohde viscometer, the results were in good agreement with the results from the Morgan assay. The results suggest that HAase inhibitory compounds extracted from the stem of S. japonica, D. coreana, and O. insularis might be multifunctional and prevent the degradation of hyaluronic acid and the induction of allergic reactions and inflammation.

Isolation of Lipoxygenase Inhibitor from Indonesian Herb

  • Alfi Khatib;Kim, Young-Chan;Chung, Shin-Kyo
    • Proceedings of the Korean Society of Postharvest Science and Technology of Agricultural Products Conference
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    • 2003.04a
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    • pp.111.2-112
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    • 2003
  • A total of 20 extracts derived from different plant family commonly used in Indonesian traditional inflammation medicine were screened for their inhibitory effect on soybean lipoxygenase (SBL) and hyaluronidase (HAse) activity. Three methanol extracts, the bark of Cinnamomum burmanni (CB), the leaves of Piper betel (PB), and fruit of Barringtonia acutangula (BA) were found to have high inhibitory effects, whereas the methanol extract of the leaves of Mimusops elengi (ME) have medium inhibitory effect. The IC50 of CB, PB, BA and ME were found to be 21.7, 16.9, 39.1 and 62.8 g/$m\ell$, respectively. Among the tested extracts, only CB inhibited HAse (IC50 = 27g/$m\ell$). CB was successively fractionated with n-hexane, ethyl acetate, butanol and water. The EtOAc fraction having the strongest activity was fractionated and some compounds were isolated and purified by a preparative HPLC(Develosil ODS-HG-5 column). Coumarin and 2-hydroxy cinnamaldehyde. were identified through the analyses of UV-Vis absorption 1H-NMR, 13C-NMR and FAB+-MS spectra.

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Isolation and Characterization of Elastase Inhibitor from Areca catechu (빈랑으로부터 Elastase 저해물질의 분리 및 특성조사)

  • 조중제;이건국;조병기;최정도
    • Journal of the Society of Cosmetic Scientists of Korea
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    • v.26 no.1
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    • pp.163-186
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    • 2000
  • We have previously screened 150 medicinal plants on the inhibition of elastase and found a significant inhibitory effects of the extracts of Areca catechu L. on the aging and inflammation against the skin tissues. To isolate and identify the compounds having biological activity, we was further purified by each of the solvent fractions, silica gel column chromatography, preparative TLC and reversed-Phase HPLC. Peak in HPLC, which coincided with the inhibitory activity against elastase, was identified as Phenolic substance using various colorimetric methods, UV, and IR. $IC_{50}$/ values of phenolic substance purified from Areca catechu were 26.9 $\mu\textrm{g}$/$m\ell$ for porcine pancreatic elastase (PPE) and 60.8 $\mu\textrm{g}$/$m\ell$ for human neutrophil elastase (HNE). This Phenolic substance showed more potent activity than those of reference compounds, oleanolic acid (76.5 $\mu\textrm{g}$/$m\ell$ for PPE, 219.2 $\mu\textrm{g}$/$m\ell$ for HNE) and ursolic acid (31.0 $\mu\textrm{g}$/$m\ell$ for PPE, 118.6 $\mu\textrm{g}$/$m\ell$ for HNE). According to the Lineweaver-Burk Plots, the inhibition against both PPE and HNE by this phenolic substance was competitive with substrate. Phenolic substance from Areca catechu exhibited high free radical scavenging effect ($SC_{50}$/ : 6 $\mu\textrm{g}$/$m\ell$) and inhibited effectively hyaluronidase activity ($IC_{50}$/: 210 $\mu\textrm{g}$/$m\ell$). These results suggest that the Phenolic substance Purified from Areca catechu showed anti-aging effect by protecting connective tissue proteins.

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Biological Activities of Extracts from Cornus kousa Fruit (산딸나무(Cornus kousa) 열매 추출물의 생리활성)

  • Lee, Eun-Ho;Lee, Seon-Ho;Cho, Young-Je
    • Journal of Applied Biological Chemistry
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    • v.58 no.4
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    • pp.317-323
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    • 2015
  • The extracted phenolic compounds from Cornus kousa fruit for biological activities as functional resources were examined. The phenolic compounds which were extracted with water and 40% ethanol from Cornus kousa fruit were $7.04{\pm}0.27$ and $4.47{\pm}0.18mg/g$, respectively. The 1,1-diphenyl-2-picrylhydrazyl free radical scavenging activity of water and ethanol extracts were 84% and 86% at $50{\mu}g/mL$phenolics, respectively. The 2,2'-Azinobis-(3-ethylbenzothiazoline-6-sulfonic acid radical decolorization activity of water and ethanol extracts were 84 and 95% at $100{\mu}g/mL$ phenolics, respectively. Antioxidant protection factor in water and ethanol extracts at $50{\mu}g/mL$ phenolics were 1.93 and 1.82 PF, respectively. Thiobarbituric acid reactive substance were 69% in water extracts and 89% in ethanol extracts at $150{\mu}g/mL$ phenolics. The inhibition activity on xanthine oxidase in water and ethanol extracts was 34 and 60%, respectively. The inhibition activity on ${\alpha}$-glucosidase was 29% in water extracts and 87% in ethanol extracts. The tyrosinase inhibitory activity was 19% in ethanol extracts. The collagenase inhibition activity of anti-wrinkle effect showed an excellent wrinkle improvement effect as 53% in water extracts and 77% in ethanol extracts at $200{\mu}g/mL$ phenolics. The hyaluronidase inhibition activity as antiinflammation effect of water extracts was confirmed to 34% of inhibition at $200{\mu}g/mL$ phenolic. The results can be expected extracts from Cornus kousa fruit to use as functional resource for antioxidant, antigout, inhibitor of carbohydrate degradation, antiwrinkle activity and antiinflammation activity.