• 제목/요약/키워드: enzyme inhibitory activity

검색결과 1,015건 처리시간 0.029초

Discovery of Chitin Deacetylase Inhibitors through Structure-Based Virtual Screening and Biological Assays

  • Liu, Yaodong;Ahmed, Sibtain;Fang, Yaowei;Chen, Meng;An, Jia;Yang, Guang;Hou, Xiaoyue;Lu, Jing;Ye, Qinwen;Zhu, Rongjun;Liu, Qitong;Liu, Shu
    • Journal of Microbiology and Biotechnology
    • /
    • 제32권4호
    • /
    • pp.504-513
    • /
    • 2022
  • Chitin deacetylase (CDA) inhibitors were developed as novel antifungal agents because CDA participates in critical fungal physiological and metabolic processes and increases virulence in soil-borne fungal pathogens. However, few CDA inhibitors have been reported. In this study, 150 candidate CDA inhibitors were selected from the commercial Chemdiv compound library through structure-based virtual screening. The top-ranked 25 compounds were further evaluated for biological activity. The compound J075-4187 had an IC50 of 4.24 ± 0.16 µM for AnCDA. Molecular docking calculations predicted that compound J075-4187 binds to the amino acid residues, including active sites (H101, D48). Furthermore, compound J075-4187 inhibited food spoilage fungi and plant pathogenic fungi, with minimum inhibitory concentration (MIC) at 260 ㎍/ml and minimum fungicidal concentration (MFC) at 520 ㎍/ml. Therefore, compound J075-4187 is a good candidate for use in developing antifungal agents for fungi control.

보중익기탕 (補中益氣湯)의 한국, 중국, 일본 처방에 대한 항염증 및 항산화 효과 비교 연구 (Comparative Study of Bojungikgitang in Korea, Japan and China on the Anti-Inflammatory and Anti-Oxidative Effects)

  • 최혜민;김희훈;이화동
    • 대한본초학회지
    • /
    • 제29권1호
    • /
    • pp.53-60
    • /
    • 2014
  • Objectives : Bojungikgitang (BJT), the Oriental medical prescription has been traditionally used about improvement of immune response and infective disease at Asian nation. In this study, we has compared about the anti-inflammatory and antioxidative effects on BJT of three countries including Korea (Korean Traditional Medicine, KTM), China (Traditional Chinese Medicine, CTM) and Japan (Japanese Traditional Medicine, JTM). Methods : We has basically using LPS-stimulated RAW 264.7 cells. The expression of these inflammatory mediators has measured using enzyme-linked immunosorbent assay (ELISA) and reverse transcription polymerase chain reaction (RT-PCR). Also, free radical scavenging assay has tested for anti-oxidative activity as well as the contents of total flavonoid and polyphenol. Results : As a result, we were founded the inhibitory effects of BJT (KTM, CTM, JTM) on LPS-induced production of NO, TNF-${\alpha}$ and IL-6 as well as the anti-oxidative activities. Especially the KTM was most effective in anti-inflammatory and anti-oxidative activities. Conclusions : These results indicate that BJT (KTM, CTM, JTM) has a good anti- inflammatory and anti-oxidative effects. But, there were degree of effects on between pharmacopoeia of the countries. Thus, further study is required that find appropriate methods for extracting as well as establish of standardized processes in order to improve the quality of BJT (KTM, CTM, JTM) as an anti-inflammatory and anti-oxidative agent for treatment of inflammatory diseases.

On-Farm and Processing Factors Affecting Rabbit Carcass and Meat Quality Attributes

  • Sethukali Anand Kumar;Hye-Jin Kim;Dinesh Darshaka Jayasena;Cheorun Jo
    • 한국축산식품학회지
    • /
    • 제43권2호
    • /
    • pp.197-219
    • /
    • 2023
  • Rabbit meat has high nutritional and dietetic characteristics, but its consumption rate is comparatively lower than other meat types. The nutritional profile of rabbit meat, by comparison with beef, pork, and poultry, is attributed to relatively higher proportions of n-3 fatty acids and low amounts of intramuscular fat, cholesterol, and sodium, indicating its consumption may provide health benefits to consumers. But, the quality attributes of rabbit meat can be originated from different factors such as genetics, environment, diet, rearing system, pre-, peri-, and post-slaughter conditions, and others. Different rabbit breeds and the anatomical location of muscles may also affect the nutritional profile and physicochemical properties of rabbit meat. However, adequate information about the effect of those two factors on rabbit meat is limited. Therefore, cumulative information on nutritional composition and carcass and meat quality attributes of rabbit meat in terms of different breeds and muscle types and associated factors is more important for the production and processing of rabbits. Moreover, some studies reported that rabbit meat proteins exhibited angiotensin-converting enzyme inhibitory characteristics and antioxidant properties. The aim of this review is to elucidate the determinants of rabbit meat quality of different breeds and its influencing factors. In addition, the proven biological activities of rabbit meat are introduced to ensure consumer satisfaction.

감태나무 에틸아세테이트 분획의 항염증 및 진통 효과 (Anti-inflammatory and Anti-nociceptive Effects of Ethyl Acetate Fraction of Lindera glauca)

  • 김종수;강보혜;박승주;양우인;김명수;이병수;차동석;이세연;권진;전훈
    • 생약학회지
    • /
    • 제53권1호
    • /
    • pp.49-56
    • /
    • 2022
  • The present study was designed to evaluate the anti-inflammatory and anti-nociceptive potential of the ethyl acetate fraction of Lindera glauca (ELG). We found that ELG significantly suppressed NO production through decreased enzyme activity and expression of iNOS in the IFN-γ/LPS-activated murine peritoneal macrophages. The treatment of ELG also down-regulated the expression of COX-2. Our western blot data revealed that inhibitory effects of ELG on these pro-inflammatory mediators were attributed to inactivation of NF-κB. In addition, ELG-fed mice showed a marked decrease in paw edema induced by subplantar injection of trypsin, suggesting in vivo anti-inflammatory potential of ELG. We further investigated the anti-nociceptive properties of ELG using thermal and chemical nociception model. We found that ELG has a strong anti-nociceptive activities in both central and peripheral mechanism. An additional combination test with naloxone revealed that opioid receptor was not involved in the ELG-mediated anti-nociception. In conclusion, ELG may possibly be used as valuable anti-inflammatory and anti-nociceptive agent for the treatment of inflammatory diseases and pains.

Inhibitory Effects of The Flower from Abeliophyllum distichum cv. Okhwang 1 on Melanogenesis in B16 F10 Cells

  • Mi-Ji Noh;Hye-Jeong Park;So-Yeon Han;Jeong-Yong Park;Seo-Hyun Yun;Soo-Yeon Kim;Tae-Won Jang;Jae-Ho Park
    • 한국자원식물학회:학술대회논문집
    • /
    • 한국자원식물학회 2021년도 춘계학술대회
    • /
    • pp.53-53
    • /
    • 2021
  • Abeliophyllum distichum Nakai (A. distichum), endemic species of Korea, is classified according to the petals and calyx colors. Recently, A. distichum cv. Okhwang 1, which has the golden flower, designated the first official cultivar improved from A. distichum species. The study on the chloroplast genome of A. distichum cv. Okhwang 1 have been reported, but no studies on bioactivity such as antioxidant, anti-inflammatory, and anti-cancer have been progressed. This study was conducted to evaluate the inhibition on melanogenesis of the flower from A. distichum cv. Okhwang 1 (FAO). Antioxidant activity was measured using DPPH and ABTS radical scavenging assays. Inhibition effects on melanogenesis of FAO were confirmed by expression of tyrosinase-related proteins and mRNAs using immunoblotting and RT-qPCR. Tyrosinase is an enzyme that regulates both stimulation and inhibition of melanogenesis. Stimulated MITF in cellular levels increases the expressions of tyrosinase, TRP-1, and TRP-2 to induce melanogenesis. As a result, FAO inhibited the expression of MITF, followed by down-regulated tyrosinase, TRP-1, and TRP-2, which lead to inhibit melanin overproduction. In conclusion, these results indicated that FAO reduced reactive oxygen species (ROS) and markedly inhibited the expression of melanin-related factors. The present study suggested providing that FAO has the potential for development as a functional cosmetic material derived from natural.

  • PDF

청상방풍탕 열수 추출물의 피부재생, 주름개선, 미백, 보습 효과 및 세포독성 평가 (Skin Regeneration, Anti-wrinkle, Whitening and Moisturizing Effects of Cheongsangbangpung-tang Aqueous Extracts with Cytotoxicity)

  • 우창윤;김동철
    • 대한한방부인과학회지
    • /
    • 제30권2호
    • /
    • pp.49-70
    • /
    • 2017
  • 목 적: 본 연구는 한의학에서 면포질환에 빈번히 사용하는 대표적인 복합처방인 청상방풍탕의 열수 추출물 동결건조물의 피부 노화 개선 효과 평가를 위하여 피부재생, 주름개선, 미백 및 보습 효과를 각각 평가하였고, 기본적인 독성 평가의 일환으로 세포독성 또한 in vitro 방법으로 평가하였다. 방 법: 본 연구에서는 human normal fibroblast(CRL-2076) 세포 및 B16/F10 murine melanoma(CRL-6475) 세포에 대한 청상방풍탕 열수 추출 동결건조물(수율 18.71%)의 세포독성을 MTT(3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyl-tetrazolium Bromide) 방법을 통해 평가하였고, B16/F10 melanoma cells의 melanin 생성 억제 정도 및 melanin 합성 필수 효소인 tyrosinase 활성 억제와 arbutin을 비교 평가하여 미백효과를 평가하였다. 또한 피부 재생 및 주름 개선 효과를 transforming growth factor(TGF)-${\beta}1$와 fibroblast의 collagen type I 합성능을 비교, phosphoramidon disodium salt(PP)와 세포외 기질의 분해에 관여하는 elastase활성 억제를 비교, oleanolic acid(OA)와 hyaluronidase, collagenase 및 matrix metalloproteinase(MMP)-1 활성 억제를 비교하여 각각 평가하였고, 마우스 피부 수분함량 변화를 관찰하여 보습효과를 평가하였다. 결 과: 본 실험의 결과, 청상방풍탕은 human normal fibroblast 세포 및 B16/F10 murine melanoma 세포에서 최고 농도인 500 mg/ml까지 유의한 세포독성이 나타나지 않았고, fibroblast의 collagen type I 합성을 증가시켰다. 또한 세포외기질 파괴와 연관된 것으로 알려진 hyaluronidase, elastase, collagenase 및 MMP-1 활성을 각각 억제하였고 melanin의 생성에 관여하는 tyrosinase의 활성 및 B16/F10 melanoma 세포의 melanin 생성을 농도 의존적으로 차단함이 관찰되었다. 이와 더불어 정상매체 대조군에 비해 청상방풍탕 경구 투여군이 투여 용량 의존적으로 마우스 피부 수분 함량을 유의성 있게 증가시켰다. 결 론: 이상의 결과에서, 청상방풍탕은 세포 독성 없이 피부재생, 주름개선, 미백 및 보습 효과를 나타남이 관찰되어 차후 피부 개선 소재로서 그 가치가 높을 것으로 판단되나 금후 개별 구성 약재 각각에 대한 효능 및 생리활성을 나타내는 화학성분의 검색과 더불어 다양한 방면으로 기전적인 연구와 피부 보호 효과에 대한 in vivo평가를 체계적으로 수행해야 할 것으로 판단된다.

참취(Aster scaber) 추출물의 생리활성 (Biological activities of Aster scaber extracts)

  • 이은호;박혜진;김나현;홍은진;박미정;이선호;김명욱;안봉전;조영제
    • 한국식품저장유통학회지
    • /
    • 제23권3호
    • /
    • pp.393-401
    • /
    • 2016
  • 참취로부터 phenolic compounds를 추출 후 항산화 효과, 건강 기능성 식품 및 미용식품 활성을 검정하여 기능성 소재로 활용 가능성을 살펴보았다. 참취에 함유되어 있는 페놀성 물질은 물과 60% ethanol을 용매로 하여 추출하였을 때 각각 11.1 mg/g, 4.18 mg/g 함량을 나타내었다. 추출물의 phenolic 농도를 $50{\sim}200{\mu}g/mL$로 조절하여 DPPH를 측정한 결과, 물 추출물과 ethanol 추출물 $50{\mu}g/mL$ phenolics 농도에서 각각 87%, 91%였고, ABTS radical decolorization도 $50{\mu}g/mL$ phenolics 농도에서 각각 99%, 99%였다. Antioxidant protection factor는 $200{\mu}g/mL$ phenolics 농도에서 물 추출물과 ethanol 추출물에서 각각 1.87 PF와 2.22 PF로 측정되었으며, TBARs값은 $50{\mu}g/mL$ phenolics농도에서 물 추출물이 95%, ethanol 추출물에서 97%를 나타내었다. Angiotensin converting enzyme(ACE) 저해능은 물 추출물에서 50.8%, ethanol 추출물에서 69.4%의 저해율을 나타내었으며, xanthine oxidase 저해능은 물 추출물은 $50{\mu}g/mL$ phenolics농도에서 91%, ethanol 추출물은 $200{\mu}g/mL$ phenolics농도에서 80%의 높은 효능을 보였다. ${\alpha}$-Amylase 저해능은 물 추출물과 ethanol 추출물에서 각각 24%, 89%로 ethanol 추출물에서 높은 효능을 보였다. Tyrosinase 저해능을 측정한 결과 물 추출물과 ethanol 추출물에서 각각 47%, 25%의 미백 효과를 나타내었다. Elastase 저해능 측정 결과 물 추출물과 ethanol 추출물에서 각각 46%, 14%로 물 추출물에서 주름 개선 효과가 상대적으로 높게 나타내었다. 이러한 결과로 보아 참취 추출물은 항산화 고혈압억제, 통풍억제, 당분해억제, 미백효과, 주름개선효과 등의 건강 기능성 식품 및 미용식품 활성 소재로서 활용 가능성이 큰 것으로 판단되었다.

The Inhibitory Mechanism of Aloe Glycoprotein (NY945) on the Mediator Release in the Guinea Pig Lung Mast Cell Activated with Antigen-Antibody Complexes

  • Ro, Jai-Youl;Lee, Byung-Chul;Chung, Myung-Hee;Lee, Seung-Ki;Sung, Chung-Ki;Kim, Kyung-Hwan;Park, Young-In
    • The Korean Journal of Physiology and Pharmacology
    • /
    • 제2권1호
    • /
    • pp.119-131
    • /
    • 1998
  • It has been reported that the glycoprotein extracted from Aloe has strong anti-inflammatory response. However, there has been no research report yet about the effect of Aloe on allergic hypersensitivity reactivity. By using guinea pig lung mast cells, this study aimed to examine the effects of Aloe glycoprotein (NY945) on the mediator releases caused by mast cell activation, and also aimed to assess the effects of NY945 on the mechanism of mediator releases in the mast cell activation. We partially purified mast cell from guinea pig lung tissues by using the enzyme digestion, the rough and the discontinuous density percoll gradient method. Mast cells were sensitized with IgG1 (anti-OA) and challenged with ovalbumin. Histamine was assayed by fluorometric analyzer, leukotrienes by radioimmunoassay. The phospholipase D activity was assessed by the production of labeled phosphatidylalcohol. The amount of mass 1, 2-diacylglycerol (DAG) was measured by the $[^3H]DAG$ produced when prelabeled with $[^3H]myristic$ acid. The phospholipid methylation was assessed by measuring the incorporation of the $[^3H]methyl$ moiety into phospholipids of cellular membranes. Pretreatment of NY945 (10 ${\mu}g$) significantly decreased histamine and leukotrienes releases during mast cell activation. The decrease of histamine release was stronger than that of leukotriene during mast cell activation. The phospholipase D activity increased by the mast cell activation was decreased by the dose-dependent manner in the pretreatment of NY945. The amount of DAG produced by PLC activity was decreased by NY945 pretreatment. The amount of mass 1, 2-diacylglycerol produced by activation of mast cells was decreased in the pretreatment of NY945. NY945 pretreatment strongly inhibited the incorporation of the $[^3H]methyl$ moiety into phospholipids. The data suggest that NY945 purified from Aloe inhibits in part an increase of 1, 2-diacylglycerol which is produced by activating mast cells with antigen-antibody reactions, which is mediated via phosphatidylcholine-phospholipase D and phosphatidylinositol-phospholipase C systems, and then followed by the inhibition of histamine release. Furthermore, NY945 reduces the production of phosphatidylcholine by inhibiting the methyltransferase I and II, which decreases the conversion of phosphatidylcholine into arachidonic acid and inhibits the production of leukotrienes.

  • PDF

동결건조 어류 알 농축물의 식품기능성 및 생리활성 (Food Functionality and Bioactivity of Vacuum Freeze-dried Fish Roe Concentrates)

  • 윤인성;김형준;강상인;김도엽;이창영;정우철;김진수;허민수
    • 한국수산과학회지
    • /
    • 제53권3호
    • /
    • pp.403-416
    • /
    • 2020
  • The purpose of this study was to evaluate the food functional properties and in vitro bioactivity of vacuum freeze-dried fish roe concentrates (FRCs) prepared from Alaska pollock Theragra chalcogramma (AP), bastard halibut Paralichthys olivaceus (BH) and skipjack tuna Katsuwonus pelamis (ST). All three species showed better buffering capacity on the alkaline side (pH 10-12) than on the acidic side. The water-holding capacities of the FRCs were 3.5, 8.5 and 4.2 g/g protein for AP, BH and ST, respectively, and were significantly higher than that of commercial egg white. The protein solubilities of the FRCs were 42.5% (AP), 50.0% (BH) and 13.9% (ST). The foaming capacities of the FRCs were not significantly different among the species (128.0% for AP, 128.3% for BH, and 143.3% for ST; P>0.05), and their foam stability was maintained at 53.0-74.2% for 60 minutes. The oil-in-water emulsifying activity indexes of AP and BH (19.5 and 20.2 ㎡/g protein, respectively) were significantly superior to that of ST (P<0.05). The 2,2-diphenyl-1-picrylhydrazyl and 2,2'-azino-bis-3-ethylbenzothia-zoline-6-sulfonic acid radical-scavenging activities (IC50, mg/mL) of the FRCs were in the ranges of 1.05-3.26 and 0.13-0.18 mg/mL, respectively, and the angiotensin I converting enzyme inhibitory activity was in the range of 0.97-1.89 mg/mL.

Cloning, Expression, Purification, and Properties of an Endoglucanase Gene (Glycosyl Hydrolase Family 12) from Aspergillus niger VTCC-F021 in Pichia pastoris

  • Pham, Thi Hoa;Quyen, Dinh Thi;Nghiem, Ngoc Minh;Vu, Thu Doan
    • Journal of Microbiology and Biotechnology
    • /
    • 제21권10호
    • /
    • pp.1012-1020
    • /
    • 2011
  • A gene coding for an endoglucanase (EglA), of the glycosyl hydrolase family 12 and derived from Aspergillus niger VTCC-F021, was cloned and sequenced. The cDNA sequence, 717 bp, and its putative endoglucanase, a 238 aa protein with a predicted molecular mass of 26 kDa and a pI of 4.35, exhibited 98.3-98.7% and 98.3-98.6% identities, respectively, with cDNA sequences and their corresponding endoglucanases from Aspergillus niger strains from the GenBank. The cDNA was overexpressed in Pichia pastoris GS115 under the control of an AOX1 promoter with a level of 1.59 U/ml culture supernatant, after 72 h of growth in a YP medium induced with 1% (v/v) of methanol. The molecular mass of the purified EglA, determined by SDS-PAGE, was 33 kDa, with a specific activity of 100.16 and 19.91 U/mg toward 1% (w/v) of ${\beta}$-glucan and CMC, respectively. Optimal enzymatic activity was noted at a temperature of $55^{\circ}C$ and a pH of 5. The recombinant EglA (rEglA) was stable over a temperature range of $30-37^{\circ}C$ and at pH range of 3.5-4.5. Metal ions, detergents, and solvents tested indicated a slightly inhibitory effect on rEglA activity. Kinetic constants ($K_m$, $V_{max}$, $k_{cat}$, and $k_{cat}/K_m$) determined for rEglA with ${\beta}$-glucan as a substrate were 4.04 mg/ml, 102.04 U/mg, 2,040.82 $min^{-1}$, and 505.05, whereas they were 10.17 mg/ml, 28.99 U/mg, 571.71 $min^{-1}$, and 57.01 with CMC as a substrate, respectively. The results thus indicate that the rEglA obtained in this study is highly specific toward ${\beta}$-glucan. The biochemical properties of rEglA make it highly valuable for downstream biotechnological applications, including potential use as a feed enzyme.