• Title/Summary/Keyword: ACE inhibitory effect

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In-silico Studies of Boerhavia diffusa (Purnarnava) Phytoconstituents as ACE II Inhibitor: Strategies to Combat COVID-19 and Associated Diseases

  • Rahul Maurya;Thirupataiah Boini;Lakshminarayana Misro;Thulasi Radhakrishnan
    • Natural Product Sciences
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    • 제29권2호
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    • pp.104-112
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    • 2023
  • COVID-19 caused a catastrophe in human health. People infected with COVID-19 also suffer from various clinical illnesses during and after the infection. The Boerhavia diffusa plant is well known for its antihypertensive activity. ACE-II inhibitors and calcium channel blockers are reported as mechanisms for the antihypertensive activity of B. diffusa phytoconstituents. Various studies have said ACE-II is the virus's binding site to attack host cells. COVID-19 treatment commonly employs a variety of synthetic antiviral and steroidal drugs. As a result, other clinical illnesses, such as hypertension and hyperglycemia, emerge as serious complications. Safe and effective drug delivery is a prime objective of the drug development process. COVID-19 is treated with various herbal treatments; however, they are not widely used due to their low potency. Many herbal plants and formulations are used to treat COVID-19 infection, in which B. diffusa is the most widely used plant. The current study relies on discovering active phytoconstituents with ACE-II inhibitory activity in the B. diffusa plant. As a result, it can be used as a treatment option for patients with COVID-19 and related diseases. Different phytoconstituents of the B. diffusa plant were selected from the reported literature. The activity of phytoconstituents against ACE-II proteins has been studied. Molecular docking and ligand-protein interaction computation tools are used in the in-silico experiment. Physicochemical, drug-likeness, water solubility, lipophilicity, and pharmacokinetic parameters are used to evaluate phytoconstituents. Liriodenine has the best drug-likeness, bioactivity, and binding score characteristics among the selected ligands. The in-silico study aims to find the therapeutic potential of B. diffusa phytoconstituents against ACE-II. Targeting ACE-II also shows an effect against SARS-CoV-2. It can serve as a rationale for designing a drug for patient infected with COVID-19 and associated diseases.

큰까치수영의 항산화 및 안지오텐신 전환 효소 저해 활성 (Antioxidant and Inhibitory Activities on Angiotensin Converting Enzyme in Lysimachia clethroides Duby)

  • 방진기;성낙술;이승은
    • Applied Biological Chemistry
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    • 제47권2호
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    • pp.265-269
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    • 2004
  • 생리활성 보유 식물자원 발굴 및 이용을 위해 큰까치수영 지상부에 대한 항산화 및 항고혈압 활성을 검정하였으며 페놀화합물의 함량은 메탄올 추출물이 2.62%, 물 추출물이 0.23%였고 메탄올 추출물에서 얻어진 용매별 분획물 중에서는 에틸차세테이트 분획이 37.76%로 가장 함량이 높았다. Linoleic acid 자동산화에 대한 저해효과는 메탄올 추출물이 반응 6일째에 83%이상의 저해율을 보여 ${\alpha}-tocopherol$의 -2%보다 탁월하게 우수였으며 각 분획물 중에서는 핵산 및 에텔 분획이 매우 효과적으로 자동산화를 저해하였다. Superoxide anion 라디칼에 대헤서는 큰까치수영의 메탄올 추출물과 물 추출물이 $5{\sim}200\;{\mu}g/ml$의 농도에서 $86{\sim}109%$$96{\sim}122%$로 항산화제인 ascorbic acid의 $-4{\sim}69%$보다 월등하게 우수한 소거능을 보였으며 DPPH 라디칼에 대해서는 에틸아세테이트분획이 $26.8\;{\mu}g/ml$$RC_{50}$로 좋은 소거 효과를 나타내었다. ACE에 대한 저해활성은 $4,000\;{\mu}g/ml$의 농도에서 물 추출물(33%)보다는 메탄올 추출물(71%)이 효과적이었으며 분획물 중에서는 n-hexane fraction(133%), ether fraction(100%) 및 ethylacetate fraction(88%) 분획이 매우 효과적인 저해활성을 나타내었다.

Cacao bean으로부터 분리된 polyphenol 성분의 화학구조분석과 ACE 저해효과 (The chemical structure of polyphenols isolated from cacao bean and their inhibitory effect on ACE)

  • 장영렬;임무현;이만종
    • Applied Biological Chemistry
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    • 제41권1호
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    • pp.110-117
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    • 1998
  • Ghana산 cacao bean으로부터 acetone으로 추출하고 Sephadex LH-20, MCI-gel CHP-20, Bondapak $C_{18}$ 및 Fuji gel ODS $G_3$, chromatography 등을 이용하여 7종의 polyphenol 화합물(compound 1 - compound 7)을 분리 정제하였고, 이들 화합물의 화학구조를 $^1H-NMR$, $^{13}C-NMR$, IR 및 MS를 사용하여 검색하였고 아울러 angiotensin converting enzyme(ACE) 저해효과를 조사 검토하였다. 분리정제한 7종의 polyphenol 화합물의 구조를 분석한 결과, compound 1: [(+)-catechin], compound 2: [(-)-epicatechin], compound 3: [procyanidin B-1, (-)-epicatechin-$(4{\beta}{\rightarrow}8)$-(+)-catechin], compound 4 : [procyanidin B-2, (-)-epicatechin-$(4{\beta}{\rightarrow}8)$-(-)-epicatechin], compound 5: [procyanidin B-7, (-)-epicatechin-$(4{\beta}{\rightarrow}6)$-(+)-catechin], compound 6 : (procyanidin B-2,3,3'-O-digallate) 및 compound 7: [cinnamtannin A-2, (-)-epicatechin-$(4{\beta}{\rightarrow}8)$-(-)-epicatechin-$(4{\beta}{\rightarrow}8)$-(-)-epicatechin-$(4{\beta}{\rightarrow}8)$-(-)-epicatechin]임을 동정하였다. ACE의 저해효과는 procyanidin B-2,3,3'-O-digallate (compound 6)가 $100\;{\um}M$에서 94.6%로 매우 우수하였으며, (+)-catechin (compound 1), (-)-epicate -chin (compound 2), procyanidin B류 (compound 3, 4, 5) 및 cinnamtannin A-2 (compound 7)도 각각 67.9%, 61.9%, 88.6%, 82.5%, 72.2% 및 82.3%의 비교적 우수한 저해효과가 있었다. 아울러 결합방식에서는 $4{\beta}{\rightarrow}6$보다 $4{\beta}{\rightarrow}8$의 결합방식이, 그리고 procyanidin 류에서는 gallate를 갖는 물질이 이를 함유하지 많은 물질보다 더욱 높은 ACE의 저해효과를 나타내었으며, 또한 hydroxyl 기가 많을수록 효소 저해효과도 증가하는 것으로 나타났다. 이와 같은 결과는 chocolate의 주원료인 cacao bean의 polyphenol 성분 또한 녹차 등에서 볼 수 있는 생리활성효과에 손색없는 것으로 판단되고, 이러한 기능성에 기초하여 chocolate, 음료 등의 식품이나 의약품의 기능성 소재로서의 산업적 응용 가능성이 높은 것으로 사료된다.

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감마선 조사에 따른 참치 자숙액의 위생화 및 기능성 변화 연구 (Effect of Gamma Irradiation on the Microbial Safety and Biological Activities of Tuna Cooking Juices)

  • 변명우
    • KSBB Journal
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    • 제27권4호
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    • pp.222-226
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    • 2012
  • In this study, the effect of gamma irradiation on the microbial contamination and biological activities of tuna cooking juices was investigated. Tuna cooking juice was by-produced during the canning processing, and had various functional components. But, it was shown that the tuna cooking juice was seriously contaminated. Gamma irradiation effectively reduced the microbial population in tuna cooking juice. Also, 1,1-diphenyl-2-picryl-hydrazyl (DPPH) radical scavenging activity, tyrosinse inhibitory activity, and ACE inhibitory activity of tuna cooking juices were all increased as a result of gamma irradiation. These results suggest that wasted tuna cooking juices can be used as a functional component in the food and cosmetic industries if the irradiation technology were applied.

Characterization and ACE Inhibitory Activity of Fermented Milk with Probiotic Lactobacillus plantarum K25 as Analyzed by GC-MS-Based Metabolomics Approach

  • Zhang, Min;Jiang, Yunyun;Cai, Miao;Yang, Zhennai
    • Journal of Microbiology and Biotechnology
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    • 제30권6호
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    • pp.903-911
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    • 2020
  • Addition of probiotics to yogurt with desired health benefits is gaining increasing attention. To further understand the effect of probiotic Lactobacillus plantarum on the quality and function of fermented milk, probiotic fermented milk (PFM) made with probiotic L. plantarum K25 and yogurt starter (L. delbrueckii ssp. bulgaricus and Streptococcus thermophilus) was compared with the control fermented milk (FM) made with only the yogurt starter. The probiotic strain was shown to survive well with a viable count of 7.1 ± 0.1 log CFU/g in the PFM sample after 21 days of storage at 4℃. The strain was shown to promote formation of volatiles such as acetoin and 2,3-butanediol with milk fragrance, and it did not cause post-acidification during refrigerated storage. Metabolomics analysis by GC-MS datasets coupled with multivariate statistical analysis showed that addition of L. plantarum K25 increased formation of over 20 metabolites detected in fermented milk, among which γ-aminobutyric acid was the most prominent. Together with several other metabolites with relatively high levels in fermented milk such as glyceric acid, malic acid, succinic acid, glycine, alanine, ribose, and 1,3-dihydroxyacetone, they might play important roles in the probiotic function of L. plantarum K25. Further assay of the bioactivity of the PFM sample showed significant (p < 0.05) increase of ACE inhibitory activity from 22.3% at day 1 to 49.3% at day 21 of the refrigerated storage. Therefore, probiotic L. plantarum K25 could be explored for potential application in functional dairy products.

구증구포 처리 대두 추출물의 항산화 활성 및 Angiotensin-I Converting Enzyme 저해 효과 (Effect on Angiotensin-I Converting Enzyme Inhibition and Antioxidant Activities of Soybean (Glycine max L.) following Steaming and Drying Nine Times)

  • 김현영;서혜영;서우덕;이미자;최만수;함현미
    • 한국식품영양학회지
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    • 제33권2호
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    • pp.167-173
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    • 2020
  • To increase the functional material content of soybean, a repetitive steaming and drying process was used. We investigated the changes in the total polyphenol content, the antioxidant activity, and the angiotensin-I converting enzyme (ACE) inhibition in soybean following nine rounds of steaming and drying. Soybean was steamed 9 times for 2 h and then dried 9 times from 55℃ to 73℃ for 3 h. The total polyphenol content in the soybean reached a maximum value of 60.47 mg GAE eq./100 g at 73℃ while the total polyphenol content in the raw soybean reached 25.17 mg GAE eq./100 g. In the raw soybean samples, the DPPH radical scavenging activity (5 mg/mL) was 8.04% but it increased by 43.29% after drying 9 times to 73℃. ABTS radical scavenging activity also improved following 9 rounds of steaming and drying. ACE inhibitory activity of the soybean dried 9 times at 73℃ was 58.94% at 10 mg/mL. These results showed that steaming and drying soybean 9 times enhanced the antioxidant activity and the ACE inhibitory activity of soybean. Therefore, more research on the biological and anti-hypertensive activity of soybean using this steaming and drying method is necessary.

맹종죽의 항산화활성을 통한 항고혈압 효능 (Anti-hypertensive Effects of ethanol extract of Phyllostachys Pubescens via Antioxidant Activity)

  • 이혜숙;박민희;김정숙;임병우;문갑순;신흥묵
    • 동의생리병리학회지
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    • 제21권3호
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    • pp.658-665
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    • 2007
  • Phyllostachys pubescens (Maengiong-Juk), a kind of the bamboo, was reported to have many beneficial pharmacological actions. in this study, of using 70% ethanol extract of Phyllostachys pubescens we investigated its efficacy on angiotensin converting enzyme (ACE) and antioxidant enzyme activities. In addition, vasorelaxant effect was examined in rat aortic rings. The inhibitory effect of ACE activity by Phyllostachys pubescens extract (PPE) was dose-dependently increased by 61.42% at 10mg/ml. PPE relaxed the pre-contracted rat aortic rings with 10$^{-6}$M phenylephrine, showing about 88% at 4.0mg/ml. Sprague Dawley (SD) rats were given different concentrations of PPE mixed in the drinking water for 10 weeks. PPE did not show any difference with control group in blood pressure, body weight (BW) and food intake. However, it revealed the highest total antioxidative effect at dose of 1.0 g/100 g BW in plasma by TEAC assay. Thiobarbituric acid reactive substance (TBARS) and protein carbonyl levels which are markers of tissue peroxidation, were significantly lowed at the same dosage. Furthermore, hepatic antioxidant enzymes such as total superoxide dismutase (SOD), glutathione peroxidase (GSH-Px), glutathione reductase (GR) and catalase activities were also significantly increased by PPE (1.0 g/100 g BW). In conclusion, we suggest that PPE might have antihypertensive effect through increasing antioxidant activities.

양파로부터 분리한 생리활성분획이 생리활성 및 지질대사에 미치는 영향 (Effect of Biologically Active Fractions from Onion on Physiological Activity and Lipid Metabolism)

  • 우희섭;안봉전;배종호;김성;최희진;한호석;최청
    • 한국식품영양과학회지
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    • 제32권1호
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    • pp.119-123
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    • 2003
  • 양파를 80% ethanol로 추출하여 Sephadek LH-20 column chromatography로 fraction I, II 및 III의 생리활성물질을 분리하여 angiotensin converting enzyme(ACE), xanthine oxidase, tyrosinase의 저해작용 효과와 지질대사를 검토하였다 Fraction I과 II의 ACE 저해작용은 50 ppm 농도에서 80% 이상의 효소 저해효과를 나타내었고 fraction III에서는 500 ppm 농도에서 90% 효소저해작용을 보였다. 100 ppm 농도에서 fraction III의 xantine oxidase 효소저해 효과는 82.5%로 나타났으며 tyrosinase의 저해효과는 42.6%이었다. 효소저해작용이 가장 강한 fraction III를 2개월 동안 고지방식이에 첨가하여 혈장 및 간장에서 지질대사에 미치는 영향을 분석한 결과 혈장에서는 총지질, 중성지질이 대조군에 비하여 유의성 있게 감소하였다. 간의 콜레스테롤량도 약 50% 정도 감소하는 결과를 얻었다.

청국장 발효과정 중 항고혈압성 peptide의 생산 및 분리 (Production and Separation of Anti-hypertensive Peptide during Chunggugjang Fermentation with Bacillus subtilis CH-1023)

  • 차원섭;복수경;김명욱;천성숙;최웅규;조영제
    • Applied Biological Chemistry
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    • 제43권4호
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    • pp.247-252
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    • 2000
  • 한국 전통장류의 기능성 탐색 연구의 일환으로 청국장 발효과정 중 고혈압을 유발하는 angiotensin converting enzyme(ACE)의 저해 peptide를 분리하고 저해효과를 검토하였다. 청국장은 Bacillus subtilis CH-1023을 이용하여 제조하였고, $20^{\circ}C,\;30^{\circ}C,\;40^{\circ}C,\;50^{\circ}C,\;60^{\circ}C$에서 $0{\sim}72$시간동안 배양하면서 protein양, protease activity, ACE 저해율을 측정하고 저해활성을 가지는 peptide를 정제 후 아미노산조성을 분석하였다. 청국장의 발효시간이 경과함에 따라 protein 함량이 증가하여 $40^{\circ}C$, 60시간에서 최대를 나타낸 후 감소하였으며, 발효시간에 따른 protease activity와 ACE 저해율은 $40^{\circ}C$, 60시간에서 최대로 나타난 후 점차 감소하였다. 따라서 Bacillus subtilis CH-1023을 이용한 청국장 제조는 $40^{\circ}C$에서 60시간 배양이 최적의 배양조건이었다. 최적 발효조건에 따라 청국장을 제조한 후 20 mM sodium phosphate buffer(pH 7.0)를 가해 추출한 추출물을 Amicon YM-3 membrane filtration과 Sephadex G-10, G-25를 이용한 gel filtration으로 부분정제 하였다. 또한 정제한 peptide는 첨가함량이 높아질수록 저해활성은 높게 나타났으며, 0.5 mg 정도의 peptide 함량으로 94.3%의 저해율을 나타내었다. 정제한 peptide의 아미노산 조성은 histidine, alanine, phenylalanine 함량이 높은 것으로 나타났다.

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고려인삼중 다당체 성분이 암독소 호르몬-L의 지방분해 작용과 안지오텐신 변환효소의 활성에 미치는 영향 (Effect of Acidic Polysaccharide Components of Korean Ginseng on Lipolytic Action of Toxohormone-L and on Activity of Angiotensin Converting Enzyme)

  • 이성동;황우익;흥전척도
    • Journal of Ginseng Research
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    • 제20권3호
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    • pp.248-255
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    • 1996
  • This study was devised to observe in vitro, the inhibitory effects of acidic polysaccharide fractions from Korean red ginseng (KRG) and white ginseng (KWG) on the lipolytic action of loxohormone-L and on angiotensin converting enzyme (ACE, peptidyldipeptidase hydrolase, EC 3.4.15.1) . The crude acidic polysaccharides (CAP) extracted from main and lateral roots of KRG and KWG were separately purified through several procedures. The total inhibitory activities on the lipolytic action of toxohormone-L of CAP from main roots of KRG and KWG was higher than those of CAP from lateral roots of KRG and KWG, respectively, and that of CAP from main root of KRG was 3.1 times higher than that of CAP from main root of KWG. The specific activity of CAP from main root of KRG was measured as 5.40 units/mg, when one unit was defined as the amount giving 50% inhibition on toxohormone-L induced lipolysls. A subfraction named PG4 3 obtained by replanted chromatography on DEAE-TOYOPEARL 650M gave the specific activity of 24.4 units/mg. On the other hand, it was found that the total inhibitory activity on ACE of CAP from lateral root of KRG was the highest among the 4 kinds of CAP, but the specific activity of CAP from lateral root of KWG was the highest.

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