• 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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    • v.29 no.2
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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.

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

  • Bang, Jin-Ki;Seong, Nak-Sul;Lee, Seung-Eun
    • Applied Biological Chemistry
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    • v.47 no.2
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    • pp.265-269
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    • 2004
  • This study was conducted to develop physiologically active plant materials from medicinal plants. Crude extracts and solvent fractions prepared from Lysimachia cletroides Duby were tested for their antioxidant and antihypertensive activities. For ellucidating antioxidant potential, inhibition rate on linoleic acid peroxidation, as well as scavenging activities on superoxide anion and 1,1-dipicrylphenylhydrazyl (DPPH) radical were evaluated. For analyzing antihypertensive effect, inhibitory activity on angiotensin converting enzyme (ACE) was done. Methanol extract of L. cletroides showed potent inhibition activity of 83% on linoleic acid peroxidation, which was more effective than -2% of ${\alpha}-tocopherol$ at $25\;{\mu}g/ml$. Methanol and water extracts exhibited strong scavenging activities of $86{\sim}109%$ and $96{\sim}122%$ on superoxide anion radical which was higher than $-4{\sim}69%$ of ascorbic acid at $5{\sim}200\;{\mu}g/ml$. Hexane, ether and ethylacetate fractions possessed 133, 100 and 88% inhibitory activities on ACE at $4,000\;{\mu}g/ml$, respectively. From the results, it was expected that Lysimachia cletroides could be a new antioxidant and antihypertensive resource.

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

  • Chang, Young-Youl;Yim, Moo-Hyun;Lee, Man-Chong
    • Applied Biological Chemistry
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    • v.41 no.1
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    • pp.110-117
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    • 1998
  • Seven kinds of polyphenol compounds having ACE activities were isolated and purified by Sephadex LH-20, MCI-gel CHP-20, ${\um}-Bondapak\;C_{18}$ and Fuji-gel ODS $G_3$ sucessively from cacao bean(Ghana). The chemical structures of each compound were determined and identified using analyzers such as $^1H-NMR$, $^{13}C-NMR$, IR, MS, polarimeter and Elemental Analysis. Inhibition effects of isolated polyphenols on angiotensin converting enzyme (concerned with hypertension) were also observed. The results obtained were as follows,; The compounds isolated and identified were confirmed and determined as 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], campound 6 (procyanidin B-2,3,3'-O -digallate), compound 7 [cinnamtannin A-2 : (-)-epicatechin-$(4{\beta}{\rightarrow}8)$-(-)-epicatechin-$(4{\beta}{\rightarrow}8)$-(-)-epicatechin-$(4{\beta}{\rightarrow}8)$-(-)-epicatechin]. In the inhibition effect on ACE, procyanidin B-2,3,3'-O-digallate (compound 6) showed a higher value of 94.6% for ACE in $100\;{\um}M$ than other compounds such as (+)-catechin (compound 1), (-)-epicatechin (compound 2), procyanidin B-1 (compound 3), procyanidin B-2 (compound 4), procyanidin B-7 (compound 5) and cinnamtannin A-2 (compound 7) showing 67.9%, 61.9%, 88.6%, 82.5%, 72.2% and 82.3% for ACE, respectively. Inhibition of $4{\beta}{\rightarrow}8$ in coupling bond on the ACE enzyme was more effective than that of $4{\beta}{\rightarrow}6$. Procyanidin containing gallate inhibited more effectively than those containing not any. It was also observed that a lot of hydroxy group in the compounds increased the inhibitory effect.

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

  • Byun, Myung-Woo
    • KSBB Journal
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    • v.27 no.4
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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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    • v.30 no.6
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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.

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

  • Kim, Hyun Young;Seo, Hye-Young;Seo, Woo Duck;Lee, Mi Ja;Choi, Man-Soo;Ham, Hyeonmi
    • The Korean Journal of Food And Nutrition
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    • v.33 no.2
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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.

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

  • Lee, Hye-Suk;Park, Min-Hee;Kim, Jung-Suk;Lim, Beong-Ou;Moon, Gap-Soon;Shin, Heung-Mook
    • Journal of Physiology & Pathology in Korean Medicine
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    • v.21 no.3
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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.

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

  • Woo, Hi-Seob;Aan, Bong-Jeun;Bae, Jong-Ho;Kim, Sung;Choi, Hee-Jin;Han, Ho-Suk;Choi, Cheong
    • Journal of the Korean Society of Food Science and Nutrition
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    • v.32 no.1
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    • pp.119-123
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    • 2003
  • From the 80% ethanol extraction of onion flesh, fraction I,II and III were separated by Sephadex LH-20 column chromatography. Fraction II and III had a high inhibitory effect on ACE and xanthine oxidase. The ACE was about 80% at 50 ppm of fraction IIand III. The xanthine oxidase was about 82.5% at 100 ppm of fraction In. This research was studied to investigate the effects of the fraction In isolated from onion on the reduction of fat accumulation in rats fed high fat diet for 2 months. The metabolism was examined by analyzing the fat in serum and liver. It was shown that cholesterol in serum was remarkably reduced in onion fraction In as compared with those of control.

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

  • Cha, Woen-Suep;Bok, Su-Kyung;Kim, Myoung-Uk;Chun, Sung-Sook;Choi, Ung-Kyu;Cho, Young-Je
    • Applied Biological Chemistry
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    • v.43 no.4
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    • pp.247-252
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    • 2000
  • As functionality investigation of Korean traditional soybean fermentation foods, an antihypertensive peptide was separated during Chunggugjang fermentation by Bacillus subtilis CH-1023 and investigated inhibitory effect against angiotensin converting enzyme. After incubation at $20^{\circ}C,\;30^{\circ}C,\;40^{\circ}C,\;50^{\circ}C,\;60^{\circ}C$ for the $0{\sim}72$ hrs, protein content, protease activity and angiotensin converting enzyme inhibitory rate were determined. The protein content and protease activity were increased and reached maximum at 60 hrs fermentation with $40^{\circ}C$ and decreased after the 60 hrs fermentation. The optimum condition for antihypertensive peptide from Chunggugjang was appeared for 60 hrs at $40^{\circ}C$. Crude extract of Chunggugjang was partially purified by Amicon YM-3 membrane filtration and Sephadex G-10, G-25 gel filtration. The purified peptide showed inhibitory rate of 94.3% with 0.5 mg peptide content. The most prominent amino acid composition of the peptide from Chunggugjang was alanine, followed by phenylalanine, histidine.

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

  • Lee, Sung-Dong;Hwang, Woo-Ik;Okuda, Hiromichi
    • Journal of Ginseng Research
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    • v.20 no.3
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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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