• Title/Summary/Keyword: ACE inhibitory

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3D-QSAR of Angiotensin-Converting Enzyme Inhibitors: Functional Group Interaction Energy Descriptors for Quantitative Structure-Activity Relationships Study of ACE Inhibitors

  • Kim, Sang-Uk;Chi, Myung-Whan;Yoon, Chang-No;Sung, Ha-Chin
    • BMB Reports
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    • v.31 no.5
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    • pp.459-467
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    • 1998
  • A new set of functional group interaction energy descriptors relevant to the ACE (Angiotensin-Converting Enzyme) inhibitory peptide, QSAR (Quantitative Structure Activity Relationships), is presented. The functional group interaction energies approximate the charged interactions and distances between functional groups in molecules. The effective energies of the computationally derived geometries are useful parameters for deriving 3D-QSAR models, especially in the absence of experimentally known active site conformation. ACE is a regulatory zinc protease in the renin-angiotensin system. Therapeutic inhibition of this enzyme has proven to be a very effective treatment for the management of hypertension. The non bond interaction energy values among functional groups of six-feature of ACE inhibitory peptides were used as descriptor terms and analyzed for multivariate correlation with ACE inhibition activity. The functional group interaction energy descriptors used in the regression analysis were obtained by a series of inhibitor structures derived from molecular mechanics and semi-empirical calculations. The descriptors calculated using electrostatic and steric fields from the precisely defined functional group were sufficient to explain the biological activity of inhibitor. Application of the descriptors to the inhibition of ACE indicates that the derived QSAR has good predicting ability and provides insight into the mechanism of enzyme inhibition. The method, functional group interaction energy analysis, is expected to be applicable to predict enzyme inhibitory activity of the rationally designed inhibitors.

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Analysis of Nutritional Characteristics and Physiological Functionality of Hypsizygus marmoreus (Brown cultivar) (갈색 느티만가닥버섯의 영양특성 및 생리기능성 분석)

  • Bolormaa, Zanabaatar;Kang, Min-Gu;Seo, Geon-Sik;Lee, Young-Wook;Lee, Jong-Soo
    • The Korean Journal of Mycology
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    • v.40 no.2
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    • pp.104-108
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    • 2012
  • In order to apply into functional food or medicinal industry, nutritional characteristics and physiological functionality of Hypsizygus marmoreus (brown cultivar) were investigated. Fruiting body of H. marmoreus contained 27.3% of crude protein, 55.8% of total sugar and 11,109.3 mg/100 g dry weight of malic acid. Furthermore, 66.7% of antihypertensive angiotensin I-converting enzyme (ACE) inhibitory activity and 37.3% of antigout xanthin oxidase inhibitory activity showed in the water extract from H. marmoreus. The economically ACE inhibitory activity (81.4%) was obtained when the fruiting body of Hysizygus marmoreus was extracted with distilled water of $50^{\circ}C$ for 12 h, even though maximal ACE inhibitory activity (84.4%) was showed the extracts from $70^{\circ}C$ for 12 h.

ACE, α-Glucosidase and Cancer Cell Growth Inhibitory Activities of Extracts and Fractions from Marine Microalgae, Nannochloropsis oculata (해양 미세조류 Nannochloropsis oculata 추출.분획물의 ACE, α-glucosidase 및 암세포 저해 활성)

  • Cha, Seon-Heui;Kim, Min-Joo;Yang, Hye-Young;Jin, Chang-Beum;Jeon, You-Jin;Oda, Tatsuya;Kim, Dae-Kyung
    • Korean Journal of Fisheries and Aquatic Sciences
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    • v.43 no.5
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    • pp.437-444
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    • 2010
  • Extracts of the marine microalgae Nannochloropsis oculata were obtained using 80% methanol (MeOH) and water. The 80% MeOH extract was further fractionated with n-hexane, chloroform, ethyl acetate (EtOAc), n-butanol (n-BuOH), and water to isolate the active fraction. Seven samples were prepared and their angiotensin converting enzyme (ACE), $\alpha$-glucosidase, and cancer cell growth inhibitory activities in vitro were determined. The most profound ACE inhibitory activity was observed in the chloroform fraction, while the others had moderate effects. By contrast, greater $\alpha$-glucosidase inhibitory activity was found in the EtOAc fraction, n-hexane fraction, and water extract of N. oculata. The antiproliferative effects of the extracts and fractions against HL-60, U937, CT-26, and SK-Hep1 cancer cells were also determined. The n-BuOH fraction had the strongest antiproliferative effects on CT-26 cells in a time-dependant manner (P<0.05). These results suggest that the extracts and fractions from N. oculata could be used as a potential functional food or as pharmaceutical ingredients.

Production of Antihypertensive Angiotensin I-Converting Enzyme Inhibitor from Malassezia pachydermatis G-14

  • Jeong, Seung-Chan;Kim, Jae-Ho;Kim, Na-Mi;Lee, Jong-Soo
    • Mycobiology
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    • v.33 no.3
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    • pp.142-146
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    • 2005
  • To produce a novel antihypertensive angiotensin I-converting enzyme (ACE) inhibitor from yeast, a yeast isolate, designated G-14 showing the highest ACE inhibitory activity was obtained and identified as Malassezia pachydermatis based on morphological, biochemical and cultural characteristics. The maximal extracellular ACE inhibitor production was obtained from M. pachydermatis G-14 when the strain was cultured in YEPD medium containing 0.5% yeast extract, 3.0% peptone and 2.0% glucose at $30^{\circ}C$ for 24 h and the final ACE inhibitory activity was 48.9% under the above condition.

Isolation of ACE Inhibiting Peptide from Thermolysin Hydrolysate of Manila clam, Ruditapes philippinarum Proteins

  • Lee, Tae-Gee;Yeum, Dong-Min;Kim, Jin-Soo;Kim, In-Soo;Kim, Seon-Bong
    • Proceedings of the Korean Society of Fisheries Technology Conference
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    • 2002.10a
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    • pp.90-91
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    • 2002
  • The angiotensin converting enzyme (ACE) generates the powerful vasoconstrictor angiotensin II by removing the C-terminal dipeptide from the precursor decapeptide angiotensin I (1). The enzyme also inactivates the vasodilator bradykinin (2). There have been many studies on ACE inhibitory substances as functional in food, and ACE inhibitory peptides were isolated (3-5). (omitted)

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Isolation of Angiotensin Converting Enzyme Inhibitory Component from the Seeds of Xanthium strumarium (창이자(蒼耳子)로부터 안지오텐신 전환효소 억제 유효 성분의 분리)

  • Lee, Yun-Mi;Kang, Dae-Gill;Kim, Myung-Gyu;Jang, Ji-Yeon;Lee, Ho-Sub
    • Journal of Physiology & Pathology in Korean Medicine
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    • v.19 no.1
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    • pp.119-123
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    • 2005
  • In the courses of in vitro screening for the angiotensin converting enzyme (ACE) inhibitory activity of the various extracts from medicinal plants, n-BuOH soluble extract of the seeds of Xanthium strumarium was found to exhibit distinctive angiotensin converting enzyme (ACE) inhibitory activity. Bioassay-guided fractionation and purification of the n-BuOH soluble extract of the seeds of Xanthium strumarium afforded a new $xanthiazone-11-{\beta}-glucopyranoside$. The ACE activity was significantly inhibited by the addition of a new $xanthiazone-11-{\beta}-glucopyranosidein$ a dose-dependent manner of which $IC_{50}$ value was $21.8\;{\mu}g/ml$.

Physiological Activities of Saccharified Cherry Tomato Gruel Containing Different Levels of Cherry Tomato Puree (방울토마토 첨가량을 달리한 당화 방울토마토죽의 항산화 및 ACE 저해 효과)

  • Kim, Jin Sook;Kim, Ja Young;Chang, Young Eun
    • Korean journal of food and cookery science
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    • v.28 no.6
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    • pp.773-779
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    • 2012
  • This study was conducted to investigate the physiological activities of saccharified cherry tomato gruel containing different levels(0, 15, 30, and 45%) of cherry tomato puree. The total phenolic compound and flavonoids contents of saccharified cherry tomato gruel with cherry tomato puree were 1.73-5.09 mg/g and 0.28-7.01 mg/g, respectively. DPPH radical scavenging activities of saccharified cherry tomato gruel with cherry tomato puree were 8.67-92.58%, respectively. The ABTS radical scavenging activities of saccharified cherry tomato gruel with cherry tomato puree ranged from 6.02 to 61.59%. The ACE inhibitory activity of cherry tomato rice gruel increased with cherry tomato puree showed a range of 38.85-62.15%, respectively. With increasing additions of cherry tomato puree, the total phenolic compound and flavonoid contents, DPPH and ABTS radical scavenging activities and, ACE inhibitory activities were increased significantly (p<0.05). In conclusion, saccharified cherry tomato gruel could be used as a gruel processing method to in order to increase the functional values of gruels.

ACE Inhibitory and Antihypertensive Effect of Chitosan Oligosaccharides in SHR (Chitosan 올리고당의 안지오텐신 전환효소 활성 억제 및 SHR에서의 고혈압 억제 특성)

  • Hong, Sang-Pill;Kim, Myung-Hee;Oh, Se-Wook;Han, Chan-Kyu;Kim, Yong-Hyun
    • Korean Journal of Food Science and Technology
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    • v.30 no.6
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    • pp.1476-1479
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    • 1998
  • Effect of chitosan oligosaccharides on the ACE (angiotensin I converting enzyme) inhibition and antihypertension in SHR (Spontaneously hypertensive rat) was examined. The ACE inhibition activity was observed in all the chitosan oligosaccharides used in this study, and chitosan trimer exhibited the highest inhibitory activity $(IC_{50}=0.9{\mu}M)$ compared with other chitosan oligosaccharides $(IC_{50}\;:\;2.4{\sim}100\;{\mu}M)$. The results suggested that chitosan trimer was a good inhibitor of ACE in molecular level. When the single oral dose (2.14 mg/kg, similar to dose level of Captopril, known as strong ACE inhibitor) of chitosan trimer was given to 8 or 21 week aged SHR, the blood pressure reduction of both SHRs in 4hrs were $27{\pm}4.8\;mmHg\;and\;36{\pm}4.3\;mmHg$, respectively. Therefore, it was suggested that chitosan trimer could be applicable as natural ACE inhibitor related to antihypertension.

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Screening of Extracts from Marine Green and Brown Algae in Jeju for Potential Marine Angiotensin-I Converting Enzyme (ACE) Inhibitory Activity (제주 자생 해양 녹조류와 갈조류 추출물로부터의 항고혈압 활성)

  • Cha, Seon-Heui;Ahn, Gin-Nae;Heo, Soo-Jin;Kim, Kil-Nam;Lee, Ki-Wan;Song, Choon-Bok;K.Cho, So-Mi;Jeon, You-Jin
    • Journal of the Korean Society of Food Science and Nutrition
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    • v.35 no.3
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    • pp.307-314
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    • 2006
  • This study was conducted to screen in vitro angiotensin converting enzyme (ACE) inhibitory activities of methanol (MeOH) and aqueous extracts which were prepared by four different extractions-80% methanol extracts(ME) at $20^{\circ}C\;and\;70^{\circ}C$, respectively and aqueous extracts (AE) at both temperatures with the residue of the MEs-of ten marine green algae and nineteen brown algae collected along Jeju coast of Korea. Most marine brown algae extracts showed higher capacities than those of marine green algae in ACE inhibitory activity. Particularly, $70^{\circ}C$ MeOH extract (70ME) of Hizikia fusiforme showed the strongest inhibition activity (about 87%) among all the extracts. Also, 70 MEs of Enteromorpha linza, Ishige sinicola, Laminaria ochotensis, Petrospongium rugosum, Sagrassum horneri, Undaria pinnatifida and $20^{\circ}C$ MeOH extracts (20ME) of Myagropsis myagroides, Petrospongium rugosum, $20^{\circ}C$ aqueous extracts (20AE) of Codium contractum, Enteromorpha compressa, and $70^{\circ}C$ aqueous extracts (70AE) of Ecklonia cava, Petrospongium rugosum showed moderate ACE inhibitory activities more than 50% and the other extracts exhibited weak activities. On tile other hand, E. cava had the best ACE inhibitory activity among 70AEs. This indicates that 70AE of E. cava contains potential anti-ACE macromolecular. We tried to proteolytic digest 70AE of E. cava to induce production of anti-ACE peptides from E. cava 70AE. The enzymes used are five pretenses including Kojizyme, Flavourzyme, Neutrase, Alcalase, and Protamex, which are food grade-commercial enzymes from Novo Co. Flavourzyme-digest of E. cava 70AE showed the highest inhibitory activity about 90%. And the five different enzymatic digests of the E. cava 70AE ranged from 2.33 to 3.56 ${\mu}g/mL$, respectively in $IC_{50}$ values of anti-ACE activity.

Antihypertensive Activity and Anti-gout Activity of Mushroom Sarcodon aspratus (능이버섯의 항고혈압 활성과 항통풍 활성)

  • Kang, Min-Gu;Bolormaa, Zanabaatar;Lee, Jong-Seok;Seo, Geon-Sik;Lee, Jong-Soo
    • The Korean Journal of Mycology
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    • v.39 no.1
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    • pp.53-56
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    • 2011
  • We collected wild mushroom, Sarcodon aspratus from Deogyu Mt. of Muju, Jeollabuk-do and physiological functionalities of its water extract were investigated. The water extracts from S. aspratus showed the highest antihypertensive angiotensin I-converting enzyme (ACE) inhibitory activity of 74.3% and also showed high anti-gout xanthine oxidase (XOD) inhibitory activity (59.6%). However, tyrosinase inhibitory activity was very low (17.3%), and antioxidant activity and SOD-likely activity were not detected. The ACE inhibitory activity of S. aspratus fruiting body was the highest when powder of the fruiting body was shaked at $30^{\circ}C$ for 24 h by distilled water. Furthermore, the XOD inhibitory activity was also the highest by extraction at $50^{\circ}C$ for 24 h with water.