• Archives of Pharmacal Research
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• v.21 no.2
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• pp.168-173
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• 1998

The epoxyalkanoyl derivatives were designed and synthesized as ACE inhibitors. Coupling of unsaturated carboxylic acids with amino acids and following epoxidation with dimethyldioxirane gave the epoxyalkanoyls with high yield. The inhibitory activity of synthesized compounds on angiotensin converting enzyme was $IC_{50}$ values of 0.06~5.5 ${\mu}M$.

• Bulletin of the Korean Chemical Society
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• v.30 no.8
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• pp.1760-1766
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• 2009

Enzymatic syntheses of water soluble Bakuchiol glycosides were carried out in di-isopropyl ether organic media using amyloglucosidase from Rhizopus mold. The reactions were carried out under conventional reflux conditions and in supercritical $CO_2$ atmospheric conditions. Out of the eleven carbohydrate molecules employed for the reaction, D-glucose, D-ribose and D-arabinose gave glycosides in yields of 9.0% to 51.4% under conventional reflux conditions. Under supercritical $CO_2$ atmosphere (100 bar pressure at 50 ${^{\circ}C}$), bakuchiol formed glycosides with Dglucose, D-galactose, D-mannose, D-fructose, D-ribose, D-arabinose, D-sorbitol and D-mannitol in yields ranging from 9% to 46.6%. Out of the bakuchiol glycosides prepared, 6-O-(6-D-fructofruranosyl)bakuchiol showed the best antioxidant (1.4 mM) and ACE inhibitory activities (0.64 mM).

• Korean Journal of Fisheries and Aquatic Sciences
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• v.25 no.3
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• pp.229-235
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• 1992

Fish protein hydrolysates(FPH) prepared from defatted mackerel meal by proteases such as complex enzymes, bromelain, alcalase, $\alpha-chymotrypsin,$ trypsin, papain and pepsin were tested for inhibitory activity against angiotensin-I converting enzyme(ACE). Among proteases tested, the hydrolysates obtained from the treatment of complex enzymes or bromelain showed relatively higher activity. ACE inhibitory activity of the hydrolysates increased until hydrolysis of 8 hrs, and was stable by heat treatment for 20min at $100^{\circ}C.$ From the profiles of fractionation of the hydrolysates with Bio-gel P-2, the most active fraction had about MW 1,450 and it's amino acid was abundant in Asp, Glu, Lys, Leu, Val and Ala. $IC_{50}\;(amounts\;of\;inhibitors\;needed\;for\;50\%\;inhibition)$ of the active fraction of the hydrolysates obtained from the treatment of complex enzyme and bromelain was 90 and $130 {\mu}g,$ respectively.

• Food Science of Animal Resources
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• v.32 no.5
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• pp.652-658
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• 2012

This study was carried out to identify the ACE (Angiotensin converting enzyme) inhibitory activity of casein hydrolysates for development of anti-hypertensive hydrolysates. Sodium caseinate was treated with six kinds of commercial proteases such as Flavourzyme, Protamex, Neutrase 1.5, Alcalase, Protease M, and Protease S for 8 h individually, and was then treated with the enzyme combination for 4 h at $45^{\circ}C$. The hydrolysate which had the highest ACE inhibitory effect was then hydrolysed successively with three digestive enzymes: pepsin, trypsin, and ${\alpha}$-chymotrypsin, at $37^{\circ}C$ for 4 h under conditions mimicking those of the gastrointestinal tract. UF (ultra filtration) treatment was applied to one of the secondary hydrolysates to determine ACE inhibitory activity. When sodium caseinate was hydrolysed by commercial proteases, the degree of hydrolysis (DH) showed 2.54 to 4.25% and after secondary hydrolysis, DH showed 4.30 to 5.22%. ACE inhibitory activity and $IC_{50}$ values decreased, and inhibition rates increased during hydrolysis. Protamex treatment showed the lowest $IC_{50}$ value ($516{\mu}g/mL$) and Flavourzyme hydrolysate showed the highest $IC_{50}$value ($866{\mu}g/mL$). As the first hydrolysate was treated with Flavourzyme, the ACE inhibitory activity increased. Neutrase hydrolysate had the highest activity with an $IC_{50}$ value ($282{\mu}g/mL$). When Neutrase plus Flavourzyme treatment was hydrolyzed by digestive enzymes, the $IC_{50}$ value ($597{\mu}g/mL$) was decreased statistically (p<0.05). As Neutrase plus Flavourzyme hydrolysate is treated by UF with MW cut-off 10,000, permeate showed $273{\mu}g/mL$ of $IC_{50}$ value, showed no difference, but retentate which has over MW 10,000 showed statistically different $IC_{50}$ value, $635{\mu}g/mL$ (p<0.05).

• The Korean Journal of Food And Nutrition
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• v.30 no.1
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• pp.59-66
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• 2017

This study investigated the quality characteristics and biological activities of rice germ fermented by Bacillus spp. During the milling process, the contents of rice germ in the rice bran (Control) were adjusted to 30% (RG30) and 70% (RG70). The approximate composition, pH, total acidity, total soluble solid, total sugar, polyphenol and flavonoid contents were measured. DPPH radical scavenging activity, xanthine oxidase (XO) and angiotensin converting enzyme (ACE) activities were also determined. We observed that the moisture content decreased after fermentation, while the crude protein was significantly increased. Fermentation remarkably lowered the pH from 5.83~6.26 to 4.77~4.93, thereby elevating the total acidity. Fermentation also increased the total solid contents, from $0.40{\sim}0.87^{\circ}Bx$ to $1.63{\sim}2.20^{\circ}Bx$. The total sugar decreased to 136.81~151.53 mg/mL from 377.56~450.64 mg/mL. Polyphenol contents were the highest in control (0.59 and 0.73 mg/mL before and after fermentation, respectively). Fermentation significantly affected the increase of the polyphenols in both rice germ 30% and 70% samples, from 0.26 and 0.28 mg GAE/g before fermentation, to 0.52 and 0.70 mg GAE/g after fermentation, respectively. There was a slight increase in the flavonoid contents after fermentation. The $IC_{50}$ value of the electron donating ability, as evaluated by the DPPH method, was the lowest in control (3.77 and 3.36 mg/mL before and after fermentation, respectively). Fermentation increased the XO inhibition activity up to 63.69% in control, 49.81% in rice germ 30%, and 59.32% in rice germ 70%. The ACE inhibition activities were also increased in the fermented control, rice germ 30% and 70%, to 40.51%, 22.69% and 33.91%, respectively.

• Journal of the Korean Society of Food Culture
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• v.19 no.1
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• pp.94-105
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• 2004

The biochemical components of Namcheondlggae, Miryangdlkkae 25, Boradlggae and Ipdlkkae 1 were measured. The samples were extracted with hot water, 60% acetone or 80% ethanol for screening physiological activity. The crude protein content (4.36%) was found in the Miryangdlkkae 25 and calcium content (497.5 mg%) was found in the Namcheondlggae among the tested 4 perilla loaves. Fructose was 30.86 mg% in the Namcheondlggae and free amino acids at all perilla leaves was detected seventeen. In Boradlggae, glutamic acid and alanine were 25.37 and 11.91 mg%. Totally nine non-volatile organic acids were also detected and the contents of malic acid and glutaric acid were 28.34 and 14.57 mg% in Boradlggae. The Miryangdlkkae 25 had the highest vitamin C amount which was 113.24 mg%. Angiotensin converting enzyme (ACE) inhibition activity of 60% acetone extract of Miryangdlkkae 25 was 39.20% when added as addition of 200 ppm level and xanthine oxidase inhibition activity of 80% ethanol extract of Boradlggae was 46.71%. Electron denoting activity of 60% acetone extract from Namcheohndlggae was the strongest inhibition activity as 98.19% when 200 ppm level of the sample extracts were added.

• Journal of Life Science
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• v.19 no.3
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• pp.390-396
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• 2009

In this study, extracts from S. officinalis were tested for antioxidative effects and inhibitory activities against $\alpha$-amylase, angiotensin converting enzyme (ACE) and xanthine oxidase (XOase). The content of total phenolic compounds in water, 60% ethanol, 60% methanol and 60% acetone extracts were 36.2, 42.7, 40.3 and 39.6 mg/g, respectively. In 60% ethanol extracts, the EDA by DPPH free radical scavenging test of S. officinalis was $66.3{\pm}2.2%$ at $200{\mu}g/ml$. The inhibition rate of ABTS was $97.6{\pm}0.1%$, the antioxidant protection factor was $2.26{\pm}0.63$ PF, and TBARS was $0.62{\pm}0.05$ (${\times}100{\mu}M$ in the control and $0.29{\pm}0.02$ (${\times}100{\mu}M$). Also in 60% ethanol extracts of S. officinalis, the inhibitory activity against XOase was 78% and was not shown to be against ACE. According to the $12.6{\pm}0.14\;mm$ of clear zone formed, the inhibition rate against $\alpha$-Amylase was 7.6% at $200{\mu}g/ml$ of phenolics content. Antimicrobial activities of 60% ethanol extracts of S. officinalis against Helicobacter pylori exhibited an inhibition rate of $12.5{\sim}66.1%$ according to the $10{\sim}15\;mm$ of clear zone at $50{\sim}200{\mu}g/ml$. The results suggest that the 60% ethanol extracts from Salvia officinalis L. will be useful as natural antioxidants and functional food sources.

• Asian Pacific Journal of Cancer Prevention
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• v.16 no.7
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• pp.2939-2946
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• 2015

Many of the anti-cancer agents currently used have an origin in natural sources including plants. Aloe vera is one such plant being studied extensively for its diverse health benefits, including cancer prevention. In this study, the cytotoxic potential of Aloe vera crude extract (ACE) alone or in combination with cisplatin in human breast (MCF-7) and cervical (HeLa) cancer cells was studied by cell viability assay, nuclear morphological examination and cell cycle analysis. Effects were correlated with modulation of expression of genes involved in cell cycle regulation, apoptosis and drug metabolism by RT-PCR. Exposure of cells to ACE resulted in considerable loss of cell viability in a dose- and time-dependent fashion, which was found to be mediated by through the apoptotic pathway as evidenced by changes in the nuclear morphology and the distribution of cells in the different phases of the cell cycle. Interestingly, ACE did not have any significant cytotoxicity towards normal cells, thus placing it in the category of safe chemopreventive agent. Further, the effects were correlated with the downregulation of cyclin D1, CYP 1A1, CYP 1A2 and increased expression of bax and p21 in MCF-7 and HeLa cells. In addition, low dose combination of ACE and cisplatin showed a combination index less than 1, indicating synergistic growth inhibition compared to the agents applied individually. In conclusion, these results signify that Aloe vera may be an effective anti-neoplastic agent to inhibit cancer cell growth and increase the therapeutic efficacy of conventional drugs like cispolatin. Thus promoting the development of plant-derived therapeutic agents appears warranted for novel cancer treatment strategies.

• Food Science of Animal Resources
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• v.43 no.1
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• pp.46-60
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• 2023

Slaughterhouse blood is a by-product of animal slaughter that can be a good source of animal protein. This research purposed to examine the functional qualities of the blood plasma from Hanwoo cattle, black goat, and their hydrolysates. Part of the plasma was hydrolyzed with proteolytic enzymes (Bacillus protease, papain, thermolysin, elastase, and α-chymotrypsin) to yield bioactive peptides under optimum conditions. The levels of hydrolysates were evaluated by 15% sodium dodecyl sulfate polyacrylamide gel electrophoresis. The antioxidant, metal-chelating, and angiotensin I-converting enzyme (ACE) inhibitory properties of intact blood plasma and selected hydrolysates were investigated. Accordingly, two plasma hydrolysates by protease (pH 6.5/55℃/3 h) and thermolysin (pH 7.5/37℃/3-6 h) were selected for analysis of their functional properties. In the oil model system, only goat blood plasma had lower levels of thiobarbituric acid reactive substances than the control. The diphenyl picrylhydrazyl radical scavenging activity was higher in cattle and goat plasma than in proteolytic hydrolysates. Ironchelating activities increased after proteolytic degradation except for protease-treated cattle blood. Copper-chelating activity was excellent in all test samples except for the original bovine plasma. As for ACE inhibition, only non-hydrolyzed goat plasma and its hydrolysates by thermolysin showed ACE inhibitory activity (9.86±5.03% and 21.77±3.74%). In conclusion, goat plasma without hydrolyzation and its hydrolysates can be a good source of bioactive compounds with functional characteristics, whereas cattle plasma has a relatively low value. Further studies on the molecular structure of these compounds are needed with more suitable enzyme combinations.

• Journal of Life Science
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• v.24 no.3
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• pp.304-310
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• 2014

Antioxidative, immunostimulating, and antihypertensive activities of hot water extracts of fermented Hizikia fusiformis were evaluated. Fermentation with lactic acid bacteria generally increased the biological activities of H. fusiformis. Fermentation with isolated Weissella sp. SH-1 resulted in 13.83-62.15% DPPH radical scavenging activity and 34.90-59.25% SOD-like activity. The maximal inhibition of ACE was 82.25%, and the maximal reduction in NO production was 46.53%. Fermentation with Lactobacillus casei resulted in 11.98-72.84% DPPH radical scavenging activity and 14.17-33.62% of SOD-like activity. The maximal inhibition of ACE was 73.31%, and the maximal reduction in NO production was 65.20%. These results hint at the applicability of fermentation with lactic acid bacteria to improve the diverse biological activities of H. fusiformis and to develop functional materials or foods.