• Journal of Microbiology and Biotechnology
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• v.26 no.10
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• pp.1675-1686
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• 2016

We characterized the probiotic properties of Lactobacillus helveticus strains KII13 and KHI1 isolated from fermented cow milk by in vitro and in vivo studies. The strains exhibited tolerance to simulated orogastrointestinal condition, adherence to Caco-2 cells, and antimicrobial activity. Both L. helveticus strains produced bioactive tripeptides, isoleucylprolyl-proline and valyl-prolyl-proline, during fermentation of milk. KII13 showed higher in vitro cholesterol-lowering activity (47%) compared with KHI1 (28%) and L. helveticus ATCC 15009 (22%), and hence, it was selected for in vivo study of cholesterol-lowering activity in atherogenic diet-fed hypercholesterolemic mice. For the study, mice were divided into four groups (viz., normal diet control group, atherogenic diet control group (HCD), KII13-atherogenic diet group (HCD-KII13), and Lactobacillus acidophilus ATCC 43121-atherogenic diet group (HCD-L.ac) as positive control). The serum total cholesterol level was significantly decreased by 8.6% and 7.78% in the HCD-KII13 and HCD-L.ac groups (p < 0.05), respectively, compared with the HCD group. Low-density lipoprotein cholesterol levels in both HCD-KII13 and HCD-L.ac groups were decreased by 13% and 11%, respectively, compared with the HCD group (both, p < 0.05). Analysis of cholesterol metabolism-related gene expression in mice liver showed increased expression of LDLR and SREBF2 genes in mice fed with KII13. By comparing all the results, we conclude that L. helveticus KII13 could be used as a potential probiotic strain to produce antihypertensive peptides and reduce serum cholesterol.

• 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.

• 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.

• Journal of the Korean Society of Food Science and Nutrition
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• v.40 no.3
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• pp.350-356
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• 2011

Styela plicata of large (9.82~11.66 g) and small (0.93~2.21 g) sizes harvested at different times was extracted with 4 different solvents (methanol, ethanol, acetone, and water). DPPH radical scavenging and reducing power was the highest in acetone extracts of small ones (38.98% and 1.724, respectively) harvested in November. The lowest radical scavenging activity was found in water extracts of large ones (12.03% and 0.114) in December. On the other hand, large ones harvested in September showed significantly higher inhibition rate of DNA damage (water, 56.54%; methanol, 55.83%; ethanol, 48.63%) than others. Overall, the water extraction of S. plicata tended to show a higher antigenotoxic effect. In addition, water extracts of large S. plicata from November showed the highest angiotensin converting enzyme (ACE) inhibitory activity (64.38%), while that of small ones from December exhibited the lowest (51.33%). Overall the results indicate that antioxidant and antihypertensive activities S. plicata are variable depending on harvesting time, size, and extraction solvent.

• Mycobiology
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• v.36 no.3
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• pp.148-151
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• 2008

A novel biomass was prepared from Pichia anomala KCCM 11473, which grew well in ginseng-steaming effluent (GSE), and its physiological functionalities and enzyme activities were determined. When the strain was cultured in the GSE (pH 6.0) at 30$^{\circ}C$ for 48 h, 1.6 mg of biomass per ml-cultures was produced. The cell-free extract of the biomass showed high antihypertensive angiotensin I-converting enzyme inhibitory activity of 72.0% and anticholesteromia HMG-CoA reductase inhibitory activity of 46.5%. The cell-free extract also showed 13.0 U per ml and 8.5 U per ml of neutral protease activity and alkaline protease, respectively.

• Proceedings of the Korean Society of Fisheries Technology Conference
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• 2000.05a
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• pp.416-417
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• 2000

Chitin, a poly $\beta$-(1longrightarrow14)-N-acetyl-D-glucosamine, is best known as a cell wall component of fungi and as a skeletal materials of invertebrates. Chitosan is derived from chitin by deacetylation in the presence of alkali. Chitosan has been developed as new physiological materials since it possesses antibacterial activity, hypocholesterolemic activity and antihypertensive action. However, the actions of chitosan in vivo still remain ambiguous as the physiological functional properties because most animal intestines, especially the human gastrointestinal tract, do not possess enzyme such as chitosanase which directly degrade the $\beta$-glucosidic linkage in chitosan, and consequently the unbroken polymers may be poorly absorbed into the human intestine. Therefore, recent studies as chitosan have attracted interest for chitosan oligosaccharides, because the oligosaccharides process not only water-soluble property but also versatile functional properties such as antitumor activity, immune-enhancing effects, enhancement of protective effects against infection with some pathogens in mice and antimicrobial activity (Kingsnorth et al., 1983, Mori et al., 1997). (omitted)

• Journal of Microbiology and Biotechnology
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• v.17 no.6
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• pp.952-959
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• 2007

His-His-Leu (HHL), a tripeptide derived from a Korean soybean paste, is an angiotensin-I-converting enzyme (ACE) inhibitor. We report here a method of producing this tripeptide efficiently by expressing tandem multimers of the codons encoding the peptide in E. coli and purifying the HHL after hydrolysis of the peptide multimers. The HHL gene, tandemly multimerized to a 40-mer, was ligated with ubiquitin as a fusion gene (UH40). UH40 was inserted into vector pET29b; the UH40 fusion protein was then produced in E. coli BL21. The recombinant UH40 protein was purified by cation-exchange chromatography with a yield of 17.3mg/l and analyzed by matrixassisted laser desorption ionization (MALDI) time-of-flight (TOF) mass spectrometry and protein N-terminal sequencing. Leucine aminopeptidase was used to cleave a 405-Da HHL monomer from the UH40 fusion protein and the peptide was purified using reverse-phase high-performance liquid chromatography (HPLC) on a C18 HPLC column, with a final yield of 6.2mg/l. The resulting peptide was confirmed to be HHL with the aid of MALDI-TOF mass spectrometry, glutamine-TOF mass spectrometry, N-terminal sequencing, and measurement of ACE inhibiting activity. These results suggest that our production method is useful for obtaining a large quantity of recombinant HHL for functional antihypertensive peptide studies.

• Journal of the Korea Academia-Industrial cooperation Society
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• v.10 no.11
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• pp.3473-3479
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• 2009

The pharmacological profile of KR-31081, a newly synthesized AT1 receptor antagonist, was evaluated in pithed rats, conscious renal hypertensive rats (RHRs) and conscious furosemide-treated beagle dogs. In pithed rats, KR-31081 (i.v.) induced a non-parallel right shift in the dose-pressor response curve to angiotensin II (ID50: 0.05 mg/kg) with a dose-dependent reduction in the maximum responses; this antagonistic effect was about 40 times more potent than losartan (ID50: 1.74 mg/kg) which showed competitive antagonism. KR-31081 did not alter the responses induced by other agonists such as norepinephrine and vasopressin. In RHRs, orally given KR-31081 produced a dose-dependent and long-lasting (>24 h) antihypertensive effect with a higher potency to losartan (ED20: 0.30 and 3.36 mg/kg, respectively). In furosemide-treated dogs, orally given KR-31081 produced a dose-dependent and long-lasting (>8h) antihypertensive effect with a rapid onset of action (time to Emax: 1-1.5 h) and 20-fold greater potency than losartan (ED20: 0.41 and 8.13 mg/kg, respectively). These results suggest that KR-31081 is a potent, orally active AT1 receptor antagonist useful for the research and diagnostic tools as an added exploratory potential.

• The Korean Journal of Mycology
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• v.39 no.3
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• pp.194-197
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• 2011

Forty eight strains of yeast were cultured in potato dextorse(PD) broth at $30^{\circ}C$ for 24 hr and centrifuged with 12,000 rpm for 20 min. After concentrated the cultures, antihypertensive angiotensin I-converting enzyme(ACE) inhibitory activities of its concentrates were investigated. Among them, the concentrates from Saccharomyces cerevisiae Y183-3 showed the highest ACE inhibitory activity of 71.8%. The ACE inhibitor from Saccharomyces cerevisiae Y183-3 was maximally produced when Saccharomyces cerevisiae Y183-3 cultured in PD broth at $30^{\circ}C$ for 36 hr.

• Korean Journal of Medicinal Crop Science
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• v.15 no.6
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• pp.391-397
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• 2007

To develop new high valuable Gugija (Lycium chinensis), biofunctionalities of Gugija standard species and its hybrids were investigated and compared with each water extracts and methanol extracts from Lycii Fructus, Lycii Folium and buds and Lycii Cortex Radicis. Among various biofunctionalities of Gugija standard species, antioxidant activity was showed the highest in methanol extracts from buds of Cheongwoon species (93%) and antihypertensive angiotensin I-converting enzyme (ACE) inhibitory activity was 84.1% in the water extracts from Lycii Cortex Radicis of Cheongyang NO.7. Futhermore, methanol extracts from Lycii Cortex Radicis of Myungan A-2 hybrid showed 93.1% of antioxidant activity and 96.9% of ACE inhibitory activity was also showed in the methanol extracts from Lycii Fructus of DO148-72(A11) hybrid. However, fibrinolytic activity and anticholesteromia HMG-CoA reductase inhibitory activity were weak or not detected in almost of Gugija standard species and its hybrids. Therefore, we finally selected Cheongwoon Gugija standard species (buds) and Myungan A-2 hybrid (Lycii Cortex Radicis) as good antioxidant sources and also DO148-72 (A11) hybrid (Lycii Fructus) as excellent antihypertensive ACE inhibitior sources for manufacturing functional food product.