• Korean Journal of Food Science and Technology
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• v.34 no.4
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• pp.737-740
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• 2002

To determine the relations between antihypertensive effect and ${\gamma}-aminobutyric$ acid, mycelial weight and pigment of Monascus, ethanol koji extracts were prepared from Monascus koji and each of three grade was classified based on ${\gamma}-aminobutyric$ acid content, glucosamine content and hue angle value, respectively. Each extract was orally administrated on male spontaneously hypertensive rats and its antihypertensive effect was compared. Most of koji extracts showed antihypertensive activity regardless of their ${\gamma}-aminobutyric$ acid content, glucosamine content or hue angle value. Therefore, hypotensive activity of koji extract was not dependent on above three components.

• Food Science of Animal Resources
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• v.43 no.1
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• pp.184-194
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• 2023

Recently, interest in food-derived bioactive peptides as promising ingredients for the prevention and improvement of hypertension is increasing. The purpose of this study was to determine the structure and antihypertensive effect of an antioxidant peptide purified from velvet antler in a previous study and evaluate its potential as a various bioactive peptide. Molecular weight (MW) and amino acid sequences of the purified peptide were determined by quadrupole time-of-flight electrospray ionization mass spectroscopy. The angiotensin I-converting enzyme (ACE) inhibition activity of the purified peptide was assessed by enzyme reaction methods and in silico molecular docking analysis to determine the interaction between the purified peptide and ACE. Also, antihypertensive effect of the purified peptide in spontaneously hypertensive rats (SHRs) was investigated. The purified antioxidant peptide was identified to be a pentapeptide Asp-Asn-Arg-Tyr-Tyr with a MW of 730.31 Da. This pentapeptide showed potent inhibition activity against ACE (IC₅₀ value, 3.72 μM). Molecular docking studies revealed a good and stable binding affinity between purified peptide and ACE and indicated that the purified peptide could interact with HOH2570, ARG522, ARG124, GLU143, HIS387, TRP357, and GLU403 residues of ACE. Furthermore, oral administration of the pentapeptide significantly reduced blood pressure in SHRs. The pentapeptide derived from enzymatic hydrolysate of velvet antler is an excellent ACE inhibitor. It might be effectively applied as an animal-based functional food ingredient.

• Journal of Medicine and Life Science
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• v.19 no.3
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• pp.79-89
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• 2022

Whereas systolic blood pressure (SBP) continuously rises with age, diastolic blood pressure (DBP) gradually decreases after the age of 55 years. Therefore, hypertension in the elderly shows the pattern of isolated systolic hypertension. There is evidence on the benefits of controlling blood pressure (BP) in elderly patients with hypertension. The BP lowering effect has also been demonstrated in patients over 80 years of age with hypertension. The BP threshold for the initiation of antihypertensive drug treatment for older adults with hypertension is gradually decreasing. The antihypertensive treatment is recommended if, despite therapeutic lifestyle modifications, SBP ≥140 mmHg or DBP ≥90 mmHg in those aged 65-79 years old, and SBP ≥140-160 mmHg or DBP ≥90 mmHg in those aged ≥80 years old. Although there is no consensus on the target BP for older adults with hypertension, a target SBP of <130-140 mmHg and DBP of <80-90 mmHg are recommended. In older adults over 80 years of age with hypertension, the target SBP is <140-150 mmHg. When the dose of antihypertensive drugs is increased to reach the target SBP, DBP may decrease to less than 70 mmHg, but it should not be <60 mmHg. Thiazide diuretics, calcium channel blockers, angiotensin-converting enzyme inhibitors, or angiotensin receptor blockers can be selected as the first-line drug for older adults with hypertension. Beta-blockers may be selected in case of compelling indications.

• Food Science of Animal Resources
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• v.35 no.6
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• pp.738-747
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• 2015

Angiotensin-converting enzyme (ACE) inhibitory activity was evaluated for the low-molecular-weight fraction (<3 kDa) obtained from milk fermentation by Bifidobacterium longum KACC91563. The ACE inhibitory activity in this fraction was 62.3%. The peptides generated from the <3 kDa fraction were identified by liquid chromatography-electrospray ionization quantitative time-of-flight mass spectrometry analysis. Of the 28 peptides identified, 11 and 16 were identified as β-casein (CN) and α_s1-CN, respectively. One peptide was identified as κ-CN. Three peptides, YQEPVLGPVRGPFPIIV, QEPVLGPVRGPFPIIV, and GPVRGPFPIIV, from β-CN corresponded to known antihypertensive peptides. We also found 15 peptides that were identified as potential antihypertensive peptides because they included a known antihypertensive peptide fragment. These peptides were as follows: RELEELNVPGEIVE (f1-14), YQEPVLGPVRGPFP (f193-206), EPVLGPVRGPFPIIV (f195-206), PVLGPVRGPFPIIV (f196-206), VLGPVRGPFPIIV (f197-206), and LGPVRGPFPIIV (f198-206) for β-CN; and APSFSDIPNPIGSENSEKTTMPLW (f176-199), SFSDIPNPIGSENSEKT- TMPLW (f178-199), FSDIPNPIGSENSEKTTMPLW (f179-199), SDIPNPIGSENSEKTTMPLW (f180-199), DIPNPIGSENSEKTTMPLW (f181-199), IPNPIGSENSEKTTMPLW (f182-199), PIGSENSEKTTMPLW (f185-199), IGSENSEKTTMPLW (f186-199), and SENSEKTTMPLW (f188-199) for α_s1-CN. From these results, B. longum could be used as a starter culture in combination with other lactic acid bacteria in the dairy industry, and/or these peptides could be used in functional food manufacturing as additives for the development of a product with beneficial effects for human health.

• Biomolecules & Therapeutics
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• v.15 no.1
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• pp.40-45
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• 2007

The vascular relaxant effects on isolated rat aorta of amlodipine camsylates (S-, R-enantiomer, and R/S-racemate), were evaluated and compared with that of S-amlodipine besylate. Furthermore, antihypertensive effects were measured in spontaneously hypertensive rat (SHR). The S-amlodipine camsylate concentration-dependently inhibited $Ca^{2+}$-induced contraction of rat aorta with a very slow onset of action (reached its maximum at 3.5h; $ED_{50}:\;1.50\;{\pm}\;0.24$ nM), having a potency 2-fold higher than those of R/S-amlodipine camsylate $(ED_{50}:\;3.36\;{\pm}\;0.91\;nM)$ and similar to those of S-amlodipine besylate $(ED_{50}:\;1.44\;{\pm}\;0.14\;nM)$, whereas the R-amlodipine camsylate has 590-fold lower vasorelaxant activity $(ED_{50}:\;886.4\;{\pm}\;49.7\;nM)$. In SHR, orally administered S-amlodipine camsylate produced a dose-dependent and long-lasting (>>10 h) antihypertensive effect $(ED_{20}:\;0.89\;mg/kg)$, with a potency 2-fold higher than those of R/S-amlodipine camsylate $(ED_{20}:\;1.82\;mg/kg)$ and similar to those of S-amlodipine besylate $(ED_{20}:\;0.71\;mg/kg)$. In contrast, the R-amlodipine camsylate has no effect even-though administrated high concentration 10 mg/kg. These results suggest that S-amlodipine camsylate has the potency and long-lasting antihypertensive activity as single enantiomer drug, and its antihypertensive effect is not significantly different to that of S-amlodipine besylate.

• The Journal of Internal Korean Medicine
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• v.38 no.6
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• pp.902-916
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• 2017

Objectives: The aim of this study was to review the clinical research on antihypertensive effects of Korean herbal medicines that function by inducing diuresis. Methods: Literature searches were performed using PubMed, Cochrane, CNKI, Wanfang, Cinii, Oasis, KISS, NDSL, RISS, DBPia, with the keywords "利水", "利尿", "高血壓", "hypertension", and "lishui." The search range included only randomized controlled trials that verified the effects of Korean herbal medicine interventions on hypertension. The selected studies were assessed by risk of bias (RoB). Results: 26 reports were selected from a total of 532 identified. For these reports, meta-analysis was performed using Revman 5.3. From this analysis, it was observed that the combined treatment of Korean medicine and antihypertensive drugs had a significantly higher total effective rate (TER) and improvement in systolic blood pressure (SBP) and diastolic blood pressure (DBP) than did the use of a single antihypertensive drug. The risk ratio of TER for lowering blood pressure was 1.25. The mean differences of SBP, DBP were -19.63 mm Hg (95% confidential interval (CI), -22.45 mm Hg, -16.80 mm Hg, p<0.00001), and -5.39 mm Hg (95% CI, -7.36 mm Hg, -3.42 mm Hg, p<0.00001) respectively. The use of Korean medicine only did not improve blood pressure, as compared to the use of an antihypertensive drug. Most of items of RoB were unclear, and the methodological quality was low. Conclusions: The combination of antihypertensive drugs and Korean medical treatment can effectively improve SBP, DBP, and TER. This finding could be widely utilized in clinical practice in Korean medicine.

• The Journal of Internal Korean Medicine
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• v.38 no.4
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• pp.443-454
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• 2017

Objectives: This study assessed the application of Oryung-san (Wuling-san or Gorei-san), a common diuretic in traditional medicine, as an antihypertensive agent. Methods: Experimental studies of the pharmacological properties of Oryung-san, including diuretic action and lowering effects on blood pressure, and toxicology and clinical trials were reviewed. Results: In pharmacology, various, relatively safe diuretics are used to lower blood pressure and are the oldest and most studied antihypertensive agents. Despite many new drug approvals, antihypertensive diuretics are frequently used in Korea and Japan where high levels of sodium uptake are common. Oryung-san has been demonstrated to have diuretic, antihypertensive, and nephroprotective effects. Conclusions: Oryung-san might be effective for lowering blood pressure based on the results of this literature review. Further evaluations and large-scale clinical trials of Oryung-san to treat primary hypertension are warranted.

• Archives of Pharmacal Research
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• v.14 no.3
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• pp.242-248
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• 1991

Antihypertensive effect of YH 334 was examined in various experimental hypertension rat models and the systemic and regional hymohynamic profiles of the compound were investigated in conscious spontaneously hypertensive rats (SHR). The antiypertensive potensive potency of YH 334 is found to be more than 10 times stronger than that of nitrendipine in the all hypertensive models. The effective doses to lower the initial blood pressure by 20% $(ED_{20})$ of YH334 were 1.4 mg/kg in normotensive rats (NR), 0.7 mglkg in SHR. 0.1 mg/kg in DOCA salt hypertensive rats (DHR) and 0.4 mg/kg in renal hypertensive rats (RHR), and the $ED_{20}$ values of nitrendipine were 15.8 mg/kg in NR, 7.1 mg/kg in SHR, 1.7 mg/kg in DHR and 4.8 mg/kg in RHR. The primary hemodynamic effect hemodynamic profile is similar to that of nitrendipine. Both compounds seem to produce potent antihypertensive effects by lowering peripheral resistance in the skeletal muscles. In the organ bath study using isolated rabbit aorta, YH 334 was found to be a potent voltage dependent calcium channel blocker without significant inhibitory effect on the receptor operated calcium channels like the most of other dihydropyridine type calcium antagonists. Furthermore, YH334 showed acute diuretic and natriuretic effects in conscious SHR, which may render the unnecessary restriction of sodium in the diet of those patients on long term hypertension therapy. This effect would provide an additional benefit to its potent antihypertensive activity.

• Environmental Mutagens and Carcinogens
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• v.18 no.2
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• pp.123-128
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• 1998

To evaluate the genotoxicity of SKP-450, an antihypertensive agent the in vitro reverse mutation assay using Salmonella typhimurium, the Chromosome aberration assay using Chinese hamster lung (CHL) cells and the in vivo micronucleus assay using bone marrow cells of ddY mice were performed. In the Reverse mutation test, SKP-450 did not induced mutagenicity in Salmonella typhimurium TA 98, TA 100, TA 1535 and TA 1537 with and without metabolic activation. In the chromosome aberration assay using CHL cells, there was no increased incidence of structural and numerical aberrations with and without metabolic activation. The in vivo induction of micronuclei was measured in polychromatic erythrocytes of bone marrow of male ddY mice at 30 hours after treatment with SKP-450 by p.o once. The results showed no increased incidence of micronucleated polychromatic erythrocytes in bone marrow of ddY male mice treated with SKP-450.

• YAKHAK HOEJI
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• v.31 no.2
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• pp.82-91
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• 1987

The effect of neurotoxic compound 6-hydroxydopamine (6-OHDA) on the change in blood pressure and contractile response of Vas deference by centrally acting agents has been studied in normal and DOCA-salt induced hypertensive rats. The treatment of neonatal rats with 6-OHDA (2$\times$100mg, 250mg Kg$^{-1}$s.c) significantly inhibited the antihypertensive and relaxant effects of Vas deference of clonidine(100$\mu\textrm{g}$ Kg$^{-1}$iv.). The simultaneous administration of desipramine with clonidine into neonatal rats decreased the antihypertensive response of clonidine although treated did not affect the relaxative response of Vas deference. Furthermore, the antihypertensive and relaxant responses of clonidine were reduced by the neonatal rats with 6-OHDA regardless of the administration of desipramine. When neonatal rats were administered with 6-OHDA, the development of DOCA-salt hypertension was prevented. These results suggest that 6-OHDA, clonidine and desipramine hada significant effect on the development and the inhibition of central hypertension mediating the central adrenergic neuron due to their affinity to the central nervous system.