• Title/Summary/Keyword: Antihypertension

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Induction of Apoptosis by Ethanol Extract of Scutellaria baicalensis in Renal ell Carcinoma Caki-1 Cells (황금(黃芩) 에탄올 추출물에 의한 인체 신세포암 Caki-1 세포의 자가세포사멸 유도)

  • Hwang, Won Deok;Im, Yong-Gyun;Son, Byoung Yil;Park, Cheol;Park, Dong Il;Choi, Yung Hyun
    • Journal of Life Science
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    • v.23 no.4
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    • pp.518-528
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    • 2013
  • Scutellaria baicalensis, belonging to the family Labiatae, is widely distributed in Korea, China, Mongolia, and eastern Siberia. It has been used in traditional medicine for various diseases, such as dysentery, pyrexia, jaundice, and carbuncles. In addition, S. baicalensis is reported to possess various beneficial pharmacological activities, including anti-inflammatory, antidiabetic, antiviral, antihypertension, antioxidant, and anticancer effects. However, the molecular mechanisms of its anticancer activity have not been clearly elucidated. In the present study, we investigated the proapoptotic effects of ethanol extract of S. baicalensis (EESB) on human renal cell carcinoma Caki-1 cells. The anti-proliferative activity of EESB was associated with apoptosis induction, which was associated with the up-regulation of death receptor 4, the Fas ligand, and Bax and the down-regulation of Bid, XIAP, and cIAP-1 proteins. EESB treatment also induced mitochondrial dysfunction, proteolytic activation of caspase-3, -8, and -9 and degradation of caspase-3 substrate proteins, such as poly (ADP-ribose) polymerase, ${\beta}$-catenin, and phospholipase C-${\gamma}1$. However, pretreatment of a pan-caspase inhibitor, z-VAD-fmk, significantly attenuated the EESB-induced apoptosis. Taken together, these findings suggest that EESB may be a potential chemotherapeutic agent. Further studies will be needed to identify the active compounds that confer the anticancer activity of S. baicalensis.

Pharmacological Profile of KR-31125, an Orally Active AT1 Receptor Antagonist (안지오텐신 수용체 리간드 KR-31125의 생체 내 활성에 관한 연구)

  • Lee, Sung-Hou
    • Journal of Life Science
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    • v.20 no.7
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    • pp.969-976
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    • 2010
  • In vivo studies of KR-31125 (2-butyl-5-dimethoxymethyl-6-phenyl-7-methyl-3-[[2'-(1H-tetrazol-5-yl) biphenyl-4-yl]methyl]-3H-imidazo[4,5-b]pyridine) were performed in pithed rats, conscious angiotensin II (AII) challenged normotensive rats, renal hypertensive rats (RHRs) and furosemide-treated beagle dogs. KR-31125 induced a non-parallel right shift in the dose-pressor response curve to AII ($ID_{50}$: 0.095 mg/kg) with a dose-dependent reduction in the maximum responses in pithed rats. Compared to losartan, this antagonistic effect was about 18 times more potent, presenting competitive antagonism. Other agonists such as norepinephrine and vasopressin did not alter the responses induced by KR-31125. Orally administered KR-31125 had no agonistic effect and dose-dependently inhibited the pressor response to AII with a slightly weaker potency ($ID_{50}$: 0.25 and 0.47 mg/kg, respectively) in the AII-challenged normotensive rat model, but with a more rapid onset of action than losartan (time to $E_{max}$: 30 min for KR-31125 and 6 hr for losartan). KR-31125 produced a dose-dependent antihypertensive effect with a higher potency than losartan in RHRs, and these effects were confirmed in furosemide-treated dogs where they presented a dose-dependent and long-lasting (>8 hr) antihypertensive effect with a rapid onset of action (time to $E_{max}$: 2-4 hr), as well as a 20-fold greater potency than losartan. These results suggest that KR-31125 is a potent, orally active $AT_1$ receptor antagonist that can be applied to the development of new diagnostic and research tools as an added exploratory potential of $AT_1$ receptor antagonist.

Effects of Walking Exercise Intervention on Body Composition, Insulin Resistance, and Blood Pressure in Elderly Obese Women with Stage 1 Hypertension (걷기운동이 1기 고혈압을 가진 비만 노인 여성의 신체조성, 인슐린 저항성 및 혈압에 미치는 영향)

  • Moon-Soo Park;Yi-Sub Kwak
    • Journal of Life Science
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    • v.33 no.10
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    • pp.791-796
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    • 2023
  • It is well known that any kind of physical activity can be a useful nonpharmacological tool in the prevention and treatment of cardiovascular diseases, including antihypertension. There is also strong evidence that suggests that people with cardiovascular disease are less active than healthy people. Therefore, the aim of this study was to investigate the effect of a 12-week walking exercise intervention program on body composition, insulin resistance, and blood pressure in obese elderly women with stage 1 hypertension. The walking exercise program was performed for 50 min, three times per week. The intensity progressively increased: RPE 11 to 12, 40-50% HRR, for weeks 1-4; RPE 12 to 13, 50-60% HRR, for weeks 5-8; and RPE 13 to 14, 60-65% HRR, for weeks 9-12. The subjects were 20 obese elderly women with stage 1 hypertension (SBP: 140-159 mmHg or DBP: 90-99 mmHg). Half were placed in the walking exercise group (EX, n=10), and half were placed in the control group (CON, n=10). At the end of the program, the EX group members had significantly lower body fat, insulin resistance, and SBP compared to the CON group members. These results suggest that undertaking a 12-week walking exercise program improves body fat, insulin resistance, and SBP, which may improve the incidence of metabolic disease in elderly obese women with stage 1 hypertension.

Decreased Nocturnal Blood Pressure Dipping in Patients with Periodic Limb Movements in Sleep (수면중 주기성 사지 운동에서 나타나는 야간 혈압 강하의 감소)

  • Lee, Mi Hyun;Choi, Jae-Won;Oh, Seong Min;Lee, Yu Jin
    • Sleep Medicine and Psychophysiology
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    • v.25 no.2
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    • pp.51-57
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    • 2018
  • Objectives: Previous studies have shown that periodic limb movements in sleep (PLMS) could be one of risk factors for cardiovascular morbidity. The purpose of this study was to investigate the association between PLMS and blood pressure changes during sleep. Methods: We analyzed data from 358 adults (176 men and 182 women) aged 18 years and older who were free from sleep apnea syndrome (Respiratory Disturbance Index < 5) and sleep disorders such as REM sleep behavior disorder or narcolepsy. Demographic characteristics, polysomnography records, and clinical variable data including blood pressure, body mass index, alcohol, smoking, and current medications were collected. In addition, self-report questionnaires including the Beck Depression Index, Epworth Sleepiness Scale and Pittsburgh Sleep Quality Index were completed. Blood pressure change from bedtime to awakening was compared between the two periodic limb movement index (PLMI) groups [low PLMI ($PLMI{\leq}15$) and high PLMI (PLMI > 15)]. Blood pressure change patterns were compared using repeated measures analysis of variance. Results: Systolic blood pressure in the high PLMI group was lower than that in the low PLMI group (p = 0.036). These results were also significant when adjusted for gender and age, but were not statistically significant when adjusted for BMI, alcohol, smoking, anti-hypertension medication use and sleep efficiency (p = 0.098). Systolic blood pressure dropped by 9.7 mm Hg in the low PLMI group, and systolic blood pressure in the high PLMI group dropped by 2.9 mm Hg. There was a significant difference in delta systolic blood pressure after sleep between the two groups in women when adjusted for age, BMI, alcohol, smoking, antihypertensive medication use and sleep efficiency (p = 0.023). Conclusion: PLMS was significantly associated with a decreasing pattern in nocturnal BP during sleep, and this association remained significant in women when adjusted for age, BMI, alcohol, smoking, antihypertension medication use and sleep efficiency related to blood pressure. We suggest that PLMS may be associated with cardiovascular morbidity.