Displaying publications 21 - 40 of 71 in total

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  1. Antihypertensive efficacy and safety of a standardized herbal medicinal product of Hibiscus sabdariffa and Olea europaea extracts (NW Roselle): A phase-II, randomized, double-blind, captopril-controlled clinical trial
    Elkafrawy N, Younes K, Naguib A, Badr H, Kamal Zewain S, Kamel M, et al.
    Phytother Res, 2020 Dec;34(12):3379-3387.
    PMID: 32725873 DOI: 10.1002/ptr.6792
    Hypertension is a public health concern that needs immediate attention upon diagnosis. The demand for natural alternatives is on the rise; Hibiscus sabdariffa and Olea europaea are traditionally used for hypertension management in Egypt. In this study, we aimed to investigate the antihypertensive efficacy and safety of two doses of an herbal product of Hibiscus sabdariffa calyxes and Olea europaea leaves (NW Roselle) in Egyptian patients with grade 1 essential hypertension. We equally randomized 134 patients to receive captopril 25 mg, low-dose NW Roselle, or high-dose NW Roselle BID for 8 weeks. No significant decrease was found in systolic blood pressure or diastolic blood pressure when we compared low-dose NW Roselle and high-dose NW Roselle to captopril (p > .05). In all groups, mean reduction in BP at 8 weeks was significant; 16.4/9.9 mmHg (p
    Matched MeSH terms: Antihypertensive Agents/pharmacology
  2. High angiotensin-I converting enzyme (ACE) inhibitory activity of Alcalase-digested green soybean (Glycine max) hydrolysates
    Hanafi MA, Hashim SN, Chay SY, Ebrahimpour A, Zarei M, Muhammad K, et al.
    Food Res Int, 2018 04;106:589-597.
    PMID: 29579964 DOI: 10.1016/j.foodres.2018.01.030
    As a protein-rich, underutilized crop, green soybean could be exploited to produce hydrolysates containing angiotensin-I converting enzyme (ACE) inhibitory peptides. Defatted green soybean was hydrolyzed using four different food-grade proteases (Alcalase, Papain, Flavourzyme and Bromelain) and their ACE inhibitory activities were evaluated. The Alcalase-generated green soybean hydrolysate showed the highest ACE inhibitory activity (IC50: 0.14 mg/mL at 6 h hydrolysis time) followed by Papain (IC50: 0.20 mg/mL at 5 h hydrolysis time), Bromelain (IC50: 0.36 mg/mL at 6 h hydrolysis time) and Flavourzyme (IC50: 1.14 mg/mL at 6 h hydrolysis time) hydrolysates. The Alcalase-generated hydrolysate was profiled based on its hydrophobicity and isoelectric point using reversed phase high performance liquid chromatography (RP-HPLC) and isoelectric point focusing (IEF) fractionators. The Alcalase-generated green soybean hydrolysate comprising of peptides EAQRLLF, PSLRSYLAE, PDRSIHGRQLAE, FITAFR and RGQVLS, revealed the highest ACE inhibitory activity of 94.19%, 99.31%, 92.92%, 101.51% and 90.40%, respectively, while their IC50 values were 878 μM, 532 μM, 1552 μM, 1342 μM and 993 μM, respectively. It can be concluded that Alcalase-digested green soybean hydrolysates could be exploited as a source of peptides to be incorporated into functional foods with antihypertensive activity.
    Matched MeSH terms: Antihypertensive Agents/pharmacology*
  3. Inhibition of angiotensin-converting enzyme activity by a partially purified fraction of Gynura procumbens in spontaneously hypertensive rats
    Hoe SZ, Kamaruddin MY, Lam SK
    Med Princ Pract, 2007;16(3):203-8.
    PMID: 17409755
    To investigate the hypotensive and angiotensin-converting enzyme (ACE) inhibitory activities of a partially purified fraction (FA-I) of the leaves of Gynura procumbens and to qualitatively analyse the putative compounds present in the fraction.
    Matched MeSH terms: Antihypertensive Agents/pharmacology*
  4. Fulltext Highlights of the 2019 Japanese Society of Hypertension Guidelines and perspectives on the management of Asian hypertensive patients
    Hoshide S, Kario K, Tomitani N, Kabutoya T, Chia YC, Park S, et al.
    J Clin Hypertens (Greenwich), 2020 03;22(3):369-377.
    PMID: 31891452 DOI: 10.1111/jch.13763
    Unlike other international guidelines but in accord with the earlier Japanese Society of Hypertension (JSH) guidelines, the 2019 JSH guidelines ("JSH 2019") continue to emphasize the importance of out-of-office blood pressure (BP) measurements obtained with a home BP device. Another unique characteristic of JSH 2019 is that it sets clinical questions about the management of hypertension that are based on systematic reviews of updated evidence. JSH 2019 states that individuals with office BP 
    Matched MeSH terms: Antihypertensive Agents/pharmacology*
  5. Toxicity study and blood pressure-lowering efficacy of whey protein concentrate hydrolysate in rat models, plus peptide characterization
    Hussein FA, Chay SY, Ghanisma SBM, Zarei M, Auwal SM, Hamid AA, et al.
    J Dairy Sci, 2020 Mar;103(3):2053-2064.
    PMID: 31882211 DOI: 10.3168/jds.2019-17462
    We evaluated the acute (single-dose) and subacute (repeated-dose) oral toxicity of alcalase-hydrolyzed whey protein concentrate. Our acute study revealed no death or treatment-related complications, and the median lethal dose of whey protein concentrate hydrolysate was >2,500 mg/kg. In the subacute study, when the hydrolysate was fed at 3 different concentrations (200, 400, and 800 mg/kg), no groups showed toxicity changes compared with controls. Then, whey protein concentrate hydrolysate was orally administered to spontaneously hypertensive rats. Results revealed significant reductions in blood pressure in a dose-dependent manner, and dosing at 400 mg/kg led to significant blood pressure reduction (-47.8 mm Hg) compared with controls (blood pressure maintained) and the findings of previous work (-21 mm Hg). Eight peptides-RHPEYAVSVLLR, GGAPPAGRL, GPPLPRL, ELKPTPEGDL, VLSELPEP, DAQSAPLRVY, RDMPIQAF, and LEQVLPRD-were sequentially identified and characterized. Of the peptides, VLSELPEP and LEQVLPRD showed the most prominent in vitro angiotensin-I converting enzyme inhibition with half-maximal inhibitory concentrations of 0.049 and 0.043 mM, respectively. These findings establish strong evidence for the in vitro and in vivo potential of whey protein concentrate hydrolysate to act as a safe, natural functional food ingredient that exerts antihypertensive activity.
    Matched MeSH terms: Antihypertensive Agents/pharmacology*
  6. Identification of angiotensin-converting enzyme inhibitory proteins from mycelium of Pleurotus pulmonarius (oyster mushroom)
    Ibadallah BX, Abdullah N, Shuib AS
    Planta Med, 2015 Jan;81(2):123-9.
    PMID: 25590365 DOI: 10.1055/s-0034-1383409
    Pleurotus pulmonarius (grey oyster mushroom) has been acknowledged as a recuperative agent for many diseases in addition to its recognition as a nutritious provision. We performed a study on P. pulmonarius mycelium for an antihypertensive effect via the angiotensin-converting enzyme inhibitory activity. The preliminary assay on the mycelial water extract demonstrated that the angiotensin-converting enzyme inhibitory activity had an IC50 value of 720 µg/mL. Further protein purifications via ammonium sulphate precipitation and RP-HPLC resulted in 60× stronger angiotensin-converting enzyme inhibitory activity than that of the mycelial water extract (IC50 = 12 µg/mL). Protein identification and characterisation by MALDI-TOF/TOF, later corroborated by LC-MS/MS, indicated three proteins that are responsible for the blood pressure lowering effects via different mechanisms: serine proteinase inhibitor-like protein, nitrite reductase-like protein, and DEAD/DEAH box RNA helicase-like protein.
    Matched MeSH terms: Antihypertensive Agents/pharmacology*
  7. Fulltext Mechanisms of the antihypertensive effects of Nigella sativa oil in L-NAME-induced hypertensive rats
    Jaarin K, Foong WD, Yeoh MH, Kamarul ZY, Qodriyah HM, Azman A, et al.
    Clinics (Sao Paulo), 2015 Nov;70(11):751-7.
    PMID: 26602523 DOI: 10.6061/clinics/2015(11)07
    This study was conducted to determine whether the blood pressure-lowering effect of Nigella sativa might be mediated by its effects on nitric oxide, angiotensin-converting enzyme, heme oxygenase and oxidative stress markers.
    Matched MeSH terms: Antihypertensive Agents/pharmacology*
  8. Blood pressure and urine metabolite changes in spontaneously hypertensive rats treated with leaf extract of Ficus deltoidea var angustifolia
    Kamal MSA, Mediani A, Kasim N, Ismail NH, Satar NA, Azis NA, et al.
    J Pharm Biomed Anal, 2022 Feb 20;210:114579.
    PMID: 35016031 DOI: 10.1016/j.jpba.2021.114579
    Ficus deltoidea var angustifolia (FD-A) reduces blood pressure in spontaneously hypertensive rats (SHR) but the mechanism remains unknown. Changes in urine metabolites following FD-A treatment in SHR were, therefore, examined to identify the mechanism of its antihypertensive action. Male SHR were given either FD-A (1000 mg kg-1 day-1) or losartan (10 mg kg-1 day-1) or 0.5 mL of ethanolic-water (control) daily for 4 weeks. Systolic blood pressure (SBP) was measured every week and urine spectra data acquisition, on urine collected after four weeks of treatment, were compared using multivariate data analysis. SBP in FD-A and losartan treated rats was significantly lower than that in the controls after four weeks of treatment. Urine spectra analysis revealed 24 potential biomarkers with variable importance projections (VIP) above 0.5. These included creatine, hippurate, benzoate, trimethylamine N-oxide, taurine, dimethylamine, homocysteine, allantoin, methylamine, n-phenylacetylglycine, guanidinoacetate, creatinine, lactate, glucarate, kynurenine, ethanolamine, betaine, 3-hydroxybutyrate, glycine, lysine, glutamine, 2-hydroxyphenylacetate, 3-indoxylsulfate and sarcosine. From the profile of these metabolites, it seems that FD-A affects urinary levels of metabolites like taurine, hypotaurine, glycine, serine, threonine, alanine, aspartate and glutamine. Alterations in these and the pathways involved in their metabolism might underlie the molecular mechanism of its antihypertensive action.
    Matched MeSH terms: Antihypertensive Agents/pharmacology
  9. Parkia speciosa empty pod prevents hypertension and cardiac damage in rats given N(G)-nitro-l-arginine methyl ester
    Kamisah Y, Zuhair JSF, Juliana AH, Jaarin K
    Biomed Pharmacother, 2017 Dec;96:291-298.
    PMID: 28992471 DOI: 10.1016/j.biopha.2017.09.095
    Parkia speciosa Hassk is a plant found abundantly in Southeast Asia region. Its seeds with or without pods and roots have been used in traditional medicine in this region to treat hypertension. Therefore, we aimed to investigate the potential effect of the plant empty pod extract on hypertension development and changes in heart induced by N(G)-nitro-l-arginine methyl ester (l-NAME) administration in rats. Twenty-four male Sprague Dawley rats were divided into four groups. Groups 1 to 3 were given l-NAME (25mg/kg, intraperitoneally) for 8 weeks. Groups 2 and 3 were also given Parkia speciosa empty pods methanolic extract (800mg/kg, orally) and nicardipine (3mg/kg, orally), concurrently with l-NAME. The last group served as the control. l-NAME reduced plasma nitric oxide level and therefore, increased systolic blood pressure, angiotensin-converting enzyme and NADPH oxidase activities as well as lipid peroxidation in the heart. Parkia speciosa extract and nicardipine treatments had significantly prevented the elevations of blood pressure, angiotensin-converting enzyme, NADPH oxidase activities and lipid peroxidation in the heart induced by the l-NAME. Parkia speciosa extract but not nicardipine prevented the reduction in plasma nitric oxide level caused by l-NAME. In conclusion, Parkia speciosa empty pods methanolic extract has a potential to prevent the development of hypertension possibly by preventing the loss of plasma nitric oxide, as well as has cardioprotective effects by reducing angiotensin-converting enzyme activity and oxidative stress in the heart in rats administered l-NAME.
    Matched MeSH terms: Antihypertensive Agents/pharmacology
  10. Fulltext Guidance on ambulatory blood pressure monitoring: A statement from the HOPE Asia Network
    Kario K, Hoshide S, Chia YC, Buranakitjaroen P, Siddique S, Shin J, et al.
    J Clin Hypertens (Greenwich), 2021 Mar;23(3):411-421.
    PMID: 33319412 DOI: 10.1111/jch.14128
    Hypertension is an important public health issue due to its association with a number of serious diseases, including cardiovascular disease and stroke. The importance of evaluating hypertension taking into account different blood pressure (BP) profiles and BP variability (BPV) is increasingly being recognized, and is particularly relevant in Asian populations given the specific features of hypertension in the region (including greater salt sensitivity and a high rate of nocturnal hypertension). Ambulatory BP monitoring (ABPM) is the gold standard for diagnosing hypertension and assessing 24-hour BP and provides data on several important parameters that cannot be obtained using any other form of BP measurement. In addition, ABPM parameters provide better information on cardio- and cerebrovascular risk than office BP. ABPM should be used in all patients with elevated BP, particularly those with unstable office or home BP, or who are suspected to have white-coat or masked hypertension. ABPM is also an important part of hypertension diagnosis and monitoring in high-risk patients. ABPM needs to be performed using a validated device and good practice techniques, and has a role both in hypertension diagnosis and in monitoring the response to antihypertensive therapy to ensure strict BP control throughout the 24-hour period. Use of ABPM in clinical practice may be limited by cost and accessibility, and practical education of physicians and patients is essential. The ABPM evidence and practice points in this document are based on the Hypertension Cardiovascular Outcome Prevention and Evidence (HOPE) Asia Network expert panel consensus recommendations for ABPM in Asia.
    Matched MeSH terms: Antihypertensive Agents/pharmacology
  11. Fulltext Hypotensive effect of Gentiana floribunda is mediated through Ca++ antagonism pathway
    Khan AU, Mustafa MR, Khan AU, Murugan DD
    BMC Complement Altern Med, 2012;12:121.
    PMID: 22883710 DOI: 10.1186/1472-6882-12-121
    Gentiana floribunda was investigated for the possible hypotensive and vasodilator activities in an attempt to rationalize its traditional use in hypertension.
    Matched MeSH terms: Antihypertensive Agents/pharmacology
  12. Fulltext Cardiovascular Disease and Use of Renin-Angiotensin System Inhibitors in COVID-19
    Kow CS, Zaidi STR, Hasan SS
    Am J Cardiovasc Drugs, 2020 Jun;20(3):217-221.
    PMID: 32281055 DOI: 10.1007/s40256-020-00406-0
    There is ongoing debate on the safety of renin-angiotensin system (RAS) inhibitors in COVID-19. Recently published studies highlight a potential relationship between cardiovascular disease (CVD) and COVID-19. This article aims to summarize the evidence on the use of RAS inhibitors in CVD patients with COVID-19, focusing on safety issues of the RAS inhibitors and their relationship with COVID-19.
    Matched MeSH terms: Antihypertensive Agents/pharmacology
  13. Apocynum venetum leaf extract, an antihypertensive herb, inhibits rat aortic contraction induced by angiotensin II: a nitric oxide and superoxide connection
    Lau YS, Kwan CY, Ku TC, Hsieh WT, Wang HD, Nishibe S, et al.
    J Ethnopharmacol, 2012 Sep 28;143(2):565-71.
    PMID: 22835814 DOI: 10.1016/j.jep.2012.07.012
    The leaves extract of Apocynum venetum (AVLE), also known as "luobuma", have long been used in traditional Chinese medicine to treat hypertension and depression in parts of China and it has been shown to possess anti-oxidant and anti-lipid peroxidation effects. AVLE (10 μg/ml) has been reported to have a long-lasting endothelium-dependent relaxant effect and this effect has been proposed to be due to its nitric oxide(NO)-releasing and superoxide anion(SOA)-scavenging properties.
    Matched MeSH terms: Antihypertensive Agents/pharmacology*
  14. Clonidine and a novel clonidine analog AL-12 cause sympathoinhibition in spontaneously hypertensive and diabetic spontaneously hypertensive rats
    Lazahari MI, Sattar MA, Abdullah NA, Khan MA, Johns EJ
    Methods Find Exp Clin Pharmacol, 2008 Apr;30(3):193-9.
    PMID: 18597003 DOI: 10.1358/mf.2008.30.3.1166221
    This study examined the sympathoinhibitory effects of clonidine and a novel clonidine analog, AL-12, in rat models of genetic hypertension and a combined state of genetic hypertension and diabetes. Rats in the treatment groups were given either clonidine or AL-12 while the respective control groups received either saline or Tween 80 for 6 days. Physiological data were collected during this period, which was followed by acute studies on day 7 when bolus administrations (i.v.) of graded doses of noradrenaline, phenylephrine and methoxamine were carried out. It was observed that in AL-12-treated nondiabetic spontaneously hypertensive rats (SHR), the pressure responses to all adrenergic agonists were greater (p < 0.05) in the treated group, while in the diabetic SHR rats a larger pressure response was observed only to noradrenaline (p < 0.05). In nondiabetic SHR rats treated with clonidine, a greater (p < 0.05) pressure response was observed only in the case of phenylephrine. In the diabetic SHR rats treated with clonidine, the pressure responses to the adrenergic agonists were similar (p > 0.05) in the treated and its control animals except that methoxamine caused a greater (p < 0.05) pressure response in the control group. The data obtained suggest that clonidine and AL-12 act possibly via vascular alpha1 and alpha2 adrenoceptors present at both pre- and postsynaptic locations.
    Matched MeSH terms: Antihypertensive Agents/pharmacology*
  15. Resistant hypertension during antituberculosis treatment: how is rifampicin implicated?
    Lee SL, Lim WJ, Chai ST
    Med J Malaysia, 2020 09;75(5):591-593.
    PMID: 32918434
    A 67-year-old mental institute resident was treated for smear-positive pulmonary tuberculosis. His background history included chronic essential hypertension which was well-controlled with amlodipine 10mg daily. However, his blood pressure became suboptimal one week into antitubercular treatment, necessitating escalation of antihypertensive therapy up to six medications. Following completion of antitubercular treatment, his blood pressure improved markedly. The number of antihypertensives was able to be reduced to only two after a month. We postulate that rifampicin has attenuated the therapeutic effect of amlodipine via potent induction of hepatic CYP3A4 but the failure to control the blood pressure even with medications unrelated to cytochrome P450 pathways raises the spectre of an additional interaction.
    Matched MeSH terms: Antihypertensive Agents/pharmacology*
  16. Fulltext Role of α1-blockers in the current management of hypertension
    Li H, Xu TY, Li Y, Chia YC, Buranakitjaroen P, Cheng HM, et al.
    J Clin Hypertens (Greenwich), 2022 Sep;24(9):1180-1186.
    PMID: 36196467 DOI: 10.1111/jch.14556
    There is emerging evidence that α1-blockers can be safely used in the treatment of hypertension. These drugs can be used in almost all hypertensive patients for blood pressure control. However, there are several special indications. Benign prostatic hyperplasia is a compelling indication of α1-blockers, because of the dual treatment effect on both high blood pressure and lower urinary tract symptoms. Many patients with resistant hypertension would require α1-blockers as add-on therapy. Primary aldosteronism screen is a rapidly increasing clinical demand in the management of hypertension, where α1-blockers are useful for blood pressure control in the preparation for the measurement of plasma aldosterone and renin. Nonetheless, α1-blockers have to be used under several considerations. Among the currently available agents, only long-acting α1-blockers, such as doxazosin gastrointestinal therapeutic system 4-8 mg daily and terazosin 2-4 mg daily, should be chosen. Orthostatic hypotension is a concern with the use of α1-blockers especially in the elderly, and requires careful initial bedtime dosing and avoiding overdosing. Fluid retention is potentially also a concern, which may be overcome by combining an α1-blocker with a diuretic.
    Matched MeSH terms: Antihypertensive Agents/pharmacology
  17. In vitro vascular effects produced by crude aqueous extract of green marine algae, Cladophora patentiramea (Mont.) Kützing, in aorta from normotensive rats
    Lim YL, Mok SL
    Med Princ Pract, 2010;19(4):260-8.
    PMID: 20516701 DOI: 10.1159/000312711
    To investigate the antihypertensive activity of aqueous extracts obtained from Malaysian coastal seaweeds and to determine the pharmacological mechanisms of the extracts on rat aorta in vitro.
    Matched MeSH terms: Antihypertensive Agents/pharmacology
  18. Fulltext Angiotensin receptor neprilysin inhibitor as a novel antihypertensive drug: Evidence from Asia and around the globe
    Lin DS, Wang TD, Buranakitjaroen P, Chen CH, Cheng HM, Chia YC, et al.
    J Clin Hypertens (Greenwich), 2021 03;23(3):556-567.
    PMID: 33305531 DOI: 10.1111/jch.14120
    Hypertension is a worldwide epidemic that continues to grow, with a subset of patients responding poorly to current treatment available. This is especially relevant in Asia, which constitutes 61% of the global population. Hypertension in Asia is a unique entity that is often salt-sensitive, nocturnal, and systolic predominant. Sacubitril/valsartan is a first-in-class angiotensin receptor neprilysin inhibitor that was first used in heart failure with reduced ejection fraction. Sacubitril inhibits neprilysin, a metallopeptidase that degrades natriuretic peptides (NPs). NPs exert sympatholytic, diuretic, natriuretic, vasodilatory, and insulin-sensitizing effects mostly via cyclic guanosine monophosphate (cGMP)-mediated pathways. As an antihypertensive agent, sacubitril/valsartan has outperformed angiotensin II receptor type 1 blockers (ARBs), with additional reductions of office systolic blood pressures ranging between 5 and 7 mmHg, in multiple studies in Asia and around the globe. The drug was well tolerated even in the elderly or those with chronic kidney disease. Its mechanisms of actions are particularly attractive for treatment of hypertension in Asia. Sacubitril/valsartan offers a novel, dual class, single-molecule property that may be considered as first-line antihypertensive therapy. Further investigations are needed to validate its safety for long-term use and to explore other potentials such as in the management of insulin resistance and obesity, which often coexist with hypertension in Asia.
    Matched MeSH terms: Antihypertensive Agents/pharmacology
  19. New flavonoid-based compound synthesis strategy for antihypertensive drug development
    Loh YC, Chan SY, Tew WY, Oo CW, Yam MF
    Life Sci, 2020 May 15;249:117512.
    PMID: 32145305 DOI: 10.1016/j.lfs.2020.117512
    Hypertension is one of the leading causes of mortality in relation to the cardiovascular conditions and easily the most overlooked and poorly managed disease in mankind. With well over 200 drugs available in the market globally, there is still an urgency to search for antihypertensive alternatives due to the subpar efficacy and unwarranted side effects of the current choices. Present studies reported over 250 types of plant-derived compounds were being investigated for potential pharmacological effects on the vasculature in the last 3 decades. There were numerous literatures that claimed various compounds exhibiting vasorelaxant properties to a certain extent with low numbers of these compounds being successfully adapted into the current medicinal practice for treatment of hypertension. The issue is the scarcity of reviews that summarizes the discovery of this field and the lack of thorough comparison of these compounds to identify which of these vasodilators should be the next face of hypertension management. Thus, this review is aiming towards identifying the relationship between a major class of plant-derived compounds, flavonoid's activity as a vasodilator with their signalling pathways and their structural characteristics according to their vasorelaxant properties. Interestingly, we found that both nitric oxide and voltage-operated calcium channels pathways, and two of the flavonoid's structural characteristics play crucial roles in eliciting strong vasorelaxant effects. We have faith that the insights of this review will serve as a reference for those researching similar topics in the future and potentially lead to the development of more promising antihypertensive alternative.
    Matched MeSH terms: Antihypertensive Agents/pharmacology
  20. Discovery of trans-3,4,4'-trihydroxystilbene as new lead vasorelaxant agent for antihypertensive drug development
    Loh YC, Chan SY, Oo CW, Yam MF
    Life Sci, 2021 Aug 01;278:119560.
    PMID: 33915131 DOI: 10.1016/j.lfs.2021.119560
    AIMS: The structure-vasorelaxant activity relationships (SARs) assessment in previous study has found that trans-3,4,4'-trihydroxystilbene (344OH) could potentially act as a vasorelaxing agent with demonstration of over 2-fold maximal relaxation (Rmax) compared to its analogue, resveratrol. The present study focuses on the mechanism of actions and pathways employed by 344OH and compared to its analogue to further speculate the SAR of stilbenoids towards vasorelaxation.

    MATERIALS AND METHODS: The 344OH employed in present study was synthesized based on the protocol in previous study. The vascular responses towards the cumulative addition of 344OH were evaluated using in vitro rat aortic rings assays.

    KEY FINDINGS: The pEC50 and Rmax values were found to be 4.33 ± 0.05 and 106 ± 3.99%, respectively. Results showed that the vasorelaxation of 344OH were predominated by G-protein-coupled muscarinic- (M3) and β2-adrenergic receptors, followed by PGI2/AC/cAMP- and NO/sGC/cGMP-dependent pathways. It was also identified that 344OH employed voltage-activated- (Kv), calcium-activated- (Kca) and inwardly-rectifying (Kir) potassium channels and act as an antagonist for both VOCC and IP3R while regulating the action potential in the vasculature.

    SIGNIFICANCE: The different position of hydroxyl substituent located in A-ring of the stilbenoid backbone in 344OH compared to resveratrol resulted in a significant difference in mechanistic actions that lead to 344OH's fast-acting and less time-dependent vasorelaxation behaviour. This has substantially increased the potential of 344OH to be developed as an effective antihypertensive drug in future. Present findings further strengthen our inferences where the SARs study approach should be carried out as the mainstream methodology in future drug development research.

    Matched MeSH terms: Antihypertensive Agents/pharmacology*
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