A novel antihypertension agent, sargachromenol D from marine brown algae, Sargassum siliquastrum, exerts dual action as an L-type Ca2+ channel blocker and endothelin A/B2 receptor antagonist

Park, Byong‐Gon; Shin, Woon‐Seob; Oh, Sangtae; Park, Gab-Man; Kim, Nam Ik; Lee, Seokjoon

doi:10.1016/j.bmc.2017.07.002

Cited by 18 publications

(11 citation statements)

References 40 publications

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Section: Hypertensionmentioning

confidence: 99%

“…Thus, four compounds isolated from Sargassum siliquastrum , including two farnesylacetones, a reduced form of one of these and sargachromenol D, displayed vasodilatory effects on the basilar artery of rabbits [60,61]. These effects were probably related with their ability to effectively antagonize the L-type Ca 2+ channel [61,62]. In this sense, although several factors are assumed to contribute to hypertension, it is clearly established that an increased vascular tone is always the final target, as this mainly mediated by increased Ca 2+ influx via L-type Ca 2+ channels in vascular smooth muscles [63].…”

Section: Hypertensionmentioning

confidence: 99%

“…In fact, L-type Ca 2+ channel blockers have been extensively used as antihypertensive agents [54]. In addition to its capacity to block the L-type Ca 2+ channel, sargachromenol D is also able to antagonise the vasoconstriction induced by endothelin-1 (ET-1), most likely due to its ability to act as an antagonist of the endothelin A and the endothelin B2 (ET A/B2 ) receptors, which can also account for its beneficial effects in hypertension [61] (Figure 4). In fact, ET-1 is a mediator with vasoconstrictor properties that has been reported to play a key role in pathological hypertension, being associated with an increased risk of major cardiovascular and cerebrovascular events [64].…”

Section: Hypertensionmentioning

confidence: 99%

“…Given the pharmacological properties of sargachromenol D as a dual antagonist L-type Ca 2+ channel and endothelin ET A/B2 receptor, a dose of 80 mg/kg of sargachromenol D was assayed orally in spontaneous hypertensive rats (SHRs). Sargachromenol D showed acute effects in SHRs by significantly decreasing both systolic and diastolic BP for 24 h after administration [61]. These authors suggested that sargachromenol D could be an appropriate drug for BP control in severe hypertension that is not controlled by conventional combinatorial therapy.…”

Section: Hypertensionmentioning

confidence: 99%

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Potential Role of Seaweed Polyphenols in Cardiovascular-Associated Disorders

et al. 2018

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The beneficial effects of various polyphenols with plant origins on different cardiovascular-associated disorders, such as hypertension, diabetes mellitus type 2 and metabolic syndrome are well known. Recently, marine crude-drugs are emerging as potential treatments in many noncommunicable conditions, including those involving the cardiovascular system. Among the active compounds responsible for these activities, seaweed polyphenols seem to play a key role. The aim of the present review is to summarise the current knowledge about the beneficial effects reported for edible seaweed polyphenols in the amelioration of these prevalent conditions, focusing on both preclinical and clinical studies. This review will help to establish the basis for future studies in this promising field.

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Section: Hypertensionmentioning

confidence: 99%

Section: Hypertensionmentioning

confidence: 99%

Section: Hypertensionmentioning

confidence: 99%

Section: Hypertensionmentioning

confidence: 99%

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Potential Role of Seaweed Polyphenols in Cardiovascular-Associated Disorders

et al. 2018

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“…[5][6][7] Endothelin 1 (ET-1), which has a strong contraction of blood vessels, could promote the mitotic effect of smooth muscle cells, and is closely related to a variety of heart and cerebrovascular disease. 8,9 Studies had evaluated the antagonistic effects of caffeic acid and ferulic acid on the biological effects of ET-1 at the level of overall animals, isolated organs, cells and subcells. Results showed that caffeic acid and ferulic acid had an antagonistic biological effect on ET-1.…”

Section: Introductionmentioning

confidence: 99%

<p>Study on the Formation of Antihypertensive Twin Drugs by Caffeic Acid and Ferulic Acid with Telmisartan</p>

Peng

et al. 2020

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Purpose: This study aimed to synthesize twin drugs from cinnamic acid compounds, caffeic acid (CFA) and ferulic acid (FLA), which can antagonize endothelin-1 (ET-1) with telmisartan through ester bonds. Moreover, the antihypertensive effect of telmisartan and its influence on blood pressure variability (BPV) were enhanced, and the bioavailability of caffeic acid and ferulic acid was improved. Methods: Six twin drugs, which were the target compounds, were synthesized. Hypertensive rats (SHR) and conscious sinoaortic-denervated (SAD) rats were spontaneously used as models for pharmacodynamic research to study the antihypertensive efficacy of these twin drugs. Wistar rats were employed as pharmacokinetic research models to investigate the pharmacokinetics of the target compounds via intragastric administration. Cellular pharmacodynamic research was also conducted on the antagonistic action on Ang II-AT1, ETA and ETB receptor. Results: Compound 1a was determined as the best antihypertensive twin drug and thus was further studied for its effect on BPV. Compared with that of telmisartan, the antihypertensive effect of compound 1a was improved (p<0.05), and the BPV was reduced (p<0.05). The bioavailability of caffeic acid and ferulic acid after hydrolysis from twin drugs could be increased to varying degrees, and the differences of the main pharmacokinetic parameters among the different forms of caffeic acid and ferulic acid were statistically significant (p<0.05 or p<0.01). Compound 1a had the best antagonistic effect on the Ang II-AT1 receptor. However, the IC 50 of Lps-2 was still two orders of magnitude higher than that of the positive drug telmisartan. Hence, the twin drugs worked by metabolizing and regenerating telmisartan and caffeic acid or ferulic acid in the body. Conclusion: The synthesized twin drugs improved telmisartan's antihypertensive effects, significantly decreased BPV in SAD rats and increased the bioavailability of caffeic acid and ferulic acid. This study serves as a basis for the development of new angiotensin receptor blocker (ARB) in the future and a reference for the development of new drugs to antagonize ET-1.

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Occurrence and Bioactivities of Minor Vitamin E Derivatives

Birringer

Frank

2019

Vitamin E in Human Health

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A novel antihypertension agent, sargachromenol D from marine brown algae, Sargassum siliquastrum, exerts dual action as an L-type Ca2+ channel blocker and endothelin A/B2 receptor antagonist

Cited by 18 publications

References 40 publications

Potential Role of Seaweed Polyphenols in Cardiovascular-Associated Disorders

Potential Role of Seaweed Polyphenols in Cardiovascular-Associated Disorders

<p>Study on the Formation of Antihypertensive Twin Drugs by Caffeic Acid and Ferulic Acid with Telmisartan</p>

Occurrence and Bioactivities of Minor Vitamin E Derivatives

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