Angiotensin I-converting enzyme (ACE) inhibition and nitric oxide (NO)-mediated antihypertensive effect of octaphlorethol A isolated from Ishige sinicola: In vitro molecular mechanism and in vivo SHR model

Ko, Seok‐Chun; Jung, Won‐Kyo; Kang, Sung-Myung; Lee, Seung‐Hong; Kang, Moon Seong; Heo, Soo‐Jin; Kang, Kyong‐Hwa; Kim, Yong‐Tae; Park, Sunjoo; Jeong, Yoonhwa; Kim, Misook; Byun, Hee‐Guk; Jeon, You‐Jin

doi:10.1016/j.jff.2015.07.003

Cited by 25 publications

(25 citation statements)

References 36 publications

(47 reference statements)

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“…Among the various phlorotannin molecules, the compounds such as eckol, phlorofucofuroeckol A, dieckol, phloroglucinol, triphlorethol-A, octaphlorethol A, and 6,6ʹ bieckol were reported for its ACE inhibition. [21,28,31,32] However, low molecular weight phlorotannin showed only less ACE inhibition. Among these phlorotannins, phlorofucofuroeckol A (pentamer), dieckol (hexamer), 6,6ʹ bieckol (hexamer), and octaphlorethol A (octamer) had shown significantly higher ACE inhibition.…”

Section: Discussionmentioning

confidence: 99%

“…The enzyme activity of ACE was determined by the methods of Cushman and Cheung [20] with slight modifications as described in Ko et al [21] Briefly, assay mixture consisting of 100 µl of the ACE enzyme (25 mU/ml) and 200 µl of 8.0 mM HHL was incubated at 37°C for 30 min. After incubation, the reaction was stopped by the addition of 600 µl of 1 M HCl.…”

Section: Ace Enzyme Activity and Inhibitor Studiesmentioning

confidence: 99%

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Exploring bioactive fraction of Sargassum wightii: In vitro elucidation of angiotensin-I-converting enzyme inhibition and antioxidant potential

Raji

Loganathan

Sakayanathan

et al. 2018

International Journal of Food Properties

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Bioactive fraction of brown algae Sargassum wightii (SWE) was obtained using silica column chromatography and preparative Thin Layer Chromatography (TLC). FT-IR and LC-mass spectrometry ESI analysis revealed presence of various phlorotannins in the SWE. The IC 50 value of SWE was found to be 59.91, 51.04, and 55.21 μg/ml for scavenging of 2,2diphenyl-1-picrylhydrazyl, 2,2-azino-bis-(3-ethylbenzothiazoline-6-sulfonic acid), and Ferric Reducing Antioxidant Power assay, respectively. SWE inhibited angiotensin-I-converting enzyme (ACE) in mixed-type manner with IC 50 value of 56.96 µg/ml and Ki value of 45 µg/ml. The dual function such as antioxidant and ACE inhibition of SWE warrants further study to understand the antihypertensive potential in vivo. ARTICLE HISTORY

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Section: Discussionmentioning

confidence: 99%

Section: Ace Enzyme Activity and Inhibitor Studiesmentioning

confidence: 99%

Exploring bioactive fraction of Sargassum wightii: In vitro elucidation of angiotensin-I-converting enzyme inhibition and antioxidant potential

Raji

Loganathan

Sakayanathan

et al. 2018

International Journal of Food Properties

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“…The renin-angiotensin system is an endogenic regulator of blood pressure, water electrolyte homeostasis and cell growth balance (2). In particular, it plays a key role in the pathology of hypertension (3).…”

Section: Introductionmentioning

confidence: 99%

A heptameric peptide purified from Spirulina sp. gastrointestinal hydrolysate inhibits angiotensin I-converting enzyme- and angiotensin II-induced vascular dysfunction in human endothelial cells

Heo

et al. 2017

International Journal of Molecular Medicine

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In this study, a marine microalga Spirulina sp.-derived protein was hydrolyzed using gastrointestinal enzymes to produce an angiotensin I (Ang I)-converting enzyme (ACE) inhibitory peptide. Following consecutive purification, the potent ACE inhibitory peptide was composed of 7 amino acids, Thr-Met-Glu-Pro-Gly-Lys-Pro (molecular weight, 759 Da). Analysis using the Lineweaver-Burk plot and molecular modeling suggested that the purified peptide acted as a mixed non-competitive inhibitor of ACE. The inhibitory effects of the peptide against the cellular production of vascular dysfunction-related factors induced by Ang II were also investigated. In human endothelial cells, the Ang II-induced production of nitric oxide and reactive oxygen species was inhibited, and the expression of inducible nitric oxide synthase (iNOS) and endothelin-1 (ET-1) was downregulated when the cells were cultured with the purified peptide. Moreover, the peptide blocked the activation of p38 mitogen-activated protein kinase. These results indicated that this Spirulina sp.-derived peptide warrants further investigation as a potential pharmacological inhibitor of ACE and vascular dysfunction.

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“…of 8 led to a reduction of 28.6 mmHg in the SBP in SHR, whereas the same dosage of the reference drug captopril decreased SBP by 31.3 mmHg. This phlorotannin 8 is less active than octaphlorethol 2 [40] since the dose of 8 used was two times higher than the dose of 2 (Table 1). Thus, the latter seems to be more promising for anti-hypertensive applications.…”

Section: Other Phlorotanninsmentioning

confidence: 94%

“…of 2 led to a reduction of 21.9 mmHg in the systolic blood pressure (SBP) in spontaneously hypertensive rats (SHR), against the 26.3 mmHg reduction obtained using the same dosage of the reference drug captopril. The anti-hypertensive effect was maintained for 6 h, and the authors suggested this effect was due to the induction of NO production, which is a vasodilator [40].…”

Section: Octaphlorethol Amentioning

confidence: 99%

Seaweed Secondary Metabolites with Beneficial Health Effects: An Overview of Successes in In Vivo Studies and Clinical Trials

et al. 2019

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Macroalgae are increasingly viewed as a source of secondary metabolites with great potential for the development of new drugs. In this development, in vitro studies are only the first step in a long process, while in vivo studies and clinical trials are the most revealing stages of the true potential and limitations that a given metabolite may have as a new drug. This literature review aims to give a critical overview of the secondary metabolites that reveal the most interesting results in these two steps. Phlorotannins show great pharmaceutical potential in in vivo models and, among the several examples, the anti-dyslipidemia activity of dieckol must be highlighted because it was more effective than lovastatin in an in vivo model. The IRLIIVLMPILMA tridecapeptide that exhibits an in vivo level of activity similar to the hypotensive clinical drug captopril should still be stressed, as well as griffithsin which showed such stunning results over a variety of animal models and which will probably move onto clinical trials soon. Regarding clinical trials, studies with pure algal metabolites are scarce, limited to those carried out with kahalalide F and fucoxanthin. The majority of clinical trials currently aim to ascertain the effect of algae consumption, as extracts or fractions, on obesity and diabetes.Studies focusing on the preparation of macroalgae extracts and their chemical characterization revealed a large range of seaweed compounds with very interesting biological activities including antitumor, anti-inflammatory, antimicrobial, antidiabetic, antivirus, antihypertensive, fat-lowering, and neuroprotective activities [12][13][14][15].The large volume of studies proving the seaweed compound activities in in vitro systems [16][17][18][19] hints the need for further advancements in the knowledge about macroalgae compound efficiency in living systems (in vivo) and their use in the development of pharmaceuticals. In vitro studies are very relevant and yield very important information, but they only represent the first step of a long process, and the results obtained rarely reveal anything about the effects of a compound in vivo, because the responses observed in vitro can be magnified, diminished, or totally different in a more complex and integrated system. In fact, in vivo studies and clinical trials are those which contribute most to truly understanding the real potential of compounds as future pharmaceuticals.In this regard, the present work intends to present insight into the results obtained in the last few years regarding secondary metabolites, such as phlorotannins, halogenated compounds, fucoxanthin, and fucosterol isolated from macroalgae, involved in in vivo studies and clinical trials, identifying the research opportunities and knowledge gaps, to valorize these compounds and their natural resources. The intention is not to present an exhaustive survey of all published works, but rather a selection of authors based on the following criteria: in-depth studies involving pure compounds most characteristic f...

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Angiotensin I-converting enzyme (ACE) inhibition and nitric oxide (NO)-mediated antihypertensive effect of octaphlorethol A isolated from Ishige sinicola: In vitro molecular mechanism and in vivo SHR model

Cited by 25 publications

References 36 publications

Exploring bioactive fraction of Sargassum wightii: In vitro elucidation of angiotensin-I-converting enzyme inhibition and antioxidant potential

Exploring bioactive fraction of Sargassum wightii: In vitro elucidation of angiotensin-I-converting enzyme inhibition and antioxidant potential

A heptameric peptide purified from Spirulina sp. gastrointestinal hydrolysate inhibits angiotensin I-converting enzyme- and angiotensin II-induced vascular dysfunction in human endothelial cells

Seaweed Secondary Metabolites with Beneficial Health Effects: An Overview of Successes in In Vivo Studies and Clinical Trials

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