The Effect of Phloroglucinol, A Component of Ecklonia cava Extract, on Hepatic Glucose Production

Yoon, Ji-Young; Choi, Hojung; Jun, Hee-Sook

doi:10.3390/md15040106

Cited by 32 publications

(24 citation statements)

References 37 publications

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“…Phloroglucinol has also been reported to have antioxidant activity and the ability to decrease the formation of advanced glycation end products . Furthur, Yoon et al reported that phloroglucinol reduced blood glucose levels in diabetes . Thus, the present study was conducted to evaluate the protective role of phloroglucinol in myocardial reperfusion injury in diabetic rats.…”

Section: Introductionmentioning

confidence: 87%

Phloroglucinol, a nutraceutical for IR‐induced cardiac damage in diabetic rats

Nayak

Ganesha

Minaz

et al. 2019

Anim Models and Exp Med

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Background: Myocardial injury due to ischemia-reperfusion (IR) is aggravated in diabetes which is associated with oxidative stress. Alleviating oxidative stress via use of antioxidants has been shown to be effective at minimizing myocardial cell death and improving cardiac function. The aim of the present study was to evaluate the cardioprotective effect of phloroglucinol against myocardial reperfusion injury (MRI) in diabetic rats.Methods: Diabetes was induced in female rats with streptozotocin (50 mg/kg). The diabetic rats were orally treated with phloroglucinol (100 and 200 mg/kg daily for 28 days). After treatment the hearts were isolated and mounted on a Langendorff apparatus. The hearts were subjected to 15 minutes of IR to induce myocardial damage. Cardiac functions including heart rate (HR), resting and developed tension, and rate of change of contraction (+dP/dt max ) were recorded. Cardiac injury biomarkers lactate dehydrogenase (LDH) and creatine kinase (CK-MB) were measured in the heart perfusate. Levels of the antioxidant enzymes reduced glutathione (GSH) and malondialdehyde (MDA) were measured. Hematoxylin and eosin (H&E) staining was also performed. Results:After IR injury, a decrease in HR and +dP/dt max in hearts from diabetic rat was seen compared to healthy rat hearts, which was reversed by phloroglucinol treatment. Myocardial infarct size, measured by H&E staining, was increased in diabetic rats compared to healthy rats and an increase in the activity of LDH and CK-MB in the heart perfusate in diabetic rats was decreased by phloroglucinol treatment.An increase in MDA levels and a decrease in levels of antioxidant enzymes were observed in diabetic rats, which was reversed with phloroglucinol treatment. Conclusion:Phloroglucinol treatment has potential therapeutic promise in the treatment of MRI in diabetes. K E Y W O R D SLangendroff apparatus, myocardial reperfusion injury, phloroglucinol, streptozotocin | 211 PRANAV NAYAK et Al.

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Section: Introductionmentioning

confidence: 87%

Phloroglucinol, a nutraceutical for IR‐induced cardiac damage in diabetic rats

Nayak

Ganesha

Minaz

et al. 2019

Anim Models and Exp Med

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“…Specifically, oral administration of PGL in diabetic rats, at a concentration of 100, 200 or 250 mg/kg (bw), improved the levels of glucose, proteins and creatinine, by exerting protective effects against diabetes-mellitus complications 10 . In mice, treatment with PGL, at 100 mg/kg (bw) dose, reduces glucose tolerance by partially inhibiting the phospho-enol pyruvate carboxy-kinase (PEPCK) and glucose-6-phosphatase (G6Pase) enzymes in the liver, and influencing the AMP-activated protein kinase α (AMPKα) signaling pathway 12 . Low doses of PGL oral administration (1-16 mg/kg) have been causatively associated with anti-anxiety effects in mice, while its high doses even up to 300 mg/kg (bw) could be well tolerated by the experimental animals 13 .…”

Section: Discussionmentioning

confidence: 99%

Exploitation of Drosophila Choriogenesis Process as a Model Cellular System for Assessment of Compound Toxicity: the Phloroglucinol Paradigm

Keramaris¹,

Κωνσταντόπουλος²,

Margaritis³

et al. 2020

Sci Rep

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Phloroglucinol (1,3,5 tri-hydroxy-benzene) (PGL), a natural phenolic substance, is a peroxidase inhibitor and has anti-oxidant, anti-diabetic, anti-inflammatory, anti-thrombotic, radio-protective, spasmolytic and anti-cancer activities. PGL, as a medicine, is administered to patients to control the symptoms of irritable bowel syndrome and acute renal colic, in clinical trials. PGL, as a phenolic substance, can cause cytotoxic effects. Administration of PGL up to 300 mg/kg (bw) is well tolerated by animals, while in cell lines its toxicity is developed at concentrations above the dose of 10 μg/ml. Furthermore, it seems that tumor or immortalized cells are more susceptible to the toxic power of PGL, than normal cells. However, studies of its cytotoxic potency, at the cellular level, in complex, differentiated and metamitotic biological systems, are still missing. In the present work, we have investigated the toxic activity of PGL in somatic epithelial cells, constituting the follicular compartment of a developing egg-chamber (or, follicle), which directs the choriogenesis (i.e. chorion assembly) process, during late oogenesis of Drosophila melanogaster. our results reveal that treatment of in vitro growing Drosophila follicles with PGL, at a concentration of 0.2 mM (or, 25.2 μg/ml), does not lead to follicle-cell toxicity, since the protein-synthesis program and developmental pattern of choriogenesis are normally completed. Likewise, the 1 mM dose of PGL was also characterized by lack of toxicity, since the chorionic proteins were physiologically synthesized and the chorion structure appeared unaffected, except for a short developmental delay, being observed. In contrast, concentrations of 10, 20 or 40 mM of PGL unveiled a dose-dependent, increasing, toxic effect, being initiated by interruption of protein synthesis and disassembly of cell-secretory machinery, and, next, followed by fragmentation of the granular endoplasmic reticulum (ER) into vesicles, and formation of autophagic vacuoles. Follicle cells enter into an apoptotic process, with autophagosomes and large vacuoles being formed in the cytoplasm, and nucleus showing protrusions, granular nucleolus and condensed chromatin. PGL, also, proved able to induce disruption of nuclear envelope, activation of nucleus autophagy (nucleophagy) and formation of a syncytium-like pattern being produced by fusion of plasma membranes of two or more individual follicle cells. Altogether, follicle cell-dependent choriogenesis in Drosophila has been herein presented as an excellent, powerful and reliable multi-cellular, differentiated, model biological (animal) system for drug-cytotoxicity assessment, with the versatile compound PGL serving as a characteristic paradigm. In conclusion, PGL is a substance that may act beneficially for a variety of pathological conditions and can be safely used for differentiated somatic-epithelial-cells at clinically low concentrations. At relatively high doses, it could potentially induce apoptotic and autophagic cell death, thus being likely ...

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“…As shown in Table 1, phloroglucinol 1 (100 mg/kg b.w.) significantly improved glucose tolerance in C57BL/6J male mice whose diet was high in fat and inhibited glucose synthesis in primary mouse hepatocytes [37]. This phlorotannin also exerts efficient cell protection against ionizing radiation and extends the survival of mice exposed to a lethal dose of γ-radiation.…”

Section: Phloroglucinolmentioning

confidence: 94%

“…13% improvement in glucose tolerance compared to untreated group. 60% inhibition of glucose synthesis in primary mouse hepatocytes [37]. ICR mice 20 mg/kg (b.w.…”

Section: Phlorotanninsmentioning

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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The Effect of Phloroglucinol, A Component of Ecklonia cava Extract, on Hepatic Glucose Production

Cited by 32 publications

References 37 publications

Phloroglucinol, a nutraceutical for IR‐induced cardiac damage in diabetic rats

Phloroglucinol, a nutraceutical for IR‐induced cardiac damage in diabetic rats

Exploitation of Drosophila Choriogenesis Process as a Model Cellular System for Assessment of Compound Toxicity: the Phloroglucinol Paradigm

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

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