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Molecular insights and therapeutic implications of nanoengineered dietary polyphenols for targeting lung carcinoma: part I

Das SS, Tambe S, Prasad Verma PR, Amin P, Singh N, Singh SK, et al.

Nanomedicine (Lond), 2022 Oct;17(23):1779-1798.
PMID: 36636930 DOI: 10.2217/nnm-2022-0133

Lung cancer is the second leading cause of cancer-related mortality globally, and non-small-cell lung cancer accounts for most lung cancer cases. Nanotechnology-based drug-delivery systems have exhibited immense potential in lung cancer therapy due to their fascinating physicochemical characteristics, in vivo stability, bioavailability, prolonged and targeted delivery, gastrointestinal absorption and therapeutic efficiency of their numerous chemotherapeutic agents. However, traditional chemotherapeutics have systemic toxicity issues; therefore, dietary polyphenols might potentially replace them in lung cancer treatment. Polyphenol-based targeted nanotherapeutics have demonstrated interaction with a multitude of protein targets and cellular signaling pathways that affect major cellular processes. This review summarizes the various molecular mechanisms and targeted therapeutic potentials of nanoengineered dietary polyphenols in the effective management of lung cancer.

Matched MeSH terms: Polyphenols/therapeutic use
The Potential Use of Honey as a Neuroprotective Agent for the Management of Neurodegenerative Diseases

Fadzil MAM, Mustar S, Rashed AA

Nutrients, 2023 Mar 23;15(7).
PMID: 37049399 DOI: 10.3390/nu15071558

As the global population ages, there is an increasing research on managing neurodegenerative diseases that mainly affect the elderly. Honey is one of the natural products and functional foods widely studied for its neuroprotective properties. This review investigates honey's effectiveness as a neuroprotective agent through in vitro, in vivo, and clinical research. The articles were browsed from three databases (PubMed, ScienceDirect, and Scopus) between the years of 2012 and 2022 using the keywords "honey" crossed with "neurodegenerative". Out of the 16 articles, six in vitro, eight in vivo, one combination study, and one clinical intervention were compiled. Among the various types of honey studied, the Tualang and Thyme honey exhibited the highest antioxidant, anti-inflammatory, and anticholinesterase activity, leading to the prevention and management of multiple neurodegenerative diseases such as Alzheimer's disease. The neuroprotective properties of honey are primarily attributed to its high polyphenol content, with quercetin and gallic acid being the most prominent. This review compiled considerable evidence of the anti-neurodegenerative properties of honey presented by in vitro and in vivo studies. However, more clinical intervention studies are required to support these findings further.

Matched MeSH terms: Polyphenols/therapeutic use
Quercetin: an effective polyphenol in alleviating diabetes and diabetic complications

Yan L, Vaghari-Tabari M, Malakoti F, Moein S, Qujeq D, Yousefi B, et al.

Crit Rev Food Sci Nutr, 2023;63(28):9163-9186.
PMID: 35468007 DOI: 10.1080/10408398.2022.2067825

Various studies, especially in recent years, have shown that quercetin has beneficial therapeutic effects in various human diseases, including diabetes. Quercetin has significant anti-diabetic effects and may be helpful in lowering blood sugar and increasing insulin sensitivity. Quercetin appears to affect many factors and signaling pathways involved in insulin resistance and the pathogenesis of type 2 of diabetes. TNFα, NFKB, AMPK, AKT, and NRF2 are among the factors that are affected by quercetin. In addition, quercetin can be effective in preventing and ameliorating the diabetic complications, including diabetic nephropathy, cardiovascular complications, neuropathy, delayed wound healing, and retinopathy, and affects the key mechanisms involved in the pathogenesis of these complications. These positive effects of quercetin may be related to its anti-inflammatory and anti-oxidant properties. In this article, after a brief review of the pathogenesis of insulin resistance and type 2 diabetes, we will review the latest findings on the anti-diabetic effects of quercetin with a molecular perspective. Then we will review the effects of quercetin on the key mechanisms of pathogenesis of diabetes complications including nephropathy, cardiovascular complications, neuropathy, delayed wound healing, and retinopathy. Finally, clinical trials investigating the effect of quercetin on diabetes and diabetes complications will be reviewed.

Matched MeSH terms: Polyphenols/therapeutic use
Polyphenols: Potential Future Arsenals in the Treatment of Diabetes

Solayman M, Ali Y, Alam F, Islam MA, Alam N, Khalil MI, et al.

Curr Pharm Des, 2016;22(5):549-65.
PMID: 26601968

Diabetes mellitus (DM) is one of the most common endocrine metabolic disorders. In addition to exercise and diet, oral anti-diabetic drugs have been used as a part of the management strategy worldwide. Unfortunately, none of the conventional anti-diabetic drugs are without side effects, and these drugs pose an economic burden. Therefore, the investigation of novel anti-diabetic regimens is a major challenge for researchers, in which nature has been the primary resource for the discovery of potential therapeutics. Many plants have been shown to act as anti-diabetic agents, in which the main active constituents are believed to be polyphenols. Natural products containing high polyphenol levels can control carbohydrate metabolism by various mechanisms, such as protecting and restoring beta-cell integrity, enhancing insulin releasing activity, and increasing cellular glucose uptake. Blackberries, red grapes, apricots, eggplant and popular drinks such as coffee, cocoa and green tea are all rich in polyphenols, which may dampen insulin resistance and be natural alternatives in the treatment of diabetes. Therefore, the aim of this review is to report on the available anti-diabetic polyphenols (medicinal plants, fruits and vegetables), their mechanisms in the various pathways of DM and their correlations with DM. Additionally, this review emphasizes the types of polyphenols that could be potential future resources in the treatment of DM via either novel regimens or as supplementary agents.

Matched MeSH terms: Polyphenols/therapeutic use*
Molecular insights and therapeutic implications of nanoengineered dietary polyphenols for targeting lung cancer: part II

Das SS, Tambe S, Prasad Verma PR, Amin P, Singh N, Singh SK, et al.

Nanomedicine (Lond), 2022 Oct;17(23):1799-1816.
PMID: 36636965 DOI: 10.2217/nnm-2022-0117

Flavonoids represent a major group of polyphenolic compounds. Their capacity to inhibit tumor proliferation, cell cycle, angiogenesis, migration and invasion is substantially responsible for their chemotherapeutic activity against lung cancer. However, their clinical application is limited due to poor aqueous solubility, low permeability and quick blood clearance, which leads to their low bioavailability. Nanoengineered systems such as liposomes, nanoparticles, micelles, dendrimers and nanotubes can considerably enhance the targeted action of the flavonoids with improved efficacy and pharmacokinetic properties, and flavonoids can be successfully translated from bench to bedside through various nanoengineering approaches. This review addresses the therapeutic potential of various flavonoids and highlights the cutting-edge progress in the nanoengineered systems that incorporate flavonoids for treating lung cancer.

Matched MeSH terms: Polyphenols/therapeutic use
Fulltext The anticancer mechanism of action of selected polyphenols in triple-negative breast cancer (TNBC)

Farghadani R, Naidu R

Biomed Pharmacother, 2023 Sep;165:115170.
PMID: 37481930 DOI: 10.1016/j.biopha.2023.115170

Breast cancer is a leadingcause of cancer-related deaths in women globally, with triple-negative breast cancer (TNBC) being an aggressive subtype that lacks targeted therapies and is associated with a poor prognosis. Polyphenols, naturally occurring compounds in plants, have been investigated as a potential therapeutic strategy for TNBC. This review provides an overview of the anticancer effects of polyphenols in TNBC and their mechanisms of action. Several polyphenols, including resveratrol, quercetin, kaempferol, genistein, epigallocatechin-3-gallate, apigenin, fisetin, hesperetin and luteolin, have been shown to inhibit TNBC cell proliferation, induce cell cycle arrest, promote apoptosis, and suppress migration/invasion in preclinical models. The molecular mechanisms underlying their anticancer effects involve the modulation of several signalling pathways, such as PI3K/Akt, MAPK, STATT, and NF-κB pathways. Polyphenols also exhibit synergistic effects with chemotherapy drugs, making them promising candidates for combination therapy. The review also highlights clinical trials investigating the potential use of polyphenols, individually or in combination therapy, against breast cancer. This review deepens the under-standing of the mechanism of action of respective polyphenols and provides valuable insights into the potential use of polyphenols as a therapeutic strategy for TNBC, and lays the groundwork for future research in this area.

Matched MeSH terms: Polyphenols/therapeutic use
Fulltext Immunomodulatory Effects of Diet and Nutrients in Systemic Lupus Erythematosus (SLE): A Systematic Review

Islam MA, Khandker SS, Kotyla PJ, Hassan R

Front Immunol, 2020;11:1477.
PMID: 32793202 DOI: 10.3389/fimmu.2020.01477

Systemic lupus erythematosus (SLE) is an autoimmune disease characterized by multiple organ involvement, including the skin, joints, kidneys, lungs, central nervous system and the haematopoietic system, with a large number of complications. Despite years of study, the etiology of SLE remains unclear; thus, safe and specifically targeted therapies are lacking. In the last 20 years, researchers have explored the potential of nutritional factors on SLE and have suggested complementary treatment options through diet. This study systematically reviews and evaluates the clinical and preclinical scientific evidence of diet and dietary supplementation that either alleviate or exacerbate the symptoms of SLE. For this review, a systematic literature search was conducted using PubMed, Scopus and Google Scholar databases only for articles written in the English language. Based on the currently published literature, it was observed that a low-calorie and low-protein diet with high contents of fiber, polyunsaturated fatty acids, vitamins, minerals and polyphenols contain sufficient potential macronutrients and micronutrients to regulate the activity of the overall disease by modulating the inflammation and immune functions of SLE.

Matched MeSH terms: Polyphenols/therapeutic use
Plant Polyphenols as Neuroprotective Agents in Parkinson's Disease Targeting Oxidative Stress

Hor SL, Teoh SL, Lim WL

Curr Drug Targets, 2020;21(5):458-476.
PMID: 31625473 DOI: 10.2174/1389450120666191017120505

Parkinson's disease (PD) is the second most prevalent progressive neurodegenerative disorder characterized by the degeneration of dopaminergic neurons in the human midbrain. Various ongoing research studies are competing to understand the pathology of PD and elucidate the mechanisms underlying neurodegeneration. Current pharmacological treatments primarily focused on improving dopamine metabolism in PD patients, despite the side effects of long-term usage. In recent years, it is recognized that oxidative stress-mediated pathways lead to neurodegeneration in the brain, which is associated with the pathophysiology of PD. The importance of oxidative stress is often less emphasized when developing potential therapeutic approaches. Natural plant antioxidants have been shown to mediate the oxidative stress-induced effects in PD, which has gained considerable attention in both in vitro and in vivo studies. Yet, clinical trials on natural polyphenol compounds are limited, restricting the potential use of these compounds as an alternative treatment for PD. Therefore, this review provides an understanding of the oxidative stress-induced effects in PD by elucidating the underlying events contributing to oxidative stress and explore the potential use of polyphenols in improving the oxidative status in PD. Preclinical findings have supported the potential of polyphenols in providing neuroprotection against oxidative stress-induced toxicity in PD. However, limiting factors, such as safety and bioavailability of polyphenols, warrant further investigations so as to make them the potential target for clinical applications in the treatment and management of PD.

Matched MeSH terms: Polyphenols/therapeutic use
Potential natural antioxidants: adjuvant effect of green tea polyphenols in periodontal infections

Ramasamy C

Infect Disord Drug Targets, 2015;15(3):141-52.
PMID: 26321324

OBJECTIVES: Polyphenols constitute the major component in green tea, which represent a cluster known as catechins. The presence of polyphenols, especially the amino acid theanine and catechins with its antioxidant properties in green tea make them ideal for medicinal- dental applications. The objective of the paper is to delineate the role of green tea polyphenols in periodontal disease.
METHODS: The Pub med data base was searched for human clinical studies, reviews pertinent to application of green tea polyphenols in periodontal health dating from Sep 1980- Sep 2014.
RESULTS: The retrieved inference from the epidemiological surveys, in vitro studies and overviews of polyphenols, postulate green tea as potential natural antioxidant. Green tea mouthwashes possess limitations, which make them ineffective during the chronic stages of periodontitis. Human studies reveal that the prognosis of periodontal disease is better when the green tea catechins are used via local drug delivery.
CONCLUSION: The maintenance of periodontal health could be enhanced by emphasizing the habit of drinking green tea in periodontitis patients. The future scope of the research demands the analysis of polyphenols at molecular level to have a better understanding of its overwhelming applications.

Matched MeSH terms: Polyphenols/therapeutic use*
Fulltext Dietary Polyphenols: A Multifactorial Strategy to Target Alzheimer's Disease

Dhakal S, Kushairi N, Phan CW, Adhikari B, Sabaratnam V, Macreadie I

Int J Mol Sci, 2019 Oct 14;20(20).
PMID: 31615073 DOI: 10.3390/ijms20205090

Ageing is an inevitable fundamental process for people and is their greatest risk factor for neurodegenerative disease. The ageing processes bring changes in cells that can drive the organisms to experience loss of nutrient sensing, disrupted cellular functions, increased oxidative stress, loss of cellular homeostasis, genomic instability, accumulation of misfolded protein, impaired cellular defenses and telomere shortening. Perturbation of these vital cellular processes in neuronal cells can lead to life threatening neurological disorders like Alzheimer's Disease, Parkinson's Disease, Huntington's Disease, Lewy body dementia, etc. Alzheimer's Disease is the most frequent cause of deaths in the elderly population. Various therapeutic molecules have been designed to overcome the social, economic and health care burden caused by Alzheimer's Disease. Almost all the chemical compounds in clinical practice have been found to treat symptoms only limiting them to palliative care. The reason behind such imperfect drugs may result from the inefficiencies of the current drugs to target the cause of the disease. Here, we review the potential role of antioxidant polyphenolic compounds that could possibly be the most effective preventative strategy against Alzheimer's Disease.

Matched MeSH terms: Polyphenols/therapeutic use*
New insights into seaweed polyphenols on glucose homeostasis

Murugan AC, Karim MR, Yusoff MB, Tan SH, Asras MF, Rashid SS

Pharm Biol, 2015 Aug;53(8):1087-97.
PMID: 25630358 DOI: 10.3109/13880209.2014.959615

CONTEXT: Polyphenol-rich marine macroalgae are gaining dietary importance due to their influence over diabetes mellitus and the role as a vital source of high-value nutraceuticals. Their assorted beneficial effects on human health include competitive inhibition of digestive enzymes, varying the activity of hepatic glucose-metabolizing enzymes, lowering the plasma glucose levels, and lipid peroxidation, delaying the aging process.
OBJECTIVE: In this paper, we review the health beneficial effects of polyphenols and phlorotannins from brown seaweeds with special emphasis on their inhibitory effects on carbohydrate-metabolizing enzymes.
METHODS: A survey of literature from databases such as Sciencedirect, Scopus, Pubmed, Springerlink, and Google Scholar from the year 1973 to 2013 was done to bring together the information relating to drug discovery from brown seaweeds as a source for diabetes treatment.
RESULTS: Over the past two decades, 20 different bioactive polyphenols/phlorotannins have been isolated and studied from 10 different brown algae. Discussion of the positive effect on the inhibition of enzymes metabolizing carbohydrates in both in vitro and in vivo experiments are included.
CONCLUSION: Despite the recent advancements in isolating bioactive compounds from seaweeds with potential health benefit or pharmaceutical behavior, studies on the polyphenol effectiveness on glucose homeostasis in human beings are very few in response to their functional characterization. Added research in this area is required to confirm the close connection of polyphenol rich seaweed-based diet consumption with glucose homeostasis and the exciting possibility of prescribing polyphenols to treat the diabetes pandemic.

Matched MeSH terms: Polyphenols/therapeutic use
Fulltext Medicinal Potential of Isoflavonoids: Polyphenols That May Cure Diabetes

Ahmed QU, Ali AHM, Mukhtar S, Alsharif MA, Parveen H, Sabere ASM, et al.

Molecules, 2020 Nov 24;25(23).
PMID: 33255206 DOI: 10.3390/molecules25235491

In recent years, there is emerging evidence that isoflavonoids, either dietary or obtained from traditional medicinal plants, could play an important role as a supplementary drug in the management of type 2 diabetes mellitus (T2DM) due to their reported pronounced biological effects in relation to multiple metabolic factors associated with diabetes. Hence, in this regard, we have comprehensively reviewed the potential biological effects of isoflavonoids, particularly biochanin A, genistein, daidzein, glycitein, and formononetin on metabolic disorders and long-term complications induced by T2DM in order to understand whether they can be future candidates as a safe antidiabetic agent. Based on in-depth in vitro and in vivo studies evaluations, isoflavonoids have been found to activate gene expression through the stimulation of peroxisome proliferator-activated receptors (PPARs) (α, γ), modulate carbohydrate metabolism, regulate hyperglycemia, induce dyslipidemia, lessen insulin resistance, and modify adipocyte differentiation and tissue metabolism. Moreover, these natural compounds have also been found to attenuate oxidative stress through the oxidative signaling process and inflammatory mechanism. Hence, isoflavonoids have been envisioned to be able to prevent and slow down the progression of long-term diabetes complications including cardiovascular disease, nephropathy, neuropathy, and retinopathy. Further thoroughgoing investigations in human clinical studies are strongly recommended to obtain the optimum and specific dose and regimen required for supplementation with isoflavonoids and derivatives in diabetic patients.

Matched MeSH terms: Polyphenols/therapeutic use
High-performance thin-layer chromatographic methods in the evaluation of the antioxidant and anti-hyperglycemic activity of Myrmecodia platytyrea as a promising opportunity in diabetes treatment

Agatonovic-Kustrin S, Morton DW, Adam A, Mizaton HH, Zakaria H

J Chromatogr A, 2017 Dec 29;1530:192-196.
PMID: 29132827 DOI: 10.1016/j.chroma.2017.11.012

The steady increase of diabetes is becoming a major burden on health care systems. As diabetic complications arise from oxidative stress, an antioxidant therapy along with anti-diabetic drugs is recommended. Myrmecodia or ant plant is highly valued as a traditional medicine in West Papua. It is used as an alternative treatment for diabetes, as the substances produced by ants can reduce blood sugar levels. The aim of this study was to develop and establish high-performance thin-layer chromatographic (HPTLC)-bioautographic methods to measure the antioxidant and hypoglycemic effects in different extracts from Myrmecodia platytyrea and to compare them with sterol content. Antioxidant activity in methanol, ethanol, dichloromethane (DCM) and ethyl acetate (EA) extracts were measured with a direct HPTLC-2,2-diphenyl-1-picrylhydrazyl free radical (DPPH) assay, while hypoglycemic effects were assessed using a newly developed α-amylase inhibitory activity assay. Stigmasterol is observed, after derivatization with anisaldehyde, as purple colored zones under visible light at hRF values of 0.66. The highest antioxidant activity was observed in the ethanol extract which is rich in polyphenols and flavonoids, while the DCM extract did not show antioxidant activity, but had significant α-amylase inhibitory activity. The highest α-amylase inhibitory activity was observed in the EA and DCM extracts and was related to their stigmasterol content.

Matched MeSH terms: Polyphenols/therapeutic use
Fulltext Regulation of autophagy by polyphenolic compounds as a potential therapeutic strategy for cancer

Hasima N, Ozpolat B

Cell Death Dis, 2014;5:e1509.
PMID: 25375374 DOI: 10.1038/cddis.2014.467

Autophagy, a lysosomal degradation pathway for cellular constituents and organelles, is an adaptive and essential process required for cellular homeostasis. Although autophagy functions as a survival mechanism in response to cellular stressors such as nutrient or growth factor deprivation, it can also lead to a non-apoptotic form of programmed cell death (PCD) called autophagy-induced cell death or autophagy-associated cell death (type II PCD). Current evidence suggests that cell death through autophagy can be induced as an alternative to apoptosis (type I PCD), with therapeutic purpose in cancer cells that are resistant to apoptosis. Thus, modulating autophagy is of great interest in cancer research and therapy. Natural polyphenolic compounds that are present in our diet, such as rottlerin, genistein, quercetin, curcumin, and resveratrol, can trigger type II PCD via various mechanisms through the canonical (Beclin-1 dependent) and non-canonical (Beclin-1 independent) routes of autophagy. The capacity of these compounds to provide a means of cancer cell death that enhances the effects of standard therapies should be taken into consideration for designing novel therapeutic strategies. This review focuses on the autophagy- and cell death-inducing effects of these polyphenolic compounds in cancer.

Matched MeSH terms: Polyphenols/therapeutic use*
Cytotoxic, apoptotic and anti-α-glucosidase activities of 3,4-di-O-caffeoyl quinic acid, an antioxidant isolated from the polyphenolic-rich extract of Elephantopus mollis Kunth

Ooi KL, Muhammad TS, Tan ML, Sulaiman SF

J Ethnopharmacol, 2011 Jun 1;135(3):685-95.
PMID: 21497647 DOI: 10.1016/j.jep.2011.04.001

The decoction of the whole plant of Elephantopus mollis Kunth. is traditionally consumed to treat various free radical-mediated diseases including cancer and diabetes.

Matched MeSH terms: Polyphenols/therapeutic use
Lignans and Polyphenols of Phyllanthus amarus Schumach and Thonn Induce Apoptosis in HCT116 Human Colon Cancer Cells through Caspases-Dependent Pathway

Mohamed SIA, Jantan I, Nafiah MA, Seyed MA, Chan KM

Curr Pharm Biotechnol, 2021;22(2):262-273.
PMID: 32532192 DOI: 10.2174/1389201021666200612173029

BACKGROUND: The anticancer effects of Phyllanthus amarus extract on various cancer cells have been investigated, however, the effects of its major constituents on HCT116 human colorectal cancer cells have not been reported.
OBJECTIVE: In the present study, we investigated the cytotoxic effect of 80% ethanol extract of P. amarus and its marker constituents (phyllanthin, hypophyllanthin, gallic acid, niranthin, greraniin, phyltetralin, isolintetralin, corilagin and ellagic acid) on HCT116 and their underlying mechanisms of action.
METHODS: Their antiproliferative and apoptotic effects on HCT 116 were performed using MTT assay and flow cytometric analysis, respectively, while caspases 3/7, 8 and 9 activities were examined using the colorimetric method. The expression of cleaved poly ADP ribose polymerase enzyme (PARP) and cytochrome c proteins was investigated by the immune-blot technique.
RESULTS AND DISCUSSION: HPLC and LC-MS/MS analyses demonstrated that the extract contained mainly lignans and polyphenols. The plant samples markedly suppressed the growth and expansion of HCT116 cells in a concentration- and time-dependent manner with no toxicity against normal human fibroblast CCD18 Co. P. amarus extract, phyllanthin and gallic acid induced mode of cell death primarily through apoptosis as confirmed by the exteriorization of phosphatidylserine. Caspases 3/7, 8, and 9 activities increased in a concentration-dependent manner following 24h treatment. The expressions of cleaved PARP (Asp 214) and cytochrome c were markedly upregulated.
CONCLUSION: P. amarus extract, phyllanthin and gallic acid exhibited an apoptotic effect on HCT116 cells through the caspases-dependent pathway.

Matched MeSH terms: Polyphenols/therapeutic use
Fulltext Therapeutic Effects of Olive and Its Derivatives on Osteoarthritis: From Bench to Bedside

Chin KY, Pang KL

Nutrients, 2017 Sep 26;9(10).
PMID: 28954409 DOI: 10.3390/nu9101060

Osteoarthritis is a major cause of morbidity among the elderly worldwide. It is a disease characterized by localized inflammation of the joint and destruction of cartilage, leading to loss of function. Impaired chondrocyte repair mechanisms, due to inflammation, oxidative stress and autophagy, play important roles in the pathogenesis of osteoarthritis. Olive and its derivatives, which possess anti-inflammatory, antioxidant and autophagy-enhancing activities, are suitable candidates for therapeutic interventions for osteoarthritis. This review aimed to summarize the current evidence on the effects of olive and its derivatives, on osteoarthritis and chondrocytes. The literature on animal and human studies has demonstrated a beneficial effect of olive and its derivatives on the progression of osteoarthritis. In vitro studies have suggested that the augmentation of autophagy (though sirtuin-1) and suppression of inflammation by olive polyphenols could contribute to the chondroprotective effects of olive polyphenols. More research and well-planned clinical trials are required to justify the use of olive-based treatment in osteoarthritis.

Matched MeSH terms: Polyphenols/therapeutic use*
Fulltext Antioxidant, antiproliferative, and antiangiogenesis effects of polyphenol-rich seaweed (Sargassum muticum)

Namvar F, Mohamad R, Baharara J, Zafar-Balanejad S, Fargahi F, Rahman HS

Biomed Res Int, 2013;2013:604787.
PMID: 24078922 DOI: 10.1155/2013/604787

In the present study, we evaluated the effect of brown seaweeds Sargassum muticum methanolic extract (SMME), against MCF-7 and MDA-MB-231 breast cancer cell lines proliferation. This algae extract was also evaluated for reducing activity and total polyphenol content. The MTT assay results indicated that the extracts were cytotoxic against breast cancer cell lines in a dose-dependent manner, with IC50 of 22 μg/ml for MCF-7 and 55 μg/ml for MDA-MB-231 cell lines. The percentages of apoptotic MCF-7-treated cells increased from 13% to 67% by increasing the concentration of the SMME. The antiproliferative efficacy of this algal extract was positively correlated with the total polyphenol contents, suggesting a causal link related to extract content of phenolic acids. Cell cycle analysis showed a significant increase in the accumulation of SMME-treated cells at sub-G1 phase, indicating the induction of apoptosis by SMME. Further apoptosis induction was confirmed by Hoechst 33342 and AO/PI staining. Also SMME implanted in vivo into fertilized chicken eggs induced dose-related antiangiogenic activity in the chorioallantoic membrane (CAM). Our results imply a new insight on the novel function of Sargassum muticum polyphenol-rich seaweed in cancer research by induction of apoptosis, antioxidant, and antiangiogenesis effects.

Matched MeSH terms: Polyphenols/therapeutic use

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