Dietary Bioactive Compounds Research Articles

DNA methylation and non-coding RNAs in metabolic disorders: Epigenetic Roles of Nutrients, Dietary Patterns and Weight Loss Interventions for Precision Nutrition.

Dysregulation of epigenetic processes and abnormal epigenetic profiles are associated with various metabolic disorders. Nutrition, as an environmental factor, can induce epigenetic changes through both direct exposure and transgenerational inheritance, continuously altering gene expression and shaping the phenotype. Nutrients consumed through food or supplementation, such as vitamin B12, folate, vitamin B6, and choline, play a pivotal role in DNA methylation, a critical process for gene regulation. Additionally, there is mounting evidence that the expression of non-coding RNAs (ncRNAs) can be modulated by the intake of specific nutrients and natural compounds, thereby influencing processes involved in the onset and progression of metabolic diseases. Evidence suggests that dietary patterns, weight-loss interventions, nutrients and nutritional bioactive compounds can modulate the expression of various miRNAs and DNA methylation levels, contributing to development of metabolic disorders such as obesity and type 2 diabetes. Furthermore, several studies have proposed that DNA methylation and microRNA (miRNA) expression could serve as biomarkers for the effects of weight-loss programs. Despite ongoing debate regarding the effects of nutrient supplementation on DNA methylation levels and the expression of ncRNAs, certain DNA methylation marks and ncRNA expressions might predict the risk of metabolic disorders and act as biomarkers for forecasting the success of therapies within the framework of precision medicine and nutrition. The role of DNA methylation and miRNA expression as potential mediators of the effects of weight loss underscores their potential as biomarkers for the outcomes of weight loss programs. This highlights the influence of dietary patterns and weight-loss interventions on the regulation of miRNA expression and DNA methylation levels, suggesting an interaction between these epigenetic factors and the body's response to weight loss.

Reinventing gut health: leveraging dietary bioactive compounds for the prevention and treatment of diseases.

The human gut harbors a complex and diverse microbiota essential for maintaining health. Diet is the most significant modifiable factor influencing gut microbiota composition and function, particularly through bioactive compounds like polyphenols, dietary fibers, and carotenoids found in vegetables, fruits, seafood, coffee, and green tea. These compounds regulate the gut microbiota by promoting beneficial bacteria and suppressing harmful ones, leading to the production of key microbiota-derived metabolites such as short-chain fatty acids, bile acid derivatives, and tryptophan metabolites. These metabolites are crucial for gut homeostasis, influencing gut barrier function, immune responses, energy metabolism, anti-inflammatory processes, lipid digestion, and modulation of gut inflammation. This review outlines the regulatory impact of typical bioactive compounds on the gut microbiota and explores the connection between specific microbiota-derived metabolites and overall health. We discuss how dietary interventions can affect disease development and progression through mechanisms involving these metabolites. We examine the roles of bioactive compounds and their metabolites in the prevention and treatment of diseases including inflammatory bowel disease, colorectal cancer, cardiovascular diseases, obesity, and type 2 diabetes mellitus. This study provides new insights into disease prevention and underscores the potential of dietary modulation of the gut microbiota as a strategy for improving health.

Isoliquiritigenin: A natural compound with a promising role in inhibiting breast cancer lung metastasis

Background and aimIsoliquiritigenin (ISL) is a dietary bioactive compound that is derived from the roots of licorice and various other plants. Accumulating evidence suggests that ISL has noteworthy anticancer activity in a variety of cancer cells, but it is currently unknown how ISL affects the invasion and migration of breast cancer (BC) cells. Hence, the purpose of this study to determine the inhibitory effect of ISL on cell invasion, migration, and metastasis of BC cells in 4T1-treated lung metastatic animal models. Experimental ProcedureISL was found to inhibit BC lung metastasis, as confirmed by MTT assay, clonogenic assay, wound healing assay, transwell assay, histological analysis, western blot and bioluminescence assay in the xenograft model. Results and conclusionThe in vitro studies revealed that ISL treatment significantly prevented BC cell invasion and migration for 24 h. ISL decreased the protein expressions of PI3K, Akt, p-Akt, mTOR, p-mTOR, matrix metalloproteinase (MMP)-2, MMP-9, and N-cadherin , thereby inhibiting BC cell invasion. In addition, ISL decreased MMP-2/9 and N-cadherin expression in lung tissues and reduced mouse 4T1 BC cell lung metastasis. Based on these findings, it suggests that ISL inhibits cell migration and invasion in BC cells by inhibiting the PI3K/Akt signaling pathway and decreasing the activation of MMP-2 and MMP-9 expression. Therefore, ISL may be useful in managing BC invasion and metastasis.

Kaempferol as a novel inhibitor of SARS-CoV-2 RNA-dependent RNA polymerase

Severe acute respiratory syndrome coronavirus 2 (SARS‐CoV‐2) has quickly become a global health pandemic. Among the viral proteins, RNA‐dependent RNA polymerase (RdRp) is responsible for viral genome replication and has emerged as a promising target against SARS‐CoV‐2 infection. Dietary bioactive compounds represent an important source of evolutionarily optimized molecules with antiviral properties against SARS-CoV-2 RdRp. We investigated the inhibitory potential effects of different phytochemicals against SARS-CoV-2 RdRp, including andrographolide, kaempferol, resveratrol, and silibinin. Unlike the other investigated compounds, kaempferol exhibited a significant dose-dependent in vitro inhibition of SARS-CoV-2 RdRp activity. To assess the binding interactions and stability of the SARS-CoV-2 RdRp-kaempferol complex, we performed in silico techniques, including molecular docking, quantum chemical calculation, and molecular dynamics simulations. We found strong binding affinities and stability between kaempferol and SARS-CoV-2 RdRp variants (Wuhan and Omicron). These findings provide valuable insights into the antiviral properties of kaempferol as a stable inhibitor of SARS-CoV-2 RdRp. Communicated by Ramaswamy H. Sarma

Nutritional Epigenomics: Bioactive Dietary Compounds in the Epigenetic Regulation of Osteoarthritis.

Nutritional epigenomics is exceptionally important because it describes the complex interactions among food compounds and epigenome modifications. Phytonutrients or bioactive compounds, which are secondary metabolites of plants, can protect against osteoarthritis by suppressing the expression of inflammatory and catabolic mediators, modulating epigenetic changes in DNA methylation, and the histone or chromatin remodelling of key inflammatory genes and noncoding RNAs. The combination of natural epigenetic modulators is crucial because of their additive and synergistic effects, safety and therapeutic efficacy, and lower adverse effects than conventional pharmacology in the treatment of osteoarthritis. In this review, we have summarized the chondroprotective properties of bioactive compounds used for the management, treatment, or prevention of osteoarthritis in both human and animal studies. However, further research is needed into bioactive compounds used as epigenetic modulators in osteoarthritis, in order to determine their potential value for future clinical applications in osteoarthritic patients as well as their relation with the genomic and nutritional environment, in order to personalize food and nutrition together with disease prevention.

Rosemary extract activates oligodendrogenesis genes in mouse brain and improves learning and memory ability

Rosemary (Rosmarinus officinalis L.) is a rich source of dietary bioactive compounds such as rosmarinic acid and carnosol with a large repertoire of pharmacological properties, including anti-inflammatory and neuroprotective activities. In the present study, we investigated rosemary as a potential new therapeutic agent for cognitive function and other symptoms of aging. In this present study, we have aimed to investigate the effects of oral administration of rosemary extract (RME) on learning and memory in the context of other biomarkers-related cognitive function and neurotransmitter levels in senescent accelerated prone 8 (SAMP8) mouse, a model of accelerating aging and Alzheimer’s disease. The Morris water maze (MWM) test showed improved spatial learning and memory behavior in RME treated SAMP8 mouse. Moreover, RME decreased Aβ42 and inflammatory cytokine levels and increased BDNF, Sirt1, and neurotransmitter levels in SAMP8 mouse. Whole-genome microarray analysis revealed that RME significantly increased gene expression related to oligodendrocyte differentiation, myelination, and ATP production in the hippocampus and decreased gene expression related to stress, neuroinflammation, and apoptosis. Also, in the SAMP8 hippocampus, RME significantly increased Olig1 and Olig2 expression. Altogether, our study is the first to report improvement of spatial learning and memory of RME, modulation of genes important for oligodendrogenesis, and Anti-neuroinflammatory effect by suppressing Aβ42 levels in mouse brain and thus highlights the prospects of RME in the treatment of cognitive dysfunction and aging.

Fine-Scale Dietary Polyphenol Intake Is Associated with Systemic and Gastrointestinal Inflammation in Healthy Adults

BackgroundPolyphenols are dietary bioactive compounds, many of which have anti-inflammatory properties. However, information on the intake of dietary polyphenols at the class and compound levels and their associations with gastrointestinal (GI) and systemic inflammation is lacking. ObjectivesEstimate dietary polyphenol intake in healthy adults and examine its relationship with GI and systemic inflammation markers. MethodsHealthy adults (n = 350) completed the United States Department of Agriculture Nutritional Phenotyping Study, an observational, cross-sectional study balanced for age, sex, and body mass index. Dietary intake, assessed via multiple 24-h recalls, was ingredientized and mapped to FooDB, a comprehensive food composition database. Dietary polyphenol intake (total, class, compound) was estimated and examined for its relationship to GI and systemic inflammation markers using linear models and random forest regressions. ResultsMean total polyphenol intake was ∼914 mg/1000 kcal/d with flavonoids as the greatest class contributor (495 mg/1000 kcal/d). Tea, coffee, and fruits were among the largest food contributors to polyphenol intake. Total polyphenol intake was negatively associated with the GI inflammation marker, fecal calprotectin (β = −0.004, P = 0.04). At the class level, polyphenols categorized as prenol lipids (β = −0.94, P < 0.01) and phenylpropanoic acids (β = −0.92, P < 0.01) were negatively associated with plasma lipopolysaccharide-binding protein, a proxy for GI permeability. Food sources of these two classes included mainly olive products. We further detected a positive association between C-reactive protein and polyphenols in the “cinnamic acids and derivatives” class using hierarchical feature engineering and random forest modeling. ConclusionsEven in healthy adults, dietary polyphenol intake was negatively associated with GI inflammation and intake of prenol lipids and phenylpropanoic acids was negatively associated with GI permeability. Relationships between polyphenol intake and inflammatory outcomes varied with the resolution—total, class, compound—of polyphenol intake, suggesting a nuanced impact of polyphenols on GI and systemic inflammation.This trial was registered at clinicaltrials.gov as NCT02367287.

Effect of Carbohydrase Treatment on the Dietary Fibers and Bioactive Compounds of Cocoa Bean Shells (CBSs).

Cocoa bean shells (CBSs) are a byproduct of the chocolate production process, representing the external layer of the cocoa bean. CBSs exhibit many interesting chemical and nutritional characteristics resulting in a very rich content of dietary fiber (DF) and antioxidant compounds such as phenolic acids and flavan-3-ols. The DF fraction of CBSs is notably rich in soluble dietary fibers (SDFs), which may be associated with fermentability and prebiotic properties. The objective of this study was the valorization of CBSs through enzymatic treatments, thereby increasing the solubility of DF and potentially augmenting fermentability. CBSs were treated both raw and defatted. Three sets of carbohydrases were used in order to impact the dietary fiber profile. Cellulase, xylanase, pectinase and their combinations were used to perform enzymatic treatments. The application of cellulase, xylanase and a combination of both enzymes proved effective in achieving a high SDF destructuring of the insoluble dietary fiber (IDF) fraction in both defatted and raw CBSs. Notably, the SDF/IDF ratio was significantly elevated in the enzymatically hydrolyzed samples (1.13-1.33) compared to the untreated CBSs (0.33). Furthermore, the various treatments did not affect the antioxidant activity or the content of the main bioactive compounds. These results provide a foundation for new opportunities in the biovalorization of CBSs through green techniques for a range of potential industrial applications in the food and nutraceutical sectors.

Nutrition Intervention and Microbiome Modulation in the Management of Breast Cancer.

Breast cancer (BC) is one of the most common cancers worldwide and a leading cause of cancer-related deaths among women. The escalating incidence of BC underscores the necessity of multi-level treatment. BC is a complex and heterogeneous disease involving many genetic, lifestyle, and environmental factors. Growing evidence suggests that nutrition intervention is an evolving effective prevention and treatment strategy for BC. In addition, the human microbiota, particularly the gut microbiota, is now widely recognized as a significant player contributing to health or disease status. It is also associated with the risk and development of BC. This review will focus on nutrition intervention in BC, including dietary patterns, bioactive compounds, and nutrients that affect BC prevention and therapeutic responses in both animal and human studies. Additionally, this paper examines the impacts of these nutrition interventions on modulating the composition and functionality of the gut microbiome, highlighting the microbiome-mediated mechanisms in BC. The combination treatment of nutrition factors and microbes is also discussed. Insights from this review paper emphasize the necessity of comprehensive BC management that focuses on the nutrition-microbiome axis.

Synergic Role of Dietary Bioactive Compounds in Breast Cancer Chemoprevention and Combination Therapies.

Breast cancer is the most common tumor in women. Chemotherapy is the gold standard for cancer treatment; however, severe side effects and tumor resistance are the major obstacles to chemotherapy success. Numerous dietary components and phytochemicals have been found to inhibit the molecular and signaling pathways associated with different stages of breast cancer development. In particular, this review is focused on the antitumor effects of PUFAs, dietary enzymes, and glucosinolates against breast cancer. The major databases were consulted to search in vitro and preclinical studies; only those with solid scientific evidence and reporting protective effects on breast cancer treatment were included. A consistent number of studies highlighted that dietary components and phytochemicals can have remarkable therapeutic effects as single agents or in combination with other anticancer agents, administered at different concentrations and via different routes of administration. These provide a natural strategy for chemoprevention, reduce the risk of breast cancer recurrence, impair cell proliferation and viability, and induce apoptosis. Some of these bioactive compounds of dietary origin, however, show poor solubility and low bioavailability; hence, encapsulation in nanoformulations are promising tools able to increase clinical efficiency.

Effects of acute consumption of a beverage based on extruded whole-grain pearl millet flour on glycemic and insulinemic control, food intake, and appetite sensation in eutrophic adults: A randomized cross-over clinical trial

ObjectivesWhole-grain pearl millet is a nutritious cereal source of dietary fiber, vitamins, minerals, and bioactive compounds. It offers health benefits such as glycemic control and satiety. Extrusion cooking for diverse formulations, including beverages, can alter its chemical composition, impacting the nutritional value. This study aimed to evaluate the sensory acceptability of an extruded millet flour beverage and its acute effects on glycemic index (GI), glycemic and insulinemic response, food intake, and subjective appetite sensations in euglycemic and eutrophic adults. MethodsThis is an acute, single-blind, randomized, controlled, cross-over clinical study comprising 14 euglycemic and eutrophic adults. Initially, beverages based on whole extruded millet flour were developed, and sensorially and chemically analyzed. Next, a clinical trial was conducted with participants undergoing four sessions and consuming one of the following options: extruded millet beverage, a maltodextrin control beverage, or a glucose solution administered in two separate sessions. Blood glucose, insulin, and appetite responses were assessed over a 2-h period, in addition to determining the GI of the beverages and analyzing food intake in the 24 h following each session. ResultsThe extruded millet flour strawberry-flavored beverage had the best sensory acceptance and was classified as having as high GI. Consumption of the extruded millet beverage showed similar glycemic and insulinemic responses, as well as appetite control and food intake of the subjects, when compared with consumption of the maltodextrin control beverage. ConclusionsIntake of the extruded millet beverage maintained glycemic and insulinemic responses, appetite control, and food intake in euglycemic and eutrophic subjects.

Non-alcoholic fatty liver disease: pathogenesis and assessing the impact of dietary bioactive compounds on the liver

Non-alcoholic fatty liver disease (NAFLD) is a pathological condition ranging from simple steatosis to non-alcoholic steatohepatitis, cirrhosis, and liver cancer. NAFLD is a complex disease mediated by metabolic, environmental, and genetic mechanisms. Many factors such as insulin resistance, lipotoxicity, inflammation, mitochondrial dysfunction, endoplasmic reticulum stress, circadian rhythm, genetics, epigenetics, dietary factors, and gut microbiota play a crucial role in the pathogenesis of NAFLD. Lifestyle changes such as healthy diet, physical activity, avoiding alcohol and smoking are involved in the NAFLD treatment. Dietary bioactive compounds including curcumin, resveratrol, catechins, quercetin, sulforaphane, epigallocatechin-3-gallate, alkaloids, vitamins, and peptides have many health promoting effects such as antioxidant, anti-inflammatory, antihypertensive, chemopreventive, and hepatoprotective. In this review, the pathophysiology of NAFLD and the effects of dietary bioactive compounds on this disease will be discussed in detail with updated information.

Profiling of bioactive compounds identified in functional gummies by metabolomics analysis using High-Resolution Accurate Mass-Spectrometry

The consumers demand for healthier and fortified products received much attention these days. The main aim of this study was to prepare functional gummies that contain beneficial bioactive compounds such as flavonoids, terpenoids, polyphenols, and phenolics. The gummies were prepared using varying concentrations of jamun pulp and pear pomace powder, which are both known for their health benefits. Optimization of the prepared gummies was done on the basis of their antioxidant profile. The bioactive compounds found in the gummies were characterized by High-Resolution Accurate Mass-Spectrometry. These bioactive compounds were divided into different categories, such as phenolic acids, flavonoids, as well as terpenoids. Analytical characterization was employed to identify both known and unknown bioactive compounds and metabolites in the optimized product. The results showed that the optimized gummies (FG3) exhibited desirable sensory, textural, and functional properties. FG3 contains a substantial amount of dietary fibre and bioactive compounds, including flavonoids, terpenoids, phenolics, triterpenes, which exhibits health benefits such as anti-cancerous, anti-inflammatory etc., Overall, the developed gummies provide a promising solution to address health-related issues.

Innovations in Wheat Bread: Using Food Industry By-Products for Better Quality and Nutrition

The evolution of wheat bread as a dietary staple underscores its essential role in providing energy, protein, fiber, and vital nutrients. To address contemporary health challenges such as type 2 diabetes and cardiovascular diseases, fortifying wheat bread with health-promoting additives becomes imperative to mitigate deficiencies resulting from refined wheat flour consumption. Functional food innovations, aligned with sustainability goals and circular economy principles, offer promising approaches for addressing these concerns. Integrating by-products from fruits and oil crops into bread formulations enhances health benefits by boosting dietary fiber, bioactive compounds, and antioxidant potential. However, gaps persist in understanding anti-nutritional substances and contaminants in final products, necessitating further research for comprehensive safety assessments. The addition of by-product raw materials significantly influences dough rheology and sensory characteristics, potentially achieving quality comparable to traditional wheat bread. Challenges include inconsistencies in bread and by-product specifications across studies, hindering direct result comparison. Overcoming these obstacles is crucial for maximizing the potential of agri-food by-products in creating healthier, sustainable bread options while maintaining safety and quality standards.

The Effects of Polod (Arenga undulatifolia) Powder towards Physicochemical Properties and Sensory Attributes of Chicken Patties

Meat products have high biological value protein and essential nutrients needed for human sustenance, but it is deficient in complex carbohydrates like dietary fibre. Thus, various strategies have been explored to increase the dietary fibre content in meat products because plants are potentially rich sources of dietary fibres and bioactive compounds. Arenga undulatifolia, commonly known as polod, is a member of the family Arecaceace and grows natively in Borneo. This study examined how incorporating polod powder produced from the stem pith of Arenga undulatifolia affects nutritional, physicochemical, and sensory aspects of chicken patties. The polod powder showed comparable functional properties to other plant powders. The chicken patties were formulated as control samples F0 (0% polod powder), F1 (2% polod powder), F2 (4% polod powder), F3 (6% polod powder). Adding 4% polod powder significantly increased (p &gt; 0.05) the patty’s protein, ash, lipid, crude fibre, dietary fibre, and energy contents. Increasing the level of polod powder considerably lowered the moisture content (p &lt; 0.05). The chewiness of the patties decreased significantly (p &lt; 0.05) at 4% and 6% polod powder levels with no significant changes in other textural parameters (p &gt; 0.05). Compared to the control sample (F0), the chicken patties with polod powder showed greater cooking yield and lower cooking loss. Compared to other formulations, F1 was most liked by sensory panellists. In conclusion, polod powder is potentially useful as a functional ingredient in the production of chicken patties.

Valorization of spent coffee ground and coffee silverskin as a source of nutrients and bioactive compounds

AbstractIn a world where a greener approach is increasingly necessary, it is mandatory to reduce waste production and reuse residues from the company's supply chain. Spent Coffee grounds (SCG) and Coffee Silverskin (CS) are two important by‐products of coffee production, being sources of important dietary fibers and bioactive compounds, which is why some authors have proposed their reuse in the nutraceutical, food and cosmetic industries. However, their nutrients chemical content has been insufficiently studied. Therefore, the aim of the present review was to investigate the main components, such as carbohydrates, dietary fibers, lipids, and bioactive compounds of SCG and CS. In addition, the most common extraction methods to obtain these aforementioned nutrients were evaluated.

Banana Peel (Musa ABB cv. Nam Wa Mali-Ong) as a Source of Value-Adding Components and the Functional Properties of Its Bioactive Ingredients.

Banana peel (BP) is the primary by-product generated during banana processing which causes numerous environmental issues. This study examines the physical attributes, proximate analysis, glycoarray profiling, antioxidant abilities, and prebiotic activity of BP. The analysis demonstrated that carbohydrates constituted the primary components of BP and the glycoarray profiling indicated that BP contains multiple pectin and hemicellulose structures. BP also contained phenolic compounds, including (+)-catechin and gallic acid, flavonoid compounds, and antioxidant activities. BP demonstrated prebiotic effects by promoting the proliferation of advantageous gut bacteria while inhibiting the growth of harmful bacteria. The prebiotic index scores demonstrated that BP exhibited a greater capacity to promote the growth of beneficial bacteria in comparison to regular sugar. The study demonstrated the potential of the BP as a valuable source of dietary fibre, bioactive compounds, and prebiotics. These components have beneficial characteristics and can be utilised in the production of food, feed additives, and functional food.

Nutritional supplement and pharmaceutical potential of &lt;i&gt;Ipomea batata&lt;/i&gt; L. leaves: A review

Sweet potatoes are an exceptionally essential crop in several parts of the world, being produced in more than 100 countries and positioned as sixth most major crop in the world. The world production of sweet potato has steadily declined with the exception of America and Sub-saharan Africa in the last decade. The study was intended to provide the latest information on sweet potato leaves and its nutritional and medicinal potential. It was first introduced into Nigeria in late 1694 through the early activities of Portuguese and Spanish explorers. Nigeria is one of the largest producers of sweet potato in sub-Saharan Africa with annual production estimated at 3.46 million tons per year. The sweet potato can, however, be harvested many times during the year considerably more than many other greens vegetables. It is one of the few vegetables that can be cultivated in both rainy and dry seasons. Sweet potato leaves are considered to be rich in protein, fibers, vitamin B, Vitamin C and minerals, such as iron, calcium, magnesium, zinc, dietary bioactive compounds, and contain more phenols than any other commercial vegetables. The pharmaceutical importance includes anti-inflammatory,anti-cancer, antioxidant, anti-diabetes and anti-mutagenic among others. Sweet potato leaves could serve as an additional leafy green vegetable and promote food security forsustainable growth.

Modulation of Tau Pathology in Alzheimer's Disease by Dietary Bioactive Compounds.

Tau is a microtubule-associated protein essential for microtubule assembly and stability in neurons. The abnormal intracellular accumulation of tau aggregates is a major characteristic of brains from patients with Alzheimer's disease (AD) and other tauopathies. In AD, the presence of neurofibrillary tangles (NFTs), which is composed of hyperphosphorylated tau protein, is positively correlated with the severity of the cognitive decline. Evidence suggests that the accumulation and aggregation of tau cause synaptic dysfunction and neuronal degeneration. Thus, the prevention of abnormal tau phosphorylation and elimination of tau aggregates have been proposed as therapeutic strategies for AD. However, currently tau-targeting therapies for AD and other tauopathies are limited. A number of dietary bioactive compounds have been found to modulate the posttranslational modifications of tau, including phosphorylation, small ubiquitin-like modifier (SUMO) mediated modification (SUMOylation) and acetylation, as well as inhibit tau aggregation and/or promote tau degradation. The advantages of using these dietary components over synthetic substances in AD prevention and intervention are their safety and accessibility. This review summarizes the mechanisms leading to tau pathology in AD and highlights the effects of bioactive compounds on the hyperphosphorylation, aggregation and clearance of tau protein. The potential of using these bioactive compounds for AD prevention and intervention is also discussed.

Role of apigenin in targeting metabolic syndrome: A systematic review.

Metabolic syndrome (MetS) is a cluster of metabolic abnormalities that has a high prevalence worldwide. Apigenin is a flavonoid present in several vegetables and fruits and has anti-inflammatory, anti-oxidant, and anti-MetS properties. This study aims to systematically review the effects of apigenin against MetS and the relevant molecular and cellular mechanisms of action, pharmacokinetics features, and potential structure-activity relationship. Electronic databases including Scopus, PubMed, Science Direct and Cochrane Library were searched for in vivo, and in vitro, and human studies with the following keywords: "apigenin" and "metabolic syndrome or insulin resistance syndrome", "fatty liver", "hypertension or blood pressure", "diabetes or blood glucose", "dyslipidemia", "heart or cardiovascular " and "obesity" in title/abstract. Data were collected from 2000 until 2021 (up to April). Only papers published in the English language were included. Forty-six full-text articles out of 1016 retrieved papers were reviewed and underwent quality assessment by investigators. Anti-obesity activity of apigenin is mainly through attenuating adipocyte differentiation by suppressing the mitotic clonal expansion and the adipogenesis-related factors. Its anti-diabetic effects can be exerted through inhibition of protein tyrosine phosphatase1B expression, maintaining the activity of anti-oxidant enzymes, reducing intracellular ROS production, cellular DNA damage, protein carbonylation, and attenuating β-cell apoptosis. Moreover, apigenin could attenuate dyslipidemia and subsequent atherosclerotic conditions through down-regulating sterol regulatory element-binding proteins (SREBP)-1c, SREBP-2, stearyl-CoA desaturase-1, and 3-hydroxy-3-methyl-glutaryl-CoA reductase. Apigenin as a dietary bioactive compound would be a promising candidate for improving MetS and its components.