Phytochemical profile and biological activities of Bromelia antiacantha extracts / Perfil fitoquímico e atividades biológicas de extratos de Bromelia antiacantha

Reports from popular medicine usually act as a basis for the development of new drugs from natural compounds with therapeutic actions for serious diseases and prevalence such as cancer. Bromelia antiacantha Bertol. is a species of the Bromeliaceae family, considered an unconventional food plant, found in the south and midwest regions of Brazil. Despite the high nutritional content and pharmacological potential of its fruits, few scientific studies report its biological actions. Thus, this study evaluates the phytochemical profile of aqueous and ethanol extracts obtained from B. antiacantha fruits, as well as their possible antioxidant, antitumor, and cytotoxic activities. The aqueous extract exhibited phenolic compounds and flavonoids, while ethanol extracts indicated the presence of flavonoids and coumarin in their composition, regardless of the region of collection. The ethanolic extract demonstrated a more promising antioxidant effect than the aqueous extract and also induced a significant inhibition in the viability of human cervical cancer cells of the SiHa strain. In addition, treatment with both extracts did not alter the viability of non-tumor cells of the immortalized human keratinocyte lineage (HaCaT). These results bring new data about extracts obtained from a native plant, edible and traditionally used in popular medicine, opening new perspectives for its possible therapeutic application.

Relatos da medicina popular costumam atuar como referencial para o desenvolvimento de novos fármacos a partir de moléculas naturais com ações terapêuticas para doenças de alta gravidade e prevalência como o câncer. Bromelia antiacantha Bertol. é uma espécie da família Bromeliaceae, considerada uma planta alimentícia não convencional (PANC), encontrada nas regiões sul e centro-oeste do Brasil. Apesar do alto teor nutritivo e potencial farmacológico de seus frutos, poucos estudos científicos relatam suas ações biológicas. Desta forma, este estudo avalia o perfil fitoquímico de extratos aquoso e etanólico obtidos de frutos de B. antiacantha, bem como a sua possível ação antioxidante, antitumoral e citotóxica. O extrato aquoso apresentou compostos fenólicos e flavonoides, enquanto os extratos etanólicos apontam a presença de flavonóides e cumarina em sua composição, independente da região de coleta. O extrato etanólico demonstrou efeito antioxidante mais promissor do que o extrato aquoso e também induziu uma inibição significativa na viabilidade de células humanas de câncer cervical da linhagem SiHa. Além disso, o tratamento com ambos extratos não alterou a viabilidade de células não tumorais da linhagem de queratinócitos humanos imortalizados (HaCaT). Estes dados trazem novas informações sobre extratos obtidos de uma espécie vegetal nativa, comestível e já utilizada tradicionalmente, mas abrindo novas perspectivas quanto a possíveis aplicações terapêuticas.

Inhibitory effects of flavonoids on glucose transporter 1 (GLUT1): From library screening to biological evaluation to structure-activity relationship.

Glucose transporter 1 (GLUT1) is mainly responsible for glucose uptake and energy metabolism, especially in the aerobic glycolysis process of tumor cells, which is closely associated with the advancement of tumors. Numerous studies have demonstrated that the inhibition of GLUT1 can decrease the growth of tumor cells and enhance drug sensitivity, so GLUT1 is considered to be a promising therapeutic target for cancer treatment. Flavonoids are a group of phenolic secondary metabolites present in vegetables, fruits, and herbal products, some of which were reported to increase cancer cells' sensitivity to sorafenib by inhibiting GLUT1. Our objective was to screen potential inhibitors of GLUT1 from 98 flavonoids and assess the sensitizing effect of sorafenib on cancer cells. and illuminate the structure-activity relationships of flavonoids with GLUT1. Eight flavonoids, including apigenin, kaempferol, eupatilin, luteolin, hispidulin, isosinensetin, sinensetin, and nobiletin exhibited significant inhibition (>50%) on GLUT1 in GLUT1-HEK293T cells. Among them, sinensetin and nobiletin showed stronger sensitizing effects and caused a sharp downward shift of the cell viability curves in HepG2 cells, illustrating these two flavonoids might become sensitizers to enhance the efficacy of sorafenib by inhibiting GLUT1. Molecular docking analysis elucidated inhibitory effect of flavonoids on GLUT1 was related to conventional hydrogen bonds, but not Pi interactions. The pharmacophore model clarified the critical pharmacophores of flavonoids inhibitors are hydrophobic groups in 3'positions and hydrogen bond acceptors. Thus, our findings would provide useful information for optimizing flavonoid structure to design novel GLUT1 inhibitors and overcome drug resistance in cancer treatment.

The content and distribution of 18 phenolic compounds in 462 batches of edible flowers from 73 species commercially available in China.

Phenolic compounds are widely distributed in plant flowers. The present study systematically analyzed 18 phenolic compounds, represented by 4 monocaffeoylquinic acids, 4 dicaffeoylquinic acids, 5 flavones and 5 other phenolic acids, in 73 species (462 batches of samples) of edible flowers by a new established and validated HPLC-UV (high-performance liquid chromatography ultraviolet) (327/217 nm) method. Among all the species analyzed, 59 species were demonstrated to contain at least one or more quantifiable phenolic compounds, especially in families of Composite, Rosaceae and Caprifoliaceae. 3-Caffeoylquinic acid was found to be the most ubiquitous phenolic compound (in 193 batches of 73 species with the content between 0.061 and 65.10 mg/g), followed by rutin and isoquercitrin. While sinapic acid, 1-Caffeoylquinic acid and 1,3-dicaffeoylquinic acid (only in 5 batches of 1 specie with the content between 0.069 and 0.12 mg/g) were the least ones both in ubiquity and concentration. Additionally, the distribution and abundances of phenolic compounds were compared between these flowers, which would be valuable for auxiliary authentication or other usages. This research covered almost all edible and medicinal flowers in the Chinese market with 18 phenolic compounds therein quantified, which delivered a bird view of phenolic compounds in a broad perspective of edible flowers.

Tilianin Protects against Nonalcoholic Fatty Liver Disease in Early Obesity Mice.

Non-alcoholic fatty liver disease (NAFLD) has emerged as one of the most frequent types of liver disease in pediatric populations with obesity. Tilianin has multiple biological activities including anti-inflammatory and antioxidant. Here, we aim to explore the functions and possible mechanisms of tilianin on NAFLD in obese children. A high-fat high-carbohydrate (HFHC) diet was used to feed 21-d-old mice. Tilianin was administered at a dose of 10 or 20 mg/kg daily. HFHC-fed mice gained weight, increased liver index. The liver showed hepatocyte ballooning, inflammatory infiltration, and steatosis. Elevated levels of alanine aminotransferase (ALT), aspartate aminotransferase (AST), gamma-glutamyl transpeptidase (GGT), low-density lipoprotein cholesterol (LDL-C) and total cholesterol (TC) and reduced the high-density lipoprotein cholesterol (HDL-C) level were found in HFHC-fed mice. Administration of tilianin significantly reduced these impairments. We further evaluated proteins related to lipid metabolism and observed that LXRα, SREBP-1c, FAS and ACC1 expression were blunted following tilianin administration. In addition, tilianin suppressed reactive oxygen species (ROS) overproduction and lipid peroxide 4-Hydroxynonenal expression, ascribed to its oxidative stress-modulating capacity. Tilianin also reversed the increase in F4/80 expression and proinflammatory cytokine levels. Of note, tilianin administration resulted in decreased protein levels of active caspase-1 and NOD-like receptor protein 3 (NLRP3) in HFHC-fed mice. Our study suggests that tilianin may ameliorate NAFLD in early obese mice by modulating lipids metabolism, oxidative stress, and inflammation, which may in part involve inhibiting NLRP3 inflammasome activation.

Systematic analysis and expression of Gossypium 2ODD superfamily highlight the roles of GhLDOXs responding to alkali and other abiotic stress in cotton.

BACKGROUND: 2-oxoglutarate-dependent dioxygenase (2ODD) is the second largest family of oxidases involved in various oxygenation/hydroxylation reactions in plants. Many members in the family regulate gene transcription, nucleic acid modification/repair and secondary metabolic synthesis. The 2ODD family genes also function in the formation of abundant flavonoids during anthocyanin synthesis, thereby modulating plant development and response to diverse stresses. RESULTS: Totally, 379, 336, 205, and 204 2ODD genes were identified in G. barbadense (Gb), G. hirsutum (Gh), G. arboreum (Ga), and G. raimondii (Gb), respectively. The 336 2ODDs in G. hirsutum were divided into 15 subfamilies according to their putative functions. The structural features and functions of the 2ODD members in the same subfamily were similar and evolutionarily conserved. Tandem duplications and segmental duplications served essential roles in the large-scale expansion of the cotton 2ODD family. Ka/Ks values for most of the gene pairs were less than 1, indicating that 2ODD genes undergo strong purifying selection during evolution. Gh2ODDs might act in cotton responses to different abiotic stresses. GhLDOX3 and GhLDOX7, two members of the GhLDOX subfamily from Gh2ODDs, were significantly down-regulated in transcription under alkaline stress. Moreover, the expression of GhLDOX3 in leaves was significantly higher than that in other tissues. These results will provide valuable information for further understanding the evolution mechanisms and functions of the cotton 2ODD genes in the future. CONCLUSIONS: Genome-wide identification, structure, and evolution and expression analysis of 2ODD genes in Gossypium were carried out. The 2ODDs were highly conserved during evolutionary. Most Gh2ODDs were involved in the regulation of cotton responses to multiple abiotic stresses including salt, drought, hot, cold and alkali.

[Regulation of myocardial ischemia reperfusion injury signal pathway by flavonoid monomer].

Acute myocardial infarction seriously endangers the health of people due to its high morbidity and high mortality. Reperfusion strategy is the preferred treatment strategy for acute myocardial infarction. However, reperfusion may lead to additional heart damage, namely myocardial ischemia reperfusion injury(MIRI). Therefore, how to reduce myocardial ischemia reperfusion injury has become one of the urgent problems to be solved in cardiovascular disease. Traditional Chinese medicine(TCM) has the multi-component, multi-channel, and multi-target advantages in the treatment of MIRI, which offers new ideas in this aspect. TCM containing flavonoids has a variety of biological activities and plays a significant role in the treatment of MIRI, which has great research and development application value. TCM containing flavonoids can regulate multiple signaling pathways of MIRI, such as phosphatidylinositol 3 kinase/kinase B(PI3K/Akt) signaling pathway, Janus kinase/signal transducer and activator of transcriptions(JAK/STAT) signaling pathway, adenosine 5'-monophosphate(AMP)-activated protein kinase(AMPK) signaling pathway, mitogen-activated protein kinase(MAPK) signaling pathway, nuclear factor-erythroid 2-related factor 2/antioxidant response element(Nrf2/ARE) signaling pathway, nuclear factor kappa-B(NF-κB) signaling pathway, silent information regulator 1(Sirt1) signaling pathway, and Notch signaling pathway. It reduces MIRI by inhibiting calcium overload, improving energy metabolism, regulating autophagy, and inhibiting ferroptosis and apoptosis. Therefore, a review has been made based on the regulation of relative signaling pathways against MIRI by TCM containing flavonoids, thus providing theoretical support and potential therapeutic strategies for TCM to alleviate MIRI.

[Content analysis and quality evaluation of main active components and mineral elements of Cynomorium songaricum in different habitats].

To clarify the content characteristics of the main active components and mineral elements of Cynomorium songaricum under different habitat conditions, and further explore the relationship between the quality of C. songaricum and habitats, this study took C. songaricum from 25 different habitats in China as the research object, and measured the contents of 8 main active components and 12 mineral elements separately. Diversity analysis, correlation analysis, principal component analysis and cluster analysis were carried out. The results showed that the genetic diversity of total flavonoids, ursolic acid, ether extract, potassium(K), phosphorus(P) and zinc(Zn) in C. songaricum was high. The coefficient of variation of crude polysaccharide, ether extract, gallic acid, protocatechuic aldehyde, catechin, epicatechin, calcium(Ca), sodium(Na), magnesium(Mg), sulfur(S), iron(Fe), manganese(Mn), selenium(Se) and nickel(Ni) were all over 36%, indicating that the quality of C. songaricum was significantly affected by habitats. There were strong synergistic and weak antagonistic effects among the contents of the 8 active components, and complex antagonistic and synergistic effects among the contents of the 12 mineral elements. Principal component analysis revealed that crude polysaccharide, ursolic acid, catechin, epicatechin and total flavonoids could be used as the characteristic components to evaluate the quality of C. songaricum, and Na, copper(Cu), Mn and Ni were the characteristic elements to evaluate the quality of C. songaricum. In cluster ana-lysis, the second group with the main active components as cluster center had better quality in terms of the content of active substances, and the second group with the mineral elements as cluster center had higher utilization potential in the exploitation of mineral elements. This study could provide a basis for resource evaluation and breeding of excellent varieties of C. songaricum in different habitats, and provide a reference for cultivation and identification of C. songaricum.

Influence of environmental conditions on the production of nutraceuticals in Italian edible plant landraces.

Autochthonous plant varieties, also referred to as landraces, represent an important genetic resource, being well-adapted to the environment in which they have been selected. Landraces usually show profiles rich in nutraceuticals, making them an effective and valuable alternative to commercial agri-products, as well as potential candidates for crop improvement programs. Basilicata region is recognized as an Italian hotspot for agrobiodiversity, due to its complex orography. Thus, this work aimed to characterize and monitor, for two successive years, the content of secondary metabolites and related antioxidant properties of seven different species, four officinal (i.e., wild fennel - Feoniculum vulgare Mill.; oregano - Origanum vulgare L.; thyme - Thymus vulgaris L.; valerian - Valeriana officinalis L.) and three fruit species (i.e., fig - Ficus carica L. cv. Dottato; sweet cherry Prunus avium L. cv. Majatica; plum - Prunus domestica L. cv. Cascavella Gialla), collected in three different sites of this region. In detail, spectrophotometric tests were performed to assess the concentration of phenolic compounds, flavonoids, and - for officinal plants - also terpenoids, together with the antiradical activity (FRAP assays). In addition, to better typify the phytocomplexes of these landraces, HPLC-DAD and GC-MS analyses were carried out. In general, officinal plants showed higher values of nutraceutical compounds and related bioactivity with respect to fruit species. The data showed how different accessions of the same species had different phytochemical profiles, according to the sampling area and the year of collection, suggesting a role for both genetic and environmental factors in determining the observed results. Therefore, the final goal of this research was also to find a possible correlation between environmental factors and nutraceutics. The greatest correlation was found in valerian, where a lower water intake seemed to lead to a higher accumulation of antioxidants, and in plum, where the flavonoid content correlated positively with high temperatures. All these outcomes contribute at valorising Basilicata landraces for their aptitude to be high-quality foods and, at the same time, promoting the preservation of the agrobiodiversity for this region.

[Rapid flavonoid-focused sub-chemome characterization of Draconis Sanguis using UPLC-Q-TOF-MS in combination with molecular weight imprinting and mass defect filtering].

Draconis Sanguis is a precious Chinese medicinal material for activating blood and resolving stasis, and its effective components are flavonoids. However, the structural diversity of flavonoids in Draconis Sanguis brings great challenges to the in-depth chara-cterization of its chemical composition profiles. To clarify the substance basis of Draconis Sanguis, ultra-high performance liquid chromatography coupled with quadrupole time-of-flight mass spectrometry(UPLC-Q-TOF-MS) was used in this study to acquire MS data of Draconis Sanguis. The molecular weight imprinting(MWI) and mass defect filtering(MDF) were developed for rapid screening of flavonoids in Draconis Sanguis. Full-scan MS and MS~2 were recorded within the mass range m/z 100-1 000 in positive ion mode. Accor-ding to previous literature, MWI was employed to hunt for reported flavonoids in Draconis Sanguis, and the mass tolerance range of [M+H]~+ was set as ±10×10~(-3). A five-point MDF screening frame was further constructed to narrow the screening range of flavonoids from Draconis Sanguis. Combined with diagnostic fragment ions(DFI) and neutral loss(NL) as well as mass fragmentation pathways, 70 compounds were preliminarily identified from the extract of Draconis Sanguis, including 5 flavan oxidized congeners, 12 flavans, 1 dihydrochalcones, 49 flavonoids dimers, 1 flavonoids trimer and 2 flavonoid derivatives. This study clarified the chemical composition of flavonoids in Draconis Sanguis. Moreover, it also showed that high-resolution MS combined with data post-processing methods such as MWI and MDF could achieve rapid characterization of the chemical composition in Chinese medicinal materials.

Synergistic Effects of Baicalin and Levofloxacin Against Hypervirulent Klebsiella pneumoniae Biofilm In Vitro.

Hypervirulent Klebsiella pneumoniae (hvKp) strains that form biofilms have recently emerged worldwide; however, the mechanisms underlying biofilm formation and disruption remain elusive. In this study, we established a hvKp biofilm model, investigated its in vitro formation pattern, and determined the mechanism of biofilm destruction by baicalin (BA) and levofloxacin (LEV). Our results revealed that hvKp exhibited a strong biofilm-forming ability, forming early and mature biofilms after 3 and 5 d, respectively. Early biofilm and bacterial burden were significantly reduced by BA + LEV and EM + LEV treatments, which destroyed the 3D structure of early biofilms. Conversely, these treatments were less effective against mature biofilm. The expression of both AcrA and wbbM was significantly downregulated in the BA + LEV group. These findings indicated that BA + LEV might inhibit the formation of hvKp biofilm by altering the expression of genes regulating efflux pumps and lipopolysaccharide biosynthesis.

The Study of the Heterogeneity of the Qualities of Argan Oils and Pomaces from Different Cooperatives in the Essaouira Region (Morocco).

In this study, a comparison of the intra-regional variation in the quality of Argan oil and pomace collected from 12 cooperatives in the Essaouira region (Morocco) during the COVID-19 period was carried out. All studied Argan pomaces together with the extraction solvents showed a significant difference (p ≤ 0.05) in the total phenolic compounds, flavonoids, and tannins contents. The proteins, residual oils, total sugars, and total reducing sugars contents in the collected pomaces vary considerably among cooperatives of origin, with maximum averages of 50.45%; 30.05%; 3.82 milligrams of glucose equivalent per gram of dry matter; and 0.53 milligrams of glucose equivalent per gram of dry matter, respectively. Therefore, it is a very valuable ingredient for livestock feed and some cosmetic products that may contain it. The remaining Argan oil content in the pomace varied significantly among cooperatives, ranging from 8.74 to 30.05%. Pomace from traditional extraction recorded the highest content (30.05%), showing that the artisanal and modern extraction processes are not standardized. The measurements of acidity, peroxide value, specific extinction coefficient at 232 nm and 270 nm, and conjugated dienes were carried out in accordance with Moroccan Standard 08.5.090 in order to qualitatively classify all investigated Argan oils. Accordingly, the analyzed oils were categorized as "extra virgin Argan oil," "fine virgin Argan oil," "ordinary virgin Argan oil," and "lampante virgin Argan oil." Therefore, several factors can explain these variations in quality grades, both endogenous and exogenous. Overall, the variation observed in the obtained result allows us to deduce the most significant variables impacting the quality of Argan products and by-products.

Quercetin 3-O rutinoside prevents gastrointestinal injury through regulation of apoptosis in 7.5 Gy total body irradiated mice.

BACKGROUND: Despite the heightened threat to unforeseen nuclear/radiological exposures worldwide, no countermeasures are currently approved to prevent gastrointestinal (GI) toxicity induced by radiation in humans. PURPOSE: In this study, we aim to establish the gastroprotective role of flavonoid, Quercetin-3-O-rutinoside (Q-3-R) against 7.5 Gy total body gamma radiation dose that contributes to the hematopoietic syndrome. METHODS: Q-3-R (10 mg/kg body weight) was administered intramuscularly to C57BL/6 male mice before exposure to 7.5 Gy and monitored for morbidity and mortality. The GI protection against radiation was ascertained by histopathological and xylose absorption studies. Intestinal apoptosis, crypt proliferation and apoptotic signaling were also investigated in different treatment groups. RESULTS: We found that Q-3-R prevented the radiation-induced loss of mitochondrial membrane potential, maintained ATP levels, regulated the apoptotic pathway, and activated crypt cell proliferation in the intestine. Radiation-induced villi and crypt damage as well as mal-absorption were significantly minimized in the Q-3-R treated group. We observed 100% survival post Q-3-R administration against 33.3% lethality in 7.5 Gy (LD33.3/30) exposed C57BL/6 mice. The Q-3-R pre-treated mice that survived the 7.5 Gy dose revealed no pathological changes related to the development of fibrosis in the intestine and thickened mucosal wall till 4 months post irradiation. Complete hematopoietic recovery was observed in these surviving mice when compared to age matched control. CONCLUSION: The findings revealed that Q-3-R regulated the apoptotic process to achieve GI protection against LD33.3/30 dose (7.5 Gy) that primarily caused death due to hematopoietic failure. The recovery observed in mice survivors suggested that this molecule may also have the potential to minimize side effects on normal tissues during radiotherapy.

The Degree of Hydroxylation of Phenolic Rings Determines the Ability of Flavonoids and Stilbenes to Inhibit Calcium-Mediated Membrane Fusion.

This paper discusses the possibility of using plant polyphenols as viral fusion inhibitors with a lipid-mediated mechanism of action. The studied agents are promising candidates for the role of antiviral compounds due to their high lipophilicity, low toxicity, bioavailability, and relative cheapness. Fluorimetry of calcein release at the calcium-mediated fusion of liposomes, composed of a ternary mixture of dioleoyl phosphatidylcholine, dioleoyl phosphatidylglycerol, and cholesterol, in the presence of 4'-hydroxychalcone, cardamonin, isoliquiritigenin, phloretin, resveratrol, piceatannol, daidzein, biochanin A, genistein, genistin, liquiritigenin, naringenin, catechin, taxifolin, and honokiol, was performed. It was found that piceatannol significantly inhibited the calcium-induced fusion of negatively charged vesicles, while taxifolin and catechin showed medium and low antifusogenic activity, respectively. As a rule, polyphenols containing at least two OH-groups in both phenolic rings were able to inhibit the calcium-mediated fusion of liposomes. In addition, there was a correlation between the ability of the tested compounds to inhibit vesicle fusions and to perturb lipid packing. We suggest that the antifusogenic action of polyphenols was determined by the depth of immersion and the orientation of the molecules in the membrane.

Prospective Associations between Cumulative Average Intake of Flavonoids and Hypertension Risk in the CArdioVascular Disease Association Study (CAVAS).

In this study, we aimed to investigate the prospective associations and their shapes between the dietary intake of total flavonoids and their seven subclasses and hypertension risk in a prospective cohort, the KoGES_CArdioVascular disease Association Study (CAVAS), and to consider obesity status as an additional factor. A total of 10,325 adults aged 40 years and older were enrolled at baseline, and 2159 patients were newly diagnosed with hypertension during a median follow-up of 4.95 years. Cumulative dietary intake was estimated using a repeated food frequency questionnaire. Incidence rate ratios (IRRs) with 95% confidence intervals (CIs) were estimated using modified Poisson models with a robust error estimator. We observed nonlinear inverse associations between total and seven subclasses of flavonoids and hypertension risk, although there was no significant association between total flavonoids and flavones with hypertension risk in the highest quartile. For men, these inverse associations tended to be pronounced in the high BMI group, particularly for anthocyanins and proanthocyanidins [IRR (95% CI) in overweight/obese men: 0.53 (0.42-0.67) for anthocyanins; 0.55 (0.42-0.71) for proanthocyanidins]. Our results suggested that consumption of dietary flavonoids may not be dose-responsive but is inversely associated with hypertension risk, particularly among overweight/obese men.

Rutin, a Flavonoid Compound Derived from Garlic, as a Potential Immunomodulatory and Anti-Inflammatory Agent against Murine Schistosomiasis mansoni.

Schistosomiasis is a tropical disease caused by trematode worms. The inflammatory response of the host to schistosome eggs leads to formation of granuloma in the liver and intestine. Praziquantel (PZQ) is still an effective treatment for schistosomiasis, however resistance development may reduce its efficacy. The current study investigated the possible immunomodulatory and anti-inflammatory action of rutin, a natural flavonoid compound isolated from garlic, on liver fibrotic markers in mice infected with S. mansoni in comparison to PZQ. Male albino CD1 mice were infected with 100 ± 2 S. mansoni cercariae/mouse and treated with garlic, rutin, or PZQ. At the end of the experiment, the liver and intestines were harvested for parasitological and histological assessment and to analyze the proinflammatory cytokine. Rutin significantly affects the pathological alterations caused by Schistosoma in the liver. This may be partially explained by a decrease in the number of eggs trapped in the tissues of the liver and a modification in the serum levels of certain cytokines, which are implicated in the formation of Schistosoma granuloma. In conclusion, rutin has strong anti-schistosome properties in vivo, raising the possibility that rutin might be further investigated as a therapy for S. mansoni.

Considerations for Optimizing Warfighter Psychological Health with a Research-Based Flavonoid Approach: A Review.

Optimal nutrition is imperative for psychological health. Oxidative stress and inflammation are underlying etiologies for alterations in psychological health. Warfighters are at risk of health concerns such as depression due to increased stress in austere environments and family separation while deployed. Over the last decade, research has demonstrated the health benefits of flavonoids found in fruits and berries. Berry flavonoids have potent antioxidant and anti-inflammatory properties by inhibiting oxidative stress and inflammation. In this review, the promising effects of various berries rich in bioactive flavonoids are examined. By inhibiting oxidative stress, berry flavonoids have the potential to modulate brain, cardiovascular, and intestinal health. There is a critical need for targeted interventions to address psychological health concerns within the warfighter population, and a berry flavonoid-rich diet and/or berry flavonoid dietary supplement intervention may prove beneficial as an adjunctive therapy. Structured searches of the literature were performed in the PubMed, CINAHL, and EMBASE databases using predetermined keywords. This review focuses on berry flavonoids' critical and fundamental bioactive properties and their potential effects on psychological health in investigations utilizing cell, animal, and human model systems.

Sustainable Production of Ajuga Bioactive Metabolites Using Cell Culture Technologies: A Review.

The genus Ajuga (Lamiaceae) is rich in medicinally important species with biological activities ranging from anti-inflammatory, antitumor, neuroprotective, and antidiabetic to antibacterial, antiviral, cytotoxic, and insecticidal effects. Every species contains a unique and complex mixture of bioactive metabolites-phytoecdysteroids (PEs), iridoid glycosides, withanolides, neo-clerodane terpenoids, flavonoids, phenolics, and other chemicals with high therapeutic potential. Phytoecdysteroids, the main compounds of interest, are natural anabolic and adaptogenic agents that are widely used as components of dietary supplements. Wild plants remain the main source of Ajuga bioactive metabolites, particularly PEs, which leads to frequent overexploitation of their natural resources. Cell culture biotechnologies offer a sustainable approach to the production of vegetative biomass and individual phytochemicals specific for Ajuga genus. Cell cultures developed from eight Ajuga taxa were capable of producing PEs, a variety of phenolics and flavonoids, anthocyanins, volatile compounds, phenyletanoid glycosides, iridoids, and fatty acids, and demonstrated antioxidant, antimicrobial, and anti-inflammatory activities. The most abundant PEs in the cell cultures was 20-hydroxyecdysone, followed by turkesterone and cyasterone. The PE content in the cell cultures was comparable or higher than in wild or greenhouse plants, in vitro-grown shoots, and root cultures. Elicitation with methyl jasmonate (50-125 µM) or mevalonate and induced mutagenesis were the most effective strategies that stimulated cell culture biosynthetic capacity. This review summarizes the current progress in cell culture application for the production of pharmacologically important Ajuga metabolites, discusses various approaches to improve the compound yield, and highlights the potential directions for future interventions.

Effect of Walnut Supplementation on Dietary Polyphenol Intake and Urinary Polyphenol Excretion in the Walnuts and Healthy Aging Study.

Among all tree nuts, walnuts contain the highest total polyphenols by weight. This secondary data analysis examined the effect of daily walnut supplementation on the total dietary polyphenols and subclasses and the urinary excretion of total polyphenols in a free-living elderly population. In this 2-year prospective, randomized intervention trial (ID NCT01634841), the dietary polyphenol intake of participants who added walnuts daily to their diets at 15% of daily energy were compared to those in the control group that consumed a walnut-free diet. Dietary polyphenols and subclasses were estimated from 24 h dietary recalls. Phenolic estimates were derived from Phenol-Explorer database version 3.6. Participants in the walnut group compared to the control group had a higher intake of total polyphenols, flavonoids, flavanols, and phenolic acids in mg/d (IQR): 2480 (1955, 3145) vs. 1897 (1369, 2496); 56 (42,84) vs. 29 (15, 54); 174 (90, 298) vs. 140 (61, 277); and 368 (246, 569) vs. 242 (89, 398), respectively. There was a significant inverse association between dietary flavonoid intake and urine polyphenol excretion; less urinary excretion may imply that some of the polyphenols were eliminated via the gut. Nuts had a significant contribution to the total polyphenols in the diet, suggesting that a single food like walnuts added to habitual diet can increase the polyphenol intake in a Western population.

Citrus × paradisi L. Fruit Waste: The Impact of Eco-Friendly Extraction Techniques on the Phytochemical and Antioxidant Potential.

Citrus fruits have been the subject of extensive research over the years due to their impressive antioxidant properties, the health benefits of flavanones, and their potential use in the prevention and treatment of chronic diseases. Grapefruit have been shown in studies to improve overall health, with numerous potential benefits, including improved heart health, reduced risk of certain cancers, improved digestive health, and improved immune system function. The development of cyclodextrin complexes is an exciting approach to increasing the content of flavanones such as naringin and naringenin in the extraction medium while improving the profile of beneficial phenolic compounds and the antioxidant profile. This research aims to optimize the extraction conditions of the flavanones naringin and naringenin with additional compounds to increase their yield from different parts of grapefruit (Citrus × paradisi L.) fruits, such as albedo and segmental membranes. In addition, the total content of phenolic compounds, flavonoids, and the antioxidant activity of ethanolic extracts produced conventionally and with -cyclodextrin was examined and compared. In addition, antioxidant activity was measured using the radical scavenging activity assay (ABTS), radical scavenging activity assay (DPPH), and ferric reducing antioxidant power (FRAP) methods. The yield of naringin increased from 10.53 ± 0.52 mg/g to 45.56 ± 5.06 mg/g to 51.11 ± 7.63 mg/g of the segmental membrane when cyclodextrins (α, ß-CD) were used; naringenin increased from 65.85 ± 10.96 µg/g to 91.19 ± 15.19 µg/g of the segmental membrane when cyclodextrins (α, ß-CD) were used. Furthermore, the results showed that cyclodextrin-assisted extraction had a significant impact in significantly increasing the yield of flavanones from grapefruit. In addition, the process was more efficient and less expensive, resulting in higher yields of flavanones with a lower concentration of ethanol and effort. This shows that cyclodextrin-assisted extraction is an excellent method for extracting valuable compounds from grapefruit.

Comparative analysis of the reactivity of anthocyanidins, leucoanthocyanidins, and flavonols using a quantum chemistry approach.

Anthocyanidins, leucoanthocyanidins, and flavonols are natural compounds mainly known due to their reported biological activities, such as antiviral, antifungal, anti-inflammatory activities, and antioxidant activity. In the present study, we performed a comparative structural, conformational, electronic, and nuclear magnetic resonance analysis of the reactivity of the chemical structure of primary anthocyanidins, leucoanthocyanidins, and flavonoids. We focused our analysis on the following molecular questions: (i) differences in cyanidin catechols ( +)-catechin, leucocyanidin, and quercetin; (ii) the loss of hydroxyl presents in the R1 radical of leucoanthocyanidin in the functional groups linked to C4 (ring C); and (iii) the electron affinity of the 3-hydroxyl group (R7) in the flavonoids delphinidin, pelargonidin, cyanidin, quercetin, and kaempferol. We show unprecedented results for bond critical point (BCP) of leucopelargonidin and leucodelphirinidin. The BCP formed between hydroxyl hydrogen (R2) and ketone oxygen (R1) of kaempferol has the same degrees of covalence of quercetin. Kaempferol and quercetin exhibited localized electron densities between hydroxyl hydrogen (R2) and ketone oxygen (R1). Global molecular descriptors showed quercetin and leucocyanidin are the most reactive flavonoids in electrophilic reactions. Complementary, anthocyanidins are the most reactive in nucleophilic reactions, while the smallest gap occurs in delphinidin. Local descriptors indicate that anthocyanidins and flavonols are more prone to electrophilic attacks, while in leucoanthocyanidins, the most susceptible to attack are localized in the ring A. The ring C of anthocyanidins is more aromatic than the same found in flavonols and leucoanthocyanidins. METHODS: For the analysis of the molecular properties, we used the DFT to evaluate the formation of the covalent bonds and intermolecular forces. CAM-B3LYP functional with the def2TZV basis set was used for the geometry optimization. A broad analysis of quantum properties was performed using the assessment of the molecular electrostatic potential surface, electron localization function, Fukui functions, descriptors constructed from frontier orbitals, and nucleus independent chemical shift.