Search

Increasing prospective phytochemical investigations and biological activities on Pueraria lobata and Trifolium pratense flowers exhibited their nutritional (food industry) pharmaceutical (anticancer, anti-inflammatory, anti-microbial, etc.) potentials. Previous studies paid great attention to the screening of isoflavones profile from phytochemicals. This study, in contrast, aimed at identifying the flavonoids from Pueraria lobata flowers or kudzu flower (KF) and Trifolium pratense flowers or red clover (RC) flowers and determining their cytotoxic activities on normal; (HEK-293) and cancer cell lines; human glioblastoma (A-172), osteosarcoma (HOS), embryonic rhabdomyosarcoma (Rd), lung carcinoma (A-549) and liver carcinoma (HepG2). The phytochemical screening using a high-performance liquid chromatography-diode array detector coupled with quadrupole time-of-flight mass spectrometry (HPLC-DAD-Q-TOF/MS) showed that 15 flavonoids, including isoflavones, flavones, flavonols, and flavanones, were identified in KF and 8 flavonoids, including isoflavones and flavonols, were found in RC. Nevertheless, the majority of flavonoid chemical constituents in KF or RC were found to be isoflavones (66.6%) and (62.5%), respectively. HPLC-DAD analysis following eco-friendly extraction of phytochemicals showed that KF contains mainly daidzein and genistein, while RC contains primarily formononetin and biochanin A. Cytotoxic activities evaluated according to IC50 values exhibited the most pronounced dose-dependent antiproliferative effect of KF and RC extracts were against HOS and Rd cancer cell lines, respectively. Accordingly, the morphological observation carried out using acridine orange/ethidium bromide and Giemsa stains revealed apoptotic activities and cell death in HOS and Rd cell lines when subjected to KF or RC extracts. Cytotoxic activities and apoptotic changes were pronounced among all cancer cell lines except for the control cells (HEK-293). Additionally, various polyphenols and flavonoids were identified and quantified in KF and RC extracts and exhibited potent radical scavenging activities. Overall, this study suggests that KF and RC could be valuable edible sources of flavonoids. The comprehensive flavonoid profiles for KF and RC may explain their remarkable biological activities and contribution to inducing antioxidant and cytotoxic activities against cancer cell lines.

Bioactive compounds like piperine (alkaloids) offer a variety of health benefits due to their biological and pharmacological potential. Piperine has been revealed to have anti-inflammatory, anti-aging, anti-diabetes, anti-bacterial, anti-ulcer, and anti-carcinogenic characteristics. Recent research has been conducted to extract piperine using effective and environmentally friendly techniques. In this study, we sought to assess the potential and efficacy of natural deep eutectic solvents to extract piperine from black pepper seeds using an ultrasound-assisted extraction technique. A Box–Behnken design combined with response surface methodology was used to evaluate the optimum extraction conditions of piperine. Extraction efficiency was evaluated based on the extraction yields of piperine, antioxidant activity, total polyphenols, and total flavonoids. The results showed that the choline chloride-citric acid-1,2-propylene glycol combination (1:2:2 molar ratio) with 25% (v/v) of water was the most effective at extracting piperine from black pepper. It was found that the extraction yield of piperine was significantly influenced by the liquid–solid ratio and extraction time. The optimal extraction conditions were determined and it was found that antioxidant activities and total polyphenol content in the piperine-rich extracts were remarkably related to the piperine content. The piperine extract purity was found to be 90%. Our results indicate that black pepper could be used as a functional food application.

Type 2 diabetes is characterized by hyperglycemia and a relative loss of β–cell function. Our research investigated the antidiabetic potential of betulin, a pentacyclic triterpenoid found primarily in birch bark and, intriguingly, in a few marine organisms. Betulin has been shown to possess diverse biological activities, including antioxidant and antidiabetic activities; however, no studies have fully explored the effects of betulin on the pancreas and pancreatic islets. In this study, we investigated the effect of betulin on streptozotocin–nicotinamide (STZ)-induced diabetes in female Wistar rats. Betulin was prepared as an emulsion, and intragastric treatments were administered at doses of 20 and 50 mg/kg for 28 days. The effect of treatment was assessed by analyzing glucose parameters such as fasting blood glucose, hemoglobin A1C, and glucose tolerance; hepatic and renal biomarkers; lipid peroxidation; antioxidant enzymes; immunohistochemical analysis; and hematological indices. Administration of betulin improved the glycemic response and decreased α–amylase activity in diabetic rats, although insulin levels and homeostatic model assessment for insulin resistance (HOMA–IR) scores remained unchanged. Furthermore, betulin lowered the levels of hepatic biomarkers (aspartate aminotransferase, alanine aminotransferase, and alpha-amylase activities) and renal biomarkers (urea and creatine), in addition to improving glutathione levels and preventing the elevation of lipid peroxidation in diabetic animals. We also found that betulin promoted the regeneration of β–cells in a dose-dependent manner but did not have toxic effects on the pancreas. In conclusion, betulin at a dose of 50 mg/kg exerts a pronounced protective effect against cytolysis, diabetic nephropathy, and damage to the acinar pancreas and may be a potential treatment option for diabetes.

Circadian rhythm disruption is increasingly considered an environmental risk factor for the development and exacerbation of inflammatory bowel disease. We have reported in a previous study that nychthemeral dysregulation is associated with an increase in intestinal barrier permeability and inflammation in mice with dextran sulfate sodium (DSS)-induced colitis. To investigate the effect of circadian rhythm disruption on the composition and diversity of the gut microbiota (GM), sixty male C57BL/6J mice were initially divided to two groups, with the shifted group (n = 30) exposed to circadian shifts for three months and the non-shifted group (n = 30) kept under a normal light–dark cycle. The mice of the shifted group were cyclically housed for five days under the normal 12:12 h light–dark cycle, followed by another five days under a reversed light–dark cycle. At the end of the three months, a colitis was induced by 2% DSS given in the drinking water of 30 mice. Animals were then divided into four groups (n = 15 per group): sham group non-shifted (Sham-NS), sham group shifted (Sham-S), DSS non-shifted (DSS-NS) and DSS shifted (DSS-S). Fecal samples were collected from rectal content to investigate changes in GM composition via DNA extraction, followed by high-throughput sequencing of the bacterial 16S rRNA gene. The mouse GM was dominated by three phyla: Firmicutes, Bacteroidetes and Actinobacteria. The Firmicutes/Bacteroidetes ratio decreased in mice with induced colitis. The richness and diversity of the GM were reduced in the colitis group, especially in the group with inverted circadian rhythm. Moreover, the GM composition was modified in the inverted circadian rhythm group, with an increase in Alloprevotella, Turicibacter, Bacteroides and Streptococcus genera. Circadian rhythm inversion exacerbates GM dysbiosis to a less rich and diversified extent in a DSS-induced colitis model. These findings show possible interplay between circadian rhythm disruption, GM dynamics and colitis pathogenesis.

Currently, the efficacy of drug therapy for post-traumatic stress disorder or PTSD leaves much to be desired, making nutraceutical support a promising avenue for treatment. Recent research has identified the protective effects of resveratrol in PTSD. Here, we tested the behavioral and neurobiological effects of combining cheese consumption with resveratrol supplements in an experimental PTSD model. Using the elevated plus maze test, we observed that cheese intake resulted in a shift from anxiety-like behavior to depressive behavior, evident in increased freezing acts. However, no significant changes in the anxiety index value were observed. Interestingly, supplementation with cheese and resveratrol only led to the elimination of freezing behavior in half of the PTSD rats. We further segregated the rats into two groups based on freezing behavior: Freezing+ and Freezing0 phenotypes. Resveratrol ameliorated the abnormalities in Monoamine Oxidize -A and Brain-Derived Neurotrophic Factor gene expression in the hippocampus, but only in the Freezing0 rats. Moreover, a negative correlation was found between the number of freezing acts and the levels of Monoamine Oxidize-A and Brain-Derived Neurotrophic Factor mRNAs in the hippocampus. The study results show promise for resveratrol supplementation in PTSD treatment. Further research is warranted to better understand the underlying mechanisms and optimize the potential benefits of resveratrol supplementation for PTSD.

Betulin is a natural triterpene, usually from birch bark, known for its potential wound-healing properties. Despite having a wide range of pharmacological targets, no studies have proposed betulin as a multitarget compound. Betulin has protective effects against cardiovascular and liver diseases, cancer, diabetes, oxidative stress, and inflammation. It reduces postprandial hyperglycemia by inhibiting α-amylase and α-glucosidase activity, combats tumor cells by inducing apoptosis and inhibiting metastatic proteins, and modulates chronic inflammation by blocking the expression of proinflammatory cytokines via modulation of the NFκB and MAPKs pathways. Given its potential to influence diverse biological networks with high target specificity, it can be hypothesized that betulin may eventually become a new lead for drug development because it can modify a variety of pharmacological targets. The summarized research revealed that the diverse beneficial effects of betulin in various diseases can be attributed, at least in part, to its multitarget anti-inflammatory activity. This review focuses on the natural sources, pharmacokinetics, pharmacological activity of betulin, and the multi-target effects of betulin on signaling pathways such as MAPK, NF-κB, and Nrf2, which are important regulators of the response to oxidative stress and inflammation in the body.

Glucocorticoids are metabolized by the CYP3A isoform of cytochrome P450 and by 11-β-hydroxysteroid dehydrogenase type 1 (11β-HSD-1). Experimental data suggest that post-traumatic stress disorder (PTSD) is associated with an increase in hepatic 11β-HSD-1 activity and a concomitant decrease in hepatic CYP3A activity. Trans-resveratrol, a natural polyphenol, has been extensively studied for its antipsychiatric properties. Recently, protective effects of trans-resveratrol were found in relation to PTSD. Treatment of PTSD rats with trans-resveratrol allowed the rats to be divided into two phenotypes. The first phenotype is treatment-sensitive rats (TSR), and the second phenotype is treatment-resistant rats (TRRs). In TSR rats, trans-resveratrol ameliorated anxiety-like behavior and reversed plasma corticosterone concentration abnormalities. In contrast, in TRR rats, trans-resveratrol aggravated anxiety-like behavior and decreased plasma corticosterone concentration. In TSR rats, hepatic 11β-HSD-1 activity was suppressed, with a concomitant increase in CYP3A activity. In TRR rats, the activities of both enzymes were suppressed. Thus, the resistance of PTSD rats to trans-resveratrol treatment is associated with abnormalities in hepatic metabolism of glucocorticoids. The free energy of binding of resveratrol, cortisol, and corticosterone to the human CYP3A protein was determined using the molecular mechanics Poisson–Boltzmann surface area approach, indicating that resveratrol could affect CYP3A activity.

Phlorotannins are secondary metabolites produced mainly by brown seaweeds (Phaeophyceae) and belong to the class of polyphenolic compounds with diverse bioactivities. The key factors in the extraction of polyphenols are the selection of a suitable solvent, method of extraction and selection of optimal conditions. Ultrasonic-assisted extraction (UAE) is one of the advanced energy-saving methods suitable for the extraction of labile compounds. Methanol, acetone, ethanol and ethyl acetate are the most commonly used solvents for polyphenol extraction. As alternatives to toxic organic solvents, a new class of green solvents, natural deep eutectic solvents (NADES), has been proposed for the efficient extraction of a wide range of natural compounds including polyphenols. Several NADES were screened previously for the extraction of phlorotannins; however, the extraction conditions were not optimized and chemical profiling of NADES extract was not performed. The purpose of this work was to study the effect of selected extraction parameters on the phlorotannin content in NADES extract from Fucus vesiculosus, optimization of extraction conditions and chemical profiling of phlorotannins in the NADES extract. A fast and green NADES-UAE procedure was developed for the extraction of phlorotannins. Optimization was performed through an experimental design and showed that NADES (lactic acid:choline chloride; 3:1) provides a high yield (137.3 mg phloroglucinol equivalents per g dry weight of algae) of phlorotannins under the following extraction conditions: extraction time 23 min, 30.0% water concentration and 1:12 sample to solvent ratio. The antioxidant activity of the optimized NADES extract was equal to that of EtOH extract. In total, 32 phlorotannins have been identified (one trimer, two tetramers, six pentamers, four hexamers, six heptamers, six octamers and seven nonamers) in NADES extracts from arctic F. vesiculosus using the HPLC-HRMS and MS/MS technique. It was noted that all the above-mentioned phlorotannins were identified in both EtOH and NADES extracts. Our results suggest that NADES could be considered as an alternative to the conventional techniques for the effective extraction of phlorotannins from F. vesiculosus with high antioxidant potential.

The microalgae Chlorella vulgaris is a cheap source of nutrients and bioactive compounds, and thus is used in many interventional studies. This study evaluated the potential effects of C. vulgaris powder on fermentation parameters; sensory, phytochemical, and antioxidant activity; and the abundance of volatile organic compounds (VOCs) of treated versus control beers. A German Pilsner-style lager beer (GPB) was brewed and supplemented with C. vulgaris at various levels (3.3, 5, and 10 g/L) after primary fermentation. The apparent °Brix and pH was used to monitor the progress of fermentation. The 2,2-diphenyl-1-picrylhydrazyl (DPPH) and hydrogen peroxide (H2O2) was used to measure the antioxidant activity of beers. Addition of C. vulgaris increased the concentration of total polyphenols, total flavonoids, and antioxidant activity of treated beers (CGB) compared to the control (GPB). Treatment had no effects (p > 0.05) on higher alcohols such as 3-methyl-1-butanol, 2-hexanol, and phenylethyl alcohol. An increase in the concentration of C. vulgaris had no significant effects on sensory perception of enriched beers. The results showed that C. vulgaris could be used as a potential ingredient for designing functional beer with improved health benefits.

Pediatric solid tumors (PSTs) are life-threatening and can lead to high morbidity and mortality rates in children. Developing novel remedies to treat these tumors, such as glioblastoma multiforme and sarcomas, such as osteosarcoma, and rhabdomyosarcoma, is challenging, despite immense attempts with chemotherapeutic or radiotherapeutic interventions. Soy (Glycine max) and kudzu roots (KR) (Pueraria spp.) are well-known phytoestrogenic botanical sources that contain high amounts of naturally occurring isoflavones. In the present study, we investigated the antioxidant and cytotoxic effects of the extracts of KR and soy molasses (SM) against PSTs. The green extraction of isoflavones from KR and SM was performed using natural deep eutectic solvents. The extracts were subsequently analyzed by high-performance liquid chromatography (HPLC)-diode array detector (DAD) coupled with high-resolution (HR) mass spectrometry (MS), which identified 10 isoflavones in KR extracts and 3 isoflavones in the SM extracts. Antioxidant and cytotoxic activities of KR and SM extracts were assessed against glioblastoma multiforme (A-172), osteosarcoma (HOS), and rhabdomyosarcoma (Rd) cancer cell lines. The KR and SM extracts showed satisfactory cytotoxic effects (IC50) against the cancer cell lines tested, particularly against Rd cancer cell lines, in a dose-dependent manner. Antioxidant activity was found to be significantly (p ≤ 0.05) higher in KR than in SM, which was consistent with the results of the cytotoxic activity observed with KR and SM extracts against glioblastoma and osteosarcoma cells. The total flavonoid content and antioxidant activities of the extracts were remarkably attributed to the isoflavone content in the KR and SM extracts. This study provides experimental evidence that HPLC-ESI-HRMS is a suitable analytical approach to identify isoflavones that exhibit potent antioxidant and anticancer potential against tumor cells, and that KR and SM, containing many isoflavones, can be a potential alternative for health care in the food and pharmaceutical industries.

The modification of chitosan represents a challenging task in obtaining biopolymeric materials with enhanced removal capacity for heavy metals. In the present work, the adsorption characteristics of chitosan modified with carboxyl groups (CTS-CAA) towards copper (II) and zinc (II) ions have been tested. The efficacy of the synthesis of CTS-CAA has been evaluated by studying various properties of the modified chitosan. Specifically, the functionalized chitosan has been characterized by using several techniques, including thermal analyses (differential scanning calorimetry and thermogravimetry), spectroscopies (FT-IR, XRD), elemental analysis, and scanning electron microscopy. The kinetics and the adsorption isotherms of CTS-CAA towards both Cu (II) and Zn (II) have been determined in the aqueous solvent under variable pH. The obtained results have been analyzed by using different adsorption models. In addition, the experiments have been conducted at variable temperatures to explore the thermodynamics of the adsorption process. The regeneration of CTS-CAA has been investigated by studying the desorption process using different eluents. This paper reports an efficient protocol to synthesize chitosan-based material perspective as regenerative adsorbents for heavy metals.

The binary xerogels TiO2-SiO2 are widely used as catalysts and their carriers in organic synthesis. Characterization and adjustment of the electrostatic properties of the surface and the local acidity inside the pores, are necessary for the further development of TiO2-SiO2 xerogels applications. This research investigates acid–base equilibria in the pores, and the surface electrostatic potential (SEP) of binary TiO2-SiO2 xerogels, by the EPR of stable pH-sensitive nitroxide radicals. These radicals are small enough to penetrate directly into the pores, and to be adsorbed onto the surface of the material under study. This makes it possible to obtain valuable information on the acidic and electrosurface properties of the studied system. The highest negative surface electrical charge associated with surface electrical potential (SEP) was equal to −196 ± 6 mV. It was induced by the surface of the sample with a 7% TiO2 content. The local acidity inside the pores of this sample was found to be higher, by approximately 1.49 pH units, as compared to that in the external bulk solution.

Modified halloysite nanotubes (HNTs-Cl) were synthesized by a coupling reaction with (3-chloropropyl) trimethoxysilane (CPTMS). The incorporation of chloro-silane onto HNTs surface creates HNTs-Cl, which has great chemical activity and is considered a good candidate as an active site that reacts with other active molecules in order to create new materials with great applications in chemical engineering and nanotechnology. The value of this work lies in the fact that improving the degree of grafting of chloro-silane onto the HNT’s surface has been accomplished by incorporation of HNTs with CPTMS under different experimental conditions. Many parameters, such as the dispersing media, the molar ratio of HNTs/CPTMS/H2O, refluxing time, and the type of catalyst were studied. The greatest degree of grafting was accomplished by using toluene as a medium for the grafting process, with a molar ratio of HNTs/CPTMS/H2O of 1:1:3, and a refluxing time of 4 h. The addition of 7.169 mmol of triethylamine (Et3N) and 25.97 mmol of ammonium hydroxide (NH4OH) led to an increase in the degree of grafting of CPTMS onto the HNT’s surface.