Search Results (33)

Andean berry (Vaccinium meridionale Swartz) is a species of berry mostly exclusive to the Andean ecosystems, mainly present in Colombia, Venezuela, Peru, and Jamaica, where it grows between 2000 and 3000 m.a.s.l. Although most of the fruit is harvested naturally, limited fruit production significantly restricts large-scale farming and sales. Most research on phytochemicals from this berry has focused on polyphenolic compounds, particularly anthocyanins such as cyanidin-3-O-galactoside and delphinidin-3-O-hexoside. These compounds have significant antioxidant potential and require appropriate post-harvest handling to preserve their stability and biological functionality. A systematic literature search was conducted covering studies from January 2000 to January 2025 across Scopus, PubMed, Web of Science, and Google Scholar. Evidence from original research includes chemical analyses, in vitro biological activity, in vivo effects in animal models, and clinical studies. Although findings suggest antiproliferative, chemoprotective, and cardioprotective properties, current evidence remains largely preclinical, and clinical validation is urgently needed. Despite its promise, challenges persist in standardizing cultivation, scaling production, and optimizing post-harvest. The berry has been incorporated into food products, but further research is essential to support its transition from experimental use to validated clinical applications. Full article

Aflatoxins (AFs) represent a major threat to poultry health and food safety due to their hepatotoxic, immunosuppressive, and carcinogenic effects. This study evaluated the chemoprotective potential of ethoxyquin (EQ) and N-acetylcysteine (NAC) in laying hens (80.8 and 33.3 mg/kg BW/d) exposed to chronic dietary AFs contamination (0.0–1.5 mg/kg). A total of 360 Hy-Line W36 Leghorn hens were monitored over 72 weeks using biochemical and histopathological analyses of liver and kidney tissues. NAC significantly (p < 0.01) increased hepatic and renal levels of reduced glutathione (GSH) and stimulated glutathione S-transferases (GST) and gamma-glutamyl transferase (GGT) activity, enhancing detoxification. Both agents significantly (p < 0.05) reduced plasma ALT and AST levels, preserved total protein concentrations, and attenuated liver and kidney hypertrophy. EQ demonstrated antioxidant effects, stabilizing enzymatic responses and limiting tissue damage. Histopathological analysis revealed fewer structural alterations and cellular degeneration, especially in the NAC-treated group (p < 0.01). These results suggest that NAC and EQ activate endogenous detoxification mechanisms, both enzymatic and non-enzymatic, effectively mitigating chronic aflatoxin toxicity. Their dietary supplementation offers a safe and sustainable chemoprotection strategy to support poultry health and productivity, particularly in regions facing high mycotoxin exposure. Full article

Saffron spice is obtained from the flower’s stigmas through a labor-intensive process. However, other organs (particularly the leaves and tepals) are often regarded as waste. To investigate the health benefits of saffron leaf by-products, an optimized methodology was developed to obtain a phenol-enriched fraction. The main components of this fraction were identified by HPLC-DAD/ESI-MS and the antiproliferative and metal-chelating effects on colon cancer cells (Caco-2) and Fe²⁺ and Cu²⁺ ions, respectively, were evaluated. The process involved the extraction of saffron leaves with a 70% hydroalcoholic solution, followed by purification using liquid chromatography. Chemical characterization revealed the presence of several phenolic compounds, including flavonoids (kaempferol, luteolin and quercetin glycosides) as major constituents; whereas, in vitro assays revealed a strong dose-dependent inhibition of cell proliferation. Likewise, the sample exhibited significant iron- and copper-chelating activity, suggesting its potential as a natural chelator to help mitigate the carcinogenic effects of metal accumulation in humans. In summary, this study underscores the potential of the saffron leaf fraction as a promising natural and complementary chemoprotective agent in colorectal cancer. Additionally, these results underscore the value of agricultural by-products, supporting a circular bioeconomy by reducing environmental impact and promoting the sustainable use of natural resources. Full article

Cisplatin is a common and highly effective chemotherapeutic agent whose nephrotoxic side effect is well-characterized. Sodium thiosulfate (STS), an FDA-approved hydrogen sulfide (H₂S) donor drug, is emerging as a chemoprotective agent against cisplatin-induced nephrotoxicity (CIN). In this study, we investigated the chemoprotective mechanism of STS in a rat model of CIN. Twenty-five male Sprague Dawley rats were randomly assigned to the following groups: HC: Healthy control (received 10 mL/kg/day of 0.9% saline intraperitoneally (ip), [n = 5]), CIN: Cisplatin (received single dose of 7 mg/kg cisplatin ip [n = 5]); CIN + PAG: Cisplatin and daily ip administration of 40 mg/kg of the H₂S inhibitor, DL-propargylglycine (PAG) for 28 days (n = 5); CIN + PAG + STS: Cisplatin and daily PAG and STS (150 µM) ip injection for 28 days; CIN + STS: Cisplatin and daily STS ip administration for 28 days (n = 5). Rats in each group were kept in metabolic cages for 24 h on day 0, 14 and 29 after cisplatin administration for urine collection. Rats were then euthanized, and kidney and blood samples were collected for analysis. Histologically, CIN was characterized by glomerular and tubular injury and significant macrophage influx and tubular apoptosis, as well as markedly increased levels of plasma and renal IL-1β, IL-6 and TNF-α and impaired renal antioxidant status compared to HC rats (p < 0.001). These pathological changes were exacerbated in CIN + PAG rats and were strongly reduced in CIN + PAG + STS rats relative to CIN + PAG rats (p < 0.01), while superior renal protection was observed in CIN + STS rats. Functionally, CIN was evidenced by markedly increased levels of serum creatinine and BUN, and significantly decreased urine creatinine, renal creatinine clearance, as well as electrolyte imbalance and urinary concentrating defect in comparison with HC (p < 0.01). These functional changes worsened significantly in CIN + PAG rats (p < 0.05) but improved in CIN + PAG + STS rats, with further improvement in CIN + STS rats to levels comparable to HC rats. Mechanistically, STS increased renal and plasma levels of H₂S, arginine, cAMP, nitric oxide (NO) and cGMP as well as SIRT3 and PGC-1α. We have shown for the first time that STS provides chemoprotection against CIN by activating renal arginine/cAMP and NO/cGMP signaling pathways and their downstream mechanisms through increased renal H₂S production. Full article

Natural products hold immense potential for drug discovery, yet many remain unexplored in vast libraries and databases. In an attempt to fill this gap and meet the growing demand for effective drugs, this study delves into the promising world of ent-kaurane diterpenoids, a class of natural products with huge therapeutic potential. With a dataset of 570 ent-kaurane diterpenoids obtained from the literature, we conducted an in silico analysis, evaluating their physicochemical, pharmacokinetic, and toxicological properties with a focus on their therapeutic implications. Notably, these natural compounds exhibit drug-like properties, aligning closely with those of FDA-approved drugs, indicating a high potential for drug development. The ranges of the physicochemical parameters were as follows: molecular weights—288.47 to 626.82 g/mol; number of heavy atoms—21 to 44; the number of hydrogen bond donors and acceptors—0 to 8 and 1 to 11, respectively; the number of rotatable bonds—0 to 11; fraction Csp3—0.65 to 1; and TPSA—20.23 to 189.53 Ų. Additionally, the majority of these molecules display favorable safety profiles, with only 0.70%, 1.40%, 0.70%, and 46.49% exhibiting mutagenic, tumorigenic, reproduction-enhancing, and irritant properties, respectively. Importantly, ent-kaurane diterpenoids exhibit promising biopharmaceutical properties. Their average lipophilicity is optimal for drug absorption, while over 99% are water-soluble, facilitating delivery. Further, 96.5% and 28.20% of these molecules exhibited intestinal and brain bioavailability, expanding their therapeutic reach. The predicted pharmacological activities of these compounds encompass a diverse range, including anticancer, immunosuppressant, chemoprotective, anti-hepatic, hepatoprotectant, anti-inflammation, antihyperthyroidism, and anti-hepatitis activities. This multi-targeted profile highlights ent-kaurane diterpenoids as highly promising candidates for further drug discovery endeavors. Full article

Lepidium draba (hoary cress) is a perennial plant belonging to the Brassicaceae family that produces two dominant glucosinolates (GLSs): glucoraphanin (GRN) and sinalbin (SBN). They represent the stored form, which is converted upon the myrosinase (Myr) hydrolysis activity to active compounds, mainly isothiocyanates (ITCs) such as sulforaphane (SFN) or p-hydroxybenzyl isothiocyanate (pHBITC). Research on ITCs that have proven anticancer, antimicrobial, and chemoprotective properties is usually conducted with pure commercially available compounds. However, these are chemically reactive, making it difficult to use them directly for preventive purposes in dietary supplements. Efforts are currently being made to prepare dietary supplements enriched with GLS and/or Myr. In this study, we report a simple but efficient chromatographic procedure for the isolation and purification of GLSs from MeOH extract from hoary cress based on a combination of ion exchange and gel permeation chromatography on DEAE-Sephadex A-25 and Sephadex LH-20. To obtain the Myr required for efficient hydrolysis of GLSs into antibacterial ITCs, we developed a rapid method for its extraction from the seeds of Lepidium sativum (garden cress). The yields of GLSs were 22.9 ± 1.2 mg GRN (purity 96%) and 10.4 ± 1.1 mg SBN (purity 92%) from 1 g of dry plant material. Both purified GLSs were used as substrates for the Myr. Analysis of the composition of hydrolysis products (HPs) revealed differences in their hydrolysis rates and in the degree of conversion from GLSs to individual ITCs catalyzed by Myr. When GRNs were cleaved, SFNs were formed in an equimolar ratio, but the formation of pHBITCs was only half that of cleaved SBNs. The decrease in pHBITC content is due to its instability compared to SFN. While SFN is stable in aqueous media during the measurement, pHBITC undergoes non-enzymatic hydrolysis to p-hydroxybenzyl alcohol and thiocyanate ions. Testing of the antimicrobial effects of the HPs formed from GRN by Myr under premix or in situ conditions showed inhibition of the growth of model prokaryotic and eukaryotic microorganisms. This observation could serve as the jumping-off point for the design of a two-component mixture, based on purified GLSs and Myr that is, usable in food or the pharmaceutical industry in the future. Full article

Breast cancer is the most frequent type of cancer in women. Oncogenic transcription factors promote the overproduction of cellular adhesion molecules and inflammatory cytokines during cancer development. Cancer cells exhibit significant upregulation of antiapoptotic proteins, resulting in increased cell survival, tumor growth, and metastasis. Research on the cell cycle-mediated apoptosis pathway for drug discovery and therapy has shown promising results. In fact, dietary phytoconstituents have been extensively researched for anticancer activity, providing indirect protection by activating endogenous defense systems. The role of polyphenols in key cancer signaling pathways could shed light on the underlying mechanisms of action. For instance, Rosmarinic Acid, a polyphenol constituent of many culinary herbs, has shown potent chemoprotective properties. In this review, we present recent progress in the investigation of natural products as potent anticancer agents, with a focus on the effect of Rosmarinic Acid on triple-negative BC cell lines resistant to hormone therapy. We highlight a variety of integrated chemical biology approaches aimed at utilizing relevant mechanisms of action that could lead to significant clinical advances in BC treatment. Full article

Red beetroot extract (E162) is a natural colorant that owes its color to betanin, its major red pigment. Betanin displays remarkable antioxidant, anti-inflammatory, and chemoprotective properties mediated by its structure and influence on gene expression. However, the betanin employed in most preclinical assays is a beetroot extract diluted in dextrin, not pure betanin, as no isolated compound is commercially available. This makes its use inaccurate concerning product content estimates and biological effect assessments. Herein, a combination of conventional extraction under orbital shaking and ultrasound-assisted extraction (UAE) to purify betanin by semi-preparative HPLC was performed. The employed methodology extracts betalains at over a 90% yield, achieving 1.74 ± 0.01 mg of pure betanin/g beetroot, a 41% yield from beetroot contents increasing to 50 %, considering the betalains pool. The purified betanin exhibited an 85% purity degree against 32 or 72% of a commercial standard evaluated by LC-MS or HPLC methods, respectively. The identity of purified betanin was confirmed by UV-Vis, LC-MS, and ¹H NMR. The combination of a conventional extraction, UAE, and semi-preparative HPLC allowed for betanin purification with a high yield, superior purity, and almost three times more antioxidant power compared to commercial betanin, being, therefore, more suitable for clinical purposes. Full article

Isorhamnetin has gained research interest for its anti-inflammatory, anti-proliferative and chemoprotective properties. In this study, human colon adenocarcinoma cells were cultured in the presence or absence of different isorhamnetin concentrations (5–150 μM) for 24 h or 48 h of cultivation to explore the impact on several parameters of viability/proliferation (mitochondrial function using an MTT test, metabolic activity, cell membrane integrity and lysosomal activity using a triple test). The intracellular generation of superoxide radicals using an NBT test and ELISA analysis was performed to observe the biosynthesis of interleukin 8 (IL-8) in cells stimulated with zymosan, as well as in basal conditions. The antiproliferative activity of isorhamnetin was demonstrated by significantly reduced values of mitochondrial and metabolic activity, integrity of cell membranes and lysosomal activity. Its high prooxidant potential was reflected by the significantly elevated generation of superoxides even in cells with low viability status. The anti-inflammatory effect of isorhamnetin was evident due to decreased IL-8 production, and the most significant decline in IL-8 concentration was observed after 24 h treatment in cells with induced inflammation. We demonstrated that isorhamnetin can suppress the proliferation of HT-29 cells, and this effect was correlated with pro-oxidative and anti-inflammatory activity of isorhamnetin. Full article

Perilla frutescens (PF) seed residue is a waste from perilla oil production that still contains nutrients and phytochemicals. This study aimed to investigate the chemoprotective action of PF seed residue crude ethanolic extract (PCE) on the inflammatory-induced promotion stage of rat colon carcinogenesis and cell culture models. PCE 0.1 and 1 g/kg body weight were administered by oral gavage to rats after receiving dimethylhydrazine (DMH) with one week of dextran sulfate sodium (DSS) supplementation. PCE at high dose exhibited a reduction in aberrant crypt foci (ACF) number (66.46%) and decreased pro-inflammatory cytokines compared to the DMH + DSS group (p < 0.01). Additionally, PCE could either modulate the inflammation induced in murine macrophage cells by bacterial toxins or suppress the proliferation of cancer cell lines, which was induced by the inflammatory process. These results demonstrate that the active components in PF seed residue showed a preventive effect on the aberrant colonic epithelial cell progression by modulating inflammatory microenvironments from the infiltrated macrophage or inflammatory response of aberrant cells. Moreover, consumption of PCE could alter rat microbiota, which might be related to health benefits. However, the mechanisms of PCE on the microbiota, which are related to inflammation and inflammatory-induced colon cancer progression, need to be further investigated. Full article

Plant secondary metabolites, known as phytochemicals, have recently gained much attention in light of the “circular economy”, to reutilize waste products deriving from agriculture and food industry. Phytochemicals are known for their onco-preventive and chemoprotective effects, among several other beneficial properties. Apple phytochemicals have been extensively studied for their effectiveness in a wide range of diseases, cancer included. This review aims to provide a thorough overview of the main studies reported in the literature concerning apple phytochemicals, mostly polyphenols, in cancer prevention. Although there are many different mechanisms targeted by phytochemicals, the Nrf2 and NF-κB signaling pathways are the ones this review will be focused on, highlighting also the existing crosstalk between these two systems. Full article

The aim of the present study was to validate the cytotoxicity, genotoxicity, and preventive potential against benzo(a)pyrene (BaP)-induced DNA damage of nine samples of thyme and chestnut honeys enriched with bee products (royal jelly and propolis, 2–10%). Cell viability was determined by the MTT [3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide] assay (0–250 mg/mL) to select nontoxic concentrations, and DNA damage (0.1–10 μg/mL) was evaluated by the alkaline single-cell gel electrophoresis or comet assay. Treatment with honey samples or royal jelly and propolis did not affect the viability of HepG2 cells up to 100 and 50 mg/mL, respectively. Treatment with 100 μM BaP significantly increased (p ≤ 0.001) the levels of the DNA strand breaks. None of the tested concentrations (0.1–10 μg/mL) of the honey samples (thyme and chestnut), royal jelly, and propolis caused DNA damage per se. All tested samples at all the concentrations used decreased the genotoxic effect of BaP. In addition, all mixtures of thyme or chestnut honeys with royal jelly or propolis showed a greater protective effect against BaP than the samples alone, being the thyme and chestnut honey samples enriched with 10% royal jelly and 10% propolis the most effective (70.4% and 69.4%, respectively). The observed protective effect may be associated with the phenolic content and antioxidant capacity of the studied samples. In conclusion, the thyme and chestnut honey samples enriched with bee products present potential as natural chemoprotective agents against the chemical carcinogen BaP. Full article

Cruciferous vegetables such as cauliflower and radish contain isothiocyanates exhibiting chemoprotective effects in vitro and in vivo. This research aimed to assess the impact of cauliflower (CIE) and radish (RIE) isothiocyanate extracts on the metabolic activity, intracellular reactive oxygen species (ROS), and LDH production of selected human colorectal adenocarcinoma cells (HCT116 and HT-29 for early and late colon cancer development, respectively). Non-cancerous colon cells (CCD-33Co) were used as a cytotoxicity control. The CIE samples displayed the highest allyl isothiocyanate (AITC: 12.55 µg/g) contents, whereas RIE was the most abundant in benzyl isothiocyanate (BITC: 15.35 µg/g). Both extracts effectively inhibited HCT116 and HT-29 metabolic activity, but the CIE impact was higher than that of RIE on HCT116 (IC₅₀: 0.56 mg/mL). Assays using the half-inhibitory concentrations (IC₅₀) of all treatments, including AITC and BITC, displayed increased (p < 0.05) LDH (absorbance: 0.25–0.40 nm) and ROS release (1190–1697 relative fluorescence units) in both cell lines. BITC showed the highest in silico binding affinity with all the tested colorectal cancer molecular markers (NF-kB, β-catenin, and NRF2-NFE2). The theoretical evaluation of AITC and BITC bioavailability showed high values for both compounds. The results indicate that CIE and RIE extracts display chemopreventive effects in vitro, but additional experiments are needed to validate their effects. Full article

Stigmasterol is an unsaturated phytosterol belonging to the class of tetracyclic triterpenes. It is one of the most common plant sterols, found in a variety of natural sources, including vegetable fats or oils from many plants. Currently, stigmasterol has been examined via in vitro and in vivo assays and molecular docking for its various biological activities on different metabolic disorders. The findings indicate potent pharmacological effects such as anticancer, anti-osteoarthritis, anti-inflammatory, anti-diabetic, immunomodulatory, antiparasitic, antifungal, antibacterial, antioxidant, and neuroprotective properties. Indeed, stigmasterol from plants and algae is a promising molecule in the development of drugs for cancer therapy by triggering intracellular signaling pathways in numerous cancers. It acts on the Akt/mTOR and JAK/STAT pathways in ovarian and gastric cancers. In addition, stigmasterol markedly disrupted angiogenesis in human cholangiocarcinoma by tumor necrosis factor-α (TNF-α) and vascular endothelial growth factor receptor-2 (VEGFR-2) signaling down-regulation. The association of stigmasterol and sorafenib promoted caspase-3 activity and down-regulated levels of the anti-apoptotic protein Bcl-2 in breast cancer. Antioxidant activities ensuring lipid peroxidation and DNA damage lowering conferred to stigmasterol chemoprotective activities in skin cancer. Reactive oxygen species (ROS) regulation also contributes to the neuroprotective effects of stigmasterol, as well as dopamine depletion and acetylcholinesterase inhibition. The anti-inflammatory properties of phytosterols involve the production of anti-inflammatory cytokines, the decrease in inflammatory mediator release, and the inhibition of inducible nitric oxide synthase (iNOS) and cyclooxygenase-2 (COX-2). Stigmasterol exerts anti-diabetic effects by reducing fasting glucose, serum insulin levels, and oral glucose tolerance. Other findings showed the antiparasitic activities of this molecule against certain strains of parasites such as Trypanosoma congolense (in vivo) and on promastigotes and amastigotes of the Leishmania major (in vitro). Some stigmasterol-rich plants were able to inhibit Candida albicans, virusei, and tropicalis at low doses. Accordingly, this review outlines key insights into the pharmacological abilities of stigmasterol and the specific mechanisms of action underlying some of these effects. Additionally, further investigation regarding pharmacodynamics, pharmacokinetics, and toxicology is recommended. Full article

Calluna vulgaris, belonging to the Ericaceae family, is an invasive plant that has widely spread from Europe all across Asia, North America, Australia and New Zealand. Being able to survive in rigid soil and environmental conditions, it is nowadays considered to be of high nature-conservation value. Known for its nutritional and medicinal properties, C. vulgaris stands out for its varied physiochemical composition, spotlighting a wide range of biological activity. Among the most important bioactive compounds identified in C. vulgaris, the phenolic components found in different parts of this herbaceous plant are the main source of its diverse pro-health properties (antioxidant, anti-inflammatory, antimicrobial, chemoprotective, etc.). Nonetheless, this plant exhibits an excellent nectariferous potential for social insects such as honeybees; therefore, comparing the bioactive compounds observed in the plant and in the final product of the beehive, namely honey, will help us understand and find new insights into the health benefits provided by the consumption of C. vulgaris-related products. Thus, the main interest of this work is to review the nutritional profile, chemical composition and biological activities of the C. vulgaris plant and its related honey in order to encourage the future exploration and use of this health-promoting plant in novel foods, pharmacological products and apitherapy. Full article