Chlorogenic Acid Research Articles

In vitro Antioxidant Activity of 5-caffeoylquinic Acid and Ester Analogues

Background: Chlorogenic acid, an ester of caffeic acid with quinic acid, also known as 5- O-caffeoylquinic acid (5-CQA), is a ubiquitous plant constituent that is an important intermediate in lignin biosynthesis. In some cases, it occurs at surprisingly high levels in the leaves and fruits of certain higher plants, such as coffee beans. Due to its catechol moiety and an extended side chain conjugation, it easily forms a resonance-stabilised phenoxy radical, accounting for its powerful antioxidant potential. Objective: The objective of this work was to determine if the esterification and methylation of 5- CQA would enhance its antioxidant activity. Methods: Two 5-CQA derivatives were prepared for this study. Chlorogenic acid was esterified with methanol over Amberlite IR120-H to obtain methyl chlorogenate, while methyl 3',4´-dimethyl chlorogenate was prepared from 5-CQA by treatment with diazomethane. Spectroscopic methods confirmed the structure of these derivatives. Their antioxidant properties were tested to establish a relationship between structure and antioxidant activity. Results: Antioxidant activity results were generated for 5-CQA and its ester analogues using eight different methods. Depending on the method applied, results were expressed as IC50/MCE50 values or as equivalents of the applied standard (ascorbic acid and Trolox). Conclusion: In most of these tests, 5-CQA showed the highest antioxidant activity compared to its derivatives. Nevertheless, due to their hydrophobic characteristics, their ester analogues remain promising antioxidant candidates in emulsifying systems.

Antibacterial, antioxidant and barrier properties of clay-doped electrospun fibers

Nowadays, packaging technologies have been extensively developed, including active and intelligent packages able to promote quality, safety, and the product shelf life. At this purpose, the aim of the study was focused on the design and development of polyvinyl alcohol-based nanofibers doped with two natural clays, montmorillonite or clinoptilolite, and loaded with chlorogenic acid, as nanofibrous membranes to control microbial contamination and oxidative state upon direct contact. The results showed that the 1 % w/w clay doping was the optimal concentration to obtain continuous and uniform nanofibers. In addition, chlorogenic acid loading (5 % w/w) into the nanofibers did not change the systems morphology, resulting in a chlorogenic acid sustained release, achieving 100 % within 24 h for all the systems with enhanced antioxidant and antimicrobial activities. Depending on their structure, the presence of the clays mineral was able to affect the aqueous vapor permeability. These results suggested the promising applications of the clay doped polyvinyl alcohol-based nanofibrous membranes as smart advanced material able to control microbial contamination and oxidative degradation to be used in biomedical field or as active packaging.

Metabolite profiles of green leaves and coffee beans as predictors of coffee sensory quality in Robusta (Coffea canephora) germplasm from the Democratic Republic of the Congo

Research on the chemical composition of coffee beans and its correlation with sensory quality is advancing, but the metabolites in coffee leaves have often been overlooked. This study investigated the metabolite profiles of roasted coffee, green beans, and coffee leaves from 39 C. canephora genotypes through LC-HRMS with an untargeted metabolomics approach. Our results showed that metabolite profiles of roasted coffee, green beans, and coffee leaves can be discriminated based on the coffee's sensory quality. The highest predictive power of coffee sensory quality was achieved with the metabolite profiles of the coffee leaves. Genotypes with varying genetic backgrounds could only be discriminated by the metabolite profiles of the coffee leaves. Metabolite marker compounds predictive of sensory quality were a putative quercetin derivate in green beans and likely physagulin E and argophyllin in coffee leaves. Estimated levels of caffeoylquinic acids, dicaffeoylquinic acids, and caffeoylquinic acid lactones were higher in roasted coffee with a lower sensory quality. These differences were not apparent in their respective green beans and coffee leaves. Overall, our study revealed the promising potential of the metabolite profile of coffee leaves as a predictive tool for coffee sensory quality and the genetic background of C. canephora.

From millets to medicine: ADMET insights into diabetes management with P. sumatrense compounds

Diabetes mellitus, a prevalent metabolic disorder characterised by impaired blood glucose regulation, has escalated into a global health crisis, exacerbated by high-glycaemic diets and unhealthy eating habits. While therapeutic agents such as acarbose mitigate diabetes by inhibiting alpha-amylase and alpha-glucosidase, their use is marred by adverse side effects, underscoring the need for safer, plant-based alternatives. This study explores the antidiabetic potential of Little Millet, an underutilised cereal grain with a low glycaemic index, rich in bioactive compounds. Unlike common staples such as wheat and rice, Little Millet contains unique compounds, including octodrine, 18,19-secoyohimban-19-oic acid, and phenylephrine, which were investigated for their novel application in diabetes management. Gas chromatography-mass spectrometry (GCMS) analysis identified 120 bioactive compounds, selected for their abundance and potential bioactivity. These compounds span fatty acids, phenols, flavonoids, organic acids, sugar alcohols, and amino acids, all of which were rigorously docked to alpha-amylase and human maltase-glucoamylase receptors. Notably, key ligands such as chlorogenic acid and 18,19-secoyohimban-19-oic acid exhibited superior binding affinities compared to acarbose, with promising drug-likeness and ADMET profiles, suggesting higher absorption and fewer side effects. A 100-ns dynamics simulation further validated the stability of these compounds, positioning them as viable candidates for diabetes treatment. These findings advance drug design and highlight the potential of incorporating Little Millet into diets for diabetes prevention. Further validation through In-vitro, In-vivo, and clinical studies is essential to fully realise their therapeutic potential. This research also opens avenues for exploring Little Millet in managing related conditions and enhancing its health benefits through breeding programmes.

Phytochemical Profile and Antioxidant and Protective Activities of Various Types of Extracts from Hyssopus officinalis L. and Grindelia robusta Nutt. Herb Grown in Poland.

The available literature indicates that Hyssopus officinalis and Grindelia robusta are raw materials with great potential for use in prevention and therapy. Therefore, the aims of this study were to assess the phytochemical profile and antioxidant and cytoprotective properties of extracts prepared using various solvents, additionally taking into account different methods of drying the plant material. Hydrodistilled oil was analysed by GC-MS. The chemical composition of the extracts was estimated by spectrophotometry and the HPLC-DAD method. Antioxidant activity was evaluated using DPPH and FRAP and measuring the intracellular level of ROS. Alamar Blue and Neutral Red tests were used to assess the cytotoxicity of the extracts on skin cells - keratinocytes and fibroblasts. The major components of hyssop essential oil were cis- (44.9%) and trans- (18.2%) pinocamphone, while borneol (16.1%), and α-pinene (12.0%) were predominant in grindelia essential oil. Flavonoids were dominant in the extracts (water:ethanol, water:methanol, and water: glycerol) from hot-air dried hyssop herb, while phenolic acids were the predominant compounds in the grindelia herb extracts. The water:ethanol hyssop extract had the highest total content of flavonoids (42.26 mg CE/mL), among which isoquercitrin and rutin were present in the highest quantities (32.61 mg/mL and 21.47 mg/mL, respectively). In the case of grindelia, the highest total phenolic acid content (26.24 mg CAE/mL) was recorded in the water:ethanol extract, and the dominant compounds among them were 1,5-dicaffeoylquinic and chlorogenic acid (10.85 and 6.39 mg/mL, respectively). The water:ethanol extract from both plants also exhibited the highest antioxidant activity in the DPPH and FRAP tests (79.19% and 1.39 mmol/L, respectively, for grindelia and 67.61% and 1.04 mmol/L for hyssop) and was most effective at reducing the level of ROS in cells. In addition, water:ethanol extracts may have a positive impact on the viability of skin cells in vitro. Water:ethanol extracts from H. officinalis and G. robusta herb are promising sources of active compounds and may find application as natural materials with valuable biological properties, which require further in vitro and in vivo testing.

Hypoxia-reoxygenation Extends the Lifespan of Caenorhabditis elegans via SKN-1- and DAF-16A-Dependent Stress Hormesis.

To study the role of hypoxia-reoxygenation and anoxia-starvation on the lifespan of C. elegans and elucidate the mechanism at molecular levels. Increasing evidence indicates that reactive oxygen species (ROS) act as signaling molecules that promote health. Hormesis occurs when a moderate stress level induces a beneficial adaptive response, protecting organisms against subsequent exposure to severe stress. Caenorhabditis elegans is a widely used model organism to study aging and displays a broad hormetic ability to couple with stress. To date, only few methods are available to induce stress hormesis in C. elegans. The objectives of this study were to explore the effects of hypoxia-reoxygenation and anoxia-starvation on the lifespan of C. elegans, exploring the involvement of ROS and oxidative stress-related pathways, and examining the hormetic property of H/R. The C. elegans were cultured in hypoxic conditions (1% O2) with OP50 bacteria for 24 h followed by reoxygenation (20% O2) (H/R) or in anoxic conditions (0% O2; 100% N2) without OP50 bacteria for 24 h followed by reoxygenation (20% O2) and food supplementation (A/S). Survivals were plotted and estimated for probability with Kaplan-Meier analysis. The H/R extended the lifespan of C. elegans, and H/R-pretreated worms showed improved resistance toward A/S compared to naïve worms. The C. elegans SKN-1 and DAF-16 are important oxidative stress response factors homologous to mammalian Nrf2 and FOXO3, respectively. Mutations in SKN-1 and DAF-16 blocked H/R-induced life extension. Next, H/R treatment in C. elegans activated both SKN-1 and DAF-16, as indicated by the upregulation of putative target genes of SKN-1 (gcs-1 and gss-1) and DAF-16 (sod-3). Moreover, pre-treatment with antioxidants (N-acetylcysteine, chlorogenic acid, and sulforaphane) reduced ROS levels and diminished the lifespan extension effect of H/R, indicating their dependency on ROS. These results provide evidence that H/R is beneficial for lifespan and stress resistance by activating the adaptive cellular response pathway (SKN-1 and DAF-16A) toward oxidative stress.

Dietary Supplementation for Retinitis Pigmentosa: A Report by the American Academy of Ophthalmology

To review the evidence on the effectiveness of dietary supplementation for retinitis pigmentosa (RP). A literature search of the PubMed database was last conducted in January 2024 to identify published English-language original research on dietary supplementation for RP. Eligible compounds included products ingested orally containing nutrients intended to supplement the diet. Studies meeting eligibility criteria were assigned a level of evidence rating by the panel methodologist. The search identified 283 citations, 15 of which met the assessment criteria. Two studies were rated level I, 11 studies were rated level II, and 2 studies were rated level III. All were single-center studies and were published between 1993 and 2022. The products evaluated included vitamin A, docosahexaenoic acid (DHA), lutein, vitamin E, goji berry (Lycium barbarum fruit) extract, and chlorogenic acid. Primary outcome measures were most commonly based on electroretinography (n= 7) or perimetry (n= 2) testing. Numerous studies highlighted data suggestive of possible efficacy for vitamin A, DHA, and lutein, yet these findings typically derived from secondary outcomes, evaluations of participant subsets, post hoc analyses, problematic interpretations of the data, or a combination thereof. Additionally, it was often unclear if the study findings represented clinically meaningful outcomes. No prominent safety concerns were reported in any study. No high-quality evidence was found to support the effectiveness of any form of dietary supplementation for RP. The findings underscore the challenges of studying this rare and slowly progressive retinal disease. Future studies should leverage the enhanced recruitment abilities from collaborative research networks to refine eligibility criteria while using novel, clinically meaningful endpoints. Proprietary or commercial disclosure may be found in the Footnotes and Disclosures at the end of this article.

Enhanced protection and bioavailability of Lycium barbarum leaf extract through encapsulation in whey protein isolate and bovine serum albumin nanoparticles

To improve the stability and bioavailabilityhe of polyphenolics in Lycium barbarum leaf, this study encapsulated L. barbarum leaf extracts (LLE) within whey protein isolate (WPI) and bovine serum albumin (BSA) nanoparticles (NPs) via self-assembly to enhance polyphenol distribution. The physicochemical properties of nanoparticles were characterized using transmission electron microscopy (TEM), Fourier transform infrared spectroscopy (FTIR), X-ray diffraction (XRD), differential scanning calorimetry (DSC) and thermogravimetric (TG), respectively. The nanoparticles also showed good physical stability at various temperatures, different pH and NaCl concentrations. Compared with BSA-LLE NPs, WPI-LLE NPs exhibited strong physical stability with encapsulation efficiency of 70.6 %. The polyphenol nanoparticles demonstrated enhanced stability in the presence of stomach acid during in vitro simulated digestion. Additionally, the nanoparticles enhanced polyphenol stability during simulated gastrointestinal digestion. Following intestinal digestion, compared with LLE, the bioaccessibility of total phenolic increased by 53.67 % (WPI-LLE NPs), with specific enhancement in compounds like kaempferol, rutin, and chlorogenic acid.

Biofunctionality of a new vinegar rich in anthocyanin from red-fleshed Niedzwetzky's apple: An ornamental plant.

In recent years, red-fleshed apple has attracted a lot of attention due to its pleasant appearance, taste, and being a valuable source of anthocyanins. Generally, different types of this apple are known as ornamental apple plants that are rarely found in various regions around the world like New Zealand, Kazakhstan, Kyrgyzstan, Australia,China, and Turkey. This study focused on the accumulation and changes of the bioactive and aroma-related volatile components at different production stages of a red-fleshed apple vinegar. The aim of this study is to produce an anthocyanin- and vitamin C-rich vinegar (NAV) from red-fleshed Niedzwetzky's apple for the first time. According to the results, in this vinegar, it wasdetermined high concentrations of total phenolic content (904.8mg-GAE/mL), total flavonoid content (0.25mg-EGCE/mL), vitamin C content (3024.3mg-AAE/mL), and 1,1-diphenyl-2-picrylhydrazyl (8.33mmol-TE/mL), as well as FRAP (13.57mmol-ISE/mL), respectively. Moreover, total anthocyanin content value was found to be 6.46mg/g. One of the components that provide the specified functional effect in this vinegar is chlorogenic acid, which constitutes the main phenolic compound, and the other one is cyanidin-3-glucoside, which is the major anthocyanin in this vinegar. The main volatile components associated with the aroma of vinegar are -acetic acid, -phenylacetic acid (5067.7µg/100mL), -phenethyl alcohol (3096.1µg/100mL), and -nonanoic acid (2939.0µg/100mL) compounds. Consequently, it is recommended to expand the range of Niedzwetzky's apples in the production and consumption of food products such as functional vinegar. Thus, a new vinegar with high functional properties will be introduced to the worldwide food industry. PRACTICAL APPLICATION: In this study, vinegar was produced from the small and dark-red-flesh-colored fruits of Niedzwetzky's apple tree, which is known in a small part of the world and is generally used as an ornamental plant due to its red-pink flowers. It has been determined that the produced vinegar has high bioavailability due to the apples with red inner flesh and high anthocyanin content and has a desirable aromatic content. Thus, a food product with high functional quality and desirable aroma, accessible to consumers all over the world, has been produced from a little-known fruit.

Effect of rosemary extract on volatile flavor profile and flavor source of skipjack tuna

A fishy odor can significantly hinder the development of products made from nutritious skipjack tuna. To address this issue, rosemary extract (RE) was used as a deodorizing agent for skipjack tuna. Multi-omics techniques, including e-nose, e-tongue, gas chromatography-ion mobility mass spectrometry (GC-IMS), and gas chromatography-mass spectrometry (GC-MS), were employed to analyze the volatile flavor compounds in the skipjack tuna meat before and after deodorization. The main fishy odors found in the skipjack tuna were identified as nonanal, heptanal, hexanal, and 1-octen-3-ol, primarily resulting from lipid oxidation. Treatment with RE solutions at concentrations of 0.8% and 1.0% completely removed nonanal, hexanal, and heptanal from the skipjack tuna meat, while the level of 1-octen-3-ol was significantly reduced by 67.21% (p < 0.05). The GC-MS analysis of the impregnated solution indicated a 31% increase in 1-octen-3-ol content at a concentration of 0.2% (p < 0.05). Additionally, skipjack tuna meat treated with 0.8% and 1.0% RE showed lower peroxide values and thiobarbituric acid reactive substances values (p < 0.05). The reduction of fishy odor by RE was directly linked to decreased lipid oxidation. Quantitative analysis of phenolics revealed that the relative content of phenolics in RE was 52.54%, with the main phenolics being chlorogenic acid, caffeic acid, and luteolin. Thus, RE shows promise in eliminating fishy odors and minimizing lipid oxidation in skipjack tuna.

Study on the activity and mechanism of herbal formula anti-infection powder (AIP) against influenza-virus-induced pneumonia through genetic susceptibility genes

Anti-infection powder (AIP), a patented Chinese herbal formulation, is used traditionally in the treatment of upper respiratory tract infections. In this study, an ethanol extract of AIP was demonstrated to inhibit influenza A virus (IAV) infection and IAV-induced pneumonia (IVP), both in vitro and in vivo, highlighting its potential mechanism of action. To determine the anti-IAV activity of AIP and to explore the possible mechanisms of inhibiting IAV-induced pneumonia. An ethanol extract was extracted from AIP and its major ingredients were determined by high-performance liquid chromatography (HPLC). An IAV-infected A549 cell model and an IAV-induced mouse pneumonia model were established to evaluate the therapeutic effects of AIP on IVP in vivo and in vitro. The mice were respectively administered AIP at high- and low-dose in different groups. The anti-IAV activity of AIP was evaluated by detecting viral load, lung lesion, lung index, suvival time, inflammatory cytokines and transcriptomic analysis in the lung tissue. The potential pathways and targets that involved in AIP against IVP were predicted by network pharmacology. Mendelian randomization (MR), colocalization analysis, and molecular docking were employed to identify novel therapeutic targets for IVP. Polymerase chain reaction (PCR) and Western blot (WB) techniques were used to confirm the effect of AIP on the expression of risk target genes in the lungs of IVP mice. In A549 cell line, AIP effectively inhibited IAV infection with IC50 values of 65.49 μg/mL. The anti-IAV activity of AIP was mainly determined by chlorogenic acid, forsythiarin, puerarin, paeoniflorin and prim-o-glucosylcimigin. Moreover, AIP inhibited the neuraminidase activity and the M gene expression in vitro. In vivo, oral administration of AIP significantly reduced viral load and improved lung tissue lesions. AIP decreased the concentration of pro-inflammatory factors such as IL-1β, TNF-α, and IFN-γ, and significantly increased the concentration of the anti-inflammatory factor IL-4. According to network pharmacology analysis, toll-like receptor signaling pathway, chemokine signaling pathway, and TNF signaling pathway may be the possible mechanisms by which AIP inhibits IVP and regulates excessive inflammatory response.Two new genes, LRG1 and PSMA4, associated with genetic susceptibility to influenza and pneumonia, predicted as potential IVP drug target genes by MR and colocalization analysis. The antiviral mechanism of AIP may be to inhibit the expression levels of LRG1 and PSMA4 in lungs of mouse IVP. AIP exhibited anti-IAV activities both in vitro and in vivo. AIP had a protective effect against pneumonia caused by influenza virus and can inhibit the progression of inflammation. This effect may be associated with its ability to inhibit the expression levels of genetic susceptibility genes (LRG1 and PSMA4) in lungs of mouse IVP. The findings of this study enhance our understanding of the role and mechanisms of AIP in the treatment of IVP.

Dynamic/static pressure-induced copolymerization and property changes of lotus seed starch with chlorogenic acid

Pressure promotes the formation of starch-polyphenol complexes, but their classification and properties are still unclear. This study aimed to elucidate the effects of dynamic high-pressure homogenization (10–50 MPa) and static hydrostatic pressure (100–500 MPa) on the copolymerization behavior and properties of lotus seed starch (LS)–endogenous polyphenol chlorogenic acid (CA) complexes. The results showed that both pressures induced LS–CA to form stable inclusion-type complexes and easily destructible noninclusion-type complexes. Increased pressure promoted the formation of inclusion-type complexes, with dynamic pressure having a particularly strong effect. However, noninclusion-type complexes began breaking down at 20 MPa under dynamic pressure and 300 MPa under static pressure. Inclusion-type complexes primarily improve starch ordering, and noninclusion-type complexes enhance water holding capacity, but excessive proportions of either type affect pasting performance. These findings offer insights into transforming specific starch structures through small molecular components and provide a theoretical basis for controlling functional starch product processing.

Unveiling the Various Analytical Techniques of Polyphenols for Pharmacological Activity and Nanotechnological Delivery in Wound Healing

Polyphenols are a diverse group of molecules known for their broad range of biological activities, making them valuable in therapeutic applications, including wound healing. Chronic wounds, which are often complicated by persistent infections and the rise of antibiotic resistance, present a significant challenge in the treatment. Traditional antibiotics are becoming less effective, necessitating the exploration of new antimicrobial agents. Polyphenols like hesperidin, chlorogenic acid, quercetin, and curcumin are promising candidates due to their natural antibacterial properties, offering an effective alternative to conventional antibiotics for treating chronic wounds. However, polyphenols face challenges such as limited stability, which can reduce their effectiveness at the wound site. Furthermore, to overcome these limitations, polymer-based systems have been developed as carriers to stabilize polyphenols and control their release over time, thereby enhancing their therapeutic efficacy. This article explores the potential of polyphenols as natural antibacterial agents and highlights various nanoparticulate systems as effective carriers for treating chronic wounds.

Study on ultrasound-assisted extraction of cold brew coffee using physicochemical, flavor, and sensory evaluation

Cold brew coffee is popular with consumers due to its simple preparation and unique taste. However, traditional cold brew coffee extraction is time consuming and inefficient, which can be improved by ultrasound-assisted extraction to enhance the product market potential. In this study, the flavor profiles and sensory differences of coffee prepared at three different ultrasonic temperatures, as well as traditional cold brew and hot brew coffee, were evaluated by consumer-based sensory evaluation, Rate-All-That-Apply, combined with the determination of the content of volatile and non-volatile components. The results showed that ultrasound assisted cold brew coffee prepared at 25 °C had a good extraction effect, with chlorogenic acid (CGA) and organic acid contents of 1.05 mg/mL and 0.97 mg/mL, respectively, which were higher than the traditional cold brew coffee obtained after 12 h of preparation, with contents of 0.53 mg/mL and 0.85 mg/mL, respectively. And the total content of volatile compounds can almost reach the results of traditional cold brew for 12 h, which were 1.25 mg/kg and 1.42 mg/kg, respectively. Sensory evaluation indicated that ultrasonic treatment enhanced the sensory attributes such as nutty and cocoa flavors in the coffee. Consumers preferred the cold brew coffee obtained via ultrasound-assisted extraction. These samples presented higher levels of sweetness, floral, and fruity flavors, which were associated with 2,5-Dimethyl-3-(2-methylpropyl)pyrazine, 2,3-Dimethyl-5-(3-methylbutyl)pyrazine, (S)-(+)-4-sec-Butylpyrazole, and styrene. In this study, we demonstrated that ultrasound-assisted extraction can help reduce the time to prepare cold brew coffee and make it possible to commercialize ultrasound-assisted cold brew coffee.

Inhibition of microbiologically influenced corrosion of Al alloy 5083 in the presence of Pseudomonas aeruginosa by Artemisia annua L

Microbiologically influenced corrosion (MIC1MIC, Microbiologically Influenced Corrosion1) of Al 5083 caused by P. aeruginosa was inhibited by A. annua aqueous extract (AAE2AAE, A. annuaAqueous Extract.2). Electrochemical measurements revealed that the adsorption of AAE on the electrode surface protected Al 5083 from MIC in a simulated marine environment with inhibition efficiency of 78 %. The adsorption layer was formed due to ionized chlorogenic acid interacting with charged Al 5083 surface, preventing bacterial adhesion and growth. Adding AAE promoted the formation of a protective Al2O3, and decreased the surface layer porosity. The pitting corrosion reduced considerably when AAE was added to biotic seawater, supporting the ICP-OES results.

Aloe ferox leaf gel extracts attenuate redox imbalance in oxidative renal injury and stimulates glucose uptake, whilst inhibiting key enzymes linked to diabetes and obesity

The worldwide prevalence of diabetes and obesity is growing rapidly. Both metabolic disorders are linked to chronic adverse complications, which include kidney dysfunctions. Medicinal plants play a crucial role in traditional healthcare, especially in developing countries. Aloe ferox, native to South Africa, has a long history of medicinal use, but its pharmacological potential is less studied compared to other Aloe species, necessitating further investigation. Therefore, the present study was conducted to determine the antioxidative, anti-obesogenic, and antidiabetic effects of A. ferox leaf gel extracts using in vitro, ex vivo, and in silico experimental models, with oxidative renal damage induced by ferrous sulfate (FeSO4). A. ferox leaf gel extracts exhibited strong antioxidant activity, inhibited digestive enzymes, and significantly improved glucose uptake. The aqueous extract demonstrated better antioxidant efficacy, leading to higher reduced glutathione (GSH) level, and superoxide dismutase (SOD) and catalase enzymes activity, along with a concurrent reduction of nitric oxide (NO) and malondialdehyde (MDA) levels. Likewise, the aqueous extract showed more potent in vitro DPPH, NO, and OH• radical scavenging activity with IC50 values of 3.64 ±0.3 μg/mL, 110.73±0.1 μg/mL, and 331.13 ±0.7 μg/mL, respectively. The aqueous extract had better inhibition of the enzyme α-amylase (IC50 = 25.73±2.5 µg/mL), whilst the ethanolic extract inhibited α-glucosidase (IC50 =663.2±0.3 µg/ml), and pancreatic lipase (IC50 =122.01±5.9 µg/mL) more strongly. Incubation of the extracts with yeast cells stimulated glucose uptake dose dependently, when ethanolic extract (IC50 = 308.01±0.7 µg/mL) showed the better activity compared to the aqueous extract (IC50 = 338.79±7.05 µg/mL). Furthermore, LC-MS analysis led to the identification of many compounds, when chlorogenic acid demonstrated a stronger molecular interaction with the active site amino acids of α-amylase and catalase compared to other compounds. However, Aloin B showed the highest affinity with α-glucosidase and 5-Hydroxyaloin A showed the lowest binding energy with lipase, and SOD enzyme. These results suggest the reno-protective effects of A. ferox leaf gel extracts against FeSO4-induced oxidative stress along with its anti-hyperglycaemic activity. Given these observed effects, A. ferox leaf gel could indeed be valuable in developing natural therapies and potential drug development for the management of these disorders. Further studies in animal models are needed to ascertain the results of this study.

Caffeoylquinic acids from Silphium perfoliatum L. show hepatoprotective effects on cholestatic mice by regulating enterohepatic circulation of bile acids

Ethnopharmacological relevanceThe incidence of cholestatic liver disease (CLD), which is primarily marked by abnormal bile acids (BAs) metabolism and can result in significant hepatic injury, is rising. Nevertheless, there remains a lack of effective treatments and drugs in clinical practice. Silphium perfoliatum L. (SP) is rich in various structural types of caffeoylquinic acid (CQA) compounds, and it is a traditional herb of North American Indians with hepatobiliary therapy effects. However, its therapeutic effect and mechanism of action on CLD have never been studied. Aim of the studyTo determine if SP-8, an extract rich in CQAs from SP, protects against cholestatic liver injury induced by alpha-naphthylisothiocyanate (ANIT) and to clarify its mechanism based on the farnesoid x receptor (FXR) signaling pathway and enterohepatic circulation of BAs. Materials and methodsThe therapeutic efficacy of SP-8 was evaluated by assessing the serum biochemical indices, inflammatory factors, and liver histopathology. Targeted metabolomics of the BAs was studied in the feces, liver, serum, and bile using UPLC-MS/MS. Additionally, a Western blot analysis was used to examine the expression levels of the peroxisome proliferator-activated receptor γ (PPARγ), the FXR, and proteins related to the synthesis and transport of BAs. 16S rRNA gene sequencing was performed to evaluate the gut microbiota (GM). Finally, molecular docking simulations were conducted to assess the interaction between seven types of CQAs from SP-8 with FXR and PPARγ. ResultsSP-8 significantly enhanced the health status of cholestatic mice induced by ANIT as evidenced by a notable reduction in the liver function indices and pro-inflammatory factors, restoration of liver pathological damage, and acceleration of BAs excretion through the feces. In addition, the levels of harmful secondary BAs in the liver and blood were significantly reduced by SP-8. Furthermore, the results of the study on the mechanism of action confirmed that SP-8 not only regulated FXR and PPARγ but also significantly ameliorated the GM structure, thereby promoting the enterohepatic circulation of BAs and achieving the homeostasis of the BAs in the blood and liver. In addition, SP-8 successfully reduced the inflammatory response by strongly suppressing the nuclear translocation of NF-κBp65. According to the molecular docking results, the extract's primary active ingredients could be the seven CQAs in SP-8, as they exhibited a strong affinity for both FXR and PPARγ. Finally, the Mantel test analysis revealed a significant correlation among cholestatic-associated parameters, the GM, and BAs. ConclusionIt was confirmed for the first time that the SP-8 extract of Silphium perfoliatum L. that is rich in seven CQAs had a strong therapeutic effect on ANIT-induced CLD. Its mechanism may involve the regulation of the FXR signaling pathway and the amelioration of the GM structure to promote the homeostasis of BAs enterohepatic circulation. This study provides a potential candidate medicinal herb and its components for the development of CLD therapeutic drugs.

Investigation into the effect of acute exposure to chlorogenic acid in male wistar mice

Chlorogenic acid (CGA) is a natural polyphenolic compound widely present in various fruits, vegetables, and plant-based foods. It has gained considerable attention due to its potential health benefits including antioxidant, hepatoprotective, antibacterial, anti-inflammatory, anti-obesity, cardioprotective, neuroprotective, central nervous system stimulator, and anti-hypertensive amongst others. There is a dearth of information about acute exposure to chlorogenic acid which is also used as a food supplement. Ninety-six male Wistar mice were weight-matched into 8 groups (n=12). Group 1 was treated with distilled water, Group 2 received 1% ethanol, while Groups 3-8 were treated with 30, 60, 120, 240, 480 and 1,000 mg/kg body weight doses of CGA, respectively. Six animals were bled and sacrificed per group 24 hours post-treatment, and the liver and kidney were excised. Sections of the organs were fixed in 10% formalin for histopathological examination. Various antioxidant parameters were assayed in the liver and kidney samples using standard methods. A liver function test was also carried out on the liver samples. Haematological analysis was carried out as well as histopathology analysis of the liver and kidney samples. The remainder of the treated mice in each group were observed for mortality 24 hours post-treatment and for two weeks. Statistical analysis was performed using one-way analysis of variance (ANOVA) with p-values less than 0.05 considered to be significant. The results of this study show that chlorogenic acid led to dose-dependent increased levels of hydrogen peroxide and albumin, increased activity of alkaline phosphatase with decreased activities and levels of alanine aminotransferase, aspartate aminotransferase and bilirubin in the liver function while there were increased hydrogen peroxide levels in the kidney. The haematological parameters were not affected and the histopathological examination complemented the results with mild to moderate lesions in the liver and none in the kidney. Although, the lethal dose (LD 50-i.e., the dose at 50% mortality) was not established in this study. Therefore, chlorogenic acid should be ingested with caution.

Protective Effect of Chlorogenic Acid Against Testicular Damage Induced By Glyphosate Isopropilamine in Rats

The aim of this subchronic toxicity study was to determine the prophylactic effect of chlorogenic acid (CGA) on the histopathologic-histologic changes and oxidative stress induced by Glyphosate isopropylamine (GLF-ISO) in testicular tissues. A sum of 42 male Wistar rats were divided into six equal groups, each containing 7 rats. For pretreatment, rats were given CGA at doses of 12.5, 25 and 50 mg/kg (po) and GLF-ISO at 787.85 mg/kg (po) for 7 weeks. GLF-ISO significantly increased malondialdehyde levels while decreasing SOD and CAT activities and GSH levels in testicular tissues. On the contrary, these parameters were improved in CGA-treated groups. Furthermore, CGA ameliorated the histopathological and histological changes in testicular tissues induced by GLF-ISO in a dose-dependent manner. The results indicate that testicular damage caused by GLF-ISO can potentially be prevented or managed by CGA.

Bioactive Compounds and Valorization of Coffee By-Products from the Origin: A Circular Economy Model from Local Practices in Zongolica, Mexico.

The by-products of green coffee processing are rich in compounds that can be recycled for their possible use in the production of beverages, fertilizers and weed control in production areas. The objective of this work was to identify the organic and inorganic bioactive compounds of green coffee and the coffee by-products related to the production of origin, such as dried cascara (skin-pulp), parchment and silverskin (unroasted), in order to investigate the role their biomolecules may have in reuse through practices and local knowledge, not yet valued. The metabolomic profile by HPLC-ESI-HRMS of the aqueous extract of the dried cascara highlighted 93 non-volatile molecules, the highest number reported for dried cascara. They belong to groups of organic acids (12), alkaloids (5), sugars (5), fatty acids (2), diglycerides (1), amino acids (18), phospholipids (7), vitamins (5), phenolic acids (11), flavonoids (8), chlorogenic acids (17), flavones (1) and terpenes (1). For the first time, we report the use of direct analysis in real-time mass spectrometry (DART-MS) for the identification of metabolites in aqueous extracts of dried cascara, parchment, silverskin and green coffee. The DART analysis mainly showed the presence of caffeine and chlorogenic acids in all the extracts; additionally, sugar adducts and antioxidant compounds such as polyphenols were detected. The mineral content (K, Ca, P, S, Mg and Cl) by EDS spectrometry in the by-products and green coffee showed a relatively high content of K in the dried cascara and green coffee, while Ca was detected in double quantity in the silverskin. These metabolomic and mineral profile data allow enhancement of the link between the quality of green coffee and its by-products and the traditional local practices in the crop-growing area. This consolidates the community's experience in reusing by-products, thereby minimizing the impact on the environment and generating additional income for coffee growers' work, in accordance with the principles of circular economy and bioeconomy.