Caffeic Research Articles

Tumor integrin targeted theranostic iron oxide nanoparticles for delivery of caffeic acid phenethyl ester: preparation, characterization, and anti-myeloma activities.

Multiple myeloma (MM) is characterized by the accumulation of malignant plasma cells preferentially in the bone marrow. Currently, emerging chemotherapy drugs with improved biosafety profiles, such as immunomodulatory agents and protease inhibitors, have been used in clinics to treat MM in both initial therapy or maintenance therapy post autologous hematopoietic stem cell transplantation (ASCT). We previously discovered that caffeic acid phenethyl ester (CAPE), a water-insoluble natural compound, inhibited the growth of MM cells by inducing oxidative stress. As part of our continuous effort to pursue a less toxic yet more effective therapeutic approach for MM, the objective of this study is to investigate the potential of CAPE for in vivo applications by using magnetic resonance imaging (MRI)-capable superparamagnetic iron oxide nanoparticles (IONP) as carriers. Cyclo (Arg-Gly-Asp-D-Phe-Cys) (RGD) is conjugated to IONP (RGD-IONP/CAPE) to target the overexpressed αvβ3 integrin on MMcells for receptor-mediated internalization and intracellular delivery of CAPE. A stable loading of CAPE on IONP can be achieved with a loading efficiency of 48.7% ± 3.3% (wt%). The drug-release studies indicate RGD-IONP/CAPE is stable at physiological (pH 7.4) and basic pH (pH 9.5) and subject to release of CAPE at acidic pH (pH 5.5) mimicking the tumor and lysosomal condition. RGD-IONP/CAPE causes cytotoxicity specific to human MM RPMI8226, U266, and NCI-H929 cells, but not to normal peripheral blood mononuclear cells (PBMCs), with IC50s of 7.97 ± 1.39, 16.75 ± 1.62, and 24.38 ± 1.71μM after 72-h treatment, respectively. Apoptosis assays indicate RGD-IONP/CAPE induces apoptosis of RPMI8226 cells through a caspase-9 mediated intrinsic pathway, the same as applying CAPE alone. The apoptogenic effect of RGD-IONP/CAPE was also confirmed on the RPMI8226 cells co-cultured with human bone marrow stromal cells HS-5 in a Transwell model to mimic the MM microenvironment in the bone marrow. In conclusion, we demonstrate that water-insoluble CAPE can be loaded to RGD-IONP to greatly improve the biocompatibility and significantly inhibit the growth of MMcells in vitro through the induction of apoptosis. This study paves the way for investigating the MRI-trackable delivery of CAPE for MM treatment in animal models in the future.

Polyphenolic profile and in vitro biological activity of Serbian orange (skin fermented white) wines

Orange wines are made from white grapes, but with prolonged skin contact during fermentation. Available data on their composition and potential health benefits are limited, so polyphenolic profile (HPLC analysis) and in vitro biological activities (enzyme inhibition, antioxidant, and anti-inflammatory) of 24 Serbian orange wines were analyzed, including the correlation between determined composition and bioactivities. The wines displayed distinct polyphenolic profiles, enabling partial differentiation based on overall polyphenol content, including dominant components (catechin, gallic and caffeic acids), along with occasional occurrences of anthocyanins. However, no discernible distinctions were noted based on grape varieties, vintage, or producer. All twenty-four orange wines showed a reasonable inhibition of digestive enzymes and lipid peroxidation, twenty-one samples reduced ROS generation in the cell-based assay, but only two suppressed both PGE2 and TXA2 production in U937 cells, implicating possible functional food properties. No significant correlation between polyphenolic profile and determined biological activities was noticed.

Nanopore analysis of salvianolic acids in herbal medicines

Natural herbs, which contain pharmacologically active compounds, have been used historically as medicines. Conventionally, the analysis of chemical components in herbal medicines requires time-consuming sample separation and state-of-the-art analytical instruments. Nanopore, a versatile single molecule sensor, might be suitable to identify bioactive compounds in natural herbs. Here, a phenylboronic acid appended Mycobacterium smegmatis porin A (MspA) nanopore is used as a sensor for herbal medicines. A variety of bioactive compounds based on salvianolic acids, including caffeic acid, protocatechuic acid, protocatechualdehyde, salvianic acid A, rosmarinic acid, lithospermic acid, salvianolic acid A and salvianolic acid B are identified. Using a custom machine learning algorithm, analyte identification is performed with an accuracy of 99.0%. This sensing principle is further used with natural herbs such as Salvia miltiorrhiza, Rosemary and Prunella vulgaris. No complex sample separation or purification is required and the sensing device is highly portable.

Characterization of dried pineapple (Ananas comosus L.) peel powder and its application as a novel functional food ingredient in cracker product

The study utilized dried pineapple peel powder (PP) as a novel functional cracker ingredient. The PP comprised 3.94 % moisture, 2.53 % fat, 3.98 % ash, 4.20 % protein, 12.05 % crude fiber, and 73.30 % carbohydrate. PP also had total phenolic content (TPC) of 729.93 mg GAE/100 g DW, total flavonoid content (TFC) of 267.97 mg QE/100 g DW, and antioxidant capacities (AOC) of 2,364.08 mg Trolox/100 g DW and 1,365.14 mg FeSO4/100 g DW, as determined by DPPH and FRAP assays, respectively. According to HPLC analysis, catechin (29.85 μg/g), vanillic acid (21.63 μg/g), and sinapic acid (13.16 μg/g) were the three most significant phenolic compounds, followed by ferulic acid, rutin, caffeic acid, quercetin, gallic acid, and coumaric acid, respectively. The substitution of PP in crackers significantly increased ash, crude fiber, TPC, TFC, and AOC (p ≤ 0.05). The sensory attributes were accepted up to 10 % PP. HPLC analysis detected phenolic compounds in the 10 % PP crackers, namely vanillic acid (4.38 μg/g), ferulic acid (1.20 μg/g), sinapic acid (0.90 μg/g), and quercetin (0.24 μg/g). This study highlights the potential of utilizing PP in functional crackers, offering a sustainable solution for pineapple peel waste management.

Uncovering the Nephroprotective Mechanism of Caffeic Acid in Renal Tubulointerstitial Fibrosis through Network Pharmacology Analysis

Background: Renal tubulointerstitial fibrosis (RTF) is a progressive kidney condition characterized by the formation of fibrotic tissue. Caffeic acid (CA), a key component of the medicinal plant Antirhea borbonica, shows promise as a potential treatment for renal fibrosis. Here, we investigated the nephroprotective effect of CA in RTF and its underlying mechanisms. Methods: RTF was induced in rats through unilateral ureteral obstruction (UUO), followed by intraperitoneal administration of CA for 5 days. We assessed kidney weight/body weight (KW/BW) ratio, serum creatinine (Scr), blood urea nitrogen (BUN), 24-h urine protein (UP), and performed histological examinations. We also analyzed the expression of fibrosis-related proteins. Genes associated with RTF and CA were identified using public databases. A protein-protein interaction (PPI) network and molecular docking studies were conducted. Results: CA treatment significantly reduced the KW/BW ratio, levels of Scr, BUN, and 24-h UP, indicating improved kidney function in UUO-induced RTF rats. Histological examination revealed reduced fibrotic changes. CA administration also led to decreased collagen deposition and downregulation of fibrosis-related protein expression. CA administration also led to decreased collagen deposition and downregulation of fibrosis-related protein expression. The PPI network analysis showed significant differential expression of 13 genes between the fibrosis and normal groups. Notably, EGFR and MAPK14 were strongly associated with CA, and CA treatment downregulated EGFR and MAPK14 protein expression in UUO rats. Conclusion: CA exhibits substantial nephroprotective effects in UUO-induced RTF rats by modulating key genes EGFR and MAPK14, and MAPK signaling pathway.

Room temperature synthesis of β-cyclodextrin functionalized graphene oxide decorated MIL-100 (Fe): A sustainable drug cargo for anticancer drug delivery

Chemotherapy remains an extensively used cancer treatment method with the accessibility of various chemotherapeutic agents. However, its effectiveness is limited by the inability to distinguish between precipitously propagating normal cells and cancer cells, leading to severe side effects. Targeted drug delivery systems (DDS), utilizing advanced nanomaterials such as nanocarriers and natural/green chemotherapeutic agents like caffeic acid (CA), offer a promising solution to overcome these challenges and improve the sustainable consumption of chemotherapeutic agents. The current study presents a self-assembled, sustainable, and straightforward method for synthesizing CA nanocarriers using β-cyclodextrin conjugated graphene oxide (β-CD-GO)-functionalized Fe-based metal-organic frameworks ((β-CD-GO@MIL-100(Fe)), herein denoted as BGw-MF, through a hydrofluoric acid (HF)-free approach. The structural, functional, and morphological attributes of obtained nanocarriers were inspected through respective characterization methods. Furthermore, the CA loading efficiency (LE) was evaluated for the obtained BGw-MF nanocarriers with fixed drug concentrations, varied CA: nanocarrier ratio (w/w), and pH of the media. The results showed that BG0.5-MF had the highest LE, reaching 56.44 ± 2.25% for a 2 w/w ratio of CA in an alkaline environment (pH 9). Moreover, the CA release pattern of BG0.5-MF-CA was more controlled, with nearly 57.07 ± 2.01% release at pH 5 and 48.04 ± 1.44% at pH 7.4 over 8 days, which might enhance the therapeutic efficiency with higher release at tumor sites. The kinetics studies were subsequently conducted to evaluate the CA release characteristics of the BG0.5-MF nanocarrier. The nanocarrier followed a pseudo-second-order kinetic model for CA release at pH 5. In-vitro cytotoxicity tests of BG0.5-MF-CA revealed significant toxicity to lung cancer cells (A549) and cell viability of 68 ± 2 %, with no evident toxicity induced to normal cells (HEK293) at 400 μg/mL dose. The findings of the present work emphasized the potential of BGw-MF nanocarriers obtained at room temperature for CA-based anticancer DDS. The high loading capacity of the nanocarriers combined with the sustainable release of the drug from the nanocomposite makes it suitable for drug delivery. Moreover, the cytotoxicity of the nanocomposite towards cancer cells establishes BG0.5-MF as a promising nanocarrier for anticancer DDS.

Study the yield and quality of bitter gourd fruit (Momordica charantia) in inoculation with two species of mycorrhizal fungi and phosphorus fertilizer under different irrigation regimes

Drought is known to be the most important constraint to the growth and yield of agricultural products in the world, and plant symbiosis with arbuscular mycorrhizal fungi (AMF) can be a way to reduce drought stress negative impacts. A two-year experiment to investigate the factorial combination of mycorrhizal fungi (Glomus mosseae, Glomus intraradices, Control) and phosphorus fertilizer (application and non-application of phosphorus) on fruit yield and phenolic acids changes bitter gourd under different irrigation regimes as a split factorial based on a randomized complete block design. Three irrigation regimes, including irrigation after 20%, 50%, and 80% available soil water content depletion (ASWD), were considered in the main plots. The results showed that under water deficit stress, fruit yield and physiological (photosynthesis rate (Pn), transpiration rate (Tr), stomatal conductance (Gs), RWC, total chlorophyll, and root colonization) parameters decreased compared to 20% ASWD, and biochemical (proline, soluble sugar, MDA, CAT, SOD, phenol) parameters and fruit phenolic acids (caffeic acid, coumaric acid, ferulic acid) increased. However, the inoculation of AMF and phosphorus fertilizer in three irrigation regimes decreased MDA content, but physiological and biochemical parameters and fruit phenolic acids were increased. In this study, the factorial combination of AMF and sufficient phosphorus improved the resistance of bitter gourd to water deficit, and this not only improved fruit yield but also increased fruit phenolic acids under 80% ASWD, which can be an innovation in the management of water resources and the production industry of medicinal plants with high antioxidant properties in water deficit areas.

Intensification of extraction process through IVDV pretreatment from Eryngium creticum leaves and stems: Maximizing yields and assessing biological activities

“Intensification of Vaporization by Decompression to the Vacuum” (IVDV) has initially emerged as a technology primarily employed for expanding and enhancing the texture of biological products. However, its recent applications have showcased significant promise in the realm of extracting bioactive molecules from various plant materials. In this context, optimization using response surface methodology was conducted to investigate the impact of IVDV pretreatment on the extractability of phenolic compounds from Eryngium creticum leaves and stems, as well as their biological activities. Using IVDV preceding the extraction led to higher total phenolic content (TPC) and enhanced antiradical activities in treated materials compared to untreated ones. The optimal processing conditions in terms of water content, steam pressure and treatment time were determined in order to maximize TPC (89.07 and 20.06 mg GAE/g DM in leaves and stems, respectively) and antiradical (DPPH) inhibition percentage (93.51% and 27.54% in leaves and stems, respectively). IVDV-treated extracts showed superior antioxidant, antibacterial and antibiofilm capacities compared to raw extracts. Using RP-UHPLC-PDA-MS, caffeic acid and rosmarinic acid were identified in IVDV-treated leaves. IVDV can be implemented as an innovative treatment applied prior to extraction to boost the recovery of biomolecules from plant matrices.

Mentha Pulegium: A Plant with Several Medicinal Properties.

The species Mentha Pulegium L. (M. pulegium L.) belongs to the family Lamiaceae, native to Europe, North Africa, and the Middle East, and the genus Mentha. It has been traditionally used in food, cosmetics, and medicines. It is a perennial, fragrant, well-liked, herbaceous plant that can grow up to half a meter tall. It is extensively used as a food flavoring, particularly for Moroccan traditional drinks. Chewing mint and M. pulegium, a relaxing and refreshing plant, can be used to treat hiccups and act as an anticonvulsant and nerve relaxant. Pennyroyal leaves that have been crushed have a pungent, spearmint-like scent. Pennyroyal is used to make herbal teas, which, while not proven to be harmful to healthy adults in small doses, are not recommended due to their liver toxicity. Infants and children can die if they consume it. Pennyroyal leaves, both fresh and dried, are particularly effective at repelling insects. Pennyroyal essential oil should never be taken internally because it is highly toxic, even in small doses, it can be fatal. This plant is used in traditional Moroccan medicine to treat a wide range of conditions, including influenza, rheumatism, migraine, infertility, ulcer, pain, gastrointestinal problems, fever, diabetes, obesity, mental and cardiac disorders, constipation, respiratory ailments, and cough. M. pulegium is a great candidate for contemporary therapeutic usage since it contains a wide variety of biologically active compounds, including terpenoids, flavonoids, alkaloids, tannins, and saponins in all its parts. Among the different parts used are the whole plant, the aerial part, the stem, and the leaves. More interestingly, the entire plant contains a variety of compounds including Pulegone, Isomenthone, Carvone, Menthofuran, Menthol, 1,8-Cineole, Piperitone, Piperitenone, Neomenthol, -humulene, and 3-octanol. Eriocitrin, Hesperidin, Narirutin, Luteolin, Isorhoifolin, Galic acid, and Rosmarinic acid are found in the leaves. p-hydroxybenzoic acid, Ferulic acid, Caffeic acid, Vanillic acid, Syringic acid, Protocatechuic acid, Cinnamic acid, Phloretic acid, o-coumaric acid, p-coumaric acid, Catechin, Epicatechin, Chrysin, Quercetin, Naringenin, Carvacrol are all found in the areal part. Alterporriol G, Atropisomer, Alterporriol H, Altersolanol K, Altersolanol L, Stemphypyrone, 6-O-methylalaternin, Macrosporin, Altersolanol A, Alterporriol E, Alterporriol D, Alterporriol A, Alterporriol B, and Altersolanol J are also found in the stem of fungus. Pulegone, Piperitone, p-Menthane-1,2,3- triol, β-elemenene, guanine (cis-), Carvacrol acetate, and Phenyl ethyl alcohol are all components of this plant's essential oils. Moreover, the study also sought to investigate and document all currently available evidence and information on the nutritional composition and therapeutic uses of this plant ornamental. Its pharmacological applications include antimicrobial, antioxidant, antihypertensive, antidiabetic, anti-inflammatory, antiproliferative, antifungal, anticancer, burn wound healing, antispasmodic, and hepatotoxicity. Finally, toxicological studies have revealed that while low doses of extracts of the plant M. pulegium are not toxic, however, its essential oils of it are extremely toxic. In order to evaluate future research needs and investigate its pharmacological applications through clinical trials, the current assessment focuses on the distribution, chemical composition, biological activities, and primary uses of the plant.

FAST MICROWAVE ASSISTED FUNCTIONALIZATION OF CARBON NANOFIBERS: A PROMISING ELECTROCHEMICAL SENSING PLATFORM FOR ELECTROACTIVE ANALYTES

This research introduces a novel approach for swiftly enhancing the electrochemical sensing capabilities of commercial screen-printed carbon electrodes through a rapid acid microwave-assisted functionalization of carbon nanofibers (f-CNFMW). A comparative analysis with the conventional refluxed system functionalization method (f-CNFRefluxed) was conducted to assess the electrochemical performance of the newly developed f-CNFMW. The voltametric study showed that f-CNF-MW significantly enhanced the electron transfer rate when testing common phenolic compounds such as hydroquinone, paracetamol, and caffeic acid. Moreover, the anodic oxidation potential for the majority of irreversible analytes was negatively shifted, indicating the high electro-catalytic activity of f-CNF-MW gained after this treatment, making it analytically useful for the electro-oxidation of some molecules that require high overpotential, mainly for purine bases and nitrite. Additionally, the developed f-CNF-MW exhibited remarkable resistance to fouling phenomena when exposed to bisphenol A and tryptophan, underscoring its potential for real-world applications. To sum up, this study highlights the potential of rapid microwave treatment in producing f-CNF-MW as a promising electrochemical nanomaterial, resulting in substantial improvements in electro-analytical capabilities compared to conventional methodologies.

Antioxidant Mechanism of Black Garlic Based on Network Pharmacology and Molecular Docking

Black garlic possesses antioxidant effects, however, its specific antioxidant mechanism remains elusive. The present study investigates the antioxidant mechanism of black garlic using network pharmacology and molecular docking techniques. By reviewing literature and collecting the Traditional Chinese Medicine Systems Pharmacology Database and Analysis Platform database, a total of 67 black garlic active ingredients and 583 potential target proteins were obtained. Taking the intersection with oxidative stress targets resulted in 357 intersection targets. After network pharmacology analysis, the core active ingredients apigenin, ferulic acid, palmitic acid, quercetin and caffeic acid were identified. The core targets are KIT, KDR and ERBB2. The core pathway is the PI3K/Akt pathway. Molecular docking results showed that KIT and ERBB2 have relatively high docking scores, and all three targets have the best binding effects with quercetin, indicating that active ingredients in black garlic such as quercetin may mainly act on targets like KIT, KDR and ERBB2 to exert antioxidant effects. Collectively, the study indicates that black garlic have good antioxidant effects at a theoretical level, providing theoretical basis for the development of functional products of black garlic.

Biotransformation of bitter gourd (Momordica charantia) by Lactobacillus plantarum and its bioactivities

Bitter gourd is renowned for its various bioactivities, including antioxidant, antiglycation, and antiplatelet aggregation. However, the bioactivity and bioavailability of plant extracts could be low. Biotransformation through Lactobacillus plantarum fermentation is capable of enhancing these beneficial properties. Therefore, the present work aimed to investigate the physical and pH profiles, total phytochemical contents, bioactive contents, and bioactivities of the juices of unfermented bitter gourd (UBG) and fermented bitter gourd at 48 (FBG-48) and 96 (FBG-96) h. Fermentation gradually altered the physical and pH profile of bitter gourd, while non-significant decrease was seen in the total flavonoid content (p > 0.05). The highest total phenolic content was observed in FBG-48, followed by UBG and FBG-96. UBG exhibited the highest total triterpenoid content, followed by FBG-48 and FBG-96. Interestingly, fermentation increased the antioxidant, antiglycation, and anti-aggregation activities of bitter gourd. FBG-48 demonstrated the highest antioxidant and antiglycation activities, with 10.77 and 8.68% higher activity, respectively, compared to UBG and FBG-96. Meanwhile, FBG-96 exhibited the highest antiglycation activity, with 60% increase. These could have been attributed to the biotransformation of tannic acid into syringic acid, and momordicoside Q into kuguacin P, along with the potential release of p-coumaric acid and caffeic acid from the cell walls. These findings demonstrated bitter gourd’s promising role in type-II diabetes complication treatment, particularly through its protein aggregation inhibition activity, and that fermentation could increase its bioactivities.

Comparison of in vivo pharmacokinetics of twelve constituents in Qihe Fenqing Yin in normal rats and diabetic rats

This paper aims to study the pharmacokinetic differences of twelve effective constituents(succinic acid, neochlorogenic acid, chlorogenic acid, cryptochlorogenic acid, protocatechuic aldehyde, caffeic acid, 5-O-ferulogeninic acid, p-coumaric acid, nuciferine, quercetin, oleanolic acid, and ursolic acid) in Qihe Fenqing Yin in normal and diabetic rats. The diabetic rat model was established by a high-fat diet combined with intraperitoneal injection of streptozocin. A UHPLC-QTRAP-MS/MS method was established for the simultaneous determination of 12 constituents in the plasma of normal rats and model rats after a single intragastric administration of Qihe Fenqing Yin. The results show that the established analytical method has a good linear relationship with the 12 components, and the specificity, accuracy, precision, and stability meet the requirements. The computational pharmacokinetic parameters are fitted by DAS 3.2.8 software, and the results show that the half-life time(t_(1/2)) of the other nine components in the model group was longer than that in the normal group except for caffeic acid, 5-O-ferulogeninic acid, and oleanolic acid. The area under curve(AUC_(0-t)) of cryptochlorogenic acid, p-coumaric acid, ursolic acid, and oleanolic acid increases compared with the normal group. Meanwhile, mean residence time(MRT) delays. The "double peaks" of quercetin and nuciferine in the normal group are not observed in the model group, suggesting that the pharmacokinetic parameters of the drugs in the disease state are significantly different.

Identification of polyphenols by UPLC-MS/MS and their potential in silico antiviral activity from medicinal plants in Trujillo, Peru

Context: Given the growing public health crisis caused by viral diseases, traditional medicine stands as one of the fundamental pillars for the study and discovery of phytometabolites with antiviral properties. It is necessary to investigate and evaluate these compounds, mostly phenolic, that could be used as drugs. Aims: To identify the polyphenols by UPLC-MS/MS and the potential in silico antiviral activity of medicinal plants in Trujillo, Peru. Methods: The ethnobotany of the eight most widely used medicinal plants in the city of Trujillo was described (Azadirachta indica A. Juss. “paradise”, Caesalpinia spinosa (Molina) Kuntze “tara”, Citrus limon (L.) Osbeck “lemon”, Clinopodium pulchellum (Kunth) Govaerts "panizara", Cordia lutea Lam. "overo", Ocimum basilicum L. "basil", Schinus molle L. "molle", and Taraxacum campylodes G.E. Haglund "dandelion"). The phytometabolites responsible for the antiviral activity were identified by LC-MS and evaluated in silico against the viral proteins NS2B/NS3 (DENV-2), NS5B (HCV), and ICP27 (HSV-1) by molecular docking using Chimera 1.16 software and molecular interaction by Maestro 13.1 software to identify the position and type of interaction. Results: Five polyphenols (chlorogenic acid, gallic acid, caffeic acid, rosmarinic acid, and rutin) were found, and in the in-silico test, the antiviral activity of chlorogenic acid stood out against DENV-2 and HCV, rutin against HCV and HSV-1, rosmarinic acid against DENV-2 and HCV. Conclusions: It is demonstrated that the medicinal plants studied contain phytometabolites that make them possible antiviral candidates, which would support their use in the traditional medicine of the province of Trujillo, Peru.

Anti-diabetic Potentials of Coffee Polyphenols: A Narrative Review

Abstract: Coffee is one of the most popular beverages in the world, with potential health benefits and anti-diabetic qualities. Numerous bioactive substances found in coffee have been studied for their possible therapeutic benefits in controlling blood glucose. Given the ubiquitous use of coffee, this article aims to review the anti-diabetic characteristics of various coffee bioactive compounds such as chlorogenic acids, caffeic acid, quinic acid, ferulic acid, and caffeine. The modulation of glucose homeostasis, improvement of insulin sensitivity, suppression of gluconeogenesis, anti-inflammatory properties, and antioxidant activity are only a few of the several mechanisms of action that have been suggested. These qualities allow coffee polyphenols to potentially have anti-- diabetic effects, opening the door to prospective medicinal uses. The molecular mechanisms underpinning the effects of coffee polyphenols on insulin signaling pathways and glucose metabolism have been clarified by in vitro investigations. In animal studies, coffee polyphenols have positively affected pancreatic function, insulin resistance, and glucose regulation. Human studies have linked drinking coffee to a lower incidence of type 2 diabetes, better glycaemic management, and increased insulin sensitivity.

A Promising Functional Food for Diabetes Prevention, Antioxidation, and Anti-inflammation of Green Coffee Bean Extract

Functional foods and nutrition have become increasingly popular in preventing and reducing the incidence of diabetes. Green coffee bean extract (GCBE) has received much interest because of the evidence that coffee consumption reduces the risk of diabetes and many inflammatory diseases. This study was designed to investigate the phytochemicals contained in GCBE and their antioxidant, anti-diabetic, and anti-inflammatory efficacies. GCBE phytochemicals were analyzed using high-performance liquid chromatography (HPLC). This analysis demonstrated that chlorogenic acid was the predominant component of GCBE, followed by caffeine and caffeic acid. The antioxidant capacity of GCBE was assessed using the 1,1-diphenyl-2-picrylhydrazyl (DPPH) and 2,2’-azinobis 3-ethylbenzothiazoline-6-sulfonic acid (ABTS) assays, demonstrating significant scavenging capacity with IC50 values of 2.96 ± 1.04 and 7.63 ± 1.03 µg/mL, respectively. The anti-hyperlipidemic efficacy of GCBE was observed through inhibiting cholesterol absorption (by increasing micelle sizes and decreasing cholesterol solubility), lipid digestion, and pancreatic lipase activity in vitro. The investigations revealed that GCBE possessed anti-hyperlipidemic properties by inhibiting cholesterol absorption, lipid digestion, and pancreatic lipase activity. Specifically, GCBE increased micelle particle sizes by ~6.5-fold, decreased cholesterol solubility by 2-fold, and reduced pancreatic lipase activity by 25%. Additionally, the in vitroanti-hyperglycemic activity of GCBE was evaluated by inhibition of α-amylase and α-glucosidase capacity. GCBE demonstrated anti-hyperglycemic activity by inhibiting α-amylase activity (32.80 ± 7.06% inhibition), while α-glucosidase activity remained unaffected. The anti-inflammatory potential of GCBE was evaluated by mRNA regulation using RT-PCR analysis. This analysis revealed that GCBE attenuated mRNA expression of COX-2, TNF-α, IL-1b, and IL-6 in LPS-induced RAW264.7 cells. GCBE’s antioxidant, anti-hyperlipidemic, and anti-hyperglycemic efficacies and its molecular mechanisms in modulating the inflammation pathway found in the present study highlight its potential as a supplement in functional foods or beverages. Doi: 10.28991/HEF-2024-05-01-08 Full Text: PDF

Process optimization, multi-gene genetic programming modeling and reliability assessment of bioactive extracts recovery from Phyllantus emblica

This study investigates the feasibility of extracting bioactive antioxidants from Phyllantus emblica leaves using a combination of ethanol-water mixture (0-100%) and heat-assisted extraction technology (HAE-T). Operating temperature (30-50°C), solid-to-liquid ratio (1:20-1:60 g/mL), and extraction time (45-180 min) were varied to determine their effects on extract total phenolic content (TPC), yield (EY), and antioxidant activity (AA). The Box-Behnken experimental design (BBD) within response surface methodology (RSM) was employed, with multi-objective process optimization using the desirability function algorithm to find the optimal process variables for maximizing TPC, EY, and AA simultaneously. The extraction process was modeled using BBD-RSM and multi-gene genetic programming (MGGP) algorithm, with model reliability assessed via Monte Carlo simulation. HPLC characterization identified betulinic acid, gallic acid, chlorogenic acid, caffeic acid, ellagic acid, and ferulic acid as bioactive constituents in the extract. The study found that a 50% ethanol solution yielded the best extraction efficiency. The optimal process parameters for maximum EY (21.6565%), TPC (67.116 mg GAE/g), and AA (3.68583 µM AAE/g) were determined as OT of 41.61°C, S:L of 1:60 g/mL, and ET of 180 min. Both BBD-RSM and MGGP-based models satisfactorily predicted the observed process responses, with BBD-RSM models showing slightly better performance. Reliability analysis indicated high certainty in the predictions, with BBD-RSM models achieving 99.985% certainty for TPC, 97.569% for EY, and 98.661% for AA values.

Biological Evaluation of Isolated Flavonoids from Cymbopogon citratus on the Absorption of Lipids in Rabbits Infected with Giardiasis

The study involves isolation of flavonoids from Cymbopogon citratus, which included (Gallic acid, Chlorogenic, Caffeic acid, Ferulic acid, Myricetin, Tran-cinnamic acid, Kaempferol, Citral, Luteolin-7-O-neohesperidoside, Cassiaoccidentalin B, Carlinoside, Isoorientin, and Cynoaroside), and assessment of their therapeutic impact on lipid absorption in rabbits with Giardiasis. Twenty adult male rabbits were divided into four groups: Negative control (C-) received only drinking water, Positive control (C+) was orally treated with parasite cysts to induce Giardiasis, Group 1 (G1) received 30 mg/kg/day of metronidazole after inducing Giardiasis, and Group 2 (G2) received 100 mg/Kg/day of isolated flavonoids post Giardiasis induction. The results revealed varying concentrations of active flavonoids in the isolated extract, with a lower treatment response observed in G2 compared to metronidazole treatment in G1. Biochemically, microsomal triglyceride transfer protein levels significantly decreased in C+ and G1 compared to C- but returned to normal after flavonoid treatment in G2. Triglycerides levels decreased significantly in the C+ group and returned to normal post-treatment, while total cholesterol and high density lipoprotein levels remained unchanged in the C+ group. Serum cholesterol was unaffected by the infection in G+ and G2 but significantly increased in G1. Total antioxidant capacity and malodialdhyde levels significantly increased in the positive group but returned to normal after treatment in G1 and G2.. KEYWORDS :Cymbopogon citrates, Giardia lamblia, Lipid profile, Microsomal triglyceride transfer protein.

Caffeic acid-grafted chitooligosaccharides downregulate MAPK and NF-kB in RAW264.7 cells.

Chitooligosaccharide (COS) is a derivative of chitosan, which is a natural macromolecular compound. COS has been shown effects in an inflammatory response. Recent reports show that COS derivatives have enhanced anti-inflammatory activity by inhibiting intracellular signals. Evaluation of the anti-inflammatory effect of caffeic acid conjugated COS chain (CA-COS) was performed in this study. The effects of CA-COS on the inflammatory response were demonstrated in lipopolysaccharide-stimulated RAW264.7 macrophages. The results showed that CA-COS inhibited nitric oxide (NO) production and downregulated the gene expression of nitric oxide synthase (iNOS), and cytokines such as tumor necrosis factor-alpha (TNF-α), IL-1β, and IL-6 without cytotoxic effect. In addition, western blot analysis showed that CA-COS inhibits the protein expression of iNOS and nuclear factor kappa B (NF-kB), including p50 and p65, and mitogen-activated protein kinase (MAPK) signaling pathways. Collectively, these results provide clear evidence for the anti-inflammatory mechanism of CA-COS that show great potential as a novel agent for the prevention and therapy of inflammatory diseases.

Green synthesis and characterization of silver nanoparticles from Ducrosia flabellifolia Boiss. aqueous extract: Anti-quorum sensing screening and antimicrobial activities against ESKAPE pathogens.

Biosynthesis of silver nanoparticles using natural compounds derived from plant kingdom is currently used as safe and low-cost technique for nanoparticles synthesis with important abilities to inhibit multidrug resistant microorganisms (MDR). ESKAPE pathogens, especially MDR ones, are widely spread in hospital and intensive care units. In the present study, AgNPs using Ducrosia flabellifolia aqueous extract were synthesized using a reduction method. The green synthesized D. flabellifolia-AgNPs were characterized by UV-Vis spectrophotometer, Scanning electron microscopy (SEM), and X-ray diffraction assays. The tested D. flabellifolia aqueous extract was tested for its chemical composition using Liquid Chromatography-Electrospray Ionization-Mass Spectrometry (LC-ESI-MS). Anti-quorum sensing and anti-ESKAPE potential of D. flabellifolia-AgNPs was also performed. Results from LC-ESI-MS technique revealed the identification of chlorogenic acid, protocatechuic acid, ferulic acid, caffeic acid, 2,5-dihydroxybenzoic acid, and gallic acid as main phytoconstituents. Indeed, the characterization of newly synthetized D. flabellifolia-AgNPs revealed spherical shape with mean particle size about 16.961±2.914 nm. Bio-reduction of silver was confirmed by the maximum surface plasmon resonance of D. flabellifolia-AgNPs at 430 nm. Newly synthetized D. flabellifolia-AgNPs were found to possess important anti-ESKAPE activity with low minimal inhibitory concentrations (MICs) ranging from 0.078 to 0.312 mg/mL, and low minimal bactericidal concentrations (MBCs) varying from 0.312 to 0.625 mg/mL. Moreover, D. flabellifolia-AgNPs were active against Candida utilis ATCC 9255, C. tropicalis ATCC 1362, and C. albicans ATCC 20402 with high mean diameter of growth inhibition at 5 mg/mL, low MICs, and minimal fungicidal concentrations values (MFCs). The newly synthetized D. flabellifolia-AgNPs were able to inhibit violacein production in Chromobacterium violaceum, pyocyanin in Pseudomonas aeruginosa starter strains. Hence, the newly synthesized silver nanoparticles using D. flabellifolia aqueous extract can be used as an effective alternative to combat ESKAPE microorganisms. These silver nanoparticles can attenuate virulence of Gram-negative bacteria by interfering with the quorum sensing system and inhibiting cell-to-cell communication.