Astragalin Research Articles

Astragalin inhibits neuronal excitability and activates neuronal autophagy in the ACC and LH of CFA mice to alleviate inflammatory pain and pain-related emotions.

Astragalin (AST), a natural flavonoid, exhibits anti-inflammatory, anti-cancer, and antioxidant properties. However, its effects and molecular mechanisms in inflammatory pain remain unclear. Therefore, this study aims to investigate the impact of AST on a Complete Freund's Adjuvant (CFA)-induced inflammatory pain mouse model and to elucidate its potential mechanisms. We employed behavioral tests, including the paw withdrawal test (PWT) and open field test (OFT), to assess pain thresholds and emotional changes in mice, while ELISA was utilized to measure the expression of inflammatory factors. Western blot analysis was performed to evaluate the expression of autophagy-related proteins, c-Fos, and pathway-related proteins. Additionally, immunofluorescence staining was conducted to assess the co-localization of neurons with autophagy-related factors and c-Fos. Our findings indicate that AST significantly reduces pain sensitivity and anxiety-like behaviors in CFA mice, similar to the analgesic Naproxen (NAP). AST treatment inhibited the expression of c-Fos, a neuronal excitability marker, in the ACC and LH of CFA mice, while upregulating the expression of autophagy-related proteins. Furthermore,AST modulates the expression of proteins associated with the CXCR4-Beclin1/VPS34 signaling pathway. In conclusion, these results suggest that AST inhibits neuronal excitability and enhances autophagy by modulating the CXCR4-Beclin1/VPS34 signaling pathway in the ACC and LH of CFA mice, leading to a reduction in pain sensitivity and anxiety-like behaviors, thereby producing analgesic effects. This study reveals a novel mechanism for the potential use of AST in the treatment of inflammatory pain and pain-related emotions, offering a promising strategy for clinical applications.

Prevention of inflammation and oxidative stress by new ingredients based on high (poly)phenols winery by‐products

AbstractBackgroundNew circular economy policies for producing high‐value ingredients and co‐products, rich in bioactive phytochemicals, have boosted valorising agro‐food residues, as sources of powerful functional compounds. In this context, (poly)phenols of winemaking by‐products have been associated with anti‐inflammatory and oxidative stress (OS) prevention. Nevertheless, this application needs stabilisation of such materials by fine‐tuning processing conditions, in a fashion compatible with the industrial capacities, to minimise the impact on the phytochemical profile. To fill these gaps, the present study uncovered the capacity of high (poly)phenol ingredients from winery by‐products (obtained by an oven a dehydration system), to modulate inflammatory and OS markers and mediators associated with intestinal inflammation.ResultsThe results confirmed minimal changes in the winery residues' (poly)phenolic burden. The ingredients obtained provided (poly)phenolic pools that reduced the secretion of inflammatory markers, namely nitrates/nitrites, IL‐6, IL‐8 and TNF‐α by up to 66.8%, 20.1%, 95.4% and 78.3%, respectively. Even more, they also prevented ROS increase, preserving the molecular machinery of cells against OS (glutathione, catalase, superoxide dismutase and glutathione peroxidase) in a significant manner. The correlation analyses allowed identifying proanthocyanidin dimer (B‐type) digallate, galloyl hexoside, ferulic acid hexoside, cyanidin 3‐O‐p‐coumaroylglucoside, as the main anti‐inflammatory compounds; and galloyl hexoside, ferulic acid hexoside, kaempferol glucoside and cyanidin 3‐O‐p‐coumaroylglucoside, as the most powerful antioxidant molecules.ConclusionThese results support the interest in winery by‐products processed according to industrial procedures as sources of compounds with anti‐inflammatory and OS prevention traits.

Optimization of UAE-NADES green extraction of bioactive compounds from chickpea (Cicer arietinum L.) sprouts using simplex lattice mixture design methodology

In the present study, a statistical tool called the simplex lattice mixture design method was used to create a new formulation of Natural Deep Eutectic Solvent (NADES) which is derived from a combination of three compounds (citric acid, glycerol, and water) to extract bioactive compounds from chickpea (Cicer arietinum L.) sprouts. The mixture (natural deep eutectic solvent) was formulated by combining three solvents including citric acid, glycerol, and water. The extraction was performed in a sonication bath for 30 min. The simultaneous optimization was performed to obtain the highest total polyphenol content (TPC), total flavonoid content (TFC) and antioxidants activity. The highest values of total polyphenol content (TPC), total flavonoid content (TFC) and antioxidant activity were 128.0 ± 0.2 mg GAE/100 g, 38.61 ± 0.03 mg CE/100 g and 2117 ± 1.8 µmol TE/100 g respectively. HPLC-DAD of the optimized extract was utilized for quantification of polyphenol compounds showing catechin as the main compound followed by chlorogenic acid, epicatechin, syringic acid, rutin, gallic acid, kaempferol 3-glucoside, ferulic acid, and coumaric acid. These findings may represent a significant advancement in the management of phenolic compound extraction for targeted uses, such as serving as alternatives to traditional antioxidants primarily employed in the food industry to improve nutritional quality. Furthermore, our research has shown that mixture designs are an efficient and useful method for structuring and optimizing experimental parameters to achieve the most accurate results with the minimum number of experiments.

Insights into the wound-healing properties of medicinally important South African Bulbine species – A comparative study

Ethnopharmacological relevanceSouth Africa harbours a large number of Bulbine (Xanthorrhoeaceae) species, which includes ethnobotanically important indigenous species. Traditionally, Bulbine leaves are used by several ethnic groups in South Africa to treat dermatological conditions including wounds, which led to the development of Bulbine-containing cosmetic products. However, scientific evidence is needed to support the claims in treating skin conditions and wound-healing. Aim of the studyThis comparative study was undertaken to investigate the wound-healing properties of five Bulbine species indigenous to South Africa, using in vitro and in vivo models. Materials and methodsFive Bulbine species, B. abyssinica, B. asphodeloides, B. frutescens, B. latifolia and B. narcissifolia were collected from natural populations in the Eastern Cape Province of South Africa. The chemical profiles of the methanol leaf extracts were acquired using ultra-performance liquid chromatography with photodiode array detection in tandem with quadrupole time-of-flight mass spectrometry. The methyl thiazolyl tetrazolium (MTT) assay and maximum tolerated concentration (MTC) assay were used to assess the in vitro and in vivo toxicity of the extracts, respectively. The in vitro scratch assay was employed to monitor cell migration and wound-closure in a HaCaT cell monolayer, following treatment with the plant extracts for 48 h. In vivo wound-healing potential was determined using the zebrafish larvae caudal fin amputation assay, assessed in three-days post fertilization larvae and various concentrations of the plant extracts were tested in both assays to determine the concentration-response effect. Data were analysed using MS Excel® enhanced with the Real Statistics add-in. Results and discussionUsing UPLC-MS, 11 major compounds were tentatively identified in the five Bulbine species. Although the compounds varied between species, all five Bulbine species contained the phenylanthraquinone, knipholone. Kaempferol glucoside was identified in four species, but not in B. abyssinica. The five Bulbine species were non-cytotoxic (cell viability > 80%) towards keratinocytes at all three tested concentrations. However, B. latifolia was toxic towards zebrafish larvae at all the tested concentrations, while the other four species were non-toxic at low concentrations. The results of the scratch assay revealed that B. abyssinica was the most active extract at 100 μg/mL. Compared to the untreated control, wound-closure notably increased by 28% (p < 0.05), 44% (p < 0.01) and 34% (p < 0.05) after 12 h, 24 h and 36 h post-treatment, respectively. Although none of the species achieved 100% caudal fin regeneration by the end of the treatment period, B. frutescens demonstrated the highest regeneration (90%) and most significant difference (p < 0.01) compared to the untreated control. ConclusionThe results revealed that the five Bulbine species have complex chemical profiles, however, they share major compound classes (i.e. phenylanthroquinones and flavonoid analogues) across the species. The study highlights the wound-healing properties of the five species, which is consistent with their traditional use.

Dietary astragalin confers protection against lipopolysaccharide-induced intestinal mucosal barrier damage through mitigating inflammation and modulating intestinal microbiota.

The intestinal mucosal barrier (IMB) damage is intricately linked with the onset of numerous intestinal diseases. Astragalin (AS), a flavonoid present in numerous edible plants, exhibits notable antioxidant and anti-inflammatory properties, demonstrating a promising impact on certain intestinal ailments. In this study, our objective was to investigate the protective effects of AS and elucidate the underlying mechanisms by which it mitigates lipopolysaccharide (LPS)-induced damage to the IMB in mice. During the experimental period, mice were subjected to a 7-day regimen of AS treatment, followed by LPS injection to induce IMB damage. Subsequently, a comprehensive evaluation of relevant biological indicators was conducted, including intestinal pathological analysis, serum inflammatory factors, intestinal tight junction proteins, and intestinal microbiota composition. Our results suggested that AS treatment significantly bolstered IMB function. This was evidenced by the enhanced morphology of the small intestine and the elevated expression of tight junction proteins, including ZO-1 and Claudin-1, in addition to increased levels of MUC2 mucin. Moreover, the administration of AS demonstrated a mitigating effect on intestinal inflammation, as indicated by the reduced plasma concentrations of pro-inflammatory cytokines such as IL-6, IL-1β, and TNF-α. Furthermore, AS treatment exerted a positive influence on the composition of the gut microbiota, primarily by augmenting the relative abundance of beneficial bacteria (including Lachnospiracea and Lactobacillus murinus), while simultaneously reducing the prevalence of the harmful bacterium Mucispirillum schaedleri. AS mitigates LPS-induced IMB damage via mitigating inflammation and modulating intestinal microbiota.

Astragalin alleviates oligoasthenospermia via promoting nuclear translocation of Nrf2 and reducing ferroptosis of testis

Oligoasthenospermia (OAS) is a global human developmental disease and the most common type of male infertility. There are currently no sufficiently effective therapeutic strategies for OAS. Wuziyanzong Pill (WZYZP) is a traditional Chinese prescription for the clinical treatment of male infertility, and its efficacy is well known in China. Therefore, due to the complexity of traditional Chinese medicine, the specific mechanism of action of WZYZP on OAS has not been elucidated. Astragalin (AG), one of the main active substances in WZYZP, has good antioxidant effect. The aim of this research is to investigate whether AG, the active substance in WZYZP, can treat OAS by promoting Nrf2 nuclear translocation and inhibiting ferroptosis. The OAS model was established by intraperitoneal injection of cyclophosphamide, and the therapeutic effects of AG and WZYZP on OAS were evaluated by detecting sperm quality, sex hormone levels and testicular pathological changes after intragastric administration of AG and WZYZP. Western blot was used to measure the expression levels of TFR1, SLC7A11, GPX4 and FTH1. The nuclear translocation of Nrf2 was detected by immunofluorescence staining and nuclear/intracellular expression of Nrf2. The results showed that AG could improve sperm quality and serum sex hormone levels in OAS rats, reduce the expression of testicular Fe2+ and TFR1, up-regulate testicular SLC7A11, GPX4 and FTH1, and inhibit testicular ferroptosis. At the same time, AG can promote the expression and nuclear translocation of Nrf2 in the testis of OAS rats. AG can alleviate OAS via promoting nuclear translocation of Nrf2 and inhibiting ferroptosis of testis.

An Overview of Pharmacological Profile of Flavonoids as Potential Molecules of Therapeutic Importance

Abstract: A growing number of research investigations have shown the multiple health benefits of flavonoids derived from plants, leading to interest in the field. Many recent studies have concentrated on flavonoids effects on human health. Flavonoids are effective against a wide spectrum of bacteria, viruses, and other pathogens. Numerous flavonoids have been demonstrated to possess antioxidative, free radical scavenging, hepatoprotective, antiinflammatory, anticancer, and coronary heart disease preventive properties. Some of novel flavonoids having therapeutic potential as new medication have been identified which include hesperetin-5′-O-β-rhamnoglucoside, Resveratrol, Astragalin (AST) Desmodinosides A-E: New Flavonoid C-glycosides, Apigenin, Luteolin, and Baicalein, rutin, hyperoside etc. Some recent developments including clinical trials of a few of the flavonoids discussed in the review provide a novel library of pharmacologically potential molecules which provides a paradigm for the treatment of several ailments such as SARS-CoV-2, Alzheimer's disease, diabetes, angina pectoris, Hepatitis C virus and Sickle cell disease (SCD) etc. The present review aims at updating recent flavonoid advancements for various pharmacological actions, from conventional therapeutic implications to upcoming clinical trials. We encourage researchers to focus on flavonoids for a variety of medicinal applications since the industrial acceptance of these compounds will determine the future growth of this field.

Study on pharmacokinetic and tissue distribution of hyperin, astragalin, kaempferol-3-O-β-D-glucuronide from rats with multiple administrations of Semen Cuscutae processed with salt solution with effect of treating recurrent spontaneous abortion.

Semen Cuscutae is a traditional Chinese medicine (TCM) that tonifies the kidneys and prevents miscarriage. According to Chinese medicine theory, kidney deficiency is one of the main causes of recurrent spontaneous abortion (RSA). The previous studies showed that raw product of Semen Cuscutae (SP) and Semen Cuscutae processed with salt solution (YP) have ameliorative effects on RSA, and that YP is superior to SP. However, the active components of YP to ameliorate RSA remain unclear and require further studies. The objective of this study is to investigate the active components of YP in ameliorating RSA. First, a rat model of RSA was established using hydroxyurea in combination with mifepristone. Aqueous decoction of YP was given by gavage to rats. Second, pregnant rats were sampled on days 5, 7, 9, 10 and 12 during the modelling period. The content of Hyperin (HY), astragalin (AS) and kaempferol-3-O-β-D-glucuronide (KA) in blood and liver, heart, spleen, lung and kidney tissues were detected by liquid chromatography-mass spectrometry (LC-MS). The pharmacodynamic indicators including progesterone (P), chorionic gonadotropin β (β-HCG), estradiol (E2), tumor necrosis factor-α (TFN-α), interleukin 4 (IL-4), and tryptophan (TRP) were measured by enzyme-linked immunosorbent assay (ELISA) Pearson's correlation analysis and grey relational analysis were used to establish the relationship between the pharmacodynamic indexes and chemical constituents. The pharmacokinetic results showed that the area under curve (AUC) value of KA was the largest. The tissue distribution results showed that astragalin was widely distributed in liver, heart, spleen, lung and kidney in the RSA model rats, while HY was detected only in the uterus, and KA was detected only in the kidney. The pearson correlationl analysis showed that KA was significantly and positively correlated with the contents of E2, P, β-HCG and TRP. Both AS and HY were significantly negatively correlated with the content of TNF-α, respectively. This study reveals the pharmacokinetics and tissue distribution of KA, AS and HY in rats with RSA. It was elucidated that all three were involved in the regulation of progesterone levels and immune function. It initially revealed the mechanism of action of YP in enhancing the improvement of RSA, and it provided a theoretical basis for the quality assessment of YP.

Astragalin improves cognitive disorder in Alzheimer's disease: Based on network pharmacology and molecular docking simulation.

We investigate the mechanism of action of astragalin (AST) in the treatment of Alzheimer's disease (AD). Network pharmacology was conducted to analyze the relationships among AST, AD, and neuroinflammation, The APP/PS1 transgenic mice with AD were used in the experiments; to be specific, the influence of AST on the behavior of mice was analyzed by Morris water maze and eight-arm radial maze tests, the tissue inflammatory factor levels were detected by ELISA, and pathological changes were analyzed by H&E and immunohistochemical staining. Analysis results of network pharmacology suggested that AST exerted the multi-target effect on neuroinflammation in AD. Through molecular docking and dynamics analyses, COX2 might be the target of AST. Moreover, animal experimental results demonstrated that AST improved the behavior of AD mice, and enhanced the motor and memory abilities, meanwhile, it suppressed the expression of inflammatory factors in tissues and the activation of microglial cells. this study discovers that AST can suppress microglial cell activation via COX2 to improve neuroinflammation in AD.

Exploring the Anticancer Potential of Astragalin in Triple Negative Breast Cancer Cells by Attenuating Glycolytic Pathway through AMPK/mTOR.

Aerobic glycolysis is crucial for cancer cells to survive, grow, and progress. In the current study, the anti-cancer effects of astragalin (ASG) on breast cancer cells and in the glycolytic pathway through AMPK/mTOR have been evaluated. The objective of this study was to examine the impact of ASG, a natural flavonoid, on glycolysis via targeting AMPK/mTOR signalling in MDA-MB-231 breast cancer cells. The study utilized ASG, which was isolated from Haplophyllum tuberculatum. The cells were treated with different concentrations of ASG (20 and 40 μg/mL), and anti- glycolytic activities were measured through cell proliferation, expression of glycolytic enzymes (HK-2, LDH-A, GLUT-1), glucose uptake, and lactate concentration assays. The MTT assay was used to assess cellular proliferation, while the glucose uptake and lactate levels were determined by employing colorimetric assays. The mRNA expression of target glycolytic enzymes was determined by qRT-PCR. The protein levels of glycolytic targets, as well as that of AMPK and mTOR, were determined by western blot. in silico docking of ASG was done with mTOR and AMPK proteins. Astragalin exhibited dose- and time-dependent anti-proliferative effects in MDA-MB-231 cells. In breast cancer cells, the mRNA and protein expression of GLUT-1, LDH-A, and HK-2 were all significantly downregulated after receiving ASG treatments. Furthermore, after ASG treatments, MDA-MB231 cells showed a significant decrease in lactate and glucose uptake compared to control cells. Mechanistically, ASG increased AMPK activation and suppressed mTOR activation in these cells. The inhibitory role of ASG on aerobic glycolysis was prevented by treatments with compound C (an AMPK inhibitor). However, combined treatment of compound C and ASG could nullify the ASG-induced anti-glycolysis effect and restore the level of p-AMPK and p-mTOR in MDA-MB231 cells. The results from molecular docking predicted that ASG had the potential to bind AMPK and mTOR, with free energy for binding, -8.2 kcal/mol and -8.1 kcal/mol, respectively. Taken together, the findings from this study indicated that ASG might modulate the AMPK/mTOR pathway to inhibit aerobic glycolysis and proliferation of MDAMB231 breast cancer.

Astragalin from Thesium chinense: A Novel Anti-Aging and Antioxidant Agent Targeting IGFR/CD38/Sirtuins.

Astragalin (AG), a typical flavonoid found in Thesium chinense Turcz (T. chinense), is abundant in various edible plants and possesses high nutritional value, as well as antioxidant and antibacterial effects. In this study, we initially predicted the mechanism of action of AG with two anti-aging and antioxidant-related protein targets (CD38 and IGFR) by molecular docking and molecular dynamics simulation techniques. Subsequently, we examined the anti-aging effects of AG in Caenorhabditis elegans (C. elegans), the antioxidant effects in zebrafish, and verified the related molecular mechanisms. In C. elegans, AG synergistically extended the lifespan of C. elegans by up-regulating the expression of daf-16 through inhibiting the expression of daf-2/IGFR and also activating the AMPK and MAPK pathways to up-regulate the expression of sir-2.1, sir-2.4, and skn-1. In oxidatively damaged zebrafish embryos, AG demonstrated a synergistic effect in augmenting the resistance of zebrafish embryos to oxidative stress by up-regulating the expression levels of SIRT1 and SIRT6 within the zebrafish embryos system via the suppression of CD38 enzymatic activity and then inhibiting the expression of IGFR through high levels of SIRT6. These findings highlight the antioxidant and anti-aging properties of AG and indicate its potential application as a supplementary ingredient in aquaculture for enhancing fish health and growth.

Separation of Non-alkaloid Toxin Lignans and New Flavonoid from Himalayan Mayapple (Podophyllum Hexandrum Royle) by High-Speed Counter-Current Chromatography and Their Anti-inflammatory Activity Evaluation

Podophyllum hexandrum Royle (Berberidaceae) is reported from the Himalayan region and China. It is also known as the Himalayan Mayapple and is reported for the treatment of constipation, fever, jaundice, liver disorders, etc. Herein, the isolation of chemical constituents using high-speed counter-current chromatography (HSCCC) from the EtOH extract of the rhizomes of Himalayan Mayapple is reported. As a result, kaempferol 3-glucoside (1), quercetin-3-O-β-D-glucopyranoside (2), quercetin 3-O-β-D-glucopyranosyl-(1→6)-3-O-ethyl-β-D-glucopyranoside (3), kaempferol 3- O-β-D-glucopyranoside (4), α-peltatin(5), podophyllotoxin (6), 4'-demethylpodophyllotoxin (7), 4',5'-didemethylpodophyllotoxin (8), and kaempferol (9)were separated. Compounds 6-9 were separated by the normal HSCCC while 1-5 were obtained by the offline-recycling HSCCC using HEMWat (1:9:4:6, v/v) solvent system. The pure components were tested in lipopolysaccharidesinduced mice macrophage cells. Compounds 6 and 7 showed significant inhibition. The nitric oxide production was inhibited by compounds 6 and 7, effectively, with IC50 values of 1.328 x 10-6 and 2.851 x 10-6 M, respectively. In this assay, kaempferol (9), a positive inhibitor expressively inhibited lipopolysaccharides-induced nitric oxide production.

Human Sensory, Taste Receptor, and Quantitation Studies on Kaempferol Glycosides Derived from Rapeseed/Canola Protein Isolates.

Beyond the key bitter compound kaempferol 3-O-(2‴-O-sinapoyl-β-d-sophoroside) previously described in the literature (1), eight further bitter and astringent-tasting kaempferol glucosides (2-9) have been identified in rapeseed protein isolates (Brassica napus L.). The bitterness and astringency of these taste-active substances have been described with taste threshold concentrations ranging from 3.3 to 531.7 and 0.3 to 66.4 μmol/L, respectively, as determined by human sensory experiments. In this study, the impact of 1 and kaempferol 3-O-β-d-glucopyranoside (8) on TAS2R-linked proton secretion by HGT-1 cells was analyzed by quantification of the intracellular proton index. mRNA levels of bitter receptors TAS2R3, 4, 5, 13, 30, 31, 39, 40, 43, 45, 46, 50 and TAS2R8 were increased after treatment with compounds 1 and 8. Using quantitative UHPLC-MS/MSMRM measurements, the concentrations of 1-9 were determined in rapeseed/canola seeds and their corresponding protein isolates. Depending on the sample material, compounds 1, 3, and 5-9 exceeded dose over threshold (DoT) factors above one for both bitterness and astringency in selected protein isolates. In addition, an increase in the key bitter compound 1 during industrial protein production (apart from enrichment) was observed, allowing the identification of the potential precursor of 1 to be kaempferol 3-O-(2‴-O-sinapoyl-β-d-sophoroside)-7-O-β-d-glucopyranoside (3). These results may contribute to the production of less bitter and astringent rapeseed protein isolates through the optimization of breeding and postharvest downstream processing.

Astragalin protects against lipopolysaccharide-triggered acute liver injury through suppression of necroptosis and inflammation and improvement of energy metabolism

Acute liver injury (ALI) is a prevalent clinical condition featured by liver inflammation and functional abnormalities resulting from various causes. Prolonged damage to liver cells can progress to chronic inflammation, fibrosis, and cirrhosis. Astragalin (AST), a natural flavonoid present in traditional medicinal and edible plants, exhibits anti-inflammatory and antioxidative properties, making it a potential therapeutic candidate for ALI. Using network pharmacology analysis, we explored the targets and pathways implicated in the regulation of AST against ALI. Our study using an ALI mouse model showed that AST effectively mitigates oxidative stress and inflammation induced by lipopolysaccharide (LPS), offering protection against LPS-induced ALI. The mechanism may involve inhibiting the tumor necrosis factor-α-driven necroptosis pathway and downregulating the hypoxia-inducible factor-1α/pyruvate kinase M2 signaling pathway, thereby suppressing enhanced glycolysis-mediated inflammatory response. Through the synergistic modulation of multiple targets and pathways, AST emerges as a promising therapeutic option for ALI, offering potential for clinical application.

Research Progress on Anti-Inflammatory Effects and Related Mechanisms of Astragalin.

Chronic inflammation is a significant contributor to the development of cancer, cardiovascular disease, diabetes, obesity, autoimmune disease, inflammatory bowel disease, and other illnesses. In the academic field, there is a constant demand for effective methods to alleviate inflammation. Astragalin (AST), a type of flavonoid glycoside that is the primary component in several widely used traditional Chinese anti-inflammatory medications in clinical practice, has garnered attention from numerous experts and scholars. This article focuses on the anti-inflammatory effects of AST and conducts research on relevant literature from 2003 to 2023. The findings indicate that AST demonstrates promising anti-inflammatory potential in various models of inflammatory diseases. Specifically, AST is believed to possess inhibitory effects on inflammation-related factors and protein levels in various in vitro cell models, such as macrophages, microglia, and epithelial cells. In vivo studies have shown that AST effectively alleviates neuroinflammation and brain damage while also exhibiting potential for treating moderate diseases such as depression and stroke; it also demonstrates significant anti-inflammatory effects on both large and small intestinal epithelial cells. Animal experiments have further demonstrated that AST exerts therapeutic effects on colitis mice. Molecular biology studies have revealed that AST regulates complex signaling networks, including NF-κB, MAPK, JAK/STAT pathways, etc. In conclusion, this review will provide insights and references for the development of AST as an anti-inflammatory agent as well as for related drug development.

Protective effect of kaempferol glucoside against lipopolysaccharide-caused acute lung injury via targeting Nrf2/NF-κB/NLRP3/GSDMD: Integrating experimental and computational studies

The current study explored the protective potential of kaempferol 3-sophoroside-7-glucoside (KSG) against acute lung injury (ALI). Pre-treatment with KSG effectively secured mice from ALI and showed similar efficaciousness to dexamethasone. KSG markedly increased the survival rate and alleviated lung pathological lesions induced by lipopolysaccharide (LPS). Furthermore, KSG attenuated differential and total cell counts in BALF (bronchoalveolar lavage fluid) and MPO (myeloperoxidase) activity. KSG counteracted the NF-κB (nuclear factor-κB) activation and significantly ameliorated the downstream inflammatory cytokine, TNF-α (tumor necrosis factor-α). Simultaneously, KSG suppressed the over-expression of NLRP3 (NOD-like receptor protein 3), caspase-1, and pro-inflammatory cytokine interleukin IL-1β (interleukine-1β) and prohibited the elevation of the pyroptotic parameter GSDMD-N (N-terminal domain of gasdermin D) induced by LPS challenge. In addition, KSG significantly enhanced Nrf2 (nuclear-factor erythroid-2-related factor) and HO-1 (heme-oxygenase-1) expression. Meanwhile, KSG mitigated lipid peroxidative markers (malondialdehyde, protein carbonyl and 4-hydroxynonenal) and boosted endogenous antioxidants (superoxide dismutase/reduced glutathione/catalase) in lung tissue. In silico analyses revealed that KSG disrupts Keap1-Nrf2 protein–protein interactions by binding to the KEAP1 domain, consequently activating Nrf2. Specifically, molecular docking demonstrated superior binding affinity of KSG to KEAP1 compared to the reference inhibitor, with docking scores of −9.576 and −6.633 Kcal/mol, respectively. Additionally, the MM-GBSA binding free energy of KSG (−67.25 Kcal/mol) surpassed that of the reference inhibitor (−56.36 Kcal/mol). Furthermore, MD simulation analysis revealed that the KSG-KEAP1 complex exhibits substantial and stable binding interactions with various amino acids over a duration of 100 ns. These findings showed the protective anti-inflammatory and anti-oxidative modulatory efficiencies of KSG that effectively counteracted LPS-induced ALI and encouraged future research and clinical applications of KSG as a protective strategy for ALI.

Lychee peel extract obtained by ultrasound-assisted extraction: bioactive compounds and functional properties

The purpose of this study was to evaluate the impact of extracting solvent composition on the concentration of bioactive compounds and functional properties of lychee peel extracts obtained by ultrasound-assisted extraction. Five conditions were evaluated with different solvent proportions: 100% water, 25% ethanol and 75% water, 50% ethanol and 50% water, 75% ethanol and 25% water, and 100% ethanol. The use of an equitable mixture of water and ethanol (50% ethanol and 50% water) resulted in extracts with a higher content of total phenolic compounds (10964.3 mg EAG 100 g-1), antioxidant activity (27.40%), and inhibition of α-glucosidase (94.31%), α-amylase (33.49%) and angiotensin-converting enzyme (ACE, 51.82%). This extract showed a diversity of phenolic compounds (quercetin 3-glucoside, procyanidin A2, B1, and B2, epicatechin, catechin, kaempferol 3-glucoside, trans-resveratrol, myricetin, and gallic acid). Therefore, extracts of lychee peel with potential anti-diabetic and anti-hypertensive activity can be obtained by ultrasound-assisted extraction. 50% water and 50% ethanol may be suggested as the extracting solvent.

Pulp or Peel? Comparative Analysis of the Phytochemical Content and Selected Cosmetic-Related Properties of Annona cherimola L., Diospyros kaki Thumb., Cydonia oblonga Mill. and Fortunella margarita Swingle Pulp and Peel Extracts.

Fruit peels might be a valuable source of active ingredients for cosmetics, leading to more sustainable usage of plant by-products. The aim of the study was to evaluate the phytochemical content and selected biological properties of hydroglycolic extracts from peels and pulps of Annona cherimola, Diospyros kaki, Cydonia oblonga, and Fortunella margarita as potential cosmetic ingredients. Peel and pulp extracts were compared for their antiradical activity (using DPPH and ABTS radical scavenging assays), skin-lightening potential (tyrosinase inhibitory assay), sun protection factor (SPF), and cytotoxicity toward human fibroblast, keratinocyte, and melanoma cell lines. The total content of polyphenols and/or flavonoids was significantly higher in peel than in pulp extracts, and the composition of particular active compounds was also markedly different. The HPLC-MS fingerprinting revealed the presence of catechin, epicatechin and rutoside in the peel of D. kaki, whereas kaempferol glucoside and procyanidin A were present only in the pulp. In A. cherimola, catechin, epicatechin and rutoside were identified only in the peel of the fruit, whereas procyanidins were traced only in the pulp extracts. Quercetin and luteolinidin were found to be characteristic compounds of F. margarita peel extract. Naringenin and hesperidin were found only in the pulp of F. margarita. The most significant compositional variety between the peel and pulp extracts was observed for C. oblonga: Peel extracts contained a higher number of active components (e.g., vicenin-2, kaempferol rutinoside, or kaempferol galactoside) than pulp extract. The radical scavenging potential of peel extracts was higher than of the pulp extracts. D. kaki and F. margarita peel and pulp extracts inhibited mushroom and murine tyrosinases at comparable levels. The C. oblonga pulp extract was a more potent mushroom tyrosinase inhibitor than the peel extract. Peel extract of A. cherimola inhibited mushroom tyrosinase but activated the murine enzyme. F. margarita pulp and peel extracts showed the highest in vitro SPF. A. cherimola, D. kaki, and F. margarita extracts were not cytotoxic for fibroblasts and keratinocytes up to a concentration of 2% (v/v) and the peel extracts were cytotoxic for A375 melanoma cells. To summarize, peel extracts from all analyzed fruit showed comparable or better cosmetic-related properties than pulp extracts and might be considered multifunctional active ingredients of skin lightening, anti-aging, and protective cosmetics.

The Phenolic Content of Pistacia lentiscus Leaf Extract and Its Antioxidant and Antidiabetic Properties.

The aims of this study were to determine the polyphenolic profile, to estimate the total phenolic and flavonoid contents, and to evaluate the antioxidant and antidiabetic activities of the extract of Pistacia lentiscus leaves, and the hydroacetonic mixture was employed as an alternative for common solvents in the extraction process. In order to explain the antidiabetic activity, molecular docking has been performed on the main constituents of the leaf extract. The characterization of the extract has been performed by high-performance liquid chromatography (HPLC) leading to the detection of 20 compounds of which gallic acid, ellagic acid, catechin, kaempferol, and quercetin 3-glucoside were identified using authentic standards. The total phenolic and flavonoid contents, assessed using the Folin-Ciocalteu and quercetin methods, were 394.5 ± 0.08 mg gallic acid equivalent/g dry extract (mg GAE/g DE) and 101.2 ± 0.095 mg quercetin equivalent/g dry extract (mg QE/g DE), respectively. On the other hand, the antioxidant activity of leaf extract, quantified by determining the ability to neutralize the free radical DPPH and β-carotene/linoleate model system, reached the values of 0.0027 ± 0.002 mg/mL and 0.128 ± 0.04 mg/mL, respectively. Regarding the antidiabetic activity, based on the inhibition of pancreatic α-amylase activity, a significant inhibition of about 68.20% with an IC50 value of 0.266 mg/mL had been observed. This finding is consistent with the molecular docking study of the main phenolic compounds of the extracts, where a remarkable binding affinity against α-amylase was observed, with values of -7.631 (kcal/mol), -6.818 (kcal/mol), and -5.517 (kcal/mol) for the major compounds catechin, quercetin-3-glucoside, and gallic acid, respectively.

Recovery of Bioactive Components from Strawberry Seeds Residues Post Oil Extraction and Their Cosmetic Potential

Recently, there has been an increased interest in the valorization of byproducts generated during fruit processing. An example of this is the waste produced during the processing of strawberries. For instance, it has been evidenced that strawberries seeds can be a valuable source of oil. The goal of this paper was to investigate the potential of strawberry seed residues after oil extraction (defatted seeds) as a source of phenolics with possible cosmetic applications. The components were recovered using water and ethanol mixture, assisted by heat, ultrasound, and microwave. The extracts were characterized through ultra-high performance liquid chromatography with spectrophotometric and mass detectors (UPLC-DAD-MS), and the biological properties of the phenolic-rich fraction were assessed using antioxidant tests and a cell viability assay on human skin fibroblasts. The study revealed that defatted strawberry seeds are rich in low molecular weight phenolics, specifically in tiliroside, kaempferol 3-glucoside, and ellagic acid. Furthermore, the phenolic-rich fraction was effective in scavenging free radicals in human skin fibroblasts and showed cytoprotective activity against oxidative stress. This evidence suggests that defatted strawberry seeds are a valuable material for further processing to obtain a beneficial additive for skincare products.