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Introduction: Helicobacter pylori infection is a major issue worldwide, with widespread prevalence, combined with its link to gastritis, peptic ulcers, gastric cancer, and mucosa-associated lymphoid tissue (MALT) lymphoma. Meanwhile, effectiveness of current treatment protocols is limited by increasing antibiotic resistance and patient compliance issues due to long regimens and side effects. Plukenetia volubilis , or sacha inchi, is a valuable source of bioactive molecules. However, studies on its antimicrobial activity, especially against H. pylori , are lacking. Methods: In this study, the anti- H. pylori activity of P. volubilis leaves water extract was explored using in vitro and in silico approaches. High-Performance Liquid Chromatography coupled to Electrospray Ionisation and Quadrupole Time-of-Flight Mass Spectrometry (HPLC-ESI- QTOF-MS-MS) analysis of the water extract from the leaves was used to characterise the chemical composition of the plant and allowed identification of some flavonoids, such as astragalin, and some phenolic compounds. Then, high-speed counter current chromatography (HSCCC) was used to fractionate the ethyl acetate partition obtained from the water extract from the leaves. Results and Discussion: The presence of flavonoids derived from kaempferol was confirmed and astragalin was isolated for the first time in P. volubilis. The P. volubilis water infusion, ethyl acetate extract and the isolated astragalin exhibited anti-bacterial activity against H. pylori J99 and two clinical isolates (e.g., minimum inhibitory concentrations of 0.53, 0.51 and 0.49 μg/mL, respectively, for clarithromycin-resistant clinical isolate SSR366). Then, using molecular docking for potential protein targets for H. pylori , it was verified that astragalin could interact with these proteins by in silico analysis. Conclusion: These findings highlight that P. volubilis and astragalin produce a bacteriostatic activity against H. pylori and may have potential to be used in treatment against H. pylori , after further research. [ABSTRACT FROM AUTHOR]

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. [ABSTRACT FROM AUTHOR]

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. [ABSTRACT FROM AUTHOR]

IntroductionHelicobacter pylori infection is a major issue worldwide, with widespread prevalence, combined with its link to gastritis, peptic ulcers, gastric cancer, and mucosa-associated lymphoid tissue (MALT) lymphoma. Meanwhile, effectiveness of current treatment protocols is limited by increasing antibiotic resistance and patient compliance issues due to long regimens and side effects. Plukenetia volubilis, or sacha inchi, is a valuable source of bioactive molecules. However, studies on its antimicrobial activity, especially against H. pylori, are lacking.MethodsIn this study, the anti-H. pylori activity of P. volubilis leaves water extract was explored using in vitro and in silico approaches. High-Performance Liquid Chromatography coupled to Electrospray Ionisation and Quadrupole Time-of-Flight Mass Spectrometry (HPLC-ESI- QTOF-MS-MS) analysis of the water extract from the leaves was used to characterise the chemical composition of the plant and allowed identification of some flavonoids, such as astragalin, and some phenolic compounds. Then, high-speed counter current chromatography (HSCCC) was used to fractionate the ethyl acetate partition obtained from the water extract from the leaves.Results and DiscussionThe presence of flavonoids derived from kaempferol was confirmed and astragalin was isolated for the first time in P. volubilis. The P. volubilis water infusion, ethyl acetate extract and the isolated astragalin exhibited anti-bacterial activity against H. pylori J99 and two clinical isolates (e.g., minimum inhibitory concentrations of 0.53, 0.51 and 0.49 μg/mL, respectively, for clarithromycin-resistant clinical isolate SSR366). Then, using molecular docking for potential protein targets for H. pylori, it was verified that astragalin could interact with these proteins by in silico analysis.ConclusionThese findings highlight that P. volubilis and astragalin produce a bacteriostatic activity against H. pylori and may have potential to be used in treatment against H. pylori, after further research.

IntroductionThe 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.MethodsDuring 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.ResultsOur 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.ConclusionAS mitigates LPS-induced IMB damage via mitigating inflammation and modulating intestinal microbiota.

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. [ABSTRACT FROM AUTHOR]

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.

Cellulose is the most abundant biomass in nature, and the development of high-value utilization technologies for cellulose is of great significance. In this work, a recombinant strain was engineered by introducing Arabidopsis thaliana glycosyltransferase (AtUGT78D2) and the cellobiose phosphorolysis route to produce astragalin from kaempferol. By optimizing the transformation conditions, the production of astragalin increased from 1053 to 3031 mg/L with the addition of cellobiose. Subsequently, the cellulose enzymatic solution was used to replace cellobiose as the carbon source and UDP-glucose precursor for producing astragalin. By optimizing enzymatic conditions and adding additives, the concentration of cellobiose significantly increased, resulting in an increase in the production of astragalin to 2279 mg/L. The adsorption strategy was employed to modulate the composition and activity of cellulase, and the ratio of cellobiose to glucose in the cellulose enzymatic solution increased from 0.73 to 1.62, with the yield of cellobiose reaching up to 5.9 g/L. Finally, the highest production of astragalin in the recombinant strain reached 2654 mg/L when the optimal ratio of cellobiose to glucose was used as the carbon source. This study provides a novel method for producing astragalin by using the enzymatic hydrolysis of microcrystalline cellulose. [Display omitted] • A recombinant strain was constructed to produce astragalin from kaempferol. • Cellulose enzymatic solution was used to replace cellobiose for astragalin production. • Cellobiose concentration significantly increased through optimizing enzymatic conditions. • The ratio of cellobiose to glucose increased with the adsorption strategy. • Astragalin production reached 2654 mg/L with cellulose enzymatic solution as a carbon source. [ABSTRACT FROM AUTHOR]

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Plants contain a large number of small-molecule compounds that are useful for targeting human health and in drug discovery. Healthy bone metabolism depends on the balance between bone-forming osteoblast activity and bone-resorbing osteoclast activity. In an ongoing study searching for 22 plant extracts effective against osteoporosis, we found that the crude extract of Euptelea polyandra Sieb. et Zucc (E. polyandra) had osteogenic bioactivity. In this study, we isolated two compounds, isoquercitrin (1) and astragalin (2), responsible for osteogenic bioactivity in osteoblastic MC3T3-E1 cells from the leaf of E. polyandra using column chromatography and the spectroscopic technique. This is the first report to isolate astragalin from E. polyandra. Compounds (1) and (2) promoted osteoblast differentiation by increasing alkaline phosphatase (ALP) activity and alizarin red S stain-positive calcium deposition, while simultaneously suppressing tartrate-resistant acid phosphatase (TRAP)-positive osteoclast differentiation in RAW264.7 cells at non-cytotoxic concentrations. Isoquercitrin (1) and astragalin (2) increased the expression of osteoblastic differentiation genes, Osterix, ALP, and Osteoprotegerin in the MC3T3-E1 cells, while suppressing osteoclast differentiation genes, TRAP, Cathepsin K, and MMP 9 in the RAW264.7 cells. These compounds may be ideal targets for the treatment of osteoporosis due to their dual function of promoting bone formation and inhibiting bone resorption. [ABSTRACT FROM AUTHOR]

AIM: To investigate the effects of astragalin (AST) on activation status of astrocytes and the expression level of autophagy-related proteins in the cortex of the anterior cingulate cortex of mice with a complete Freund's adjuvant (CFA)-induced inflammatory pain model. METHODS: Twenty-four 6-month-old male C57BL/6 mice were randomly divided into four groups: control group, saline group, CFA model group and CFA+60 mg/kg AST administration group, and six mice in each group. Mice in the AST administration group received 60 mg/kg AST by intraperitoneal injection on a body weight basis for 21 d. The paw withdrawal threshold in each group of mice was evaluated by the von Frey test. The expression levels of autophagy-related factors LC3, p62, ATG12 and beclin-1, and astrocyte activation were detected by multiplex immunofluorescence staining in the anterior cingulate cortex of mice in each group. Western blot was used to measure the levels of autophagy-related proteins LC3, p62, ATG12 and beclin-1 in the anterior cingulate cortex of mice in each group. RESULTS: Behavioural tests showed that AST significantly increased mechanical pain thresholds in CFA mice (P<0. 05). The results from multiple immunofluorescent staining showed that AST significantly increased the fluorescence intensity of LC3 (P<0. 01), ATG12 (P<0. 01) and beclin-1 (P<0. 05), attenuated the fluorescence intensity of p62 (P<0. 05), and inhibited the activation of astrocytes in the anterior cingulate cortex of CFA mice. Western blot results further confirmed that AST significantly increased the expressions of LC3 (P<0. 01), ATG12 (P<0. 01), beclin-1 (P<0. 01), and decreased the expression of p62 (P<0. 05) in the anterior cingulate cortex of CFA mice. CONCLUSION: AST relieves CFA-induced inflammatory pain of mice, and its analgesic mechanism may be related to the inhibition of activation of cortical astrocytes in the anterior cingulate cortex and the promotion of autophagy in CFA mice. [ABSTRACT FROM AUTHOR]

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.

AIM: To investigate the aldose reductase (AR) inhibition capacity of astragalin (AST) against streptozoticin-induced diabetic cataracts (DCs) in rats. METHODS: Ex vivo investigations were conducted by treating the lens of a goat placed for 72h in artificial aqueous humor (AAH) of pH 7.8 at room temperature with cataract-causing substance (55 mmol/L of galactose) and in vivo studies were performed on rats via induction with streptozotocin. AST was administered at different dose levels and scrutinize for DC activity. RESULTS: In diabetic rats, AST improved the body weight, blood insulin, and glucose as well as the levels of galactitol in a dose-dependent way, other biochemical parameters i.e. inflammatory mediators and cytokines, and also suppress AR activity. The level of the antioxidant parameters such as superoxide dismutase (SOD), catalase (CAT), and glutathione (GSH) activity were also altered on a diabetic lens after the administration of the AST. CONCLUSION: AST protects against lens opacification to avoid cataracts and polyols formation, indicating that it could be used as a potential therapeutic agent for diabetes.

To overcome the shortcomings of traditional extraction methods, such as long extraction time and low efficiency, and considering the low content and high complexity of total flavonoids in Artemisia absinthium L., in this experiment, we adopted ultrasound-assisted enzymatic hydrolysis to improve the yield of total flavonoids, and combined this with molecular docking and network pharmacology to predict its core constituent targets, so as to evaluate its antitumor activity. The content of total flavonoids in Artemisia absinthium L. reached 3.80 ± 0.13%, and the main components included Astragalin, Cynaroside, Ononin, Rutin, Kaempferol-3-O-rutinoside, Diosmetin, Isorhamnetin, and Luteolin. Cynaroside and Astragalin exert their cervical cancer inhibitory functions by regulating several signaling proteins (e.g., EGFR, STAT3, CCND1, IGFIR, ESR1). Gene Ontology (GO) and Kyoto Encyclopedia of Genes and Genomes (KEGG) pathway enrichment analysis showed that the anticancer activity of both compounds was associated with the ErbB signaling pathway and FoxO signaling pathway. MTT results showed that total flavonoids of Artemisia absinthium L. and its active components (Cynaroside and Astragalin) significantly inhibited the growth of HeLa cells in a concentration-dependent manner with IC50 of 396.0 ± 54.2 μg/mL and 449.0 ± 54.8 μg/mL, respectively. Furthermore, its active components can mediate apoptosis by inducing the accumulation of ROS. [ABSTRACT FROM AUTHOR]

Naturally occurring flavonoids have long been utilized as essential templates for the development of novel drugs and as critical ingredients for functional foods. Astragalin (AG) is a natural flavonoid that can be isolated from a variety of familiar edible plants, such as the seeds of green tea, Morus alba L., and Cuscuta chinensis. It is noteworthy that AG has a wide range of pharmacological activities and possesses therapeutic effects against a variety of diseases, covering cancers, osteoarthritis, osteoporosis, ulcerative colitis, mastitis, obesity, diabetes mellitus, diabetic complications, ischemia/reperfusion injury, neuropathy, respiratory diseases, and reproductive system diseases. This article reviewed the natural source and pharmacokinetics of AG and systematically summarized the pharmacological activities and potential mechanisms of AG in treating diverse diseases in order to promote the development of AG as a functional food, in doing so providing references for its clinical application in disease therapy. [ABSTRACT FROM AUTHOR]

Afrah E Mohammed,1,&ast; Sahar S Alghamdi,2,3 Ashwag Shami,1,&ast; Rasha Saad Suliman,4 Kawther Aabed,1 Modhi O Alotaibi,1 Ishrat Rahman5 1Department of Biology, College of Science, Princess Nourah bint Abdulrahman University, Riyadh, 11671, Saudi Arabia; 2Department of Pharmaceutical Sciences, College of Pharmacy, King Saud Bin Abdulaziz University for Health Sciences, Riyadh, Saudi Arabia; 3King Abdullah International Medical Research Center (KAIMRC), Riyadh, Saudi Arabia; 4Department of Pharmacy, Fatima College of Health Sciences, Abu Dhabi, 3798, United Arab Emirates; 5Department of Basic Dental Sciences, College of Dentistry, Princess Nourah bint Abdulrahman University, Riyadh, 11671, Saudi Arabia&ast;These authors contributed equally to this workCorrespondence: Ishrat Rahman, Department of Basic Dental Sciences, College of Dentistry, Princess Nourah bint Abdulrahman University, P.O. Box 84428, Riyadh, 11671, Saudi Arabia, Email imrahman@pnu.edu.saIntroduction: Biogenic silver nanoparticles (AgNPs) may be a feasible therapeutic option in the research and development towards selectively targeting specific cancers and microbial infections, lending a role in precision medicine. In-silico methods are a viable strategy to aid in drug discovery by identifying lead plant bioactive molecules for further wet lab and animal experiments.Methods: Green synthesis of M-AgNPs was performed using the aqueous extract from the Malvaviscus arboreus leaves, characterized using UV spectroscopy, FTIR, TEM, DLS, and EDS. In addition, Ampicillin conjugated M-AgNPs were also synthesized. The cytotoxic potential of the M-AgNPs was evaluated using the MTT assay on MDA-MB 231, MCF10A, and HCT116 cancer cell lines. The antimicrobial effects were determined using the agar well diffusion assay on methicillin-resistant S. aureus (MRSA) and S. mutans, E. coli, and Klebsiella pneumoniae. Additionally, LC-MS was used to identify the phytometabolites, and in silico techniques were applied to determine the pharmacodynamic and pharmacokinetic profiles of the identified metabolites.Results: Spherical M-AgNPs were successfully biosynthesized with a mean diameter of 21.8 nm and were active on all tested bacteria. Conjugation with ampicillin increased the susceptibility of the bacteria. These antibacterial effects were most predominant in Staphylococcus aureus (p < 0.0001). M-AgNPs had potent cytotoxic activity against the colon cancer cell line (IC50=29.5 μg/mL). In addition, four secondary metabolites were identified, Astragalin, 4-hydroxyphenyl acetic acid, Caffeic acid, and Vernolic acid. In silico studies identified Astragalin as the most active antibacterial and anti-cancer metabolite, binding strongly to the carbonic anhydrase IX enzyme with a comparatively higher number of residual interactions.Discussion: Synthesis of green AgNPs presents a new opportunity in the field of precision medicine, the concept centered on the biochemical properties and biological effects of the functional groups present in the plant metabolites used for reduction and capping. M-AgNPs may be useful in treating colon carcinoma and MRSA infections. Astragalin appears to be the optimal and safe lead for further anti-cancer and anti-microbial drug development.Keywords: biogenic AgNPs, LC-MS, Astragalin, biological activity

Astragalin (AG), a natural flavonoid present in white mulberry and plants belonging to Rosaceae and other families, has various biological functions. However, the potential mechanism through which it protects the liver from injury caused by oxidative stress has not yet been reported. In this study, we aimed to elucidate the mechanism underlying the hepatoprotective effect of AG. We found that AG treatment inhibited the oxidative stress caused by H2O2 and promoted Nrf2 nuclear translocation in an LO2 cell model. Furthermore, the expression of Nrf2 and its downstream antioxidant genes was increased. In the C57BL/6J mouse model, we found AG treatment prevented alcohol-induced acute liver injury in mice by reducing lipid peroxidation and enhancing antioxidant activity. Consistent with in vitro results, we observed elevated expression of Nrf2 and its downstream antioxidant genes in mouse liver tissues. To further explore the underlying mechanisms, bioinformatics analysis was used to detect miRNAs and lnc RNAs that regulate the expression of Nrf2. Our findings suggest that AG may protect the liver from damage caused by oxidative stress by modulating the lnc XIST/miR-155-5p/Nrf2 axis.

The current study was designed to determine the curative potential of astragalin (AST) against polystyrene microplastics (PS-MPs) induced hepatic toxicity in rats. PS-MPs exposure decreased the expression of Nrf-2 and anti-oxidant enzymes, while increasing Keap-1 expression. The activities of glutathione-S-transferase, catalase, glutathione, glutathione peroxidase, superoxide dismutase, glutathione reductase and heme oxygenase-1 were decreased, besides the levels of malondialdehyde and reactive oxygen species were also increased following the exposure of PS-MPs. The intoxication of PS-MPs elevated aspartate aminotransferase, alanine transaminase, alkaline phosphatase levels, as well as cyclooxygenase-2 activity, interleukin-6, interleukin-1 beta, nuclear factor-kappa B and tumor necrosis factor-alpha levels were also escalated. Furthermore, Bcl-2 expression was down-regulated, while Bax and Caspase-3 expressions were upregulated following PS-MPs exposure. Histopathological assessment revealed substantial liver damages in PS-MPs treated rats. However, AST supplementation substantially recovered PS-MPs-induced damages and histological anomalies. Therefore, AST can be used as a curative agent to treat PS-MPs-prompted hepatotoxicity due to its anti-apoptotic, anti-inflammatory and anti-oxidant potentials.

Ultraviolet (UV) radiation is a non-ionizing radiation, which has a cytotoxic potential, and it is therefore necessary to protect against it. Human skin is exposed to the longer-wavelength components of UV radiation (UVA and UVB) from the sun. In the present paper, we focused on the study of eight organic UV-absorbing compounds: astragalin, beta-carotene, 2,4-dihydroxybenzophenone, 2-hydroxy-4-methoxybenzophenone, hyperoside, 3-(4-methylbenzylidene)camphor, pachypodol, and trans-urocanic acid, as possible protectives of skin cells against UVA and UVB radiation. Their protective effects on skin cell viability, ROS production, mitochondrial membrane potential, liposomal permeability, and DNA integrity were investigated. Only some of the compounds studied, such as trans-urocanic acid and hyperoside, had a significant effect on the examined hallmarks of UV-induced cell damage. This was also confirmed by an atomic force microscopy study of morphological changes in HaCaT cells or a study conducted on a 3D skin model. In conclusion, hyperoside was found to be a very effective UV-protective compound, especially against UVA radiation. Commonly used sunscreen compounds such as 2,4-dihydroxybenzophenone, 2-hydroxy-4-methoxybenzophenone, and 3-(4-methylbenzylidene)camphor turned out to be only physical UV filters, and pachypodol with a relatively high absorption in the UVA region was shown to be more phototoxic than photoprotective. [ABSTRACT FROM AUTHOR]

Summary: This study aims to reveal the stability of cellulose nanocrystals (CNCs) and astragalin/tangeretin co‐stabilised Pickering emulsion under different environmental factors such as ionic strengths, pH values, thermal treatment, freeze–thaw treatment, sodium ascorbate, and storage condition. Results showed that the astragalin and CNCs co‐stabilised Pickering emulsion (AST‐CPE) could maintain a stable appearance, typical spherical morphology droplets, and steady physical stability under various conditions, including ionic strength at low 20 mm, pH values 2–8, thermal treatment (65, 85, and 135 °C), the addition of sodium ascorbate, and storage at 4 °C for 35 days. It is noteworthy that AST‐CPE showed higher emulsion physical stability at pH 2 (56.67%) and pH 8 (53.33%). The co‐stabilised Pickering emulsion structure has a firm and physically stable system. Moreover, it could effectively protect the bioactive substance by expanding its application in food delivery vehicles. [ABSTRACT FROM AUTHOR]

Senile plaques composed of β-amyloid protein (Aβ) and neurofibrillary tangles (NFTs) composed of intracellular hyper-phosphorylated tau are major causes of cognitive impairment and neuronal damage in Alzheimer disease (AD). Astragalin (AST), a naturally-occurring flavonoid compound, was reported to have neuroprotective effects in the brain, but its effects in AD remain unknown. Herein, the learning and memory deficits were alleviated and neuronal damage in the hippocampus were inhibited after the senescence-accelerated mouse prone 8 (SAMP8) mouse were given AST (5 mg/kg or 10 mg/kg) daily by gavage for 2 months. Furthermore, AST reduced Aβ1−40 and Aβ1−42 deposition, decreased β-carboxyl-terminal fragment (β-CTF) protein level and tau hyper-phosphorylation, but increased α-CTF protein level and glycogen synthase kinase-3beta (GSK-3β) phosphorylation in hippocampus of SAMP8 mice. Meanwhile, the effects of AST on AD were also explored in vitro by treating primary neurons with amyloid-β1–42 oligomers (Aβ1−42O). Consistently, AST also alleviated amyloid-β1–42 oligomers (Aβ1−42O)-induced neuronal damage, amyloid plaques, and tau phosphorylation in vitro model. Of note, estrogen receptor (ER)α and ERβ expression in the hippocampus of SAMP8 mice and Aβ1−42O-treated neurons was significantly decreased but their levels were increased by AST. Moreover, in vivo and in vitro experiments revealed that ER antagonist, Fulvestrant, reversed the effects caused by AST. Altogether, our investigation indicates that AST may ameliorate cognitive deficits and AD-type pathologies in SAMP8 mice and Aβ1−42O-treated neurons through upregulating ERα and ERβ expression. Our findings indicate the value of AST as a potential reagent for AD treatment. [ABSTRACT FROM AUTHOR]

Isorhamnetin-3-O-glucoside and astragalin, flavonol glucosides, were isolated from the petals of Paeonia lactiflora as neurite outgrowth-promoting compounds. Isoquercitrin, formed by demethylating the B ring of isorhamnetin-3-O-glucoside or by adding a hydroxyl group to the B ring of astragalin, was evaluated for neurite outgrowth-promoting activity and was compared with the activities of isorhamnetin-3-O-glucoside and astragalin. The activities of isorhamnetin, kaempferol, and quercetin, aglycones corresponding to isorhamnetin-3-O-glucoside, astragalin, and isoquercitrin, respectively, were also evaluated. Isorhamnetin-3-O-glucoside and astragalin showed much stronger neurite outgrowth-promoting activities than the activities of the other tested flavonoids. They exhibited relatively weak anti-oxidant activities and moderate AChE inhibitory activities compared to the activities of the other tested flavonoids. Isorhamnetin-3-O-glucoside and astragalin promoted morphological neurite outgrowth and the expression of neurofilaments induced by NGF in PC12 cells. Isorhamnetin-3-O-glucoside and astragalin might be candidate compounds as neural differentiation agents in peripheral nerves and functional food ingredients preventing cognitive decline. [ABSTRACT FROM AUTHOR]

Insulin resistance is an element of metabolic syndrome, manifested as a decrease in glucose uptake, which often leads to a variety of complications, including type 2 diabetes. Astragalin is a natural flavonoid, isolated from traditional medicinal plants, such as Cuscuta chinensis, that has been shown to exhibit a variety of pharmacological activities with anti-inflammatory, antioxidant, neuroprotective, cardioprotective, antiobesity, antiosteoporotic, anticancer, antiulcer, and antidiabetic properties. However, the mechanism of astragalin on insulin resistance has not yet been elucidated. To this end, we examined the effect of astragalin on palmitic acid-induced insulin resistance in HepG2 cells. The effects of the co-incubation of PA and astragalin on the cell viability, superoxide dismutase, fat content, and markers of oxidative stress in HepG2 cells were measured. The results show that astragalin restored the cell viability, reduced oxidative stress, and insulin resistance in palmitic acid treated HepG2 cells. The protective effect of astragalin on palmitic acid-induced lipotoxicity in HepG2 cells was through inhibition of NF-κB and JNK signaling pathways. [ABSTRACT FROM AUTHOR]

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 Fe 2+ 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., Competing Interests: There are no conflicts of interest in our work and the manuscript was published with the consent of all authors. On behalf of my co-authors, I would like to state that the work described here is original research that has never been published before and is not under consideration for publication elsewhere., (© 2024 The Authors.)

Introduction: 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., Methods: 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., Results: 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., Conclusion: AS mitigates LPS-induced IMB damage via mitigating inflammation and modulating intestinal microbiota., Competing Interests: The authors declare that the research was conducted in the absence of any commercial or financial relationships that could be construed as a potential conflict of interest., (Copyright © 2024 Tang, Lin, Yang, Xu, Lin, Yang, Huang and Wu.)

Moringa oleifera leaves are cultivated in warm regions of Brazil for commercial ends due to their nutritional and biological properties. This study evaluated, by chemometric tools, the influence of seasonality (winter, spring, autumn, and summer), growing area in Brazil (South, Southeast, and Northeast), and regrowth age (40 and 80 days) in antioxidant potential, and biochemical markers determined by HPLC-DAD. The results obtained in the present study showed that all the parameters evaluated were affected by seasonality, regrowth age, and growing region. The content of phenolic compounds and antioxidant activity using the ABTS method was higher in samples cultivated in the southeast (59.4 mg GAE g−1 and 346 µmol TEAC g−1, respectively). The highest antioxidant activities evaluated by DPPH and FRAP methods were obtained from leaves of the southeast and northeast. In addition, young leaves presented higher antioxidant potential and total phenolic content. The cultivation region significantly influenced the content of chlorogenic acid, isoquercitrin, and astragalin, which ranged from 4.2 to 7.2 mg g−1, 8.0 to 10.7 mg g−1, and 2.2 to 3.8 mg g−1, respectively. In addition, a positive correlation between solar radiation and temperature with caffeic acid, rutin, phenolic compounds, and antioxidant assay from the DPPH method was observed. Additionally, the RGB pattern of the images of these leaves was correlated with the levels of compounds with antioxidant activity. Models generated through machine learning showed good performances, and ABTS and rutin analyses developed the best models with a coefficient of determination above 75 %. Thus, color patterns can be used to measure the antioxidant activity by the ABTS method and to determine the rutin concentration in M. oleifera leaves.

Flavonoid rich foods are described as superfoods because of their potent antioxidant properties. They are natural antioxidants and have various health oriented biological benefits such as anti-inflammatory, immunomodulatory, antiviral and anticarcinogenic properties. Identification of flavonoids in the isolated butanolic extract of Carica papaya L. cultivar ‘Red Lady’ leaf using UPLC-Q-ToF-MS/MS is the highlight of the study. In the present study, 11 flavonoids were detected in the butanolic extract among them, luteolin, astragalin, 2-(3,4-Dihydroxy-5-methoxyphenyl)-3,5,7- trihydroxy-6-metoxy-2,3 dihydro-4H-chromen-4-one and quercetin dimer are new reports in C. papaya leaves. Flavonoids in butanolic extract were fractionated by preparative HPTLC and obtained 4 flavonoid bands. Flavonoids in each band were identified using UPLC-Q-ToF-MS. Antioxidant activity of butanolic extract and its fractions separated by preparative HPTLC were determined by FRAP assay and DPPH free radical scavenging assay. Butanolic extract showed a dose (0.05mg/ml, 0.1 mg/ml, 0.2mg/ml, 0.4mg/ml and 0.8mg/ml) dependent increment in antioxidant activity. Assay of the bands obtained by preparative HPTLC analysis showed that those containing quercetin and its glucoside derivatives have more antioxidant activity than those containing kaempferol and its glucoside derivatives.

Rationale: Neuroinflammation can be alleviated via M2 microglia polarization, which could promote the recovery of perimenopausal depression. Astragalin (AST) possesses anti-neuroinflammatory activity. However, the effects of AST on perimenopausal depression and the molecular mechanism in regulating microglia polarization remained unknown. Objectives: The purpose was to investigate the effects of AST on mice with simulated perimenopausal depression through regulating microglia polarization. It was aimed to clarify the molecular mechanism related to the interleukin-4 receptor (IL-4R)/janus kinase (JAK) 1/signal transducer and activator of transcription (STAT) 6 signaling pathway. Methods: The ovariectomy (OVX)/chronic unpredictable mild stress (CUMS)-induced murine model of perimenopausal depression was established and treated with AST. Then the depression-like behaviors and cognitive ability of mice were examined. After that, we detected the markers of microglia polarization and its regulatory signals. In addition, lipopolysaccharides (LPS)/adenosine triphosphate (ATP)-induced inflammatory BV2 model were used to verify the potential molecular mechanism. Results: AST alleviated perimenopausal depression-like behaviors and memory deficits. AST alleviated microglia activation and increased Ki67-positive cells in dentate gyrus (DG). The viability of BV2 decreased by LPS/ATP was raised by AST. Moreover, both in vivo and in vitro, AST switched microglia from M1 phenotype caused by OVX/CUMS or LPS/ATP to M2 phenotype. The IL-4R/JAK1/STAT6 signaling was restored, and the levels of inducible nitric oxide synthase (iNOS), nuclear NF-KappaB-p65 were reduced by AST. Importantly, AST showed prevention against the ubiquitination modification and degradation of STAT6. Conclusions: Our results revealed new insights into molecular mechanism associated with microglia polarization in the effect of AST on the mouse model of perimenopausal depression. [ABSTRACT FROM AUTHOR]

Inhibition of adipogenesis is crucial and is a key area of research to develop antiobesity drugs. In this study, 3-O-glucoside of kaempferol (astragalin) was isolated from Moringa oleifera leaves and evaluated for its lipolytic and antiadipogenic activity in 3T3-L1 adipocytes. Astragalin has substantially reduced the triglycerides content and lipid accumulation in 3T3-L1 adipocytes and enhanced the glycerol release in a dose dependent manner. The assay for secreted adipocytokines confirmed that, astragalin at a concentration of 20 µg/mL significantly (p <.01) increased the secretion of adiponectin, but decreased leptin secretion in 3T3-L1 adipocytes. In molecular studies, both the mRNA expression and corresponding protein expression of PPAR-γ, C/EBP-α, FAS, and leptin genes were downregulated while that of adiponectin was upregulated in astragalin treated groups. Taken together, astragalin of M. oleifera promotes lipolysis, suppresses adipogenesis in 3T3-L1 adipocytes, and may be considered as an effective candidate to treat obesity aliments. [ABSTRACT FROM AUTHOR]

More than 40% of infertile men are diagnosed with oligoasthenozoospermia and the incidence is still rising, but the effective treatments are not been found until now. Astragalin, one of the main active ingredients in traditional Chinese medicine, may be effective in the treatment of oligoasthenozoospermia. This study investigated the pharmacological effects of astragalin for treatment of oligoasthenozoospermia in male mice, induced by cyclophosphamide (CTX). Male mice were intraperitoneally injected by CTX (50 mg/kg), and astragalin (30 mg/kg) was given via oral gavage once daily. RNA-seq analysis highlighted astragalin upregulated gene expression of anti-apoptosis (AKT1and BCL2-XL), cell proliferation (ETV1, MAPKAPK2, and RPS6KA5) and synthesis of testosterone (STAR, CYP11A1, and PRKACB), but downregulated gene expression of cell apoptosis (BAD, BCL-2, CASPASE9, and CASPASE3) in mouse testis. Astragalin also significantly reversed the reduction in body weight, reproductive organs index, and sperm parameters (sperm concentration, viability, and motility) induced by CTX, and restored testicular abnormal histopathologic morphology induced by CTX. Furthermore, astragalin dramatically rescued the gene expression related to spermatogenesis (AKT1, BCL-2, CASPASE9, CASPASE3, MAPKAPK2, RPS6KA5, STAR, and PRKACB), and increased the level of testosterone by improving related proteins (STAR, CYP11A1, PRKACB) for oligoasthenozoospermia induced by CTX. In conclusion, astragalin may be a potential beneficial agent for oligoasthenozoospermia by increasing the testosterone levels in testis. [ABSTRACT FROM AUTHOR]

Moringa oleifera Lam. has multiple biological properties that are applicable to developing cosmeceuticals. The objective of this study was to evaluate anti-inflammatory effects of M. oleifera on normal human keratinocytes. The antiinflammatory effects of water extract and 50% ethanol extract of M. oleifera leaves, and of the bioactive compound astragalin, on UVB-irradiated human keratinocytes were investigated. The levels of inflammatory mediators IL-1, IL-8, NO and PGE2 released from keratinocytes were measured using ELISA and Griess assays. UVB irradiation increased the release of IL-1, IL-8 and PGE2 into cell culture media after 24 h. The effect was significantly decreased by treatments with astragalin and M. oleifera leaf extracts, of which the 50% ethanol extract showed stronger inhibition than the water extract. These results suggest that this extract is a potential ingredient in products for relieving UVB-induced skin inflammation. Astragalin could be used as a bioactive positive control in the quality control of the extract.

[Display omitted] • Astragalin (AST) ameliorated the inflammatory and pathological changes as well as functional abnormalities of lipopolysaccharide (LPS)-induced acute liver injury. • AST inhibited the tumor necrosis factor (TNF)-α-driven receptor-interacting protein kinase 1 (RIPK1)-mediated necroptosis signaling pathway. • AST suppressed the activation of the hypoxia-inducible factor-1α/pyruvate kinase M2 (HIF-1α/PKM2) signaling pathway. • AST hindered the enhanced glycolysis of M1 macrophages. 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. [ABSTRACT FROM AUTHOR]

• ATFP coupled with prep-HPLC for purification of astragalin was established. • Recovery of astragalin from Flaveria bidentis was 99.5% using the ATFP method. • Using the established ATFP coupled with prep-HPLC, the purity of astragalin was 98.8%. The strategy of aqueous two-phase flotation (ATPF) followed by preparative high performance liquid chromatography (prep-HPLC) was established and used for the separation of astragalin from Flaveria bidentis. In the ATPF, the effects of sublation solvent, solution pH, (NH 4) 2 SO 4 concentration in aqueous solution, cosolvent, N 2 flow rate, flotation time and volumes of the PEG phase on the recovery of astragalin were investigated in detail, and the optimal conditions of ATPF were selected: 50 wt% PEG1000 ethanol solvent as the flotation solvent, pH 4, 350 g/L of (NH 4) 2 SO 4 concentration in 5 % ethanol aqueous phase, 40 mL/min of N 2 flow rate, 30 min of flotation time, 10.0 mL of flotation solvent volume and twice. After ATPF enrichment, the flotation product was further purified by prep-HPLC. As determined by HPLC, the purity of astragalin was 98.8 %. [ABSTRACT FROM AUTHOR]

Background/Aims: Astragalin (kaempferol-3-O-β-D-glucoside) is a flavonoid isolated from the leaves of persimmon or Rosa agrestis. Astragalin exhibits various anti-inflammatory properties; however, little is known about its therapeutic potential for inflammatory bowel disease (IBD). This study aims to investigate the anti-inflammatory effect of astragalin via blockade of the nuclear factor κB (NF-κB) signaling pathway in human colonic epithelial cells and a murine colitis model. Methods: HCT-116 and HT-29 human colonic epithelial cells were pretreated with astragalin and stimulated with tumor necrosis factor-α (TNF-α). Cell viability was assessed by the MTS assay. Real-time reverse transcription polymerase chain reaction was used to analyze the messenger RNA expression of the inflammatory cytokines interleukin (IL)-6 and IL-8. The effect of astragalin on the NF-κB pathway was evaluated by Western blot analysis of inhibitor of NF-κB alpha (IκBα) phosphorylation/degradation and by electrophoretic mobility shift assay. Dextran sulfate sodium (DSS)-induced acute murine colitis model was used for in vivo experiments. Results: Astragalin strongly suppressed the expression of proinflammatory cytokines in human colonic epithelial cells in a dose-dependent manner. Western blot analysis showed that astragalin inhibited IκBα phosphorylation/degradation. Additionally, astragalin reduced the DNA binding activity of NF-κB. Astragalin alleviated colon shortening and improved the pathologic scores in DSS-induced acute murine colitis model. Furthermore, astragalin reduced the level of phosphorylated IκBα and decreased the production of the inflammatory cytokines IL-6, IL-8, and TNF-α in the DSS-treated colon mucosa. Conclusions: Astragalin exerted an anti-inflammatory effect through NF-κB pathway inhibition and attenuated murine colitis. Astragalin is thus a potential therapeutic agent for IBD.

Spinifex littoreus Burm.f.Merr. Coastal shrubs used for the treatment of a wide variety of diseases such as galactogenic, blistering agent, antihelmenthic, antipyretic, antidiruetic, anti – haemorrhages, antileukaemias and anti-inflammatory. It is rich in flavonoids and known to possess various biological activities. Fresh leaves of Spinifex littoreus have been examined for their bioactive flavonoids. The flavonol Kaempferol, flavonol glycoside astragalin have been identified. The structure of isolated polyphenolic compounds were characterised with the help of physical methods like UV, 1H NMR, 13C NMR, Chemical reactions, Chromatographic techniques and hydrolytic studies The in-vitro studies showed that the isolated flavonol glycosides have been found to contain ample anti-oxidant property with the help of ELISA method.

Graviola, soursop, or guanabana (Annona muricata L.), is an ethnomedical fruit consumed to alleviate headache, diarrhea, diabetes, and cancer. Pericarp is the inedible part of graviola least studied in comparison to seeds and leaves, even thought, it contains the highest concentration of graviola total polyphenols. Anticancer effect of graviola pericarp has been demonstrated in crude extracts attributing the effect to acetogenins, however, crude extracts contain several active molecules. Thus, the present work aimed to fractionate and purify an ethanolic crude extract from graviola pericarp. Purified graviola pericarp fraction (PGPF) was evaluated on cancerous and non-cancerous cell lines, and then was identified by NMR, TOF-MS, and HPLC. Finally, an in silico analysis was performed to predict targets cancer-related of the molecule detected. Our results revealed IC50 values for cervix adenocarcinoma (HeLa), hepatocellular carcinoma (HepG2), triple-negative breast cancer (MDA-MB-231), and non-cancerous cell line (HaCaT) of 92.85 ± 1.23, 81.70 ± 1.09, 84.28 ± 1.08, and 170.2 ± 1.12 µg PGPF/mL, respectively. In vitro therapeutic indexes estimated as quantitative relationship between safety and efficacy of PGPF were 1.83, 2.08, and 2.02 for HeLa, HepG2, and MDA-MB-231, respectively. The NMR analysis revealed astragalin (kaempferol-3-O-glucoside) in PGPF, a flavonoid not reported in graviola pericarp until now. Astragalin identity was confirmed by TOF-MS and HPLC. In silico results support previous reports about astragalin modulating proteins such as Bcl-2, CDK2, CDK4, MAPK and RAF1. Also, results suggest that astragalin may interact with other cancer-related proteins not associated previously with astragalin. In conclusion, astragalin may be contributing to the anticancer effect observed in graviola pericarp extracts.

This study aimed to explore the mechanism of the development of lung adenocarcinoma (LUAD) treated by astragalin. Transcriptome sequencing was performed to obtain the gene profile of LUAD treated by astragalin. Combining with bioinformatics analysis including differential gene screening, function enrichment analysis (gene ontology and KEGG), and ceRNA construction, we obtained the novel mechanism of lncRNA mediated miRNA/mRNA axis. Then, the cell experiments were performed to examine the role of lncRNA in cell proliferation, migration and invasion, and apoptosis for LUAD treated with astragalin. Moreover, the tumor formation in nude mice was carried out to detect the ceRNA mechanism in LUAD treated by astragalin in vivo. The lncRNA mediated ceRNA network was obtained, that is, LINC00852 LINC00582/miR-140-3p/PDPK1 played an important role in LUAD treated by astragalin. Function experiments indicated that si-LINC00852 inhibited LUAD cell proliferation, migration and invasion, and promoted cell apoptosis via miR-140-3p/PDPK1 (p < 0.05, p < 0.01). The animal experiments further confirmed that si-LINC00852 inhibited tumor growth through miR-140-3p/PDPK1 in vivo. Conversely, this study provides comprehensive insights into the diagnostic and therapeutic implications of LINC00582 in LUAD, LINC00582 mediated miR-140-3p/PDPK1 axis was the novel drug target of astragalin for treating LUAD., (© 2024 Wiley Periodicals LLC.)

The seeds of Chinese horse chestnut are used as a source of starch and escin, whereas the potential use of whole plant has been ignored. The astringency and bitterness of tea produced from the leaves and flowers were found to be significantly better than those of green tea, suggesting that the enriched flavonoids maybe sensory determinates. During 47 flavonoids identified in leaves and flowers, seven flavonol glycosides in the top 10 including astragalin and isoquercitrin were significantly higher content in flowers than in leaves. The crude proteins of flowers could catalyze flavonol glucosides' formation, in which three glycosyltransferases contributed to the flavonol glucosylation were screened out by multi-dimensional integration of transcriptome, evolutionary analyses, recombinant enzymatic analysis and molecular docking. The deep exploration for flavonol profile and glycosylation provides theoretical and experimental basis for utilization of flowers and leaves of Aesculus chinensis as additives and dietary supplements. [ABSTRACT FROM AUTHOR]

Cissus rotundifolia has been reported to possess various biological activities such as anti-diabetic, anti-fertility, anti-hyperlipidemic, anti-malarial, anti-osteoporotic, and anti-parasitic activities. Therefore in the present study, eleven selected constituents of Cissus rotundifolia which includes aconitic acid, astragalin, acteoside, aliospiroside A, beta amyrin, bergenin, formononetin, gallic acid, isovitexin, isoorientin, and isoquercitrin were studied on the docking behavior of human neutrophil elastase (HNE), matrix metalloproteinases (MMP 2 and MMP 9), and tyrosinase by using PatchDock method. Furthermore, molecular physicochemical, bioactivity score/drug-likeness, ADME (absorption, distribution, metabolism, and excretion), and toxicity analyses were also carried out using Molinspiration, Swiss ADME, and ProTox-II methods, respectively. The molecular physicochemical investigation showed that three ligands such as acteoside, aliospiroside A, and isoorientin have three violations for Lipinski's rule of five. Similarly, ADME analysis one ligand (formononetin) predicated to have high blood-brain barrier (BBB) permeability effect. The docking studies showed that isovitexin exhibited the highest atomic contact energy (−341.61 kcal/mol) for human neutrophil elastase (HNE), more over alliospiroside A has shown maximum atomic contact energy for both matrix metalloproteinases (MMP 2 [−618.00 kcal/mol] and MMP 9 [−634.73 kcal/mol]). Furthermore, isoquercitrin has exhibited the highest atomic contact energy (−145.70 kcal/mol) for tyrosinase. Thus, the present investigation outcome provides new knowledge in understanding eleven Cissus rotundifolia constituents as possible novel inhibitors against HNE, MMP 2, MMP 9, and tyrosinase. [ABSTRACT FROM AUTHOR]

Metabolic disturbances in different tissue cells and obesity are caused by excessive calorie intake, and medicinal plants are potential sources of phytochemicals for combating these health problems. This study investigated the role of methanolic extract of the folklore medicinal plant Lysimachia candida (LCM) and its phytochemical, astragalin, in managing obesity in vivo and in vitro. Administration of LCM (200 mg/kg/body weight) daily for 140 days significantly decreased both the body weight gain (15.66%) and blood triglyceride and free fatty acid levels in high‐fat‐diet‐fed male Wistar rats but caused no substantial change in leptin and adiponectin levels. The protein expression of adipogenic transcription factors in visceral adipose tissue was significantly reduced. Further, the 3T3‐L1 cell‐based assay revealed that the butanol fraction of LCM and its isolated compound, astragalin, exhibited antiadipogenic activity through downregulating adipogenic transcription factors and regulatory proteins. Molecular docking studies were performed to depict the possible binding patterns of astragalin to adipogenesis proteins. Overall, we show the potential antiobesity effects of L. candida and its bioactive compound, astragalin, and suggest clinical studies with LCM and astragalin. [ABSTRACT FROM AUTHOR]

Abstract Background Astragalin (AG), a flavonoid from many traditional herbs and medicinal plants, has been described to exhibit in vitro anti-inflammatory activity. The paper aimed to study the effects of astragalin on anti-inflammatory, anti-oxidative ability and apoptosis signaling pathway in brain tissue of rats with cerebral ischemia-reperfusion injury, and to explore its possible mechanism. Methods The rat model of focal cerebral ischemia-reperfusion injury was established by suture method. It was randomly divided into 5 groups, sham operation group, ischemia-reperfusion (I/R) treatment group, and astragalin treatment I / R group (12.5, 25, 50 mg / kg). After 24 h of reperfusion, the neurological deficits of the rats were analyzed and HE staining was performed. The volume of cerebral infarction was calculated by triphenyltetrazolium chloride (TTC) staining, and the apoptosis of nerve cells was detected by TUNEL staining. In addition, the content of malondialdehyde (MDA), nitric oxide (NO), superoxide dismutase (SOD), glutathione (GSH) assay and glutathione peroxidase (GSH-Px) were measured in rat brain tissue. Western blot analysis was used to determine the expression of related proteins. Results Compared with I/R group, the neurological deficit score and infarct volume of I/R rats were reduced in the astragalin treatment group. In the astragalin treatment group, MDA and NO levels in I/R rats were reduced, antioxidant enzymes and superoxide dismutase (SOD) activity were increased. In the astragalin treatment group, NF-κB (p65) and cyclooxygenase-2 (COX-2) expression levels were down-regulated, NF-E2-related factor 2 (Nrf2) nucleus and heme oxygenase-1 (HO-1) protein expression levels were up-regulated. In addition, the astragalin treatment can inhibit apoptosis, down-regulate Bax and cleaved caspase-3 expression, up-regulate Bcl-Xl expression. Conclusion The antioxidant properties of astragalin may play an important role in improving cerebral ischemia-reperfusion injury.

The seeds of Chinese horse chestnut are used as a source of starch and escin, whereas the potential use of whole plant has been ignored. The astringency and bitterness of tea produced from the leaves and flowers were found to be significantly better than those of green tea, suggesting that the enriched flavonoids maybe sensory determinates. During 47 flavonoids identified in leaves and flowers, seven flavonol glycosides in the top 10 including astragalin and isoquercitrin were significantly higher content in flowers than in leaves. The crude proteins of flowers could catalyze flavonol glucosides' formation, in which three glycosyltransferases contributed to the flavonol glucosylation were screened out by multi-dimensional integration of transcriptome, evolutionary analyses, recombinant enzymatic analysis and molecular docking. The deep exploration for flavonol profile and glycosylation provides theoretical and experimental basis for utilization of flowers and leaves of Aesculus chinensis as additives and dietary supplements.

The traditional use of the M. charantia L. plant to treat coughs, fever and expectoration is widely practiced in different cultures, but its effectiveness and safety still require scientific investigation. This study sought to perform a chemical analysis and evaluate the antitussive, expectorant and antipyretic effects of the ethanolic extract of M. charantia leaves (EEMc) in rats and mice. The EEMc was subjected to chemical analysis by HPLC-DAD, revealing the presence of the flavonoids astragalin and isoquercetin. Acute oral toxicity in mice did not result in deaths, although changes in liver weight and stool consistency were observed. EEMc demonstrated an antitussive effect at doses of 100 and 300 mg/kg in mice subjected to cough induction by citric acid nebulization. Furthermore, it showed expectorant activity at a dose of 300 mg/kg, assessed based on the elimination of the phenol red marker in bronchoalveolar lavage. In the evaluation of antipyretic activity in rats, fever induced by Saccharomyces cerevisiae was reduced at all doses tested during the first hour after treatment. This innovative study identified the presence of astragalin and isoquercetin in EEMc and indicated that the extract has antitussive, expectorant and antipyretic properties. Therefore, EEMc presents itself as a promising option in herbal medicine for the treatment of respiratory symptoms and fever., (© 2024 Wiley-VHCA AG, Zurich, Switzerland.)

Background: 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., Objective: 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., Method: 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., Result: 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., Conclusion: 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., (Copyright© Bentham Science Publishers; For any queries, please email at epub@benthamscience.net.)

Natural plant extracts have gained significant attention in research due to their low toxicity, and potent antioxidant, and anti-aging properties. The present study investigated the phytochemical composition of a fermented rose extract (FRE), and evaluated its antioxidant, skin whitening, and anti-aging activities in vitro . The results showed that the FRE was rich in polyphenols and flavonoids. A total of 13 major compounds were identified by Liquid Chromatography-Mass Spectrometry (LC-MS), with astragalin as the primary component. In vitro , analysis of antioxidant activity showed that FRE effectively eliminated 1,1-diphenyl-2-picrylhydrazyl (DPPH) radicals and 2,2'-azino-bis (3-ethylbenzothiazoline-6-sulfonic acid) (ABTS) radicals and dose-dependent reduced intracellular reactive oxygen species (ROS) levels. The FRE dose-dependent inhibited tyrosinase, collagenase, and hyaluronidase activity, reduced intracellular melanin synthesis, up-regulated the expression of collagen type I alpha 1 (COL1A1) and collagen type III alpha 1 (COL3A1), and down-regulated matrix metalloproteinases (MMPs) expression. Additionally, treatment with FRE significantly downregulated the expression of mitogen-activated protein kinase 1 (MAPK1), suggesting that FRE may modulate MAPK signaling pathways for skin anti-aging.

Gastric cancer is a common malignant cancer, which is one of the most affected cancers by PI3K/AKT signaling. Here, we investigated the anti‐tumor role of Astragalin, a natural flavonoid compound, in gastric cancer and explored the underlying molecular mechanism. Three well‐established gastric cancer cell lines and xenograft mouse model were used to examine the anti‐tumor effect of Astragalin by using CCK‐8, transwell assays, and Western blot. Tumor burden of xenograft mice with Astragalin administration was monitored and determined during and at end of the experiments. Astragalin could effectively inhibit cell viability of gastric cancer cells and possessed good anti‐tumor activity in xenograft mice. In addition, astragalin induced the expression of apoptotic signaling proteins, suppressed the migration and invasion cancer cells, and inhibited the PI3K/AKT signaling pathway significantly. In contrast, epidermal growth factor stimulation was able to block the anti‐tumor activity of Astragalin. In conclusion, astragalin exerts its anticancer activities through inhibiting PI3K/AKT signaling, which highlights its potential for the treatment of gastric cancer. [ABSTRACT FROM AUTHOR]

Isorhamnetin-3-O-glucoside and astragalin, flavonol glucosides, were isolated from the petals of Paeonia lactiflora as neurite outgrowth-promoting compounds. Isoquercitrin, formed by demethylating the B ring of isorhamnetin-3-O-glucoside or by adding a hydroxyl group to the B ring of astragalin, was evaluated for neurite outgrowth-promoting activity and was compared with the activities of isorhamnetin-3-O-glucoside and astragalin. The activities of isorhamnetin, kaempferol, and quercetin, aglycones corresponding to isorhamnetin-3-O-glucoside, astragalin, and isoquercitrin, respectively, were also evaluated. Isorhamnetin-3-O-glucoside and astragalin showed much stronger neurite outgrowth-promoting activities than the activities of the other tested flavonoids. They exhibited relatively weak anti-oxidant activities and moderate AChE inhibitory activities compared to the activities of the other tested flavonoids. Isorhamnetin-3-O-glucoside and astragalin promoted morphological neurite outgrowth and the expression of neurofilaments induced by NGF in PC12 cells. Isorhamnetin-3-O-glucoside and astragalin might be candidate compounds as neural differentiation agents in peripheral nerves and functional food ingredients preventing cognitive decline.

Obesity is a persistent and continuously expanding social health concern. Excessive fat mass accumulation is associated with increased risk of chronic diseases including diabetes, atherosclerosis, non-alcoholic steatohepatitis, reproductive dysfunctions and certain types of cancer. Alchemilla monticola Opiz. is a perennial plant of the Rosaceae family traditionally used to treat inflammatory conditions and as a component of weight loss herbal mixtures. In the search for bioactive leads with potential anti-adipogenic effect from A. monticola extract (ALM), we have employed nuclear magnetic resonance (NMR) based metabolomics to obtain data for the phytochemical profile of the extract. Further, molecular docking simulation was performed against key adipogenic targets for selected pure compounds, present in the ALM extract. Evaluation of the biological activity was done in human adipocytes exposed to ALM (5, 10 and 25 μg/ml), pure astragalin (AST) or quercitrin (QUE) both at the concentrations of 5, 10 and 25 μM. Investigation of the molecular pathways involved was performed through real-time quantitative PCR and Western blot analyses. According to the docking predictions strong putative affinity was revealed for both AST and QUE towards peroxisome proliferator-activated receptor gamma (PPARγ) and phosphoinositide 3-kinase (PI3K). Assessment of the intracellular lipid accumulation revealed anti-adipogenic activity of ALM. Correspondingly, the expression of the adipogenic genes CCAAT/enhancer-binding protein alpha (CEBPA) and PPARG was downregulated upon ALM and AST treatment. The Western blotting results exposed protein kinase B (AKT), PI3K and PPARγ as targets for the inhibitory effect of ALM and AST on adipogenesis. Collectively, we provide a broader insight of the phytochemical composition of A. monticola. Additionally, we demonstrate the anti-adipogenic effect of ALM and its active compound AST in human adipocytes. Furthermore, PI3K/AKT signaling pathway is identified to mediate the ALM anti-adipogenic action. Hence, the ALM extract and its secondary metabolite AST are worth further exploration as potentially active agents in obesity management.