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Objective: This study aims to investigate the mechanism of Tetrastigma hemsleyanum Diels et Gilg flavonoids (THF) on acute hepatic injury (AHI). Methods: First, high-performance liquid chromatography (HPLC) fingerprints were established to obtain the main chemical components of THF. According to the network pharmacology databases, collect active targets of AHI and potential targets. Using interaction targets to construct a protein-protein interaction (PPI) network, followed by Gene Ontology (GO) and Kyoto Encyclopedia of Genes and Genomes (KEGG) enrichment analysis. Finally, the affinity between the core targets and the main active ingredients was verified by molecular docking. Next, verified network pharmacology predictions with animal experiments. Mice were treated with THF (20, 40, and 80 mg/kg) for 7 days, and then built an acute liver injury model (lipopolysaccharide [LPS], 10 mg/kg). Detecting the liver biochemical indices, observe the liver pathological changes, and verify the key signaling pathway targets. Results: HPLC showed that the main components of THF were quercetin and kaempferol. Seven active ingredients and 193 potential targets were screened, and 259 disease targets related to acute liver injury, quercetin, and kaempferol may be the main active ingredients in THF. PPI network analysis showed that tumor necrosis factor (TNF), interleukin-6 (IL-6), and tumor protein 53 (TP53) were potential targets of THF for the treatment of AHI. KEGG analysis showed that the phosphoinositide 3-kinase (PI3K)/protein kinase B (AKT) signaling pathway might be one of the main pathways in the treatment of AHI. The molecular docking results showed that active compounds both have strong binding activity with potential targets in PPI. In vivo experiments showed that THF could reduce the fibrosis and inflammation of liver tissue etc. Meanwhile, it could downregulate the alanine aminotransferase (ALT), aspartate aminotransferase (AST), IL-6, tumor necrosis factor alpha (TNF-α), C-reactive protein (CRP) levels, and the protein expressions of phosphorylated phosphoinositide 3-kinase (p-PI3K), phosphorylated protein kinase B (p-AKT), and the ratio of BCL2-associated X (BAX)/B-cell lymphoma-2 (BCL-2) in the liver tissue of the mice with acute liver injury and upregulate the level of interleukin-10 (IL-10). Conclusion: The treatment of acute liver injury with THF is characterized by multicomponents and multitargets, and its mechanism may be related to the alleviation of the inflammatory response, reduction of apoptosis, and regulation of the PI3K/AKT signaling pathway., Competing Interests: The authors declare no conflicts of interest., (Copyright © 2025 Lingling Li et al. Mediators of Inflammation published by John Wiley & Sons Ltd.)

Background: The traditional Chinese medicine Tetrastigma Hemsleyanum (TH) is employed in treating respiratory diseases; however, the aerial parts by which its total flavonoids alleviate acute lung injury (ALI) are still unknown. This study investigated the protective effect and mechanism of Tetrastigma Hemsleyanum flavonoids (THF) in lipopolysaccharide (LPS)-induced ALI in mice., Methods: Firstly, the total flavonoids from the above-ground part of TH were extracted. Subsequently, the composition of THF was analyzed using LC-MS. In vivo, the impact of THF on ALI mice was assessed through lung histopathology and the evaluation of various inflammatory factors' expression in mice. After treating RAW264.7 cells with THF in vitro, changes in inflammatory markers were examined upon LPS stimulation, and mRNA expression levels of inflammatory factors were detected using RT-qPCR. Finally, Western blot analysis was performed to determine TLR4/NF-κB pathway-associated proteins expression., Results: In summary, a total of 24 flavonoids have been identified in THF. In vivo and vitro results show that THF effectively reduces the damage caused by LPS inflammation by blocking the expression and release of inflammatory factors. THF alleviates inflammatory injury by modulating the TLR4/NF-KB pathway., Conclusion: The results suggest that flavonoids exhibit a potent anti-inflammatory effect and effectively mitigate LPS-induced injury both in vivo and in vitro. We suggested that these flavonoids exert their therapeutic effects by modulating the TLR4/NF-KB pathway. In conclusion, the development of THF is anticipated to represent a promising new pharmaceutical for treatingALI., Competing Interests: Declaration of competing interest The authors declare that they have no known competing financial interests or personal relationships that could have appeared to influence the work reported in this paper. The author is an Editorial Board Member/Editor-in-Chief/Associate Editor/Guest Editor for [Journal name] and was not involved in the editorial review or the decision to publish this article., (Copyright © 2024 Elsevier B.V. All rights reserved.)

Ampelopsin, a flavonoid with a wide variety of biological activities, has been proposed to be a potent antitumor agent. However, the mechanism by which Ampelopsin shows anti-breast cancer activity remains unclear. Therefore, this study will explore the mechanism of Ampelopsin's anti-breast cancer activity by culturing MDA-MB-231 and MCF-7 breast cancer cells. Cell Counting Kit-8 (CCK-8) method and plate cloning method were used to detect the proliferation inhibition of breast cancer cells. Fluorescence microscopy was used to detect mitochondrial membrane potential (MMP). 2',7'-Dichlorodihydrofluorescein diacetate (DCFH-DA) method was used to determine the content of intracellular reactive oxygen species (ROS). Hoechst 33258 staining was used to detect the apoptotic morphological changes. Transmission electron microscope was used to observe the mitochondrial structure. Western blot was used to detect the protein expression of Bax and Bcl-2. The results showed that Ampelopsin could significantly inhibit the proliferation of breast cancer cells, and promote cells apoptosis. In addition, the occurrence of apoptosis in breast cancer cells was associated with mitochondrial dysfunction, including the loss of mitochondrial membrane potential, the production of large amounts of reactive oxygen species, and the up-regulation of Bax/Bcl-2 expression. In conclusion, Ampelopsin-induced mitochondria damage leads to loss of mitochondria membrane potential, overproduction of ROS and activation of Bax, increasing mitochondria membrane permeability and ultimately inducing breast cell apoptosis. These findings provided a new perspective on the role of Ampelopsin in breast cancer prevention and treatment.

This study aimed to investigate the effects of the total flavonoids of Radix Tetrastigma (RTF) on inflammation-related hepatocellular carcinoma (HCC) development. Extracted RTF was diluted to different concentrations for subsequent experiments. HCC cells were cotreated with lipopolysaccharide (LPS) and RTF to investigate the effects of RTF on LPS-stimulated HCC cells. A CCK-8 kit was used to measure cell proliferation. Apoptosis was detected with a flow cytometer. Cell migration and invasion were quantified by wound healing and Transwell assays, respectively. The expression of TLR4 and COX-2 and activation of the NF-κB pathway were determined by Western blotting. Treatment with LPS significantly enhanced cell proliferation and decreased the apoptosis rate, while cell migration and invasion were notably upregulated. RTF suppressed the proliferation and invasion induced by LPS stimulation and promoted HCC cell apoptosis. The protein levels of Bax and cleaved caspase-3 were decreased and that of Bcl-2 was increased by LPS in HCC cells, which could be rescued by RTF. RTF significantly inhibited the LPS-induced expression of the proinflammatory mediators IL-6 and IL-8 in HCC cells. Mechanistically, with RTF treatment, the upregulated expression of TLR4 and COX-2 induced by LPS was obviously downregulated. Furthermore, the phosphorylation of NF-κB/p65 was significantly decreased in LPS-stimulated cells after supplementation with RTF. Our study suggests that RTF exerts a significant inhibitory effect on the LPS-induced enhancement of the malignant behaviors of HCC cells via inactivation of TLR4/NF-κB signaling. RTF may be a promising chemotherapeutic agent to limit HCC development and inflammation-mediated metastasis.

Objective: Tetrastigma hemsleyanum, a rare and endangered medicinal plant, has attracted much attention due to its immunoregulatory and hepatoprotective activities. This study aimed to evaluate the anti-inflammatory effects and underlying mechanisms of total flavonoids from T. hemsleyanum(TFT)on Con A-induced hepatitis in mice., Methods: TFT (1, 2 and 4 g/kg) and a positive control drug bifendate (200 mg/kg) were administered intragastrically to mice once daily for 10 consecutive days. On the 10th day, the model autoimmune of hepatitis was established by intravenous injection of Con A (20 mg/kg) 1 h after drug administration. Liver injury was assessed by serum levels of alanine amino transferase (ALT and AST) and histopathology 8 h after Con A injection. The levels of pro-inflammatory Th17 cytokines (IL-17, IL-6) and anti-inflammatory Treg cytokines (IL-10, TGF-β1) in serum were evaluated by ELISA, the levels of Th17 and Treg cells infiltrated into spleen were investigated by flow cytometry methods, and hepatic tissue transcription factor Foxp3 and RORγt mRNA were determined using quantitative real-time PCR., Results: Pretreatment with TFT and bifendate significantly reduced the serum levels of ALT and AST, and attenuated histopathological alterations in Con A-induced liver injury. With respect to samples treated with Con A alone, TFT and bifendate pretreatments differentially attenuated the increase of serum inflammatory factors interleukin (IL)-17 and IL-6 levels, the proportions of Th17 cells in spleen and the expression of RORγt in hepatic tissues. Meanwhile, TFT and bifendate pretreatments could enhance the percentage of Treg cells in spleen and the expression of Foxp3 in hepatic tissues, as well as the levels of transforming growth factor (TGF)-β1, IL-10 in serum., Conclusion: The anti-inflammatory effects of TFT was mediated by regulating Treg/Th17 immune homeostasis, which, therefore, suppressed the inflammatory immune response. This study provided scientific basis for the further researches and clinical applications of Tetrastigma hemsleyanum.

The main flavonoid components of Radix Tetrastigma (RTF) were extracted and identified by UPLC-TOF/MS. In vitro , RTF prevented inflammation in RAW 264.7 cells by suppressing morphological (both cell and nucleus) changes, and decreasing nitric oxide (NO), inducible nitric oxide synthase (iNOS), and cyclooxygenase-2 (COX-2) contents. Exposure to LPS also leads to oxidant damage, and RTF alleviated damage to mitochondria, decreased O 2 - accumulation, and restored the glutathione level. RTF intervention decreased the expression of c-Jun N-terminal kinase (JNK) and p38 phosphorylation, accompanied by downregulation of nuclear factor erythroid 2-related factor 2 (Nrf2) and forkhead box protein O1 (FoxO1). In vivo , aging of Caenorhabditis elegans (C. elegans) by paraquat (PQ) was observed through lifespan, lipofuscin, and enzyme analysis. RTF protected against damage in N2 worms but not in daf-16 mutants. Gene expression was further assessed, and p38/PMK-1 and Nrf2/SKN-1 expression in worms was suppressed by PQ, which was reversed by RTF treatment. Together, these results suggested that RTF could help ameliorate inflammation-induced damage through JNK, p38 and Nrf2 pathways.

Flavonoids are a ubiquitous multifunctional group of phenolics of paramount importance for the terrestrial plants involved in protection from biotic and abiotic stresses, color and chemical signaling and other functions. Deciphering of in situ absorption of foliar Flv is important but was thought to be impossible due to a strong overlap with other pigments, complex in situ chemistry of Flv and sophisticated leaf optics. We deduced in situ absorbance of foliar Flv and introduced a concept of specific absorbance spectrum indicative of each pigment group contribution to light absorption and provided a rationale for the choice of spectral bands for non-destructive assessment of Flv in leaves with variable content of other pigments including anthocyanins. Only a narrow band 400-430nm was suitable for Flv assessment, however the effect of other pigments remained substantial, so subtraction of their contribution was necessary. The devised leaf absorbance-based algorithm allowed estimating Flv with error below 21%. Absorption by Flv in plant tissues might extend into the blue and can be commensurate to that of chlorophylls and carotenoids. The potential capacity of Flv to shield the cell in situ from the visible light might be essential for assessments of high light stress tolerance of plants., (Copyright © 2017 Elsevier GmbH. All rights reserved.)

In this study, a rapid and sensitive analytical method was developed for the determination of 10 major compounds (procyanidin B1, catechin, procyanidin B2, rutin, isoquercitrin, kaempferol-3-O-rutinoside, astragalin, quercitrin, quercetin, and kaempferol) in Tetrastigma hemsleyanum by using ultra-performance liquid chromatography coupled with triple-quadrupole tandem mass spectrometry (UPLC-MS/MS) in multiple-reaction monitoring (MRM) mode. UPLC-MS/MS assay with negative ion mode was performed on a Waters CORTECS C18 (2.1 mm x 100 mm, 1.6 μm) with the mobile phase consisting of acetonitrile (A) and 0.1% aqueous formic acid (B) in gradient elution at a flow rate of 0.25 mL · min(-1) and the column temperature was set at 45 °C. Under the optimized chromatographic conditions, good separation for 10 target compounds were obtained including chiral isomer procyanidins B1 and B2 were completely separated within 8.5 min. Satisfactory linearity was achieved with wide linear range and fine determination coefficient (r > 0.996 6), the overall recoveries were ranged from 95.44%-110.40% with the RSD ranging from 2.37%-8.69%. It is the first report about simultaneous analysis of 10 major flavonoids components in Tetrastigma hemsleyanum by using UPLC-MS/MS method, which affords highly sensitive, specific, speedy and efficient method for quality control of Tetrastigma hemsleyanum

Objective: To develop a method for separation and quantitative determination of four flavonoids in Tetrastigma hemsleyanum., Methods: The Separation was performed on a Waters Preparative scale LC-MS autopurification system. Several spectral analyses, such as NMR,HR-MS and UV were used to identify the chemical structures. Quantitative assay was performed on a UHPLC Phenomenex Kinetex C18 column (100 mm x 4.6 mm, 2.6 µm) with the mobile phase consisting of acetonitrile( B) and water containing 0. 1% formic acid (A) in a gradient mode at a flow rate of 0.4 mL/min. The column temperature was at 30 °C and the optimum detection wavelength of DAD was set at 350 nm., Results: Four flavonoids were isolated from the root of Tetrastigma hemsleyanum, which were identified as rutin, isoquercitrin, kaempferol-3-O-rutinoside and astragalin. As to quantitative analysis, a good separation of four flavonoids with in 17.5 min, the linear range of rutin, isoquercitrin, kaempferol-3-O-rutinoside and astragalin was 0.283-11.32 µg/mL (r1 = 0.9998), 0.311-12.44 µg/mL (r2 = 0.9994), 0.277-11.08 µg/mL (r3 = 0.9995) and 0.103-2.06 µg/mL (r4 = 0.9990), respectively. The average recovery (n = 6) was 99.75% (RSD = 2.15%), 98.73% (RSD = 2.58%) ,98. 03% (RSD = 2.23%), and 97.62% (RSD = 1.95%), respectively., Conclusion: Four flavonoids are isolated from the root of Tetrastigma hemsleyanum for the first time, and the UHPLC method is simple, rapid and accurate, which can be used for quantitative analysis of multi-component of Tetrastigma hemsleyanum and provide a novel approach for evaluation of the quality of Tetrastigma hemsleyanum comprehensively.

Four new flavonoids including three C-glycosidic flavonoids, named tetrastigma A-D (1-4) and five known flavones (5-9) were isolated from the herbs of Tetrastigma obtectum (Wall.) Planch. The structures of 1-4 were elucidated by 1D- and 2D-NMR and HR mass spectrometric methods. Compound 1 caused significant enhancement in glucose consumption by insulin-resistant HepG2 cells compared with control cells. In addition, compound 1 stimulated phosphorylation of AMPK, which plays an important role in glycometabolism., (© 2013.)

Objective: To study the optimum extraction technology of total flavonoids and total triterpenoids from Tetrastigma planicaule and their antioxidant activity., Methods: Optimized the extraction of total flavonoids and total triterpenoids using an L9 (3(4)) orthogonal array design, and the antioxidant activity was extimated by FRAP assay, salicylicl acid assay and ABTS assay., Results: The best extraction conditions for total flavonoids from Tetrastigma planicaule were as follows: 70 degrees C of 70% ethanol ultrasound-assisted extracting for 1 h and extracting three times, and total triterpenoids was:70 degrees C of 60% ethanol microwave extracting for 5 min and extracting two times. Compared with the positive control samples VC and tea polyphenol, the activity of reducing Fe3+ antioxidant and scavenging ABTS + * of flavonoids from Tetrastigma planicaule was higher than that of tea polyphenol, but scavenging OH * was lower than theirs;, Conclusion: The method of using ultrasound-assisted extraction to extract total flavonoids and microwave extraction to extract total triterpenoids is the best, the extracts of Tetrastigma planicaule also shows certain antioxidative activity.

The interaction between bovine serum albumin (BSA) and the anticancer drug molecule ampelopsin (AMP) was investigated using fluorescence spectroscopy, circular dichroism (CD) spectra, and time-resolved spectra under simulated physiological conditions. Fluorescence data showed that the intrinsic fluorescence of BSA was strongly quenched by AMP in terms of a dynamic quenching process. Binding constants and binding sites were calculated. The thermodynamic parameters indicated that the hydrogen bonding and weak van der Waals force played a major role in the interaction. The site marker competitive experiments suggested that the binding site of AMP and BSA was probably located on site III. Based on the Förster's theory, the average binding distance between AMP and BSA was obtained (r=5.47nm). The binding of AMP and BSA leaded to conformational changes of BSA according to synchronous fluorescence spectra, CD data and mean fluorescence lifetime values., (Copyright © 2011 Elsevier B.V. All rights reserved.)

Chronic administration of myricetin (100 and 300 mg kg⁻¹, p.o., for 4 weeks) isolated from Vitis vinifera (Vitaceae) ameliorated hypertension and oxidative stress induced by deoxycorticosterone acetate (DOCA)-salt in rats. Myricetin treatment reduced systolic blood pressure, vascular reactivity changes and reversed the DOCA-induced increase in heart rate. Urinary sodium excretion was significantly decreased in animals treated with myricetin compared to the DOCA group when measured by flame photometer. The cumulative concentration response curve of serotonin (5-HT) and angiotensin II (Ang II) were shifted towards the right in rats treated with myricetin using the isolated rat fundus strip and ascending colon, respectively. Increased levels of thiobarbituric acid reactive substances and decreased levels of superoxide dismutase, catalase and reduced glutathione in the heart tissue were observed in animals treated with DOCA, which were reversed by myricetin. Thus, myricetin shows antihypertensive and antioxidant properties in the DOCA model of hypertension.

Objective: To detect the in vitro total phenolics, flavonoids contents and antioxidant activity of essential oil, various organic extracts from the leaves of tropical medicinal plant Tetrastigma from Sabah., Methods: The dry powder leaves of Tetrastigma were extracted with different organic solvent such as hexane, ethyl acetate, chloroform, butanol and aqueous methanol. The total phenolic and total flavonoids contents of the essential oil and various organic extracts such as hexane, ethyl acetate, chloroform, butanol and aqueous ethanol were determined by Folin - Ciocalteu method and the assayed antioxidant activity was determined in vitro models such as antioxidant capacity by radical scavenging activity using α, α-diphenyl- β-picrylhydrazyl (DPPH) method., Results: The total phenolic contents of the essential oil and different extracts as gallic acid equivalents were found to be highest in methanol extract (386.22 mg/g) followed by ethyl acetate (190.89 mg/g), chloroform (175.89 mg/g), hexane (173.44 mg/g), and butanol extract (131.72 mg/g) and the phenolic contents not detected in essential oil. The antioxidant capacity of the essential oil and different extracts as ascorbic acid standard was in the order of methanol extract > ethyl acetate extract >chloroform> butanol > hexane extract also the antioxidant activity was not detected in essential oil., Conclusions: The findings show that the extent of antioxidant activity of the essential oil and all extracts are in accordance with the amount of phenolics present in that extract. Leaves of Tetrastigma being rich in phenolics may provide a good source of antioxidant., (Copyright © 2011 Hainan Medical College. Published by Elsevier B.V. All rights reserved.)

Objective: The feasibility of producting flavonoids from callus of Tetrastigma hemsleyanum was investigated through callus induction, proliferation, differentiation and determination of flavonoids., Methods: The leaves of sterile plantlet, leaves and stems of wild plants were used as explants to induce calluses; The root tuber, the leaves and calluses were selected for the determination of flavonoids. With ethanol as the solvent, the total flavonoids were extracted by ultrasonic and determined by spectrophotometry at 500 nm after stained with NaNO2-Al(NO3) 3., Results: The optimum medium where the calluses were induced was 2/3MS +2.0 mg/L 6-BA +2.0 mg/L NAA; MS +2.0 mg/L 6-BA +2.0 mg/L NAA was the optimum for callus proliferation; for callus root differentiation, the optimum medium was 1/2MS +1.0 mg/L 6-BA +1.0 mg/L NAA. The content of total flavonoids was 31.121 mg/g in root tuber, 12.830 mg/g in leaves while it was up to 18.088 mg/g in calluses., Conclusion: The calluses had a high level of total flavonoids, it could produce flavonoids through the calluses induced by Tetrastigma hemsleyanum in a large scale. In that case, the pressing requirement in medical market will be solved.

A facile method based on high-performance liquid chromatography coupled with electrospray ionization tandem mass spectrometry (HPLC/(-)ESI-MSn) has been established for the analyses of polyphenol compounds in the root and stems of Parthenocissus laetevirens. Two characteristic fragments [C3O2 (68 Da) and C2H2O (42 Da)] were utilized for the structural identification of polyphenols. Based on the reference standards, the fragment C3O2 was presented when the compound possessed a 2,3-dihydro-1H-indene-4, 6-diol moiety. Meanwhile, the C2H2O fragment (42 Da) yielded from the resorcinol ring was confirmed by resveratrol and three synthesized compounds identified as (E)-5-styrylbenzene-1,3-diol, (E)-4-styrylphenol and (E)-4-(3,4,5-trimethoxystyryl)phenol. FTICR-MSn was performed to further confirm the structures of the fragments. Overall, 15 polyphenol compounds were characterized. Three polyphenol compounds were initially and tentatively characterized from P. laetevirens for the first time, and one was proposed as a novel compound. Furthermore, a pair of stereoisomers was readily distinguished by breakdown curves, and the trans-, cis-isomers could be identified by HPLC/DAD-UV spectra., (Copyright (c) 2009 John Wiley & Sons, Ltd.)

Upright counter-current chromatography (CCC) with a two-phase solvent system composed of n-hexane-ethyl acetate-methanol-water (1:2:1:2, v/v/v/v) was applied to the isolation and purification of polyphenols from the roots of Parthenocissus laetevirens. Two cis-trans isomeric resveratrol dimers - quadrangularin A and parthenocissin A - were obtained from the crude sample in a one-step separation, with purities of 95.4 and 97.6%, respectively, as determined by HPLC. The structures of these two compounds were identified by (1)H NMR and (13)C NMR. Furthermore, their antioxidant activities were determined by beta-carotene bleaching assay. The antioxidant activities of quadrangularin A and parthenocissin A were higher than that of vitamin C in this model.