CELL BIOCHEMISTRY AND FUNCTION
·
2024
·Vol. 42
·期 8
·e70015
·
IF 2.8
Yang Yu,Tianchan Zhang,Xin Li,Tianyang Yu,Fanci Meng,Yifeng Luan,Huifang Cong,Xiuhong Wu
Perimenopausal syndrome is a significant issue that disturbs women's metabolism, mood and quality of life. Apigenin (4′,5,7-trihydroxyflavone) is a natural flavonoid that exhibits antioxidant, anti-inflammatory and anticancer effects. The present study aims to investigate the effect of apigenin on perimenopausal syndrome by combining bioinformatics analysis with in vivo experiments. The mouse model with perimenopausal syndrome was established using 4-vinylcyclohexene diepoxide (VCD) treatment. Apigenin alleviated VCD-induced disorder of estrous cycle and shrinkage of ovarian tissue. The reduction of anti-Muller hormone and the increase of follicle stimulation hormone and luteinizing hormone triggered by VCD were reversed by apigenin in a dose-dependent manner. Apigenin suppressed the VCD-induced decrease of primordial, primary, secondary and antral follicle number in ovarian tissue. Oxidative stress in ovarian tissue was activated by VCD treatment through increasing the reactive oxygen species production. High concentration of apigenin significantly reversed the alteration induced by VCD. Apigenin alleviated VCD-induced cell apoptosis through regulating Bax, Bcl-2, cleaved PARP1 and caspase-3. Furthermore, the phosphorylation of AKT and FOXO3a was inhibited by VCD and activated by apigenin in a dose-dependent manner. Collectively, apigenin effectively mitigates the ovarian dysfunction through suppressing oxidative stress and apoptosis via the AKT/FOXO3a signaling pathway. Summary Perimenopausal syndrome characterized by endocrine disorders, and hormone disorders has caused physical and mental damage to the majority of women. This study aims to explore a safe and effective method for perimenopausal syndrome treatment. Apigenin is a natural flavonoid that has protective effects on ovary, while the effect and mechanism of apigenin on perimenopausal syndrome is still unclear. This study's principal finding was that apigenin alleviated the estrous cycle disorder, follicle development inhibition and hormone level disorder in model with perimenopausal syndrome. Additionally, apigenin suppressed oxidative stress and apoptosis via activating the AKT/FOXO3a signaling pathway in the ovarian tissue of perimenopausal mice model. This work provides an effective approach for the remission and treatment of perimenopausal syndrome.
研究领域:
药理学
·
内分泌学
·
妇科学
·
生物信息学
·
分子生物学
✓ 已验证
产品关联
DOI
PubMed
高影响因子
Journal of Inorganic and Organometallic Polymers and Materials
·
2024
·
IF 3.9
Pang Wanyu,Gao Yali,Chang Xile,Du Guodong,Hu Zhiyong,Hu Tuoping,Ma Xuemei
An ultra-sensitive paper-based sensor for the rapid and specific detection of apigenin in Scutellaria barbata D. Don was developed. The construction process of the proposed apigenin sensor was to grow ZIF-8 in situ with MXene as a template on carbon paper (CP) electrode. The MXene with excellent conductivity and ZIF-8 with porous structure showed synergistic effect in promoting electron transfer and increasing the number of binding sites, thus providing a highly sensitive detection for apigenin. Under optimal conditions, the sensor showed an excellent linear relationship in the range of 0.01 to 10 µM, with a detection limit of 2.6 nM. This study not only constructed a new sensing platform for sensitive detection of apigenin, but also provided a new method for the detection of apigenin in Scutellaria barbata D. Don, which was of great significance for promoting the construction of an electrochemical sensor for apigenin.
研究领域:
分析化学
·
植物化学
·
电化学传感器
✓ 已验证
产品关联
DOI
高影响因子
Oncotarget
·
2016
·
IF 5.008
Yuan Qin,Dong Zhao,Hong-gang Zhou,Xing-hui Wang,Wei-long Zhong,Shuang Chen,Wen-guang Gu,Wei Wang,Chun-hong Zhang,Yan-rong Liu,Hui-juan Liu,Qiang Zhang,Yuan-qiang Guo,Tao Sun,Cheng Yang
Apigenin is a naturally occurring compound with anti-inflammatory, antioxidant, and anticancer properties. In this study, we investigated the effects of apigenin on migration and metastasis in experimental human hepatocellular carcinoma (HCC) cell lines in vitro and in vivo . Apigenin dose-dependently inhibited proliferation, migration, and invasion by PLC and Bel-7402 human HCC cells. It also suppressed tumor growth in PLC cell xenografts without altering body weight, thereby prolonging survival. Apigenin reduced Snai1 and NF-κB expression, reversed increases in epithelial-mesenchymal transition (EMT) marker levels, increased cellular adhesion, regulated actin polymerization and cell migration, and inhibited invasion and migration by HCC cells. Apigenin may therefore inhibit EMT by inhibiting the NF-κB/Snail pathway in human HCC.
研究领域:
肿瘤学
·
分子生物学
·
药理学
✓ 已验证
产品关联
DOI
PubMed
高影响因子
FOOD CHEMISTRY
·
2016
·
IF 4.052
Zhiqiang Xiong,Wei Liu,Lei Zhou,Liqiang Zou,Jun Chen
It has been revealed that some polyphenols can prevent enzymatic browning caused by polyphenoloxidase (PPO). Apigenin, widely distributed in many fruits and vegetables, is an important bioactive flavonoid compound. In this study, apigenin exhibited a strong inhibitory activity against PPO, and some reagents had synergistic effect with apigenin on inhibiting PPO. Apigenin inhibited PPO activity reversibly in a mixed-type manner. The fact that inactivation rate constant ( k ) of PPO increased while activation energy ( E a ) and thermodynamic parameters (Δ G , Δ H and Δ S ) decreased indicated that the thermosensitivity and stability of PPO decreased. The conformational changes of PPO were revealed by fluorescence emission spectra and circular dichroism. Atomic force microscopy observation suggested that the dimension of PPO molecules was larger after interacting with apigenin. Moreover, computational docking simulation indicated that apigenin bound to PPO and inserted into the hydrophobic cavity of PPO to interact with some amino acid residues.
研究领域:
生物化学
·
食品科学
·
分子生物学
·
酶学
✓ 已验证
产品关联
DOI
PubMed
高影响因子
BIOMEDICINE & PHARMACOTHERAPY
·
2023
·
IF 7.5
Chang Liu,Xiao Guo,Yutong Chen,Meijun Zhao,Shuai Shi,Zheng Luo,Jian Song,Zhihong Zhang,Wenchuang Yang,Keyi Liu
Prolonged exposure to UV light can lead to photo-ageing of the skin. Therefore, the development and application of anti-photoaging drugs is urgent. In this study, we co-loaded apigenin (Apn) and doxycycline (Doc), a broad-spectrum inhibitor of matrix metalloproteinases (MMPs), into flexible liposomes to exert anti-photoaging effects by combating oxidative stress, anti-inflammation, reducing the activation of MMPs and preventing collagen loss. The results showed that we prepared a flexible liposome (A/ D -FLip) containing Apn and Doc. Its appearance, particle size and Zeta potential were normal and it had good encapsulation efficiency, drug loading, in vitro release and transdermal efficiency. In cellular experiments, A/ D -FLip could inhibit oxidative stress damage, reduce inflammatory factors and decrease the activation of MMPs in Human immortalized keratinocytes (HaCaT) cells; in animal experiments, A/ D -FLip could inhibit skin damage and reduce skin collagen loss by decreasing the activation of MMPs, thus inhibiting skin photoaging in mice. In conclusion, A/ D -FLip has good anti-photoaging effects and it has the potential to become an effective skin care product or drug against UV damage and skin photoaging in the future.
研究领域:
药剂学
·
皮肤科
·
美容护肤品
✓ 已验证
产品关联
DOI
PubMed
高影响因子
Frontiers in Pharmacology
·
2020
·
IF 4.225
Zhang Jiaqi,Liang Xiaoqiang,Li Jiacheng,Yin Hao,Liu Fangchen,Hu Cheng,Li Ling
Overuse of acetaminophen (APAP) is a major cause of drug-induced liver failure at the clinics. Apigenin (API) is a natural flavonoid derived from Matricaria chamomilla. The aim of the present study was to investigate the amelioration function of API in APAP-induced hepatotoxicity both in vitro and in vivo and investigate its potential mechanisms. Analysis results of the activities of serum alanine and aspartate aminotransferases (ALT and AST), malondialdehyde, myeloperoxidase (MPO), and reactive oxygen species (ROS) demonstrated therapeutic effects of API. MTT assay results revealed that API attenuated APAP and its metabolic product, N-acetyl-p-benzoquinone imine (NAPQI) induced cytotoxicity in a dose-dependent manner in human liver cells, L-02 cells. Subsequently, metabolomic results of cells and serum analyses demonstrated an aberrant level of carnitine palmitoyltransferase I (CPT1A). We established that API stimulated CPT1A activity in mice liver tissues and L-02 cells. Molecular docking analyses revealed potential interaction of API with CPT1A. Further investigation of the role of CPT1A in L0-2 cells revealed that API reversed cytotoxicity via the AMP-activated protein kinase (AMPK)/GSK-3β signaling pathway and compound C, which is a selective AMPK inhibitor, inhibited activation of CPT1A induced by API. API was bound to the catalytic region of AMPK as indicated by molecular docking results. In addition, compound C suppressed nuclear translocation of nuclear factor erythroid 2–related factor 2 (NRF2) that is enhanced by API and inhibited the antioxidative function of API. In summary, the study demonstrates that API attenuates APAP-induced hepatotoxicity by activating the AMPK/GSK-3β signaling pathway, which subsequently promotes CPT1A activity and activates the NRF2 antioxidant pathway.
研究领域:
药理学
·
毒理学
·
细胞生物学
·
分子生物学
✓ 已验证
DOI
PubMed
高影响因子
MOLECULES
·
2026
·Vol. 31
·期 16
·2768
·
IF 5.1
Chenliang Li,Lijin Xiao,Wei Wu,Lingyang Kong,Shuyuan Yue,Zhijie Zhan,Jiao Xu,Wei Ma
Apigenin (API) is a flavonoid compound widely distributed in nature. The global prevalence of asthma is increasing year by year, influenced by various factors and difficult to cure completely, and new drugs and therapies are constantly emerging. Although API is a low-toxicity flavonoid compound, its poor water solubility and low bioavailability present limitations in the treatment of asthma. In this study, the structure of API was chemically modified by introducing acyl and alkyl groups while preserving its original structure. The structures were identified using FT-IR,1H-NMR and13C-NMR spectroscopy, yielding derivatives (A–J). To further investigate the effects of structural modifications on API’s biological activity, an ovalbumin (OVA)-induced asthma model was established in mice to evaluate the antioxidants’ activity. Hematoxylin-eosin staining was used to observe pathological changes in lung tissue, and oxidative stress-related parameters, including ROS, SOD, and MDA, were measured to assess the derivatives’ protective effects against oxidative damage. The results showed that the 10 synthetic derivatives exhibited varying degrees of oxidative stress during treatment. Compared with the model group, the API derivative treatment group significantly reduced ROS and MDA levels and increased SOD activity. Moreover, treatment with the compounds reduced the levels of pro-inflammatory cytokines, including TNF-α, IL-6, and IL-1β, and decreased serum IgE levels. Histopathological examination further demonstrated that the compounds alleviated inflammatory cell infiltration and tissue damage in the lungs. Structure-activity analysis indicated that, among the 10 derivatives, the tri-substituted API derivatives exhibited superior antioxidant activity compared to the di-substituted API derivatives. By modifying the chemical structure of API, its antioxidant activity in OVA-induced bronchial asthma was significantly enhanced. 5,7,4′-O-triethyl API and 5,7,4′-O-triacetyl API demonstrated therapeutic effects comparable to those of dexamethasone and show promise as lead compounds for the development of novel asthma treatments.
✓ 已验证
产品关联
DOI
高影响因子
FOOD CHEMISTRY
·
2024
·
IF 8.5
Yaqi Liu,Chao Yuan,Bo Cui,Meng Zhao,Bin Yu,Li Guo,Pengfei Liu,Yishan Fang
In an effort to improve the application performance of apigenin, β-cyclodextrin metal–organic frameworks (BCDMOFs) known as porous materials were used to encapsulate apigenin via an innovative pH-adjusted method. The embedment efficiency had a significant positive pH dependence, reaching a maximum of 79.2 % ± 1.2 % at pH 12. Scanning electron microscopy, X-ray diffraction, Fourier transform infrared spectroscopy, and thermogravimetric analysis demonstrated formation of apigenin/BCDMOFs composites, and exposure of BCDMOFs pores facilitated high embedment efficiency. Storage stability experiment and kinetic analysis showed degradation of apigenin/BCDMOFs composites was less than that of apigenin alone. Apigenin stability was increased by approximately 18 % after 7 days. BCDMOFs effectively encapsulated and controlled the release of apigenin, and the composites exhibited improved application performance in vitro .
研究领域:
药物化学
·
材料科学
·
食品科学
✓ 已验证
DOI
PubMed
高影响因子
ACS Applied Nano Materials
·
2024
·
IF 5.3
Zhi-Hang He,Han-Xiao Tang,Yan-Zheng Pan,Min Cen,Zhi-Juan Zhang
The oxygen consumption during chemodynamic therapy (CDT) can lead to severe cellular hypoxia, resulting in an increase in the hypoxia inducible factor-1α (HIF-1α) level, which hinders the effectiveness of CDT and induces tumor metastasis. Here, we propose a strategy of synergistic therapy between CDT and the HIF-1α inhibitor to avoid the limitations of CDT and reduce the risk of metastasis. Herein, based on the coordination between Fe3+ and apigenin (API, HIF-1α inhibitor), we constructed a hyaluronic acid (HA)-modified API-Fe nanoparticles (AF@HA NPs) for synergetic chemotherapy and glutathione (GSH)-activated self-enhancing CDT. AF@HA NPs have high drug loading capacity, stability, and biocompatibility. Furthermore, the overexpressed GSH in cancer cells can reduce Fe3+ to Fe2+, weakened the coordination between API and Fe, and promoted the release of API for chemotherapy. Fe2+ could react with endogenous H2O2 to generate hydroxyl groups for CDT. In addition, the released API could inhibit the expression of HIF-1α and increase the sensitivity of cells to reactive oxygen species (ROS), thereby achieving a synergistic effect between self-enhancing CDT and chemotherapy. The results of in vitro and in vivo experiments indicated that AF@HA NPs could effectively inhibit tumor growth and suppress the lung metastasis of tumor cells.
研究领域:
纳米技术
·
癌症治疗
·
药理学
·
生物医学工程
·
分子生物学
✓ 已验证
产品关联
DOI
高影响因子
CHINESE JOURNAL OF POLYMER SCIENCE
·
2022
·Vol. 40
·期 10
·1259-1268
·
IF 3.815
Nabipour Hafezeh,Wang Xin,Song Lei,Hu Yuan
In this work, apigenin was chosen as a raw material to synthesize a novel epoxy monomer (DGEA), while the bio-based epoxy resin was further obtained after curing with 4,4′-diaminodiphenylmethane (DDM). The control samples were prepared by curing diglycidyl ether of bisphenol A (DGEBA) with DDM. The non-isothermal differential scanning calorimeter (DSC) method was utilized to further investigate the curing behavior and curing kinetics of the DGEA/DDM system. Despite no flame retardant active elements, the DGEA/DDM thermoset still exhibited exceptional anti-flammability. Specifically, the DGEA/DDM thermoset reached a V-0 rating in the UL-94 test and owned a high limiting oxygen index (LOI) value of 37.0%, while DGEBA/DDM resins were consumed completely in the vertical combustion test with a low LOI of 23.0%. Furthermore, the microscale combustion calorimetry (MCC) results manifested that compared with DGEBA/DDM resins, both PHRR and THR values of the DGEA/DDM resins were dropped by 84.0% and 57.6%, respectively. Additionally, the DGEA/DDM resin also presented higher storage modulus and tensile strength compared with DGEBA/DDM one. Particularly, in contrast with that of the cured DGEBA/DDM one (156 °C), the DGEA/DDM thermoset displayed an extremely high glass transition temperature (232 °C). This study breaks new ground on how to produce bio-based monomers with aromatic structures and achieve high-performance thermosetting polymers.
研究领域:
材料科学
·
化学工程
✓ 已验证
产品关联
DOI
高影响因子
INTERNATIONAL JOURNAL OF PHARMACEUTICS
·
2023
·
IF 5.8
Chang Liu,Xiaojun Zhang,Huiying Yang,Meijun Zhao,Yanhong Liu,Risheng Zhao,Ziqing Li,Meng Sun
Ischemic heart disease (IHD) is a cardiac disorder in which myocardial damage occurs as a result of myocardial ischemia and hypoxia. Evidence suggests that oxidative stress and inflammatory responses are critical in the development of myocardial ischemia. Therefore, the combination of antioxidant and anti-inflammatory applications is an effective strategy to combat ischemic heart disease. In this paper, polyethylene glycol (PEG)-modified cationic liposomes were used as carriers to deliver apigenin (Apn) with small interfering RNA (siRNA) targeting the receptor for glycosylation end products (RAGE) (siRAGE) into cardiomyocytes to prevent myocardial ischemic injury through antioxidant and anti-inflammatory effects. Our results showed that we successfully prepared cationic PEG liposomes loaded with Apn and siRAGE (P-CLP-A/R) with normal appearance and morphology, particle size and Zeta potential, and good encapsulation rate, drug loading and in vitro release degree. In vitro , P-CLP-A/R was able to prevent oxidative stress injury in H9C2 cells, downregulate the expression of RAGE, reduce the secretion of cellular inflammatory factors and inhibit apoptosis through the RAGE/NF-κB pathway; In vivo , P-CLP-A/R was able to prevent arrhythmia and myocardial pathological injury, and reduce apoptosis and the area of necrotic myocardium in rats. In conclusion, P-CLP-A/R has a protective effect on myocardial ischemic injury and is expected to be a potential drug for the prevention of ischemic heart disease in the future.
✓ 已验证
DOI
PubMed
高影响因子
Frontiers in Immunology
·
2026
·
IF 7
Haiyu Shen,Guoguo Zhi,Zihao Li,Xueqiao Yan,Zhirui Du,Shaoyang Zhang,Ruichen Yang,Xiuying Ma,Huijuan Liu,Funeng Geng,Baojie Li
BackgroundFractures are common yet lack effective pharmacological treatments. Apigenin, a natural flavone, has anti-inflammatory and pro-osteogenic effects. Here, we examined its impact on fracture healing—a multistep process involving hematoma formation, soft callus formation (endochondral differentiation), hard callus formation (osteogenic differentiation), and bone remodeling—and investigated the underlying mechanisms.MethodsFemoral fracture and calvarial injury models were established to evaluate the effects of apigenin. Local apigenin treatment was initiated at postoperative time points to compare the impact of administration timing. Fracture healing was assessed by radiography, micro-CT, histological analysis, and immunostaining. In vitro cultures were performed to examine the effects of apigenin on mesenchymal stem cell (MSC) differentiation. Quantitative PCR, Western blotting, RNA sequencing, and flow cytometry were used to evaluate inflammatory responses and chondrogenic and osteogenic differentiation. Ikbkb knockdown and BAY 11–7082 treatment were used to examine the involvement of IKKβ/NF-κB signaling. Molecular docking and molecular dynamics simulations were performed to investigate the potential interaction between apigenin and IKKβ, which was examined by cellular thermal shift assay (CETSA).ResultsApigenin significantly improved fracture healing when treatment was initiated on postoperative day 5, whereas treatment initiated on day 1 showed no clear therapeutic effect. Apigenin reduced inflammatory responses in the fracture callus and suppressed NF-κB signaling. BAY 11–7082 produced effects similar to those of apigenin in the femoral fracture model, and combined treatment did not produce a clear additional benefit. In BMSCs, apigenin promoted chondrogenic differentiation and attenuated the suppression of chondrogenic markers under inflammatory conditions, whereas its effects on osteogenic differentiation were less consistent. Ikbkb knockdown also enhanced chondrogenic differentiation, and addition of apigenin after Ikbkb knockdown produced no further clear increase. Molecular docking, molecular dynamics simulations, and CETSA provided supportive evidence for a potential interaction between apigenin and IKKβ.ConclusionsThrough modulation of IKKβ/NF-κB signaling, apigenin acts on both inflammatory responses and MSC differentiation to enhance fracture healing. The therapeutic effect was most evident when treatment was initiated on postoperative day 5, during the transition from inflammation to cartilage formation. These findings suggest that appropriately timed apigenin treatment may represent a potential strategy for improving fracture repair.
✓ 已验证
DOI
高影响因子
危险品化学品经营许可证（带存储）