Nanoscience and Nanotechnology Letters
·
2020
·Vol. 12
·期 8
·1022-1029
·
IF 1.128
Liu Ming,Lin Chen,Huang Xiaoqing,Lin Yuxiang
Natural flavonoid formononetin (FN) has anticancer effects, but the hydrophobic structure, characteristics of the short half-life in vivo, limiting its clinical wide-ranging application. In this study, FN loaded Pluronic (PF)@folic acid (FA) micelles (FN-PF@FA), were prepared
to improve the solubility, bioavailability and targeting. FA coupling PF was prepared by carbodiimide crosslinker chemical method, FN-PF@FA micelles were prepared by modified film hydration method, and compared the antitumor activity of FN loaded micelles with free FN In Vitro. The
spherical smooth surface of FN-PF@FA micelles had smaller particle size (112.3±5.3 nm), high encapsulation efficiency (86.14±2.68%), high negative zeta potential (-25.8±0.57 mV), low critical concentration CMC (0.03 mg/mL), and better sustained release profile. In addition,
FN-PF@FA micelles have a positive targeting effect on oral squamous cell carcinoma cells (SCC3). In 48 hours, the growth inhibition of 50% (GI50) was 28.6±1.2 μg/mL for FN and 17.4±0.78 μg/mL for FN-PF, the dose dropped by nearly 38.46%. In addition, the GI50
value of FN-PF@FA was 9.5±0.3 μg/mL, 66.43% lower than FN and 44.83% lower than FN-PF. Furthermore, the laser scanning confocal microscopy revealed that the conjugation of FA significantly improves the active targeting ability of micelles. FN-PF@FA micelles have the potential
to target the release of anticancer drugs with higher bioavailability, further provides a new avenue for the application of traditional Chinese medicine extract in oral malignant tumor.
研究领域:
药学
·
肿瘤学
·
纳米技术
·
药物递送系统
✓ 已验证
DOI
高影响因子
MEDIATORS OF INFLAMMATION
·
2018
·
IF 3.549
Dacheng Wu,Keyan Wu,Qingtian Zhu,Weiming Xiao,Qing Shan,Zhigang Yan,Jian Wu,Bin Deng,Yan Xue,Weijuan Gong,Guotao Lu,Yanbing Ding
Formononetin is a kind of isoflavone compound and has been reported to possess anti-inflammatory properties. In this present study, we aimed to explore the protective effects of formononetin on dextran sulfate sodium- (DSS-) induced acute colitis. By intraperitoneal injection of formononetin in mice, the disease severity of colitis was attenuated in a dose-dependent manner, mainly manifesting as relieved clinical symptoms of colitis, mitigated colonic epithelial cell injury, and upregulations of colonic tight junction proteins levels (ZO-1, claudin-1, and occludin). Meanwhile, our study found that formononetin significantly prevented acute injury of colonic cells induced by TNF-α in vitro, specifically manifesting as the increased expressions of colonic tight junction proteins (ZO-1, claudin-1, and occludin). In addition, the result showed that formononetin could reduce the NLRP3 pathway protein levels (NLRP3, ASC, IL-1β) in vivo and vitro, and MCC950, the NLRP3 specific inhibitor, could alleviate the DSS-induced mice acute colitis. Furthermore, in the foundation of administrating MCC950 to inhibit activation of NLRP3 inflammasome, we failed to observe the protective effects of formononetin on acute colitis in mice. Collectively, our study for the first time confirmed the protective effects of formononetin on DSS-induced acute colitis via inhibiting the NLRP3 inflammasome pathway activation.
研究领域:
药理学
·
免疫学
·
胃肠病学
✓ 已验证
产品关联
DOI
PubMed
高影响因子
MATERIALS & DESIGN
·
2025
·
IF 7.9
Jingmei Huang,Ning Wang,Xiaoxiao Huang,Shihong Huang,Guoliang Xie,Jianfeng Zhang,Zhengzhao Li
Traumatic brain injury (TBI) is characterized by oxidative stress, neuroinflammation, and microglial dysregulation, leading to secondary neuronal damage. Here, we constructed coordination polymer nanoenzymes (Fe-FN CPs) with multiple enzyme-like activities and favorable biocompatibility. In vitro, Fe-FN CPs suppressed ROS accumulation, reduced pro-inflammatory cytokine release, and promoted microglial polarization toward the M2 phenotype. In vivo, Fe-FN CPs enhanced antioxidant defense, alleviated mitochondrial damage and cerebral edema, restored blood–brain barrier integrity, and improved cognitive performance. Mechanistically, Fe-FN CPs achieved dual regulation by inhibiting pro-inflammatory M1 polarization while promoting anti-inflammatory M2 polarization. These findings demonstrate that Fe-FN CPs exert potent neuroprotective effects and provide a promising nanomedicine strategy for TBI therapy based on natural active compounds.
✓ 已验证
产品关联
DOI
高影响因子
JOURNAL OF ETHNOPHARMACOLOGY
·
2026
·
IF 6.8
Xiaotian Gao,Xiaoniao Chen,Luying Qiao,Yingtao Zhang,Xiaoling Liu,Sifan Yang,Yan Zheng,Xun Chen,Xu Wang,Ran Liu,Zheyi Dong,Qian Wang,Quan Hong
Ethnopharmacological relevance Formononetin (FMN) is a natural isoflavone found in several medicinal plants. Its effects on diabetic retinal and renal microvascular injury and EGR1/VEGF-related endothelial responses remain incompletely defined. Aim of the study To assess whether FMN attenuates early diabetes-associated retinal and renal injury and whether EGR1 is involved. Materials and methods Alloxan-induced diabetic rabbits received FMN orally at 25 mg/kg/day from Week 4 to Week 16 after pretreatment renal and OCT/OCTA assessment. Renal function, histopathology, retinal flat mounts, longitudinal OCTA, and tissue EGR1/VEGF expression were examined. High-glucose-treated retinal, renal microvascular, and umbilical vein endothelial cells were used for functional assays. EGR1 overexpression, VEGFA promoter reporter assays, SPR, docking, and molecular dynamics simulations were also performed. Results FMN lowered serum creatinine, blood urea nitrogen, and urinary albumin-to-creatinine ratio, and reduced renal histopathological injury. It also attenuated retinal capillary loss, retinal thinning, and OCTA abnormalities despite persistent hyperglycemia. Retinal and renal tissues from FMN-treated rabbits showed lower EGR1 and VEGF expression. In endothelial cells, FMN reduced EGR1 and VEGF expression, abnormal tube formation, permeability, invasion, ROS, and inflammatory mediator release, while increasing NO-related signals. EGR1 overexpression weakened several effects and increased VEGFA promoter activity through the predicted EGR1-binding sequence. SPR detected FMN–EGR1 binding with a K_D of 3.245 μM. Computational analyses provided structural context. Conclusions FMN attenuated early diabetes-associated retinal and renal injury and was linked to EGR1/VEGF-related endothelial responses. The data support EGR1 involvement but do not establish it as the sole target or mediator of FMN.
✓ 已验证
产品关联
DOI
高影响因子
JOURNAL OF EVOLUTIONARY BIOCHEMISTRY AND PHYSIOLOGY
·
2026
·Vol. 62
·期 3
·608-621
·
IF 0.5
Xu Haoting,Gao Zhengwen,Lu Yan,Ge Xin,Jia Di,Zhou Quanbin
Pressure ulcers (PUs) represent a significant clinical challenge
in immobilized patients and the aging population, characterized
by persistent inflammation, impaired tissue regeneration, and dysregulated healing
processes. In this study, we systematically investigated the therapeutic
potential of formononetin (FMN) extracted from traditional Chinese
medicine in preventing and treating PUs. Experimental results from
the magnetically induced ischemia-reperfusion PUs rat model demonstrated
that FMN intervention accelerated wound healing rates, with a clear
dose-response relationship observed. Histopathological examination
(H&E staining) revealed substantial improvements in tissue architecture, including
enhanced epidermal integrity and reduced inflammatory infiltration.
Moreover, the expression of pro-inflammatory cytokines TNF-α, IL-6,
and IL-1β in the wound tissue was reduced. FMN inhibited apoptosis
by down-regulating the expression of cleaved caspase-3 and Bax in
pressure ulcer tissues and up-regulating the expression of Bcl-2.
In addition, FMN promotes collagen deposition and expression of
α-SMA and collagen I in wound tissue, thereby improving tissue remodeling.
Integrated bioinformatic and Western blot validation identified simultaneous
regulation of NF-κB and PI3K-Akt pathways as the core mechanism.
These results reveal that FMN may facilitate PUs healing through dual
mechanisms, suppressing inflammation and apoptosis via NF-κB inhibition,
and promoting cell survival and tissue repair via PI3K-Akt activation. This
suggests that FMN has the potential to be a drug for the preventive
and therapeutic effects of PUs and lays the foundation for the clinical
development of FMN-based treatment options.
✓ 已验证
DOI
高影响因子
Chinese Herbal Medicines
·
2026
·
IF 11.2
Aifen Liu,Jingyan Hu,Weili Yu,Chuanyu Cang,Chuanjing Shi,Xi Wang,Rui Wang,Xuanwei Cai,Fengbo Zhao,Lei Zhang
Objective Polycystic ovary syndrome (PCOS) is an endocrine and metabolic disorder characterized by ovulatory dysfunction. Formononetin (FMN), a bioactive compound derived from leguminous plants, including Glycyrrhiza uralensis , Trifolium pratense , and Astragalus membranaceus , exhibits anti-inflammatory and anti-fibrotic properties. This study aimed to evaluate the therapeutic effects of FMN in a PCOS rat model and elucidate its underlying molecular mechanisms. Methods A PCOS-like model was established in 3-week-old female Sprague-Dawley rats by daily dehydroepiandrosterone (DHEA) injections. The efficacy of FMN was assessed by monitoring estrous cycles, hormone levels, glucose tolerance, and ovarian tissue morphology. Network pharmacology and transcriptome sequencing were used to predict the molecular targets and signaling pathways of FMN. The binding and stabilizing effects of FMN on suppressor of cytokine signaling 3 (SOCS3) were confirmed using molecular docking, molecular dynamics (MD) simulations, and cellular thermal shift assay (CETSA)-Western blotting (WB) (CETSA-WB). The expression of SOCS3, inflammation- and fibrosis-related markers, and the components of the transforming growth factor beta1 (TGF- β 1)/Smad pathway were quantified by quantitative polymerase chain reaction (qPCR), Western blotting, and immunohistochemistry. Functional validation was performed using SOCS3 small interfering RNA (siRNA). Results DHEA successfully induced a PCOS-like phenotype, including disrupted estrous cycle, hyperandrogenism, an elevated luteinizing hormone to follicular stimulating hormone (LH/FSH) ratio, insulin resistance, and abnormal ovarian morphology. FMN treatment significantly reversed these abnormalities and reduced ovarian collagen deposition. Network pharmacology and transcriptome analyses indicated that the therapeutic efficacy of FMN was primarily attributable to its anti-fibrotic and anti-inflammatory properties, with SOCS3 identified as a potential key molecule. Molecular docking and MD simulations, along with CETSA-WB, further revealed that FMN directly binds to SOCS3, enhancing its stability and thereby inhibiting ovarian fibrosis in PCOS. Moreover, qPCR, Western blotting, and immunohistochemistry confirmed that FMN regulates the TGF- β 1/Smad signaling pathway. Importantly, SOCS3siRNA abolished fibrotic-related collagen levels and phosphorylated signal transducer and activator of transcription 3 (p-STAT3) expression, supporting the notion that FMN ameliorates PCOS-induced ovarian fibrosis via SOCS3. Conclusion FMN alleviated ovarian dysfunction and hyperandrogenism in DHEA-induced PCOS rats by stabilizing SOCS3 and inhibiting TGF- β 1/Smad signaling, thereby attenuating ovarian fibrosis and inflammation. This reveals a novel SOCS3-centered mechanism for FMN and underscores its therapeutic potential for PCOS.
✓ 已验证
DOI
高影响因子
JOURNAL OF PHARMACY AND PHARMACOLOGY
·
2026
·Vol. 78
·期 2
·
IF 3.7
Wang Baoying,Liu Hui,Zhang Changjing,Yan Xiangli,Xu Erping,Bai Ming,Li Yucheng
ObjectivesFormononetin (FMN) is known for its significant neuroprotective effects, this study aims to investigate the antidepressant potential and underlying mechanisms of FMN.MethodsAntidepressant efficacy was evaluated in corticosterone (CORT)-induced depression models. In vivo, CORT-exposed mice received FMN to assess behavioral and hippocampal changes (dendritic spine density, synaptic markers: MAP-2/GAP-43). In silico, network pharmacology and molecular docking predicted FMN’s binding affinity and enriched pathways. In vitro, HT22 cells pretreated with FMN (10 μM, 6 h) were subjected to CORT injury, with mechanistic validation via ERα antagonist (MPP) and ERK inhibitor (PD98059).Key findingsFMN alleviated depressive-like behaviors and preserved hippocampal integrity in mice. Bioinformatics analysis revealed FMN’s strong binding to ER subtypes and enrichment in estrogen/MAPK pathways. In vitro, FMN pretreatment activated the ERK-CREB-BDNF axis in CORT-injured HT22 cells, enhancing neuronal survival and synaptic function. The activation was ERα/ERK-dependent, as evidenced by the abolition of protective effects following pharmacological inhibition with MPP (ERα antagonist) or PD98059 (ERK inhibitor). Concomitantly, in vivo FMN treatment restored hippocampal p-ERK/ERK ratios in mice, directly corroborating the ERK-CREB-BDNF pathway activation and highlighting its efficacy in reversing CORT-induced signaling deficits.ConclusionFMN exerts antidepressant effects via ERα-mediated neurotrophic signaling (ERK-CREB-BDNF), offering a mechanistic foundation for natural antidepressant development.
✓ 已验证
DOI
高影响因子
Biochemistry and Cell Biology
·
2021
·Vol. 99
·期 2
·
IF 3.626
Guangwei Liu,Wenxia Zhao,Jiameng Bai,Jianjiao Cui,Haowei Liang,Baoping Lu
Autoimmune hepatitis (AIH) is a chronic inflammatory liver disease that seriously threatens the health of humans globally. Formononetin (FMN) is a natural herb extract with multiple biological functions. In this study, an experimental model of AIH was established in mice through the use of concanavalin A (ConA). To investigate the effects of FMN on ConA-induced hepatitis, the mice were pretreated with 50 or 100 mg/kg body mass of FMN. The results show that FMN alleviated ConA-induced liver injury of mice in a dose-dependent manner. Moreover, pretreatment with FMN inhibited the apoptosis of hepatocytes in the ConA-treated mice through downregulating the expression of pro-apoptotic proteins (Bax, cleaved caspase 9, and cleaved caspase 3) and upregulating the expression of anti-apoptotic protein (Bcl-2). It was also found that the levels of proinflammatory cytokines were greatly reduced in the serum and liver tissues of mice pretreated with FMN. Further studies showed that FMN reduced the level of phosphorylated nuclear factor kappa B (p-NF-κB) p65 and enhanced the level of IκBα (inhibitor of NF-κB), suggesting that FMN inhibits the activation of the NF-κB signaling pathway. In addition, FMN inhibited activation of the NOD-like receptor protein 3 (NLRP3) inflammasome. Therefore, FMN could be a promising agent for the treatment of AIH.
研究领域:
免疫学
·
药理学
·
肝病学
✓ 已验证
DOI
PubMed
高影响因子
JOURNAL OF FOOD COMPOSITION AND ANALYSIS
·
2022
·
IF 4.52
Jiahui Ji,Lianggong Zhao,Xiaohua Liu,Huifang Wu,Donghan Wang,Dan Liu,Xinyue Chen,Shilan Feng
In this study, a natural extract from the plant Radix hedysari (ER) was proven to be useful for the green synthesis of silver nanoparticles (AgNPs) and ER-AgNPs in particular. Considering the complexity of plant extracts, high-pressure liquid chromatography (HPLC) was effective at confirming the components of ER, surprisingly, formononetin was found to comprise more than 85% of the total contents. Since formononetin was confirmed to be the primary component of ER, this compound was also used as the basis to synthesize AgNPs designated FMT-AgNPs that was highly pure and of high quality. The FMT-AgNPs functionalized by formononetin were optimized for further study. A simple, fast and sensitive colorimetric method detect formothion was achieved using FMT-AgNPs. A wide linear range from 0.1 μM to 10 μM was established with a low limit of detection (LOD) of 14.6 nM. Since formononetin performed multiple roles during the synthesis, it was confirmed that the mechanism of detection was based on aldol condensation , intermolecular hydrogen bonds and electrostatic attraction between formononetin and formothion. Finally, the green synthesized FMT-AgNPs were further applied in typical fruit and vegetable samples, indicating that FMT-AgNPs were potentially highly useful.
研究领域:
纳米技术
·
分析化学
·
药学
·
环境科学
✓ 已验证
产品关联
DOI
高影响因子
NEUROSCIENCE
·
2025
·
IF 2.8
Siqi Quan,Mengyuan Li,Zhouli Yue,Hui Liu,Shuaijun Peng,Roujia Guo,Xiaoyan Fang,Yucheng Li
Neuroinflammation and oxidative stress are major pathogenic drivers of depression, with the Keap1/Nrf2/HO-1 pathway serving as a key regulator of both processes. Formononetin (FMN) is a naturally occurring isoflavone with anti-inflammatory and antioxidant activities; however, its potential to exert antidepressant effects through activation of this pathway has not been investigated. In this study, lipopolysaccharide (LPS, 1 mg/kg, i.p.) was used to induce neuroinflammation and depressive-like behaviors in mice, and FMN (20 or 40 mg/kg) was administered for seven days prior to LPS challenge. FMN dose-dependently alleviated LPS-induced behavioral deficits, including reduced sucrose preference, decreased locomotor activity, and prolonged immobility in the tail suspension test. Hematoxylin-eosin (HE) and Nissl staining revealed that FMN markedly attenuated LPS-induced hippocampal neuronal damage. FMN also inhibited microglial activation, as evidenced by reduced Iba-1 expression, decreased NF-κB phosphorylation, and downregulation of both mRNA and protein levels of pro-inflammatory cytokines, including IL-1β, TNF-α, and IL-6. Furthermore, LPS-induced lipid peroxidation was significantly attenuated, as indicated by lower levels of 4-hydroxynonenal (4-HNE). Molecular docking suggested a potential direct interaction between FMN and Keap1, while Western blot analysis confirmed that FMN downregulated Keap1 and upregulated Nrf2 and HO-1 protein expression. Collectively, these findings demonstrate that FMN alleviates LPS-induced neuroinflammation and depressive-like behaviors, likely through activating the Keap1/Nrf2/HO-1 pathway, supporting its potential as a preventive candidate for inflammation-associated depression.
研究领域:
神经药理学
·
分子生物学
·
精神病学
·
炎症研究
·
氧化应激
✓ 已验证
产品关联
DOI
PubMed
高影响因子
MICROCHEMICAL JOURNAL
·
2026
·
IF 5.2
Pengge Wei,Yao Sun,Ting Gong,Jing Zhao,Longshan Zhao
A novel DES-assisted dummy template magnetic MIP (DES-MMIP) was fabricated for selective formononetin extraction. • DES-MMIP exhibited high adsorption capacity (26.85 mg·g −1 ) and excellent selectivity (IF = 5.04). • Magnetic separation enabled rapid adsorbent recovery within seconds, eliminating time-consuming centrifugation or filtration. • The DES-MMIP method achieved 97.33–98.67% recoveries from Astragalus extract with a green DES-based synthesis route. Selective separation of low-abundance bioactive compounds from complex herbal matrices remains challenging. Herein, a magnetic molecularly imprinted polymer (DES-MMIP) was developed for rapid and specific recognition of formononetin from Astragalus . For the first time, a dummy template (daidzein), a deep eutectic solvent (ChCl:MAA = 1:2) together with 4-vinylpyridine (4-VP) as dual functional monomers, and Fe 3 O 4 @SiO 2 magnetic nanoparticles were integrated into a single molecularly imprinted system. The material was characterized by transmission electron microscopy, Fourier-transform infrared spectroscopy, X-ray diffraction, X-ray photoelectron spectroscopy, and vibrating sample magnetometry. Adsorption experiments showed that DES-MMIP exhibits excellent binding affinity and markedly higher selectivity for formononetin over structural analogs (biochanin A, genistein, daidzin) and coexisting interferents (luteolin, resveratrol). The magnetic core-shell structure enables rapid separation within seconds. Under optimized conditions, the DES-MMIP exhibited a high adsorption capacity of 17.22 mg/g for formononetin with an imprinting factor ( IF ) of 5.04. The method showed good linearity over the concentration range of 5–100 μg mL −1 ( r = 0.9996), with a limit of detection (LOD) of 0.6 μg mL −1 . The recoveries of formononetin from spiked Astragalus extracts ranged from 97.33% to 98.67% with a relative standard deviation (RSD) of 0.67% ( n = 3). This work provides a convenient, efficient, and green adsorbent for formononetin enrichment and offers a generalizable paradigm for isolating other low-abundance active components from traditional Chinese medicines. Download: Download high-res image (99KB) Download: Download full-size image
✓ 已验证
产品关联
DOI
高影响因子
Food Bioscience
·
2023
·
IF 5.2
Lijun Zheng,Hongjia Xu,Hanxin Zhang,Caihong Shi,Wei Zhou,Xiangrong Zhang
This study aims to characterize formononetin (FMN) and perilla seed oil (PSO) co-loaded nanostructured lipid carriers (NLC). FMN-PSO-NLC was prepared by melt-emulsification ultrasonic method. The average particle size of FMN-PSO-NLC was 117.5 ± 3.7 nm, with PDI of 0.240 ± 0.017 and zeta potential of −36.7 ± 0.7 mV. Differential scanning calorimetry (DSC), X-ray diffractometry (XRD), and Fourier transform infrared spectroscopy (FTIR) studies revealed that the formation of FMN-PSO-NLC was accompanied by changes in crystallinity and intermolecular interactions. FMN-PSO-NLC dispersions possessed pseudoplastic flow from the rheological studies. FMN-PSO-NLC possessed sustained-release of FMN for 24 h. FMN-PSO-NLC was more easily digested than that of PSO in vitro digestion. The antioxidant activity and stability of FMN-PSO-NLC were significantly improved. This study provides a formulation design for improving the stability, antioxidant activity of FMN and delaying the oxidation of PSO.
研究领域:
药学
·
纳米技术
·
食品科学
·
材料科学
✓ 已验证
产品关联
DOI
高影响因子
危险品化学品经营许可证（带存储）