Frontiers in Nutrition
·
2025
·
IF 5.1
Zhanding Cui,Jinlong Liu,Jinlong Wang,Jing Zhang,Yimei Cao,Kun Li,Zhixun Zhao,Hong Yuan,Xingwen Bai,Xueqing Ma,Pinghua Li,Yuanfang Fu,Huifang Bao,Dong Li,Qiang Zhang,Zaixin Liu,Kai Li,Tong Xu,Zengjun Lu
This study delves into the antiviral efficacy of Formononetin (FMN) and Mizoribine (MZR) against the Porcine Reproductive and Respiratory Syndrome Virus (PRRSV), a virus with a considerable economic impact and a current void in effective treatments. FMN and MZR were found to inhibit various PRRSV strains in vitro, predominantly in the early stages of viral infection. Noteworthy was the observation of their synergistic effects when combined with Ribavirin. The study underscores the antiviral potential of FMN and MZR, particularly emphasizing their low cytotoxicity at specific concentrations. These results position FMN and MZR as promising antiviral agents against PRRSV, underscoring their low cytotoxicity and efficacy in early-stage viral inhibition. Such findings pave the way for their potential inclusion in future PRRSV management strategies.
研究领域:
兽医学
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病毒学
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药理学
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产品关联
DOI
PubMed
高影响因子
INTERNATIONAL JOURNAL OF MOLECULAR SCIENCES
·
2025
·Vol. 26
·期 11
·5280
·
IF 4.9
Hongjuan Cui,Yan Zhao,Wei Li,Huanjie Cui,Jiahong Han,Enbo Cai
Formononetin is widely used in anti-tumor research, but its poor water solubility leads to low absorption and poor utilization efficiency in vivo, limiting further development. The triphenylphosphine cation was partially attached to the 7-position hydroxyl group of formononetin to specifically target it into the mitochondria of tumor cells to enhance the anti-tumor effect. Detailed structural characterization via 1 H-NMR and 13 C-NMR analysis confirmed the physical properties and chemical structures of 21 newly synthesized derivatives. The effects of these derivatives on tumor cells were assessed by in vitro and computational methods. MTT results from four tumor cell lines showed that formononetin derivatives containing triphenylphosphine had stronger anti-tumor activity than formononetin and exhibited more cytotoxic effects in cancer cells than in normal cells. In particular, the final product 2c (IC 50 = 12.19 ± 1.52 μM) showed more potent anti-tumor activity against A549 cells. It was also superior to formononetin and 5-FU. To identify the potential biological targets, the core-expressed gene SHMT2 in lung cancer mitochondria was screened using network pharmacology technology, and molecular docking analysis confirmed the stable binding of the end products to the amino acid residues of the core genes through the formation of hydrogen bonds and via other interactions. In addition, molecular docking simulations further confirmed that the end product exhibited excellent stability when bound to SHMT2 . These results suggest that triphenylphosphine-containing formononetin derivatives are worthy of further exploration in the search for novel drug candidates for the treatment of cancer.
研究领域:
药理学
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肿瘤学
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计算生物学
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产品关联
DOI
PubMed
高影响因子
AAPS PHARMSCITECH
·
2025
·Vol. 26
·期 5
·1-14
·
IF 4
Liu Hongting,Sun Yao,Cai Shihao,Zhao Conglu,xu Xiang,Xu Aiguo,Zhou Honggang,Yang Cheng,Gu Xiaoting,Ai Xiaoyu
Idiopathic pulmonary fibrosis (IPF) is a progressive lung disease of unknown cause, with few effective therapies available and high mortality rates. Our preceding research indicated that formononetin (FMN) could improve the symptoms of the bleomycin-induced pulmonary fibrosis and be a promising drug against IPF. In this study, an inhalable formononetin-loaded poly(lactic-co-glycolic) acid (PLGA) large porous microspheres (FMN-PLGA-MSs) was prepared by the method of emulsion solvent evaporation. SEM showed that FMN-PLGA-MSs were loose particles existing many pores on the surfaces, and the measured mean geometric diameter was more than 10 µm. The encapsulation efficiency (EE) and drug loading efficiency (DL) were 87.72 ± 6.34% and 4.18 ± 0.30%. FMN in FMN-PLGA-MSs could be rapidly released within 2 h and sustainably released for 21 d. Cell tests and q-RT-PCR tests showed that FMN could inhibit the activation of fibroblasts and the deposition of extracellular matrix (ECM) by acting on the TGF-β1/Smad3 signaling pathway. FMN-PLGA-MSs showed higher antifibrotic effects than free FMN oral administration in the pulmonary fibrosis models of mice, remarkably improving pulmonary function, decreasing hydroxyproline levels, and attenuating lung injuries. By formulating formononetin into microsphere preparations, its solubility can be significantly enhanced, enabling effective pulmonary drug delivery. This approach not only improves lung targeting but also reduces systemic toxicity. Additionally, it facilitates superior lung deposition and extends the retention time of the formononetin within the lungs. Taken together, FMN-PLGA-MSs may be a promising inhaled medication for the treatment of IPF. Graphical Formononetin (FMN) can improve the symptoms of idiopathic pulmonary fibrosis (IPF). Large porous microparticle can improve lung retention and lung targeting. FMN is loaded in poly(lactic-co-glycolic)acid (PLGA) to get microspheres (FMN-PLGA-MSs) for intratracheal instillation treatment of IPF. FMN-PLGA-MSs remarkably improved pulmonary function, decreased hydroxyproline, and attenuated lung injuries. FMN-PLGA-MSs are promising intratracheal instillation medication for the treatment of IPF.
研究领域:
药学
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呼吸病学
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分子生物学
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产品关联
DOI
PubMed
高影响因子
JOURNAL OF SEPARATION SCIENCE
·
2018
·Vol. 41
·期 15
·3060-3068
·
IF 2.415
Yu-Zhen Zhang,Jiawei Zhang,Ling Tan,Zhining Xia,Chong-Zhi Wang,Lian-Di Zhou,Qihui Zhang,Chun-Su Yuan
Thermo-responsive magnetic molecularly imprinted polymers were prepared by simple surface molecular imprinting polymerization for the selective adsorption and enrichment of formononetin from Trifolium pretense by temperature regulation. Using formononetin as a template, N -isopropylacrylamide as the thermo-responsive functional monomer, and methacrylic acid as an assisting functional monomer, the polymers were synthesized on the surface of the magnetic substrate. The results show that imprinted polymers attained controlled adsorption of formononetin in response to the temperature change, with large adsorption capacity (16.43 mg/g), fast kinetics (60 min) and good selectivity at 35°C compared with that at 25 and 45°C. The selectivity experiment indicated that the materials had excellent recognition ability for formononetin and the selectivity factors were between 1.32 and 2.98 towards genistein and daidzein. The excellent linearity was attained in the range of 5–100 μg/mL, with low detection limits and low quantitation limits of 0.017 and 0.063 μg/mL, respectively. Furthermore, the thermo-responsive magnetic molecularly imprinted polymers were successfully utilized for enriching and purifying formononetin from Trifolium pretense . The analytical results indicate that the imprinted polymers are promising materials for selective identification and enrichment of formononetin in complicated herbal medicines by simple temperature-responsive regulation.
研究领域:
材料科学
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药学
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DOI
PubMed
高影响因子
International Journal of Electrochemical Science
·
2023
·
IF 1.5
Li Sun,Xueliang Wang,Na Zou,Hongying Li,Zhangyu Yu
The interaction of formononetin (FN) with herring sperm DNA has been studied by electrochemical methods, UV-Vis spectroscopy and fluorescence. On a poly L-cysteine film modified electrode (PLC/GCE), FN showed a couple of well-defined voltammetric peaks in 0.1 M acetate buffer of pH 5.3. As adding the herring sperm DNA into above solution, the peak current of FN decreased and no new peaks appeared. Based on the electrochemical results, the binding constant and binding ratio between FN and herring sperm DNA were determined to be 1.98×10 4 M -3 and 1:3, respectively. The UV-Vis spectroscopy indicated that the maximum absorption of FN had obviously hyperchromic effect and red shift after the interaction of DNA and FN. The interaction of DNA and FN can also make the fluorescence intensity of FN enhancement. The electrochemical and spectroscopic results indicated that the interaction of FN to DNA was an intercalative mode.
研究领域:
生物化学
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药理学
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DOI
高影响因子
RSC Advances
·
2020
·Vol. 10
·期 54
·32897-32905
·
IF 3.119
Xinyue Chen,Jiahui Ji,Gengen Shi,Zhiyuan Xue,Xianglin Zhou,Lianggong Zhao,Shilan Feng
This study linked natural plant materials and nanomaterials; reporting an environmentally friendly, non-toxic and efficient method for the green synthesis of gold nanoparticles (AuNPs) using an ethyl acetate extract of Radix Hedysari (EAR). The components of the extract were identified using HPLC and it was found that formononetin accounted for more than 90% of the total contents. We predicted that formononetin in EAR plays a crucial role in green synthesis. Thus, formononetin was used as a standard reductant to synthesize AuNPs, and the result confirmed our prediction. The synthetic mechanism was also discussed in detail in the article. Moreover, EAR–AuNPs realized the sensitive and selective colorimetric detection of ferrous ions (Fe2+) among other metal ions, and were applied to spiked tap water with a low detection limit of 1.5 μM in a wide range from 10 μM to 500 μM. EAR–AuNPs were green synthesized using Radix Hedysari extract for the first time and were successfully applied in real sample detection.
研究领域:
纳米生物学
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环境科学
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分析化学
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DOI
PubMed
高影响因子
INTERNATIONAL JOURNAL OF PHARMACEUTICS
·
2021
·
IF 5.875
Yeli Wang,Zian Deng,Xinmiao Wang,Yugang Shi,Ying Lu,Sheng Fang,Xianrui Liang
Improving solubility and administration route of isoflavone formononetin (FMN) are critical factors to improve its bioavailability in the oral cavity. This study fabricated fast-dissolving nanofibers containing FMN/methyl- β -cyclodextrin (FMN/Me- β -CD) inclusion complex. The solubility of FMN could be increased by approximately 50 times at 20 mM aqueous Me- β -CD. Interactions and thermodynamic parameters of the host-guest inclusion complex were studied by a fluorescence quenching method. The structure and mechanisms of the complex were further studied by molecular docking and molecular dynamics. Finally, polyvinyl-alcohol (PVA) nanofibrous webs containing the FMN/Me- β -CD inclusion complex were fabricated by electrospinning. The dissolution test demonstrated that the FMN/Me- β -CD/PVA nanofibers can be dissolved in artificial saliva within approximately 2 s. This study shows the potential of Me- β -CD inclusion and electrospinning to improve solubility and administration route of isoflavones.
研究领域:
药剂学
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生物化学
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材料科学
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产品关联
DOI
PubMed
高影响因子
AAPS PHARMSCITECH
·
2024
·Vol. 25
·期 8
·1-18
·
IF 3.4
Zou Zhihui,Xue Yuanyuan,Adu-Frimpong Michael,Wang ChengWei,Jin Zhou,Xu Ying,Yu Jiangnan,Xu Ximing,Zhu Yuan
This study aimed to construct a self-microemulsion drug delivery system (SMEDDS) for Formononetin (FMN) to improve its solubility and bioavailability while combining the nanocrystals (NCs) technology. The SMEDDS prescription composition was optimized with a pseudo-three-phase diagram, followed by a series of in vitro and in vivo evaluations of the selected optimal prescriptions. FMN-NCs loaded SMEDDS showed a homogeneous spherical shape in the Transmission electron microscope and the particle size was measured as (20.65 ± 1.42) nm. The in vitro cumulative release rate in each dissolution medium within 30 min was higher than 80%, much higher than that of FMN (6%) and FMN-NCs (40%); Cellular experiments confirm that the formulation has a high safety profile and significantly promotes cellular uptake. The results of pharmacokinetics and intestinal absorption in rats showed that the relative bioavailability of FMN-NCs and FMN-NCs loaded SMEDDS were (154.80 ± 3.76)% and (557.73 ± 32.88)%, respectively, and both of them significantly increased the rate and extent of absorption of the drug in intestinal segments. FMN-NCs loaded SMEDDS significantly enhanced the solubility and bioavailability of FMN. Graphical
研究领域:
药剂学
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药物递送
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生物医学工程
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产品关联
DOI
PubMed
高影响因子
Chemical Biology & Drug Design
·
2023
·Vol. 103
·期 1
·e14363
·
IF 3
Chun Li,Yuxin Xie,Shaoyu Hu,Hong Yu,Yunke Xu,Hongping Shen,Yuan Yuan,Long Gu,Bangming Pu
Hepatocellular carcinoma (HCC) is a life-threatening disease for which there is no cure. Traditional Chinese medicine is a treasure trove of Medicinals that has been used for thousands of years. In China, the traditional herb pair, Curcumae Rhizoma and Sparganii Rhizoma (CR-SR) represent a classic herbal combination used for the treatment of HCC. However, the drug targets and pharmacological mechanism of action of CR-SR in the treatment of HCC are unclear. To address this, we screened the active components and drug targets of CR-SR from the Traditional Chinese Medicine Systems Pharmacology (TCMSP) database and a high-throughput experiment- and reference-guided database of traditional Chinese medicines (HERB database). Combined with the weighted co-expression network analysis of dataset GSE76427, we constructed an active component-target-disease regulatory network. It was found that CR-SR's active components for HCC treatment included trans-gondoic acid, beta-sitosterol, stigmasterol, hederagenin, and formononetin. These compounds specifically targeted the genes Estrogen Receptor 1 ( ESR1 ), Cyclin A2 ( CCNA2 ), Checkpoint Kinase 1 ( CHEK1 ), and Nuclear Receptor Coactivator 2 ( NCOA2 ). ESR1 , CCNA2 , and CHEK1 genes showed significant differences in survival prognosis, expression levels, and statistical significance during the pathological stage. Moreover, their high affinity for formononetin was determined through molecular docking analysis. Cell assays and high-throughput sequencing were performed to reveal that the inhibitory effect of formononetin on HepG2 cell proliferation was related to hepatocyte metabolism and cell cycle regulation-related pathways. This study provides insights into potential HCC treatments.
研究领域:
肿瘤学
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药理学
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生物信息学
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产品关联
DOI
PubMed
高影响因子
PLoS One
·
2021
·Vol. 16
·期 1
·e0245050
·
IF 3.24
Yin Chen,Dong Wei,Jin Zhao,Xiangnan Xu,Jingyu Chen
Background
The antioxidant and anti-inflammatory features of Formononetin, an isoflavone constituent extracted from traditional Chinese medicine, have been reported. The present study investigated that whether Formononetin plays a benefit on hyperoxic ALI.
Methods
C57BL/6 mice were exposed to hyperoxia for 72 h to produce experimental hyperoxic ALI model. Formononetin or vehicle was administrated intraperitoneally. Samples from the lung were collected at 72 h post hyperoxia exposure for further study. Pulmonary microvascular endothelial cells isolated from the lung of C57BL/6 mice were used for in vitro study.
Results
Formononetin pretreatment notably attenuated hyperoxia-induced elevating pulmonary water content, upregulation of proinflammatory cytokine levels and increasing infiltration of neutrophil in the lung. Western blot analyses showed that Formononetin enhanced the expression of nuclear factor erythroid-2-related factor 2 (Nrf2) which is a key transcription factor regulating the expression of heme oxygenase-1 (HO-1). Formononetin increased HO-1 expression and activity compared with vehicle-treated animals. Moreover, Formononetin reversed hyperoxia-caused the reduction of M2 macrophage polarization. However, pretreatment of a HO-1 inhibitor reduced the protective effect of Formononetin on hyperoxic ALI. Cell study showed that the Formononetin-induced upregulation of HO-1 was abolished when the Nrf2 was silenced.
Conclusions
Formononetin pretreatment reduces hyperoxia-induced ALI via Nrf2/HO-1-mediated antioxidant and anti-inflammatory effects.
研究领域:
药理学
·
肺病学
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免疫学
·
分子生物学
✓ 已验证
DOI
PubMed
高影响因子
COMBINATORIAL CHEMISTRY & HIGH THROUGHPUT SCREENING
·
2025
·Vol. 29
·期 4
·717-730
·
IF 1.7
Yuling Wei,Wenhui Wu,Min Duan,Ting Li,Mei Liu,Jinyan Li
IntroductionChronic atrophic gastritis (CAG) is the initial phase in the carcinogenesis of gastric cancer (GC). Therefore, effective treatment for CAG is important in reducing the risk of GC progression. As an isoflavone compound, formononetin (FMN) has been identified as a potential therapeutic agent for acute gastric ulcers and GC. However, no study has reported the protective effect of FMN against CAG and its underlying mechanism. This study aimed to explore the therapeutic effects of FMN on CAG and its underlying mechanisms in vitro.MethodsNetwork pharmacology was applied to predict the core targets of FMN therapy in CAG. The CAG cell model was developed using N-methyl-N’-nitro-N-nitrosoguanidine (MNNG)-triggered human gastric epithelial cells (GES-1). The CCK-8 assay was applied to estimate cellular viability. The expression of inflammatory cytokines in cell supernatant was detected by ELISA. The protein levels and localization of nuclear receptor coactivator 1 (NCOA1), c-Jun, and c-Fos were evaluated using western blotting and immunofluorescence staining. Cell apoptosis was measured using flow cytometry.ResultsNetwork pharmacology analysis identified c-Jun as the core target of FMN in the treatment of CAG, with biological processes primarily involving the regulation of apoptosis and inflammation. In vitro, MNNG exposure reduced GES-1 cell viability as well as increased inflammation and cellular apoptosis, and these effects were reversed by FMN treatment. In detail, FMN decreased the protein levels of NCOA1, c-Jun, and c-Fos in MNNG-triggered GES-1 cells. The activator protein-1 (AP-1) inhibitor T-5224 enhanced the effects of FMN treatment on cell viability, inflammatory response, and apoptosis in MNNG-triggered GES-1 cells.DiscussionThis study employed network pharmacology analysis to identify FMN's therapeutic targets for CAG and validated the underlying mechanisms in vitro. While these results are promising, in vivo validation is required to confirm the efficacy of FMN. A comparative pharmacological evaluation against existing therapeutic agents and bioactive compounds would further elucidate FMN's therapeutic potential for CAG treatment.ConclusionFMN ameliorated the cell damage that MNNG triggered in GES-1 cells. The mechanism involved the anti-inflammatory and anti-apoptotic effects of FMN via modulation of the NCOA1/AP-1 signaling axis. The present preliminary study found FMN to exhibit a potential therapeutic effect against CAG.
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DOI
高影响因子
Molecular Brain
·
2019
·Vol. 12
·期 1
·1-12
·
IF 4.051
Wang Xin-shang,Guan Shao-yu,Liu An,Yue Jiao,Hu Li-ning,Zhang Kun,Yang Liu-kun,Lu Liang,Tian Zhen,Zhao Ming-gao,Liu Shui-bing
Chronic pain is commonly accompanied with anxiety disorder, which complicates treatment. In this study, we investigated the analgesic and anxiolytic effects of Formononetin (FMNT), an active component of traditional Chinese medicine red clover ( Trifolium pratense L.) that is capable of protecting neurons from N-methyl-D-aspartate (NMDA)-evoked excitotoxic injury, on mice suffering from complete Freund’s adjuvant (CFA)-induced chronic inflammatory pain. The results show that FMNT administration significantly reduces anxiety-like behavior but does not affect the nociceptive threshold in CFA-injected mice. The treatment reverses the upregulation of NMDA, GluA1, and GABA A receptors, as well as PSD95 and CREB in the basolateral amygdala (BLA). The effects of FMNT on NMDA receptors and CREB binding protein (CBP) were further confirmed by the potential structure combination between these compounds, which was analyzed by in silico docking technology. FMNT also inhibits the activation of the NF-κB signaling pathway and microglia in the BLA of mice suffering from chronic inflammatory pain. Therefore, the anxiolytic effects of FMNT are partially due to the attenuation of inflammation and neuronal hyperexcitability through the inhibition of NMDA receptor and CBP in the BLA.
研究领域:
药理学
·
神经科学
·
疼痛研究
·
传统中药
✓ 已验证
DOI
PubMed
高影响因子
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