Microorganisms
·
2025
·Vol. 13
·期 6
·1203
·
IF 4.2
Zhenhe Liu,Haolong Qiu,Yucong Jiang,Yuxi Mo,Linlin Lu,Yan Wang,Dandan Hu,Xingju Song
Toxoplasma gondii, an obligate intracellular protozoan parasite infecting nucleated cells of warm-blooded vertebrates, causes severe complications in immunocompromised hosts. Current therapies remain limited by suboptimal efficacy and toxicity, necessitating novel anti-toxoplasmic agents. Piceatannol (PIC), a natural stilbenoid, demonstrates multifaceted bioactivity including antimicrobial and anti-parasitic effects, suggesting therapeutic potential againstT. gondii. Our previous study revealed PIC’s potent anti-parasitic activity, selectively inhibitingT. gondiiproliferation and altering parasite morphology without host cytotoxicity. In this study, mechanistic analyses indicated that PIC disrupts mitochondrial integrity in tachyzoites, reducing mitochondrial membrane potential and ATP production while elevating ROS levels. Transcriptomic profiling identified significant suppression of oxidative phosphorylation-related genes, consistent with mitochondrial dysfunction. These findings establish PIC as a promising candidate targetingT. gondiithrough the mechanism of mitochondrial impairment.
研究领域:
寄生虫学
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药理学
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细胞生物学
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DOI
PubMed
高影响因子
JOURNAL OF AGRICULTURAL AND FOOD CHEMISTRY
·
2025
·
IF 6.2
Jiazeng Yang,Zhuoxin Guo,Wenlong Zha,Jiachen Zi
Piceatannol, a stilbene widely found in many types of foods, shows a variety of effects on the cardiovascular system, nervous system, and skin. Its low abundance in nature impedes its development. Microbial cell factories offer a green and sustainable approach to the production of natural products. In this study, we screened two 4-coumarate:coenzyme A ligases (4CLs), nine stilbene synthases (STSs), and five 4-hydroxyphenylacetate-3-hydroxylases (4HPA3Hs) to construct multiple bioconversion routes from p-coumaric acid to piceatannol in a single Saccharomyces cerevisiae strain. Then, the supply of p-coumaric acid and malonyl-CoA was enhanced, and NADPH and FADH2 regenerations were optimized, resulting in establishment of yPi101 which produced 127 mg/L and 442 mg/L piceatannol in a flask and by fed-batch fermentation, respectively. This is the first report of the de novo production of piceatannol in a single S. cerevisiae strain and represents the highest piceatannol yield.
研究领域:
合成生物学
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微生物工程
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天然产物合成
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DOI
PubMed
高影响因子
TOXICOLOGY IN VITRO
·
2020
·
IF 2.959
Lili Jiang,Zhen Wang,Xiaoyu Wang,Shujuan Wang,Zhe Wang,Yong Liu
Piceatannol is a natural polyphenol compound found in passion fruit and blueberry with several biological activities . However, it is unclear whether piceatannol affects the activity of human UDP-glucuronosyltransferases (UGTs) enzymes. The present study aims to assess the potential inhibitory effect of piceatannol against UGTs enzymes, as well as to evaluate its potential food-drug interactions risk via UGTs inhibition. We systematically evaluated the inhibitory effects of piceatannol on UGTs using high-performance liquid chromatography by measuring the formation rates for 4-methylumbelliferoneglucuronide and imipramine N-glucuronide. The results indicated that piceatannol displayed broad-spectrum inhibition against human UGTs. Kinetic analysis showed that inhibition of piceatannol on UGT1A6 and UGT1A7 followed noncompetitive inhibition mechanism, while the inhibition on UGT1A8 and UGT1A9 obeyed competitive and mixed inhibition mechanism, respectively. The quantitative prediction of risks showed that the coadministration of piceatannol with drugs primarily cleared by UGT1A6, UGT1A7, UGT1A8, and UGT1A9 may result in potential food-drug interaction. In conclusion, additional caution should be taken when piceatannol and food containing piceatannol are co-administered with drugs metabolized by UGTs.
研究领域:
药理学
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生物化学
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食品安全
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产品关联
DOI
PubMed
高影响因子
IMMUNOLOGIC RESEARCH
·
2025
·Vol. 73
·期 1
·1-20
·
IF 3.1
Xu Cong,Lu Chenqi,Wang Wu,Wang Zhimin,Qiu Yang,Han Min,Yang Jun,Li Shanglin
Autoimmune hepatitis (AIH) is an immune-mediated liver disease that currently lacks viable drug treatment methods. This study is to explore the role of piceatannol (PIC) in ConA-induced AIH and the related mechanisms. A mouse model of AIH was established by injecting ConA (i.v.), and PIC was administered as an intervention. The protective effect of PIC was evaluated by the liver function, liver pathology, and serum levels of inflammatory factors. Subsequently, network pharmacology was used to predict the pathways and targets of PIC in the treatment of AIH, and the predicted results were validated using flow cytometry, molecular docking, surface plasmon resonance (SPR) and so on. Finally, the immunosuppressive effect of PIC was further validated in a mouse heart transplantation model. PIC can improve liver function decline and reduce pathological liver damage, as well as inhibit the increase of serum inflammatory factor levels in mice with AIH induced by ConA. The protective effect is achieved by suppressing the immune activity of T cells and macrophages through binding to c-Jun. PIC can also extend the survival of cardiac allografts and inhibit acute rejection reactions. These results indicated that PIC can significantly improve ConA-induced AIH in mice by inhibiting the immune activity of T cells and macrophages through binding to c-Jun. PIC can also extend the survival of cardiac allografts in mice and inhibit acute rejection responses. The above results indicated that PIC may serve as a promising immunosuppressant and be effective for AIH.
研究领域:
免疫学
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肝病学
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药理学
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分子生物学
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产品关联
DOI
PubMed
高影响因子
Frontiers in Veterinary Science
·
2022
·
IF 3.471
Jiang Yucong,Shi Yuehong,Hu Dandan,Song Xingju
Toxoplasma gondii is an obligate intracellular protozoan that infects the nucleated cells of warm-blooded animals and causes life-threatening disease in immunocompromised patients. Due to the limited effectiveness and prominent side effects of existing drugs, there is an urgent need to develop new therapeutic options against T. gondii. Piceatannol is a natural plant compound with multiple functions such as antibacterial, antileukemic and antiparasitic activities. In the present study, the anti-T. gondii activity of piceatannol was evaluated. Piceatannol potently inhibited Toxoplasma with a half-maximal effective concentration (EC50) of 28.10 μM. Piceatannol showed a significant inhibitory effect on intracellular proliferation, inhibiting intracellular parasites at a rate of 98.9% when treatment with 100 μM piceatannol. However, the invasion ability of tachyzoites was not affected by piceatannol. By immunofluorescence assay, we noted that the parasite showed abnormalities in cell division after exposure to piceatannol. To determine the in vivo effect of piceatannol on acute infection, a model was established by infecting BALB/c mice with the virulent RH strain of T. gondii. Mice infected with 500 tachyzoites showed a significant therapeutic effect when treated with 15 mg/kg of piceatannol. These results suggest that piceatannol is a promising drug for the treatment of T. gondii.
研究领域:
寄生虫学
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药理学
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免疫学
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产品关联
DOI
PubMed
高影响因子
Frontiers in Microbiology
·
2026
·
IF 5.8
Liyuan Zhang,Yuwen Liu,Daoqun Li,Junwen Luan,Leiliang Zhang
The resurgence of mpox, caused by the mpox virus (MPXV), has intensified the demand for effective antiviral agents. This study evaluates the antiviral activity of piceatannol, a natural polyphenol, utilizing vaccinia virus (VACV) as a model due to the genetic conservation between the two viruses. In vitro experiments demonstrated that piceatannol significantly inhibited VACV replication through both extracellular enveloped virus (EEV), and intracellular mature virus (IMV), with median effective concentrations (EC 50 ) of 76.27 μM, and 63.93 μM, respectively. Further analysis revealed that piceatannol also reduced VACV entry and replication in HeLa cells. Molecular docking studies revealed a stable interaction between piceatannol and the palmitoylated F13 protein of VACV, with a calculated binding energy of−19.06 kcal/mol. This interaction suggests a mechanism by which piceatannol inhibits the generation of EEV. Additionally, piceatannol effectively limited the spread of VACV in cell cultures and exhibited significant virucidal effects on both the IMV and EEV forms. Collectively, our findings suggest that piceatannol holds promise as a therapeutic agent against orthopoxviruses infections by modulating key viral processes, warranting further exploration in clinical settings.
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产品关联
DOI
PubMed
高影响因子
INTERNATIONAL JOURNAL OF BIOLOGICAL MACROMOLECULES
·
2024
·
IF 7.7
Xinxu Yan,Baolong Feng,Hongjie Song,Lili Wang,Yehui Wang,Yulin Sun,Xiaoshuang Cai,Yating Rong,Xibo Wang,Yutang Wang
Natural Xanthine oxidase (XOD) inhibitors represent promising therapeutic agents for hyperuricemia (HUA) treatment due to their potent efficacy and favorable safety profiles. This study involved the construction of a comprehensive database of 315 XOD inhibitors and development of 28 machine learning-based QSAR models. The ChemoPy light gradient boosting machine model exhibited the best performance (AUC = 0.9371 and MCC = 0.7423). This model identified three potential XOD inhibitors from the FooDB database: daphnetin, 7-hydroxycoumarin, and piceatannol. Molecular docking and dynamics simulations revealed favorable interactions, with piceatannol showing a remarkable stability through hydrogen bonding and hydrophobic interactions. ADME predictions suggested that all three compounds possess desirable drug-like properties and safety characteristics. Subsequent in vitro enzyme inhibition assays validated computational predictions, with piceatannol exhibiting the strongest inhibitory activity (IC 50 = 8.80 ± 0.05 μM). Multispectroscopic analyses revealed that piceatannol–XOD binding was predominantly mediated by hydrogen bonding and van der Waals forces, which induced conformational changes characterized by decreased α-helical content and increased proportions of β-sheets, β-turns, and random coils. This study presents an efficient strategy for the identification of natural XOD inhibitors, elucidates the molecular mechanism of piceatannol-mediated XOD inhibition, and establishes a foundation for its therapeutic application in HUA treatment.
研究领域:
药理学
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药物化学
·
生物信息学
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分子生物学
·
药物发现
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产品关联
DOI
PubMed
高影响因子
RSC Advances
·
2020
·Vol. 10
·期 8
·4529-4537
·
IF 3.119
Lili Jiang,Zhen Wang,Xiaoyu Wang,Shujuan Wang,Jun Cao,Yong Liu
Due to their association with type 2 diabetes mellitus treatment, α-glucosidase inhibitors have attracted increasing attention of researchers. In this study, we systemically investigated the kinetics and inhibition mechanism of piceatannol on α-glucosidase. Enzyme kinetics analyses showed that piceatannol exhibited strong inhibition on α-glucosidase in a non-competitive manner. Spectroscopy analyses indicated that piceatannol could bind with α-glucosidase to form complexes via high affinity. Further, computational molecular dynamics and molecular docking studies validated that the binding of piceatannol was outside the catalytic site of α-glucosidase, which would induce conformational changes of α-glucosidase and block the entrance of substrate, causing declines in α-glucosidase activities. Our results provide useful information not only for the inhibition mechanism of piceatannol against α-glucosidase but also for a novel target site for developing novel α-glucosidase inhibitors as potential therapeutic agents in the treatment of type 2 diabetes mellitus.
研究领域:
药理学
·
生物化学
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产品关联
DOI
PubMed
高影响因子
Food Bioscience
·
2025
·
IF 5.9
Ruilu Sun,Wei Li,Minjie Liao,Yiran Yu,Yao Mou,Junfu Ji,Fang Chen,Xiaosong Hu,Lingjun Ma
Resveratrol (RES) and its catechol analog piceatannol (PIC), natural polyphenols, exhibit benefits in relieving glucose metabolism disorders. This study compared their effects on glucose metabolism regulation through in vivo and in vitro studies combined with quantitative analysis. Results showed that PIC significantly ameliorated insulin resistance and inhibited gluconeogenesis in obese mice, exhibiting superior efficacy to RES. Specifically, the area under the curve (AUC) of the intraperitoneal glucose tolerance test (IPGTT) was 2007.38 mmol・L −1 ・h for PIC, lower than 2450.88 mmol・L −1 ・h for RES; the phosphoenolpyruvate carboxykinase (PEPCK) concentration was 172.80 ng・L −1 in the PIC group, lower than 182.12 ng・L −1 in the RES group. At equimolar phenolic hydroxyl concentrations, PIC promoted greater glucose uptake and glycogen accumulation in human hepatocellular carcinoma (HepG2) cells compared to RES. Additionally, PIC accelerated tricarboxylic acid (TCA) cycle flux toward glucose utilization. These findings indicate that PIC is more effective than RES in regulating glucose metabolism, highlighting the critical role of the catechol moiety. This study provides guidance for screening natural bioactive polyphenols.
研究领域:
药理学
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生物化学
·
营养学
·
细胞生物学
·
代谢紊乱
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产品关联
DOI
高影响因子
Natural Product Communications
·
2024
·
IF 1.5
Meng S. Cheong,Lutfun Nahar,Satyajit D. Sarker,Hui Cao,Wai S. Cheang,Jianbo Xiao
Piceatannol is a stilbenoid, which has shown bioactivities in various cell culture models. However, its stability in cell culture medium is not clear. Here, UPLC-MS/MS was applied in situ to analyze the degradation products of piceatannol in Dulbecco's Modified Eagle's Medium (DMEM) and cell culture to investigate the compound's stability in DMEM. During the incubation with cell culture medium (at 4 and 37 °C), several piceatannol derivatives, such as an oxidation product (m/z 243.06), a reduction product (m/z 247.09), dimers (m/z 485.12 and 487.14) and trimers (m/z 727.18) were detected, which demonstrated the instability of piceatannol in cell culture conditions. To confirm if the new products during the incubation were generated due to the instability of piceatannol, ascorbic acid was added. The presence of ascorbic acid could significantly slow the degradation rate of piceatannol and the generation of piceatannol derivatives, which proved that the new products were generated by the degradation of piceatannol and indicated that the instability of piceatannol might be related to its antioxidant activity.
研究领域:
生物化学
·
药物化学
·
分析化学
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产品关联
DOI
高影响因子
Food & Function
·
2017
·Vol. 9
·期 1
·371-378
·
IF 3.247
Yan Zhang,Li-Hong Zhang,Xi Chen,Ning Zhang,Guang Li
Aging is a complex process that is accompanied by neurological damage. Chronic injection of D-galactose (D-gal) can accelerate the aging process similar to natural aging and is commonly used to build an aging model to investigate aging. In the present study, the effects of piceatannol on D-gal-induced aging in mice were evaluated. Piceatannol treatment showed an observable anti-aging effect. Results obtained in vivo showed that piceatannol retained spontaneous motor activity and enhanced spatial learning and memory abilities in mice in which aging was induced by D-gal. Morphometric analysis displayed that piceatannol prevented D-gal-induced neuronal loss, increased the number of Nissl bodies, and promoted cell proliferation in the hippocampus and cortex. Piceatannol also significantly decreased the level of MDA and elevated SOD and CAT activity in the hippocampal and cortical tissues. Furthermore, western blotting results revealed that piceatannol treatment noticeably reversed the suppression of Nrf2 nuclear translocation and increased the expressions of HO-1 and NOQ1 in mice with aging induced by D-gal. Furthermore, piceatannol activated the Nrf2 pathway in natural aging mice, whereas treatment with the Nrf2 inhibitor brusatol reversed the increased expressions of Nrf2, HO-1, and NOQ1. In conclusion, treatment with piceatannol ameliorates behavioral disorder and brain injury in an aging mouse model; this suggests that piceatannol is a promising pharmaceutical candidate for the treatment of age-associated diseases.
研究领域:
老年学
·
神经科学
·
药理学
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产品关联
DOI
PubMed
高影响因子
JOURNAL OF MOLECULAR STRUCTURE
·
2023
·
IF 3.8
Lixia Yuan,Min Liu,Yongfang Ren,Yihao Zhu
Piceatannol (PIC), oxyresveratrol (OXY), and soy protein isolate (SPI) are essential dietary molecules. This study evaluated the interaction between PIC/OXY and SPI using multiple spectroscopic techniques and molecular docking simulations. The static quenching mechanism was confirmed by steady-state fluorescence, Förster resonance energy transfer (FRET), and time-resolved fluorescence (TRF) spectroscopy. The binding affinity of PIC to SPI was stronger than that of OXY, and the interactions were spontaneous and exothermic. The subtle change in the secondary structure of SPI after the addition of PIC or OXY can be ascertained by analyzing the surface hydrophobicity, sulfhydryl group content, particle size, zeta potential, and α-helical content. The emulsifying and foaming properties of SPI were enhanced after complexing with PIC/OXY. The thermodynamic parameters and molecular docking results demonstrated that PIC and OXY bound to SPI at the same sites, and that van der Waals forces (vdW forces) and hydrogen bonding (H-bonding) were the main interaction forces. In addition, the results also showed that the encapsulation of SPI can enhance the antioxidant activity of PIC and OXY. The in vitro gastrointestinal digestion of PIC and OXY in the absence or presence of SPI was evaluated. This study can be used as a reference for further research on the digestion and absorption of SPI−PIC/OXY complexes and as a guide for healthy diets.
研究领域:
食品科学
·
营养学
·
生物化学
·
分子生物学
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DOI
高影响因子
危险品化学品经营许可证（带存储）