PESTICIDE BIOCHEMISTRY AND PHYSIOLOGY
·
2023
·
IF 4.7
Ke Hu,Rongyu Li,Feixu Mo,Yi Ding,Aiai Zhou,Xue Guo,Ruotong Li,Min Li,Minggui Ou,Ming Li
Dendrobium officinale Kimura et Migo is a traditional Chinese herbal medicinal plant . However, the frequent occurrence of soft rot disease (SRD) is one of the most harmful diseases in D. officinale production in recent years, which can seriously affect its yield and quality. In this study, the major pathogenic fungus (SR-1) was isolated from D. officinale with typical symptoms of SRD, and was identified as Fusarium oxysporum through morphological and molecular identification. The biological activities of five natural products were determined against F. oxysporum using a mycelial growth inhibition assay. The results showed that osthole had the highest antifungal activity against F. oxysporum , with an EC 50 value of 6.40 mg/L. Scanning electron microscopy (SEM) showed that osthole caused F. oxysporum mycelia to shrink and deform. Transmission electron microscopy (TEM) showed that the organelles were blurred and the cell wall was thickened in the presence of osthole. The sensitivity of F. oxysporum to calcofluor white (CFW) staining was significantly enhanced by osthole. Relative conductivity measurements and propidium iodide (PI) observation revealed that osthole had no significant effect on the cell membrane. Further experiments showed that the activity of chitinase and β-1,3-glucanase were decreased, and expression levels of chitinase and β-1,3-glucanase related genes were significantly down-regulated after treatment with osthole. In conclusion, osthole disrupted the cell wall integrity and dynamic balance of F. oxysporum , thereby inhibiting normal mycelial growth.
研究领域:
植物病理学
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药用植物学
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产品关联
DOI
PubMed
高影响因子
PROGRESS IN ORGANIC COATINGS
·
2024
·
IF 6.5
Yanru Qin,Shupeng Wang,Yong Fan,Li Wang,Chengchun Zhang,Jie Zhao,Luquan Ren
Excessive underwater drag, coupled with a heavy marine fouling, not only adversely affects the operation and speed of ships but also leads to increased energy and fuel consumption. Inspired by the remarkable drag reduction and anti-biofouling capabilities of dolphin skin, we have developed a flexible polyurethane (PU) coating infused with osthole (OST). This coating not only exhibits exceptional drag reduction by postponing the boundary layer transition from laminar to turbulent flow but also demonstrates robust anti-biofouling properties under both dynamic and static scenarios. The resultant PU x /OST y composite coating achieved the drag reduction efficiency of 8.20 % to 12.65 % with mean flow velocities ranging from 1 to 6 m/s. The PU x /OST y surfaces also displayed highly enhanced anti-biofouling performances, with ∼98.4 % and 97.5 % reduction for green algae Chlorella and the diatom N. closterium , respectively, as well as ∼99.4 % reduction against P. pantotrophus . Furthermore, the PU x /OST y coating had amazing durability in extreme environments, such as light aging, cycle sand abrasion, thermal aging, ultrasonic treatment, and tape-peeling. Therefore, this study underscores the potential of the bioinspired flexible coating for the application of underwater devices with prominent drag reduction and antifouling performance.
研究领域:
材料科学
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海洋生物学
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DOI
高影响因子
TOXICOLOGY LETTERS
·
2025
·
IF 2.9
Siyu Liu,Guode Zhao,Yingyun Xu,Yang Wang,Zifang Ding,Weiwei Li,Ying Peng,Jiang Zheng
Osthole (OST), a coumarin derivative, is one of the major components of Cnidium monnieri (L.) Cussion. OST was reported to induce apoptosis in hepatocytes. Elevated serum ALT and AST were documented in Sprague-Dawley rats after administration of OST. In the present study, OST was found to be metabolized to a phenol metabolite which was further metabolically oxidized to the corresponding quinone methide intermediate. A glutathione conjugate derived from the reactive metabolite was detected in vitro and in vivo . The structures of the metabolites were verified by chemical analysis. CYP3A4 and CYP1A2 were the major enzymes to catalyze the oxidation reactions. Pre-treatment with 1-aminobenzotriazole or ketoconazole decreased the susceptibility of primary hepatocytes to the cytotoxicity of OST. The findings provided solid evidence that the metabolic activation of OST correlated with the cytotoxicity of OST.
研究领域:
药理学
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毒理学
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产品关联
DOI
PubMed
高影响因子
Chemical Biology & Drug Design
·
2025
·Vol. 105
·期 5
·e70113
·
IF 3.3
Ming Tong,Meng Liu,Liang Chen,Yi-he Lin,Qing Zheng
Liver fibrosis is pathologically associated with ferroptosis. Osthole (OST) has good therapeutic effects on liver fibrosis. Our study sought to investigate the pharmacological effects of OST on ferroptosis in hepatic stellate cells (HSCs) during the development of liver fibrosis and define the mechanisms involved. The in vivo model of liver fibrosis was established by CCl 4 treatment. MTT and EDU assays were used to assess cell viability and proliferation, respectively. The interaction between myocyte enhancer factor 2A (MEF2A) and Y-box binding protein 1 (YBX1) was analyzed by dual luciferase reporter and chromatin immunoprecipitation (ChIP) assays. OST treatment alleviated CCl 4 -induced liver fibrosis in mice by activating ferroptosis. OST induced ferroptosis in HSCs and inhibited the activation of HSCs in vitro, while these effects of OST were reversed by MEF2A overexpression or YBX1 overexpression. Mechanistically, MEF2A activated the Wnt/β-catenin signaling by transcriptionally facilitating YBX1 expression. As expected, the inactivation of Wnt/β-catenin signaling or YBX1 knockdown could reverse the regulatory effect of MEF2A upregulation on the activation of HSCs and ferroptosis in OST-treated HSCs. OST mitigated liver fibrosis by inducing ferroptosis in HSCs and repressing the activation of HSCs through inhibiting the MEF2A/YBX1/Wnt/β-catenin axis.
研究领域:
药理学
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分子生物学
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肝脏病学
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产品关联
DOI
PubMed
高影响因子
JOURNAL OF EXPERIMENTAL & CLINICAL CANCER RESEARCH
·
2018
·Vol. 37
·期 1
·1-11
·
IF 6.217
Dai Xuanxuan,Yin Changtian,Zhang Yi,Guo Guilong,Zhao Chengguang,Wang Ouchen,Xiang Youqun,Zhang Xiaohua,Liang Guang
Background Triple-negative breast cancer (TNBC) is an aggressive subgroup of human breast cancer. Patients with TNBC have poor clinical outcome as they are non-responsive to current targeted therapies. There is an urgent need to identify new therapeutic targets and develop more effective treatment options for TNBC patients. Osthole, a natural product from C. monnieri, has been shown to inhibit certain cancer cells. However, the mechanisms of action as well as its effect on TNBC cells are not currently known.Methods We investigated the effect of osthole in cultured TNBC cells as well as in a xenograft model of TNBC growth. We also used a high-throughput proteomics platform to identify the direct binding protein of osthole.Results We found that osthole inhibited the growth of a panel of TNBC cells and induced apoptosis in both cultured cells and TNBC xenografts. We used a high-throughput proteomics platform and identified signal transducer and activator of transcription 3 (STAT3) as a potential binding protein of osthole. We further show that osthole suppressed STAT3 in TNBC cells to inhibit growth and induce apoptosis. Overexpressing STAT3 in TNBC reduced the effectiveness of osthole treatment.Conclusion sThese results provide support for osthole as a potential new therapeutic agent for the management of TNBC. Moreover, our results indicate that STAT3 may be targeted for the development of novel anti-TNBC drugs.
研究领域:
肿瘤学
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分子生物学
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药理学
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产品关联
DOI
PubMed
高影响因子
Journal of Oncology
·
2021
·
IF 4.375
Jie Mei,Tiejun Wang,Shaojie Zhao,Yan Zhang
Osthole (OST) is a plant-derived compound that can inhibit the proliferation of tumor cells and has a tumor-suppressive effect in multiple types of cancers. However, the mechanisms of OST-mediated breast cancer (BrCa) inhibition were still largely unknown. In this study, we made full use of the GSE85871 dataset to identify potential targets of OST in BrCa via multiple bioinformatics analysis. Next, a series of in vitro experiments were conducted to check the role of GNG7 in BrCa and the relationship between OST and GNG7. Through a series of bioinformatics analyses, GNG7 was identified as a potential target of OST, which could be significant upregulated by OST exposure in BrCa cells. Besides, GNG7 was lowly expressed in BrCa tissues compared with normal breast tissues, and BrCa patients with low GNG7 expression had shorter overall survival (OS) and relapse-free survival (RFS) compared with those with high GNG7 expression. Moreover, GNG7 silencing significantly enhanced cell proliferation and inhibited apoptosis, and exogenous overexpression of GNG7 showed reverse effects on BrCa cells. Last but not least, GNG7 inhibition could notably rescue OST-mediated cytotoxic effects. In summary, we identified GNG7 as a novel target for OST in BrCa and a potential tumor suppressor. Thus, OST could be therapeutically beneficial for BrCa through a GNG7-dependent mechanism.
研究领域:
癌症生物学
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分子生物学
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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
JOURNAL OF SOLUTION CHEMISTRY
·
2022
·Vol. 51
·期 10
·1199-1208
·
IF 2
Wu Jieyu,Yin Tianxiang,Wang Xiaoyong
Deep eutectic solvents (DES), as a new type of green solvent, show great advantages of easy preparation and no need of purification after synthesis and great potential applications in various fields. Osthole has shown wide variety of pharmacological functions like antimicrobial, anti-inflammatory, antioxidant, or anti-cancerous. To explore the efficient delivery of osthole, we have designed a new DES based on osthole and DL-menthol with molar ratio of 1:15. The interaction between osthole and DL-menthol was checked and verified by 1 HNMR and FT-IR spectra. The physicochemical properties and anti-bacterial activity of the DES were investigated. Low viscosity and higher anti-bacterial activity against S. aureus make the DES suitable for the dermal or transdermal delivery of osthole. Therefore, the results presented herein indicated that DES may serve as a new strategy for the application of active pharmaceutical ingredients.
研究领域:
药学
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材料科学
·
化学
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DOI
高影响因子
Biochemistry and Cell Biology
·
2017
·Vol. 95
·期 4
·
IF 1.895
Junhong Guan,Xiangtai Wei,Shengtao Qu,Tao Lv,Qiang Fu,Ye Yuan
Stroke is a common cerebrovascular disease in aging populations, and constitutes the second highest principle cause of mortality and the principle cause of permanent disability, and ischemic stroke is the primary form. Osthole is a coumarin derivative extracted from the fruits of Cnidium monnieri (L.) Cusson. In this study, we established a rat model of middle cerebral artery occlusion/reperfusion (MCAO/R) in vivo and found that MCAO/R caused cerebral infarction, hippocampus neuronal injury and apoptosis, and also activated the Notch 1 signaling pathway. However, treatment with osthole further enhanced the activity of Notch 1 signaling and reduced the cerebral infarction as well as the hippocampus neuronal injury and apoptosis induced by MCAO/R in a dose-dependent manner. The same results were observed in a primary neuronal oxygen glucose deficiency/reperfusion (OGD/R) model in vitro, and the effect of osthole could be blocked by an inhibitor of Notch 1 signaling, N-[N-(3,5-difluorophenacetyl)-l-alanyl]-S-phenylglycine tert-butyl ester (DAPT). Therefore, we demonstrated that osthole injection prevented rat ischemia–reperfusion injury via activating the Notch 1 signaling pathway in vivo and in vitro in a dose-dependent manner, which may be significant for clinical treatment of ischemic stroke.
研究领域:
神经科学
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药理学
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分子生物学
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DOI
PubMed
高影响因子
PHARMAZIE
·
2021
·Vol. 76
·期 10
·503-506
·
IF 1.267
Pan Liuliu,Zhang Xiaodan,Wang Danhan,Huang Min,Huang Qiusui,Duan Ping,Mei Jie
Discovering compounds with anti-cervical cancer effect and clarifying their targets will help promoting the precise treatment of cervical cancer. The present study intended to clarify the effect of osthole on cervical cancer cells, and to explore the possibility of DCLK1 as its target.
Annexin V-PE staining and flow cytometry methods were used to determine cell apoptosis. Meanwhile, apoptosis related biomarkers were probed by immunoblotting. The MTT assay was employed to study the effect of osthole in combined with or without LRRK2-IN-1 (a DCLK1 inhibitor) on cell proliferation.
Then, combination index was determined. To examine the interaction of osthole with DCLK1, molecular docking was carried out. Based on the biological database from cBioPortal, the association between DCLK1 and clinical manifestations of cervical cancer were evaluated. The results showed that
osthole can significantly induce apoptosis of HeLa and Me-180. When combined with LRRK2-IN-1, the effect of osthole on cell proliferation was antagonized, suggesting that it might competitive binding to DCLK1. Furthermore, molecular docking showed that osthole interacts with Val468 residues
of DCLK1 to form hydrogen bonds. The analysis of database showed that DCLK1 frequently mutant and deleted in cervical cancer, and is related to cell survival, tumor progression and recurrence. However, no obvious correlations were found between DCLK1 and lymphatic metastasis/differentiation.
In conclusion, osthole significantly inhibits the survival of cervical cancer cells. It's probably target DCLK1 mechanistically via interacting with Val468. DCLK1 could be a potential therapeutic target for cervical cancer.
研究领域:
肿瘤学
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药理学
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分子生物学
·
癌症研究
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产品关联
DOI
PubMed
高影响因子
MEDIATORS OF INFLAMMATION
·
2018
·
IF 3.549
Yiyi Jin,Jianchang Qian,Xin Ju,Xiaodong Bao,Li Li,Suqing Zheng,Xiong Chen,Zhongxiang Xiao,Xuemei Chen,Weiwei Zhu,Weixin Li,Wencan Wu,Guang Liang
Inflammation is a key factor in the pathogenesis of ALI. Therefore, suppression of inflammatory response could be a potential strategy to treat LPS-induced lung injury. Osthole, a natural coumarin extract, has been reported to protect against acute kidney injury through an anti-inflammatory mechanism, but its effect on ALI is poorly understood. In this study, we investigated whether osthole ameliorates inflammatory sepsis-related ALI. Results from in vitro studies indicated that osthole treatment inhibited the LPS-induced inflammatory response in mouse peritoneal macrophages through blocking the nuclear translocation of NF-κB. Consistently, the in vivo studies indicated that osthole significantly prolonged the survival of septic mice which was accompanied by inflammation suppression. In the ALI mouse model, osthole effectively inhibited the development of lung tissue injury, leukocytic recruitment, and cytokine productions, which was associated with inhibition of NF-κB nuclear translocation. These findings provide evidence that osthole was a potent inhibitor of NF-κB and inflammatory injury and suggest that it could be a promising anti-inflammatory agent for therapy of septic shock and acute lung injury.
研究领域:
药理学
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免疫学
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病理学
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分子生物学
✓ 已验证
产品关联
DOI
PubMed
高影响因子
Insects
·
2023
·Vol. 14
·期 9
·725
·
IF 3
Fang Dong,Xin Chen,Xingyuan Men,Zhuo Li,Yujun Kong,Yiyang Yuan,Feng Ge
Simple SummaryThe excessive utilization of chemical pesticides has resulted in the emergence of pesticide resistance, the disturbance of ecosystems, environmental degradation, and health hazards. Botanical pesticides offer a promising alternative to chemical pesticides, as they have minimal impacts on human health and the environment. Osthole, which has shown pesticidal activities, is the primary bioactive compound inCnidium monnieri(L.) Cusson. In this study, we assessed osthole for its contact toxicity, antifeedant activity, and oviposition preference against three agricultural pests: theTetranychus urticae,Myzus persicae, andBactrocera dorsalis, using laboratory bioassays. Osthole exhibited pesticidal effects against theT. urticaeandM. persicae, impeding their fecundity and development. Additionally, it demonstrated significant antifeedant activity against theT. urticaeand acted as a potent attractant for oviposition by theB. dorsalis. These findings highlight and expand the potential of osthole as a botanical pesticide for the control of these agricultural pests.AbstractOsthole, the dominant bioactive constituent in theCnidium monnieri, has shown acute pesticidal activities. However, its detailed toxicity, antifeedant, and oviposition preference effects against agricultural pests have not been fully understood, limiting its practical use. This study aimed to investigate the contact toxicity, antifeedant activity, and oviposition preference of osthole against three agricultural pests (Tetranychus urticae,Myzus persicae, andBactrocera dorsalis). Our results showed that theCnidium monnieri(L.) Cusson (CMC) has a high osthole content of 11.4 mg/g. Osthole exhibited a higher level of acute toxicity against theT. urticaeto four other coumarins found in CMC. It showed significant pesticidal activity againstT. urticaeandM. persicaefirst-instar nymphs and adults in a dose-dependent manner but not againstB. dorsalisadults. Osthole exposure reduced the fecundity and prolonged the developmental time of theT. urticaeandM. persicae. Leaf choice bioassays revealed potent antifeedant activity in theT. urticaeandM. persicae. Furthermore, the femaleB. dorsalisshowed a distinct preference for laying eggs in mango juice with 0.02 mg/mL osthole at 48 h, a preference that persisted at 96 h. These results provide valuable insights into the toxicity, repellent activity, and attractant activity of osthole, thereby providing valuable insights into its potential efficacy in pest control.Keywords:botanical pesticide;osthole;antifeedant;oviposition preference;Tetranychus urticae;Myzus persicae;Bactrocera dorsalis
研究领域:
害虫管理
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植物化学
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农业科学
✓ 已验证
产品关联
DOI
PubMed
高影响因子
BIOMEDICINE & PHARMACOTHERAPY
·
2025
·
IF 7.5
Yinlan Xu,Hejun Liu,Haonan Guo,Jinmei Zheng,Ling Tao,Weidong Wu
Non-small cell lung cancer (NSCLC) is the major type of malignant tumor in the lungs. Emerging epidemiological evidence implicates environmental copper exposure as a potential risk modulator for NSCLC progression. This study investigated the effects of low-dose Copper (Cu) exposure on A549 cells and evaluated the therapeutic potential of two natural compounds, osthole and matrine. The results demonstrated that Cu exposure (5 μg/mL, 12 h) significantly promoted the migration, invasion and colony formation of A549 cells ( P < 0.05), accompanied by a reduction in cell apoptosis, a decrease in ROS levels and an increase in mitochondrial membrane potential. Meanwhile, osthole and matrine treatment could reverse these phenotypes and arrest the cell cycle of A549 in the G1 phase. Transmission electron microscopy results revealed that Cu exposure induced slightly swollen mitochondria and as well as the increase in the number of mitochondria, while osthole and matrine treatments resulted in severe degenerative changes in mitochondria. Both qPCR and Western blot examinations indicated that Cu exposure promoted the expression of PGC-1α but inhibited the expressions of STAT1, TNF-α and IL-2. Osthole treatment could down-regulate the expression of PGC-1α and up-regulate the expressions of STAT1, TNF-α and IL-2, while matrine treatments could up-regulate the expressions of STAT1 and TNF-α and down-regulate the expressions of PGC-1α and IL-2. Taken together, these findings indicate that low-dose Cu exposure can promote the proliferation, migration, invasion and mitochondrial damage of A549 cells, while osthole and matrine treatments inhibit Cu effects by regulating the STAT1, BGC-1 α, TNF-α and IL-2.
研究领域:
肿瘤学
·
环境毒理学
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药理学
·
细胞生物学
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分子生物学
·
天然产物化学
✓ 已验证
产品关联
DOI
PubMed
高影响因子
危险品化学品经营许可证（带存储）