PHYSIOLOGICAL AND MOLECULAR PLANT PATHOLOGY
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2026
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IF 3.3
Zhangrui Luo,Jiaxing Yu,Jiaohong Li,Xiaomao Wu
Rosa roxburghii Tratt., a vitamin C-rich edible and medicinal fruit native to southwest China, plays a vital role in poverty alleviation and economic development in mountainous regions. In this study, Neofusicoccum parvum was identified for the first time as a pathogen causing fruit rot in R. roxburghii . Koch's postulates were fulfilled by re-isolating the fungus from artificially inoculated fruits, confirming its pathogenicity. Morphological and molecular analyses further validated the pathogen's identity. The optimal growth conditions for N. parvum were determined to be 28–30 °C and pH 5, with D-fructose and NH 4 Cl as the preferred carbon and nitrogen sources, respectively. Continuous light exposure was found to maximize mycelial growth. Among six tested plant extracts, osthol, Scutellariae Radix extract, and matrine exhibited notable antifungal activity, with osthol showing the highest efficacy (EC 50 = 30.57 μg/mL). Field trials demonstrated that 1% osthol emulsion in water (EW), applied at 300–500-fold dilution, achieved 60.68%–77.57% control efficacy against fruit rot after 21 d of the second application. This performance was comparable to the chemical fungicide 10% difenoconazole water dispersible granule (WG) (67.58%–81.04% efficacy at 5000–7000-fold dilution). This study provides a scientific basis for the biocontrol of N. parvum -induced fruit rot disease in R. roxburghii .
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PEST MANAGEMENT SCIENCE
·
2023
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IF 4.1
Weizhen Wang,Linan He,Zhuzhu Zhang,Wenzhi Li,Jia Chen,Tingting Chen,Youhua Long
BACKGROUND Kiwifruit rot is an important disease caused by different fungal pathogens, which can lead to huge economic loss in the kiwifruit industry. The aims of this study were to discover an effective botanical compound that significantly inhibits the pathogens causing kiwifruit rot, evaluate its control efficacy against this disease, and reveal the underlying mechanisms. RESULTS A strain of Fusarium tricinctum (GF-1), isolated from diseased kiwifruit, could cause fruit rot in both Actinidia chinensis var. chinensis and Actinidia chinensis var. deliciosa . Different botanical chemicals were used for antifungal activity test against GF-1 and thymol was the most effective one with a 50% effective concentration (EC 50 ) of 30.98 mg L −1 . The minimal inhibitory concentration (MIC) of thymol against GF-1 was 90 mg L −1 . Control efficacy of thymol against kiwifruit rot was evaluated and the results indicated that thymol could effectively decrease the occurrence and spread of kiwifruit rot. The mechanisms underlying the antifungal activity of thymol against F. tricinctum were investigated, and it showed that thymol could significantly damage the ultrastructure, destroy the plasma membrane integrity, and instantaneously increase energy metabolisms of F. tricinctum . Further investigations indicated that thymol could extend shelf life of kiwifruit by increasing their storability. CONCLUSION Thymol can effectively inhibit F. tricinctum that is one of the causal agents of kiwifruit rot. Multiple modes of action are involved in the antifungal activity. The results of this study indicate that thymol can be a promising botanical fungicide to control kiwifruit rot and provide useful references for thymol application in agriculture system. © 2023 Society of Chemical Industry.
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NAUNYN-SCHMIEDEBERGS ARCHIVES OF PHARMACOLOGY
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2022
·Vol. 396
·期 4
·683-692
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IF 3.195
Huang Hui,Xue Jie,Xie Tao,Xie Mei-Lin
Osthole is a natural coumarin substance that has an inhibitory effect on hepatic cancer, but its radiosensitization effect on hepatoma cells has not been reported. This study aimed to investigate the effect of osthole. Human HCC-LM3 and SK-Hep-1 hepatoma cells were used and treated with or without osthole, irradiation, or their combination; the cell survival, migration, colony formation, DNA damage repair, intracellular lactic acid content, and glycolysis-related glycogen synthase kinase-3β (GSK-3β), p-GSK-3β, AMP-activated protein kinase (AMPK), p-AMPK, mammalian target of rapamycin (mTOR), p-mTOR, glucose transporter-1 (GLUT-1), GLUT-3, and pyruvate kinase isozyme type M2 (PKM2) protein expressions were determined. Compared with the irradiation group, the osthole plus irradiation group could further decrease the survival rate, migration, colony formation, and DNA damage repair of both hepatoma cells, indicating a synergistic effect of the combination treatment. Moreover, the combination of osthole and irradiation could decrease the content of intracellular lactic acid, ratios of intracellular p-GSK-3β/GSK-3β and p-mTOR/mTOR proteins, and expressions of intracellular GLUT-1/3 and PKM2 proteins, and increase the ratio of intracellular p-AMPK/AMPK proteins. Osthole can increase the radiosensitivity of hepatoma cells, and its radiosensitization mechanisms may be related to glycolytic inhibition by attenuating the GSK-3β/AMPK/mTOR pathway.
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JOURNAL OF AGRICULTURAL AND FOOD CHEMISTRY
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2022
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IF 5.895
Ruige Yang,Zhiyan Liu,Meiyue Han,Liping Cui,Yong Guo
To discover novel natural-product-based insecticide candidates, herein, a variety of osthole-derived N-benzoylthioureas were synthesized and assessed for their insecticidal activities against three insect pests. An insecticidal assay showed that most of the target osthole-derived N-benzoylthioureas displayed a more potent and broad-spectrum insecticidal effect than the parent osthole after the introduction of N-benzoylthioureas on the C-3′ position of osthole. Compound B24 displayed the most potent growth inhibitory (GI) effect on Mythimna separata Walker, with a final corrected mortality rate of 82.1% when treated with a concentration of 1 mg/mL, which was 1.64- and 1.53-fold higher in comparison to osthole and the botanical insecticide toosendanin, respectively. Compounds B22, B23, and B25 displayed a more promising aphicidal effect on Myzus persicae Sulzer, and their LD50 values were 0.015, 0.017, and 0.019 μg/larvae, respectively, superior to the commercially available insecticide rotenone (0.024 μg/larvae). Derivatives B19, B20, B23, and B25 displayed more potent larvicidal activity against Plutella xylostella Linnaeus, with LC50 values of 0.22, 0.26, 0.15, and 0.30 mg/mL, respectively, exceeding that of rotenone (0.37 mg/mL). Furthermore, both compounds B19 and B23 against P. xylostella were found to be more effective than rotenone in a control efficacy assay under greenhouse conditions. The structure–activity relationship (SAR) suggested that osthole-derived N-benzoylthioureas are more active in most cases when the R group is an electron-withdrawing group than when it is an electron-donating group, especially for halogenated groups. Additionally, the potent compounds B19 and B23 possessed good selectivity and were less toxic to non-target organisms. This study suggests that these osthole-derived N-benzoylthioureas could be further studied in depth as eco-friendly natural product pesticides in crop protection.
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ACS Applied Materials & Interfaces
·
2023
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IF 9.5
Chuanyi Gu,Chunru Wang,Wenjie Ma,Yunli Gao,Junyao Li,Qing Jin,Xiaochen Wu
Bacterial infections severely threaten human health; therefore, it is important to endow the matrix for tissue engineering with antibacterial efficiency. The loading of antibacterial drugs on nanomaterials provides an efficient strategy to realize synergistic antibacterial efficiency. By depositing various metal–organic frameworks, such as UIO-66, onto konjac glucomannan (KGM), composite hydrogels (KGM/UIO-66) were created. These hydrogels were used as drug carriers, enabling the development of antibacterial hydrogels with high drug loading capacities (e.g., the maximum loading amount of pterostilbene on KGM/UIO-66 reached 0.157 mg/mg) and sustained drug release. The resulting KGM/UIO-66/pterostilbene hydrogel exhibited a three-dimensional porous structure, excellent biocompatibility, antibacterial efficiency, and anti-inflammatory activity. It effectively protected cells from bacterial attacks while ensuring cell adhesion and proliferation, demonstrating great potential as a three-dimensional substrate for biomedical applications, including tissue engineering and regenerative medicine.
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Frontiers in Chemistry
·
2022
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IF 5.545
Kuang Yi,Xia Yunlong,Wang Xing,Rao Qingqing,Yang Shengxiang
4-hydroxyl coumarin (HC), an important intermediate during the synthesis procedure of rodenticide and anti-cardiovascular drug, shows highly medicinal value and economic value. To achieve the efficient adsorption of HC from natural biological samples, a novel magnetic surface molecularly imprinted polymer (HC/SMIPs) was constructed by employing methacrylic acid (MAA) as functional monomer, organic silane modified magnetic particles as matrix carrier and HC as template molecule. Due to the numerous specific imprinted cavities on the HC/SMIPs, the maximum adsorption capacity of HC/SMIPs for 4-hydroxycoumarin could reach to 22.78 mg g−1 within 20 min. In addition, HC/SMIPs exhibited highly selective adsorption for 4-hydroxycoumarin compared with other active drug molecules (osthole and rutin) and showed excellent regeneration performance. After 8 cycles of adsorption-desorption tests, the adsorption capacity of HC/SMIPs just slightly decreased by 6.64%. The efficient selective removal and easy recycle of 4-hydroxycoumarin from biological samples by HC/SMIPs made a highly promising to advance the application of imprinting polymers in complex practical environments.
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PESTICIDE BIOCHEMISTRY AND PHYSIOLOGY
·
2023
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IF 4.7
Duo Lai,Delin Wang,Xuehua Shao,Jian Qin,Qingli Zhuang,Hanhong Xu,Weiqiang Xiao
Blue mold induced by Penicillium choerospondiatis is a primary cause of growth and postharvest losses in the fruit of Phyllanthus emblica . There is an urgent need to explore novel and safe fungicides to control this disease. Here, we demonstrated osthole, a natural coumarin compound isolated from Cnidium monnieri , exhibited a strong inhibitory effect on mycelia growth, conidial germination rate and germ tube length of P. choerospondiatis , and effectively suppressed the blue mold development in postharvest fruit of P. emblica . The median effective concentration of osthole was 9.86 mg/L. Osthole treatment resulted in cellular structural disruption, reactive oxygen species (ROS) accumulation, and induced autophagic vacuoles containing cytoplasmic components in fungal cells. Transcriptome analysis revealed that osthole treatment led to the differentially expressed genes mainly enriched in the cell wall synthesis, TCA cycle, glycolysis/ gluconeogenesis , oxidative phosphorylation . Moreover, osthole treatment led to increase genes expression involved in peroxisome , autophagy and endocytosis . Particularly, the autophagy pathway related genes ( PcATG1 , PcATG3 , PcATG15 , PcATG27 , PcYPT7 and PcSEC18 ) were prominently up-regulated by osthole. Summarily, these results revealed the potential antifungal mechanism of osthole against P. choerospondiatis . Osthole has potentials to develop as a natural antifungal agent for controlling blue mold disease in postharvest fruits.
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STRAHLENTHERAPIE UND ONKOLOGIE
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2023
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IF 3.1
Huang Hui,Xue Jie,Xie Mei-Lin,Xie Tao
Purpose Osthole possesses anti-tumor activities. However, whether osthole can have a radiosensitization effect on hepatic cancer remains unclear. Here, an HCC-LM3 cells-inoculated subcutaneous transplanted tumor was adopted to explore the effect of osthole. Methods The tumor-bearing mice were treated with 100 mg/kg osthole for 12 days, 4 Gy irradiation twice, or their combination. The tumor volume and weight, lactic acid content, glycolytic enzyme activities, and protein expression of glycogen synthase kinase 3β (GSK-3β), p‑GSK-3β, mammalian target of rapamycin (mTOR), p‑mTOR, AMP-activated protein kinase (AMPK), p‑AMPK, glucose transporter 1/3, and pyruvate kinase M2 were determined. The GSK-3β-overexpressed HCC-LM3 or SK-Hep‑1 cell models were also adopted to verify the effects of osthole on expression of these proteins. Results The tumor volume and weight, lactic acid content, and glycolytic enzyme activities in tumor tissues were lower in the osthole + radiation group than in the radiation group. Moreover, osthole could reverse the radiation-induced increments of p‑GSK-3β/GSK-3β and p‑mTOR/mTOR protein ratios and the expression of glucose transporter 1/3 and pyruvate kinase M2 proteins in tumor tissues, and increase the protein ratio of p‑AMPK/AMPK. The effects of osthole on these glycolysis-related proteins were also observed in GSK-3β-overexpressed HCC-LM3 or SK-Hep‑1 cell models. Conclusion Osthole has a radiosensitizing effect on subcutaneous transplanted hepatocellular carcinoma, and its mechanism may be related to inhibition of GSK-3β/AMPK/mTOR pathway-controlled glycolysis.
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PESTICIDE BIOCHEMISTRY AND PHYSIOLOGY
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2023
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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.
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Journal of Oncology
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2021
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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.
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PHARMAZIE
·
2021
·Vol. 76
·期 10
·503-506
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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.
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Oxidative Medicine and Cellular Longevity
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2021
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IF 6.543
Lijun Fang,Wei Wang,Jiazheng Chen,Anju Zuo,Hongmei Gao,Tao Yan,Pengqi Wang,Yujia Lu,Ruijuan Lv,Feng Xu,Yuguo Chen,Linmao Lyu
Idiopathic pulmonary fibrosis (IPF) is a chronic progressive lung disease characterized by the extensive accumulation of myofibroblasts and collagens. However, the exact mechanism that underlies this condition is unclear. Growing evidence suggests that NADPH oxidases (NOXs), especially NOX4-derived oxidative stress, play an important role in the development of lung fibrosis. Bleomycin (BLM) is a tumor chemotherapeutic agent, which has been widely employed to establish IPF animal models. Osthole (OST) is an active constituent of the fruit of Cnidium ninidium. Here, we used an in vivo mouse model and found that OST suppressed BLM-induced body weight loss, lung injury, pulmonary index increase, fibroblast differentiation, and pulmonary fibrosis. OST also significantly downregulated BLM-induced NOX4 expression and oxidative stress in the lungs. In vitro, OST could inhibit TGF-β1-induced Smad3 phosphorylation, differentiation, proliferation, collagen synthesis, NOX4 expression, and ROS generation in human lung fibroblasts in a concentration-dependent manner. Moreover, NOX4 overexpression could prevent the above effects of OST. We came to the conclusion that OST could significantly attenuate BLM-induced pulmonary fibrosis in mice, via the mechanism that involved downregulating TGF-β1/NOX4-mediated oxidative stress in lung fibroblasts.
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