AQUACULTURE
·
2025
·
IF 3.9
Fei Yang,Zhiqiang Zhang,Shenye Qu,Gaoxue Wang,Qing Yu,Fei Ling
Micropterus salmoides rhabdovirus (MSRV) is a prominent pathogen that mainly endangers largemouth bass fry, which often causes devastating diseases to largemouth bass and leads to huge economic losses in aquaculture. So far, there is no approved effective measure to control MSRV infection. In the study, 24 magnolol derivatives were used to conduct anti-MSRV activity screening by RT-qPCR, and the results indicated that 5,5′-diallyl-3,3′-dinitro-[1,1′-biphenyl]-2,2′-diol (M3) exhibited the best anti-MSRV efficiency with IC 50 of 0.92 μM. Moreover, further study showed that the CPE induced by MSRV was obviously weaken by M3, and the viral titers were also significantly decreased by M3 within 96 h after MSRV infection ( p < 0.05). Next, the anti-MSRV mechanism of M3 was preliminarily investigated, and the findings illustrated that M3 did not directly act on MSRV virion which had no effect on the infectivity of MSRV. Furthermore, the adsorption of MSRV onto GCO cells was not hindered by M3. The results of cell cycle detected by flow cytometry demonstrated that M3 altered the state of cell cycle arrest in S phase induced by MSRV, influencing the environment required for virus replication. In addition, observation of survival rate and determination of viral load were conducted to further verify the antiviral activity of M3 against MSRV. The results illustrated that administration with M3 at the dose of 20 mg/kg via intraperitoneal injection significantly enhanced the survival rate of largemouth bass infected with MSRV by 35.98 % ( p < 0.01). Moreover, the viral loads of liver, spleen and kidney were significantly decreased by M3 on day 3 and day 5 post MSRV infection ( p < 0.05). Finally, the antiviral effects of M3 against aquatic rhabdoviruses spring viremia of carp virus (SVCV) and infectious hematopoietic necrosis virus (IHNV) were explored, and the results demonstrated that M3 evidently lessened the production of CPE induced by SVCV and IHNV, and inhibited the proliferation of SVCV and IHNV in EPC cells in a dose-dependent manner, with IC 50 of 2.92 μM and 2.78 μM, respectively. To sum up, M3 exhibits a high antiviral activity against MSRV, and is expected to be developed into antiviral specific drugs against rhabdoviruses in aquaculture.
研究领域:
水产养殖学
·
病毒学
·
药理学
✓ 已验证
产品关联
DOI
高影响因子
JOURNAL OF DRUG DELIVERY SCIENCE AND TECHNOLOGY
·
2024
·
IF 4.5
Guohao Mu,Fang Peng,Ziyin Zhang,John M. Brameld,Peter Rose,Xiaogang Yang,Zhi-jiang Jiang,Xi He,Bencan Tang
This study designed and developed a novel three-layer electrostatic, slow-releasing nanoparticle drug delivery system for the treatment of ulcerative colitis. The nanoparticles were composed of layers of zein-based polydopamine, chitosan and cellulose acetate phthalate to form a polyelectrolyte multilayer core−shell nanoparticle structure. The anti-inflammatory natural product magnolol was chosen to be the model drug for the study. The nanoparticles (260.50 ± 23.90 nm) were prepared with layer-by-layer coating and then assessed in vitro and in vivo using a mouse model of ulcerative colitis. The in vitro data confirmed the slow-releasing and pH-dependent characteristics of particles. Quantitative analysis of the in vivo distribution of Mag in mice showed significantly higher concentrations in colonic tissue than in the upper gastrointestinal tract (854.6 ng/g vs 291.5–351.1 ng/g, respectively). Histological and pro-inflammatory cytokine analysis indicated that the nanoparticles had a significant anti-inflammatory effect and were protective against DSS-induced structural damage of the colonic mucosal structure. These results confirm that this nano-delivery system could increase the levels of Mag reaching the colon, resulting in greater efficacy than free Mag in treating UC in this mouse model.
研究领域:
药剂学
·
炎症性肠病研究
·
生物材料
✓ 已验证
产品关联
DOI
高影响因子
AQUACULTURE
·
2025
·
IF 3.9
Shenye Qu,Yihang Liu,Kaiyuan Lu,Yunlong Qin,Jiacheng Qin,Jietao Liu,Xiaohu Wu,Gaoxue Wang,Fei Ling
Ichthyophthirius multifiliis infections constitute a critical challenge demanding urgent resolution in global aquaculture systems. Although over 20 chemicals and natural products have demonstrated efficacy against I. multifiliis in the past two decades, the translation of these findings into clinically viable antiparasitic agents has progressed slowly, with the development of novel potent therapeutics remaining a major challenge. In this study, six novel magnolol-derived compounds were rationally designed through structural optimization of the magnolol scaffold. All synthesized compounds exhibited potent antiparasitic activity against both theront and tomont stages of I. multifiliis . Compound C1 showed superior efficacy to magnolol, with 18-fold and 26-fold lower EC 50 values against theronts (0.035 mg/L) and tomonts (0.024 mg/L) in vitro, respectively. Notably, these activity surpassed the potency of malachite green. Moreover, compound C1 showed lower toxicity than malachite green. ADMET and Density functional theory (DFT) calculations revealed that compound C1 had a favorable electrostatic potential (ESP) distribution and a lower energy gap between Highest Occupied Molecular Orbital (HOMO) and Lowest Unoccupied Molecular Orbital (LUMO), indicating good druggability. Integrated in silico strategy identified Mapk3 (mitogen-activated protein kinase 3) as the primary therapeutic target mediating C1's antiparasitic effects. Protein-Protein Interaction (PPI) network analysis, along with Gene Ontology (GO) and Kyoto Encyclopedia of Genes and Genomes (KEGG) pathway enrichment analysis, suggested that compound C1 might disrupt lipid metabolism and lipoxygenases pathways by modulating Mapk3 expression, thereby exerting potent antiparasitic effects. These findings establish compound C1 as the most potent anti- I. multifiliis agent reported to date. Its potential application in aquaculture may provide valuable insights for addressing this critical bottleneck issue.
研究领域:
药理学
·
水产养殖学
·
计算化学
✓ 已验证
DOI
高影响因子
AQUACULTURE
·
2023
·
IF 4.5
Jietao Liu,Shenye Qu,Tao Wang,Bin Yang,Xiang Liu,Gaoxue Wang,Pengfei Li,Qing Yu,Fei Ling
Natural products have gained recognition as a valuable resource and have significant implications in the field of aquaculture. Nevertheless, the limited water solubility of drugs, leading to compromised bioavailability, has been a persistent challenge in the realm of pharmaceutical research. Magnolol as a natural product, the low solubility leads to limited activity against Ichthyophthirius multifiliis , which severely limits the application of magnolol. Nanosuspensions are considered to be an important strategy to improve the solubility and bioavailability of insoluble drugs. The purpose of this study is to fabricate nanosuspensions that can effectively improve the solubility and antiparasitic activity of magnolol. Magnolol nanosuspensions (MNs) containg Pluronic F68 as a stabilizer was prepared by the solvent-antisolvent precipitation method. The results of TEM , DSC and FTIR analysis showed that the surfactant attached to the surface of magnolol, and the nanosuspensions process significantly reduced the crystallinity and improved the solubility and dissolution rate of magnolol. The Central Composite Design was adopted to investigate the effects of independent variables viz. amount of temperature (A), the ratio of pluronic F68 to magnolol ( w /w) (B), and churning time (C) on particle size (Y), obtaining optimum nanosuspensions with a size of 32.03 nm. Compared with free magnolol, the release rate of magnolol in 119 nm and 35 nm MNs was significantly improved, and the release rate of magnolol was increased from 28.13% to 58.45% and 85.70% within 60 min. Further, the antiparasitic activity of MNs was measured. The results showed the reduction in drug particle size leads to an enhancement in the insecticidal activity of magnolol. Altogether, this study proposes a promising strategy to enhance activity by increasing the solubility of natural products.
研究领域:
水产养殖
·
药剂学
·
天然产物研究
✓ 已验证
产品关联
DOI
高影响因子
PESTICIDE BIOCHEMISTRY AND PHYSIOLOGY
·
2021
·
IF 3.963
Feixu Mo,Xianfeng Hu,Yi Ding,Rongyu Li,Youhua Long,Xiaomao Wu,Ming Li
Rice sheath blight is a destructive fungal disease caused by Rhizoctonia solani . To find a safe and green measure, the biological activity of six plant extracts against R. solani was determined by mycelial growth rate method. The results showed that magnolol possessed better antifungal activities against R. solani , with an EC 50 value of 7.47 mg/L. further action mechanism of magnolol against R. solani was carried out. Studies by scanning electron microscopy (SEM) showed that the morphology of R. solani mycelia was deformation and surface folds. Transmission electron microscope (TEM) observation on treated R. solani showed that magnolol could induce cytoplasmic membrane rupture and cytoplasmic membrane even disappeared completely accompanied with cellular debris was covered around this fungal, and the mycelia treated with magnolol showed fluorescence after PI staining. Further study showed that the content of malondialdehyde (MDA) and activity of chitinase , β-1,3-glucanase and relative conductivity of mycelia were increased, while the content of soluble protein and activities of catalase (CAT), polyphenol oxidase (PPO), superoxide dismutase (SOD), succinate dehydrogenase (SDH) and NAD-malate dehydrogenase (NAD-MDH) were significantly decreased. These results indicated that magnolol could significantly damage the plasma membrane of R. solani , and interfere with cell respiratory metabolism, thus inhibiting the growth of mycelium.
研究领域:
植物学
·
真菌学
·
药理学
✓ 已验证
产品关联
DOI
PubMed
高影响因子
Journal of Pharmaceutical Analysis
·
2013
·
IF 0
Nan Zhou,Xia-Shi Zhu
Ionic liquids functionalized β-cyclodextrin polymer, a mono-6-deoxy-6-(1,2-dimethylimidazolium)-β-cyclodextrin iodide polymer (ILs-β-CDCP), was synthesized as a solid-phase adsorbent coupled with high-performance liquid chromatography for separating or analyzing magnolol in drug samples. The results showed that magnolol was adsorbed rapidly on ILs-β-CDCP and eluted with methanol. Under the optimum conditions, preconcentration factor of the proposed method was 12. The linear range, limit of detection (LOD), correlation coefficient ( R ) and relative standard deviation (RSD) were found to be 0.02–8.00 μg/mL, 1.9 ng/mL, 0.9992 and 2.76% ( n =3, c =2.00 μg/mL), respectively. The interaction between ILs-β-CDCP and magnolol was studied through the inclusion constant, FTIR and TGA analysis. This proposed method has been successfully applied to the determination of magnolol in real samples.
研究领域:
分析化学
·
药物分析
✓ 已验证
产品关联
DOI
PubMed
Artificial Cells Nanomedicine and Biotechnology
·
2018
·
IF 3.026
Pinggang Ding,Hongxue Shen,Jianan Wang,Jianming Ju
The aim of this study was to prepare two novel magnolol (MO)-loaded binary mixed micelles (MO-M) using biocompatible copolymers of Soluplus (SOL) and Solutol® HS15 (HS15), SOL and d-alpha-tocopheryl polyethylene glycol 1000 succinate (TPGS), to improve magnolol’s poor solubility and its oral bioavailability. The organic solvent evaporation method was used to obtain two MO-M by optimization; one was prepared by using SOL and HS15 (MO-H), and the other was prepared by using SOL and TPGS (MO-T). The entrapment efficiency (EE%) and drug loading (DL%) of MO-T were 94.61 ± 0.91% and 4.03 ± 0.19%, respectively, and the MO-H has higher EE% and DL% (98.37 ± 1.23%, 4.12 ± 0.16%). TEM results showed that the morphology of MO-M was homogeneous and was spherical in shape. The dilution stability of MO-M did not undergo significant changes. Permeability of MO-M across a Caco-2 cell monolayer was enhanced in Caco-2 cell transport models. The pharmacokinetics study showed that the relative oral bioavailability of MO-T and MO-H increased by 2.39- and 2.98-fold, respectively, compared to that of raw MO. This indicated that MO-H and MO-T could promote absorption of MO in the gastrointestinal tract. Collectively, the mixed micelles demonstrated greater efficacy as a drug delivery system. The development of these novel mixed micelles is valuable for resolving the poor solubility and bioavailability of drugs.
研究领域:
药剂学
·
生物医学工程
✓ 已验证
产品关联
DOI
PubMed
高影响因子
POLYMER DEGRADATION AND STABILITY
·
2022
·
IF 5.204
Wenwen Guo,Fuwei Liang,Shun Chen,Diantang Zhang,Wenbing Li,Kun Qian,Yang Xu,Bin Fei
A magnolol-derived bisphosphate (MBDPP) was successfully synthesized from the substitution reaction between magnolol and diphenyl phosphoryl chloride. MBDPP was subsequently applied for the fabrication of intrinsically anti-flammable bismaleimide (BMI) thermosets. The effect of MBDPP on the curing kinetics of BMI systems was investigated by the non-isothermal DSC technology, showing that the addition of MBDPP increased the reaction activation energy of the BMI system owing to the steric hindrance of MBDPP. With only 2 wt% of MBDPP, the BMI thermoset achieved an LOI of 35.0% and UL-94 V-0 grade. Besides, the PHRR, MARHE, THE, TSP and mean SEA of the BMI thermoset with 2 wt% of MBDPP were declined by 26%, 33%, 27%, 34% and 50%, respectively, compared to those of the unmodified BMI. The enhanced anti-flammability and smoke suppression performances of the BMI thermosets were attributed to the formation of an intact, expansive and thermally resistant char layer by the presence of MBDPP. Such a char layer effectively blocked the transportation of combustible degradation products to the flame and the thermal radiation of heat to the polymer matrix, so as to slow down the heat release rate and smoke emission.
研究领域:
材料科学
·
化学工程
✓ 已验证
产品关联
DOI
高影响因子
CHEMICAL ENGINEERING JOURNAL
·
2020
·
IF 10.652
Yu Qi,Zhihuan Weng,Kewen Zhang,Jinyan Wang,Shouhai Zhang,Cheng Liu,Xigao Jian
Development of sustainable bio-based epoxy resins having better comprehensive properties than available petroleum-based epoxy resins is of paramount importance for alleviation of energy pressure and enrichment of the potent category of high-performance epoxy resins. In this study, a fully bio-based epoxy resin precursor (DGEM) was synthesized from a naturally occurring magnolol through a highly efficient one step process. The bio-based epoxy resin obtained was then cured with 4, 4′-diaminodiphenyl sulfone (DDS) and compared to the petroleum-based commercial diglycidylether of bisphenol A (DGEBA). After curing with DDS, DGEM/DDS showed higher glass transition temperature than DGEBA/DDS which was 279 °C and 231 °C, respectively. The char yield (in N 2 ), storage modulus and flexural modulus of the former were 1.9-fold, 47.5%, and 41.3% higher than those of the latter, respectively. Interestingly, bio-based epoxy resin of DGEM exhibited excellent processability with extremely low viscosity of 0.155 Pa·s at room temperature and a broader processing window than DGEBA/DDS as well. To exhibit such an excellent processability is very rare for high-performance epoxy resins. In addition, the cured DGEM/DDS also showed outstanding intrinsic flame retardancy, which passed the V-0 rate of UL-94 test. This study offers an opportunity to prepare bio-based epoxy resins with better properties than DGEBA and exhibits great promise in cutting-edge applications.
研究领域:
材料科学
·
化学工程
·
生物质利用
✓ 已验证
产品关联
DOI
高影响因子
JOURNAL OF THE ELECTROCHEMICAL SOCIETY
·
2025
·Vol. 172
·期 4
·047515
·
IF 3.3
Jiajia Lu,Zhiyuan Zheng,Lina Liu,Ningxuan Liu,Yuanyuan You,Xiang Zhou,Ling Lu,Jia Tao,Shaobin Li,Zibin Song,Peng Zhao
Magnolol and honokiol are significant phenolic isomers derived from Magnolia officinalis and are considered promising candidates for potent anticancer drugs. A convenient and rapid method for the simultaneous analysis of magnolol and honokiol is essential for investigating their mechanisms of action and pharmacokinetics. In this study, we developed a composite electrode based on a copper-chelated porous coordination network (PCN-224(Cu)) and carbon nanotubes (CNT). Experimental results demonstrated that the PC-CNT/GCE exhibited a substantial redox potential difference (∼0.14 V) between magnolol and honokiol under differential pulse voltammetry. The modified electrode enabled the simultaneous detection of both compounds in a mixture, showing a linear increase in response current with detection limits (LOD = 3σ/s) of 2.65 μM for magnolol and 11.4 μM for honokiol. Additionally, the sensor exhibited sensitivities of 54.894 μA mM−1 for honokiol and 46.677 μA mM−1 for magnolol. These findings suggest that PCN-224(Cu)-based electrodes hold great potential for the efficient analysis of phenolic isomers in Magnolia officinalis. Furthermore, this study provides a foundation for new applications of porous coordination networks in electrochemical sensing.
研究领域:
分析化学
·
药理学
·
中药学
✓ 已验证
产品关联
DOI
高影响因子
JOURNAL OF FISH DISEASES
·
2023
·Vol. 46
·期 12
·1413-1423
·
IF 2.5
Zhao Zhang,Jing Li,Gaoxue Wang,Fei Ling
Aeromonas hydrophila and A. veronii are widespread and important critical pathogenic bacteria in the aquaculture industry and cause severe economic damage. At present, magnolol has been proved to be a broad-spectrum antibacterial activity, such as A. hydrophila , Staphylococcus aureus and Streptococcus mutans . In order to explore the cause of in vivo disease resistance of magnolol and promote its safe application in aquaculture, the pathological detection and changes in immune indicators of fish after feeding with magnolol were conducted in this paper. Results showed that the diets supplemented with magnolol (3 g magnolol/kg commercial feed) significantly increase the expression level of anti-inflammatory cytokines ( IL-10 , TGF-β and IL-4 ) in the liver of goldfish ( p < .05). Additionally, the expression levels of proinflammatory cytokines ( IL-1β , IL-8 and IFN-γ ) did not increase significantly. Subsequently, this study investigated the resistance of goldfish to A. hydrophila and A. veronii infection after feeding with magnolol. The results showed that the survival rates of treatment groups fed 3 g magnolol/kg commercial feed daily increased by 23.1% and 38.5% after 10 days post A. hydrophila and A. veronii ( p = .0351) infection, respectively. Meanwhile, growth performance (body weight and length), major internal organs (liver, spleen, kidney and intestine) and the serum biochemistry indicators (ATL and AST) all exhibited no significant adverse effects after the goldfish fed with magnolol for 30 days. TP showed an increasing concentration in the treatment group ( p < .05). Results of the mRNA expression of stress response indicated that the expression level of cyp1a and hsp70 was significantly down-regulated after a 30-day treatment ( p < .05), and the two genes recovered to the similar level as the control group after a commercial feed diet. In brief, the diets supplemented with magnolol protected the host from the excessive immune response caused by A. hydrophila and A. veronii via enhancing its anti-inflammatory capacity and had no adverse effects with feeding.
研究领域:
水产养殖学
·
免疫学
·
分子生物学
✓ 已验证
产品关联
DOI
PubMed
高影响因子
JOURNAL OF AGRICULTURAL AND FOOD CHEMISTRY
·
2025
·
IF 6.2
Shenye Qu,Yihang Liu,Jietao Liu,Xiaohu Wu,Pengfei Li,Qing Yu,Gaoxue Wang,Fei Ling
Aquaculture is a rapidly growing sector of global food production, playing a vital role in poverty alleviation, food security, and income generation. However, it faces substantial challenges, particularly due to infections caused by the protozoan Ichthyophthirius multifiliis, leading to reduced yields and economic losses. In this study, two classes of magnolol derivatives (M1–M26) were synthesized and evaluated for their parasiticidal activity against I. multifiliis theronts and tomonts. Based on the determined EC50 values, two significant convolutional neural networks (CNNs) and pharmacophore models were developed, guiding the design and synthesis of three new compounds. Among these, compound new-1 exhibited superior parasiticidal efficacy both in vitro and in vivo compared to magnolol and the commercial parasiticide methylene blue, with EC50 values of 0.197 and 0.252 mg/L, respectively. Toxicity assays demonstrated that compound new-1 showed no significant harmful effects on goldfish and zebrafish embryos at effective concentrations. Further, in silico and experimental analyses identified CDK2 as a molecular target for compound new-1, which disrupted the reproduction and exerts parasiticidal activity against I. multifiliis. Additionally, compound new-1 exhibited antifungal activity against Aspergillus flavus with a MIC of ∼0.8 mg/mL, suggesting its potential application in food preservation. This study provides valuable insights into the development of magnolol-based agents for aquaculture.
研究领域:
水产养殖
·
药物化学
·
计算生物学
·
分子生物学
✓ 已验证
DOI
PubMed
高影响因子
危险品化学品经营许可证（带存储）