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COLLOIDS AND SURFACES B-BIOINTERFACES · 2019 · IF 3.973

Enzyme cum pH dual-responsive controlled release of avermectin from functional polydopamine microcapsules

Hongjian Wen,Hongjun Zhou,Li Hao,Huayao Chen,Hua Xu,Xinhua Zhou

Novel enzyme cum pH dual-responsive microcapsule were prepared with an aim to enhance the utilization of pesticides and reduce environmental pollution. The synthetic procedure involved the introduction of urea bonds by forming a covalent bond between isocyanate–functionalized polydopamine (PDA) microcapsules and polyethyleneimine (PEI). The prepared AVM@PDA-IPTS-PEI microcapsules could effectively protect avermectin (AVM) from ultraviolet radiation, and thus decelerate the decomposition rate; the cumulative release showed positive correlations with pH and the urease activity. The AVM release rate was highest at pH 10. At pH 7, the release rate was enhanced after addition of urease, showing improved urease-responsive property under neutral or weak base condition. Especially at pH 7 in presence of urease, the release behavior was in agreement with the Logistic model and able to describe the S-shaped/sigmoidal release profiles, whereas Korsmeyer–Peppas model was better suited in the absence of urease, as the value of K 1 was smaller than 0.45, suggesting that the behavior was controlled by Fick’s diffusion. AVM@PDA-IPTS-PEI displayed better adhesion property than AVM, and the microcapsule ameliorated foliage wettability. AVM@PDA-IPTS-PEI exhibited the insecticidal property similarly with AVM, which can be used for reducing the applied quantity of pesticides and improving their efficacy.

研究领域: 农业科学 · 材料科学 · 环境科学
✓ 已验证 产品关联 DOI PubMed 高影响因子
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ENVIRONMENTAL TOXICOLOGY AND PHARMACOLOGY · 2023 · IF 4.3

Silybin mitigates chronic Avermectin exposure-induced intestinal damage and growth inhibition in carp

Guanglu Wang,Yue Xin,Kaixin Ping,Xuhui Xu,Ying Sun,Xing Li,Xinying Guan,Jingquan Dong

Avermectins, as a new type of environmental pollutant, have received significant attention in recent years. Previous research has shown that acute exposure to avermectins can induce oxidative stress and inflammation in non-target fish species, such as carp. Flavonoid lignans, particularly Silybin, have demonstrated promising biological activities, including regulation of non-alcoholic fatty liver and cerebral ischemia-reperfusion injury. This study aims to investigate the impact of dietary supplementation with Silybin on the intestinal damage in carp caused by chronic exposure to avermectins and to improve the health status and production of carp in aquaculture. Silybin was used as a dietary supplement by adding it to the experimental feed, and an animal experimental model was utilized to assess its effects on oxidative stress, inflammation, and cell apoptosis in carp intestine. Additionally, intestinal barrier integrity, digestive capacity, and fish growth were evaluated. The results indicated that dietary supplementation with Silybin effectively alleviated the oxidative stress induced by chronic exposure to avermectins in carp intestine. Furthermore, Silybin improved intestinal barrier integrity and digestive capacity by modulating the Nrf2/Keap1 pathway. This study demonstrates that dietary supplementation with Silybin can effectively mitigate the intestinal damage caused by chronic exposure to avermectins in carp, providing a sustainable solution for the aquaculture industry to enhance the overall health and production of cultured fish. The research expands our understanding of avermectin environmental pollution and offers a potential remediation approach.

研究领域: 水产养殖 · 环境毒理学 · 药理学 · 鱼类生理学
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COMPARATIVE BIOCHEMISTRY AND PHYSIOLOGY C-TOXICOLOGY & PHARMACOLOGY · 2024 · IF 3.9

Ferulic acid alleviates cardiac injury by inhibiting avermectin-induced oxidative stress, inflammation and apoptosis

Qiao Wang,Shasha Zhang,Jiahao Ding,Zhiqiang Zhang,Xinxuan Li,Yuxin Chen,Yangye Zhu,Danping Zeng,Jingquan Dong,Yi Liu

Avermectin (AVM) is a broad-spectrum antibiotic from the macrolide class, extensively employed in fisheries and aquaculture. Nevertheless, its indiscriminate utilisation has resulted in a substantial accumulation of remnants in the aquatic ecosystem, potentially inflicting significant harm to the cardiovascular system of aquatic species. Ferulic acid (FA) is a naturally occurring compound in wheat grain husks. It possesses potent anti-inflammatory and antioxidant properties, which can help reduce cardiovascular damage. Additionally, its affordability makes it an excellent option for aquaculture usage as a feed additive. This article explored the potential of FA as a feed additive to protect against AVM-induced heart damage in carp. We subjected carp to AVM for 30 days and provided them with a diet of 400 mg/kg of FA. FA substantially reduced the pathogenic damage to heart tissue caused by AVM, as shown through hematoxylin-eosin staining. The biochemical analysis revealed that FA markedly enhanced the activity of antioxidant enzymes catalase (CAT), glutathione (GSH), and total antioxidant capacity (T-AOC) while reducing the malondialdehyde (MDA) content. Furthermore, qPCR analysis demonstrated a substantial increase in the mRNA levels of transforming growth factor-β1 ( tgf-β1 ) and interleukin-10 ( il-10 ) simultaneously, significantly reducing the expression levels of interleukin-10 ( il-6 ), interleukin-1β ( il-1β ), tumor necrosis factor-α ( tnf-α ) and inductible nitric oxide synthase ( inos ). Through the mitochondrial apoptotic route, FA reduced AVM-induced cell death in carp heart cells by upregulating bcl-2 while downregulating the mRNA expression levels of bax , fas , caspase8 and caspase9 . In summary, FA alleviated cardiac injury by inhibiting AVM-induced oxidative stress, inflammatory response, and apoptosis in carp heart tissue.

CAS / MDL: 71751-41-2 1135-24-6
研究领域: 水产养殖学 · 毒理学 · 药理学
✓ 已验证 产品关联 DOI PubMed 高影响因子
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INTERNATIONAL JOURNAL OF BIOLOGICAL MACROMOLECULES · 2026 · IF 8.7

Design-informed construction of self-sufficient cytochrome P450 fusion enzymes for efficient avermectin oxidation

Chao Xiang,Jia-Jia Mou,Yue Jiang,Yu-Ke Cen,Ya-Ping Xue,Yu-Guo Zheng

Cytochrome P450 enzymes hold immense potential as biocatalysts for oxidative reactions but often suffer from inefficient electron transfer due to their reliance on transient interactions with redox partners (RPs). To overcome this limitation, we constructed self-sufficient fusion enzymes by fusing the avermectin-oxidizing P450-Ema1-M212A to selected RPs. Linker sequences were primarily optimized experimentally, while computational modeling, including AlphaFold3-predicted multi-protein assemblies and molecular dynamics simulations, was used as an auxiliary tool to assess feasible linker lengths and interpret the structural basis by which optimized linker design enhances electron-transfer efficiency. Based on literature precedent and preliminary structural considerations, a series of fusion constructs with varying linker sequences and lengths was constructed. Molecular dynamics simulations suggested a structural rationale for why a linker length of 9 amino acids exhibited optimal enzymatic activity, as it stabilized a functional conformation, minimized structural fluctuations, and maintained a favorable distance between the heme and Fe₂S₂ clusters for efficient electron transfer. Experimental characterization confirmed that the F4 variant exhibited substantially increased activity over the non-fusion version. Kinetic analysis demonstrated a significantly enhanced k cat / K m ratio, indicating accelerated catalysis without compromising substrate binding. For the synthesis of 4″-oxo-avermectin, a key intermediate of emamectin, the F4 variant achieved 90% conversion within 8 h, far exceeding the performance of the non-fused system. This study establishes an experimentally driven, semi-rational framework for constructing self-sufficient P450 fusion enzymes, highlighting the synergy between computational prediction and protein engineering for developing powerful biocatalysts with high industrial application potential.

CAS / MDL: 53-59-8
✓ 已验证 产品关联 DOI PubMed 高影响因子
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INDUSTRIAL CROPS AND PRODUCTS · 2026 · IF 6.4

ROS-responsive cinnamaldehyde-based delivery system for targeted delivery and controlled release of avermectin

Yuying Xie,Yangchun Ge,Zhuochao Shen,Yupeng Qiu,Haohua Zhang,Changmeng Sun,Jiangkuan Tang,Honglei Wang,Bingke Li,Junran Xu,Ping Liang,Xuqiang Peng,Lanlan Zhai,Zhongyu Li,Zhihui Li

ROS-triggered release of avermectin from cinnamaldehyde-based delivery system; • Enhanced insecticidal efficacy against Plutella xylostella larvae; • Improved leaf adhesion and favorable plant safety profile; • Stable carriers with high drug loading capacity and encapsulation efficiency. To achieve precise delivery and controlled release of pesticides, this study designed and developed a reactive oxygen species (ROS)-responsive nano-pesticide triggered by the excessively high ROS levels in pests, enabling precise and efficient control of target pests. Using the natural compound cinnamaldehyde as the core, an ROS-responsive amphiphilic small molecule was synthesized, and hydrophobic pesticide avermectin-loaded micelle suspension were successfully prepared through self-assembly. Characterization results showed that the avermectin-loaded micelle suspension had an average particle size of 136.0 nm, a drug loading capacity of 17.78 ± 0.13%, and an encapsulation efficiency of 77.05 ± 0.55%, significantly enhancing the adhesion of pesticides to leaf surfaces. In vitro release experiments confirmed that under micelle suspension, the cumulative release rate was minimal over 50 h, while under simulated high ROS conditions in pests, the cumulative release rate reached 86.02% ± 1.69% over 50 h. Indoor bioassays demonstrated that the micelle suspension exhibited superior efficacy against Plutella xylostella larvae compared to conventional pesticides. Plant safety experiments indicated that the micelle suspension possesses favorable safety profiles. Download: Download high-res image (140KB) Download: Download full-size image This study develops a ROS-responsive pesticide delivery system using self-assembled cinnamaldehyde-based amphiphilic molecules. Upon ingestion by Plutella xylostella larvae, elevated ROS triggers the release of abamectin, leading to efficient pest control.

✓ 已验证 DOI 高影响因子
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INTERNATIONAL JOURNAL OF BIOLOGICAL MACROMOLECULES · 2024 · IF 7.7

Fabrication and property of the avermectin-attapulgite composites regulated by mixed-surfactants and sodium alginate

Xiaoguang Zhang,Jiexiang Liu,Ruili Bai

OA-AP, DTAB-AP, DDBAB-AP complexes were synthesized by introducing surfactants of OA, DTAB and DDBAB into attapulgite (AP). The complexes were systematically characterized. The appearance of new diffraction peaks at low angle indicated a new lamellar structure of OA (DTAB, DDBAB)-AP complexes. Then, the pesticide avermectin (AV) composites of AV/DTAB-OA-AP, AV/DDBAB-OA-AP, sodium alginate (SA) @AV/DTAB-OA-AP and SA@AV/DDBAB-OA-AP were prepared and investigated detailedly. The basal spacings of AV/DTAB-OA-AP and AV/DDBAB-OA-AP were bigger than those of OA-AP and DTAB(DDBAB)-AP. The existences of AV, surfactants and SA molecules of the composites were further confirmed. Furthermore the effect of SA on AV release behaviors of SA@AV/DTAB (DDBAB)-OA-AP microspheres was investigated and compared. Compared to AV/DTAB (DDBAB)-OA-AP, the released rate of the microspheres decreased remarkably. The AV release behaviors of AV/DTAB (DDBAB)-OA-AP could be fitted with pseudo second-order model, while the first-order model was better to describe those of the microspheres. Finally, the bioassay of the microspheres were studied and analyzed. The microspheres had a longer duration and control effect on Mythimna separata . This study could be helpful to provide a pesticide delivery system to improve the utilization efficiency of pesticides.

CAS / MDL: 1119-94-4
研究领域: 农药科学 · 材料科学 · 农业科学
✓ 已验证 产品关联 DOI PubMed 高影响因子
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ACS Applied Nano Materials · 2026 · IF 5.8

Three-in-One Diblock Copolymer Nanoparticles for a Sprayable Pickering Emulsion-Based Avermectin Delivery Platform

Siqi Zheng,Xinyi Wu,Siqi Zhu,Yong Gao

Abstract In this study, diblock copolymer nanoparticles featuring amino-functionalized poly(N,N-dimethylacrylamide) (PDMA) shells and cinnamaldehyde (CA)-loaded poly(diacetone acrylamide) (PDAAM) cores, denoted as NH2-D86D80/CA, were fabricated through RAFT-mediated aqueous polymerization induced self-assembly (PISA). The resultant NH2-D86D80/CA nanoparticles possessed excellent emulsifying performance, prominent antioxidant activity, and tunable surface charge properties. Sprayable oil-in-water Pickering emulsions were subsequently constructed employing the synthesized NH2-D86D80/CA as Pickering emulsifiers. Relative to Pickering emulsions stabilized by non-aminated D86D80/CA counterparts, NH2-D86D80/CA-stabilized Pickering emulsions showed improved foliar retention. Furthermore, NH2-D86D80/CA-stabilized oil-in-water Pickering emulsions were developed as a delivery system for avermectin (Avm). The formulated Avm delivery platform demonstrated superior oxidative stability and excellent insecticidal activity against Rhopalosiphum padi. Bioassay results indicated that the developed formulation demonstrated concentration-dependent insecticidal efficacy while maintaining favorable crop safety at optimal application concentrations.

✓ 已验证 DOI 高影响因子
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International Journal of Polymer Science · 2018 ·Vol. 2018 ·期 1 ·7584281 · IF 1.718

A Comparison Study of Antiultraviolet and Sustained Release Properties of Polydopamine/Avermectin Microcapsule and Microsphere

Zhichuan Shen,Xinhua Zhou,Huina Qiu,Hua Xu,Huayao Chen,Hongjun Zhou

By using dopamine (DA) as the monomer, the model drug avermectin (AVM) was loaded on polydopamine microspheres (AVM/PDAMS) and polydopamine microcapsules (AVM@PDAMC) by the method of impregnation and encapsulation, respectively. The materials’ structures were systematically characterized using Fourier transform infrared spectroscopy (FTIR), zeta potential analysis, scanning electron microscopy (SEM), thermogravimetric analysis (TGA), and differential scanning calorimetry (DSC). The comparison of antiultraviolet capability as well as release behaviors under different pH values of the materials were studied. The results showed that a spherical appearance was observed from both materials. The use of AVM/PDAMS and AVM@PDAMC made the decomposition temperature of AVM increase to 235°C and 245°C, respectively. After being exposed to ultraviolet light for 1400 min, the residual ratios of AVM of AVM/PDAMS and AVM@PDAMC were 42% and 54%, respectively. Both AVM/PDAMS and AVM@PDAMC showed acid sensitivity. AVM/PDAMS and AVM@PDAMC took about 13 h and 60 h to reach the release rate of 50% under pH 3. The release process of AVM/PDAMS could be explained by the Weibull model at pH 3, while the release behavior of AVM@PDAMC fitted the Baker–Lonsdale equation. At pH 7 and pH 9, both of the delivery materials followed the Korsmeyer–Peppas model and belonged to the Fick diffusion.

✓ 已验证 DOI 高影响因子
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PESTICIDE BIOCHEMISTRY AND PHYSIOLOGY · 2022 · IF 4.966

Non-target toxic effects of avermectin on carp spleen involve oxidative stress, inflammation, and apoptosis

Tianmeng Zhang,Zhuhua Dong,Feixue Liu,Enzhuang Pan,Nana He,Fenfen Ma,Xinyu Wu,Yan Wang,Jingquan Dong

Avermectin is one of the most widely used pesticides, but its toxicity to non-target organisms, especially aquatic organisms , has been ignored. Therefore, an acute spleen injury model of avermectin in carp was established to assess the non-target toxicity of avermectin to carp. In this study, 3.005 μg/L and 12.02 μg/L were set as the low and high dose groups of avermectin, respectively, and a four days acute exposure experiment was conducted. Pathological structure observation showed that avermectin damaged spleen tissue structure and produced inflammatory cell infiltration . Biochemical analysis showed that avermectin significantly reduced the activities of antioxidant enzymes CAT, SOD, and GSH-px, but increased the content of MDA, a marker of oxidative damage. Avermectin exposure also significantly increased the transcription levels of inflammatory cytokines such as IL-1β, IL-6, TNF-α, and INOS, and also significantly enhanced the activity of the inflammatory mediator iNOS, but suppressed the transcription levels of anti-inflammatory factors TGF-β1 and IL-10. In addition, TUNEL detected that the apoptosis rate increased significantly with the increase of avermectin dosage, and the transcription levels of apoptosis-related genes BAX, P53, and Caspase 3/9 also increased in a dose-dependent manner. This study is preliminary evidence that avermectin induces spleen injury in carp through oxidative stress , inflammation, and apoptosis, which has important implications for subsequent studies on the effects of avermectin on non-target organisms.

CAS / MDL: 65195-55-3
研究领域: 水生生物学 · 毒理学 · 环境科学
✓ 已验证 产品关联 DOI PubMed 高影响因子
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FISH & SHELLFISH IMMUNOLOGY · 2023 · IF 4.7

Quercetin attenuates avermectin-induced cardiac injury in carp through inflammation, oxidative stress, apoptosis and autophagy

Baoshi Xu,Jilei Yin,Jingchao Qiang,Jiajie Gan,Xuhui Xu,Xing Li,Zunhan Hu,Zibo Dong

As an important antibiotic, avermectin (AVM) has been widely used in China, but its unreasonable application has caused serious harm to the water environment. In view of the various pharmacological effects of quercetin (QUE), such as anti-inflammatory and antioxidant, the scientific hypothesis that “QUE may cause carp poisoning by inhibiting AVM” was proposed in this study. However, its protective effect in AVM -induced heart damage has not been reported. QUE reduced the symptoms of AVM toxicity and decreased the levels of creatine kinase , lactate dehydrogenase , and creatine kinase in the serum of carp. By histological observation, QUE was found to significantly reduce cardiac fiber swelling in carp. A DHE fluorescence probe study showed that QUE was able to inhibit AVM -induced accumulation of reactive oxygen species (ROS) in carp myocardium . We found that QUE significantly increased the intracellular antioxidant enzymes CAT, T-AOC and GSH enzyme activity and reduced intracellular MDA content. In addition, QUE significantly increased il-10 and tgf-β1 expression, and significantly down-regulated tnf-α , il-6 , il-1β and inos expression. Tunel assay showed that QUE attenuated AVM -induced apoptosis, significantly decreased the transcript levels of pro-apoptosis-related genes, and increased the expression of anti-apoptosis-related genes. We also detected the protein expression of LC3 in the AVM group and QUE + AVM group, and found that the expression of LC3 was significantly increased in both groups compared with the Control group, but after adding QUE, the expression of LC3 was significantly decreased compared with the AVM group. In addition, the transcript levels of p62 and atg5 were also detected by qPCR. QUE significantly increased the expression of p62 and decreased the expression of atg5 , suggesting that QUE could attenuate AVM -induced cardiac autophagy in carp. This study will provide preliminary evidence of the principle of QUE attenuating AVM -induced myocardial injury in carp from four aspects, including oxidative stress , inflammatory response, apoptosis and autophagy, and provide a theoretical basis for its prevention and treatment.

CAS / MDL: 71751-41-2 117-39-5
研究领域: 水生毒理学 · 药理学 · 环境科学
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FISH & SHELLFISH IMMUNOLOGY · 2024 · IF 4.1

Ferulic acid alleviates avermectin induced renal injury in carp by inhibiting inflammation, oxidative stress and apoptosis

Qiulu Li,Kaixin Ping,Yannan Xiang,Ying Sun,Zunhan Hu,Shujuan Liu,Xinying Guan,Mian Fu

Avamectin (AVM), a macrolide antibiotic, is widely used in fisheries, agriculture, and animal husbandry, however, its irrational use poses a great danger to aquatic organisms. Ferulic acid (FA) is a natural chemical found in the cell walls of plants. It absorbs free radicals from the surrounding environment and acts as an antioxidant. However, the protective effect of FA against kidney injury caused by AVM has not been demonstrated. In this study, 60 carp were divided into the control group, AVM group (2.404 μg/L), FA+AVM group and FA group (400 mg/kg). Pathological examination, quantitative real-time PCR (qPCR), reactive oxygen species (ROS) and western blot were used to evaluate the preventive effect of FA on renal tissue injury after AVM exposure. Histological findings indicated that FA significantly reduced the swelling and infiltration of inflammatory cells in the kidney tissues of carp triggered by AVM. Dihydroethidium (DHE) fluorescent probe assay showed that FA inhibited the accumulation of kidney ROS. Biochemical results showed that FA significantly increased glutathione (GSH) content, total antioxidant capacity (T-AOC) and catalase (CAT) activity, and decreased intracellular malondialdehyde (MDA) content. In addition, western blot results revealed that the protein expression levels of Nrf2 and p-NF-κBp65 in the carp kidney were inhibited by AVM, but reversed by the FA. The qPCR results exhibited that FA significantly increased the mRNA levels of tgf-β1 and il-10 , while significantly down-regulated the gene expression levels of tnf-α , il-6 and il-1β . These data suggest that FA can reduce oxidative stress and renal tissue inflammation induced by AVM. At the same time, FA inhibited the apoptosis of renal cells induced by AVM by decreasing the transcription level and protein expression level of Bax, and increasing the transcription level and protein expression level of Bcl2, PI3K and AKT. This study provides preliminary evidence for the theory that FA reduces the level of oxidative stress, inflammation response and kidney tissue damage caused by apoptosis in carp, providing a theoretical basis for the prevention and treatment of the AVM.

CAS / MDL: 71751-41-2 1135-24-6
研究领域: 水生毒理学 · 药理学 · 生物化学 · 分子生物学
✓ 已验证 产品关联 DOI PubMed 高影响因子
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INTERNATIONAL JOURNAL OF BIOLOGICAL MACROMOLECULES · 2024 · IF 7.7

High-performance delivery capsules co-assembled from lignin and chitosan with avermectin for sustainable pest management

Xuan Li,Yixin Yun,Yitong Wang,Wanbin Zhu,Quan Bu,Yaxun Fan,Hongliang Wang

Inexpensive biomass materials hold great potential for the development of green delivery systems aimed at improving the extremely low utilization efficiency of pesticides. However, current systems face challenges in achieving both high encapsulation rates and drug loading capacities. This study introduces a novel method using chitosan (CS) and sodium lignosulfonate (SL) to co-assemble with avermectin (AVM), a widely used hydrophobic pesticide, forming AVM-CS-SL micro-nano capsules. Engineered under optimized conditions of pH 5 and 40 °C, the capsules exhibit an AVM encapsulation efficiency of 84.27 % and a loading capacity of 90 %. The AVM-CS-SL capsules demonstrate multifunctional attributes that enhance pesticide application. The capsules, with an average diameter of 356 nm, facilitate stable embedding in leaf grooves and enable effective adhesion to leaf surfaces, thereby improving their resistance to wash-off by rain compared to conventional formulations. Their core-shell structure protects AVM from photodegradation, ensuring long-term stability and efficacy. The capsules also exhibit enhanced bioactivity, with higher mortality rates in Plutella xylostella larvae and low genotoxicity to Vicia faba plants. These findings highlight the strategy of developing multifunctional delivery systems by the co-assembled carrier materials with active ingredients, offering an effective solution for the sustainable development of society and environment.

CAS / MDL: 8061-51-6
研究领域: 农业科学 · 材料科学 · 环境科学
✓ 已验证 产品关联 DOI PubMed 高影响因子
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