AQUACULTURE
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2021
·
IF 4.242
Xiao Tu,Chenxi Duan,Siwei Wu,Shengli Fu,Jianmin Ye
Monogenean parasites are responsible for severe economic losses of both freshwater and marine aquaculture industries. Current chemotherapeutic treatments are consuming, expensive, and harmful to water quality and human health. Medicinal plants are a reliable source of alternative anthelmintic agents. In the pursuit of novel anti-monogenean drugs, in vivo anthelminthic efficacy of 26 selected phytochemical compounds was studied, by choosing Gyrodactylus kobayashi infecting goldfish ( Carassius auratus ) as a model. The screening results showed that four compounds (plumbagin (PLB), thymoquinone, osthole and psoralen) had the highest activity against G. kobayashii with EC 99 value ranging from 0.4 to 4.0 mg/L after 48-h exposure. Among these active compounds, PLB was the most efficacious one and selected for the next study. In vitro trials revealed the clear anti-parasitic effects of PLB, with complete death at 45 min of exposure at a concentration of 2.0 mg/L, withdrawal of PLB afterward did not lead to the recovery of the exposed parasites. Bathing G. kobayashii infected goldfish in PLB also significantly reduced the worm burden, with an extremely low EC 50 value of 0.09 mg/L after 48-h immersion. The results also showed that one short bath using very low concentrations of 0.4–0.7 mg/L for 30–60 min was effective in eliminating G. kobayashii infection with no visible fish toxicity. Acute toxicity assay indicated the 48-h LC 50 of PLB against goldfish was 0.657 mg/L. Furthermore, SEM analysis displayed that PLB-mediated worm killing was associated with the tegumental damages. As seen by TEM , in vivo treatment against G. kobayashii with PLB also caused vacuolization and lysis of parasite's tegument, besides, differing degrees of damage to vitelline cells were observed in treated worms. Collectively, simple chemical structure along with the potent efficacy demonstrated that PLB could serve as an ideal leading compound in the development of a commercial drug to control Gyrodactylus infections in aquaculture
研究领域:
水产养殖学
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药理学
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寄生虫学
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DOI
高影响因子
Immunity Inflammation and Disease
·
2023
·Vol. 11
·期 9
·e1025
·
IF 3.2
Lijie Zhang,Dongxue Liang,Linlin Liu,Lihua Liu
Background Obesity-related asthma, a specific type of asthma, tends to have more severe symptoms and more frequent exacerbations, and it is insensitive to standard medications. Plumbagin (PLB) has many positive effects on human health. However, it remains unclear whether PLB protects against obesity-related asthma. The study investigated the effect of PLB on obesity-related asthma. Methods Four-week-old male C57BL6/J mice were fed either standard-chow diet or high-fat diet (HFD). The mice were sensitized to 100 μg ovalbumin (OVA) once a week and intraperitoneally injected with 1 mg/kg PLB once daily from Week 10 to 11 and then challenged with 10 μg OVA twice a day on Week 12. The lung tissue and bronchoalveolar lavage fluid (BALF) were collected 48 h after the first OVA challenge. Results HFD enhanced inflammatory cell infiltration within the airways and increased total inflammatory cell and eosinophil counts, levels of eosinophil-related inflammatory cytokines, including interleukin-4 (IL-4), IL-5, and eotaxin in BALF, and oxidative stress in the lung tissues of asthmatic mice. PLB reduced inflammatory cell infiltration in the airway walls, levels of eosinophil-related inflammatory cytokines in BALF, and oxidative stress in lung tissues of obese asthmatic mice. In addition, PLB restored HFD-induced decreases in adenosine monophosphate-activated protein kinase (AMPK) phosphorylation. Conclusion The study suggested that HFD exacerbated inflammation and oxidative stress, while PLB probably alleviated inflammation and oxidative stress and activated AMPK pathway to attenuate obesity-associated asthma. Thus, PLB likely had the potential to treat obesity-related asthma.
研究领域:
药理学
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免疫学
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呼吸医学
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肥胖研究
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DOI
PubMed
高影响因子
Materials Today Bio
·
2026
·
IF 11
Xueying Bao,Huanhuan Wang,Man Li,Zhuangzhuang Zheng,Xuanzhong Wang,Jianfeng Guo,Xin Jiang
Docetaxel (DTX)-based concurrent chemoradiotherapy (CCRT) is an important treatment for locally advanced non-small cell lung cancer (NSCLC), but its efficacy is limited by systemic toxicity and radioresistance. Here, we propose an oxidative priming strategy using plumbagin (PLB), a natural redox modulator, to disrupt tumor redox homeostasis and enhance DTX-mediated chemoradiotherapy. PLB markedly sensitized NSCLC cells to DTX, reducing the effective DTX concentration by 33.3-fold in LLC cells and 18-fold in A549 cells. To overcome the pharmacokinetic mismatch between DTX and PLB, we developed a folate receptor-targeted PEGylated liposomal nanoformulation for synchronized co-delivery. This formulation amplified intracellular ROS accumulation to approximately 2.5 times that induced by X-ray alone and 3.3 times that induced by (DTX + PLB)-NP alone, thereby enhancing radiation-induced DNA damage and apoptosis. In vivo, X-ray combined with the targeted nanoformulation achieved a tumor inhibition rate of 99%, while maintaining stable body weight and showing no obvious hematological, hepatic, or renal toxicity. This study provides a redox-guided nanomedicine strategy to enhance DTX-based CCRT for NSCLC at low doses while maintaining favorable preliminary biosafety.
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DOI
PubMed
高影响因子
International Journal of Pharmaceutics-X
·
2026
·
IF 7.9
Xiang Wang,Hengrui Li,Le Wang,Yihan Ma,Miao Qin,Ruonan Sun,Jing Hu
Tumor hypoxia is a major barrier to oxygen-dependent photodynamic therapy (PDT), markedly limiting its therapeutic efficacy in hepatocellular carcinoma (HCC). Herein, a self‑oxygenating and redox-amplifying metal-organic framework (MOF) nanoplatform is constructed by co-loading sorafenib (Sor) and plumbagin (PLB) into a surface galactose functionalized Mn-porphyrinic PCN-224(Mn) (PM) framework to afford SorPLB@Gal-PM for asialoglycoprotein receptor (ASGPR)-mediated HCC targeting. The Mn-porphyrin centers endow SorPLB@Gal-PM with catalase-like activity, enabling in situ decomposition of endogenous H 2 O 2 to generate O 2 and thereby sustaining 1 O 2 -based PDT under irradiation. Meanwhile, Sor/PLB co-delivery, together with PLB-mediated GPX4 suppression, promotes oxidative stress amplification. In hypoxic liver cancer stem cell-like C5WN1 cells, SorPLB@Gal-PM elicits markedly enhanced intracellular ROS upon irradiation, showing approximately 3.4-fold and 2.9-fold higher DCFH-DA signals than SorPLB@Gal-PCN-224 and PM, respectively, accompanied by downregulation of hypoxia-inducible factor-1α (HIF-1α) and glutathione peroxidase 4 (GPX4). In a C5WN1 tumor-bearing nude mouse model, SorPLB@Gal-PM combined with irradiation achieves the most potent tumor suppression with a tumor inhibition rate of 83.70% ± 4.12%. Collectively, SorPLB@Gal-PM provides a hypoxia-adaptive nanoplatform integrating Mn-assisted self‑oxygenation and redox-amplified chemo-PDT for effective HCC therapy.
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DOI
PubMed
高影响因子
PHYTOMEDICINE
·
2025
·
IF 8.3
Zhi-Hua Deng,Liang-Jun He,Shanshan Wei,Chang-Sheng Li,Ya Chen,Xin-Yi Ai,Chatchai Chaotham,Supat Jiranusornkul,Pei-Cheng Zhang,Zhuo Luo,Shang-Ping Xing,Jie Yang
Background Targeting tumor metabolic reprogramming, particularly de novo lipogenesis (DNL) regulated by acetyl-CoA carboxylase 1 (ACC1), constitutes a promising therapeutic strategy. Non-small cell lung cancer (NSCLC) is a predominant subtype of lung cancer, characterized by limited treatment options and poor prognosis. Plumbagin (PLB), a natural naphthoquinone, exhibits broad antitumor activity. However, its direct targets and mechanisms in NSCLC remain unclear. Purpose This study aims to identify the molecular targets of PLB and elucidate its antitumor mechanism in NSCLC. Methods High-resolution mass spectrometry, in conjunction with a biotin-labeled PLB probe, was utilized to identify the direct targets of PLB. Surface plasmon resonance (SPR), streptavidin-based immunoprecipitation, and molecular dynamics simulation were employed to confirm the direct interaction between PLB and ACC1. ACC1 knockdown NSCLC cells were generated using siRNAs, followed by colony formation, wound-healing, and transwell assays. Tissue microarray analysis of clinical NSCLC samples was conducted to assess ACC1 expression and its clinical relevance. Lipid metabolites in NSCLC cells and tissues were quantified using an ELISA, and lipid droplet formation was observed via BODIPY staining. The in vivo therapeutic efficacy of PLB was evaluated using NSCLC xenograft models. Results Proteomic analysis identified ACC1 as a direct PLB target. Binding assays and SPR analyses confirmed the specific interaction between PLB and ACC1, and structural simulations revealed that PLB binds to the carboxyltransferase domain of ACC1 with high affinity. Importantly, tissue microarray analysis revealed that ACC1 was significantly overexpressed in tumor tissues of patients with NSCLC, and high expression of ACC1 was positively correlated with poor prognosis. Mechanistically, PLB inhibited the ACC1/FASN/SCD1 lipogenic axis, resulting in a substantial reduction in lipid metabolites and lipid droplet accumulation. Furthermore, exogenous palmitic acid supplementation partially reversed the antitumor effects of PLB, whereas ACC1 knockdown synergistically enhanced PLB’s antitumor efficacy. In NSCLC xenograft models, PLB significantly inhibited tumor growth by targeting the ACC1/FASN/SCD1 pathway and reducing key lipid metabolites. Conclusion Our findings identify PLB as a novel ACC1 inhibitor that suppresses NSCLC by targeting the ACC1/FASN/SCD1 axis-mediated DNL pathway, highlighting its potential as a metabolic modulator for NSCLC therapy.
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PubMed
高影响因子
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