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更新于：2025-05-07

Toosendanin

川楝素

更新于：2025-05-07

概要

基本信息

药物类型

化学药

别名-

靶点-

作用方式-

作用机制-

治疗领域

肿瘤神经系统疾病其他疾病

在研适应症

胶质母细胞瘤

非在研适应症-

原研机构

University of Pennsylvania

在研机构

University of Pennsylvania

非在研机构-

权益机构-

最高研发阶段临床前

首次获批日期-

最高研发阶段(中国)-

特殊审评-

结构/序列

分子式C30H38O11

InChIKeyNAHTXVIXCMUDLF-RFNFAWMESA-N

CAS号58812-37-6

关联

100 项与川楝素相关的临床结果

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100 项与川楝素相关的转化医学

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100 项与川楝素相关的专利（医药）

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425

项与川楝素相关的文献（医药）

2025-03-01·Pesticide Biochemistry and Physiology

Toosendanin inhibits the growth of Spodoptera litura by inducing metabolic dysfunction in the midgut

Article

作者: He, BinSheng ; Liang, ShangJin ; Bao, MeiHua ; Huang, Qiao ; Zhou, Yi ; Huang, QiYan ; Zuo, MengTing ; Li, Hai Gang

The Spodoptera litura, a crucial polyphagous pest, has emerged as a major threat to the agricultural sector. Regrettably, despite ongoing efforts, scientists have yet to uncover a safe and efficient control medication to tackle this pressing issue. Toosendanin (TSN), a commercial insecticidal active ingredient used to manage various pests in the field, has adverse effects on Spodoptera litura. However, the effects of TSN on the midgut of S. litura larvae remain unclear. This study explored the mechanism of TSN-induced toxicity and its inhibitory effects on larval growth and development using intestinal pathology, intestinal digestive enzyme activity determination, and intestinal transcriptome sequencing. The results indicated that TSN treatment led to pathological changes in the midgut structure. Analysis of digestive enzyme activity revealed that TSN inhibited the activities of acetyl CoA carboxylase, lipase, α-amylase, and trypsin. Simultaneously, it upregulated superoxide dismutase and reduced malondialdehyde content. Transcriptome analysis revealed that 2151 genes were significantly differentially expressed in the midgut after TSN exposure; the analysis highlighted significant enrichment of DEGs in areas such as hydrolase activity, carbohydrate metabolism, and peptide metabolism. Notably, some key enzymes involved in lipid metabolism, protein metabolism, and carbohydrate metabolism, such as pancreatic triacylglycerol lipase-like, pancreatic lipid-related protein 2-like, lipase3, alpha-amylase, trypsin, and chymotrypsin were downregulated following TSN treatment. This study's findings suggest that TSN causes midgut damage and inhibits larval growth by inducing metabolic dysfunction in the midgut.

2025-02-26·Journal of Agricultural and Food Chemistry

Nanoporous 3D Polyurethane for Toosendanin Adsorption, Encapsulation, and High-Efficient Utilization

Article

作者: Li, Jia ; Wu, Yu-zhen ; Wang, Song ; Wang, Yong-hong ; Chai, Tian-hua ; Wang, Kang ; Ma, Zhiqing ; Li, Wen-kui ; Chen, GuangYou

Nanoporous 3D-polyurethane (3D-PU) was prepared based on nano-CaCO₃ templated controllably confined polymerization assembly and weak acid etching strategies. Nanopores with diameters ranging from 48 to 72 nm were distributed on 3D-PU, facilitating its high BET surface area of 468.0 m²/g. The 3D-PU exhibited enhanced adsorption selectivity to multi-H-bond donors and acceptors, multirings contained compounds based on pore filling, hydrogen-bonding, and π-π interactions; therefore, the novel 3D-PU had promising adsorption ability to toosendanin (TSN) with a maximum theoretical adsorption capacity of 361.6 mg/g. Adsorption isotherm, kinetic, and thermodynamic investigations revealed that the adsorption was heterogeneous and was supported by multiple adsorption sites, controlled by a chemical adsorption mechanism, endothermic, spontaneous, and with increased entropy. Based on the optimized adsorption, the loading capacity (LC) of 3D-PU toward TSN attained 23.4%. After encapsulation, the effective period of TSN was extended to 11 days, the photolysis half-life of TSN was increased 3.2 times, and the LC₅₀ for Aphis citricola was reduced approximately 6.0 times, indicating that 3D-PU effectively improved the performance of TSN. The porous 3D-PU can serve as a promising carrier for more pesticide adsorption, encapsulation, safe, highly efficient, and environmentally friendly utilization.

2025-01-01·Phytomedicine

Toosendanin alleviates acute lung injury by reducing pulmonary vascular barrier dysfunction mediated by endoplasmic reticulum stress through mTOR

Article

作者: Fu, Tianmei ; Wang, Cheng ; Yu, Kuai ; Mao, Xiaocheng ; Wu, Chenggao ; Yin, Fang ; Tang, Hong ; Wei, Caihui ; Liu, Xiaohua ; Le, Aiping ; Liu, Hongfei ; Fang, Yangyang ; Zhang, Zhanglin

BACKGROUNDAcute lung injury (ALI) and acute respiratory distress syndrome (ARDS) are severe clinical conditions with limited treatment options. Toosendanin (TSN), a triterpenoid compound with anti-inflammatory effects, has unclear efficacy in ALI.PURPOSEThis study aimed to evaluate TSN's protective effects on ALI and the related mechanisms.METHODSLipopolysaccharide (LPS)-induced ALI models were developed in vivo and in vitro. Endothelial permeability was measured using Evans Blue dye; lipid reactive oxygen species (ROS) and apoptosis were assessed using flow cytometry. Malondialdehyde (MDA) and superoxide dismutase (SOD) levels were determined, and cell viability was measured. mRNA and protein expression were quantified using qRT-PCR and Western blotting. Network pharmacology and surface plasmon resonance were used to identify and validate TSN's targets.RESULTSTSN reduced endothelial permeability and LPS-induced ALI. It lowered ROS levels, lipid peroxidation, endoplasmic reticulum (ER) stress, and apoptosis, both in vitro and in vivo. Network pharmacology identified mTOR as a key target of TSN, and surface plasmon resonance analysis confirmed TSN's direct binding to mTOR, underscoring mTOR's role in TSN's protective effects against ALI. Western blotting showed that TSN inhibits mTOR and its phosphorylation. In vitro, the mTOR activator MHY1485 reversed TSN's protective effects, increasing ER stress, apoptosis, and endothelial permeability. In vivo, TSN and rapamycin synergistically protected against ALI.CONCLUSIONThis study is the first to demonstrate that TSN protects against ALI by targeting the mTOR pathway, regulating ER stress and apoptosis and mitigating endothelial damage. These findings suggest a novel approach for ALI treatment and underscore TSN's potential clinical value.

100 项与川楝素相关的药物交易

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