International Journal of Environmental Research
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2017
·Vol. 11
·期 4
·515-521
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IF 0.927
Fu Wei,Huang Kai,Cai Hong-Hong,Li Jian,Zhai De-Li,Dai Zhi-Cong,Du Dao-Lin
Heavy metal pollution of the soil has become a global threat to the terrestrial environment, food security, and human health due to their non-biodegradable and high persistent characteristics in the soil. However, the effective measurements for the restoration of these polluted soils are rare; therefore, this study was conducted to investigate the role of four naturalized plants ( Celosia argentea , Praxelis clematidea , Eupatorium adenophora , and Solidago canadensis ) as potential resources for the remediation of cadmium
contamination through a tolerance and accumulation experiment. The plants’ morphological phenotype (growth and biomass), physiological phenotype (relative chlorophyll content, leaf nitrogen content, root cell activity, and reactive oxygen species), and cadmium accumulation were evaluated using the hydroponic method. The results showed that cadmium induced an excess of reactive oxygen species in the roots, and the growth of C. argentea is depressed greatly. Praxelis clematidea , E. adenophora , and S. canadensis were identified to have a higher tolerance to cadmium accumulation and could be used as potential species for phytoremediation after further investigation of the actual remediation results in the field.
研究领域:
环境科学
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植物学
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生态学
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土壤学
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DOI
高影响因子
Phytochemistry Letters
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2025
·
IF 1.4
Yan-Peng Liang,Qian Gao,Hong Chen,Rui Ma,Xiao-Bo Zhao,Xiao-Jie Jin,Jian Zhang,Yan-Ping Shi,Wei Ha
Alzheimer’s disease, a progressive neurodegenerative disorder of the central nervous system, presents a complex pathological mechanism that limits the efficacy of conventional single-target drugs. Utilizing the unique advantages of natural products in multi-target intervention, this study employed the active component 1- O -acetylbritannilactone (ABL) from Inula britannica L. as the parent structure. Guided by the multi-target directed ligands (MTDLs) strategy, four novel derivatives (ABL-1 to ABL-4) were successfully designed and synthesized by introducing acetylcholinesterase (AChE) inhibitory pharmacophores into the ABL scaffold. In vitro pharmacological evaluation demonstrated that ABL-2, ABL-3, and ABL-4 not only preserved the anti-neuroinflammatory activity of the parent compound but also endowed compound ABL with AChE inhibitory potency. Notably, ABL-4 displayed the most promising dual efficacy profile, achieving an AChE inhibition rate of 40.09 ± 0.73 % at 30 μM and an anti-neuroinflammatory activity (EC 50 = 8.43 ± 0.5 μM). Molecular docking simulations revealed that the dual-target synergistic mechanism of ABL derivatives arises from hydrogen bonding and π-π stacking interactions with key residues of both AChE and inducible nitric oxide synthase (iNOS). This work not only validates the feasibility of the MTDLs strategy in optimizing natural product scaffolds but also provides a structurally novel lead compound with significant potential for developing multi-target anti-AD therapeutics.
研究领域:
药理学
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神经科学
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药物化学
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DOI
高影响因子
Journal of Analytical Methods in Chemistry
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2021
·
IF 2.193
Guanjun Nan,Lina Zhang,Zhengzheng Liu,Yu Liu,Yan Du,Hongwen Zhao,Hongxia Zheng,Rong Lin,Guangde Yang,Shaohua Zheng
Eupatorium fortunei Turcz. is a widely used Chinese herbal medicine in China. In this study, a gas chromatography-triple quadrupole mass spectrometry (GC-MS/MS) method was developed and validated to simultaneously determine the contents of p-cymene, thymol, neryl acetate, and β-caryophyllene in roots, stems, and leaves of Eupatorium fortunei Turcz. harvested at different growth periods. All four constituents could be detected in leaves, three could be detected in stems except β-caryophyllene, and only thymol could be detected in roots. The order of the total contents of four constituents in different parts was leaves > stems > roots. It indicated that the leaves could be the proper medicinal parts of Eupatorium fortunei Turcz. The content of four constituents in leaves varied a lot among different growth periods and showed an M-shaped change trend with the growth of Eupatorium fortunei Turcz. The four constituents accumulated to the highest values in early July followed by mid-September. Accordingly, the best harvest time of Eupatorium fortunei Turcz. is early July and mid-September.
研究领域:
药用植物学
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分析化学
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植物科学
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DOI
PubMed
高影响因子
ACS Applied Materials & Interfaces
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2017
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IF 7.504
Qing-Shan Liu,Ran Deng,Qing-Fang Yan,Lin Cheng,Yongming Luo,Keqin Li,Xiaoying Yin,Xiaoyan Qin
In order to efficiently screen and isolate β-tubulin inhibitors, β-tubulin was immobilized on core–shell PMMA/CS (poly(methyl methacrylate)/Chitosan) nanoparticles to produce a new type of immobilized affinity material named β-tubulin-immobilized nanoparticles (β-TIN). The selectivity and adsorption performance of β-TIN were characterized using various control drugs. The β-TIN, the paclitaxel molecularly imprinted ploymers (MIP), and the C18 adsorbing material were compared for selectivity and enrichment ratio. Microtubule-targeting antitumor compounds were screened and isolated from a typical Chinese medicine, Chloranthus multistachys, by β-TIN. Three active compounds (curcolnol, zedoarofuran, and codonolactone) in Chloranthus multistachys extract were captured successfully. Microscale thermophoresis demonstrated that these three compounds strongly bind to β-tubulin, and the dissociation constants (Kd) between the three active compounds and β-tubulin were 1820 ± 0.68 nM, 1640 ± 0.52 nM, and 284 ± 1.00 nM, respectively. Moreover, the binding affinity between codonolactone and β-tubulin was greater than that between paclitaxel and β-tubulin. The antitumor activities of the three compounds were confirmed by the microtubule inhibition model, and the results showed a similar antitumor mechanism as paclitaxel. Molecular dynamics simulations were performed to preliminarily investigate the potential binding sites and the structure–activity relationship between the three active molecules and β-tubulin. Our study is the first to report the use of this novel material which is highly efficient in capturing low-content β-tubulin inhibitors from a complex mixture. The three screened compounds exhibited potential antineoplastic activity, and these lead compounds utilize a new mechanism of action with promising development prospects. Because β-TIN is easily prepared, displays excellent adsorption and selectivity for targets, and can effectively maintain the steric conformation and activities of target proteins, it will be very useful in the screening of lead compounds for different drug target proteins.
研究领域:
药学
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纳米技术
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生物技术
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癌症研究
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药物发现
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DOI
PubMed
高影响因子
FITOTERAPIA
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2023
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IF 3.4
Xionghua Sun,Mei Zhu,Wei Xia,Xihan Xu,Jian Zhang,Xiaogang Jiang
Eupatorium lindleyanum DC . has been used as a functional food in China for a long time. However, the antifibrotic activity of total sesquiterpenoids from Eupatorium lindleyanum DC . (TS-EL) is still unknown. In this study, we discovered that TS-EL reduced the increase in α-smooth muscle actin (α-SMA), type I collagen and fibronectin content, the formation of cell filaments and collagen gel contraction in transforming growth factor-β1-stimulated human lung fibroblasts. Intriguingly, TS-EL did not change the phosphorylation of Smad2/3 and Erk1/2. TS-EL decreased the levels of serum response factor (SRF), a critical transcription factor of α-SMA, and SRF knockdown alleviated the transition of lung myofibroblasts. Furthermore, TS-EL significantly attenuated bleomycin (BLM)-induced lung pathology and collagen deposition and reduced the levels of two profibrotic markers, total lung hydroxyproline and α-SMA. TS-EL also decreased the levels of SRF protein expression in BLM-induced mice. These results suggested that TS-EL attenuates pulmonary fibrosis by inhibiting myofibroblast transition via the downregulation of SRF.
研究领域:
药理学
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肺科学
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分子生物学
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产品关联
DOI
PubMed
高影响因子