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JOURNAL OF AGRICULTURAL AND FOOD CHEMISTRY · 2018 · IF 3.412

Preparation and Characterization of Butachlor/(2-Hydroxypropyl)-β-cyclodextrin Inclusion Complex: Improve Soil Mobility and Herbicidal Activity and Decrease Fish Toxicity

Qianqian Geng,Jingchan Xie,Xin Wang,Mengling Cai,Hui Ma,Hanwen Ni

A water-soluble inclusion complex for butachlor was prepared by complexation with (2-hydroxypropyl)-β-cyclodextrin (HP-β-CD). Phase solubility results indicated a 1:1 stoichiometric ratio with an apparent stability constant of 864.3 M–1 in the obtained solid complex. The formation of the complex was confirmed by 1H nuclear magnetic resonance, Fourier transform infrared, and differential scanning calorimetry spectra. Coupled with the molecular docking results, butachlor was considered to be completely included in HP-β-CD cavity. Butachlor complexation with HP-β-CD decreased its adsorption capacity and enhanced its mobility in soil. The inclusion complex displayed better herbicidal activities than free butachlor. The 96 h median lethal concentration values of the inclusion complex and free butachlor was 2.30 and 0.65 mg L–1, respectively, for zebrafish, indicating that the complexation could significantly reduce toxicity to fishes. The present study provides an approach to develop environment-friendly formulations using CDs for herbicides.

研究领域: 环境科学 · 农业科学
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Inorganics · 2022 ·Vol. 10 ·期 11 ·202 · IF 3.149

A 2D Porous Zinc-Organic Framework Platform for Loading of 5-Fluorouracil

Liang Qin,Fenglan Liang,Yan Li,Jiana Wu,Shiyuan Guan,Meiyin Wu,Shiling Xie,Manshi Luo,Deyun Ma

A hydrostable 2D Zn-based MOF, {[Zn(5-PIA)(imbm)]·2H2O}n(1) (5-H2PIA = 5-propoxy-isophthalic acid, imbm = 1,4-di(1H-imidazol-1-yl)benzene), was synthesized and structurally characterized. Complex1shows good water and thermal stability based on the TGA and PXRD analyses and displays a 2D framework with 1D channels of 4.8 × 13.8 and 10.0 × 8.3 Å2along theaaxis. The 5-fluorouracil (5-FU) payload in activated complex1(complex1a) is 19.3 wt%, and the cumulative release value of 5-FU at 120 h was about 70.04% in PBS (pH 7.4) at 310 K. In vitro MTT assays did not reveal any cytotoxic effect of NIH-3T3 and HEK-293 cells when the concentration of1was below 500 μg/mL and 5 μg/mL, respectively. No morphological abnormalities were observed on zebrafish exposed to complex1.Keywords:zinc-organic framework;drug delivery;5-fluorouracil;MTT assays;zebrafish toxicity

研究领域: 材料科学与工程 · 医学 · 药理学
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INORGANICA CHIMICA ACTA · 2018 · IF 2.264

A water-stable and biofriendly 2D anionic zinc(II) metal–organic framework for drug delivery

Yang Zhang,Jian Wang

A water-stable 2D Zn-based MOF with chemical formulae [(Me 2 NH 2 ) 4 Zn 2 (FDC) 4 ] n ( 1 ) (FDC = 2,5-furandicarboxylate) was synthesized and structurally characterized. TGA and PXRD results show high thermal and water stability for 1 . 1 exhibits a 2D (4,4) net with 1D channel of 7.2 × 7.2 Å 2 along the c axis. Desolvated 1 adsorbs around 11.4 wt% 5-Fluorouracil and the cumulative release value of 5-Fluorouracil at 48 h was about 96.5% and 99% in PBS (pH = 7.4 and pH = 6.0) at 37 °C, respectively. The in vivo Zebrafish toxicity tests and in vitro MTT assays of 1 at different concentrations results reveal that 1 is nontoxic.

研究领域: 材料科学 · 药学 · 生物医学工程
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MOLECULES · 2019 ·Vol. 24 ·期 20 ·3806 · IF 3.06

Toxicity Reduction of Euphorbia kansui Stir-Fried with Vinegar Based on Conversion of 3-O-(2′E,4′Z-Decadi-enoyl)-20-O-acetylingenol

Qiao Zhang,Yi Zhang,Shi-Kang Zhou,Kan Wang,Min Zhang,Pei-Dong Chen,Wei-Feng Yao,Yu-Ping Tang,Jian-Hua Wu,Li Zhang

The dried roots ofEuphorbia kansuiS.L.Liou ex S.B.Ho have long been used to treat edema in China. However, the severe toxicity caused byEuphorbia kansui(EK) has seriously restricted its clinical application. Although EK was processed with vinegar to reduce its toxicity, the detailed mechanisms of attenuation in toxicity of EK stir-fried with vinegar (VEK) have not been well delineated. Diterpenoids are the main toxic ingredients of EK, and changes in these after processing may be the underlying mechanism of toxicity attenuation of VEK. 3-O-(2′E,4′Z-decadienoyl)-20-O-acetylingenol (3-O-EZ) is one of the diterpenoids derived from EK, and the content of 3-O-EZ was significantly reduced after processing. This study aims to explore the underlying mechanisms of toxicity reduction of VEK based on the change of 3-O-EZ after processing with vinegar. Based on the chemical structure of 3-O-EZ and the method of processing with vinegar, simulation experiments were carried out to confirm the presence of the product both in EK and VEK and to enrich the product. Then, the difference of peak area of 3-O-EZ and its hydrolysate in EK and VEK were detected by ultra-high-performance liquid chromatography (UPLC). Furthermore, the toxicity effect of 3-O-EZ and its hydrolysate, as well as the underlying mechanism, on zebrafish embryos were investigated. The findings showed that the diterpenoids (3-O-EZ) in EK can convert into less toxic ingenol in VEK after processing with vinegar; meanwhile, the content of ingenol in VEK was higher than that of EK. More interestingly, the ingenol exhibited less toxicity (acute toxicity, developmental toxicity and organic toxicity) than that of 3-O-EZ, and 3-O-EZ could increase malondialdehyde (MDA) content and reduce glutathione (GSH) content; cause embryo oxidative damage by inhibition of the succinate dehydrogenase (SDH) and superoxide dismutase (SOD) activity; and induce inflammation and apoptosis by elevation of IL-2 and IL-8 contents and activation of the caspase-3 and caspase-9 activity. Thus, this study contributes to our understanding of the mechanism of attenuation in toxicity of VEK, and provides the possibility of safe and rational use of EK in clinics.Keywords:Euphorbia kansui;diterpenoids;vinegar processing;zebrafish toxicity

CAS / MDL: 154071-48-4 1461-15-0
研究领域: 药理学 · 毒理学 · 中药学 · 化学 · 生物学
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