6363-00-4Relevant academic research and scientific papers
A kind of leptine-containing brain-targeted nano-preparation and preparation method thereof
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Paragraph 0044-0046; 0049, (2022/03/27)
The present invention discloses a brain-targeted nanopharmacene containing hookerine, which is a nuclear material with 60% - γ-PFGA as a core shell structure nanoparticle, a shell material with a core shell structure nanoparticles in PLA-SS-PEG-A2, a nano-formulation with a core shell structure prepared by E-TPGS as a nonionic surfactant, a nano-preparation with a core shell structure prepared by loading hook vine alkali or at the same time supporting hook vine alkali and Tariquidar. Brain targeting nanopharmaceuticals containing hookerine containing hook vine are small in size, structurally stable, have sustained release and controlled release effects, overcome the difficulty of low encapsulation rate of hook vine alkali, and improve the brain targeting of hook vine base.
A stage-specific cancer chemotherapy strategy through flexible combination of reduction-activated charge-conversional core-shell nanoparticles
Han, Lingfei,Wang, Yingming,Huang, Xiaoxian,Liu, Bowen,Hu, Lejian,Ma, Congyu,Liu, Jun,Xue, Jingwei,Qu, Wei,Liu, Fulei,Feng, Feng,Liu, Wenyuan
, p. 6532 - 6549 (2019/09/10)
Precision medicine has increased the demand for stage-specific cancer chemotherapy. Drugs with different properties are needed for different stages of tumor development, which is, inducing rapid destruction in the early stage and facilitating deep penetration in the advanced stage. Herein, we report a novel reduction-activated charge-conversional core-shell nanoparticle (CS NP) formula based on ring-closing metathesis of the thiamine disulfide system (TDS) to deliver the chemotherapeutic agent-gambogic acid (GA). Methods: The shell consisted of hyaluronic acid-all-trans retinoid acid with a disulfide bond as the linker (HA-SS-ATRA). The core was selected from poly (γ-glutamic acid) with different grafting rates of the functional group (Fx%) of TDS. GA/CF100%S NPs, with the strongest reduction-responsive drug release, and GA/CF60%S NPs with the strongest penetration have been finally screened. On this basis, a stage-specific administration strategy against a two-stage hepatocellular carcinoma was proposed. Results: The developed CS NPs have been confirmed as inducing reduction-activated charge conversion from about -25 to +30 mV with up to 95% drug release within 48 h. The administration strategy, GA/CF100%S NPs for the early-stage tumor, and sequential administration of GA/CF60%S NPs followed by GA/CF100%S NPs for the advanced-stage tumor, achieved excellent tumor inhibition rates of 93.86±2.94% and 90.76±6.43%, respectively. Conclusions: Our CS NPs provide a novel platform for charge conversion activated by reduction. The stage-specific administration strategy showed great promise for cancer therapy.
Thiocarbonyl Surrogate via Combination of Potassium Sulfide and Chloroform for Dithiocarbamate Construction
Tan, Wei,J?nsch, Niklas,?hlmann, Tina,Meyer-Almes, Franz-Josef,Jiang, Xuefeng
supporting information, p. 7484 - 7488 (2019/10/08)
An efficient and practical thiocarbonyl surrogate via combination of potassium sulfide and chloroform was established. A variety of dithiocarbamates were afforded along with four new chemical bond formations in a one-pot reaction in which the thiocarbonyl
Design, synthesis and biological evaluation of brain-targeted thiamine disulfide prodrugs of ampakine compound LCX001
Xiao, Dian,Meng, Fan-Hua,Dai, Wei,Yong, Zheng,Liu, Jin-Qiu,Zhou, Xin-Bo,Li, Song
, (2016/05/24)
: Ampakine compounds have been shown to reverse opiate-induced respiratory depression by activation of amino-3-hydroxy-5-methyl-4-isoxazolepropionic acid (AMPA) glutamate receptors. However, their pharmacological exploitations are hindered by low blood-brain barrier (BBB) permeability and limited brain distribution. Here, we explored whether thiamine disulfide prodrugs with the ability of "lock-in" can be used to solve these problems. A series of thiamine disulfide prodrugs 7a-7f of ampakine compound LCX001 was synthesized and evaluated. The trials in vitro showed that prodrugs 7e, 7d, 7f possessed a certain stability in plasma and quickly decomposed in brain homogenate by the disulfide reductase. In vivo, prodrug 7e decreased the peripheral distribution of LCX001 and significantly increased brain distribution of LCX001 after i.v. administration. This compound showed 2.23- and 3.29-fold greater increases in the AUC0-t and MRT0-t of LCX001 in brain, respectively, than did LCX001 itself. A preliminary pharmacodynamic study indicated that the required molar dose of prodrug 7e was only one eighth that of LCX001 required to achieve the same effect in mice. These findings provide an important reference to evaluate the clinical outlook of ampakine compounds.
Deep eutectic mixture catalysed the synthesis of disulfides using Bunte salts as thiol surrogates
Zhou, Yongsheng
, p. 332 - 335 (2015/08/18)
Bunte salts, easily prepared from odourless sodium thiosulfates and various alkyl and aryl halides, acted as thiol surrogates for preparation of disulfides in the presence of hydrogen peroxide and a Bronsted-acidic deep eutectic mixture. The reaction proceeded smoothly to give the corresponding disulfide products in moderate to good yields, leaving odourless sodium bisulfite and water as the by-products. Moreover, this catalytic system could be readily recovered and reused several times without significant loss in activity.
Quaternary bis-ammonium salt precursors and their uses as prodrugs having an antiparasitic activity
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Page/Page column 9, (2010/02/14)
The invention concerns drug precursors with antimalarial effect, characterised in that it consists in quaternary bis-ammonium salts of general formula (I) wherein A and A′, identical or different, are respectively either a group A1 and A′1 of formula (1)
Antimicrobial activity of organic thiosulfates (Bunte salts)
Stefanska,Starosciak,Orzeszko,Kazimierczuk
, p. 190 - 192 (2007/10/03)
A number of organic thiosulfates (Bunte salts) were prepared from appropriate primary bromides or iodides. In the case of substrates with long aliphatic chains, an addition of benzyltrimethylammonium chloride as phase transfer catalyst was very successful
