125414-41-7Relevant articles and documents
Fabrication of eco-friendly nanofibrous membranes functionalized with carboxymethyl-β-cyclodextrin for efficient removal of methylene blue with good recyclability
Liu, Yinli,Wu, Dequn,Wang, Xueli,Yu, Jianyong,Li, Faxue
, p. 37715 - 37723 (2018)
Considering the excellent thermo-mechanical properties, chemical stability and low cost of biodegradable aliphatic-aromatic copolyesters, they are an ideal matrix when functionalized for capturing pollutants in wastewater. In this work, biodegradable poly((butylene succinate-co-terephthalate)-co-serinol terephthalate) (PBSST) copolyesters with amino side group (-NH2) were first synthesized through copolymerization, followed by grafting carboxymethyl-β-cyclodextrin (CM-β-CD) into PBSST molecular chains via amidation reaction to prepare PBSST-g-β-CD. The corresponding nanofibrous membranes were then fabricated by electrospinning as adsorbents for efficiently removing cationic dye methyl blue (MB) from aqueous solutions. The adsorption performance of the nanofibrous membranes was fitted well with pseudo-second-order model and Langmuir isotherm model. The maximum adsorption capacity was 543.48 mg g?1 for MB along with a removal efficiency of 98% after five regeneration cycles, indicating the high adsorption capacity and good recyclability of nanofibrous membranes. The adsorbents possess features of high adsorption capacity, eco-friendliness and easy operation, and exhibit great potential for disposing of printing-dying wastewater.
High Drug Loading, Reversible Disulfide Core-Cross-Linked Multifunctional Micelles for Triggered Release of Camptothecin
Ling, Longbing,Ismail, Muhammad,Du, Yawei,Xia, Qing,He, Wei,Yao, Chen,Li, Xinsong
, p. 5479 - 5492 (2018)
Nanomedicines in polymeric therapeutics present a potential treatment for cancers. However, their clinical effectiveness still has room to be improved. Herein, reduction-responsive reversibly core-cross-linked micelles based on the poly(ethylene glycol)-dihydrolipoic acid (MeO-PEG2k-DHLA) conjugate were developed for triggered intracellular release of camptothecin (CPT). Coupling two molecules of dihydrolipoic acid (DHLA) to methyl-terminated PEG (Mw 2000) through a labile ester bond was performed by solution-phase condensation reaction. Due to the amphiphilic property, the MeO-PEG2k-DHLA conjugate formed micelles that were readily cross-linked with disulfide formation dispersed in water. These sole cross-linked micelles were 74.9 nm in hydrodiameter, as analyzed by dynamic light scattering (DLS). The nanostructures demonstrated excellent stability against extensive dilution, while rapidly dissociating under 10 mM glutathione (GSH), highlighting their potential for drug delivery. Interestingly, CPT was modified with a disulfide linkage and subsequently conjugated to the MeO-PEG2k-DHLA polymer scaffold. Core-cross-linking of the micelles achieved high drug loading of CPT (31.81%, wt %) and demonstrated that CPT release at pH 7.4 was significantly declined by cross-linking (i.e., less than 15% release in 24 h), whereas more than 90% of CPT was released under 10 mM GSH condition. In vitro cellular uptake and MTT assays showed that CPT-conjugated MeO-PEG2k-DHLA micelles were effectively internalized into tumor cells to induce the cytotoxic effects against HepG-2 and MCF-7 cells. Importantly, in vivo pharmacokinetics analysis demonstrated the nanoscale feature of micelles makes CPT to present longer retention time, resulting in a higher accumulation at tumor sites. Taken together, the disulfide core-cross-linked MeO-PEG2k-DHLA multifunctional micelles with high drug loading and excellent stability are potential candidates for tumor-targeting drug delivery.
Immucillins in custom catalytic-site cavities
Murkin, Andrew S.,Clinch, Keith,Mason, Jennifer M.,Tyler, Peter C.,Schramm, Vern L.
, p. 5900 - 5903 (2008)
Neighboring-group participation in the reaction catalyzed by purine nucleoside phosphorylase involves a compression mode between the 5′- and 4′-ribosyl oxygens, facilitated by His257. The His257Gly mutant opens a space in the catalytic site. Hydrophobic 5′-substituted Immucillins are transition-state analogue inhibitors of this mutant enzyme. Dissociation constants as low as 2 pM are achieved, with Km/Kd as high as 400,000,000.
Multimerization increases tumor enrichment of peptide–photosensitizer conjugates
Zhao, Jisi,Li, Shuang,Jin, Yingying,Wang, Jessica Yijia,Li, Wenjing,Wu, Wenjie,Hong, Zhangyong
, (2019)
Photodynamic therapy (PDT) is an established therapeutic modality for the management of cancers. Conjugation with tumor-specific small molecule ligands (e.g., short peptides or peptidomimetics) could increase the tumor targeting of PDT agents, which is ve
Design and Synthesis of Galactose-Biotin Lipid Materials for Liposomes to Promote the Hepatoma Cell–Targeting Effect
Ding, Ruihua,Li, Zhenjie,Wang, Jianyi,Zhu, Xueyan,Zhao, Zhuang,Wang, Mian
, p. 3074 - 3081 (2019)
A series of novel low-toxic hepatoma cell–targeting lipid materials were designed and synthesized, in which monogalactose, digalactose, and galactose-biotin were used as targeting moieties and hydrophilic heads while stearate was used as hydrophobic tail (Mono-Gal-ST, Di-Gal-ST, and Gal-Biotin-ST). The corresponding galactose-biotin-modified liposomes (Mono-Gal-LPs, Di-Gal-LPs, and Gal-Biotin-LPs) and conventional liposomes (LPs) were prepared. These galactose-biotin-modified liposomes can distinguish hepatoma cells from other tissue cells owing to the recognition of asialoglycoprotein receptor by galactose group. Moreover, the ability of liposomes to distinguish hepatoma cells from normal hepatocytes follows a trend of LPs Mono-Gal-LPs Di-Gal-LPs Gal-Biotin-LPs, which is attributed to the cluster glycoside effect and the synergistic effect of galactose and biotin. In addition, the endocytosis of these galactose-biotin-modified liposomes were competitively inhibited by galactose, further confirming these liposomes entered hepatoma cells via asialoglycoprotein receptor–mediated pathway.
Integration of a Diselenide Unit Generates Fluorogenic Camptothecin Prodrugs with Improved Cytotoxicity to Cancer Cells
Zhao, Jintao,Wang, Zihua,Zhong, Miao,Xu, Qianhe,Li, Xinming,Chang, Bingbing,Fang, Jianguo
, p. 17979 - 17991 (2021/12/13)
A diselenide/disulfide unit was introduced into camptothecin (CPT), and two selenoprodrugs (e.g., CPT–Se3 and CPT–Se4) were identified to show improved potency in killing cancer cells and inhibiting tumor growth in vivo. Interestingly, the intrinsic fluorescence of CPT was severely quenched by the diselenide bond. Both the selenoprodrugs were activated by glutathione with a nearly complete recovery of CPT’s fluorescence. The activation of prodrugs was accompanied by the production of selenol intermediates, which catalyzed the constant conversion of glutathione and oxygen to oxidized glutathione and superoxides. The diselenide unit is widely employed in constructing thiol-responsive materials. However, the selenol intermediates were largely ignored in the activation process prior to this study. Our work verified that integration of the diselenide unit may further enhance the parent drug’s efficacy. Also, the discovery of the fluorescence quenching property of the diselenide/disulfide bond further shed light on constructing novel theranostic agents.
ENGINEERED ANTIBODIES AS MOLECULAR DEGRADERS THROUGH CELLULAR RECEPTORS
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Page/Page column 3; 77, (2021/04/17)
The present disclosure provides, in one aspect, bifunctional compounds that can be used to promote or enhance degradation of certain circulating proteins. In certain embodiments, the circulating protein mediates a disease and/or disorder in a subject, and treatment or management of the disease and/or disorder requires degradation, removal, or reduction in concentration of the circulating protein in the subject. Thus, in certain embodiments, administration of a compound of the disclosure to the subject removes or reduces the circulation concentration of the circulating protein, thus treating, ameliorating, or preventing the disease and/or disorder.
