Publications by authors named "Jian-Cheng Wang"

104 Publications

[Physiological response of Xinjiang wild walnut germplasm to low temperature stress].

Ying Yong Sheng Tai Xue Bao 2020 Aug;31(8):2558-2566

College of Life Sciences, Shihezi University, Shihezi 832003, Xinjiang, China.

We examined the physiological response of 1-year-old branches of 37 Xinjiang wild walnut germplasm resources in Gongliu wild walnut forest under cold temperatures (-20 ℃ and 4 ℃) for 12 hours, compared the responses with that of . The relative conductivity (REC), free proline (PRO), soluble sugar (SS), malondialdehyde (MDA) content and peroxidase (POD) activity were measured in an artificial climate chamber by simulating spring low temperature. Subordinate function and principal component analysis were used to evaluate the physiological response of walnut germplasm to low temperature. The results showed that the REC, PRO, SS, MDA content and POD activity of Xinjiang wild walnut were increased. By evaluating the relationship between low temperature resistance and habitat, we found that cold tolerance level was middle valley > east valley > west valley > general valley. Xinjiang wild walnut showed stronger cold tolerance than . Seven germplasm with cold resistance were selected from the total 37 wild walnut germplasm in Xinjiang, which provided a reference for improving walnut varieties and their responses to sudden weather change in late spring and other growing stages.
View Article and Find Full Text PDF

Download full-text PDF

Source
http://dx.doi.org/10.13287/j.1001-9332.202008.002DOI Listing
August 2020

Engineering a "three-in-one" hirudin prodrug to reduce bleeding risk: A proof-of-concept study.

J Control Release 2021 Sep 1;338:462-471. Epub 2021 Sep 1.

Beijing Key Laboratory of Molecular Pharmaceutics and New Drug Delivery Systems, State Key Laboratory of Natural and Biomimetic Drugs, School of Pharmaceutical Sciences, Peking University, Beijing, China; Laboratory of innovative formulations and pharmaceutical excipients, Ningbo Institute of Marine Medicine, Peking University, Beijing, China. Electronic address:

An ideal anticoagulant should have at least three properties including targeted delivery to the thrombosis site, local activation or releasing to centralize the anti-thrombosis effects and thus reduce the bleeding risks, and long persistence in circulation to avoid repeated administration. In the present study, we sought to test a "three-in-one" strategy to design new protein anticoagulants. Based on these criteria, we constructed two hirudin prodrugs, R824-HV-ABD and ABD-HV-R824. The R824 peptide can bind phosphatidylserine on the surface of the procoagulant platelets and thus guide the prodrug to the thrombosis sites; albumin-binding domain (ABDs) can bind the prodrug to albumin, and thereby increase its persistence in circulation; the hirudin (HV) core in the prodrug is flanked by factor Xa recognition sites, thus factor Xa at the thrombosis site can cleave the fusion proteins and release the activated hirudin locally. Hirudin prodrugs were able to bind with procoagulant platelets and human serum albumin in vitro with high affinity, targeted concentrated and prevented the formation of occlusive thrombi in rat carotid artery injury model. Their effective time was significantly extended compared to native hirudin, and R824-HV-ABD showed a significantly improved half-life of about 24 h in rats. The bleeding time of prodrug-treated mice was much shorter than that of hirudin-treated mice. The results from the proof-of-concept studies, for the first time, demonstrate that "three-in-one" prodrug strategy may be a good solution for protein or peptide anticoagulants to reduce their bleeding risks.
View Article and Find Full Text PDF

Download full-text PDF

Source
http://dx.doi.org/10.1016/j.jconrel.2021.08.058DOI Listing
September 2021

SIMPLE is an endosomal regulator that protects against non-alcoholic fatty liver disease by targeting the lysosomal degradation of EGFR.

Hepatology 2021 Jul 28. Epub 2021 Jul 28.

Department of Cardiology, State Key Laboratory of Cardiovascular Disease, Fuwai Hospital, National Center for Cardiovascular Diseases, Chinese Academy of Medical Sciences and Peking Union Medical College, Beijing, China.

Background & Aims: Nonalcoholic fatty liver disease (NAFLD) has become a tremendous burden for public health, however, there is no drug for NAFLD therapy at present. Impaired endo-lysosome-mediated protein degradation is observed in a variety of metabolic disorders, such as atherosclerosis, type 2 diabetes mellitus and NAFLD. Small integral membrane protein of lysosome/late endosome (SIMPLE) is a regulator of endosome-to-lysosome trafficking and cell signaling. But the role that SIMPLE plays in NAFLD progression remains unknown. Here we investigated SIMPLE function in NAFLD development and sophisticated mechanism therein.

Approach & Results: This study found in vitro knockdown of SIMPLE significantly aggravated lipid accumulation, inflammation in hepatocytes treated with metabolic stimulation. Consistently, in vivo experiments showed that liver-specific Simple-knockout (Simple-HKO) mice exhibited more severe high-fat diet (HFD)-, high-fat-high-cholesterol diet (HFHC)-, and methionine-choline-deficient diet (MCD)- induced steatosis, glucose intolerance, inflammation, and fibrosis than those fed with normal-chow diet. Meanwhile, RNA-sequencing demonstrated the up-regulated signaling pathways and signature genes involved in lipid metabolism, inflammation and fibrosis in Simple-HKO mice compared to control mice under metabolic stress. Mechanically, we found SIMPLE directly interact with epidermal growth factor receptor (EGFR). SIMPLE deficiency results in dysregulated degradation of EGFR, subsequently hyperactivated EGFR phosphorylation, exaggerating NAFLD development. Moreover, we further demonstrated that using EGFR inhibitor or silencing EGFR expression could ameliorate lipid accumulation induced by the knockdown of SIMPLE.

Conclusions: SIMPLE ameliorated NASH by prompting EGFR degradation and can also be a potential therapeutic candidate for NASH.
View Article and Find Full Text PDF

Download full-text PDF

Source
http://dx.doi.org/10.1002/hep.32075DOI Listing
July 2021

Retrotransverse Foramen and Retrotransverse Groove Anatomic Variations of the Atlas Vertebra in the Chinese Population.

World Neurosurg 2021 Aug 27;152:e193-e200. Epub 2021 May 27.

Department of Neurosurgery, the First Affiliated Hospital of Soochow University, Suzhou, China. Electronic address:

Objective: To analyze the prevalence of retrotransverse foramen (RTF) or retrotransverse groove (RTG) anatomic variations in Chinese atlas vertebra (C1).

Methods: Three-dimensional volume-rendered computed tomography angiography images of 427 subjects (264 males, 163 females; 17-87 years old) were reviewed and evaluated using dedicated software. The prevalence of RTF and RTG anatomic variation of C1 was analyzed.

Results: RTF anatomic variants were present in 50 (11.7%) atlases. Bilateral RTF, unilateral left RTF, and unilateral right RTF were present in 16 (3.8%), 20 (4.9%), and 14 (3.3%) vertebrae. Comparison between males and females revealed differences in bilateral RTF (P = 0.010) and unilateral left RTF (P = 0.008). RTG anatomic variants were present in 113 (26.5%) atlases. Bilateral RTG, unilateral left RTG, and unilateral right RTG were present in 39 (9.1%), 30 (7.0%), and 44 (10.3%) vertebrae. Comparison between males and females revealed differences in RTG (P = 0.000), bilateral RTG (P = 0.006), and unilateral left RTG (P = 0.034). RTF was detected in 36 cases on the left and 30 cases on the right. RTG was detected in 69 cases on the left and 79 cases on the right. There were no side differences in the prevalence of RTF and RTG.

Conclusions: The incidence of RTG is higher than the incidence of RTF. Incidence of bilateral RTF, bilateral RTG, unilateral left RTF, unilateral left RTG, and RTG differed between males and females. Preoperative understanding of these variations using three-dimensional computed tomography angiography is helpful for safe execution of upper cervical posterior approach surgery.
View Article and Find Full Text PDF

Download full-text PDF

Source
http://dx.doi.org/10.1016/j.wneu.2021.05.065DOI Listing
August 2021

Study on the Hg removal characteristics and synergistic mechanism of iron-based modified biochar doped with multiple metals.

Bioresour Technol 2021 Jul 2;332:125086. Epub 2021 Apr 2.

College of Electrical and Power Engineering, Taiyuan University of Technology, Taiyuan 030024, PR China. Electronic address:

An iron-based composite adsorbent with biochar as the support was prepared by coprecipitation and the sol-gel method. Both single-iron-based modified biochar without doping with other metals and iron-based modified biochar doped with multiple metals (Ce, Cu, Co, Mn) were synthesised. The adsorption kinetics were analysed, and temperature-programmed desorption measurements were performed to reveal the inherent difference in mechanism between the oxidation and adsorption of Hg by the modified biochar and to elucidate the key mechanism of Hg removal. The results show that the removal of Hg by the modified biochar mainly includes adsorption and oxidation processes. The adsorption process is divided into two stages, external and internal mass transfer, both of which occur via multilayer adsorption. HgO and Hg-OM are the main forms of Hg present on the modified biochar surface. Doped metal oxides can play a synergistic role in enhancing the mercury removal performance of the modified biochar.
View Article and Find Full Text PDF

Download full-text PDF

Source
http://dx.doi.org/10.1016/j.biortech.2021.125086DOI Listing
July 2021

Tumor Necrosis Factor α-Induced Protein 8-Like 2 Alleviates Nonalcoholic Fatty Liver Disease Through Suppressing Transforming Growth Factor Beta-Activated Kinase 1 Activation.

Hepatology 2021 Sep 26;74(3):1300-1318. Epub 2021 Jul 26.

Department of Cardiology, State Key Laboratory of Cardiovascular Disease, Fuwai Hospital, National Center for Cardiovascular Diseases, Chinese Academy of Medical Sciences and Peking Union Medical College, Beijing, China.

Background And Aims: NAFLD prevalence has increased rapidly and become a major global health problem. Tumor necrosis factor α-induced protein 8-like 2 (TIPE2) plays a protective role in a cluster of liver diseases, such as autoimmune hepatitis, hepatitis B, and hepatocellular carcinoma. However, the function of TIPE2 in NAFLD remains unknown. Here, we investigated the role of TIPE2 in the development of NAFLD.

Approach And Results: Our study found that in vitro overexpression or knockout of TIPE2 significantly ameliorated or aggravated lipid accumulation and inflammation in hepatocytes exposed to metabolic stimulation, respectively. Consistently, in vivo hepatic steatosis, insulin resistance, inflammation, and fibrosis were alleviated in hepatic Tipe2-transgenic mice but exaggerated in hepatic Tipe2-knockout mice treated by metabolic challenges. RNA sequencing revealed that TIPE2 was significantly associated with the mitogen-activated protein kinase pathway. Mechanistic experiments demonstrated that TIPE2 bound with transforming growth factor beta-activated kinase 1 (TAK1), prevented tumor necrosis factor receptor-associated factor 6-mediated TAK1 ubiquitination and subsequently inhibited the TAK1 phosphorylation and activation of TAK1-c-Jun N-terminal kinase (JNK)/p38 signaling. Further investigation showed that blocking the activity of TAK1 reversed the worsening of hepatic metabolic disorders and inflammation in hepatic-specific Tipe2-knockout hepatocytes and mice treated with metabolic stimulation.

Conclusions: TIPE2 suppresses NAFLD advancement by blocking TAK1-JNK/p38 pathway and is a promising target molecule for NAFLD therapy.
View Article and Find Full Text PDF

Download full-text PDF

Source
http://dx.doi.org/10.1002/hep.31832DOI Listing
September 2021

Annexin A1 alleviates kidney injury by promoting the resolution of inflammation in diabetic nephropathy.

Kidney Int 2021 07 3;100(1):107-121. Epub 2021 Mar 3.

The Institute of Cardiovascular Sciences, Institute of Systems Biomedicine, School of Basic Medical Sciences, Beijing, China; Key Laboratory of Molecular Cardiovascular Science, Ministry of Education, Beijing, China; Key Laboratory of Cardiovascular Molecular Biology and Regulatory Peptides, Ministry of Health, Beijing, China; Beijing Key Laboratory of Cardiovascular Receptors Research, Beijing, China; Department of Physiology and Pathophysiology, Peking University Health Science Center, Beijing, China; China National Clinical Research Center for Neurological Diseases, Tiantan Hospital, Advanced Innovation Center for Human Brain Protection, The Capital Medical University, Beijing, China. Electronic address:

Since failed resolution of inflammation is a major contributor to the progression of diabetic nephropathy, identifying endogenously generated molecules that promote the physiological resolution of inflammation may be a promising therapeutic approach for this disease. Annexin A1 (ANXA1), as an endogenous mediator, plays an important role in resolving inflammation. Whether ANXA1 could affect established diabetic nephropathy through modulating inflammatory states remains largely unknown. In the current study, we found that in patients with diabetic nephropathy, the levels of ANXA1 were upregulated in kidneys, and correlated with kidney function as well as kidney outcomes. Therefore, the role of endogenous ANXA1 in mouse models of diabetic nephropathy was further evaluated. ANXA1 deficiency exacerbated kidney injuries, exhibiting more severe albuminuria, mesangial matrix expansion, tubulointerstitial lesions, kidney inflammation and fibrosis in high fat diet/streptozotocin-induced-diabetic mice. Consistently, ANXA1 overexpression ameliorated kidney injuries in mice with diabetic nephropathy. Additionally, we found Ac2-26 (an ANXA1 mimetic peptide) had therapeutic potential for alleviating kidney injuries in db/db mice and diabetic Anxa1 knockout mice. Mechanistic studies demonstrated that intracellular ANXA1 bound to the transcription factor NF-κB p65 subunit, inhibiting its activation thereby modulating the inflammatory state. Thus, our data indicate that ANXA1 may be a promising therapeutic approach to treating and reversing diabetic nephropathy.
View Article and Find Full Text PDF

Download full-text PDF

Source
http://dx.doi.org/10.1016/j.kint.2021.02.025DOI Listing
July 2021

Gram-Scale Synthesis of Cu(II)@COF via Solid-State Coordination Approach for Catalysis of Alkyne-Dihalomethane-Amine Coupling.

Inorg Chem 2021 Mar 17;60(5):3393-3400. Epub 2021 Feb 17.

College of Chemistry, Chemical Engineering and Materials Science, Collaborative Innovation Centre of Functionalized Probes for Chemical Imaging in Universities of Shandong, Key Laboratory of Molecular and Nano Probes, Ministry of Education, Shandong Normal University, Jinan 250014, People's Republic of China.

A novel covalent organic framework material , which contains chelating coordination environments, was synthesized at the gram level under mild conditions. In addition, its Cu(II)-loaded complex of was prepared by impregnating in an acetonitrile solution of CuCl via a solid-state coordination approach. The obtained Cu(II)-loaded can be used as a highly active heterogeneous catalyst to catalyze the alkyne-dihalomethane-amine coupling reactions.
View Article and Find Full Text PDF

Download full-text PDF

Source
http://dx.doi.org/10.1021/acs.inorgchem.0c03783DOI Listing
March 2021

Syntheses and structures of three macrocyclic supramolecular complexes and one Zn-containing coordination polymer generated from a semi-rigid multidentate N-containing ligand.

Acta Crystallogr C Struct Chem 2021 Jan 1;77(Pt 1):29-39. Epub 2021 Jan 1.

College of Chemistry, Chemical Engineering and Materials Science, Collaborative Innovation Center of Functionalized Probes for Chemical Imaging in Universities of Shandong, Key Laboratory of Molecular and Nano Probes, Ministry of Education, Shandong Provincial Key Laboratory of Clean Production of Fine Chemicals, Shandong Normal University, Jinan, Shandong 250014, People's Republic of China.

Semirigid organic ligands can adopt different conformations to construct coordination polymers with more diverse structures when compared to those constructed from rigid ligands. A new asymmetric semirigid organic ligand, 4-{2-[(pyridin-3-yl)methyl]-2H-tetrazol-5-yl}pyridine (L), has been prepared and used to synthesize three bimetallic macrocyclic complexes and one coordination polymer, namely, bis(μ-4-{2-[(pyridin-3-yl)methyl]-2H-tetrazol-5-yl}pyridine)bis[dichloridozinc(II)] dichloromethane disolvate, [ZnCl(CHN)]·2CHCl, (I), the analogous chloroform monosolvate, [ZnCl(CHN)]·CHCl, (II), bis(μ-4-{2-[(pyridin-3-yl)methyl]-2H-tetrazol-5-yl}pyridine)bis[diiodidozinc(II)] dichloromethane disolvate, [ZnI(CHN)]·2CHCl, (III), and catena-poly[[[diiodidozinc(II)]-μ-4-{2-[(pyridin-3-yl)methyl]-2H-tetrazol-5-yl}pyridine] chloroform monosolvate], {[ZnI(CHN)]·CHCl}, (IV), by solution reaction with ZnX (X = Cl and I) in a CHCl/CHOH or CHCl/CHOH mixed solvent system at room temperature. Complex (I) is isomorphic with complex (III) and has a bimetallic ring possessing similar coordination environments for both of the Zn cations. Although complex (II) also contains a bimetallic ring, the two Zn cations have different coordination environments. Under the influence of the I anion and guest CHCl molecule, complex (IV) displays a significantly different structure with respect to complexes (I)-(III). C-H...Cl and C-H...N hydrogen bonds, and π-π stacking or C-Cl...π interactions exist in complexes (I)-(IV), and these weak interactions play an important role in the three-dimensional structures of (I)-(IV) in the solid state. In addition, the fluorescence properties of L and complexes (I)-(IV) were investigated.
View Article and Find Full Text PDF

Download full-text PDF

Source
http://dx.doi.org/10.1107/S2053229620016083DOI Listing
January 2021

Catalytic Asymmetric Synthesis of Chiral Covalent Organic Frameworks from Prochiral Monomers for Heterogeneous Asymmetric Catalysis.

J Am Chem Soc 2020 10 22;142(40):16915-16920. Epub 2020 Sep 22.

College of Chemistry, Chemical Engineering and Materials Science, Collaborative Innovation Center of Functionalized Probes for Chemical Imaging in Universities of Shandong, Key Laboratory of Molecular and Nano Probes, Ministry of Education, Shandong Normal University, Jinan 250014, P. R. China.

Direct synthesis, postsynthetic modification, and chiral induction have been recognized as three powerful methods to synthesize chiral covalent organic frameworks (CCOFs). However, catalytic asymmetric methodology, as the most important and effective synthetic approach to access chiral organics, has not been enabled for CCOFs synthesis thus far. Herein we report, for the first time, the construction of CCOFs from prochiral monomers via catalytic asymmetric polymerization. The obtained propargylamine-linked CCOFs can be the highly reusable chiral catalysts to promote asymmetric Michael addition reactions. The concept of catalytic asymmetric polymerization might open a new route for constructing the CCOFs that are not possible with the existing CCOF synthetic methods.
View Article and Find Full Text PDF

Download full-text PDF

Source
http://dx.doi.org/10.1021/jacs.0c07461DOI Listing
October 2020

Improving long circulation and procoagulant platelet targeting by engineering of hirudin prodrug.

Int J Pharm 2020 Nov 10;589:119869. Epub 2020 Sep 10.

Beijing Key Laboratory of Molecular Pharmaceutics and New Drug Delivery Systems, State Key Laboratory of Natural and Biomimetic Drugs, School of Pharmaceutical Sciences, Peking University, Beijing, China. Electronic address:

To reduce systemic bleeding risks during anticoagulant treatment, a new concept named "precise anticoagulation" was proposed to localize the effects of anticoagulants via the targeted delivery of prodrugs to the coagulation site. In this study, the fusion protein Annexin V-hirudin 3-ABD (hAvHA) was constructed to achieve the prolonged circulation and targeted delivery of hirudin to coagulation sites. hAvHA was inactive as a prodrug, and it could bind to albumin during circulation. The drug was quickly activated via factor Xa-mediated cleavage once coagulation occurred, and hirudin was efficiently released to exert antithrombin activity in vitro. The hAvHA protein could be activated in mouse blood and exert significant anticoagulation effects. The results of FITC labeling illustrated that hAvHA bound to procoagulant platelets, suggesting the Annexin V modification permits targeted delivery to sites of thrombosis. hAvHA bound to albumin in vitro with an equilibrium dissociation constant of 8 pM, suggesting the ABD modification permitted prolonged circulation in vivo. Moreover, the bleeding time was much shorter in hAvHA-treated mice than in hirudin-treated mice. Therefore, our results suggested that that hAvHA is a potential and promising anticoagulant in vivo.
View Article and Find Full Text PDF

Download full-text PDF

Source
http://dx.doi.org/10.1016/j.ijpharm.2020.119869DOI Listing
November 2020

Biological activities of siRNA-loaded lanthanum phosphate nanoparticles on colorectal cancer.

J Control Release 2020 12 27;328:45-58. Epub 2020 Aug 27.

Beijing Key Laboratory of Molecular Pharmaceutics and New Drug Delivery Systems, State Key Laboratory of Natural and Biomimetic Drugs, School of Pharmaceutical Sciences, Peking University, XueYuan Rd 38, Haidian District, Beijing 100191, China.

Lanthanum can reduce absorption of phosphate by forming lanthanum phosphate complexes after oral administration of lanthanum carbonate tablets (FOSRENOL®) in patients. Based on the pH-responsive interaction of phosphate and lanthanum ions, the chitosan coated siRNA-loaded lanthanum phosphate nanoparticles (CS/LaP/siRNA NPs) were prepared for improving cancer treatment, in which polysaccharide chitosan was used as the outer shell to control the excessive growth of lanthanum phosphate complexes, and enable intestinal mucoadhesion. The CS/LaP/siEGFR NPs exhibited significant biological activities in human colorectal cancer HT-29 cells by the synergistic effects of siEGFRs and lanthanum ions, such as downregulation of EGFR and upregulation of miR-34a. Furthermore, significant tumor growth inhibition was observed in both transgenic C57BL/6-Apc/Nju cancer mouse model and AOM/DSS chemically induced orthotopic colorectal cancer mouse model after intestinal instillation administration of CS/LaP/siEGFR NPs. Therefore, the lanthanum-based siRNA delivery system would provide a potential and efficient strategy for the treatment of colorectal cancers.
View Article and Find Full Text PDF

Download full-text PDF

Source
http://dx.doi.org/10.1016/j.jconrel.2020.08.027DOI Listing
December 2020

Polyarginine-Mediated siRNA Delivery: A Mechanistic Study of Intracellular Trafficking of PCL-R15/siRNA Nanoplexes.

Mol Pharm 2020 05 30;17(5):1685-1696. Epub 2020 Mar 30.

Beijing Key Laboratory of Molecular Pharmaceutics and New Drug Delivery Systems, State Key Laboratory of Natural and Biomimetic Drugs, School of Pharmaceutical Sciences, Peking University, XueYuan Rd 38, Haidian Dist, Beijing 100191, P. R. China.

As a cell-penetrating peptide, polyarginine is widely used in drug delivery systems based on its membrane permeation ability. Previously, we developed the mPEG-PLA--polyarginine(R15) triblock copolymer, which exhibited a high siRNA delivery efficiency both and . As a continued effort, here the amphiphilic diblock polymer PCL-R15 was synthesized as a simplified model to further elucidate the structure-activity relationship of arginine-based amphiphilic polymers as siRNA delivery systems, and the cellular trafficking mechanisms of the PCL-R15/siRNA nanoplexes were investigated to understand the interaction patterns between the nanoplexes and cells. Compared to the R15/siRNA complexes, the introduction of PCL moiety was found to result in the stronger interactions with cells and the enhanced transfection efficiency after the formation of condensed nanoplexes. Caveolae-mediated endocytosis and clathrin-mediated endocytosis were major routes for the internalization of PCL-R15/siRNA nanoplexes. The intracellular release of siRNA from nanoplexes was confirmed by fluorescence resonance energy transfer assay. It was also noticed that the internalized PCL-R15/siRNA nanoplexes were transported through digestive routes and trapped in lysosomes, which may be the bottleneck for efficient siRNA delivery of PCL-R15/siRNA nanoplexes. This study investigated the relationship between the polymer structure of PCL-R15 and the cellular interaction patterns, which may render implications on the rational design of polyarginine-based siRNA delivery systems.
View Article and Find Full Text PDF

Download full-text PDF

Source
http://dx.doi.org/10.1021/acs.molpharmaceut.0c00120DOI Listing
May 2020

Microfluidic-Based Holonomic Constraints of siRNA in the Kernel of Lipid/Polymer Hybrid Nanoassemblies for Improving Stable and Safe In Vivo Delivery.

ACS Appl Mater Interfaces 2020 Apr 20;12(13):14839-14854. Epub 2020 Mar 20.

Beijing Key Laboratory of Molecular Pharmaceutics and New Drug Delivery Systems, State Key Laboratory of Natural and Biomimetic Drugs, School of Pharmaceutical Sciences, Peking University, 38 Xueyuan Road, Beijing 100191, China.

A safe and efficient delivery system is critical for clinical application of siRNA. However, the conventional electrostatic interaction-based siRNA nanoplexes with bulk mixing preparation were always unsatisfactory for its stability and safety. In this study, the new core-shell lipid/PCL-PEI/siRNA nanoparticles (LPS NPs) endowing holonomic constraint of siRNA in the inner core were prepared by microfluidic technology. On the microfluidic chip, siRNAs were completely compressed into the inner hydrophilic core of reverse PCL-PEI micelles at a low N/P ratio of 5, followed by coating a neutral lipid membrane to form core-shell nanoparticles, which had a uniform size (120.2 ± 1.4 nm) and a negative charge (-8.8 ± 1.6 mV). Compared to bulk mixing-based LMS NPs, the lower usage of cationic PCL-PEI materials and stronger protection of siRNA in serum were found in the microfluidic-based LPS NPs. Furthermore, it was demonstrated that the LPS NPs exhibited significant downregulation of EGFR mRNA and protein expression level both in vitro and in vivo, and showed significant inhibition of tumor growth following systemic administration along with no obvious systemic toxicity. These findings demonstrated that the microfluidic-based lipid/polymer hybrid nanoassemblies would offer a promising siRNA delivery system for clinical application.
View Article and Find Full Text PDF

Download full-text PDF

Source
http://dx.doi.org/10.1021/acsami.9b22781DOI Listing
April 2020

Encapsulated microRNA by gemcitabine prodrug for cancer treatment.

J Control Release 2019 12 13;316:317-330. Epub 2019 Nov 13.

Beijing Key Laboratory of Molecular Pharmaceutics and New Drug Delivery Systems, State Key Laboratory of Natural and Biomimetic Drugs, School of Pharmaceutical Sciences, Peking University, XueYuan Rd 38, Haidian Dist, Beijing 100191, China.

Although microRNAs (miRNAs) function as the important tumor gene regulators, they still confront with many challenges in systemic delivery. Here, the amphiphilic gemcitabine-oleic acid prodrugs (GOA) binding miRNAs with hydrogen bond are assembled into nanoparticles (GOA/miR NPs) through hydrophobic interaction via denaturation-annealing processes and nano-precipitation technique. The non-cationic GOA/miR NPs with an average size of ~150 nm and a zeta potential of ~ - 15 mV exhibit a stable encapsulation of miRNAs with non-sequence selectivity. Either miR-122 or miR-34a encapsulated in the GOA/miR NPs is efficiently delivered into HepG2 cells and significantly downregulate the expression levels of target gene after lysosome escape and pH-responsive disassembly. Moreover, in vivo experiments demonstrate that the GOA/miR-122 NPs exhibit higher tumor accumulation. Compared to GOA micelles, GOA/miR-122 NPs displayed stronger tumor inhibition (73% regression) after intravenous injection in nude mice xenografted with HCC, along with rapid clearance in normal liver tissues. Furthermore, there is no significant influence on biochemical indicators and immune factors during the systematic administration of GOA/miR-122 NPs. The non-cationic GOA/miR NPs engineered by hydrogen bond interaction and hydrophobic forces show the enhanced synergistic antitumor efficacy and good biosafety, which will provide a potential nanomedcine for HCC treatment.
View Article and Find Full Text PDF

Download full-text PDF

Source
http://dx.doi.org/10.1016/j.jconrel.2019.11.010DOI Listing
December 2019

Efficacy of melanoma patients treated with PD-1 inhibitors: Protocol for an overview, and a network meta-analysis of randomized controlled trials.

Medicine (Baltimore) 2019 Jul;98(27):e16342

Gansu Province Hospital Rehabilitation Center, China.

Background: Melanoma is a malignant tumor of melanocytes that produces pigments and can occur in the whole body. It is characterized by strong invasiveness, high metastasis rate and poor prognosis, and brings heavy burden to patients and society. In order to find the most effective and safe treatment measures, in this study, a network meta-analysis (NMA) for randomized controlled trials (RCTs) of advanced melanoma treated with PD-1 inhibitors will be conducted based on the existing systematic reviews (SRs) of PD-1 inhibitor in the treatment of advanced melanoma.

Methods: PubMed, EMBASE, Web of Science and the Cochrane Library were searched on December 18, 2018 to obtain systematic reviews of PD-1 inhibitor in the treatment of advanced melanoma. Assessing the Methodological Quality of Systematic Reviews (AMSTAR2) will be used to assess the methodological quality of systematic reviews, Grading of Recommendations Assessment, Development, and Evaluation (GRADE) approach will be applied to evaluate the evidence quality of outcome measures, and the Cochrane's risk of bias tool will be utilized to appraise risks of bias of each embedded RCTs. And the outcomes are overall survival (OS), progression-free survival (PFS) and objective response rate (ORR). Hazard ratio (HR) or odds ratio (OR) with their 95% confidence interval (CI) were used to synthesize dichotomous outcomes, while the mean difference (MD) for the continuous variables. R3.5.1 will be used to create a network evidence map for direct and indirect comparative analysis.

Results: This study will provide a comprehensive summary of the current evidences related to the efficacy and safety of PD-1 inhibitor in advanced melanoma.

Conclusion: Our findings will be useful to assist clinicians make reasonable decisions to the treatment of advanced melanoma.

Ethics And Communication: It is unnecessary for this NMA to acquire an ethical approval, because it is based on published researches.

Prospero Registration Number: CRD42019120017.
View Article and Find Full Text PDF

Download full-text PDF

Source
http://dx.doi.org/10.1097/MD.0000000000016342DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC6635302PMC
July 2019

Regulating intracellular fate of siRNA by endoplasmic reticulum membrane-decorated hybrid nanoplexes.

Nat Commun 2019 06 20;10(1):2702. Epub 2019 Jun 20.

Beijing Key Laboratory of Molecular Pharmaceutics and New Drug Delivery Systems, State Key Laboratory of Natural and Biomimetic Drugs, School of Pharmaceutical Sciences, Peking University, 100191, Beijing, China.

Most cationic vectors are difficult to avoid the fate of small interfering RNA (siRNA) degradation following the endosome-lysosome pathway during siRNA transfection. In this study, the endoplasmic reticulum (ER) membrane isolated from cancer cells was used to fabricate an integrative hybrid nanoplexes (EhCv/siRNA NPs) for improving siRNA transfection. Compared to the undecorated Cv/siEGFR NPs, the ER membrane-decorated EhCv/siRNA NPs exhibits a significantly higher gene silencing effect of siRNA in vitro and a better antitumor activity in nude mice bearing MCF-7 human breast tumor in vivo. Further mechanistic studies demonstrate that functional proteins on the ER membrane plays important roles on improving cellular uptake and altering intracellular trafficking pathway of siRNA. It is worth to believe that the ER membrane decoration on nanoplexes can effectively transport siRNA through the endosome-Golgi-ER pathway to evade lysosomal degradation and enhance the silencing effects of siRNA.
View Article and Find Full Text PDF

Download full-text PDF

Source
http://dx.doi.org/10.1038/s41467-019-10562-wDOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC6586638PMC
June 2019

Effects of different interventions on animal models of ischemic stroke: Protocol for an overview and a network meta-analysis.

Medicine (Baltimore) 2019 Apr;98(17):e15384

Gansu Provincial Hospital, Lanzhou City, Gansu Province, China.

Background: Ischemic stroke often leads to lifelong disability or death in stroke patients. It is one of the most common causes of death and disability worldwide, so it is a global health problem. The objective of this protocol is to provide the methods for using overview and network meta-analysis to identify the more effective intervention for infarct volume and neurobehavioral score in animal models of ischemic stroke.

Methods: A systematic literature search will be conducted in PubMed and Embase to obtain relevant systematic reviews on December 11, 2018. Assessing the Methodological Quality of Systematic Reviews (AMSTAR2) and SYRCLE's risk of bias tool will be used to assess quality of the included reviews and risk of bias of randomized controlled trials (RCTs) for animal studies. Infarct volume and neurobehavioral score will be chosen as primary and secondary outcomes. The relative effect size of the treatment will be calculated using the standardized mean difference (SMD) and 95% confidence interval (CI). R 3.5.1 through the GEMTC package will be used to perform a network meta-analysis to synthesize direct and indirect evidence.

Results: The results of this paper will be submitted to a peer-reviewed journal for publication.

Conclusion: Our study can provide a reference for further clinical practice and can be compared with clinical trial results to obtain a more credible therapeutic effect of this intervention.

Ethics And Communication: Formal ethical approval is unnecessary, because this study is based on published researches.

Prospero Registration Number: CRD42019126811.
View Article and Find Full Text PDF

Download full-text PDF

Source
http://dx.doi.org/10.1097/MD.0000000000015384DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC6831226PMC
April 2019

Enhanced anti-tumor efficiency of gemcitabine prodrug by FAPα-mediated activation.

Int J Pharm 2019 Mar 21;559:48-57. Epub 2019 Jan 21.

Beijing Key Laboratory of Molecular Pharmaceutics and New Drug Delivery Systems, State Key Laboratory of Natural and Biomimetic Drugs, School of Pharmaceutical Sciences, Peking University Health Science Center, Beijing 100191, China.

Gemcitabine (Gem) as an anti-cancer agent has been limited by its short circulation time and rapid metabolism that reflects in low tumor uptake and low therapeutic efficiency. To improve its anti-tumor activity, a novel FAPα enzyme-activated prodrug of Z-GP-Gem modified at 4-amino group of Gem was developed, which could effectively release parent Gem based on the specific cleavage via FAPα enzyme-activation in tumor microenvironment. Compared to Gem, the Z-GP-Gem prodrug exhibited significantly enhanced inhibition of both tumor growth and pulmonary metastasis in BALB/c mice bearing orthotopic breast 4T1 tumors. The Z-GP-Gem prodrug has a prolonged circulation time and a high tumor uptake based on the modification of Z-GP dipeptide at 4-amino group of Gem. These eventually caused a marked improvement in the systemic toxicity and the tumor growth inhibition in 4T1 cells. More interestingly, the unexpected depletion of tumor-associated fibroblast (TAF) was observed during the treatment of Z-GP-Gem prodrug in animal model. Therefore, these findings demonstrated that the FAPα-activated prodrug Z-GP-Gem would be a desirable approach for tumor therapy by intravenous administration.
View Article and Find Full Text PDF

Download full-text PDF

Source
http://dx.doi.org/10.1016/j.ijpharm.2019.01.032DOI Listing
March 2019

Long non-coding RNA LINC01133 silencing exerts antioncogenic effect in pancreatic cancer through the methylation of DKK1 promoter and the activation of Wnt signaling pathway.

Cancer Biol Ther 2019 22;20(3):368-380. Epub 2018 Dec 22.

a Department of General Surgery , Ruijin Hospital Affiliated to Shanghai Jiaotong University School of Medicine , Shanghai , P.R. China.

Recent studies have acknowledged the critical roles played by long non-coding RNAs (lncRNAs) in the development and progression of pancreatic cancer. Therefore, the present study aimed to elucidate the mechanism underlying on how LINC01133 regulates the Wnt signaling pathway in pancreatic cancer. A microarray-based gene expression analysis was performed to identify the differentially expressed lncRNAs in pancreatic cancer. In addition, ectopic expression assays, knockdown experiments and gene reporter assays were conducted to clarify the role of LINC01133 in pancreatic cancer and to understand the interaction between LINC01133 and the methylation of DKK1 promoter. The expression of LINC01133, DKK1, and other genes related to the Wnt signaling pathway was also measured. EDU staining, scratch test and Transwell assay were employed to measure the proliferation, migration and invasion of pancreatic cancer cells, respectively. GSE32676 and GSE16515 revealed that LINC01133 was upregulated in pancreatic cancer, which was also associated with increased DKK1 methylation and higher expression of genes related to the Wnt signaling pathway, although the expression of DKK1 decreased in pancreatic cancer. In addition, LINC01133 bound to the promoter region of DKK1, resulting in the trimethylation of H3K27 and decreased DKK1 expression, while the expression of Wnt-5a, MMP-7, and β-catenin increased upon LINC01133 binding. Finally, over-expressed LINC01133 enhanced the growth, proliferation, migration, metastasis, and invasion of pancreatic cancer cells. The present study clarified the distinct effect of LINC01133 on pancreatic cancer. In summary, by inducing the methylation of DKK1 promoter, LINC01133 silencing suppresses the development of pancreatic cancer cells through the Wnt signaling pathway.
View Article and Find Full Text PDF

Download full-text PDF

Source
http://dx.doi.org/10.1080/15384047.2018.1529110DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC6370374PMC
May 2020

EZH2-Mediated microRNA-139-5p Regulates Epithelial-Mesenchymal Transition and Lymph Node Metastasis of Pancreatic Cancer.

Mol Cells 2018 Sep 18;41(9):868-880. Epub 2018 Sep 18.

Department of General Surgery, Ruijin Hospital Affiliated to Shanghai Jiaotong University School of Medicine, Shanghai 200025, P.R. China.

Pancreatic cancer (PC) is one of the most aggressive cancers presenting with high rates of invasion and metastasis, and unfavorable prognoses. The current study aims to investigate whether EZH2/miR-139-5p axis affects epithelial-mesenchymal transition (EMT) and lymph node metastasis (LNM) in PC, and the mechanism how EZH2 regulates miR-139-5p. Human PC and adjacent normal tissues were collected to determine expression of EZH2 and miR-139-5p, and their relationship with clinicopathological features of PC. Human PC cell line was selected, and treated with miR-139-5p mimics/inhibitors, EZH2 vector or shEZH2 in order to validate the regulation of EZH2-mediated miR-139-5p in PC cells Dual-luciferase report gene assay and chromatin immunoprecipitation assay were employed to identify the relationship between miR-139-5p and EZH2. RT-qPCR and Western blot analysis were conducted to determine the expression of miR-139-5p, EZH2 and EMT-related markers and ZEB1/2. Tumor formation ability and cell activity were also analyzed. Highly-expressed EZH2 and poorly-expressed miR-139-5p were detected in PC tissues, and miR-139-5p and EZH2 expressions were associated with patients at Stage III/IV, with LNM and highly-differentiated tumors. EZH2 suppressed the expression of miR-139-5p through up-regulating Histone 3 Lysine 27 Trimethylation (H3K27me3). EMT, cell proliferation, migration and invasion were impeded, and tumor formation and LNM were reduced in PC cells transfected with miR-139-5p mimics and shEZH2. MiR-139-5p transcription is inhibited by EZH2 through up-regulating H3K27me3, thereby down-regulation of EZH2 and up-regulation of miR-139-5p impede EMT and LNM in PC. In addition, the EZH2/miR-139-5p axis presents as a promising therapeutic strategy for the treatment of PC.
View Article and Find Full Text PDF

Download full-text PDF

Source
http://dx.doi.org/10.14348/molcells.2018.0109DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC6182224PMC
September 2018

[email protected]: A Metal-Organic-Framework-Based Bifunctional Composite Catalyst for a One-Pot Sequential Asymmetric Morita-Baylis-Hillman Reaction.

Inorg Chem 2019 Apr 9;58(8):4722-4730. Epub 2018 Oct 9.

College of Chemistry, Chemical Engineering and Materials Science, Collaborative Innovation Centre of Functionalized Probes for Chemical Imaging in Universities of Shandong, Key Laboratory of Molecular and Nano Probes, Ministry of Education , Shandong Normal University , Jinan 250014 , P. R. China.

A chiral ionic liquid (CIL) moiety of a l-pyrrolidin-2-ylimidazole-decorated homochiral UiO-68-type metal-organic framework, UiO-68-CIL (1), was successfully prepared by the combination of a new premodified chiral CIL ligand (HL-CIL) and ZrCl via a solvothermal method. The TiO-loaded [email protected] (2) was prepared by impregnating 1 in a toluene solution of Ti(OPr) and sequential in situ hydrolysis. The obtained 2 can be a bifunctional asymmetric heterogeneous catalyst to successfully promote the one-pot Morita-Baylis-Hillman reaction starting from aromatic alcohols in a tandem way.
View Article and Find Full Text PDF

Download full-text PDF

Source
http://dx.doi.org/10.1021/acs.inorgchem.8b02132DOI Listing
April 2019

Improved Cell Transfection of siRNA by pH-Responsive Nanomicelles Self-Assembled with mPEG- b-PHis- b-PEI Copolymers.

ACS Appl Mater Interfaces 2018 Jul 19;10(26):21847-21860. Epub 2018 Jun 19.

Beijing Key Laboratory of Molecular Pharmaceutics and New Drug Delivery Systems, State Key Laboratory of Natural and Biomimetic Drugs, School of Pharmaceutical Sciences , Peking University , Xueyuan Road 38 , Beijing 100191 , China.

Here, the novel pH-responsive nanomicelles self-assembled with amphipathic meo-poly(ethylene glycol)- b-poly(l-histidine)- b-polyethylenimine (mPEG- b-PHis- b-PEI, EHE) copolymers based on hydrophobic interaction of PHis with deprotonation of imidazoles were developed for siRNA transfection. The cationic nanomicelles could electrostatically compact siRNA into stable EHE/siRNA nanoplexes with a hydrodynamic diameter of ∼190 nm and present a low toxicity in normal physiological condition (pH ∼ 7.4). Different from pH-irresponsive ECE/siRNA nanoplexes based on mPEG- b-poly(ε-caprolactone)- b-PEI (ECE), the EHE/siRNA nanoplexes exhibited a higher cellular uptake along with an increased ζ-potential (from +18 to +32 mV) when the pH changed from 7.4 to 6.8 (extracellular acidic microenvironments). After cell internalization, the EHE/siRNA nanoplexes also exhibited an enhanced nanostructural disassembling and release of siRNA from lysosomal acidic microenvironments (pH ∼ 5.5). Furthermore, it was demonstrated that the EHE/siEGFR nanoplexes downregulated the expression levels of the corresponding mRNA and protein more efficiently than ECE/siEGFR in HeLa cells. The improved siRNA silencing effects of EHE/siEGFR nanoplexes resulted from the higher cellular uptake and enhanced endosomal/lysosomal escape, which is associated with the pH-responsive disassembly of nanostructure as well as the synergistic "proton sponge" effects of PHis and PEI in EHE copolymers. Therefore, the pH-responsive EHE nanomicelles would be promising and potential carriers for cell transfection of siRNA.
View Article and Find Full Text PDF

Download full-text PDF

Source
http://dx.doi.org/10.1021/acsami.8b04301DOI Listing
July 2018

[email protected]: A MOF-Based Bifunctional Composite Triphase-Transfer Catalyst for Sequential One-Pot Azide-Alkyne Cycloaddition in Water.

Inorg Chem 2017 Jul 26;56(14):8341-8347. Epub 2017 Jun 26.

College of Chemistry, Chemical Engineering and Materials Science, Collaborative Innovation Centre of Functionalized Probes for Chemical Imaging in Universities of Shandong, Key Laboratory of Molecular and Nano Probes, Ministry of Education, Shandong Normal University , Jinan 250014, P. R. China.

A CuI-loaded and n-pentadecyl-attached imidazolium salt decorated UiO-67-type metal-organic framework ([email protected], 2) based on a new premodified ligand L (n-pentadecyl-attached imidazolium (IM) decorated dicarboxylic acid) and ZrCl is reported. Compound 2 can be a bifunctional composite heterogeneous phase-transfer catalyst to promote the azide-alkyne cycloaddition (HO, air, 80 °C) from corresponding halogenated compounds and sodium azide as a sequential one-pot procedure with high yields and excellent regioselectivity.
View Article and Find Full Text PDF

Download full-text PDF

Source
http://dx.doi.org/10.1021/acs.inorgchem.7b01025DOI Listing
July 2017

Progress in Pharmacological Sciences in China.

Mol Pharmacol 2017 09 12;92(3):188-192. Epub 2017 Apr 12.

Department of Health Sciences, National Natural Science Foundation of China (J.-C.W., Y.Z., L.W., E.D.) and School of Pharmaceutical Sciences, Peking University (J.-C.W.), Beijing, China

Pharmacology is the science that investigates the interactions between organisms and drugs and their mechanisms. Pharmacology plays a translational role in modern medicine, bridging basic research and the clinic. With its economy booming, China has invested an enormous amount of financial and human resources in pharmacological research in the recent decade. As a result, major breakthroughs have been achieved in both basic and clinical research, with the discovery of many potential drug targets and biomarkers that has made a sizable contribution to the overall advancement of pharmacological sciences. In this article, we review recent research efforts and representative scientific achievements and discuss future challenges and directions for the pharmacological sciences in China.
View Article and Find Full Text PDF

Download full-text PDF

Source
http://dx.doi.org/10.1124/mol.116.108167DOI Listing
September 2017

Copper(II)-Silver(I) Macrocyclic Metal-Organic Framework: A Highly Efficient Reusable Triplet Oxygen Collector and Singlet Oxygen Generator.

Inorg Chem 2017 Feb 23;56(3):1049-1052. Epub 2017 Jan 23.

College of Chemistry, Chemical Engineering and Materials Science, Collaborative Innovation Center of Functionalized Probes for Chemical Imaging in Universities of Shandong, Key Laboratory of Molecular and Nano Probes, Ministry of Education, Shandong Normal University , Jinan 250014, P. R. China.

The generation of highly reactive oxygen (O) is very significant for a variety of applications such as degradation, bleaching, chemical synthesis, photodynamic therapy for tumor treatment, and others. Herein, we report a novel peroxide-dianion-embedded bimetallic macrocycle, [[email protected]] (2), that can completely release the inserted peroxide dianion as the singlet oxygen (O) via a H-assisted disproportionation process in methanol. Notably, the resulting empty AgCuL(ClO) (3) is able to trap oxygen (O) from air and fixes it in the macrocycle host as a peroxide dianion; furthermore, it releases it as O again in the presence of H. So, the bimetallic macrocycle [AgCuL] herein behaves as a highly efficient reusable triplet oxygen receptor and singlet oxygen generator.
View Article and Find Full Text PDF

Download full-text PDF

Source
http://dx.doi.org/10.1021/acs.inorgchem.6b02918DOI Listing
February 2017

Transdermal Permeation and Anti-Inflammation Activities of Novel Sinomenine Derivatives.

Molecules 2016 Nov 17;21(11). Epub 2016 Nov 17.

College of Chemistry and Chemical Engineering, Hunan University, Changsha 410082, Hunan, China.

Sinomenine is extracted from Sinomenii caulis (a traditional Chinese medicine), and it is used as the active ingredient in rheumatic arthritis treatments. It has been used in clinical applications for decades. However, there are some disadvantages, including low activity in transdermal permeation and a high dosage being clinically required. To overcome these defects, sinomenine was used as a primer, and structural modification was performed. In our study, eight new compounds were screened out by transdermal permeation in vitro and anti-inflammatory response in vitro and in vivo. Compound 1a exhibited the most potent transdermal permeation and anti-inflammatory activity. Based on these results, further development of this compound may be warranted.
View Article and Find Full Text PDF

Download full-text PDF

Source
http://dx.doi.org/10.3390/molecules21111520DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC6273864PMC
November 2016

Corrigendum to "Irbesartan Ameliorates Diabetic Nephropathy by Suppressing the RANKL-RANK-NF-B Pathway in Type 2 Diabetic db/db Mice".

Mediators Inflamm 2016;2016:3151986. Epub 2016 Oct 18.

Department of Nephrology, ZhuJiang Hospital, Southern Medical University, Guangzhou 510280, China.

[This corrects the article DOI: 10.1155/2016/1405924.].
View Article and Find Full Text PDF

Download full-text PDF

Source
http://dx.doi.org/10.1155/2016/3151986DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC5088271PMC
October 2016

Cu(ii)/Cu(0)@UiO-66-NH: base [email protected] as heterogeneous catalysts for olefin oxidation and reduction.

Chem Commun (Camb) 2016 Nov 20;52(89):13116-13119. Epub 2016 Oct 20.

College of Chemistry, Chemical Engineering and Materials Science, Collaborative Innovation Center of Functionalized Probes for Chemical Imaging in Universities of Shandong, Key Laboratory of Molecular and Nano Probes, Ministry of Education, Shandong Normal University, Jinan 250014, P. R. China.

Two copper-loaded MOF materials, namely Cu(ii)@Ui-O-66-NH (1) and Cu(0)@UiO-66-NH (2), are reported. They can, respectively, serve as highly efficient heterogeneous catalysts for olefin oxidation and hydrogenation under mild conditions. Complete styrene hydrogenation occurs in 15 min at ambient temperature with quantitative yield.
View Article and Find Full Text PDF

Download full-text PDF

Source
http://dx.doi.org/10.1039/c6cc06076eDOI Listing
November 2016

Micro-CuI-MOF: reversible iodine adsorption and catalytic properties for tandem reaction of Friedel-Crafts alkylation of indoles with acetals.

Chem Commun (Camb) 2016 Oct;52(86):12702-12705

College of Chemistry, Chemical Engineering and Materials Science, Collaborative Innovation Center of Functionalized Probes for Chemical Imaging in Universities of Shandong, Key Laboratory of Molecular and Nano Probes, Ministry of Education, Shandong Normal University, Jinan, 250014, P. R. China.

We report a convenient approach, the first of its kind, to construct a microscale [email protected] composite catalytic host-guest system for an organic tandem reaction. The reported porous CuI-MOF is able to reversibly adsorb molecular iodine at room temperature. The obtained [email protected] host-guest system can be a highly heterogeneous catalyst to promote the Friedel-Crafts alkylation of indoles with acetals in a one-pot two-step fashion under solvent-free conditions at room temperature.
View Article and Find Full Text PDF

Download full-text PDF

Source
http://dx.doi.org/10.1039/c6cc07027bDOI Listing
October 2016
-->