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Trinuclear gold-catalyzed site-selective alkylation of peptides

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Science China Chemistry 2025年第01期 249-256页

作者： Qing-Yun Fang Chengyihan Gu Yinghan Chen Wencheng Yan Yong Liang Weipeng Li Chengjian Zhu Jie Han Jin Xie State Key laboratory of Coordination Chemistry Jiangsu Key Laboratory of Advanced Organic Materials Chemistry and Biomedicine Innovation Center (Chem BIC) School of Chemistry and Chemical Engineering Nanjing University Green Catalysis Center College of Chemistry Zhengzhou University State Key laboratory of Natural Medicines China Pharmaceutical University

Selective modification of peptides has always been a challenging issue. The selective alkylation of peptides can alter the biological activity and physical properties of molecules, and it has gained significant research interest. We herein disclose an intriguing gold-catalyzed alkylation of peptides using bench-stable unactivated alkyl bromides under photoredox catalysis. A wide range of structurally diverse primary, secondary and tertiary alkyl bromides serve as effective coupling partners to precisely connect with the α-C(sp3)–H in glycine residue of peptides. This protocol demonstrates an exceptionally broad scope for alkyl halides and excellent tolerance for a wide range of useful functional groups. A series of relay transformations to construct cyclic peptides, to proceed click reaction and to realize peptide fluorescence labeling further enhance its synthetic practicality. In addition, mechanistic studies and density functional theory(DFT) calculations reveal an inner-sphere and subsequent outersphere single electron transfer(SET) mechanism.

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Pathogenesis, diagnosis, and treatment of epilepsy: electromagnetic stimulation-mediated neuromodulation therapy and new technologies

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Neural Regeneration Research 2025年第4期20卷 917-935页

作者： Dian Jiao Lai Xu Zhen Gu Hua Yan Dingding Shen Xiaosong Gu Academy of Medical engineering and Translational Medicine Tianjin UniversityTianjinChina Key laboratory of Advanced Drug Delivery Systems of Zhejiang Province College of Pharmaceutical SciencesZhejiang UniversityHangzhouZhejiang ProvinceChina Affiliated Hospital of Nantong University NantongJiangsu ProvinceChina

Epilepsy is a severe,relapsing,and multifactorial neurological *** regarding the accurate diagnosis,prognosis,and in-depth pathogenesis are crucial for the precise and effective treatment of *** pathogenesis of epilepsy is complex and involves alterations in variables such as gene expression,protein expression,ion channel activity,energy metabolites,and gut microbiota *** results are lacking for conventional treatments for *** resection of lesions,drug therapy,and non-drug interventions are mainly used in clinical practice to treat pain associated with ***-pharmacological treatments,such as a ketogenic diet,gene therapy for nerve regeneration,and neural regulation,are currently areas of research *** review provides a comprehensive overview of the pathogenesis,diagnostic methods,and treatments of *** also elaborates on the theoretical basis,treatment modes,and effects of invasive nerve stimulation in neurotherapy,including percutaneous vagus nerve stimulation,deep brain electrical stimulation,repetitive nerve electrical stimulation,in addition to non-invasive transcranial magnetic stimulation and transcranial direct current *** studies have shown that electromagnetic stimulation-mediated neuromodulation therapy can markedly improve neurological function and reduce the frequency of epileptic ***,many new technologies for the diagnosis and treatment of epilepsy are being ***,current research is mainly focused on analyzing patients’clinical manifestations and exploring relevant diagnostic and treatment methods to study the pathogenesis at a molecular level,which has led to a lack of consensus regarding the mechanisms related to the disease.

关键词： diagnosis drug treatment electroencephalography epilepsy monitoring epilepsy nerve regeneration neurostimulation non-drug interventions pathogenesis prediction

Feasibility of drug delivery to the eye’s posterior segment by topical instillation of PLGA nanoparticles

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Asian Journal of pharmaceutical Sciences 2017年第4期12卷 394-399页

作者： Kohei Tahara Keiichi Karasawa Risako Onodera Hirofumi Takeuchi laboratory of pharmaceutical engineering Gifu Pharmaceutical University

We investigated the delivery of drugs to the posterior segment of the eye by non-invasive topical instillation using submicron-sized poly(D,L-lactide-co-glycolide)(PLGA) nanoparticles(NPs). Surface-modified PLGA NPs were developed to improve the drug delivery efficiency to the retina and were administered as topical eye drops to mice. Chitosan(CS) and glycol chitosan(GCS), which are mucoadhesive polymers, and polysorbate 80(P80) were used as surface modifiers, and have been reported to increase the association of NPs with ***-6 was used as a model drug and fluorescent marker, and after ocular administration of PLGA NP eye drops, the fluorescence intensity of coumarin-6 was observed in the retina. The fluorescence image analysis indicated that there are several possible routes to the retina and fates of PLGA NPs in ocular tissue, and that these pathways involved the corneal,non-corneal, or uveal routes. Delivery to the mouse retina segments after topical administration was increased by surface modification with CS, GCS, or P80. Surface-modified PLGA NPs are a promising method for retinal drug delivery via topical instillation.

关键词： PLGA Nanoparticles Topical instillation Retina Surface modification

Role of copper chelating agents: between old applications and new perspectives in neuroscience

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Neural Regeneration Research 2025年第3期20卷 751-762页

作者： Rosalba Leuci Leonardo Brunetti Vincenzo Tufarelli Marco Cerini Marco Paparella Nikola Puvača Luca Piemontese Department of Pharmacy-pharmaceutical Science University of Bari Aldo MoroBariItaly Department of Precision and Regenerative Medicine and Jonian Area(DiMePRe-J) Section of Veterinary Science and Animal ProductionUniversity of Bari Aldo MoroBariItaly Department of engineering Management in Biotechnology Faculty of Economics and Engineering Management in Novi SadUniversity Business Academy in Novi SadNovi SadSerbia

The role of copper element has been an increasingly relevant topic in recent years in the fields of human and animal health, for both the study of new drugs and innovative food and feed supplements. This metal plays an important role in the central nervous system, where it is associated with glutamatergic signaling, and it is widely involved in inflammatory processes. Thus, diseases involving copper(Ⅱ) dyshomeostasis often have neurological symptoms, as exemplified by Alzheimer's and other diseases(such as Parkinson's and Wilson's diseases). Moreover, imbalanced copper ion concentrations have also been associated with diabetes and certain types of cancer, including glioma. In this paper, we propose a comprehensive overview of recent results that show the importance of these metal ions in several pathologies, mainly Alzheimer's disease, through the lens of the development and use of copper chelators as research compounds and potential therapeutics if included in multi-target hybrid drugs. Seeing how copper homeostasis is important for the well-being of animals as well as humans, we shortly describe the state of the art regarding the effects of copper and its chelators in agriculture, livestock rearing, and aquaculture, as ingredients for the formulation of feed supplements as well as to prevent the effects of pollution on animal productions.

关键词： agriculture Alzheimer's disease chelators copper feed supplements multi-target

Zirconium-mediated Synthesis and Crystal Structure of 3,6-Diiodo-4,5-dialkyl-phthalic Acid Dimethyl Ester

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Chinese Journal of Structural Chemistry 2015年第9期34卷 1347-1356页

作者：李旭东王会李君秋门奕灿曲红梅 Key laboratory of Systems Bioengineering Ministry of EducationTianjin Key Laboratory of Biological and Pharmaceutical EngineeringDepartment of Pharmaceutical EngineeringSchool of Chemical Engineering and TechnologyTianjin University

A novel series of para-diiodobenzene derivatives, 3,6-diiodo-4,5-dialkyl-phthalic acid dimethyl esters, were prepared via cycloaddition of two TMS-substituted alkynes and dimethyl acetylenedicarboxylate, which was mediated by zirconocene. After iodination, three new compounds of 3,6-diiodo-4,5-dimethyl（dipropyl, dibutyl）-phthalic acid dimethyl esters （3a, 3b, 3c） were synthesized in high region-selectivity and yields, and characterized by NMR. The crystal structures were determined by single-crystal X-ray diffraction. The crystal of 3a （C12H121204, Mr = 474.02） belongs to the triclinic system, space group Pi with a = 7.6238（10）, b = 9.4571（12）, c = 10.8221（14） A, a = 66.611（10）, fl = 88.511（12）, 7 ： 77.604（11）% V= 697.93（16） A3, Z= 2, F（000） = 444, Dc = 2.256 mg/m3, g = 4.509 mm-1, T=133（2） K, S = 1.014, R = 0.0229 and wR = 0.0547 for 2644 observed reflections with I 〉 20（/）; the crystal of 3b （C16H201204, Mr - 530.12） is of triclinic system, space group Pi with a = 9.4122（19）, b = 10.626（2）, c = 11.353（2） A, a = 97.90（3）, fl = 113.83（3）, y = 110.22（3）°, V= 922.6（3） A3, Z- 2, F（000） = 508, Dc - 1.908 mg/m3, g = 3.422 mm-1, T = 113（2） K, S = 1.115, R = 0.0428 and wR = 0.1072 for 3971 observed reflections with I〉 20（/）; the crystal of 3c （ClsH241204, Mr = 558.17） belongs to the monoclinic system, space group P21/c with a = 26.396（2）, b = 8.7560（8）, c = 25.7970（18） A, fl = 91.721（4）o, V= 5959.6（8） A3, Z = 12, F（000） = 3240, Dc = 1.866 mg/m3,/z = 3.184 mm-l, T= 113（2） K, S = 1.154, R = 0.0424 and wR = 0.0766 for 13056 observed reflections with I 〉 20（/）.

关键词： zirconocene 3,6-diiodo-4,5-dialkyl-phthalic acid dimethyl ester,para-diiodobenzene derivative crystal structure X-ray diffraction NMR

Crystal Structure,Photoluminescence and Theoretical Studies of Diethyl 4,5-di(thienyl)-3,6-bis(trimethylsilyl)phthalate

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Chinese Journal of Structural Chemistry 2013年第10期32卷 1560-1566页

作者：唐建可牛心蕙蒋丽丽曲红梅 Key laboratory of Systems Bioengineering Ministry of EducationTianjin Key Laboratory of Biological and Pharmaceutical EngineeringDepartment of Pharmaceutical Engineering School of Chemical Engineering and TechnologyTianjin University

The crystal structure of the title compound, diethyl 4,5-di（thienyl）-3,6-bis（trime- thylsilyl）phthalate （C26H3404S2Si2, Mr = 530.83）, has been determined by single-crystal X-ray diffraction. The crystal belongs to the orthorhombic system, space group Pccn with a = 43.008（5）, b = 10.9000（12）, c = 11.9357（14） A, V= 5595.3（11） A3, Z = 8, F（000） = 2256, Dc= 1.260 mg/m3, p = 0.305 mm-1, T = 113（2） K, S = 1.090, R = 0.0413 and wR = 0.0969 for 5952 observed reflections with 1 〉 2o（/）. The benzene ring system is planar and makes dihedral angles of 63.7（2） and 72.5（4） with the two thienyl rings A （C（23）-C（26）, S（2）） and B （C（19）-C（22）, S（1））, respectively. The UV-vis absorption and fluorescence of the title compound were discussed. The molecular structure of the title compound has been optimized using DFT method at the B3LYP/6-31G（d） level. The computational results showed that the optimized geometer parameters are consistent well with the experiment data. The vertical ionization potential, vertical electron affinity and frontier orbitals were also discussed.

关键词： crystal structure benzene derivatives orthorhombic system,photoluminescence B3LYP/6-31G(d)

Crystal Structure and Interaction with DNA of [Ni(phen)(mal)(H_2O)_2]·3H_2O

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Chinese Journal of Structural Chemistry 2007年第1期26卷 59-62页

作者：高恩君程卯生于影孙亚光 laboratory of Coordination Chemistry Shenyang Institute of Chemical Technology College of pharmaceutical engineering Shenyang Pharmaceutical University

A new complex [Ni（phen）（mal）（H2O）2]·3H2O （phen = 1,10-phenanthroline, real^2- = malonic acid） has been synthesized by the reaction of nickel nitrate, phen and malonic acid. EA, IR spectra and X-ray single-crystal diffraction were carried out to determine the composition and crystal structure of the title complex. Crystal data： monoclinic system, space group P2/c,α = 8.937（3）, b = 12.163（5）, c = 9.725（3） A,β = 119.36°, C15H19N2O9Ni,Mr= 430.03, Z = 2, F（000） = 446, V= 921.3 A3, Dc = 1.550 g/cm^3, μ= 1.104 mm^-1, -10≤h≤10, -12≤k≤ 14, -11≤1≤7, R = 0.0261 and wR = 0.0609 for 4376 （Rint = 0.0203） independent reflections and 1631 observed ones （I 〉 2σ（I））. Ni（Ⅱ） exhibits an octahedral coordination geometry, with hydrogen bonds and π-π interactions stabilizing the whole structure. UV spectrum of the complex interacting with protamine DNA indicates that the title compound interacts with DNA via insertion mode with bonding constant Kb of 1. 11 × 10^4.

关键词： Ni( Ⅱ ) molecular structure weak interaction DNA

Formulation design of granules prepared by wet granulation method using a multi-functional single-punch tablet press to avoid tableting failures

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Asian Journal of pharmaceutical Sciences 2018年第2期13卷 113-119页

作者： Takashi Osamura Yoshiko Takeuchi Risako Onodera Masahiro Kitamura Yoshiteru Takahashi Kohei Tahara Hirofumi Takeuchi laboratory of pharmaceutical engineering Gifu Pharmaceutical University pharmaceutical Technology Department Sawai Pharmaceutical Co.Ltd

We previously determined "Tableting properties" by using a multi-functional single-punch tablet press(GTP-1). We plotted "Compactability" on the x-axis against "Manufacturability"on the y-axis to allow visual evaluation of "Tableting properties". Here, we examined whether this evaluation method can be used in the formulation design of tablets prepared by wet granulation. We used the GTP-1 to measure "Tableting properties" with different amounts of binder, disintegrant, and lubricant, and compared the results with those of tableting on a commercial rotary tableting machine. Tableting failures(capping and binding in particular) occurred when samples that had been evaluated as having poor "Compactability" or"Manufacturability" on the GTP-1 were compressed on the rotary tableting machine. Thus,our evaluation method predicted tableting failure at the commercial scale. The method will prove useful for scaling up production.

关键词： tableting formulation design wet granulation capping binding single-punch tablet press

Utilizing engineered extracellular vesicles as delivery vectors in the management of ischemic stroke:a special outlook on mitochondrial delivery

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Neural Regeneration Research 2025年第8期20卷 2181-2198页

作者： Jiali Chen Yiyang Li Xingping Quan Jinfen Chen Yan Han Li Yang Manfei Zhou Greta Seng Peng Mok Ruibing Wang Yonghua Zhao Institute of Chinese Medical Sciences State Key Laboratory of Quality Research in Chinese MedicineUniversity of MacaoTaipaMacao Special Administrative RegionChina Department of Pharmacy Hunan Provincial People’s Hospitalthe First Affiliated Hospital of Hunan Normal UniversityChangshaHunan ProvinceChina Department of Electrical and Computer engineering University of MacaoTaipaMacao Special Administrative RegionChina Department of pharmaceutical Sciences Faculty of Health SciencesUniversity of MacaoTaipaMacao Special Administrative RegionChina

Ischemic stroke is a secondary cause of mortality worldwide,imposing considerable medical and economic burdens on *** vesicles,serving as natural nanocarriers for drug delivery,exhibit excellent biocompatibility in vivo and have significant advantages in the management of ischemic ***,the uncertain distribution and rapid clearance of extracellular vesicles impede their delivery *** utilizing membrane decoration or by encapsulating therapeutic cargo within extracellular vesicles,their delivery efficacy may be greatly ***,previous studies have indicated that microvesicles,a subset of large-sized extracellular vesicles,can transport mitochondria to neighboring cells,thereby aiding in the restoration of mitochondrial function post-ischemic *** extracellular vesicles have also demonstrated the capability to transfer mitochondrial components,such as proteins or deoxyribonucleic acid,or their sub-components,for extracellular vesicle-based ischemic stroke *** this review,we undertake a comparative analysis of the isolation techniques employed for extracellular vesicles and present an overview of the current dominant extracellular vesicle modification *** the complex facets of treating ischemic stroke,we also delineate various extracellular vesicle modification approaches which are suited to different facets of the treatment ***,given the burgeoning interest in mitochondrial delivery,we delved into the feasibility and existing research findings on the transportation of mitochondrial fractions or intact mitochondria through small extracellular vesicles and microvesicles to offer a fresh perspective on ischemic stroke therapy.

关键词： delivery engineering extracellular vesicles identification ischemic stroke isolation mitochondria targeting strategy therapeutic effects