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Mechanism of action of the bile acid receptor TGR5 in obesity

Acta Pharmaceutica Sinica B 2024年第2期14卷 468-491页

作者： Weijun Lun Qihao Yan Xinghua Guo Minchuan Zhou Yan Bai Jincan He Hua Cao Qishi Che Jiao Guo Zhengquan Su Guangdong Engineering research Center of Natural Products and New Drugs Guangdong Provincial University Engineering Technology Research Center of Natural Products and DrugsGuangdong Pharmaceutical UniversityGuangzhou 510006China Guangdong Metabolic Disease research Center of Integrated Chinese and Western Medicine Key Laboratory of Glucolipid Metabolic DisorderMinistry of Education of ChinaGuangdong TCM Key Laboratory for Metabolic DiseasesGuangdong Pharmaceutical UniversityGuangzhou 510006China School of Public Health Guangdong Pharmaceutical UniversityGuangzhou 510310China School of Chemistry and Chemical Engineering Guangdong Pharmaceutical UniversityZhongshan 528458China Guangzhou Rainhome Pharm&Tech Co. Ltd.Science CityGuangzhou 510663China

G protein-coupled receptors(GPCRs)are a large family of membrane protein receptors,and Takeda G protein-coupled receptor 5(TGR5)is a member of this *** a membrane receptor,TGR5 is widely distributed in different parts of the human body and plays a vital role in regulating metabolism,including the processes of energy consumption,weight loss and blood glucose *** studies have shown that TGR5 plays an important role in glucose and lipid metabolism disorders such as fatty liver,obesity and *** the global obesity situation becoming more and more serious,a comprehensive explanation of the mechanism of TGR5 and filling the gaps in knowledge concerning clinical ligand drugs are urgently *** this review,we mainly explain the anti-obesity mechanism of TGR5 to promote the further study of this target,and show the electron microscope structure of TGR5 and review recent studies on TGR5 ligands to illustrate the specific binding between TGR5 receptor binding sites and ligands,which can effectively provide new ideas for ligand research and promote drug research.

关键词： Obesity TGR5 Bile acids Ligand Appetite Metabolism GLP-1 Inflammation

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Changes in Metabolites and Allelopathic Effects of Non-Pigmented and Black-Pigmented Lowland Indica Rice Varieties in Phosphorus Deficiency

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Rice science 2024年第4期31卷 434-448,I0025,I0026页

作者： Liyana SARA Sompop SAEHENG Panupong PUTTARAK Lompong KLINNAWEE Division of Biological Science Faculty of SciencePrince of Songkla UniversitySongkhla 90110Thailand Division of Health and Applied Sciences Faculty of SciencePrince of Songkla UniversitySongkhla 90110Thailand Plant Cell and Physiology for Sustainable Agriculture research Unit Faculty of SciencePrince of Songkla UniversitySongkhla 90110Thailand department of Pharmacognosy and pharmaceutical Botany Faculty of Pharmaceutical SciencesPrince of Songkla UniversitySongkhla 90110Thailand Phytomedicine and pharmaceutical Biotechnology Excellence Center Prince of Songkla UniversitySongkhla 90110Thailand

Phosphorus(P) levels alter the allelopathic activity of rice seedlings against lettuce seeds. In this study, we investigated the effect of P deficiency on the allelopathic potential of non-pigmented and pigmented rice varieties. Rice seedlings of the white variety Khao Dawk Mali(KDML105, non-pigmented) and the black varieties Jao Hom Nin(JHN, pigmented) and Riceberry(RB, pigmented) were cultivated under high P(HP) and low P(LP) conditions. Morphological and metabolic responses to P deficiency were investigated. P deficiency inhibited shoot growth but promoted root growth of rice seedlings in all three varieties. Moreover, P deficiency led to decreased cytosolic phosphate(Pi) and total P concentrations in both shoot and root tissues. The subsequent reduction in internal P concentration enhanced the accumulation of phenolic compounds in both shoot and root tissues of the seedlings. Subsequently, allelopathy-based inter-and intra-specific interactions were assessed using water extracts from seedlings of the three varieties grown under HP and LP conditions. These extracts were tested on seeds of lettuce, the weed Dactyloctenium aegyptium, and the same rice variety. The shoot and root extracts from P-deficient seedlings reduced the germination of all recipient plants. Specifically, the shoot extract from P-deficient KDML105 seedlings reduced the germination index(GI) of lettuce seeds to 1%, while those from P-deficient RB and JHN seedlings produced GIs of 32% and 42%, respectively. However, when rice seeds were exposed to their own LP shoot and root extracts, their GIs increased up to 4-fold, compared with the HP extracts. Additionally, the shoot extracts from P-deficient plants also stimulated the germination of D. aegyptium by about 2–3-fold, whereas the root extracts did not have this effect. Therefore, P starvation led to the accumulation and exudation of phenolics in the shoots and roots of rice seedlings, altering their allelopathic activities. To adapt to P defici

关键词： phosphorus deficiency non-pigmented and black-pigmented rice phenolics extract allelopathy

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Jun12682,a potent SARS-CoV-2 papain-like protease inhibitor with exceptional antiviral efficacy in mice

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Acta Pharmaceutica Sinica B 2024年第9期14卷 4189-4192页

作者： Mianling Yang Meehyein Kim Peng Zhan department of Medicinal Chemistry Key Laboratory of Chemical Biology(Ministry of Education)School of Pharmaceutical SciencesShandong UniversityJi’nan 250012China Infectious Diseases Therapeutic research Center Korea Research Institute of Chemical Technology(KRICT)Daejeon 34114Republic of Korea

Recently,a collaborative research study published in Science,led by Jun Wang,Xufang Deng,Eddy Arnold,and Francesc Xavier Ruiz1,identified a series of potent small molecule inhibitors that specifically target SARS-CoV-2 papain-like protease(PLpro).The study demonstrated nanomolar PLpro inhibitory potency with Ki values ranging from 13.2 to 88.2 nmol/*** employing a structure-based drug design strategy,the researchers discovered an exceptionally promising compound,named Jun12682,that effectively targets both the newly discovered ubiquitin Val70(Val70Ub)-binding site and the known blocking loop(BL2)groove near the S4 subsite of ***,studies on the mechanism of action revealed that Jun12682 inhibits the deubiquitinating and deISGylating activities of PLpro,which are crucial for antagonizing the host’s innate immune response upon viral *** biology studies confirmed the“two-pronged”binding mode of Jun12682,aligning perfectly with their drug design ***,Jun12682 exhibited potent antiviral activity against SARS-CoV-2 and its variants,including nirmatrelvir-resistant mutants,in Caco-2 cells(EC50:0.44e2.02 mmol/L).It is noteworthy that its oral administration significantly improved survival rates and alleviated both lung virus loads and histopathological lesions in a lethal SARS-CoV-2 mouse *** conclusion。

关键词： SARS-CoV-2 Papain-like protease Broad-spectrum Anti-drug resistance Drug candidate

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A new hydrophobic deep eutectic solvent composed of menthol and tris(2-ethylhexyl) phosphate for solvent bar microextraction of parabens from biological fluids

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Emerging Contaminants 2024年第2期10卷 135-145页

作者： Nabil N.AL-Hashimi Husam Abed Alfattah Khaleel I.Assaf Asma A.Fakhoury Saja H.Hamed Amjad H.El-Sheikh Khairi M.Fahelelbom The Hashemite University Faculty of Pharmaceutical SciencesDepartment of Pharmaceutical ChemistryP.O.Box 330127Zarqa13133Jordan The Hashemite University Faculty of ScienceDepartment of ChemistryP.O.Box 150459Zarqa13115Jordan Al-Balqa Applied University Faculty of ScienceDepartment of Chemistry19117 Al-SaltJordan The Hashemite University Faculty of Pharmaceutical SciencesDepartment of Pharmaceutics and Pharmaceutical TechnologyP.O.Box 330127Zarqa13133Jordan Al Ain University College of PharmacyDepartment of Pharmaceutical SciencesP.O.Box 64141Al AinAl AinUnited Arab Emirates

Parabens are antimicrobial preservatives with extensive applications in cosmetics,toiletries,pharmaceuticals,and *** the legitimate concerns relating to their potential to disrupt multiple endocrine functions,it becomes imperative to prioritize the development of innovative bioanalytical techniques for effectively monitoring their presence in biological *** this study,an efficient solvent bar microextraction(SBME)was established,utilizing new hydrophobic deep eutectic solvents(DEs)to determine methylparaben and propylparaben in urine and plasma *** DEs comprising menthol and tris(2-ethylhexyl)phosphate(M-TEHP)at various molar ratios were synthesized for the first time to enhance the extraction capacity and promote the eco-friendliness of the DE used as an extraction ***-transform infrared(FT-IR)and proton nuclear magnetic resonance(1H NMR)spectroscopies were employed to confirm and investigate the properties of the successful synthesis(M-TEHP)DE at a molar ratio of 1:*** synthesized DE exhibits low microbial toxicity and can be considered an eco-friendly solvent for ***,quantum-chemical calculations were utilized to predict synthesized DE's structure and interaction energy with selected *** influential operational factors of DE-SBME on the extraction efficiency(EE%)of both parabens were evaluated using response surface methodology based on central composite design,and a total of 30 extraction tests were conducted to determine the optimal *** optimized DE-SBME,in combination with HPLC-DAD,exhibited low detection limits(0.54–0.91μg L^(−1)),excellent linearity(R^(2)≥0.9993),precise results(RSDs≤7.6%),satisfactory recoveries(92–97%)and negligible matrix ***,it had remarkable effectiveness and applicability in determining selected parabens in real urine and plasma samples.

关键词： Hydrophobic deep eutectic solvent Solvent bar microextraction Parabens Response surface methodology and central composite design HPLC-DAD Urine and plasma

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Oral delivery of ferroptosis inducers for effective treatment of hepatic fibrosis

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Nano research 2024年第8期17卷 7621-7630页

作者： Yinglan Yu Shunlong Zhang Yongfeng Xu Hao Shao Lei Luo College of pharmaceutical Sciences Southwest UniversityChongqing 400715China

Liver fibrosis is characterized by the excessive accumulation of extracellular matrix(ECM),which is primarily produced by activated hepatic stellate cells(HSCs).However,effective therapies for hepatic fibrosis are currently *** is a promising anti-fibrotic drug candidate,but its clinical application is hindered by limited ***,we present a novel oral delivery platform that enhances the HSCs uptake of artesunate and induces potent *** platform is vitamin Adecorated nanoparticles encapsulated with *** multifunctional ligand vitamin A interacts with retinol-binding proteins that are highly expressed on the intestinal epithelium to promote transcytosis,highly expressed on the surface of HSCs but lowly expressed in normal *** oral administration,this oral delivery platform enhances transepithelial transport in the intestine,improves drug accumulation in the liver,and continuously increases HSCs uptake of *** drug release in HSCs,artesunate depletes glutathione peroxidase 4 and glutathione,effectively initiating *** vivo experiments demonstrate that this strategy induces pronounced ferroptosis,efficiently relieving liver *** work provides a proof-ofconcept demonstration that an oral delivery strategy for ferroptosis inducers may be beneficial for liver fibrosis treatment.

关键词： liver fibrosis hepatic stellate cells oral delivery intestinal epithelium ferroptosis

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Microstructure and properties of coarse-grained WC-10Co cemented carbides with different carbon contents during heat treatments

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Rare Metals 2024年第4期43卷 1786-1792页

作者： Yuan-Feng Xie Xing-Cheng Xie Zhong-Wu Li Rui-Jun Cao Zhong-Kun Lin Qing Li Chen-Guang Lin Powder Metallurgy and Special Materials research department General Research Institute for Nonferrous MetalsBeijing100088China

The effects of cryogenic treatment(CT)and tempering-cryogenic treatment(TCT)on the microstructure and properties of coarse-grained WC-10Co cemented carbides with different carbon contents were *** binder phase,WC mean grain sizes,W solubility in the binder,relative magnetic s aturation,densities,hardness,wear resistance and second phase precipitation of cemented carbides with different heat treatments were *** results show that there are significant changes of microstructure and properties in the samples with CT and TCT,especially due to the precipitation of metastable nanoparticles W_(x)Co_(y)C_(z) in the binder during the heat treatments of CT and *** the simultaneous combination of microstructure and nanoparticle-reinforced binder,a dramatically improved combination of hardness and wear resistance of the samples after TCT has been achieved.

关键词： Cryogenic treatment Tempering Coarsegrained cemented carbide Carbon content Nanoparticlereinforced binder

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Sodium cholesterol sulfate mediated mitoxantrone prodrug electrostatic nanocomplexes: achieving the therapeutic efficacy and safety of mitoxantrone

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Science China Chemistry 2024年

作者： Erwei Zhao Lingxiao Li Jingyi Zhang Yaqiao Li Rong Chai Bowen Zhang Jialin Xing Minglong Huang Lurong Zhang Xiaohui Pu Zhonggui He Bingjun Sun department of Pharmaceutics Wuya College of Innovation Shenyang Pharmaceutical University department of Bioengineering Graduate School of Engineering The University of Tokyo Peking Union pharmaceutical Factory Ltd. State Key Laboratory of Antiviral Drugs School of Pharmacy Henan University Joint International research Laboratory of Intelligent Drug Delivery Systems Ministry of Education Shenyang Pharmaceutical University

Forming electrostatic nanocomplexes(ENCs) with counter-ions can improve the delivery efficiency of chemotherapy ***, water-soluble chemotherapy drugs like mitoxantrone(MTO), have limited affinity for counter-ions, posing challenges in the creation of stable ENCs. Herein, MTO was connected to fatty alcohols of varying chain lengths(C8, C12, C16) via disulfide bonds, forming hydrophobic prodrugs. We found that conjugating MTO to fatty alcohols significantly improved its affinity for the counter-ion sodium cholesterol sulfate(SCS). Among the designed prodrugs, conjugated to fatty alcohols with longer carbon chain lengths exhibited heightened affinity for SCS, resulting in the formation of more stable ENCs. However,extending the carbon chain also slowed the rate of drug release. Overall, compared with MTO solution, these ENCs demonstrated comparable therapeutic efficacy while causing minimal damage to healthy tissues, especially for MTO-SS-C16 ENCs. Our research provides new insights for constructing stable and safe ENCs for hydrophilic drugs like MTO.

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A review of structural modification and biological activities of oleanolic acid

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Chinese Journal of Natural Medicines 2024年第1期22卷 15-30页

作者： YANG Huali DENG Minghui JIA Hongwei ZHANG Kaicheng LIU Yang CHENG Maosheng XIAO Wei State Key Laboratory of New-tech for Chinese Medicine pharmaceutical Process Jiangsu Kanion Pharmaceutical Co.Ltd.Lianyungang 222001China Key Laboratory of Structure-Based Drug Design&Discovery of Ministry of Education School of Pharmaceutical EngineeringShenyang Pharmaceutical UniversityShenyang 110016China

Oleanolic acid(OA),a pentacyclic triterpenoid,exhibits a broad spectrum of biological activities,including antitumor,antiviral,antibacterial,anti-inflammatory,hepatoprotective,hypoglycemic,and hypolipidemic *** its initial isolation and identification,numerous studies have reported on the structural modifications and pharmacological activities of OA and its *** this,there has been a dearth of comprehensive reviews in the past two decades,leading to challenges in subsequent research on *** on the main biological activities of OA,this paper comprehensively summarized the modification strategies and structureactivity relationships(SARs)of OA and its derivatives to provide valuable reference for future investigations into OA.

关键词： Oleanolic acid Derivatives Pentacyclic triterpenoid Structural modification Biological activities

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Author correction to“Immune-awakening Saccharomyces-inspired nanocarrier for oral target delivery to lymph and tumors”[Acta Pharmaceutica Sinica B 12(2022)4501-4518]

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Acta Pharmaceutica Sinica B 2024年第3期14卷 1478-1482页

作者： Yuling Mao Xiudan Wang Caishun Chen Qinfu Zhao Yanfeng Liu Jinghai Zhang Siling Wang department of Pharmaceutics School of PharmacyShenyang Pharmaceutical University103 Wenhua RoadShenyang110016China department of Biomedical Engineering School of Medical DevicesShenyang Pharmaceutical University103 Wenhua RoadShenyang110016China School of Life Science and Bio-pharmaceutics Shenyang Pharmaceutical University103 Wenhua RoadShenyang110016China

The authors regret that there is an error in the article Fig.9D1 due to the mistake of copying and pasting in the process of assembling figures and negligence in the proofreading,and also a mislabled error in the supp... 详细信息

关键词： correction supporting proof

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Seismic control of multi-degrees-of-freedom structures by vertical mass isolation method using MR dampers

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Earthquake Engineering and Engineering Vibration 2024年第2期23卷 503-510页

作者： Mohamad Shahrokh Abdi Masoud Nekooei Mohammad-Ali Jafari department of Civil Engineering Marivan BranchIslamic Azad UniversityMarivan ***Iran department of Civil Engineering Science and Research BranchIslamic Azad UniversityTehran ***Iran Structural department of Transmission and Distribution research Center Niroo Research Institute(NRI)Tehran ***Iran

Vertical mass isolation(VMI)is one of the novel methods for the seismic control of *** this method,the entire structure is assumed to consist of two mass and stiffness subsystems,and an isolated layer is located among *** this study,the magnetorheological damper in three modes:passive-off,passive-on,and semi-active mode with variable voltage between zero and 9 volts was used as an isolated layer between two ***-degrees-of-freedom structures with 5,10,and 15 floors in two dimensions were examined under 11 pairs of near field *** each level,the displacement of MR dampers was taken into *** responses of maximum displacement,maximum inter-story drift,and maximum base shear in controlled and uncontrolled buildings were compared to assess the suggested approach for seismic control of the *** to the results,the semi-active control method can reduce the response by more than 12%compared to the uncontrolled mode in terms of maximum displacement of the mass subsystem of the *** method can reduce more than 16%and 20%of the responses compared to the uncontrolled mode in terms of maximum inter-story drift and base shear of the structure,respectively.

关键词： seismic control vertical mass isolation base shear magnetorheological damper semi-active control

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