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aloe emodin promotes mucosal healing by modifying the differentiation fate of enteroendocrine cells via regulating cellular free fatty acid sensitivity

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Acta Pharmaceutica Sinica B 2024年第9期14卷 3964-3982页

作者： Weilian Bao Jiaren Lyu Guize Feng Linfeng Guo Dian Zhao Keyuan You Yang Liu Haidong Li Peng Du Daofeng Chen Xiaoyan Shen Department of Pharmacology&the Key Laboratory of Smart Drug Delivery Ministry of Education School of PharmacyFudan UniversityShanghai 201210China Department of Natural Medicine School of PharmacyFudan UniversityShanghai 201210China Department of Colorectal and Anal Surgery Xinhua HospitalShanghai Jiao Tong University School of MedicineShanghai 200092China Shanghai Colorectal Cancer Research Center Shanghai 200092China

The proper differentiation and reorganization of the intestinal epithelial cell population is critical to mucosal regeneration post *** retaining cells(LRCs)expressing SRY-box transcription factor 9(SOX9)promote epithelial repair by replenishing LGR5 t intestinal stem cells(ISCs).While,LRCs are also considered precursor cells for enteroendocrine cells(EECs)which exacerbate mucosal damage in inflammatory bowel disease(IBD).The factors that determine LRC-EEC differentiation and the effect of intervening in LRC-EEC differentiation on IBD remain *** this study,we investigated the effects of a natural anthraquinone called aloe emodin(derived from the Chinese herb rhubarb)on mucosal healing in IBD *** findings demonstrated that aloe emodin effectively interfered with the differentiation to EECs and preserved a higher number of SOX9t LRCs,thereby promoting mucosal ***,we discovered that aloe emodin acted as an antagonist of free fatty acid receptors(FFAR1),suppressing the FFAR1-mediated Gbg/serine/threonine-protein kinase(AKT)pathway and promoting the translocation of forkhead box protein O1(FOXO1)into the nucleus,ultimately resulting in the intervention of differentiation *** findings reveal the effect of free fatty acid accessibility on EEC differentiation and introduce a strategy for promoting mucosal healing in IBD by regulating the FFAR1/AKT/FOXO1 signaling pathway.

关键词： LRCs ISCs EECs IBD SOX9 aloe emodin FFAR1 FOXO1

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Antibacterial and Alkali-responsive Cationic Waterborne Polyurethane Based on Modification of aloe emodin

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Chemical Research in Chinese Universities 2023年第2期39卷 266-275页

作者： XIONG Xiaoyan LI Xiaobin ZHU Zifan ZHANG Ending SHI Jun LU Mangeng Guangzhou Institute of Chemistry Chinese Academy of SciencesGuangzhou510650P.R.China University of Chinese Academy of Sciences Beijing100049China Guangdong Provincial Key Laboratory of Organic Polymer Materials for Electronics Guangzhou510650China New Materials Research Institute of CASCHEM(Chongqing)Co. Ltd.Chongqing400714China CASH GCC Shaoguan Research Institute of Advanced Materials Shaoguan512440China

Cationic water-based polyurethane(CWPU)was synthesized to explore aloe-emodin modifies to obtain CWPU materials with better comprehensive *** provides a simple way to synthesize antibacterial waterborne polyurethane,which is to introduce the end-blocking group of herbal extracts into the *** contains synergistic antibacterial effect of herbal antibacterial and quaternary ammonium ion on Escherichia *** makes the material resist the erosion of bacterial,and increase the service life of *** the pH value of the environment changes,the UV absorbance of the aloe-emodin modified cationic water-based polyurethane(AE-CWPU)also ***,within a certain detection range,AE-CWPU has great applications in the field of smart response *** modified thermodynamic properties have been improved,and the mechanical properties basically maintained the maximum stress,and the elongation at break was reduced.

关键词： Waterborne polyurethane aloe emodin Quaternary ammonium salt Antibacterial pH response

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Selective Solid-phase Extraction of aloe emodin from aloe by Molecularly Imprinted Polymers

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Chemical Research in Chinese Universities 2013年第4期29卷 663-666页

作者： TIAN Ming-lei LEE Yu-ri PARK Dong-wha ROW Kyung-ho College of Chemistry and Environmental Engineering Yangtze University Jingzhou 434023 P R. China Department of Chemical Engineering Regional Innovation Center for Environmental Technology of Thermal Plasma Inha University Ineheon 402-751 Korea

The extraction and separation of aloe emodin were optimized via selective molecularly imprinted solid-phase extraction. Molecularly imprinted polymer was prepared from the functional monomer, methacrylic acid and a mixture of ethanol/dodecanol（90/10, volume ratio） as porogen. It overcomes the common problems of imprin- ting biological polar compounds and shows high selectivity compared favorably with those of non-imprinted polymer and commercially available C18 and silica cartridges in similar aloe emodin tests. Good linearity was obtained be- tween 0.002 and 2.5 mg/mL（r2=0.998） with relative standard deviations below 3.3%.

关键词： aloe emodin Molecularly imprinted polymer Solid-phase extraction High performance liquid chromato- graphy

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Isopropanol-conjugated aloe emodin Carbazole as Artificial Probes for Enterococcus faecalis DNA

Isopropanol-conjugated Aloe Emodin Carbazole as Artificial P...

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中国化学会·第十六届全国有机合成化学学术研讨会

作者：梁馨元 Mohammad Fawad Ansari Cheng-He Zhou 西南大学 School of Chemistry and Chemical Engineering Southwest University Jamia Millia Islamia

Structural characteristics of aloe emodin endow natural superior resources with good interactions on DNA via multiple modes,thus aloe emodin derivatives exhibit extensive potential in medicinal *** the basis of our previous work in carbazoles with a library of potent candidate probes for biomolecular processes,herein our interest is to combine aloe emodin scaffold with carbazole via isopropanol bridge to develop a series of new potential hybrid candidates of artificial probes for sensitive bacterial DNA in clinic.

关键词： aloe emodin carbazole antibacterial probe DNA

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Unique Azolyl Acylhydrazonyl Hybridization of aloe emodins to Access Potential Antibacterial Agents

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Chinese Journal of Chemistry 2024年第15期42卷 1741-1758页

作者： Yi-Xin Wang Zhao Deng Aisha Bibi Bo Fang Cheng-He Zhou Institute of Bioorganic&Medicinal Chemistry Key Laboratory of Applied Chemistry of Chongqing MunicipalitySchool of Chemistry and Chemical EngineeringSouthwest UniversityChongqing 400715China College of Pharmacy National&Local Joint Engineering Research Center of Targeted and Innovative TherapeuticsChongqing Key Laboratory of Kinase Modulators as Innovative MedicineChongqing University of Arts and SciencesChongqing 402160China

A type of unique azole-hybridized acylhydrazonyl aloe emodins(AAEs)were developed as new antibacterial agents for combating bacterial *** target AAEs showed strong antibacterial activities,especially,tetrazolylthioether AAE 27a exhibited broad antibacterial spectrum with 16-256 folds and 8-64 folds more active antibacterial efficacy than the reference drugs aloe emodin and norfloxacin,*** AAE 27a also gave low hemolysis and cytotoxicity,as well as favorable *** mechanism explorations revealed that tetrazolylthioether AAE 27a could cause bacterial membrane depolarization and damage the cell membrane,resulting in nucleic acid ***,compound 27a could intercalate into DNA to impede its replication and form supramolecular 27a-DNA gyrase complex to disturb the function of DNA *** findings would provide valuable insights for the further exploration of azolyl acylhydrazonyl aloe emodins as new potential antibacterial candidates.

关键词： aloe emodin Hydrazone Heterocycle Antibacterial Membrane damage

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