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Acta Pharmaceutica Sinica B 2024年第2期14卷 517-532页

作者： Shuang Xiang Xiaoyun Lu International Cooperative laboratory of Traditional chinese medicine modernization and Innovative Drug Discovery of chinese Ministry of Education(MOE) Guangdong Provincial Key Laboratory of New Drug Design and EvaluationGuangzhou City Key Laboratory of Precision Chemical Drug DevelopmentSchool of PharmacyJinan UniversityGuangzhou 510632China

Neurotrophic receptor kinase(NTRK) fusions are actionable oncogenic drivers of multiple pediatric and adult solid tumors,and tropomyosin receptor kinase(TRK) has been considered as an attractive therapeutic target for "pan-cancer" harboring these ***,two generations TRK inhibitors have been *** representative second-generation inhibitors selitrectinib and repotrectinib were designed to overcome clinic acquired resistance of the first-generation inhibitors larotrectinib or entrectinib resulted from solvent-front and gatekeeper on-target ***,xDFG(TRKAG667C/A/S,homologous TRKCG696C/A/S) and some double mutations still confer resistance to selitrectinib and repotrectinib,and overcoming these resistances represents a major unmet clinical *** this review,we summarize the acquired resistance mechanism of the first-and second-generation TRK inhibitors,and firstly put forward the emerging selective type Ⅱ TRK inhibitors to overcome xDFG mutations mediated ***,we concluded our perspectives on new challenges and future directions in this field.

关键词： NTRK fusions TRK kinase Clinical resistance xDFG mutations Selective type II inhibitors

Design and optimization of a greener sinomenine hydrochloride preparation process considering variations among different batches of the medicinal herb

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chinese Journal of Chemical Engineering 2024年第7期71卷 77-90页

作者： Dandan Ren Jiale Xie Tianle Chen Haibin Qu Xingchu Gong Pharmaceutical Informatics Institute College of Pharmaceutical SciencesZhejiang UniversityHangzhou 310058China National key laboratory of chinese medicine modernization Zhejiang UniversityHangzhou 310058China Jinhua Institute of Zhejiang University Jinhua 321016China

The current methods used to industrially produce sinomenine hydrochloride involve several issues,including high solvent toxicity,long process flow,and low atomic utilization efficiency,and the greenness scores of the processes are below 65 *** solve these problems,a new process using anisole as the extractant was *** exhibits high selectivity for sinomenine and can be connected to the subsequent water-washing *** alkalization of the medicinal material,heating extraction,water washing,and acidification crystallization were carried *** process was modeled and *** design space was *** recommended operating ranges for the critical process parameters were 3.0–4.0 h for alkalization time,60.0–80.0℃ for extraction temperature,2.0–3.0(volume ratio)for washing solution amount,and 2.0–2.4 mol·L^(-1) for hydrochloric acid *** new process shows good robustness because different batches of medicinal materials did not greatly impact crystal purity or sinomenine transfer *** sinomenine transfer rate was about 20%higher than that of industrial *** greenness score increased to 90 points since the novel process proposed in this research solves the problems of long process flow,high solvent toxicity,and poor atomic economy,better aligning with the concept of green chemistry.

关键词： Sinomenine hydrochloride Process optimization Anisole

Nuciferine alleviates collagen-induced arthritic in rats by inhibiting the proliferation and invasion of human arthritis-derived fibroblast-like synoviocytes and rectifying Th17/Treg imbalance

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chinese Journal of Natural medicines 2024年第4期22卷 341-355页

作者： WANG Hao GENG Xiaolong AI Fangbin YU Zhilun ZHANG Yan ZHANG Beibei LV Cheng GAO Ruiyang YUE Bei DOU Wei The MOE key laboratory of Standardization of chinese medicines Shanghai Key Laboratory of Compound Chinese Medicinesand the SATCM Key Laboratory of New Resources and Quality Evaluation of Chinese MedicineInstitute of Chinese Materia MedicaSchool of Traditional Chinese Materia MedicaShanghai University of Traditional Chinese Medicine(SHUTCM)Shanghai 201203China

Rheumatoid arthritis(RA)is a chronic autoimmune disorder marked by persistent synovial inflammation and joint degradation,posing challenges in the development of effective ***,an alkaloid found in lotus leaf,has shown promising anti-inflammatory and anti-tumor effects,yet its efficacy in RA treatment remains *** study investigated the antiproliferative effects of nuciferine on the MH7A cell line,a human RA-derived fibroblast-like synoviocyte,revealing its ability to inhibit cell proliferation,promote apoptosis,induce apoptosis,and cause G1/S phase ***,nuciferine significantly reduced the migration and invasion capabilities of MH7A *** therapeutic potential of nuciferine was further evaluated in a collagen-induced arthritis(CIA)rat model,where it markedly alleviated joint swelling,synovial hyperplasia,cartilage injury,and inflammatory *** also improved collagen-induced bone erosion,decreased pro-inflammatory cytokines and serum immunoglobulins(IgG,IgG1,IgG2a),and restored the balance between T helper(Th)17 and regulatory T cells in the spleen of CIA *** results indicate that nuciferine may offer therapeutic advantages for RA by decreasing the proliferation and invasiveness of FLS cells and correcting the Th17/Treg cell imbalance in CIA rats.

关键词： Rheumatoid arthritis Collagen-induced arthritis Fibroblast-like synoviocyte Immune imbalance Nuciferine

Early Growth Response Gene-1 Deficiency Interrupts TGFβ1 Signaling Activation and Aggravates Neurodegeneration in Experimental Autoimmune Encephalomyelitis Mice

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Neuroscience Bulletin 2024年第3期40卷 283-292页

作者： Yunyi Lan Xinyan Han Fei Huang Hailian Shi Hui Wu Liu Yang Zhibi Hu Xiaojun Wu Shanghai key laboratory of Compound chinese medicines The Ministry of Education Key Laboratory for Standardization of Chinese MedicinesThe State Administration of TCM Key Laboratory for New Resources and Quality Evaluation of Chinese MedicineInstitute of Chinese Materia MedicaShanghai University of Traditional Chinese MedicineShanghai201203China Central laboratory Shuguang Hospital Affiliated to Shanghai University of Traditional Chinese MedicineShanghai200021China

Early growth response protein 1(Egr-1)triggers the transcription of many genes involved in cell growth,differentiation,synaptic plasticity,and ***,its mechanism in neuronal survival and degeneration is still poorly *** study demonstrated that Egr-1 was down-regulated at mRNA and protein levels in the central nervous system(CNS)of experimental autoimmune encephalomyelitis(EAE)***-1 knockout exacerbated EAE progression in mice,as shown by increased disease severity and incidence;it also aggravated neuronal apoptosis,which was associated with weakened activation of the BDNF/TGFβ1/MAPK/Akt signaling pathways in the CNS of EAE ***,Egr-1 siRNA promoted apoptosis but mitigated the activation of BDNF/TGFβ1/MAPK/Akt signaling in SH-SY5Y *** results revealed that Egr-1 is a crucial regulator of neuronal survival in EAE by regulating TGFβ1-mediated signaling activation,implicating the important role of Egr-1 in the pathogenesis of multiple sclerosis as a potential novel therapy target.

关键词： Early growth response protein 1 Transforming growth factor-beta 1 Multiple sclerosis Experimental autoimmune encephalomyelitis Neurodegeneration

Antibacterial Activity of Plants in Cirsium:A Comprehensive Review

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chinese Journal of Integrative medicine 2024年第9期30卷 835-841页

作者： TANG Xiao-meng XIE Ming-xia GOU Jun-li CHEN Liang TIAN Jin-long ZHANG Xia LU You-yuan WANG Han-qing College of Pharmacy Ningxia Medical UniversityYinchuanNingxia750004China College of Traditional chinese medicine Hunan University of Chinese MedicineChangsha410007China General Hospital of Ningxia Medical University YinchuanNingxia750004China Ningxia Regional Characteristic Traditional chinese medicine Collaborative Innovation Center Co-constructed by the Province and Ministry Ningxia Engineering and Technology Research Center for Modernization of Regional Characteristic Traditional Chinese MedicineNingxia Medical UniversityYinchuan750004China key laboratory of Ningxia Minority medicine modernization Ministry of EducationYinchuan750004China

As ethnic medicine,the whole grass of plants in Cirsium was used as *** review focuses on the antimicrobial activity of plants in Cirsium,including antimicrobial components,against different types of microbes and bacteriostatic *** results showed that the main antimicrobial activity components in Cirsium plants were flavonoids,triterpenoids and phenolic acids,and the antimicrobial ability varied according to the species and the content of *** them,phenolic acids showed a strong antibacterial ability against Acinetobacter baumannii,Pseudomonas aeruginosa,and Enterococcus *** antibacterial mechanisms include:(1)damaging the cell membrane,cell walls,mitochondria and nucleus of bacteria;(2)inhibiting the synthesis of proteins and nucleic acids;(3)suppressing the synthesis of enzymes for tricarboxylic acid cycle pathways and glycolysis,and then killing the bacteria via inhibition of energy ***,most research results on antimicrobial activity of Cirsium plants are reported based on in vitro *** evidence from clinical data and comprehensive evaluation are needed.

关键词： Cirsium traditional use antibacterial active components bacteriostatic activity bacteriostatic mechanism chinese medicine

Potential role of the protein interactome in translating TCM theory and clinical practice into modern biomedical knowledge

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chinese Journal of Natural medicines 2024年第5期22卷 385-386页

作者： CHEN Qian FAN Xiaohui Pharmaceutical Informatics Institute College of Pharmaceutical SciencesZhejiang UniversityHangzhou 310058China National key laboratory of chinese medicine modernization Innovation Center of Yangtze River DeltaZhejiang UniversityJiaxing 314100China

With the awarding of the 2015 Nobel Prize in Physiology or medicine to chinese pharmacologist Tu Youyou,and the significant contributions of traditional chinese medicine(TCM)for coronavirus disease 2019(COVID-19),TCM has garnered increasing attention and interest *** advanced research progress has been made in the efficacy research,mechanism elucidation and target prediction of TCM in recent years[1].

关键词： Protein interactome Traditional chinese medicine Therapeutic effectiveness

Electroacupuncture ameliorates blood-brain barrier disruption after ischemic stroke through histone acetylation regulation at the matrix metalloproteinase 9 and tissue inhibitor of metalloproteinase 2 genes

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Journal of Traditional chinese medicine 2024年第4期44卷 734-744页

作者： CHEN Yonglin OUYANG Ling MENG Lingling WU Bufan PENG Rou LIU Sitong HOU Dan WANG Yaling JING Xinyue LU Shengfeng FU Shuping key laboratory of Acupuncture and medicine Research of Ministry of Education Nanjing University of Chinese MedicineNanjing 210023China

OBJECTIVE:To explore whether the regulation of matrix metalloproteinase 9(MMP-9)/tissue inhibitors of MMPs(TIMPs)gene expression through histone acetylation is a possible mechanism by which electroacupuncture(EA)protects blood-brain barrier(BBB)integrity in a middle cerebral artery occlusion(MCAO)rat ***:Male Sprague-Dawley rats were divided into four groups:the sham group,the MCAO group,the MCAO+EA(MEA)group,and the MCAO+EA+HAT inhibitor(HATi)*** MCAO model was generated by blocking the middle cerebral *** was applied to Baihui(GV20).Samples were collected 1 or 3 d after *** function scores and Evans blue extravasation were employed to evaluate the poststroke *** effect of EA on MMP-9/TIMPs gene expression was assessed by real-time fluorescence quantitative polymerase chain reaction(RT-qPCR)and chromatin immunoprecipitation(ChIP).RESULTS:Our results showed that EA treatment prominently improved neurological function and ameliorated BBB *** RT-qPCR assay showed that EA reduced the expression of MMP-9 and promoted TIMP-2 mRNA expression,but HATi reversed these effects of *** addition,ChIP results revealed that EA decreased the enrichment of H3K9ace/H3K27ace at MMP-9 promoters and notably stimulated the recruitment of H3K9ace/H3K27ace at TIMP-2 ***:EA treatment at Baihui(GV20)regulates the transcription of MMP-9 and TIMP-2 through histone acetylation modification in the acute stage of stroke,which preserves the structural integrity of the BBB in MCAO *** findings suggested that the histone acetylation-mediated transcriptional activity of target genes may be a crucial mechanism of EA treatment in stroke.

关键词： blood-brain barrier matrix metalloproteinase 9 tissue inhibitor of metalloproteinases electroacupuncture histone acetylation

Shexiang Tongxin Dropping Pill Promotes Angiogenesis through VEGF/eNOS Signaling Pathway on Diabetic Coronary Microcirculation Dysfunction

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chinese Journal of Integrative medicine 2024年第10期30卷 886-895页

作者： CUI Xin-yu LIU Tian-hua BAI Ya-li ZHANG Meng-di LI Guo-dong ZHANG Yu-ting YUAN Yue-ying ZHANG Ya-wen YU Li-shuang HAN Li-na WU Yan School of Traditional chinese medicine Beijing University of Chinese Medicine key laboratory of Traditional chinese medicine Syndrome and Formula Ministry of Education Beijing University of Chinese Medicine Beijing Research Institute of chinese medicine Beijing University of Chinese Medicine

Objective: To study the effect of Shexiang Tongxin Dropping Pill(STDP) on angiogenesis in diabetic cardiomyopathy mice with coronary microcirculation dysfunction(CMD). Methods: According to a random number table, 6 of 36 SPF male C57BL/6 mice were randomly selected as the control group, and the remaining 30 mice were injected with streptozotocin intraperitoneally to replicate the type 1 diabetes model. Mice successfully copied the diabetes model were randomly divided into the model group, STDP low-dose group [15 mg/(kg·d)], medium-dose group [30 mg/(kg·d)], high-dose group [60 mg/(kg·d)], and nicorandil group [15 mg/(kg·d)], 6 in each group. The drug was given by continuous gavage for 12 weeks. The cardiac function of mice in each group was detected at the end of the experiment, and coronary flow reserve(CFR) was detected by chest Doppler technique. Pathological changes of myocardium were observed by hematoxylin-eosin staining, collagen fiber deposition was detected by masson staining, the number of myocardial capillaries was detected by platelet endothelial cell adhesion molecule-1 staining, and the degree of myocardial hypertrophy was detected by wheat germ agglutinin staining. The expression of the vascular endothlial growth factor(VEGF)/endothelial nitric oxide synthase(eNOS) signaling pathway-related proteins in myocardial tissue was detected by Western blot. Results: Compared with the model group, medium-and high-dose STDP significantly increased the left ventricular ejection fraction and left ventricular fraction shortening(P<0.01), obviously repaired the disordered cardiac muscle structure, reduced myocardial fibrosis, reduced myocardial cell area, increased capillary density, and increased CFR level(all P<0.01). Western blot showed that high-dose STDP could significantly increase the expression of VEGF and promote the phosphorylation of vascular endothelial growth factor receptor 2, phosphoinositide 3-kinase, protein kinase B, and eNOS(P<0.05 or P<0.01). Co

关键词： Shexiang Tongxin Dropping Pill angiogenesis coronary microcirculation dysfunction diabetic cardiomyopathy type 1 diabetes

Protective Effect of Silibinin on Lipopolysaccharide-Induced Endotoxemia by Inhibiting Caspase-11-Dependent Cell Pyroptosis

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chinese Journal of Integrative medicine 2024年第10期30卷 917-926页

作者： OU Jin-ying LIU Shan-hong TANG Dong-kai SHI Ling-zhu YAN Li-jun HUANG Jing-yan ZOU Li-fang QUAN Jing-yu YOU Yan-ting CHEN Yu-yao YU Lin-zhong LU Zi-bin Third Level Research laboratory of State Administration of Traditional chinese medicine School of Traditional Chinese Medicine Southern Medical University Guangdong Provincial key laboratory of chinese medicine Pharmaceutics School of Traditional chinese medicine Southern Medical University

Objective: To explore the protective effect and the underlying mechanism of silibinin(SIB), one of the active compounds from Silybum marianum(L.) Gaertn in endotoxemia. Methods: Mouse peritoneal macrophage were isolated via intraperitoneally injection of BALB/c mice with thioglycolate medium. Cell viability was assessed using the cell counting kit-8, while cytotoxicity was determined through lactate dehydrogenase cytotoxicity assay. The protein expressions of interleukin(IL)-1α, IL-1β, and IL-18 were determined by enzyme-linked immunosorbent assay. Intracellular lipopolysaccharide(LPS) levels were measured by employing both the limulus amoebocyte lysate assay and flow cytometry. Additionally, proximity ligation assay was employed for the LPS and caspase-11 interaction. Mice were divided into 4 groups: the control, LPS, high-dose-SIB(100 mg/kg), and low-dose-SIB(100 mg/kg) groups(n=8). Zebrafish were divided into 4 groups: the control, LPS, high-dose-SIB(200 μmol/L), and low-dose-SIB(100 μmol/L) groups(n=30 for survival experiment and n=10 for gene expression analysis). The expression of caspase-11, gasdermin D(GSDMD), and N-GSDMD was determined by Western blot and the expressions of caspy2, gsdmeb, and IL-1β were detected using quantitative real-time PCR. Histopathological observation was performed through hematoxylineosin staining, and protein levels in bronchoalveolar lavage fluid were quantified using the bicinchoninicacid protein assay. Results: SIB noticeably decreased caspase-11 and GSDMD-mediated pyroptosis and suppressed the secretion of IL-1α, IL-1β, and IL-18 induced by LPS(P<0.05). Moreover, SIB inhibited the translocation of LPS into the cytoplasm and the binding of caspase-11 and intracellular LPS(P<0.05). SIB also attenuated the expression of caspase-11 and N-terminal fragments of GSDMD, inhibited the relative cytokines, prolonged the survival time, and up-regulated the survival rate in the endotoxemia models(P<0.05). Conclusions: SIB can inhibit pyrop

关键词： caspase-11 endotoxemia inflammation pyroptosis silibinin

Mapping out the reaction network of humin formation at the initial stage of fructose dehydration in water

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Green Energy & Environment 2024年第6期9卷 1016-1026页

作者： Xing Fu Yexin Hu Ping Hu Hui Li Shuguang Xu Liangfang Zhu Changwei Hu key laboratory of Green Chemistry and Technology Ministry of EducationCollege of ChemistrySichuan UniversityChengduSichuan610064China State key laboratory of Southwestern chinese medicine Resources Innovative Institute of Chinese Medicine and PharmacyChengdu University of Traditional Chinese MedicineChengduSichuan611137China

The formation of humins hampers the large-scale production of 5-hydroxymethylfurfural(HMF)in ***,a detailed reaction network of humin formation at the initial stage of fructose-to-HMF dehydration in water is delineated by combined experimental,spectroscopic,and theoretical *** bimolecular reaction pathways to build up soluble humins are *** is,the intermolecular etherification of β-furanose at room temperature initiates the C12 path,whereas the C-C cleavage of a-furanose at 130-150℃ leads to C11 path,and that of open-chain fructose at 180℃ to C11' *** successive intramolecular dehydrations and condensations of the as-formed bimolecular intermediates lead to three types of soluble *** show that the C12 path could be restrained by using HCl or AlCl_(3) catalyst,and both the C12 and C110 paths could be effectively inhibited by adding THF as a co-solvent or accelerating heating rate via microwave heating.

关键词： Carbohydrates 5-hydroxymethylfurfural Reaction network Soluble humins Tautomer