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Acta Pharmaceutica Sinica B 2020年第7期10卷 1294-1308页

作者： Yahui Huang Shuqiang Chen Shanchao Wu Guoqiang Dong Chunquan Sheng Department of Medicinal Chemistry School of PharmacySecond Military Medical UniversityShanghai 200433China School of Pharmaceutical Sciences Zhengzhou UniversityZhengzhou 450001China

A great challenge in multi-targetingdrug discovery is to identify drug-like lead compounds with therapeutic advantages over single target inhibitors and drug combinations.Inspired by our previous efforts in designing antitumor evodiamine derivatives,herein selective histone deacetylase 1(HDAC1)and topoisomerase 2(TOP2)dual inhibitors were successfully identified,which showed potent in vitro and in vivo antitumor potency.Particularly,compound 30 a was orally active and possessed excellent in vivo antitumor activity in the HCT116 xenograft model(TGI=75.2%,150 mg/kg,p.o.)without significant toxicity,which was more potent than HDAC inhibitor vorinostat,TOP inhibitor evodiamine and their combination.Taken together,this study highlights the therapeutic advantages of evodiamine-based HDAC1/TOP2 dual inhibitors and provides valuable leads for the development of novel multi-targeting antitumor agents.

关键词： evodiamine Histone deacetylase Topoisomerase Dual inhibitors Antitumor activity

evodiamine inhibits high-fat diet-induced colitis-associated cancer in mice through regulating the gut microbiota

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Journal of Integrative Medicine 2021年第1期19卷 56-65页

作者： Li-qing Zhu Li Zhang Jia Zhang Guo-lin Chang Gang Liu Dan-dan Yu Xiao-min Yu Mi-sheng Zhao Bin Ye Department of Pathogenic Biology Chongqing Medical UniversityChongqing 400016China Research Center for Molecular Medicine and TumorChongqing Medical UniversityChongqing 400016China Department of Clinical LaboratoryThe First Affiliated Hospital of Wenzhou Medical UniversityWenzhou 325023Zhejiang ProvinceChina Department of PathophysiologyChongqing Medical UniversityChongqing 400016China Department of Clinical LaboratoryWenzhou People’s HospitalWenzhou 325023Zhejiang ProvinceChina Department of EmergencyUniversity-Town Hospital of Chongqing Medical UniversityChongqing 401331China

Objective:High-fat diet is one of the main risk factors that disrupt the balance of gut microbiota,which eventually will induce colorectal cancer(CRC).evodiamine(EVO)is a wildly used multifunctional traditional Chinese medicine extract.In this study,we investigated the role of gut microbiota in high-fat dietpropelled CRC and the potential of EVO for CRC chemoprevention.Methods:Gut microbiota,serum D-lactic acid and endotoxin from 38 patients with colon cancer and 18 healthy subjects were detected by quantitative real-time polymerase chain reaction and enzyme-linked immunosorbent assay(ELISA).In addition,body mass index,phospho-signal transducer and activator of transcription 3(p-STAT3)expression in cancer tissues and paracancerous tissues were detected by immunohistochemistry.A mouse intestinal inflammatory tumor model was established by azomethane/sodium dextran sulfate,followed by treatment with EVO and 5-aminosalicylic acid(ASA).Gut microbiota and inflammatory factors were detected by quantitative polymerase chain reaction,while serum D-lactic acid and endotoxin were detected by ELISA.Furthermore,cell proliferation,cell apoptosis,and interleukin(IL)-6/STAT3/P65 pathway were evaluated by 5-ethynyl-20-deoxyuridine,terminal-deoxynucleotidyl transferase-mediated nick-end labeling,and Western blot assays.Results:In patients with colon cancer,the numbers of Enterococcus faecalis and Escherichia coli were increased,while those of Bifidobacterium,Campylobacter and Lactobacillus were decreased.Serum endotoxin and D-lactic acid levels and p-STAT3 levels were significantly increased.In the mouse model,both EVO and ASA inhibited tumor formation,decreased the proliferation of tumor cells,and induced apoptosis of tumor cells.Compared with the control group,the numbers of E.faecalis and E.coli were decreased,while Bifidobacterium,Campylobacter and Lactobacillus numbers were increased.In the EVO group,serum endotoxin and D-lactic acid levels and inflammatory factors were significantly decreased.Further,the IL6/STAT3/P65 signa

关键词： evodiamine Gut microbiota Colitis-associated cancer Signal transducer and activator of transcription 3

evodiamine Inhibits Angiotensin Ⅱ-Induced Rat Cardiomyocyte Hypertrophy

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Chinese Journal of Integrative Medicine 2018年第5期24卷 359-365页

作者： HE Na GONG Qi-hai ZHANG Feng ZHANG Jing-yi LIN Shu-xian HOU Hua-hua WU Qin SUN An-sheng Key Laboratory of Basic Pharmacology of Guizhou Departmentof Pharmacology Zunyi Medical College Zunyi GuizhouProvince (563099) China

Objective: To investigate the effects of evodiamine(Evo), a component of evodiaminedia rutaecarpa(Juss.) Benth, on cardiomyocyte hypertrophy induced by angiotensin Ⅱ(Ang Ⅱ) and further explore the potential mechanisms. Methods: Cardiomyocytes from neonatal Sprague Dawley rats were isolated and characterized, and then the cadiomyocyte cultures were randomly divided into control, model(Ang Ⅱ 0.1 μmol/L), and Evo(0.03, 0.3, 3 μmol/L) groups. The cardiomyocyte surface area, protein level, intracellular free calcium([Ca]i) concentration, activity of nitric oxide synthase(NOS) and content of nitric oxide(NO) were measured, respectively. The m RNA expressions of atrial natriuretic factor(ANF), calcineurin(CaN), extracellular signal-regulated kinase-2(ERK-2), and endothelial nitric oxide synthase(e NOS) of cardiomyocytes were analyzed by real-time reverse transcriptionpolymerase chain reaction. The protein expressions of calcineurin catalytic subunit(CnA) and mitogen-activated protein kinase phosphatase-1(MKP-1) were detected by Western blot analysis. Results: Compared with the control group, Ang Ⅱ induced cardiomyocytes hypertrophy, as evidenced by increased cardiomyocyte surface area, protein content, and ANF m RNA expression; increased intracellular free calcium([Ca]i) concentration and expressions of CaN m RNA, CnA protein, and ERK-2 m RNA, but decreased MKP-1 protein expression(P<0.05 or P<0.01). Compared with Ang Ⅱ, Evo(0.3, 3 μmol/L) significantly attenuated Ang Ⅱ-induced cardiomyocyte hypertrophy, decreased the [Ca]i concentration and expressions of CaN m RNA, CnA protein, and ERK-2 m RNA, but increased MKP-1 protein expression(P<0.05 or P<0.01). Most interestingly, Evo increased the NOS activity and NO production, and upregulated the e NOS m RNA expression(P<0.05). Conclusion: Evo significantly attenuated Ang Ⅱ-induced cardiomyocyte hypertrophy, and this effect was partly due to promotion of NO production, reduction of [Ca]i concentration, and inhibition of CaN and ERK-2 signal transduction pathways.

关键词： evodiamine cardiomyocyte hypertrophy angiotensin Ⅱ calcineurin extracellular signal regulated kinase-2 nitric oxide

Peroxidase-mimicking evodiamine/indocyanine green nanoliposomes for multimodal imaging-guided theranostics for oral squamous cell carcinoma

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Bioactive Materials 2021年第7期6卷 2144-2157页

作者： Zheng Wei Huihui Zou Gongyuan Liu Chuanhui Song Chuanchao Tang Sheng Chen Guorong Zhang Jianchuan Ran Yufeng Wang Xiteng Yin Yu Cai Wei Han Department of Oral and Maxillofacial Surgery Nanjing Stomatological HospitalMedical School of Nanjing University30 Zhongyang Road210008NanjingChina Clinical Research Institute Zhejiang Provincial People’s HospitalPeople’s Hospital of Hangzhou Medical CollegeNo.158 Shangtang RoadHangzhou310014Zhejiang ProvinceChina Pediatric Dentistry Nanjing Stomatology HospitalMedical School of Nanjing UniversityNo 30 Zhongyang RoadNanjing210008China Department of Orthodontics Nanjing Stomatological HospitalMedical School of Nanjing UniversityNo 30 Zhongyang RoadNanjing210008China Central Laboratory of Stomatology Nanjing Stomatological HospitalMedical School of Nanjing University30 Zhongyang Road210008NanjingChina Department of Oral Pathology Nanjing Stomatological HospitalMedical School of Nanjing UniversityNanjingChina Department of Chemistry City University of Hong Kong83 Tat Chee AvenueHong Kong SARChina

Here,evodiamine(EVO)and the photosensitizer indocyanine green(ICG)were integrated into a liposomal nanoplatform for noninvasive diagnostic imaging and combinatorial therapy against oral squamous cell carcinoma(OSCC).EVO,as an active component extracted from traditional Chinese medicine,not only functioned as an antitumor chemotherapeutic agent but was also capable of 68Ga-chelation,thus working as a contrast agent for positron emission tomography/computed tomography(PET/CT)imaging.Moreover,EVO could exhibit peroxidase-like catalytic activity,converting endogenous tumor H2O2 into cytotoxic reactive oxygen species(ROS),enabling Chemo catalytic therapy beyond the well-known chemotherapy effect of EVO.As proven by in vitro and in vivo experiments,guided by optical imaging and PET/CT imaging,we show that the theragnostic liposomes have a significant inhibiting effect on in situ tongue tumor through photodynamic therapy combined with chemodynamic chemotherapy.

关键词： Oral squamous cell carcinoma evodiamine Peroxidase-mimicking Trimodal antitumor therapy

Theoretical development and mechanism research of evodiamine's antitumor effect

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Medical Theory and Hypothesis 2022年第3期5卷 21-26页

作者： Li-Ping Liu Tian-Xiang Lei De-Liang Li Feng Li Ping-Xiang Li Ke-Li Ge Cheng-Shan Ma Medicine College Qingdao UniversityQingdao 266023China Linyi People's Hospital Linyi 276000China Affiliated Hospital of Qingdao University Qingdao 266023China Zibo Bashan Wanjie Hospital Zibo 255213China Shandong Provincial Hospital Affiliated to Shandong First Medical University Jinan 250000China

evodiamine(EVO),one of the bioactive components of traditional Chinese medicine,has been widely concerned for its anti-tumor properties in recent years.In this review,the anti-tumor mechanism of EVO was reviewed from the aspects of inducing tumor cell apoptosis(internal pathway,external pathway and other pathways),inducing autophagy,inhibiting tumor stem cells,inhibiting cell proliferation and migration,inhibiting peripheral vascular proliferation,and recent research progress of EVO anti-tumor drugs.

关键词： evodiamine anti-tumor apoptosis autophagy cancer stem cells

Regulatory effects of evodiamine on glucose metabolism-related factors in CT26 colorectal carcinoma-bearing mice

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Precision Medicine Research 2022年第4期4卷 12-17页

作者： Jiang-Yue Yu Kui Chen Ruo-Qin Zhao Li-Qun Wang Chao Gong Shen-Zhou Huang Yun-Juan Zheng Pei-Wen Zhu Xin-Ran Song Fang-Hua Wu General Surgery Fujian Medical University Affiliated Fuzhou First HospitalFuzhou 350009China College of Forestry Shanxi Agricultural UniversityJinzhong 030801China School of Bioengineering Tianjin Modern Vocational Technology CollegeTianjin 300350China

Objective:To investigate the therapeutic effect of evodiamine(EVO)on the expression of hexokinase(HK),lactate dehydrogenase A(LDHA),and pyruvate kinase M(PKM),key enzymes of glycolysis,in the tumor-bearing mice after modeling mouse colon cancer cells(CT26).Methods:A tumor-bearing mouse model was generated by administering axillary injection of CT26 and intraperitoneally injecting different doses of EVO.The therapeutic effects of EVO on CT26 tumor-bearing mice were evaluated by measuring the thymus and spleen indices,tumor volume,tumor suppression rate,and other related indicators in the tumor tissues of mice in each group after the administration of EVO,in addition,histopathological changes in the tumor tissues of the mice in the groups were studied by hematoxylin and eosin staining.The expression levels of HK,LDHA,and PKM in the tumor tissues of each group of mice were measured by performing Western blot to investigate the mechanism of EVO treatment in CT26 tumor-bearing mice.Results:EVO inhibited the growth of tumors in CT26-bearing mice and enhanced their splenic and thymic indices.Western blot results showed that EVO reduced the expression levels of HK,LDHA,and PKM proteins in the tumor tissues of CT26 tumor-bearing mice.Conclusion:EVO has a therapeutic effect on CT26 tumor-bearing mice,and its mechanism of action may be related to the low expression of key enzymes HK,LDHA and PKM of glycolysis in tumor tissues.

关键词： evodiamine mouse colon cancer cells tumor-bearing mice glycolysis hexokinase lactate dehydrogenase A pyruvate kinase M

Combination of evodiamine with Berberine Reveals a Regulatory Effect on the Phenotypic Transition of Colon Epithelial Cells Induced by CCD-18Co

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Chinese Medical Sciences Journal 2020年第3期35卷 195-206页

作者： Chao Huang Keming Xiang Bingjun Liang Weixuan Huang Fanjun Zhang Yuwan Shao Xiulian Wang Haosheng Liu Weizeng Shen Department of Traditional Chinese Medicine Affiliated Bao’an Hospital of ShenzhenSouthern Medical UniversityShenzhen 518100China Community Healthy Service Center Shenzhen Bao’an Traditional Chinese Medicine Hospital GroupShenzhen 518100China

Objective Transdifferentiation exists between stromal cells or between stromal cells and cancer cells.evodiamine and berberine are predominant pharmacological components of Zuojin pill,a prescription of Traditional Chinese Medicine,playing crucial functions in remolding of tumor microenvironment.This study aimed to explore the effect of combination of evodiamine with berberine(cBerEvo)on the phenotypic transition of colon epithelial cells induced by tumor-associated fibroblasts,as well as the involved mechanisms.Methods Human normal colon epithelial cell line HCoEpiC cells were treated with the prepared conditioned medium of CCD-18 Co,a human colon myofibroblast line,to induce epithelial-mesenchymal transition.Phase contrast microscope was used to observe the morphological changes.Epithelial-mesenchymal transition markers including E-cadherin,vimentin and alpha-smooth muscle actin(α-SMA)were observed with immunofluorescence microscopy.Migration was assessed by wound healing assay.Western blotting was used to detect the expressions of E-cadherin,vimentin,α-SMA,Snail,ZEB1 and Smads.Results In contrast to the control,the tumor-associated fibroblasts-like CCD-18 Co cells induced downregulation of E-cadherin and up-regulation of vimentin,α-SMA,Snail and ZEB1(P<0.05),and promoted migration of HCoEpiCs(P<0.05),with over expression of Smads including Smad2,p-Smad2,Smad3,p-Smad3 and Smad4(P<0.05),which were abolished by a transforming growth factor-β(TGF-β)receptor inhibitor LY364947 and by cBerEvo in a concentration dependent manner.In addition,cBerEvo-inhibited ratios of p-Smad2/Smad2 and p-Smad3/Smad3 were also dose dependent.Conclusion The above results suggest that cBerEvo can regulate the differentiation of colon epithelial cells induced by CCD-18 Co through suppressing activity of TGF-β/Smads signaling pathway.

关键词： evodiamine berberine tumor microenvironment epithelial-mesenchymal transition TGF-βsignaling

Ethanol extract from radix of Actinidia chinensis and evodiamine regulated CCR7 expression in SW480 cells

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中国现代医学杂志 2011年第3期21卷 336-347页

作者： Yan-qin Zhou Zhi-qun Zhou Hui-yin Li Ting-ting Guo Guo Chen Ying He Li-qun Kang Yu-xiang Chen School of Pharmacy Central South University Changsha Hunan 410013 P.R. China

Objective To identify anti-tumor effects of the ethanol extract from radix of Actinidia chinensis(EERAC) and evodiamine(Evo) on colon carcinoma SW480 cells,and investigate their regulation of CCR7 expression and the underlying mechanism in colon carcinoma.Methods Radix of Actinidia chinensis was extracted by ethanol.MTT assay and growth curve method were used to detect the inhibition of SW480 cells after being treated with EERAC and Evo.RT-PCT and Western-blot were used to detect the CCR7 expression regulated by EERAC and Evo at the level of protein and mRNA respectively in SW480 cells.Results MTT results showed that EERAC and Evo significantly inhibited the growth of SW480 cells with obvious time-and dose-dependent effect.The 50% inhibitory concentration(IC50) of EERAC was 9.14 mg/mL,while the IC50 of Evo was 2.11 μg/mL.RT-PCR results showed that the expression of CCR7 mRNA in EERAC and Evo group was 29.99% and 18.03% respectively,which was obviously lower than that(56.27%) in control group.Western-blot proved that the expression of CCR7 protein in EERAC and Evo group was 29.03% and 15.28% respectively,which was also significantly reduced when compared to that of 42.48% in control group.Conclusion Ethanol extract from radix of Actinidiae chinensis and evodiamine could effectively inhibit proliferation and growth of SW480 cells,significantly down-regulate the functional expression of CCR7,and thereby suppress the tumor metastasis.

关键词： EERAC evodiamine tumor metastasis CCR7

A new strategy of enhancing absorptivity and safety for evodiamine: polyamidoamine derivatives modified by polyethylene glycol chain

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Traditional Medicine Research 2021年第2期6卷 100-110页

作者： Yao-Chun Gao Yuan-Sheng Lao Meng-Xue Zhang Nan Li Chen-Yang Wu Zheng-Qi Dong Institute of Medicinal Plant Development Chinese Academy of Medical SciencesPeking Union Medical CollegeBeijing 100193China Key Laboratory of Bioactive Substances and Resources Utilization of Chinese Herbal Medicine Ministry of EducationChinese Academy of Medical SciencesPeking Union Medical CollegeBeijing 100094China Key Laboratory of New Drug Discovery Based on Classic Chinese Medicine Prescription Beijing 100700China

Background:Traditional Chinese medicine involves complex ingredients and mixtures of ingredients that often exhibit low bioavailability,and excipients are often lacking to increase the absorption-enhancing effects.This study modified the generation 4 polyamidoamine dendrimer with polyethylene glycol of different molecular weights(5000,2000,1000)to form a series of polyamidoamine-co-polyethylene glycol(PAMAM-co-PEG)as a novel class of oral absorption enhancers.evodiamine,the major alkaloid found in the traditional Chinese medicine Wu Zhu Yu(Fructus Evodiae),was used as a model drug to verify the absorption-enhancing effects and the safety of this alkaloid.Methods:This study utilized the solubility determination method documented in the Pharmacopoeia of the People’s Republic of China(2015 edition)and the D0 values recommended in the US FDA guidelines to comprehensively evaluate the solubility of evodiamine.The permeability of evodiamine was assessed using the apparent permeability coefficient in experiments based on in vitro cell models.Multiple aspects of the biological safety of PAMAM-co-PEG were explored using the MTT assay,LDH assay,and total protein release of the rat intestinal tract.Moreover,the absorption-enhancing effects of PAMAM-co-PEG at different molecular weights on evodiamine were verified via the use of in vitro cell models and in vivo intestinal loop circulation experiments with rats.Results:evodiamine exhibited low solubility and permeability and was classified into class IV compounds using the biopharmaceutical classification system.PAMAM-co-PEG 2000 demonstrated improvement in the biosafety and absorption-enhancement effect of evodiamine at a specific concentration.This study showed that 0.05%(w/v)of PAMAM-co-PEG 2000 increased the cumulative penetration of evodiamine via cell transport by 1.32 times,and 0.10%(w/v)of PAMAM-co-PEG 2000 increased the area under curve value of evodiamine by 1.31 times.Conclusion:evodiamine possesses low solubility and permeability and leads to poor oral bioavailabi

关键词： Polyamidoamine dendrimers Polyethylene glycol Intestinal absorption enhancer Bioavailability evodiamine Fructus Evodiae

evodiamine improves lipid profile in high-fat diet-fed mice by facilitating reverse cholesterol transport

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中国药理学与毒理学杂志 2019年第10期 926-926页

作者： WANG Li-mei HOU Xing-ming DU Yi-xuan JIANG Kun TAN Lin-hai LUAN Da-zhi XU Chao-fan HU Ding-xin WANG Ke-wei Department of Pharmacology Qingdao University School of Pharmacy

OBJECTIVE Reverse cholesterol transport（RCT） is a pivotal pathway involved in transporting excess cholesterol from peripheral tissues to the liver for excretion in the bile and eventual y the feces. In the present study we identified the naturally occurring alkaloid evodiamine as alipid-lowing inducer by facilitating RCT in highfat diet（HFD）-fed mice. METHODS Hep G2 cells were first exposed to 0.6 m M FFA（palmitic acid/oleic acid, 1:2）for 24 h to induce the liversteatosis before treated with or without evodiamine foran additional 24 h. Atorvastatin was used as apositive control. Intracellular lipid deposition was analyzed by Oil Red O staining. Male ICR mice were fed HFD initially for 4 weeks to induce hyperlipidemia. After induction of hyperlipidemia, evodiamine was intragastrically administered in the dose of 10 mg · kg;per day for 4 weeks to the mice. The levels of triglyceride（TG）, total cholesterol（TC）, high-density lipoprotein cholesterol（HDL-C） and low-density lipoprotein cholesterol（LDL-C）in the serum were determinedto evaluate the metabolic lipid profiles in the HFD-fed mice. Hematoxylin and eosin（H&E） staining was performed for fat accumulation examination. Western blotting and quantitative real time polymerase chain reaction（q RT-PCR） were used to assess the expression of proteins and m RNAs correlated with RCT in the liver and small intestine, including ATP-binding cassette transporter A1（ABCA1）, ABCG1, ABCG5,ABCG8, scavenger receptor class B type 1（SR-B1） and Niemann-Pick type C1 Like 1（NPC1L1）. RESULTS Oil Red O staining revealed that evodiamine markedly attenuated hepatic fat accumulation caused by FFA in HepG2 cells. In HFD-fed mice, evodiamine significantly reduced serum TG, TC and LDL-C but not HDL-C. Besides, evodiamine significantly decreased hepatic lipid accumulation revealed by H&E staining. Moreover, evodiamine increased ABCG1 expression in the liver and raised NPC1L1 expression in the small intestine. CONCLUSION evodiamine improves lipid metabolic profile in HFD-fed mice by increasing exp

关键词： evodiamine reverse cholesterol transport ABCG1 NPC1L1