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In vitro inhibitory effects of plumbagin,the promising antimalarial candidate,on human cytochrome P450 enzymes

Asian Pacific Journal of Tropical Medicine 2015年第11期8卷 894-898页

作者： Wiriyaporn Sumsakul Wanna Chaijaroenkul Kesara Na-Bangchang Graduate Program in Biomedical Sciences.Faculty of Allied Health Sciences Thammasat University Center of Excellence in Pharmacology and Molecular Biology Graduate Program in Bioclinical SciencesChulabhorn International College of MedicineThammasat University

Objective:To investigate the propensity of plumbagin to inhibit the three isoforms of human cytochrome P450(CYP),ie.,CYP1A2,CYP2C19,and CYP3A4 using human liver microsomes in ***:Inhibitory effects of plumbagin on the three human CYP isoformswere investigated using pooled human liver *** O-deethylation,omeprazole hydroxylation and nifedipine oxidation were used as selective substrates for CYP1A2,CYP2C19 and CYP3A4 activities,*** of paracetamol,5-hydroxyomeprazole,and oxidized nifedipine were determined in microsomal incubation mixture using high performance liquid ***:plumbagin showed significantinhibitory effects on all CYP *** with the most potent activity on CYP2C19-mediated omeprazole *** IC50(concentration that inhibits enzyme activity by 50%) values of plumbagin and nootkatone(selective inhibitor) for CYP2C19 were(0.78±0.01) and(27.31±0.66) μM,*** inhibitory activities on CYP1 A2-mediated phenacetin O-deethylation and CYP3A4-mediated nifedipine oxidation were *** IC_(50) values of plumbagin and-naphthoflavone(selective inhibitor) for CYP1A2 were(1.39±0.01) and(0.02±.0.36) μM,*** corresponding IC_(50) values of plumbagin and ketoconazole(selective inhibitor) for CYP3A4 were(2.37+0.10) and(0.18±0.06) μM,***:Clinical relevance of the interference of human drug metabolizing enzymes should be aware of for further development scheme of plumbagin as antimalarial drug when used in combination with other antimalarial drugs which are metabolized by these CYP isoforms.

关键词： Metabolism Human liver microsomes plumbagin Cytoch

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Self-assembled metal-organic frameworks nanocrystals synthesis and application for plumbagin drug delivery in acute lung injury therapy

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Chinese Chemical Letters 2022年第1期33卷 324-327页

作者： Yang Wang Qing Li Mengsheng Deng Kuijun Chen Jianmin Wang State Key Laboratory of Trauma Burns and Combined InjuryDepartment of Surgical ResearchDaping HospitalArmy Medical UniversityChongqing 400042China School of Chemistry and Chemical Engineering Yangzhou UniversityYangzhou 225002China

Metal-organic frameworks(MOFs)have recently allured a variety of concern in the fields of ***,exploring their biomedical applications is still a relatively new *** this work,zeolite imidazole skeleton-8(ZIF-8)was reported for the first time as a drug carrier for the treatment of lung *** ZIF-8 nanoparticles encapsulating plumbagin(PLB)are achieved by a facile physical adsorption *** electron microscopy(SEM),powder X-ray diffraction(PXRD)and UV–vis absorption spectrum were conducted to investigate the physical properties of ZIF-8 and PLB@*** animal model,the collagen fibers deposition produced by severe lung injury is significantly *** secretion of inflammatory factor TGF-βand IL-6 were efficiently dropped by the combination of plumbagin and *** the same time,the expressions of collagen I,α-SMA and TNF-αwere also *** strategy puts forth a promising blueprint in the application of MOF materials,especially in biomedical fields.

关键词： ZIF-8 plumbagin Drug delivery Lung injury

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Suppressive Effects of plumbagin on Invasion and Migration of Breast Cancer Cells via the Inhibition of STAT3 Signaling and Down-regulation of Inflammatory Cytokine Expressions

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Bone Research 2013年第4期1卷 362-370页

作者： Wei Yan Bing Tu Yun-yun Liu Ting-yu Wang Han Qiao Zan-jing Zhai Hao-wei Li Ting-ting Tang Shanghai Key Laboratory of Orthopaedic Implants Department of Orthopaedic SurgeryShanghai Ninth People's HospitalShanghai Jiao Tong University School of Medicine Wendeng Zhenggu Hospital of Shandong Province Department of Gynecology and Obstetrics Wendeng Center Hospital of Weihai City Department of Pharmacy Shanghai Ninth People's HospitalShanghai Jiao Tong University School of Medicine

Objective： The aim of this study was to investigate the effects of plumbagin （PL）, a naphthoquinone derived from the medicinal plant plumbago zeylanica, on the invasion and migration of human breast cancer cells. Methods： Human breast cancer MDA-MB-231SArfp cells were treated with different concentrations of plum- bagin for 24 h. The effects of plumbagin on the migration and invasion were observed by a transwell method. The expressions of IL-1α, IL-1β, IL-6, IL-8, TGF-β, TNFα, MMP-2 and MMP-9 mRNA in MDA-MB-231SArfp cells were detected using Real-Time PCR. MDA-MB-231SArfp cells were treated with plumbagin at different concentrations for 45 minutes. The activation of STAT3 was detected by western blot. Following this analysis, STAT3 in MDA-MB-231SArfp cells was knocked out using specific siRNA, mRNA levels of IL-1α, TGF-β, MMP-2 and MMP-9 were then detected. Consequently, MDA-MB-231SArfp cells were injected intracardially into BALB/c nude mice to construct a breast cancer bone metastatic model. The mice were injected intra- peritoneally with plumbagin. Non-invasive in vivo monitoring, X-ray imaging and histological staining were performed to investigate the effects of plumbagin on the invasion and migration of breast cancer cells in vivo. Results： The in vitro results showed that plumbagin could suppress the migration and invasion of breast cancer cells and down-regulate mRNA expressions of IL-1α TGF-β, MMP-2 and MMP-9. Western blotting demonstrated that plumbagin inhibited the activation of STAT3 signaling in MDA-MB-231SArfp cells. The inactivation of STAT3 was found to have an inhibitory effect on the expressions of IL-1α, TGF-β, MMP-2 and MMP-9. In vivo studies showed that plumbagin inhibited the metastasis of breast cancer cells and decreased osteolytic bone metastases, as well as the secretion of MMP-2 and MMP-9 by tumor cells at metastatic lesions. Conclusions： plumbagin can suppress the invasion and migration of breast cancer cells via the inhibition of STAT3

关键词： plumbagin breast cancer invasion migration

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Inhibitory activities of plumbagin on cell migration and invasion and inducing activity on cholangiocarcinoma cell apoptosis

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Asian Pacific Journal of Tropical Medicine 2018年第7期11卷 430-435页

作者： Luxsana Panrit Tullayakorn Plengsuriyakarn Pongsakorn Martviset Kesara Na-Bangchang Drug Discovery and Development Center Thammasat University Center of Excellence in Molecular Biology and Pharmacology of Malaria and Cholangiocarcinoma Chulabhorn International College of MedicineThammasat University Graduate Program in Bioclinical Sciences Chulabhorn International College of Medicine Thammasat University Faculty of Medical Technology Rangsit University

Objective: To investigate the cytotoxic, apoptotic and inhibitory activities on cell migration and invasion of plumbagin in the human cholangiocarcinoma(CCA) cell line(CL-6) in comparison with human embryonic fibroblast cell line(OUMS). Methods: Cytotoxicity activity was evaluated using MTT assay. Inhibitory effect on cell migration and invasion were investigated using label-free real-time cell analysis and QCM ECMatrix cell invasion chamber, respectively. Apoptotic activity was evaluated using flow cytometry and Cell Event? Caspase 3/7 assay. Results: Based on results of the cytotoxicity test in CL-6 cells, 50% inhibitory concentration(IC_(50), Mean±SD) values of plumbagin and the standard drug 5-fluorouracil were(24.00±3.33) and(1 036.00±137.77) μmol/L, respectively. The corresponding values for OUMS cells were(57.00±5.23) and(2 147.00±209.98) μmol/L, respectively. The selectivity index was 2.28. The inhibitory activities of plumbagin on cell migration and invasion were potent and concentration-dependent with IC_(50) of 25.0 μmol/L and complete inhibition at 25.0 μmol/L. Flow cytometry analysis showed that plumbagin at 12.5 μmol/L(half IC_(50)) induced CL-6 cell apoptosis(43.24% of control) through stimulation of caspase 3/7 activities. Complete cell apoptosis was observed at 12.5 μmol/L. Conclusions: The cytotoxic activity and inhibition of migration and invasion including apoptosis induction in the human CCA cell line(CL-6) suggest that plumbagin could be a promising candidate for CCA chemotherapeutics. However, its relatively low selective cytotoxic effect on CCA cells is a major concern.

关键词： Cholangiocarcinoma plumbagin Cancer migration Cancer invasion Apoptosis

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plumbagin Enhances TRAIL-mediated Apoptosis through Up-regulation of Death Receptor in Human Melanoma A375 Cells

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Journal of Huazhong University of Science and Technology(Medical Sciences) 2010年第4期30卷 458-463页

作者：李家文沈琴彭锐陈嵘袆蒋苹李艳秋张丽卢静静 Department of Dermatology Union Hospital Tongji Medical College Huazhong University of Science and Technology Oversea Education School Hubei University of Chinese Medicine

Tumor necrosis factor-related apoptosis-inducing ligand (TRAIL) is a promising anti-cancer agent. However, emergence of drug resistance limits its potential use. plumbagin is a natural quinonoid compound isolated from plant. In this study, induced apoptosis effect of the combined treatment with plumbagin and TRAIL on human melanoma A375 cell line was examined and possible mechanism was investigated. The cells were divided into four groups: control group, plumbagin group (plumbagin, 5 or 10 μmol/L), TRAIL group (TRAIL, 30 ng/mL) and plumbagin+TRAIL group (combined treatment group). The apoptosis, and the expression of DR4 and DR5 were detected by flow cytometry. The activities of caspase-8 and caspase-3 were determined by colorimetric assay. The results showed that the apoptosis rate was 8.3% in TRAIL group, 10.35%–16.94% in plumbagin group and 52.39%–65.39% in combined treatment group, respectively, with the difference being significant between combined treatment group and plumbagin or TRAIL group (Pplumbagin alone could markedly up-regulate DR5 mRNA and protein expression, and slightly increase DR4 mRNA and protein expression. Treatment of human melanoma A375 cells with plumbagin resulted in the activation of Caspase-3, but not Caspase-8. These results suggest that plumbagin might be useful for TRAIL-based treatment for melanoma.

关键词： plumbagin TRAIL DR5 DR4 apoptosis melanoma

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plumbagin ameliorates immune inflammatory diseases

Plumbagin ameliorates immune inflammatory diseases

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第九届全国免疫学学术大会

作者： Kai Zhang Huan Zhang Zhenyi Xue Yan Li Wen Li Zhihui Zhang Yurong Da Zhi Yao Rongxin Zhang Research Center of Basic Medical Science Department of ImmunologyBasic Medical CollegeKey Laboratory of Educational Ministry of ChinaTianjin Medical University

Background:plumbagin(PL,5-hydroxy-2-methyl-1,4-naphthoquinone)is an herbal compound derived from medicinal plants of the Droseraceae,plumbaginaceae,Dioncophyllaceae,and Ancistrocladaceae *** have shown that PL exerts immunomodulatory activity and may be a novel drug candidate for immune-related disease *** sclerosis(MS)is a chronic human autoimmune disease characterized by inflammatory demyelination and subsequent axon injury in the central nervous system(CNS).Experimental autoimmune encephalomyelitis(EAE),an animal model of MS,is widely used to study the mechanisms of autoimmune inflammation in *** fibrosis is one kind of common chronic liver disease,which is caused by variety of pathogenic factors include inflammatory *** isn’t anindependent disease,but always company with chronic *** macrophages were recruited and the increase of exudate macrophages contributed inflammatory cells infiltration around the ***:In this study,we investigated the therapeutic effect of plumbagin in inflammatory diseases,including MS and liver ***,we also explored its potential mechanism of PL in ***:Two animal models of inflammatory disease,EAE and chronic liver fibrosis model,were used to investigate the effect of plumbagin in immune *** were observed and tissues,lumber spinal cords from EAE mice and livers from chronic liver fibrosis mice,were acquired and stained to assay the therapeutic effect of ***,the effect of plumbagin on dendritic cells(DCs)and macrophages were explored to find its potential mechanism of ***:PL could ameliorate the clinical symptoms of EAE,including central nervous system(CNS)inflammation and *** could reverse TAA-induced collagen deposition,inflammatory cell infiltration,and liver functional abnormality in chronic liver fibrosis *** differentiation,maturation,and function of human monocyte-deriv

关键词： plumbagin dendritic cell inflammation experimental autoimmune encephalomyelitis liver fibrosis

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plumbagin protects liver against thioacetamide-induced fulminant hepatic failure and chronic liver fibrosis by target on macrophages and hepatic stellate cells

Plumbagin protects liver against thioacetamide-induced fulmi...

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第十届全国免疫学学术大会

作者： Zimu Zhang Huan Zhang Huafeng Wang Dan Wang Xixi Cheng Zhenyi Xue Yan Li Lijuan Zhang Yurong Da Zhi Yao Rongxin Zhang Tianjin Medical University

Aims:In this study,we investigated the effect of plumbagin on liver protection in acute and chronic damage induced by thioacetamide(TAA).Methods:We construct the animal model of liver *** describe the hepatoprotection mechanism of the plumbagin,we evaluated the effects of plumbagin on mice liver damage by the aspects of inflammatory infiltration,hepatocytes protection,and *** also studied the probable molecular mechanism of plumbagin using RAW264.7 and LX-2 cell in ***:Histochemistry staining showed that plumbagin not only inhabit inflammatory infiltration by preventing the recruitment of macrophages but also have the function of protecting hepatocytes from damage in acute and chronic *** liver fibrosis model,extracellular matrix such as COL-I/III was degraded via suppressing LX-2 activation and proliferation,induced apoptosis with treatment of *** in vitro promoted AMPK phosphorylation to compete transcriptional coactivator p300 against with p ***,plumbagin attenuated NFκB,Stat3,and Akt/m TOR signaling pathways thereby regulating LX-2 survival,activation,and proliferation in *** also found that NFκB pathway of RAW264.7 was suppressed by plumbagin in ***:plumbagin appears to be a powerful candidate who can protect the liver from acute and chronic damage by targeting on macrophages and hepatic stellate cells.

关键词： plumbagin Fulminant hepatic failure Liver fibrosis LX-2 Inflammation

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plumbagin对人高转移大细胞肺癌细胞系抑制作用的研究

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中华肿瘤防治杂志 2012年第4期19卷 268-271,275页

作者：于涛刘刚祖玲玲王伟强李永文天津医科大学总医院肿瘤内科天津300052 天津医科大学总医院普通外科天津300052 天津医科大学总医院肺癌研究所天津300052

目的:研究plumbagin对人高转移大细胞肺癌L9981细胞系的体外抗肿瘤作用,并初步探讨其机制。方法:不同浓度plumbagin处理L9981细胞系,采用MTT法观察对肿瘤细胞增殖的影响,确定药物IC50;采用流式细胞术检测对细胞系诱导凋亡的作用;采用Boy... 详细信息

目的:研究plumbagin对人高转移大细胞肺癌L9981细胞系的体外抗肿瘤作用,并初步探讨其机制。方法:不同浓度plumbagin处理L9981细胞系,采用MTT法观察对肿瘤细胞增殖的影响,确定药物IC50;采用流式细胞术检测对细胞系诱导凋亡的作用;采用Boyden小室侵袭实验检测对体外侵袭力的抑制作用。以IC50plumbagin处理L9981细胞系,于处理后6、24、48h收获细胞,以实时定量PCR方法检测Bcl-2、Bax、VEGF和CYCD1等基因的mRNA表达变化。结果:MTT法显示,plumbagin明显抑制L9981细胞系的细胞增殖(F=39.535,P=0.000),IC50为9.0μmol/L;Plum-bagin对L9981细胞系具有体外诱导凋亡作用(F=23.671,P=0.000),且明显抑制其体外侵袭能力。Bodyen小室侵袭实验检测对照组和plumbagin组平均穿膜细胞数分别为228.17±55.12和9.83±3.87,差异有统计学意义,t=13.598,P=0.000。plumbagin处理L9981细胞系后不同时间点检测结果显示,Bcl-2、VEGF和CYCD1基因表达均逐渐降低,bax基因表达逐渐增高,组间差异有统计学意义(F=13.520,P=0.000;F=15.778,P=0.000;F=10.163,P=0.000;F=18.635,P=0.000)。结论:plumbagin对大细胞肺癌L9981细胞系具有明确的抗肿瘤作用。plumbagin通过多种作用机制发挥其抑癌作用,显示了其成为抗大细胞肺癌药物的前景。

关键词：肺肿瘤 plumbagin 增殖凋亡侵袭

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plumbagin Inhibits Inflammatory Response and Bone Loss in Experimental Chronic Peridontitis Rats

Plumbagin Inhibits Inflammatory Response and Bone Loss in Ex...

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中华口腔医学会第六次全国口腔药学学术会议

作者： Tingyu Wang Xinyi Zheng Han Qiao Fang Gu Yunwu Li Feihua Wu Department of Pharmacy Shanghai Ninth People's Hospital Shanghai JiaoTong University School of Medicine College of Stomatology Shanghai JiaoTong University School of Medicine Shanghai Key Laboratory of Orthopaedic Implant Department of Orthopaedics Surgery Shanghai Ninth People's Hospital Shanghai Jiao Tong University School of Medicine

Aim Chronic periodontitis(CP) is one of the most common oral diseases which causes alveolar bone absorption and tooth loss in adults. In this study,we aimed to remedy chronic periodontitis with plumbagin(PL), one widely-investigated pharmacologic drug derived from traditional Chinese medical herb. Methods Experimental chronic peridontitis is established by ligate and Porphyromonas gingivalis(Pg) stimulation in Sprague-Dawley rats(SD rats). The rats were injected with PL(2, 4, and 6 mg·kg·d, ip) for 4 weeks to evaluate the anti-inflammation property of PL. Results Results indicated that PL inhibits CP progression by down regulating the expressions of TNF-α, IL-1β and ***, PL administration decelerated bone destruction in the rat with CP,evidenced by the aveolar bone loss(ABL) and H&E staining results. Conclusion With the given data, conclusion could be made that PL suppressed CP by down regulating the expressions of TNF-α, IL-1β and IL-6 and by inhibiting the bone loss.

关键词： plumbagin chronic periodontitis tumor necrosis factor alpha interleukin 1β interleukin 6 bone loss

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The antitumorigenic effect of plumbagin through inhibition the function and activation of myeloid-derived suppressor cells in pancreatic cancer

The antitumorigenic effect of plumbagin through inhibition t...

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第十一届全国免疫学学术大会

作者： Qi Zhang Guan Zhiyu Miao Guolin Cheng Yingnan Yao Zhi Rongxin Zhang Tianjin medical university Weifang medical university

Objective:Pancreatic cancer is one of the most malignant *** is urgent to discover new drugs and treatment ***(PLB)has shown potent antitumor effects in preclinical ***,the functional role of PLB in tumor immunity remained *** derived suppressor cells(MDSCs)are important cell mediated tumor immune *** this study,we explored the role of PLB in regulating the differentiation of

关键词： Pancreatic cancer plumbagin MDSCs Tumor immune micro-environment immune escape

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