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Acta Pharmaceutica Sinica B 2024年第7期14卷 3266-3280页

作者： Wenfeng Li Shuming Chen Jing Lang Jing Luo Jiahui Chen Liping Zhang Zhijie Sun Deli Dong Department of Pharmacology China Pharmaceutical UniversityNanjing 210009China

The drugs extending healthspan in clinic have always been *** is an FDA-approved clinical antiprotozoal *** is rapidly metabolized to tizoxanide after absorption in *** previous studies find that nitazoxanide and its metabolite tizoxanide induce mild mitochondrial uncoupling and activate cellular AMPK,oral nitazoxanide protects against experimental hyperlipidemia,hepatic steatosis,and ***,we demonstrate that both nitazoxanide and tizoxanide extend the lifespan and healthspan of Caenorhabditis elegans through Akt/AMPK/sir 2.1/daf16 ***,both nitazoxanide and tizoxanide improve high glucose-induced shortening of *** *** has been a clinical drug with a good safety profile,we suggest that it is a novel anti-aging drug.

关键词： nitazoxanide Tizoxanide C.elegans Healthspan Lifespan AMPK Akt Mitochondrial uncoupling

Anthelmintics nitazoxanide protects against experimental hyperlipidemia and hepatic steatosis in hamsters and mice

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Acta Pharmaceutica Sinica B 2022年第3期12卷 1322-1338页

作者： Fengfeng Li Man Jiang Minghui Ma Xuyang Chen Yidan Zhang Yixin Zhang Yuanyuan Yu Yunfeng Cui Jiahui Chen Hui Zhao Zhijie Sun Deli Dong Department of Pharmacology(the State-Province Key Laboratories of Biomedicine-Pharmaceutics of China Key Laboratory of Cardiovascular ResearchMinistry of Education)College of PharmacyHarbin Medical UniversityHarbin 150086China Translational Medicine Research and Cooperation Center of Northern China Heilongjiang Academy of Medical SciencesHarbin Medical UniversityHarbin 150086China Department of Pharmacology China Pharmaceutical UniversityNanjing 211198China

Lipid metabolism disorders contribute to hyperlipidemia and hepatic *** is ideal to develop drugs simultaneous improving both hyperlipidemia and hepatic *** is an FDA-approved oral antiprotozoal drug with excellent pharmacokinetic and safety *** found that nitazoxanide and its metabolite tizoxanide induced mild mitochondrial uncoupling and subsequently activated AMPK in Hep G2 *** administration of nitazoxanide inhibited high-fat diet(HFD)-induced increases of liver weight,blood and liver lipids,and ameliorated HFD-induced renal lipid accumulation in *** significantly improved HFD-induced histopathologic changes of hamster *** the hamsters with pre-existing hyperlipidemia and hepatic steatosis,nitazoxanide also showed therapeutic *** administration of nitazoxanide improved HFD-induced hepatic steatosis in C57BL/6J mice and western diet(WD)-induced hepatic steatosis in Apoe-/-*** present study suggests that repurposing nitazoxanide as a drug for hyperlipidemia and hepatic steatosis treatment is promising.

关键词： nitazoxanide Tizoxanide Hyperlipidemia Hepatic steatosis AMPK Autophagy SQSTM1/P62 Mitochondrial uncoupling

Discovery of nitazoxanide-based derivatives as autophagy activators for the treatment of Alzheimer’s disease

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Acta Pharmaceutica Sinica B 2020年第4期10卷 646-666页

作者： Xiaokang Li Jian Lu Yixiang Xu Jiaying Wang Xiaoxia Qiu Lei Fan Baoli Li Wenwen Liu Fei Mao Jin Zhu Xu Shen Jian Li State Key Laboratory of Bioreactor Engineering Shanghai Key Laboratory of New Drug DesignSchool of PharmacyEast China University of Science and TechnologyShanghai 200237China School of Medicine and Life Sciences Nanjing University of Chinese MedicineNanjing 210023China Center for Drug Safety Evaluation and Research State Key Laboratory of Drug ResearchShanghai Institute of Materia MedicaChinese Academy of SciencesShanghai 201203China

Drug repurposing is an efficient strategy for new drug *** latest study found that nitazoxanide(NTZ),an approved anti-parasite drug,was an autophagy activator and could alleviate the symptom of Alzheimer’s disease(AD).In order to further improve the efficacy and discover new chemical entities,a series of NTZ-based derivatives were designed,synthesized,and evaluated as autophagy activator against *** compounds were screened by the inhibition of phosphorylation of p70S6K,which was the direct substrate of mammalian target of rapamycin(mTOR)and its phosphorylation level could reflect the mTOR-dependent autophagy *** these analogs,compound 22 exhibited excellent potency in promotingβ-amyloid(Aβ)clearance,inhibiting tau phosphorylation,as well as stimulating autophagy both in vitro and in ***’s more,22 could effectively improve the memory and cognitive impairments in APP/PS1 transgenic AD model *** results demonstrated that 22 was a potential candidate for the treatment of AD.

关键词： Alzheimer’s disease Autophagy nitazoxanide β-amyloid Tau protein

Introducing nitazoxanide as a promising alternative treatment for symptomatic to metronidazole-resistant giardiasis in clinical isolates

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Asian Pacific Journal of Tropical Medicine 2016年第9期9卷 866-871页

作者： Tahereh Mikaeili Galeh Abdolhassan Kazemi Mahmoud Mahami-Oskouei Behzad Baradaran Adel Spotin Seddigheh Sarafraz Majid Karamat Immunology Research Center Tabriz University of Medical Sciences Department of Parasitology and Mycology Faculty of MedicineTabriz University of Medical Sciences East Azerbaijan Province Health Center Tabriz Health Center

Objective:To identify the frequencies(F) of ferredoxin and nitroreductase mutations were identified on Iranian clinical isolates of Giardia lamblia in order to predict whether the nitazoxanide can be prescribed as suitable drug for symptomatic to metronidazoleresistant ***:Forty Giardia lamblia isolates as of 38 symptomatic and two metronidazole-resistant patients were collected from *** were extracted and amplified by targeting ferredoxin and Gl NR *** amplicons were directly sequenced to determine gene ***:The various amino acid substitutions(F:20%,Haplotype diversity:0.891,Tajima's D:-0.44013) were identified by analyzing ferredoxin gene in four symptomatic and two resistant ***,two haplotypes(F:5%,HD:0.345; Tajima's D:0.77815) characterized in metronidazole-resistant isolates of Gl NR,however,no point mutations was found in symptomatic ***:Non-synonymous mutations of ferredoxin oxidoreductase gene reduce translational regulatory protein's binding affinity which concludes reduction of ferredoxin expression and its *** leads to decrease in metronidazole drug delivery into the *** in these isolates may lead to their resistance to *** to low synonymous mutations of Gl NR demonstrates that nitazoxanide can be prescribed as promising alternative treatment for symptomatic to metronidazole-resistant giardiasis in Iranian clinical isolates.

关键词： Giardia lamblia Ferredoxin oxidoreductase Nitroreductase nitazoxanide Metronidazole

Voltammetric quantitation of nitazoxanide by glassy carbon electrode

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Journal of Pharmaceutical Analysis 2013年第6期3卷 452-455页

作者： Rajeev Jain Rajeev Kumar Yadav Jahangir Ahmad Rather School of Studies in Chemistry Jiwaji University

The present study reports voltammetric reduction of nitazoxanide in Britton-Robinson （B-R） buffer by cyclic and square-wave voltammetry at glassy carbon electrode. A versatile fully validated voltammetric method for quantitative determination of nitazoxanide in pharmaceutical formulation has been proposed. A squrewave peak current was linear over the nitazoxanide concentration in the range of 20-140 ~tg/mL. The limit of detection （LOD） and limit of quantification （LOQ） was calculated to be 5.23 la~/mL and 17.45 la~/mL, respectively.

关键词： nitazoxanide Squarewave voltammetry Glassy carbon electrode Pharmaceuticalformulation

Validated stability indicating methods for determination of nitazoxanide in presence of its degradation products

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Journal of Pharmaceutical Analysis 2012年第2期2卷 105-116页

作者： Nouruddin W.Ali Samah Sayed Abbas Hala El-Sayed Zaazaa Maha Mohamed Abdelrahman Mohamed Abdelkawy Analytical Chemistry Department Faculty of PharmacyBeni-Suef UniversityHussin El-Shafey StreetBeni-Suef CityEgypt Analytical Chemistry Department Faculty of PharmacyCairo UniversityKasr El-Aini Street11562CairoEgypt

Three sensitive,selective and reproducible stability-indicating methods are presented for determination of nitazoxanide (NTZ),a new anti-protozoal drug,in presence of its degradation *** A utilizes the first derivative of ratio spectra spectrophotometry by measurement of the amplitude at 364.4 nm using one of the degradation products as a *** B is a chemometric-assisted spectrophotometry,where principal component regression (PCR) and partial least squares (PLS) were *** two approaches were successfully applied to quantify NTZ in presence of degradation products using the information included in the absorption spectra in the range 260-360 *** C is based on the separation of NTZ from its degradation products followed by densitometric measurement of the bands at 254 *** separation was carried out on silica gel 60F 254,using chloroform-methanol-ammonia solution-glacial acetic acid (95:5:1:1 by volume,pH=5.80) as a developing *** methods are suitable as stability-indicating methods for the determination of NTZ in presence of its degradation products either in bulk powder or in pharmaceutical *** analysis of the results has been carried out revealing high accuracy and good precision.

关键词： nitazoxanide Degradation Derivative spectrophotometry Chemometrics TLC-densitometry Stability-indicating methods

Treatment of chronic viral hepatitis with nitazoxanide and second generation thiazolides

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World Journal of Gastroenterology 2009年第15期15卷 1805-1808页

作者： Emmet B Keeffe Jean-Franois Rossignol The Romark Institute for Medical Research TampaFlorida and SausalitoCaliforniaUnited States and the Division of Gastroenterology and HepatologyDepartment of MedicineStanford University Medical Center The Romark Institute for Medical Research TampaFloridaUnited States and the Division of Gastroenterology and HepatologyDepartment of MedicineStanford University Medical Center

nitazoxanide,the first thiazolide,was originally developed for the treatment of Cryptosporidium *** recently,antiviral activity of nitazoxanide against hepatitis B virus(HBV)and hepatitis C virus was recognized in in vitro *** basic studies led to phaseⅡclinical trials that demonstrated the safety and efficacy of nitazoxanide in combination with peginterferon,with or without ribavirin,in the treatment of chronic hepatitis C genotype *** sustained virologic response rate was 79%and 80%in two studies,which was higher than the response rate of 50%with the standard of care with peginterferon plus *** very preliminary studies of patients with chronic hepatitis B,nitazoxanide suppressed serum HBV DNA and led to loss of hepatitis B e antigen in the majority of patients and hepatitis B surface antigen in approximately a quarter of *** controlled studies of naive and nonresponder patients with chronic hepatitis C genotype 1 are underway,new second generation and controlled release thiazolides are being developed,and future studies of patients with chronic hepatitis B are planned.

关键词： Hepatitis C Hepatitis C virus nitazoxanide

nitazoxanide干混悬剂及伊维菌素复方干混悬剂的研究

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Nitazoxanide干混悬剂及伊维菌素复方干混悬剂的研究

作者：尚炜中国农业科学院

学位级别：硕士

nitazoxanide(NTZ)是一种具有广阔应用前景的高效、广谱抗动物与人体寄生虫、细菌和真菌感染药物,在我国还没有该产品上市,为充分发掘其兽医临床上的应用潜力,本文进行了NTZ干混悬剂的研究。初步探讨了NTZ制备方法:以2-氨基-5-硝基... 详细信息

nitazoxanide(NTZ)是一种具有广阔应用前景的高效、广谱抗动物与人体寄生虫、细菌和真菌感染药物,在我国还没有该产品上市,为充分发掘其兽医临床上的应用潜力,本文进行了NTZ干混悬剂的研究。初步探讨了NTZ制备方法:以2-氨基-5-硝基-噻唑和邻乙酰水杨酰氯作为合成起始原料,经酰化反应、乙醇重结晶而得。得到的产物经过薄层色谱法、HPLC法、IR法、UV法、HNMR法和MS等方法结构确证为NTZ,产率为35%～45%,通过建立的HPLC法检测含量可达到99%。以沉降体积比、再分散性、pH值为考察指标,采用正交设计试验对NTZ干混悬剂处方进行筛选,并考察优选处方的流体性能、粒径分布及稳定性。建立了一种简单快速、专属性强和灵敏度高的反相高效液相色谱法测定NTZ干混悬剂的含量,以控制该制剂的质量。色谱柱为迪马Diamonsil C(4.6×200,5μm)柱,流动相为0.2%磷酸水溶液:乙腈=50:50(V/V),检测波长:346nm,流速1mL/min。NTZ浓度在17.9～107.2μg/mL范围内,浓度与峰面积线性关系良好(r=0.9998)。NTZ的平均回收率为103.47%,RSD=0.64%,n=8,方法简便,精密度良好。将50mg/mL NTZ干混液,常温放置,分别于1h、2h、3h、4h、24h、48h、72h、96h、120h和144h时取样,经HPLC法测定,发现NTZ混悬液室温放置144h后依然十分稳定。取三个不同批次的NTZ干混悬剂样品,铝箔袋包装在温度为40±2℃,相对湿度为75%±5%的恒温箱中放置3个月。分别于0、1、2、3个月各取样一次,每次按混悬剂稳定性重点考察项目检测该干混悬剂物理性状(性状、色泽、沉降容积比、再分散性)和化学性状(含量、pH值和降解产物)的变化。结果表明该制剂经加速试验,3个月后含量仍在质量标准范围内,该制剂在常规温度加速试验条件下稳定。制定了NTZ(原料)、对照品及其干混悬剂质量标准(草案)与起草说明。为考察NTZ在使用过程中的安全性,用NTZ原料药进行昆明系小白鼠急性毒性试验。结果表明,NTZ小鼠经口LD为4712.38mg/kg,属于低毒。进行了NTZ干混悬剂对犬复孔绦虫的疗效试验。选择自然感染复孔绦虫的犬6只,按200mg/kg bw的剂量一次口服此干混悬剂(按NTZ计100mg/kg bw)。结果表明,该制剂对犬复孔绦虫有良好的驱杀作用。制备了一种伊维菌素复方干混悬剂,并建立了此制剂的高效液相色谱含量测定方法,对其原料药和制剂进行小白鼠急性毒性试验,并对其临床驱除犬消化道线虫效果进行了初步观察。

关键词：抗寄生虫药 nitazoxanide 伊维菌素干混悬剂制备临床试验