[논문]Bioanalysis of niclosamide in plasma using liquid chromatography-tandem mass and application to pharmacokinetics in rats and dogs

Choi, Hae-In; Kim, Taeheon; Lee, Seung-Won; Woo Kim, Jin; Ju Noh, Yoon; Kim, Gwan-Young; Jin Park, Hyun-; Chae, Yoon-Jee; Lee, Kyeong-Ryoon; Kim, Soo-Jin; Koo, Tae-Sung

doi:10.1016/j.jchromb.2021.122862

[해외논문] Bioanalysis of niclosamide in plasma using liquid chromatography-tandem mass and application to pharmacokinetics in rats and dogs 원문보기

Journal of chromatography. B, Analytical technologies in the biomedical and life sciences, v.1179, 2021년, pp.122862 -

Choi, Hae-In (Graduate School of New Drug Discovery and Development, Chungnam National University) , Kim, Taeheon (Life Science Research Institute) , Lee, Seung-Won (Graduate School of New Drug Discovery and Development, Chungnam National University) , Woo Kim, Jin (Graduate School of New Drug Discovery and Development, Chungnam National University) , Ju Noh, Yoon (Graduate School of New Drug Discovery and Development, Chungnam National University) , Kim, Gwan-Young (Life Science Research Institute) , Jin Park, Hyun- (Life Science Research Institute) , Chae, Yoon-Jee (College of Pharmacy, Woosuk University) , Lee, Kyeong-Ryoon (Laboratory Animal Resource Center, Korea Research Institute of Bioscience and Biotechnology) , Kim, Soo-Jin (Clinical Development Division, Daewoong Therapeutics Inc. Republic of Korea<) , Koo, Tae-Sung

Abstract ▼ AI-Helper

Abstract Niclosamide, which is an anti-tapeworm drug, was developed in 1958. However, recent studies have demonstrated the antiviral effects of niclosamide against the SARS-CoV-2 virus, which causes COVID-19. In this study, we developed and validated a quantitative analysis method for the determination of niclosamide in rat and dog plasma using liquid chromatography–tandem mass spectrometry (LC–MS/MS), and used this method for pharmacokinetic studies. Biological samples were prepared using the protein precipitation method with acetonitrile. Ibuprofen was used as an internal standard. The mobile phase used to quantify niclosamide in rat or dog plasma consisted of 10 mM ammonium formate in distilled water-acetonitrile (30:70, v/v) or 5 mM ammonium acetate–methanol (30:70, v/v). An XDB-phenyl column (5 µm, 2.1 × 50 mm) and a Kinetex® C18 column (5 µm, 2.1 × 500 mm) were used as reverse-phase liquid chromatography columns for rat and dog plasma analyses, respectively. Niclosamide and ibuprofen were detected under multiple reaction monitoring conditions using the electrospray ionization interface running in the negative ionization mode. Niclosamide presented linearity in the concentration ranges of 1–3000 ng/mL (r = 0.9967) and 1–1000 ng/mL (r = 0.9941) in rat and dog plasma, respectively. The intra- and inter-day precision values were < 7.40% and < 6.35%, respectively, for rat plasma, and < 3.95% and < 4.01%, respectively, for dog plasma. The intra- and inter-day accuracy values were < 4.59% and < 6.63%, respectively, for rat plasma, and < 12.1% and 99.8%) and low metabolic stability. These results can be helpful for further developing and understanding the pharmacokinetic characteristics of niclosamide to expand its clinical use. Highlights Several Clinical studies of niclosamide on COVID-19 are active. Information on analytical methods in biological samples is limited. A reliable LC-MS/MS method was developed and validated in rat and dog plasma. The developed LC-MS/MS method is simple, rapid, sensitive, and accurate. This method was successfully applied to pharmacokinetic study in rats and dogs.

Keyword

참고문헌 (23)

1 Zu Z.Y. Jiang M.D. Xu P.P. Chen W. Ni Q.Q. Lu G.M. Zhang L.J. Coronavirus disease (COVID-19): a perspective from China Radiology 296 2020 2019 E15 E25 10.1148/radiol.2020200490

상세보기
2 Wang Q. Zhang Y. Wu L. Niu S. Song C. Zhang Z. Lu G. Qiao C. Hu Y. Yuen K.-Y. Structural and functional basis of SARS-CoV-2 entry by using human ACE2 Cell 181 2020 894 904.e9 10.1016/j.cell.2020.03.045 32275855

상세보기
3 Zhu N. Zhang D. Wang W. Li X. Yang B. Song J. Zhao X. Huang B. Shi W. Lu R. A novel coronavirus from patients with pneumonia in China N. Engl. J. Med. 382 2020 2019 727 733 10.1056/NEJMoa2001017

상세보기
4 Singhal T. A review of coronavirus disease-2019 (COVID-19) The indian journal of pediatrics 87 2020 281 286 10.1007/s12098-020-03263-6 32166607

상세보기
5 Weinbach E.C. GARBUS J. Mechanism of action of reagents that uncouple oxidative phosphorylation Nature 221 1969 1016 1018 10.1038/2211016a0 4180173

상세보기
6 Arend R.C. Londoño-Joshi A.I. Samant R.S. Li Y. Conner M. Hidalgo B. Alvarez R.D. Landen C.N. Straughn J.M. Buchsbaum D.J. Inhibition of Wnt/β-catenin pathway by niclosamide: A therapeutic target for ovarian cancer Gynecol. Oncol. 134 2014 112 120 10.1016/j.ygyno.2014.04.005 24736023

상세보기
7 Burock S. Daum S. Keilholz U. Neumann K. Walther W. Stein U. Phase II trial to investigate the safety and efficacy of orally applied niclosamide in patients with metachronous or sychronous metastases of a colorectal cancer progressing after therapy: the NIKOLO trial BMC cancer 18 2018 1 7 10.1186/s12885-018-4197-9 29291726

상세보기
8 Monin M.B. Krause P. Stelling R. Bocuk D. Niebert S. Klemm F. Pukrop T. Koenig S. The anthelmintic niclosamide inhibits colorectal cancer cell lines via modulation of the canonical and noncanonical Wnt signaling pathway J. Surg. Res. 203 2016 193 205 10.1016/j.jss.2016.03.051 27338550

상세보기
9 Schweizer M.T. Haugk K. McKiernan J.S. Gulati R. Cheng H.H. Maes J.L. Dumpit R.F. Nelson P.S. Montgomery B. McCune J.S. A phase I study of niclosamide in combination with enzalutamide in men with castration-resistant prostate cancer PLoS ONE 13 2018 e0198389 10.1371/journal.pone.0202709

상세보기
10 Gassen N.C. Niemeyer D. Muth D. Corman V.M. Martinelli S. Gassen A. Hafner K. Papies J. Mösbauer K. Zellner A. SKP2 attenuates autophagy through Beclin1-ubiquitination and its inhibition reduces MERS-Coronavirus infection Nat. Commun. 10 2019 1 16 10.1038/s41467-019-13659-4 30602773

상세보기
11 Gassen N.C. Papies J. Bajaj T. Dethloff F. Emanuel J. Weckmann K. Heinz D.E. Heinemann N. Lennarz M. Richter A. Analysis of SARS-CoV-2-controlled autophagy reveals spermidine, MK-2206, and niclosamide as putative antiviral therapeutics BioRxiv 2020 10.1101/2020.04.15.997254
12 Wu C.-J. Jan J.-T. Chen C.-M. Hsieh H.-P. Hwang D.-R. Liu H.-W. Liu C.-Y. Huang H.-W. Chen S.-C. Hong C.-F. Inhibition of severe acute respiratory syndrome coronavirus replication by niclosamide Antimicrob. Agents Chemother. 48 2004 2693 2696 10.1128/AAC.48.7.2693-2696.2004 15215127

상세보기
13 S. Jeon, M. Ko, J. Lee, I. Choi, S.Y. Byun, S. Park, D. Shum, S. Kim, Identification of antiviral drug candidates against SARS-CoV-2 from FDA-approved drugs, Antimicrobial Agents and Chemotherapy, 64 (2020) e00819-20, https://doi.org/ 10.1128/AAC.00819-20.
14 NIH U. S. National Library of Medicine, ClinicalTrials.gov https://www.clinicaltrials.gov/ct2/results?recrs=&cond=COVID-19&term=niclosamide&cntry=&state=&city=&dist= (accessed 07 March 2021).
15 Doran G. Stevens M.M. Simultaneous determination of niclosamide and its degradates in water by LC-MS/MS Anal. Methods 6 2014 6871 6877 10.1039/C4AY01074D

상세보기
16 Jiang H. Zhang Y. Chen X. Lv J. Zou J. Simultaneous determination of pentachlorophenol, niclosamide and fenpropathrin in fishpond water using an LC-MS/MS method for forensic investigation Anal. Methods 5 2013 111 115 10.1039/C2AY25685A

상세보기
17 Chang Y.-W. Yeh T.-K. Lin K.-T. Chen W.-C. Yao H.-T. Pharmacokinetics of anti-SARS-CoV agent niclosamide and its analogs in rats J. Food Drug Anal. 14 2006 329 333 10.38212/2224-6614.2464

상세보기
18 U.S. Food and Drug Administration, Guidance for Industry Bioanalytical Method Validation 2018
19 European Medicines Agency, Guideline on Bioanalytical Method Validation (2011).
20 Ji Y.-G. Shin Y.-M. Jeong J.-W. Choi H.-I. Lee S.-W. Lee J.-H. Lee K.-R. Koo T.-S. Determination of motolimod concentration in rat plasma by liquid chromatography-tandem mass spectrometry and its application in a pharmacokinetic study J. Pharm. Biomed. Anal. 179 2020 112987 10.1016/j.jpba.2019.112987

상세보기
21 Jeong S.-H. Jang J.-H. Cho H.-Y. Oh I.-J. Lee Y.-B. A sensitive UPLC–ESI–MS/MS method for the quantification of cinnamic acid in vivo and in vitro: application to pharmacokinetic and protein binding study in human plasma Journal of Pharmaceutical Investigation 50 2020 159 172 10.1007/s40005-019-00444-0

상세보기
22 Fan J. de Lannoy I.A. Pharmacokinetics Biochem Pharmacol 87 2014 93 120 10.1016/j.bcp.2013.09.007 24055064

상세보기
23 El-Kattan A.F. Oral bioavailability assessment: basics and strategies for drug discovery and development 2017 Wiley 7

LOADING...

활용도 분석정보

상세보기

다운로드

내보내기

활용도 Top5 논문

해당 논문의 주제분야에서 활용도가 높은 상위 5개 콘텐츠를 보여줍니다.
더보기 버튼을 클릭하시면 더 많은 관련자료를 살펴볼 수 있습니다.

내보내기 구분	파일저장 인쇄 메일전송
구성항목	기본정보 상세정보 관리번호, 논문명, 저널/프로시딩명, 저자 , 발행년, 권, 호, 시작페이지, 끝페이지, 발행기관 관리번호, 논문명, 대등논문명, 저자 , 저널/프로시딩명, 발행기관, 발행년, 발행언어, 권, 호, 시작페이지, 끝페이지, ISBN, ISSN, 주제분야, 키워드, 초록(한글), 초록(영문), 저자(소속기관)
저장형식	Text(ASCII format) Excel format RefWorks Direct Export RIS format (for Reference Manager, ProCite, EndNote), Scholar's Aids, Mendeley
메일정보	받는사람 (필수) @ 보내는사람 (선택) @ 제목 내용 KISTI 검색결과 이메일 서비스
안내	총 건의 자료가 검색되었습니다. 다운받으실 자료의 인덱스를 입력하세요. (1-10,000) 검색결과의 순서대로 최대 10,000건 까지 다운로드가 가능합니다. 데이타가 많을 경우 속도가 느려질 수 있습니다.(최대 2~3분 소요) 다운로드 파일은 UTF-8 형태로 저장됩니다. 파일의 내용이 제대로 보이지 않을실 때는 웹브라우저 상단의 보기 -> 인코딩 -> 자동선택 여부를 확인하십시오. ~ Text(ASCII format) Excel format

연합인증

[해외논문] Bioanalysis of niclosamide in plasma using liquid chromatography-tandem mass and application to pharmacokinetics in rats and dogs 원문보기

Abstract ▼ AI-Helper

Keyword

참고문헌 (23)

이 논문을 인용한 문헌

연구과제 타임라인

활용도 분석정보

활용도 Top5 논문

관련 콘텐츠

원문 보기

원문 URL 링크

오픈액세스(OA) 유형

AI-Helper ※ AI-Helper는 오픈소스 모델을 사용합니다.

선택된 텍스트

연합인증

[해외논문] Bioanalysis of niclosamide in plasma using liquid chromatography-tandem mass and application to pharmacokinetics in rats and dogs 원문보기

Abstract ▼ AI-Helper

Keyword

참고문헌 (23)

이 논문을 인용한 문헌

연구과제 타임라인

전체(0) 논문(0) 특허(0) 보고서(0)

전체(0) 논문(0) 특허(0) 보고서(0)

활용도 분석정보

활용도 Top5 논문 더보기

관련 콘텐츠

원문 보기

원문 URL 링크

오픈액세스(OA) 유형

AI-Helper ※ AI-Helper는 오픈소스 모델을 사용합니다.

선택된 텍스트

활용도 Top5 논문