{"status":"ok","message-type":"work","message-version":"1.0.0","message":{"indexed":{"date-parts":[[2025,10,11]],"date-time":"2025-10-11T00:49:17Z","timestamp":1760143757792,"version":"build-2065373602"},"reference-count":10,"publisher":"MDPI AG","issue":"5","license":[{"start":{"date-parts":[[2024,2,28]],"date-time":"2024-02-28T00:00:00Z","timestamp":1709078400000},"content-version":"vor","delay-in-days":0,"URL":"https:\/\/creativecommons.org\/licenses\/by\/4.0\/"}],"funder":[{"DOI":"10.13039\/501100001809","name":"National Natural Science Foundation of China","doi-asserted-by":"publisher","award":["82273889","2023NSFSC0657","2022CDLZ-17"],"award-info":[{"award-number":["82273889","2023NSFSC0657","2022CDLZ-17"]}],"id":[{"id":"10.13039\/501100001809","id-type":"DOI","asserted-by":"publisher"}]},{"DOI":"10.13039\/501100004829","name":"Science and Technology Department of Sichuan Province","doi-asserted-by":"publisher","award":["82273889","2023NSFSC0657","2022CDLZ-17"],"award-info":[{"award-number":["82273889","2023NSFSC0657","2022CDLZ-17"]}],"id":[{"id":"10.13039\/501100004829","id-type":"DOI","asserted-by":"publisher"}]},{"name":"Cooperative Project of Sichuan University and Luzhou","award":["82273889","2023NSFSC0657","2022CDLZ-17"],"award-info":[{"award-number":["82273889","2023NSFSC0657","2022CDLZ-17"]}]}],"content-domain":{"domain":[],"crossmark-restriction":false},"short-container-title":["Molecules"],"abstract":"<jats:p>Bitespiramycin, has been shown to have a therapeutic effect against respiratory tract inflammation, including a potential effect against COVID-19. A current clinical trial in China showed that bitespiramycin was an effective treatment for severe pneumonia and intracranial infection. However, there is lack of an analytical method to elucidate the distribution of bitespiramycin. In this study, a highly sensitive, rapid and reliable UPLC\u2013MS\/MS method was developed to comprehensively characterize the bitespiramycin distribution in various bio-samples, which is significantly improved upon the published work. A rapid sample preparation method was developed by using n-butanol as the solvent to extract bitespiramycin from different bio-samples. The extract was then directly analyzed by UPLC\u2013MS\/MS coupled with an alkaline-resistant column after centrifugation which avoids the time-consuming concentration process under nitrogen and redissolution. The method was employed to accurately quantify bitespiramycin and its metabolites in rat plasma, tissues, and human cerebrospinal fluid. Notably, the presence of bitespiramycin and its metabolites was identified for the first time in various rat organs including brain, testis, bladder and prostate as well as in human cerebrospinal fluid. This newly developed approach shows great promise for drug distribution assays including other antibiotics and can help elucidate the ADME of bitespiramycin.<\/jats:p>","DOI":"10.3390\/molecules29051037","type":"journal-article","created":{"date-parts":[[2024,2,28]],"date-time":"2024-02-28T06:14:22Z","timestamp":1709100862000},"page":"1037","update-policy":"https:\/\/doi.org\/10.3390\/mdpi_crossmark_policy","source":"Crossref","is-referenced-by-count":0,"title":["Study of Bitespiramycin Distribution in Rats and Cerebrospinal Fluid of Patients by a Sensitive LC-MS\/MS Method with Rapid Sample Preparation"],"prefix":"10.3390","volume":"29","author":[{"given":"Yujie","family":"Zhang","sequence":"first","affiliation":[{"name":"School of Pharmacy, Southwest Medical University, Luzhou 646000, China"}],"role":[{"role":"author","vocabulary":"crossref"}]},{"given":"Jingjie","family":"Cao","sequence":"additional","affiliation":[{"name":"School of Pharmacy, Southwest Medical University, Luzhou 646000, China"}],"role":[{"role":"author","vocabulary":"crossref"}]},{"given":"Jiahan","family":"Su","sequence":"additional","affiliation":[{"name":"School of Pharmacy, Southwest Medical University, Luzhou 646000, China"}],"role":[{"role":"author","vocabulary":"crossref"}]},{"given":"Tingting","family":"He","sequence":"additional","affiliation":[{"name":"School of Pharmacy, Southwest Medical University, Luzhou 646000, China"}],"role":[{"role":"author","vocabulary":"crossref"}]},{"given":"Qianru","family":"Wang","sequence":"additional","affiliation":[{"name":"School of Pharmacy, Southwest Medical University, Luzhou 646000, China"}],"role":[{"role":"author","vocabulary":"crossref"}]},{"given":"Feng","family":"Wei","sequence":"additional","affiliation":[{"name":"Shanghai Tonglian Pharmaceutical Co., Ltd., Shanghai 201611, China"}],"role":[{"role":"author","vocabulary":"crossref"}]},{"given":"Xin","family":"Guo","sequence":"additional","affiliation":[{"name":"Luzhou New Drug Safety Evaluation Research Center, Luzhou 646000, China"}],"role":[{"role":"author","vocabulary":"crossref"}]},{"given":"Qibing","family":"Mei","sequence":"additional","affiliation":[{"name":"School of Pharmacy, Southwest Medical University, Luzhou 646000, China"},{"name":"Luzhou New Drug Safety Evaluation Research Center, Luzhou 646000, China"}],"role":[{"role":"author","vocabulary":"crossref"}]},{"ORCID":"https:\/\/orcid.org\/0000-0003-0857-2217","authenticated-orcid":false,"given":"Jing","family":"Zeng","sequence":"additional","affiliation":[{"name":"School of Pharmacy, Southwest Medical University, Luzhou 646000, China"}],"role":[{"role":"author","vocabulary":"crossref"}]}],"member":"1968","published-online":{"date-parts":[[2024,2,28]]},"reference":[{"key":"ref_1","doi-asserted-by":"crossref","first-page":"2850","DOI":"10.1016\/j.apsb.2021.02.024","article-title":"Repurposing CFDA-approved drug carrimycin as an antiviral agent against human coronaviruses, including the currently pandemic SARS-CoV-2","volume":"11","author":"Yan","year":"2021","journal-title":"Acta Pharm. Sin. B"},{"key":"ref_2","unstructured":"U. S. National Library of Medicine (2024, February 19). Study to Evaluate Safety and Efficacy of Carrimycin for Treatment of Severe COVID-19 in Hospitalized Patients, Available online: https:\/\/clinicaltrials.gov\/study\/NCT04672564."},{"key":"ref_3","doi-asserted-by":"crossref","first-page":"126","DOI":"10.1186\/s13046-022-02350-0","article-title":"Targeting selenoprotein H in the nucleolus suppresses tumors and metastases by Isovalerylspiramycin I","volume":"41","author":"Cui","year":"2022","journal-title":"J. Exp. Clin. Cancer Res."},{"key":"ref_4","doi-asserted-by":"crossref","first-page":"402","DOI":"10.1016\/j.jpba.2012.03.013","article-title":"Identification of multi components in bitespiramycin by liquid chromatography-mass spectrometry","volume":"66","author":"Wang","year":"2012","journal-title":"J. Pharm. Biomed. Anal."},{"key":"ref_5","first-page":"1183","article-title":"Analysis of components of bitespiramycin by HPLC","volume":"44","author":"Yang","year":"2009","journal-title":"Acta Pharm. Sin. B"},{"key":"ref_6","doi-asserted-by":"crossref","first-page":"343","DOI":"10.1080\/00498250500087580","article-title":"Structural identification of bitespiramycin metabolites in rat: A single oral dose study","volume":"35","author":"Shi","year":"2005","journal-title":"Xenobiotica"},{"key":"ref_7","first-page":"431","article-title":"Metabolites of A Novel Antibiotic Bitespiramycin in Rat Urine and Bile","volume":"4","author":"Shi","year":"2004","journal-title":"Chin. Chem. Lett."},{"key":"ref_8","doi-asserted-by":"crossref","first-page":"45","DOI":"10.1016\/S1570-0232(03)00205-8","article-title":"Determination of three major components of bitespiramycin and their major active metabolites in rat plasma by liquid chromatography-ion trap mass spectrometry","volume":"791","author":"Zhong","year":"2003","journal-title":"J. Chromatogr. B"},{"key":"ref_9","first-page":"1396","article-title":"Tissue distribution of bitespiramycin and spiramycin in rats","volume":"25","author":"Shi","year":"2004","journal-title":"Acta Pharmacol. Sin."},{"key":"ref_10","first-page":"973","article-title":"Pharmacokinetics of kelimycin tablets in beagle dogs","volume":"36","author":"Gao","year":"2019","journal-title":"J. Shenyang Pharma Univ."}],"container-title":["Molecules"],"original-title":[],"language":"en","link":[{"URL":"https:\/\/www.mdpi.com\/1420-3049\/29\/5\/1037\/pdf","content-type":"unspecified","content-version":"vor","intended-application":"similarity-checking"}],"deposited":{"date-parts":[[2025,10,10]],"date-time":"2025-10-10T14:06:15Z","timestamp":1760105175000},"score":1,"resource":{"primary":{"URL":"https:\/\/www.mdpi.com\/1420-3049\/29\/5\/1037"}},"subtitle":[],"short-title":[],"issued":{"date-parts":[[2024,2,28]]},"references-count":10,"journal-issue":{"issue":"5","published-online":{"date-parts":[[2024,3]]}},"alternative-id":["molecules29051037"],"URL":"https:\/\/doi.org\/10.3390\/molecules29051037","relation":{},"ISSN":["1420-3049"],"issn-type":[{"type":"electronic","value":"1420-3049"}],"subject":[],"published":{"date-parts":[[2024,2,28]]}}}