{"status":"ok","message-type":"work","message-version":"1.0.0","message":{"indexed":{"date-parts":[[2026,5,16]],"date-time":"2026-05-16T06:46:39Z","timestamp":1778913999184,"version":"3.51.4"},"reference-count":40,"publisher":"MDPI AG","issue":"21","license":[{"start":{"date-parts":[[2021,10,26]],"date-time":"2021-10-26T00:00:00Z","timestamp":1635206400000},"content-version":"vor","delay-in-days":0,"URL":"https:\/\/creativecommons.org\/licenses\/by\/4.0\/"}],"funder":[{"name":"Natural Science Foundation of Jiangxi Province, China","award":["20192ACBL20020"],"award-info":[{"award-number":["20192ACBL20020"]}]},{"name":"Natural Science Foundation of Jiangxi Province, China","award":["20202BABL206156"],"award-info":[{"award-number":["20202BABL206156"]}]},{"DOI":"10.13039\/501100001809","name":"National Natural Science Foundation of China","doi-asserted-by":"publisher","award":["81960636"],"award-info":[{"award-number":["81960636"]}],"id":[{"id":"10.13039\/501100001809","id-type":"DOI","asserted-by":"publisher"}]},{"DOI":"10.13039\/501100001809","name":"National Natural Science Foundation of China","doi-asserted-by":"publisher","award":["82073745"],"award-info":[{"award-number":["82073745"]}],"id":[{"id":"10.13039\/501100001809","id-type":"DOI","asserted-by":"publisher"}]}],"content-domain":{"domain":[],"crossmark-restriction":false},"short-container-title":["Molecules"],"abstract":"<jats:p>As antimicrobial resistance has been increasing, new antimicrobial agents are desperately needed. Azalomycin F, a natural polyhydroxy macrolide, presents remarkable antimicrobial activities. To investigate its pharmacokinetic characteristics in rats, the concentrations of azalomycin F contained in biological samples, in vitro, were determined using a validated high-performance liquid chromatography\u2013ultraviolet (HPLC-UV) method, and, in vivo, samples were assayed by an ultra-high performance liquid chromatography\u2013tandem mass spectrometric (UPLC\u2013MS\/MS) method. Based on these methods, the pharmacokinetics of azalomycin F were first investigated. Its plasma concentration-time courses and pharmacokinetic parameters in rats were obtained by a non-compartment model for oral (26.4 mg\/kg) and intravenous (2.2 mg\/kg) administrations. The results indicate that the oral absolute bioavailability of azalomycin F is very low (2.39 \u00b1 1.28%). From combinational analyses of these pharmacokinetic parameters, and of the results of the in-vitro absorption and metabolism experiments, we conclude that azalomycin F is absorbed relatively slowly and with difficulty by the intestinal tract, and subsequently can be rapidly distributed into the tissues and\/or intracellular f of rats. Azalomycin F is stable in plasma, whole blood, and the liver, and presents plasma protein binding ratios of more than 90%. Moreover, one of the major elimination routes of azalomycin F is its excretion through bile and feces. Together, the above indicate that azalomycin F is suitable for administration by intravenous injection when used for systemic diseases, while, by oral administration, it can be used in the treatment of diseases of the gastrointestinal tract.<\/jats:p>","DOI":"10.3390\/molecules26216464","type":"journal-article","created":{"date-parts":[[2021,10,26]],"date-time":"2021-10-26T23:54:33Z","timestamp":1635292473000},"page":"6464","update-policy":"https:\/\/doi.org\/10.3390\/mdpi_crossmark_policy","source":"Crossref","is-referenced-by-count":4,"title":["Pharmacokinetics of Azalomycin F, a Natural Macrolide Produced by Streptomycete Strains, in Rats"],"prefix":"10.3390","volume":"26","author":[{"given":"Su","family":"He","sequence":"first","affiliation":[{"name":"Biotechnological Engineering Center for Pharmaceutical Research and Development, Jiangxi Agricultural University, Nanchang 330045, China"}],"role":[{"role":"author","vocabulary":"crossref"}]},{"given":"Wenjia","family":"Zhao","sequence":"additional","affiliation":[{"name":"Biotechnological Engineering Center for Pharmaceutical Research and Development, Jiangxi Agricultural University, Nanchang 330045, China"}],"role":[{"role":"author","vocabulary":"crossref"}]},{"given":"Peibo","family":"Li","sequence":"additional","affiliation":[{"name":"Guangdong Engineering and Technology Research Center for Quality and Efficacy Re-Evaluation of Post-Marketed TCM, State Key Laboratory of Biocontrol and Guangdong Provincial Key Laboratory of Plant Resources, School of Life Sciences, Sun Yat-sen University, Guangzhou 510275, China"}],"role":[{"role":"author","vocabulary":"crossref"}]},{"given":"Wenqing","family":"Tu","sequence":"additional","affiliation":[{"name":"Research Institute of Poyang Lake, Jiangxi Academy of Sciences, Nanchang 330012, China"}],"role":[{"role":"author","vocabulary":"crossref"}]},{"given":"Kui","family":"Hong","sequence":"additional","affiliation":[{"name":"Key Laboratory of Combinatorial Biosynthesis and Drug Discovery, Ministry of Education, School of Pharmaceutical Sciences, Wuhan University, Wuhan 430071, China"}],"role":[{"role":"author","vocabulary":"crossref"}]},{"given":"Duoduo","family":"Zhang","sequence":"additional","affiliation":[{"name":"Biotechnological Engineering Center for Pharmaceutical Research and Development, Jiangxi Agricultural University, Nanchang 330045, China"}],"role":[{"role":"author","vocabulary":"crossref"}]},{"given":"Tongke","family":"Zhang","sequence":"additional","affiliation":[{"name":"Biotechnological Engineering Center for Pharmaceutical Research and Development, Jiangxi Agricultural University, Nanchang 330045, China"}],"role":[{"role":"author","vocabulary":"crossref"}]},{"ORCID":"https:\/\/orcid.org\/0000-0002-4944-1144","authenticated-orcid":false,"given":"Ganjun","family":"Yuan","sequence":"additional","affiliation":[{"name":"Biotechnological Engineering Center for Pharmaceutical Research and Development, Jiangxi Agricultural University, Nanchang 330045, China"}],"role":[{"role":"author","vocabulary":"crossref"}]}],"member":"1968","published-online":{"date-parts":[[2021,10,26]]},"reference":[{"key":"ref_1","doi-asserted-by":"crossref","first-page":"874","DOI":"10.1126\/science.aaf9286","article-title":"Achieving global targets for antimicrobial resistance","volume":"353","author":"Laxminarayan","year":"2016","journal-title":"Science"},{"key":"ref_2","doi-asserted-by":"crossref","first-page":"e99","DOI":"10.1016\/S1473-3099(17)30485-1","article-title":"Surveillance for control of antimicrobial resistance","volume":"18","author":"Tacconelli","year":"2018","journal-title":"Lancet Infect. 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