{"status":"ok","message-type":"work","message-version":"1.0.0","message":{"indexed":{"date-parts":[[2025,11,21]],"date-time":"2025-11-21T06:02:35Z","timestamp":1763704955661},"reference-count":37,"publisher":"American Society for Microbiology","issue":"9","license":[{"start":{"date-parts":[[2014,9,1]],"date-time":"2014-09-01T00:00:00Z","timestamp":1409529600000},"content-version":"tdm","delay-in-days":0,"URL":"https:\/\/journals.asm.org\/non-commercial-tdm-license"}],"content-domain":{"domain":["journals.asm.org"],"crossmark-restriction":true},"short-container-title":["Antimicrob Agents Chemother"],"published-print":{"date-parts":[[2014,9]]},"abstract":"<jats:title>ABSTRACT<\/jats:title>\n          <jats:p>\n            Macrolactin A (MA) and 7-\n            <jats:italic>O<\/jats:italic>\n            -succinyl macrolactin A (SMA), polyene macrolides containing a 24-membered lactone ring, show antibiotic effects superior to those of teicoplanin against vancomycin-resistant enterococci and methicillin-resistant\n            <jats:named-content xmlns:xlink=\"http:\/\/www.w3.org\/1999\/xlink\" content-type=\"genus-species\" xlink:type=\"simple\">Staphylococcus aureus<\/jats:named-content>\n            . MA and SMA are currently being evaluated as antitumor agents in preclinical studies in Korea. We evaluated the potential of MA and SMA for the inhibition or induction of human liver cytochrome P450 (CYP) enzymes and UDP-glucuronosyltransferases (UGTs)\n            <jats:italic>in vitro<\/jats:italic>\n            to assess their safety as new molecular entities. We demonstrated that MA and SMA are potent competitive inhibitors of CYP2C9, with\n            <jats:italic>\n              K\n              <jats:sub>i<\/jats:sub>\n            <\/jats:italic>\n            values of 4.06 \u03bcM and 10.6 \u03bcM, respectively. MA and SMA also weakly inhibited UGT1A1 activity, with\n            <jats:italic>\n              K\n              <jats:sub>i<\/jats:sub>\n            <\/jats:italic>\n            values of 40.1 \u03bcM and 65.3 \u03bcM, respectively. However, these macrolactins showed no time-dependent inactivation of the nine CYPs studied. In addition, MA and SMA did not induce CYP1A2, CYP2B6, or CYP3A4\/5. On the basis of an\n            <jats:italic>in vitro-in vivo<\/jats:italic>\n            extrapolation, our data strongly suggested that MA and SMA are unlikely to cause clinically significant drug-drug interactions mediated via inhibition or induction of most of the CYPs involved in drug metabolism\n            <jats:italic>in vivo<\/jats:italic>\n            , except for the inhibition of CYP2C9 by MA. Similarly, MA and SMA are unlikely to inhibit the activity of UGT1A1, UGT1A4, UGT1A6, UGT1A9, and UGT2B7 enzymes\n            <jats:italic>in vivo<\/jats:italic>\n            . Although further investigations will be required to clarify the\n            <jats:italic>in vivo<\/jats:italic>\n            interactions of MA with CYP2C9-targeted drugs, our findings offer a clearer understanding and prediction of drug-drug interactions for the safe use of MA and SMA in clinical practice.\n          <\/jats:p>","DOI":"10.1128\/aac.00018-14","type":"journal-article","created":{"date-parts":[[2014,6,3]],"date-time":"2014-06-03T06:12:01Z","timestamp":1401775921000},"page":"5036-5046","update-policy":"http:\/\/dx.doi.org\/10.1128\/asmj-crossmark-policy-page","source":"Crossref","is-referenced-by-count":14,"title":["Metabolic Drug-Drug Interaction Potential of Macrolactin A and 7-\n            <i>O<\/i>\n            -Succinyl Macrolactin A Assessed by Evaluating Cytochrome P450 Inhibition and Induction and UDP-Glucuronosyltransferase Inhibition\n            <i>In Vitro<\/i>"],"prefix":"10.1128","volume":"58","author":[{"given":"Soo Hyeon","family":"Bae","sequence":"first","affiliation":[{"name":"College of Pharmacy and Integrated Research Institute of Pharmaceutical Sciences, The Catholic University of Korea, Bucheon, Republic of Korea"}],"role":[{"role":"author","vocabulary":"crossref"}]},{"given":"Min Jo","family":"Kwon","sequence":"additional","affiliation":[{"name":"College of Pharmacy and Integrated Research Institute of Pharmaceutical Sciences, The Catholic University of Korea, Bucheon, Republic of Korea"}],"role":[{"role":"author","vocabulary":"crossref"}]},{"given":"Jung Bae","family":"Park","sequence":"additional","affiliation":[{"name":"College of Pharmacy and Integrated Research Institute of Pharmaceutical Sciences, The Catholic University of Korea, Bucheon, Republic of Korea"}],"role":[{"role":"author","vocabulary":"crossref"}]},{"given":"Doyun","family":"Kim","sequence":"additional","affiliation":[{"name":"College of Pharmacy and Integrated Research Institute of Pharmaceutical Sciences, The Catholic University of Korea, Bucheon, Republic of Korea"}],"role":[{"role":"author","vocabulary":"crossref"}]},{"given":"Dong-Hee","family":"Kim","sequence":"additional","affiliation":[{"name":"Research and Development Center, Daewoo Pharmaceutical Co., Ltd., Busan, Republic of Korea"}],"role":[{"role":"author","vocabulary":"crossref"}]},{"given":"Jae-Seon","family":"Kang","sequence":"additional","affiliation":[{"name":"Department of Pharmacy, Kyungsung University, Busan, Republic of Korea"}],"role":[{"role":"author","vocabulary":"crossref"}]},{"given":"Chun-Gyu","family":"Kim","sequence":"additional","affiliation":[{"name":"Department of Pharmaceutical Engineering, Inje University, Gimhae, Gyeongnam, Republic of Korea"}],"role":[{"role":"author","vocabulary":"crossref"}]},{"given":"Euichaul","family":"Oh","sequence":"additional","affiliation":[{"name":"College of Pharmacy and Integrated Research Institute of Pharmaceutical Sciences, The Catholic University of Korea, Bucheon, Republic of Korea"}],"role":[{"role":"author","vocabulary":"crossref"}]},{"given":"Soo Kyung","family":"Bae","sequence":"additional","affiliation":[{"name":"College of Pharmacy and Integrated Research Institute of Pharmaceutical Sciences, The Catholic University of Korea, Bucheon, Republic of Korea"}],"role":[{"role":"author","vocabulary":"crossref"}]}],"member":"235","reference":[{"key":"e_1_3_2_2_2","doi-asserted-by":"publisher","DOI":"10.1021\/ja00201a036"},{"key":"e_1_3_2_3_2","doi-asserted-by":"publisher","DOI":"10.1002\/cbdv.200890155"},{"key":"e_1_3_2_4_2","doi-asserted-by":"publisher","DOI":"10.7164\/antibiotics.54.333"},{"key":"e_1_3_2_5_2","doi-asserted-by":"publisher","DOI":"10.1007\/s12272-011-0117-0"},{"key":"e_1_3_2_6_2","doi-asserted-by":"publisher","DOI":"10.1111\/j.1365-2672.2005.02614.x"},{"key":"e_1_3_2_7_2","doi-asserted-by":"publisher","DOI":"10.1139\/w03-084"},{"key":"e_1_3_2_8_2","doi-asserted-by":"publisher","DOI":"10.1021\/np070070k"},{"key":"e_1_3_2_9_2","doi-asserted-by":"publisher","DOI":"10.1016\/j.tetlet.2003.11.055"},{"key":"e_1_3_2_10_2","doi-asserted-by":"publisher","DOI":"10.1021\/ja980203b"},{"key":"e_1_3_2_11_2","doi-asserted-by":"publisher","DOI":"10.1021\/ja017177t"},{"key":"e_1_3_2_12_2","doi-asserted-by":"publisher","DOI":"10.1021\/jo049556l"},{"key":"e_1_3_2_13_2","doi-asserted-by":"publisher","DOI":"10.1128\/AAC.50.5.1701-1709.2006"},{"key":"e_1_3_2_14_2","doi-asserted-by":"publisher","DOI":"10.1002\/bmc.2786"},{"key":"e_1_3_2_15_2","doi-asserted-by":"publisher","DOI":"10.1124\/dmd.31.7.815"},{"key":"e_1_3_2_16_2","doi-asserted-by":"publisher","DOI":"10.1016\/j.taap.2009.12.016"},{"key":"e_1_3_2_17_2","volume-title":"Guideline on the investigation of drug interactions","author":"European Medicines Agency","year":"2010","unstructured":"European Medicines Agency. 2010. 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