Karstmycins A−H, trichostatin analogues with PTP1B inhibitory activities from Streptomyces sp. DX6D14

Karstmycins A−H, trichostatin analogues with PTP1B inhibitory activities from Streptomyces sp. DX6D14 | Authorea try { document.documentElement.classList.add('js'); } catch (e) { } var _gaq = _gaq || []; _gaq.push(['_setAccount', 'G-8VDV14Y67G']); _gaq.push(['_trackPageview']); (function() { var ga = document.createElement('script'); ga.type = 'text/javascript'; ga.async = true; ga.src = ('https:' == document.location.protocol ? 'https://ssl' : 'http://www') + '.google-analytics.com/ga.js'; var s = document.getElementsByTagName('script')[0]; s.parentNode.insertBefore(ga, s); })(); Skip to main content Preprints Collections Wiley Open Research IET Open Research Ecological Society of Japan All Collections About About Authorea FAQs Contact Us Quick Search anywhere Search for preprint articles, keywords, etc. Search Search ADVANCED SEARCH SCROLL This is a preprint and has not been peer reviewed. Data may be preliminary. 15 September 2025 V1 Latest version Share on Karstmycins A−H, trichostatin analogues with PTP1B inhibitory activities from Streptomyces sp. DX6D14 Authors : Li Yang , Zi-Peng Wang , Jing-Zhe Yuan , Qing-Yun Ma , Qing-Yi Xie , Jiao-Cen Guo , Qing Liu , Hao-Fu Dai , Wen-Jun Li , Bao-Zhu Fang , Duqiang Luo , and Youxing Zhao [email protected] Authors Info & Affiliations https://doi.org/10.22541/au.175792346.69860510/v1 Published Journal of Natural Products Version of record Peer review timeline 125 views 71 downloads Contents Abstract Supplementary Material Information & Authors Metrics & Citations View Options References Figures Tables Media Share Abstract Eight pairs of undescribed trichostatin analogues enantiomers, (±)-karstmycins A−H ( 1a / 1b – 8a / 8b ), and three new enantiomers ( 9a – 11a ) together with five known analogues ( 9b – 11b , 12 , and 13 ) were isolated from karst cave derived Streptomyces sp. DX6D14. The structures and absolute configurations of the new compounds were determined by extensive spectroscopic analysis, as well as NMR chemical shifts and electronic circular dichroism (ECD) calculations. Compounds 1 and 2 were rare trichostatins featuring a nitrile group and compounds 3 − 5 were characterized by a unique a piperidin-2-one moiety at the end of the branched C 7 side chain. Compounds 3a and 3b showed PTP1B inhibitory activity with IC 50 values of 26.52 ± 2.03 and 11.60 ± 2.29 μM, respectively, compared to the positive control sodium orthovanadate (IC 50 : 13.80 ± 0.90 μM). Kinetic study indicated that the most potent compound 3b was a mixed-type inhibitor for PTP1B. Molecular docking simulation revealed that 3b simultaneously interacted with the catalytic site and peripheral site of PTP1B. Supplementary Material File (manuscript.docx) Download 19.52 MB Information & Authors Information Version history V1 Version 1 15 September 2025 Peer review timeline Published Journal of Natural Products Version of Record 24 Dec 2025 Published Copyright This work is licensed under a Non Exclusive No Reuse License. Keywords ptp1b inhibitory activity streptomyces sp. trichostatin Authors Affiliations Li Yang Institute of Tropical Bioscience and Biotechnology View all articles by this author Zi-Peng Wang Institute of Tropical Bioscience and Biotechnology View all articles by this author Jing-Zhe Yuan Institute of Tropical Bioscience and Biotechnology View all articles by this author Qing-Yun Ma Institute of Tropical Bioscience and Biotechnology View all articles by this author Qing-Yi Xie Institute of Tropical Bioscience and Biotechnology View all articles by this author Jiao-Cen Guo Institute of Tropical Bioscience and Biotechnology View all articles by this author Qing Liu Sun Yat-sen University State Key Laboratory of Biocontrol View all articles by this author Hao-Fu Dai Institute of Tropical Bioscience and Biotechnology View all articles by this author Wen-Jun Li Sun Yat-sen University State Key Laboratory of Biocontrol View all articles by this author Bao-Zhu Fang Xinjiang Institute of Ecology and Geography View all articles by this author Duqiang Luo Hebei University View all articles by this author Youxing Zhao [email protected] Institute of Tropical Bioscience and Biotechnology View all articles by this author Metrics & Citations Metrics Article Usage 125 views 71 downloads .FvxKWukQNSOunydq8rnd { width: 100px; } Citations Download citation Li Yang, Zi-Peng Wang, Jing-Zhe Yuan, et al. Karstmycins A−H, trichostatin analogues with PTP1B inhibitory activities from Streptomyces sp. DX6D14. Authorea . 15 September 2025. DOI: https://doi.org/10.22541/au.175792346.69860510/v1 If you have the appropriate software installed, you can download article citation data to the citation manager of your choice. Simply select your manager software from the list below and click Download. For more information or tips please see 'Downloading to a citation manager' in the Help menu . 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