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Volume 25
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Article

Antibacterial and Antitumor Activities of Synthesized Sarumine Derivatives

by
Fangzhou Yang
1,2,
Bin Jia
1,
Hongli Wen
1,
Xiufang Yang
1 and
Yangmin Ma
1,*
1
Key Laboratory of Chemical Additives for China National Light Industry, College of Chemistry and Chemical Engineering, Shaanxi University of Science & Technology, Xi’an 710021, China
2
Department of Applied Biology and Chemical Technology and Research Institute for Smart Energy, The Hong Kong Polytechnic University, Hung Hom, Hong Kong, China
*
Author to whom correspondence should be addressed.
Int. J. Mol. Sci. 2024, 25(22), 12412; https://doi.org/10.3390/ijms252212412
Submission received: 31 October 2024 / Revised: 9 November 2024 / Accepted: 14 November 2024 / Published: 19 November 2024
(This article belongs to the Special Issue Application of Natural Products in Biomedicine and Pharmacotherapy: 2nd Edition)
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Abstract

Our aim in this study was to explain the biological activity of the latest azafluoranthene. The natural product sarumine (12) and its derivatives (13–17) were synthesized and evaluated for their antibacterial and antitumor activities. The synthesis involved a simplified reaction pathway based on biaryl-sulfonamide-protected cyclization, and the compounds were characterized and studied using spectroscopic methods (1HNMR and 13CNMR). Most of the compounds demonstrated improved antibacterial activity. Notably, sarumine demonstrated potent activity against S. aureus and B. subtilis, with an MIC of 8 μg/mL, showing comparable inhibitory effects to the positive control. Furthermore, molecular simulation studies indicated that sarumine exhibited significant binding affinity to FabH. The inhibitory effect of Cl was superior to the others on the structure, and the antitumor activity result also suggested that the inhibitory ability in PC-3 displayed by the R1 derivatives of F and Cl substitutions was better than that of MDA-MB-231. These findings suggest that sarumine and its derivatives may represent new and promising candidates for further study.
Keywords: sarumine; antibacterial activity; total synthesis; molecular dock sarumine; antibacterial activity; total synthesis; molecular dock

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MDPI and ACS Style

Yang, F.; Jia, B.; Wen, H.; Yang, X.; Ma, Y. Antibacterial and Antitumor Activities of Synthesized Sarumine Derivatives. Int. J. Mol. Sci. 2024, 25, 12412. https://doi.org/10.3390/ijms252212412

AMA Style

Yang F, Jia B, Wen H, Yang X, Ma Y. Antibacterial and Antitumor Activities of Synthesized Sarumine Derivatives. International Journal of Molecular Sciences. 2024; 25(22):12412. https://doi.org/10.3390/ijms252212412

Chicago/Turabian Style

Yang, Fangzhou, Bin Jia, Hongli Wen, Xiufang Yang, and Yangmin Ma. 2024. "Antibacterial and Antitumor Activities of Synthesized Sarumine Derivatives" International Journal of Molecular Sciences 25, no. 22: 12412. https://doi.org/10.3390/ijms252212412

APA Style

Yang, F., Jia, B., Wen, H., Yang, X., & Ma, Y. (2024). Antibacterial and Antitumor Activities of Synthesized Sarumine Derivatives. International Journal of Molecular Sciences, 25(22), 12412. https://doi.org/10.3390/ijms252212412

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