Anti-SARS-CoV-2 and anticancer properties of triptolide and its derived carbonized nanomaterials

Rubina Kousar¹, Tahira Akhtar², Chin-Jung Lin³, Timofey Lebedev⁴, Yi-Chuan Li⁵, Chih-Chao Yang⁶, Wei-Jan Wang⁵, Hsiao-Fan Chen⁷, Wen-Chi Su⁸, Pulak Kumar Biswas⁹, Najm Us Saqib⁹, Sefealem Assefa Belay¹, Tzu-Chi Chang⁹, Da-Wei Guo¹⁰, Qiangdu Li¹¹, Bbumba Patrick¹², Muhammad Usama², Chen-Shiou Wu¹³, Wen-Lung Ma¹⁴, Yuh-Pyng Sher¹⁵, Chih-Ching Huang³, Mien-Chie Hung¹⁶, Xing-Guo Li¹⁷

Affiliations

¹ Graduate Institute of Biomedical Sciences, China Medical University, Taichung, 406040, Taiwan; Graduate Institute of Biochemistry and Molecular Biology, China Medical University, Taichung, 406040, Taiwan; Research Center for Cancer Biology, China Medical University, Taichung, 406040, Taiwan; Cancer Biology and Precision Therapeutics Center, China Medical University, Taichung, 406040, Taiwan; Department of Biological Science and Technology, China Medical University, Taichung, 406040, Taiwan.
² Graduate Institute of Biomedical Sciences, China Medical University, Taichung, 406040, Taiwan; Graduate Institute of Biochemistry and Molecular Biology, China Medical University, Taichung, 406040, Taiwan; Research Center for Cancer Biology, China Medical University, Taichung, 406040, Taiwan; Cancer Biology and Precision Therapeutics Center, China Medical University, Taichung, 406040, Taiwan; Institute of Translational Medicine and New Drug Development, China Medical University, Taichung, 406040, Taiwan.
³ Department of Bioscience and Biotechnology, National Taiwan Ocean University, Keelung, 20224, Taiwan.
⁴ Department of Cancer Cell Biology, Engelhardt Institute of Molecular Biology, Russian Academy of Sciences, 119991, Moscow, Russia.
⁵ Research Center for Cancer Biology, China Medical University, Taichung, 406040, Taiwan; Cancer Biology and Precision Therapeutics Center, China Medical University, Taichung, 406040, Taiwan; Department of Biological Science and Technology, China Medical University, Taichung, 406040, Taiwan.
⁶ Department of Biological Science and Technology, China Medical University, Taichung, 406040, Taiwan.
⁷ Graduate Institute of Biomedical Sciences, China Medical University, Taichung, 406040, Taiwan; Research Center for Cancer Biology, China Medical University, Taichung, 406040, Taiwan; Cancer Biology and Precision Therapeutics Center, China Medical University, Taichung, 406040, Taiwan; Graduate Institute of Cell Biology, China Medical University, Taichung, 406040, Taiwan.
⁸ Graduate Institute of Biomedical Sciences, China Medical University, Taichung, 406040, Taiwan; International Master's Program of Biomedical Sciences, China Medical University, Taichung, 406040, Taiwan; Department of Medical Research, China Medical University Hospital, Taichung, 404327, Taiwan.
⁹ Graduate Institute of Biomedical Sciences, China Medical University, Taichung, 406040, Taiwan; Graduate Institute of Biochemistry and Molecular Biology, China Medical University, Taichung, 406040, Taiwan; Research Center for Cancer Biology, China Medical University, Taichung, 406040, Taiwan; Cancer Biology and Precision Therapeutics Center, China Medical University, Taichung, 406040, Taiwan.
¹⁰ Department of Post-Baccalaureate Veterinary Medicine, Asia University, Taichung, 413305, Taiwan.
¹¹ Department of Psychiatry, The Third Municipal Hospital of Weihai, Shandong Province, China.
¹² Graduate Institute of Biomedical Sciences, China Medical University, Taichung, 406040, Taiwan; Graduate Institute of Biochemistry and Molecular Biology, China Medical University, Taichung, 406040, Taiwan; Research Center for Cancer Biology, China Medical University, Taichung, 406040, Taiwan; Cancer Biology and Precision Therapeutics Center, China Medical University, Taichung, 406040, Taiwan; International Master's Program of Biomedical Sciences, China Medical University, Taichung, 406040, Taiwan.
¹³ Graduate Institute of Biomedical Sciences, China Medical University, Taichung, 406040, Taiwan; Graduate Institute of Biochemistry and Molecular Biology, China Medical University, Taichung, 406040, Taiwan; Research Center for Cancer Biology, China Medical University, Taichung, 406040, Taiwan; Cancer Biology and Precision Therapeutics Center, China Medical University, Taichung, 406040, Taiwan; Department of Medical Research, Taichung Veterans General Hospital, Taichung, 407219, Taiwan.
¹⁴ Graduate Institute of Biomedical Sciences, China Medical University, Taichung, 406040, Taiwan.
¹⁵ Graduate Institute of Biomedical Sciences, China Medical University, Taichung, 406040, Taiwan; Graduate Institute of Biochemistry and Molecular Biology, China Medical University, Taichung, 406040, Taiwan; Research Center for Cancer Biology, China Medical University, Taichung, 406040, Taiwan; Cancer Biology and Precision Therapeutics Center, China Medical University, Taichung, 406040, Taiwan; Center for Molecular Medicine, China Medical University Hospital, Taichung, 404327, Taiwan.
¹⁶ Graduate Institute of Biomedical Sciences, China Medical University, Taichung, 406040, Taiwan; Graduate Institute of Biochemistry and Molecular Biology, China Medical University, Taichung, 406040, Taiwan; Research Center for Cancer Biology, China Medical University, Taichung, 406040, Taiwan; Cancer Biology and Precision Therapeutics Center, China Medical University, Taichung, 406040, Taiwan; Center for Molecular Medicine, China Medical University Hospital, Taichung, 404327, Taiwan. Electronic address: mhung@cmu.edu.tw.
¹⁷ Graduate Institute of Biomedical Sciences, China Medical University, Taichung, 406040, Taiwan; Graduate Institute of Biochemistry and Molecular Biology, China Medical University, Taichung, 406040, Taiwan; Research Center for Cancer Biology, China Medical University, Taichung, 406040, Taiwan; Cancer Biology and Precision Therapeutics Center, China Medical University, Taichung, 406040, Taiwan. Electronic address: xli@mail.cmu.edu.tw.

PMID: 40147583
DOI: 10.1016/j.canlet.2025.217677

Free article

Anti-SARS-CoV-2 and anticancer properties of triptolide and its derived carbonized nanomaterials

Rubina Kousar et al. Cancer Lett. 2025.

Free article

. 2025 Jun 1:619:217677.

doi: 10.1016/j.canlet.2025.217677. Epub 2025 Mar 25.

Authors

Affiliations

¹ Graduate Institute of Biomedical Sciences, China Medical University, Taichung, 406040, Taiwan; Graduate Institute of Biochemistry and Molecular Biology, China Medical University, Taichung, 406040, Taiwan; Research Center for Cancer Biology, China Medical University, Taichung, 406040, Taiwan; Cancer Biology and Precision Therapeutics Center, China Medical University, Taichung, 406040, Taiwan; Department of Biological Science and Technology, China Medical University, Taichung, 406040, Taiwan.
² Graduate Institute of Biomedical Sciences, China Medical University, Taichung, 406040, Taiwan; Graduate Institute of Biochemistry and Molecular Biology, China Medical University, Taichung, 406040, Taiwan; Research Center for Cancer Biology, China Medical University, Taichung, 406040, Taiwan; Cancer Biology and Precision Therapeutics Center, China Medical University, Taichung, 406040, Taiwan; Institute of Translational Medicine and New Drug Development, China Medical University, Taichung, 406040, Taiwan.
³ Department of Bioscience and Biotechnology, National Taiwan Ocean University, Keelung, 20224, Taiwan.
⁴ Department of Cancer Cell Biology, Engelhardt Institute of Molecular Biology, Russian Academy of Sciences, 119991, Moscow, Russia.
⁵ Research Center for Cancer Biology, China Medical University, Taichung, 406040, Taiwan; Cancer Biology and Precision Therapeutics Center, China Medical University, Taichung, 406040, Taiwan; Department of Biological Science and Technology, China Medical University, Taichung, 406040, Taiwan.
⁶ Department of Biological Science and Technology, China Medical University, Taichung, 406040, Taiwan.
⁷ Graduate Institute of Biomedical Sciences, China Medical University, Taichung, 406040, Taiwan; Research Center for Cancer Biology, China Medical University, Taichung, 406040, Taiwan; Cancer Biology and Precision Therapeutics Center, China Medical University, Taichung, 406040, Taiwan; Graduate Institute of Cell Biology, China Medical University, Taichung, 406040, Taiwan.
⁸ Graduate Institute of Biomedical Sciences, China Medical University, Taichung, 406040, Taiwan; International Master's Program of Biomedical Sciences, China Medical University, Taichung, 406040, Taiwan; Department of Medical Research, China Medical University Hospital, Taichung, 404327, Taiwan.
⁹ Graduate Institute of Biomedical Sciences, China Medical University, Taichung, 406040, Taiwan; Graduate Institute of Biochemistry and Molecular Biology, China Medical University, Taichung, 406040, Taiwan; Research Center for Cancer Biology, China Medical University, Taichung, 406040, Taiwan; Cancer Biology and Precision Therapeutics Center, China Medical University, Taichung, 406040, Taiwan.
¹⁰ Department of Post-Baccalaureate Veterinary Medicine, Asia University, Taichung, 413305, Taiwan.
¹¹ Department of Psychiatry, The Third Municipal Hospital of Weihai, Shandong Province, China.
¹² Graduate Institute of Biomedical Sciences, China Medical University, Taichung, 406040, Taiwan; Graduate Institute of Biochemistry and Molecular Biology, China Medical University, Taichung, 406040, Taiwan; Research Center for Cancer Biology, China Medical University, Taichung, 406040, Taiwan; Cancer Biology and Precision Therapeutics Center, China Medical University, Taichung, 406040, Taiwan; International Master's Program of Biomedical Sciences, China Medical University, Taichung, 406040, Taiwan.
¹³ Graduate Institute of Biomedical Sciences, China Medical University, Taichung, 406040, Taiwan; Graduate Institute of Biochemistry and Molecular Biology, China Medical University, Taichung, 406040, Taiwan; Research Center for Cancer Biology, China Medical University, Taichung, 406040, Taiwan; Cancer Biology and Precision Therapeutics Center, China Medical University, Taichung, 406040, Taiwan; Department of Medical Research, Taichung Veterans General Hospital, Taichung, 407219, Taiwan.
¹⁴ Graduate Institute of Biomedical Sciences, China Medical University, Taichung, 406040, Taiwan.
¹⁵ Graduate Institute of Biomedical Sciences, China Medical University, Taichung, 406040, Taiwan; Graduate Institute of Biochemistry and Molecular Biology, China Medical University, Taichung, 406040, Taiwan; Research Center for Cancer Biology, China Medical University, Taichung, 406040, Taiwan; Cancer Biology and Precision Therapeutics Center, China Medical University, Taichung, 406040, Taiwan; Center for Molecular Medicine, China Medical University Hospital, Taichung, 404327, Taiwan.
¹⁶ Graduate Institute of Biomedical Sciences, China Medical University, Taichung, 406040, Taiwan; Graduate Institute of Biochemistry and Molecular Biology, China Medical University, Taichung, 406040, Taiwan; Research Center for Cancer Biology, China Medical University, Taichung, 406040, Taiwan; Cancer Biology and Precision Therapeutics Center, China Medical University, Taichung, 406040, Taiwan; Center for Molecular Medicine, China Medical University Hospital, Taichung, 404327, Taiwan. Electronic address: mhung@cmu.edu.tw.
¹⁷ Graduate Institute of Biomedical Sciences, China Medical University, Taichung, 406040, Taiwan; Graduate Institute of Biochemistry and Molecular Biology, China Medical University, Taichung, 406040, Taiwan; Research Center for Cancer Biology, China Medical University, Taichung, 406040, Taiwan; Cancer Biology and Precision Therapeutics Center, China Medical University, Taichung, 406040, Taiwan. Electronic address: xli@mail.cmu.edu.tw.

PMID: 40147583
DOI: 10.1016/j.canlet.2025.217677

Abstract

The COVID-19 pandemic remains an ongoing global health threat, yet effective treatments are still lacking. This has led to a high demand for complementary/alternative medicine, such as Chinese herbal medicines for curbing the COVID-19 pandemic. Given the dual anticancer and antiviral activities of many herbal drugs, they may hold a multifaceted potential to tackle both cancer and SARS-CoV-2. Triptolide is the major bioactive compound isolated from Tripterygium wilfordii Hook F (TwHF), a traditional Chinese medicinal herb recognized for its beneficial pharmacological properties in many diseases, including cancer and viral infection. However, its application in the clinic has been greatly limited due to its toxicity and poor water solubility. Here, from a screen of a natural compound library of Chinese Pharmacopoeia, we identified triptolide as a top candidate to inhibit cell entry of SARS-CoV-2. We demonstrated that triptolide robustly blocked viral entry at nanomolar concentrations in cellular models, with broad range activity against emerging Omicron variants of SARS-CoV-2. Mechanistically, triptolide disrupted the interaction of SARS-CoV-2 spike protein with its receptor ACE2. Furthermore, we synthesized water-soluble, triptolide-derived carbon quantum dots. Compared to triptolide, these highly biocompatible nanomaterials exhibited prominent antiviral capabilities against Omicron variants of SARS-CoV-2 with less cytotoxicity. Finally, we showed that triptolide-derived carbonized materials excelled in their anticancer properties compared to triptolide and Minnelide, a water-soluble analog of triptolide. Together, our results provide a rationale for the potential development of triptolide-carbonized derivatives as a promising antiviral candidate for the current pandemic and future outbreaks, as well as anticancer agents.

Keywords: Angiotensin-converting enzyme 2; Anticancer; Carbon quantum dots; Coronavirus disease 2019; Severe acute respiratory syndrome coronavirus 2; Triptolide.

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Conflict of interest statement

Declaration of competing interest The authors declare that they have no known competing financial interests or personal relationships that could have appeared to influence the work reported in this paper.

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Anti-SARS-CoV-2 and anticancer properties of triptolide and its derived carbonized nanomaterials

Affiliations

Anti-SARS-CoV-2 and anticancer properties of triptolide and its derived carbonized nanomaterials

Authors

Affiliations

Abstract

Conflict of interest statement

MeSH terms

Substances

LinkOut - more resources

Full Text Sources

Miscellaneous