Design, synthesis and biological activity of novel Xuetongsu derivatives as potential anticancer agents by inducing apoptosis
Xuetongsu (XTS, Schisanlactone E) is one of the main active compounds and considered as the star molecule isolated from Kadsura heteroclita (Roxb.) Craib. In order to improve XTS anti-tumour bioactivities, a series of novel XTS derivatives were designed and synthesised by introducing an amide bond a...
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| Format: | Article |
| Language: | English |
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Taylor & Francis Group
2025-12-01
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| Series: | Journal of Enzyme Inhibition and Medicinal Chemistry |
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| Online Access: | https://www.tandfonline.com/doi/10.1080/14756366.2025.2482140 |
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| author | Qi Jiang Hui Zhong Cong Wu Jia Li Jingmin Chen Xudong Zhou Bin Li Huanghe Yu Wei Wang Wenbing Sheng |
| author_facet | Qi Jiang Hui Zhong Cong Wu Jia Li Jingmin Chen Xudong Zhou Bin Li Huanghe Yu Wei Wang Wenbing Sheng |
| author_sort | Qi Jiang |
| collection | DOAJ |
| description | Xuetongsu (XTS, Schisanlactone E) is one of the main active compounds and considered as the star molecule isolated from Kadsura heteroclita (Roxb.) Craib. In order to improve XTS anti-tumour bioactivities, a series of novel XTS derivatives were designed and synthesised by introducing an amide bond at the parent. Anti-proliferative assays on four different human tumour cell lines (BGC-823, HepG-2, HCT-116, and MCF-7) showed that the anti-tumour activities of most derivatives increased greatly compared to the parent XTS, and especially, compounds A-7, A-14, and A-18 exhibited multiple anti-tumour effects. Among them, compound A-7 has the best biological activities on the four tumour cell lines with the IC50 values ranging from 13.86 to 20.71 μM, which could significantly increase the fraction of apoptotic cells according to flow cytometry experience. Further study demonstrated that A-7 could induce apoptosis on HepG-2 cells through influencing the key apoptotic related proteins, such as Bcl-2, Bax, and cleaved Caspase-3. |
| format | Article |
| id | doaj-art-79728f3e436149dfb4f3bfa9303d2517 |
| institution | OA Journals |
| issn | 1475-6366 1475-6374 |
| language | English |
| publishDate | 2025-12-01 |
| publisher | Taylor & Francis Group |
| record_format | Article |
| series | Journal of Enzyme Inhibition and Medicinal Chemistry |
| spelling | doaj-art-79728f3e436149dfb4f3bfa9303d25172025-08-20T02:16:21ZengTaylor & Francis GroupJournal of Enzyme Inhibition and Medicinal Chemistry1475-63661475-63742025-12-0140110.1080/14756366.2025.2482140Design, synthesis and biological activity of novel Xuetongsu derivatives as potential anticancer agents by inducing apoptosisQi Jiang0Hui Zhong1Cong Wu2Jia Li3Jingmin Chen4Xudong Zhou5Bin Li6Huanghe Yu7Wei Wang8Wenbing Sheng9School of Pharmacy, Hunan University of Chinese Medicine, Changsha, ChinaSchool of Pharmacy, Hunan University of Chinese Medicine, Changsha, ChinaSchool of Pharmacy, Hunan University of Chinese Medicine, Changsha, ChinaSchool of Pharmacy, Hunan University of Chinese Medicine, Changsha, ChinaSchool of Pharmacy, Hunan University of Chinese Medicine, Changsha, ChinaSchool of Pharmacy, Hunan University of Chinese Medicine, Changsha, ChinaSchool of Pharmacy, Hunan University of Chinese Medicine, Changsha, ChinaSchool of Pharmacy, Hunan University of Chinese Medicine, Changsha, ChinaSchool of Pharmacy, Hunan University of Chinese Medicine, Changsha, ChinaSchool of Pharmacy, Hunan University of Chinese Medicine, Changsha, ChinaXuetongsu (XTS, Schisanlactone E) is one of the main active compounds and considered as the star molecule isolated from Kadsura heteroclita (Roxb.) Craib. In order to improve XTS anti-tumour bioactivities, a series of novel XTS derivatives were designed and synthesised by introducing an amide bond at the parent. Anti-proliferative assays on four different human tumour cell lines (BGC-823, HepG-2, HCT-116, and MCF-7) showed that the anti-tumour activities of most derivatives increased greatly compared to the parent XTS, and especially, compounds A-7, A-14, and A-18 exhibited multiple anti-tumour effects. Among them, compound A-7 has the best biological activities on the four tumour cell lines with the IC50 values ranging from 13.86 to 20.71 μM, which could significantly increase the fraction of apoptotic cells according to flow cytometry experience. Further study demonstrated that A-7 could induce apoptosis on HepG-2 cells through influencing the key apoptotic related proteins, such as Bcl-2, Bax, and cleaved Caspase-3.https://www.tandfonline.com/doi/10.1080/14756366.2025.2482140Xuetongsuanti-tumor bioactivityapoptosisapoptotic related proteinsmolecular docking |
| spellingShingle | Qi Jiang Hui Zhong Cong Wu Jia Li Jingmin Chen Xudong Zhou Bin Li Huanghe Yu Wei Wang Wenbing Sheng Design, synthesis and biological activity of novel Xuetongsu derivatives as potential anticancer agents by inducing apoptosis Journal of Enzyme Inhibition and Medicinal Chemistry Xuetongsu anti-tumor bioactivity apoptosis apoptotic related proteins molecular docking |
| title | Design, synthesis and biological activity of novel Xuetongsu derivatives as potential anticancer agents by inducing apoptosis |
| title_full | Design, synthesis and biological activity of novel Xuetongsu derivatives as potential anticancer agents by inducing apoptosis |
| title_fullStr | Design, synthesis and biological activity of novel Xuetongsu derivatives as potential anticancer agents by inducing apoptosis |
| title_full_unstemmed | Design, synthesis and biological activity of novel Xuetongsu derivatives as potential anticancer agents by inducing apoptosis |
| title_short | Design, synthesis and biological activity of novel Xuetongsu derivatives as potential anticancer agents by inducing apoptosis |
| title_sort | design synthesis and biological activity of novel xuetongsu derivatives as potential anticancer agents by inducing apoptosis |
| topic | Xuetongsu anti-tumor bioactivity apoptosis apoptotic related proteins molecular docking |
| url | https://www.tandfonline.com/doi/10.1080/14756366.2025.2482140 |
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