Novel polycyclic meroterpenoids with protein tyrosine phosphatase 1B inhibitory activity isolated from desert-derived fungi Talaromyces sp. HMT-8

doi:10.1007/s13659-025-00530-x

Natural Products and Bioprospecting ›› 2025, Vol. 15 ›› Issue (5): 46-46.DOI: 10.1007/s13659-025-00530-x

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Novel polycyclic meroterpenoids with protein tyrosine phosphatase 1B inhibitory activity isolated from desert-derived fungi Talaromyces sp. HMT-8

Xin-yi Zhai¹, Jin-jie Liu², Cui-duan Wang¹, Yi-fan Dou¹, Jian-hua Lv¹, Li-an Wang¹, Jin-xiu Zhang¹, Zhuang Li¹

1. College of Life Sciences, Hebei Normal University, Shijiazhuang, 050000, People's Republic of China;
2. School of Land Science and Space Planning, Hebei GEO University, Shijiazhuang, 050000, People's Republic of China

Received:2025-05-30 Online:2025-11-06
Contact: Jin-xiu Zhang,E-mail:xiudou882003@163.com;Zhuang Li,E-mail:lizhuang@hebtu.edu.cn
Supported by:
This work was supported by the Science Research Start-up Fund for Doctor of Hebei Normal University (grant numbers L2023B22 and L2024B16); Hebei Province Agricultural Science and Technology Achievement Transformation Fund Project (grant numbers 2025JNZ-S25); and the HeBei Edible Fungi Innovation Team of Modern Seed Industry Science and Technology (grant numbers 21326315D).

Novel polycyclic meroterpenoids with protein tyrosine phosphatase 1B inhibitory activity isolated from desert-derived fungi Talaromyces sp. HMT-8

Xin-yi Zhai¹, Jin-jie Liu², Cui-duan Wang¹, Yi-fan Dou¹, Jian-hua Lv¹, Li-an Wang¹, Jin-xiu Zhang¹, Zhuang Li¹

1. College of Life Sciences, Hebei Normal University, Shijiazhuang, 050000, People's Republic of China;
2. School of Land Science and Space Planning, Hebei GEO University, Shijiazhuang, 050000, People's Republic of China

通讯作者: Jin-xiu Zhang,E-mail:xiudou882003@163.com;Zhuang Li,E-mail:lizhuang@hebtu.edu.cn
基金资助:
This work was supported by the Science Research Start-up Fund for Doctor of Hebei Normal University (grant numbers L2023B22 and L2024B16); Hebei Province Agricultural Science and Technology Achievement Transformation Fund Project (grant numbers 2025JNZ-S25); and the HeBei Edible Fungi Innovation Team of Modern Seed Industry Science and Technology (grant numbers 21326315D).

Abstract

Abstract: Seven previously undescribed polycyclic meroterpenoids talarines K-Q (1-7), along with five known ones (8-12), were isolated from desert-derived fungi Talaromyces sp. HMT-8. The structure of the novel compounds were elucidated using spectroscopic methods, including electronic circular dichroism (ECD), HRESIMS and nuclear magnetic resonance (NMR) spectroscopy. Among the isolated meroterpenoids, compounds 3, 5, and 7 exhibited rare chlorine substitution patterns. Halogenation, particularly chlorination, is uncommon in natural meroterpenoids and implies the involvement of halogenase enzymes during biosynthesis. Compounds 1-12 were evaluated for their inhibitory activity against protein tyrosine phosphatase 1B (PTP1B). Compounds 1-4 and 12 exhibited inhibitory activity against PTP1B with IC₅₀ values ranging from 1.74 to 17.60 μM. Among them, compounds 2 and 12 displayed significant inhibitory effects with an IC₅₀ value of 1.74 and 3.03 μM, respectively. Furthermore, Molecular docking analysis revealed that compounds 2 and 12 bind tightly to the catalytic site of PTP1B, forming key hydrogen bonding and hydrophobic interactions. Enzyme kinetics studies further demonstrated that both compounds act as competitive inhibitor.

Key words: Talaromyces sp., Polycyclic meroterpenoids, PTP1B, Enzyme kinetics, Molecular docking

摘要： Seven previously undescribed polycyclic meroterpenoids talarines K-Q (1-7), along with five known ones (8-12), were isolated from desert-derived fungi Talaromyces sp. HMT-8. The structure of the novel compounds were elucidated using spectroscopic methods, including electronic circular dichroism (ECD), HRESIMS and nuclear magnetic resonance (NMR) spectroscopy. Among the isolated meroterpenoids, compounds 3, 5, and 7 exhibited rare chlorine substitution patterns. Halogenation, particularly chlorination, is uncommon in natural meroterpenoids and implies the involvement of halogenase enzymes during biosynthesis. Compounds 1-12 were evaluated for their inhibitory activity against protein tyrosine phosphatase 1B (PTP1B). Compounds 1-4 and 12 exhibited inhibitory activity against PTP1B with IC₅₀ values ranging from 1.74 to 17.60 μM. Among them, compounds 2 and 12 displayed significant inhibitory effects with an IC₅₀ value of 1.74 and 3.03 μM, respectively. Furthermore, Molecular docking analysis revealed that compounds 2 and 12 bind tightly to the catalytic site of PTP1B, forming key hydrogen bonding and hydrophobic interactions. Enzyme kinetics studies further demonstrated that both compounds act as competitive inhibitor.

关键词: Talaromyces sp., Polycyclic meroterpenoids, PTP1B, Enzyme kinetics, Molecular docking

Xin-yi Zhai, Jin-jie Liu, Cui-duan Wang, Yi-fan Dou, Jian-hua Lv, Li-an Wang, Jin-xiu Zhang, Zhuang Li. Novel polycyclic meroterpenoids with protein tyrosine phosphatase 1B inhibitory activity isolated from desert-derived fungi Talaromyces sp. HMT-8[J]. Natural Products and Bioprospecting, 2025, 15(5): 46-46.

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Novel polycyclic meroterpenoids with protein tyrosine phosphatase 1B inhibitory activity isolated from desert-derived fungi Talaromyces sp. HMT-8

Novel polycyclic meroterpenoids with protein tyrosine phosphatase 1B inhibitory activity isolated from desert-derived fungi Talaromyces sp. HMT-8

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