1. Monoterpene Indole Alkaloids with Ca v 3.1 T-Type Calcium Channel Inhibitory Activity from Catharanthus roseus .
- Author
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Deng ZT, Li WY, Wang L, Zhou ZP, Wu XD, Ding ZT, and Zhao QS
- Subjects
- Calcium Channel Blockers chemistry, Calcium Channels, T-Type metabolism, Dose-Response Relationship, Drug, Indole Alkaloids chemistry, Molecular Conformation, Molecular Docking Simulation, Molecular Dynamics Simulation, Molecular Structure, Monoterpenes chemistry, Plant Extracts chemistry, Structure-Activity Relationship, Calcium Channel Blockers pharmacology, Calcium Channels, T-Type chemistry, Catharanthus chemistry, Indole Alkaloids pharmacology, Monoterpenes pharmacology, Plant Extracts pharmacology
- Abstract
Catharanthus roseus is a well-known traditional herbal medicine for the treatment of cancer, hypertension, scald, and sore in China. Phytochemical investigation on the twigs and leaves of this species led to the isolation of two new monoterpene indole alkaloids, catharanosines A ( 1 ) and B ( 2 ), and six known analogues ( 3 - 8 ). Structures of 1 and 2 were established by
1 H-,13 C- and 2D-NMR, and HREIMS data. The absolute configuration of 1 was confirmed by single-crystal X-ray diffraction analysis. Compound 2 represented an unprecedented aspidosperma-type alkaloid with a 2-piperidinyl moiety at C-10. Compounds 6 - 8 exhibited remarkable Cav 3.1 low voltage-gated calcium channel (LVGCC) inhibitory activity with IC50 values of 11.83 ± 1.02, 14.3 ± 1.20, and 14.54 ± 0.99 μM, respectively.- Published
- 2021
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