从 中分离得到具有 Ca3.1T 型钙通道抑制活性的单萜吲哚生物碱。
Monoterpene Indole Alkaloids with Ca3.1 T-Type Calcium Channel Inhibitory Activity from .
机构信息
Key Laboratory of Medicinal Chemistry for Natural Resource, Ministry of Education and Yunnan Province, School of Chemical Science and Technology, Yunnan University, Kunming 650091, China.
State Key Laboratory of Phytochemistry and Plant Resources in West China, Kunming Institute of Botany, Chinese Academy of Sciences, Kunming 650201, China.
出版信息
Molecules. 2021 Oct 28;26(21):6516. doi: 10.3390/molecules26216516.
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 () and B (), and six known analogues (-). Structures of and were established by H-, C- and 2D-NMR, and HREIMS data. The absolute configuration of was confirmed by single-crystal X-ray diffraction analysis. Compound represented an unprecedented aspidosperma-type alkaloid with a 2-piperidinyl moiety at C-10. Compounds - exhibited remarkable Ca3.1 low voltage-gated calcium channel (LVGCC) inhibitory activity with IC values of 11.83 ± 1.02, 14.3 ± 1.20, and 14.54 ± 0.99 μM, respectively.
是一种在中国用于治疗癌症、高血压、烫伤和溃疡的知名传统草药。对该物种的嫩枝和叶子的植物化学研究导致分离出两种新的单萜吲哚生物碱，卡特兰辛 A()和 B()，以及六种已知类似物 (-)。和的结构通过 H-、C- 和 2D-NMR 以及 HREIMS 数据确定。的绝对构型通过单晶 X 射线衍射分析确定。化合物代表了一种前所未有的阿皮斯多马型生物碱，在 C-10 位具有 2-哌啶基部分。化合物 - 表现出显著的 Ca3.1 低电压门控钙通道 (LVGCC) 抑制活性，IC 值分别为 11.83 ± 1.02、14.3 ± 1.20 和 14.54 ± 0.99 μM。
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