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Monoterpene Indole Alkaloids with Cav3.1 T-Type Calcium Channel Inhibitory Activity from Catharanthus roseus.


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 1H-, 13C- 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 Cav3.1 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.

SUBMITTER: Deng ZT 

PROVIDER: S-EPMC8587030 | biostudies-literature | 2021 Oct

REPOSITORIES: biostudies-literature

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Monoterpene Indole Alkaloids with Ca<sub>v</sub>3.1 T-Type Calcium Channel Inhibitory Activity from <i>Catharanthus roseus</i>.

Deng Zhen-Tao ZT   Li Wen-Yan WY   Wang Lei L   Zhou Zhi-Ping ZP   Wu Xing-De XD   Ding Zhong-Tao ZT   Zhao Qin-Shi QS  

Molecules (Basel, Switzerland) 20211028 21


<i>Catharanthus roseus</i> 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 (<b>1</b>) and B (<b>2</b>), and six known analogues (<b>3</b>-<b>8</b>). Structures of <b>1</b> and <b>2</b> were established by <sup>1</sup>H-, <sup>13</sup>C- and 2D-NMR, and HREIMS data. The absolute configura  ...[more]

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