Two New Classes of T-Type Calcium Channel Inhibitors with New Chemical Scaffolds from Ganoderma cochlear,Organic Letters

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Two New Classes of T-Type Calcium Channel Inhibitors with New Chemical Scaffolds from Ganoderma cochlear
Organic Letters ( IF 4.9 ) Pub Date : 2015-05-29 00:00:00 , DOI: 10.1021/acs.orglett.5b01353
Feng-Jiao Zhou _{1,

2} , Yin Nian ₃ , Yongming Yan _{1,

4} , Ye Gong ₃ , Qi Luo _{1,

4} , Yu Zhang ₁ , Bo Hou ₁ , Zhi-Li Zuo ₁ , Shu-Mei Wang ₂ , He-Hai Jiang ₃ , Jian Yang _{3,

5} , Yong-Xian Cheng ₁

Affiliation

T-type calcium channel (TTCC) inhibitors hold great potential for the treatment of a variety of neurological disorders. Cochlearoids A–E (1–5), five pairs of dimeric meroterpenoid enantiomers, and cochlearines A (6) and B (7), two pairs of enantiomeric hybrid metabolites, were isolated and characterized from Ganoderma cochlear. Biological evaluation found that compounds (+)-1, (−)-3, and (±)-6 significantly inhibited Ca_v3.1 TTCC and showed noticeable selectivity against Ca_v1.2, Ca_v2.1, Ca_v2.2, and K_v11.1 (hERG) channels.

中文翻译：

两种新类别的T型钙通道抑制剂和来自灵芝的新型化学支架

T型钙通道（TTCC）抑制剂在治疗多种神经系统疾病方面具有巨大潜力。Cochlearoids A-E（1 - 5），5双二聚体meroterpenoid对映体的，和cochlearines A（6）和B（7）中，两对映异构体混合的代谢产物，分离并从特征灵芝耳蜗。生物学评估发现，化合物（+）- 1，（-）- 3和（±）-6显着抑制Ca _v 3.1 TTCC并显示出对Ca _v 1.2，Ca _v 2.1，Ca _v 2.2和K _v的显着选择性11.1（hERG）通道。

更新日期：2015-05-29

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