Institute for Inheritance-Based Innovation of Chinese Medicine, School of Pharmaceutical Sciences, Health Science Center, Shenzhen University, Shenzhen 518060, PR China.
School of Pharmacy, Lanzhou University, Lanzhou 730000, PR China.
J Org Chem. 2022 Jun 17;87(12):7643-7648. doi: 10.1021/acs.joc.2c00145. Epub 2022 Jun 5.
Aquilarines A () and B (), two unprecedented sesquiterpenoid-chromone heterohybrids, were isolated from agarwood. is an alkaloid featuring an unusual pyridine nucleus, and possesses a rare sesquiterpenoid-chromone skeleton via a C-C bond. A plausible biosynthetic pathway for and was proposed. Both and could significantly inhibit the expression of extracellular matrix components, and α-SMA at low concentrations in TGF-β1 induced two types of kidney cells (NRK 52E and NRK 49F) featuring selective inhibition of Smad3 instead of Smad2 phosphorylation, showing their potential in renal fibrosis.
水黄皮素 A()和 B()，两种前所未有的倍半萜-色酮杂合体，从琼脂木中分离得到。 是一种具有不寻常吡啶核的生物碱， 具有罕见的倍半萜-色酮骨架，通过 C-C 键连接。提出了 和 的可能生物合成途径。 和 在低浓度时均能显著抑制 TGF-β1诱导的两种肾细胞（NRK 52E 和 NRK 49F）中细胞外基质成分和 α-SMA 的表达，选择性抑制 Smad3而不是 Smad2 的磷酸化，显示了它们在肾纤维化中的潜力。
