ROSTAFUROXIN

CAS号:156722-18-8
英文名:(3S,5R,8R,9S,10S,13R,14S,17R)-17-(3-furyl)-10,13-dimethyl-2,3,4,5,6,7, 8,9,11,12,15,16-dodecahydro-1H-cyclopenta[a]phenanthrene-3,14,17-triol
中文名:ROSTAFUROXIN
CBNumber:CB21253997
分子式:C23H34O4
分子量:374.51
MOL File:156722-18-8.mol

ROSTAFUROXIN化学性质

ROSTAFUROXIN性质、用途与生产工艺

生物活性 Rostafuroxin (PST 2238) 是一种洋地黄毒苷衍生物，一种口服有效的 Na+,K+-ATPase (ATP1A1) 抑制剂。Rostafuroxin 与 ATP1A1 胞外域特异性结合，并阻断呼吸道合胞病毒 (RSV) 触发的 EGFR Tyr845 磷酸化。Rostafuroxin 具有抗高血压和抗 RSV 活性。
体外研究

Rostafuroxin (PST 2238) competitively inhibits Ouabain (HY-B0542) binding and signaling. Rostafuroxin antagonizes the molecularand functional effects of Ouabain by reversing the ouabain-induced, Src-dependent Na ⁺ ,K ⁺ -ATPase phosphorylation and activation.
Rostafuroxin (0.125-128 μM; for 24 h post treatment) has less than 20% reduction in cell viability in A549 cells and HSAEC. Rostafuroxin inhibits the expression of RSV-GFP in HSAEC (IC ₅₀ =1.8 μM) and A549 cells (IC ₅₀ =14.8 μM).
Rostafuroxin displaced [ ³ H]Ouabain from the dog kidney Na ⁺ ,K ⁺ -ATPase receptor (IC50=1.5 nM), is devoid of cardiac inotropic activity in isolated guinea pig atria, and shows no affinity up to 10 ^-4 M with general (R1, R2, a1, a2, A1, A2, M1, M2, H1, H2, 5-HT1, 5-HT2, Ca2+ channels, TXA2/PGH2, PAF, GABAA, GABAB, DA-NE-5-HT uptake, glutammate,glycine, benzodiazepine) and hormonal (estrogenic, progestinic, androgenic, mineralcorticoid) receptors.

体内研究

Rostafuroxin (PST 2238; 1 mg/kg/day; gavage; for 3 weeks) decreases SBP and improves acetylcholine-induced relaxation.

Animal Model:	Male 7-week-old Wistar rats
Dosage:	1 mg/kg
Administration:	Gavage; daily; for 3 weeks
Result:	Decreased SBP, improved acetylcholine-induced relaxation via enhanced nitric oxide synthesis and bioavailability, decreased superoxide anion generation from NAD(P)H oxidase and cyclooxygenase-2 and reduced cytoplasmic tyrosine kinase Src phosphorylation.