Category: bromides-buliding-blocksIn 2021 ,《Synthesis and anti-inflammatory activity of saponin derivatives of δ-oleanolic acid》 was published in European Journal of Medicinal Chemistry. The article was written by Liu, Liu; Li, Haobin; Hu, Kaiwen; Xu, Qinglong; Wen, Xiaoan; Cheng, Keguang; Chen, Caiping; Yuan, Haoliang; Dai, Liang; Sun, Hongbin. The article contains the following contents:
Pentacyclic triterpenes (PTs) are the active ingredients of many medicinal herbs and pharmaceutical formulations, and are well-known for their anti-inflammatory activity. Recently, the anti-inflammatory effects of AMP-activated protein kinase (AMPK) have also drawn much attention. In this study, the authors found that a variety of naturally occurring PTs sapogenins and saponins could stimulate the phosphorylation of AMPK, and identified δ-oleanolic acid as a potent AMPK activator. Based on these findings, 23 saponin derivatives of δ-oleanolic acid were synthesized in order to find more potent anti-inflammatory agents with improved pharmacokinetic properties. The results of cellular assays showed that saponin I significantly inhibited LPS-induced secretion of pro-inflammatory factors TNF-α and IL-6 in THP1-derived macrophages. Preliminary mechanistic studies showed that I stimulated the phosphorylation of AMPK and acetyl-CoA carboxylase (ACC). The bioavailability of I was significantly improved in comparison with its aglycon. More importantly, I showed significant anti-inflammatory and liver-protective effects in LPS/D-GalN-induced fulminant hepatic failure mice. Taken together, PTs saponins hold promise as therapeutic agents for inflammatory diseases. In the experiment, the researchers used many compounds, for example, (2R,3R,4S,5S,6S)-2-Bromo-6-(methoxycarbonyl)tetrahydro-2H-pyran-3,4,5-triyl triacetate(cas: 21085-72-3Category: bromides-buliding-blocks)
(2R,3R,4S,5S,6S)-2-Bromo-6-(methoxycarbonyl)tetrahydro-2H-pyran-3,4,5-triyl triacetate(cas: 21085-72-3) may be used for the synthesis of HMR1098-S-Glucuronide Methyl Ester, a new K-ATP-blocking agent being developed as a drug for prevention of sudden cardiac death.Category: bromides-buliding-blocks
Referemce:
Bromide – Wikipedia,
bromide – Wiktionary