509-20-6
基本信息
烏頭原鹼
烏頭原總堿
WTYJ對照品
烏頭原堿(標(biāo)準(zhǔn)品)
ACONINE 烏頭原堿
烏頭原堿(滴定法95%)
Jesaconine
ACONINE USP/EP/BP
Aconine (Jesaconine)
20-ethyl-1,6,16-trimethoxy-4-(methoxymethyl)aconitane-3,8,13...
20-Ethyl-1α,6α,16β-trimethoxy-4-(methoxymethyl)aconitane-3α,8,13,14α,15α-pentol
(15S,16S)-20-Ethyl-1α,6α,16-trimethoxy-4-(methoxymethyl)aconitane-3α,8β,13β,14α,15-pentol
Aconitane-3,8,13,14,15-pentol,20-ethyl-1,6,16-trimethoxy-4-(methoxymethyl)-, (1a,3a,6a,14a,15a,16b)-
Aconitane-3,8,13,14,15-pentol, 20-ethyl-1,6,16-trimethoxy-4-(methoxymethyl)-, (1α,3α,6α,14α,15α,16β)-
(1alpha,3alpha,6alpha,14alpha,15alpha,16beta)-20-Ethyl-1,6,16-trimethoxy-4-(methoxymethyl)aconitane-3,8,13,14,15-pentol
物理化學(xué)性質(zhì)
常見問題列表
1)提取:草烏中主要成分為烏頭堿生物堿,將干燥草烏塊根約4.8kg粉碎至約過1~2號篩,粉碎的顆粒分裝到6L的分液漏斗中,用1000mL25%的氨水浸泡藥材2~4小時,再用二氯甲烷浸泡草烏顆粒藥材,浸泡24小時,每隔兩天滲漉一次,總共提取4次,減壓回收溶劑,合并浸膏,稱重得膏率為20.10~23.20g/kg,浸膏4℃保存?zhèn)溆?。?8-19%的HCl溶液超聲溶解草烏浸膏,過濾水液層除去草烏中油狀物,用約40%NaOH溶液沉淀水液層,大量黃白色沉淀出現(xiàn),放冷,過濾沉淀,沉淀冷凍干燥,稱重得黃白色沉淀為7.2~7.9g/kg,4℃保存?zhèn)溆谩?/p>
2)烏頭原堿的分離:取部分NaOH堿液的黃白色沉淀用200-300目硅膠分離,用正己烷/乙酸乙酯為流動相,沖洗硅膠色譜柱。用薄層色譜跟蹤烏頭堿至烏頭堿的點消失即停止柱分離。所得的烏頭堿粗品經(jīng)二氯甲烷重結(jié)晶得到烏頭原堿純品。
NF-κB
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Treatment with Aconine significantly inhibits the RANKL-induced transcriptional activity of NF-κB in a dose-dependent manner. Aconine inhibits RANKL-induced osteoclast differentiation in RAW264.7 cells by suppressing the activation of NF-κB and NFATc1 and the expression of the cell-cell fusion molecule DC-STAMP. Aconine (0.125, 0.25 μM) does not affect the viability of RAW264.7 cells, but dose-dependently inhibits RANKL-induced osteoclast formation and bone resorptive activity. Aconine dose-dependently inhibits the RANKL-induced activation of NF-κB and NFATc1 in RAW264.7 cells, and subsequently reduces the expression of osteoclast-specific genes (c-Src, β3-Integrin, cathepsin K and MMP-9) and the expression of dendritic cell-specific transmembrane protein (DC-STAMP), which plays an important role in cell-cell fusion.