烏頭原堿
| 中文名稱 | 烏頭原堿 |
|---|---|
| 中文同義詞 | 烏頭原鹼;烏頭原堿;烏頭原堿(標(biāo)準(zhǔn)品);烏頭原堿(滴定法95%);ACONINE 烏頭原堿;烏頭原總堿;WTYJ對(duì)照品;烏頭原堿(對(duì)照品) |
| 英文名稱 | ACONINE |
| 英文同義詞 | ACONINE;(15S,16S)-20-Ethyl-1α,6α,16-trimethoxy-4-(methoxymethyl)aconitane-3α,8β,13β,14α,15-pentol;20-Ethyl-1α,6α,16β-trimethoxy-4-(methoxymethyl)aconitane-3α,8,13,14α,15α-pentol;(1alpha,3alpha,6alpha,14alpha,15alpha,16beta)-20-Ethyl-1,6,16-trimethoxy-4-(methoxymethyl)aconitane-3,8,13,14,15-pentol;Jesaconine;Aconitane-3,8,13,14,15-pentol,20-ethyl-1,6,16-trimethoxy-4-(methoxymethyl)-, (1a,3a,6a,14a,15a,16b)-;Aconine (Jesaconine);Aconitane-3,8,13,14,15-pentol, 20-ethyl-1,6,16-trimethoxy-4-(methoxymethyl)-, (1α,3α,6α,14α,15α,16β)- |
| CAS號(hào) | 509-20-6 |
| 分子式 | C25H41NO9 |
| 分子量 | 499.6 |
| EINECS號(hào) | |
| 相關(guān)類別 | 生物堿;中草藥成分;植物提取物;中藥對(duì)照品;標(biāo)準(zhǔn)品;對(duì)照品;植提標(biāo)準(zhǔn)品;chemical reagent;pharmaceutical intermediate;phytochemical;reference standards from Chinese medicinal herbs (TCM).;standardized herbal extract;Alkaloids;標(biāo)準(zhǔn)品-中藥標(biāo)準(zhǔn)品;標(biāo)準(zhǔn)品 -中藥標(biāo)準(zhǔn)品;標(biāo)準(zhǔn)品，對(duì)照品 |
| Mol文件 | 509-20-6.mol |
| 結(jié)構(gòu)式 |  |
烏頭原堿 性質(zhì)
| 熔點(diǎn) | 129-131℃ |
|---|---|
| 比旋光度 | D +23° |
| 沸點(diǎn) | 590.79°C (rough estimate) |
| 密度 | 1.42 |
| 折射率 | 1.6000 (estimate) |
| 儲(chǔ)存條件 | -20°C Freezer |
| 溶解度 | 可溶于氯仿（少許）、DMSO（少許） |
| 酸度系數(shù)(pKa) | 9.52(at 25℃) |
| 形態(tài) | 固體 |
| 顏色 | 灰白色至淺黃色 |
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(hào)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(shí)，再用二氯甲烷浸泡草烏顆粒藥材，浸泡24小時(shí)，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(dòng)相，沖洗硅膠色譜柱。用薄層色譜跟蹤烏頭堿至烏頭堿的點(diǎn)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。
Aconine 抑制核因子 κB 受體活化劑配體誘導(dǎo)的 NF-κB 激活。|
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.