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Prim-O-glucosylcimifugin/升麻甙 {[allProObj[0].p_purity_real_show]}

货号:A540157 同义名: 升麻苷;升麻素苷 / 1''-O-Glucosylcimifugin; Cimifugin beta-D-glucopyranoside

Prim-O-glucosylcimifugin是一种从沙棘根(Saposhnikovia divaricata)中提取的天然产物,能够抑制 TNF-α 刺激下平滑肌细胞的增殖,并通过调节 JAK2/STAT3 信号通路抑制 iNOS 和 COX-2 表达。

Prim-O-glucosylcimifugin/升麻甙 化学结构 CAS号:80681-45-4
Prim-O-glucosylcimifugin/升麻甙 化学结构
CAS号:80681-45-4
Prim-O-glucosylcimifugin/升麻甙 3D分子结构
CAS号:80681-45-4
Prim-O-glucosylcimifugin/升麻甙 化学结构 CAS号:80681-45-4
Prim-O-glucosylcimifugin/升麻甙 3D分子结构 CAS号:80681-45-4
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Prim-O-glucosylcimifugin/升麻甙 纯度/质量文件 产品仅供科研

货号:A540157 标准纯度: {[allProObj[0].p_purity_real_show]}
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产品名称 eNOS iNOS nNOS 其他靶点 纯度
1400W 2HCl +

eNOS, Ki: 50 μM

++++

iNOS, Kd: <7 nM

++

nNOS, Ki: 2 μM

99%+
H-Arg(NO2)-OMe·HCl +++

eNOS, Ki: 39 nM

++

iNOS, Ki: 4.4 μM

+++

nNOS, Ki: 15 nM

98%
1. 鼠标悬停在“+”上可以显示相关IC50的具体数值。"+"越多,抑制作用越强。2. "✔"表示该化合物对相应的亚型有抑制作用,但抑制强度暂时没有相关数据。

Prim-O-glucosylcimifugin/升麻甙 生物活性

描述 Prim-O-glucosylcimifugin is a natural product isolated and purified from the root of Saposhnikovia divaricata (Turcz.) Schischk., which can inhibit the proliferation of SMC(smooth muscle cell) stimulated by TNF-alpha, increase the proportion of G0/G1 phase.

Prim-O-glucosylcimifugin/升麻甙 细胞实验

Cell Line
Concentration Treated Time Description References
B16-F10 cells 50 μM and 100 μM 48 hours To evaluate the effect of POG on apoptosis and proliferation of B16-F10 cells. The results showed that POG exhibited no cytotoxic effect on B16-F10 cells. J Immunother Cancer. 2019 Aug 28;7(1):231.
CD8 T-lymphocytes 50 μM and 100 μM 48 hours To evaluate the effect of POG on apoptosis and proliferation of CD8 T-lymphocytes. The results showed that POG exhibited no cytotoxic effect on CD8 T-lymphocytes and did not affect their proliferation. J Immunother Cancer. 2019 Aug 28;7(1):231.
PMN-MDSCs 50 μM and 100 μM 48 hours To evaluate the effect of POG on apoptosis and proliferation of PMN-MDSCs. The results showed that POG exhibited no cytotoxic effect on PMN-MDSCs but could specifically inhibit the proliferation of PMN-MDSCs. J Immunother Cancer. 2019 Aug 28;7(1):231.
Human tendon stem/progenitor cells (hTSPCs) 20 μmol·L−1 once every 2 days for 7 days POG treatment enhanced colony formation and proliferative capacity of hTSPCs and reduced senescence markers Bone Res. 2023 Oct 23;11(1):54.
Rat tendon stem/progenitor cells (rTSPCs) 20 μmol·L−1 long-term passage from P3 to P12 POG treatment significantly enhanced self-renewal and proliferative capacities of rTSPCs, reduced senescence markers, and restored tenogenic differentiation potential Bone Res. 2023 Oct 23;11(1):54.
RAW 264.7 mouse macrophage cells 12.5, 25, 50 μg/mL 1 hour To evaluate the inhibitory effect of Prim-O-glucosylcimifugin on LPS-induced cytokine production. Results showed that Prim-O-glucosylcimifugin significantly inhibited the production of TNF-α, IL-1β, and IL-6, and increased the level of IL-10. Int Immunopharmacol. 2013 Jun;16(2):139-47.
RAW264.7 cells 12.5, 25, 50 μmol/mL 24 hours POG significantly suppressed the production of inflammatory factors (TNF-α, IL-1β, IL-6) in LPS-induced RAW264.7 cells and inhibited inflammatory responses by suppressing the phosphorylation of ERK1/2, AKT, JNK1/2, IκB-α, P38, and P65. Front Pharmacol. 2022 May 18;13:882924.
Human SGC7901 GC cell line 100 μM To evaluate the inhibitory effects of POG and its metabolite cimifugin on COX-2 expression, results showed that POG and cimifugin downregulated COX-2 expression Biomol Ther (Seoul). 2016 Jul 1;24(4):418-25.
A549/DDP cells 0–10 μM 48 hours Decreased GST activity by ∼5%, decreased GSTPi1 expression by ∼18%, decreased GSTM1 expression by ∼50%, increased intracellular platinum accumulation by ∼30%, enhanced cell apoptosis by ∼10% Front Pharmacol. 2021 May 28;12:678126.
A549 cells 0–10 μM 48 hours Decreased GST activity by ∼10%, decreased GSTPi1 expression by ∼33%, decreased GSTM1 expression by ∼70%, increased intracellular platinum accumulation by ∼56%, enhanced cell apoptosis by ∼10% Front Pharmacol. 2021 May 28;12:678126.

Prim-O-glucosylcimifugin/升麻甙 动物实验

Species
Animal Model
Administration Dosage Frequency Description References
C57BL/6 mice B16-F10 melanoma model Intraperitoneal injection 100 mg/kg/day and 200 mg/kg/day Once daily for 14 days To evaluate the dose-dependent effect of POG on B16-F10 tumor growth. The results showed that POG significantly inhibited tumor growth in a dose-dependent manner, and 200 mg/kg had no significant effect on the body weight of mice. J Immunother Cancer. 2019 Aug 28;7(1):231.
Rats Partial transection tendon injury model in 18-month-old rats Oral 50 mg/kg body weight per day Once daily for 2 months Oral POG significantly improved tendon self-healing capacity in aged rats, reducing inflammation and senescence markers Bone Res. 2023 Oct 23;11(1):54.
BALB/c male mice LPS-induced acute lung injury model Intraperitoneal injection 2.5, 5, 10 mg/kg Single dose, lasting 7 hours To evaluate the protective effect of Prim-O-glucosylcimifugin on LPS-induced acute lung injury. Results showed that Prim-O-glucosylcimifugin significantly reduced inflammatory cell infiltration, edema, and MPO activity in lung tissues, and improved histopathological changes. Int Immunopharmacol. 2013 Jun;16(2):139-47.
C57BL/6 mice DSS-induced ulcerative colitis model Intraperitoneal injection 2.5, 5, 10 mg/kg 7 consecutive days POG improved clinical scores, colonic length, and body weight in DSS-induced ulcerative colitis mice, repaired pathological damage to the intestinal mucosa, inhibited levels of inflammatory factors (IL-1β, TNF-α, IL-6), and repaired the intestinal immune barrier by upregulating the expression of tight junction proteins (Occludin, Claudin-3, ZO-1). Additionally, POG regulated the richness and structure of intestinal microbiota. Front Pharmacol. 2022 May 18;13:882924.
Wistar rats Formalin-induced tonic nociceptive response model and CFA-induced rat arthritis pain model Subcutaneous injection 1, 3, 10, 30 mg/kg Single dose or consecutive administration for 7 days To evaluate the anti-nociceptive effects of POG in inflammatory nociception, results showed that POG dose-dependently inhibited nociceptive responses without tolerance, reduced serum TNFα, IL-1β, and IL-6 levels, and decreased spinal PGE2 and COX-2 expression Biomol Ther (Seoul). 2016 Jul 1;24(4):418-25.

Prim-O-glucosylcimifugin/升麻甙 参考文献

[1]Song J, Zheng SR, et al. Pharmacokinetic Interaction of astragaloside IV with atractylenolide I and prim-O-glucosylcimifugin in male Sprague Dawley rats. Planta Med. 2014 Feb;80(2-3):187-92.

[2]Li Y, Zhao L, et al. Comparative pharmacokinetics of prim-O-glucosylcimifugin and cimifugin by liquid chromatography-mass spectrometry after oral administration of Radix Saposhnikoviae extract, cimifugin monomer solution and prim-O-glucosylcimifugin monomer solution to rats. Biomed Chromatogr. 2012 Oct;26(10):1234-40.

Prim-O-glucosylcimifugin/升麻甙 实验方案

计算器
存储液制备 1mg 5mg 10mg

1 mM

5 mM

10 mM

2.13mL

0.43mL

0.21mL

10.67mL

2.13mL

1.07mL

21.35mL

4.27mL

2.13mL

Prim-O-glucosylcimifugin/升麻甙 技术信息

CAS号80681-45-4
分子式C22H28O11
分子量 468.45
SMILES Code CC([C@@H]1CC2=C(OC)C(C(C=C(O3)CO[C@@]4([H])[C@H](O)[C@@H](O)[C@H](O)[C@H](O4)CO)=O)=C3C=C2O1)(O)C
MDL No. MFCD09037394
别名 升麻苷;升麻素苷 ;1''-O-Glucosylcimifugin; Cimifugin beta-D-glucopyranoside; PGCN; Cimifugin 7-glucoside
运输蓝冰
InChI Key XIUVHOSBSDYXRG-UVTAEQIVSA-N
Pubchem ID 14034912
存储条件

In solvent -20°C: 3-6个月 -80°C: 12个月

Pure form Sealed in dry, 2-8°C

溶解方案

DMSO: 145 mg/mL(309.53 mM),注意:DMSO长时间开封后,会吸水并导致溶解能力下降,请避免使用长期开封的DMSO

请根据您的动物给药指南选择适当的溶解方案。
以下溶解方案都请先按照体外实验的方式配制澄清的储备液,再依次添加助溶剂:
——为保证实验结果的可靠性,澄清的储备液可以根据储存条件,适当保存;体内实验的工作液,建议现用现配,当天使用; 以下溶剂前显示的百分比是指该溶剂在终溶液中的体积占比;如在配制过程中出现沉淀、析出现象,可以通过加热和/或超声的方式助溶
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