Kansuinine A
(Synonyms: 甘遂萜酯A) 目录号 : GC62527
Kansuinine A 抑制 IL-6 诱导的 Stat3 的激活。Kansuinine A 有抗病毒和抗肿瘤活性。
Cas No.:57701-86-7
Sample solution is provided at 25 µL, 10mM.
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Quality Control & SDS
- View current batch:
- Purity: >99.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Kansuinine A inhibits IL-6-induced Stat3 activation. Kansuinine A possesses antiviral and anticancer activity[1][2].
[1]. Jong Sun Chang, et al. Kansuinine A and Kansuinine B from Euphorbia kansui L. inhibit IL-6-induced Stat3 activation. Planta Med. 2010 Oct;76(14):1544-9.
[2]. Xiaoyun Shu, et al. Bioassay-guided separation of the proinflammatory constituents from the roots of Euphorbia kansui. J Nat Med. 2010 Jan;64(1):98-103.
| Cas No. | 57701-86-7 | SDF | |
| 别名 | 甘遂萜酯A | ||
| 分子式 | C37H46O15 | 分子量 | 730.75 |
| 溶解度 | DMSO : ≥ 100 mg/mL (136.85 mM) | 储存条件 | Store at -20°C |
| General tips | 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。 储备液的保存方式和期限：-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。 为了提高溶解度，请将管子加热至37℃，然后在超声波浴中震荡一段时间。 |
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| Shipping Condition | 评估样品解决方案：配备蓝冰进行发货。所有其他可用尺寸：配备RT，或根据请求配备蓝冰。 | ||
| 制备储备液 | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 1.3685 mL | 6.8423 mL | 13.6846 mL |
| 5 mM | 0.2737 mL | 1.3685 mL | 2.7369 mL |
| 10 mM | 0.1368 mL | 0.6842 mL | 1.3685 mL |
| 第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量） | ||||||||||
| 给药剂量 | mg/kg |  |
动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
| 第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系GLPBIO为您提供正确的澄清溶液配方） | ||||||||||
| % DMSO % % Tween 80 % saline | ||||||||||
| 计算重置 | ||||||||||
计算结果:
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，
体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL saline，混匀澄清。
1. 首先保证母液是澄清的；
2.
一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
3. 以上所有助溶剂都可在 GlpBio 网站选购。
LC-MS/MS method for determination of Kansuinine A in rat plasma and its application to a rat pharmacokinetic study
Biomed Chromatogr 2022 Mar;36(3):e5282.PMID:34806205DOI:10.1002/bmc.5282.
Kansuinine A is a macrocyclic jatrophane diterpene isolated from the plant Euphorbia kansui Liou. It exhibits many pharmacological activities including cytoxic, antitumor, antiallergic and proinflammatory effects. In the present study, a simple and sensitive LC-MS/MS method was established and validated for the determination of Kansuinine A in rat plasma. After methanol-mediated protein precipitation, chromatographic separation was achieved on an Acquity BEH C18 column (2.1 × 100 mm, 1.7 μm) using acetonitrile and 0.1% formic acid in water as mobile phase by gradient elution. Kansuinine A and IS were quantified in negative multiple reaction monitoring mode with ion transitions at m/z 731.1-693.2 for Kansuinine A and m/z 723.2-623.1 for IS. The method showed excellent linearity over the range 1-500 ng/ml. The intra- and inter-day precisions (relative standard deviation) were 2.13-4.28 and 3.83-7.67%, respectively, whereas accuracy (relative error) ranged from -4.17 to 3.73%. The extraction recovery, stability and matrix effect met the requirement of the regulations issued by the US Food and Drug Administration. The validated method was successfully applied to the pre-clinical pharmacokinetic study of Kansuinine A in rats after oral administration (20 mg/kg) and intravenous administration (2 mg/kg). This study provides valuable reference for the further study of E. kansui liou, especially for the drug development and clinical application of Kansuinine A.
Kansuinine A and Kansuinine B from Euphorbia kansui L. inhibit IL-6-induced Stat3 activation
Planta Med 2010 Oct;76(14):1544-9.PMID:20379953DOI:10.1055/s-0030-1249805.
The current study was performed to examine the mechanisms underlying the potential effects of E. KANSUI on IL-6-induced cellular signaling in human hepatoma cells. We found that two diterpenoids, Kansuinine A and B, from E. KANSUI have an inhibitory effect on IL-6-induced Stat3 activation by activating ERK1/2. Inhibition of MEK significantly blocked the effects of Kansuinine A and B on IL-6-induced Stat3 activation and tyrosine phosphorylation. These results suggest that blocking of IL-6-induced signal transduction is partially due to the sustained activation of ERK1/2 by Kansuinine A and B, which in turn results in an increase of Stat3 serine phosphorylation and SOCS-3 expression. Treatment with Kansuinine A and B represents a novel method to block these IL-6-induced effects.
Kansuinine A Ameliorates Atherosclerosis and Human Aortic Endothelial Cell Apoptosis by Inhibiting Reactive Oxygen Species Production and Suppressing IKKβ/IκBα/NF-κB Signaling
Int J Mol Sci 2021 Sep 24;22(19):10309.PMID:34638650DOI:10.3390/ijms221910309.
Reactive oxygen species (ROS)-induced vascular endothelial cell apoptosis is strongly associated with atherosclerosis progression. Herein, we aimed to examine whether Kansuinine A (KA), extracted from Euphorbia kansui L., prevents atherosclerosis development in a mouse model and inhibits cell apoptosis through oxidative stress reduction. Atherosclerosis development was analyzed in apolipoprotein E-deficient (ApoE-/-) mice fed a high-fat diet (HFD) using Oil Red O staining and H&E staining. Human aortic endothelial cells (HAECs) were treated with KA, followed by hydrogen peroxide (H2O2), to investigate the KA-mediated inhibition of ROS-induced oxidative stress and cell apoptosis. Oil Red O staining and H&E staining showed that atherosclerotic lesion size was significantly smaller in the aortic arch of ApoE-/- mice in the HFD+KA group than that in the aortic arch of those in the HFD group. Further, KA (0.1-1.0 μM) blocked the H2O2-induced death of HAECs and ROS generation. The H2O2-mediated upregulation of phosphorylated IKKβ, phosphorylated IκBα, and phosphorylated NF-κB was suppressed by KA. KA also reduced the Bax/Bcl-2 ratio and cleaved caspase-3 expression, preventing H2O2-induced vascular endothelial cell apoptosis. Our results indicate that KA may protect against ROS-induced endothelial cell apoptosis and has considerable clinical potential in the prevention of atherosclerosis and cardiovascular diseases.
Bioassay-guided separation of the proinflammatory constituents from the roots of Euphorbia kansui
J Nat Med 2010 Jan;64(1):98-103.PMID:19844773DOI:10.1007/s11418-009-0366-0.
In view of the toxic inflammatory reaction induced by Euphorbia kansui roots, a traditional Chinese medicine used for the treatment of edema, ascites, and asthma, the 95% ethanol extract was found to have a significant stimulating effect on inflammatory cells. Bioassay-guided separation of the 95% ethanol extract from the roots of E. kansui led to the isolation of five diterpenoids whose structures were identified by (1)H, (13)C NMR spectroscopy and HR-ESI-MS as kansuinine B (1), Kansuinine A (2), kansuiphorin C (3), 3-O-benzoyl-20-deoxyingenol (4), and 3-O-(2'E,4'Z-decadienoyl)-20-O-acetylingenol (5). The proinflammatory effect of compounds 1-5 was evaluated in vitro in models of inflammation using exoteric mice splenic lymphocytes (SPL) and rat peritoneal macrophages (PMphi). Compounds 1, 2, and 5 markedly promoted SPL proliferation and NO production by PMphi at concentrations from 0.78 to 12.50 microg/mL. Hence the three compounds are believed to be important proinflammatory components of the roots of E. kansui.
Bio-guided isolation of the cytotoxic terpenoids from the roots of Euphorbia kansui against human normal cell lines L-O2 and GES-1
Int J Mol Sci 2012;13(9):11247-11259.PMID:23109850DOI:10.3390/ijms130911247.
The dried roots of Euphorbia kansui (kansui) have been used for centuries in China as a herbal medicine for edema, ascites, and asthma. The 95% ethanol extract showed a significant inhibition of cell proliferation against human normal cell lines L-O2 and GES-1. Bioassay-guided separation of the 95% ethanol extract from the roots of E. kansui led to the isolation of 12 diverse terpenoids whose structures were identified by (1)H, (13)C NMR spectroscopy and ESI-MS as Kansuinine A (1), kansuinine B (2), kansuinine C (3), kansuiphorin C (4), 3-O-(2'E,4'Z-decadienoyl)-20-O-acetylingenol (5), 3-O-(2'E,4'Edecadienoyl)-20-O-acetylingenol (6), 3-O-(2'E,4'Z-decadienoyl)-20-deoxyingenol (7), 3-O-benzoyl-20-deoxyingenol (8), 5-O-benzoyl-20-deoxyingenol (9), kansenone (10), epi-kansenone (11), euphol (12). All these 12 terpernoids were evaluated in vitro for cytotoxicity on L-O2 and GES-1 cell lines. Most ingenane-type diterpenoids and 8-ene-7-one triterpenoids (5-11) exhibited a relatively lower IC(50) value; therefore, these compounds had stronger cytotoxicity against human normal cell lines L-O2 and GES-1 with dose-dependent relationships. These results will be significantly helpful to reveal the mechanism of toxicity of kansui and to effectively guide safer clinical application of this herb.