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Kansuinine A Sale

(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。

Kansuinine A Chemical Structure

Cas No.:57701-86-7

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5 mg
¥4,482.00
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10 mg
¥7,515.00
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产品描述

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.

Chemical Properties

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
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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
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Research Update

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.