苍耳亭

用途药理抗肿瘤研究生物活性靶点体外研究体内研究

苍耳亭

CAS号:26791-73-1
英文名:xanthatin
中文名:苍耳亭
CBNumber:CB51390675
分子式:C15H18O3
分子量:246.3
MOL File:26791-73-1.mol

苍耳亭化学性质

熔点 :114.5-115°
比旋光度 :D30 -20° (ethanol)
储存条件 :2-8°C
沸点 :444.3±45.0 °C(Predicted)
密度 :1.10±0.1 g/cm3(Predicted)

苍耳亭性质、用途与生产工艺

用途
苍耳亭（标准品）用于含量测定、鉴别、药理实验、活性筛选等。
药理抗菌、消炎作用、祛风散热,除湿解毒。
抗肿瘤研究
苍耳子的毒性源于其富含的倍半帖内酯类化合物,这类成分常含有α,β不饱和y内酯结构,是其生物活性的一个主要基团。研究表明，从苍耳属(Xanthium L.)植物(如苍耳子)中提取得到的倍半黏内酯化合物苍耳亭( Xanthatin),在体内外实验中均显示出较强的抗肿瘤活性,其对非小细胞肺癌的生长存在显著的抑制作用,且对正常肺上皮细胞生长影响较小。
生物活性 Xanthatin 从 Xanthium strumarium 叶子中提取，诱导细胞凋亡 (apoptosis)。Xanthatin 通过抑制 PGE2 的合成和 5-脂氧合酶的活性而显示出抗炎活性。Xanthatin 抑制布鲁氏菌的 IC50 值为 2.63 μg/ mL，对寄生虫特异性锥虫硫磷还原酶具有不可逆的弱抑制作用。
靶点

IC50: apoptosis; 3.8 μM (VEGFR2 kinase); 2.63 µg/mL ( T. b. brucei )

体外研究

Xanthatin is against T. b. brucei with an IC ₅₀ value of 2.63 µg/mL and exhibits weak irreversible inhibition of parasite specific trypanothione reductase.Xanthatin (0-40 μM; 24 hours) has obscure inhibition effect on the proliferation of HUVEC in the absence of VEGF.Xanthatin (5-40 μM; 24 hours) inhibits breast cancer cell proliferation in a dose responsive manner. Xanthatin inhibits HCC1937, MDA-MB-415, SK-BR-3, MCF-7 and MDA-MB-231 with IC ₅₀ values of 81 μM, 31 μM, 38 μM, 30 μM, and 17 μM, respectively.Xanthatin (0-10 μM; 24 hours) dose dependently suppresses the phosphorylation of STAT3 (Ser727), at the same time, it also results in a rapid dephosphorylation of down-stream kinases of STAT3, including PI3K and Akt, including PI3K (p-PI3K p85 _tyr458 ) and Akt.

Cell Proliferation Assay

Cell Line:	HUVEC cells
Concentration:	0 μM, 5 μM, 10 μM, 15 μM, 20 μM, 30 μM, 40 μM
Incubation Time:	24 hours
Result:	Inhibited cell growth from dose 10 μM in the presence of vEGF.

Cell Viability Assay

Cell Line:	HCC1937, MDA-MB-415, SK-BR-3, MCF-7 and MDA-MB-231 cells
Concentration:	5, 10, 15, 20, 30, and 40 μM
Incubation Time:	24 hours
Result:	Inhibited breast cancer cell growth.

Western Blot Analysis

Cell Line:	HUVEC cells
Concentration:	0, 3, and 10 μM
Incubation Time:	24 hours
Result:	Inhibited VEGFR2 downstream signaling pathways and blocked VEGF-induced STAT3 activation in HUVEC.

体内研究

Xanthatin (intragastric administration; 20 mg/kg; once daily; 25 days) leads to significant inhibition of tumor volume. And this compound is well-tolerated and exhibits no significant difference in weight compares to the vehicle group.

Animal Model:	Transplanted MDA-MB-231 cells into mice and constucted human breast cancer xenograft mouse model
Dosage:	20 mg/kg; once daily; 25 days
Administration:	Intragastric administration
Result:	Supressed tumor growth and tumor angiogenesis in vivo.

化学性质来源于菊科植物苍耳Xanthium sibiricum干燥成熟带总苞的果实
用途用于含量测定/鉴定/药理实验等。
药理药效:抗菌、消炎作用。