Brevilin A

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

Brevilin A 是一种从 Centipeda minima 中分离出来的倍半萜内酯，可抑制 janus 激酶活性并阻断癌细胞中的 STAT3 信号传导，具有抗肿瘤活性。

Brevilin A is a sesquiterpene lactone isolated from Centipeda minima, inhibits janus kinase activity and blocks STAT3 signaling in cancer cells with anti-tumor activity.?Brevilin A is a selective inhibitor of JAK-STAT signal pathway by attenuating the JAKs activity and blocking STAT3 signaling (IC50 =?10.6 μM) in Cancer Cells.Brevilin A induces apoptosis and autophagy via mitochondrial pathway and PI3K/AKT/mTOR inactivation in colon adenocarcinoma cell CT26.antitumourIn vitro activity against Giardia intestinalis was used for bioassay-guided fractionation of crude extracts from C. minima.?The sesquiterpene lactone, Brevilin A was isolated and found to have antigiardial activity (IC50 = 16.1 μM) and was similarly active in vitro against Entamoeba histolytica (IC50 between 4.5 and 9 μM) and against Plasmodium falciparum (IC50 = 9.42 μM).?

Cell Viability Assay Cell Line:A549R cells Concentration:1-20 μM Incubation Time:24 hours Result:Exhibited STAT3 signaling inhibition in a dose dependent manner with IC50 value of 10.6 μM.Cell Proliferation Assay Cell Line:CNE-2 cells Concentration:0-50 μM Incubation Time:24, 48, and 72 hours Result:Showed IC50 values in CNE-2 cells with treatment times of 24, 48, and 72 h of 7.93, 2.60, and 22.26 μM, respectively.Apoptosis Analysis Cell Line:DU145 and MDA-MB-468 cells Concentration:10 μM Incubation Time:24 and 48 hours Result:Decreased c-Myc and CyclinD1 after 24 h and 48 h treatment, increased cleaved PARP after 24 h treatment.Western Blot Analysis Cell Line:A549R cells Concentration:12.5 and 25 μM Incubation Time:24 hours Result:Inhibits STAT3 phosphorylation in A549R cells.

Animal Model:Male BALB/c nude mice injected with CNE-2 cellsDosage:10 and 20 mg/kg Administration:Oral gavage; 10 and 20 mg/kg; once daily; 16 days Result:Decreased average tumor volumes and weights treated with 20 mg/kg by 36.3% and 46.0%, respectively, compared to vehicle control.Inhibited the protein expression of p-AKT and p-STAT3 at both low and high doses.

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Microbiology/Virology

Antifection

Antifection|JAK|STAT

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16503-32-5

346.41

C20H26O5

>98% (HPLC)

DMSO:100 mg/mL (288.67 mM; Need ultrasonic)

C/C=C(C)\C(O[C@H]1[C@@]([C@@H]2C)([H])[C@@](OC2=O)([H])C[C@@H](C)[C@@]3([H])[C@]1(C(C=C3)=O)C)=O

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(-20℃)

With Ice Pack

≥ 2 years