Oridonin

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

冬凌草甲素是一种活性二萜化合物，具有多种药理活性，包括抗氧化、抗肿瘤和抗炎等。

Oridonin is an active diterpenoid compound isolated from the plant Rabdosia Rrubescens, has various pharmacological activities, including antioxidant, anti-tumor capacities and anti-inflammation; inhibits AKT kinase activity (AKT1 and AKT2 IC50=8.4 and 8.9 uM) and interacts with the ATP-binding pocket of AKT, inhibits growth of ESCC in vitro and patient derived xenografts in vivo; inhibits vascular inflammation by blocking NF-κB and MAPK activation.

Oridonin is an ATP-competitive inhibitor of AKT with IC50s of 8.4 and 8.9 μM for AKT1 and AKT2, respectively. Oridonin (5, 10 or 20 μM) obviously inhibits the growth of KYSE70, KYSE410 and KYSE450 ESCC cells via targeting AKT1/2. Oridonin (10 or 20 μM) causes G2/M phase cell cycle arrest in KYSE70, KYSE410 and KYSE450 cells, and induces apoptosis in these three cell lines at 20 μM. In addition, Oridonin (5, 10 or 20 μM) in combination with cisplatin or 5-FU enhances the inhibition of esophageal squamous cell carcinoma (ESCC) cell growth. Oridonin (0.1 and 1 μM) preferentially suppresses AKT/mTOR signaling. Oridonin (1 μM) also selectively suppresses growth of breast cancer cells with hyperactivation of AKT signaling.

Oridonin (160 mg/kg, p.o.) shows significant reduction in the tumor growth without obvious weigh loss in SCID mice bearing EG9 and HEG18 tumor cells. Oridonin treatment also suppresses the expression of Ki-67, phosphorylated AKT, GSK-3β or mTOR in mice. Oridonin (15 mg/kg, i.p.) impairs cell growth in breast cancer with hyperactivation of AKT signaling in nude mice.

NSC 250682

Natural Products

Terpenoids

Others|Akt1|Akt2

Cancer

——

28957-04-2

364.438

C20H28O6

>98% (HPLC)

Ethanol: 28 mg/mL (76.83 mM); DMSO: 72 mg/mL (197.57 mM); Water: <1 mg/mL （ < 1 mg/ml refers to the product slightly soluble or insoluble )

C=C([C@H](CC1)[C@H]2O)C([C@@]32[C@]4(O)[C@@H](O)[C@]5([H])C(C)(C)CC[C@H](O)[C@@]5(CO4)[C@@]31[H])=O

Kaur-16-en-15-one, 7a,20-epoxy-1a,6b,7,14-tetrahydroxy-, (14R)- (8CI)

(-20℃)

With Ice Pack

≥ 2 years