28957-04-2 Usage
Description
Oridonin is a diterpenoid that has been found in R. rubescens and has anti-inflammatory and anticancer properties. It is an inhibitor of AKT1 and AKT2 (IC50s = 8.4 and 8.9 μM, respectively). Oridonin inhibits proliferation of KYSE70, KYSE410, and KYSE450 esophageal cancer cells in a dose-dependent manner, halts the cell cycle at the G2/M phase, and induces apoptosis when used at a concentration of 20 μM. It decreases the expression of cleaved poly(ADP-ribose) polymerase (PARP), caspase-3, caspase-7, and Bims and the protein levels of phosphorylated AKT and reduces AKT activity. Oridonin reduces tumor growth in patient-derived mouse tumor models when administered at doses of 40 and 160 mg/kg. Oridonin is also an inhibitor of NLRP3 inflammasome assembly and activation. It inhibits inflammation in wild-type, but not Nlrp3-/-, mice in a model of high-fat diet-induced type 2 diabetes when administered at a dose of 3 mg/kg.
Uses
Oridonin is an effective anticancer agent due to its ability to inhibit proliferation and induce apoptosis of human osteosarcoma cells. Blocks Wnt/β-catenin signalling.
Pharmacokinetics
The anti-inflammatory property of oridonin has been well documented in various immunological diseases. The compound is able to counteract the expression of COX-2 and NOS-2 in the murine RAW 264.7 macrophage cell line activated with LPS. The mechanism underlies the direct interference of the compound with the active region of NF-κB, thereby blocking its nuclear localisation and reducing inflammation (Leung et al., 2005). Shang et al. (2016) observed the efficacy of oridonin against RA-FLS proliferation. They found that oridonin inhibited cell proliferation and promoted cell apoptosis in IL-1β–treated FLS through phosphorylation of ERK1/2 and JNK in a dose-dependent manner. Oridonin is also reported to restrict the release of pro-inflammatory cytokines in LPS-activated RAW264.7 macrophages (Shang et al., 2016).
References
1) He?et al.?(2018),?Oridonin is a covalent NLRP3 inhibitor with strong anti-inflammasome activity; Nat. Commun.,?9?2550
2) Huang?et al.?(2018),?Oridonin inhibits vascular inflammation by blocking NF-kB and MAPK activation; Eur. J. Pharmacol.,?826?133
3) Sun?et al.?(2018),?Oridonin inhibits aberrant AKT activation in breast cancer; Oncotarget,?9?23878
4) Li?et al.?(2018),?Oridonin inhibits migration, invasion, adhesion and TGF-?1-induced epithelial-mesenchymal transition of melanoma cells by inhibiting the activity?of PI3K/Akt/GSK-3? signaling pathway; Oncol. Lett.,?15?1362
5) Lu et al. (2018),?Oridonin exerts anticancer effect on osteosarcoma by activating PPARγ and inhibiting Nrf2 pathway; Cell Death Dis.,?9?15
Check Digit Verification of cas no
The CAS Registry Mumber 28957-04-2 includes 8 digits separated into 3 groups by hyphens. The first part of the number,starting from the left, has 5 digits, 2,8,9,5 and 7 respectively; the second part has 2 digits, 0 and 4 respectively.
Calculate Digit Verification of CAS Registry Number 28957-04:
(7*2)+(6*8)+(5*9)+(4*5)+(3*7)+(2*0)+(1*4)=152
152 % 10 = 2
So 28957-04-2 is a valid CAS Registry Number.
InChI:InChI=1/C20H28O6/c1-9-10-4-5-11-18-8-26-20(25,19(11,14(9)22)15(10)23)16(24)13(18)17(2,3)7-6-12(18)21/h10-13,15-16,21,23-25H,1,4-8H2,2-3H3/t10?,11?,12?,13?,15?,16-,18?,19?,20+/m0/s1
