28957-04-2 Usage
Description
Oridonin is a diterpenoid compound derived from Rabdosia rubescens, which exhibits anti-inflammatory and anticancer properties. It acts as an inhibitor of AKT1 and AKT2, with IC50s of 8.4 and 8.9 μM, respectively. Oridonin has been shown to inhibit the proliferation of various cancer cells, including esophageal and osteosarcoma cells, and possesses the ability to block Wnt/β-catenin signaling.
Uses
Used in Anticancer Applications:
Oridonin is used as an effective anticancer agent for its ability to inhibit the proliferation and induce apoptosis of human osteosarcoma cells. It blocks Wnt/β-catenin signaling, which plays a crucial role in cancer development and progression. Additionally, Oridonin inhibits the proliferation of esophageal cancer cells in a dose-dependent manner, halts the cell cycle at the G2/M phase, and induces apoptosis at a concentration of 20 μM. It also reduces tumor growth in patient-derived mouse tumor models when administered at doses of 40 and 160 mg/kg.
Used in Anti-inflammatory Applications:
Oridonin is used as an anti-inflammatory agent, as it inhibits the assembly and activation of the NLRP3 inflammasome. This inhibition of inflammation is observed in wild-type mice but not in Nlrp3-/mice, suggesting its specificity in targeting the NLRP3 inflammasome. When administered at a dose of 3 mg/kg, Oridonin has been shown to reduce inflammation in a model of high-fat diet-induced type 2 diabetes.
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