Cepharanthine

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Chemical Structure| 481-49-2 同义名 : 千金藤碱 ;O-Methylcepharanoline;NSC-623442;Cepharanthin;6',12'-Dimethoxy-2,2'-dimethyl-6,7-[methylenebis- (oxy)]oxyacanthan
CAS号 : 481-49-2
货号 : A508305
分子式 : C37H38N2O6
纯度 : 97%
分子量 : 606.707
MDL号 : MFCD00210482
存储条件：

Pure form Inert atmosphere,2-8°C

In solvent -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 50 mg/mL(82.41 mM)，配合低频超声助溶，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO
动物实验配方：

2%DMSO+30% PEG 300+5% Tween 80+water 5 mg/mL

生物活性
描述 Cepharanthine is an alkaloid derived from Stephania cepharantha Hayata, with possesses anti-inflammatory and antioxidative activities. CEP (Cepharanthine) dose-dependently inhibited the release of TNF-α, IL-6, and IL-1β in LPS-stimulated RAW264.7 cells. Significantly, CEP dose-dependently suppressed NF-κB activation, IκBα degradation, and phosphorylation of ERK, JNK, and p38 induced by LPS. In vivo, it was also observed that CEP attenuated lung histopathologic changes and down-regulated the level of pro-inflammatory cytokines, including TNF-α, IL-1β, and IL-6, in the mouse acute lung injury model[3]. CEP inhibited Ca2+-induced swelling, depolarization, Cyt.c release, and the release of Ca2+ in a concentration dependent manner. CEP also inhibited Ca2+-induced generation of reactive oxygen species and Fe/ADP-induced swelling and lipid peroxidation. Furthermore, CEP suppressed Ca2+-induced thiol modification of adenine nucleotide transloase (ANT)[4]. Cepharanthine attenuates muscle and kidney injuries induced by limb ischemia/reperfusion (I/R)[5]. CEP attenuates cerebral I/R injury probably by inhibiting microglia activation and NLRP3 (NLR Family Pyrin Domain Containing 3) inflammasome-induced inflammation and reducing oxidative stress via suppressing 12/15-LOX signaling[6]. CEP could inhibit growth and motility of MCF-7 and MDA-MB-231 breast cancer cell[7].
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

1.65mL

0.33mL

0.16mL

8.24mL

1.65mL

0.82mL

16.48mL

3.30mL

1.65mL
参考文献

[1]Hua P, Sun M, et al. Cepharanthine induces apoptosis through reactive oxygen species and mitochondrial dysfunction in human non-small-cell lung cancer cells. Biochem Biophys Res Commun. 2015 May 1;460(2):136-42.

[2]Matsuda K, Hattori S, et al. Cepharanthine inhibited HIV-1 cell-cell transmission and cell-free infection via modification of cell membrane fluidity. Bioorg Med Chem Lett. 2014 May 1;24(9):2115-7.

[3]Huang H, Hu G, Wang C, Xu H, Chen X, Qian A. Cepharanthine, an alkaloid from Stephania cepharantha Hayata, inhibits the inflammatory response in the RAW264.7 cell and mouse models. Inflammation. 2014 Feb;37(1):235-46

[4]Nagano M, Kanno T, Fujita H, Muranaka S, Fujiwara T, Utsumi K. Cepharanthine, an anti-inflammatory drug, suppresses mitochondrial membrane permeability transition. Physiol Chem Phys Med NMR. 2003;35(2):131-43

[5]Kao MC, Chung CY, Chang YY, Lin CK, Sheu JR, Huang CJ. Salutary Effects of Cepharanthine against Skeletal Muscle and Kidney Injuries following Limb Ischemia/Reperfusion. Evid Based Complement Alternat Med. 2015;2015:504061

[6]Zhao J, Piao X, Wu Y, Liang S, Han F, Liang Q, Shao S, Zhao D. Cepharanthine attenuates cerebral ischemia/reperfusion injury by reducing NLRP3 inflammasome-induced inflammation and oxidative stress via inhibiting 12/15-LOX signaling. Biomed Pharmacother. 2020 Jul;127:110151

[7]Gao S, Li X, Ding X, Qi W, Yang Q. Cepharanthine Induces Autophagy, Apoptosis and Cell Cycle Arrest in Breast Cancer Cells. Cell Physiol Biochem. 2017;41(4):1633-1648