生物活性

• 描述Monoamine oxidase (MAO) is an important enzyme in the metabolism of a wide range of endogenous monoamine neurotrasmitters such as noradrenaline, dopamine, and serotonin (5-HT), and also catalyzes as well the removal of exogenous amines. Paeonol, originated from the traditional Chinese medicine, is a naturally occuring MAO inhibitor with IC₅₀ values of 54.6 μM and 42.5 μM for MAO-A and MAO-B, respectively. Paeonol dose- and time- dependently induced not only antiproliferation activity and apoptosis but also autophagy via blocking the Akt/mTOR pathway in A2780 and SKOV3 cells. In addition, combination treatment with Paeonol and an autophagy inhibitor (3-methyladenine and hydroxychloroquine) showed significant synergetic effects on inhibiting cell viability and promoting apoptosis in vitro and in the A2780 xenograft model, without severe side effects. Paeonol at 50 and 100μM prevented IL-1β-induced inflammatory response by inhibiting numerous factors of osteoarthritis(OA), including IL-6, TNF-a, NOX2, PTGS2, NUCB2/nesfatin-1, ICAM-1, VCAM-1, MMP-3/13, degradation of type II collagen, and NF-kB activation through the rescue of IkBa in human primary chondrocytes.

• 动物研究
  剂量	Mice: 20 mg/kg[3] (i.p.); 20 mg/kg - 80 mg/kg[4] (p.o.) Rat: 2.5 mg/kg - 10 mg/kg[5] (i.v.); 30 mg/kg - 100 mg/kg[2] (i.p.); 100 mg/kg, 200 mg/kg[6] (p.o.)
  给药途径	i.p., p.o., i.v.
  动物药代数据	Animal Rats[5] Dose 5 mg/kg Administration i.v. Vd 394 ± 22.8 L/kg A 11.17 ± 0.93 μg/ml B 1.72 ± 0.18 μg/ml AUC 114.8 ± 10.3 μg·min/ml T1/2β 30.6 ± 1.70 min CL 49.3 ± 1.85 ml/min/kg α 0.26 ± 0.03 1/min β 0.023 ± 0.002 1/min