Synthesis of twin drugs of paeonol and study on their degradation dynamics properties and anti-inflammatory activities / 中国药学杂志

ABSTRACT

OBJECTIVE: To synthesize the ester condensation products of paeonol by coupling paeonol or its analogues with naproxen and investigate the anti-inflammatory activities of the products. METHODS: Five compounds were synthesized by condensing paeonol or its analogues with naproxen by DCC method. An HPLC method was established for determination of the content of the target products, and their degradation dynamics under pH 1.2, 5.0 and 7.4 buffer conditions at 37℃ was studied. The anti-inflammatory activities of the compounds were evaluated in xylene-induced mouse ear swelling model. RESULTS: Five new compounds were synthesized and confirmed by MS and H-NMR. Degradation kinetic experiments showed that these compounds were stable in buffers of different pHs. All the compounds showed anti-inflammatory activities. CONCLUSION: All the compounds are stable and exhibit potent anti-inflammatory activities.