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Diverse epoxy grayanane diterpenoids with analgesic activity from the roots of Pieris formosa
Chang-Shan Niu1, Yong Li1, Yun-Bao Liu1
1State Key Laboratory of Bioactive Substance and Function of Natural Medicines, Institute of Materia Medica, Peking Union Medical College, Chinese Academy of Medical Sciences, Beijing 100050, People's Republic of China.
Abstract:
In our on-going study to investigate components with analgesic activity, eight new grayanane diterpenoids, epoxypieristoxins A-H (1-8), along with one known compound (9) were isolated from the roots of Pieris formosa. Their structures with absolute configurations were characterized by a series of spectroscopic methods and X-ray diffraction. Notably, compounds 1-5 represented the first example of natural grayanane diterpenoids possessed a 10,14-epoxy group. Whereas, compounds 6-7 were the first example of grayanane diterpenoid with a 7,10-epoxy group. Biological assays showed that compounds 1-3 and 5-8 displayed significant analgesic activity at a dose of 5.0 mg/kg (ip) compared to the vehicle tests (p < .05).
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