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典型文献
Discovery of Kalmane Diterpenoids as Potent Analgesics from the Flowers of Rhododendron dauricum
文献摘要:
Kalmane diterpenoids,featuring a 5/8/5/5 tetracyclic carbon skeleton,are very rare in nature.The flowers of Rhododendron dauricum L.(Ericaceae)were phytochemically investigated for the first time,leading to the isolation of eight kalmane diterpenoids(1-8)including four new ones,named rhodokalmanols A-D(1-4).The structures of 1-8 were elucidated by comprehensive spectroscopic methods and 13C NMR-DP4+analysis,and the absolute configurations of 1,2,4,and 5 were defined by single-crystal X-ray diffraction analysis with Cu Kα radiation.Rhodokalmanol A(1)represents the first 5,8-epoxykalmane diterpenoid and also the first kalm-15(16)-ene diterpenoid.Rhodokalmanols B-D(2-4)are the first examples of kalm-7(8)-ene,kalm-16(17)-ene,and 8α-methoxykalmane diterpenoids,respectively.All the isolated kalmane diterpenoids 1-8 exhibited significant analgesic effects,and rhodokalmanol C(3)and kalmanol(8)expressed more potent analgesic activity than morphine at doses of 0.2 and 0.04 mg/kg.The preliminary structure-activity relationships of kalmane diterpenoids as potent analgesics are discussed.
文献关键词:
作者姓名:
Yuanyuan Feng;Suqin Zha;Biao Gao;Hanqi Zhang;Pengfei Jin;Guijuan Zheng;Yilin Ma;Guangmin Yao
作者机构:
Hubei Key Laboratory of Natural Medicinal Chemistry and Resource Evaluation,School of Pharmacy,Tongji Medical College,Huazhong University of Science and Technology,Wuhan,Hubei 430030,China
引用格式:
[1]Yuanyuan Feng;Suqin Zha;Biao Gao;Hanqi Zhang;Pengfei Jin;Guijuan Zheng;Yilin Ma;Guangmin Yao-.Discovery of Kalmane Diterpenoids as Potent Analgesics from the Flowers of Rhododendron dauricum)[J].中国化学(英文版),2022(09):1019-1027
A类:
Kalmane,Diterpenoids,Analgesics,dauricum,phytochemically,kalmane,rhodokalmanols,DP4+analysis,Rhodokalmanol,epoxykalmane,kalm,Rhodokalmanols,methoxykalmane,rhodokalmanol,kalmanol
B类:
Discovery,as,Potent,from,Flowers,Rhododendron,diterpenoids,featuring,tetracyclic,carbon,skeleton,rare,nature,flowers,Ericaceae,were,investigated,first,leading,isolation,eight,including,four,new,ones,named,structures,elucidated,by,comprehensive,spectroscopic,methods,13C,NMR,absolute,configurations,defined,single,crystal,ray,diffraction,radiation,represents,also,ene,examples,respectively,All,isolated,exhibited,significant,effects,expressed,more,potent,activity,than,morphine,doses,preliminary,relationships,analgesics,discussed
AB值:
0.426441
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