title: Bioactive metabolites of Schisanlactone E transformed by Cunninghamella blakesleana AS 3.970.
abstract: Schisanlactone E (SE) is a major triterpene obtained from the plants of genus Kadsura. The aim of this research was to investigate the transformed metabolites of SE by fungi and evaluate the bioactivities of these products. After screening 10 strains of filamentous fungi, Cunninghamella blakesleana AS 3.970 was chosen as a potent organism to be used for the biotransformation of SE. 13 metabolites were obtained and determined to be new compounds through the use of spectroscopic data, including UV, 1D-, 2D-NMR, and HR-ESIMS. Furthermore, in an in vitro bioassay, metabolites 7 and 9 showed moderate inhibitory effects on the nitric oxide production in LPS-induced macrophages with IC50 values of 16.73, 5.91 μM, respectively; 9 could inhibit the proliferation of acetaldehyde-induced HSC-T6 cells, with the IC50 value of 21.4 μM. Preliminary findings on the structure-activity relationships for these metabolites were also discussed.
authors.affiliation: College of Pharmacy, Dalian Medical University, Dalian 116044, People's Republic of China.
authors.forename: Zhen-Peng
authors.initials: ZP
authors.lastname: Mai
authors.affiliation: College of Pharmacy, Dalian Medical University, Dalian 116044, People's Republic of China; State Key Laboratory of Bioactive Substance and Function of Natural Medicines, Institute of Materia Medica, Chinese Academy of Medical Sciences and Peking Union Medical College, Beijing 100050, People's Republic of China; Chinese People's Liberation Army 210 Hospital, Dalian 116021, People's Republic of China.
authors.forename: Chao
authors.initials: C
authors.lastname: Wang
authors.affiliation: Chinese People's Liberation Army 210 Hospital, Dalian 116021, People's Republic of China.
authors.forename: Yan
authors.initials: Y
authors.lastname: Wang
authors.affiliation: College of Pharmacy, Dalian Medical University, Dalian 116044, People's Republic of China.
authors.forename: Hou-Li
authors.initials: HL
authors.lastname: Zhang
authors.affiliation: College of Pharmacy, Dalian Medical University, Dalian 116044, People's Republic of China.
authors.forename: Bao-Jing
authors.initials: BJ
authors.lastname: Zhang
authors.affiliation: TCM and Ethnomedicine Innovation & Development Laboratory, School of Pharmacy, Hunan University of Chinese Medicine, Changsha 410208, People's Republic of China. Electronic address: wangwei402@hotmail.com.
authors.forename: Wei
authors.initials: W
authors.lastname: Wang
authors.affiliation: College of Pharmacy, Dalian Medical University, Dalian 116044, People's Republic of China.
authors.forename: Xiao-Kui
authors.initials: XK
authors.lastname: Huo
authors.affiliation: College of Pharmacy, Dalian Medical University, Dalian 116044, People's Republic of China.
authors.forename: Shan-Shan
authors.initials: SS
authors.lastname: Huang
authors.affiliation: College of Pharmacy, Dalian Medical University, Dalian 116044, People's Republic of China.
authors.forename: Chang-Yuan
authors.initials: CY
authors.lastname: Wang
authors.affiliation: College of Pharmacy, Dalian Medical University, Dalian 116044, People's Republic of China.
authors.forename: Ke-Xin
authors.initials: KX
authors.lastname: Liu
authors.affiliation: College of Pharmacy, Dalian Medical University, Dalian 116044, People's Republic of China; Chinese People's Liberation Army 210 Hospital, Dalian 116021, People's Republic of China.
authors.forename: Xiao-Chi
authors.initials: XC
authors.lastname: Ma
authors.affiliation: Chinese People's Liberation Army 210 Hospital, Dalian 116021, People's Republic of China. Electronic address: wxbbenson0653@sina.com.
authors.forename: Xiao-Bo
authors.initials: XB
authors.lastname: Wang
mesh_terms: D000818:Animals; D001711:Biotransformation; D002460:Cell Line; D020093:Cunninghamella / Q000378:metabolism*; D020128:Inhibitory Concentration 50; D032135:Kadsura / Q000737:chemistry*; D008264:Macrophages / Q000187:drug effects*; D051379:Mice; D015394:Molecular Structure; D009569:Nitric Oxide / Q000096:biosynthesis; D013329:Structure-Activity Relationship; D014315:Triterpenes / Q000737:chemistry* / Q000378:metabolism
chemical_list: D014315:Triterpenes; C000597713:schisanlactone E; D009569:Nitric Oxide
keywords: Biotransformation; HSC-T6 cell inhibition; Kadsura; NO production inhibition; Schisanlactone E