title: Biotransformation of imperatorin by Penicillium janthinellum. Anti-osteoporosis activities of its metabolites.
abstract: Imperatorin (IMP) is a major constituent of many herbal medicines and possesses anti-osteoporosis activity. The present research work aimed to study the biotransformation processes of IMP and evaluated the anti-osteoporosis activity of the transformed metabolites. Among 18 strains of filamentous fungi screened, Penicillium janthinellum AS 3.510 exhibited good capability to metabolise IMP to the new derivatives. Ten transformed products were isolated and purified, and their structures were identified accurately based on spectroscopic data. Eight metabolites (2-8 and 10) were novel and previously unreported. The major biotransformation reactions involved hydroxylation of the prenyloxy side-chain and the lactone ring-opening reaction of furocoumarin skeleton. In addition, anti-osteoporosis activities of all products (1-10) were evaluated using MC3T3-E1 cells. The results showed that products 5 and 8 had the best bioactivities in increasing MC3T3-E1 cell growth. These products could be used in future therapeutic regimens for treating osteoporosis.
authors.affiliation: College of Pharmacy, Dalian Medical University, Dalian 116044, China.
authors.forename: Xia
authors.initials: X
authors.lastname: Lv
authors.forename: Dan
authors.initials: D
authors.lastname: Liu
authors.forename: Jie
authors.initials: J
authors.lastname: Hou
authors.forename: Peipei
authors.initials: P
authors.lastname: Dong
authors.forename: Libin
authors.initials: L
authors.lastname: Zhan
authors.forename: Li
authors.initials: L
authors.lastname: Wang
authors.forename: Sa
authors.initials: S
authors.lastname: Deng
authors.forename: Changyuan
authors.initials: C
authors.lastname: Wang
authors.forename: Jihou
authors.initials: J
authors.lastname: Yao
authors.forename: Xiaohong
authors.initials: X
authors.lastname: Shu
authors.forename: Kexin
authors.initials: K
authors.lastname: Liu
authors.forename: Xiaochi
authors.initials: X
authors.lastname: Ma
mesh_terms: D000818:Animals; D001711:Biotransformation; D002460:Cell Line; D049109:Cell Proliferation / Q000187:drug effects; D004365:Drugs, Chinese Herbal / Q000737:chemistry / Q000378:metabolism* / Q000494:pharmacology; D011564:Furocoumarins / Q000737:chemistry / Q000378:metabolism* / Q000494:pharmacology; D006801:Humans; D051379:Mice; D015394:Molecular Structure; D010006:Osteoblasts / Q000166:cytology / Q000187:drug effects*; D010024:Osteoporosis / Q000188:drug therapy / Q000503:physiopathology; D010407:Penicillium / Q000378:metabolism*
chemical_list: D004365:Drugs, Chinese Herbal; D011564:Furocoumarins; C031534:imperatorin