title: Bufadienolides with cytotoxic activity from the skins of Bufo bufo gargarizans.
abstract: Twelve new bufadienolides (1-12), along with fourteen known analogues (13-26) were isolated from the skins of Bufo bufo gargarizans Cantor. Their chemical structures were elucidated on the basis of NMR, HRESIMS and X-ray diffraction analysis. Compound 1 was an unusual bufadienolide with 3,19-epoxy moiety and A/B trans ring junction. Compounds 2-4 were rare bufadienolides possessing 10-H or 10-carboxyl units. All the isolated compounds were tested for their cytotoxic effects on HepG2, A549 and HeLa cells. Six new compounds (2, 3, 5, 6, 10 and 12) displayed significant anti-proliferative activities with IC50 values ranging from 0.049 to 1.856 μM. Arenobufagin (24) exhibited the most potent cytotoxic activity with IC50 value 0.011 μM. In addition, the present data provided more insight into the structure-activity relationships of bufadienolides.
authors.affiliation: Department of Natural Medicinal Chemistry, China Pharmaceutical University, Nanjing 210009, PR China; Institute of Traditional Chinese Medicine and Natural Products, College of Pharmacy, Jinan University, Guangzhou 510632, PR China.
authors.forename: Bao-Jing
authors.initials: BJ
authors.lastname: Li
authors.affiliation: Institute of Traditional Chinese Medicine and Natural Products, College of Pharmacy, Jinan University, Guangzhou 510632, PR China.
authors.forename: Hai-Yan
authors.initials: HY
authors.lastname: Tian
authors.affiliation: Institute of Traditional Chinese Medicine and Natural Products, College of Pharmacy, Jinan University, Guangzhou 510632, PR China.
authors.forename: Dong-Mei
authors.initials: DM
authors.lastname: Zhang
authors.affiliation: JNU-HKUST Joint Laboratory for Neuroscience and Innovative Drug Research, Jinan University, Guangzhou 510632, PR China.
authors.forename: Yu-He
authors.initials: YH
authors.lastname: Lei
authors.affiliation: Institute of Traditional Chinese Medicine and Natural Products, College of Pharmacy, Jinan University, Guangzhou 510632, PR China; JNU-HKUST Joint Laboratory for Neuroscience and Innovative Drug Research, Jinan University, Guangzhou 510632, PR China. Electronic address: cpuwanglei@126.com.
authors.forename: Lei
authors.initials: L
authors.lastname: Wang
authors.affiliation: Institute of Traditional Chinese Medicine and Natural Products, College of Pharmacy, Jinan University, Guangzhou 510632, PR China. Electronic address: rwjiang2008@126.com.
authors.forename: Ren-Wang
authors.initials: RW
authors.lastname: Jiang
authors.affiliation: Department of Natural Medicinal Chemistry, China Pharmaceutical University, Nanjing 210009, PR China; Institute of Traditional Chinese Medicine and Natural Products, College of Pharmacy, Jinan University, Guangzhou 510632, PR China; JNU-HKUST Joint Laboratory for Neuroscience and Innovative Drug Research, Jinan University, Guangzhou 510632, PR China. Electronic address: chyewc@gmail.com.
authors.forename: Wen-Cai
authors.initials: WC
authors.lastname: Ye
mesh_terms: D000818:Animals; D002018:Bufanolides / Q000737:chemistry* / Q000302:isolation & purification; D002023:Bufo bufo; D006367:HeLa Cells / Q000187:drug effects; D056945:Hep G2 Cells / Q000187:drug effects; D006801:Humans; D015394:Molecular Structure; D012867:Skin / Q000737:chemistry*
chemical_list: D002018:Bufanolides
keywords: Bufadienolides; Cytotoxicity; Skins of Bufo bufo gargarizans