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| Content Provider | World Health Organization (WHO)-Global Index Medicus |
|---|---|
| Author | Tian, Hai-Yan Yuan, Xiao-Feng Jin, Lu Li, Juan Luo, Cheng Ye, Wen-Cai Jiang, Ren-Wang |
| Description | Author Affiliation: Tian HY ( Institute of Traditional Chinese Medicine and Natural Products, College of Pharmacy, Jinan University, Guangzhou 510632, PR China.); Yuan XF ( Institute of Traditional Chinese Medicine and Natural Products, College of Pharmacy, Jinan University, Guangzhou 510632, PR China.); Jin L ( Institute of Traditional Chinese Medicine and Natural Products, College of Pharmacy, Jinan University, Guangzhou 510632, PR China.); Li J ( Institute of Traditional Chinese Medicine and Natural Products, College of Pharmacy, Jinan University, Guangzhou 510632, PR China.); Luo C ( State Key Laboratory of Drug Research, Shanghai Institute of Materia Medica, Chinese Academy of Sciences, 555 Zu Chong Zhi Road, Shanghai 201203, PR China.); Ye WC ( Institute of Traditional Chinese Medicine and Natural Products, College of Pharmacy, Jinan University, Guangzhou 510632, PR China. Electronic address: chyewc@gmail.com.); Jiang RW ( Institute of Traditional Chinese Medicine and Natural Products, College of Pharmacy, Jinan University, Guangzhou 510632, PR China. Electronic address: trwjiang@jnu.edu.cn.) |
| Abstract | Molecular docking studies have shown that Δ(8,14)-anhydrobufalin (1) exhibited more potent binding affinity on androgen receptor (AR) than Δ(14,15)-anhydrobufalin (2) and bufalin (3). To validate the docking results, compounds 1 and 2 were synthesized. The AR competitive binding assay indicated that the IC50 values of 1-3 were 1.9, >50 and >50µM (relative binding affinity), respectively, which confirmed that our theoretical binding mode was reliable and predictable. Furthermore, compound 1 was found to show more potent inhibitory activity against the androgen dependent LNCaP cancer cells than the androgen independent PC3 cancer cells, but exhibited less inhibition on the Na(+)/K(+) ATPase as compared with the parent compound 3. To the best of our knowledge, compound 1 represented the first AR antagonist derived from bufadienolide discovered through a series of combined approaches of molecular docking and actual experimental validation. |
| File Format | HTM / HTML |
| ISSN | 00092797 |
| Volume Number | 207 |
| e-ISSN | 18727786 |
| Journal | Chemico-Biological Interactions |
| Language | English |
| Publisher | Elsevier |
| Publisher Date | 2014-01-25 |
| Publisher Place | Ireland |
| Access Restriction | One Nation One Subscription (ONOS) |
| Subject Keyword | Discipline Biochemistry Discipline Pharmacology Androgen Receptor Antagonists Pharmacology Bufanolides Prostatic Neoplasms Metabolism Pathology Receptors, Androgen Amino Acid Sequence Chemistry Binding, Competitive Drug Effects Cell Line, Tumor Chromatography, High Pressure Liquid Crystallography, X-ray Dose-response Relationship, Drug Drug Screening Assays, Antitumor Humans Hydrophobic And Hydrophilic Interactions Male Models, Molecular Molecular Sequence Data Sequence Alignment Journal Article Research Support, Non-u.s. Gov't |
| Content Type | Text |
| Resource Type | Article |
| Subject | Medicine Toxicology |
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