Norlignans, acylphloroglucinols, and a dimeric xanthone from Hypericum chinense.
Two new norlignans, hyperiones A (1) and B (2), three new acylphloroglucinols, aspidinol C (3) and hyperaspidinols A (5) and B (6), the known compound aspidinol D (4), and the symmetrical dimeric xanthone hyperidixanthone (7) were isolated from Hypericum chinense. Their structures were established by spectroscopic analysis. In an antibacterial assay using a panel of multidrug-resistant (MDR) strains, compounds 3 and 4 exhibited promising activity against the NorA efflux protein overexpressing MDR Staphylococcus aureus strain SA-1199B with a minimum inhibitory concentration (MIC) of 2 μg/mL (8.4 μM) and 4 μg/mL (16.8 μM), respectively. The positive control antibiotic norfloxacin showed activity at MIC 32 μg/mL (100 μM).
School of Pharmacy, Fudan University, Shanghai, People's Republic of China.
Wei
W
Wang
Yi Han
YH
Zeng
Khadijo
K
Osman
Kamlesh
K
Shinde
Mukhlesur
M
Rahman
Simon
S
Gibbons
Qing
Q
Mu
D000818:Animals; D001426:Bacterial Proteins / Q000187:drug effects; D024901:Drug Resistance, Multiple, Bacterial / Q000187:drug effects*; D004365:Drugs, Chinese Herbal / Q000737:chemistry / Q000302:isolation & purification* / Q000494:pharmacology; D020902:Hypericum / Q000737:chemistry*; D017705:Lignans / Q000737:chemistry / Q000302:isolation & purification* / Q000494:pharmacology; D051379:Mice; D008826:Microbial Sensitivity Tests; D015394:Molecular Structure; D027425:ATP-Binding Cassette, Sub-Family C Proteins / Q000187:drug effects; D009643:Norfloxacin / Q000494:pharmacology; D019906:Nuclear Magnetic Resonance, Biomolecular; D010696:Phloroglucinol / Q000031:analogs & derivatives* / Q000737:chemistry / Q000302:isolation & purification* / Q000494:pharmacology; D018515:Plant Leaves / Q000737:chemistry; D013211:Staphylococcus aureus / Q000187:drug effects / Q000378:metabolism*; D013752:Tetracycline / Q000494:pharmacology; D044004:Xanthones / Q000737:chemistry / Q000302:isolation & purification* / Q000494:pharmacology
D001426:Bacterial Proteins; D004365:Drugs, Chinese Herbal; D017705:Lignans; D027425:ATP-Binding Cassette, Sub-Family C Proteins; D009643:Norfloxacin; D010696:Phloroglucinol; D013752:Tetracycline; D044004:Xanthones; C075040:NorA protein, Staphylococcus; C009689:xanthone