- Modified tetra-oxygenated xanthones analogues as anti-MRSA and P. aeruginosa agent and their synergism with vancomycin
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Five isolated xanthones from the C. cochinchinense and G. mangostana were evaluated and tested for antibacterial activities. Isolated 4 and 5 exhibited potent anti-MRSA and P. aeruginosa activity, but showed poor pharmacokinetic properties via ADMET prediction. It led us to improve pharmacokinetic properties of 4 and 5 by partially modifying them in acidic condition yielding fourteen analogues. It was found that analogues 4b, 4d and 5b possessed proper pharmacokinetic properties, while only 4b exhibited the best anti-MRSA and P. aeruginosa activity. The SEM results indicated that 4b may interact with or damage the cell wall of MRSA and P. aeruginosa. Moreover, a combination of 4b and vancomycin exhibits synergistic effect against both MRSA and P. aeruginosa at MIC value of 4.98 (MIC = 18.75 μg/mL for 4b) and 9.52 μg/mL (MIC = 75 μg/mL for 4b), respectively.
- Boonnak, Nawong,Chantrapromma, Suchada,Kaewpiboon, Chutima,Sathirakul, Korbtham
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supporting information
(2020/08/21)
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- Design, synthesis and structure-activity relationships of mangostin analogs as cytotoxic agents
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In order to better understand the structure-activity relationship of mangostin, a series of xanthone derivatives based on α-mangostin were designed and synthesized. All the compounds were evaluated for their cytotoxicity against a panel of five human canc
- Chi, Xiao-Qian,Zi, Cheng-Ting,Li, Hong-Mei,Yang, Liu,Lv, Yong-Feng,Li, Jin-Yu,Hou, Bo,Ren, Fu-Cai,Hu, Jiang-Miao,Zhou, Jun
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p. 41377 - 41388
(2019/01/03)
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- Chemistry of α-mangostin. Studies on the semisynthesis of minor xanthones from Garcinia mangostana
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α-Mangostin is the major prenylated xanthone from Garcinia mangostana and it has been used also in recent times as starting material for the semisynthetic preparation of various biologically active derivatives. Its structure is characterised by the presence of few functional groups amenable to chemical manipulations, but present in the molecule in multiple instances (three phenolic hydroxyl groups, two prenyl chains and two unsubstituted aromatic carbons). This study represents a first approach to the systematic investigation of the reactivity of α-mangostin and describes the semisynthesis of some minor xanthones isolated from G. mangostana.
- Morelli, Carlo F.,Biagiotti, Marco,Pappalardo, Valeria M.,Rabuffetti, Marco,Speranza, Giovanna
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supporting information
p. 750 - 755
(2015/12/24)
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- Cytotoxic and NF-κB inhibitory constituents of the stems of Cratoxylum cochinchinense and their semisynthetic analogues
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A new caged xanthone (1), a new prenylxanthone (2), seven known xanthones, and a known sterol glucoside were isolated from the stems of Cratoxylum cochinchinense, collected in Vietnam. Compounds 1 and 2 were determined structurally by analysis of their sp
- Ren, Yulin,Matthew, Susan,Lantvit, Daniel D.,Ninh, Tran Ngoc,Chai, Heebyung,Fuchs, James R.,Soejarto, Djaja D.,De Blanco, Esperanza J. Carcache,Swanson, Steven M.,Kinghorn, A. Douglas
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experimental part
p. 1117 - 1125
(2011/07/30)
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