PMID- 25973489
OWN - NLM
STAT- MEDLINE
DCOM- 20150629
LR  - 20150514
IS  - 1934-578X (Print)
IS  - 1555-9475 (Linking)
VI  - 10
IP  - 4
DP  - 2015 Apr
TI  - Anti-vancomycin-resistant Enterococcus faecium and E. faecalis activities of 
      (-)-gossypol and derivatives from Thespesia garckeana.
PG  - 613-6
AB  - The root extract of Thespesia garckeana yielded three known oxidatively coupled 
      sesquiterpenoids, namely (-)-gossypol (1) and two of its derivatives 
      (-)-6-methoxygossypol (2) and (+)-6,6'-dimethoxygossypol (3), and the stem bark 
      afforded (E)-docosyl-3-(3,4-dihydroxyphenyl) acrylate (4), stigmasterol (5) and 
      betulinic acid (6). The structures of the isolated compounds were determined on 
      the basis of full spectral data (1D and 2D NMR and HRMS) and comparison with 
      literature values. Compound 1 showed potent antibacterial activity against 
      vancomycin-resistant Enterococcus faecium (VRE) with IC50/MIC/MBC values of 
      1.71/4.82/19.31 microM, respectively, whereas the reference standard vancomycin was 
      found to be inactive. The mono- and di-methoxylated derivatives of this compound, 
      (-)-6-methoxygossypol (2) and (+)-6,6'-dimethoxygossypol (3), were less active 
      with respective IC50/MIC/MBC values of 2.73/4.70/9.40 microM and 6.14/18.32/18.32 microM 
      against this microbe. Compound 2 was more potent than 1 against the low level VRE 
      strain with I50/MIC/MBC values of 4.34/9.40/9.40 microM (vs 5.23/19.31/19.3 microM for 
      1). This compound also showed interesting activities against Candida glabrata 
      with an I50 value of 2.97 microM, but was less active against methicillin-resistant 
      S. aureus (MRSA) exhibiting an IC50 value of 17.33 microM. Compound 1 demonstrated 
      modest activity against the
FAU - Masila, Veronica M
AU  - Masila VM
FAU - Midiwo, Jacob O
AU  - Midiwo JO
FAU - Zhang, Jin
AU  - Zhang J
FAU - Gisacho, Bonface M
AU  - Gisacho BM
FAU - Munayi, Renee
AU  - Munayi R
FAU - Omosa, Leonidah K
AU  - Omosa LK
FAU - Wiggers, Frank T
AU  - Wiggers FT
FAU - Jacob, Melissa R
AU  - Jacob MR
FAU - Walker, Larry A
AU  - Walker LA
FAU - Muhammad, Ilias
AU  - Muhammad I
LA  - eng
PT  - Journal Article
PT  - Research Support, Non-U.S. Gov't
PL  - United States
TA  - Nat Prod Commun
JT  - Natural product communications
JID - 101477873
RN  - 0 (Anti-Bacterial Agents)
RN  - 6Q205EH1VU (Vancomycin)
RN  - KAV15B369O (Gossypol)
SB  - IM
MH  - Anti-Bacterial Agents/chemistry/pharmacology
MH  - Enterococcus faecalis/*drug effects
MH  - Enterococcus faecium/*drug effects
MH  - Gossypol/*analogs & derivatives/chemistry/pharmacology
MH  - Malvaceae/*chemistry
MH  - Vancomycin/*pharmacology
MH  - Vancomycin Resistance
EDAT- 2015/05/15 06:00
MHDA- 2015/06/30 06:00
CRDT- 2015/05/15 06:00
PHST- 2015/05/15 06:00 [entrez]
PHST- 2015/05/15 06:00 [pubmed]
PHST- 2015/06/30 06:00 [medline]
PST - ppublish
SO  - Nat Prod Commun. 2015 Apr;10(4):613-6.