2. Academic Validation
  3. Photoactivated 2,3-distyrylindoles kill multi-drug resistant bacteria

Photoactivated 2,3-distyrylindoles kill multi-drug resistant bacteria

  • Bioorg Med Chem Lett. 2018 Jun 1;28(10):1879-1886. doi: 10.1016/j.bmcl.2018.04.001.
Leslie Edwards 1,  Danielle Turner 1,  Cody Champion 1,  Megha Khandelwal 1,  Kailee Zingler 1,  Cassidy Stone 2,  Ruwini D Rajapaksha 2,  Jing Yang 3,  Mahinda I Ranasinghe 2,  Alexander Kornienko 2,  Liliya V Frolova 4,  Snezna Rogelj 5
Affiliations

Affiliations

  • 1 Department of Biology, New Mexico Tech, 801 Leroy Place, Socorro, NM 87801, USA.
  • 2 Department of Chemistry, New Mexico Tech, 801 Leroy Place, Socorro, NM 87801, USA.
  • 3 Department of Chemistry and Chemical Biology, The University of New Mexico, 1 University of New Mexico, NM 87131, USA.
  • 4 Department of Chemistry, New Mexico Tech, 801 Leroy Place, Socorro, NM 87801, USA. Electronic address: liliya.frolova@nmt.edu.
  • 5 Department of Biology, New Mexico Tech, 801 Leroy Place, Socorro, NM 87801, USA. Electronic address: snezna.rogelj@nmt.edu.
PMID: 29673980 DOI: 10.1016/j.bmcl.2018.04.001
Abstract

Compounds based on the 2,3-distyrylindole scaffold were found to exhibit bactericidal properties upon irradiation with white light. At the concentration of 1 μM, the lead compound 1 completely (CA. 109 CFU/mL) eradicated such Gram-positive organisms as S. aureus (MRSA, MSSA), E. faecalis (VRE), S. pyogenes and S. mutans when irradiated with white light for 2 min. At the concentration of 5 μM and in the presence of polymyxin E at non-bactericidal 1.25 μg/mL concentration, 1 also showed a 7-log to 9-log reductions in Bacterial counts of such Gram-negative organisms as multi-drug resistant (MDR) A. baumannii, MDR P. aeruginosa, E. coli and Klebsiella pneumoniae (CRE: KPC and NDM-1), also when irradiated with white light for 2 min. The structure-activity relationship studies revealed that unsubstituted at benzene rings 2,3-distyrylindole 2 was most potent and gave a 5-order of magnitude eradication of a MRSA strain at the concentration of 30 nM upon irradiation with white light. Initial mechanistic experiments revealed the disruption of Bacterial cell membrane, but indicated that singlet oxygen production, which is commonly associated with photodynamic therapy, may not play a role in the bactericidal effects of the 2,3-distyrylindoles.

Keywords

CRE; Light-activated; MRSA; Multi-drug resistance; S. mutans; VRE.

Figures
嗨！很高兴为您提供帮助！

尊敬的 MCE 客户您好，
请您选择所在区域，我们将转接对应客服为您服务！

热门区域

A

B

C

F

G

H

J

L

N

Q

S

T

X

Y

Z

热 A B C F G H J L N Q S T X Y Z