PMID- 7748198
OWN - NLM
STAT- MEDLINE
DCOM- 19950609
LR  - 20220311
IS  - 0006-2952 (Print)
IS  - 0006-2952 (Linking)
VI  - 49
IP  - 8
DP  - 1995 Apr 18
TI  - Inhibition of human immunodeficiency virus type-1 integrase by curcumin.
PG  - 1165-70
AB  - Curcumin (diferuloylmethane) is the yellow pigment in turmeric (Curcuma longa L.) 
      that is widely used as a spice, food coloring (curry) and preservative. Curcumin 
      exhibits a variety of pharmacological effects including antitumor, 
      anti-inflammatory, and anti-infectious activities and is currently in clinical 
      trials for AIDS patients. The effects of curcumin have been determined on 
      purified human immunodeficiency virus type 1 (HIV-1) integrase. Curcumin has an 
      inhibitory concentration50 (IC50) for strand transfer of 40 microM. Inhibition of 
      an integrase deletion mutant containing only amino acids 50-212 suggests that 
      curcumin interacts with the integrase catalytic core. Two structural analogs, 
      methyl cinnamate and chlorogenic acid, were inactive. Energy minimization studies 
      suggest that the anti-integrase activity of curcumin could be due to an 
      intramolecular stacking of two phenyl rings that brings the hydroxyl groups into 
      close proximity. The present data suggest that HIV-1 integrase inhibition may 
      contribute to the antiviral activity of curcumin. These observations suggest new 
      strategies for antiviral drug development that could be based upon curcumin as a 
      lead compound for the development of inhibitors of HIV-1 integrase.
FAU - Mazumder, A
AU  - Mazumder A
AD  - Laboratory of Molecular Pharmacology, National Cancer Institute, Bethesda, MD 
      20892-4255, USA.
FAU - Raghavan, K
AU  - Raghavan K
FAU - Weinstein, J
AU  - Weinstein J
FAU - Kohn, K W
AU  - Kohn KW
FAU - Pommier, Y
AU  - Pommier Y
LA  - eng
PT  - Journal Article
PT  - Research Support, U.S. Gov't, P.H.S.
PL  - England
TA  - Biochem Pharmacol
JT  - Biochemical pharmacology
JID - 0101032
RN  - 0 (Antiviral Agents)
RN  - EC 2.7.7.- (DNA Nucleotidyltransferases)
RN  - EC 2.7.7.- (Integrases)
RN  - IT942ZTH98 (Curcumin)
SB  - IM
MH  - Antiviral Agents/*pharmacology
MH  - Base Sequence
MH  - Binding Sites
MH  - Curcumin/*pharmacology
MH  - DNA Nucleotidyltransferases/*antagonists & inhibitors/genetics
MH  - Dose-Response Relationship, Drug
MH  - HIV-1/*enzymology
MH  - Integrases
MH  - Molecular Sequence Data
MH  - Structure-Activity Relationship
EDAT- 1995/04/18 00:00
MHDA- 1995/04/18 00:01
CRDT- 1995/04/18 00:00
PHST- 1995/04/18 00:00 [pubmed]
PHST- 1995/04/18 00:01 [medline]
PHST- 1995/04/18 00:00 [entrez]
AID - 0006-2952(95)98514-A [pii]
AID - 10.1016/0006-2952(95)98514-a [doi]
PST - ppublish
SO  - Biochem Pharmacol. 1995 Apr 18;49(8):1165-70. doi: 10.1016/0006-2952(95)98514-a.