Inhibition of HIV-1 integrase by flavones, caffeic acid phenethyl ester (CAPE) and related compounds

Fesen, Mark R.; Pommier, ﻿Yves; Leteurtre, François; Hiroguchi, Satoshi; Yung, Jessie; Kohn, Kurt W.

doi:10.1016/0006-2952(94)90291-7

Cited by 315 publications

(261 citation statements)

References 42 publications

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“…Statistical significance was determined using Student's t test, and P \ 0.05 was considered significant effects on normal healthy cells (Cassileth et al 2008;Engdal et al 2009). Recently, caffeic acid phenethyl ester (CAPE), obtained from honeybee propolis (Grunberger et al 1998), has attracted notice in that it represented antitumoral (Chiao et al 1995), anti-inflammatory (Michaluart et al 1999;Orban et al 2000), antiviral (Fesen et al 1994), antioxidant (Bhimani et al 1993), and anti-angiogenic (Liao et al 1999) effects. Although the ability of CAPE to induce apoptosis has been reported for various types of cancer, very little is known about the effects of CAPE on human CCRF-CEM cells (Michaluart et al 1999;Fesen et al 1994;Chiao et al 1995;Grunberger et al 1998;Orban et al 2000;Bhimani et al 1993;Liao et al 1999).…”

Section: Discussionmentioning

confidence: 99%

“…Antiproliferative ability of CAPE has been considered as a new anticancer treatment modality and has been studied in many cancers and cell lines both in vivo and in vitro (Crazzolara and Bendall 1999;Borrelli et al 2002;Son and Lewis 2002;Lee et al 2000;Demestre et al 2009). Several studies reported that the antitumoral effect of CAPE was possibly related to the alteration of redox potentials resulting in apoptosis, suppression of lipid peroxidation, inhibition of ornithine decarboxylase, and protein synthesis, and inhibition of activation of nuclear factor kappa B (NF-jB; Li et al 2000;Berger et al 1992;Rao et al 1992;Michaluart et al 1999;Sud'ina et al 1993;Fesen et al 1994). Interestingly, it was also shown that CAPE exerts apoptotic effect and suppresses the growth of transformed cells in a specific manner (Chiao et al 1995).…”

Section: Introductionmentioning

confidence: 99%

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Caffeic acid phenethyl ester triggers apoptosis through induction of loss of mitochondrial membrane potential in CCRF-CEM cells

Avcı

Gündüz

Baran

et al. 2010

J Cancer Res Clin Oncol

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Purpose CAPE (caffeic acid phenethyl ester) is one of the most valuable and investigated component of propolis which is composed by honeybees. In the current study, we aimed at examining apoptotic effects of CAPE on CCRF-CEM leukemic cells and at determining the roles of mitochondrial membrane potential (MMP) in cell death. Methods Trypan blue and XTT methods were used to evaluate the cytotoxicity. Apoptosis was examined by ELISA-based oligonucleotide and acridine orange/ethidium bromide dye techniques. Loss of mitochondrial membrane potential was evaluated using JC-1 dye by flow cytometric analysis and under fluorescent microscope. Results We detected the time-and dose-dependent increases in cytotoxic effect of CAPE on CCRF-CEM cells. ELISA and acridine orange/ethidium bromide results showed that apoptotic cell population increased significantly in CCRF-CEM cells exposed to increasing concentrations of CAPE. On the other hand, there was significant loss of MMP determined in response to CAPE in CCRF-CEM cells.Conclusion This in vitro data by being supported with clinical data may open the way of the potential use of CAPE for the treatment of leukemia.

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Section: Discussionmentioning

confidence: 99%

Section: Introductionmentioning

confidence: 99%

Caffeic acid phenethyl ester triggers apoptosis through induction of loss of mitochondrial membrane potential in CCRF-CEM cells

Avcı

Gündüz

Baran

et al. 2010

J Cancer Res Clin Oncol

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“…The relative inhibitory potencies of BEA, EN I and EN MK1688 on HIV-1 integrase were comparable to those of baicalein (IC 50 , 1.2 mM) and robinetin (IC 50 , 5.9±1.9 mM), which are strong HIV-1 integrase inhibitors. 19 Lutzke et al 20 reported a hexapeptide inhibitor of HIV-1 integrase, the sequence of which is HCKFWW, and suggested that it acts at or near the catalytic site of integrase. Owing to their structural characteristics, cyclic hexadepsipeptides could inhibit the oligomerization of the enzyme that is essential for catalytic activity.…”

Section: Evaluation Of Anti-reverse Transcriptase Activitymentioning

confidence: 99%

Beauvericin and enniatins H, I and MK1688 are new potent inhibitors of human immunodeficiency virus type-1 integrase

Shin

Song

et al. 2009

J Antibiot

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Some enniatins (ENs) reportedly exhibit antiretroviral activities in vivo. The potential inhibitory activities of cyclic hexadepsipeptides such as beauvericin (BEA) and ENs H, I and MK1688 were investigated in vitro against human immunodeficiency virus type-1 (HIV-1) integrase and Moloney murine leukemia virus reverse transcriptase. BEA, EN I and EN MK1688 exhibited strong inhibitory activities against HIV-1 integrase, whereas EN H showed relatively weak activity. None of the examined compounds showed anti-reverse transcriptase activity. BEA was the most effective inhibitor of the tested cyclic hexadepsipeptides in inhibiting HIV-1 integrase. These results indicate the potential of cyclic hexadepsipeptides as a new class of potent inhibitors of HIV-1 integrase.

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“…The antioxidant effectiveness of hydroxyflavones has also been related to the number of hydroxyl groups in the molecule, and also to their hydrogen radical donating abilities [2]. In relation to their antioxidant properties, beneficial effects of flavones have also been reported for cancer [3], bacterial [1,4] or viral infections [5] and inflammatory diseases [4,6].…”

Section: Introductionmentioning

confidence: 99%

The alkyl chain length of 3-alkyl-3′,4′,5,7-tetrahydroxyflavones modulates effective inhibition of oxidative damage in biological systems: Illustration with LDL, red blood cells and human skin keratinocytes

Filipe¹,

Silva²,

Seixas³

et al. 2009

Biochemical Pharmacology

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Please cite this article as: Filipe P, Silva AMS, Seixas RSGR, Pinto DCGA, Santos A, Patterson LK, Silva JN, Cavaleiro JAS, Freitas JP, Mazière J-C, Santus R, Morlière P, The alkyl chain length of 3-alkyl-3',4',5,7-tetrahydroxyflavones modulates effective inhibition of oxidative damage in biological systems: illustration with LDL, red blood cells and human skin keratinocytes, Biochemical Pharmacology (2008), doi:10.1016/j.bcp.2008 This is a PDF file of an unedited manuscript that has been accepted for publication. As a service to our customers we are providing this early version of the manuscript. The manuscript will undergo copyediting, typesetting, and review of the resulting proof before it is published in its final form. Please note that during the production process errors may be discovered which could affect the content, and all legal disclaimers that apply to the journal pertain. A c c e p t e d M a n u s c r i p t 1 2 3 4 5 6 7 8 9 10 11 12 13 14 15 16 17 18 19 20 21 22 23 24 25 26 27 28 29 30 31 32 33 34 35 36 37 38 39 40 41 42 43 44 45 46 47 48 49 50 51 52 53 54 55 56 57 58 59 60 61 62 63 64 production. The F1H, F4H and Q are found rather inactive under these conditions. At concentrations in the micromolar range, a marked protection against the cytotoxic effects of the t-BuOOH-induced oxidative stress in human skin NCTC 2544 keratinocytes is also exhibited by the four FnH antioxidants and is comparable to that of Q. Thus, the four FnH species under study may be considered as potent antioxidants which manifest complementary anti-oxidative actions in biological systems of markedly different complexity.

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Inhibition of HIV-1 integrase by flavones, caffeic acid phenethyl ester (CAPE) and related compounds

Cited by 315 publications

References 42 publications

Caffeic acid phenethyl ester triggers apoptosis through induction of loss of mitochondrial membrane potential in CCRF-CEM cells

Caffeic acid phenethyl ester triggers apoptosis through induction of loss of mitochondrial membrane potential in CCRF-CEM cells

Beauvericin and enniatins H, I and MK1688 are new potent inhibitors of human immunodeficiency virus type-1 integrase

The alkyl chain length of 3-alkyl-3′,4′,5,7-tetrahydroxyflavones modulates effective inhibition of oxidative damage in biological systems: Illustration with LDL, red blood cells and human skin keratinocytes

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