scholarly journals Anti-HIV-1 activity in human primary cells and Anti-HIV-1 RT inhibitory activity of extracts from the red seaweed Acanthophora spicifera

2016 ◽  
Vol 10 (35) ◽  
pp. 621-625 ◽  
Author(s):  
Cesar Richter Nogueira Caio ◽  
Christina Nunes de Palmer Paixão Izabel ◽  
Cesar Cirne-Santos Claudio ◽  
Roberto Soares Stephens Paulo ◽  
Campos Villaça Roberto ◽  
...  
Keyword(s):  
Inhibitory Activity ◽  
Red Seaweed ◽  
Primary Cells ◽  
Human Primary Cells ◽  
Anti Hiv ◽  
Hiv 1

Synthesis and anti-HIV Activity of New Fused Chromene Derivatives Derived from 2-Amino-4-(1-naphthyl)-5-oxo-4H,5H-pyrano[3,2- c]chromene-3-carbonitrile

2013 ◽  
Vol 68 (3) ◽  
pp. 229-238 ◽  
Author(s):  
Najim A. Al-Masoudi ◽  
Hamid H. Mohammed ◽  
Aws M. Hamdy ◽  
Omer A. Akrawi ◽  
Nadi Eleya ◽  
...  
Keyword(s):  
Spectral Data ◽  
Inhibitory Activity ◽  
Activity Screening ◽  
Anti Hiv ◽  
Hiv 1

A new series of pyrano-chromene and pyrimido pyrano-chromene derivatives were synthesized starting from 2-amino-4-(1-naphthyl)-5-oxo-4H,5H-pyrano[3,2-c]chromene-3-carbonitrile (6). The structures of the synthesized compounds were elucidated by spectral data. Compounds 6-11, 13-15 and 18 have been selected for an inhibitory activity screening against HIV-1 and HIV-2 in MT-4 cells.

scholarly journals Inhibition of Human Immunodeficiency Virus Type 1 Infectivity by Secretory Leukocyte Protease Inhibitor Occurs Prior to Viral Reverse Transcription

Blood ◽  
1997 ◽  
Vol 90 (3) ◽  
pp. 1141-1149 ◽  
Author(s):  
Tessie B. McNeely ◽  
Diane C. Shugars ◽  
Mary Rosendahl ◽  
Christina Tucker ◽  
Stephen P. Eisenberg ◽  
...  
Keyword(s):  
Human Immunodeficiency Virus ◽  
Protease Inhibitor ◽  
Viral Infection ◽  
Reverse Transcription ◽  
Inhibitory Activity ◽  
Virus Binding ◽  
Viral Dna ◽  
Immunodeficiency Virus ◽  
Anti Hiv ◽  
Hiv 1

Abstract Infection of monocytes with human immunodeficiency virus type 1Ba-L (HIV-1Ba-L ) is significantly inhibited by treatment with the serine protease inhibitor, secretory leukocyte protease inhibitor (SLPI). SLPI does not appear to act on virus directly, but rather the inhibitory activity is most likely due to interaction with the host cell. The current study was initiated to investigate how SLPI interacts with monocytes to inhibit infection. SLPI was found to bind to monocytes with high affinity to a single class of receptor sites (∼7,000 receptors per monocyte, KD = 3.6 nmol/L). The putative SLPI receptor was identified as a surface protein with a molecular weight of 55 ± 5 kD. A well-characterized function of SLPI is inhibition of neutrophil elastase and cathepsin G. However, two SLPI mutants (or muteins) that contain single amino acid substitutions and exhibit greatly reduced protease inhibitory activity still bound to monocytes and retained anti–HIV-1 activity. SLPI consists of two domains, of which the C-terminal domain contains the protease inhibiting region. However, when tested independently, neither domain had potent anti–HIV-1 activity. SLPI binding neither prevented virus binding to monocytes nor attenuated the infectivity of any virus progeny that escaped inhibition by SLPI. A polymerase chain reaction (PCR)-based assay for newly generated viral DNA demonstrated that SLPI blocks at or before viral DNA synthesis. Therefore, it most likely inhibits a step of viral infection that occurs after virus binding but before reverse transcription. Taken together, the unique antiviral activity of SLPI, which may be independent of its previously characterized antiprotease activity, appears to reside in disruption of the viral infection process soon after virus binding.

scholarly journals Synergistic Combinations of the CCR5 Inhibitor VCH-286 with Other Classes of HIV-1 Inhibitors

2014 ◽  
Vol 58 (12) ◽  
pp. 7565-7569 ◽  
Author(s):  
Odalis Asin-Milan ◽  
Mohamed Sylla ◽  
Mohamed El-Far ◽  
Geneviève Belanger-Jasmin ◽  
Alpha Haidara ◽  
...  
Keyword(s):  
Inhibitory Activity ◽  
Single Agent ◽  
Drug Classes ◽  
Additive Interactions ◽  
Anti Hiv ◽  
Ccr5 Inhibitor ◽  
Synergistic Combinations ◽  
Hiv 1

ABSTRACTHere, we evaluated thein vitroanti-HIV-1 activity of the experimental CCR5 inhibitor VCH-286 as a single agent or in combination with various classes of HIV-1 inhibitors. Although VCH-286 used alone had highly inhibitory activity, paired combinations with different drug classes led to synergistic or additive interactions. However, combinations with other CCR5 inhibitors led to effects ranging from synergy to antagonism. We suggest that caution should be exercised when combining CCR5 inhibitorsin vivo.

scholarly journals Anti-HIV-1 protease activity of the crude extracts and isolated compounds from Auricularia polytricha

2019 ◽  
Vol 19 (1) ◽  
Author(s):  
Chanin Sillapachaiyaporn ◽  
Sunita Nilkhet ◽  
Alison T. Ung ◽  
Siriporn Chuchawankul
Keyword(s):  
Natural Products ◽  
Inhibitory Activity ◽  
Edible Mushroom ◽  
2D Nmr ◽  
Antiretroviral Drugs ◽  
Significant Inhibition ◽  
Fatty Esters ◽  
Auricularia Polytricha ◽  
Anti Hiv ◽  
Hiv 1

Abstract Background Acquired immunodeficiency syndrome (AIDS) is caused by the Human immunodeficiency virus type-1 (HIV-1). HIV-1 protease (HIV-1 PR) is an essential enzyme for the HIV replication, and therefore, it is an important target for antiretroviral drugs development, particularly from natural products. Auricularia polytricha (AP) is an edible mushroom with several important therapeutic properties. These properties will be investigated as HIV-1 PR inhibitors. Methods The sequential hexane (APH), ethanol (APE) and water (APW) extracts from AP were screened for inhibitory activity against HIV-1 PR. The extract that consistently showed the strong HIV-1 PR inhibition was further investigated for its phytochemical constituents. The compounds were purified by column chromatography. The isolated compounds were structurally elucidated using 1D and 2D NMR, HRMS, FTIR, and GC/MS techniques. Each compound was screened against HIV-1 PR to determine its inhibitory activity and to provide an explanation for the activity found in the extract. Results Hexane crude extract of AP (APH) exhibited significant inhibition on HIV-1 PR activity. Four major compounds isolated from APH fraction were identified to be two triacylglycerols, linoleic acid and ergosterol. Moreover, all four compounds showed significant inhibition of HIV-1 PR activity. Conclusion The findings from this study suggest that AP is a good source of fatty esters, fatty acids and ergosterol. These natural products exhibit anti-HIV-1 properties by blocking HIV-1 PR. These important biological results warrant further development of AP as an alternative antiretroviral drug.

Naturally Occurring Pyrrolizidines: Inhibition of α-Glucosidase 1 and Anti-HIV Activity of One Stereoisomer

1992 ◽  
Vol 3 (5) ◽  
pp. 273-277 ◽  
Author(s):  
D. L. Taylor ◽  
R. Nash ◽  
L. E. Fellows ◽  
M. S. Kang ◽  
A. S. Tyms
Keyword(s):  
Inhibitory Activity ◽  
Pyrrolizidine Alkaloid ◽  
Virus Growth ◽  
Processing Enzymes ◽  
Naturally Occurring ◽  
Antiviral Effects ◽  
Castanospermum Australe ◽  
Glycoprotein Processing ◽  
Anti Hiv ◽  
Hiv 1

Alexine, a naturally occurring pyrrolizidine alkaloid, isolated from Alexa leiopetala, and four stereoisomers, isolated from Castanospermum australe, were investigated for inhibitory activity against the growth of HIV-1. Only treatment with the 7,7a-diepialexine restricted virus growth (IC50 0.38 mm) although it was less active than the indolizidine alkaloid castanospermine (IC50 0.02 mm). The antiviral effects of 7,7a-diepialexine, like castanospermine, correlated with the inhibitory activity against purified pig kidney α-glucosidase 1 of the glycoprotein processing enzymes and the reduced cleavage of the precursor HIV-1 glycoprotein gp160.

scholarly journals Inhibition of Human Immunodeficiency Virus Type 1 Infectivity by Secretory Leukocyte Protease Inhibitor Occurs Prior to Viral Reverse Transcription

Blood ◽  
1997 ◽  
Vol 90 (3) ◽  
pp. 1141-1149 ◽  
Author(s):  
Tessie B. McNeely ◽  
Diane C. Shugars ◽  
Mary Rosendahl ◽  
Christina Tucker ◽  
Stephen P. Eisenberg ◽  
...  
Keyword(s):  
Human Immunodeficiency Virus ◽  
Protease Inhibitor ◽  
Viral Infection ◽  
Reverse Transcription ◽  
Inhibitory Activity ◽  
Virus Binding ◽  
Viral Dna ◽  
Immunodeficiency Virus ◽  
Anti Hiv ◽  
Hiv 1

Infection of monocytes with human immunodeficiency virus type 1Ba-L (HIV-1Ba-L ) is significantly inhibited by treatment with the serine protease inhibitor, secretory leukocyte protease inhibitor (SLPI). SLPI does not appear to act on virus directly, but rather the inhibitory activity is most likely due to interaction with the host cell. The current study was initiated to investigate how SLPI interacts with monocytes to inhibit infection. SLPI was found to bind to monocytes with high affinity to a single class of receptor sites (∼7,000 receptors per monocyte, KD = 3.6 nmol/L). The putative SLPI receptor was identified as a surface protein with a molecular weight of 55 ± 5 kD. A well-characterized function of SLPI is inhibition of neutrophil elastase and cathepsin G. However, two SLPI mutants (or muteins) that contain single amino acid substitutions and exhibit greatly reduced protease inhibitory activity still bound to monocytes and retained anti–HIV-1 activity. SLPI consists of two domains, of which the C-terminal domain contains the protease inhibiting region. However, when tested independently, neither domain had potent anti–HIV-1 activity. SLPI binding neither prevented virus binding to monocytes nor attenuated the infectivity of any virus progeny that escaped inhibition by SLPI. A polymerase chain reaction (PCR)-based assay for newly generated viral DNA demonstrated that SLPI blocks at or before viral DNA synthesis. Therefore, it most likely inhibits a step of viral infection that occurs after virus binding but before reverse transcription. Taken together, the unique antiviral activity of SLPI, which may be independent of its previously characterized antiprotease activity, appears to reside in disruption of the viral infection process soon after virus binding.

Anti-HIV 1 Activity of Xanthones from the Bark of Mammea harmandii

2018 ◽  
Vol 13 (1) ◽  
pp. 1934578X1801300 ◽  
Author(s):  
Ponsiri Liangsakul ◽  
Chutima Kuhakarn ◽  
Sakchai Hongthong ◽  
Surawat Jariyawat ◽  
Kanoknetr Suksen ◽  
...  
Keyword(s):  
Reverse Transcriptase ◽  
Ethyl Acetate ◽  
Cytotoxic Activity ◽  
Inhibitory Activity ◽  
Spectroscopic Data ◽  
Methanol Extract ◽  
Ethyl Acetate Fraction ◽  
Chemical Structures ◽  
Anti Hiv ◽  
Hiv 1

A new xanthone glycoside 1 together with four known flavonoid derivatives, astilbin (2), neoastilbin (3), isoastilbin (4), and epicatechin (5) were isolated from the ethyl acetate fraction partitioned from the methanol extract of the bark of Mammea harmandii. The chemical structures of all isolated compounds were established on the basis of their spectroscopic data. Compound 1 exhibited selective significant inhibitory activity in the anti-syncytium assay with an EC50 value of 11.44 μM (SI = 14.03) while it was found inactive against HIV 1 reverse transcriptase as well as cytotoxic activity.

scholarly journals Anti-HIV Activity of Alkaloids from Dasymaschalon echinatum

2018 ◽  
Vol 13 (1) ◽  
pp. 1934578X1801300 ◽  
Author(s):  
Samreang Bunteang ◽  
Waraporn Chanakul ◽  
Sakchai Hongthong ◽  
Chutima Kuhakarn ◽  
Watcharra Chintakovid ◽  
...  
Keyword(s):  
Reverse Transcriptase ◽  
Inhibitory Activity ◽  
First Report ◽  
Aerial Parts ◽  
Amide Derivatives ◽  
Bioassay Guided Fractionation ◽  
First Time ◽  
Anti Hiv ◽  
Hiv 1

Bioassay-guided fractionation of the aerial parts of Dasymaschalon echinatum led to the isolation of five known aristolactams; aristolactam AII (1), aristolactam BII (2), piperolactam A (3), piperolactam C (4), and goniopedaline (5), together with two aphorphine alkaloids; duguevalline (6) and noraristolodione (7) and two amide derivatives; asperphenamate (8), and N -benzoyl-L-phenylalaninol (9). Alkaloids 2 and 7 were isolated for the first time from the Dasymaschalon genus. The anti-HIV 1 reverse transcriptase (RT) activity of all isolated compounds was determined. Except for aristolactam BII (2), this is the first report of the anti-HIV 1-RT activity of compounds 1 and 3-9. Compounds 1, 3, 5, 6 and 8 showed weak anti-HIV 1-RT inhibitory activity with IC50 ranging from 112.74 to 225.55μM.

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