A Homodimeric Sporamin-Type Trypsin Inhibitor with Antiproliferative, HIV Reverse Transcriptase-Inhibitory and Antifungal Activities from Wampee (Clausena lansium) Seeds

2003 ◽  
Vol 384 (2) ◽  
pp. 289-293 ◽  
Author(s):  
T.B. Ng ◽  
S.K. Lam ◽  
W.P. Fong
Keyword(s):  
Reverse Transcriptase ◽  
Trypsin Inhibitor ◽  
Simple Procedure ◽  
Inhibitory Effect ◽  
Exchange Chromatography ◽  
Proteinase K ◽  
Human Leukemia ◽  
Hiv Reverse Transcriptase ◽  
Rabbit Reticulocyte Lysate System ◽  
Reticulocyte Lysate

Abstract A homodimeric trypsin inhibitor with a molecular mass of 54 kDa was isolated from the seeds of Clausena lansium (Lour) Skeels with a very simple procedure comprising extraction with an aqueous buffer and ion exchange chromatography on CM-cellulose. It inhibited trypsin with an IC50 of 2.2 nM but was without any inhibitory effect on chymotrypsin and proteinase K. The uptake of MTT by human leukemia HL60 and hepatoma Hep G2 cells was inhibited with an IC50 of 100 uM. Translation in the cellfree rabbit reticulocyte lysate system was inhibited with an IC50 of 3.6 uM. The activity of HIV-1 reverse transcriptase was reduced in the presence of the trypsin inhibitor. The trypsin inhibitor exerted antifungal activity toward Physalospora piricola but not Mycosphaerella arachidicola, Botrytis cinerea, Fusarium oxysporum or Coprinus comatus.

Anti-Aids Agents, 2: Inhibitory Effect of Tannins on HIV Reverse Transcriptase and HIV Replication in H9 Lymphocyte Cells

1990 ◽  
Vol 53 (3) ◽  
pp. 587-595 ◽  
Author(s):  
Gen-ichiro Nonaka ◽  
Itsuo Nishioka ◽  
Makoto Nishizawa ◽  
Takashi Yamagishi ◽  
Yoshiki Kashiwada ◽  
...  
Keyword(s):  
Reverse Transcriptase ◽  
Inhibitory Effect ◽  
Hiv Reverse Transcriptase ◽  
Hiv Replication

Evaluation and characterization of trypsin inhibitor from rice bean with inhibitory activity against gut proteases of Spodoptera litura

2015 ◽  
Vol 70 (11-12) ◽  
pp. 287-295
Author(s):  
Rajan Katoch ◽  
Kanika Sharma ◽  
Sunil Kumar Singh ◽  
Neelam Thakur
Keyword(s):  
Trypsin Inhibitor ◽  
Spodoptera Litura ◽  
Insect Pests ◽  
Inhibitory Effect ◽  
Exchange Chromatography ◽  
Rice Bean ◽  
Growth And Survival ◽  
Potential Strategy ◽  
The Stability

Abstract Trypsin inhibitor (TI) in rice bean (Vigna umbellata) varied spatio-temporally in different parts of the plant, with the highest level (30.9 mg/g d.w.) noted in the maturing seeds of genotype BRS-2 at 160 days after planting (DAP). The TI from rice bean seeds was isolated and purified approximately 182-fold, with a final yield of 29% using ammonium sulfate precipitation, ion exchange chromatography through DEAE-Sepharose, gel permeation through Superdex-75, and finally by affinity chromatography using a trypsin-Sepharose column. The purified TI showed a single band on SDS-PAGE under reducing conditions with an apparent molecular mass of 24 kDa. The highest activity of purified inhibitor (about 90%) was recorded at pH 4.0 at 37 °C, suggesting the stability of the inhibitor under acidic conditions. The TI exhibited an inhibitory effect against Spodoptera litura larvae. A progressive decline in larval weight, growth, and survival rate of larval development was observed after feeding S. litura larvae on a diet supplemented with increasing concentrations of rice bean TI. The highest TI content in the seeds nearing maturity correlates to the role of TIs in protecting against insect pests. The study clarifies the role of rice bean protease inhibitors as a potential strategy against insectpests of economic importance.

RNA aptamers and HIV reverse transcriptase : molecular basis of their interactions and the evaluation of aptamer resistance

2019 ◽  
Author(s):  
◽  
Phuong Dinh Minh Nguyen
Keyword(s):  
Reverse Transcriptase ◽  
Reverse Transcription ◽  
Immune Deficiency Syndrome ◽  
Inhibitory Effect ◽  
Proteolytic Processing ◽  
Rna Aptamers ◽  
Rna Aptamer ◽  
Hiv Reverse Transcriptase ◽  
Functional Features ◽  
Hiv Rt

[ACCESS RESTRICTED TO THE UNIVERSITY OF MISSOURI AT REQUEST OF AUTHOR.] Human Immunodeficiency virus (HIV) is a pandemic Lentivirus that causes acquired immune deficiency syndrome (AIDS) in infected individuals. One of the critical steps in HIV replication is the reverse transcription of viral RNA to generate viral DNA, which will be integrated into the host genome to generate materials for the production of new viruses. The enzyme responsible for this reverse transcription process is HIV reverse transcriptase (RT). Because of its importance in HIV life cycle, RT has been a common target for HIV inhibitors. In recent years, RNA aptamers have emerged as potential inhibitors against HIV RT. Although previous studies had shown that the inhibitory effect of RNA aptamers against HIV RT comes from their ability to compete with primer/template for binding to RT, the molecular details of RT-RNA aptamer interaction are still limited. The work described herein highlights advancements in identifying the functional features of a broad-spectrum RNA aptamer and elucidating the molecular details in the interaction of this aptamer and the target RT. Furthermore, this work explores the potential use of anti HIV aptamers in studying RT maturation by proteolytic processing.

Inhibitory effect against polymerase and ribonuclease activities of HIV-reverse transcriptase of the aqueous leaf extract ofTerminalia triflora

2002 ◽  
Vol 16 (8) ◽  
pp. 778-780 ◽  
Author(s):  
V. S. Martino ◽  
P. López ◽  
J. J. Martinez Irujo ◽  
M. Sanromán ◽  
M. T. Cuevas ◽  
...  
Keyword(s):  
Reverse Transcriptase ◽  
Leaf Extract ◽  
Inhibitory Effect ◽  
Hiv Reverse Transcriptase ◽  
Aqueous Leaf Extract

scholarly journals Inhibitory Effect of 2,3,5,6-Tetrafluoro-4-[4-(aryl)-1H-1,2,3-triazol-1-yl]benzenesulfonamide Derivatives on HIV Reverse Transcriptase Associated RNase H Activities

2016 ◽  
Vol 17 (8) ◽  
pp. 1371 ◽  
Author(s):  
Nicolino Pala ◽  
Francesca Esposito ◽  
Dominga Rogolino ◽  
Mauro Carcelli ◽  
Vanna Sanna ◽  
...  
Keyword(s):  
Reverse Transcriptase ◽  
Inhibitory Effect ◽  
Rnase H ◽  
Hiv Reverse Transcriptase

New Efavirenz Derivatives and 1,2,3-Triazolyl-phosphonates as Inhibitors of Reverse Transcriptase of HIV-1

2018 ◽  
Vol 18 (17) ◽  
pp. 1494-1505 ◽  
Author(s):  
Carolina C.P. Costa ◽  
Nubia Boechat ◽  
Monica M. Bastos ◽  
Fernando de C. da Silva ◽  
Andressa Marttorelli ◽  
...  
Keyword(s):  
Reverse Transcriptase ◽  
Triazole Ring ◽  
Biological Evaluation ◽  
World Health ◽  
Hiv Reverse Transcriptase ◽  
Ic50 Values ◽  
Health Organization ◽  
Hiv Drugs ◽  
Immunodeficiency Syndrome ◽  
New Compounds

Background: According to the World Health Organization (WHO), the fight against Acquired Immunodeficiency Syndrome (AIDS) is still one of the most significant challenges facing humanity. Worldwide, it is estimated that 36.7 million people are infected by the Human Immunodeficiency Virus (HIV). Despite the variety of available drugs, the search for new enzymatic inhibitors of HIV is still important due to the presence of adverse effects and the development of resistant strains. Therefore, the present study aimed to design, synthesize, and biologically evaluate novel inhibitors of HIV Reverse Transcriptase (RT). Materials and Methods: These compounds were obtained in two series, and compounds in both series contain a 1,2,3-triazole ring in their structures. The compounds in the first series are Efavirenz (EFV) analogues with the N-1 position substituted by another important fragment as described in the medicinal chemistry literature on anti-HIV drugs. The second series has a phosphonate chain similar to that in the structure of Tenofovir Disoproxil Fumarate (TDF). Results and Conclusion: The results of the biological evaluation showed that all compounds presented high RT inhibition values and lower or comparable inhibitory concentrations (the concentration needed to reduce the enzymatic activity by 50%, IC50 values, 0.8-1.9 µM). Among the compounds in the first series, the three with the lowest IC50 values had values between 0.8-0.9 µM, and of those in the second series, the most potent had an IC50 value of 1.1 µM; compounds in both series were equipotent to TDF (1.2 µM). Thus, the new compounds could be considered lead compounds for the development of new antiretroviral compounds.

scholarly journals Interaction of HIV reverse transcriptase with structures mimicking recombination intermediates.

2003 ◽  
Vol 278 (30) ◽  
pp. 28354-28355
Author(s):  
Aarti Raja ◽  
Jeffrey J. DeStefano
Keyword(s):  
Reverse Transcriptase ◽  
Hiv Reverse Transcriptase

scholarly journals Use of an Oligoribonucleotide Containing the Polypurine Tract Sequence as a Primer by HIV Reverse Transcriptase

1995 ◽  
Vol 270 (47) ◽  
pp. 28169-28176 ◽  
Author(s):  
Gloria M. Fuentes ◽  
Lorna Rodríguez-Rodríguez ◽  
Philip J. Fay ◽  
Robert A. Bambara
Keyword(s):  
Reverse Transcriptase ◽  
Hiv Reverse Transcriptase ◽  
Polypurine Tract
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