In vitro Anti-HIV and Antimicrobial Activities of a Halogenated Monoterpene from a Namibian Plocamium Species of Marine Algae

2020 ◽  
Vol 16 (3) ◽  
pp. 363-367
Author(s):  
Aina N. Shiyanga ◽  
Michael Knott ◽  
Petrina Kapewangolo
Keyword(s):  
Antibacterial Activity ◽  
Reverse Transcriptase ◽  
Biological Activities ◽  
Red Alga ◽  
Diffusion Method ◽  
Klebsiella Pneumonia ◽  
Halogenated Monoterpenes ◽  
Anti Hiv ◽  
Hiv 1

Background: The marine red alga Plocamium naturally produces halogenated monoterpenes with varied biological activities. In our continuing efforts to discover new lead compounds for the treatment of HIV/AIDS as well as novel antibacterial compounds, various Namibian Plocamium species have been investigated. Methods: A rare but known compound namely 1E,3R,4S,5E,7Z-1-bromo-3,4,8-trichloro-7- (dichloromethyl)-3-methylocta-1,5,7-triene (1) was isolated from a Namibian Plocamium red alga. The anti-HIV activity of compound 1 was investigated against three HIV enzymes namely, HIV protease, reverse transcriptase and integrase. In addition, compound 1 was also screened for antibacterial activity against selected microbes using the disc diffusion method. Results: Compound 1 demonstrated selective in vitro inhibition against HIV-1 integrase with a 50% inhibition concentration of <0.06 mM. Weak inhibitory activity was observed against HIV-1 reverse transcriptase and protease. Compound 1 also showed antibacterial activity against Staphylococcus aureus (ATCC 25923), Alcaligenes faecalis (ATCC 8750) and Serratia marcescens (ATCC 8100) with MIC values of 0.65 mM, and 1.29 mM for Klebsiella pneumonia (ATCC 13883). Conclusion: The results of this study highlight the potential of halogenated monoterpenes from red seaweed as possible leads in the development of new anti-HIV and antimicrobial pharmaceuticals.

scholarly journals Glycosylated Flavonoids from Psidium guineense as Major Inhibitors of HIV-1 Replication in vitro

2017 ◽  
Vol 12 (7) ◽  
pp. 1934578X1701200
Author(s):  
Joseph T Ortega ◽  
Omar Estrada ◽  
Maria L Serrano ◽  
Whendy Contreras ◽  
Giovannina Orsini ◽  
...  
Keyword(s):  
Antiviral Activity ◽  
Reverse Transcriptase ◽  
In Silico ◽  
Biological Activities ◽  
In Silico Prediction ◽  
Flavonoid Quercetin ◽  
Derivatives Of ◽  
Anti Hiv ◽  
Hiv 1

Flavonoids are present in practically all plants and many biological activities have been described for them. The flavonoid quercetin is a common molecule for which anti-HIV activity has been demonstrated. Avicularin and guajaverin are derivatives of quercetin with a glycoside substituent in their structure. In this work, a mixture of both derivatives was purified from an extract of Psidium guinense. The mixture exhibited activity against HIV-1 in vitro, with an IC50 of approximately 8.5 μg/mL, which compares favorably with the IC50 of 53 μg/mL of quercetin. The mixture also inhibited HIV-1 reverse transcriptase (RT), with an IC50 of 7.2 μM, compared to 0.6 μM for quercetin. These results are in agreement with the in silico prediction for the interaction of these flavonoids with RT and suggest that the glycosylic moiety could favor the transport of the compound into the cell. However, the glycosidic moiety might be cleaved intracellularly, being the resultant quercetin responsible for the antiviral activity.

An Approach towards the Synthesis of Potential Metal-Chelating TSAO-T Derivatives as Bidentate Inhibitors of Human Immunodeficiency virus Type 1 Reverse Transcriptase

1998 ◽  
Vol 9 (5) ◽  
pp. 412-421 ◽  
Author(s):  
C Chamorro ◽  
M-J Camarasa ◽  
M-J Pérez-Pérez ◽  
E de Clercq ◽  
J Balzarini ◽  
...  
Keyword(s):  
Human Immunodeficiency Virus ◽  
Reverse Transcriptase ◽  
Human Immunodeficiency Virus Type ◽  
Virus Type ◽  
Parent Compound ◽  
Immunodeficiency Virus ◽  
Anti Hiv ◽  
Hiv 1

Novel derivatives of the potent human immunodeficiency virus type 1 (HIV-1) reverse transcriptase (RT) inhibitor TSAO-T have been designed, synthesized and tested for their in vitro antiretro-viral activity against HIV. These TSAO-T derivatives have been designed as potential bidentate inhibitors of HIV-1 RT, which combine in their structure the functionality of a non-nucleoside RT inhibitor (TSAO-T) and a bivalent ion-chelating moiety (a β-diketone moiety) linked through an appropriate spacer to the N-3 of thymine of TSAO-T . Some of the new compounds have an anti-HIV-1 activity comparable to that of the parent compound TSAO-T, but display a markedly increased antiviral selectivity. There was a clear relationship between antiviral activity and the length of the spacer group that links the TSAO molecule with the chelating moiety. A shorter spacer invariably resulted in increased antiviral potency. None of the TSAO-T derivatives were endowed with anti-HIV-2 activity.

scholarly journals Antibacterial and Toxicity Evaluation of Eastern Medicine Formulation Eczegone for the Management of Eczema

Dose-Response ◽  
2020 ◽  
Vol 18 (3) ◽  
pp. 155932582095679
Author(s):  
Muhammad Amjad Chishti ◽  
Ejaz Mohi-Ud-Din ◽  
Shahbaz Ahmad Zakki ◽  
Muhammad Rahil Aslam ◽  
Sheraz Siddiqui ◽  
...  
Keyword(s):  
Antibacterial Activity ◽  
Safety Evaluation ◽  
Diffusion Method ◽  
In Vitro Toxicity ◽  
Klebsiella Pneumonia ◽  
Lawsonia Inermis ◽  
Disk Diffusion Method ◽  
Skin Keratinocytes

The present study was conducted to evaluate the antibacterial activity, in vitro and in vivo cytotoxicity, cell viability and safety of Eastern Medicine coded medicinal formulation Eczegone comprising extracts of Azadirachta indica (Azin) , Fumaria indica (Fuin) , Sphaeranthus indicus (Spin) and Lawsonia inermis (Lain). This work also evaluated antibacterial activity of Eczegone formulation having above mentioned plants ethanolic extracts against different bacteria’s by disk diffusion method. In vitro toxicity of Eczegone formulation was investigated by using human skin keratinocytes HaCaT cell line, crystal violet stained cells, and methyl tetrazolium cytotoxicity (MTT) assay. In vivo acute oral and dermal cytotoxicity was determined by using Swiss albino mice and albino rabbits, respectively. The Eczegone formulation showed antibacterial activity against 3 gram negative bacteria including Escherichia coli, Klebsiella pneumonia, Proteus vulgaris and a gram positive Staphylococcus aureus. We didn’t observe any toxic effect of Eczegone formulation on the skin keratinocytes. Furthermore, the Ezcegone formulation was non-irritant according to draize score (OECD TG404, 2002). After rigorous safety evaluation by in vitro and in vivo acute oral and dermal toxicity analysis, we concluded that Eczegone formualtion possessses antibacterial effects and is safe, non-toxic, non-irritant, and the drug would be subjected for further biochemical and clinical studies.

Sensitivity of V75I HIV-1 reverse transcriptase mutant selected in vitro by acyclovir to anti-HIV drugs

AIDS ◽  
2010 ◽  
Vol 24 (2) ◽  
pp. 319-323 ◽  
Author(s):  
Moira A McMahon ◽  
Janet D Siliciano ◽  
Rahul M Kohli ◽  
Robert F Siliciano
Keyword(s):  
Reverse Transcriptase ◽  
Hiv Drugs ◽  
Anti Hiv ◽  
Hiv 1

scholarly journals In Vitro Antiviral Activity of the Novel, Tyrosyl-Based Human Immunodeficiency Virus (HIV) Type 1 Protease Inhibitor Brecanavir (GW640385) in Combination with Other Antiretrovirals and against a Panel of Protease Inhibitor-Resistant HIV

2007 ◽  
Vol 51 (9) ◽  
pp. 3147-3154 ◽  
Author(s):  
Richard Hazen ◽  
Robert Harvey ◽  
Robert Ferris ◽  
Charles Craig ◽  
Phillip Yates ◽  
...  
Keyword(s):  
Human Immunodeficiency Virus ◽  
Antiviral Activity ◽  
Protease Inhibitor ◽  
Reverse Transcriptase ◽  
In Vitro Assays ◽  
Immunodeficiency Virus ◽  
Anti Hiv ◽  
Hiv 1

ABSTRACT Brecanavir, a novel tyrosyl-based arylsulfonamide, high-affinity, human immunodeficiency virus type 1 (HIV-1) protease inhibitor (PI), has been evaluated for anti-HIV activity in several in vitro assays. Preclinical assessment of brecanavir indicated that this compound potently inhibited HIV-1 in cell culture assays with 50% effective concentrations (EC50s) of 0.2 to 0.53 nM and was equally active against HIV strains utilizing either the CXCR4 or CCR5 coreceptor, as was found with other PIs. The presence of up to 40% human serum decreased the anti-HIV-1 activity of brecanavir by 5.2-fold, but under these conditions the compound retained single-digit nanomolar EC50s. When brecanavir was tested in combination with nucleoside reverse transcriptase inhibitors, the antiviral activity of brecanavir was synergistic with the effects of stavudine and additive to the effects of zidovudine, tenofovir, dideoxycytidine, didanosine, adefovir, abacavir, lamivudine, and emtricitabine. Brecanavir was synergistic with the nonnucleoside reverse transcriptase inhibitor nevirapine or delavirdine and was additive to the effects of efavirenz. In combination with other PIs, brecanavir was additive to the activities of indinavir, lopinavir, nelfinavir, ritonavir, amprenavir, saquinavir, and atazanavir. Clinical HIV isolates from PI-experienced patients were evaluated for sensitivity to brecanavir and other PIs in a recombinant virus assay. Brecanavir had a <5-fold increase in EC50s against 80% of patient isolates tested and had a greater mean in vitro potency than amprenavir, indinavir, lopinavir, atazanavir, tipranavir, and darunavir. Brecanavir is by a substantial margin the most potent and broadly active antiviral agent among the PIs tested in vitro.

Synthesis and anti-HIV-1 Activity of [1-[2′,5′-Bis-O-(Tert-Butyldimethylsilyl)-β-L-Ribofuranosyl]Thymine]-3′-Spiro-5″-(4″-Amino-1″,2″-Oxathiole-2″,2″-Dioxide) (L-TSAO-T), the L-enantiomer of the Highly Specific HIV-1 Reverse Transcriptase Inhibitor TSAO-T

1995 ◽  
Vol 6 (6) ◽  
pp. 365-370 ◽  
Author(s):  
S. T. Ingate ◽  
M.-J. Camarasa ◽  
E. De Clercq ◽  
J. Balzarini
Keyword(s):  
Reverse Transcriptase ◽  
Transcriptase Inhibitor ◽  
Reverse Transcriptase Inhibitor ◽  
Anti Hiv ◽  
Hiv 1 ◽  
Antiretroviral Activity

The L-isomer of the potent HIV-1-RT inhibitor TSAO-T has been stereospecifically synthesized and tested for its ‘ in vitro’ antiretroviral activity against HIV-1. Unlike the D-isomer, the L-isomer did not show appreciable inhibition of HIV-1 replication. The cytotoxicity was comparable with the cytotoxicity of the D-enantiomer.

scholarly journals HIV-1 Protease and Reverse Transcriptase Inhibitory Activities of Curcuma aeruginosa Roxb. Rhizome Extracts and the Phytochemical Profile Analysis: In Vitro and In Silico Screening

2021 ◽  
Vol 14 (11) ◽  
pp. 1115
Author(s):  
Chanin Sillapachaiyaporn ◽  
Panthakarn Rangsinth ◽  
Sunita Nilkhet ◽  
Nuntanat Moungkote ◽  
Siriporn Chuchawankul
Keyword(s):  
Antioxidant Activity ◽  
Reverse Transcriptase ◽  
In Silico ◽  
Active Sites ◽  
Profile Analysis ◽  
Total Phenolic ◽  
Inhibitory Activities ◽  
Anti Hiv ◽  
Hiv 1

Human immunodeficiency virus type-1 (HIV-1) infection causes acquired immunodeficiency syndrome (AIDS). Currently, several anti-retroviral drugs are available, but adverse effects of these drugs have been reported. Herein, we focused on the anti-HIV-1 activity of Curcuma aeruginosa Roxb. (CA) extracted by hexane (CA-H), ethyl acetate (CA-EA), and methanol (CA-M). The in vitro HIV-1 protease (PR) and HIV-1 reverse transcriptase (RT) inhibitory activities of CA extracts were screened. CA-M potentially inhibited HIV-1 PR (82.44%) comparable to Pepstatin A (81.48%), followed by CA-EA (67.05%) and CA-H (47.6%), respectively. All extracts exhibited moderate inhibition of HIV-1 RT (64.97 to 76.93%). Besides, phytochemical constituents of CA extracts were identified by GC-MS and UPLC-HRMS. Fatty acids, amino acids, and terpenoids were the major compounds found in the extracts. Furthermore, drug-likeness parameters and the ability of CA-identified compounds on blocking of the HIV-1 PR and RT active sites were in silico investigated. Dihydroergocornine, 3β,6α,7α-trihydroxy-5β-cholan-24-oic acid, and 6β,11β,16α,17α,21-Pentahydroxypregna-1,4-diene-3,20-dione-16,17-acetonide showed strong binding affinities at the active residues of both HIV-1 PR and RT. Moreover, antioxidant activity of CA extracts was determined. CA-EA exhibited the highest antioxidant activity, which positively related to the amount of total phenolic content. This study provided beneficial data for anti-HIV-1 drug discovery from CA extracts.

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