Biomimetic synthesis and anti-HIV activity of dimeric phloroglucinols

Chauthe, Siddheshwar Kisan; Bharate, Sandip B.; Sabde, Sudeep; Mitra, Debashis; Bhutani, K. K.; Singh, Inder Pal

doi:10.1016/j.bmc.2010.01.023

Cited by 45 publications

(22 citation statements)

References 26 publications

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“…In fact, assays for detecting anti‐HIV activity utilized in the recent years by many authors actually involve CEM‐GFP as target cells. However, p24 release in supernatants [Ahmed et al, ; Brahmbhatt et al, ; Chauthe et al, ; Bodiwala et al, , ], fluorimetric detection of the absorbance of the samples in black optiplate [Kumari et al, ], both these two [Gruber et al, ; Modi et al, , ] or fluorescence values expressed as mean fluorescence intensity [Gruber et al, ], but in no case % of GFP positive cells, were used to calculate IC 50 values. Thus, all the above‐mentioned methods do not give information on number/percentage of cells in which HIV‐1 replication is impeded by the drug.…”

Section: Discussionmentioning

confidence: 99%

“…Following infection, the effect of HIV‐Tat on HIV‐LTR was responsible for GFP up‐regulation [Ramautar et al, ]. Several recent reports demonstrated that variants of this method could be useful to investigate the effects of compounds on HIV infection [Gruber et al, ; Ahmed et al, ; Brahmbhatt et al, ; Chauthe et al, ; Bodiwala et al, , ; Kumari et al, ; Modi et al, , ]. Surprisingly, however, inhibition of infection in no case was evaluated by flow cytometry analysis, expressed as % of GFP positive cells.…”

Section: Introductionmentioning

confidence: 99%

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Testing anti‐HIV activity of antiretroviral agents in vitro using flow cytometry analysis of CEM‐GFP cells infected with transfection‐derived HIV‐1 NL4‐3

Frezza

Grelli

Federico

et al. 2015

Journal of Medical Virology

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An assay, specifically optimized to evaluate the anti-HIV activity of antiretrovirals by flow cytometry analysis, is described. As widely used anti-HIV agents, zidovudine (AZT), abacavir (ABC), 2',3'-dideoxyinosine (DDI), lamivudine (3TC), nevirapine (NVP), and efavirenz (EFV), and as drugs of recent approval raltegravir (RAL), etravirine (ETR), and rilpivirine (RPV), were utilized as reference drugs. HIV-1 NL4-3 virus was prepared by transfection of HEK293T cells with purified plasmid DNA and quantified by p24 antigen-capture assay. For infection, CEM-GFP cells were exposed to vehicle or to several concentrations of the drugs for 2 hr at 37 °C before HIV-1 NL4-3 was added to each sample. The adsorption was prolonged for 3 hr at 37 °C. After 72 hr of incubation, HIV-induced GFP expression in infected CEM-GFP cells was assessed by flow cytometry analysis and expressed as % positive cells. For comparison, p24 production in supernatants was assessed by a commercial ELISA kit. On the basis of IC50 values, the anti-HIV activity, as assayed by this method, was EFV > 3TC > AZT > NVP > DDI > ABC and ETR > RPV > RAL. The comparison between the IC50 values calculated through flow cytometry and p24 production revealed overlapping results, showing that the optimized protocol of CEM-GFP infection with HIV NL4-3 is a suitable method to perform quantitative, rapid and low-expensive screening tests to evaluate the in vitro effect of new candidate anti-HIV drugs.

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Section: Discussionmentioning

confidence: 99%

Section: Introductionmentioning

confidence: 99%

Testing anti‐HIV activity of antiretroviral agents in vitro using flow cytometry analysis of CEM‐GFP cells infected with transfection‐derived HIV‐1 NL4‐3

Frezza

Grelli

Federico

et al. 2015

Journal of Medical Virology

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“…There is little literature precedent of phloroglucinol reactions with unsaturated aldehydes, but aryl aldehydes form 2:1 adducts. 12 A recent patent reports a preparation of calix [4]arene from cinnamaldehyde and phloroglucinol. 13 Initially, we evaluated a number of Lewis acid catalysts, as depicted in Table 1.…”

Section: Rapid Assembly Of the Procyanidin A Skeletonmentioning

confidence: 99%

Rapid assembly of the procyanidin A skeleton

Kraus

Geraskin

2017

Tetrahedron Letters

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“…The overall effect of arzanol shows it has anti-HIV activity by inhibiting HIV-1 replication in T cells. Plant derived phloroglucinols and synthetically derived dimeric phloroglucinols are also being proved for their anti-HIV activity [39]. …”

Section: Other Pharmacological Rolementioning

confidence: 99%

Arzanol, a Potent mPGES‐1 Inhibitor: Novel Anti‐Inflammatory Agent

Kothavade

Nagmoti

Bulani

et al. 2013

The Scientific World Journal

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Arzanol is a novel phloroglucinol α-pyrone, isolated from a Mediterranean plant Helichrysum italicum (Roth) Don ssp. microphyllum which belongs to the family Asteraceae. Arzanol has been reported to possess a variety of pharmacological activities. However, anti-inflammatory, anti-HIV, and antioxidant activities have been studied in some detail. Arzanol has been reported to inhibit inflammatory transcription factor NFκB activation, HIV replication in T cells, releases of IL-1β, IL-6, IL-8, and TNF-α, and biosynthesis of PGE2 by potentially inhibiting mPGES-1 enzyme. Diversity of mechanisms of actions of arzanol may be useful in treatment of disease involving these inflammatory mediators such as autoimmune diseases and cancer. This review presents comprehensive information on the chemistry, structure-activity relationship, and pharmacological activities of arzanol. In addition this review discusses recent developments and the scope for future research in these aspects.

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Biomimetic synthesis and anti-HIV activity of dimeric phloroglucinols

Cited by 45 publications

References 26 publications

Testing anti‐HIV activity of antiretroviral agents in vitro using flow cytometry analysis of CEM‐GFP cells infected with transfection‐derived HIV‐1 NL4‐3

Testing anti‐HIV activity of antiretroviral agents in vitro using flow cytometry analysis of CEM‐GFP cells infected with transfection‐derived HIV‐1 NL4‐3

Rapid assembly of the procyanidin A skeleton

Arzanol, a Potent mPGES‐1 Inhibitor: Novel Anti‐Inflammatory Agent

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