Neoflavonoids as Inhibitors of HIV-1 Replication by Targeting the Tat and NF-κB Pathways

Olmedo, Dionisio A.; López-Pérez, Jose Luis; Olmo, Esther del; Bedoya, Luis Miguel; Sancho, Rocı́o; Alcamı́, José; Muñóz, Eduardo; Feliciano, Arturo San; Gupta, Mahabir P.

doi:10.3390/molecules22020321

Cited by 8 publications

(4 citation statements)

References 54 publications

(56 reference statements)

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“…The desired product 59 ( 61 or 63 ) was isolated using silica gel column chromatography (Schemes 3, 4). The characterizations of coumarin 55 – 64 were previous reported in references (Smitha and Sanjeeva Reddy, 2004; Takaishi et al, 2008; Cavar et al, 2009; Sun et al, 2011; Zhang et al, 2011; Serra et al, 2012; Olmedo et al, 2017).…”

Section: Methodsmentioning

confidence: 73%

Discovery of Coumarin as Microtubule Affinity-Regulating Kinase 4 Inhibitor That Sensitize Hepatocellular Carcinoma to Paclitaxel

et al. 2019

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Hepatocellular carcinoma (HCC) is one of the most prevalent cancers worldwide. Nowadays, pharmacological therapy for HCC is in urgent needs. Paclitaxel is an effective drug against diverse solid tumors, but commonly resisted in HCC patients. We recently have disclosed that microtubule affinity-regulating kinase 4 (MARK4) increases the microtubule dynamics and confers paclitaxel resistance in HCC, suggesting MARK4 as an attractive target to overcome paclitaxel resistance. Herein, we synthesized and identified coumarin derivatives 50 as a novel MARK4 inhibitor. Biological evaluation indicated compound 50 directly interacted with MARK4 and inhibited its activity in vitro , suppressed cell viability and induced apoptosis of HCC cells in a MARK4-dependent manner. Importantly, compound 50 significantly increased the drug response of paclitaxel treatment to HCC cells, providing a promise strategy to HCC treatment and broadening the application of paclitaxel in cancer therapy.

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Section: Methodsmentioning

confidence: 73%

Discovery of Coumarin as Microtubule Affinity-Regulating Kinase 4 Inhibitor That Sensitize Hepatocellular Carcinoma to Paclitaxel

et al. 2019

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“…5N5O) [23], inhibition of HIV-1 reverse transcriptase [24,25], and anti-inflammatory activity [26], among others. Our present study indicates moderate antimicrobial activity, as presented in Table S1.…”

Section: In Vitro Biological Activity Antimicrobial Investigation Of ...mentioning

confidence: 99%

Preliminary Investigation of the Lewis Acid-Mediated Reactions of Phenols and Ethyl Phenylpropiolate as a Synthetic Route to Flavonoids and Antimicrobial Profile of the Resultant 7-Hydroxy-4-Phenyl-2h-Chromen-2-One and Analogs

Umoh,

Bojase,

Masesane

et al. 2023

JCSN

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Synthetic chemists are increasingly exploring alternative routes to target products, considering factors like environmental threats, side product formation, cost, and efficiency. This is coupled with the health challenges that require urgent responses from new chemical entities. In this context, antimicrobial resistance has exacerbated global diseases, making them difficult to treat with prescribed drugs and causing a persistent public health crisis. These triggered our interest in the search for alternative antimicrobial agents, exploring different synthetic strategies for known bioactive natural compounds for further investigations. In this study, Lewis acid catalyst (FeCl3) and tetrahydrofuran as solvents in the one-pot synthesis of (neo)flavonoid derivatives from readily available phenols and ethyl phenylpropiolate were discovered to afford the coumarins in yields of 43–95%. The synthetic derivatives of 7-hydroxy-4-phenyl-2H-chromen-2-one and analogs obtained were biologically investigated for antimicrobial activity. The compounds showed moderate to poor antimicrobial activity. The effects of different substituents (-R) on the yield of the reaction are also discussed. Future studies should enhance the yield of derivative products and use different assay models for biological activity studies to fully explore the compounds` biorelevance.

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“…4-phenylcoumarin derivatives called neoflavanoids were synthesized and their anti-HIV effects were assessed on MT-2 infected cells in vitro [46]. It suggested that the acyl group was essential for the inhibition of both the Tat and NF-kB pathway [56]. The HIV-replication inhibitory activity of a 4-phenyl coumarins mesouol (extracted from Marila pluricostata) has been studied in Jurkat T cells.…”

Section: Anti-hivmentioning

confidence: 99%

Coumarin: An emerging antiviral agent

Mishra

Pandey

Manvati

2020

Heliyon

202

117

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Viral infections are responsible for many illnesses, and recent outbreaks have raised public health concerns. Despite the availability of many antiviral drugs, they are often unsuccessful due to the generation of viral mutants and less effective against their target virus. Identifying novel antiviral drugs is therefore of critical importance and natural products are an excellent source for such discoveries. Coumarin is one such natural compound that is a potential drug candidate owing to its properties of stability, solubility, and low toxicity. There are numerous evidences showing its inhibitory role against infection of various viruses such as HIV, Influenza, Enterovirus 71 (EV71) and coxsackievirus A16 (CVA16). The mechanisms involve either inhibition of proteins essential for viral entry, replication and infection or regulation of cellular pathways such as Akt-Mtor (mammalian target of rapamycin), NF-κB (nuclear factor kappa-light-chain-enhancer of activated B cells), and anti-oxidative pathway including NrF-2 (The nuclear factor erythroid 2 (NFE2)-related factor 2). This review summarizes the present state of understanding with a focus on coumarin's antiviral effect and their possible molecular mechanisms against Influenza virus, HIV, Hepatitis virus, Dengue virus and Chikungunya virus.

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Neoflavonoids as Inhibitors of HIV-1 Replication by Targeting the Tat and NF-κB Pathways

Cited by 8 publications

References 54 publications

Discovery of Coumarin as Microtubule Affinity-Regulating Kinase 4 Inhibitor That Sensitize Hepatocellular Carcinoma to Paclitaxel

Discovery of Coumarin as Microtubule Affinity-Regulating Kinase 4 Inhibitor That Sensitize Hepatocellular Carcinoma to Paclitaxel

Preliminary Investigation of the Lewis Acid-Mediated Reactions of Phenols and Ethyl Phenylpropiolate as a Synthetic Route to Flavonoids and Antimicrobial Profile of the Resultant 7-Hydroxy-4-Phenyl-2h-Chromen-2-One and Analogs

Coumarin: An emerging antiviral agent

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