Evaluation of Fourteen Aurone Derivatives as Potential Anti-Cancer Agents

Alsaif, Ghaida; Almosnid, Nadin; Hawkins, Ian; Taylor, Zachary E.; Knott, Deborah L.T.; Handy, Scott T.; Altman, Elliot; Gao, Ying

doi:10.2174/1389201018666170502112303

Cited by 10 publications

(7 citation statements)

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“…Apoptosis in each group was evaluated and analyzed by ArrayScan VTI High Content Screening reader (Thermo Scientific, MA, United States). The Excitation/Emission wavelengths for Hoechst 33,342, FITC-Annexin V, and PI were 350/461 nm, 494/518 nm, and 535/617 nm, respectively ( Alsaif et al, 2017 ).…”

Section: Methodsmentioning

confidence: 99%

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Sensitization effect of kaempferol from persimmon leaves on HepG2 hepatoma cells with ABT-199 resistance and its molecular mechanisms

Chen

Jiang²,

Gao³

et al. 2022

Front. Pharmacol.

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ABT-199 (venetoclax) is the first-in-class selective B-cell lymphoma 2 (BCL2) inhibitor, which is known to be ineffective towards liver cancer cells. Here, we investigated the efficacy and the underlying molecular processes of the sensitization effect of kaempferol isolated from persimmon leaves (KPL) on the ABT-199-resistant HepG2 cells. The effects of various doses of KPL coupled with ABT-199 on the proliferation of HepG2 cells and on the H22 liver tumor-bearing mouse model were examined, as well as the underlying mechanisms. Our findings showed that ABT-199 alone, in contrast to KPL, had no significant impact on hepatoma cell growth, both in vitro and in vivo. Interestingly, the combination therapy showed significantly higher anti-hepatoma efficacy. Mechanistic studies revealed that combining KPL and ABT-199 may promote both early and late apoptosis, as well as decrease the mitochondrial membrane potential in HepG2 cells. Western blot analysis showed that combination of KPL and ABT-199 significantly reduced the expression of the anti-apoptotic proteins Bcl-2, Bcl-xL, and Mcl-1, raised the expression of Bax and cleaved caspase 3, and enhanced cytochrome C release and Bax translocation. Therefore, KPL combined with ABT-199 has a potential application prospect in the treatment of hepatocellular carcinoma.

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Section: Methodsmentioning

confidence: 99%

“…The Excitation/Emission wavelengths for Hoechst 33,342, FITC-Annexin V, and PI were 350/461 nm, 494/518 nm, and 535/617 nm, respectively (Alsaif et al, 2017).…”

Section: Apoptosis Assaymentioning

confidence: 98%

Sensitization effect of kaempferol from persimmon leaves on HepG2 hepatoma cells with ABT-199 resistance and its molecular mechanisms

Chen

Jiang²,

Gao³

et al. 2022

Front. Pharmacol.

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“…Aurones (2-benzylidene-1-benzofuran-3(2H)-one) are a class of naturally occurring avonoid derivatives responsible for the pigments in some owering plants, such as the yellow rocket snapdragon. 1 There has been a recent increase in the study of aurones due to their bioactivities; 2 including anti-inammatory, [3][4][5][6] anti-microbial, 5,7,8 and anticancer [9][10][11] properties. In addition, there has been an interest in aurones as uorescent markers due to their visible range excitation and emission spectra, tunable uorescence properties, and their potential bioavailability.…”

Section: Introductionmentioning

confidence: 99%

Aurone-derived 1,2,3-triazoles as potential fluorescence molecules in vitro

et al. 2022

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“…33,41 The present route for the synthesis of 2,5dihydro-1,2-oxaphosphole-2-oxide core is highly adaptable with simple reaction procedures and hence eliminates the use of expensive precursors (Figure 1). As phospha-coumaranones (phospha-γ-lactones) are analogues of coumaranones (coumaran derivatives) by structure and as coumaranones are potential antiplasmodial, 42 antifungal, 43 anti-neoplasia, 44 and anticancer 45 agents, we have designed the synthesis of their phosphorus analogues bearing a cyclic phosphonic acid group (hydroxy group located on the phosphoryl group), which easily facilitates ring opening operations in vivo metabolic processes (hydrolysis) and hence acts as potential prodrugs. 46 This has motivated us to investigate the anti-pancreatic cancer activity and to identify the mechanistic aspects of cell cycle inhibition.…”

Section: ■ Introductionmentioning

confidence: 99%

Synthesis and Anti-Pancreatic Cancer Activity Studies of Novel 3-Amino-2-hydroxybenzofused 2-Phospha-γ-lactones

et al. 2021

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A series of 3-amino-2-hydroxybenzofused 2-phosphalactones ( 4a–l ) has been synthesized from the Kabachnik–Fields reaction via a facile route from a one-pot three-component reaction of diphenylphosphite with various 2-hydroxybenzaldehyes and heterocyclic amines in a new way of expansion. The in vitro anti-cell proliferation studies by MTT assay have revealed them as potential Panc-1, Miapaca-2, and BxPC-3 pancreatic cell growth inhibitors, and the same is supported by molecular docking, QSAR, and ADMET studies. The MTT assay of their SAHA derivatives against the same cell lines evidenced them as potential HDAC inhibitors and identified 4a , 4b , and 4k substituted with 1,3-thiazol, 1,3,4-thiadiazol, and 5-sulfanyl-1,3,4-thiadiazol moieties on phenyl and diethylamino phenyl rings as potential ones. Additionally, the flow cytometric analyses of 4a , 4b , and 4k against BxPC-3 cells revealed compound 4k as a lead compound that arrests the S phase cell cycle growth at low micromolar concentrations. The ADMET properties have ascertained their inherent pharmacokinetic potentiality, and the wholesome results prompted us to report it as the first study on anti-pancreatic cancer activity of cyclic α-aminophosphonates. Ultimately, this study serves as a good contribution to update the existing knowledge on the anticancer organophosphorus heterocyclic compounds and elevates the scope for generation of new anticancer drugs. Further, the studies like QSAR, drug properties, toxicity risks, and bioactivity scores predicted for them have ascertained the synthesized compounds as newer and potential drug candidates. Hence, this study had augmented the array of α-aminophosphonates by adding a new collection of 3-amino-2-hydroxybenzofused 2-phosphalactones, a class of cyclic α-aminophosphonates, to it, which proved them as potential anti-pancreatic cancer agents.

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Evaluation of Fourteen Aurone Derivatives as Potential Anti-Cancer Agents

Abstract: Aurone derivatives devoid of the unusual oxygenation found in the coumaranone fragment are potential leads for new anti-cancer agents.

Cited by 10 publications

References 0 publications

Sensitization effect of kaempferol from persimmon leaves on HepG2 hepatoma cells with ABT-199 resistance and its molecular mechanisms

Sensitization effect of kaempferol from persimmon leaves on HepG2 hepatoma cells with ABT-199 resistance and its molecular mechanisms

Aurone-derived 1,2,3-triazoles as potential fluorescence molecules in vitro

Synthesis and Anti-Pancreatic Cancer Activity Studies of Novel 3-Amino-2-hydroxybenzofused 2-Phospha-γ-lactones

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