Natural products: An upcoming therapeutic approach to cancer

Dutta, Sayanta; Mahalanobish, Sushweta; Saha, Sukanya; Ghosh, Shatadal; Sil, Parames C.

doi:10.1016/j.fct.2019.04.012

Cited by 216 publications

(145 citation statements)

References 222 publications

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“…From ancient times, various natural products have been used as traditional medicines and are rich sources of bioactive compounds 1,2 . Chromones (4H-chomen-4-one, 4H-1-benzopyran-4-one) are widely distributed oxygen-containing natural heterocyclic compounds from the plants of Polygonaceae, Umbelliferae, Sterculiaceae, Rhamnaceae, Liliaceae, Asteraceae etc., with a benzoylated c-pyrone ring which is a part of the structure of flavonoid skeletons [3][4][5] .…”

Section: Introductionmentioning

confidence: 99%

“…11 4-((1-((3-Carboxy-6-methyl-4-oxo-4H-chromen-2-yl)amino)propan-2-yl)oxy)-3-(phenylsulfonyl)-1,2,5-oxadiazole 2-oxide (14b) Yield: 35.6% 1. H NMR (400 MHz, DMSO-d 6 ) d (ppm): 11.72 (s, 1H, -COOH), 8.58 (s, 1H, -NH-), 8.00-7.99 (d, 2H, J ¼ 7.2 Hz, 2 0 ,6 0 -ArH), 7.84-7.80 (t, 1H, J ¼ 7.2 Hz, 4 0 -ArH), 7.74 (s, 1H, 5-ArH), 7.65-7.61 (t, 2H, J ¼ 7.4 Hz, 3 0 ,5 0 -ArH), 7.48-7 47.…”

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confidence: 99%

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Antiproliferative chromone derivatives induce K562 cell death through endogenous and exogenous pathways

Jiao

Huang

et al. 2020

Journal of Enzyme Inhibition and Medicinal Chemistry

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A series of furoxan derivatives of chromone were prepared. The antiproliferative activities were tested against five cancer cell lines HepG2, MCF-7, HCT-116, B16, and K562, and two normal human cell lines L-02 and PBMCs. Among them, compound 15a exhibited the most potent antiproliferative activity. It was also found 15a produced more than 8 mM of NO at the peak time of 45 min by Griess assay. Generally, antiproliferative activity is positively related to NO release to some extent. Further in-depth studies on apoptosis-related mechanisms showed that 15a caused S-phase cell cycle arrest in a concentrationdependent manner and induced apoptosis significantly through mitochondria-related pathways. Human apoptosis protein array assay also demonstrated 15a increased the expression levels of pro-apoptotic Bax, Bad, HtrA2 and Trail R2/DR5. The expression of catalase and cell cycle blocker claspin were similarly upregulated. In balance, 15a induced K562 cells death through both endogenous and exogenous pathways.

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Section: Introductionmentioning

confidence: 99%

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confidence: 99%

Antiproliferative chromone derivatives induce K562 cell death through endogenous and exogenous pathways

Jiao

Huang

et al. 2020

Journal of Enzyme Inhibition and Medicinal Chemistry

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“…To include kinase-targeted compounds, as such a choice is already proven to be successful [41,42]; 3. To explore natural products, which are a promising source of anticancer drugs [43][44][45]; 4. To take into account the repositioning of approved compounds, as drug repurposing presents an increasing interest in cancer research, by removing many costs associated with several steps of drug development [46][47][48][49].…”

Section: Screened Chemical Librariesmentioning

confidence: 99%

Large-Scale Virtual Screening Against the MET Kinase Domain Identifies a New Putative Inhibitor Type

et al. 2020

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By using an ensemble-docking strategy, we undertook a large-scale virtual screening campaign in order to identify new putative hits against the MET kinase target. Following a large molecular dynamics sampling of its conformational space, a set of 45 conformers of the kinase was retained as docking targets to take into account the flexibility of the binding site moieties. Our screening funnel started from about 80,000 chemical compounds to be tested in silico for their potential affinities towards the kinase binding site. The top 100 molecules selected—thanks to the molecular docking results—were further analyzed for their interactions, and 25 of the most promising ligands were tested for their ability to inhibit MET activity in cells. F0514-4011 compound was the most efficient and impaired this scattering response to HGF (Hepatocyte Growth Factor) with an IC 50 of 7.2 μ M. Interestingly, careful docking analysis of this molecule with MET suggests a possible conformation halfway between classical type-I and type-II MET inhibitors, with an additional region of interaction. This compound could therefore be an innovative seed to be repositioned from its initial antiviral purpose towards the field of MET inhibitors. Altogether, these results validate our ensemble docking strategy as a cost-effective functional method for drug development.

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“…Throughout history, natural substances were widely used to treat various diseases [1]. Food of plant origin is associated with health-profitable benefits [2] related to bioactive compounds [3].…”

Section: Introductionmentioning

confidence: 99%

“…Importantly, a combination of phytochemicals in whole foods may be more protective against carcinogenesis due to their additive or synergistic effects [6,7]. Recently, natural substances gained great interest through their anticancer potential mediated via an ability to affect various cancer-associated signaling pathways [8] in different stages of carcinogenesis [1]. Above all, natural compounds exert antiproliferative, proapoptotic, antiangiogenic, antimutagenic, and overall genoprotective abilities [4,[9][10][11].…”

Section: Introductionmentioning

confidence: 99%

Fluctuations of Histone Chemical Modifications in Breast, Prostate, and Colorectal Cancer: An Implication of Phytochemicals as Defenders of Chromatin Equilibrium

et al. 2019

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Natural substances of plant origin exert health beneficiary efficacy due to the content of various phytochemicals. Significant anticancer abilities of natural compounds are mediated via various processes such as regulation of a cell’s epigenome. The potential antineoplastic activity of plant natural substances mediated by their action on posttranslational histone modifications (PHMs) is currently a highly evaluated area of cancer research. PHMs play an important role in maintaining chromatin structure and regulating gene expression. Aberrations in PHMs are directly linked to the process of carcinogenesis in cancer such as breast (BC), prostate (PC), and colorectal (CRC) cancer, common malignant diseases in terms of incidence and mortality among both men and women. This review summarizes the effects of plant phytochemicals (isolated or mixtures) on cancer-associated PHMs (mainly modulation of acetylation and methylation) resulting in alterations of chromatin structure that are related to the regulation of transcription activity of specific oncogenes, which are crucial in the development of BC, PC, and CRC. Significant effectiveness of natural compounds in the modulation of aberrant PHMs were confirmed by a number of in vitro or in vivo studies in preclinical cancer research. However, evidence concerning PHMs-modulating abilities of plant-based natural substances in clinical trials is insufficient.

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Natural products: An upcoming therapeutic approach to cancer

Cited by 216 publications

References 222 publications

Antiproliferative chromone derivatives induce K562 cell death through endogenous and exogenous pathways

Antiproliferative chromone derivatives induce K562 cell death through endogenous and exogenous pathways

Large-Scale Virtual Screening Against the MET Kinase Domain Identifies a New Putative Inhibitor Type

Fluctuations of Histone Chemical Modifications in Breast, Prostate, and Colorectal Cancer: An Implication of Phytochemicals as Defenders of Chromatin Equilibrium

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