High Throughput Screening of Natural Products for Anti‐mitotic Effects in MDA‐MB‐231 Human Breast Carcinoma Cells

Mazzio, Elizabeth; Badisa, Ramesh B.; Mack, Nzinga; Deiab, S.; Soliman, Karam F.A.

doi:10.1002/ptr.5065

Cited by 28 publications

(19 citation statements)

References 61 publications

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“…These biological tests are often a cloned enzyme catalytic assay, a receptor binding assay, a protein-protein interaction assay or even a whole pathway (Ishibashi and Ohtsuki, 2008;Xie et al, 2018), to name but a few. Biological testing targeting whole-cells was also reported against cancer cells (Mazzio et al, 2014;Kant et al, 2016), virus-infected cells (Yi et al, 2004;Dai et al, 2012), or microorganisms (Correia et al, 2008;Figueroa-López et al, 2014;St-Pierre et al, 2018). Extracts showing activity on those tests are selected and submitted to fractionation by chromatography.…”

Section: Strategies For Identification Of Bioactive Compounds From Crmentioning

confidence: 99%

Unraveling Plant Natural Chemical Diversity for Drug Discovery Purposes

Lautie

Russo

Ducrot³

2020

Front. Pharmacol.

156

120

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The screening and testing of extracts against a variety of pharmacological targets in order to benefit from the immense natural chemical diversity is a concern in many laboratories worldwide. And several successes have been recorded in finding new actives in natural products, some of which have become new drugs or new sources of inspiration for drugs. But in view of the vast amount of research on the subject, it is surprising that not more drug candidates were found. In our view, it is fundamental to reflect upon the approaches of such drug discovery programs and the technical processes that are used, along with their inherent difficulties and biases. Based on an extensive survey of recent publications, we discuss the origin and the variety of natural chemical diversity as well as the strategies to having the potential to embrace this diversity. It seemed to us that some of the difficulties of the area could be related with the technical approaches that are used, so the present review begins with synthetizing some of the more used discovery strategies, exemplifying some key points, in order to address some of their limitations. It appears that one of the challenges of natural product-based drug discovery programs should be an easier access to renewable sources of plant-derived products. Maximizing the use of the data together with the exploration of chemical diversity while working on reasonable supply of natural product-based entities could be a way to answer this challenge. We suggested alternative ways to access and explore part of this chemical diversity with in vitro cultures. We also reinforced how important it was organizing and making available this worldwide knowledge in an "inventory" of natural products and their sources. And finally, we focused on strategies based on synthetic biology and syntheses that allow reaching industrial scale supply. Approaches based on the opportunities lying in untapped natural plant chemical diversity are also considered.

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Section: Strategies For Identification Of Bioactive Compounds From Crmentioning

confidence: 99%

Unraveling Plant Natural Chemical Diversity for Drug Discovery Purposes

Lautie

Russo

Ducrot³

2020

Front. Pharmacol.

156

120

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“…Evidence-Based Complementary and Alternative Medicine At the same time, the RGC extract as a whole is equally capable of inhibiting angiogenesis, inducing apoptosis in cancer cells [34] and as a cytostatic agent [7]. Moreover, its medicinal value has been described in the scientific literature for its multidimensional therapeutic value, also effective against harmful intestinal and periodontal bacteria [9,41], hepatitis carcinoma virus [15], severe acute respiratory syndrome corona [42] and as an anti-inflammatory [11,[43][44][45].…”

Section: Discussionmentioning

confidence: 99%

“…Traditional use of herbs to treat diverse human illnesses dates back to thousands of years, but in today's society the use of natural product remedies is defined amongst others under the classification of "complementary and alternative medicines" (CAMs) [1][2][3]. The field of CAM is of global interest, in particular to augment traditional chemotherapies, prevent cancer remission, or serve as basic chemopreventive strategies [4][5][6][7].…”

Section: Introductionmentioning

confidence: 99%

“…Rhus chinensis gall (RCG) is the abnormal growth of Rhus chinensis leaves caused by Chinese aphid Schlechtendalia chinensis [8,9], also used for decades by indigenous people in the treatment of diarrhea, hemorrhage, and inflammation [10][11][12][13][14][15][16][17]. In a recent study conducted in our laboratory, a high-throughput screening of natural products revealed the extract of RGC to halt the proliferation of human breast cancer cells [7] and inhibit hLDH-A [18], an enzyme which plays a significant role in driving aggressive malignancies [2,[19][20][21], chemo-and radiotherapy resistance [22,23], tumorigenic potential [24][25][26], and metastatic processes [22]. It is believed that the abundance of lactic acid produced and released by tumor cells assists in invasion and motility [27] where a low pH weakens the extracellular stroma which helps tumor cells to dislodge and burrow in the blood and lymphatic systems [28].…”

Section: Introductionmentioning

confidence: 99%

See 1 more Smart Citation

1,2,3,4,6-Penta-O-galloylglucose within Galla Chinensis Inhibits Human LDH-A and Attenuates Cell Proliferation in MDA-MB-231 Breast Cancer Cells

Deiab

Mazzio

Eyunni

et al. 2015

Evidence-Based Complementary and Alternative Medicine

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A characteristic feature of aggressive malignancy is the overexpression of lactic acid dehydrogenase- (LDH-) A, concomitant to pericellular accumulation of lactate. In a recent high-throughput screening, we identified Rhus chinensis (Mill.) gallnut (RCG) (also known as Galla Chinensis) extract as a potent (IC50 < 1 µg/mL) inhibitor of human LDH-A (hLDH-A). In this study, through bioactivity guided fractionation of the crude extract, the data demonstrate that penta-1,2,3,4,6-O-galloyl-β-D-glucose (PGG) was a primary constituent responsible for hLDH-A inhibition, present at ~9.95 ± 0.34% dry weight. Theoretical molecular docking studies of hLDH-A indicate that PGG acts through competitive binding at the NADH cofactor site, effects confirmed by functional enzyme studies where the IC50 = 27.32 nM was reversed with increasing concentration of NADH. Moreover, we confirm protein expression of hLDH-A in MDA-231 human breast carcinoma cells and show that PGG was toxic (LC50 = 94.18 µM), parallel to attenuated lactic acid production (IC50 = 97.81 µM). In a 72-hour cell proliferation assay, PGG was found to be a potent cytostatic agent with ability to halt cell division (IC50 = 1.2 µM) relative to paclitaxel (IC50 < 100 nM). In summary, these findings demonstrate that PGG is a potent hLDH-A inhibitor with significant capacity to halt proliferation of human breast cancer cells.

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“…Speranskia tuberculata is endemic to northern China and occurs on grassy slopes, grasslands, and thickets. The entire plant is commonly used for Chinese traditional medicine (Mazzio et al, 2014). Although S. tuberculata is not listed in the IUCN Red List, it is exhibiting a general decreasing trend or even disappearing completely in many distributional areas because of agricultural intensification and over-exploitation of natural population resources.…”

mentioning

confidence: 99%

Development and characterization of novel EST‐SSR markers for Speranskia tuberculata (Euphorbiaceae)

et al. 2016

Appl Plant Sci

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Premise of the study:The first set of expressed sequence tag–simple sequence repeat (EST-SSR) markers were developed and characterized for Speranskia tuberculata (Euphorbiaceae), a traditional medicinal plant endemic to northern China, to explore the effects of recent habitat fragmentation on the genetic diversity and structure of this species.Methods and Results:In this study, a total of 18 novel polymorphic microsatellite (EST-SSR) markers were developed for S. tuberculata using high-throughput transcriptome sequencing. Analysis of 24 individuals of S. tuberculata from four natural populations revealed their robust polymorphic reliability. The number of alleles per locus ranged from two to 11, while the expected and observed heterozygosity per marker varied from 0.187 to 0.827 and 0.042 to 0.917, respectively. Of these markers, 13 showed good amplification results in the closely related species S. cantonensis.Conclusions:These newly generated SSR markers are expected to provide novel tools for genetic studies of S. tuberculata, which will contribute to the conservation and sustainable use of the species’ wild genetic resources.

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High Throughput Screening of Natural Products for Anti‐mitotic Effects in MDA‐MB‐231 Human Breast Carcinoma Cells

Cited by 28 publications

References 61 publications

Unraveling Plant Natural Chemical Diversity for Drug Discovery Purposes

Unraveling Plant Natural Chemical Diversity for Drug Discovery Purposes

1,2,3,4,6-Penta-O-galloylglucose within Galla Chinensis Inhibits Human LDH-A and Attenuates Cell Proliferation in MDA-MB-231 Breast Cancer Cells

Development and characterization of novel EST‐SSR markers for Speranskia tuberculata (Euphorbiaceae)

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