The screening toolbox of bioactive substances from natural products: A review

Wang, Bochu; Deng, Jia; Gao, Yimeng; Zhu, Liancan; He, Rui; Xu, Yingqian

doi:10.1016/j.fitote.2011.08.007

Cited by 61 publications

(36 citation statements)

References 152 publications

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“…In this section we present a brief overview of assays used to determine bioactivities of phytochemicals on the protein-, cell-, or organism level. For further information on the topic, we refer the reader to the following excellent reviews: (Agarwal et al, 2014;Butterweck and Nahrstedt, 2012;Fallarero et al, 2014;Wang et al, 2011a). Methods for activity assaying that are based on simple chemical reactions, such as some widely used methods to determine in vitro antioxidant properties (e.g., the 2,2-diphenyl-1-picrylhydrazyl (DPPH) radical scavenging assay), have been reviewed elsewhere (Gulcin, 2012;Moon and Shibamoto, 2009) and will not be discussed in detail here.…”

Section: Considerations Regarding the Choice Of Bioassaysmentioning

confidence: 99%

Discovery and resupply of pharmacologically active plant-derived natural products: A review

2015

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Medicinal plants have historically proven their value as a source of molecules with therapeutic potential, and nowadays still represent an important pool for the identification of novel drug leads. In the past decades, pharmaceutical industry focused mainly on libraries of synthetic compounds as drug discovery source. They are comparably easy to produce and resupply, and demonstrate good compatibility with established high throughput screening (HTS) platforms. However, at the same time there has been a declining trend in the number of new drugs reaching the market, raising renewed scientific interest in drug discovery from natural sources, despite of its known challenges. In this survey, a brief outline of historical development is provided together with a comprehensive overview of used approaches and recent developments relevant to plant-derived natural product drug discovery. Associated challenges and major strengths of natural product- Europe PMC Funders Author ManuscriptsEurope PMC Funders Author Manuscripts based drug discovery are critically discussed. A snapshot of the advanced plant-derived natural products that are currently in actively recruiting clinical trials is also presented. Importantly, the transition of a natural compound from a "screening hit" through a "drug lead" to a "marketed drug" is associated with increasingly challenging demands for compound amount, which often cannot be met by re-isolation from the respective plant sources. In this regard, existing alternatives for resupply are also discussed, including different biotechnology approaches and total organic synthesis.While the intrinsic complexity of natural product-based drug discovery necessitates highly integrated interdisciplinary approaches, the reviewed scientific developments, recent technological advances, and research trends clearly indicate that natural products will be among the most important sources of new drugs also in the future.

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Section: Considerations Regarding the Choice Of Bioassaysmentioning

confidence: 99%

Discovery and resupply of pharmacologically active plant-derived natural products: A review

2015

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“…The evaluation of bioactive compounds or mixtures on specific cells is usually conducted through bioassays and molecular tests (Barros et al, 2007;Meca et al, 2010;Muller-Riebau et al, 1995;Skotti et al, 2014;Zambonelli et al, 1996). Plant extracts, either aqueous or in organic solvents, have shown antimicrobial activity when examined by different screening models (Wang et al, 2011) mainly towards finding successful drug candidates. Biological activity of plant extracts is being investigated through alterations in photosynthetic mechanism or stress status of plants (Bouchagier et al, 2008;Bouchagier and Efthimiadis, 2010), bioassays (Abou-Jawdah et al, 2004;Daferera et al, 2003), tissue or cell culture (Wang et al, 2011), receptor enzyme (Peelman et al, 2006) and biochromatography (He et al, 2008;Kotecha et al, 2007;Kvalheim et al 2011).…”

Section: Introductionmentioning

confidence: 99%

Biological activity of selected Greek medicinal and aromatic plants extracts on Alternaria alternata

Tarantilis¹,

Skotti²,

Kountouri³

et al. 2016

Emir. J. Food Agric

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In this study, the biological activity of selected Greek medicinal and aromatic plants on the phytopathogenic fungus Alternaria alternata was investigated. Biological activity was screened on crude aqueous extracts and their aqueous phase (ap-pt) after further extraction with petroleum ether. All the Lamiaceae species examined were found to enhance significantly the mycelium growth. Melissa officinalis extracts caused the highest stimulation in mycelium growth, (+109.1%) the ap-pt, and (+51.6%) its crude extract. All ap-pt extracts stimulated conidia production, but Melissa officinalis caused the highest effect (+349.3%). Crude extracts of Salvia officinalis stimulated highly conidial production (+65%) whereas Hyssopus. officinalis and Origanum vulgare inhibited conidia production at 33.3% and 50.0% respectively. The differences in biological activity between crude and ap-pt extracts for each plant species were attributed through the calculation of correspondent synergism ratios (SR) to the interaction between volatile and water -soluble. Rosmarinic acid, detected as the most abundant phenolic compound in all extracts analyzed and found to correlate strongly (R= 0.84) with the stimulation effect on spore production of A. alternata.

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“…Some of these biomacromolecules are important drug targets and the drug must act at the target site within the cell membrane. The chromatographic stationary phase that contains live cell membranes can mimic the physiological process and selectively bind active compounds in sample, making CMC a suitable technique for the identification of active components in complex sample matrices, such as NPs [16][17][18][19].…”

Section: Introductionmentioning

confidence: 99%

Development of an analytical method coupling cell membrane chromatography with gas chromatography–mass spectrometry via microextraction by packed sorbent and its application in the screening of volatile active compounds in natural products

Wang

2015

Journal of Chromatography B

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The screening toolbox of bioactive substances from natural products: A review

Cited by 61 publications

References 152 publications

Discovery and resupply of pharmacologically active plant-derived natural products: A review

Discovery and resupply of pharmacologically active plant-derived natural products: A review

Biological activity of selected Greek medicinal and aromatic plants extracts on Alternaria alternata

Development of an analytical method coupling cell membrane chromatography with gas chromatography–mass spectrometry via microextraction by packed sorbent and its application in the screening of volatile active compounds in natural products

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