| In vitro: |
| Planta Med. 2017 Feb;83(3-04):232-238. | | The Plant-Derived Naphthoquinone Droserone Inhibits In Vitro Measles Virus Infection.[Pubmed: 27420351 ] | The naphthoquinone Droserone (1) is a natural product occurring in dicotyledonous plants.
METHODS AND RESULTS:
We have now observed that the addition of 1 during infection of tissue culture cells with measles virus considerably reduced the infection. Interestingly, the infection was inhibited only when Droserone (1) was added during virus entry, but not when added to the cells prior to virus uptake or after virus uptake. These findings suggest that 1 interacts with viral particles to reduce infectivity. The formation of progeny measles virus particles was inhibited to 50 % by Droserone (1) at a concentration (IC50) of approximately 2 μM with a half-maximal cytotoxicity (CC50) of about 60 μM for Vero cells. Other tested naphthoquinone derivatives, among them the likewise natural plumbagin (2), but also synthetic analogs, were either more cytotoxic or not as effective as 1.
CONCLUSIONS:
Thus, our data do not support the development of naphthoquinone derivatives into antiviral compounds, but suggest that they may be interesting research tools to study measles virus entry into cells. | | J Exp Bot. 2010 Mar;61(3):911-22. | | Induced production of antifungal naphthoquinones in the pitchers of the carnivorous plant Nepenthes khasiana.[Pubmed: 20018905] | Nepenthes spp. are carnivorous plants that have developed insect capturing traps, evolved by specific modification of the leaf tips, and are able to utilize insect degradation products as nutritional precursors. A chitin-induced antifungal ability, based on the production and secretion to the trap liquid of Droserone and 5-O-methylDroserone, is described here.
METHODS AND RESULTS:
Such specific secretion uniquely occurred when chitin injection was used as the eliciting agent and probably reflects a certain kind of defence mechanism that has been evolved for protecting the carnivory-based provision of nutritional precursors. The pitcher liquid containing Droserone and 5-O-methylDroserone at 3:1 or 4:1 molar ratio, as well as the purified naphthoquinones, exerted an antifungal effect on a wide range of plant and human fungal pathogens. When tested against Candida and Aspergillus spp., the concentrations required for achieving inhibitory and fungicidal effects were significantly lower than those causing cytotoxicity in cells of the human embryonic kidney cell line, 293T.
CONCLUSIONS:
These naturally secreted 1,4-naphthoquinone derivatives, that are assumed to act via semiquinone enhancement of free radical production, may offer a new lead to develop alternative antifungal drugs with reduced selectable pressure for potentially evolved resistance. |
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Cell. 2018 Jan 11;172(1-2):249-261.e12. doi: 10.1016/j.cell.2017.12.019.IF=36.216(2019)
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ACS Nano. 2018 Apr 24;12(4): 3385-3396. doi: 10.1021/acsnano.7b08969.IF=13.903(2019)
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