| Description: |
Eupalinolide A and Eupalinolide B induce the expression of HSP70 via the activation of HSF1 by inhibiting the interaction between HSF1 and HSP90. They could be beneficial for use in cosmetics and medicines as a consequence of their inhibitory action on UV-induced skin damage and melanin production. |
| Targets: |
HSP (e.g. HSP90) |
| In vitro: |
| Biochem Pharmacol. 2012 Apr 1;83(7):909-22. | | Purification and characterization of HSP-inducers from Eupatorium lindleyanum.[Pubmed: 22245466] | The expression of heat shock proteins (HSPs), particularly HSP70, provides resistance to stressors. We recently reported that ultraviolet (UV)-induced melanin production and skin damage were suppressed in transgenic mice expressing HSP70 and that an extract of Eupatorium lindleyanum induces the expression of HSP70 in cells.
METHODS AND RESULTS:
Here we report the purification of Eupalinolide A and B (EA and EB) from E. lindleyanum, and describe their actions as HSP-inducers. Eupalinolide A and EB both induced the expression of HSP70 in cells at concentrations that did not significantly affect cell viability. Treatment of cells with Eupalinolide A or EB activated heat shock factor 1 (HSF1), while the artificial suppression of HSF1 expression diminished the Eupalinolide A - or EB-mediated induction of HSP70 expression. Furthermore, EB inhibited the interaction between HSF1 and HSP90, which is known to inhibit the activity of HSF1. These findings suggest that Eupalinolide A and EB induce the expression of HSP70 via the activation of HSF1 by inhibiting the interaction between HSF1 and HSP90. Eupalinolide A and EB both induced the expression of HSP70 synergistically with other stressors. Furthermore, pre-treatment of cells with Eupalinolide A or EB suppressed melanin production and stressor-induced apoptosis. These effects were suppressed by the artificial suppression of HSP70 expression. In vivo, the percutaneous administration of EB induced the expression of HSP70 and suppressed UVB radiation-induced damage, inflammatory responses and melanin production in the skin.
CONCLUSIONS:
These results suggest that Eupalinolide A and EB could be beneficial for use in cosmetics and medicines as a consequence of their inhibitory action on UV-induced skin damage and melanin production. |
|
| In vivo: |
| J Chromatogr B Analyt Technol Biomed Life Sci. 2015 May 16;995-996C:1-7. | | Pharmacokinetics of eupalinolide A, eupalinolide B and hyperoside from Eupatorium lindleyanum in rats by LC/MS/MS.[Pubmed: 26011510] | A simple, selective, and sensitive LC/MS/MS method was developed and validated for simultaneous determination of Eupalinolide A, eupalinolide B, and hyperoside in rat plasma. Plasma samples were processed by protein precipitation with acetonitrile.
METHODS AND RESULTS:
The three analytes, together with internal standard (IS, lysionotin), were separated on a Venusil MP-C18 column (50mm×2.1mm, 3μm) using a mobile phase of methanol and 10mM ammonium acetate (45:55, v/v) with isocratic elution. Mass spectrometric detection was performed by multiple-reaction monitoring mode via electrospray ionization source. Linear calibration curves were obtained for the following concentration range: 1.28-640ng/mL for Eupalinolide A; 1.98-990ng/mL for EB; and 2.00-1000ng/mL for HYP. The intra- and inter-day precision was less than 10.25%, and the accuracy was between 89.16% and 110.63%. The extraction recovery of the analytes and IS from rat plasma was above 88.75%.
CONCLUSIONS:
The validated method has been successfully applied to pharmacokinetic studies of the three analytes following intragastric administration of Eupatorium lindleyanum extract at a single dose of 100, 250, and 625mg/kg to Sprague-Dawley rats, respectively. The pharmacokinetic results may help to better understand the pharmacological actions of the herb E. lindleyanum. |
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