CYTOSTATIC ACTIVITY OF SOME CANARY ISLANDS SPECIES OF<i>RUTACEAE</i>

Gonzalez, Amanda; Darias, V.; Alonso, Gloria del Barrio; Boada, J; Rodríguez-Luis, Francisco

doi:10.1055/s-0028-1097543

Cited by 14 publications

(1 citation statement)

References 2 publications

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“…Under daylight none of the compounds were found to be toxic up to 100 µM, which is consistent with the LC 50 values of 340 µM described for 5-MOP, 8-MOP, and 5,8dimethoxypsoralen on HeLa cells. 43 Following UV-A irradiation a number of compounds showed an increase in toxicity, which was particularly striking for 6b and 7b which exhibited photoinduced dose modifications of >200 and >150, respectively. The "irradiated" LC 50 values found for 5-and 8-MOP (2.5 µM) were again in agreement with those described for HeLa and A 431 cells (2.5-4.3 µM).…”

Section: T H I S C O N T E N T Imentioning

confidence: 98%

Alkoxypsoralens, Novel Nonpeptide Blockers of Shaker-Type K⁺ Channels: Synthesis and Photoreactivity

et al. 1998

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A series of psoralens and structurally related 5,7-disubstituted coumarins was synthesized and investigated for their K+ channel blocking activity as well as for their phototoxicity to Artemia salina and their ability to generate singlet oxygen and to photomodify DNA. After screening the compounds on Ranvier nodes of the toad Xenopus laevis, the affinities of the most promising compounds, which proved to be psoralens bearing alkoxy substituents in the 5-position or alkoxymethyl substituents in the neighboring 4- or 4'-position, to a number of homomeric K+ channels were characterized. All compounds exhibited the highest affinity to Kv1.2. 5,8-Diethoxypsoralen (10d) was found to be an equally potent inhibitor of Kv1.2 and Kv1.3, while lacking the phototoxicity normally inherent in psoralens. The reported compounds represent a novel series of nonpeptide blockers of Shaker-type K+ channels that could be further developed into selective inhibitors of Kv1.2 or Kv1. 3.

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Section: T H I S C O N T E N T Imentioning

confidence: 98%