New method for recognition of sterol signalling molecules: Methinium salts as receptors for sulphated steroids

0442567 - ÚMG 2015 RIV US eng J - Článek v odborném periodiku
Kejík, Z. - Bříza, T. - Králová, Jarmila - Mikula, I. - Poučková, P. - Martásek, P. - Král, V.
New method for recognition of sterol signalling molecules: Methinium salts as receptors for sulphated steroids.
Steroids. Roč. 94, February 2015 (2015), s. 15-20. ISSN 0039-128X. E-ISSN 1878-5867
Grant CEP: GA TA ČR(CZ) TE01020028; GA ČR(CZ) GAP303/11/1291; GA MŠMT(CZ) LH14008; GA MŠMT(CZ) CZ.1.07/2.300/30.0060; GA MŠMT(CZ) ED1.1.00/02.0109
Institucionální podpora: RVO:68378050
Klíčová slova: Polymethinium salts * Sulphated sterols * Molecular recognition * Synthetic receptors
Kód oboru RIV: EB - Genetika a molekulární biologie
Impakt faktor: 2.513, rok: 2015

In this work, we studied indolium and benzothiazolium pentamethine salts 1-3 as novel type of receptors for the recognition of sulphated signalling molecules (sulphated steroids: oestrone, pregnenolone and cholesterol sulphate). A recognition study was performed in an aqueous medium (1mM phosphate buffer (H2O:MeOH; 99:1 (v/v))) at pH 7.34. The tested salts displayed a high affinity for these sulphated analytes, mainly for cholesterol sulphate. However, no interaction between the salts and control, non-sulphated sterol analytes (cholesterol and bile acid) was observed. The highest affinity for the sulphated steroids was observed for benzothiazole salt 1. This salt also displayed different spectral behaviour from that observed for carbocyanine salts 2 and 3. In this presence of cholesterol sulphate, benzothiazole salt 1 displayed significant spectral changes depending on the medium used: a blue shift in the aqueous medium and a red shift in the methanolic one (H2O:MeOH; 2:1 (v/v)). Subsequently preliminary in vivo study showed that, salt 1 significantly inhibits a growth of breast carcinoma on Nu/nu mice model.
Trvalý link: http://hdl.handle.net/11104/0245398