Sterol effect on interaction between amphidinol 3 and liposomal membrane as evidenced by surface plasmon resonance

Amphidinol 3 was shown to possess 1000 and 5300 times higher affinity for both cholesterol- and ergosterol-containing liposomes, respectively than that without sterol by SPR. The affinity of amphidinol 3 (AM3) to phospholipid membranes in the presence and absence of sterol was examined by surface pl...

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Bibliographic Details
Published in:Bioorganic & medicinal chemistry letters 2010-04, Vol.20 (7), p.2215-2218
Main Authors: Swasono, Respati T., Mouri, Ryota, Morsy, Nagy, Matsumori, Nobuaki, Oishi, Tohru, Murata, Michio
Format: Article
Language:English
Subjects:
Alkenes - chemistry
Amphidinol
Biological and medical sciences
Cholesterol
Cholesterol - chemistry
Ergosterol
Ergosterol - chemistry
General pharmacology
Liposomes - chemistry
Medical sciences
Pharmacognosy. Homeopathy. Health food
Pharmacology. Drug treatments
Pyrans - chemistry
Sterols - chemistry
Surface Plasmon Resonance
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Summary:Amphidinol 3 was shown to possess 1000 and 5300 times higher affinity for both cholesterol- and ergosterol-containing liposomes, respectively than that without sterol by SPR. The affinity of amphidinol 3 (AM3) to phospholipid membranes in the presence and absence of sterol was examined by surface plasmon resonance (SPR) experiments. The results showed that AM3 has 1000 and 5300 times higher affinity for cholesterol- and ergosterol-containing liposomes, respectively, than those without sterol. The two-state reaction model well reproduced the sensor grams, which indicated that the interaction is composed of two steps, which correspond to binding to the membrane and internalization to form stable complexes.
ISSN:0960-894X
1464-3405
DOI:10.1016/j.bmcl.2010.02.025