Detail of "141099-60-7"

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7b-hydroxycholesterol blocked at C-3-OH inhibits growth of rat glioblastoma in vivo: comparison between 7b-hydroxycholesteryl-3b(ester)-oleate and 7b-hydroxycholesteryl-3b-O(ether)-oleyl

All Rights Reserved. 7b-hydroxycholesterol blocked at C-3-OH inhibits growth of rat glioblastoma in vivo: comparison between 7b-hydroxycholesteryl-3b(ester)-oleate and 7b-hydroxycholesteryl-3b-O(ether)-oleyl. Rakotoarivelo, Clovis; Adamczyk, Monika; Desgeorges, Michel; Langley, Keith; Lorentz, Jean-Georges; Mann, Andre; Ricard, Damien; Scherrer, Elisabeth; Privat, Alain; Mersel, Marcel (Unite 583 de l'INSERM, Institut des Neurosciences de Montpellier, Montpellier 34091, Fr.). Anticancer Research, 26(3A), 2053-2062 (English) 2006 International Institute of Anticancer Research. CODEN: ANTRD4. ISSN: 0250-7005.Chemicals with cas numbers 916154-13-7 and 141099-60-7 also play role. DOCUMENT TYPE: Journal CA Section: 1 (Pharmacology) Background: It was previously demonstrated that the 7b-hydroxycholesteryl-3b(ester)-oleate (7b-ester) possesses antitumor properties against the exptl. rat C6 glioblastoma. The effect of an analog of this mol., 7b-hydroxycholesterol-3b-O(ether)-oleyl (7b-ether), was investigated. Materials and Methods: Liposomes contg. no oxysterol (control), 7b-ether or 7b-ester were injected into tumors induced by C6 cells in rat brain cortex. At defined times, the animals were sacrificed, the tumors stained with cresyl violet and their vols. measured by densitometry. Oxysterol clearance was assessed by quantification from lipid extn. of treated tumors. Results: The clearance of the new compd. was slower than that of the 7b-ester form. The 7b-ether and 7b-ester forms displayed similar antitumor activities against 3-day-old tumors. In contrast, the 7b-ether form was more active on well-developed glioblastoma: 75 nmol inhibited tumor growth by 70% compared to controls, while the 7b-ester had no effect under such conditions. The 7b-ether form had a cytostatic rather than a cytotoxic effect. In addn., the compn. of the liposomes did not affect the antitumor activity. Conclusion: Only blockade of the C-3-OH group is required for the antitumor effect of this kind of oxysterol. It is suggested that the absence of "etherases" enhances the antitumor activity of this type of compd. Thus, an original therapeutic approach for glioblastoma treatment may be envisaged with such compds. .