کد مقاله | کد نشریه | سال انتشار | مقاله انگلیسی | نسخه تمام متن |
---|---|---|---|---|
5513144 | 1540982 | 2017 | 8 صفحه PDF | دانلود رایگان |
عنوان انگلیسی مقاله ISI
Synthesis, in vitro and in vivo biological evaluation of new oxysterols as modulators of the liver X receptors
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کلمات کلیدی
موضوعات مرتبط
علوم زیستی و بیوفناوری
بیوشیمی، ژنتیک و زیست شناسی مولکولی
زیست شیمی
پیش نمایش صفحه اول مقاله
چکیده انگلیسی
Liver X Receptor (LXR) modulators have shown potential as drugs since they target genes affecting metabolism and fatty acid synthesis. LXR antagonists are of particular interest since they are able to reduce the synthesis of complex fatty acids and glucose uptake. Based on molecular modeling, five new cholesterol mimics were synthesized, where four contained a hydroxyl group in the 22-S-position. The new compounds were screened in vitro against several genes affecting lipid metabolism. The compound that performed best in vitro was a dimethylamide derivative of 22(S)-hydroxycholesterol and it was chosen for in vivo testing. However, the blood plasma analysis from the in vivo tests revealed a concentration lower than needed to give any response, indicating either rapid metabolism or low bioavailability.
ناشر
Database: Elsevier - ScienceDirect (ساینس دایرکت)
Journal: The Journal of Steroid Biochemistry and Molecular Biology - Volume 165, Part B, January 2017, Pages 323-330
Journal: The Journal of Steroid Biochemistry and Molecular Biology - Volume 165, Part B, January 2017, Pages 323-330
نویسندگان
Ove Alexander Høgmoen Ã
strand, Elvar Ãrn Viktorsson, Aleksander Lim Kristensen, Dag Ekeberg, Hanne Røberg-Larsen, Steven Ray Wilson, Mari Gabrielsen, Ingebrigt Sylte, Arild Christian Rustan, G. Hege Thoresen, PÃ¥l Rongved, Eili Tranheim Kase,