کد مقاله | کد نشریه | سال انتشار | مقاله انگلیسی | نسخه تمام متن |
---|---|---|---|---|
10738336 | 1046702 | 2011 | 5 صفحه PDF | دانلود رایگان |
عنوان انگلیسی مقاله ISI
Potency of inhibition of human DNA topoisomerase I by flavones assessed through physicochemical parameters
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کلمات کلیدی
Nrf2energy of the highest occupied molecular orbitalkeap1 - buy1ROS - ROSHomo - انسان، هوموhighest occupied molecular orbital - بالاترین مدول مولکولی اشغال شدهSinglet oxygen quenching - خنک کردن اکسیژن تکAnticancer drugs - داروهای ضد سرطانDiphenols - دیفنول هاFree radicals - رادیکال آزادFlavones - فلاونRedox regulation - مقررات RedoxKelch-like ECH-associated protein 1 - پروتئین مرتبط با ECH کلچ 1Reactive oxygen species - گونههای فعال اکسیژن
موضوعات مرتبط
علوم زیستی و بیوفناوری
بیوشیمی، ژنتیک و زیست شناسی مولکولی
سالمندی
پیش نمایش صفحه اول مقاله
چکیده انگلیسی
DNA topoisomerases, enzymes involved in DNA replication and transcription, are known as targets for anticancer drugs. Among the various types of topoisomerase inhibitors, flavones (F) have been identified as promising compounds. In this study, it is shown that the potency of flavones acting as topoisomerase I inhibitors can be ranked according to their redox properties and their 3D structure. Linear correlations were observed between the topoisomerase I inhibition activity exerted by five flavones (chrysin, apigenin, kaempferol, fisetin, quercetin) and experimental and theoretical redox parameters of F. Moreover, theoretical calculations of the dihedral angle O1-2-1â²-2â² in the flavone molecules indicate the importance of their structural and steric features in their potency as topoisomerase I inhibitors. It is suggested that the flavones might interact with the DNA-topoisomerase I complex after their oxidation into quinones via autoxidation, enzymatic oxidation, or reactions with reactive oxygen species. Our investigation opens a new strategy quantitatively based on redox and 3D structural parameters in the search for the most active flavones as anticancer drug candidates inhibiting topoisomerase I.
ناشر
Database: Elsevier - ScienceDirect (ساینس دایرکت)
Journal: Free Radical Biology and Medicine - Volume 51, Issue 7, 1 October 2011, Pages 1406-1410
Journal: Free Radical Biology and Medicine - Volume 51, Issue 7, 1 October 2011, Pages 1406-1410
نویسندگان
René V. Bensasson, Vincent Zoete, Akino Jossang, Bernard Bodo, Paola B. Arimondo, Edward J. Land,