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Synthesis and Biological Activities of Mangiferin Derivatives

Author: WuZuoFeng
Tutor: WuQiuYe
School: Second Military Medical University
Course: Medicinal Chemistry
Keywords: Mangiferin Aglycone Cholesterol acyltransferase Inhibitors Cytotoxic
CLC: R284.1
Type: Master's thesis
Year: 2009
Downloads: 429
Quote: 3
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Abstract


Isolation and structural modification of natural products , has been one of the important way for people to find and discover new drugs . Is also one of the best shortcuts of drug research in China . Mangiferin isolated from Anemarrhena the polyphenols Dihydroxydiphenyl and Pyrones reported to have a variety of biological activity , the the mangiferin antidiabetic activity , is the main active ingredient Chinese medicine Anemarrhena treatment diabetes . Structural modification of mangiferin , found that the activity of the the mangiferin aglycone on some of the targets is stronger than mangiferin , synthesis of different substituted aglycone , and in accordance with the structural design of drugs sub Flatten the principle of mangiferin aglycone structural modification , we introduced in mangiferin on diabetes sulfonamide or sulfonylurea group ; Second, its 1,3 -position hydroxyl benzyl structural modification . By Friedel-Crafts reaction , cyclization, acylation , replaced etherification reaction , a total of 40 synthetic compounds . 38 compounds were first reported and confirmed by HNMR, MS, IR and elemental analysis . The multiple models of pharmacological activity screening of target compounds , the initial in vitro pharmacological screening : The results show that these compounds have some biological activity of diabetes , target enzyme DPP-IV ; but found that the 4 - position sulfonamides cholesterol acyltransferase (ACAT1 and ACAT2) having a strong inhibitory activity ; 1,3-position hydroxy - benzyl derivatives are preferably tumor cell inhibition . Their structure-activity relationship study , summed introduced in the structure of the meta-substituted phenyl piperazine can significantly enhance the inhibitory activity , by computer - aided drug design and other means . The success of this project dibenzo pyrone on the selective introduction of a sulfa active group , and found that the double benzene pyrone 4 - bit sulfonamides strong inhibition of the ability of cholesterol acyltransferase . Due to the limited number of compounds , such compounds active role with sulfonamide side chain structure-activity relationship between cholesterol acyltransferase inhibition remains to be further studied .

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CLC: > Medicine, health > Chinese Medicine > Of Pharmacy > Traditional Chinese medicine chemical > Chemical analysis and identification
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