Quick Menu

Upcoming Journals
  • No Upcoming Journals

Journal of Complementary and Alternative Medical Research

Journal of Complementary and Alternative Medical Research, ISSN: 2456-6276,Vol.: 2, Issue.: 4

 

Original-research-article

 

Flavonoids and Biflavonoids of Amentoflavone Class as Potential Psychoactive Drug Leads

 

 

Abeer Moawad1* and Mohamed Hifnawy2

1Department of Pharmacognosy, Faculty of Pharmacy, Beni-Suef University, Beni-Suef, 62514, Egypt.

2Department of Pharmacognosy, Faculty of Pharmacy, Cairo University, Cairo, Egypt.

 

Abstracts

 

Aims: There are several reported interactions between amentoflavone and CNS receptors especially GABA receptors and also reported interaction between flavonoids and opioid receptors. The current study determines other related compounds of amentoflavone, hinokiflavone and other flavonoid monomers with potential CNS activity.

Study Design: Natural and semisynthetic derivative of biflavonoids of amentoflavone and hinokiflavone class and several flavonoid monomers were screened for their binding ability to CNS receptor and neurotransmitter transporters using the Psychoactive Drug Screening Program (PDSP) University of North Carolina at Chapel Hill.

Methodology: Natural and semisynthetic flavonoid derivatives were subjected to binding assays with 44 receptors and transporters. Only compounds showing ≥50% binding inhibition in the primary assay were subjected to secondary binding assay.

Results: In the secondary binding assay; significant binding with rat benzodiazepine receptor, dopamine transporter, GABAA, norepinephrine transporter and Sigma 2 receptors were observed. (+) Catechin and sakurantin showed significant binding with dopamine transporter (Ki= 1 and 1.6 nM respectively) compared to the positive control (GBR 12909; Ki= 1 nM) in addition to the biflavonoid 7,7″,4‴-trimethyl-2,3-dihydroamentoflavone (16517) which showed activity at Ki= 172 nM and we present the first report of its 13C NMR data. Semi synthesis afforded the new derivative 7,7″,4‴-trimethyldihydrohinokiflavone but it was inactive towards the screened receptors and neurotransmitter transporters.

Conclusion: Studying the structure-activity relationship revealed that methylation of amentoflavone decreased their ability to bind with rBZP, GABAA receptor and NET except for 7,7″,4‴-trimethyl-2,3-dihydroamentoflavone which was the most active among biflavonoids toward DAT. On the other hand, methylation of naringenin created new binding capability of sakurantin. Configurations of the chiral center at C-3 and hydroxylation pattern at ring B in flavan-3-ols greatly affect binding with dopamine transporter. Dihydrohinokiflavone and its trimethyl derivatives were completely inactive. Our study reveals new biological activity of some common flavonoids that may be promising drugs leads.

 

Keywords :

CNS; catechin; dopamine transporter; sakurantin; amentofavone; NMR.

 

Full Article - PDF    Page 1-9    Article Metrics

 

DOI : 10.9734/JOCAMR/2017/32856

Review History    Comments

Search this site

Advanced Search

Announcement & News

SCOPUS selected Annual Research & Review in Biology (ARRB)

We are delighted to inform that famous indexing organization SCOPUS (from Elsevier) selected  A...

Index Copernicus Evaluation Result Released

We are delighted to inform that Index Copernicus (a leading indexing organization from Pol...

Journal Repository (JR): Permanent Digital Archiving of SDI journals

SDI is happy to announce that all our journals are now permanently archived in Journal Repository (J...

Index Copernicus Value of British Journal of Medicine and Medical Research

  We are delighted to inform that Index Copernicus (a leading indexing organization ...

SDI journal got 35th ranking in Publons

We are delighted to announce (as of 04/01/2016) that British Journal of Medicine and Medical Re...

Growth of SDI and world publication market

As of 2014, total 25,064 journals are competing in World market of journal publication. In 2011, tot...

Publication and site statistics (up to Sept, 2015)

  Number of submission: 22181 (Total up to Sept, 2015) Number of published paper: 10949&n...

Index Medicus selected 15 SDI journals

We are delighted to inform that Index Medicus (IMSEAR) has selected following 15 SDI journals for in...

SCIENCEDOMAIN international received 5844 submissions in 2013

SCIENCEDOMAIN international is pleased to announce that it has received 5844 submissions in 2013, ac...

Science (IF: 31) report confirmed the high standard of SDI journal

As per a recent report (Link) of Science journal (present Impact factor 31), one of our journal (Bri...



SCIENCEDOMAIN Awards

  • No Awards listed.

Browser Compatibility : Mozila firefox, Google Crome and IE 7 & above. Creative Commons License Terms & Condition   |   Privacy Policy   |   Join Us   |   Help   |   Contact Us
© Copyright 2010-2017, SCIENCEDOMAIN international. All rights reserved.