Document Detail

Modifications of andrographolide to increase some biological activities: a patent review (2006 - 2011).
MedLine Citation:
PMID:  22329509     Owner:  NLM     Status:  MEDLINE    
INTRODUCTION: Andrographis paniculata Nees, Acanthaceae, is a well-recognised medicinal plant in Asia. It has been reported to possess a variety of biological activities. The main constituent of A. paniculata is andrographolide (Androg). Since the plant is known to treat many diseases, Androg was modified for many biological activities to treat and prevent a variety of diseases.
AREA COVERED: This review surveys the patents from 2006 to 15 November 2011 for antibacterials, antivirals, antidiabetic, anticancer, analgesic, antipyretic and anti-inflammatory analogues. SciFinder database was used to search for the patent work using the keywords 'andrographolide', 'andrographolide derivatives', 'andrographolide analogues' and later additional limits, that is, 'patent' and 'years', 'Clinical trial' and 'years' were searched. Espacenet was also searched for 'andrographolide', 'andrographolide derivatives' and 'andrographolide analogues'.
EXPERT OPINION: Androg is a good pharmacophore for many pharmacological activities. Esterification at either one or more of the three hydroxyls with short/long chains, heterocyclic, aromatic fatty acids was attempted and tested for a variety of activities. Most of the responses were positive. Other modifications were epoxidation at Δ(7(18)) along with esterifications with various carboxylic acids for anticancer activity. 15-Alkylidene analogues were investigated for α-glucosidase inhibition. The improvement of activities have not yet been proven to be due to the increase in the ability of analogues to reach the targets as prodrugs or the new feature structures fitted to the receptors. It seems that substitution with active compounds, such as lipoic acid, is a new trend for modification.
Chantana Aromdee
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Publication Detail:
Type:  Journal Article; Review     Date:  2012-02-14
Journal Detail:
Title:  Expert opinion on therapeutic patents     Volume:  22     ISSN:  1744-7674     ISO Abbreviation:  Expert Opin Ther Pat     Publication Date:  2012 Feb 
Date Detail:
Created Date:  2012-02-20     Completed Date:  2012-06-22     Revised Date:  2013-11-06    
Medline Journal Info:
Nlm Unique ID:  9516419     Medline TA:  Expert Opin Ther Pat     Country:  England    
Other Details:
Languages:  eng     Pagination:  169-80     Citation Subset:  IM    
Khon Kaen University, Department of Pharmaceutical Chemistry, 123 Mitraparp Rd, Muang Khon Kaen 40002, Thailand.
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MeSH Terms
Analgesics / pharmacology
Anti-Infective Agents / pharmacology
Anti-Inflammatory Agents / pharmacology
Antineoplastic Agents, Phytogenic / pharmacology
Antipyretics / pharmacology
Diterpenes / chemistry,  pharmacology*
Drug Design
Hypoglycemic Agents / pharmacology
Legislation, Drug
Molecular Structure
Patents as Topic
Structure-Activity Relationship
Reg. No./Substance:
0/Analgesics; 0/Anti-Infective Agents; 0/Anti-Inflammatory Agents; 0/Antineoplastic Agents, Phytogenic; 0/Antipyretics; 0/Diterpenes; 0/Hypoglycemic Agents; 410105JHGR/andrographolide

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