Andrographolide: progression in its modifications and applications - a patent review (2012 - 2014).

INTRODUCTION: Extraction, isolation and modifications of andrographolide (Androg) is extensively investigated and patented. The prominent activities were vastly modified for anticancer and antivirals. Many products related to Androg are commercially available, thus the section 'Interaction of Androg and Andrographis paniculata dried extract with drugs' is included. AREAS COVERED: The data in this review are searched and selected from SciFinder and Espacenet for the patents, with the keywords: Andrographolide and Andrographolide analogs, and the results were refined by the years. EXPERT OPINION: Modifications of Androg have been done to nearly all of the possible sites, and now screening tests for any new activities had been settled down. Categorizing the analogs that have been developed is not clear cut since some diseases can develop into others, for example, inflammation and some viral infections can develop into cancer. Currently, investigation of the mode of action and the mechanisms at the molecular level are intensively ongoing. Producing new chemotherapeutic agents from Androg looks promising. The main problem of using Androg in therapeutic applications is its insolubility in aqueous media. Those modified analogs' esters, ethers or salts, have to be considered for the stability of pharmaceutical preparations, and transformation in biological fluids after administration. Further stages of drug development are required for those promising analogs.