Inula sesquiterpenoids: structural diversity, cytotoxicity and anti-tumor activity. (March 2014)

• Record Type: Journal Article
• Authors: Wang, Guo-Wei; Qin, Jiang-Jiang; Cheng, Xiang-Rong; Shen, Yun-Heng; Shan, Lei; Jin, Hui-Zi; Zhang, Wei-Dong
• Is Part Of: Expert opinion on investigational drugs. Volume 23:Number 3(2014:Mar.)
• Page Start: 317
• Page End: 345
• Publication Date: 2014-03
• Subjects: Drugs -- Design -- Periodicals; Drugs, Investigational -- Bibliography; Drugs, Investigational -- Periodicals; 615.1
• DOI: 10.1517/13543784.2014.868882
• Languages: English
• ISSNs: 1354-3784

Abstract

<abstract> <title> <x xml:space="preserve">Abstract</x> </title> <p> <bold> <italic>Introduction:</italic> </bold> The plants of the genus <italic>Inula</italic> (Asteraceae) are widely distributed throughout Europe, Africa and Asia, and many of these plants have long been used in folk medicine. This genus is a rich source of sesquiterpenoids, which exhibit a wide range of biological activities. Recently, a series of bioactive sesquiterpenoid dimers, with unusual carbon skeletons, have been reported and these have gathered considerable interest.</p> <p> <bold> <italic>Areas covered:</italic> </bold> This article systematically reviews sesquiterpenoids isolated from the genus <italic>Inula</italic> that have appeared in literature up to August 2013, critically highlighting their anti-tumoral activities and relevant mechanistic insights. The authors also discuss the initial structure–activity relationships for the cytotoxic and anti-tumoral activities of the <italic>Inula</italic> sesquiterpenoids. Finally, the authors discuss the challenges and potential applications of these sesquiterpenoids in the future.</p> <p> <bold> <italic>Expert opinion:</italic> </bold> Cytotoxic and anti-tumor activities of <italic>Inula</italic> sesquiterpenoids have been extensively studied since the 1970s. One promising compound, Japonicone A, a dimeric sesquiterpene lactone from traditional herb <italic>Inula japonica, </italic> has displayed potent <italic>in vitro</italic> and <italic>in vivo</italic> anti-tumor activity against Burkitt's lymphoma. Additionally, acetylbritannilactone is thought to be capable of suppressing the abnormal vascular smooth muscle cell proliferation, with the induction of apoptosis <italic>in vivo</italic> and <italic>in vitro.</italic> In this regard, it may be worthwhile further investigating acetylbritannilactone in patients with vascular restenosis. Furthermore, given the anti-inflammatory property of britanin, clinical studies on chronic bronchitis and asthma, using the ethanol extract of <italic>I. japonica, </italic> are currently underway in South Korea. However, despite demonstrating good therapeutic effects, additional pharmacological and toxicological studies are still needed.</p> </abstract>