Anti-inflammatory and anticancer compounds isolated from Ventilago madraspatana Gaertn., Rubia cordifolia Linn. and Lantana camara Linn. Subhalakshmi Ghosh a , Madhushree Das Sarma a , Amarendra Patra b and Banasri Hazra a a Department of Pharmaceutical Technology, Jadavpur University, Kolkata, India, and b Department of Chemistry, University College of Science, Kolkata, India Abstract Objectives The aim was to search for anti-inflammatory and anticancer compounds from three medicinal plants, viz. Ventilago madraspatana Gaertn., Rubia cordifolia Linn. and Lantana camara Linn. Methods The NO• scavenging potential of selected plant extracts was determined on LPS/IFN-g activated murine peritoneal macrophage cultures, and iNOS and COX-2 expres- sion was evaluated by Western blot analysis. Bio-assay guided fractionation yielded four compounds: physcion and emodin from V. madraspatana, 1-hydroxytectoquinone from R. cordifolia, and oleanonic acid from L. camara. The anti-inflammatory activity of these compounds was tested through the carrageenan-induced rat-paw oedema model. They were then tested against a murine tumour (Ehrlich ascites carcinoma), and three human cancer cell lines, namely A375 (malignant skin melanoma), Hep2 (epidermoid laryngeal carcinoma) and U937 (lymphoma). Key findings All four compounds dose dependently inhibited NO• through suppression of iNOS protein without affecting macrophage viability. Physcion and emodin caused 65–68% reduction of oedema volume at 40 mg/kg, which validated their in-vivo anti-inflammatory effect. 1-hydroxytectoquinone and oleanonic acid exhibited promising cytotoxicity against A375 cells. Conclusions Ethnomedical reports on these traditional medicinal plants have been ratio- nalised through an insight into the anti-inflammatory as well as anticancer potential of four constituents, characterised to be prospective candidates for designing novel therapeutic agents. Keywords anticancer activity; anti-inflammatory activity; inducible nitric oxide synthase; Lantana camara; Rubia cordifolia; Ventilago madraspatana Introduction Inflammatory diseases are a longstanding medical problem and a major cause of morbidity worldwide. To get symptomatic relief in inflammatory conditions such as arthritis and rheumatism, treatment mostly involves the application of steroidal and non-steroidal anti- inflammatory drugs (NSAIDs), which are in great demand these days. However, prolonged use of NSAIDs often leads to renal problems, gastrointestinal irritation and other side effects, while some of these specific COX-2 inhibitors, such as rofecoxib and celecoxib, have recently been implicated in a high possibility of myocardial infarction/strokes, and have been marketed with a ‘black-box’ warning. [1] The inflammatory pathway is characterised by several mediators, one of which is the nitric oxide radical (NO•). It is generated from the terminal guanido-nitrogen of l-arginine through a five-electron oxidation process, aided by the NADPH-dependent enzyme known as nitric oxide synthase (NOS; EC 1.14.13.39). [2] During inflammatory reactions in mammals, the Ca 2+ -independent inducible form of nitric oxide synthase (iNOS) is stimulated by either bacterial lipopolysaccharide (LPS, a bacterial endotoxin), or pro- inflammatory cytokines (IFN-g, TNF-a, IL-1b), and expressed within macrophages, hepa- tocytes, and endothelial or smooth muscle cells. [2] This leads to the generation of NO•, which plays an essential role in the defence system of the host. However, in the event of Research Paper JPP 2010, 62: 1158–1166 © 2010 The Authors Journal compilation © 2010 Royal Pharmaceutical Society of Great Britain Received October 1, 2009 Accepted May 17, 2010 DOI 10.1111/j.2042-7158.2010.01151.x ISSN 0022-3573 Correspondence: Banasri Hazra, Department of Pharmaceutical Technology, Jadavpur University, Kolkata 700032, India. E-mail: banasrihazra@yahoo.co.in; hazra1@vsnl.com 1158 Downloaded from https://academic.oup.com/jpp/article/62/9/1158/6135655 by guest on 10 May 2023