Activity-guided investigation ofCarissa carandas(L.) roots for anti-inflammatory constituents

Abstract

The present study was structured to investigate the anti-inflammatory potential of the extracts, fractions and compounds isolated from Carissa carandas (L.) roots. Bioassay guided fractionation of methanol extract based on inhibitory potential towards proinflammatory mediators (TNF-α, IL-1β and nitric oxide (NO)) led to the identification of stigmasterol (1), lupeol (2), oleanolic acid (3), carissone (4) and scopoletin (5) as potential anti-inflammatory agents. Carissone (4) (IC50 = 20.1 ± 2.69 μg/mL) and scopoletin (5) (IC50 = 24.6 ± 1.36 μg/mL) exhibited significant inhibition of NO production comparable to specific NO inhibitor (L-NAME; IC50 = 19.82 ± 1.64 μg/mL) without affecting the cell viability. Also, 4 and 5 at a concentration of 30 μM were found to inhibit 41.88-53.44% of TNF-α and IL-1β. To the best of our knowledge, this is the first report displaying the anti-inflammatory effects of C. carandas (L.) roots, partially mediated by inhibition of TNF-α, IL-1β and NO.

Ethnopharmacology, phytochemistry, and biotechnological advances of family Apocynaceae: A review

“…Moreover, β‐sitosterol, stigmasterol, sitosterol glucoside (119) , and cholest‐5‐en‐3‐β‐ol (120) were previously isolated from Carissa carandas roots by various researchers (Balakrishnan et al, ; Bhaskar & Balakrishnan, ; Hegde et al, ). The stigmasterol from Carissa carandas was reported for marked anti‐inflammatory activity (Galipalli et al, ). Recently, Bhadane and Patil () investigated antioxidative and anti‐inflammatory potential of methanolic extracts of Carissa carandas leaves by activity‐guided fractionation and 20‐hydroxypreganan‐18‐oic acid (121) was reported as a potential antioxidative and anti‐inflammatory steroid with t EC 50 values 546.4 and 498.5 μg/ml, respectively, for DPPH and OH − radical scavenging activities.…”

The Genus Carissa: An Ethnopharmacological, Phytochemical and Pharmacological Review

“…They found out that lupeol ( 1 ) and oleanolic acid ( 15) exhibited potential anti-inflammatory activities [56]. …”

“…They found out that carissone ( 26 ) exhibited potential anti-inflammatory agents as well as significant inhibition of NO production comparable to specific NO inhibitor without affecting the cell viability [56]. …”

“…They are mostly hydroxybenzoic and hydroxycinnamic acid derivatives. There has been increased interest towards natural and synthetic phenyl propanoids for medicinal use as antioxidant, UV screens, anticancer, antivirus, anti-inflammatory, wound healing and antibacterial activities [10, 55, 56]. …”

“…In a separate study to investigate the anti-inflammatory potential of root methanol extracts of C. carandas involving bioassay guided fractionation of extract based on inhibitory potential towards proinflammatory mediators (TNF-a, IL-1b and NO), it was found out that lupeol ( 1 ), oleanolic acid ( 15) , carissone ( 26 ), stigmasterol ( 86 ), and scopoletin ( 104 ) possess potential anti-inflammatory agents. Carissone ( 26 ) and scopoletin ( 104 ) exhibited significant inhibition of NO production comparable to specific NO inhibitor without affecting the cell viability [56]. C. spinarum has been used traditionally for the treatment of inflammation-related disorders such as rheumatic pain and to relieve fever.…”