In vitro and in vivo anti-inflammatory activity of Tetrastigma sulcatum leaf extract, pure compound and its derivatives

Abstract

The severity and perseverance of the in ammation have been demonstrated in many health conditions.The limitations of existing medications, propose the need for newer alternative anti-in ammatory medications. In our earlier studies, we demonstrated the topical anti-in ammatory potential of crude ethanolic extract of Tetrastigma sulcatum leaves and its fractions. In the present study, we further explored anti-in ammatory activity of T. sulcatum extract, fractions, pure compound and its derivatives using in vitro and in vivo bioassay techniques. We attempted to isolate a pure compound from leaf extract and was identi ed as Friedelan-3β-ol (CI) and its derivatives Friedelinol acetate (C II) and Friedelinol methyl ether (C III) were synthesized. Treatment with crude extract and its fractions demonstrated a signi cant reduction in the mRNA expression levels of pro-inflammatory cytokines (IL-1β, IL-6, TNF-α) and nitric oxide (NO) production in LPS-stimulated in ammation in RAW 264.7 cells.Likewise, compounds CI, CII and CIII showed a similar pattern of signi cant inhibition of proin ammatory cytokines and NO production. In vivo study in Carrageenan induced paw-in ammatory mice model demonstrated reduced paw oedema and proin ammatory cytokines levels in a dose-dependent manner upon treatment of extract, its fractions, pure compound (CI), and their derivatives (CII and CIII.). The docking study showed all the compounds (CI, CII and CIII) share common residues with Dexamethasone. TNF-α exhibited the most interacting residues with the compounds. The present study con rmed the T. sulcatum 's anti-in ammatory activity, suggesting Friedelan-3β-ol as an active component in a crude extract.

Anti-arthritic efficacy of Bombax ceiba ethanolic extract in a murine model for rheumatoid arthritis using in vivo, in vitro and radiological analysis

“…A variety of mediators, including cytokines (IL-1B and TNF-alpha), GM-CSF, interferons, and PGDF, are released during chronic inflammation. These mediators are responsible for pain, bone and cartilage degradation, and severe impairment [ 21 ].Standard drug and hydro-alcoholic Bombax ceiba extract, on the other hand, can significantly suppress paw swelling and decrease paw volume in both acute and chronic phases, which may be due to the suppression of inflammatory mediators released due to Freund's adjuvant induction [ 22 ]. Though the exact mechanism of inflammation suppression is unknown, it can be connected with the presence of alkaloids and flavonoids in suppressing inflammation and antioxidant activity [ 23 ].…”

“…The serum was isolated from the blood of experimental animals by clotting at room temperature for 30 minutes. TNF-alpha and IL-6 protein concentrations in serum were measured using ELISA kits and the method was carried out according to the manufacturer's instructions [ 17 ].…”