Caralluma umbellata Haw. protects liver against paracetamol toxicity and inhibits CYP2E1

Introduction: Paracetamol is a potent hepatotoxin and may cause severe acute hepatocellular injury. The present study was intended to assess the hepatoprotective potential of Caralluma umbellata Haw. (Asclepiadaceae) (C. umbellata) against paracetamol-induced hepatotoxicity in vitro and in vivo experimental models.

Methods: Preliminary analysis for antioxidant and hepatoprotective property was evaluated for methanolic (MCU), aqueous (ACU) and hydro methanolic (HCU) extracts of C. umbellata using in vitro cell-free antioxidant such as DPPH, ABTS, nitric oxide, lipid peroxidation models and cell-based hepatoprotective study using BRL3A cells. In vivo, hepatoprotective activity was studied in paracetamol treated male Wistar albino rats. Furthermore, molecular mechanism behind the protective effect of MCU was explored by RT PCR technique by utilizing cytochrome P450 (CYP) CYP2E1.

Results: C. umbellata extracts especially, MCU showed a better antioxidant property. MCU offered significant dose-dependent protection against paracetamol-induced hepatic damage in both in vitro and in vivo assays by improving all the biochemical findings towards the normal range. In a mechanism-based study, MCU has offered significant down-regulation (p < 0.05) of CYP2E1. These findings were in line with the hepatoprotective activity findings where MCU showed significant protection.

Conclusion: In conclusion, these findings suggest that MCU possess hepatoprotective activity. One of the possible mechanisms behind the protective effect of MCU is found to be inhibition of CYP2E1.