DISCUSSION ON ALLIUM SATIVUM, AND ALOE BARBADENSIS ETHANOL EXTRACTS ON PARACETAMOL – INDUCED HEPATOTOXICITY IN ALBINO RATS

Ethanolic extraction of the homogenized dried cloves of A. sativum and A. barbadensis gave a relatively low percentage yield 6.8 and 11.8 % respectively. This may  suggest that most of the chemical components of the plants have low solubility in ethanol (Table 1 ).This could explain the use of aqueous extract of most medicinal plants by traditional medicine practitioners for the sole purpose of achieving high yield and potency as documented by Sofowora (1993).

            Paracetamol induced oxidative stress and hepatotoxicity in all the treated animals,as reflected by significant increase (p < 0.05) in TBARS, AST, ALT, ALP and Bilirubin levels and a significant decrease (p < 0.05 ) in GSH, SOD, CAT and Protein. This analgesic and antipyretic drug (paracetamol) is quite safe at therapeutic doses and normally undergoes glucuronidation and sulfation to the corresponding conjugates.
When acetaminophen intake far exceeds therapeutic doses, the glucuronidation and sulfation pathways are saturated and the cytochrome P 450 pathways become increasingly important. However, with time hepatic glutathione is depleted faster than it can be regenerated and accumulation of a reactive and toxic metabolite occurs. In the absence of intracellular antioxidants such as glutathione, this reactive metabolite (N – acetyl-P- benzoquinone imine, NAPQI) reacts with nucleophilic groups present on cellular macromolecules such as protein or lipids and alter the homeostasis of calcium resulting in hepatotoxicity (Katzung, 1998).

            The significant increase (p < 0.05) in glutathione level observed after treatment of animals with extracts of A. sativum and A. barbadensis suggests hepatoprotection.The actual mechanism of hepatoprotection of these extracts is not well understood; however chemical constituents of plant extracts have been shown to exhibit antioxidant properties. For example, flavonoids have been reported to contain antioxidant properties (Gosh et al, 2007).These antioxidant properties of extracts may have contributed to hepatoprotection displayed in this work. Further, cells have a number of mechanisms to protect themselves from the toxic effect of reactive oxygen species (ROS). Glutathione is an intracellular reductant, widely distributed in cells and plays major role in catalysis, metabolism and transport. It protects cells against free radicals, peroxides and other toxic compounds (Fairhust et al, 1982).In the present study, the effectiveness of these extracts were demonstrated using paracetamol induced rats which is a known model for both hepatic glutathione depletion and injury. Therefore, the level of glutathione is of crucial importance in liver injury caused by paracetamol. Our results are in line with a research work by Gosh et al (2007), because we found that after A. sativum and A. barbadensis supplementation, the GSH level increased significantly (p < 0.05) in a dose dependent manner as compared with paracetamol treated showing that exogenous ethanolic extracts might provide a means to recover reduced GSH levels and to prevent tissue disorders and injuries (Gosh et al, 2007).

            From the results, a significant decrease ( p < 0.05 ) was observed in the level of TBARS, the end products of lipid peroxidation in the liver of rats treated with extracts of A. sativum and A. barbadensis as compared to paracetamol treated (Appendix I).The increase in TBARS levels in liver suggests enhanced lipid peroxidation leading to tissue damage. Pretreatment with ethanolic extracts of A. sativum and A. barbadensis significantly reversed these changes in a dose dependent pattern. Hence it maybe possible that the mechanism of hepatoprotection of the extracts is due to their ability to reduce or prevent lipid preoxidations.

            The result on super oxide dismutase (SOD)) showed a significant decrease (P < 0.05) in the concentration of SOD in the rats treated with paracetamol in comparison with the control group. This reduced significantly after treatment of animals with extracts of A. sativum and A. barbadensis in a dose dependent manner, showing a reversal in the toxicity effect and antioxidant action. phenols are very important plant constituents because of their free radical scavenging ability and antioxidant action due to their hydroxyl groups. These extracts according to the works of sofowora, 1993 is found to contain phenolic compounds in significant amount, which attributes to its rationality of possessing antioxidant activity.
           Significant increase (p < 0.05) in the level of catalase (CAT) after treatment of animals with extracts was observed. This implies that the extracts poses antioxidant activity. Hydrogen peroxide is a harmful by product of many normal metabolic processes, to prevent damage; it must be quickly converted into other less dangerous substances. To this end, catalase is frequently used by cells to rapidly catalyze the decomposition of hydrogen peroxide into less   reactive gaseous oxygen and water molecules. The was a significant difference (p< 0.05) produced between the lowest dosage (200 µg/ml) and the highest dosage of (800 µg/ml) of the extracts showing that the extracts are more effective at high concentration, of which A. sativum was more effective. Our result is in line with the work of Gosh et al, 2007 were he worked on hepatoprotection and antioxidant activity of some medicinal plants.
        The significant increase (p < 0.05) of AST in rats treated with paracetamol overdose show that the paracetamol affected the liver hepatocytes causing the enzymes to leak into the blood stream. However, treatment with ethanolic extracts of A. sativum and A.  barbadensis, caused a significant decrease (p< 0.05) in a dose dependant manner showing that the extracts contains compounds that can be effective in the protection and treatment of liver damage. Serum transaminase AST is an important liver enzyme because it indicates the condition of the liver (Nelson et al, 2000). Liver degeneration due to drug toxicity is accompanied by leakage of liver enzymes from injured hepatocytes into the blood. These transaminases are most useful for monitoring the degree of recovery of a damaged liver. This is in line with the work of Sorimuthu et al, 2005 where the antioxidant property of A. barbadensis was observed in streptozotocin – induced diabetes in rats.

    The significant decrease (p < 0.05) in serum ALT as compared with the paracetamol treated group observed after treatment with extracts suggests hepatoprotective activity of the extracts. Serum ALT catalysis the conversion of alanine to pyruvate and glutamate, and is released in a similar manner. Therefore, ALT is more specific to the liver and thus an important parameter for detecting liver injury (Nelson et al, 2000 From the results, it shows that both extracts have high medicinal value but A. sativum was more effective.
            Our result demonstrated that the ethanolic extracts of A. sativum and A. barbadensis caused significant inhibition (p < 0.05) in the level of serum alkaline phosphatase in a dose dependent manner.
Alkaline phosphatase is another liver marker enzyme that is used to check liver dysfunction. Serum ALP and bilirubin levels are related to the function of hepatic cell. Increase in serum level of ALP is due to increased synthesis, in the presence of increasing biliary pressure (Gosh et al, 2007).
            Bilirubin, the end product of heme metabolism is essential in diagnosis of liver damage. The normal range is 0.1 – 0.5 mg / dl in animals. When the level reaches above 2 mg / dl, Jaundice becomes clinically obvious. From the results obtained, the extracts decreased bilirubin level significantly (p< 0. 05)as compared with the control group (Appendix II).Effective control of alkaline phosphatase activity and bilirubin level points towrds an early improvement in secretory mechanism of hepatic cells.

            From the results, the level of albumin decreased due to its increased catabolism with little effect on globulin level. The administration of the extracts of A. sativum and A. barbadensis reduced this abnormality to an extent (with extract of A. sativum showing a higher effect. plasma proteins are very important in the body and provide a useful diagnostic aid. Albumin performs an important function in binding many substances, reducing their availability and toxic actions. Thus the binding (conjugation) of bilirubin protects the newborn child against the toxic action of this substances, preventing it from penetrating the blood-brain–barrier. The binding ability of albumin to drugs is reduced in hypoalbuminaemia when binding sites are blocked by various metabolites.                   

            In the histology result, the photomicrograph shows that the liver has necrosis characterized by distortion of the liver pattern (Walter et al, 1996). Necrosis is known as death of liver hepatic cells and paracetamol over dose is known to cause bridge necrosis a type of necrosis caused from extensive damage of adjacent liver cells and Central portal vein. This could be seen clearing and cells regenerating after administration of extracts of A. sativum and A. barbadensis showing that the extracts contains some components capable of protecting the liver from drug toxicity.
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