ORIGINAL�ARTICLE ABSTRACT Objective: To compare the hepatoprotective effects of aqueous extract of Cassia fistula leaves and Silymarin on Acetaminophen induced hepatotoxicity. Study Design: An experimental study in mice. Place and Duration of Study: The study was conducted in the department of Pharmacology and Therapeutics, Multidisciplinary research laboratory of Islamic International Medical College, Riphah International University. The duration of study was from 16 Mar, 2016 to 16 Mar, 2017. Materials and Methods: In present study simple random sampling was done by Balloting method and sixty adult Balb/c Albino mice were divided in four groups having 15 mice each. Mice in control group A were given normal diet and fresh water. Mice in experimental group B (positive control) were given Acetaminophenat dose of 100mg /kg /day orally for six weeks. Mice in experimental group C were treated with Acetaminophen(100mg/Kg) with concurrent 400mg/Kg body weight of Cassia fistula (Aqueous extract) orally for six weeks once daily while in experimental group D mice received 750 mg/kg body weight of Silymarin orally in form of aqueous suspension in 2% Cremophor1E for 6 weeks once daily concurrently treated with Acetaminophen(100mg/Kg).The cardiac puncture was done after six weeks and 2.5cc blood was collected from each mice for assessment of biochemical markers including Serum Alanine Aminotransferase (ALT) and Serum Aspartate Aminotransferase (AST). Results: The mean value of serum ALT level was 130.4.30 ±42.90 in Group B as compared to control Group having mean value of ALT 37.30 ± 8.32. The mean value of ALT was 62.22± 19.27 and 53.90± 25.06 in Group C and in Group D respectively. In Group B mean value of serum level of AST was 134.3± 15.56 as compared to control Group A having mean value of AST31.40± 10.05.The mean value of AST in Group C and Group D were 66.40±20.50 and 44.67± 20.37 respectively. Conclusion: The Silymarin is more beneficial than aqueous extract of Cassia fistula leaves in ameliorating hepatotoxic effects of Acetaminophen. Key Words: Acetaminophen, Cassia fistula leaves, Hepatoprotective, Silymarin. considered toxic to liver. The incidence of DILI is 1 in 4 10,000 to 1 in 100,000. In humans the most common cause of drug induced liver failure is a c e t a m i n o p h e n ( Pa ra c e t a m o l , N - a c e t y l - p - 5 aminophenol,APAP) toxicity. It is safe at therapeutic doses but at larger doses it can cause serious liver 6,7 injury. The cytochrome P-450 oxidation of acetaminophen overdose result in formation of reactive metabolite N-acetyl-p-benzoquinone imine 8 (NAPQI) which initiates toxicity. It depletes glutathione and binds to cellular proteins, especially 7,9,11 in mitochondria and cause hepatotoxicity. Previous studies have also identified NAPQI as important factor in acetaminophen induced 8 hepatotoxicity. Previous studies have identified s o m e h e p a t o p r o t e c t i v e a g e n t s a g a i n s t acetaminophen induced hepatotoxicity. Silymarin Introduction Liver is a vital organ having role in metabolism of carbohydrates, proteins and lipids, bile production, maintenance of homeostasis, detoxification and 1,2 vitamin storage. Drug induced liver injury (DILI) is the leading cause of acute liver failure in most 3 countries. There are more than 1000 drugs Comparing Hepatoprotective Effects of Aqueous Extract of Cassia Fistula (Amaltas) Leaves and Silymarin Rukhsana Munawar, Adnan Jehangir, Akbar Waheed Correspondence: Dr. Rukhsana Munawar Department of Pharmacology Islamic International Medical College Riphah International University, Islamabad E-mail: dr.rukhsana33@gmail.com Department of Pharmacology Islamic International Medical College Riphah International University, Islamabad Funding Source: NIL; Conflict of Interest: NIL Received: Dec 27, 2017; Revised: Jul 09, 2018 Accepted: Jul 16, 2018 Hepatoprotective Effects of Cassia Fistula Leaves & Silymarin JIIMC 2018 Vol. 13, No.3 137 leaves were boiled in distilled water for 30 minutes. These were kept for 3 days with intermittent shaking. These were filtered by Whatman No1 filter paper. The aqueous extract was obtained by concentrated 17,19 the filtrate by rotary flash evaporator. The mice were divided into four groups randomly, each group consisting of 15 mice. Mice in Control Group A were given normal diet and fresh water o r a l l y. E x p e r i m e n t a l G r o u p B w a s g i v e n Acetaminophen 100mg/Kg orally in diet for 6 weeks 20 once daily. Experimental Group C was treated with acetaminophen 100mg/Kg with concurrent 400 mg/kg body weight of Cassia fistula(Aqueous 21 Extract) orally for 6 weeks once daily. Experimental Group D was treated with acetaminophen 100mg/Kg orally with concurrent 750 mg/kg BW of Silymarin in form of aqueous suspension in 2% 22 Cremophor1E for 6 weeks once daily. After six weeks cardiac puncture was done and blood samples were taken for evaluation of Serum Alanine Aminotransferase (ALT) and Serum Aspartate Aminotransferase (AST) levels. The data was analyzed by using Statistical package for social sciences (SPSS) version 22. The biochemical parameters ALT and AST were calculated by using Mean ± Standard deviation (SD). The mean difference between control and other groups was calculated by applying ANOVA. The Post Hoc Tuckey test was applied for comparison of mean difference between groups. p-value 0f <0.05 was considered statistically significant. Results The serum ALT and AST levels were significantly raised (p<0.00) in Acetaminophen treated Group B as compared to control Group A. The serum ALT and AST were reduced in Cassia fistula treated Group C and Silymarin treated Group D and in comparison, the results showed significant reduction in serum (SLM) is one of them having antioxidant, anti- i n f l a m m a t o r y, a n t i f i b r o t i c , a n t i v i r a l a n d 1,12,14 immunomodulatory actions. The Silymarin has hepatoprotective and antioxidant role by inhibiting 1,15 free radicals. Herbal medicines represent one of the most important fields of traditional medicine throughout the world. Cassia fistula (Family Leguminosae, Sub- family Caesalpinea) is a very common plant known for its medical properties. It is commonly called Amaltas. The antioxidant property is possessed by 16 polyphenol and flavonoids. Previous studies showed work done on methanolic and ethanolic extracts of Cassia fistula leaves. In present study aqueous extract was used to explore hepatoprotective effect of Cassia fistula leaves and its hepatoprotective effect was compared with Silymarin on Acetaminophen induced hepatotoxicity in mice and this comparison was not found in previous studies. The aim of present study was to compare hepatoprotective effects of Cassia fistula leaves and Silymarin on acetaminophen induced hepatotoxicity. Materials and Methods An experimental study was carried out in the department of Pharmacology and Therapeutics, Multidisciplinary research laboratory of Islamic International Medical College in collaboration with National Institute of Health Sciences (NIH), Islamabad from Mar 2015 to Mar 2016. Approval of synopsis was authorized by the Ethical Review Committee of Islamic International Medical College. Mice weighing 30-50grams with normal ALT and AST levels were included in the study and mice weighing less than 30grams and more than 50grams with abnormal liver function tests were excluded. Sixty Balb/c healthy albino mice were selected randomly by balloting method. A perfect living condition indistinguishable to their class with adjusted dietary supplement was given under temperature of 24±2ºC with a 12 hour light and dark cycle. Cassia fistula leaves were collected from Race course park, Rawalpindi. The leaves were air dried and then authenticated by herbarium department of National Agricultural Centre, Islamabad. The external dirt of freshly collected leaves was removed by washing with tap water. The leaves were shade dried and crushed coarsely by hand. About 400 gm of these Table I: Comparison of Serum ALT Level between the Groups (n=60) P value < 0.00 P value <0.05 =significant Hepatoprotective Effects of Cassia Fistula Leaves & Silymarin JIIMC 2018 Vol. 13, No.3 138 In present study significant improvement (p < 0.05) in serum levels of ALT and AST in Group D is observed which was given Acetaminophen followed by Silymarin. This was also revealed by study of Amir Mohammad Kazemifar et al., who demonstrated the hepatoprotective property of Silymarin in Acetaminophen induced hepatotoxicity in male 25 Sprague-Dawley rats. In present study a significant reduction (p < 0.05) was observed in raised serum levels of ALT and AST in Group C which was given Acetaminophen followed by Cassia fistula as compared to Group B which was given Acetaminophen. The hepatoprotective effect of ethanolic extract of Cassia fistula leaves was observed in study of Pradeep et al. at dose of 500mg/kg/day for 7 days against subacute Carbon Tetrachloride (CCl4) induced hepatic injury in rats. He 17 found significant improvement in levels of ALT, AST. Das et al. also proved the hepatoprotective effect of aqueous extract of fruit pulp of Cassia fistula against 18 liver damage induced by CCl4 in Albino rats. Our findings are in accordance with study of Jehangir et al. who obser ved significant reduction in biochemical parameters including ALT, AST, ALP and total bilirubin by ethanolic extract of Cassia fistula leaves against hepatotoxicity induced by Isoniazid 27 and Rifampicin. The better hepatoprotective effect of aqueous extract of Cassia fistula leaves could be proven with increasing duration of study. Further studies are required to see hepatoprotective effect of Cassia fistula leaves with higher doses and by use of different routes of administration. The molecular mechanism responsible for reducing biochemical and histopathological parameters can be explored by further studies. Conclusion In present study significant hepatoprotective effect was shown by aqueous extract of Cassia fistula leaves probably due to presence of flavonoids. Silymarin demonstrated better hepatoprotective effect than Cassia fistula against Acetaminophen induced hepatotoxicity. REFERENCES 1. Vargas-Mendoza N, Madrigal-Santillán E, Morales-González Á, Esquivel-Soto J, Esquivel-Chirino C, y González-Rubio MG-L, et al. Hepatoprotective effect of silymarin. World journal of hepatology. 2014; 6: 144. 2. Pandit A, Sachdeva T, Bafna P. Drug-induced hepatotoxicity: levels of ALT and AST in Silymarin treated Group D as compared to Cassia fistula treated Group C. Discussion Drug induced liver injury is an unresolved health problem and Acetaminophen is known to cause 23 hepatic damage at high doses. The reactive metabolite NAPQI has been implicated to play a role 8,24 in hepatic damage. The present study is designed to compare hepatoprotective effects of aqueous extract of Cassia fistula leaves and Silymarin on A c eta m i n o p h e n i n d u c e d h e p ato tox i c i t y by measuring biochemical parameters including serum ALT and AST. In present study hepatotoxicity is induced in Group B with Acetaminophen. Group C and Group D were given aqueous extract of Cassia fistula leaves and Silymarin with concurrent Acetaminophen respectively to ameliorate the hepatotoxic effects of Acetaminophen on serum levels of ALT and AST. In the present study mice in experimental group B showed abnormal increase in serum levels of ALT and AST which were given Acetaminophen. This is in accordance with findings of Amir Mohammad Kazemifar et al., who induced hepatotoxicity in male Sprague-Dawley rats with single oral dose of Acetaminophen 800mg/kg by gavage with an orogastric canula and he observed significant 25 increase in levels of ALT and AST. This is also consistent with study of Abel Felipe Freitage who found significant changes in LFTs due to hepatotoxic 26 effect of Acetaminophen. Table II: Post hoc Tukey's test for mul�ple comparison of ALT between the Groups Table III: Post hoc Tukey's Test for Mul�ple Comparison of AST between the Groups Hepatoprotective Effects of Cassia Fistula Leaves & Silymarin JIIMC 2018 Vol. 13, No.3 139 Hepatoprotective Effects of Cassia Fistula Leaves & Silymarin JIIMC 2018 Vol. 13, No.3 chronically exposed to hydrogen sulfide; modulating influence of TNF-α cytokine genetic polymorphism. Daru. 2013; 21: 28. 16. Kalaiyarasi C, Karthika K, Lalithkumar P, Ragupathi G, Saravanan S. In vitro anti-oxidant activity of various solvent fractions of Cassia fistula L. pods. Journal of Pharmacognosy and Phytochemistry. 2014; 3: 73-6. 17. Pradeep K, Mohan C, Anand K, Karthikeyan S. Effect of pretreatment of Cassia fistula Linn. leaf extract against subacute CCl 4 induced hepatotoxicity in rats. 2005. 18. Das S, Sarma G, Barman S. Hepatoprotective activity of aqueous extract of fruit pulp of Cassia fistula (AFCF) against carbon tetrachloride (CCL4) induced liver damage in albino rats. J Clin Diagn Res. 2008; 2: 1133-8. 19. Sutar GV, Dass K, Einstein JW. Screening of different leaf extracts of Cassia fistula Linn for investigation of hypolipidemic activity in two different rat models. International Letters of Natural Sciences. 2015;3. 20. Kane AE, Mitchell SJ, Mach J, Huizer-Pajkos A, McKenzie C, Jones B, et al. Acetaminophen hepatotoxicity in mice: Effect of age, frailty and exposure type. Experimental gerontology. 2016;73:95-106. 21. Kumar A. A review on hepatoprotective herbal drugs. Int J Res Pharm Chem. 2012; 2: 96-102. 22. El-Lakkany NM, Hammam OA, El-Maadawy WH, Badawy AA, Ain-Shoka AA, Ebeid FA. Anti-inflammatory/anti- fibrotic effects of the hepatoprotective silymarin and the schistosomicide praziquantel against Schistosoma mansoni-induced liver fibrosis. Parasit Vectors. 2012;5: 767–73. 23. Yoon E, Babar A, Choudhary M, Kutner M, Pyrsopoulos N. Acetaminophen-induced hepatotoxicity: a comprehensive update. Journal of clinical and translational hepatology. 2016; 4: 131. 24. Hinson JA, Roberts DW, James LP. Mechanisms of acetaminophen-induced liver necrosis. Adverse Drug Reactions: Springer. 2010. p. 369-405. 25. Kazemifar AM, Hajaghamohammadi AA, Samimi R, Alavi Z, Abbasi E, Asl MN. Hepatoprotective property of oral silymarin is comparable to n-acetyl cysteine in acetaminophen poisoning. Gastroenterology research. 2012; 5: 190. 26. Freitag AF, Cardia GFE, da Rocha BA, Aguiar RP, Silva-Comar FMdS, Spironello RA, et al. Hepatoprotective Effect of Silymarin (Silybum marianum) on Hepatotoxicity Induced by Acetaminophen in Spontaneously Hypertensive Rats. Evidence-Based Complementary and Alternative Medicine. 2015. 27. Jehangir A, Nagi A, Shahzad M, Zia A. The hepato-protective effect of Cassia fistula (amaltas) leaves in isoniazid and rifampicin induced hepatotoxicity in rodents. Biomedica. 2010; 26: 25-9. A review. 2012. 3. Gómez-Lechón MJ, Tolosa L. Human hepatocytes derived from pluripotent stem cells: a promising cell model for drug hepatotoxicity screening. Archives of toxicology. 2016; 90: 2049-61. 4. Haque T, Sasatomi E, Hayashi PH. Drug-induced liver injury: pattern recognition and future directions. Gut and liver. 2016; 10: 27. 5. Jaeschke H, McGill MR, Ramachandran A. Oxidant stress, mitochondria, and cell death mechanisms in drug-induced liver injury: lessons learned from acetaminophen hepatotoxicity. Drug metabolism reviews. 2012; 44: 88-106. 6. McGill MR, Williams CD, Xie Y, Ramachandran A, Jaeschke H. Acetaminophen-induced liver injury in rats and mice: comparison of protein adducts, mitochondrial dysfunction, and oxidative stress in the mechanism of toxicity. Toxicology and applied pharmacology. 2012; 264: 387-94. 7. Jaeschke H, McGill MR, Williams CD, Ramachandran A. Current issues with acetaminophen hepatotoxicity—a clinically relevant model to test the efficacy of natural products. Life sciences. 2011; 88: 737-45. 8. Kheradpezhouh E, Ma L, Morphett A, Barritt GJ, Rychkov GY. TRPM2 channels mediate acetaminophen-induced liver damage. Proceedings of the National Academy of Sciences. 2014; 111: 3176-81. 9. Ward J, Kanchagar C, Veksler-Lublinsky I, Lee RC, McGill MR, Jaeschke H, et al. Circulating microRNA profiles in human patients with acetaminophen hepatotoxicity or ischemic hepatitis. Proceedings of the National Academy of Sciences. 2014; 111: 12169-74. 10. Kon K, Kim JS, Uchiyama A, Jaeschke H, Lemasters JJ. Lysosomal iron mobilization and induction of the mitochondrial permeability transition in acetaminophen- induced toxicity to mouse hepatocytes. Toxicological Sciences. 2010; 117: 101-8. 11. Antoine DJ, Dear JW, Lewis PS, Platt V, Coyle J, Masson M, et al. Mechanistic biomarkers provide early and sensitive detection of acetaminophen-induced acute liver injury at first presentation to hospital. Hepatology. 2013; 58: 777-87. 12. Polyak SJ, Morishima C, Lohmann V, Pal S, Lee DY, Liu Y, et al. Identification of hepatoprotective flavonolignans from silymarin. Proceedings of the National Academy of Sciences. 2010; 107: 5995-9. 13. Polyak SJ, Ferenci P, Pawlotsky JM. Hepatoprotective and antiviral functions of silymarin components in hepatitis C virus infection. Hepatology. 2013; 57: 1262-71. 14. Bahmani M, Shirzad H, Rafieian S, Rafieian-Kopaei M. Silybum marianum: beyond hepatoprotection. Journal of evidence-based complementary & alternative medicine. 2015; 20: 292-301. 15. Mandegary A, Saeedi A, Eftekhari A, Montazeri V, Sharif E. Hepatoprotective effect of silyamarin in individuals 140