Curcumin Analogues, PGV-0 and GVT-0, Inhibit Cholesterol Absorption Through The Reduction on Lipase Activity

  • IKA PUSPITA SARI UNIVERSITAS GADJAH MADA
  • ARIEF NURROCHMAD UNIVERSITAS GADJAH MADA
  • IRFAN MURIS SETIAWAN UNIVERSITAS GADJAH MADA
  • SARDJIMAN SARDJIMAN UNIVERSITAS GADJAH MADA

Abstract

Curcumin has been known to reduce cholesterol levels in hyperlipidemic state. Faculty of Pharmacy Universitas Gadjah Mada (UGM) synthesized curcumin analogues namely PGV-0 and GVT-0. Like curcumin, both PGV-0 and GVT-0 exhibit anti-inflammatory activities. The aims of this study were to determine the effect and the mechanism of curcumin analogues PGV-0 and GVT-0 on regulation of cholesterol levels in serum. This study was aimed to examine whether PGV-0 and GVT-0 affected cholesterol levels through cholesterol absorption which is regulated by lipase enzyme. To determine the reduction in cholesterol levels, rats were feed with high fat diet (HFD) for 45 days. PGV-0 and GVT-0 were given on day 31-45 at doses of 40 mg/kg bw and 60 mg/kg bw consecutively. Total cholesterol and lipase activity in serum were measured and then statistically analyzed using ANOVA and t-test. The increase of cholesterol levels was markedly reduced by the treatment with both curcumin analogues. Furthermore, lipase activity was clearly inhibited by the treatment with PGV-0 and GVT-0, suggesting that these compounds inhibit cholesterol levels through the reduction of lipase enzyme activity

References

1. Reksohadiprodjo MH, Timmerman H, Sardjiman, Supardjan AM, Sudibyo M, Sugiyanto, et al. 2004, Derivatives of benzylidene cyclohexanone, benzylidene cyclopentanone and benzylidene acetone, and therapeutics use thereof, US Patent, US 6,777,447 B2.
2. Rao DS, Sekhara NC, Satyanarayana MN, Srinivasan M. Effect of curcumin on serum and liver cholesterol levels in the rat. J Nutr. 1970.100(11):1307-15.
3. Asai A, Miyazawa T. Dietary curcuminoids prevent high-fat diet-induced lipid accumulation in rat liver and epididymal adipose tissue. J Nutr. 2001.131(11):2932-2935.
4. Babu PS, Srinivasan K. Hypolipidemic action of curcumin, the active principle of turmeric (Curcuma longa) in streptozotocin induced diabetic rats. Mol Cell Biochem. 1997.166(1-2):169-175.
5. Ramirez-Tortosa MC, Mesa MD, Aguilera MC, Quiles JL, Baro L, Ramirez-Tortosa CL, et al. Oral administration of a turmeric extract inhibits LDL oxidation and has hypocholesterolemic effects in rabbits with experimental atherosclerosis. Atherosclerosis. 1999.147(2):371-378.
6. Alwi I, Santoso T, Suyono S, Sutrisna B, Suyatna FD, Kresno SB, Ernie S. The effect of curcumin on lipid level in patients with acute coronary syndrome. Acta Med Indones. 2008.40(4):201-10.
7. Baum L, Cheung SK, Mok VC, Lam LC, Leung VP, Hui E, et al. Curcumin effects on blood lipid profile in a 6-month human study. Pharmacol Res. 2007. 56(6):509-14.
8. Soni KB, Kuttan R. Effect of oral curcumin administration on serum peroxides and cholesterol levels in human volunteers. Indian J Physiol Pharmacol. 1992.36(4):273-275.
9. Da’i M. Pengaruh gugus β-diketon terhadap daya reduksi kurkumin dan turunannya pada ion ferri [skripsi]. Yogyakarta: Fakultas Farmasi, Universitas Gadjah Mada; 1998.
10. Sardjiman. Synthesis of some new series of curcumin analogues, antioxydative, antiinflammatory, antibacterial activities and qualitative–structure activity relationships [dissertation]. Yogyakarta: Gadjah MadaUniversity; 2000.
11. Nugroho AE, Sardjiman, Maeyama K. Efek sitotoksik dan atiproliferasi dari gamavuton-0 pada kultur sel leukemia basofilik tikus. Majalah Farmasi Indonesia. 2009.20(2):84-90.
12. Kalpana C, Rajasekharan KN, Menon VP. Modulatory effects of curcumin and curcumin analog on circulatory lipid profiles during nicotine-induced toxicity in Wistar rats. J Med Food. 2005.8(2):246-50.
13. Arafa HMM. Curcumin attenuates diet-induced hypercholesterolemia in rats. Med Sci Monit. 2005.11(7):BR228-34.
14. Sakuma Y, Hagihara H, Nagayoshi A, Ohne K, Mutoh S, Ito Y, et al. Effect of FR 145237, an aryl-CoA:cholesterol acyltransferase inhibitor, on diet-induced hypercholesterolemia in diabetic rats. Life Sci. 1997.60(6):351-6.
15. Breitz J, Mest HJ. A new derivative of tradipil (AR 12456) as apotential new antiatherosclerotic drug. Cardiovasc Drugs Rev. 1991.9:385-97.
16. Beynen AC, Lemmens AG, Katan MB De Bruijne DD, Van Zupthen LF. Cholesterol metabolism and esterases in four strains of rats with different cholesterolemic responses to a high-cholesterol, high-cholate diet. Comp Biochem Physiol B. 1987.87(1):41-8.
17. Monte MJ , Jimenez R. Effects of hypercholesterolemia-inducing diet on biliary electrolytes and lipid secretion in the rat. Int J Exp Pathol.1993.74(2):203-10.
18. Hasimun P, Sukandar EY, Adnyana IK, Tjahjono DH. A simple method for screening antihyperlipidemic agents. Int J Pharmacol. 2011.7(1):74-8.
Published
2013-09-30
How to Cite
SARI, IKA PUSPITA et al. Curcumin Analogues, PGV-0 and GVT-0, Inhibit Cholesterol Absorption Through The Reduction on Lipase Activity. JURNAL ILMU KEFARMASIAN INDONESIA, [S.l.], v. 11, n. 2, p. 123-126, sep. 2013. ISSN 2614-6495. Available at: <http://jifi.farmasi.univpancasila.ac.id/index.php/jifi/article/view/204>. Date accessed: 05 nov. 2024.
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Vol 11 No 2 (2013): JIFI
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