Department of Biochemistry, Federal University of Santa Catarina, Florianópolis, SC, Brazil.
Libyan J Med. 2010 Jun 8;5. doi: 10.3402/ljm.v5i0.4891.
This study investigated the hepatoprotective effect and antioxidant properties of phloroacetophenone (2',4',6'-trihydroxyacetophenone - THA), an acetophenone derived from the plant Myrcia multiflora. MATERIAL #ENTITYSTARTX00026;
The free radical scavenging activity in vitro and induction of oxidative hepatic damage by carbon tetrachloride (CCl(4)) (0.5 ml/kg, i.p.) were tested in male Swiss mice (25±5 g).
This compound exhibited in vitro antioxidant effects on FeCl(2)-ascorbate-induced lipid peroxidation (LPO) in mouse liver homogenate, scavenging hydroxyl and superoxide radicals, and 2,2-diphenyl-1-picrylhydrazyl. The in vivo assays showed that THA significantly (p<0.01) prevented the increases of hepatic LPO as measured by the levels of thiobarbituric acid-reactive substances, mitochondrial swelling. It also protected hepatocytes against protein carbonylation and oxidative DNA damage. Consistent with these observations, THA pre-treatment normalized the activities of antioxidant enzymes, such as catalase, glutathione peroxidase, and superoxide dismutase, and increased the levels of reduced glutathione (GSH) in CCl(4)-treated mice. In addition, THA treatment significantly prevented the elevation of serum enzymatic activities of alanine amino transferase, aspartate amino transferase, and lactate dehydrogenase, as well as histological alterations induced by CCl(4). Silymarin (SIL) (24 mg/kg), a known hepatoprotective drug used for comparison, led to a significant decrease (p<0.01) in activities of theses enzymes in way very similar to that observed in pre-treatment with THA.
These results suggest that the protective effects are due to reduction of oxidative damage induced by CCl(4) resulting from the antioxidant properties of THA.
本研究调查了 phloroacetophenone(2',4',6'-三羟基苯乙酮 - THA)的肝保护作用和抗氧化特性,这种苯乙酮来源于桃金娘科植物桃金娘。
在雄性瑞士小鼠(25±5 g)中测试了体外清除自由基活性和四氯化碳(CCl4)(0.5 ml/kg,ip)诱导的氧化肝损伤。
该化合物在体外对小鼠肝匀浆中 FeCl2-抗坏血酸诱导的脂质过氧化(LPO)表现出抗氧化作用,清除羟自由基和超氧自由基,以及 2,2-二苯基-1-苦基肼。体内试验表明,THA 显著(p<0.01)阻止了丙二醛含量的增加,丙二醛是肝 LPO 的指标,还防止了线粒体肿胀、肝蛋白质羰基化和氧化 DNA 损伤。与这些观察结果一致,THA 预处理使抗氧化酶的活性正常化,如过氧化氢酶、谷胱甘肽过氧化物酶和超氧化物歧化酶,并增加了 CCl4 处理小鼠中还原型谷胱甘肽(GSH)的水平。此外,THA 治疗显著防止了丙氨酸氨基转移酶、天冬氨酸氨基转移酶和乳酸脱氢酶的血清酶活性升高,以及 CCl4 诱导的组织学改变。水飞蓟素(SIL)(24 mg/kg)是一种用于比较的已知保肝药物,其作用与 THA 预处理非常相似,显著降低了这些酶的活性(p<0.01)。
这些结果表明,保护作用是由于 THA 的抗氧化特性减少了 CCl4 诱导的氧化损伤。