Sobeh Mansour, Mahmoud Mona F, Petruk Ganna, Rezq Samar, Ashour Mohamed L, Youssef Fadia S, El-Shazly Assem M, Monti Daria M, Abdel-Naim Ashraf B, Wink Michael
Institute of Pharmacy and Molecular Biotechnology, Heidelberg University, Heidelberg, Germany.
Department of Pharmacology and Toxicology, Faculty of Pharmacy, Zagazig University, Zagazig, Egypt.
Front Pharmacol. 2018 Jun 5;9:566. doi: 10.3389/fphar.2018.00566. eCollection 2018.
is widely used in folk medicine. A polyphenol-rich extract from its leaves demonstrated a plethora of substantial pharmacological properties. The extract showed solid antioxidant properties and protected human keratinocytes (HaCaT cells) against UVA damage. The extract also reduced the elevated levels of ALT, AST, total bilirubin (TB), total cholesterol (TC) and triglycerides (TG) in rats with acute CCl intoxication. In addition to reducing the high MDA level, the extract noticeably restored GSH and SOD to the normal control levels in liver tissue homogenates and counteracted the deleterious histopathologic changes in liver after CCl injection. Additionally, the extract exhibited promising anti-inflammatory activities where it inhibited LOX, COX-1, and COX-2 with a higher COX-2 selectivity than that of indomethacin and diclofenac and reduced the extent of lysis of erythrocytes upon incubation with hypotonic buffer solution. extract also markedly reduced leukocyte numbers with similar activities to diclofenac in rats challenged with carrageenan. Additionally, administration of the extract abolished writhes induced by acetic acid in mice and prolonged the response latency in hot plate test. Meanwhile, the identified polyphenolics from the extract showed a certain affinity for the active pockets of 5-lipoxygenase (5-LOX), cyclooxygenase-1 (COX-1) and cyclooxygenase-2 (COX-2) explaining the observed anti-inflammatory activities. Finally, 87 secondary metabolites (mostly phenolics) were tentatively identified in the extract based on LC-MS/MS analyses. displays good protection against oxidative stress, free radicals, and could be a good candidate for treating oxidative stress related diseases.
它在民间医学中被广泛使用。其叶子中富含多酚的提取物具有大量显著的药理特性。该提取物具有强大的抗氧化特性,可保护人类角质形成细胞(HaCaT细胞)免受紫外线A损伤。该提取物还降低了急性四氯化碳中毒大鼠体内升高的谷丙转氨酶(ALT)、谷草转氨酶(AST)、总胆红素(TB)、总胆固醇(TC)和甘油三酯(TG)水平。除了降低高丙二醛(MDA)水平外,该提取物还能使肝组织匀浆中的谷胱甘肽(GSH)和超氧化物歧化酶(SOD)显著恢复至正常对照水平,并对抗四氯化碳注射后肝脏中有害的组织病理学变化。此外,该提取物表现出有前景的抗炎活性,它抑制脂氧合酶(LOX)、环氧化酶-1(COX-1)和环氧化酶-2(COX-2),对COX-2的选择性高于吲哚美辛和双氯芬酸,并且在与低渗缓冲溶液孵育时降低红细胞的裂解程度。该提取物还能显著减少角叉菜胶攻击的大鼠体内白细胞数量,其活性与双氯芬酸相似。此外,给予该提取物可消除小鼠体内由乙酸诱导的扭体反应,并延长热板试验中的反应潜伏期。同时,从提取物中鉴定出的多酚类物质对5-脂氧合酶(5-LOX)、环氧化酶-1(COX-1)和环氧化酶-2(COX-2)的活性口袋表现出一定亲和力,这解释了观察到的抗炎活性。最后,基于液相色谱-串联质谱(LC-MS/MS)分析,在提取物中初步鉴定出87种次生代谢产物(大多为酚类)。它对氧化应激、自由基具有良好的保护作用,可能是治疗氧化应激相关疾病的良好候选药物。