野牡丹和紫锦木叶片混合物甲醇提取物对大鼠的协同胃保护活性。
Synergistic gastroprotective activity of methanolic extract of a mixture of Melastoma malabathricum and Muntingia calabura leaves in rats.
作者信息
Halim Siti Zawanah, Zakaria Zainul Amiruddin, Omar Maizatul Hasyima, Mohtarrudin Norhafizah, Wahab Ikarastika Rahayu Abdul, Abdullah Muhammad Nazrul Hakim
机构信息
Department of Biomedical Science, Faculty of Medicine and Health Sciences, Universiti Putra Malaysia, 43400, Serdang, Selangor, Malaysia.
Integrative Pharmacogenomics Institute (iPROMISE), Level 7, FF3 Building, Universiti Teknologi MARA, 42300, Puncak Alam, Selangor, Malaysia.
出版信息
BMC Complement Altern Med. 2017 Nov 9;17(1):488. doi: 10.1186/s12906-017-1992-9.
BACKGROUND
Melastoma malabathricum L. (family Melastomaceae; MM) and Muntingia calabura L. (family Elaeocarpaceae; MC) have been separately reported to possess gastroprotective activity. In an attempt to develop a pharmaceutical product with antiulcer potential, the synergistic gastroprotective activity of methanolic extract of a mixture of MM and MC (MMMC) at various ratios was evaluated in rat models.
METHODS
Rats were pre-treated orally with 2% Tween 80 (vehicle), 100 mg/kg ranitidine (reference drug) or MMMC (ratios of 1:1, 1:3 and 3:1 (v/v); doses of 15, 150 or 300 mg/kg) and then subjected to the ethanol-induced gastric ulcer or pyloric ligation assays. Stomach of rats from the former assay was collected and subjected to the macroscopic and microscopic observations, and enzymatic and non-enzymatic antioxidant studies while the gastric juice content and tissue from the latter assay were subjected to the antisecretory activity study. The UHPLC analysis of MMMC was also performed.
RESULT
MMMC, in the ratio 1:1, demonstrated the most effective (P < 0.001) gastroprotective activity indicated by the highest reduction in ethanol-induced ulcer area formation. These macroscopic findings were supported by the microscopic observations. Except for pH and total acidity, MMMC also significantly (P < 0.001) reduced the volume of gastric content but increased the gastric wall mucus content in the pyloric-ligation test. MMMC also demonstrated remarkable antioxidant activity indicated by the highest total phenolic content (TPC) value and oxygen radical absorbance capacity (ORAC) activity with the recorded IC value of approximately 53 μg/mL for the 2,2- diphenyl-1-picrylhydrazyl (DPPH) scavenging activity. MMMC also improved the catalase (CAT), superoxide dismutase (SOD), glutathione (GSH), prostaglandin E2 (PGE2) and malondialdehyde (MDA) activities of the gastric tissue intoxicated by ethanol. UHPLC analysis of MMMC confirmed the presence several flavonoid-based bioactive compounds.
CONCLUSION
MMMC, at the ratio of 1:1 (v/v), exerts gastroprotective activity partly by activating its antisecretory and antioxidant activities, and via modulation of the gastric tissue endogenous antioxidant system.
背景
分别有报道称毛稔(野牡丹科;MM)和杨叶肖槿(杜英科;MC)具有胃保护活性。为了开发一种具有抗溃疡潜力的药品,在大鼠模型中评估了不同比例的毛稔和杨叶肖槿混合物(MMMC)甲醇提取物的协同胃保护活性。
方法
大鼠口服给予2%吐温80(赋形剂)、100mg/kg雷尼替丁(参比药物)或MMMC(比例为1:1、1:3和3:1(v/v);剂量为15、150或300mg/kg)进行预处理,然后进行乙醇诱导的胃溃疡或幽门结扎试验。收集前一试验中大鼠的胃进行大体和显微镜观察、酶促和非酶促抗氧化研究,而后一试验中的胃液含量和组织进行抗分泌活性研究。还对MMMC进行了超高效液相色谱分析。
结果
比例为1:1的MMMC表现出最有效的(P<0.001)胃保护活性,表现为乙醇诱导的溃疡面积形成减少最多。这些大体观察结果得到了显微镜观察的支持。在幽门结扎试验中,除pH值和总酸度外,MMMC还显著(P<0.001)减少了胃内容物的体积,但增加了胃壁黏液含量。MMMC还表现出显著的抗氧化活性,表现为总酚含量(TPC)值最高和氧自由基吸收能力(ORAC)活性最高,2,2-二苯基-1-苦基肼(DPPH)清除活性的记录IC值约为53μg/mL。MMMC还改善了乙醇中毒胃组织的过氧化氢酶(CAT)、超氧化物歧化酶(SOD)、谷胱甘肽(GSH)、前列腺素E2(PGE2)和丙二醛(MDA)活性。MMMC的超高效液相色谱分析证实存在几种基于黄酮类的生物活性化合物。
结论
比例为1:1(v/v)的MMMC部分通过激活其抗分泌和抗氧化活性以及调节胃组织内源性抗氧化系统发挥胃保护活性。
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