Kotha Peddanna, Badri Kameswara Rao, Nagalapuram Ramya, Allagadda Rajasekhar, Chippada Appa Rao
Department of Biochemistry, Sri Venkateswara University, Tirupati, India.
Minority Men's Health Initiative, Transdisciplinary Collaborative Center, Hampton University, Hampton, Virginia, USA.
Cell Physiol Biochem. 2017;43(4):1689-1702. doi: 10.1159/000484030. Epub 2017 Oct 18.
BACKGROUND/AIMS: Diabetes mellitus is a pandemic metabolic disorder that is affecting a majority of populations in recent years. There is a requirement for new drugs that are safer and cheaper due to the side effects associated with the available medications.
We investigated the anti-diabetic activity of leaves of Anisomeles malabarica following bioactivity guided fractionation. The different solvent (hexane, ethyl acetate, methanol and water) extracts of A. malabarica leaves were used in acute treatment studies to evaluate and identify the active fraction. The ethyl acetate extract was subjected to further fractionation using silica gel column chromatography and the compounds were identified by LC-SRM/MS and GC-MS. Additional chronic treatment studies were carried out using this active fraction (AMAF) for 30 days in experimental diabetic rats. Fasting blood glucose (FBG), glycosylated hemoglobin (HbA1c), plasma insulin levels and glucose tolerance were measured along with insulin resistance/sensitivity indicators (HOMA-IR, HOMA-β and QUICKI) to assess the beneficial effects of A. malabarica in the management of diabetes mellitus.
Among the different solvent extracts tested, ethyl acetate extract showed maximum (66%) anti-hyperglycemic activity. The hexane and ethyl acetate (1: 1) fraction that has maximum anti-diabetic activity was identified as active fraction of A. malabarica (AMAF). The FBG, HbA1c, plasma insulin levels and insulin sensitivity/resistance indicators such as glucose tolerance, HOMA-IR, HOMA-β and QUICKI were significantly improved to near normal in diabetic rats treated with AMAF. Further, we identified key flavonoids and fatty acids as the anti-diabetic active principles from the AMAF of A. malabarica leaves.
The results of our study suggest that Anisomeles malabarica has potential anti-diabetic activity in STZ induced diabetic rats.
背景/目的:糖尿病是一种大流行的代谢紊乱疾病,近年来影响着大多数人群。由于现有药物存在副作用,因此需要更安全、更便宜的新药。
我们在生物活性导向分级分离后,研究了马拉巴罗勒叶片的抗糖尿病活性。马拉巴罗勒叶片的不同溶剂(己烷、乙酸乙酯、甲醇和水)提取物用于急性治疗研究,以评估和鉴定活性成分。乙酸乙酯提取物通过硅胶柱色谱进一步分级分离,化合物通过液相色谱-质谱/质谱联用仪(LC-SRM/MS)和气相色谱-质谱联用仪(GC-MS)进行鉴定。使用该活性成分(AMAF)对实验性糖尿病大鼠进行了为期30天的额外慢性治疗研究。测量空腹血糖(FBG)、糖化血红蛋白(HbA1c)、血浆胰岛素水平和葡萄糖耐量,以及胰岛素抵抗/敏感性指标(HOMA-IR、HOMA-β和QUICKI),以评估马拉巴罗勒在糖尿病管理中的有益作用。
在所测试的不同溶剂提取物中,乙酸乙酯提取物显示出最大(66%)的降血糖活性。具有最大抗糖尿病活性的己烷和乙酸乙酯(1:1)馏分被鉴定为马拉巴罗勒的活性成分(AMAF)。在用AMAF治疗的糖尿病大鼠中,FBG、HbA1c、血浆胰岛素水平和胰岛素敏感性/抵抗指标,如葡萄糖耐量、HOMA-IR、HOMA-β和QUICKI,均显著改善至接近正常水平。此外,我们从马拉巴罗勒叶片的AMAF中鉴定出关键黄酮类化合物和脂肪酸为抗糖尿病活性成分。
我们的研究结果表明,马拉巴罗勒在链脲佐菌素诱导的糖尿病大鼠中具有潜在的抗糖尿病活性。