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Anti-diabetic and lipid-lowering effects of drimane sesquiterpenoids isolated from Zygogynum pancheri.
Chemico-Biological Interactions ( IF 4.7 ) Pub Date : 2020-06-27 , DOI: 10.1016/j.cbi.2020.109167
Sahla Belhadj 1 , Henda Keskes 2 , Cécile Apel 3 , Fanny Roussi 3 , Marc Litaudon 3 , Olfa Hentati 4 , Noureddine Allouche 2
Affiliation  

Recently, it has been shown that drimane-type sesquiterpenoids isolated from Zygogynum pancheri, a species native to New Caledonia, possessed significant α-amylase inhibitory activities. To further explore their antidiabetic potential, we investigated the effect of 1β-O-(E-cinnamoyl)-6α-hydroxy-9epi-polygodial (D) and 1β-E-O-p-methoxycinnamoyl-bemadienolide (L), two of the most active compounds of the series, on diabetic model rats. Compounds D and L (2 mg kg/day) were daily and orally administrated for 30 days to streptozotocin (STZ) (150 mg/kg) induced male diabetic Wistar rats. Animals were allocated into five groups of six rats. Comparatively to diabetic rats, treatments with D and L compounds were able to significantly (P < 0.05) decrease Fasting Blood Glucose (FBG) (70.15%, 71.02%), serum total cholesterol (46.27% and 39.38%), triglycerides (56.60% and 58.15%), creatinine (37.31% and 36.49%) and uric acid levels (67.76% and 69.68%), respectively. Compounds D and L also restored the altered plasma enzyme (aspartate aminotransferase, AST (47.83% and 43.20%), alanine aminotransferase, ALT (49.76% and 48.35%, alkaline phosphatase, ALP (72.78% and 73.21%)) and lactate dehydrogenase, LDH (47.95% and 53.93%) levels to near normal, respectively. Administration of Glymepiride, significantly (p < 0.05) reduced FBG (73.94%) in STZ induced diabetic rats. Additionally, the compounds D and L exhibited inhibitory effects in vivo on lipase activity of diabetic rats (54.83% and 52.25%), respectively. The outcomes of this study suggested that these two drimanes could be considered as efficient hypoglycemic, hypolipidemic and antiobesity agents for diabetes management and its complications.



中文翻译:

从Zygogynum pancheri分离的drimane倍半萜类化合物的抗糖尿病和降脂作用。

最近,已经显示从新喀里多尼亚原生种的合子(Zygogynum pancheri)分离的drimane型倍半萜类具有显着的α-淀粉酶抑制活性。为了进一步探讨其抗糖尿病的潜力,我们研究了1β- O-E-肉桂酰基)-6α-羟基-9 Epi - polygodial(D)和1β- E - O - p的作用-甲氧基肉桂酰基-甜菜烯内酯(L),该系列中最活跃的两种化合物,用于糖尿病模型大鼠。每天将化合物D和L(2mg kg /天)口服给予链脲佐菌素(STZ)(150mg / kg)诱导的雄性糖尿病Wistar大鼠,持续30天。将动物分为五组,每组六只大鼠。与糖尿病大鼠相比,用D和L化合物治疗可显着(P <0.05)降低空腹血糖(FBG)(70.15%,71.02%),血清总胆固醇(46.27%和39.38%),甘油三酸酯(56.60%和58.15%),肌酐(37.31%和36.49%)和尿酸水平(分别为67.76%和69.68%)。化合物D和L还恢复了改变的血浆酶(天冬氨酸转氨酶,AST(47.83%和43.20%),丙氨酸转氨酶,ALT(49.76%和48.35%),碱性磷酸酶,ALP(72.78%和73.21%)和乳酸脱氢酶, LDH(分别为47.95%和53.93%)达到接近正常水平。格列美脲的施用显着(p  <0.05)降低了STZ诱导的糖尿病大鼠的FBG(73.94%)。此外,化合物D和L在体内具有抑制作用对糖尿病大鼠脂肪酶活性的影响分别为54.83%和52.25%。这项研究的结果表明,这两种drimane可以被认为是糖尿病管理及其并发症的有效降糖,降血脂和抗肥胖药。

更新日期:2020-09-03
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