Anti-diabetic and lipid-lowering effects of drimane sesquiterpenoids isolated from Zygogynum pancheri
Anti-diabetic and lipid-lowering effects of drimane sesquiterpenoids isolated from Zygogynum pancheri
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DOI：
10.1016/j.cbi.2020.109167
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发表时间：
2020-10-01
影响因子：
5.1
通讯作者：
Allouche, Noureddine
中科院分区：
文献类型：
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作者：
Belhadj, Sahla;Keskes, Henda;Allouche, Noureddine
最近的研究表明，从产于新喀里多尼亚的Zygogynum Pancheri中分离得到的德里曼型倍半萜类化合物具有显著的α-淀粉酶抑制活性。为了进一步探索它们的抗糖尿病作用，我们研究了该系列中最有效的两个化合物1β-O-(E-肉桂酰基)-6α-羟基-9-表没食子酸(D)和1-β-E-O-甲氧基肉桂酰基-苯二烯内酯(L)对糖尿病模型大鼠的作用。用链脲佐菌素(15 0 mg/kg)诱导雄性Wistar大鼠糖尿病模型，每日灌胃给予化合物D和L(2 mg kg/d)，连续30d。动物被分成五组，每组六只大鼠。与糖尿病大鼠相比，D组和L组能显著降低空腹血糖(70.15%和71.02%)、血清总胆固醇(46.27%和39.38%)、甘油三酯(56.60%和58.15%)、肌酐(37.31%和36.49%)和尿酸(67.76%和69.68%)。化合物D和L还能使谷草转氨酶(47.83%和43.20%)、丙氨酸氨基转移酶(49.76%和48.35%)、碱性磷酸酶(72.78%和73.21%)和乳酸脱氢酶(47.95%和53.93%)恢复到接近正常水平。甘美比利显著降低STZ诱导的糖尿病大鼠的空腹血糖(73.94%)(p<；0.05)。此外，化合物D和L对糖尿病大鼠体内脂肪酶活性的抑制率分别为54.83%和52.25%。本研究结果提示，这两种地尔蒙可被认为是治疗糖尿病及其并发症的有效降糖、降血脂和抗肥胖药。
Recently, it has been shown that drimane-type sesquiterpenoids isolated from Zygogynum pancheri, a species native to New Caledonia, possessed significant a-amylase inhibitory activities. To further explore their antidiabetic potential, we investigated the effect of 1 beta-O-(E-cinnamoyl)-6 alpha-hydroxy-9epi-polygodial (D) and 1 beta-E-Op-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.