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Abstract：
Twelve terpenoids were evaluated in the treatment of type 2 diabetes mellitus: seven monoterpenes (geranyl acetate (1), geranic acid (2), citral (3), geraniol (4), methyl geranate (5), nerol (6), and citronellic acid (7)), three sesquiterpenes (farnesal (8), farnesol (9), and farnesyl acetate (10)), one diterpene (geranylgeraniol (11)), and one triterpene (squalene (12)) were selected to carry out a study on normoglycemic and streptozotocin-induced diabetic mice. Among these, 2, 3, 7, 8, 9, and 10 showed antihyperglycemic activity in streptozotocin-induced diabetic mice. They were then selected for evaluation in oral sucrose and lactose tolerance tests (OSTT and OLTT) as well as in an oral glucose tolerance test (OGTT). In the OSTT and OLTT, compounds 3, 7, 8, 9, and 10 showed a reduction in postprandial glucose peaks 2 h after a sucrose or lactose load (comparable to acarbose). In the case of the OGTT, 2, 7, 8, 9, and 10 showed a reduction in postprandial glucose peaks 2 h after a glucose load (comparable to canagliflozin). Our results suggest that the control of postprandial hyperglycemia may be mediated by the inhibition of disaccharide digestion, such as sucrose and lactose, and the regulation of the absorption of glucose. The first case could be associated with an ∝ -glucosidase inhibitory effect and the second with an inhibition of the sodium-glucose type 1 (SGLT-1) cotransporter. Finally, five acyclic terpenes may be candidates for the development and search for new α-glucosidase and SGLT-1 cotransporter inhibitors.
摘要：
在2型糖尿病的治疗中评估了十二种萜类化合物：七个单萜（乙酸香叶酯（1），香叶酸（2），柠檬醛(3),香叶醇（4），叶酸甲酯（5），nerol（6），和香茅酸（7）），三个倍半萜(法尼醇(8)，法尼醇（9），和乙酸法呢酯（10）），一种二萜（香叶基香叶醇（11）），选择一种三萜（角鲨烯（12））对正常血糖和链脲佐菌素诱导的糖尿病小鼠进行研究。其中,2、3、7、8、9和10在链脲佐菌素诱导的糖尿病小鼠中显示出抗高血糖活性。然后选择它们用于口服蔗糖和乳糖耐受试验(OSTT和OLTT)以及口服葡萄糖耐受试验(OGTT)中的评估。在OSTT和OLTT中,化合物3、7、8、9和10在蔗糖或乳糖负荷后2小时显示餐后葡萄糖峰降低(与阿卡波糖相当)。在OGTT的情况下，图2、7、8、9和10显示葡萄糖负荷后2小时餐后葡萄糖峰的减少(与canagliflozin相当)。我们的结果表明，餐后高血糖的控制可能是通过抑制二糖消化来介导的，如蔗糖和乳糖，和调节葡萄糖的吸收。第一种情况可能与α-葡萄糖苷酶抑制作用有关，第二种情况可能与钠-葡萄糖1型（SGLT-1）协同转运蛋白的抑制作用有关。最后,五种无环萜烯可能是开发和寻找新的α-葡萄糖苷酶和SGLT-1协同转运蛋白抑制剂的候选化合物。
