Department of Molecular Sciences, Swedish University of Agricultural Sciences, P. O. Box 7015, SE-750 07, Uppsala, Sweden.
Department of Molecular Medicine and Surgery, Endocrine and Diabetes Unit, Karolinska Institutet, Karolinska University Hospital, SE-171 76, Stockholm, Sweden.
Sci Rep. 2019 Jan 24;9(1):627. doi: 10.1038/s41598-018-37517-3.
The global prevalence of type 2 diabetes is increasing rapidly; consequently there is great need for new and novel therapeutic options. Gynostemma pentaphyllum (GP) is a traditional medicinal plant, mainly present in Southeast Asian countries, that has been reported to exert antidiabetic effects, by stimulating insulin secretion. The specific compound responsible for this effect is however as yet unidentified. Screening for discovery and identification of bioactive compounds of an herbal GP extract, was performed in isolated pancreatic islets from spontaneously diabetic Goto-Kakizaki (GK) rats, a model of type 2 diabetes, and from non-diabetic control Wistar rats. From this herbal extract 27 dammarane-type saponins, including two novel compounds, were isolated and their structure was elucidated by mass spectrometry and NMR spectroscopy. One of the dammarane-type triterpenoid showed a glucose-dependent insulin secretion activity. This compound, gylongiposide I, displays unique abilities to stimulate insulin release at high glucose levels (16.7 mM), but limited effects at a low glucose concentration (3.3 mM). Further studies on this compound, also in vivo, are warranted with the aim of developing a novel anti-diabetic therapeutic with glucose-dependent insulinogenic effect.
全球 2 型糖尿病的患病率正在迅速上升；因此，非常需要新的和新颖的治疗选择。绞股蓝（GP）是一种传统的药用植物，主要存在于东南亚国家，据报道具有抗糖尿病作用，通过刺激胰岛素分泌。然而，负责这种作用的特定化合物尚未确定。从自发性糖尿病 Goto-Kakizaki（GK）大鼠（2 型糖尿病模型）和非糖尿病对照 Wistar 大鼠的分离胰岛中，对绞股蓝提取物的生物活性化合物的发现和鉴定进行了筛选。从这种草药提取物中分离出 27 种达玛烷型皂苷，包括两种新化合物，并通过质谱和 NMR 光谱阐明了它们的结构。一种达玛烷型三萜显示出葡萄糖依赖性胰岛素分泌活性。这种化合物，绞股蓝苷 I，在高葡萄糖水平（16.7 mM）下具有独特的刺激胰岛素释放的能力，但在低葡萄糖浓度（3.3 mM）下作用有限。还需要对该化合物进行进一步的体内研究，目的是开发一种具有葡萄糖依赖性胰岛素生成作用的新型抗糖尿病治疗药物。
