Rebaudioside A, from leaves of Stevia rebaudiana, inhibits α-glucosidase activity with IC50=35.01μg/ml[1]. Rebaudioside A has been used in studies related to hypertension treatment, diabetes management, and dental caries prevention[2].
In vitro, Rebaudioside A pretreatment at 1mM for 2h can significantly stimulate the release of glucagon-like peptide 1 (GLP-1) from STC-1 cells[3]. Treatment with 5.0μM Rebaudioside A for 24 hours significantly increased the expression of CYP3A29 mRNA in IPEC-J2 cells[4]. Rebaudioside A (10−6mol/L) incubation for 60 minutes significantly increased insulin secretion in isolated mouse pancreatic islets stimulated by glucose at 16.7mM[5].
In vivo, Rebaudioside A (20mg/kg/day; administered twice daily; i.p.) treatment for 8 weeks can prevent liver damage caused by the administration of thioacetamide (200mg/kg; administered three times weekly, i.p.), and maintain collagen content in Wistar rats[6]. Oral administration of Rebaudioside A and Honokiol micelles (100mg/kg/day) for 15 consecutive days can inhibit tumor growth in the H22 solid tumor model of mice, without affecting the body weight of the mice[7].
References:
[1] Adari B R, Alavala S, George S A, et al. Synthesis of rebaudioside-A by enzymatic transglycosylation of stevioside present in the leaves of Stevia rebaudiana Bertoni[J]. Food chemistry, 2016, 200: 154-158.
[2] Wang Y, Luo X, Chen L, et al. Natural and low‐caloric rebaudioside A as a substitute for dietary sugars: A comprehensive review[J]. Comprehensive Reviews in Food Science and Food Safety, 2023, 22(1): 615-642.
[3] Noya-Leal F, van der Wielen N, Behrens M, et al. Rebaudioside A from Stevia rebaudiana stimulates GLP-1 release by enteroendocrine cells via bitter taste signalling pathways[J]. Food & Function, 2023, 14(15): 6914-6928.
[4] Thøgersen R, Petrat-Melin B, Zamaratskaia G, et al. In vitro effects of rebaudioside A, stevioside and steviol on porcine cytochrome p450 expression and activity[J]. Food Chemistry, 2018, 258: 245-253.
[5] Abudula R, Jeppesen P B, Rolfsen S E D, et al. Rebaudioside A potently stimulates insulin secretion from isolated mouse islets: studies on the dose-, glucose-, and calcium-dependency[J]. Metabolism, 2004, 53(10): 1378-1381.
[6] Casas‐Grajales S, Reyes‐Gordillo K, Cerda‐García‐Rojas C M, et al. Rebaudioside A administration prevents experimental liver fibrosis: An in vivo and in vitro study of the mechanisms of action involved[J]. Journal of Applied Toxicology, 2019, 39(8): 1118-1131.
[7] Wang J, Yang H, Li Q, et al. Novel nanomicelles based on rebaudioside A: a potential nanoplatform for oral delivery of honokiol with enhanced oral bioavailability and antitumor activity[J]. International journal of pharmaceutics, 2020, 590: 119899.
Rebaudioside A(从甜叶菊叶片中提取)可抑制α-葡萄糖苷酶活性,IC50值为35.01μg/ml[1]。Rebaudioside A已被应用于高血压治疗、糖尿病调控及龋齿防治等研究领域[2]。
在体外,1mM浓度的Rebaudioside A预处理STC-1细胞2小时,可显著促进胰高血糖素样肽-1(GLP-1)的释放[3]。5.0μM浓度的Rebaudioside A处理IPEC-J2细胞24小时,能显著提升CYP3A29 mRNA表达水平[4]。10−6mol/L浓度的Rebaudioside A孵育60分钟,可显著增强由16.7mM葡萄糖刺激的离体小鼠胰岛的胰岛素分泌[5]。
在体内,Rebaudioside A(20mg/kg/day,每日两次腹腔注射)持续处理8周,可预防硫代乙酰胺(200mg/kg,每周三次腹腔注射)诱导的Wistar大鼠肝损伤并维持胶原蛋白含量[6]。连续15天口服Rebaudioside A与和Honokiol胶束(100mg/kg/day),能抑制H22实体瘤小鼠模型的肿瘤生长,且不影响小鼠体重[7]。
















