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Product name: Stevioside
Synonym name: Eupatorin; Rebaudin; Stevin; Steviosin
Catalogue No.: BP1342
Cas No.: 57817-89-7
Formula: C38H60O18
Mol Weight: 804.88
Botanical Source: Stevia rebaudiana (Bertoni) Hemsl.
Physical Description:
Type of Compound: Diterpenoids
Purity: 95%~99%
Analysis Method: HPLC-DAD or/and HPLC-ELSD
Identification Method: Mass, NMR
Packing: Brown vial or HDPE plastic bottle
Storage: Store in a well closed container, protected from air and light. Put into refrigerate or freeze for long term storage.
Whenever possible, you should prepare and use solutions on the same day. However, if you need to make up stock solutions in advance, we recommend that you store the solution as aliquots in tightly sealed vials at -20℃. Generally, these will be useable for up to two weeks.
The product could be supplied from milligrams to grams
Inquire for bulk scale.
Description:
Stevioside is a safe natural sweetener, has no allergic reactions, suited for both diabetics, and PKU patients, as well as for obese persons intending to lose weight by avoiding sugar supplements in the diet. Stevioside enjoys a dual positive effect by acting as an antihyperglycemic and a blood pressure-lowering substance, it may have therapeutic potential in the treatment of type 2 diabetes and the metabolic syndrome.Stevioside exerts anti-inflammatory and anti-apoptotic properties by inhibiting the release of cytokines and the activation of TLR2 and proteins of the NF-κB and MAPK signaling pathways, as well as caspase-3 and Bax.
References:
Int Immunopharmacol. 2014 Sep;22(1):192-9.
Stevioside inhibits inflammation and apoptosis by regulating TLR2 and TLR2-related proteins in S. aureus-infected mouse mammary epithelial cells.
METHODS AND RESULTS:
The object of this study was to investigate the anti-inflammatory and anti-apoptosis function of Stevioside and the possible molecular mechanisms for such activity in Staphylococcus aureus (S. aureus)-infected mouse mammary epithelial cells (MMECs). The cells were treated with varying doses of Stevioside before infection with S. aureus. The live/dead cells were detected by immunofluorescence microscopy. The pro-inflammatory cytokines were determined by ELISA. The mRNA of TLR2 and proteins related to NF-κB, MAPK and apoptosis were analyzed by q-PCR. The relative protein expression levels were determined by Western blot. The results indicated that Stevioside inhibited the mRNA and protein expression of TNF-α, IL-6 and IL-1β dose-dependently in S. aureus-stimulated MMECs. Stevioside suppressed the S. aureus-induced expression of TLR2 and proteins of the NF-κB and MAPK pathways as well as apoptosis. The mRNA levels of IκBα, p38, ERK, JNK, p65, caspase-3 and Bax were not influenced by the Stevioside treatment.
CONCLUSIONS:
Stevioside exerts anti-inflammatory and anti-apoptotic properties by inhibiting the release of cytokines and the activation of TLR2 and proteins of the NF-κB and MAPK signaling pathways, as well as caspase-3 and Bax.
Braz Oral Res. 2014 Jan-Feb;28(1).
Effects of lactose-containing stevioside sweeteners on dental biofilm acidogenicity.
The aim of this study was to evaluate the effect of a commercial lactose-containing Stevioside sweetener on biofilm acidogenicity in vivo.
METHODS AND RESULTS:
Nine volunteers refrained from brushing their teeth for 3 days in five phases. On the 4th day of each phase, the pH of the biofilm was measured by the "Strip method". Interproximal plaque pH was measured before and up to 60 minutes after a 10 mL mouthrinse for 1 minute with the test solutions: I - sweetener with 93% lactose and 7% Stevioside; II - sweetener with 6.8% saccharin, 13.6% cyclamate, and 0.82% Stevioside; III - 18% sucrose solution (positive control); IV - mineral water (negative control); and V- 93% lactose solution. The results revealed that the most pronounced pH fall was found with sucrose (positive control), followed by the 93% lactose solution, the sweetener with lactose + Stevioside, the sweetener with saccharin + cyclamate + Stevioside, and finally water (negative control). According to the area under the curve, the two sweeteners containing Stevioside were significantly different, and the sweetener with lactose + Stevioside was significantly different from water but not from sucrose. The critical pH for dentin demineralization (pH ≤ 6.5) was reached by all volunteers after rinsing with sucrose solution, lactose solution, and the Stevioside+ lactose sweetener.
CONCLUSIONS:
Analysis of the data suggests that lactose-containing Stevioside sweeteners may be cariogenic, especially to dentin.
Metabolism. 2003 Mar;52(3):372-8.
Antihyperglycemic and blood pressure-reducing effects of stevioside in the diabetic Goto-Kakizaki rat.
Stevioside, a glycoside present in the leaves of the plant, Stevia rebaudiana Bertoni (SrB), has acute insulinotropic effects in vitro. Its potential antihyperglycemic and blood pressure-lowering effects were examined in a long-term study in the type 2 diabetic Goto-Kakizaki (GK) rat.
METHODS AND RESULTS:
Rats were fed 0.025 g x kg(-1) x d(-1) of Stevioside (purity > 99.6%) for 6 weeks. An intra-arterial catheter was inserted into the rats after 5 weeks, and conscious rats were subjected to arterial glucose tolerance test (2.0 g x kg(-1)) during week 6. Stevioside had an antihyperglycemic effect (incremental area under the glucose response curve [IAUC]): 985 +/- 20 (Stevioside) versus 1,575 +/- 21 (control) mmol/L x 180 minutes, (P <.05), it enhanced the first-phase insulin response (IAUC: 343 +/- 33 [Stevioside] v 136 +/- 24 [control] microU/mL insulin x 30 minutes, P <.05) and concomitantly suppressed the glucagon levels (total AUC: 2,026 +/- 234 [Stevioside] v 3,535 +/- 282 [control] pg/mL x 180 minutes, P <.05). In addition, Stevioside caused a pronounced suppression of both the systolic (135 +/- 2 v 153 +/- 5 mm Hg; P <.001) and the diastolic blood pressure (74 +/- 1 v 83 +/- 1 mm Hg; P <.001). Bolus injections of Stevioside (0.025 g x kg(-1)) did not induce hypoglycemia. Stevioside augmented the insulin content in the beta-cell line, INS-1. Stevioside may increase the insulin secretion, in part, by induction of genes involved in glycolysis. It may also improve the nutrient-sensing mechanisms, increase cytosolic long-chain fatty acyl-coenzyme A (CoA), and downregulate phosphodiesterase 1 (PDE1) estimated by the microarray gene chip technology.
CONCLUSIONS:
In conclusion, Stevioside enjoys a dual positive effect by acting as an antihyperglycemic and a blood pressure-lowering substance; effects that may have therapeutic potential in the treatment of type 2 diabetes and the metabolic syndrome.
HPLC of Stevioside
HNMR of Stevioside
Storage conditions：Short-term storage at 2~8℃, long-term storage at -20 ~ -80℃
294.9800
-.2684
-.2681
1.5121
.4847
.3162
Low
61.9142
7.1296
No
No
No
No
Yes
No
0.0
Yes
No
No
No
Stevioside is a natural sweetener isolated from the South American plant stevia rebaudiana. Due to its high sweetness and low calorie characteristics, it has attracted widespread attention in the food, pharmaceutical, and health supplement sectors in recent years. As an orally active compound, steviol glycosides not only exhibit a significant sweetening effect but also exhibit various potential pharmacological activities, including lowering blood pressure, lowering blood sugar, antioxidant, anti-inflammatory, and anti-tumor effects, demonstrating their therapeutic potential in chronic metabolic diseases and related pathological conditions. This paper will systematically review the chemical structure and physicochemical properties of steviol glycosides, plant origin and extraction methods, pharmacological activity and mechanism of action, druggability evaluation, and pharmacokinetic characteristics, and will explore in depth the clinical application prospects.
The chemical name of steviol glycoside is (structural formula omitted), molecular formula C₃₈H₆₀O₁₈, molecular weight 804.8800. Its structure belongs to diterpenoid saponins, with a steviol core skeleton connecting multiple glucose residues to form a complex glycoside structure. This polysaccharide structure endows steviol glycosides with high hydrophilicity, showing a low LogP value (-0.2684), water solubility of 1.5121, and a polar surface area (TPSA) as high as 294.98 Ų, indicating strong polarity and good water solubility.
The molecular structure of steviol glycosides contains multiple hydroxyl groups and ether bonds, forming a stable molecular conformation. Its low blood-brain barrier permeability and lack of hERG channel inhibition suggest its high safety. The Ames test result was 0.0, indicating that steviol glycosides pose no significant genotoxic risk, laying a solid safety foundation for its use as a food additive and for drug development.
Stevia glycosides are mainly found in the leaves of stevia, with content varying depending on the variety, growing environment, and harvesting time. Stevia belongs to the Asteraceae family, native to South American countries such as Paraguay and Brazil, and is now widely cultivated in many regions around the world. Steviol glycoside extraction typically involves extracting dried leaves with water or alcohol solvents, combined with modern technologies such as ultrasound-assisted extraction, thermal reflux, or microwave-assisted extraction to improve extraction efficiency.
The extract is filtered, concentrated, and purified by column chromatography to obtain high-purity steviol glycosides. In recent years, the application of supercritical CO₂ extraction and membrane separation technologies has further improved the extraction purity and process economy of steviol glycosides. In addition, research on chemical modifications and biosynthetic pathways based on steviol glycoside structures has provided new ideas and methods for its production.
Research on the pharmacological activity of steviol glycosides covers multiple aspects, mainly focusing on its metabolic regulation and antioxidant and anti-inflammatory effects.
Steviol glycosides have demonstrated significant hypoglycemic effects in diabetes models. It promotes glucose uptake and metabolism by activating the AMPK (5' AMP-activated protein kinase) signaling pathway, improving insulin sensitivity. At the same time, steviol glycosides can inhibit SGLT2 (sodium-glucose cotransporter 2) activity, reduce renal glucose reabsorption, and lower blood sugar levels. In addition, stevia glycosides also regulate glucose kinase (GCK) expression, promote liver glucose metabolism, and collectively improve glucose metabolism disorders.
Steviol glycosides have the effect of dilating blood vessels and lowering blood pressure. Their mechanism involves enhancing nitric oxide (NO) synthesis and inhibiting angiotensin-converting enzyme (ACE) activity, thereby improving vascular function. In addition, steviol glycosides also have blood pressure-lowering effects by regulating the sympathetic nervous system and sodium channels.
Steviol glycosides can significantly eliminate free radicals, enhance antioxidant enzyme activity in the body, and reduce oxidative stress damage. Its anti-inflammatory effect manifests as inhibiting pro-inflammatory cytokines (such as TNF-α, IL-6) and nuclear factor κB (NF-κB) signaling pathways, reducing tissue inflammatory responses and protecting cells from inflammation-mediated damage.
Preliminary studies have shown that steviol glycosides exert certain antitumor activity by inducing tumor cell apoptosis, inhibiting cell proliferation and migration. Its mechanism of action involves regulating cyclins, promoting mitochondrial apoptosis, and inhibiting tumor-related signaling pathways (such as PI3K/Akt).
The multi-target mechanism of steviol glycosides forms the basis for its various pharmacological effects. Through molecular biology and pharmacological research, several key targets have been identified:
The synergistic regulation of these targets forms a multidimensional pharmacological network of steviol glycosides, enhancing their therapeutic potential in metabolic diseases and inflammation-related conditions.
Steviol glycosides have a large molecular weight (804.88 Da) and high polarity (TPSA 294.98 Ų), which limits their oral bioavailability and membrane permeability. Its LogP value was -0.2684, indicating strong hydrophilicity, but low blood-brain barrier permeability, limiting the efficacy of drugs in the central nervous system.
In terms of safety, steviol glycosides do not inhibit hERG channels, and the Ames test is negative, indicating low genotoxicity risk and a solid safety foundation. Moderate water solubility, which is beneficial for formulation design and in vivo distribution.
Pharmacokinetic studies show that after oral administration, steviol glycosides are partially hydrolyzed in the gastrointestinal tract to form steviol alcohol, which can be absorbed and exert biological activity. Steviol glycosides themselves are poorly absorbed, but their metabolites have certain biological activity. The liver is the main metabolic organ, primarily undergoing transformation through glucosidase enzymes. The main excretory routes are bile and urine.
Overall, the druggability of steviol glycosides is limited by their molecular structure and pharmacokinetic properties, but through strategies such as structural modification, nanocarrier encapsulation, and combination therapy, their in vivo kinetic performance is expected to improve and enhance clinical application potential.
As a natural sweetener, steviol glycosides have been widely used in the food industry to replace traditional sugars, offering advantages of low calorie content and low glycemic load. Its pharmacological activity gives it promising prospects as an adjunct therapy for diabetes, hypertension, and metabolic syndrome.
Future clinical research should focus on the following directions:
With advances in molecular biology and medicinal chemistry, structural modification and target optimization of steviol glycosides will further advance their potential as novel natural medicines.
As a natural diterpene glycoside derived from stevia, stevia glycosides show broad application prospects due to their unique sweet flavor and diverse pharmacological activities. Its multi-target mechanism of action in diabetes, hypertension, and inflammation-related diseases provides a rich example for pharmacological research of natural products. Despite challenges in druggability such as high molecular weight and low absorption rates, advances in modern drug design and formulation technology have provided strong support for the clinical translation of steviol glycosides. In the future, through in-depth mechanistic research and clinical validation, steviol glycosides are expected to become a safe and effective natural medicine, contributing new strategies and options for the prevention and treatment of metabolic diseases and related chronic diseases.
Shenshuai
Wenjing
Hedandan
