Steviol
Steviol, a natural sweetener, it inhibits proliferation of the gastrointestinal cancer cells intensively. Steviol can treat polycystic kidney disease, it slowed cyst growth, in part, by reducing AQP2 transcription, promoted proteasome, and lysosome-mediated AQP2 degradation. Steviol can induce a significant increase in CYP3A29 expression.
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Providing storage is as stated on the product vial and the vial is kept tightly sealed, the product can be stored for up to
24 months(2-8C).
Wherever 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 -20C. Generally, these will be useable for up to two weeks. Before use, and prior to opening the vial we recommend that you allow your product to equilibrate to room temperature for at least 1 hour.
Need more advice on solubility, usage and handling? Please email to: service@chemfaces.com
The packaging of the product may have turned upside down during transportation, resulting in the natural compounds adhering to the neck or cap of the vial. take the vial out of its packaging and gently shake to let the compounds fall to the bottom of the vial. for liquid products, centrifuge at 200-500 RPM to gather the liquid at the bottom of the vial. try to avoid loss or contamination during handling.
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Oncotarget. 2018 May 29;9(41):26299-26308.
Steviol, a natural product inhibits proliferation of the gastrointestinal cancer cells intensively.[Pubmed:
29899860 ]
New anticancer agents with lower toxicity have been always urged because of drug resistance associated with overused chemotherapy agents.
METHODS AND RESULTS:
In this study, Steviol, a colonic metabolite of natural sweetener and also a component in leaves of stevia rebaudiana bertoni, was found to possess intensive anticancer activity on the human gastrointestinal cancer cells. Steviol inhibited six human gastrointestinal cancer cells intensively as 5-fluorouracil did at 100 μg/mL. The inhibition mechanism follows mitochondrial apoptotic pathway that was evidenced by increase of Bax/Bcl-2 ratio, activation of p21 and p53; and caspase 3-independent mechanism was also involved.
These results are consistent with the miRNA expression analysis.
The most regulated miRNAs in the Steviol treated gastrointestinal cancer cells were miR-203a-3p (log2 =1.32) and miR-6088 (log2 =-2.54) in HCT-116, miR-1268b (log2 =19.85) and miR-23c (log2 =-2.05) in MKN-45.
CONCLUSIONS:
In view of the metabolic characteristics of Steviol and its cytotoxicity on the cancer cells, Steviol could be a chemotherapy agent potentially for cancer treatment.
Food Chem. 2018 Aug 30;258:245-253.
In vitro effects of rebaudioside A, stevioside and steviol on porcine cytochrome p450 expression and activity.[Pubmed:
29655729 ]
The physiological effects of the Stevia-derived compounds, rebaudioside A, stevioside and Steviol have been the focus of several studies due to their use as sweeteners in food. Despite that, little is known about their potential food-drug interactions.
METHODS AND RESULTS:
In the present study, IPEC-J2 cells and primary hepatocytes were used to investigate the effect of rebaudioside A, stevioside and Steviol on cytochrome p450 (CYP) mRNA expression. Moreover, hepatic microsomes were used to investigate direct interactions between the compounds and specific CYP activity. In IPEC-J2 no changes in mRNA expression of CYP1A1 or CYP3A29 were observed with the Stevia-derived compounds. In primary hepatocytes all three tested compounds induced a significant increase in CYP3A29 expression. The tested compounds had no direct effect on specific CYP activity.
CONCLUSIONS:
In conclusion, rebaudioside A, stevioside and Steviol induce only minor or no changes to the CYP expression and activity, and are not likely to cause food-drug interactions.
Biomed Pharmacother. 2018 May;101:754-762.
Steviol slows renal cyst growth by reducing AQP2 expression and promoting AQP2 degradation.[Pubmed:
29524884 ]
Overexpression of aquaporin 2 (AQP2) was observed and suggested to be involved in fluid secretion leading to cyst enlargement in polycystic kidney disease (PKD). The cyst expansion deteriorates the renal function and, therefore, therapies targeting cyst enlargement are of clinical interest. Of note, inhibition of vasopressin function using vasopressin 2 receptor (V2R) antagonist which decreased cAMP production along with AQP2 production and function can slow cyst growth in ADPKD. This finding supports the role of AQP2 in cyst enlargement. Steviol, a major metabolite of the sweetening compound stevioside, was reported to retard MDCK cyst growth and enlargement by inhibiting CFTR activity. Interestingly, its efficacy was found to be higher than that of CFTRinh-172. Since Steviol was also found to produce diuresis in rodent, it is likely that Steviol might have an additional effect in retarding cyst progression, such as inhibition of AQP2 expression and function.
METHODS AND RESULTS:
Here, we investigated the effect of Steviol on AQP2 function and on cyst growth using an in vitro cyst model (MDCK and Pkd1-/- cells). We found that Steviol could markedly inhibit cyst growth by reducing AQP2 expression in both Pkd1-/- and MDCK cells. Real-time PCR also revealed that Steviol decreased AQP2 mRNA expression level as well. Moreover, a proteasome inhibitor, MG-132, and the lysosomotropic agent, hydroxychloroquine (HCQ) were found to abolish the inhibitory effect of Steviol in Pkd1-/- cells. Increased lysosomal enzyme marker (LAMP2) expression following Steviol treatment clearly confirmed the involvement of lysosomes in Steviol action.
CONCLUSIONS:
In conclusion, our finding showed for the first time that Steviol slowed cyst growth, in part, by reducing AQP2 transcription, promoted proteasome, and lysosome-mediated AQP2 degradation. Due to its multiple actions, Steviol is a promising compound for further development in the treatment of PKD.
Oncol Lett. 2018 Apr;15(4):5250-5256.
The natural sweetener metabolite steviol inhibits the proliferation of human osteosarcoma U2OS cell line.[Pubmed:
29552164]
Steviol is the colonic metabolite of the natural sweetener Steviol glycosides. It does not diffuse to the blood and the half maximal inhibitory concentration of Steviol is longer compared with that of current chemotherapy agents, including 5-fluorouracil and doxorubicin.
METHODS AND RESULTS:
The present study demonstrated that Steviol inhibits the proliferation of the human osteosarcoma U2OS cell line in a dose- and time-dependent manner, and that the inhibition rate is comparative with that of doxorubicin and 5-fluorouracil. The mechanism of this anticancer activity is also investigated. The results indicated that Steviol inhibits U2OS cells through inducing G1 phase cell cycle arrest, downregulating the ability of colony formation via a mitochondrial apoptotic pathway, which was indicated by an increase of the Bax/Bcl-2 ratio and activation of cyclin-dependent kinase inhibitor 1, tumor protein 53 and cyclin-dependent kinase; whereas a Survivin and Caspase 3-independent mechanism was involved.
CONCLUSIONS:
Considering that Steviol appears minimally in the plasma during metabolism, and possesses a median lethal dose of 100-fold greater compared with that of 5-fluorouracil, it may become a potential chemotherapy agent.
