| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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| 25mg |
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| 50mg |
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| 100mg |
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| Other Sizes |
| Targets |
Human Endogenous Metabolite
Protodioscin targets cancer cells and metabolic pathways. It displays cytotoxicity against various cancer cell lines including leukemia, colon cancer, and prostate cancer (GI50 ≤ 2 µM). It has anti-lipidemic, anti-tumor, and cardiovascular protective effects. It inhibits α-amylase and pancreatic lipase activity. |
|---|---|
| ln Vitro |
In vitro, protodioscin displays cytotoxicity against a range of cancer cells, including leukemia, colon cancer, and prostate cancer cells with GI50 ≤ 2 µM. It is cytotoxic against most cell lines from leukemia and solid tumors in the NCI's human cancer panel, with selective activity against MOLT-4 leukemia cells. It inhibits α-amylase and pancreatic lipase.
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| ln Vivo |
Significant improvements in glucose intolerance are observed with protodioscin (5 and 10 mg/kg), which also lowers serum levels of UA, BUN, Cr, TC, and TG. By suppressing the activation of nuclear factor-κB, c-Jun N-terminal kinase, p38 mitogen-activated protein kinase, extracellular signal-regulated kinase, and p38, protodioscin dramatically lowers renal concentrations of IL-1β, IL-6, and TNF-α[1]. In rats, protodioscin decreases the number of apoptotic nerve cells brought on by MCAO, lowers the death rate, and prevents the rise in neurological impairment scores and infarct volume. Protodioscin reverses the protein expression of NF-κB (in the nucleus and cytoplasm) and IκBα (in the cytoplasm) induced by MCAO in rats, attenuates the alteration of important apoptins, and reduces the release of pro-inflammatory cytokines in serum[2]. Rats fed a high-fat diet have a coagulation time that is approximately 50% longer than that of rats given a protodioscin injection (0.5 mg/kg, ip). Protodioscin shows promise in reducing blood levels of both lipoproteins, particularly LDL, which raises the HDL/LDL ratio[3].
In vivo, protodioscin demonstrates anti-lipidemic, anti-tumor, and cardiovascular protective effects. Significant improvements in glucose intolerance are observed with protodioscin at 5 and 10 mg/kg, which also lowers serum uric acid levels. It has antihyperlipidemic effects. |
| Enzyme Assay |
In vitro cytotoxicity assays for protodioscin involve culturing cancer cell lines (e.g., leukemia, colon cancer, prostate cancer) and treating them with the compound at concentrations ranging from 0.1-100 µM. Cell viability is assessed by SRB or MTT assays after 48-72 hours. GI50 values are determined from dose-response curves. Enzyme inhibition assays for α-amylase and pancreatic lipase are performed using colorimetric substrates.
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| Cell Assay |
For in vitro cell assays, cancer cell lines are cultured in appropriate media and treated with protodioscin at various concentrations. Cell proliferation is measured by SRB or MTT assays. Apoptosis is assessed by flow cytometry. Cell cycle analysis is performed by propidium iodide staining. The compound's effects on signaling pathways are evaluated by Western blot.
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| Animal Protocol |
For in vivo animal studies, protodioscin is typically administered to rodents via oral gavage at doses of 5-10 mg/kg. Glucose tolerance tests are performed to assess effects on glucose metabolism. Serum uric acid and lipid levels are measured. Anti-tumor efficacy is evaluated in xenograft models. Tissue distribution and pharmacokinetic studies are performed by LC-MS/MS.
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| ADME/Pharmacokinetics |
Protodioscin (MW 1049.20) has the molecular formula C51H84O22. It is a steroidal saponin found in fenugreek and Tribulus terrestris. The compound consists of aglycone and glycone moieties. It is stable under recommended storage conditions. It is an endogenous metabolite with anti-lipidemic, anti-tumor, and cardiovascular protective effects.
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| Toxicity/Toxicokinetics |
The compound is for research use only. No specific toxicity data are available. As a natural product, it is expected to have moderate toxicity at high doses. Its cytotoxic activity against cancer cells suggests potential effects on rapidly dividing cells. Standard laboratory safety precautions should be followed.
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| References |
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| Additional Infomation |
Protodioscin is a spirostane glycoside composed of a trisaccharide α-L-rhamnose-(1→4)-[α-L-rhamnose-(1→2)]-β-D-glucose linked via a glycosidic bond to the 3-position of 26-(β-D-glucopyranoyl)-3β,22-dihydroxyfuranost-5-ene. It is found in various plants, including yam, asparagus, and fenugreek. It is a metabolite. It is a steroidal saponin, a trisaccharide derivative, a β-D-glucoside, a pentacyclic triterpenoid, and a cyclic hemiacetal. Functionally, it is associated with diosgenin. It is derived from the hydride of spirostane. Protodioscin has been reported in Dioscorea collettii, Dioscorea deltoidea, and other organisms with relevant data. See also: Fenugreek seeds (partial).
Protodioscin (CAS# 55056-80-9) is the main steroidal saponin in fenugreek with anti-lipidemic, anti-tumor, and cardiovascular protective effects. It has not been approved as a therapeutic drug but is widely used in research on cancer, diabetes, and cardiovascular disease. It displays potent cytotoxicity against various cancer cell lines and is a valuable tool in anticancer drug discovery. |
| Molecular Formula |
C51H84O22
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|---|---|
| Molecular Weight |
1049.20
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| Exact Mass |
1048.545
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| CAS # |
55056-80-9
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| PubChem CID |
441891
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| Appearance |
White to off-white solid powder
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| Density |
1.5±0.1 g/cm3
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| Index of Refraction |
1.632
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| LogP |
3.64
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| Hydrogen Bond Donor Count |
13
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| Hydrogen Bond Acceptor Count |
22
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| Rotatable Bond Count |
14
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| Heavy Atom Count |
73
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| Complexity |
1900
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| Defined Atom Stereocenter Count |
31
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| SMILES |
C[C@H]1[C@H]2[C@H](C[C@@H]3[C@@]2(CC[C@H]4[C@H]3CC=C5[C@@]4(CC[C@@H](C5)O[C@H]6[C@@H]([C@H]([C@@H]([C@H](O6)CO)O[C@H]7[C@@H]([C@@H]([C@H]([C@@H](O7)C)O)O)O)O)O[C@H]8[C@@H]([C@@H]([C@H]([C@@H](O8)C)O)O)O)C)C)O[C@@]1(CC[C@@H](C)CO[C@H]9[C@@H]([C@H]([C@@H]([C@H](O9)CO)O)O)O)O
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| InChi Key |
LVTJOONKWUXEFR-UEZXSUPNSA-N
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| InChi Code |
InChI=1S/C51H84O22/c1-20(19-65-45-39(60)38(59)35(56)30(17-52)69-45)9-14-51(64)21(2)32-29(73-51)16-28-26-8-7-24-15-25(10-12-49(24,5)27(26)11-13-50(28,32)6)68-48-44(72-47-41(62)37(58)34(55)23(4)67-47)42(63)43(31(18-53)70-48)71-46-40(61)36(57)33(54)22(3)66-46/h7,20-23,25-48,52-64H,8-19H2,1-6H3/t20-,21+,22+,23+,25+,26-,27+,28+,29+,30-,31-,32+,33+,34+,35-,36-,37-,38+,39-,40-,41-,42+,43-,44-,45-,46+,47+,48-,49+,50+,51-/m1/s1
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| Chemical Name |
(2S,3R,4R,5R,6S)-2-[(2R,3S,4S,5R,6R)-4-hydroxy-2-(hydroxymethyl)-6-[[(1S,2S,4S,6R,7S,8R,9S,12S,13R,16S)-6-hydroxy-7,9,13-trimethyl-6-[(3R)-3-methyl-4-[(2R,3R,4S,5S,6R)-3,4,5-trihydroxy-6-(hydroxymethyl)oxan-2-yl]oxybutyl]-5-oxapentacyclo[10.8.0.02,9.04,8.013,18]icos-18-en-16-yl]oxy]-5-[(2S,3R,4R,5R,6S)-3,4,5-trihydroxy-6-methyloxan-2-yl]oxyoxan-3-yl]oxy-6-methyloxane-3,4,5-triol
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
H2O: 50 mg/mL (47.66 mM)
DMSO: 50 mg/mL (47.66 mM) |
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (2.38 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.5 mg/mL (2.38 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 2.5 mg/mL (2.38 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 0.9531 mL | 4.7655 mL | 9.5311 mL | |
| 5 mM | 0.1906 mL | 0.9531 mL | 1.9062 mL | |
| 10 mM | 0.0953 mL | 0.4766 mL | 0.9531 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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