| Size | Price | Stock | Qty |
|---|---|---|---|
| 1mg |
|
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| Other Sizes |
| Targets |
alpha-Glucosidase (IC50: 41.7 uM in yeast)
|
|---|---|
| ln Vitro |
In vitro enzyme assays demonstrate that Ganoderlactone D exhibits potent inhibitory activity against yeast alpha-glucosidase with an IC50 value of 41.7 uM. This inhibitory effect is comparable to other known alpha-glucosidase inhibitors from natural sources. The compound's highly oxygenated lanostane structure contributes to its enzyme inhibition profile. No other specific biological activities (e.g., cytotoxicity, anti-inflammatory) have been reported for this compound.
|
| ln Vivo |
No specific in vivo data available for Ganoderlactone D. As an alpha-glucosidase inhibitor, it has potential for postprandial blood glucose reduction in animal models of diabetes. Related compounds from Ganoderma lucidum have demonstrated hypoglycemic effects in streptozotocin-induced diabetic rats. In vivo studies would involve oral administration of the compound (e.g., 10-100 mg/kg) prior to a glucose load and measurement of blood glucose levels at multiple time points (0-120 minutes).
|
| Enzyme Assay |
Recombinant or yeast alpha-glucosidase enzyme is incubated with varying concentrations of Ganoderlactone D (0.1-1000 uM) in phosphate buffer (pH 6.8) at 37degC for 10 minutes. The substrate p-nitrophenyl-alpha-D-glucopyranoside (pNPG, 5 mM) is added to initiate the reaction. After incubation for 20-30 minutes, the reaction is terminated by adding sodium carbonate (Na2CO3, 1 M). The amount of released p-nitrophenol is measured spectrophotometrically at 405 nm. The percentage of enzyme inhibition is calculated relative to control wells without inhibitor. IC50 values are determined by fitting dose-response curves using non-linear regression analysis (IC50 = 41.7 uM).
|
| Cell Assay |
No published cell-based assays for Ganoderlactone D. For intestinal alpha-glucosidase inhibition studies, Caco-2 human intestinal epithelial cells can be used. Cells are cultured in DMEM with 10% FBS and grown to confluence on transwell inserts. Differentiated Caco-2 cells express brush border alpha-glucosidases. Cells are treated with Ganoderlactone D (10-200 uM) for 30-60 minutes, followed by addition of maltose or sucrose as substrate. Glucose produced from disaccharide hydrolysis is measured by glucose oxidase-peroxidase (GOD-POD) colorimetric assay. Inhibition of glucose production indicates alpha-glucosidase inhibitory activity. Cell viability is assessed by MTT assay.
|
| Animal Protocol |
No published in vivo animal study for Ganoderlactone D. Based on its alpha-glucosidase inhibitory activity, a typical in vivo protocol would involve oral administration of Ganoderlactone D (10-100 mg/kg) to ICR mice or Sprague-Dawley rats. The compound is formulated in 0.5% carboxymethylcellulose (CMC-Na) or 10% DMSO in saline. After 30 minutes, sucrose or maltose (2 g/kg) is administered orally. Blood samples are collected from the tail vein at 0, 30, 60, and 120 minutes post-glucose load. Blood glucose levels are measured using a glucometer or glucose assay kit. The area under the curve (AUC) for blood glucose is calculated. Reduction in AUC compared to control indicates in vivo alpha-glucosidase inhibition.
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| ADME/Pharmacokinetics |
No specific pharmacokinetic data for Ganoderlactone D. As a triterpenoid with high molecular weight (474.59) and LogP 1.4, its oral bioavailability may be moderate. Based on related Ganoderma triterpenoids (ganoderic acids), oral absorption is likely but may be limited by poor aqueous solubility. Metabolism would occur in the liver via phase I (oxidation, reduction) and phase II (conjugation) enzymes. Plasma half-life and clearance have not been determined. Solubility: soluble in DMSO (typical solubility ~20-50 mg/mL).
|
| Toxicity/Toxicokinetics |
No specific toxicity data for Ganoderlactone D. Ganoderma lucidum triterpenoids as a class are considered to have low toxicity. In traditional medicine, Ganoderma lucidum has been used for centuries with minimal adverse effects. Acute toxicity studies of related triterpenoids in rodents show LD50 values > 2000 mg/kg. Chronic administration (90 days) at doses up to 500 mg/kg is generally well tolerated. No significant genotoxicity, hepatotoxicity, or nephrotoxicity has been reported. For research use only.
|
| References | |
| Additional Infomation |
Ganoderlactone D is a triterpenoid compound. Ganoderlactone D has been reported in Ganoderma lucidum, and relevant data are available for reference.
Ganoderlactone D (CAS: 1801934-15-5) is a natural product isolated from Ganoderma lucidum, a medicinal mushroom used in traditional Chinese medicine. The compound is a highly oxygenated lanostane-type triterpenoid. It has inhibitory activity against yeast alpha-glucosidase with an IC50 of 41.7 microM. Molecular formula: C27H38O7, molecular weight: 474.59. Appearance: white to off-white solid powder. Solubility: soluble in DMSO. Storage: powder at -20degC for 3 years; in solvent at -80degC for 6 months. Protect from light. The compound has been reported with data available in PubChem (CID: 122184970). Reference: Inhibitory Effects of Highly Oxygenated Lanostane Derivatives from the Fungus Ganoderma lucidum on P-Glycoprotein and alpha-Glucosidase. J Nat Prod. 2015;78(8):1868-1876. Not approved for clinical use. |
| Molecular Formula |
C27H38O7
|
|---|---|
| Molecular Weight |
474.5864
|
| Exact Mass |
474.261
|
| CAS # |
1801934-15-5
|
| PubChem CID |
122184970
|
| Appearance |
White to off-white solid powder
|
| LogP |
1.4
|
| Hydrogen Bond Donor Count |
3
|
| Hydrogen Bond Acceptor Count |
7
|
| Rotatable Bond Count |
1
|
| Heavy Atom Count |
34
|
| Complexity |
1030
|
| Defined Atom Stereocenter Count |
9
|
| SMILES |
O1C(CC[C@]1(C)[C@@]1([H])CC([C@@]2(C)C3[C@H](CC4C(C)(C)[C@H](CC[C@]4(C)C=3C([C@H]([C@@]21C)O)=O)O)O)=O)=O
|
| InChi Key |
OCCKLFZPYIWUFJ-WBLDVHJPSA-N
|
| InChi Code |
InChI=1S/C27H38O7/c1-23(2)14-11-13(28)19-20(24(14,3)9-7-16(23)29)21(32)22(33)26(5)15(12-17(30)27(19,26)6)25(4)10-8-18(31)34-25/h13-16,22,28-29,33H,7-12H2,1-6H3/t13-,14-,15+,16-,22+,24-,25-,26-,27-/m0/s1
|
| Chemical Name |
(3S,5R,7S,10S,12S,13R,14R,17S)-3,7,12-trihydroxy-4,4,10,13,14-pentamethyl-17-[(2S)-2-methyl-5-oxooxolan-2-yl]-2,3,5,6,7,12,16,17-octahydro-1H-cyclopenta[a]phenanthrene-11,15-dione
|
| HS Tariff Code |
2934.99.9001
|
| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month Note: This product requires protection from light (avoid light exposure) during transportation and storage. |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
|
| Solubility (In Vitro) |
May dissolve in DMSO (in most cases), if not, try other solvents such as H2O, Ethanol, or DMF with a minute amount of products to avoid loss of samples
|
|---|---|
| Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400 (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.1071 mL | 10.5354 mL | 21.0708 mL | |
| 5 mM | 0.4214 mL | 2.1071 mL | 4.2142 mL | |
| 10 mM | 0.2107 mL | 1.0535 mL | 2.1071 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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