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| 5mg |
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| Other Sizes |
| Targets |
Tumulosic acid inhibits DNA topoisomerase I and II. It also inhibits KLK5 (kallikrein 5) protease activity. It shows IC₅₀ values of 14.84 µM against KLK5 and 10.48 µM against trypsin proteases, while exhibiting weak inhibitory effects on KLK7 and chymotrypsin C (19.5% and 4.0%, respectively, at 100 µM). It also modulates immune responses and inhibits tumor cell proliferation.
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| ln Vitro |
Tumulosic acid exhibits anti-KLK5 activity that is dose-dependent (IC50=19.3 μM)[1]. Human keratinocytes produce less LL-37 when treated with tumorinosic acid[1]. Tumulosic acid demonstrated a weak inhibitory effect on KLK7 and chymotrypsin C proteases (19.5% and 4.0%, respectively, at 100 μM), but it demonstrated IC50 values of 14.84 and 10.48 μM against KLK5 and trypsin proteases[1].
Tumulosic acid displays dose-dependent anti-KLK5 activity (IC₅₀ = 19.3 µM). It decreases LL-37 production in human keratinocytes. It inhibits DNA topoisomerase I and II by 83.3% and 75.5%, respectively, when used at a concentration of 100 µM. It also inhibits trypsin protease with an IC₅₀ of 10.48 µM. |
| ln Vivo |
Tumulosic acid has been shown to modulate immune responses, inhibit tumor cell proliferation, and protect liver function. Its mechanism involves regulation of signaling pathways related to inflammation and oxidative stress. As a triterpenoid from Poria cocos, it may contribute to the pharmacological effects of this medicinal fungus. Further in vivo studies are needed to fully characterize its therapeutic potential.
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| Enzyme Assay |
Non-cell-based assays for tumulosic acid include DNA topoisomerase inhibition assays using purified topoisomerase I and II enzymes. The enzyme is incubated with DNA substrate in the presence of various concentrations of the compound, and topoisomerase activity is measured by detecting DNA relaxation or supercoiling. KLK5 protease inhibition assays use purified KLK5 enzyme and fluorogenic peptide substrates. The IC₅₀ values are determined from dose-response curves.
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| Cell Assay |
Western Blot Analysis[1]
Cell Types: Normal human epidermal keratinocytes (NHEKs) Tested Concentrations: 1 μM and 10 μM Incubation Duration: 23 h in the presence of 10 μM cycloheximide Experimental Results: diminished LL-37 production in epidermal keratinocytes. Cell-based assays for tumulosic acid use normal human epidermal keratinocytes (NHEKs) to assess effects on LL-37 production. Cells are treated with the compound at 1 µM and 10 µM for 23 hours in the presence of 10 µM cycloheximide. Decreased LL-37 production is measured. For anti-tumor studies, cancer cell lines can be used to assess inhibition of proliferation. Cytotoxicity is assessed using standard cell viability assays. |
| Animal Protocol |
In vivo studies of tumulosic acid are limited. As a triterpenoid with anti-inflammatory, immunomodulatory, and anti-tumor activities, it has potential for evaluation in animal models of inflammation, cancer, and liver disease. Standard protocols for these models involve administration of the compound followed by measurement of relevant endpoints. Further studies are needed to characterize its in vivo efficacy and safety.
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| ADME/Pharmacokinetics |
Tumulosic acid has a molecular formula of C₃₁H₅₀O₄ and a molecular weight of 486.73 g/mol. It is soluble in DMSO (25 mg/mL, 51.36 mM) with ultrasonic warming to 60°C. Storage: 4°C, protect from light; in solvent: -80°C for 6 months, -20°C for 1 month. Purity is ≥98%. It appears as a white to off-white solid powder.
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| Toxicity/Toxicokinetics |
Tumulosic acid is a triterpenoid that inhibits KLK5 protease activity (IC₅₀ = 14.84 µM) and suppresses the proteolytic processing of LL-37 in keratinocytes at ≤10 µM. It also inhibits DNA topoisomerase I and II. It has been shown to modulate immune responses, inhibit tumor cell proliferation, and protect liver function. Standard laboratory safety practices should be followed when handling this compound.
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| References | |
| Additional Infomation |
Tumulosic is a triterpenoid compound. It has been reported in Daedalea dickinsii, Rhodofomitopsis lilacinogilva, and other organisms with available data.
Tumulosic acid is a triterpenoid found in Poria cocos with diverse biological activities. It inhibits DNA topoisomerase I and II (83.3% and 75.5% at 100 µM) and KLK5 protease activity (IC₅₀ = 14.84 µM). It decreases LL-37 production in human keratinocytes. It has been shown to modulate immune responses, inhibit tumor cell proliferation, and protect liver function. Its mechanism involves regulation of signaling pathways related to inflammation and oxidative stress. It is for research use only. |
| Molecular Formula |
C31H50O4
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|---|---|
| Molecular Weight |
486.73
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| Exact Mass |
486.371
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| Elemental Analysis |
C, 76.50; H, 10.35; O, 13.15
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| CAS # |
508-24-7
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| PubChem CID |
12314446
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| Appearance |
White to off-white solid powder
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| LogP |
6.76
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| Hydrogen Bond Donor Count |
3
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| Hydrogen Bond Acceptor Count |
4
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| Rotatable Bond Count |
6
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| Heavy Atom Count |
35
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| Complexity |
915
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| Defined Atom Stereocenter Count |
8
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| SMILES |
CC(C)C(=C)CCC(C1C(CC2(C1(CCC3=C2CCC4C3(CCC(C4(C)C)O)C)C)C)O)C(=O)O
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| InChi Key |
XADJANKGURNTIA-YEXRKOARSA-N
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| InChi Code |
InChI=1S/C31H50O4/c1-18(2)19(3)9-10-20(27(34)35)26-23(32)17-31(8)22-11-12-24-28(4,5)25(33)14-15-29(24,6)21(22)13-16-30(26,31)7/h18,20,23-26,32-33H,3,9-17H2,1-2,4-8H3,(H,34,35)/t20-,23-,24+,25+,26+,29-,30-,31+/m1/s1
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| Chemical Name |
(2R)-2-[(3S,5R,10S,13R,14R,16R,17R)-3,16-dihydroxy-4,4,10,13,14-pentamethyl-2,3,5,6,7,11,12,15,16,17-decahydro-1H-cyclopenta[a]phenanthren-17-yl]-6-methyl-5-methylideneheptanoic acid
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| Synonyms |
Polyporenic Acid B; Tumulosic Acid
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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 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)
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| 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
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| 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 | 2.0545 mL | 10.2726 mL | 20.5453 mL | |
| 5 mM | 0.4109 mL | 2.0545 mL | 4.1091 mL | |
| 10 mM | 0.2055 mL | 1.0273 mL | 2.0545 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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