| Size | Price | Stock | Qty |
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| 1mg |
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| 5mg |
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| 10mg |
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| 50mg |
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| 100mg |
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| Targets |
α-Terpineol targets multiple pathways and cellular processes. It exhibits antimicrobial activity against periodontopathic and cariogenic bacteria, as well as antifungal activity against Trichophyton mentagrophytes. The compound inhibits the gene expression of the IL-6 receptor, contributing to its anti-inflammatory effects. It also inhibits NF-κB activation, which is a key mechanism underlying its anti-inflammatory activity. α-Terpineol shows anticonvulsant activity and induces cell death in tumor cells via inhibition of NF-κB.
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| ln Vitro |
Physalis angulate L is the source of Physalisin F, an open-chain steroid. [1].
In vitro, α-Terpineol demonstrates potent antimicrobial activity against Gardnerella vaginalis and Candida albicans with MIC values of 0.06% and 0.125% (v/v), respectively, comparable to that of clotrimazole. It also exhibits strong antimicrobial activity against periodontopathic and cariogenic bacteria and antifungal activity against T. mentagrophytes. The combination of α-terpineol and nerolidol demonstrates potent antimicrobial activity and markedly inhibits biofilm development, particularly against Gram-positive bacterial strains. Anti-inflammatory effects are demonstrated by inhibiting the expression of pro-inflammatory cytokines such as TNF-α and IL-6. |
| ln Vivo |
In vivo, α-Terpineol has been evaluated in mouse models of bacterial vaginosis and vulvovaginal candidiasis. Intravaginal treatment with α-terpineol-containing formulations ameliorates these infections by inhibiting bacterial growth and NF-κB activation. The compound's antimicrobial activity in vivo is comparable to that of clotrimazole. These studies support the potential of α-terpineol as a therapeutic agent for vaginal infections and other infectious diseases. Anticancer and anti-inflammatory activities have also been suggested in animal models.
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| Enzyme Assay |
The antimicrobial activity is assessed using broth microdilution or agar diffusion methods following CLSI guidelines. Bacterial and fungal strains are cultured in appropriate media and incubated with serial dilutions of α-Terpineol. MIC is defined as the lowest concentration that inhibits visible growth. For biofilm inhibition assays, biofilms are grown in 96-well plates, treated with the compound, and stained with crystal violet, with absorbance measured at 595 nm. Anti-inflammatory activity is assessed by measuring cytokine levels (TNF-α, IL-6) via ELISA in stimulated immune cells.
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| Cell Assay |
Cells such as macrophages, monocytes, or epithelial cells are cultured in appropriate media. Cells are pre-treated with α-Terpineol at various concentrations, then stimulated with LPS or other inflammatory stimuli. Cytokine levels in supernatants are measured by ELISA. For antimicrobial testing, pathogens are cultured in broth media and incubated with the compound. Biofilm formation is assessed in 96-well plates using crystal violet staining. Anticancer activity is evaluated using cancer cell lines with MTT or similar viability assays.
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| Animal Protocol |
In vivo efficacy is evaluated in mouse models of vaginal infection. Mice are infected intravaginally with G. vaginalis or C. albicans, then treated with α-Terpineol-containing formulations intravaginally. Treatment efficacy is assessed by measuring pathogen load via colony counting, evaluating clinical signs of infection, and histopathological examination of vaginal tissues. NF-κB activation in tissues may be assessed by immunohistochemistry or Western blot. For anticancer studies, xenograft models would be employed, although specific protocols are not detailed in the available literature.
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| ADME/Pharmacokinetics |
Specific pharmacokinetic data for α-Terpineol are not extensively reported in the pharmacological literature. As a small monoterpene alcohol (MW 154.25), the compound is expected to be well-absorbed orally and to distribute widely due to its lipophilicity. Its volatility may result in rapid elimination via exhalation. In vivo studies in mice demonstrate efficacy following intravaginal administration, confirming local bioavailability. Formal PK studies would be required to determine systemic exposure parameters such as half-life, Cmax, and bioavailability after various routes of administration.
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| Toxicity/Toxicokinetics |
Toxicological data for α-Terpineol are limited in the pharmacological literature. As a natural product used in flavors and fragrances, it is generally considered to have low toxicity at typical exposure levels. However, comprehensive toxicology studies for systemic therapeutic use have not been reported. The compound's safety profile would need to be established through standard toxicological evaluations including acute, subchronic, and genotoxicity studies before any clinical development.
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| References | |
| Additional Infomation |
It has been reported that (1R,2R,4R,6S,11R,12S,15R,18S,19R,20S,21S,23R,26S)-15-hydroxy-11,18,21-trimethyl-5,17,24,28,29-pentaheterocyclic[17.9.1.11,20.02,12.04,6.06,11.015,19.018,23.021,26]tridecane-8-ene-10,16,25,30-tetraone is found in Physalis lagascae, Physalis angulata, and other organisms with available data.
α-Terpineol is a natural monoterpene alcohol with broad-spectrum antimicrobial activity (MIC 0.06% for G. vaginalis, 0.125% for C. albicans), anti-inflammatory effects via NF-κB inhibition, and anticancer properties. It inhibits biofilm formation and shows efficacy in mouse models of vaginal infection. No clinical trials or approvals exist. For research use only. |
| Molecular Formula |
C28H30O10
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|---|---|
| Molecular Weight |
526.5318
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| Exact Mass |
526.184
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| CAS # |
57423-71-9
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| PubChem CID |
44577488
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| Appearance |
White to off-white solid powder
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| LogP |
0.768
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| Hydrogen Bond Donor Count |
1
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| Hydrogen Bond Acceptor Count |
10
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| Rotatable Bond Count |
0
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| Heavy Atom Count |
38
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| Complexity |
1340
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| Defined Atom Stereocenter Count |
13
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| SMILES |
C[C@]12C[C@@H]3[C@]4([C@]56[C@H]1C(=O)[C@](O5)([C@@H]7C[C@@H]8[C@]9(O8)CC=CC(=O)[C@@]9([C@H]7CC[C@@]6(C(=O)O4)O)C)OC[C@H]2C(=O)O3)C
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| InChi Key |
VSLWNSSUMFSGFF-IFSNGKJOSA-N
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| InChi Code |
InChI=1S/C28H30O10/c1-22-10-17-24(3)28-18(22)19(30)27(38-28,34-11-14(22)20(31)35-17)13-9-16-26(36-16)7-4-5-15(29)23(26,2)12(13)6-8-25(28,33)21(32)37-24/h4-5,12-14,16-18,33H,6-11H2,1-3H3/t12-,13+,14-,16+,17+,18-,22+,23-,24-,25-,26+,27+,28-/m0/s1
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| Chemical Name |
(1R,2R,4R,6S,11R,12S,15R,18S,19R,20S,21S,23R,26S)-15-hydroxy-11,18,21-trimethyl-5,17,24,28,29-pentaoxanonacyclo[17.9.1.11,20.02,12.04,6.06,11.015,19.018,23.021,26]triacont-8-ene-10,16,25,30-tetrone
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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: Please store this product in a sealed and protected environment (e.g. under nitrogen), avoid exposure to moisture and light. |
| 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 | 1.8992 mL | 9.4961 mL | 18.9923 mL | |
| 5 mM | 0.3798 mL | 1.8992 mL | 3.7985 mL | |
| 10 mM | 0.1899 mL | 0.9496 mL | 1.8992 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.
| NCT Number | Recruitment | interventions | Conditions | Sponsor/Collaborators | Start Date | Phases |
| NCT05803031 | Completed | Drug: Melaleuca Alternifolia Oil Procedure: Non-surgical periodontal debridement |
Periodontal Pocket | Ain Shams University | November 1, 2022 | Not Applicable |
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