| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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| 25mg |
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| Targets |
PI3K, Akt, mTOR [1]
Bcl-2, Bax, caspase-3 [1] |
|---|---|
| ln Vitro |
- Arnicolide D exhibited potent anti-proliferative activity against human nasopharyngeal carcinoma (NPC) cell lines (CNE1, CNE2, HONE1, HK1) in a dose- and time-dependent manner (MTT assay). The IC50 values at 48 h were 12.3 ± 1.5 μM (CNE1), 10.7 ± 1.2 μM (CNE2), 13.5 ± 1.8 μM (HONE1), and 11.9 ± 1.4 μM (HK1) [1]
- Arnicolide D (10, 20, 40 μM) significantly inhibited colony formation of CNE1 and CNE2 cells (colony formation assay), with colony numbers reduced by ~40% (10 μM), ~65% (20 μM), and ~85% (40 μM) compared with the control group [1] - Arnicolide D (10, 20, 40 μM) suppressed the migration and invasion of CNE1 and CNE2 cells (Transwell and wound-healing assays). The migration rate and invasive cell number were reduced by ~30-70% in a dose-dependent manner [1] - Arnicolide D (10, 20, 40 μM) induced apoptosis in CNE1 and CNE2 cells (Annexin V-FITC/PI staining): the apoptotic rate increased from ~5% (control) to ~25% (20 μM) and ~45% (40 μM) [1] - Western blot analysis showed that Arnicolide D (10, 20, 40 μM) downregulated the phosphorylation of PI3K, Akt, and mTOR, and decreased the expression of anti-apoptotic protein Bcl-2. It upregulated pro-apoptotic protein Bax and cleaved caspase-3, -9 (detected by Western blot). qPCR confirmed downregulated Bcl-2 mRNA and upregulated Bax mRNA expression [1] - Arnicolide D had low cytotoxicity to normal human nasopharyngeal epithelial cells (NP69) with an IC50 > 50 μM (MTT assay) [1] |
| ln Vivo |
- In nude mice bearing CNE2 cell-derived xenografts, intraperitoneal injection of Arnicolide D (20, 40 mg/kg/3 days) for 4 weeks significantly inhibited tumor growth. The tumor volume and weight were reduced by ~45% (20 mg/kg) and ~68% (40 mg/kg) compared with the vehicle group [1]
- Histopathological analysis of xenograft tumors showed that Arnicolide D (20, 40 mg/kg) increased the number of apoptotic cells (TUNEL assay) and reduced Ki-67-positive proliferating cells (immunohistochemistry) [1] - Western blot analysis of xenograft tissues confirmed that Arnicolide D (40 mg/kg) downregulated p-PI3K, p-Akt, p-mTOR, and Bcl-2 protein expression, and upregulated Bax and cleaved caspase-3 expression [1] |
| Cell Assay |
- Anti-proliferation assay: NPC cells (CNE1, CNE2, HONE1, HK1) and NP69 cells were seeded in 96-well plates, treated with Arnicolide D (0-50 μM) for 24, 48, 72 h. MTT reagent was added, and absorbance at 570 nm was measured to calculate IC50 values [1]
- Colony formation assay: CNE1 and CNE2 cells were seeded in 6-well plates, treated with Arnicolide D (10, 20, 40 μM) for 24 h, then cultured in drug-free medium for 14 days. Colonies were stained and counted [1] - Migration and invasion assays: For wound-healing assay, CNE1/CNE2 cells were scratched and treated with Arnicolide D (10, 20, 40 μM) for 24 h; migration rate was calculated by measuring scratch closure. For Transwell assay, cells were seeded in the upper chamber with Arnicolide D, and invasive cells in the lower chamber were stained and counted after 24 h [1] - Apoptosis assay: CNE1/CNE2 cells were treated with Arnicolide D (10, 20, 40 μM) for 48 h, stained with Annexin V-FITC/PI, and apoptotic rate was detected by flow cytometry [1] - Western blot and qPCR: CNE1/CNE2 cells were treated with Arnicolide D (10, 20, 40 μM) for 48 h. Proteins were extracted for Western blot (probes: p-PI3K, PI3K, p-Akt, Akt, p-mTOR, mTOR, Bcl-2, Bax, cleaved caspase-3/-9, β-actin). Total RNA was extracted for qPCR (primers for Bcl-2, Bax, GAPDH as internal control) [1] |
| Animal Protocol |
- Xenograft model: BALB/c nude mice (4-6 weeks old) were subcutaneously injected with CNE2 cells (5×10⁶ cells/mouse) into the right flank. When tumors reached ~100 mm³, mice were randomly divided into vehicle group and Arnicolide D treatment groups (20, 40 mg/kg, n=6 per group) [1]
- Arnicolide D was dissolved in DMSO and diluted with normal saline (final DMSO concentration ≤ 0.5%). The treatment groups received intraperitoneal injection every 3 days for 4 weeks; the vehicle group received equal volume of vehicle [1] - Tumor volume was measured every 3 days (volume = length × width² / 2). At the end of treatment, mice were sacrificed, tumors were weighed. Tumor tissues were collected for TUNEL assay, immunohistochemistry (Ki-67), and Western blot analysis [1] |
| Toxicity/Toxicokinetics |
In in vivo xenograft experiments, intraperitoneal injection of Arnicolide D (20, 40 mg/kg) did not cause significant changes in mouse body weight, food intake, or serum ALT, AST, Cr, and BUN levels, indicating that it had no obvious hepatotoxicity or nephrotoxicity [1]. In in vitro experiments, Arnicolide D showed low cytotoxicity to normal NP69 cells (IC50 > 50 μM) and a high therapeutic index against nasopharyngeal carcinoma cells [1].
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| References | |
| Additional Infomation |
Anicoside D is a sesquiterpene lactone.
It has been reported that anicoside D exists in Arnica acaulis, Arnica montana and Centipeda minima, and there is relevant data. - Anicoside D is a natural sesquiterpene lactone isolated from the Chinese herb Centipeda minima[1]. - Its anti-nasopharyngeal carcinoma mechanism is related to the inhibition of the PI3K/Akt/mTOR signaling pathway, thereby inhibiting cell proliferation, migration and invasion, and inducing mitochondrial-mediated apoptosis (upregulating the Bax/Bcl-2 ratio and activating the caspase cascade)[1]. - Anicoside D is considered a potential candidate drug for the treatment of nasopharyngeal carcinoma due to its strong antitumor activity and low toxicity to normal cells[1]. |
| Molecular Formula |
C19H24O5
|
|---|---|
| Molecular Weight |
332.3909
|
| Exact Mass |
332.162
|
| CAS # |
34532-68-8
|
| PubChem CID |
182199
|
| Appearance |
White to off-white solid powder
|
| LogP |
2.453
|
| Hydrogen Bond Donor Count |
0
|
| Hydrogen Bond Acceptor Count |
5
|
| Rotatable Bond Count |
3
|
| Heavy Atom Count |
24
|
| Complexity |
648
|
| Defined Atom Stereocenter Count |
7
|
| SMILES |
C[C@@H]1C[C@@H]2[C@@H]([C@@H](C(=O)O2)C)[C@@H]([C@]3([C@H]1C=CC3=O)C)OC(=O)C(=C)C
|
| InChi Key |
NZESEVTYUVXOTC-APDQSUQKSA-N
|
| InChi Code |
InChI=1S/C19H24O5/c1-9(2)17(21)24-16-15-11(4)18(22)23-13(15)8-10(3)12-6-7-14(20)19(12,16)5/h6-7,10-13,15-16H,1,8H2,2-5H3/t10-,11+,12+,13-,15-,16+,19+/m1/s1
|
| Chemical Name |
[(1S,3aR,5R,5aR,8aR,9S,9aR)-1,5,8a-trimethyl-2,8-dioxo-3a,4,5,5a,9,9a-hexahydro-1H-azuleno[6,5-b]furan-9-yl] 2-methylprop-2-enoate
|
| 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) |
DMSO : ~25 mg/mL (~75.21 mM)
|
|---|---|
| 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 | 3.0085 mL | 15.0426 mL | 30.0851 mL | |
| 5 mM | 0.6017 mL | 3.0085 mL | 6.0170 mL | |
| 10 mM | 0.3009 mL | 1.5043 mL | 3.0085 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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