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| ln Vitro |
By blocking farnesyl transferase, which activates the RAS proto-oncogene and is assumed to be a major factor in 20–30% of human cancers, arglabin exhibits its anti-tumor effect. In fact, it prevents farnesyl transferase (FTase) from incorporating farnesyl pyrophosphate into the human H-ras protein [2].
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| ln Vivo |
In ApoE2.Ki animals fed a high-fat diet, Arglabin decreased inflammation and plasma lipids, enhanced autophagy, and shifted tissue macrophages toward an anti-inflammatory phenotype [1].
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| Animal Protocol |
In Vivo Efficacy in ApoE2.Ki Mice:** Female ApoE2.Ki mice, 6 weeks of age, were fed a high-fat diet for 13 weeks. They were randomly divided into two groups. The first group (control, n=4) received intraperitoneal injections of 5 µL dimethyl sulfoxide (vehicle) twice daily. The second group (arglabin, n=4) received intraperitoneal injections of arglabin at a dose of 2.5 ng/g body weight, also twice daily. After 13 weeks, under isoflurane anesthesia, blood was collected in EDTA tubes for plasma analysis of cytokines, lipids, and anti-oxLDL antibodies. Hearts and descending aortas were excised for histological and immunohistochemical studies. [1]
* **In Vivo Studies with Nlrp3-/- Mice:** Female ApoE2.Ki/Nlrp3-/- mice, 6 weeks of age, were also fed a high-fat diet for 13 weeks. One group was treated with vehicle, and another group was treated with arglabin (2.5 ng/g body weight, twice daily) following the same protocol as above, to assess the dependency of arglabin's effects on NLRP3. [1] * **Atherosclerotic Lesion Analysis:** After euthanasia, hearts were cut directly under and parallel to the leaflets. The upper portions were embedded in optimal cutting temperature medium. One hundred serial cryosections, each 10 µm thick, were prepared from the top of the left ventricle. Ten sections, each separated by 90 µm, were stained for lipids with Oil Red O and counterstained with Harris hematoxylin. The mean lesion size in these 10 sections was used to evaluate the lesion size in the aortic sinus for each animal. For the whole aorta (en face), the descending thoracic and abdominal aorta were cleaned, processed, and stained with Oil Red O. The extent of atherosclerosis was assessed with computer-assisted histomorphometry. [1] * **Immunohistochemistry for Macrophage Phenotyping:** Frozen serial sections (10 µm) of proximal aortas from control and arglabin-treated ApoE2.Ki mice fed an HFD were analyzed by immunohistochemistry. This involved double immunostaining with antibodies against the macrophage marker F4/80 combined with either the M1 marker IL-1β or the M2 marker CD206. The number of positive cells within a high-powered field was quantified. [1] |
| References | |
| Additional Infomation |
Arglabin is an organic heterotetracyclic compound belonging to the guaiacene sesquiterpene lactone family. Its structure involves the substitution of acrylic acid at the 2-position with a 4-hydroxy-3,8-dimethyl-1,3a,4,5,6,7-hexahydroazine-5-yl group, where the double bond on the seven-membered ring is epoxidized, and the hydroxyl and carboxyl groups undergo a condensation reaction to generate the corresponding γ-lactone. It is found in plants of the genus Artemisia glabella. Arglabin-DMA HCl is the hydrochloride salt of an adduct of dimethylamine and an enyl lactone, and has been successfully used in Kazakhstan for the treatment of breast cancer, colon cancer, ovarian cancer, and lung cancer. It is both an antitumor drug and a metabolite. It is an organic heterotetracyclic compound, a γ-lactone, an epoxide, and a sesquiterpene lactone. Arglabin has been reported in Artemisia argyi and Pentzia eenii, and available data are available.
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| Molecular Formula |
C15H18O3
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|---|---|
| Molecular Weight |
246.31
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| Exact Mass |
246.125
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| CAS # |
84692-91-1
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| PubChem CID |
5574924
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| Appearance |
White to light yellow solid powder
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| Density |
1.2±0.1 g/cm3
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| Boiling Point |
404.6±45.0 °C at 760 mmHg
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| Melting Point |
102 °C
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| Flash Point |
171.3±23.3 °C
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| Vapour Pressure |
0.0±0.9 mmHg at 25°C
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| Index of Refraction |
1.571
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| LogP |
1.74
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| Hydrogen Bond Donor Count |
0
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| Hydrogen Bond Acceptor Count |
3
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| Rotatable Bond Count |
0
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| Heavy Atom Count |
18
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| Complexity |
506
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| Defined Atom Stereocenter Count |
5
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| SMILES |
CC1=CC[C@@]23[C@H]1[C@@H]4[C@@H](CC[C@@]2(O3)C)C(=C)C(=O)O4
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| InChi Key |
UVJYAKBJSGRTHA-CUZKYEQNSA-N
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| InChi Code |
InChI=1S/C15H18O3/c1-8-4-7-15-11(8)12-10(9(2)13(16)17-12)5-6-14(15,3)18-15/h4,10-12H,2,5-7H2,1,3H3/t10-,11+,12-,14-,15+/m0/s1
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| Chemical Name |
(1R,3S,6S,10S,11R)-3,12-dimethyl-7-methylidene-2,9-dioxatetracyclo[9.3.0.01,3.06,10]tetradec-12-en-8-one
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| Synonyms |
Arglabin (+)-Arglabin
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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) |
DMSO : ≥ 100 mg/mL (~406.01 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (10.15 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 (10.15 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 (10.15 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 | 4.0599 mL | 20.2996 mL | 40.5992 mL | |
| 5 mM | 0.8120 mL | 4.0599 mL | 8.1198 mL | |
| 10 mM | 0.4060 mL | 2.0300 mL | 4.0599 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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