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| 10mg |
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| ln Vivo |
Tubeimoside II exhibited anti-inflammatory activity in a TPA-induced mouse ear edema model. When applied topically at doses of 0.0075, 0.037, 0.075, and 0.11 µmol per ear, it inhibited ear edema in a dose-dependent manner, with inhibition rates of 37.7%, 56.6%, 84.9%, and 100%, respectively. Its activity was stronger than that of tubeimoside I.[1]
In an in vivo antitumor test against transplantable mouse sarcoma S180 in BALB/c mice, intraperitoneal administration of tubeimoside II at 12 mg/kg/day for 1, 2, and 3 consecutive days resulted in tumor inhibition rates of 43.3%, 49.8%, and 60.1%, respectively, showing stronger activity than tubeimoside I.[1] In a two-stage mouse skin carcinogenesis model (initiated by DMBA, promoted by TPA), topical application of tubeimoside II (0.5 mg per painting, simultaneously with TPA) completely inhibited tumor formation up to the 18th week. Mice treated with tubeimoside II had smooth skin, unlike the inflammatory foci seen in the control group. Oral administration of tubeimoside II (dissolved in drinking water at 0.1 g/L ad libitum throughout the promotion stage) reduced the average number of tumors per mouse from 15.5 (control) to 10.0 by the 18th week, although the percentage of tumor-bearing mice remained the same (93.3%).[1] |
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| Animal Protocol |
For the anti-inflammatory test, tubeimoside II was dissolved in acetone and applied topically to both surfaces of each ear of male ICR mice 30 minutes before topical application of the irritant TPA (2 µg in 20 µL acetone). Ear thickness was measured 5 hours after TPA treatment.[1]
For the in vivo antitumor test, BALB/c mice were inoculated subcutaneously with S180 tumor cells. Tubeimoside II was administered intraperitoneally at a dose of 12 mg/kg/day on the indicated days (1, 2, or 3 consecutive days post-inoculation). Tumors were excised and weighed 20 days after inoculation to calculate the inhibition rate.[1] For the two-stage skin carcinogenesis study, the backs of female ICR mice were shaved and initiated with a single topical dose of DMBA (100 µg). Promotion was performed by applying TPA (1 µg) topically twice a week starting one week after initiation. For topical intervention, tubeimoside II (0.5 mg in acetone) was applied simultaneously with each TPA treatment. For oral intervention, tubeimoside II was dissolved in drinking water at a concentration of 0.1 g/L and provided ad libitum to mice throughout the promotion stage. Tumor incidence and number were recorded weekly.[1] |
| Toxicity/Toxicokinetics |
In ICR mice, the acute LD50 of tubeimoside II was determined to be 21 ± 3 mg/kg. [1]
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| References | |
| Additional Infomation |
Tubeimoside II is a triterpenoid compound. It has been reported that Tubeimoside II exists in Bolbostemma paniculatum, and related data have been reported. Tubeimoside II is an oleanane-type triterpenoid saponin (a cyclic disaccharide) isolated from the tuber of Bolbostemma paniculatum (a traditional Chinese medicine). Studies have shown that the C-16 hydroxyl group in its structure plays an important role in enhancing its biological activity (anti-inflammatory, antitumor, and antitumor-promoting) and reducing its acute toxicity, superior to tubeimoside I. Based on its stronger efficacy and lower toxicity in these models, Tubeimoside II is considered the most promising cancer chemoprevention and chemotherapy drug among tubeimoside I, II, and III. [1]
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| Molecular Formula |
C63H98O30
|
|---|---|
| Molecular Weight |
1335.43424367905
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| Exact Mass |
1334.614
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| CAS # |
115810-12-3
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| PubChem CID |
14037387
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| Appearance |
White to off-white solid powder
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| Density |
1.5±0.1 g/cm3
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| Index of Refraction |
1.643
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| LogP |
4.36
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| Hydrogen Bond Donor Count |
15
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| Hydrogen Bond Acceptor Count |
30
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| Rotatable Bond Count |
4
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| Heavy Atom Count |
93
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| Complexity |
2740
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| Defined Atom Stereocenter Count |
0
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| InChi Key |
GBWAAJJGXQJTTA-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C63H98O30/c1-25-46-47(89-51-43(77)38(72)29(67)21-82-51)45(79)53(85-25)91-48-39(73)30(68)22-83-54(48)93-56(80)63-14-13-57(2,3)15-27(63)26-9-10-34-59(5)16-28(66)50(60(6,24-65)33(59)11-12-61(34,7)62(26,8)17-35(63)69)92-55-49(42(76)40(74)31(20-64)87-55)90-52-44(78)41(75)32(23-84-52)86-36(70)18-58(4,81)19-37(71)88-46/h9,25,27-35,38-55,64-69,72-79,81H,10-24H2,1-8H3
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| Chemical Name |
7,8,18,28,29,35,51,55,56,58-decahydroxy-30,54-bis(hydroxymethyl)-13,18,37,41,48,48,53,54-octamethyl-57-(3,4,5-trihydroxyoxan-2-yl)oxy-3,5,10,12,15,21,24,26,31,33-decaoxadecacyclo[39.9.3.211,14.222,25.134,38.01,46.04,9.027,32.037,42.045,53]octapentacont-44-ene-2,16,20-trione
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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 (~74.88 mM)
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|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (1.87 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 (1.87 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 (1.87 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 | 0.7488 mL | 3.7441 mL | 7.4882 mL | |
| 5 mM | 0.1498 mL | 0.7488 mL | 1.4976 mL | |
| 10 mM | 0.0749 mL | 0.3744 mL | 0.7488 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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