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| 10mg |
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| 25mg |
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| ln Vitro |
- Formosanin C enhanced the proliferation of concanavalin A-stimulated mouse splenic lymphocytes by 45% at 20 μM and increased mouse peritoneal macrophage phagocytic activity by 38% at 30 μM. It also inhibited the proliferation of S180 sarcoma cells and Hela cervical cancer cells, with IC50 values of 42 μM (S180) and 48 μM (Hela) after 72 hours of treatment [1]
- In human hepatocellular carcinoma HepG2 cells, Formosanin C showed concentration-dependent antiproliferative effects: at 50 μM, it reduced cell viability by 52% (MTT assay) and disrupted cellular metabolism (lactate and pyruvate levels decreased by 35% and 40%, glutamine and alanine levels decreased by 30% and 32%, detected via 1H-NMR). It also induced G0/G1 cell cycle arrest (G0/G1 ratio increased by 28% at 50 μM) without significant apoptosis (apoptotic rate <8%, Annexin V-FITC staining) [2] |
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| ln Vivo |
- In a mouse S180 sarcoma xenograft model, Formosanin C (10 mg/kg, 20 mg/kg, intraperitoneal injection, once daily for 14 days) reduced tumor weight by 60% and tumor volume by 55% at 20 mg/kg compared to the vehicle group. It also enhanced immune function: spleen and thymus weights increased by 32% and 28%, and LPS-stimulated splenic lymphocyte proliferation increased by 45% [1]
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| Cell Assay |
- Splenic lymphocyte proliferation assay ([1]): Mouse splenocytes were isolated and seeded (2×10⁵ cells/well) in 96-well plates, stimulated with 5 μg/mL concanavalin A, and treated with Formosanin C (5-40 μM) for 48 hours. MTT reagent was added, and absorbance at 570 nm was measured to calculate proliferation rate [1]
- Macrophage phagocytosis assay ([1]): Mouse peritoneal macrophages were seeded (1×10⁵ cells/well) in 24-well plates, treated with Formosanin C (10-50 μM) for 24 hours, then incubated with fluorescent microspheres (1:100 ratio) for 2 hours. Phagocytic rate was counted via fluorescence microscopy [1] - HepG2 cell assays ([2]): 1. Viability test: HepG2 cells (5×10³ cells/well) were treated with Formosanin C (10-100 μM) for 72 hours, and viability was detected by MTT assay [2] 2. Metabolic profiling: HepG2 cells (2×10⁵ cells/well) were treated with 50 μM Formosanin C for 48 hours. Metabolites were extracted with methanol-water (2:1, v/v), centrifuged, and analyzed via 1H-NMR; concentrations were quantified with Chenomx NMR Suite [2] 3. Cell cycle analysis: HepG2 cells were treated with Formosanin C (20-80 μM) for 48 hours, fixed with 70% ethanol, stained with propidium iodide, and analyzed via flow cytometry [2] |
| Animal Protocol |
- S180 xenograft model establishment ([1]): Male ICR mice (6-8 weeks old) were subcutaneously injected with 1×10⁷ S180 cells into the right flank. After 7 days (tumor volume ~50 mm³), mice were divided into 3 groups (n=8): vehicle control, Formosanin C 10 mg/kg, Formosanin C 20 mg/kg [1]
- Drug administration ([1]): Formosanin C was dissolved in 0.5% DMSO + 0.9% normal saline, administered via intraperitoneal injection once daily for 14 days; vehicle group received the same solvent [1] - Detection ([1]): Mice were sacrificed on day 15. Tumor weight/volume, spleen/thymus weights were measured; splenic lymphocyte proliferation was detected by MTT assay [1] |
| Toxicity/Toxicokinetics |
- Formacin C (10-20 mg/kg, intraperitoneal injection, 14 days) did not affect mouse body weight (change <5%), nor did it cause liver and kidney pathological damage (no necrosis/inflammation observed by HE staining) [1] - At a concentration as high as 80 μM, Formacin C did not reduce the viability of normal human hepatocytes (LO2 cells), and the viability was >90% compared with the control group [2]
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| References | |
| Additional Infomation |
Taiwan yam saponin C is a steroidal saponin isolated from plants of the Dioscorea genus (such as Taiwan yam). Its antitumor activity in [1] is related to enhancing cell-mediated immunity (lymphocyte proliferation, macrophage phagocytosis) [1]. The antitumor effect of Taiwan yam saponin C on HepG2 cells in [2] is related to glycolysis and amino acid metabolism disorders, which are crucial for energy supply and biosynthesis in cancer cells [2].
|
| Molecular Formula |
C51H82O20
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|---|---|
| Molecular Weight |
1015.1848
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| Exact Mass |
1014.539
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| CAS # |
50773-42-7
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| PubChem CID |
73597
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| Appearance |
White to off-white solid powder
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| Density |
1.4±0.1 g/cm3
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| Index of Refraction |
1.621
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| LogP |
5.72
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| Hydrogen Bond Donor Count |
10
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| Hydrogen Bond Acceptor Count |
20
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| Rotatable Bond Count |
9
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| Heavy Atom Count |
71
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| Complexity |
1900
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| Defined Atom Stereocenter Count |
29
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| SMILES |
C[C@@H]1CC[C@@]2([C@H]([C@H]3[C@@H](O2)CC4[C@@]3(CC[C@H]5[C@H]4CC=C6[C@@]5(CC[C@@H](C6)O[C@H]7[C@@H]([C@H]([C@@H]([C@H](O7)CO)O[C@H]8[C@@H]([C@@H]([C@H]([C@@H](O8)C)O[C@H]9[C@H]([C@@H]([C@H]([C@@H](O9)C)O)O)O)O)O)O)O[C@H]2[C@@H]([C@@H](C([C@@H](O2)C)O)O)O)C)C)C)OC1
|
| InChi Key |
OZIHYFWYFUSXIS-KORJSKJVSA-N
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| InChi Code |
InChI=1S/C51H82O20/c1-20-10-15-51(62-19-20)21(2)32-30(71-51)17-29-27-9-8-25-16-26(11-13-49(25,6)28(27)12-14-50(29,32)7)66-48-44(70-46-39(59)36(56)34(54)23(4)64-46)41(61)43(31(18-52)67-48)69-47-40(60)37(57)42(24(5)65-47)68-45-38(58)35(55)33(53)22(3)63-45/h8,20-24,26-48,52-61H,9-19H2,1-7H3/t20-,21+,22+,23+,24+,26+,27-,28+,29?,30+,31-,32+,33+,34?,35-,36-,37+,38+,39-,40-,41+,42+,43-,44-,45+,46+,47+,48-,49+,50+,51-/m1/s1
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| Chemical Name |
(2S,3S,4R,5R,6S)-2-[(2S,3R,4S,5R,6S)-4,5-dihydroxy-6-[(2R,3S,4S,5R,6R)-4-hydroxy-2-(hydroxymethyl)-6-[(1S,4S,5'R,6R,7S,8R,9S,12S,13R,16S)-5',7,9,13-tetramethylspiro[5-oxapentacyclo[10.8.0.02,9.04,8.013,18]icos-18-ene-6,2'-oxane]-16-yl]oxy-5-[(2S,3R,4R,6S)-3,4,5-trihydroxy-6-methyloxan-2-yl]oxyoxan-3-yl]oxy-2-methyloxan-3-yl]oxy-6-methyloxane-3,4,5-triol
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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) |
DMSO : ~100 mg/mL (~98.50 mM)
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|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (2.46 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. Solubility in Formulation 2: ≥ 2.5 mg/mL (2.46 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (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 corn oil and mix evenly. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 0.9850 mL | 4.9252 mL | 9.8504 mL | |
| 5 mM | 0.1970 mL | 0.9850 mL | 1.9701 mL | |
| 10 mM | 0.0985 mL | 0.4925 mL | 0.9850 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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