Gracillin (Synonyms: NSC 698787) |
Catalog No.GN10533
One-Click Copy Product Info
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Gracillin, as a natural steroidal saponin component of D. quinqueloba, has antitumour, antimicrobial, antioxidant, pro‐apoptotic and anti‐inflammatory properties.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 19083-00-2
Sample solution is provided at 25 µL, 10mM.
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Gracillin, as a natural steroidal saponin component of D. quinqueloba, has antitumour, antimicrobial, antioxidant, pro‐apoptotic and anti‐inflammatory properties[1].
In vitro, Gracillin markedly inhibited the viability of RKO, SW480 and HCT116 cells, with IC50 of 3.118, 2.671 and 5.473μM, respectively. Gracillin (0, 2.5, 5 or 10μM; 36h) also stimulated apoptosis in human CRC cells in a dose-dependent manner[1]. Gracillin obviously inhibited the proliferation of A549 cells with IC50 of 2.54μmol/L in a concentration-dependent and time-dependent manner and induced morphological changes[2]. Gracillin inhibited the gastric tumor BGC823 cell proliferation in a concentration-dependent manner with IC50 of 8.3μM and gastric tumor SGC7901 cell proliferation with IC50 of 8.9μM in the range of 0-15μM[3]. Gracillin (0-12μM; 12h) induced TIPE2 expression in BGC-823 cells in a concentration-dependent manner[3]. Gracillin had dose-dependent inhibitory effects on the mitochondrial function in various human cancer cell lines derived from lung, colorectum, prostate, pharynx, and liver with IC50 of ~1-5μM[4].
In vivo, Gracillin (1 or 2mg/kg; i.p.; administered 8 times over 14 days) dose-dependently inhibited the growth of HCT116 cell-derived xenograft tumors in BALB/c nude mice while maintaining stable body weight[1]. Fish treated with 1mg/kg Gracillin carried significantly fewer parasites than the control, and the acute toxicity LD50 of Gracillin for grass carp was 1.64mg/kg[5].
References:
[1] Yang L, et al. Gracillin shows potent efficacy against colorectal cancer through inhibiting the STAT3 pathway. J Cell Mol Med. 2021 Jan;25(2):801-812.
[2] Yang J, et al. Gracillin Isolated from Reineckia carnea Induces Apoptosis of A549 Cells via the Mitochondrial Pathway. Drug Des Devel Ther. 2021 Jan 20;15:233-243.
[3] Liu W, et al. Beneficial Effects of Gracillin From Rhizoma Paridis Against Gastric Carcinoma via the Potential TIPE2-Mediated Induction of Endogenous Apoptosis and Inhibition of Migration in BGC823 Cells. Front Pharmacol. 2021 Sep 24;12:669199.
[4] Min HY, et al. The natural compound gracillin exerts potent antitumor activity by targeting mitochondrial complex II. Cell Death Dis. 2019 Oct 24;10(11):810.
5[5] Zheng W, et al. Antiparasitic efficacy of Gracillin and Zingibernsis newsaponin from Costus speciosus (Koen ex. Retz) Sm. against Ichthyophthirius multifiliis. Parasitology. 2015 Mar;142(3):473-9.
| Cell experiment [1]: | |
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Cell lines |
A549 cells |
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Preparation Method |
A549 cells were cultured in 6-well plates at a density of 1.5×105/well and cultured for 12h, and then treated with a series of concentrations of Gracillin (0.25, 0.5, 1, 2, 4µM) for 24h. The cells were stained with Hoechst 33258 staining buffer and the morphology of apoptosis was observed by fluorescence microscopy. |
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Reaction Conditions |
0.25, 0.5, 1, 2, 4 µM; 24h |
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Applications |
Gracillin induced morphological changes in apoptosis of A549 cells by fluorescence microscopy after staining with Hoechst33258. Compared with the blank group, the Gracillin treatment group showed the typical morphological characteristics of apoptotic cells, specifically, the number of cells was relatively reduced, the nucleus was pyknotic, the chromatin condensed into lumps under the nuclear membrane, and showed bright blue fluorescence staining. |
| Animal experiment [2]: | |
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Animal models |
Female BALB/c nude mice |
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Preparation Method |
HCT116 cells were harvested and then transplanted subcutaneously (5×106 cells in 100μL of PBS) on the right flank of the mice.The mice were randomly divided into three groups, which were injected intraperitoneal every other day with Gracillin (1mg/kg or 2mg/kg) or PBS (control) till the tumours' volume reached ~100 mm3. |
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Dosage form |
1mg/kg or 2mg/kg; i.p.; 8 times |
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Applications |
Results clearly show that the volume and weight of the tumours were lower in the Gracillin treated mice when compared to the control group. This inhibitory effect was in a clear dose dependent manner. |
References: [1] Yang J, et al. Gracillin Isolated from Reineckia carnea Induces Apoptosis of A549 Cells via the Mitochondrial Pathway. Drug Des Devel Ther. 2021 Jan 20;15:233-243. [2] Yang L, et al. Gracillin shows potent efficacy against colorectal cancer through inhibiting the STAT3 pathway. J Cell Mol Med. 2021 Jan;25(2):801-812. | |
| Cas No. | 19083-00-2 | SDF | |
| Synonyms | NSC 698787 | ||
| Canonical SMILES | CC1CCC2(C(C3C(O2)CC4C3(CCC5C4CC=C6C5(CCC(C6)OC7C(C(C(C(O7)CO)O)OC8C(C(C(C(O8)CO)O)O)O)OC9C(C(C(C(O9)C)O)O)O)C)C)C)OC1 | ||
| Formula | C45H72O17 | M.Wt | 884.48 |
| Solubility | ≥ 174.4mg/mL in DMSO, Limited solubility in EtOH | Storage | 4°C, protect from light |
| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 1.1306 mL | 5.653 mL | 11.3061 mL |
| 5 mM | 226.1 μL | 1.1306 mL | 2.2612 mL |
| 10 mM | 113.1 μL | 565.3 μL | 1.1306 mL |
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
g
μL
Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)
Calculation results:
Working concentration: mg/ml;
Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid 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 master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL saline, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.
Quality Control & SDS
- View current batch:
- Purity: >98.00% Appearance: A solid
- COA (Certificate of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 30 reference(s) in Google Scholar.)