OSW-1 (Synonyms: Orsaponin) |
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Catalog No.GC46194
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OSW-1 is a specific antagonist of osterol-binding protein (OSBP) and OSBP-related protein 4 (ORP4).
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 145075-81-6
Sample solution is provided at 25 µL, 10mM.
OSW-1(Orsaponin) is a saponin found in Heterosmilax yunnanensis, inhibits oxysterol-binding protein (OSBP) and its paralog OSBP-related protein 4 (ORP4), and shows antiviral and anticancer activities[1]. OSW-1(Orsaponin) has been shown to repress cancer progression through inhibiting cell proliferation, arresting cell cycle, inducing apoptosis and Golgi stress response, as well as suppressing migration, invasion and angiogenesis by regulating miRNAs expression and various signaling pathways[2].
In vitro, OSW-1(Orsaponin) induced more apoptotic cells (MDA-MB-231 vs MDA-MB-453 cells, 52.5% vs 60.5%) than control groups after incubation with 100 ng/mL OSW-1 for 24 hours. Apoptosis ratio in OSW-1(Orsaponin) treatment groups was significantly elevated compared with control groups. OSW-1(Orsaponin) groups showed more apoptotic cells than control groups both in MDA-MB-231 and MDA-MB-453 cells. Compared with non- OSW-1(Orsaponin)-treated controls, both cleaved PARP and cleaved caspase 3 expressions in protein levels were increased in OSW-1(Orsaponin)-treated groups. Furthermore, the overexpressed cleaved poly ADP-ribose polymerase (PARP) and cleaved caspase 3 were found in 100 ng/mL OSW-1(Orsaponin)-treated cells than those in 50 ng/mL OSW-1-treated cells[3].
In vivo, OSW-1(Orsaponin) was injected intraperitoneally (0.01 mg/kg diluted in PBS in 500 µl, daily) in treated group when heterotopic xenograft tumor model in nude mouse subcutaneously inoculated by LoVo cells. Compared with the control group, the treated group observed a decrease in tumor size and weight without significant side effects, with fewer Ki-67-positive cells and more apoptotic cells[4]. OSW-1(Orsaponin)-treated tumor tissues had countless apoptotic cells, but few apoptotic cells in the control group, suggesting that OSW-1 suppressed colon tumor proliferation through apoptosis in vivo. A number of necrotic foci within the tumor tissues of control mice, but not in OSW-1(Orsaponin) mice, suggesting that tumor growth speed may be greater in control mice than OSW-1(Orsaponin)-treated mice[5].

Fig 1 Overview of the anticancer mechanisms of OSW-1 in cancer cells
References:
[1] Burgett AW, et al. Natural products reveal cancer cell dependence onoxysterol-binding proteins.Nat Chem Biol. 2011 Aug 7;7(9):639-47.
[2] Zhan Z, Liu Z, Lai J, Zhang C, Chen Y, Huang H. Anticancer Effects and Mechanisms of OSW-1 Isolated From Ornithogalum saundersiae: A Review. Front Oncol. 2021 Sep 23;11:747718.
[3] Ding X, Li Y, Li J, Yin Y. OSW-1 inhibits tumor growth and metastasis by NFATc2 on triple-negative breast cancer. Cancer Med. 2020 Aug;9(15):5558-5569.
[4] Zhang Y, Fang F, Fan K, Zhang Y, Zhang J, Guo H, et al. Effective Cytotoxic Activity of OSW-1 on Colon Cancer by Inducing Apoptosis In Vitro and In Vivo. Oncol Rep (2017) 37(6):3509–19.
[5] Yanhong,Zhang,Fengqi,et al.Effective cytotoxic activity of OSW-1 on colon cancer by inducing apoptosis in vitro and in vivo[J].Oncology Reports, 2017, 37(6).
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Cell experiment [1]: |
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Cell lines |
Human breast cancer cell lines |
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Preparation method |
Human breast cancer (1×104 cells/well) were inoculated into 96-well plates and incubated overnight. Cells were treated with various concentrations of OSW-1(Orsaponin) (12.5, 25, 50, 100 ng/mL) for 24, 48 and 72 hours, then, the cytotoxicity was detected with cell count kit 8 (CCK8). |
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Reaction Conditions |
12.5, 25, 50, 100 ng/mL |
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Applications |
OSW-1(Orsaponin) doses varying from 12.5 to 100 ng/mL significantly reduced TNBC cell viability in a dose- and time-dependent manner. |
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Animal experiment [2]: |
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Animal models |
BALB/c-nu male mice (5–6 weeks of age, weighing 15–17 g) |
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Preparation method |
Under sterile conditions, a 200-μL suspension (100 μL PBS and 100 μL Matrigel) of LN18 cells (1× 107 cells/mouse) was inoculated subcutaneously into the right armpit of nude mice. When the tumor volume reached 200 mm3, the mice were randomly divided into two groups with five mice in each group. The mice from the experimental and control groups were intraperitoneally injected with OSW-1 (0.01 mg/kg, diluted in 100 μL PBS) and the same volume of saline, respectively, every day for consecutive 21 days. |
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Dosage form |
0.01 mg/kg |
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Applications |
In OSW-1 treatment group, the tumors were evidently smaller, compared to the the control group; particularly, an evident reductionin the average tumor volume and weight was observed in the OSW-1 group. However, no signifcant diference was observed regarding the body weight between the two groups, indicating the low toxicity of OSW-1 in vivo. The western blotting assays of tumor tissue lysates showed that OSW-1 inhibited the expression levels of p-PI3K and p-Akt1 in the OSW-1 treatment group compared to the control group. Collectively, these results demonstrated OSW-1 inhibited glioma tumor progression by targeting PI3K/AkT signaling pathways in vivo. |
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References: [1] Ding X, Li Y, Li J, Yin Y. OSW-1 inhibits tumor growth and metastasis by NFATc2 on triple-negative breast cancer. Cancer Med. 2020 Aug;9(15):5558-5569. [2] Zhan Z, Liu Z, Zhang C, Gao H, Lai J, Chen Y, Huang H. Anticancer effects of OSW-1 on glioma cells via regulation of the PI3K/AKT signal pathway: A network pharmacology approach and experimental validation in vitro and in vivo. Front Pharmacol. 2022 Sep 5;13:967141. |
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| Cas No. | 145075-81-6 | SDF | |
| Synonyms | Orsaponin | ||
| Canonical SMILES | O=C(CCC(C)C)[C@@H](C)[C@@]1(O)[C@@H](O[C@@H]2OC[C@H](O)[C@H](O[C@@H]3OC[C@@H](O)[C@H](O)[C@H]3OC(C4=CC=C(OC)C=C4)=O)[C@H]2OC(C)=O)C[C@@]5([H])[C@]6([H])CC=C7C[C@@H](O)CC[C@]7(C)[C@@]6([H])CC[C@@]51C | ||
| Formula | C47H68O15 | M.Wt | 873 |
| Solubility | Methanol: soluble | Storage | Store at -20°C, protect from light, stored under nitrogen |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
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| 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 | 1.1455 mL | 5.7274 mL | 11.4548 mL |
| 5 mM | 229.1 μL | 1.1455 mL | 2.291 mL |
| 10 mM | 114.5 μL | 572.7 μL | 1.1455 mL |
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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.
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Quality Control & SDS
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- Purity: >98.00% Appearance: A solid
- COA (Certificate of Analysis)
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Average Rating: 5 (Based on Reviews and 25 reference(s) in Google Scholar.)
