Swainsonine (0-40 μM; 12 h) demonstrates antiproliferative action in U251 and LN444 cells [2]. Swainsonine (30 μM; 12 h) stimulates cell engraftment and cell cycle induction in G2/M phase, and lowers CyclinD1 and Swainsonine (30 μM; 12 h) reduces tumor cell migration and right side [2].

In mice, cisplatin plus swansonine (1 mg/kg; intraperitoneal injection; twice daily for 10 days) increased antitumor effectiveness [3].

Cell Viability Assay[2]
Cell Types: U251, LN444 cells
Tested Concentrations: 0, 10, 20, 30, 40 µM
Incubation Duration: 12 hrs (hours)
Experimental Results: Inhibits cell viability in a dose-dependent manner and is not cytotoxic to normal brain cells.

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Cell cycle analysis[2]
Cell Types: U251 Cell
Tested Concentrations: 30 µM
Incubation Duration: 12 hrs (hours)
Experimental Results: Induced cell cycle arrest in G2/M phase.

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Apoptosis analysis [2]
Cell Types: U251 Cell
Tested Concentrations: 30 µM
Incubation Duration: 12 h
Experimental Results: Cell apoptosis was induced, and the expression of cleaved-Caspase-3 and cleaved-Caspase-9 was Dramatically increased.

Animal/Disease Models: 87 60-day-old male C57BL/6 mice [3]
Doses: 1 mg/kg (cisplatin; 0.25 mg/kg, ip, every other day for 10 days)
Route of Administration: ip; twice (two times) daily, The results lasted for ten days: the ascites volume of mice was Dramatically diminished by 63.5%, and the percentage of cells in G0/G1, S and G2 phases was Dramatically diminished.

Toxicity Summary
Swanesenine inhibits the activity of glycoside hydrolases, particularly N-linked glycosylation enzymes. Inhibition of Golgi mannosidase II and other α-mannosidases leads to the accumulation of atypical heterozygous glycoproteins and oligosaccharides, as these substances cannot be processed normally. This also results in intracellular vacuolation. (L1248, A3092, A3093)

[1]. Inhibition of lysosomal alpha-mannosidase by swainsonine, an indolizidine alkaloid isolated from Swainsona canescens. Biochem J. 1980 Nov 1;191(2):649-51.

[2]. Swainsonine represses glioma cell proliferation, migration and invasion by reduction of miR-92a expression. BMC Cancer. 2019 Mar 19;19(1):247. doi: 10.1186/s12885-019-5425-7.

[3]. Increased antitumor efficacy by the combined administration of swainsonine and cisplatin in vivo. Phytomedicine. 2011 Sep 15;18(12):1096-101.

Swainsonine is an indolithidine alkaloid isolated from the plant Swainsonine, with three hydroxyl substituents at positions 1, 2, and 8. It possesses antitumor activity, immunoadjuvant activity, EC 3.2.1.114 (mannosyl oligosaccharide 1,3-1,6-α-mannosidase) inhibitory activity, and plant metabolite activity. It is a potent α-mannosidase inhibitor derived from Swainsonine. Swainsonine also exhibits anti-metastatic, anti-proliferative, and immunomodulatory activities. It has been reported to exist in Slafractonia leguminicola, Oxytropis glabra, and other organisms with relevant data. Swanesenine is a plant toxin found in legumes (Fabaceae, Astragalus, and Swainsona) and certain fungi (Metarhizium anisopliae, Rhizoctonia solani). It is known to cause a potentially fatal central nervous system disease in livestock called "hysteria," a significant cause of economic losses in the livestock industry. Swanesenine, along with another bioactive compound from Rhizoctonia solani—slavamine—may cause a disease called "drooling" in livestock that ingest contaminated feed. (L1248, A3092) Swanesenine is an indolithidine alkaloid from the plant Swainsonine, a potent α-mannosidase inhibitor. It also possesses anti-metastatic, anti-proliferative, and immunomodulatory activities.

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Mechanism of Action
Tridolgosir competitively inhibits α-mannosidase II (αMII), an enzyme responsible for processing the N-linked sugars of newly synthesized glycoproteins, which are transported to the cell surface via the Golgi apparatus. The resulting highly branched sugar structures can bind to lectin-phytohemagglutinin (L-PHA) and are expressed in different types of tumors, leading to a metastatic phenotype. This metastatic phenotype is associated with increased tumor invasiveness in animals and can lead to other human malignancies. Inhibition of αMII reduces carbohydrates bound to L-PHA, thereby decreasing the activity of tumor-invasive and metastatic cells, slowing tumor growth, and increasing the content of "mixed" carbohydrates on the cell surface. Mixed carbohydrates may enhance cytokine activation in lymphocytes, thereby increasing the sensitivity of tumors to lymphokine-activated cells and natural killer cells.

C8H15NO3

173.2096

173.105

72741-87-8

51683

Light yellow to brown solid powder

1.38±0.1 g/cm3

353.3±21.0 °C at 760 mmHg

144-145 ºC

209.7±20.7 °C

0.0±1.8 mmHg at 25°C

1.609

-0.79

3

4

0

12

176

4

C1C[C@H]([C@@H]2[C@@H]([C@@H](CN2C1)O)O)O

FXUAIOOAOAVCGD-WCTZXXKLSA-N

InChI=1S/C8H15NO3/c10-5-2-1-3-9-4-6(11)8(12)7(5)9/h5-8,10-12H,1-4H2/t5-,6-,7-,8-/m1/s1

(1S,2R,8R,8aR)-1,2,3,5,6,7,8,8a-octahydroindolizine-1,2,8-triol

2934.99.9001

Powder      -20°C    3 years

                     4°C     2 years

In solvent   -80°C    6 months

                  -20°C    1 month

Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)

DMSO : ~10 mg/mL (~57.73 mM)
Ethanol : ~10 mg/mL (~57.73 mM)
H2O : ~3.57 mg/mL (~20.61 mM)

Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.

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Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)
*Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution.
Injection Formulation 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline)
Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil)
Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals).

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Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)]
*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.
Injection Formulation 5: 2-Hydroxypropyl-β-cyclodextrin : Saline = 50 : 50 (i.e. 500 μL 2-Hydroxypropyl-β-cyclodextrin → 500 μL Saline)
Injection Formulation 6: DMSO : PEG300 : castor oil : Saline = 5 : 10 : 20 : 65 (i.e. 50 μL DMSO → 100 μLPEG300 → 200 μL castor oil → 650 μL Saline)
Injection Formulation 7: Ethanol : Cremophor : Saline = 10： 10 : 80 (i.e. 100 μL Ethanol → 100 μL Cremophor → 800 μL Saline)
Injection Formulation 8: Dissolve in Cremophor/Ethanol (50 : 50), then diluted by Saline
Injection Formulation 9: EtOH : Corn oil = 10 : 90 (i.e. 100 μL EtOH → 900 μL Corn oil)
Injection Formulation 10: EtOH : PEG300：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL EtOH → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline)

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Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium)
Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose
Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals).

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Oral Formulation 3: Dissolved in PEG400
Oral Formulation 4: Suspend in 0.2% Carboxymethyl cellulose
Oral Formulation 5: Dissolve in 0.25% Tween 80 and 0.5% Carboxymethyl cellulose
Oral Formulation 6: Mixing with food powders

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Note: Please be aware that the above formulations are for reference only. InvivoChem strongly recommends customers to read literature methods/protocols carefully before determining which formulation you should use for in vivo studies, as different compounds have different solubility properties and have to be formulated differently.

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 (Please use freshly prepared in vivo formulations for optimal results.)