1. Anti-infection Metabolic Enzyme/Protease Apoptosis
  2. Bacterial Fungal Endogenous Metabolite Apoptosis
  3. Citrinin

Citrinin (NSC 186) is a mycotoxin that causes food contamination and has different toxic effects. Citrinin is an effective oral anticancer agent. Citrinin has various regulatory effects on mouse immune system, including regulating the number of immune cells, inducing apoptosis and autophagy of immune cells, altering toll-like receptor expression and cytokine production. Citrinin can induce oxidative stress and lead to early apoptosis of oocytes. Low doses of Citrinin have neuroprotective effects against glutamate-induced excitotoxicity in rat cortical neurons. In addition, Citrinin also has antibacterial activity.

For research use only. We do not sell to patients.

Citrinin Chemical Structure

Citrinin Chemical Structure

CAS No. : 518-75-2

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1 mg USD 70 In-stock
5 mg USD 220 In-stock
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Based on 1 publication(s) in Google Scholar

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  • Biological Activity

  • Purity & Documentation

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Description

Citrinin (NSC 186) is a mycotoxin that causes food contamination and has different toxic effects. Citrinin is an effective oral anticancer agent. Citrinin has various regulatory effects on mouse immune system, including regulating the number of immune cells, inducing apoptosis and autophagy of immune cells, altering toll-like receptor expression and cytokine production. Citrinin can induce oxidative stress and lead to early apoptosis of oocytes. Low doses of Citrinin have neuroprotective effects against glutamate-induced excitotoxicity in rat cortical neurons. In addition, Citrinin also has antibacterial activity[1][2][3][4][5].

IC50 & Target

Microbial Metabolite

 

Cellular Effect
Cell Line Type Value Description References
HCT-116 IC50
> 10 μM
Compound: 13
Cytotoxicity against human HCT116 cells after 72 hrs by SRB assay
Cytotoxicity against human HCT116 cells after 72 hrs by SRB assay
[PMID: 21761866]
HL-60 IC50
> 10 μM
Compound: 13
Cytotoxicity against human HL60 cells after 72 hrs by MTT assay
Cytotoxicity against human HL60 cells after 72 hrs by MTT assay
[PMID: 21761866]
KB IC50
> 10 μM
Compound: 13
Cytotoxicity against human KB cells after 72 hrs by SRB assay
Cytotoxicity against human KB cells after 72 hrs by SRB assay
[PMID: 21761866]
In Vitro

Citrinin (0.1-1000 nM; 24 h) has neuroprotective effects in glutamate-treated rat cortical neurons (at low doses)[2].
Citrinin (1-10 μg/mL; 6 h) induces late apoptosis of immune cells[3].
Citrinin (1-10 μg/mL; 6 h) increases the rate of Bax/Bcl-2 expression in freshly isolated spleen cells[3].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Apoptosis Analysis[3]

Cell Line: Splenocytes and MLN cells from a SPF mouse ages 7 seven weeks old
Concentration: 1, 5 and 10 μg/mL
Incubation Time: 6 h
Result: Significantly increased the number of late apoptotic cells, but not in early apoptotic cells.

Western Blot Analysis[3]

Cell Line: Splenocytes
Concentration: 1, 5 and 10 μg/mL
Incubation Time: 6 h
Result: Decreased the level of Bcl-2, and the expression of Bax was not affected.
In Vivo

Citrinin (1-10 mg/kg; Oral gavage; 14 days) has a variety of immunomodulatory effects in mice and may change the normal function of the immune system[3].
Citrinin (2 mg/kg; Oral administration; 3 weeks) has an antitumor effect in a mouse breast cancer model induced by DMBA (HY-W011845)[4].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Female BALB/c mice aged seven weeks old[3]
Dosage: 1, 5, or 10 mg/kg
Administration: Oral gavage (i.g.); 14 days
Result: Significantly reduced the populations of F4/80+ cells and CD19+ cells in spleen and MLN.
Increased the populations of CD4+, CD8+ and CD4+CD25+Foxp3+ cells in MLN.
Increased the populations of CD8+ cells and decreased the populations of CD19+ cells in intra-epithelial, lamina propria and Peyers patches lymphocytes.
Reduced IgM antibody production in serum.
Increased the ratios of Bax/Bcl-2 in the spleen.
Up-regulated the expression of Atg5, Beclin-1 and TLR 2 in the spleen.
Animal Model: DMBA (HY-W011845) treated swiss albino female mice aged 6-7 weeks old (25-30 g) [4]
Dosage: 2 mg/kg
Administration: Oral administration (p.o.); 3 weeks
Result: Reduced the weight of both breasts, and reduced cell proliferation in the breast.
Did not cause necrosis in the cells, the characteristics of the carcinoma such as intraductal calcification, injured tissue, fibrosed with ductal hyperplasia, and histopathological characteristics indicative of preneoplasia still remained.
Decreased genotoxic damage, damage index and damage frequency in breast and non-tumor cells induced by DMBA (HY-W011845).
Did not increase micronuclei or chromosomal bridge formation in hepatocytes of the animals.
Showed apoptotic effects of induction of binucleated cells in hepatic tissue.
Molecular Weight

250.25

Formula

C13H14O5

CAS No.
Appearance

Solid

Color

Light yellow to yellow

SMILES

O=C1C(C)=C2[C@H]([C@@H](OC=C2C(O)=C1C(O)=O)C)C

Structure Classification
Initial Source

Monascus specie

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

-20°C, stored under nitrogen

*In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen)

Solvent & Solubility
In Vitro: 

DMSO : 50 mg/mL (199.80 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 3.9960 mL 19.9800 mL 39.9600 mL
5 mM 0.7992 mL 3.9960 mL 7.9920 mL
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (stored under nitrogen). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

  • Molarity Calculator

  • Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass
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Volume
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Molecular Weight *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

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Volume (start)

V1

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Concentration (final)

C2

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Volume (final)

V2

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

  • Protocol 1

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% Saline

    Solubility: ≥ 1.25 mg/mL (5.00 mM); Clear solution

    This protocol yields a clear solution of ≥ 1.25 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (12.5 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

    Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
  • Protocol 2

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in Saline)

    Solubility: 1.25 mg/mL (5.00 mM); Suspended solution; Need ultrasonic

    This protocol yields a suspended solution of 1.25 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (12.5 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

    Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

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g

Dosing volume
(per animal)

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Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
DMSO +
+
%
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%
Saline
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Calculation results:
Working solution concentration: mg/mL
Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).

*In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen)

The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Purity & Documentation

Purity: 99.72%

References

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (stored under nitrogen). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 3.9960 mL 19.9800 mL 39.9600 mL 99.9001 mL
5 mM 0.7992 mL 3.9960 mL 7.9920 mL 19.9800 mL
10 mM 0.3996 mL 1.9980 mL 3.9960 mL 9.9900 mL
15 mM 0.2664 mL 1.3320 mL 2.6640 mL 6.6600 mL
20 mM 0.1998 mL 0.9990 mL 1.9980 mL 4.9950 mL
25 mM 0.1598 mL 0.7992 mL 1.5984 mL 3.9960 mL
30 mM 0.1332 mL 0.6660 mL 1.3320 mL 3.3300 mL
40 mM 0.0999 mL 0.4995 mL 0.9990 mL 2.4975 mL
50 mM 0.0799 mL 0.3996 mL 0.7992 mL 1.9980 mL
60 mM 0.0666 mL 0.3330 mL 0.6660 mL 1.6650 mL
80 mM 0.0500 mL 0.2498 mL 0.4995 mL 1.2488 mL
100 mM 0.0400 mL 0.1998 mL 0.3996 mL 0.9990 mL
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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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Citrinin
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