2. Metabolic Enzyme/Protease
  3. 11β-HSD Endogenous Metabolite
  4. Lunularin

Lunularin is an inhibitor of 11β-hydroxysteroid dehydrogenase 1, with an IC50 of 45.44 μM and a Ki of 35.8 μM against human 11β-HSD1, and an IC50 of 17.39 μM and a Ki of 10.31 μM against rat 11β-HSD1. Lunularin upregulates the transcription levels of Sirt1 and Hmox1 genes in the liver. Lunularin reduces food intake and body weight gain, and decreases blood glucose levels in mice fed a high-fat diet. Lunularin inhibits LPS-induced TLR4-mediated NF-κB pathway activation and nitric oxide production. Lunularin inhibits the proliferation and colony formation of renal cancer and colon cancer cells, and exhibits cancer cell-specific cytotoxicity. Lunularin binds to the steroid-binding site of human 11β-HSD1 and the steroid/NADPH-binding region of rat 11β-HSD1, but does not inhibit 11β-HSD2 or mouse 11β-HSD1. Lunularin can be used in research related to diet-induced obesity, renal cancer, colorectal cancer, inflammatory diseases and metabolic syndrome.

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Lunularin

Lunularin Chemical Structure

CAS No. : 37116-80-6

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Lunularin Related Antibodies

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Description

Lunularin is an inhibitor of 11β-hydroxysteroid dehydrogenase 1, with an IC50 of 45.44 μM and a Ki of 35.8 μM against human 11β-HSD1, and an IC50 of 17.39 μM and a Ki of 10.31 μM against rat 11β-HSD1. Lunularin upregulates the transcription levels of Sirt1 and Hmox1 genes in the liver. Lunularin reduces food intake and body weight gain, and decreases blood glucose levels in mice fed a high-fat diet. Lunularin inhibits LPS-induced TLR4-mediated NF-κB pathway activation and nitric oxide production. Lunularin inhibits the proliferation and colony formation of renal cancer and colon cancer cells, and exhibits cancer cell-specific cytotoxicity. Lunularin binds to the steroid-binding site of human 11β-HSD1 and the steroid/NADPH-binding region of rat 11β-HSD1, but does not inhibit 11β-HSD2 or mouse 11β-HSD1. Lunularin can be used in research related to diet-induced obesity, renal cancer, colorectal cancer, inflammatory diseases and metabolic syndrome[1][2][3][4].

Cellular Effect
Cell Line Type Value Description References
A549 IC50
150 μM
Compound: Lunularin
Cytotoxic activity against human A549 cells assessed as reduction in cell viability incubated for 24 hrs by MTT assay
Cytotoxic activity against human A549 cells assessed as reduction in cell viability incubated for 24 hrs by MTT assay
[PMID: 30848895]
J774 IC50
> 512 μM
Compound: HO21
Cytotoxicity against mouse J774 cells assessed as cell viability after 48 hrs by resazurin assay
Cytotoxicity against mouse J774 cells assessed as cell viability after 48 hrs by resazurin assay
[PMID: 25884114]
MRC5 IC50
200 μM
Compound: Lunularin
Cytotoxic activity against human MRC5 cells assessed as reduction in cell viability incubated for 24 hrs by MTT assay
Cytotoxic activity against human MRC5 cells assessed as reduction in cell viability incubated for 24 hrs by MTT assay
[PMID: 30848895]
In Vitro

Lunularin (0.5×-1.5×; 26.8-80.4 nmol/g) dose-dependently inhibits the proliferation of 786-O human renal adenocarcinoma cells, with greater activity than dihydroresveratrol alone at concentrations relevant to kidney tissue levels[2].
Lunularin (0.5×-1.5×; 26.8-80.4 nmol/g) dose-dependently inhibits the proliferation of A498 human renal carcinoma cells, with greater activity than dihydroresveratrol alone at concentrations relevant to kidney tissue levels[2].
Lunularin (1×; 53.6 nmol/g) significantly inhibits the clonogenic growth of 786-O human renal adenocarcinoma cells at concentrations relevant to kidney tissue levels, with enhanced activity when combined with dihydroresveratrol[2].
Lunularin (1×100; 53.6 nmol/g) significantly inhibits the clonogenic growth of A498 human renal carcinoma cells at concentrations relevant to kidney tissue levels, with enhanced activity when combined with dihydroresveratrol[2].
Lunularin (0.5×-1.5×; 30.25-90.75 nmol/g) inhibits the proliferation of HCT-116 human colorectal carcinoma cells, with enhanced activity when combined with dihydroresveratrol at concentrations relevant to colonic tissue levels[2].
Lunularin (1×; 60.5 nmol/g; 12 days) significantly inhibits the clonogenic growth of HT-29 human colon adenocarcinoma cells at concentrations relevant to colonic tissue levels, with enhanced activity when combined with dihydroresveratrol[2].
Lunularin (0.5×-1.5×; 30.25-90.75 nmol/g) dose-dependently inhibits LPS-induced NO production in RAW264.7 mouse macrophages, with enhanced activity when combined with dihydroresveratrol at concentrations relevant to colonic tissue levels[2].
Lunularin (0.5×-1.5×; 30.25-90.75 nmol/g) dose-dependently inhibits LPS-induced SEAP production in HEK-Blue mTLR-4 cells (targeting the TLR-4-mediated NF-κB pathway), with greater activity than resveratrol alone at concentrations relevant to colonic tissue levels[2].
Lunularin (20-100 μM; 30 min to standard assay conditions) competitively inhibits human liver microsomal 11β-HSD1 with an IC50 of 45.44 μM and a Ki of 35.8 μM by binding to the enzyme's steroid-binding site[4].
Lunularin (12.5-100 μM; 30 min to standard assay conditions) acts as a mixed inhibitor of rat liver microsomal 11β-HSD1 with an IC50 of 17.39 μM and a Ki of 10.31 μM by binding to the enzyme's combined NADPH and steroid-binding region[4].
Lunularin does not inhibit mouse liver microsomal 11β-HSD1 activity[4].

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

Lunularin Related Antibodies
In Vivo

Lunularin (24 mg/kg; intraperitoneal injection; 3 times per week; 8 weeks) in 13-month-old C57BL/6JRj mice on a high fat, high sugar diet slightly reduces feed intake and body weight gain, lowers blood glucose levels, and increases hepatic Sirt1 and Hmox1 mRNA expression, but does not mimic the full metabolic effects of caloric restriction[1].
Lunularin is a gut microbiota-derived metabolite of resveratrol, is highly abundant in mouse tissues, biological fluids, and gastrointestinal tract compared to resveratrol itself, and is eliminated when gut microbiota is depleted via antibiotics[2].

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

Animal Model: C57BL/6JRj (13-month-old, diet-induced obesity model)[1]
Dosage: 24 mg/kg
Administration: intraperitoneal injection; 3 times per week; 8 weeks
Result: Slightly reduced feed intake to 2.81 ± 0.1 g per day.
Showed a highly significant reduction in body weight gain over the study period.
Had slightly lower blood glucose levels after 8 weeks of treatment.
Had significantly elevated hepatic Sirt1 mRNA levels
Had significantly elevated hepatic Hmox1 mRNA level.
Reached mean liver tissue concentrations of 28.8 pmol/g liver.
Did not alter plasma levels of cholesterol, insulin, leptin, or adiponectin; did not alter hepatic phosphorylated AMPK levels, major urinary protein levels, or hepatic mRNA levels of Pck1, Pgc1α, Foxo3, or Tnfα.
Molecular Weight

214.26

Formula

C14H14O2
CAS No.
Appearance

Solid

Color

White to off-white

SMILES

OC1=CC=C(CCC2=CC=CC(O)=C2)C=C1
Structure Classification
Initial Source
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

4°C, stored under nitrogen

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

Solvent & Solubility
In Vitro: 

DMSO : 100 mg/mL (466.72 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 4.6672 mL 23.3361 mL 46.6723 mL
5 mM 0.9334 mL 4.6672 mL 9.3345 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)

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

This equation is commonly abbreviated as: C1V1 = C2V2

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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: ≥ 2.5 mg/mL (11.67 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 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: ≥ 2.5 mg/mL (11.67 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 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: 99.87%

SDS (393 KB)

COA (244 KB) HNMR (134 KB) RP-HPLC (87 KB) MS (132 KB)

Handling Instructions (2659 KB)
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 4.6672 mL 23.3361 mL 46.6723 mL 116.6807 mL
5 mM 0.9334 mL 4.6672 mL 9.3345 mL 23.3361 mL
10 mM 0.4667 mL 2.3336 mL 4.6672 mL 11.6681 mL
15 mM 0.3111 mL 1.5557 mL 3.1115 mL 7.7787 mL
20 mM 0.2334 mL 1.1668 mL 2.3336 mL 5.8340 mL
25 mM 0.1867 mL 0.9334 mL 1.8669 mL 4.6672 mL
30 mM 0.1556 mL 0.7779 mL 1.5557 mL 3.8894 mL
40 mM 0.1167 mL 0.5834 mL 1.1668 mL 2.9170 mL
50 mM 0.0933 mL 0.4667 mL 0.9334 mL 2.3336 mL
60 mM 0.0778 mL 0.3889 mL 0.7779 mL 1.9447 mL
80 mM 0.0583 mL 0.2917 mL 0.5834 mL 1.4585 mL
100 mM 0.0467 mL 0.2334 mL 0.4667 mL 1.1668 mL
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Lunularin Related Classifications

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.

Keywords:

Lunularin37116-80-611β-HSDEndogenous Metabolite11beta-HSD11β-hydroxysteroid dehydrogenases11 beta-hydroxysteroid dehydrogenaseHmox111β-hydroxysteroid dehydrogenase 1human 11β-HSD1TLR4-mediated NF-κB pathwayrat 11β-HSD1micecolon cancer cellsSirt1liverrenal cancer cellsInhibitorinhibitorinhibit

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