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  4. Isorhynchophylline

Isorhynchophylline is an alkaloid isolated from Crocus sativus with anticancer, antihypertensive, anti-inflammatory, and neuroprotective properties. Isorhynchophylline can be applied to cardiovascular and neurological disorders, and cancer studies.

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Isorhynchophylline Chemical Structure

Isorhynchophylline Chemical Structure

CAS No. : 6859-01-4

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Based on 1 publication(s) in Google Scholar

Other Forms of Isorhynchophylline:

Isorhynchophylline Related Antibodies

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  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

Description

Isorhynchophylline is an alkaloid isolated from Crocus sativus with anticancer, antihypertensive, anti-inflammatory, and neuroprotective properties. Isorhynchophylline can be applied to cardiovascular and neurological disorders, and cancer studies[1][2][3][4][5][6][7][8][9][10][11][12][13].

Cellular Effect
Cell Line Type Value Description References
HL-60 IC50
> 40 μM
Compound: 6
Cytotoxicity against human HL60 cells after 48 hrs by MTT assay
Cytotoxicity against human HL60 cells after 48 hrs by MTT assay
[PMID: 21070010]
Microglia IC50
19 μM
Compound: 6
Inhibition of LPS-stimulated NO release in rat cortical microglial cells assessed as nitrite accumulation after 48 hrs
Inhibition of LPS-stimulated NO release in rat cortical microglial cells assessed as nitrite accumulation after 48 hrs
[PMID: 18588343]
SW480 IC50
> 40 μM
Compound: 6
Cytotoxicity against human SW480 cells after 48 hrs by MTT assay
Cytotoxicity against human SW480 cells after 48 hrs by MTT assay
[PMID: 21070010]
In Vitro

Isorhynchophylline (0.0625-40 µM, 48 h) shows cytotoxicity against human HL60 cells and SW480 cells (MTT assay), with IC50s greater than 40 μM[1].
Isorhynchophylline (3-15 µg/mL, 48 h) inhibits LPS-stimulated NO release in rat cortical microglial cells assessed as nitrite accumulation[2].
Isorhynchophylline (0.1-10.0 μM, 24 h) effectively inhibits angiotensin II-induced proliferation in rat vascular smooth muscle cells, at least in part, due to increased NO production and regulation of the cell cycle[3].
Isorhynchophylline (0-300 μM, 48 h) exerts anticancer and anti-metastatic effects through regulation of multiple signaling cascades (abatement of phospho-p38, etc.) in hepatocellular carcinoma cells [4].
Isorhynchophylline (1-50 μM, 2 h) protects PC12 cells against Beta-Amyloid-induced apoptosis via PI3K/Akt signaling pathway[5].
Isorhynchophylline (1-80 μM, 24 h) attenuates proliferation and migration of synovial fibroblasts via the FOXC1/β-catenin axis[6].
Isorhynchophylline (5-200 μM, 48 h) alleviates cartilage degeneration in osteoarthritis by activating autophagy in chondrocytes[7].
Isorhynchophylline (30 μM, 24 h) relieves ferroptosis-induced nerve damage after intracerebral hemorrhage via miR-122-5p/TP53/SLC7A11 pathway in hippocampal HT-22 cells[8].

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

Isorhynchophylline Related Antibodies

Cell Viability Assay[3]

Cell Line: Rat vascular smooth muscle cells treated with Ang II (1.0 μM)
Concentration: 0.1, 1, 10 μM
Incubation Time: 24 h
Result: Attenuated Ang II-induced cell proliferation in a concentration-dependent manner.
Abolished Ang-II induced VMSC proliferation at the highest concentration (10 μM).

Cell Cycle Analysis[3]

Cell Line: Rat vascular smooth muscle cells treated with Ang II (1.0 μM)
Concentration: 0.1, 1, 10 μM
Incubation Time: 24 h
Result: Significantly decreased the percentage of cells in S and G2/M phases, and increased the percentage of cells in G0/G1 phase (1.0 μM and 10.0 μM).

Real Time qPCR[3]

Cell Line: Rat vascular smooth muscle cells treated with Ang II (1.0 μM)
Concentration: 0.1, 1, 10 μM
Incubation Time: 24 h
Result: Suppressed the overexpression of c-fos mRNA in a concentration-dependent manner.
Decreased the over-expression of OPN and PCNA mRNA at 1.0 μM and 10.0 μM.
In Vivo

Isorhynchophylline (20-40 mg/kg, i.g., daily, 8 weeks) ameliorates D-galactose (HY-N0210)-induced learning and memory deficits in mice, at least in part, by enhancing the antioxidant status and anti-inflammatory effects of brain tissue through inhibition of NFκB signaling[9].
Isorhynchophylline (50 μM, the first day of every week from the 5th to the 8th week after surgery) alleviates osteoarthritis in rat osteoarthritis models, with decreasing OARSI score and the reduction of joint space[7].
Isorhynchophylline (10-40 mg/kg, i.g., 7 days) exerts antidepressant-like effects in mice at least in part by inhibiting monoamine oxidase[10].
Isorhynchophylline (20-40 mg/kg, i.g., daily, 8 weeks) alleviates learning and memory impairments induced by aluminum chloride in mice[11].
Isorhynchophylline (20  mg/kg, i.p., 14 or 42 days) alleviates silicon-dioxide-induced lung injury in mice, with reducing inflammatory responses and fibrosis[12].

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

Animal Model: D-galactose-induced cognitive deficits (Ten-week-old male ICR mice received a daily subcutaneous injection of D-gal at a dose of 100 mg/kg for 8 weeks)[9]
Dosage: 20, 40 mg/kg
Administration: Given intragastrically (i.g.), daily, 8 weeks
Result: Shortened the mean latency to find the platform at the 4th day (20 mg/kg).
Led to a significant increase in the number of target crossings (40 mg/kg).
Attenuated oxidative stress (enhanced the level of GSH, attenuated MDA).
Decreased the production of NO and the mRNA expression of iNOS in the brain (40 mg/kg).
Decreased the production of PGE2 and the mRNA expression of COX-2 (40 mg/kg).
Suppressed the protein level of p-IκBα (40 mg/kg).
Molecular Weight

384.47

Formula

C22H28N2O4
CAS No.
Appearance

Solid

Color

White to off-white

SMILES

O=C(NC1=C2C=CC=C1)[C@@]32[C@@](C[C@H](/C(C(OC)=O)=C\OC)[C@@H](CC)C4)([H])N4CC3
Structure Classification
Initial Source
Shipping

Room temperature in continental US; may vary elsewhere.
Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 2 years
-20°C 1 year
Solvent & Solubility
In Vitro: 

DMSO : 100 mg/mL (260.10 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 2.6010 mL 13.0049 mL 26.0098 mL
5 mM 0.5202 mL 2.6010 mL 5.2020 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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

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

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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: ≥ 2.75 mg/mL (7.15 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.75 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (27.5 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% Corn Oil

    Solubility: ≥ 2.75 mg/mL (7.15 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.75 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (27.5 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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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).
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: 99.82%

SDS (479 KB)

COA (251 KB) LCMS (95 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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 2.6010 mL 13.0049 mL 26.0098 mL 65.0246 mL
5 mM 0.5202 mL 2.6010 mL 5.2020 mL 13.0049 mL
10 mM 0.2601 mL 1.3005 mL 2.6010 mL 6.5025 mL
15 mM 0.1734 mL 0.8670 mL 1.7340 mL 4.3350 mL
20 mM 0.1300 mL 0.6502 mL 1.3005 mL 3.2512 mL
25 mM 0.1040 mL 0.5202 mL 1.0404 mL 2.6010 mL
30 mM 0.0867 mL 0.4335 mL 0.8670 mL 2.1675 mL
40 mM 0.0650 mL 0.3251 mL 0.6502 mL 1.6256 mL
50 mM 0.0520 mL 0.2601 mL 0.5202 mL 1.3005 mL
60 mM 0.0433 mL 0.2167 mL 0.4335 mL 1.0837 mL
80 mM 0.0325 mL 0.1626 mL 0.3251 mL 0.8128 mL
100 mM 0.0260 mL 0.1300 mL 0.2601 mL 0.6502 mL
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Isorhynchophylline 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:

Isorhynchophylline6859-01-4SODNF-κBSuperoxide DismutaseNuclear factor-κBNuclear factor-kappaBLearning and memory impairmentsAntioxidantAnti-inflammatoryHL60SW480CytotoxicityICRInhibitorinhibitorinhibit

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