1. Apoptosis
  2. Apoptosis
  3. Leachianone A

Leachianone A, isolated from Radix Sophorae, has anti-malarial, anti-inflammatory, and cytotoxic potent. Leachianone A induces apoptosis involved both extrinsic and intrinsic pathways.

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Leachianone A Chemical Structure

Leachianone A Chemical Structure

CAS No. : 97938-31-3

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Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
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Based on 1 publication(s) in Google Scholar

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Description

Leachianone A, isolated from Radix Sophorae, has anti-malarial, anti-inflammatory, and cytotoxic potent[1]. Leachianone A induces apoptosis involved both extrinsic and intrinsic pathways[2].

Cellular Effect
Cell Line Type Value Description References
HL-60 IC50
11.3 μM
Compound: 4
Cytotoxicity against human HL60 cells after 96 hrs by MTT assay
Cytotoxicity against human HL60 cells after 96 hrs by MTT assay
[PMID: 10843587]
RAW264.7 IC50
11.3 μM
Compound: 13
Antiinflammatory activity in mouse RAW264.7 cells assessed as inhibition of LPS-stimulated nitric oxide production after 24 hrs by Griess method
Antiinflammatory activity in mouse RAW264.7 cells assessed as inhibition of LPS-stimulated nitric oxide production after 24 hrs by Griess method
[PMID: 26073007]
In Vitro

Leachianone A (0-20 μg/ml; 24-72 hours) exhibits a marked inhibition on the survival of HepG2 cells time- and dose-dependently manner, IC50 values are 6.9 μg/ml, 3.4 μg/ml and 2.8 μg/ml in cells with 24-, 48- and 72-hours treatment, respectively[1].
Leachianone A (10-30 μg/ml; 48 hours) indicates that at low concentration of LA (10 μg/ml), a substantial amount of cells is primarily in the early phase of apoptosis, at higher concentrations, induces a shift of the cell population to late apoptotic/ necrotic stage[1].
Leachianone A (10-30 μg/ml; 48 hours) decreases the precursor of caspase-3 in a dose-dependent manner, reduces the protein level of the pro-forms of upstream initiator caspases, caspases-8 and -9, decreases two downstream substrates, namely inhibitor of caspase-activated DNase(ICAD) and poly-ADP-ribose polymerase (PARP) in HepG2 cells[1].

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

Cell Viability Assay[1]

Cell Line: HepG2 cells
Concentration: 0 μg/ml, 2 μg/ml, 4 μg/ml, 6 μg/ml, 8 μg/ml, 10 μg/ml, 12 μg/ml, 14 μg/ml, 16 μg/ml, 18 μg/ml, 20 μg/ml
Incubation Time: 24-72 hours
Result: Inhibited HepG2 cells survival.

Apoptosis Analysis[1]

Cell Line: HepG2 cells
Concentration: 48 hours
Incubation Time: 10, 20, and 30 μg/ml
Result: Induced the proportion of annexin V-stained cells in both the early and late apoptotic stage.

Western Blot Analysis[1]

Cell Line: HepG2 cells
Concentration: 48 hours
Incubation Time: 10, 20, and 30 μg/ml
Result: Decreased the protein expression of caspase-3, caspases-8 and -9, reduced ICAD and PARP protein expression.
In Vivo

Leachianone A (intravenously injection; 20 mg/kg, 30 mg/kg; once daily; 30 days) significantly diminishes the tumor volume by 17-54% in LA-treated nude mice, when compared with those solely given the vehicle[1].

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

Animal Model: Male nude mice with human hepatoma HepG2 cells[1]
Dosage: 20 mg/kg; 30 mg/kg
Administration: Intravenously injection; 20 mg/kg, 30 mg/kg; once daily; 30 days
Result: Suppressed the tumor growth in vivo.
Molecular Weight

438.51

Formula

C26H30O6

CAS No.
Appearance

Solid

Color

Off-white to light yellow

SMILES

O=C1C[C@@H](C2=CC=C(O)C=C2OC)OC3=C(C[C@H](C(C)=C)C/C=C(C)\C)C(O)=CC(O)=C13

Structure Classification
Initial Source
Shipping

Room temperature in continental US; may vary elsewhere.

Storage

4°C, sealed storage, away from moisture and light

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)

Solvent & Solubility
In Vitro: 

DMSO : 100 mg/mL (228.04 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 2.2804 mL 11.4022 mL 22.8045 mL
5 mM 0.4561 mL 2.2804 mL 4.5609 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 (sealed storage, away from moisture and light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

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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    90% Corn Oil

    Solubility: ≥ 5 mg/mL (11.40 mM); Clear solution

    This protocol yields a clear solution of ≥ 5 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 (50.0 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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(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:
%
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%
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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 (sealed storage, away from moisture and light)

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: 99.44%

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 (sealed storage, away from moisture and light). 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 2.2804 mL 11.4022 mL 22.8045 mL 57.0112 mL
5 mM 0.4561 mL 2.2804 mL 4.5609 mL 11.4022 mL
10 mM 0.2280 mL 1.1402 mL 2.2804 mL 5.7011 mL
15 mM 0.1520 mL 0.7601 mL 1.5203 mL 3.8007 mL
20 mM 0.1140 mL 0.5701 mL 1.1402 mL 2.8506 mL
25 mM 0.0912 mL 0.4561 mL 0.9122 mL 2.2804 mL
30 mM 0.0760 mL 0.3801 mL 0.7601 mL 1.9004 mL
40 mM 0.0570 mL 0.2851 mL 0.5701 mL 1.4253 mL
50 mM 0.0456 mL 0.2280 mL 0.4561 mL 1.1402 mL
60 mM 0.0380 mL 0.1900 mL 0.3801 mL 0.9502 mL
80 mM 0.0285 mL 0.1425 mL 0.2851 mL 0.7126 mL
100 mM 0.0228 mL 0.1140 mL 0.2280 mL 0.5701 mL
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    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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Leachianone A
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HY-N2281
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