2. Anti-infection MAPK/ERK Pathway Apoptosis Cell Cycle/DNA Damage Epigenetics Immunology/Inflammation NF-κB
  3. Bacterial p38 MAPK Apoptosis PARP Bcl-2 Family Caspase Interleukin Related COX PERK JNK NF-κB NO Synthase SOD
  4. Continentalic acid

Continentalic acid is a diterpenoid organic acid. Continentalic acid exhibits multiple activities including anti-inflammatory, antioxidant, neuroprotective, antibacterial and antitumor effects. Continentalic acid alleviates oxidative stress, reduces pro-inflammatory cytokine production, inhibits MAPK phosphorylation and neutrophil infiltration, and induces growth inhibition and apoptosis of cancer cells. Continentalic acid can be used in research related to traumatic brain injury, cancer, inflammation and infections.

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

Continentalic acid

Continentalic acid Chemical Structure

CAS No. : 19889-23-7

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Other Forms of Continentalic acid:

Continentalic acid Related Antibodies

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p38 MAPK Akt1 p38α p38β MAPK13 p38δ p38γ

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PARP PARP1 PARP2 PARP3 PARP4 TNKS1/PARP5A TNKS2/PARP5B PARP7 PARP10 PARP14 PARP15 PARP12 PARP16

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Bcl-2 Bcl-xL Bcl-W Mcl-1 Bfl-1 Bcl-B Bax Bak Bim BNIP3 Bad

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Caspase 1 Caspase 2 Caspase 3 Caspase 4 Caspase 5 Caspase 6 Caspase 7 Caspase 8 Caspase 9 Caspase 10 Caspase 12 Caspase Caspase 11 Caspase-13

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IL-1 IL-2 IL-3 IL-4 IL-5 IL-6 IL-8 IL-10 IL-12 IL-13 IL-15 IL-17 IL-23 IL-7 IL-33 IL-22 IL-18

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COX COX-1 COX-2 COX-3

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JNK1 JNK2 JNK3 JNK

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NF-κB NF-κB1/p50 RelA/p65 RelB c-Rel

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nNOS iNOS eNOS

  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

Description

Continentalic acid is a diterpenoid organic acid. Continentalic acid exhibits multiple activities including anti-inflammatory, antioxidant, neuroprotective, antibacterial and antitumor effects. Continentalic acid alleviates oxidative stress, reduces pro-inflammatory cytokine production, inhibits MAPK phosphorylation and neutrophil infiltration, and induces growth inhibition and apoptosis of cancer cells. Continentalic acid can be used in research related to traumatic brain injury, cancer, inflammation and infections[1][2][3][4][5].

In Vitro

Continentalic acid (10-100 μM; 24-72 h) inhibits the growth of human hepatocellular carcinoma HepG2 cells in a time- and dose-dependent manner, with an IC50 of 50 μM[1].
Continentalic acid (25-100 μM; 72 h) induces apoptosis in human hepatocellular carcinoma HepG2 cells, including morphological changes and DNA fragmentation[1].
Continentalic acid (10-100 μM; 48 h) regulates the expression of apoptosis-related proteins in human hepatoma HepG2 cells, upregulates the levels of caspase-3, Bak and Bax, induces PARP cleavage, and downregulates the level of Bcl-2[1].
Continentalic acid (1-20 μM) dose-dependently inhibits the production of IL-6, IL-8, MMP-13, COX-2 and PGE2 stimulated by IL-1β in human osteoarthritic chondrocytes[3].
Continentalic acid (1-20 μM; 24 h) dose-dependently inhibits the phosphorylation of p38, ERK1/2 and JNK mitogen-activated protein kinases (MAP kinases) in IL-1β-stimulated human osteoarthritic chondrocytes[3].
Continentalic acid (10 μM) inhibits IL-1β-induced nuclear translocation of NF-κB/p65 in human osteoarthritic chondrocytes after 1 h of incubation[3].
Continentalic acid (8-16 µg/mL; 24 h) potently inhibits the growth of methicillin-sensitive Staphylococcus aureus ATCC 25923, methicillin-resistant Staphylococcus aureus ATCC 33591, and 12 clinical methicillin-resistant Staphylococcus aureus (MRSA) isolates, with an MIC value of 8-16 µg/mL[4].

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

Continentalic acid Related Antibodies

Apoptosis Analysis[1]

Cell Line: human hepatocarcinoma HepG2 cells
Concentration: 10, 25, 50, 100 μM
Incubation Time: 72 h
Result: Induced distinct apoptotic morphological changes in HepG2 cells by 72 h, including cell shrinkage, nuclear and cytoplasmic condensation, chromatin condensation, and polylobation or fragmentation of nuclei.
Caused visible apoptotic changes in cells treated with 25, 50, and 100 μM continentalic acid.\nInduced dose-dependent DNA ladder formation in HepG2 cells after 72 h of incubation.
Caused clear laddering observed at concentrations of 25, 50, and 100 μM.

Western Blot Analysis[3]

Cell Line: IL-1β-stimulated human osteoarthritis (OA) chondrocytes
Concentration: 1, 3, 5, 10, 20 μM
Incubation Time: 24 h
Result: Significantly inhibited IL-1β-stimulated phosphorylation of p38, ERK1/2, and JNK protein kinases in a dose-dependent manner.
In Vivo

Continentalic acid (10-100 mg/kg; i.p.; single administration 30 min prior to LPS treatment) exerts a dose-dependent protective effect against LPS (HY-D1056)-induced acute lung injury in BALB/c mice[2].
Continentalic acid (0.97 mg/kg; i.p.; once daily; for 30 consecutive days) exerts significant anti-arthritic efficacy in MIA-induced osteoarthritis rats, restores weight-bearing balance, and prevents cartilage damage and proteoglycan loss[3].
Continentalic acid (1-50 mg/kg; i.p.; once daily for 14 consecutive days) exerts potent neuroprotective activity in a mouse traumatic brain injury (TBI) model[5].

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

Animal Model: BALB/c mice (6-week-old male, 27-33 g, traumatic brain injury weight-drop model)[5]
Dosage: 1 mg/kg; 10 mg/kg; 50 mg/kg
Administration: i.p.; daily; 14 days
Result: Reduced neurological severity score.
Restored paw withdrawal threshold.
Reduced cortical histopathological damage, increased neuronal count, and reduced cerebral microbleeds compared to the TBI group.
Downregulated mRNA and protein expression of GFAP, Iba1, TLR4, NF-κB, and cleaved caspase-3; upregulated mRNA and protein expression of IκB-α and Bcl-2 compared to the TBI group.
Reduced TBI-induced DNA damage compared to the TBI group.
Reduced levels of NO, LPO, IL-1β, and TNF-α; increased levels of GST, GSH, catalase, and SOD compared to the TBI group.
Animal Model: BALB/c (male, 3-4 weeks old, 22-26 g, LPS-induced acute lung injury)[2]
Dosage: 10 mg/kg; 50 mg/kg; 100 mg/kg
Administration: i.p.; single dose 30 minutes pre-LPS
Result: Achieved an 80% 24-hour survival rate at 100 mg/kg (vs. 20% in LPS-only group); showed no protective effect on mortality at 10 mg/kg.
Significantly reduced LPS-induced pyrexia at 50 mg/kg and 100 mg/kg).
Reduced lung wet/dry ratio dose-dependently at all three doses, with marked inhibition at 100 mg/kg.
Significantly elevated lung tissue levels of GSH, GST, catalase, and SOD at all three doses, with largest increases at 100 mg/kg.
Significantly reduced lung tissue MDA levels and both plasma and lung tissue NO levels at all three doses, with effects increasing with dose.
Significantly inhibited LPS-induced increases in lung tissue IL-1β, IL-6, and TNF-α at all three doses.
Normalized total neutrophil counts (NEU) to near control levels at 50 mg/kg and 100 mg/kg; normalized WBC counts to control levels at 100 mg/kg.
Reduced lung injury scores dose-dependently; reduced neutrophilic infiltration and improved tracheal architecture at these doses.
Reduced lung tissue MPO activity at all three doses, with significant inhibition at 100 mg/kg.
Significantly reduced lung tissue iNOS expression and significantly increased Nrf2 protein expression at 100 mg/kg.
Molecular Weight

302.45

Formula

C20H30O2
CAS No.
Appearance

Solid

Color

White to off-white

SMILES

C[C@]12[C@@](CCC3=C[C@](C=C)(C)CC[C@@]23[H])([H])[C@@](C)(CCC1)C(O)=O
Structure Classification
Initial Source
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

4°C, protect from light

*In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)

Solvent & Solubility
In Vitro: 

DMSO : 100 mg/mL (330.63 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 3.3063 mL 16.5317 mL 33.0633 mL
5 mM 0.6613 mL 3.3063 mL 6.6127 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 (protect from 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    40% PEG300    5% Tween-80    45% Saline

    Solubility: 2.5 mg/mL (8.27 mM); Suspended solution; Need ultrasonic

    This protocol yields a suspended solution of 2.5 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 (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 (8.27 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
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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).

*In solvent : -80°C, 6 months; -20°C, 1 month (protect from 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
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 (protect from 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 3.3063 mL 16.5317 mL 33.0633 mL 82.6583 mL
5 mM 0.6613 mL 3.3063 mL 6.6127 mL 16.5317 mL
10 mM 0.3306 mL 1.6532 mL 3.3063 mL 8.2658 mL
15 mM 0.2204 mL 1.1021 mL 2.2042 mL 5.5106 mL
20 mM 0.1653 mL 0.8266 mL 1.6532 mL 4.1329 mL
25 mM 0.1323 mL 0.6613 mL 1.3225 mL 3.3063 mL
30 mM 0.1102 mL 0.5511 mL 1.1021 mL 2.7553 mL
40 mM 0.0827 mL 0.4133 mL 0.8266 mL 2.0665 mL
50 mM 0.0661 mL 0.3306 mL 0.6613 mL 1.6532 mL
60 mM 0.0551 mL 0.2755 mL 0.5511 mL 1.3776 mL
80 mM 0.0413 mL 0.2066 mL 0.4133 mL 1.0332 mL
100 mM 0.0331 mL 0.1653 mL 0.3306 mL 0.8266 mL
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Continentalic acid 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:

Continentalic acid19889-23-7Bacterialp38 MAPKApoptosisPARPBcl-2 FamilyCaspaseInterleukin RelatedCOXPERKJNKNF-κBNO SynthaseSODpoly ADP ribose polymerase ILCyclooxygenaseProtein kinase R-like endoplasmic reticulum kinasePKR-like endoplasmic reticulum kinasec-Jun N-terminal kinaseNuclear factor-κBNuclear factor-kappaBNitric oxide synthasesNOSSuperoxide DismutaseiNOSIκB-αcleaved caspase-3GFAPcaspase-3Bcl-2BakTLR-4Iba1Inhibitorinhibitorinhibit

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