[CAS NO. 484-12-8] Osthole
PRODUCTS SPECIFICATIONS [484-12-8]
DESCRIPTION [484-12-8]
Overview
| MDL | MFCD00076049 |
|---|---|
| Molecular Weight | 244.29 |
| Molecular Formula | C15H16O3 |
| SMILES | O=C1C=CC2=CC=C(OC)C(C/C=C(C)\C)=C2O1 |
9 Publications Citing Use of MCE
- [1]Acta Pharmacol Sin. 2019 May;40(5):608-619.
- [2]Acta Pharmacol Sin. 2018 Jan;39(1):74-84.
- [3]Acta Pharmacol Sin. 2017 Aug;38(8):1120-1128.
- [4]J Neurosci Res. 2019 Dec;97(12):1689-1705.
- [5]Invest Ophthalmol Vis Sci. 2020 Aug 3;61(10):38.
- [6]Front Physiol. 2018 Nov 21;9:1650.
- [7]J Healthc Eng. 2022 Mar 24;2022:7099097.
- [8]Biol Pharm Bull. 2020;43(9):1315-1323.
- [9]SSRN. 2021 Feb.
Summary
Osthole (Osthol) is a natural antihistamine alternative. Osthole may be a potential inhibitor of histamine H 1 receptor activity. Osthole also suppresses the secretion of HBV in cells.
IC50 & Target
Histamine H 1 receptor [1]
In Vitro
Osthole (p<0.0001) and Fexofenadine (p<0.001) inhibit increased HRH-1 mRNA expression induced by histamine in the study group. This result is also observed in cells cultured with histamine/Osthole; where combined substances decreased HRH-1 mRNA expression compared to histamine (p<0.0001) [1] . Assessment of cell viability does not detect obvious toxicity when Osthole is used at a dose up to 100 µM. However, when the dose reached 500 µM, Osthole started to show toxic effect. Based on these observations, Osthole is used in all in vitro studies at the dose range of 10 to 100 µM. Osthole dose-dependently promotes osteoblast differentiation, as shown by the upregulation of osteoblast differentiation marker genes such as type I collagen ( col1 ), bone sialoprotein ( BSP ) and osteocalcin ( OC ) (2 days of culture). Osthole promotes ALP activity in mouse primary osteoblasts in a dose-dependent manner [2] .
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
In Vivo
Subcutaneous injection of Osthole at a dose of 5 mg/kg per day onto mouse calvariae significantly stimulates local bone formation, as shown by histologic analysis of calvarial samples harvested 2 weeks after the last injection and stained with H&E orange G. Histomorphometric analysis reveals that Osthole has a significant effect on bone formation as potent as the positive control, the microtubule inhibitor TN-16. This effect, however, is not seen when Osthole is used at a dose of 1 mg/kg per day. Intraperitoneal injection of Osthole for 8 weeks significantly reverses bone loss in the ovariectomized rats. Histologic examination of the L4samples stained with trinitrophenol poinsettia demonstrates a partial recovery of the trabecular structure in ovariectomized rats treated with Osthole. Histomorphometric analysis shows that treatment with Osthole significantly increases total BMD, trabecular bone volume, and trabecular thickness and decreases trabecular separation [2] .
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Appearance
Solid
Source
Shipping
Room temperature in continental US; may vary elsewhere.
Storage
| Powder | -20°C | 3 years |
|---|---|---|
| 4°C | 2 years | |
| In solvent | -80°C | 6 months |
| -20°C | 1 month |
Solvent & Solubility
DMSO : ≥ 100 mg/mL ( 409.35 mM )
* "≥" means soluble, but saturation unknown.
Stock Solutions
| Concentration Solvent Mass | 1 mg | 5 mg | 10 mg |
|---|
| 1 mM | 4.0935 mL | 20.4675 mL | 40.9350 mL |
| 5 mM | 0.8187 mL | 4.0935 mL | 8.1870 mL |
| 10 mM | 0.4093 mL | 2.0467 mL | 4.0935 mL |
References
- [1] Kordulewska NK, et al. Changes in gene expression induced by histamine, fexofenadine and osthole: Expression of histamine H1 receptor, COX-2, NF-κB, CCR1, chemokine CCL5/RANTES and interleukin-1β in PBMC allergic and non-allergic patients. Immunobiology.
- [2] Tang DZ, et al. Osthole stimulates osteoblast differentiation and bone formation by activation of beta-catenin-BMP signaling. J Bone Miner Res. 2010 Jun;25(6):1234-45.
- [3] Sun W, et al. Osthole pretreatment alleviates TNBS-induced colitis in mice via both cAMP/PKA-dependent and independent pathways. Acta Pharmacol Sin. 2017 Aug;38(8):1120-1128.
- [4] Zhang ZR, et al. Osthole: A Review on Its Bioactivities, Pharmacological Properties, and Potential as Alternative Medicine. Evid Based Complement Alternat Med. 2015;2015:919616.
Synonyms