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Synonym name:
Catalogue No.: BP0512
Cas No.: 73069-25-7
Formula: C21H22O7
Mol Weight: 386.4
Botanical Source: Peucedanum praeruptorum
Purity: 95%~99%
Analysis Method: HPLC-DAD or/and HPLC-ELSD
Identification Method: Mass, NMR
Packing: Brown vial or HDPE plastic bottle
Can be supplied from milligrams to grams.
For Reference Standard and R&D, Not for Human Use Directly.
Inquire for bulk scale.
Description:
Praeruptorin A exerts neuroprotective, anti-osteoclastogenic, anti-inflammatory, distinct relaxant effects, it is beneficial to facilitate nestin expression in myocarditis,and suitable in treatment of early myocarditis. Praeruptorin A can significantly up-regulate UGT1A1 expression in HepG2 cells partially via the CAR-mediated pathway. Praeruptorin A inhibited p38/Akt-c-Fos-NFATc1 signaling and PLCγ-independent Ca2+ oscillation.
References:
J Nat Prod. 2015 Apr 24;78(4):776-82.
Praeruptorin a inhibits in vitro migration of preosteoclasts and in vivo bone erosion, possibly due to its potential to target calmodulin.
Excessive activity and/or increased number of osteoclasts lead to bone resorption-related disorders. Here, we investigated the potential of Praeruptorin A to inhibit migration/fusion of preosteoclasts in vitro and bone erosion in vivo.
METHODS AND RESULTS:
Praeruptorin A inhibited the RANKL-induced migration/fusion of preosteoclasts accompanied by the nuclear translocation of NFATc1, a master regulator of osteoclast differentiation. Antimigration/fusion activity of Praeruptorin A was also confirmed by evaluating the mRNA expression of fusion-mediating molecules. In silico binding studies and several biochemical assays further revealed the potential of Praeruptorin A to bind with Ca(2+)/calmodulin and inhibit its downstream signaling pathways, including the Ca(2+)/calmodulin-CaMKIV-CREB and Ca(2+)/calmodulin-calcineurin signaling axis responsible for controlling NFATc1. In vivo application of Praeruptorin A significantly reduced lipopolysaccharide-induced bone erosion, indicating its possible use to treat bone resorption-related disorders.
CONCLUSIONS:
In conclusion, Praeruptorin A has the potential to inhibit migration/fusion of preosteoclasts in vitro and bone erosion in vivo by targeting calmodulin and inhibiting the Ca(2+)/calmodulin-CaMKIV-CREB-NFATc1 and/or Ca(2+)/calmodulin-calcineurin-NFATc1 signaling axis.
PLoS One. 2014 Feb 21;9(2):e88974.
Anti-osteoclastogenic activity of praeruptorin A via inhibition of p38/Akt-c-Fos-NFATc1 signaling and PLCγ-independent Ca2+ oscillation.
A decrease of bone mass is a major risk factor for fracture. Several natural products have traditionally been used as herbal medicines to prevent and/or treat bone disorders including osteoporosis. Praeruptorin A is isolated from the dry root extract of Peucedanum praeruptorum Dunn and has several biological activities, but its anti-osteoporotic activity has not been studied yet.
METHODS AND RESULTS:
The effect of Praeruptorin A on the differentiation of bone marrow-derived macrophages into osteoclasts was examined by phenotype assay and confirmed by real-time PCR and immunoblotting. The involvement of NFATc1 in the anti-osteoclastogenic action of Praeruptorin A was evaluated by its lentiviral ectopic expression. Intracellular Ca(2+) levels were also measured. Praeruptorin Ainhibited the RANKL-stimulated osteoclast differentiation accompanied by inhibition of p38 and Akt signaling, which could be the reason for Praeruptorin A-downregulated expression levels of c-Fos and NFATc1, transcription factors that regulate osteoclast-specific genes, as well as osteoclast fusion-related molecules. The anti-osteoclastogenic effect of Praeruptorin A was rescued by overexpression of NFATc1. Praeruptorin A strongly prevented the RANKL-induced Ca(2+) oscillation without any changes in the phosphorylation of PLCγ.
CONCLUSIONS:
Praeruptorin A could exhibit its anti-osteoclastogenic activity by inhibiting p38/Akt-c-Fos-NFATc1 signaling and PLCγ-independent Ca(2+) oscillation.
Phytother Res. 2011 Apr;25(4):550-6.
Praeruptorin A inhibits lipopolysaccharide-induced inflammatory response in murine macrophages through inhibition of NF-κB pathway activation.
Praeruptorin A (PA) is a pyranocoumarin compound isolated from the dried root of Peucedanum praeruptorum Dunn (Umbelliferae). However, the antiinflammatory effect of PA has not been reported.
METHODS AND RESULTS:
The present study investigated the antiinflammatory effect of PA in lipopolysaccharide (LPS)-stimulated RAW 264.7 macrophage cells. PA significantly inhibited the LPS-induced production of nitric oxide (NO), interleukin-1β (IL-1β) and tumor necrosis factor-α (TNF-α). The mRNA and protein expressions of inducible nitric oxide synthase (iNOS), IL-1β and TNF-α were also suppressed by this compound. Further study showed that PA decreased the cytoplasmic loss of inhibitor κB-α (IκB-α) protein and inhibited the translocation of NF-κB from cytoplasm to nucleus.
CONCLUSIONS:
Taken together, the results suggest that PA may exert antiinflammatory effects in vitro in LPS-stimulated RAW 264.7 macrophages through inhibition of NF-κB signal pathway activation.
Pharmacology & Clinics of Chinese Materia Medica, 2007, 23(3):21-3.
Praeruptorin A upregulates expression of nestin in experimental autoimmune myocarditis of rats
To investigate the influence of dl-Praeruptorin A(Pd-Ia) on expression of intermediate filament protein nestin and its cardioprotective actions in myocarditis.[WT5"HZ]
METHODS AND RESULTS:
Effect of Pd-Ia on expression of nestin was evaluated in rats that had recovered from experimental autoimmune myocarditis(EAM).Wistar rats were divided into 5 groups,including group sham,group natural saline,group solvent control(polyethylene glycol),group Pd-Ia 1.0 mg/kg,and group positive control(verapamil0.5 mg/kg),respectively.Thereafter,all animals were immunized with pig cardiac myosin on day 0.Drugs were administered twice through abdominal cavity on day 20 and day 21,respectively.Four hours after second administration,rats are executed.Expression of nestin in myocardium was detected by Western blot analysis.Heart weight/body weight ratio,myocardial enzyme spectrum,and histopathology were measured simultaneously. Results:Pd-Ia upregulated expression of nestin and relieved myocardial injury in EAM of rats.Values of relative optic density in Pd-Ia(1.0 mg/kg) group were increased from 37.5 ± 3 to 61 ± 4(P0.05,vs solvent,n=5).
CONCLUSIONS:
[WT5"BZ] Pd-Ia was beneficial to facilitate nestin expression in myocarditis,and suitable in treatment of early myocarditis.
Storage conditions：Short-term storage at 2~8℃, long-term storage at -20 ~ -80℃
92.0400
3.1854
3.1854
.0151
3.0194
6.7647
High
85.3997
3.7180
Yes
Yes
No
No
No
Yes
0.0
No
Yes
Yes
Yes
DL-Praeruptorin A (CAS No.: 73069-25-7) is an important natural compound derived from the traditional Chinese medicinal herb Peucedanum (Peucedanum praeruptorum Dunn), belonging to the furanocoumarin-class compounds. In recent years, with the rapid development of natural product pharmacology and molecular targeted therapy, Baihua Qianhujiasin has attracted widespread attention due to its multi-target and multi-mechanism biological activity, especially its potential therapeutic effects in malignant tumors such as liver cancer. Liver cancer, a malignant tumor with high incidence and mortality rates worldwide, has complex molecular mechanisms and drug resistance issues that prompt researchers to continuously explore new treatment strategies. Baihua Qianhujia Methyl demonstrates strong anti-tumor potential by regulating multiple key oncogenes and signaling pathways, making it an important candidate for natural drug development.
This paper will systematically review the chemical structure and physicochemical properties of White-flowered Qianhujiasu, plant origin and extraction methods, pharmacological activity studies, mechanisms of action and molecular targets, druggability evaluation and pharmacokinetics, as well as its clinical application prospects and development prospects, aiming to provide a theoretical foundation and reference for in-depth research and clinical translation of this compound.
White-flowered pre-horaxin belongs to the furanocoumarin-class compounds, with a molecular formula of C_22H_26O_6 and a molecular weight of 386.40. Its chemical structure features the combination of furan rings with the coumarin-backed framework, forming a unique dihydrofuranocoumarin. This structure gives it good lipid solubility and a bioactive basis.
In terms of physicochemical properties, the LogP value of White-flowered Frontal-Cercosin is 3.1854, indicating moderate lipid solubility, which facilitates cell membrane penetration and distribution in vivo. Its topological pole surface area (TPSA) is 92.04 Ų, indicating moderate molecular polarity, which may affect oral absorption and blood-brain barrier permeability. Low water solubility (0.0151 mg/mL) suggests limited solubility in the aqueous phase, suggesting that bioavailability may be improved through formulation optimization. Notably, White-flowered Qianhujia has a high blood-brain barrier penetration ability, suggesting its potential application value in central nervous system diseases. Additionally, the hERG channel inhibition test results were negative, indicating a low risk of cardiotoxicity; The Ames test was negative, indicating no significant genotoxicity.
White-flowered Frontal-Leaf Methylene is mainly found in the roots of the Umbelliferae plant Peucedanum (Peucedanum praeruptorum Dunn), with a higher content in White-flowered Yellow-Flowered Leaf varieties. Qianhu is widely used in traditional Chinese medicine to dispel wind and cold, promote lung function, and stop cough, attracting attention due to its abundance of furanocoumarin-type compounds.
The extraction method typically uses organic solvent extraction combined with chromatography separation technology. Common extraction processes include:
In recent years, with the development of green chemistry and process optimization, new technologies such as supercritical CO_2 extraction and microwave-assisted extraction have also been applied to the extraction of White-flowered Qiaohujia, significantly improving extraction efficiency and purity, and reducing environmental pollution.
Baihua Qianhujia has multiple biological activities, especially outstanding in anti-tumor, anti-inflammatory, antioxidant, and neuroprotective properties. His research in the field of liver cancer is particularly in-depth, mainly reflected in the following aspects:
Multiple in vitro cell experiments and in vivo animal model studies have shown that Alucanda Cyphalin can significantly inhibit the proliferation, migration, and invasion of liver cancer cells, inducing apoptosis. Its anti-tumor effects are closely related to the regulation of various key oncogenes and signaling pathways.
White-flowered precursor exerts anti-inflammatory effects by inhibiting the expression of inflammatory mediators such as PTGS2 (COX-2), reducing inflammatory responses. At the same time, it has the ability to scavenge free radicals, reduce oxidative stress damage, and protect cellular function.
Due to its excellent blood-brain barrier penetration, Baihua Qianhujiasin also shows potential in neuroprotection, reducing nerve cell damage, inhibiting neuroinflammation, and improving neurological dysfunction.
The mechanism of Baihua Qianhujia's anti-liver cancer mechanism involves multiple signaling pathways and key molecular targets, mainly including:
Through the synergistic effect of these multi-target and multi-pathway approaches, Baihua Qianhujiasin effectively inhibits the occurrence and progression of liver cancer, demonstrating a complex and comprehensive anti-tumor mechanism.
The druggability evaluation of Baihua Qianhujiasin shows it has good potential for drug development:
In terms of pharmacokinetics, existing studies show that Baihua Qianhujia has good absorption and distribution characteristics in the body, but its metabolic and excretion pathways have not been fully elucidated. Preliminary data suggest it is mainly metabolized by the liver and may involve the cytochrome P450 enzyme system; the activity and toxicity of these metabolites require further study. Additionally, low water solubility and potential first-pass effects may affect oral bioavailability, requiring optimization through novel delivery systems such as nanoformulations and solid dispersions.
As a multi-target natural product, White-flowered Qianhujia has significant anti-liver cancer activity and good safety, showing potential as a novel anti-tumor drug. The future clinical application prospects are mainly reflected in the following aspects:
However, clinical research on White-flowered Qianhujiasin is still in its early stages, and systematic pharmacokinetics, toxicological evaluations, and clinical trial data are still lacking. In the future, research on its pharmacodynamics, pharmacokinetics, and safety should be strengthened to promote its transition from laboratory to clinical application.
As a natural product with a unique chemical structure and multiple biological activities, Baihua Qianhujia shows broad application prospects in the treatment of major diseases such as liver cancer. Its multi-target and multi-mechanism mode of action provides new ideas and directions for the development of natural anti-tumor drugs. Although significant progress has been made in research on Baihua Qianhujiasu, further improvement in pharmacokinetics, toxicology, and clinical validation is needed to promote its safe and effective clinical use. In the future, by integrating modern medicinal chemistry, molecular biology, and pharmaceutical technologies, Baihua Qianhujiasu is expected to become a major breakthrough in the field of natural product pharmacology, bringing new treatment hope to liver cancer patients.
Shenshuai
Wenjing
Hedandan
