Product name: Daphnetin
Synonym name: 7,8-Dihydroxycoumarin; Daphnetol
Catalogue No.: BP0449
Cas No.: 486-35-1
Formula: C₉H₆O₄
Mol Weight: 178.143
Botanical Source: Daphne koreanum Nakai
Physical Description:
Type of Compound: Coumarins

Purity: 95%~99%
Analysis Method: HPLC-DAD or/and HPLC-ELSD
Identification Method: Mass, NMR
Packing: Brown vial or HDPE plastic bottle

Storage: Store in a well closed container, protected from air and light. Put into refrigerate or freeze for long term storage.
Whenever possible, you should prepare and use solutions on the same day. However, if you need to make up stock solutions in advance, we recommend that you store the solution as aliquots in tightly sealed vials at -20℃. Generally, these will be useable for up to two weeks.

The product could be supplied from milligrams to grams
Inquire for bulk scale.




Chengdu Biopurify Phytochemicals Ltd. is a leading company in the research, development, manufacture and marketing of High Quality Phytochemicals and Extracts(especially Active Ingredients from Traditional Chinese Medicine，TCM), Natural Active Pharmaceutical Ingredients worldwide.
The main services:
A. Supply active ingredients and reference standards of TCM, from mgs to kgs scale
B. Custom extraction and purification, target Herb Active Ingredients
C. Custom synthesis and semi-synthesis for Natural Active Ingredients
D. CR(contract research), CM(contract manufacture) and PD(process development) services from lab scale, pilot scale to commercial scale(GMP is also available)
E. TCM compounds library for drug screen,more than 3000 compounds available, many of them are rare and unique.

NMR of Daphnetin

HPLC of Daphnetin

Storage conditions：Short-term storage at 2~8℃, long-term storage at -20 ~ -80℃

Introduction/Overview

Daphnetin (7,8-dihydroxycoumarin, CAS number: 486-35-1) is a natural coumarin-type compound, mainly found in plants of the genus Daphne. As an orally effective protein kinase inhibitor, daschinder has attracted attention for its multi-target, multi-pathway pharmacological activity. In recent years, with in-depth research into its mechanisms of anti-inflammatory, anti-tumor, antimalarial, and cell-protective effects, rychinde has shown broad application potential in the field of natural product pharmacology. This paper aims to systematically review the chemical structure and physicochemical properties of daphne extraction, plant origin and extraction methods, pharmacological activity and mechanism of action, druggability evaluation, and clinical application prospects, with the aim of providing theoretical basis and research directions for its subsequent drug development and clinical translation.

Chemical structure and physicochemical properties

The chemical structure of rychine is 7,8-dihydroxycoumarin, with the molecular formula C9H6O4 and a molecular weight of 178.14. Its structural core is the coumarin-based skeleton, and the presence of hydroxyl groups at the 7th and 8th positions gives it strong polarity and bioactivity. In terms of physicochemical properties, the LogP value of ryphasin is about 1.0, indicating moderate lipid solubility that facilitates cell membrane penetration. The polar surface area (TPSA) is 77.76 Ų, indicating a certain degree of water solubility and good hydrogen bond receptor capacity (four hydrogen bond receptors), which are crucial for binding to biological macromolecules. The molecular structure of daphne is stable, and it is not prone to hepatotoxicity, cardiotoxicity, or hERG channel inhibition, demonstrating good safety profiles.

Plant Origins and Extraction Methods

Daphne is mainly found in Daphne genkwa and Daphne odora. In traditional Chinese medicine, these plants are often used for anti-inflammatory, analgesic, and anti-tumor treatments, with daphne considered one of their main active ingredients.

The extraction method typically combines solvent extraction with chromatographic separation. Common extraction solvents include polar solvents such as ethanol, water, and methanol. The typical extraction process is:

1. Crush dried plant samples.
2. Extraction is performed using reflux or ultrasound-assisted extraction, with the extract concentrated.
3. Purification is performed by silica gel column chromatography or high-performance liquid chromatography (HPLC) to obtain high-purity ruquin.

In recent years, the application of supercritical CO2 extraction and membrane separation technologies has gradually improved extraction efficiency and purity, providing technical support for the industrial production of ryphan.

Pharmacological activity research

Daphne exhibits a variety of significant pharmacological activities, including anti-inflammation, anti-tumor, antimalarial, and cell protection.

Anti-inflammatory activity

Ruchinin can significantly inhibit the production of pro-inflammatory factors such as tumor necrosis factor-α (TNF-α) and interleukin-1β (IL-1β), reduce the generation of reactive oxygen species (ROS) and the lipid peroxidation product malondialdehyde (MDA), thereby alleviating inflammatory responses. This action gives daphin the potential of rheumatoid arthritis and other chronic inflammatory diseases.

Antitumor activity

Daphne exhibits inhibitory effects on various tumor cells, especially prominent in liver cancer cells. It promotes autophagy by inducing reactive oxygen species-mediated apoptosis and regulating the AMPK/Akt/mTOR signaling pathway, thereby inhibiting tumor cell proliferation and migration. In addition, romanin acts on various tumor-related targets such as BCL2, STAT3, TOP1, TERT, PIK3CA, MMP9, EGFR, TP53, NFKB1, and AKT1, exerting synergistic anti-cancer effects across multiple targets.

Antimalarial activity

Daphne has significant malaria-killing activity, inhibiting the growth and reproduction of malaria parasites, providing new ideas for the development of antimalarial drugs.

Cell protective effects

Daphthenin induces protective autophagy by modulating the AMPK/Akt/mTOR pathway, reducing oxidative stress damage and protecting cells from various pathological stimuli.

Mechanism of action and molecular targets

As a protein kinase inhibitor, daphin targets several key kinases, including epidermal growth factor receptor (EGFR), protein kinase A (PKA), and protein kinase C (PKC). Its IC50s are 7.67 μM, 9.33 μM, and 25.01 μM, respectively, demonstrating strong enzyme inhibitory activity.

In its anti-tumor mechanism, daphne works through the following pathways:

• Reactive oxygen species-induced apoptosis: Daphne promotes increased intracellular ROS levels, activates mitochondrial apoptosis pathways, and induces programmed death of tumor cells.
• Regulation of the AMPK/Akt/mTOR signaling pathway: Daphne activates AMPK, inhibits Akt and mTOR signaling, induces autophagy, and suppresses tumor cell proliferation.
• Multi-target regulation: Daphne comprehensively regulates cell growth, apoptosis, migration, and immune responses by regulating key targets such as BCL2 (anti-apoptotic protein), STAT3 (transcription factor), TOP1 (topoisomerase), TERT (telomerase), PIK3CA (PI3K subunit), MMP9 (matrix metalloproteinase), EGFR, TP53 (tumor suppressor protein), NFKB1 (nuclear factor κB), and AKT1.

In its anti-inflammatory mechanism, daphne inhibits the NF-κB signaling pathway, reduces the expression of pro-inflammatory factors, lowers oxidative stress, and alleviates inflammatory responses.

Druggability evaluation and pharmacokinetics

The molecular weight of ryphane is 178.14, which classifies it as a small molecule drug. Its LogP value is 1.0, indicating moderate lipid solubility, which is beneficial for oral absorption. The TPSA was 77.76, which fits the ideal range for oral bioavailability of the drug. It has 4 hydrogen bond receptors, meeting the requirements for effective binding between drug molecules and target proteins.

In terms of safety, daphne has no significant hepatotoxicity or cardiotoxicity, and does not inhibit hERG channels, reducing the risk of arrhythmias. The low permeability of the blood-brain barrier suggests a lower risk of side effects in the central nervous system, but also limits its application in brain diseases.

Currently, pharmacokinetic data on thyloxin are limited. Preliminary studies show good oral absorption, but metabolic pathways and clearance mechanisms in vivo require further study. Ames-induced mutagenic test results are still unclear, and additional genotoxicity assessments are needed.

Prospects and outlooks for clinical applications

With its multi-target and multi-mechanism pharmacological properties, Rychloquin has broad clinical application potential:

• Rheumatoid arthritis: By inhibiting inflammatory factors and oxidative stress, daphne is expected to become a new type of anti-inflammatory drug that improves chronic inflammation and alleviates joint damage.
• Liver cancer and other malignant tumors: The antitumor activity and multi-target regulation of daschinol offer new ideas for tumor treatment, especially in adjuvant therapy for drug-resistant and recurrent tumors.
• Antimalarial: As a natural malaria-killing active ingredient, daphne can be a candidate molecule for antimalarial drug development, especially in regions where drug-resistant malaria parasites are prevalent.
• Cell protection and antioxidant effects: By regulating autophagy and apoptosis, daphne may play a protective role in neurodegenerative and metabolic diseases.

Future research should focus on pharmacokinetic optimization, formulation development, and clinical safety evaluation of daxin. At the same time, by integrating modern molecular biology techniques, the study deeply analyzes its molecular mechanisms and uncovers more potential targets, laying a solid foundation for its clinical translation.

Conclusion

As a natural coumarin-derived with multiple biological activities, daphne demonstrates excellent pharmacological activity and druggability. Its research progress in anti-inflammation, anti-tumor, antimalarial, and cell protection fully demonstrates the important value of natural products in modern drug development. Although pharmacokinetics and clinical research on thyphine are still in the early stages, its unique mechanism of action and good safety signal broad prospects as a novel drug candidate. In the future, through multidisciplinary collaboration, Ruinxiang is expected to become an effective drug for treating various complex diseases and make an important contribution to human health.