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Product name: Arnicolide D
Synonym name: Plenolin methacrylate
Catalogue No.: BP4032
Cas No.: 34532-68-8
Formula: C19H24O5
Mol Weight: 332.396
Botanical Source: Centipeda minima（L.）A.Br.et Aschers.
Physical Description:
Type of Compound: Terpenoids
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.
For Reference Standard and R&D, Not for Human Use Directly.
Storage conditions：Short-term storage at 2~8℃, long-term storage at -20 ~ -80℃
69.6700
2.2682
2.2681
.0909
4.6019
20.4438
High
59.6883
4.8213
No
Yes
No
No
Yes
No
0.0
Yes
Yes
Yes
Yes
Arnicolide D is a sesquiterpene lactone naturally derived from the Asteraceae plant Centipeda minima. As a sesquiterpene lactone compound, Arnica Chenalin D has attracted widespread attention in natural medicinal chemistry and pharmacology due to its remarkable antitumor and anti-inflammatory activities. In recent years, with the deepening exploration of the potential of natural products in disease treatment, Arnica Chenalone D, due to its multi-target regulatory capability and good druggability parameters, has become an important candidate for the research and development of novel anti-tumor and anti-inflammatory drugs.
This review aims to systematically summarize the chemical structure and physicochemical properties of Arnica Chenulone D, plant origin and extraction and separation methods, pharmacological activity and mechanism of action, molecular targets, druggability evaluation, and pharmacokinetic characteristics, and finally explore its clinical application prospects and future research directions, providing theoretical basis and reference for subsequent basic research and drug development.
The chemical name of Arnica Chenalone D is sesquiterpene lactone, with the molecular formula C20H28O4 and a molecular weight of 332.3960. Its structural core is a sesquiterpene skeleton, containing a typical lactone ring structure that imparts its unique biological activity. According to molecular structure analysis, Arnicula Chenalone D has moderate hydrophobicity, with a LogP value of 2.2682, indicating good lipid solubility, which facilitates cell membrane penetration and distribution in vivo.
Its topological pole surface area (TPSA) is 69.67 Ų, indicating that the molecule has moderate polarity, which facilitates binding to biomacromolecules such as protein receptors. Low water solubility (0.0909 mg/mL) suggests limited solubility in the aqueous phase, which may affect its bioavailability. Notably, Arniculone D has a high blood-brain barrier penetration ability, which opens up potential applications in neurological diseases.
In terms of safety, the hERG channel inhibition test was negative, indicating a low risk of cardiotoxicity; The Ames mutagenicity test result was 0.0, indicating no significant mutagenicity and a solid safety foundation.
Arnicula Planlactone D is mainly isolated from Centipeda minima, a plant in the Asteraceae family. C. minima is widely distributed in parts of Asia and is commonly used in traditional Chinese medicine to treat colds, inflammation, tumors, and other diseases. This plant is rich in sesquiterpene compounds, with Arnica Chenaltone D being one of the important bioactive components.
During extraction, dried whole plants or above-ground parts are typically used as raw materials. Ethanol or methanol is first used for rough extraction, followed by liquid-liquid partitioning, column chromatography (such as silica gel columns, reversed-phase C18 columns), and high-performance liquid chromatography (HPLC) for multi-step separation and purification techniques, ultimately yielding high-purity Arnica Chenalone D. Modern extraction technologies such as ultrasound-assisted extraction and microwave-assisted extraction are also applied to improve extraction efficiency and purity.
Optimizing the extraction process not only affects yield but also relates to maintaining compound activity and the feasibility of subsequent drug development. Current research focuses mainly on improving extraction purity, reducing process costs, and achieving large-scale production.
Arnica Chenlactone D exhibits significant antitumor activity, capable of inhibiting the proliferation of various tumor cell lines. In vitro cell experiments show that Arnica Chenlactone D induces cell cycle arrest in tumor cells, blocking cell cycle progression and inhibiting cell division. Its ability to induce apoptosis and oncosis further promotes tumor cell death.
Specific mechanisms include activating endogenous apoptosis pathways, regulating the expression of Bcl-2 family proteins, promoting mitochondrial membrane potential loss, releasing cytochrome c, and activating caspase cascades, ultimately leading to apoptosis. Additionally, Arnica Chenolide D can induce cell swelling and death, a mode of cell death different from apoptosis, characterized by cell swelling and membrane rupture, possibly achieved by regulating intracellular ion channels and energy metabolism.
Arnica Chenalone D also shows good anti-inflammatory activity. By modulating various inflammation-related targets, it suppresses the production and release of inflammatory factors, thereby reducing inflammatory responses. Research shows that Arnicula Chenalone D can inhibit the expression of pro-inflammatory cytokines such as IL-6 and TNF-α, and suppress the activation of signaling pathways for signal transduction and transcription activator factor 3 (STAT3) and nuclear factor κB (NF-κB).
Additionally, Arnicula Chenalin D inhibits inflammatory mediator synthases such as cyclooxygenase 1 (PTGS1), cyclooxygenase 2 (PTGS2), and nitric oxide synthase 2 (NOS2), reducing the production of inflammatory mediators like prostaglandins and nitric oxide. It regulates the inflammation-related ion channels TRPV1 and TRPA1, further modulating inflammation and pain responses.
In summary, Arnica Chenalone D exerts dual anti-inflammatory and anti-tumor pharmacological effects through multi-target and multi-pathway synergistic effects.
The pharmacological mechanism of Arnica Chenalone D involves multiple cellular signaling pathways and key molecular targets, demonstrating its multi-target pharmacological properties.
Arnicula Chenalone D can interfere with the expression of cell cycle regulatory proteins, blocking the progression of tumor cells during the G0/G1 or G2/M phases and inhibiting cell proliferation. The specific mechanism may involve regulating the expression levels of cyclin-dependent kinases (CDKs) and their inhibitors (such as p21, p27).
By activating the caspase family proteins, Arnica Chenalone D induces the classic mitochondria-dependent apoptosis pathway. It promotes the release of cytochrome C, activates caspase-9 and caspase-3, and leads to nuclear DNA fragmentation and apoptosis formation.
In terms of swelling and death, Arnica Chenalone D may regulate cell membrane ion channels (such as TRPV1, TRPA1) and imbalance energy metabolism, leading to cell swelling and membrane integrity damage, thereby promoting cell death.
Arnica Chenalone D significantly inhibits activation of the STAT3 and NF-κB signaling pathways, reduces the expression of pro-inflammatory factors IL-6 and TNF-α, and alleviates inflammatory responses. Its regulation of CASP1 helps inhibit inflammasome activation and reduces the release of the inflammatory mediator IL-1β.
Additionally, Arnica Gallolide D reduces the synthesis of prostaglandins and nitric oxide by inhibiting PTGS1, PTGS2, and NOS2, thereby alleviating inflammatory symptoms. Regulation of TRPV1 and TRPA1 helps alleviate inflammation-related pain.
From the perspective of druggability, Arnica Chenalone D has superior medicinal properties. Its molecular weight of 332.4 complies with the Lipinski rule, and LogP 2.27 shows moderate lipid solubility, which is beneficial for oral absorption and cell membrane penetration. TPSA 69.67 Ų indicates moderate polarity, which facilitates binding to target proteins.
Low water solubility (0.0909 mg/mL) may limit its oral bioavailability, and solubility is improved through pharmacological methods such as nanocarriers and solid dispersions. Its high blood-brain barrier permeability offers possibilities for treating central nervous system diseases.
In terms of safety, the hERG channel has no inhibitory effects, reducing the risk of cardiotoxicity; The Ames test was negative, indicating no significant mutagenicity and good safety.
Although pharmacokinetic data are limited, preliminary in vivo experiments show that Arnica Carriageolide D has good stability and metabolic characteristics, mainly metabolized and excreted by the liver, with a moderate half-life. In the future, further systematic pharmacokinetic studies are needed, including absorption, distribution, metabolism, excretion (ADME), and toxicological assessment.
Arnica Chenolide D, with its unique sesquiterpene lactone structure and multi-target pharmacological activity, shows broad application prospects in anti-tumor and anti-inflammatory fields. Its inhibitory effects on various tumor cells and its ability to induce cell death provide important candidate molecules for the development of novel anti-tumor drugs. Especially in the treatment of drug-resistant tumors and complex inflammatory microenvironment-related tumors, Arnica Carriageolone D may play a synergistic role.
Its anti-inflammatory activity gives it potential application value in inflammatory diseases such as rheumatoid arthritis, inflammatory bowel disease, and neuroinflammation. Its high blood-brain barrier penetration offers new possibilities for treating neurological diseases.
However, the clinical translation of Arnica Chenalone D still faces many challenges, including poor water solubility, limited bioavailability, insufficient in vivo metabolic stability, and insufficient safety verification. Future research should focus on:
Through multidisciplinary collaboration, Arnica Chenolide D is being promoted from the laboratory to clinical application, benefiting patients.
Arnica Chenolide D, a natural sesquiterpene lactone derived from Centipeda minima, has become a hot topic in natural medicine research due to its remarkable antitumor and anti-inflammatory activities. Its unique chemical structure, multi-target mechanism of action, and solid safety foundation give it the potential to become a novel anti-tumor and anti-inflammatory drug.
Although there is currently a preliminary understanding of its pharmacological effects and druggability, further in-depth research is needed on its molecular mechanisms, pharmacokinetic characteristics, and clinical application potential. In the future, by integrating modern medicinal chemistry, molecular biology, and pharmaceutical technologies, Arnica Chenolide D is expected to become a major breakthrough in the development of natural product drugs, providing new strategies and options for the treatment of cancer and inflammatory diseases.
In summary, Arnica Chenolide D is a natural product with great research value and development potential, and it is expected to play a greater role in future drug development.
Shenshuai
Wenjing
Hedandan
