Synonym name:
Catalogue No.: BP0574
Cas No.: 877822-40-7
Formula: C₂₄H₃₀O₉
Mol Weight: 462.495
Botanical Source: Eupatorium lindleyanum

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.

HPLC of Eupalinolide A

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

Introduction/Overview

Eupalinolide A (CAS No.: 877822-40-7) is a natural product derived from plants of the Eupalinolide genus, and has attracted widespread attention in recent years due to its multi-target pharmacological activity. As a Yes-associated protein (YAP) degrader and heat shock protein 70 (HSP70) inducer, wild horse chasmallolactone A exhibits unique regulatory effects in various biological processes including apoptosis, autophagy regulation, and stem cell differentiation. Its significant efficacy in treating hepatocellular carcinoma (HCC) and in disease models such as traumatic tendon ectopic ossification (HO) suggests its potential clinical application value. This paper systematically reviews the chemical structure and physicochemical properties of Wild Horse Arunolactone A, plant origin and extraction methods, pharmacological activity and mechanism of action, druggability evaluation, and future clinical application prospects, aiming to provide scientific support for basic research and drug development in related fields.

Chemical structure and physicochemical properties

Wild horse apollolactone A belongs to the sesquiterpene lactone class of compounds, with a molecular formula of C_26H_34O_7 and a molecular weight of 462.4950. Its structural features include an lactone ring and multiple oxygen-containing functional groups, giving it high polarity and bioactivity. In terms of physicochemical properties, the LogP value of Wild Horse Chase Lactone A is 1.5669, showing moderate lipid solubility that facilitates cell membrane penetration. Its topological pole surface area (TPSA) is 125.43 Ų, indicating a good polarity distribution that facilitates binding with biological macromolecules such as proteins. Water solubility is 0.7923, indicating moderate solubility in the aqueous phase, facilitating absorption and distribution in the body. It is worth noting that wild horse chaolactone A has high blood-brain barrier penetration ability and no hERG channel inhibitory activity; Ames-induced mutagenic test results were negative, indicating good safety and drug potential.

Plant Origins and Extraction Methods

Wild Horse Runner Lactone A is mainly isolated from plants of the Wild Horse genus, especially abundant in traditional Chinese medicinal materials such as Wild Horse Chase (Eupatorium lindleyanum DC.). Plants of this genus are widely distributed in China and East Asia, and have traditionally been used to treat various inflammatory and tumor diseases. During extraction, organic solvents (such as ethanol and methanol) are often used for reflux extraction of dried plant material, followed by liquid-liquid separation, column chromatography (silica gel, C18 reversed phase column), and high-performance liquid chromatography (HPLC) purification, ultimately obtaining high-purity wild horse astragalone A. In recent years, the application of ultrasound-assisted extraction and supercritical fluid extraction technologies has improved extraction efficiency and purity, laying the foundation for large-scale production.

Pharmacological activity research

Antitumor activity

Wild horse chasmunolide A showed significant tumor suppression effects in hepatocellular carcinoma cell lines (MHCC97-L, HCCLM3). By inducing intracellular reactive oxygen species (ROS) production, it activates the extracellular signal-regulated kinase (ERK) pathway, promotes cancer cell autophagy, and thereby inhibits tumor growth. Additionally, wild horse chasing lactone A can degrade YAP protein, inhibit abnormal activation of the Hippo signaling pathway, and reduce tumor cell proliferation and migration. In animal experiments, wild horse chasmalloxide A significantly inhibited the volume of xenografts in hepatocellular carcinoma, demonstrating good in vivo anti-tumor activity.

Anti-ectopic ossification and stem cell regulation

Wild horse chasinolide A can inhibit osteogenic differentiation of tendon-derived stem cells (TDSCs) and alleviate trauma-induced ectopic ossification of the Achilles tendon. This mechanism of action is related to its regulation of stem cell fate and may be achieved by inhibiting signaling pathways related to bone formation. This property provides a new drug target for treating post-traumatic ossification diseases.

Cell protective effects

In the skin cell model PAM212, wild horse chasmalone A demonstrated protective effects, effectively resisting UVB, menadione-induced oxidative stress, and apoptosis induced by heat shock. This protective effect is closely related to its induction of HSP70 expression. As a molecular chaperone protein, HSP70 can stabilize cellular protein structures and reduce cellular stress damage.

Mechanism of action and molecular targets

The pharmacological effects of Wild Horse Alapidone A involve multiple signaling pathways and key molecular targets, with the specific mechanisms as follows:

1. YAP degradation and Hippo pathway regulation
   YAP, as a key transcriptional co-activator of the Hippo signaling pathway, plays an important role in cell proliferation and tumorigenesis. Wild horse chasinolide A promotes the degradation of YAP protein, inhibits its nuclear transcriptional activity, and blocks tumor cell proliferation and migration.

2. ROS/ERK signaling pathway activation
   Wild horse chaolactone A induces increased intracellular ROS levels, activates the ERK pathway, and promotes autophagy. Autophagy, as a cellular stress response mechanism, helps clear damaged organelles and proteins, inhibiting tumor cell survival.

3. HSP70 induction
   Wild horse chaolactone A upregulates HSP70 expression, enhancing cellular tolerance to environmental stress and reducing apoptosis. This mechanism plays a key role in protecting skin cells from damage caused by UV rays and oxidative stress.

4. Anti-apoptosis and gene regulation
   Wild horse chasing lactone A affects various molecules related to apoptosis, including MCL1, BCL2, STAT3, etc., regulating cell survival signals and promoting cancer cell apoptosis.

5. Matrix metalloproteinase-2 (MMP2) and tumor microenvironment regulation
   By inhibiting MMP2 activity, Wild Horse Chasinolide A reduces the invasion and metastasis ability of tumor cells.

6. Other targets
   Wild horse chasin-lactone A also interacts with molecules such as TOP1, TOP2A, HIF1A, MAPK1, ESR1, and CYP19A1, demonstrating its multi-target regulatory properties.

Druggability evaluation and pharmacokinetics

The druggability evaluation of Wild Horse Chase Lactone A indicates its promising potential for drug development. Its molecular weight is moderate, and the LogP value indicates good lipid-water balance, which is beneficial for oral absorption and membrane penetration. TPSA values suggest it may have good bioavailability. Moderate water solubility, facilitating formulation development. Importantly, Wild Horse Chasing Neolactone A can cross the blood-brain barrier, expanding its potential applications in central nervous system diseases.

In terms of safety, Wild Horse Chasing Lactone A does not inhibit hERG channels, reducing the risk of cardiotoxicity. Ames test negative results indicate that it does not exhibit mutagenicity and is relatively safe. Current research on its pharmacokinetics is still in its early stages, and in vivo metabolic pathways, half-life, and excretion mechanisms need to be further systematically elucidated to guide clinical dose design.

Prospects and outlooks for clinical applications

Wild horse chasing lactone A, with its unique multi-target pharmacological activity, shows broad clinical application prospects. Its anti-tumor effect in hepatocellular carcinoma treatment offers new treatment approaches for liver cancer patients, especially with potential advantages in the management of drug-resistant and recurrent tumors. Additionally, Wild Horse Chasmal Lactone A inhibits traumatic tendon ectopic ossification, providing an innovative drug candidate for orthopedics and rehabilitation medicine.

Future research should focus on the following areas:

1. Preclinical safety and pharmacokinetic studies
   Systematically evaluate the toxicological characteristics and in vivo metabolic kinetics of Wild Horse Lap Lactone A to ensure the safety and efficacy of its clinical application.

2. An in-depth analysis of the mechanism of action
   Utilizing genomics, proteomics, and metabolomics technologies, it comprehensively reveals its multi-target regulatory network and optimizes drug design.

3. Formulation development and drug delivery route exploration
   Based on its physicochemical properties, it is developing efficient and stable formulation forms and exploring diverse approaches such as oral administration, injection, and local administration.

4. Clinical trial design
   Combining its pharmacological characteristics, a reasonable clinical trial protocol was designed to verify its efficacy and safety in liver cancer and ossification diseases.

5. Combination medication strategies
   Exploring the synergistic effects of Wild Horse Pulsinolide A with existing antitumor or antiossification drugs to enhance treatment outcomes and reduce side effects.

Conclusion

Wild horse chasing lactone A, as a natural compound with multi-target regulatory capabilities, has become a hot topic in natural drug research due to its significant activity in tumor suppression, stem cell differentiation regulation, and cell protection. Its excellent druggability and safety have laid a solid foundation for clinical translation. In the future, through in-depth mechanistic research and preclinical evaluation, Wild Horse Chasinolide A is expected to develop into a novel drug for treating hepatocellular carcinoma and traumatic ectopic ossification, providing effective clinical treatment methods and promoting the development of natural product pharmacology and precision medicine.