| Catalog No | Package | Original Price | Price | Inventory | Quantity | Operating |
|---|---|---|---|---|---|---|
| BP4695-5mg | 5mg | $590.00 | Sign in |
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Storage conditions：Short-term storage at 2~8℃, long-term storage at -20 ~ -80℃
In recent years, natural products have attracted significant attention as important resources for drug discovery and development, due to their unique chemical structures and diverse biological activities. 5,9-epi-Phlomiol, as a novel natural compound due to its remarkable anti-inflammatory activity and good safety, has become a research hotspot in the field of natural product pharmacology. As the pathological basis of various diseases, inflammation has complex regulatory mechanisms involving multiple signaling pathways and molecular targets. 5,9-epi-phlomiol demonstrates broad anti-inflammatory potential by modulating multiple inflammation-related targets such as IL-6, STAT3, TNF, and NFKB1. This paper aims to systematically review the chemical structure and physicochemical properties of 5,9-epi-Phlomiol, plant origin and extraction methods, pharmacological activity and mechanism, druggability evaluation, and pharmacokinetic characteristics, and to explore its clinical application prospects and development trends, providing theoretical basis and reference for subsequent research and clinical translation.
5,9-epi-Phlomiol has the molecular formula C_24H_34O_7 and molecular weight of 438.3820, belonging to the sesquiterpene class of natural products. Its structural features include multiple hydroxyl and epoxy groups, giving it high polarity and water solubility. According to calculations, its LogP value is -2.0533, indicating strong hydrophilicity, and the TPSA (Topological Polarity Surface Area) is 215.8300, further supporting its high polarity characteristics. The water solubility index was 48.1472, indicating that this compound has good solubility in the aqueous phase. Polar groups in the structure facilitate hydrogen bonding with biological macromolecules, enhancing their binding ability to target proteins. Notably, 5,9-epi-Phlomiol has low blood-brain barrier permeability, suggesting limited distribution in the central nervous system, which is beneficial for avoiding central side effects. Additionally, the hERG channel inhibition test results were negative, indicating a low risk of cardiotoxicity; The Ames mutagenic test result was 0.0, indicating good genotoxicity safety.
5,9-epi-Phlomiol mainly comes from several species of the genus Phlomis in the Lamiaceae family, with particularly high levels in Phlomis umbrosa and Phlomis fruticosa. These plants are widely distributed along the Mediterranean coast and parts of Asia, and have traditionally been used as anti-inflammatory and analgesic herbs. During extraction, ethanol or methanol is usually used as solvent, and crude extracts are obtained by ultrasound-assisted extraction or reflux extraction methods. Subsequently, separation and purification were performed using liquid-liquid partitioning, column chromatography (silica gel column, reversed-phase C18 column), and high-performance liquid chromatography (HPLC), ultimately obtaining high-purity 5,9-epi-Phlomiol. In recent years, supercritical CO_2 extraction technology has also been introduced to improve extraction efficiency and reduce the use of organic solvents, in line with green chemistry principles. Optimization of extraction processes not only increases yield but also ensures the biological activity and stability of the compounds.
Pharmacological activity studies of 5,9-epi-Phlomiol have mainly focused on its anti-inflammatory effects. Both in vitro cell models and in vivo animal models showed that this compound exhibited significant anti-inflammatory effects. In macrophage lines (such as RAW 264.7), 5,9-epi-phlomiol can significantly inhibit LPS-induced release of inflammatory factors, including IL-6, TNF-α, and NO production. This action is closely related to its regulation of inflammation-related signaling pathways.
In mouse inflammation models (such as carrageenan-induced plantar edema), 5,9-epi-Phlomiol significantly reduced tissue swelling and infiltration of inflammatory cells, demonstrating good anti-inflammatory activity. Additionally, this compound also demonstrates certain protective effects in neuroinflammation models, suggesting its potential application value in chronic inflammatory diseases.
In addition to its anti-inflammatory effects, preliminary studies have found that 5,9-epi-phlomiol has certain antioxidant activity, can scavenge free radicals, and reduce cellular damage caused by oxidative stress. This characteristic may further promote its application in the treatment of inflammation-related diseases.
The anti-inflammatory mechanism of 5,9-epi-Phlomiol involves multiple signaling pathways and multiple molecular targets. Its main targets include:
Overall, 5,9-epi-Phlomiol regulates inflammatory responses through multiple targets and pathways, demonstrating a multi-layered anti-inflammatory mechanism and laying a solid foundation for its development as an anti-inflammatory drug.
Druggability evaluations of 5,9-epi-phlomiol indicate good safety and drug properties. Its molecular weight of 438.3820 is moderate, which fits the molecular weight range of most oral medications. A lower LogP value (-2.0533) reflects its strong hydrophilicity, which facilitates dissolution and distribution in body fluids, but may limit its ability to penetrate cell membranes. A high TPSA value (215.8300) suggests strong polarity, which may affect oral absorption and bioavailability.
The low permeability of the blood-brain barrier reduces the risk of central nervous system side effects, but also limits its application in central inflammatory diseases. The hERG channel inhibition test was negative, and the Ames test result was 0.0, indicating low cardiotoxicity and genotoxicity risks and good safety.
Regarding pharmacokinetics, although current data are limited, based on its physicochemical properties, 5,9-epi-Phlomiol may have rapid in vivo clearance and limited oral bioavailability. In the future, in vivo pharmacokinetic studies are needed to clarify its absorption, distribution, metabolism, and excretion (ADME) characteristics, providing a basis for formulation design and route optimization.
Given the significant regulatory effects and good safety profile of 5,9-epi-Phlomiol on various inflammation-related targets, it holds broad application prospects in anti-inflammatory drug development. Inflammatory diseases such as rheumatoid arthritis, inflammatory bowel disease, chronic obstructive pulmonary disease, and neuroinflammation may all become potential indications. Additionally, its regulatory effects on TRPV1 and TRPA1 suggest its value in managing inflammatory pain.
Future research should focus on the following areas:
In addition, combined with modern drug design concepts, 5,9-epi-Phlomiol can also serve as a lead compound, optimizing its efficacy and pharmacokinetic properties through structural modification, thereby expanding its range of applications.
5,9-epi-Phlomiol, as a natural product with a unique structure and broad anti-inflammatory activity, demonstrates excellent pharmacological activity and safety. Its multi-target mechanism of action provides new strategies and ideas for anti-inflammatory treatment. Although research on its pharmacokinetics and clinical applications is still in its early stages, its excellent druggability parameters and rich bioactivity suggest enormous development potential. In the future, through multidisciplinary collaboration combined with modern drug development technologies, 5,9-epi-Phlomiol is expected to become a new generation of safe and effective anti-inflammatory drugs, bringing hope to patients with inflammatory diseases.
