| Catalog No | Package | Original Price | Price | Inventory | Quantity | Operating |
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Storage conditions：Short-term storage at 2~8℃, long-term storage at -20 ~ -80℃
Gentianine, CAS number 439-89-4, is a naturally occurring lactone pyridine alkaloid that combines the structural characteristics of pyridine and pyranopyridine. As an important active ingredient in Gentianaceae plants, gentiopicroside has attracted widespread attention in the field of natural product pharmacology in recent years due to its unique chemical structure and multi-target biological activity. Especially in terms of anti-inflammatory effects, Gentiana extract has shown significant potential, involving multiple inflammation related signaling pathways and targets, and has good safety and pharmacological parameters. This article aims to systematically review the chemical properties, plant sources, pharmacological activities, and mechanisms of action of Gentiana macrophylla, and explore its future development prospects in clinical applications by combining pharmacological evaluation and pharmacokinetic data.
Qinqiansu A is a lactone pyridine alkaloid with a molecular weight of 175.1870, which contains a complex skeleton of pyridine ring and pyranopyridine ring in its structure. Its molecular formula and structural characteristics endow the compound with moderate lipid solubility (LogP=1.2663) and polar surface area (TPSA=39.19 Å ²), achieving a good balance between water solubility (0.9811) and lipid solubility. In addition, the high blood-brain barrier permeability of Gentiana macrophylla indicates its potential application value in central nervous system diseases. Importantly, Gentiana extract did not exhibit hERG channel inhibition and the Ames mutagenicity test result was 0, indicating its high safety and reduced the risk of cardiac and genetic toxicity.
The lactone ring and pyridine skeleton in its chemical structure provide the basis for its biological activity, especially playing a key role in binding to inflammation related proteins. The multifunctionality in structure enables it to regulate multiple signaling pathways, making it an ideal candidate molecule for multi-target drug design.
Gentiana extract is mainly found in Gentianaceae plants, especially in the rhizomes of Gentiana spp. In traditional Chinese medicine, the root of Gentiana macrophylla is widely used for clearing heat and detoxifying, dispelling wind and dampness, etc. Modern research has confirmed that its active ingredient, Gentiana macrophylla A, has a high content. Common plants containing Gentiana macrophylla Pall. and Gentiana scabra Bunge contain Gentiana macrophylla A.
The extraction method usually involves solvent extraction combined with column chromatography purification. The specific process is as follows: first, crude extraction is carried out using ethanol or methanol, followed by removal of impurities through liquid-liquid distribution, and then separation and purification are performed using silica gel column chromatography or high-performance liquid chromatography (HPLC). In recent years, the application of ultrasound assisted extraction and microwave-assisted extraction technologies has improved the extraction efficiency and purity of Gentiana macrophylla extract, while reducing the amount of solvent and extraction time. In addition, supercritical CO ₂ extraction technology has also been explored for efficient and green extraction, which meets the environmental requirements of modern natural product extraction.
After extraction and purification, the structure of Gentiana macrophylla extract was identified by various analytical methods such as nuclear magnetic resonance (NMR), mass spectrometry (MS), and infrared spectroscopy (IR) to ensure its chemical purity and structural accuracy.
The pharmacological activities of Gentiana macrophylla extract are mainly reflected in anti-inflammatory, analgesic, and neuroprotective aspects. A large number of in vitro and in vivo experiments have shown that gentian extract can significantly inhibit the expression and release of various inflammatory factors, alleviate inflammatory reactions, and has potential therapeutic value for inflammatory diseases.
Qinqiansu A exhibits potent anti-inflammatory activity by regulating inflammatory mediators and signaling pathways. In vitro cell models, gentian extract can inhibit the expression of pro-inflammatory factors such as IL-6, TNF - α, and inducible nitric oxide synthase (NOS2) in macrophages and other immune cells, reducing the release of inflammatory mediators. In animal models, gentian extract significantly reduces edema, erythema, and cell infiltration at the site of inflammation, demonstrating good anti-inflammatory effects.
Qinqiansu A has a regulatory effect on pain related ion channels such as TRPV1 and TRPA1, and can alleviate inflammatory and neuropathic pain. Related studies have shown that gentian extract exerts analgesic effects by inhibiting the activation of these ion channels, reducing the transmission of pain signals.
In addition to anti-inflammatory and analgesic effects, Gentiana extract also exhibits certain neuroprotective effects, which may be related to its regulation of the STAT3 and NFKB1 signaling pathways. In addition, the effect of Gentiana macrophylla extract on apoptosis related protein CASP1 suggests its potential role in regulating cell death and immune response.
The multi-target mechanism of action of Gentiana macrophylla is an important basis for its pharmacological activity. Through molecular biology and proteomic studies, it has been confirmed that Gentiana extract can regulate multiple inflammation related signaling pathways and targets.
IL-6, as a pro-inflammatory cytokine, plays a key role in various inflammatory diseases. Gentiana extract can inhibit the expression of IL-6 and the activation of its downstream transcription factor STAT3, block the transmission of inflammatory signals, and alleviate inflammatory reactions.
Qinqiansu significantly inhibits the expression of cyclooxygenases (PTGS1 and PTGS2, i.e. COX-1 and COX-2), reduces prostaglandin synthesis, and decreases the production of inflammatory mediators. In addition, its inhibitory effect on TNF - α and NOS2 further reduces the inflammatory amplification effect.
TRPV1 and TRPA1 are important ion channels involved in pain and inflammation perception. Gentiana extract acts directly or indirectly on these channels, reducing their activation and relieving inflammation related pain.
Gentiana extract can inhibit the activation of NFKB1, prevent the transcription of pro-inflammatory genes, and exert anti-inflammatory and immune regulatory effects.
By affecting the activity of CASP1, gentiopicroside regulates inflammation related cell apoptosis processes, which may help control inflammatory cell damage.
In summary, the synergistic effect of Gentiana macrophylla A on multiple targets and pathways forms a complex anti-inflammatory network, demonstrating good pharmacological activity and potential therapeutic value.
The pharmacological parameters of Gentiana macrophylla extract indicate that it has good potential for drug development. The molecular weight of 175.1870 conforms to Lipinski's rule, with a LogP of 1.2663, indicating moderate lipid solubility and favorable absorption and distribution in vivo. The TPSA value of 39.19 Å ² is relatively low, indicating its good cell membrane permeability and blood-brain barrier penetration ability, which is particularly important for the treatment of central nervous system diseases.
The water solubility is 0.9811, which meets the solubility requirements for oral administration. The high permeability of the blood-brain barrier supports its potential application in neuroinflammation and brain diseases. The negative results of hERG channel inhibition and Ames test indicate that the cardiotoxicity and genotoxicity risks of Gentiana macrophylla are low, and its safety is good.
Pharmacokinetic studies have shown that the oral absorption of Gentiana macrophylla is good, widely distributed in the body, with a moderate half-life. The metabolic pathway is mainly through the liver enzyme system, and the excretion pathway is mainly through the kidneys. Its metabolites did not show significant toxicity, providing a good foundation for subsequent drug development.
As a multi-target natural product, Gentiana extract has significant anti-inflammatory and analgesic activities, as well as good safety and pharmacological properties, demonstrating broad clinical application prospects.
Qinqiansu A has potential therapeutic value in various inflammatory diseases such as rheumatoid arthritis, inflammatory bowel disease, and chronic obstructive pulmonary disease. Its multi-target regulatory mechanism helps overcome the limitations of single target drugs, reduce drug resistance and side effects.
The high permeability of the blood-brain barrier makes gentian extract potentially valuable for neuroinflammation, post-stroke inflammatory response, and neurodegenerative diseases such as Alzheimer's disease and Parkinson's disease. Its dual effects on neuroprotection and inflammation regulation provide new ideas for the comprehensive treatment of neurological diseases.
In response to chronic pain and neuropathic pain, gentiopicol A exhibits good analgesic effects by regulating TRPV1 and TRPA1 channels, and is expected to become a candidate molecule for novel analgesic drugs.
Although the pharmacological mechanism of action of Gentiana macrophylla has been preliminarily elucidated, its clinical translation still requires further research. In the future, efforts should be made to strengthen its in vivo pharmacokinetics, toxicology evaluation, and validation of preclinical animal models. At the same time, combining modern medicinal chemistry and drug design techniques, optimizing its structure, improving activity and selectivity, and reducing potential side effects.
In addition, the research on the combination therapy of Gentiana macrophylla with other drugs, the long-term safety evaluation of chronic disease medication, and the development of dosage forms are also key directions for the future.
As a naturally occurring lactone pyridine alkaloid with a unique structure, Gentiana macrophylla has great potential for drug development due to its multi-target anti-inflammatory and analgesic activities, good drug properties, and safety. Its application prospects in inflammatory and neurological diseases are broad, and it is worth further in-depth research and clinical development. In the future, with the continuous clarification of molecular mechanisms and the advancement of drug research and development technology, gentian extract is expected to become an important representative of the new generation of natural anti-inflammatory drugs, providing effective new strategies for the treatment of related diseases.
