+86-28-82633987
Product name: Methysticin
Synonym name:
Catalogue No.: BP0945
Cas No.: 495-85-2
Formula: C15H14O5
Mol Weight: 274.272
Botanical Source: Piper methysticum Forst
Physical Description:
Type of Compound: Miscellaneous
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.
HPLC of Methysticin
HNMR of Methysticin
Storage conditions：Short-term storage at 2~8℃, long-term storage at -20 ~ -80℃
53.9900
2.0232
2.0232
.0936
4.1477
3.6306
High
80.9612
3.2811
Yes
Yes
Yes
No
No
Yes
0.3
No
Yes
Yes
Yes
Methysticin (CAS number: 495-85-2) is a kavalolide compound mainly found in extracts of Piper methysticum. As a traditional herbal medicine from the South Pacific region, kava is widely used in folk medicine for its unique sedating, anxiolytic, and analgesic effects. As an important active ingredient in Kava extracts, anesthetic pepper bitter has attracted significant attention in pharmacology and natural product chemistry in recent years due to its induction of the cytochrome P450 enzyme system, especially CYP1A1, as well as its potential regulatory function on analgesic-related targets.
This paper aims to systematically review the chemical structure and physicochemical properties, plant origin and extraction methods, pharmacological activity and mechanism of action, druggability evaluation, and pharmacokinetic characteristics of anesthetic pepper bitter extract, and to explore its clinical application prospects in the treatment of analgesic and related diseases. By integrating existing literature, it is hoped to provide a theoretical foundation and practical guidance for further research and development of anesthetic pepper and bitter alcohol.
Anesthetic pepper bitter is a carvanolactone compound, with a molecular formula of C_15H_14O_5 and a molecular weight of 274.2720. Its structural features include a benzene ring system containing multiple oxygen functional groups, characterized by strong lipid solubility and certain polarity. Its LogP value is 2.0232, indicating moderate lipid solubility, which is beneficial for transmembrane absorption and blood-brain barrier penetration. The topological pole surface area (TPSA) is 53.99 Ų, supporting its good bioavailability in vivo.
The water solubility of anesthetic pepper-bitter is relatively low (0.0936 mg/mL), which somewhat limits its oral bioavailability, but its high blood-brain barrier permeability gives it potential for central nervous system function. In terms of safety, anesthetic pepper-bitter acid did not show hERG channel inhibitory activity, suggesting a low risk of cardiotoxicity; The Ames test result was 0.3, indicating a low genotoxicity risk.
Anesthetic pepper-bitter is mainly found in the roots and rhizomes of the Kava plant. Kava (Piper methysticum) is a plant in the Piperaceae family, native to the islands of the South Pacific. It is an important medicinal plant in local traditional medicine used to relieve anxiety, promote sleep, and relieve pain. The root of kava contains various kavalactones, with the highest content of anesthetic pepper bitter, which is one of its main active components.
Common extraction methods for anesthetic pepper bitter include organic solvent extraction, supercritical fluid extraction, and liquid chromatography separation. Traditional extraction often uses ethanol or methanol as solvent, combined with ultrasonic-assisted extraction to improve extraction efficiency. Subsequently, separation and purification are performed using liquid chromatography (such as HPLC) technology to ensure the purity and activity of anesthetic pepper bitter. In recent years, green extraction technologies such as supercritical CO_2 extraction have gained attention for their environmental friendliness and efficiency, providing new ideas for the industrial production of anesthetic pepper-bitter extract.
The pharmacological activity of anesthetic pepper-bitter is mainly concentrated in the central nervous system, especially showing significant effects in analgesia, anxiety reduction, and neuroprotection. Its analgesic effects may be closely related to the regulation of various neurotransmitter systems and receptors.
Anesthetic pepper bitter extract exerts its analgesic effect by modulating various pain-related targets. The targets involved include:
The multi-target mechanism gives anesthesia pepper-bitter compound multidimensional regulatory potential in analgesic treatment.
Anesthetic pepper bitter also demonstrated the ability to induce cytochrome P450 enzyme CYP1A1, suggesting its potential impact on drug metabolism and detoxification. Additionally, some studies suggest it has anti-inflammatory, antioxidant, and neuroprotective effects, but the related mechanisms still need further clarification.
The mechanism of action of anesthetic pepper-bitter is complex, involving multiple signaling pathways and various molecular targets. Its induction of CYP1A1 may mediate through aromatic hydrocarbon receptors (AhR), modulating cellular metabolic capacity against exogenous compounds. This mechanism not only affects drug metabolism dynamics but may also be involved in cellular antioxidant defenses.
In terms of analgesia mechanisms, narcotic pepper and bitter compounds directly or indirectly regulate the TRPV1 and TRPA1 plasma channels, modulating pain signal transmission; Regulate neurotransmitter release and neuronal excitability by activating or antagonizing CNR1 and opioid receptors (OPRM1, OPRK1, OPRD1); At the same time, it affects PTGS1/2 activity, reduces the production of inflammatory mediators, and alleviates inflammatory pain. Its regulation of SLC6A4 and DRD2 may improve pain-related emotional disorders.
Both molecular docking and in vitro experiments support the high affinity of anesthetic-pepper kosarin with the above targets, suggesting that its multi-target synergistic effect is the basis for its significant pharmacological effects.
Anesthetic pepper bitter extract has good druggability parameters. Its molecular weight of 274.27 complies with the Lipinski rule, with a moderate LogP value, supporting good membrane permeability and oral absorption. The TPSA value is moderate, which helps the blood-brain barrier penetrate and meets the requirements of central nervous system activity. Although water-soluble is relatively low, its bioavailability can be improved through formulation optimization.
In terms of safety, the anesthetic pepper bitter did not show hERG channel inhibition, reducing the risk of cardiovascular toxicity; Ames test results showed that it has low genotoxicity and good safety.
Pharmacokinetic studies show that anesthetic pepper and kossosu are rapidly absorbed orally, have a moderate plasma half-life, and can effectively reach the central nervous system. Its metabolism is mainly through the hepatic cytochrome P450 enzyme system, especially the induction of CYP1A1, which may affect the metabolic rate of the drug itself and those of shared drugs, suggesting that drug interactions should be considered in clinical applications.
As the active ingredient in Kava extract, anesthetic pepper bitter has the potential to become a novel analgesic drug due to its multi-target analgesic effects and good central nervous system penetration ability. Its multi-mechanism synergistic effect is expected to overcome the limitations of traditional single-target analgesics, reducing resistance and side effects.
Additionally, the induced properties of CYP1A1 by anesthesia pepper bitter extract provide new research directions for drug metabolism regulation and detoxification therapy. In the future, its application potential can be explored in neurodegenerative diseases, anxiety disorders, and chronic pain syndromes.
However, clinical research on anesthetic pepper-bitter extract is still in its early stages, and systematic pharmacokinetics, safety evaluation, and clinical efficacy validation still require extensive work. Optimization of formulation technology, determination of dosage ranges, and long-term safety monitoring are key areas of future research.
As a natural product of the kavalactone class, anesthetic pepper bitter extract, with its unique chemical structure and multi-target pharmacological activity, shows broad application prospects in pain relief and central nervous system disease treatment. Its favorable druggability parameters and safety profile lay the foundation for clinical development. In the future, through in-depth molecular mechanism research, pharmacokinetic analysis, and clinical trials, anesthetic pepper bitter extract is expected to become a major breakthrough in the field of natural product pharmacology, promoting the transformation of natural medicines into modern medicines.
Shenshuai
Wenjing
Hedandan
