Synonym name:
Catalogue No.: BP0763
Cas No.: 4491-19-4
Formula: C34H47NO10
Mol Weight: 629.747
Botanical Source: Alkaloid from roots of Aconitum chasmanthum, Aconitum ferox, Aconitum falconeri, Aconitum franchetti and Aconitum violaceum (Ranunculaceae)
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.
Storage conditions：Short-term storage at 2~8℃, long-term storage at -20 ~ -80℃
Indaconitine is a natural alkaloid isolated from plants of the Aconitum genus, belonging to the dihydroaconitine class of compounds. As one of the important active ingredients in traditional Chinese medicine "Aconitum", aconitine has received widespread attention in recent years due to its significant pharmacological activity, especially its potential application in the field of analgesia. Aconitum alkaloids have become an important subject of natural product pharmacology research due to their complex chemical structures and multi-target mechanisms of action. Indiaconitine not only exhibits unique analgesic effects, but also involves multiple neurotransmitters and inflammation related targets, suggesting that it may regulate pain perception and inflammatory response through multiple pathways.
This article aims to systematically review the chemical structure and physicochemical properties, plant sources and extraction methods, pharmacological activity and mechanism of action, pharmacological evaluation and pharmacokinetic characteristics of aconitine, and explore its application prospects and challenges in clinical analgesic treatment, in order to provide theoretical support and reference for the in-depth research and drug development of this natural product.
The molecular formula of aconitine is C36H51NO9, with a molecular weight of 629.7470, belonging to the complex dihydroaconitine alkaloids. Its structural features include a polycyclic terpene skeleton containing multiple ester groups and hydroxyl groups, with a complex structure and significant stereochemical characteristics. The LogP value of aconitine is 2.3740, indicating its moderate lipid solubility, which is beneficial for cell membrane penetration. Its topological polar surface area (TPSA) is 133.2200, indicating a high molecular polarity that may affect its ability to pass through biofilms and pharmacokinetic properties.
The low water solubility (0.1245 mg/mL) suggests limited solubility in the aqueous phase, which poses a certain challenge for its formulation development. The low permeability of the blood-brain barrier may limit the direct action of the central nervous system, but also reduce the risk of central toxic side effects. The negative result of hERG channel inhibition experiment indicates a low risk of cardiac toxicity. The Ames mutagenicity test result is 0.6, indicating a low risk of genotoxicity and a certain level of safety.
Overall, the physicochemical properties of aconitine provide the basis for its pharmacological activity, while also placing specific requirements on its clinical application and formulation development.
Indiaconitine is mainly found in plants of the Aconitum genus, such as Aconitum carmichaelii and its related species. Aconitum plants are widely distributed in temperate and subtropical regions of Asia, and have always been used as traditional Chinese medicinal materials for pain relief, anti-inflammatory, and anti rheumatic treatment.
The extraction of aconitine is usually carried out using organic solvent extraction method, combined with liquid-liquid distribution, column chromatography and other separation and purification techniques. The specific steps include:
In recent years, with the advancement of separation technology and analytical methods, the extraction and purification efficiency of aconitine has significantly improved, providing sufficient material basis for its pharmacological research.
The pharmacological activity of aconitine mainly focuses on its analgesic effect, and it also exhibits certain anti-inflammatory and neuroregulatory functions. Its analgesic effect has been validated in various animal models, including inflammatory pain, neuropathic pain, and acute pain models.
Aconitine exerts analgesic effects through various mechanisms involving both the central and peripheral nervous systems. In vivo experiments have shown that aconitine can significantly reduce pain responses caused by thermal and mechanical stimuli, and the effect is dose-dependent. Compared with traditional analgesics, aconitine has shown unique advantages in relieving chronic pain, especially in neuropathic pain models.
Aconitine can inhibit the release of inflammatory mediators, such as prostaglandins (PTGS1, PTGS2 related pathways) and various inflammatory factors, and alleviate local inflammatory reactions. Its anti-inflammatory effect provides auxiliary support for the analgesic effect, especially playing an important role in the relief of inflammatory pain.
Indiaconitine has regulatory effects on various neurotransmitter receptors, including dopamine receptor (DRD2) and multiple opioid receptors (OPRD1, OPRM1, OPRK1), suggesting that it may participate in pain regulation by modulating the neurotransmitter system. In addition, aconitine also has a certain impact on the serotonin transporter protein (SLC6A4), which may improve emotional pain experiences.
Overall, the multi-target effects of aconitine make it have high potential for application in pain management.
The analgesic mechanism of aconitine is complex, involving multiple signaling pathways and molecular targets, mainly including the following aspects:
Aconitine can regulate TRPV1 and TRPA1 channels, two transient receptor potential channels that play a key role in pain perception and inflammatory response. By inhibiting the activity of TRPV1 and TRPA1, aconitine reduces the transmission of pain signals and the release of inflammatory mediators, thereby achieving analgesic and anti-inflammatory effects.
Indiaconitine has an excitatory effect on the μ - type (OPRM1), δ - type (OPRD1), and κ - type (OPRK1) opioid receptors, enhancing the analgesic effect of the endogenous opioid system. The activation of opioid receptors not only relieves pain, but also regulates emotions and stress responses, improving patients' quality of life.
Aconitum alkaloids inhibit the activity of cyclooxygenase (PTGS1 and PTGS2), reduce prostaglandin synthesis, and alleviate inflammatory reactions. This mechanism is similar to nonsteroidal anti-inflammatory drugs (NSAIDs), but the multi-target effect of aconitine may bring more comprehensive therapeutic effects.
Indiaconitine affects the neurotransmitter balance of the central nervous system by regulating dopamine receptor DRD2 and serotonin transporter SLC6A4, and participates in emotional regulation and cognitive processing of pain. This regulatory effect helps alleviate common anxiety and depression symptoms in patients with chronic pain.
In summary, aconitine exerts significant analgesic and anti-inflammatory effects through multi-target and multi pathway synergistic effects.
Indiaconitine has shown certain advantages in medicinal properties, but there are also challenges.
The molecular weight of aconitine is relatively large (629.7470), with high polarity (TPSA 133.22) and low water solubility (0.1245 mg/mL), which may limit its oral absorption and bioavailability. Its LogP value (2.3740) indicates moderate lipid solubility, which is beneficial for cell membrane penetration, but the blood-brain barrier permeability is low, suggesting that it mainly acts on the peripheral nervous system and reduces central toxic side effects.
The hERG channel inhibition experiment result was negative, indicating a low risk of cardiotoxicity from aconitine. The Ames mutagenicity test result is 0.6, indicating a low risk of genotoxicity and a good safety basis. In addition, both traditional usage experience and modern toxicology studies have not found significant acute and chronic toxicity, but further systematic evaluation is still needed.
At present, there is limited research on the metabolic pathway of aconitine, and it is speculated that it is mainly metabolized through the liver cytochrome P450 enzyme system, which may pose a risk of drug interactions. Future research needs to focus on its metabolic kinetics and interactions with other drugs to guide safe clinical drug use.
Given the poor water solubility of aconitine, the development of formulations requires the use of nanocarriers, liposomes, or solid dispersions to improve its bioavailability and stability. In addition, the development of sustained-release formulations and targeted drug delivery systems is expected to enhance their efficacy and reduce side effects.
As a natural product with multi-target analgesic effects, aconitine has shown broad clinical application prospects.
The current analgesic drugs suffer from addiction, drug resistance, and multiple side effects. Indiaconitine may provide a novel analgesic strategy by regulating multiple targets such as TRP channels and opioid receptors. Especially in the fields of neuropathic pain and chronic inflammatory pain, aconitine is expected to become an effective and safe alternative drug.
The anti-inflammatory effect of aconitine provides a theoretical basis for its application in diseases such as rheumatoid arthritis and neuritis. Its regulatory effect on the neurotransmitter system also suggests its potential for neuroprotection and improvement of pain related psychiatric symptoms.
Although aconitine has significant pharmacological activity, its low water solubility and blood-brain barrier permeability limit its clinical application. Future research should focus on:
Through interdisciplinary collaboration, aconitine is expected to become an important candidate for the development of natural analgesic drugs.
As an important active ingredient in Aconitum plants, aconitine has shown great potential for drug development due to its multi-target and multi mechanism analgesic and anti-inflammatory effects. Its complex chemical structure and unique pharmacological properties provide valuable examples for the pharmacological research of natural products. Despite challenges such as poor water solubility and pharmacokinetic limitations, the development of modern medicinal chemistry and formulation technology has provided the possibility for its clinical translation.
In the future, in-depth pharmacological mechanism research, drug efficacy optimization, and clinical validation will promote the application of aconitine and its derivatives in pain management, meeting the urgent clinical demand for safe and effective analgesic drugs. As an important research object in the field of natural product pharmacology, the development and application prospects of aconitine are worth looking forward to.
