Bicuculline CAS 485-49-4

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Bicuculline is a natural alkaloid mainly found in the poppy genus, CAS 485-49-4, Molecular formula C20H17NO6, white or light yellow crystalline powder, not easily soluble in water, has good solubility in organic solvents such as ethanol, chloroform, methanol, etc. It is a weakness analgesic that can relieve mild to moderate pain and can be used to treat symptoms such as cough and diarrhea. Belonging to GABA_A receptor competitive antagonists, it affects neural signal transmission by inhibiting the activity of GABA. This compound is sensitive to light and is commonly used in neuroscience research, such as reversing the effects of GABA uptake inhibitors on blood pressure or inducing synaptic plasticity in midbrain dopamine neurons. Its derivatives such as methyl bromide and methyl iodide are used as specific receptor antagonists in electrophysiological experiments, such as studying changes in Arc gene mRNA expression levels in combination with propofol. In the study of epilepsy mechanisms, it is also used as a tool compound to explore GABAergic nervous system function.

Bicuculline, also known as mountain turtle alkaloids or painful tannins, is a class of isoquinoline alkaloids derived from plants in the family Paeoniaceae. Its molecular formula is C ₂ ₀ H ₂ N ₂ O ₂, and it has a unique four ring skeleton structure. Since its discovery in the mid-20th century, scientists have revealed its multiple values in pain relief, sedation, anti-inflammatory, cardiovascular regulation, and neuroscience research through in-depth research on its pharmacological mechanisms.

Clinical application: combination of traditional analgesia and modern treatment

 

1. Analgesia and Sedation: Relieving Multiple Types of Pain
Houttuynia cordata alkaloids exert analgesic effects by inhibiting excessive excitation of the central nervous system, blocking nerve conduction pathways, and reducing pain signal transmission. Its clinical applications cover:

Acute pain: Used to relieve headaches, lower back pain, toothache, and postoperative pain. The oral dose is 20-60mg/time, which can quickly relieve symptoms.
Chronic pain: It has a significant improvement effect on joint redness, swelling, heat pain, and limited mobility caused by rheumatoid arthritis, rheumatoid arthritis, etc. Its mechanism is related to inhibiting prostaglandin synthesis and reducing aseptic inflammation.

 

Neuropathic pain: By regulating the function of the GABAergic nervous system, it has potential therapeutic value for neuropathic pain such as trigeminal neuralgia and sciatica.
Sedation assistance: As a central inhibitor, paeoniflorin can reduce anxiety levels and improve sleep quality in patients with neurasthenia, and is commonly used as an adjuvant therapy for insomnia.

2. Anti inflammation and immune regulation: repair of tissue damage
Houttuynia cordata alkaloids inhibit the activation and migration of inflammatory cells, reduce the release of pro-inflammatory factors such as TNF - α and IL-6, and thus alleviate inflammatory reactions such as tissue redness and swelling. Its application scenarios include:

Soft tissue injury: promotes the absorption of local swelling, congestion, and exudation after fractures or sprains, accelerating the recovery process.

 

Ulcerative diseases: have an adjuvant therapeutic effect on mucosal injuries such as gastric ulcers and duodenal ulcers, which may be related to their inhibition of gastric acid secretion and promotion of mucosal repair.

Autoimmune diseases: Animal experiments have shown that paeoniflorin can downregulate the joint swelling index of rheumatoid arthritis model rats, indicating its immunomodulatory potential.
3. Cardiovascular regulation: Improvement of blood pressure and microcirculation
Berberine can achieve antihypertensive effects by dilating peripheral vascular smooth muscle and reducing peripheral resistance, while increasing coronary flow and alleviating myocardial ischemia. Its clinical indications include:

Hypertension: The use of antihypertensive drugs such as Captopril and Nifedipine alone or in combination can effectively control blood pressure and reduce complications such as headaches and dizziness.

 

Angina pectoris: By improving myocardial oxygen supply, relieving pain and difficulty breathing behind the sternum, and reducing the risk of acute myocardial infarction.
Sequelae of cerebrovascular disease: promoting the recovery of neurological deficits such as hemiplegia and aphasia may be related to improving cerebral microcirculation and reducing free radical damage.
4. Diuretic effect: Adjuvant treatment for edema
Berberine can increase glomerular filtration rate, promote water excretion, and produce diuretic effects. It is applicable to:

Renal edema: Adjuvant treatment for edema caused by chronic nephritis, nephrotic syndrome, etc., to reduce cardiac afterload.
Cardiogenic edema: Used in combination with diuretics such as furosemide to enhance drainage and improve symptoms of heart failure.

Research Tool: The Key to Neuroscience and Pharmacology Research

 

1. GABA receptor antagonists: regulators of neural signal transduction
Houttuynia cordata alkaloids are competitive antagonists of GABA_A receptors, which affect neural signal transduction by inhibiting the activity of GABA (gamma aminobutyric acid). Its scientific research applications include:

Epilepsy mechanism research: Bicuculline as a tool compound, explore the role of GABAergic nervous system in epileptic seizures. For example, in a rat model, paeoniflorin can reverse the blood pressure elevation caused by the GABA uptake inhibitor 3-piperidinecarboxylic acid, while the GABAB receptor antagonist CGP 35348 has no such effect, revealing the specificity of GABA_A receptors in blood pressure regulation.

 

Synaptic plasticity study: In midbrain dopamine neurons, paeoniflorin or picrotoxin can weaken GABA mediated inhibitory effects and induce long-term potentiation (LTP), providing a model for studying the mechanism of cocaine addiction.
Neurotransmitter interactions: Combining anesthesia agents such as propofol, studying the changes in Arc gene mRNA expression levels, and revealing the association between the GABA system and memory formation.

2. Vasoactive research: regulatory mechanism of arterial constriction
Berberine has the effect of constricting tubular arteries, and its scientific research value is reflected in:

Cardiovascular pharmacology model: used to screen vasodilators, such as pre treating rat arterial rings with paeoniflorin and observing the antagonistic effects of drugs such as nitroglycerin and nitroprusside.

 

Pathogenesis of hypertension: Exploring the relationship between increased peripheral vascular resistance and hypertension, providing targets for the development of new antihypertensive drugs.
3. Exploration of anti-cancer activity: a leap from traditional to cutting-edge
Although the anticancer effect of paeoniflorin is still in the preclinical research stage, its potential has attracted attention:

Cell cycle arrest: Preliminary experiments have shown that paeoniflorin can induce the G2/M phase arrest of human liver cancer cell line HepG2, and its mechanism is related to the activation of Caspase-3 and upregulation of Bax/Bcl-2 ratio.
Combination therapy strategy: Combined with topoisomerase inhibitors such as camptothecin, it may enhance anti-cancer effects through multi-target synergistic effects.

Agricultural Innovation: The Development Potential of Green Pesticides

 

1. Disease and pest control: environmentally friendly application of natural alkaloids
The anti-cancer mechanism of paeoniflorin inspires scientists to explore its use in agriculture:

Insect repellents: reduce crop damage by interfering with the insect nervous system. For example, spraying paeoniflorin on cotton leaves can significantly reduce the feeding amount of cotton bollworms.
Fungicide development: It has inhibitory effects on plant pathogens such as rice blast fungus and wheat Fusarium graminearum, and its mechanism is related to the damage to the integrity of bacterial cell membranes.

 

2. Plant growth regulation: improvement of stress resistance
Houttuynia cordata alkaloids may enhance plant stress resistance by regulating endogenous hormone levels

Drought stress tolerance: Under drought conditions, the stomatal conductance of wheat seedlings treated with paeoniflorin decreased, water transpiration decreased, and survival rate increased.
Saline alkali land improvement: Promote root growth of maize seedlings under salt stress, increase potassium ion absorption, and alleviate sodium ion toxicity.

Future potential: prospects for cross disciplinary applications in multiple fields

 

1. Treatment of neurodegenerative diseases
The neuroprotective effect of paeoniflorin provides possibilities for its application in fields such as Alzheimer's disease and Parkinson's disease

A β toxicity antagonism: Animal experiments have shown that paeoniflorin can reduce A β - ₁₋₄₂ - induced hippocampal neuronal apoptosis, and its mechanism is related to activating the Nrf2/ARE pathway and upregulating glutathione levels.
Dopaminergic neuron protection: In Parkinson's disease models, pretreatment with paeoniflorin can increase the survival rate of dopaminergic neurons in the substantia nigra by 40%, possibly by inhibiting oxidative stress.
2. Individualized medicine and precision medicine
The dose adjustment strategy based on genetic polymorphism can optimize the clinical efficacy of paeoniflorin:

 

UGT1A1 gene testing: For UGT1A1 * 28 homozygous patients, reducing the dose of irinotecan (a derivative of paeoniflorin) can significantly reduce the risk of severe neutropenia.
Drug interaction monitoring: When used in combination with CYP3A4 inhibitors (such as ketoconazole), the dosage of paeoniflorin should be adjusted to avoid toxicity accumulation.

3. Nanotechnology and delivery system innovation
Nano carriers can improve the bioavailability of paeoniflorin and reduce side effects:

Liposomal encapsulation: Encapsulating paeoniflorin in pH sensitive liposomes can achieve tumor tissue-specific release and enhance anti-cancer effects.
Polymer microspheres: extend the action time of paeoniflorin through controlled release technology, reduce the frequency of administration, and improve patient compliance.

Bicuculline (the alkaloid from the Bicuculus plant) is a natural compound with a unique chemical structure and significant biological activity. Its chemical properties can be elaborated from multiple aspects.
From a physical standpoint, Bicuculline typically appears as a pale yellow crystalline powder. This appearance feature makes it easy to identify and handle in the laboratory. Its melting point is 215℃, which is beneficial for determining its purity and stability. In its pure form, Bicuculline can remain in a solid state at higher temperatures without decomposing.
In terms of solubility, Bicuculline exhibits good solubility in organic solvents such as methanol, ethanol, and dimethyl sulfoxide (DMSO), which makes it convenient for dissolution and use in cell experiments and drug formulation. However, its solubility in water is poor, which limits its application in certain aqueous solution systems. Additionally, Bicuculline is soluble in benzene, chloroform, and ethyl acetate, and slightly soluble in ethanol and ether. These solubility data provide a reference for its use under different experimental conditions.
The chemical stability of Bicuculline is influenced by various factors. When in a dry and protected from light environment, it can remain relatively stable. However, it should be avoided from coming into contact with strong acids, strong bases, or oxidants to prevent decomposition reactions. It is worth noting that Bicuculline is sensitive to light and may undergo degradation or structural changes under light conditions. Therefore, it needs to be stored in a dark place and attention should be paid to the light conditions during experimental operations. This property is particularly important in drug storage and experimental design to ensure that its activity and effectiveness are not affected.
In terms of biological activity, the chemical properties of Bicuculline are closely related to its role as a GABAA receptor antagonist. It achieves its biological effect by competitively binding to the GABAA receptor, blocking the inhibitory neural transmission of γ-aminobutyric acid (GABA), thereby exerting its antagonistic action. This antagonistic effect makes Bicuculline highly applicable in the field of neuroscience research, such as for studying the role of GABAergic neural transmission in epilepsy, anxiety, and cognitive functions. Additionally, Bicuculline also inhibits calcium-activated potassium channels (SK channels) and blocks slow afterhyperpolarization (slow AHP), further influencing the excitability of neurons. These biological activities make Bicuculline an important tool for studying the electrophysiological characteristics of neurons and the interaction of neurotransmitters.
The chemical properties of Bicuculline are also reflected in its molecular structure. It belongs to the phthaloylisoquinoline class of compounds and has a complex molecular structure, including an isoquinoline ring and a furan-benzo-dioxane system. This structural feature endows Bicuculline with unique chemical and biological activities, making it a research hotspot in the fields of natural product chemistry and medicinal chemistry.

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