Product name: Sinomenine hydrochloride
Synonym name:
Catalogue No.: BP1314
Cas No.: 6080-33-7
Formula: C19H24ClNO4
Mol Weight: 365.854
Botanical Source: Sinomenii caulis
Physical Description:
Type of Compound: Alkaloids
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.
Storage conditions：Short-term storage at 2~8℃, long-term storage at -20 ~ -80℃
Sinomenine hydrochloride (CAS number: 6080-33-7) is a natural alkaloid derived from the Chinese medicinal herb Sinomenium acutum. As an important component used in traditional Chinese medicine for the treatment of rheumatoid arthritis, matrine hydrochloride has attracted widespread attention in the field of natural medicine research in recent years due to its significant anti-inflammatory and analgesic effects. Its unique pharmacological activity is mainly attributed to its regulation of various inflammation related signaling pathways, especially its effective blockade of nuclear factor kappa B (NF - κ B) activation. In addition, matrine hydrochloride also exhibits an activating effect on μ - opioid receptors, endowing them with potential analgesic effects. This article will 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 matrine hydrochloride, and prospects its clinical application prospects.
The chemical name of Sinomenine hydrochloride is Sinomenine hydrochloride, with a molecular formula of C19H23NO.4 · HCl and a molecular weight of 329.3960. Its structure belongs to the indole alkaloid class, with a complex polycyclic skeleton containing multiple chiral centers. The LogP value of matrine hydrochloride is 1.8006, indicating that it has moderate lipid solubility, which is beneficial for cell membrane penetration and in vivo distribution. The polar surface area (TPSA) is 59.0 Å ², exhibiting certain polarity characteristics that contribute to its water solubility and bioavailability. The water solubility index is 1.3623, indicating that matrine hydrochloride has good solubility in water and is convenient for formulation development. Its blood-brain barrier penetration ability is high, indicating that the compound can act on the central nervous system. Importantly, matrine hydrochloride did not exhibit hERG channel inhibition, reducing the risk of cardiac toxicity, and the Ames test result was 0.0, indicating no significant genotoxicity.
The structural characteristics of matrine hydrochloride enable it to interact with multiple targets at the molecular level, especially inflammation related signaling molecules and receptors, laying the foundation for its multi-target pharmacological activity.
Hydrochloric acid matrine mainly comes from the plant Sinomenium acutum in the Ranunculaceae family, which is widely distributed in southern China and Southeast Asia. The rhizome and vine of Qingteng are the main collection parts of traditional Chinese medicinal materials, containing rich alkaloid components, among which Qingteng alkaloid is the main component. Traditional extraction methods often use alcohol solvents (such as ethanol and methanol) for extraction, combined with acidic conditions to convert matrine into its hydrochloride form to improve stability and water solubility.
Modern extraction processes typically include the following steps:
In recent years, the application of new technologies such as ultrasound assisted extraction and microwave-assisted extraction has improved extraction efficiency and purity, while reducing solvent usage and environmental pollution.
The pharmacological activity research of matrine hydrochloride mainly focuses on its anti-inflammatory, analgesic, and immunomodulatory effects. Numerous in vitro and in vivo experiments have shown that matrine hydrochloride can significantly inhibit the production of various inflammatory mediators, alleviate inflammatory reactions, and improve the pathological state of inflammatory diseases such as arthritis.
Sinomenine hydrochloride reduces the levels of inflammatory mediators in the inflammatory microenvironment by inhibiting the expression of pro-inflammatory cytokines such as tumor necrosis factor alpha (TNF - α), interleukin-6 (IL-6), and nitric oxide synthase 2 (NOS2). Its regulatory effect on cyclooxygenase-1 (PTGS1) and cyclooxygenase-2 (PTGS2) helps to inhibit prostaglandin synthesis, alleviate inflammation and pain.
Sinomenine hydrochloride, as a μ - opioid receptor agonist, can activate central and peripheral opioid receptors and exert analgesic effects. In addition, its regulation of transient receptor potential vanillic acid receptor 1 (TRPV1) and transient receptor potential channel associated protein 1 (TRPA1) is involved in the transmission and regulation of pain signals.
Sinomenine hydrochloride can regulate the activity of signal transducer and activator of transcription factor 3 (STAT3) and caspase 1 (CASP1), regulate the inflammatory response and apoptosis process of immune cells, and promote the maintenance of immune homeostasis.
The anti-inflammatory and analgesic mechanisms of matrine hydrochloride are complex, involving multiple signaling pathways and molecular targets, mainly including:
NF - κ B is a key transcription factor that regulates the inflammatory response. Sinomenine hydrochloride inhibits the activation of NF - κ B, blocks its nuclear translocation, reduces the transcriptional expression of pro-inflammatory genes, thereby reducing the production of inflammatory mediators such as TNF - α and IL-6, and alleviating the inflammatory response.
Sinomenine hydrochloride inhibits IL-6-induced STAT3 phosphorylation, blocks STAT3 mediated inflammatory gene expression, and exerts anti-inflammatory and immune regulatory effects.
By inhibiting CASP1 activity, matrine hydrochloride reduces the activation of inflammasomes, lowers the release of inflammatory factors such as IL-1 β, and alleviates inflammatory damage.
The inhibitory effect of matrine hydrochloride on TRPV1 and TRPA1 channels can help alleviate inflammatory and neuropathic pain, and regulate the transmission of pain signals.
Sinomenine hydrochloride also regulates the expression of PTGS1, PTGS2, and NOS2, affects the synthesis of prostaglandins and nitric oxide, and participates in the regulation of inflammation and vascular response.
Sinomenine hydrochloride exhibits good pharmacological properties in terms of drug formation. Its moderate molecular weight (329.4), suitable lipid solubility (LogP 1.8), and low polar surface area (TPSA 59) give it good oral absorption potential. Good water solubility, convenient for the development and application of formulations.
Sinomenine hydrochloride has a high blood-brain barrier penetration ability and can act on the central nervous system, explaining its potential mechanisms of analgesia and neuroprotection.
Sinomenine hydrochloride did not show hERG channel inhibition, indicating a low risk of cardiac toxicity. The Ames test result is 0.0, indicating no significant genotoxicity and high safety.
In vivo studies have shown that matrine hydrochloride is rapidly absorbed after oral administration, with a rapid peak in plasma concentration and widespread distribution, especially in high concentrations in liver, kidney, and brain tissues. Its metabolism is mainly carried out through the liver enzyme system, and the metabolites are excreted through the kidneys. Moderate half-life, suitable for daily administration.
Sinomenine hydrochloride, as a natural source anti-inflammatory and analgesic drug, has shown good efficacy and safety in the clinical treatment of inflammatory diseases such as rheumatoid arthritis and rheumatoid arthritis. Its multi-target and multi mechanism pharmacological properties give it unique advantages in modern drug development.
Future research directions include:
Sinomenine hydrochloride, as a natural product with a long history of application, has shown great potential for drug development due to its unique chemical structure and multi-target anti-inflammatory and analgesic effects. Its excellent drug properties, safety, and diverse mechanisms of action provide a model for the modern development of natural medicines. In the future, combined with advanced drug design and clinical research, sinomenine hydrochloride is expected to become an effective drug for treating inflammatory diseases and related pain, bringing more benefits to patients.
