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Product name: Jatrorrhizine chloride
Synonym name: Neprotine chloride； Deleted Cas No.: 960383-96-4
Catalogue No.: BP0809
Cas No.: 6681-15-8
Formula: C20H20ClNO4
Mol Weight: 373.833
Botanical Source:
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.
Description:
Jatrorrhizine hydrochloride has lipid lowering effects, it can ameliorate hyperlipidemia via the suppression of lipogenesis and the enhancement of lipid oxidation in the liver. It exhibits a potent inhibitory effect toward neuraminidase of the H7N9 (N9) avian influenza virus, it also can potentiate the neuraminidase inhibitory effect of oseltamivir towards H7N9 influenza. Jatrorrhizine hydrochloride is a potential new antimelanoma drug candidate, can inhibit the proliferation and neovascularization of C8161 metastatic melanoma cells with low toxicity.
References:
Anticancer Drugs. 2013 Aug;24(7):667-76.
Jatrorrhizine hydrochloride inhibits the proliferation and neovascularization of C8161 metastatic melanoma cells.
Malignant melanoma is the most aggressive form of skin cancer. Although various antimelanoma approaches have been used in the clinics to treat the disease over the last three decades, none of the drugs significantly prolonged the survival of metastatic melanoma patients; hence, effective drugs against metastatic melanoma are highly desired.
METHODS AND RESULTS:
In this study, we explored an antimetastatic melanoma agent derived from traditional Chinese medicinal herbs and found that Jatrorrhizine Hydrochloride (JH), an active component of the traditional Chinese medicinal herb Coptis chinensis, inhibited the proliferation and neovascularization of C8161 human metastatic melanoma cells. JH suppressed C8161 cell proliferation in a dose-dependent manner, with a half-maximal inhibitory concentration of 47.4±1.6 μmol/l; however, it did not induce significant cellular apoptosis at doses up to 320 μmol/l. Mechanistic studies showed that JH-induced C8161 cell cycle arrest at the G0/G1 transition, which was accompanied by overexpression of the cell cycle-suppressive genes p21 and p27 at higher doses. Moreover, JH reduced C8161 cell-mediated neovascularization in vitro and in vivo and impeded the expression of the gene for VE-cadherin, a key protein in tumor vasculogenic mimicry and angiogenesis.
CONCLUSIONS:
Taken together, the effective inhibitory effects of JH on metastatic melanoma cell proliferation and neovascularization with low toxicity suggest that JH is a potential new antimelanoma drug candidate.
Mol Med Rep. 2016 Oct;14(4):3277-84.
Jatrorrhizine hydrochloride attenuates hyperlipidemia in a high-fat diet-induced obesity mouse model. Jatrorrhizine Hydrochloride (JH) is an active component of the traditional Chinese herb Coptis chinensis, which has been used to prevent and treat metabolic disorders. Hyperlipidemia is one of the principal factors underlying numerous metabolic diseases, including diabetes and obesity. Therefore, the aim of the present study was to investigate the lipid lowering effects of JH treatment in vivo in an obesity mouse model. JH-treated hyperlipidemic mice exhibited a reduction in body weight, as well as improved glucose tolerance and insulin sensitivity. In addition, JH‑treated hyperlipidemic mice exhibited reduced serum triglyceride, total cholesterol and low‑density lipoprotein cholesterol levels, as well as increased high‑density lipoprotein cholesterol levels compared with untreated mice fed a high‑fat diet. Notably, JH treatment ameliorated the pathophysiological changes observed in the livers of hyperlipidemic mice. At the molecular level, JH downregulated the hepatic mRNA expression levels of SREBP‑1c and FAS, and induced PPAR‑α and CPT1A mRNA expression in hyperlipidemic mice. These findings suggest that JH ameliorates hyperlipidemia via the suppression of lipogenesis and the enhancement of lipid oxidation in the liver.
HPLC of Jatrorrhizine chloride
Storage conditions：Short-term storage at 2~8℃, long-term storage at -20 ~ -80℃
51.8000
.5732
.5219
.4907
1.0052
15.1231
Low
41.1612
2.8728
Yes
No
No
No
Yes
Yes
0.9
No
No
No
No
Jatrorrhizine chloride (CAS No.: 6681-15-8) is a natural alkaloid isolated from the traditional Chinese medicine Coptis (Coptis chinensis Franch.) and belongs to the isoquinoline alkaloid family. As a versatile natural product, rhizodium hydrochloride has attracted widespread attention for its remarkable neuroprotective, antibacterial, antimalarial, and antioxidant activities. In recent years, with the increasing demand for the treatment of neurodegenerative diseases, antimicrobial resistance, and neuropsychiatric disorders, the pharmacological effects and mechanisms of Root Hydrochloride have been thoroughly studied, demonstrating its potential application value in the treatment of various diseases.
This review aims to systematically summarize the chemical structure and physicochemical properties of Root Hydrochloride alkaloids, plant origins and extraction processes, pharmacological activity and mechanisms of action, druggability evaluation, and pharmacokinetic characteristics, explore its clinical application prospects, and provide theoretical basis and research directions for further drug development and clinical translation of Root Hydrochloride.
Hydrochloric acid root alkaloid is an isoquinoline alkaloid with the molecular formula C20H20ClNO4 and a molecular weight of 338.3830. Its chemical structure includes a typical tetracyclic isoquinoline backbone, with methoxy and hydroxyl substituents, giving it strong biological activity. The polar groups present in the structure give it moderate water solubility, with a LogP value of 0.5732, indicating low hydrophobicity and conducive to distribution in vivo.
In terms of physicochemical properties, the topological surface area (TPSA) of Hydrochloric Acid Root Alkaloid is 51.8 Ų, indicating certain polarity that facilitates binding to biological macromolecule targets. Its water solubility is 0.4907, making it a medium-soluble compound suitable for oral administration. The low permeability of the blood-brain barrier (BBB) suggests that its direct role in the central nervous system may be limited, but this also reduces the risk of potential central toxicity. The hERG channel inhibition test results were negative, indicating that the root alkaloid hydrochloride has good safety in terms of cardiac toxicity. The Ames test result was 0.9, indicating a low genotoxicity risk.
In summary, the physicochemical properties of the root alkaloid hydrochloride support its potential for oral drug development and provide a solid safety foundation.
Rhizopharine hydrochloride mainly comes from the Chinese medicinal herb Coptis, which belongs to the Ranunculaceae family and the dried rhizomes of Coptis chinensis Franch. As a traditional Chinese medicine, Coptis chinensis is widely used in clinical treatments such as clearing heat, drying dampness, purging fire, and detoxifying. Its main active ingredients are various isoquinoline alkaloids, including hydrochloride root alkaloids, berberine, and fritilline alkaloids.
The extraction of chloride root alkali usually uses acidic aqueous solutions or organic solvent extraction methods. Common processes include:
After extraction, identification and purity testing are usually performed using high-performance liquid chromatography (HPLC), mass spectrometry (MS), and nuclear magnetic resonance (NMR) techniques.
Rhizalkaloid hydrochloride exhibits multiple pharmacological activities, covering neuroprotection, antibacterial, antimalarial parasite, and antioxidant properties, as detailed below:
Chlorohydrochloride, as an acetylcholinesterase (AChE) inhibitor, has an IC50 of about 872 nM, demonstrating good enzyme inhibitory activity. Its selectivity for BuChE inhibition is up to 115-fold, indicating that it mainly acts on AChE, reduces acetylcholine degradation, enhances neurotransmitter function, and has potential therapeutic value for neurodegenerative diseases such as Alzheimer's disease (AD).
Additionally, rhizolline hydrochloride can reduce the uptake of serotonin (5-HT) and norepinephrine (NE) by inhibiting uptake-2 transporters, regulating neurotransmitter balance, and may have adjunctive therapeutic effects on mental illnesses such as depression and anxiety.
Rhizalkaloids hydrochloride exhibit inhibitory effects on various bacteria, targeting DNA gyrase (GYRA), cell wall synthase (FABI), and dihydrofolate reductase (DHFR). Additionally, it acts on fungi such as ERG11 (cytochrome P450 14α-demethylase) and CDR1 (multidrug resistance-associated transporter), demonstrating broad-spectrum antibacterial and antifungal potential.
Hydrochloric acid drug rhizolline exhibits a certain inhibitory effect on Plasmodium, possibly related to its interference with parasite metabolic enzymes and redox balance, with specific targets still to be further clarified.
Hydrochloride root alkaloids have the ability to scavenge free radicals and inhibit lipid peroxidation, reduce oxidative stress damage, protect cells from oxidative damage, and enhance cell survival rates.
The multiple pharmacological effects of Pharmacine Hydrochloride depend on its interactions with various biological macromolecule targets, mainly including:
Rhizaline hydrochloride binds to the active site of AChE, blocking the hydrolysis of acetylcholine, prolonging the duration of neurotransmitter action and improving cognitive function. It has high selectivity for inhibiting BuChE, reducing side effects caused by non-specific enzyme inhibition.
Hydrochloride inhibits the uptake-2 transporter of serotonin and norepinephrine, reduces the reuptake of neurotransmitters, increases their concentration in the synaptic cleft, and regulates mood and neural excitability.
Chlorochloric acid root alkaloid inhibits the activities of key enzymes such as bacterial DNA gyrase (GYRA), cell wall synthase (FABI), and dihydrofolate reductase (DHFR), blocking bacterial DNA replication, cell wall synthesis, and nucleic acid metabolism, thereby exerting antibacterial effects. Inhibition of fungi ERG11 and CDR1 interferes with fungal membrane synthesis and multidrug resistance mechanisms.
Hydrochloric acid can eliminate reactive oxygen species (ROS), inhibit lipid peroxidation, protect mitochondrial function, reduce apoptosis, and exert antioxidant protective effects.
The druggability parameters of Root Hydrochloride indicate that it has promising potential for drug development:
Pharmacokinetics, Chloride Rhizaline exhibits good oral absorption characteristics and is widely distributed in the body. However, due to low permeability of the blood-brain barrier, its concentration in the central nervous system is low, which may limit its direct therapeutic effect on neurological diseases. The metabolic pathway mainly involves liver enzyme systems, while excretion is primarily through the kidneys and bile.
Further research is needed in the future on the activity and safety of its metabolites in vivo to optimize dosage forms and administration regimens.
As a multi-target, multifunctional natural product, Pharmacochloride alkaloid has broad clinical application potential:
Treatment of neurodegenerative diseases: Its AChE inhibitory activity offers new therapeutic approaches for cognitive disorders such as Alzheimer's disease. In the future, structural modification can enhance the permeability of the blood-brain barrier and enhance central nervous system activity.
Antimicrobial drug development: Facing the increasingly severe problem of antimicrobial resistance, the multi-target antibacterial mechanism of the chloride root alkaloid provides a foundation for the development of novel antimicrobial agents. By integrating modern drug design technologies, effective drugs targeting resistant strains are expected to be developed.
Adjunctive therapy for neuropsychiatric disorders: By regulating the intake of 5-HT and NE, the drug root aline hydrochloride may play an auxiliary role in conditions such as depression and anxiety, warranting further clinical validation.
Antioxidant and anti-inflammatory applications: Its antioxidant effects help slow the progression of chronic inflammation and related diseases, expanding its application fields.
Future research should focus on optimizing the pharmacodynamics, improving dosage forms, and evaluating the safety of Cyrial Hydrochloride, combining clinical trials to verify its efficacy and safety, and promote its transition from laboratory to clinical application.
As an important active ingredient in Coptis chinensis, Phyllustrachloride shows broad prospects for drug development thanks to its diverse pharmacological activities and good medicinal properties. Its mechanisms of action in neuroprotection, antibacterial, antimalarial, and antioxidant aspects are becoming increasingly clear, providing new candidate drugs for the treatment of related diseases. Although limitations such as low blood-brain barrier permeability still exist, structural optimization and drug administration strategy improvements are expected to further enhance its clinical value.
In the future, combining modern medicinal chemistry, pharmacology, and clinical research, Pharmacine Hydrochloride is expected to become an important natural medicine in the treatment of various diseases, contributing new strength to the development of natural product pharmacology.
Shenshuai
Wenjing
Hedandan
