Pharmacological effects and metabolite analysis of Matrine

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 The metabolite content of drugs in organisms is minimal, and it is not easy to isolate and prepare pure products. The metabolite structure is complex, and it is also challenging to obtain metabolites by chemical synthesis. Thus the study of metabolite analysis of drugs in organisms is minimal.

Bitter ginseng is the dried root of bitter legume ginseng. The secondary metabolites currently isolated from bitter ginseng are mainly alkaloids and flavonoids, in addition to a few phenolic, triterpenoid, phenylpropanoid, fatty acid, and amino acid components. Domestic and foreign research focuses on its alkaloid components. The alkaloids extracted, isolated, and identified from the bitter ginseng plant now include bitter ginseng alkaloids, oxymatrine, iso-bitter ginseng alkaloids, hydroxy bitter ginseng alkaloids, lacustrine, oxymatrine, etc. 


Metabolite identification refers to identifying and characterizing the small molecules (metabolites) present in a biological sample, such as blood, urine, or tissue. This can be accomplished using various techniques, including mass spectrometry, nuclear magnetic resonance (NMR) spectroscopy, and chromatography.

The use of liquid mass spectrometry (LCMS) technology allows for the separation and purification of metabolite samples and the identification and quantitative analysis of trace drug metabolites that were previously difficult to identify. Medicilon can provide drug metabolite analysis services for our customers.

Bitter ginseng alkaloids are extracted from the dried roots, plants, and fruits of bitter ginseng by organic solvents such as ethanol and are generally total bitter ginseng alkaloids, of which bitter ginseng alkaloids and oxidized bitter ginseng alkaloids have the highest content.

1. Pharmacological study of bitter ginseng alkaloids

In Preclinical research, pharmacological studies are research studies that investigate the effects of drugs on living organisms. These studies are conducted to understand the mechanisms of drug action, the optimal dosage, and potential side effects. Various pharmacological studies include in vitro, in vivo, and clinical trials.

Pharmacological studies are essential to drug development and are used to understand new drugs' potential benefits and risks.

In vitro studies are conducted in laboratory settings using cell cultures or isolated tissues. These studies provide information on the cellular and molecular mechanisms of drug action.

In vivo studies are conducted on living organisms like animals or humans. These studies provide information on the pharmacokinetics and pharmacodynamics of drugs and their safety and efficacy.

Pharmacological studies on bitter ginseng alkaloids found that its pharmacological effects are pervasive, mainly antitumor, anti-liver damage, treatment of cardiovascular and cerebrovascular diseases, anti-virus, hypolipidemic, anti-inflammatory, and other pharmacological effects.

(1) Anti-tumor effects

Studies have shown that matrine can inhibit the proliferation of tumor cells and induce tumor cell differentiation. The mechanism is that matrine can interfere with the tumor cell cycle, inhibit the telomerase activity of tumor cells, and change the expression of oncogenes and tumor-related proteins. Matrine can induce apoptosis and inhibit autophagy of tumor cells and has a particular inhibitory effect on tumor invasion and metastasis. Some researchers in China studied the effects of matrine on apoptosis and PEG10 gene expression in hepatocellular carcinoma cells and found that marine had an inhibitory effect on HepG2 proliferation at a mass concentration of more than 0.1g·L(-1), and the inhibitory effect was enhanced with the increase of drug concentration and action time; the mitochondrial membrane potential of HepG2 cells treated with matrix decreased significantly, and the expression levels of PEG10 gene and protein were downregulated. 

The mitochondrial membrane potential of HepG2 cells was significantly reduced, and the PEG10 gene and protein expression levels were down-regulated by bitter ginseng. In addition, bitter ginseng alkaloids could regulate the telomerase activity of HepG2 cells and affect their cell cycle, which is closely related to the antitumor activity of bitter ginseng alkaloids.

(2) Anti-liver injury effect

Matrine can inhibit hepatitis B surface antigen and e antigen secreted by cells during hepatitis B virus DNA transfection, and the rate of inhibition increases with the increase of drug concentration. After entering the transfected cells, bitter ginseng alkaloids can rapidly close the DNA genetic information of the hepatitis B virus, further destroy the DNA replication template of the hepatitis B virus, and at the same time, change the biochemical characteristics of hepatocyte plasma to inhibit hepatitis B virus replication without causing hepatitis B virus mutation. Picrasidine can also indirectly improve patients' clinical symptoms and promote the recovery of liver function by regulating the body's immune function.

2. Analysis of metabolites of Matrine

Liquid mass spectrometry (HPLC-MS), also called liquid chromatography-mass spectrometry, uses liquid chromatography as the separation system and mass spectrometry as the detection system. The sample is ionized and separated from the mobile phase in the mass spectrometry part. Then the ion fragments are separated by mass number by the mass analyzer of the mass spectrometry, and the detector obtains the mass spectra.

The experimental conditions of liquid chromatography-electrospray ionization ion trap mass spectrometry were optimized to study the primary metabolites of bitter ginseng base and oxidized bitter ginseng base in rats. The urine samples were collected from 0 to 24 h. The metabolites in the urine samples were enriched and purified by a C18 column and then injected into the samples for analysis under optimal conditions.

Liquid mass spectrometry combines the high separation performance of chromatography and the high discriminatory characteristic ability of mass spectrometry to form a perfect modern analytical technique, so it is crucial to apply liquid mass spectrometry to the study of bitter ginseng alkaloid metabolite analysis.

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