Anti-inflammatory activity and metabolite analysis of Duhaldea cappa Chrysanthemum extract in rats

 Duhaldea cappa chrysanthemum belongs to traditional Chinese medicine in China. The study found that Duhaldea cappa chrysanthemum extract has an antibacterial effect on Staphylococcus aureus, a new antibacterial drug resource with potential for development. 

The analysis of metabolites in the feces of rats after the administration of Duhaldea cappa extract is of great significance for the rational use of this herb and the development of new dosage forms. MetID plays a key role in drug discovery, preclinical development, and clinical development and is crucial for drug safety research and new drug development.

Generally speaking, herbal medicines have antimicrobial activity due to various chemical components in the extracts. The analysis of metabolites of the active ingredients of herbal medications in animals and humans is essential for elucidating the effectiveness of herbal medicines, exploring the principles of action of the active ingredients, and explaining the rationality of the compounding of herbal medicines.

Moreover, the research on analyzing metabolites of traditional Chinese medicine components also provides a valuable theoretical and practical basis for discovering new active ingredients, synthesizing new drugs, and developing new prodrugs. Medicilon provides drug MetID services. Its pharmacokinetic laboratory has passed the GLP certification of NMPA. The experimental research follows the guidelines of ICH, NMPA, and FDA. It can design and carry out in vivo and in vitro pharmacokinetics according to customer needs. Provide customers with a complete set of pharmacokinetic evaluation and optimization services. 

Chinese medicine and its preparations are mainly administered orally, absorbed in the gastrointestinal tract, distributed to target organs to exert therapeutic effects, and then metabolized and excreted from the body. The gastrointestinal tract is the central part of drug absorption and has a specific metabolic impact on drugs. Some drugs that are difficult to be absorbed may be transformed into easily absorbed components under the action of intestinal flora, so intestinal flora plays a vital role in the efficacy of drugs. Moreover, traditional Chinese medicine's metabolic process and mechanism of activity in vivo and its preparations are complex. We are studying the in vivo process, and natural medicinal substances after direct oral administration are challenging. Therefore, the analysis of metabolites in animals of the extracts of Eryngium lambda and the study of the in vitro metabolic law of the main medicinal substances in Eryngium lambda can lay a specific foundation for the study of the in vivo process of medicinal herbs.

1. Study on the antibacterial and anti-inflammatory activities of the extracts of Aconite

It has been reported that some researchers in China have used different solvents to extract the herb and evaluated the antibacterial and anti-inflammatory activities of the extract. The authors first used water and ethanol at different concentrations to remove the seasoning. Then they evaluated the antibacterial and anti-inflammatory activities of the sections with varying solvents of extraction using the Oxford cup method, test tube twofold dilution method, and LPS-stimulated RAW 264.7 cell model, respectively.

The results showed that the aqueous extract, 30% ethanol extract, 60% ethanol extract, and 80% ethanol extract at a raw drug concentration of 1.0 g-ml~(-1) had inhibitory effects on S. aureus. The MIC values of each extract against S. aureus were:250 mg-ml~(-1), 125 mg-ml~(-1), 62.5 mg-ml~(-1), 250 mg-ml~(-1), among which 60% ethanolic extract had the best inhibitory effect. The different quotes had no toxic effect on cells by acting on RAW 264.7 cells in the range of 0~250 μg-ml~(-1) for 24 h. The various extracts effectively inhibited the release of NO from LPS-stimulated RAW 264.7 cells in the field of 50-250 μg-ml~(-1), with 60% ethanol extract showing better antibacterial and anti-inflammatory activities. Therefore, 60% ethanol as the extraction solvent of the extracts prepared from Lepidium lamblia had better antibacterial and anti-inflammatory activities.

2. Analysis of metabolites of Duhaldea cappa Extract in rats

The metabolites in the feces of rats after the administration of Duhaldea cappa extract provide a reference for the subsequent research and development of this medicinal herb. It was reported that an investigator used ultra-performance liquid chromatography-triple quadrupole time-of-flight mass spectrometry (UPLC-Q-TOF-MS/MS) to detect the metabolites in the feces of rats after oral administration of extracts of Euphorbia lamblia at a dose of 100 g-kg~(-1) per administration. The chemical structure of the metabolites was identified using an RRHD Eclipse Plus C_(18) column (2.1 mm×100 mm, 1.8 μm) with a mobile phase of 0.1% formic acid aqueous solution-0.1% formic acid acetonitrile solution in gradient elution, an electrospray ionization source was selected, scanning was performed in negative ion mode, the accurate mass determination was performed using sodium formate calibration standards, and data processing was performed using software such as Metabolite Detect (MICR OTOF 2.3).

As a result, 22 metabolites, including prototype M8 (1,3-O-caffeoylquinic acid), M1~M4 (isomerization products of dihydro mono caffeoylquinic acid), M5 (sulfate esterification products of dihydrocaffeic acid), M6~M7 (methylation products of monocaffeoylquinic acid) were detected in rat feces. Therefore, the metabolic pathways of caffeoylquinic acid active ingredients in rat feces after the administration of Duhaldea cappa extract are mainly methylation and reduction reactions.

For treating infectious diseases, Duhaldea cappa chrysanthemum has both traditional experience and a microbiological basis in some parts of China and is a promising natural antimicrobial agent for development. 

The analysis of metabolites in rats administered with Duhaldea cappa extract can help to understand the mechanism of the antimicrobial effect of Duhaldea cappa, which can provide a reference for the subsequent research and development of this medicinal herb.