[Research progress on chemical constituents and pharmacological effects of Glechomae Herba and prediction of its Q-markers].

Glechomae Herba, the dried aerial part of Glechoma longituba(Labiatae), has the effects of promoting urination, draining dampness, and relieving stranguria. It has received wide attention in recent years owing to the satisfactory efficacy on lithiasis. Amid the in-depth chemical and pharmacological research, it has been found that Glechomae Herba has antibacterial, anti-inflammatory, antioxidant, antithrombotic, hepatoprotective, cholagogic, antitumor, hypoglycemic, and lipid-lowering effects. The main chemical constituents are volatile oils, flavonoids, terpenoids, phenylpropanoids, and organic acids. This paper summarized the chemical constituents and pharmacological effects of Glechomae Herba. Based on genetic relationship of plants, the characteristics, efficacy, and pharmacokinetics of the chemical constituents, and the potential of these constituents as quality markers(Q-markers), it was summed up that ursolic acid, caffeic acid, rosmarinic acid, luteolin-7-O-diglucuronide, apigenin, apigenin-7-O-diglucuronide, apigetrin, and glechone can be the candidate Q-markers of Glechomae Herba.

Research progress on chemical constituents and pharmacological effects of Glechomae Herba and prediction of its Q-markers / 中国中药杂志

Glechomae Herba, the dried aerial part of Glechoma longituba(Labiatae), has the effects of promoting urination, draining dampness, and relieving stranguria. It has received wide attention in recent years owing to the satisfactory efficacy on lithiasis. Amid the in-depth chemical and pharmacological research, it has been found that Glechomae Herba has antibacterial, anti-inflammatory, antioxidant, antithrombotic, hepatoprotective, cholagogic, antitumor, hypoglycemic, and lipid-lowering effects. The main chemical constituents are volatile oils, flavonoids, terpenoids, phenylpropanoids, and organic acids. This paper summarized the chemical constituents and pharmacological effects of Glechomae Herba. Based on genetic relationship of plants, the characteristics, efficacy, and pharmacokinetics of the chemical constituents, and the potential of these constituents as quality markers(Q-markers), it was summed up that ursolic acid, caffeic acid, rosmarinic acid, luteolin-7-O-diglucuronide, apigenin, apigenin-7-O-diglucuronide, apigetrin, and glechone can be the candidate Q-markers of Glechomae Herba.

Screening out key compounds of Glechomae Herba for antiurolithic activity and quality control based on spectrum-effect relationships coupled with UPLC-QDA.

Glechomae Herba (GH) has been widely used in the treatment of urolithiasis, especially kidney stones, in China and Southeast Asia. Pharmacological studies have suggested that the antioxidant property of GH contributes to its anticalculus effect. CaSR is one of the main locations of kidney stones, and the mechanism of action of CaSR inhibitors in the treatment of kidney stones is similar to that of GH. However, until now, the antiurolithic chemical compounds in GH and their interaction with CaSR remain unknown. In our study, we revealed the interaction between the active compounds in GH and the active compounds in CaSR inhibitors by using spectrum-effect relationship analysis, pharmacodynamics, and molecular docking techniques. The results showed ten common peaks from the fingerprints of GH extracts from different regions. Pharmacological experiments showed that GH could significantly treat renal tissue lesions. Chlorogenic acid (CA), rosmarinic acid (RA), P5, luteolin, apigenin, and P9 were screened after the analysis of spectrum-effect relationships. In vitro validation experiments showed that all the screened compounds had inhibitory effects on the development of kidney stones in our model. The molecular docking results showed that the above compounds could be docked with CaSR in a natural state, and the docking score was less than 7. This work constructs a general model for the combination of UPLC-QDA and antiurolithic drugs, studies the spectrum-effect relationship of GH, and provides a new possibility for the development of new antiurolithic drugs.

Chemical composition and anti-complement activity of Glechomae Herba collected in different months.

Glechomae Herba (GH) is derived from the dried aerial part of Glechoma longituba (Nakai) Kupr., which is harvested from spring to autumn. It has the effects of clearing heat and detoxification. The aim of this paper was to study the chemical composition and the anti-complement activity of GH collected in different months. Ultra-high-performance liquid chromatography coupled to quadrupole time-of-flight tandem mass spectrometry based on predicted compounds screening and diagnostic ion filter strategy was developed for identifying the chemical composition of GH collected in different months. A total of 102 compounds-40 chlorogenic acids (CGAs), 32 phenolic acids, and 30 flavonoids-were reasonably identified in GH. Thirty-four CGAs were discovered in GH for the first time. The correlations between chemical compositions and anti-complement activities of GH collected in different months were analyzed. Phenolic acids and flavonoids were found to be negatively correlated with anti-complement activity, and CGAs were positively correlated with anti-complement activity. At the same time, six CGA standards had obvious anti-complement activity. It was demonstrated that different harvest months had a significant impact on the difference in chemical composition and anti-complement activity of GH. And CGAs might play an important role in the anti-complement activity of GH.

Structural characterization and anti-complement activity of polysaccharides from Glechomae Herba / 中草药

Objective: To isolate and purify the homogeneous polysaccharides from Glechomae Herba through the guidance of anti-complement activity, and study their structures. Methods: Crude polysaccharides from Glechomae Herba were extracted by water extraction and alcohol precipitation, then homogeneous polysaccharides were separated by DEAE-52 and Sephadex G-100 column chromatography. The structures of homogeneous polysaccharides were characterized by HPGPC, IR, GC, methylation and NMR, and their anti-complement activities were also determined. Results: Two homogeneous polysaccharides GLP-1 and GLP-2 were obtained with the molecular weight of 5 370 and 20 040. They were both heteropolysaccharides composed of arabinose and galactose with the ratio of 1:6.3 and 1:4.9, respectively. Conclusion: The structures of GLP-1 and GLP-2 further elucidate the pharmacodynamic basis of their anti-complement activities and provide basis for screening natural complement inhibitors.

Comprehensive metabolic profile of phenolic acids and flavonoids in Glechomae Herba using ultra-high-performance liquid chromatography coupled to quadrupole-time-of-flight tandem mass spectrometry with diagnostic ion filtering strategy.

Glechomae Herba (GH), a traditional Chinese medicine, is commonly used for the treatment of urolithiasis and cholelithiasis based on its diuretic and cholagogic actions. However, relatively few studies have been conducted to describe this medicine's metabolites. Therefore, an ultra-high-performance liquid chromatography coupled to quadrupole time of flight tandem mass spectrometry (UHPLC-QTOF-MS/MS) analysis with diagnostic product ions and neutral loss filtering strategy was established for the metabolic profiling profile of GH. First, an analytical method was established to detect the compounds in GH extracts and complex rat biosamples, including urine, bile, plasma and feces, after oral administration of GH extracts based on the holistic fingerprint approach utilizing UHPLC-QTOF-MS/MS. Second, the exogenously sourced ions were filtered out by the MarkerView software incorporated in Microsoft Office. Third, the diagnostic product ions and neutral loss filtering strategy were developed for the rapid identification of the metabolites. Finally, a total of 91 constituents, including 13 prototype compounds and 78 metabolites, were unambiguously or reasonably identified in rat biosamples. The metabolites were mainly eliminated by urine (82 metabolites) and bile (19 metabolites), and notably few metabolites were eliminated through feces (4 metabolites). Glucuronidation, methylation and sulfation were the primary metabolic pathways of phenolic acids and flavonoids. The primarily urine and bile elimination of metabolites may be related to the anti-urolithiasis and anti-cholelithiasis effects of GH. This work demonstrated the feasibility of an integrated strategy for the rapid identification of the metabolites after oral administration of GH extracts provided essential data for exploring the bioactive ingredients of GH in the treatment of urolithiasis and cholelithiasis.

Geographical discrimination of Glechomae Herba based on fifteen phenolic constituents determined by LC-MS/MS method combined with chemometric methods.

Glechomae Herba (GH) is rich in bioactive phenolic constituents and is widely used for treatment of cholelithiasis, urolithiasis and dropsy. The simultaneous determination of phenolic constituents in GH from different geographical origins is significant for authentication and quality control purposes. In this study, we developed a strategy integrating targeted analysis and chemometric methods for quality evaluation and discrimination of GH from different geographical origins. Firstly, an accurate and reliable liquid chromatography-tandem mass spectrometry method was developed for simultaneous quantification of 15 phenolic constituents in GH from different geographical origins. The established method was well validated in terms of desirable specificity, linearity, precision and accuracy. Secondly, the quantitative data were subjected to principal component analysis and orthogonal partial least squares discriminant analysis. Thirdly, a heatmap visualization was employed for clarifying the distribution of 15 phenolic compounds in GH from different geographical origins. These results indicated that GH samples from Shandong province obviously differ from those from other provinces in the content of bioactive phenolic constituents. Collectively, the proposed platform might be a suitable tool for quality evaluation and discrimination of GH from different geographical origins, providing promising perspectives in tracking the formulation processes of traditional Chinese medicine products.