Terpenoids from Glechoma hederacea var. longituba and Their Biological Activities

Glechoma hederacea var. longituba (common name: ground-ivy) has been used for the treatment of asthma, bronchitis, cholelithiasis, colds, and inflammation. In the present study, three new sesquiterpene glycosides (1–3), two new diterpene glycosides (4–5), and four known compounds (6–9) were isolated from its MeOH extract. Structure elucidation was performed for the five new compounds (1–5) using 1D and 2D NMR, HRESIMS, ECD calculation, and chemical methods. All the isolates (1–9) were assessed for their anti-neuroinflammatory activity on nitric oxide (NO) production in lipopolysaccharide (LPS)-activated BV-2 cells, nerve growth factor (NGF) secretion stimulation activity in C6 glioma cells, and cytotoxic activity against four human cancer cell lines (A549, SK-OV-3, SK-MEL-2, and HCT15). Compounds 2 and 5–7 exhibited inhibitory effects on NO production with IC50 values of 52.21, 47.90, 61.61, and 25.35 μM, respectively. Compound 5 also exhibited a significant stimulating effect on NGF secretion (122.77 ± 8.10%). Compound 9 showed potent cytotoxic activity against SK-OV-3 (IC50 3.76 μM) and SK-MEL-2 (IC50 1.48 μM) cell lines, while 7 displayed a strong cytotoxic activity against SK-MEL-2 (IC50 9.81 μM) cell line

Compositional Characteristics of Glucuronide Conjugates in Regional Glechoma hederacea var. longituba Herbal Extracts Using a Set of Polyphenolic Marker Compounds

Glechoma hederacea var. longituba (GHL) is one of many herbal plants widely used in hot herbal teas and in oriental prescriptions to treat various diseases. Although the beneficial effects of GHL may be influenced by differences in the composition of active constituents in the herbal extracts, there are few reports on the compositional characteristics of GHL herbal extracts to date. In this study, liquid chromatography–mass spectrometry technology was used for comparative analysis of constituents in hot-water extracts of GHL samples obtained from various cultivating provinces in South Korea. A set of marker panel consisting of nine polyphenolic compounds, including glucuronide conjugates in particular, was constructed and used to monitor the compositional characteristics in each GHL extract. Our findings show that some of the marker compounds, including rosmarinic acid, were persistently observed as major constituents in the analyses of the 22 GHL sample extracts, whereas, interestingly, other marker compounds such as polyphenol-glucuronic acid conjugates displayed dramatic differences in compositional ratios. This chromatographic approach using the marker compound panel can be applied to qualitatively and quantitatively evaluate compositional characteristics in the GHL extracts, and can also be useful for quality assays of the GHL herbal plant in medicinal and industrial fields.

Protective effect of Glechoma hederacea extract against gallstone formation in rodent models

Background Our current study aimed to evaluate the effect of an Glechoma hederacea extract (Hitrechol®) in normal rats and gallstone diseased mice to explore its underlying mechanisms. Normal rats and C57BL/6 mice with/without cholesterol gallstone were used in this study. Methods To monitor the effect of Hitrechol® on bile secretion, bile flow rates at 15 min interval until 2 h post-dosing in normal rats treated with vehicle and Hitrechol® were compared using multiple t-test with a p < 0.05 considered as statistically significant different. To further evaluate the effect of Hitrechol® against the development of gallstone in lithogenic diet treated mice, mice were treated with vehicle or Hitrechol® (QD-once daily or TID-three times daily) for 3 weeks followed by comparing the levels of bile composition among the treatment groups. In addition, the anti-oxidative biomarkers in liver and anti-inflammatory biomarkers in serum were detected and compared among all the treatment groups to evaluate the hepato-protective effect of Hitrechol®. The obtained levels of biomarkers and bile composition were compared among different treatment groups using one-way ANOVA tests followed by Tukey’s multiple comparisons with p < 0.05 considered as statistically significant. Results Despite no significant impact on the bile flow rate, Hitrechol® TID treatment dramatically decreased size and amount of gallstone crystals and total cholesterol level (p < 0.05), as well as total bile acid (p < 0.05) and several types of bile acid (p < 0.05) levels in gallstone disease model mice. Hitrechol® TID treatment could significantly decrease the frequencies of hepatocyte necrosis and lipid aggregation notably as well as increase the antioxidant enzyme level (p < 0.05) in the liver. Conclusions Our findings for the first time demonstrated the beneficial effect of Hitrechol® against gallstone via its litholytic, liver-protective and antioxidant activities.

ANTI-INFLUENZA ACTIVITY OF PLANT EXTRACTS OF THE LAMIACEAE FAMILY

In this work, it was revealed that water and ethanol extracts of the plants Nepeta cataria, Nepeta sibirica, Scutellaria baicalensis, Hyssopus officinalis, Betonica officinalis, and water extracts of Dracocephalum moldavica, Glechoma hederacea, Mentha arvensis, Prunella vulgaris, Melissa officinalis ethanol extracts of Mentha piperita, Mentha crispa, Origanum vulgare, Hyssopus officinalis, Salvia verticillata showed antiviral activity against the influenza virus subtype H5N1. Aqueous extracts of Nepeta cataria and Glechoma hederacea (NI 3.75) showed the highest antiviral effect against the H5N1 subtype. It was revealed the antiviral activity against influenza virus subtype H3N2 of aqueous and ethanol extracts of Scutellaria baicalensis, Mentha piperita, Mentha arvensis, Mentha crispa, aqueous extract of Dracocephalum moldavica and ethanol extracts of Glechoma hederacea, Origanum vulgare, Prunella vulgaris, Hyssopus officinalis, Betonica officinalis, Salvia verticillata. Ethanolic extract of Betonica officinalis (NI 4.25) showed the highest virus neutralizing activity against the H3N2 subtype. It was carried out chemical analysis of the aerial parts of plants of the Lamiaceae family. It was shown that the highest content of flavonols was observed in Dracocephalum nutans (4.47±0.04%), the highest content of tannins was found in Mentha arvensis (17.62 ± 0.78%), and the highest content catechins were found in Nepeta cataria (0.43 ± 0.007%). Thus, plant extracts of the Lamiaceae family are promising sources for further studies to develop new antiviral drugs.

Protective Effect of Glechoma Hederacea Extract Against Gallstone Formation in Rodent Models

Background: Our current study aimed to evaluate the effect of an Glechoma Hederacea extract (Hitrechol ®) in normal rats and gallstone diseased mice to explore its underlying mechanisms. Normal rats and C57BL/6 mice with/without cholesterol gallstone were used in this study. Methods: To monitor the effect of Hitrechol ®️ on bile secretion, bile flow rates at 15 min interval until 2 hours post-dosing in normal rats treated with vehicle and Hitrechol ®️ were compared using multiple t-test with a p<0.05 considered as statistically significant different. To further evaluate the effect of Hitrechol ®️ against the development of gallstone, mice were treated with vehicle or Hitrechol (QD-once daily or TID-three times daily) for 3 weeks followed by comparing the levels of bile composition among the treatment groups. In addition, the anti-oxidative biomarkers in liver and anti-inflammatory biomarker in serum were detected and compared among all the treatment groups to evaluate the hepato-protective effect of Hitrechol ®️. The obtained levels of biomarkers and bile composition were compared among different treatment groups using one-way ANOVA tests followed by Tukey’s mutiple comparisons with p<0.05 considered as statistically significant. Results: Despite no significant impact on the bile flow rate, Hitrechol TID treatment dramatically decreased size and amount of gallstone crystals and total cholesterol level (p<0.05), as well as total bile acid (p<0.05) and several types of bile acid (p<0.05) levels in gallstone diseased model mice. Hitrechol ®️ TID treatment could significantly decrease the frequencies of hepatocyte necrosis and lipid aggregation notably as well as increase the antioxidant enzymes level (p<0.05) in liver. Conclusions: Our findings for the first time demonstrated the beneficial effect of Hitrechol ®️ against gallstone via its litholytic, liver-protective and antioxidant activities.