ABSTRACT
Objective:To study the effects of total flavonoids from Baeckea frutescens on the proliferation, migration, invasion, apoptosis and cell morphology changes of cervical cancer SiHa cells.Methods:Cervical cancer SiHa cells were treated with different concentrations of total flavonoids from Baeckea frutescens. CCK8 method was used to detect the proliferation and 50% inhibiting concentration (IC 50) of SiHa cells in vitro. The control group without drug treatment and the experimental group with drug concentration IC 50 were set. Transwell migration and invasion experiments were used to detect the changes of cell migration and invasion ability in vitro in the experimental group and the control group. Laser scanning confocal microscope was adopted for observing the morphological changes of apoptosis in the experimental group and the control group. Flow cytometry was used to detect the apoptosis rates of the experimental group and the control group. Results:Total flavonoids from Baeckea frutescens inhibited the proliferation of cervical cancer SiHa cells in a concentration-dependent manner. After 48 hours of action, the IC 50 value was 110.8 mg/L. In the migration experiment, the number of transmembrane cells in the control group was 644.00±10.54 and the number of transmembrane cells in the experimental group was 266.00±5.57, with a statistically significant difference ( t=54.942, P<0.001). In the invasion experiment, the number of transmembrane cells in the control group was 298.00±14.36, and the number of transmembrane cells in the experimental group was 85.00±8.62, with a statistically significant difference ( t=38.247, P<0.001). Laser scanning confocal microscope observation showed that in the experimental group, the cell membrane crumpled and lost its original morphology, and the nucleus showed typical apoptotic morphologies such as fragments of different sizes and irregular shapes, and nuclear edge aggregation; but no apoptotic cells were observed in the control group. Flow cytometry showed that the apoptosis rate in the control group was (2.95±1.36)%, and the apoptosis rate in the experimental group was (27.54±1.94)%, with a statistically significant difference ( t=-17.949, P<0.001). Conclusion:Total flavonoids from Baeckea frutescens have obvious inhibitory effects on the proliferation, migration and invasion of cervical cancer SiHa cells cultured in vitro, and promote their apoptosis.
ABSTRACT
@#The objectives of the study were to screen prostaglandin E2 receptor 4 antagonist from active compounds of Baeckea frutescens L. and to explore its anti-rheumatoid arthritis effect.The HEK293T-EP4 cell antagonist screening model was established in vitro. Homogeneous time-resolved fluorescence (HTRF) technique was used to screen the active compounds of Baeckea frutescens L..SPF grade ICR male mice were randomly divided into control group, model group, methotrexate group, and Baeckea frutescens L.compound BF-2 (100, 50 and 25 mg/kg) groups. The collagen-induced arthritis (CIA) mouse model was established in vivo. The swelling volume of the toes of mice was measured, and the pathological examination was analyzed by staining with hematoxylin and eosin.SPF grade ICR mice, male, were randomly divided into control group, BF-2 (100, 50 and 25 mg/kg) group, and aspirin group.The acetic acid-induced body writhing test was observed.The EP4 in vitro antagonist screening model was successfully established.The preliminary screening results found that BF-2, BF-20, BF-11 and BF-12 had strong EP4 antagonistic activity [(102.11 ± 3.45)%, (90.31 ± 3.59)%, (75.72 ± 1.79)% and (76.84 ± 1.64)%], and BF-2 had the strongest antagonistic activity (IC50 = 0.99 ± 0.08 μg/mL).BF-2 could significantly inhibit the toe swelling of CIA mice, and relieve the degradation of articular cartilage matrix and inflammatory cell infiltration.At the same time, compared with the control group, the writhing times of the mice in each dose of BF-2 were significantly reduced.In this study, BF-2 of Baeckea frutescens L.was selected as an EP4 antagonist, which has potential anti-rheumatoid arthritis activity.
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Phytochemical investigation of the aerial parts of Baeckea frutescens resulted in the isolation of three new mono- or sesquiterpene-based meroterpenoids, frutescones S-U (1-3), and one pair of new (±)-5,7-dihydroxy-8-isobutyryl-6-methyldihydroflavonol (4). Their structures and absolute configurations were established by HR-ESI-MS, 1D and 2D NMR, and quantum chemical ECD calculation. Compound 1 exhibited inhibitory effect on NO production in LPS-activated RAW 264.7 macrophages with an IC value being 0.81 μmol·L.
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In the present study, we carried out a phytochemical investigation of the ethanol extract of the aerial parts of Baeckea frutescens, which resulted in the isolation of two new flavonoid glycosides, myricetin 3-O-(5″-O-galloyl)-α-L-arabinofuranoside (1), 6-methylquercetin 7-O-β-D-glucopyranoside (2), one new methylchromone glycoside, 7-O-(4', 6'-digalloyl)-β-D-glucopyranosyl-5-hydroxy-2-methylchromone (3), together with three known compounds (4-6). The structures of these isolated compounds were established on the basis of 1D and 2D NMR techniques and chemical methods. The anti-inflammatory activities of the compounds 1-6 were evaluated for their inhibitory effects against cyclooxygenases-1 and -2 in vitro. Compounds 1-6 showed potent COX-1 and COX-2 inhibiting activities in vitro with IC values ranging from 1.95 to 5.54 μmol·L and ranging from 1.01 to 2.27 μmol·L, respectively.
Subject(s)
Anti-Inflammatory Agents , Chemistry , Cyclooxygenase 1 , Chemistry , Cyclooxygenase 2 , Chemistry , Cyclooxygenase Inhibitors , Chemistry , Flavonoids , Chemistry , Molecular Structure , Myrtaceae , Chemistry , Plant Components, Aerial , Chemistry , Plant Extracts , ChemistryABSTRACT
In the present study, we carried out a phytochemical investigation of the ethanol extract of the aerial parts of Baeckea frutescens, which resulted in the isolation of two new flavonoid glycosides, myricetin 3-O-(5″-O-galloyl)-α-L-arabinofuranoside (1), 6-methylquercetin 7-O-β-D-glucopyranoside (2), one new methylchromone glycoside, 7-O-(4', 6'-digalloyl)-β-D-glucopyranosyl-5-hydroxy-2-methylchromone (3), together with three known compounds (4-6). The structures of these isolated compounds were established on the basis of 1D and 2D NMR techniques and chemical methods. The anti-inflammatory activities of the compounds 1-6 were evaluated for their inhibitory effects against cyclooxygenases-1 and -2 in vitro. Compounds 1-6 showed potent COX-1 and COX-2 inhibiting activities in vitro with IC values ranging from 1.95 to 5.54 μmol·L and ranging from 1.01 to 2.27 μmol·L, respectively.
Subject(s)
Anti-Inflammatory Agents , Chemistry , Cyclooxygenase 1 , Chemistry , Cyclooxygenase 2 , Chemistry , Cyclooxygenase Inhibitors , Chemistry , Flavonoids , Chemistry , Molecular Structure , Myrtaceae , Chemistry , Plant Components, Aerial , Chemistry , Plant Extracts , ChemistryABSTRACT
Objective To determinate the contents of α-pinene, β-pinene, eucalyptol and linalool in Baeckea frutescens by reference substances method and reference extract method respectively; To explore the feasibility of replacing single component reference by control extracts in assay. Methods The GC system consisted of a quartz column DB-5 (60 m×0.25 mm×0.25 μm); The temperature programming rose from 80 ℃ (15 min) to 90 ℃ by 1 ℃/min, lasting 2 min, then 10 ℃/min to 110 ℃, then 25 ℃/min to 240 ℃, lasting 8 min in the end; The temperature of the entrance of capillary vessel column was 250 ℃, and the temperature of the detector was 250 ℃. Results α-pinene, β-pinene, eucalyptol and linalool were in a good linear relationship within each concentration scope (r≥0.999). The average recovery rates were in the range of 96.5%–102.2%. The results of t-test demonstrated that there is no significant difference between the two methods. Conclusion The reference extract method can be used as a quality evaluation pattern for Baeckea frutescens.