| In vitro: |
| J Pharm Pharmacol. 2007 Jun;59(6):891-7. | | An extract of Apium graveolens var. dulce leaves: structure of the major constituent, apiin, and its anti-inflammatory properties.[Pubmed: 17637182] | Flavonoids, natural compounds widely distributed in the plant kingdom, are reported to affect the inflammatory process and to possess anti-inflammatory as well as immunomodulatory activity in-vitro and in-vivo.
METHODS AND RESULTS:
Since nitric oxide (NO) produced by inducible nitric oxide synthase (iNOS) is one of the inflammatory mediators, the effects of the ethanol/water (1:1) extract of the leaves of Apium graveolens var. dulce (celery) on iNOS expression and NO production in the J774.A1 macrophage cell line stimulated for 24 h with Escherichia coli lipopolysaccharide (LPS) were evaluated.
The extract of A. graveolens var. dulce contained Apiin as the major constituent (1.12%, w/w, of the extract). The extract and Apiin showed significant inhibitory activity on nitrite (NO) production in-vitro (IC50 0.073 and 0.08 mg mL(-1) for the extract and Apiin, respectively) and iNOS expression (IC50 0.095 and 0.049 mg mL(-1) for the extract and Apiin, respectively) in LPS-activated J774.A1 cells. The croton-oil ear test on mice showed that the extract exerted anti-inflammatory activity in-vivo (ID50 730 microg cm(-2)), with a potency seven-times lower than that of indometacin (ID50 93 microg cm(-2)), the non-steroidal anti-inflammatory drug used as reference.
CONCLUSIONS:
Our results clearly indicated the inhibitory activity of the extract and Apiin in-vitro on iNOS expression and nitrite production when added before LPS stimulation in the medium of J774.A1 cells. The anti-inflammatory properties of the extract demonstrated in-vivo might have been due to reduction of iNOS enzyme expression. | | Pharm Biol. 2016;54(1):174-9. | | Compounds from Sedum caeruleum with antioxidant, anticholinesterase, and antibacterial activities.[Pubmed: 25845643] | This is the first study on the phytochemistry, antioxidant, anticholinesterase, and antibacterial activities of Sedum caeruleum L. (Crassulaceae).
The objective of this study is to isolate the secondary metabolites and determine the antioxidant, anticholinesterase, and antibacterial activities of S. caeruleum.
METHODS AND RESULTS:
Six compounds (1-6) were isolated from the extracts of S. caeruleum and elucidated using UV, 1D-, 2D-NMR, and MS techniques. Antioxidant activity was investigated using DPPH(•), CUPRAC, and ferrous-ions chelating assays. Anticholinesterase activity was determined against acetylcholinesterase (AChE) and butyrylcholinesterase (BChE) enzymes using the Ellman method. Antibacterial activity was performed according to disc diffusion and minimum inhibitory concentration (MIC) methods.
Isolated compounds were elucidated as ursolic acid (1), daucosterol (2), β-sitosterol-3-O-β-D-galactopyranoside (3), apigenin (4), apigetrin (5), and Apiin (6). The butanol extract exhibited highest antioxidant activity in all tests (IC50 value: 28.35 ± 1.22 µg/mL in DPPH assay, IC50 value: 40.83 ± 2.24 µg/L in metal chelating activity, and IC50 value: 23.52 ± 0.44 µg/L in CUPRAC), and the highest BChE inhibitory activity (IC50 value: 36.89 ± 0.15 µg/L). Moreover, the chloroform extract mildly inhibited (MIC value: 80 µg/mL) the growth of all the tested bacterial strains.
CONCLUSIONS:
Ursolic acid (1), daucosterol (2), β-sitosterol-3-O-β-D-galactopyranoside (3), apigenin (4), apigetrin (5), and Apiin (6) were isolated from Sedum caeruleum for the first time. In addition, a correlation was observed between antioxidant and anticholinesterase activities of bioactive ingredients of this plant. |
|
| In vivo: |
| Ann Nutr Metab. 2006;50(3):167-72. | | Bioavailability of apigenin from apiin-rich parsley in humans.[Pubmed: 16407641] | Absorption and excretion of apigenin after the ingestion of Apiin-rich food, i.e. parsley, was tested.
METHODS AND RESULTS:
Eleven healthy subjects (5 women, 6 men) in the age range of 23-41 years and with an average body mass index of 23.9 +/- 4.1 kg/m2 took part in this study. After an apigenin- and luteolin-free diet, a single oral bolus of 2 g blanched parsley (corresponding to 65.8 +/- 15.5 micromol apigenin) per kilogram body weight was consumed. Blood samples were taken at 0, 4, 6, 7, 8, 9, 10, 11 and 28 h after parsley consumption and 24-hour urine samples were collected. Apigenin was analyzed in plasma, urine and red blood cells by means of HPLC-ECD.
On average, a maximum apigenin plasma concentration of 127 +/- 81 nmol/l was reached after 7.2 +/- 1.3 h with a high range of variation between subjects. For all participants, plasma apigenin concentration rose after bolus ingestion and fell within 28 h under the detection limit (2.3 nmol/l). The average apigenin content in 24-hour urine was 144 +/- 110 nmol/24 h corresponding to 0.22 +/- 0.16% of the ingested dose. The flavone could be detected in red blood cells without showing dose-response characteristics.
CONCLUSIONS:
A small portion of apigenin provided by food reaches the human circulation and, therefore, may reveal biological effects. |
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