Introduction
Search for active antidiabetic constituents
Suppressive effects of the methanol extract from the roots and stems of S. reticulata on postprandial blood glucose elevation in sugar-loaded rats
Unique thiosugar sulfonium sulfates, salacinol (1) and kotalanol (3), were isolated as the active principles by bioassay-guided separation using the maltase and sucrase inhibitory activities
A series of other thiosugar sulfonium constituents, neosalacinol (2), neokotalanol (4), and related isolates (5–8) from plans of the genus Salacia
Thiosugar sulfoniums (1–6) as a novel class of α-glucosidase inhibitors
IC50 (μM) [(μg/mL)] | |||||||
---|---|---|---|---|---|---|---|
Rata | Saccharomyces cerevisiaeb | Bacillus stearothermophilusc) | |||||
Maltase | Sucrase | Isomaltase | Maltase | Sucrase | Maltase | Sucrase | |
Salacinol (1) | 6.0 [2.0] | 1.3 [0.42] | 1.3 [0.44] | > 100 | > 100 | > 100 | > 100 |
Neosalacinol (2) | 22.2 [5.7] | 2.5 [0.65] | 0.68 [0.17] | > 100 | > 100 | ||
Kotalanol (3) | 2.0 [0.86] | 0.43 [0.18] | 1.8 [0.78] | > 100 | > 100 | ||
Neokotalanol (4) | 1.6 [0.54] | 1.5 [0.53] | 0.46 [0.16] | > 100 | > 100 | > 100 | > 100 |
Ponkoranol (5) | 5.6 [2.2] | 0.41 [0.16] | 4.6 [1.8] | > 100 | > 100 | ||
Neoponkoranol (6) | 5.1 [1.6] | 1.0 [0.32] | 1.4 [0.43] | > 100 | > 100 | ||
Salaprinol (7) | > 329 [> 100] | > 329 [> 100] | 14 [4.4] | ||||
Neosalaprinol (8) | > 444 [> 100] | 90 [20] | 6.5 [1.5] | ||||
1a | [> 400] | [> 400] | |||||
Acarbose | 1.7 [1.1] | 1.5 [1.0] | 645 [417] | > 100 | > 100 | 0.20 [0.13] | 0.021 [0.014] |
Voglibose | 1.3 [0.34] | 0.22 [0.060] | 2.2 [0.58] | > 100 | > 100 | > 100 | > 100 |
Miglitol | 8.2 [1.7] | 0.43 [0.090] | 4.6 [0.96] | > 100 | > 100 | > 100 | > 100 |
1-Deoxynojirimycin | 0.67 [0.11] | 0.12 [0.020] | 0.26 [0.042] | > 100 | > 100 | 84.3 [13.8] | 2.4 [0.39] |
IC50 (μM) | Ki (μM) | |
---|---|---|
Salacinol (1) | 4.9 | 0.44 |
Neosalacinol (2) | 9.0 | 1.2 |
Kotalanol (3) | 3.9 | 0.32 |
Neokotalanol (4) | 3.9 | 0.33 |
Ponkoranol (5) | 5.0 | 0.32 |
Neoponkoranol (6) | 4.0 | 0.70 |
Acarbose | 15.2 | 2.6 |
Voglibose | 1.3 | 0.17 |
Miglitol | 3.7 | 0.57 |
1-Deoxynojirimycin | 0.96 | 0.071 |
Terpenoid and polyphenol constituents with aldose reductase inhibitory activity
IC50 (μM) | |
---|---|
Friedelan-3-one-29-ol (17) | 98 |
Maytenfolic acid (23) | 72 |
3β,22 β-Dihydroxyolean-12-en-29-oic acid (24) | 26 |
Tingenine B (32) | 7.0 |
Tingenone (33) | 13 |
Regeol A (34) | 30 |
Triptocalline A (35) | 14 |
Celahin C (38) | 95 |
Mangiferin (41) | 3.2 |
Epalrestat | 0.0072 |
Quantitative evaluation of principal sulfonium constituents as characteristic marker molecules
Evaluation of hot water extract from the stems of S. chinensis (SCE) as a functional food material for improving the effects on blood glucose and HbA1c levels in animal models
Dose | Food intake | Water intake | Body weight (g) | ||||||||
---|---|---|---|---|---|---|---|---|---|---|---|
(%) | (g/day, average) | Day 0 | Day 3 | Day 6 | Day 9 | Day 12 | Day 15 | Day 18 | Day 20 | ||
Control | – | 3.5 ± 0.1 | 4.0 ± 0.7 | 32.9 ± 0.6 | 35.6 ± 0.7 | 36.4 ± 0.4 | 36.9 ± 0.5 | 38.1 ± 0.4 | 39.2 ± 0.5 | 40.3 ± 0.4 | 41.0 ± 0.4 |
SCE | 0.05 | 3.6 ± 0.1 | 2.5 ± 0.1** | 33.4 ± 0.5 | 36.1 ± 0.3 | 36.8 ± 0.2 | 37.4 ± 0.2 | 38.6 ± 0.3 | 39.3 ± 0.2 | 40.8 ± 0.3 | 41.3 ± 0.3 |
Neokotalanol (4) | 0.0003 | 3.5 ± 0.2 | 2.5 ± 0.2** | 32.2 ± 0.5 | 35.1 ± 0.4 | 35.8 ± 0.4 | 36.0 ± 0.4 | 37.2 ± 0.4 | 37.8 ± 0.4 | 39.4 ± 0.4 | 40.1 ± 0.4 |
Voglibose | 0.0001 | 4.5 ± 0.2 | 3.3 ± 0.2 | 33.0 ± 0.5 | 36.2 ± 0.4 | 36.3 ± 0.5 | 37.1 ± 0.3 | 38.0 ± 0.4 | 39.0 ± 0.2 | 40.2 ± 0.3 | 40.8 ± 0.4 |
Dose | HbA1c (%) | ||
---|---|---|---|
(%) | Day 0 | Day 20 | |
Control | – | 6.1 ± 0.0 | 6.5 ± 0.2 |
SCE | 0.05 | 6.1 ± 0.1 | 6.0 ± 0.1* |
Neokotalanol (4) | 0.0003 | 5.9 ± 0.1 | 5.9 ± 0.1** |
Voglibose | 0.0001 | 5.9 ± 0.1 | 6.0 ± 0.1* |