Table 1.
Molecules that inhibit glycosyltransferase activity
| Category | Source of natural product | Representative substances | Inhibited Gtfs reported | Evidence of cariostatic efficacy in vivo | Reference |
|---|---|---|---|---|---|
| Inhibitors derived from natural products | |||||
| Catechin-based polyphenols | Camellia sinensis (black, green and oolong tea) | Theaflavin (-)-Epigallocatechin gallate (-)-Epicatechin gallate |
GtfB (solution) GtfB (solution) GtfB (solution) |
Yes (as crude tea extract) Yes (as crude tea extract) Yes (as crude tea extract) | (26–31) |
| Flavonoids | Apis mellifera propolis (bee hive) | Apigenin | GtfB, GtfC, and GtfD (solution/surface) | Yes | (36, 37) |
| Kaempferol | GtfB, GtfC, and GtfD (solution/surface) | No | (36) | ||
| Vaccinium macrocarpon (cranberry) | Myricetin | GtfB (surface) | No | (42) | |
| Proanthocyanidin oligomers | Cranberry | A-type proanthocyanidin oligomers | GtfB (surface) | Yes | (42, 43) |
| Apple | Condensed tannins | Crude Gtfs (solution) | No | (44) | |
| Polymeric polyphenols | Oolong tea | OTF6 | GtfB and GtfD (solution) | Yes (as crude tea extract) | (26, 48) |
| Cocoa bean hust | Polymeric epicatechins | GtfB, GtfC, and GtfD (solution) | No | (49, 50) | |
| Others | Rheedia gardneriana | 7-Epiclusianone | GtfB and GtfC (solution) | No | (51) |
|
Azadirachta indica (Neem) Melaphis chinensis (Chinese Nutgall) |
Gallotannin Gallotannin |
Crude Gtfs (solution) Crude Gtfs (solution) |
No No |
(52) (53) |
|
| Synthesized inhibitors | |||||
| Quaternary ammonium | Crude Gtfs (solution) | No | (54) | ||
| Aliphatic amines | Crude Gtfs (solution) | No | (54) | ||
| 1-Deoxynojirimycin | GtfB, GtfC, and GtfD (solution/surface) | No | (24, 57) | ||
| Tris(hydroxymethyl) aminomethane | Crude Gtfs (solution/surface) | No | (56) | ||
| Trichloro-galactosucrose | GtfB, GtfC, and GtfD (solution/surface) | No | (24) | ||
| Acarbose | GtfB, GtfD (solution) | No | (57) | ||
| Maltose | GtfB (solution) | No | (57) | ||
| Nojirimycin | GtfB (solution) | No | (57) | ||
| Quinoxaline derivative | GtfC and GtfD (solution) | Yes | (58) | ||
| Metal ions and oxidizing agents | Zn2+ | GtfB, GtfC, and GtfD (solution) | No | (24) | |
| Cu2+ | GtfB, GtfC, and GtfD (solution/surface) | No | (24) | ||
| Fe2+ | GtfB, GtfC, and GtfD (solution/surface) | No | (24) | ||
| Fe3+ | GtfB, GtfC, and GtfD (solution/surface) | No | (24) | ||
| Rose bengal | GtfB, GtfC, and GtfD (solution/surface) | No | (24) | ||
| Hypochlorite | GtfB, GtfC, and GtfD (solution/surface) | No | (24) | ||
| Antibodies | Antibody to GtfB | GtfB and GtfC (solution/surface) | Yes | (66, 68, 69) | |
| Antibody to GtfC | GtfB and GtfC (solution/surface) | No | (66) | ||
| Antibody to GtfD | GtfD (solution), GtfC (surface) | No | (66) |