| In vitro: |
| Bioorg Med Chem. 2017 Jul 15;25(14):3706-3713. | | Screening for bioactive natural products from a 67-compound library of Glycyrrhiza inflata.[Pubmed: 28522265] | Licorice shows a variety of pharmacological activities. This work aims to discover bioactive natural products from one botanical source of licorice, Glycyrrhiza inflata. A total of 67 free phenolics were isolated to form a compound library.
METHODS AND RESULTS:
Based on the bioactivities of licorice, these compounds were screened using cell- or enzyme-based bioassay methods. A total of 11 compounds exhibited potent cytotoxic activities against three human cancer cell lines (HepG2, SW480 and MCF7), while showed little toxicity on human normal cell lines LO2 and HEK293T.
CONCLUSIONS:
A number of chalcones showed remarkable anti-inflammatory activities. Among them, 2 (licochalcone B, IC50 8.78μM), 10 (licoagrochalcone C, IC50 9.35μM) and 13 (licochalcone E, IC50 9.09μM) exhibited the most potent inhibitory activities on LPS-induced NO production, whereas 1, 8, 10, 12 and 13 (IC50 13.9, 7.27, 2.44, 6.67 and 3.83μM) showed potent inhibitory activities on NF-κB transcription. Nine prenylated phenolics were found to be PTP1B inhibitors. Particularly, licoagrochalcone A (4), kanzonol C (7), 2'-hydroxyisolupalbigenin (35), gancaonin Q (45), glisoflavanone (50) and Glabrol (53) showed IC50 values of 0.31-0.97μM. Compounds 24 (semilicoisoflavone B, IC50 0.25μM), 26 (allolicoisoflavone B, IC50 0.80μM) and 64 (glabridin, IC50 0.10μM) showed noticeable tyrosinase inhibitory activities.
Most of the above bioactive compounds were reported for the first time. | | Arch Pharm Res. 2010 Feb;33(2):237-42. | | Inhibitory activity of diacylglycerol acyltransferase by glabrol isolated from the roots of licorice.[Pubmed: 20195824 ] | Acyl-coenzyme A: diacylglycerol acyltransferase (DGAT, EC 2.3.1.20) catalyzes triglyceride synthesis in the glycerol phosphate pathway. It has relations with the excess supply and accumulation of triglycerides. Therefore, DGAT inhibitors may act as a potential therapy for obesity and type 2 diabetes.
METHODS AND RESULTS:
Five flavonoids were isolated from the ethanol extracts of licorice roots, using an in vitro DGAT inhibitory assay. One isoprenyl flavonoid showed most potential inhibition of DGAT on five flavonoids (1-5). On the basis of spectral evidences, the compound was identified as Glabrol (5). Compound 5 inhibited rat liver microsomal DGAT activity with an IC50 value of 8.0 microM, but the IC50 value for four flavonoids (1-4) was more than 100 microM. In addition, Glabrol showed a noncompetitive type of inhibition against DGAT.
CONCLUSIONS:
These data suggest that potential therapy for the treatment in obesity and type 2 diabetes patients by licorice roots might be related with its DGAT inhibitory effect. | | J Nat Prod. 1980 Mar-Apr;43(2):259-69. | | Antimicrobial agents from higher plants. Antimicrobial isoflavanoids and related substances from Glycyrrhiza glabra L. var. typica.[Pubmed: 7381508] |
METHODS AND RESULTS:
Bioassay-directed fractionation of Glycyrrhiza glabra L. var. typica resulted in the isolation and characterization of glabridin (I), Glabrol (2), glabrene (3), 3-hydroxyGlabrol (4), 4'-O-methylglabridin (5), 3'-methoxyglabridin (6), formononetin (7), phaseollinisoflavan (8), hispaglabridin A (9), hispaglabridin B (13), salicylic acid and O-acetyl salicylic acid. Of these, hispaglabridin A, hispaglabridin B, 4'-O-methylglabridin, glabridin, Glabrol and 3-hydroxyGlabrol possess significant antimicrobial activity in vitro; hispaglabridin A, hispaglabridin B, 3'-methoxyglabridin, 4'-O-methylglabridin 3-hydroxyGlabrol, phaseollinisoflavan, salicylic acid, and O, acetyl salicylic acid are newly found in Glycyrrhiza sp.; and hispaglabridin A, hispaglabridin B, 3'-methoxyglabridin, 4'-O-methylglabridin, and 3-hydroxyGlabrol are new to the literature and their structures are proposed herein. |
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