Drug intelligence / Profile preview

13-methylberberine

Development stage
Preclinical
Modality
Small Molecules
Administration
Oral
01

Overview

**13-methylberberine** is a semisynthetic derivative of the plant alkaloid berberine, structurally distinguished by a methyl group at the 13-position. It exhibits enhanced **anti-adipogenic and antitumor activities** compared to berberine, attributed to its effects on adipocyte differentiation and lipid metabolism. The compound **inhibits key adipogenic transcription factors** such as peroxisome proliferator-activated receptor gamma (PPARγ) and CCAAT enhancer binding protein alpha (C/EBPα), reduces expression of sterol regulatory element-binding protein 1 (SREBP-1), and activates the AMP-activated protein kinase (AMPK) signaling pathway. These actions contribute to reduced lipid accumulation and adipogenesis, with the anti-adipogenic effect requiring **AMPK activation**. In addition, 13-methylberberine has shown improved cell uptake and retention over berberine, suggesting superior pharmacokinetics for use as an anti-obesity and metabolic syndrome agent. It also demonstrates antibacterial and antitumor effects, making it of research interest in obesity, cancer, and metabolic disease models[1][3][6].

Other names
13-MB13-methylberberinium chloride13-methylberberine chloride5,6-dihydro-9,10-dimethoxy-13-methyl-benzo[g]-1,3-benzodioxolo[5,6-a]quinolizinium5,6-dihydro-2,3-(methylenedioxy)-9,10-dimethoxy-13-methyldibenzo[a,g]quinoliziniumBenzo[g]-1,3-benzodioxolo[5,6-a]quinolizinium, 5,6-dihydro-9,10-dimethoxy-13-methyl-16,17-dimethoxy-21-methyl-5,7-dioxa-13-azoniapentacyclo(11.8.0.02,10.04,8.015,20)henicosa-1(13),2,4(8),9,14,16,18,20-octaeneDTXSID40191981DTXSID-40191981DTXSID 401919819,10-Dimethoxy-13-methyl-5,6-dihydrobenzo[g]-1,3-benzodioxolo[5,6-a]quinolizinium
02

Targets

AMPK (Adenosine monophosphate–activated protein kinase)PRKCI (Protein kinase C iota)AKT (RAC-alpha serine/threonine-protein kinase)CEBPA (C/EBPα)SREBP-1 / SREBF1 (SREBP-1)PPARG (Peroxisome proliferator-activated receptor gamma)

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