Trigonelline (chloride)

Trigonelline is an alkaloid that has been found in L. japonicus and an active metabolite of niacin that has diverse biological activities.^1,2,3,4 It increases levels of the brown fat marker proteins PRDM16, PGC-1α, and UCP1 in 3T3-L1 adipocytes when used at a concentration of 75 µM.¹ Trigonelline inhibits degranulation of, and decreases the production of IL-6 and TNF-α in, activated primary mouse bone marrow mast cells (BMMCs).² In vivo, trigonelline (200 mg/kg) reduces serum IgE levels, pulmonary immune cell infiltration, and mucus secretion in a mouse model of ovalbumin-induced allergic asthma. It reduces serum levels of IL-1β, IL-6, IL-18, and malondialdehyde (MDA) and renal cell apoptosis, as well as increases protein levels of peroxisome proliferator-activated receptor γ (PPARγ) in a rat model of high-fat diet- and streptozotocin-induced type 2 diabetic nephropathy when administered at a dose of 40 mg/kg.³ Trigonelline (50 mg/kg) reduces hepatic de novo lipogenesis, induces hepatic autophagy, and prevents weight gain, insulin resistance, and hepatic steatosis in a mouse model of high-cholesterol and high-fat diet-induced non-alcoholic fatty liver disease (NAFLD).⁴

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1. Choi, M., Mukherjee, S., and Yun, J.W. Trigonelline induces browning in 3T3-L1 white adipocytes. Phytother Res. 35(2), 1113-1124 (2021).

2. Zhang, W., Zhang, Y., Chen, S., et al. Trigonelline, an alkaloid from Leonurus japonicus Houtt., suppresses mast cell activation and OVA-induced allergic asthma. Front. Pharmacol. 12, 687970 (2021).

3. Li, Y., Li, Q., Wang, C., et al. Trigonelline reduced diabetic nephropathy and insulin resistance in type 2 diabetic rats through peroxisome proliferator-activated receptor-γ. Exp. Ther. Med. 18(2), 1331-1337 (2019).

4. Sharma, L., Lone, N.A., Knott, R.M., et al. Trigonelline prevents high cholesterol and high fat diet induced hepatic lipid accumulation and lipo-toxicity in C57BL/6J mice, via restoration of hepatic autophagy. Food Chem. Toxicol. 121, 283-296 (2018).