Trilobatin, a natural product isolated and purified from the herbs of Lithocarpus pachyphyllus with anti-oxidant effect, potentially inhibits the LPS-induced inflammatory response by suppressing the NF-κB signaling pathway and is a potential effective α-glucosidase inhibitor for management of postprandial hyperglycemia with less side effect.
Trilobatin/三叶甙 细胞实验
Cell Line
Concentration
Treated Time
Description
References
Primary cortical neurons
12.5, 25, 50 µM
24 hours
To evaluate the protective effect of Trilobatin on corticosterone-induced neuronal injury. Results showed that Trilobatin concentration-dependently inhibited corticosterone-induced cytotoxicity, restored cell viability, and reduced LDH release.
J Agric Food Chem. 2025 Mar 5;73(9):5163-5179
C2C12 myotubes
0.1, 1.0, 10 µM
24 hours
Trilobatin prevented palmitate-induced insulin resistance by enhancing glucose uptake and the phosphorylation of IRS1 and AKT, and recovered the translocation of GLUT4 from cytoplasm to membrane.
Chin Med. 2020 Oct 12;15:110
Huh 7 cells
0.1, 1.0, 10, 50, 100 µM
24 hours
High concentrations of Trilobatin significantly induced the proliferation of Huh 7 cells.
Molecules. 2019 Sep 18;24(18):3390
HepG2 cells
50 µM or 100 µM
24 hours
High concentrations of Trilobatin significantly induced the proliferation of HepG2 cells. Compared to the control, incubation with 50 or 100 μM trilobatin for 24 h increased the number of viable HepG2 cells by 35% and 50% respectively.
Molecules. 2019 Sep 18;24(18):3390
BV2 cells
12.5-50 µM
48 hours
TLB concentration-dependently increased cell viability by inhibiting the HMGB1/TLR4/NF-κB signaling pathway
TLB significantly attenuated Aβ25–35-induced HT22 cell death, as evidenced by MTT assay and LDH release. TLB dramatically mitigated cell death after Aβ25–35 insult via decreasing the intracellular and mitochondrial ROS overproduction and restoring antioxidant enzyme activities, as well as suppressing apoptosis.
Front Pharmacol. 2020 May 19;11:584
Trilobatin/三叶甙 动物实验
Species
Animal Model
Administration
Dosage
Frequency
Description
References
KK-Ay mice
Type 2 diabetes model
Intragastric administration
10 and 20 mg/kg
Twice a day for 28 weeks
TLB significantly reduced the high fasting blood glucose level and insulin resistance and promoted the tolerances to exogenous glucose and insulin in KK-Ay mice. Moreover, TLB reduced the content of reactive oxygen species; enhanced antioxidant enzymes activities, including serum catalase, glutathione peroxidase, and superoxide dismutase; and regulated the abnormal parameters of lipid metabolism, including triglyceride, high-density lipoprotein-cholesterol, low-density lipoprotein-cholesterol, and free fatty acid.
Trilobatin significantly improved insulin resistance by decreasing fasting blood glucose and insulin in serum, enhancing the phosphorylation of IRS1 and AKT, and recovering the expression and translocation of GLUT4 in ob/ob mice.
Chin Med. 2020 Oct 12;15:110
C57BL/6 mice
Diabetic model
Intragastric administration
10 mg/kg
Single dose, blood glucose measured at 0, 15, 30, 60 and 120 minutes
Trilobatin significantly attenuated the intake of glucose in C57BL/6 mice, indicating its activity as an SGLT1/2 inhibitor.
Molecules. 2019 Sep 18;24(18):3390
C57BL/6J mice
DSS-induced ulcerative colitis model
Oral gavage
10, 20, 40 mg/kg
Once daily for 5 consecutive days
TLB significantly alleviated DSS-induced UC symptoms, including weight loss, colon length shortening, and improvement in histopathological lesions. TLB also reduced proinflammatory cytokines (IL-1β, IL-6, TNF-α) and increased anti-inflammatory cytokines (IL-4, IL-10, IL-22).
Adv Sci (Weinh). 2025 Mar;12(10):e2412234
Mice
Exhaustive exercise-induced fatigue model
Gavage
2.5, 5, 10 mg/kg
Twice a day for 28 days
TLB alleviates exhaustive exercise-induced fatigue and oxidative stress by mediating the Nrf2/ARE/ferroptosis signaling pathway
Front Pharmacol. 2022 Jun 24;13:913367
Sprague-Dawley rats
High-fat diet-induced obese rat model
Intragastric gavage
30 mg/kg, 60 mg/kg, 120 mg/kg
Once daily for four weeks
Trilobatin significantly reduced body and liver weight gain induced by a high-fat diet, and the accumulation of perirenal fat, epididymal fat, and brown fat in SD obese rats. Additionally, Trilobatin increased the concentrations of short-chain fatty acids (SCFAs), especially butyrate, and significantly altered the composition of gut microbiota.
Nutrients. 2021 Mar 10;13(3):891
Rice
Purple rice
Foliar spray
30 mg/L
Once
Exogenous application of Trilobatin significantly increased the total flavonoid content and total antioxidant capacity of purple rice grains
Plants (Basel). 2024 Dec 3;13(23):3389
APP/PS1 transgenic mice
Alzheimer's disease model
Intragastrically
4, 8 mg/kg/day
Twice a day for 3 months
TLB significantly and dose-dependently ameliorated the cognitive deficits in the two AD animal models
Acta Pharmacol Sin. 2022 Oct;43(10):2482-2494
C57BL/6J wild-type mice
Chronic unpredictable mild stress (CUMS)-induced depressive-like behavior model
Gavage
5, 10, 20 mg/kg
Twice daily for 4 weeks
To evaluate the alleviative effect of Trilobatin on CUMS-induced depressive-like behavior. Results showed that Trilobatin dose-dependently increased body weight, improved sucrose preference, reduced immobility time, and restored mitochondrial dynamic balance and antioxidant enzyme activities.
J Agric Food Chem. 2025 Mar 5;73(9):5163-5179
ICR mice
Cisplatin-induced acute kidney injury model
Intragastric administration
50 and 100 mg/kg
10 consecutive days
TLB significantly reversed the inhibition of CRE, BUN, and MDA levels compared with the cisplatin group and significantly alleviated cisplatin-induced renal pathological changes. TLB alleviated cisplatin-induced nephrotoxicity by regulating the AKT/MAPK signaling pathway and apoptosis.
ACS Omega. 2022 Oct 13;7(42):37401-37409
Caenorhabditis elegans
Wild-type N2 and various mutant strains
Administration via NGM medium
62.5, 125, 250 μM
Continuous administration until the end of the experiment
TLB significantly extended lifespan, enhanced antioxidant capacity, and acted through the SKN1/SIRT3/DAF16 signaling pathway
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