Metabolic & Cardiometabolic

oleanolic acid activates TGR5

Leans support(Animal or laboratory evidence) Metabolic & Cardiometabolic 🐭 Non-human evidence

RefutedContestedStrong support

consensus score 1.00

⚖️ Thin evidence — read the needle loosely. The score shows which way the studies lean, but there are too few independent, high-quality ones to place it firmly. Expect this to move as better evidence arrives.

Why the rating is limited: animal or laboratory evidence.

The studies that point for or against this claim are all animal or laboratory studies. They do not establish the claimed effect in people.

Before this limit: strong support. Final rating: leans support.

📅 Last reviewed: 2026-08-11 ⓘ

Evidence ladder

How far up the ladder this claim has climbed. A high consensus on a low rung means "consistent so far," not "proven in people."

Top evidence so far: Animal studies (Animal)

MechanismIn-vitroAnimalObservationalRCTMeta-analysis

How the studies fall

2 support 0 contradict 0 tested null 0 mixed · 2 sources, 2 independent groups

What the evidence shows

H3's first arm. Oleanolic acid is a genuine TGR5 agonist and the receptor is the right one — TGR5 activation stimulates GLP-1, unlike FXR which suppresses it (claim-intestinal-fxr-activation-suppresses-glp1).

The evidence (3)

Source	Grade	Stance	Quality	Finding
Liu S, Chen X, Chen D, Yu B, Zheng P, Luo Y, He J, Huang Z 2025 · The Journal of nutritional biochemistry	animal	supports	moderate	Oleanolic acid inhibited appetite through the TGR5/cAMP signalling pathway, tying the triterpenoid directly to TGR5 activation in vivo.
Moon DO 2025 · Biomedicines	mechanism	supports	low	Review with original docking on cryo-EM TGR5 (PDB 7BW0, CB-Dock2): 'OA and curcumin both exhibited binding scores of −8.8 kcal/mol and occupied the canonical orthosteric pocket defined by residues in TM3 and TM6.' In-silico binding pose only, no activation assay; author: 'docking results are hypothesis-generating rather than definitive evidence.'
Zhai Z, Zeng W, Niu KM, Wang R, Sheng P, Hu L, Guo X, Liu J, Cai L 2025 · Journal of Agricultural and Food Chemistry	in-vitro	supports	moderate	Piglets fed 50 mg/kg oleanolic acid for 20 days: OA 'significantly reduces serum and intestinal total bile acid concentrations, suppresses TGR5 expression' and promotes intestinal cell proliferation. In TGR5/pCREB-Luc cells it was hyocholic acid (HCA), not OA, that 'activates the TGR5/AMPK pathway'. The paper's model is that OA lowers the bile-acid ligand pool and so dampens TGR5 signalling; it does not show OA activating TGR5. Abstract only.

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Educational only, not medical advice. Grades and scores reflect published evidence weighted by study design and quality; see the methodology.