Objective: To investigate therapeutic mechanism in Jasminum amplexicaule (Oleaceae) and verify its main active component as quality control markers Methods: Established mouse models of diarrhea, intestinal angina, and inflammation were firstly used to select herb fractions with optimum efficacy, followed by an in vitro experiment to determine key targets associated with effects of J. amplexicaule extract. The selected fractions were isolated and purified, its components were identified, and the obtained compounds were verified for their effects on NF-kappa B and iNOS. Finally, effective compounds were administered to rats, their plasma pharmacokinetic parameters were calculated, and quality markers (QMs) reflecting therapeutic activities of J. amplexicaule were confirmed. Results: Trichloromethane and ethyl acetate fractions had significant anti-diarrheal, anti-inflammatory, and analgesic effects. The trichloromethane fraction also reduced BDNF, p38 MAPK, p-p38 MAPK, NF-kappa B p65, and p-NF-kappa B p65 levels in the ileum in a rhubarb-induced diarrhea mouse model. Additionally, it inhibited LPS-induced NF-kappa B transcription and nitric oxide (NO) production in RAW264.7 macrophages, which suppressed iNOS expression. Therefore, the trichloromethane fraction was further investigated. QMs candidate selection identified 17 compounds, and results of in-vitro therapeutic validation indicated that methyl caffeate and isochlorogenic acid B had the strongest anti-diarrheal, anti-inflammatory, and analgesic activities. After being validated by a UHPLC-MS-MS method, concentrations of these target compounds were accurately determined in the rat plasma and pharmacokinetic parameters were calculated. C-max, t(max), and t(1/2) were respectively 575.35 ng/mL (2.963 nmol/mL), 0.5 h, and 0.45 h for methyl caffeate and 262.03 ng/mL (0.5034nmol/mL), 0.25 h, and 2.03 h for isochlorogenic acid B. Because these candidate compounds exhibited favorable pharmacokinetics, they were considered as QMs of J. amplexicaule. Conclusions: The present study accurately and effectively identified QMs of J. amp lexicaule that act as indicators of efficacy and quality. (C) 2019 Tianjin Press of Chinese Herbal Medicines. Published by Elsevier B.V. All rights reserved.