AbstractIntroductionCecropia angustifolia Trécul. is a native Andean plant containing high levels of pentacyclic triterpenes (PTs), including several isobaric molecules that serve as chemical markers. Preclinical studies suggest that PTs positively modulate metabolic and vascular diseases. However, their low oral absorption reduces their bioactive effects.ObjectiveThe objective of this study was (1) to improve the absorption of PTs from C. angustifolia and (2) to establish a platform to produce biomass or botanical reference material using a strategy for their accumulation.MethodsMALDI‐TOF and UPLC‐MS were used to characterize and quantify PTs in different matrices. An in vitro platform for PT production was established. Chemical profiles of triterpenes were also evaluated from wild and in vitro herbal material using TLC coupled with mass spectrometry.ResultsTo overcome the low absorption of PTs, a premier raw material was used, which increased their bioavailability to 9.2%. Active ingredients in herbal material can vary, and there is an urgent need for standardized extracts using pharmacokinetics as an effective tool to reveal the dynamics of active ingredients in vivo. A temporary immersion system was produced as a promising platform with a total PT accumulation exceeding 50% of the content in the dry fraction, indicating it is a feasible mechanism to produce biomass or botanical reference material.ConclusionsPlant tissue culture is a promising eco‐friendly technology for phytochemical production and a modern strategy to protect biodiversity in natural assets. Alternative and modern, yet environmentally friendly production methods are needed to meet the large demand for herbal products.