Biodistribution of andrographolide to assess the interior‐exterior relationship between the lung and intestine using microPET

Abstract

Background One classic traditional Chinese medicine theory is that the “lung and intestine are exterior‐interiorly related”; however, this has not been confirmed experimentally. The aim of this study was to provide a biological basis for the theory by measuring the tissue distribution of andrographolide. Methods Acute pneumonia was induced in a mouse model by repeated stimulation with lipopolysaccharide. The distribution of andrographolide in mice was observed by positron emission tomography (PET) imaging with [ 18 F]‐labeled andrographolide, and changes in the in vivo distribution before and after modeling were compared. Subsequently, the consistency of pathological changes in lung and intestine was confirmed by observation of pathological sections. Finally, the results were verified by cytokine detection. Results The value of organ uptake, pathological changes and inflammatory factor expression of the lung and intestine were consistent. The concentration of andrographolide in the lung and intestine increased significantly, and was confirmed by pathology and enzyme‐linked immunosorbent assays (ELISA). Conclusions Micro‐positron emission tomography (microPET) can be used to visually observe the distribution of medicinal ingredients in vivo, and [ 18 F]‐andrographolide can be used as a tool to assess the interior‐exterior relationship between the lung and intestine.

Andrographolide: A review of its pharmacology, pharmacokinetics, toxicity and clinical trials and pharmaceutical researches

“…In terms of distribution, this natural ingredient in mice was surveyed through positron emission tomography (PET) imaging with [18F]‐labeled andrographolide, the researcher found that the concentration of andrographolide in lung and intestine increased significantly, which the result was corroborated by pathology and enzyme‐linked immunosorbent assays (ELISA) (Zhang & Cui, 2020). As a carrier protein of numerous agents, human serum albumin (HSA) is proved to be contributive for drug transport.…”

Chromatogram profile of andrographolide-glucuronate and andrographolide glycine in rabbit feces extract

“…Moreover, a recent study reported that [11]. F-andrographolide was also distributed in all organs with a majority accumulation in the liver of acute pneumonia Kunming mice [7]. Andrographolide could alter and/or enhance the bioavailability of other drugs when given simultaneously.…”

“…In fact, carrying out a pharmacokinetic study is not as easy as expected, due to various metabolic processes and enzymatic hydrolysis that are encountered by the bioactive compound of the extracts in the body. Andrographolide, a major diterpenoid compound of Andrographis paniculata, has been extensively explored for its pharmacology activities and pharmacokinetics [4][5][6][7][8][9][10]. Oral administration of a non-steroid anti-inflammatory drug together with andrographolide in rabbits has improved the ADME of this diterpenoid compound [4].…”