Lianweng Granules Alleviate Intestinal Barrier Damage via the IL-6/STAT3/PI3K/AKT Signaling Pathway with Dampness-Heat Syndrome Diarrhea.
Jianyu LvYuchen FuYu GaChao HanYimeng FanYuanyuan WeiSijia HaoZhihui HaoPublished in: Antioxidants (Basel, Switzerland) (2024)
Dampness-heat syndrome diarrhea (DHSD) is a common clinical disease with a high prevalence but still has no satisfactory therapeutic medicine, so the search for a safe and effective drug candidate is ongoing. This study aims to explore the efficacy and mechanisms of Lianweng granules (LWG) in the treatment of DHSD and to identify the blood transport components of LWG. We assessed the efficacy of LWG in DHSD by various in vivo metrics such as body weight, disease activity index (DAI), histopathologic examination, intestinal barrier function, levels of inflammatory, apoptotic biomarkers, and oxidative stress. We identified the blood components of LWG using ultra-high performance liquid chromatography-mass spectrometry/mass spectrometry (UHPLC-MS/MS), and the resolved key components were used to explore the relevant targets. We next predicted the potential mechanisms of LWG in treating DHSD using network pharmacology and molecular docking based on the relevant targets. Finally, the mechanisms were validated in vivo using RT-qPCR, Western blotting, ELISA, and immunofluorescence and evaluated in vitro using Cell Counting Kit-8 (CCK-8), small interfering RNA, cellular enthusiasm transfer assay (CETSA), and drug affinity response target stability (DARTS). Ninety-one pharmacodynamic components of LWG enter the bloodstream and exert possible therapeutic effects. In vivo, LWG treatment improved body weight, reduced colonic injury and DAI scores, lowered inflammation, oxidative stress, and apoptosis markers, and partially restored intestinal barrier function in DHSD mice. Guided by network pharmacology and molecular docking, it is suggested that LWG may exert therapeutic effects by inhibiting IL-6/STAT3/PI3K/AKT signaling. LWG significantly decreased the expression of IL-6, p-STAT3, p-PI3K, p-AKT, and other proteins. These findings were supported by in vitro experiments, where CETSA, DARTS, and siRNA evidenced LWG's targeting of STAT3. LWG targeted STAT3 to inhibit inflammation, oxidative stress, and apoptosis in the colon, thereby restoring the intestinal barrier function to some extent and exerting a therapeutic effect on DHSD.
Keyphrases
- oxidative stress
- pi k akt
- signaling pathway
- molecular docking
- cell proliferation
- body weight
- cell cycle arrest
- mass spectrometry
- ms ms
- induced apoptosis
- disease activity
- diabetic rats
- ultra high performance liquid chromatography
- tandem mass spectrometry
- dna damage
- ischemia reperfusion injury
- liquid chromatography
- molecular dynamics simulations
- epithelial mesenchymal transition
- cell death
- systemic lupus erythematosus
- rheumatoid arthritis
- cancer therapy
- high performance liquid chromatography
- simultaneous determination
- poor prognosis
- case report
- single cell
- south africa
- irritable bowel syndrome
- heat shock
- juvenile idiopathic arthritis
- replacement therapy
- risk factors
- endoplasmic reticulum stress
- rheumatoid arthritis patients
- type diabetes
- drug induced
- cell therapy
- long non coding rna
- high throughput
- hyaluronic acid
- ulcerative colitis
- skeletal muscle
- escherichia coli
- clostridium difficile
- drug delivery