UPLC-Q-TOF-MS based investigation into the bioactive compounds and molecular mechanisms of Lamiophlomis Herba against hepatic fibrosis

Jingzi Chen; Jiaming Ge; Weisan Chen; Ying Zhao; Tianbao Song; Kun Fu; Xiankuan Li; Yanchao Zheng

doi:10.1016/j.phymed.2023.155085

UPLC-Q-TOF-MS based investigation into the bioactive compounds and molecular mechanisms of Lamiophlomis Herba against hepatic fibrosis

Phytomedicine. 2023 Dec:121:155085. doi: 10.1016/j.phymed.2023.155085. Epub 2023 Sep 16.

Authors

Jingzi Chen¹, Jiaming Ge², Weisan Chen², Ying Zhao², Tianbao Song², Kun Fu³, Xiankuan Li⁴, Yanchao Zheng⁵

Affiliations

¹ Chinese Medicine Rehabilitation Department, Tianjin Nankai Hospital, Tianjin, 300100, China.
² School of Chinese Materia Medical, Tianjin University of Traditional Chinese Medicine, Tianjin, 301617, China; Tianjin Key Laboratory of Therapeutic Substance of Traditional Chinese Medicine, Tianjin 301617, China.
³ Second Teaching Hospital of Tianjin University of Traditional Chinese Medicine, Tianjin, 300120, China.
⁴ School of Chinese Materia Medical, Tianjin University of Traditional Chinese Medicine, Tianjin, 301617, China; Tianjin Key Laboratory of Therapeutic Substance of Traditional Chinese Medicine, Tianjin 301617, China. Electronic address: lixiankuan@tjutcm.edu.cn.
⁵ School of Chinese Materia Medical, Tianjin University of Traditional Chinese Medicine, Tianjin, 301617, China; Tianjin Key Laboratory of Therapeutic Substance of Traditional Chinese Medicine, Tianjin 301617, China. Electronic address: zhengyanchao@tjutcm.edu.cn.

PMID: 37757709
DOI: 10.1016/j.phymed.2023.155085

Abstract

Background: Lamiophlomis Herba (LH) is a valuable traditional medicinal plant found on the Qinghai-Tibetan Plateau that promotes blood circulation, removes blood stasis, and has antibacterial and anti-inflammatory properties. The main components of LH are iridoid glycosides, phenethyl alcohol glycosides, flavonoids, and polysaccharides.

Purpose: To investigate the mechanism of the anti-liver fibrosis effects of LH and screen for its bioactive compounds.

Study design: Screening LH marker components and validating the LH anti-liver fibrosis mechanism.

Methods: The active ingredients of LH were identified using UPLC-Q-TOF-MS, and HotMap combined with principal components analysis (PCA) was used to screen for marker components. Network pharmacology and molecular docking techniques were used to predict the potential anti-fibrotic targets of LH. Immunofluorescence, enzyme-linked immunosorbent assay (ELISA), real-time PCR (RT-PCR), and western blotting were used for experimental validation and mechanistic studies.

Results: Fifteen compounds that actively contributed to the cluster were identified as marker compounds. Acteoside, 8-O-acetyl shanzhiside methyl ester (8-O-ASME), Luteolin, Shanzhiside Methyl ester (SME), Loganin, Loganate were the main active components. Network pharmacology and molecular docking studies have shown that LH might improve liver fibrosis, inflammation, and oxidative stress, which might be related to key targets such as PTGS2, MAPK, EGFR, AKT1, SRC, Fn1, Col3a1, Col1a1, and PC-III. The results of ELISA, RT-PCR and western blot experiments showed that Acteoside, 8-O-ASME, Luteolin, SME, Loganin, Loganate, and the LH group could reduce the levels of fibronectin, Col1a1, Col3a1, α-SMA, Col-Ⅳ, LN, and PC-Ⅲ.

Conclusion: LH improves liver fibrosis induced by HSC-T6 cells and inhibits the deposition of extracellular matrix (ECM) in hepatocytes, resulting in a decrease in the degree of liver fibrosis and a good anti-liver fibrosis effect.

Keywords: Bioactive compounds; Lamiophlomis herba; Mechanisms; Network pharmacology; UPLC-Q-TOF-MS.

MeSH terms

Drugs, Chinese Herbal*
Esters
Humans
Liver Cirrhosis / drug therapy
Luteolin*
Molecular Docking Simulation

Substances

acteoside
loganin
Luteolin
Esters
Drugs, Chinese Herbal