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ABSTRACT
Leonurus japonicus Houtt is an important anti-skin pigmentation herb used in traditional Chinese medicine. However, the molecular basis for this activity is complex and not fully understood. In this study, water and ethanol extracts and polysaccharide extract from L. japonicus (LJPs) were analyzed by LC-MS/MS and HPLC-DAD separately. Cytotoxicity was analyzed by using CCK-8, antioxidant activity using flow cytometer, anti-MMPs, anti-tyrosinase and signalling pathway analysis using Western blotting to investigate their anti-melanogenesis function. The results showed that the water and ethanol extracts contained alkaloids, flavonoids, and phenolic acids. The LJPs mainly contain glucose, fucose, glucuronic acid, mannose, threonine and arginine, and structure characterization by FITR analyses indicated that LJPs have β- or α-D-glycosidic bonds and contain pyranose rings. The L. japonicus extracts displayed high cell viability at their maximum concentration. The water extract and polysaccharides significantly reduced lipopolysaccharide (LPS)-induced intracellular reactive oxygen species (ROS) content and exhibited a cytoprotective role. Also, these extracts displayed higher matrix metalloproteinase-2 (anti-MMP-2), anti-MMP-9 and anti-tyrosinase activities. Furthermore, the polysaccharides displayed significantly greater inhibitory effect on intracellular ROS and tyrosinase protein expression than α-arbutin and ursolic acid used for the clinical treatment of skin pigmentation. This study also investigated the polysaccharide inhibition of melanin synthesis by repressing the expression of melanocytic lineage-specific transcription factor (MITF) and melanogenic enzymes via modulation of the phosphoinositide 3-kinase (PI3K-Akt-mTOR) and β-catenin pathways. The overall results indicate that L. japonicus is a promising candidate for anti-pigmentation treatment.
Acknowledgements
The authors acknowledge funding from the research project of Beijing Institute of Chinese Medicine (YJS-2022-14). We thank Dr Ping Li for her important contribution to the conceptualisation and design of this study.
Declaration of conflicting interests
The author(s) declared no potential conflicts of interest with respect to the research, authorship, and/or publication of this article.
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Notes on contributors
Lin Zhang
Dr Lin Zhang graduated from the Western Sydney University with two Master's degree and a PhD. He has 16 years in biochemistry research and chemistry research experience. During my studies, he has published several academic papers and applied for several patents.
Cheang Soo Khoo
Dr Cheang Khoo graduated from the University of New South Wales with Bsc, a Master's degree and a PhD. He has 35 years in chemistry research experience in Western Sydney University. During his studies, he has published several academic papers.
ZhiKai Xiahou
Dr Zhikai Xiahou graduated from the Shandong Agricultural University with Bsc, Capital Normal University with a Master’s degree and University of Chinese Academy of Sciences with a PhD. He has 5 years in Molecular Biology Research, including CRISPR-Cas9 gene editing, transcriptome sequencing, real-time fluorescence quantitative PCR, molecular cloning, cell culture, immuno-technique. During his studies, he has published several academic papers.
Narsimha Reddy
Dr Narsimha Reddy graduated from the Osmania University with BSc and a Master’s degree and from Indian Institute of Technology with a PhD. He has more than 20 in Relationship bewteen structure of compounds from medinal plants and their bioactivity, and NMR studies experience. During his studies, he has published several academic papers and book chpaters.
Yue Li
Mr Yue Li (Associate Pharmacist) graduated from the China Pharmaceutical University with Bsc. He has 17 years of pharmaceutical analysis experience in Department of Instrument Management & Analysis. During his studies, he has published several academic papers.
Jingjing Lv
Dr Jingjing Lv graduated from the Henan University of Chinese Medicine with Bsc, Beijing University of Chinese Medicine with a Master’s degree and a PhD. He has 9 years in Dermatological research in Beijing Hospital of Traditional Chinese Medicine. During his studies, he has published several academic papers.
Meihe Sun
Mr Meihe Sun graduated from the Kaifeng University. He has 5 years in new medicine R&D and Chemical technological experience. During his studies, he has received a number of national patents as well as a awards for scientific and technological progress in Henan province.
Heming Fan
Ms Heming Fan graduated from the Beijing City University with a Bsc. She has 9 years in medicinal plant research and chemistry research experience in Beijing Institute of Chinese Medicine. During her studies, she has applied for several patents for health care products.
Xian Zhang
Mr Xian Zhang (Associate Pharmacist) graduated from the Beijing University of Chinese Medicine with Bsc degree and from Nanjing University with a Master’s degree. He has 22 years in in pharmaceutical analysis experience. During his studies, he has published several academic papers and received several national patents.