Tamaractam, a New Bioactive Lactam from Tamarix ramosissima, Induces Apoptosis in Rheumatoid Arthritis Fibroblast-Like Synoviocytes

Autor: Yang Niu, Jing Zhao, Huai-Qin Han, Zhen-Hua Miao, Li Weiqi, Li Juan, Xun-Xia Zhao, Yao Yao, Na Sun, Cheng-Shuai Jiang
Jazyk: angličtina
Rok vydání: 2017
Předmět:
0301 basic medicine
rheumatoid arthritis
Lactams
growth inhibitory activity
Electrospray ionization
Pharmaceutical Science
Nanotechnology
tamaractam
Article
Cell Line
Analytical Chemistry
Flow cytometry
Arthritis
Rheumatoid
lcsh:QD241-441
03 medical and health sciences
chemistry.chemical_compound
0302 clinical medicine
lcsh:Organic chemistry
Bromide
Tamarix ramosissima
fibroblast-like synoviocytes
apoptosis
Drug Discovery
medicine
Humans
Medicine
Chinese Traditional
Physical and Theoretical Chemistry
Fibroblast
Cell Proliferation
030203 arthritis & rheumatology
TUNEL assay
medicine.diagnostic_test
Tamaricaceae
Organic Chemistry
Fibroblasts
Cell cycle
Synoviocytes
Molecular biology
Deoxyepinephrine
030104 developmental biology
medicine.anatomical_structure
chemistry
Chemistry (miscellaneous)
Apoptosis
Lactam
Molecular Medicine
Zdroj: Molecules, Vol 22, Iss 1, p 96 (2017)
Molecules; Volume 22; Issue 1; Pages: 96
Molecules : A Journal of Synthetic Chemistry and Natural Product Chemistry
ISSN: 1420-3049
Popis: Chemical investigation of Tamarix ramosissima Ledeb, a traditional herbal medicine used for rheumatoid arthritis (RA) treatment in northwest China, led to the discovery of a new phenolic aromatic rings substituted lactam, tamaractam (1), together with the previously reported compounds cis-N-feruloyl-3-O-methyldopamine (2) and trans-N-feruloyl-3-O-methyldopamine (3). The structures of the compounds were determined by high resolution electrospray ionization mass spectroscopy (HRESIMS) and 1D and 2D-NMR experiments, as well as comparison with the literature data. The effects of the three compounds on the viability of RA fibroblast-like synoviocytes (RA-FLS) were assessed by 3-(4,5-dimethyl-2-thiazolyl)-2,5-diphenyl-2-H-tetrazolium bromide (MTT) assay. Pro-apoptosis effect of compound 1 in RA-FLS was further investigated by terminal deoxynucleotidyl transferase-mediated dUTP nick-end labeling (TUNEL) assay, activated caspase-3/7 level assessment using luminescence assay, and sub-G1 fraction measurement using flow cytometry. It was found that these three compounds displayed variable proliferation inhibitory activity in RA-FLS, and compound 1 exhibited the strongest effect. Compound 1 could remarkably induce cellular apoptosis of RA-FLS, increase activated caspase-3/7 levels, and significantly increase sub-G1 fraction in the cell cycle. The results suggested that compound 1 may inhibit the proliferation of RA-FLS through apoptosis-inducing effect, and these compounds may contribute to the anti-RA effect of T. ramosissima.
Databáze: OpenAIRE
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