70475-59-1Relevant articles and documents
Synthesis, biological evaluation, and docking studies of a novel sulfonamido-based gallate as pro-chondrogenic agent for the treatment of cartilage
Lin, Xiao,Chai, Ling,Liu, Buming,Chen, Hailan,Zheng, Li,Liu, Qin,Lin, Cuiwu
, (2017)
Gallic acid (GA) and its derivatives are anti-inflammatory agents and are reported to have potent effects on Osteoarthritis (OA) treatment. Nonetheless, it is generally accepted that the therapeutic effect and biocompatibility of GA is much weaker than it
Effect of a novel synthesized sulfonamido-based gallate-SZNTC on chondrocytes metabolism in vitro
Liu, Qin,Li, Mu-Yan,Lin, Xiao,Lin, Cui-Wu,Liu, Bu-Ming,Zheng, Li,Zhao, Jin-Min
, p. 127 - 138 (2014)
The ideal therapeutic agent for treatment of osteoarthritis (OA) should have not only potent anti-inflammatory effect but also favorable biological properties to restore cartilage function. Gallic acid (GA) and its derivatives are anti-inflammatory agents
Gallic acid hydrogen sulfide derivative and preparation method and medical application thereof
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Paragraph 0063; 0071; 0072, (2021/03/31)
The invention discloses a gallic acid hydrogen sulfide derivative and a preparation method and medical application thereof. The general formula of the gallic acid hydrogen sulfide derivative is A-Y-X,and A is gallic acid; Y is -C (O) O-, -C (O) NH-, -C (O) OC (O)-, -C (O) NHCH2 C (O)- or is absent, and when Y is absent, the compound is A-X; X is a moiety capable of releasing hydrogen sulfide alone or in combination with A. Compared with gallic acid and existing classic non-steroidal anti-inflammatory drugs, the gallic acid hydrogen sulfide derivative has the advantages that the anti-inflammatory activity is equivalent or enhanced, the side effects of gastrointestinal tracts and cardiovascular diseases are weakened, and the gallic acid hydrogen sulfide derivative has high anti-tumor activity and good cardiovascular and neuroprotective effects.
Syntheses, Structures, and Bioactivity Evaluation of some Transition Metal Complexes with Aroylbis(N,N-diethylthioureas) Derived from Natural Compounds
Thang Pham, Chien,Thuy Pham, Thu,Ha Nguyen, Viet,Nguyet Trieu, Thi,Huy Nguyen, Hung
, p. 1383 - 1391 (2021/05/21)
Two novel benzoylthioureas derived from gallic acid, (tri-O-acetyl)galloyl-N,N-diethylthiourea HL1, and cinnamic acid, cinnamoyl-N,N-diethylthiourea HL2 have been successfully prepared and characterized by means of elemental analysis
Structure-activity relationship study and biological evaluation of SAC-Garlic acid conjugates as novel anti-inflammatory agents
Bi, Jingjie,Wang, Wenqing,Du, Junxi,Chen, Kun,Cheng, Kui
, p. 233 - 245 (2019/07/02)
A series of S-allyl-L-cysteine (SAC) with garlic acid conjugates as anti-inflammatory agents were designed and synthesized. Among the 40 tested compounds, SMU-8c exhibited the most potent inhibitory activity to Pam3CSK4-induced nitric oxide (NO) in RAW264.7 macrophages with IC50 of 22.54 ± 2.60 μM. The structure-activity relationship (SAR) study suggested that the esterified carboxyl group, carbon chain extension and methoxylation phenol hydroxy could improve the anti-inflammatory efficacy. Preliminary anti-inflammatory mechanism studies showed that SMU-8c significantly down-regulated the levels of Pam3CSK4 triggered TNF-α cytokine in human THP-1 cells, mouse RAW 264.7 macrophages, as well as in ex-vivo human peripheral blood mononuclear cells (PBMC) with no influence on cell viability. SMU-8c specifically blocked the Pam3CSK4 ignited secreted embryonic alkaline phosphatase (SEAP) signaling with no influence to Poly I:C or LPS triggered TLR3 or TLR4 signaling. Moreover, SMU-8c suppressed TLR2 in HEK-Blue hTLR2 cells and inhibited the formation of TLR1-TLR2, and TLR2-TLR6 complex in human PBMC. In summary, SMU-8c inhibited the TLR2 signaling pathway to down-regulate the inflammation cytokines, such as NO, SEAP and TNF-α, to realize its anti-inflammatory activity.