961-29-5Relevant articles and documents
Discovery of isoliquiritigenin analogues that reverse acute hepatitis by inhibiting macrophage polarization
Yang, Junjie,Hu, Fanjie,Guo, Chengjun,Liang, Yuqing,Song, Haiying,Cheng, Kui
, (2021/06/15)
Screening a natural product library of 850 compounds yield isoliquiritigenin as an effective anti-inflammatory agent by inhibiting the production of pro-inflammatory NO induced by Pam3CSK4, while its activity accompanied by toxicity. Further studies obtained the optimized isoliquiritigenin derivative SMU-B14, which can inhibit Pam3CSK4 triggered toll-like receptor 2 (TLR2) signaling with low toxicity and high potency. Preliminary mechanism studies indicated that SMU-B14 worked through TLR2/MyD88, phosphorylation of IKKα/β, leading to the reduce degradation of NF-κB related IKBα and p65 complex, then inhibited the production of inflammatory cytokines, such as TNF-α, IL-6, IL-1β both in human and murine cell lines. Subsequent polarization experiments showed SMU-B14 significant reversed the polarization of M1 phenotype primary macrophage activated by Pam3CSK4 in vitro, and reduced the infiltration of neutrophil and polarization of M1-type macrophage, decreased serum alanine transaminase (ALT), as a result protected liver from being injured in vivo. In summary, we obtained an optimized lead compound SMU-B14 and found it functionally blocked TLR2/MyD88/NF-κB signaling pathway to down-regulate the production of inflammatory cytokines resulted significant liver protection property.
Isoliquiritigenin Derivatives Inhibit RANKL-Induced Osteoclastogenesis by Regulating p38 and NF-κB Activation in RAW 264.7 Cells
Choi, Jung-Won,Hwang, Ki-Chul,Jeong, Seongtae,Kim, Kundo,Kim, Sang Woo,Lee, Jiyun,Lee, Seahyoung,Lee, Yunmi,Lim, Soyeon,Oh, Sena
, (2020/09/17)
Bone diseases may not be imminently life-threatening or a leading cause of death such as heart diseases or cancers. However, as aging population grows in almost every part of the world, they surely impose significant socioeconomic burden on the society, not to mention the patients and their families. Osteoporosis is the most common type of bone disease, which frequently develops in seniors, especially in postmenopausal women. Although currently several anti-osteoclastic drugs designed to suppress excessive osteoclast activation, a major cause of osteoporosis, are commercially available, accompanying adverse effects ranging from mild to severe have been reported as well. Natural products have become increasingly popular because of their effectiveness with fewer side effects. Isoliquiritigenin (ILG), a natural flavonoid from licorice, has been reported to suppress osteoclast differentiation and activation. In the present study, newly synthesized ILG derivatives were screened for their anti-osteoporotic activity as more potent substitute candidates to ILG. Out of the 12 ILG derivatives tested, two compounds demonstrated significantly improved bone loss in vitro by inhibiting both osteoclastogenesis and osteoclast activity. The results of the present study indicate that these compounds may serve as a potential drug for osteoporosis and warrant further studies to evaluate their in vivo efficacy.
A different synthesis method of glycyrrhizin
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Paragraph 0028; 0035-0037; 0040-0042; 0047-0048, (2019/05/11)
The invention discloses a synthesis method of glycyrrhizin, is to Paeonia suffruticosa Andr. (tree peony bark) phenol and P-hydroxy-formaldehyde as raw materials, under the action of the alkaline catalyst through claessen - Schmidt condensation reaction of direct synthesis of 4 '- methoxy - 2', 4 - dihydroxy chalcone, then under the effect of the hydrobromide in the molecule of the ether linkage of the disconnect, is transformed into the 2 ', 4, 4' - three hydroxy chalcone is isoliquiritigenin, after recrystallizing and obtain high-purity isoliquiritigenin. Paeonia suffruticosa Andr. (tree peony bark) phenol and P-hydroxybenzaldehyde feeding ratio is: Paeonia suffruticosa Andr. (tree peony bark) phenol (mol): P-hydroxybenzaldehyde (mol)=1:1. Synthesis of the isoliquiritigenin carried out at normal temperature, few synthesis steps, short reaction time, does not require the complicated separation can be carried out continuously, the conversion of raw materials is high, the total yield can reach 85%, with a purity of 96% or more. Synthetic process green environmental protection, Paeonia suffruticosa Andr. (tree peony bark) phenol cheap raw materials, product of low production cost.
