1477-44-7Relevant articles and documents
Structure-based design of glycyrrhetinic acid derivatives as potent anti-sepsis agents targeting high-mobility group box-1
Wang, Yuanyuan,Yu, Zongmin,Yuan, Hu,Chen, Hao,Xie, Ning,Wang, Zhibin,Sun, Qingyan,Zhang, Weidong
, (2020/11/27)
Novel Glycyrrhetinic Acid (GA) derivatives with fused heterocycles on A ring were structure-based designed and synthesized. Their potential anti-inflammatory effects were investigated by a classical LPS stimulated macrophage model. Surface plasmon resonance (SPR) was used to verify the binding of GA analogues with HMGB1. A preliminary structure–activity relationship was summarized and an analogue GA-60 with ortho-methoxybenzyl pyrozole showed stronger anti-inflammatory effect and higher affinity for HMGB1 with a Kd value of 12.5 μM. In addition, this compound exhibited excellent inhibitory functions on NO (96%), TNF-α (94%), and IL-6 (100%), by interfering with phosphorylation of p38, ERK, JNK MAPKs, as well as that of NF-κB p65 and IKKα/β. Moreover, GA-60 extended the survival of either the classic CLP-induced or LPS-induced sepsis mouse models. Molecular modeling predictions further supported these findings, clearly indicating that inhibiting HMGB1 release, using fused heterocyclic GA derivatives, is a promising strategy for treatment of sepsis.
Synthesis and inhibition of α-glucosidase of methyl glycyrrhetinate glycosides
Zhang, Wei,Wang, He-Ying,Wang, Huai-Xu,Zhu, Zhen-Yuan
supporting information, p. 1874 - 1880 (2019/07/22)
The synthesis of the methyl glycyrrhetinate glycosides and inhibition of α-glucosidase were studied. The carboxyl group of glycyrrhetinic acid was methylated, and glucose and galactose were introduced into the hydroxyl group to obtain compounds 7 and 12.
Application of acetyl glycyrrhetinic acid methyl ester in preparation of medicine for treating viral hepatitis B
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Paragraph 0025; 0028-0031, (2020/11/25)
The invention relates to application of acetyl glycyrrhetinic acid methyl ester in preparation of a medicine for treating viral hepatitis B. Specifically, the invention provides an application of a compound shown as a formula (1), namely 3 beta-acetoxy-11-carbonyl oleanane-12-ene-30-carboxylic acid methyl ester, in preparation of a medicine for preventing and treating hepatitis B virus infection diseases. The compound shown in the formula (1) has remarkable activity of inhibiting HBeAg secreted by HepG2.2. 15 cells; under the concentration of 100 micrograms per milliliter, the intensity of inhibiting HBeAg secretion is 51.4% and is 3.78 times that of a positive control drug alpha-interferon (10000 units per milliliter) and 4.94 times that of lamivudine (100 micrograms per milliliter) respectively; under the concentration, the inhibition ratio of the lamivudine to HBV-DNA replication is 94.6%, and the inhibition strength (the inhibition ratio of 3-TC with the concentration of 100 micrograms per milliliter to HBV-DNA is 88.4%) of the lamivudine is higher than that of lamivudine with the same concentration and is 3.1 times that of high-concentration alpha-interferon (10000 units per milliliter). Therefore, the acetyl glycyrrhetinic acid methyl ester can be expected to be used for preparing non-nucleoside medicines for treating hepatitis B virus infection diseases; specifically, the compound can be used for preparing an HBV-DNA inhibitor and an HBeAg inhibitor, and the preparation method of the compound is simple in step, low in cost, wide in raw material source and easy for industrial production.
