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Updated: Sep 11, 2026

Preparation of Enantiopure Non-Activated Aziridines and Synthesis of Biemamide B, D, and epiallo-Isomuscarine
Published on: June 13, 2022
Design and Synthesis of Anemoside B4 Derivatives as Pyruvate Carboxylase-Targeting Therapeutic Agents for Atopic
Heng Li1, Yexin Du1, Qiurong Li1
1College of Pharmaceutical Sciences, Suzhou Medical College of Soochow University, Soochow University, Suzhou, Jiangsu215123, China.
Abstract:
Although injectable anemoside B4 (AB4) has therapeutic potential for atopic dermatitis (AD), its clinical use is restricted by safety and pharmacokinetic issues. Therefore, we designed 42 AB4 derivatives, established a preliminary SAR for anti-inflammatory and antiallergic activities, and selected three promising compounds for in vivo evaluation in an AD mouse model, leading to the identification of B4-39 as the lead compound. In a DNCB-induced AD mouse model, topical B4-39 (6.6 mg/kg) was more effective than dexamethasone and free from its side effects, while matching the efficacy of crisaborole at a much lower dose and providing better skin barrier repair. Mechanistically, B4-39 targets pyruvate carboxylase (PC)─a novel therapeutic target in AD─modulating the TCA cycle to suppress dendritic cell activation and concurrently inhibiting NF-κB and NLRP3 inflammasome signaling. Given its enhanced efficacy, steroid-sparing safety, novel PC-targeted action, and favorable topical delivery, B4-39 is a highly promising candidate for AD treatment.
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