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To integrate the active advantages of 18β‐glycyrrhetinic acid (18β‐GA) and emodin, improve bioavailability, increase efficiency, and reduce toxicity, a one‐step innovative synthetic route was set up for the first time: 4‐dimethylaminopyridine (DMAP) was used as catalyst, 1‐ethyl‐(3‐dimethylaminopropyl)carboimide hydrochloride (EDCI) as condensation agent, dry dichloromethane (DCM) as solvent at 25 °C for 12 h, the three target products were obtained and purified by high performance liquid chromatography (HPLC), the chemical structures of them were characterized by nuclear magnetic resonance (NMR) technique and high resolution electron ionization mass spectrometry (HREI‐MS), namely, 18β‐glycyrrhetinic acid‐3‐emodin ester (1, yield 78.83 %, known), di‐18β‐glycyrrhetinic acid‐1‐emodin ester (2, yield 6.49 %, new), and di‐18β‐glycyrrhetinic acid‐8‐emodin ester (3, yield 1.81 %, new). To estimate their effects of the products on toxicity in zebrafish embryos and juvenile fishes, the two precursors and three target products were assayed involving in hatching rate, survival rate, morphology, heart rate, and apoptosis of cardiomyocytes. The results showed that the target products enhanced the hatching and survival rate of zebrafish embryos, decreased the malformation rate and the apoptosis of cardiomyocytes. It should be suggested that the one‐step synthesis route with high yield makes the industrial application of the target products possible due to significantly reduced toxicity. The two new by‐products provide potential candidates for the applications of pharmaceutical industry in the future.

Background Rumex japonicus Houtt (R. japonicus) is mainly used to treat various skin diseases in Southeast Asia. However, there are few researches on its quality evaluation methods and anti-fungal activity. Objective To establish the quality control criteria for the effective parts from R. japonicus against psoriasis. Method High-performance liquid chromatography (HPLC) was established for its fingerprint, the similarity evaluation, cluster (CA) and principal component analysis (PCA) were used to reveal the differences of those fingerprints among the tested R. japonicus. Network pharmacology analyzed the relationship between the components and psoriasis, revealing the potential targets of R. japonicus. Oxford cup anti-candida albicans experiment was used to verify the antifungal activity of R. japonicus. Results HPLC was developed for R. japonicus fingerprint by optimizing for 10 batches of quinquennial R. japonicus from different habitats, the 18 common peaks were identified with 10 characteristic peaks such as rutin, quercetin, aloe-emodin, nepodin, emodin, musizin-8-O-β-D-glucoside, chrysophanol, emodin-8-O-β-D-glucopyranoside, chrysophanol-8-O-β-D-glucopyranoside, and aloin, respectively; The network pharmacology-based analysis showed a high correlation between R. japonicus and psoriasis, revealing the potential targets of R. japonicus. The oxford cup anti-candida albicans experiment displayed a significant activity response to emodin-8-O-β-D-glucopyranoside and the ethyl acetate fraction of R. japonicus acidic aqueous extract. Conclusions A new and optimized HPLC method was created, the research provides an experimental basis for the development of effective drugs related to candida albicans. Highlights The fingerprint of R. japonicus was organically combined with network pharmacology to further clarify its criteria for quality control.

Rumex japonicus Houtt. (RJH) is a kind of Traditional Chinese Medicine (TCM) widely used in the treatment of serious skin diseases such as psoriasis. To further explore its bioactive components, the five-year root of RJH was used, the nuclear magnetic resonance (NMR) technique was employed with DMSO-d6 solvent for chemical structures, the scavenging capacity of the free radicals (DPPH, alkyl, –OH, and ˙O−2) was evaluated by electron spin resonance (ESR) method. In the results, seven compounds that were wholly characterized as anthraquinones (1 and 2), its c-glycosides (4–7), and flavonoid glycoside (3) especially for the hydrogen atoms from –OH groups located at phenol rings and glucose moieties. The compound 4 and 5 showed the significant bioac-tivity with the IC50 values (DPPH: 23.34 and 23.25 μM; alkyl: 20.27 and 20.15 μM; –OH: 26.03 and 25.50 μM; and ˙O−2: 14.69 and 14.68 μM, respectively). In conclusion, the DMSO-d6 solvent could make active protons be expressed clearly for accurate assignments. The compounds 4 and 5 could be suggested to be applied for potential candidates for related drugs.