A new naphthoquinone derivative (1) together with twenty-three known compounds (2–24), were isolated from the aerial parts of Rubia cordifolia L. Their structures were elucidated on the basis of NMR and HR-ESIMS data. Compounds 1–13 were assessed for their inhibitory effects on NO production in LPS-stimulated RAW 264.7 macrophage cells. Compounds 2-6 exhibited significant inhibitory activities with IC₅₀ values of 21.37, 13.81, 24.56, 20.32, and 30.08 μmol·L⁻¹, respectively. Graphical Abstract

Background: This study aims to develop a fingerprint analysis method using ultra-high performance liquid chromatography (UPLC) for Moutan Cortex sourced from different regions. The objective is to establish quality control standards validated through the integration of chemometric methods and component structure theory. Methods: The mobile phase for UPLC consisted of acetonitrile (A) and a 0.1% aqueous formic acid solution (B), with gradient elution set as follows: 0–1 min, 8% A → 15% A; 1–8 min, 15% A → 18% A; 8–10 min, 18% A → 30% A; 10–15 min, 30% A → 35% A; 15–20 min, 35% A → 85% A; 20–21 min, 85% A → 8% A; and 21–26 min, 8% A → 8% A. Chemical markers significantly affecting Moutan Cortex from various regions were screened, and their identification was based on comparison with reference materials and content determination. Results: A total of 15 chemical markers were identified, including gallic acid, oxypaeoniflorin, catechin, methyl gallate, paeonolide, apiopaeonoside, albiflorin, paeoniflorin, benzoic acid, 1,2,3,6-tetra-O-galloyl-D-glucose, 1,2,3,4,6-pentagalloylglucose, mudanpioside C, benzoyloxypaeoniflorin, benzoylpaeoniflorin, and paeonol. These markers align with component structure theory, allowing for an analysis of the structural characteristics of Moutan Cortex from different regions. Conclusions: The findings provide a valuable reference for the future quality evaluation of traditional Chinese medicine preparations, enhancing the understanding of the material basis components in Moutan Cortex from diverse sources.

Dehydroabietic acid (DHA) is a naturally occurring diterpene with relevant biological activities. 7-Oxodehydroabietic acid as a highly oxidized state derivative from Dehydroabietic acid (DHA) showing good activities. However, the reported compounds did not include triazole derivatives. To discover novel potent anti-inflammatory diterpenoids, a series of hybrids of 7-Oxodehydroabietic acid containing 1,2,3-triazole moiety were designed and synthesized. The anti-inflammatory activity of the new compounds was assessed towards BV2 cell lines using L-NMMA (IC50 = 42.36 ± 2.47 µM) as a positive control. Compared with the L-NMMA, anti-inflammatory effect (NO inhibitory activities) was found in these novel molecules, especially compounds 9 (IC50 = 8.00 ± 0.83 µM), 10 (IC50 = 8.44 ± 0.89 µM), 15 (IC50 = 8.13 ± 0.97 µM) and 16 (IC50 = 8.84 ± 1.10 µM). The anti-inflammatory activity of compounds 9, 10, 15 and 16 in vivo are underway.

To discover novel, potent anti-inflammatory diterpenoids, a series of hybrids of 7-oxodehydroabietic acid bearing a 1,2,3-triazole moiety was designed and synthesized. The target compounds were characterized by means of ¹H NMR, ¹³C NMR, and ESI-HRMS. All the compounds were evaluated for their anti-inflammatory activity towards BV2 cell lines using L-NMMA (IC₅₀ = 42.36 ± 2.47 µM) as a positive control. Most showed good anti-inflammatory activities, especially compounds 10 (IC₅₀ = 8.40 ± 0.98 µM), 15 (IC₅₀ = 10.74 ± 2.67 µM), 16 (IC₅₀ = 10.96 ± 1.85 µM), and 17 (IC₅₀ = 9.76 ± 1.27 µM), which exhibited potent anti-inflammatory effects on BV2 cell lines.