Aristolochic acid analogues (AAAs) are a class of nitrophenanthrene derivatives predominantly occurring in Aristolochiaceae plants. Over the past decades, academic research has mostly focused on its strong adverse reactions such as nephrotoxicity and carcinogenicity. In contrast, their potential pharmacological activities—including anti-inflammatory, analgesic, and antitumor effects—have remained relatively underexplored, resulting in an imbalanced understanding of this compound class. In the face of the dual characteristics of toxicity and efficacy of this type of component, how to balance its toxicity and medicinal value is the key. Methods such as processing, compatibility, and structural modification may reduce adverse reactions, which could provide guarantees for the safe use of such components and traditional Chinese medicine. This review integrates current global advances in AAAs research, with a particular focus on their pharmacological activities and detoxification strategies, to provide references for the clinical application of drugs containing AAAs.

Pugongying (Taraxaci Herba) is a well-established medicinal and edible herb with a long history of use in traditional Chinese medicine, known for its heat-clearing, detoxifying, anti-inflammatory, and swelling-reducing properties. The Chinese Pharmacopoeia defines Taraxaci Herba as the dried whole plant of Taraxacum mongolicum, Taraxacum borealisinense, or several other closely related species within the genus Taraxacum (Asteraceae), making it a typical multi-origin herbal medicine. Taraxaci Herba comprises numerous species with highly similar interspecific morphological characteristics. Coupled with diverse ecological conditions across producing areas, this has led to mixed botanical origins in the marketplace and inconsistent quality of medicinal materials, thereby compromising the efficacy and safety of clinical use. This review summarizes recent advances in molecular identification technologies and quality evaluation methods for Taraxaci Herba, outlines the current status of quality control and comprehensive quality assessment research, and proposes future research perspectives. The aim is to provide a scientific reference for the standardization of medicinal materials, the selection of high-quality germplasm resources, and the high-quality development of the Taraxaci Herba industry.

Objective To investigate the chemical constituents and anti-inflammatory activity of the dried roots of Tibetan medicine Carpesium lipskyi. Methods The ethanol extract of C. lipskyi was isolated and purified using chromatographic techniques including silica gel column chromatography and Sephadex LH-20 gel column chromatography. The structures of the compounds were identified based on their physicochemical properties, spectroscopic methods (MS, NMR), and literature data. The in vitro anti-inflammatory activity of the compounds was evaluated using a lipopolysaccharide (LPS)-induced inflammatory model in mouse macrophage RAW264.7 cells. Results Nine compounds were isolated from the roots of C. lipskyi and identified as (1R,7R,10R,11S)-1-hydroxy-eudesma-3(4),5(6)-dien-11-oic acid methyl ester (1), (1R,4S,5R,7R)-1-acetoxy-11-hydroxy-eremophil-9(10)-ene (2), careudesmane D (3), isoalantolactone (4), 11-hydroxy-eremophil-1(10)-en-2,9-dione (5), carperemophilane A (6), carperemophilane B (7), protocatechuyl aldehyde (8), and umbelliferone (9). Compounds 2 and 7 inhibited LPS-induced NO production in RAW264.7 cells with half maximal inhibitory concentration (IC₅₀) values of (13.62 ± 1.30) μmol/L and (19.47 ± 2.67) μmol/L, respectively. Conclusion Compound 1 is a new eudesmane-type sesquiterpene and designated as carpesiol A, and compound 2 is a new eremophilane-type sesquiterpene and designated as carpesiol B. Compounds 3—7 were isolated from this plant for the first time. Compounds 2 and 7 show potential for development as anti-inflammatory drugs.

Objective To investigate the chemical constituents from the ethanol extract of the bark of Spondias pinnata and preliminarily evaluate their anti-inflammatory activity. Methods Various chromatographic techniques were employed to isolate and purify the constituents from the extract. Their structures were elucidated by spectroscopic methods including NMR spectroscopy, as well as GFN2NMR and computational chemistry approaches. The anti-inflammatory activity of the new compound was evaluated using an LPS/IFN-γ-induced MH-S cell inflammation model in vitro. Results Ten compounds were isolated from the ethanol extract of the bark of S. pinnata and identified as (5R,6S)-6-[(7E,9R)-9-hydroxy-10-({(15R,16R)-17-butoxycarbonyl-15,16-dihydroxypropoxy})but-7-en-7-yl]-6-hydroxy-1,1-dimethylcyclohexan-3-one (1), ampelopsisionoside (2), (2E,4E,1'R,3'S,5'R,8'S)-dihydrophaseic acid 3'-O-β-D-glucopyranoside (3), N-benzoyl-D-phenylalanine (2R)-2-(benzoylamino)-3-phenylpropyl ester (4), isolariciresinol-4-O-β-D-glucopyranoside (5), (+)-lyoniresin-4-yl-β-D-glucopyranoside (6), demethoxymatteucinol (7), 4'-hydroxy-3-O-β-D-glucopyranoside flavone (8), (2S)-2-hydroxynaringenin-4'-O-β-D-glucoside (9), and (S)-(-)-N-benzoylphenylalaninol (10). Compound 1 significantly inhibited the expression of TNF-α (P < 0.05) and IL-6 (P < 0.01) at a concentration of 10 μmol/L. Moreover, at 20 μmol/L, it markedly ameliorated the LPS/IFN-γ-induced morphological changes in MH-S cells. Conclusion Compound 1 is a new compound, named as spondias A. Compounds 2—4 and 7—10 were isolated from the genus Spondias for the first time, while compounds 5—6 were obtained from this species for the first time. The bioassay results indicate that compound 1 inhibits the transformation of MH-S cells to the M1 phenotype, suggesting its potential anti-inflammatory activity.

Objective To investigate the chemical constituents of Buxus microphylla and their anti-hepatocarcinoma activity in vitro. Methods The compounds were isolated and purified by column chromatography of silica gel, reversed-phase C₁₈, Sephadex LH-20, semi-preparative HPLC and preparative TLC. Their structures were elucidated by physicochemical properties and spectral analyses. The cytotoxicity of the isolates against human hepatocellular carcinoma HepG2 and Hep3B cells was assessed using the MTT assay. Flow cytometry was employed to analyze cell apoptosis. Western blotting was used to detect the expression of proteins related to cell apoptosis. Results Eighteen compounds were isolated and identified from the 70% ethanol extract of B. microphylla, including hederagenin (1), 3-O-β-D-glucopyranosylspinasterol (2), fagraeanolide (3), rel-(2α,3β)-7-O-methylcedrusin (4), caruilignan D (5), (7′S,8R,8′S)-isolariciresinol (6), 3-hydroxy-1,2-dimethoxyanthrone (7), 1-methoxy-2,3-methylenedioxyanthrone (8), 1,2,3-trimethoxyanthrone (9), syringaldehyde (10), syringic acid (11), vanillic acid (12), p-hydroxybenzoic acid (13), polygital (14), 9-pentacosenoic acid (15), rhamnakoside B (16), lupeol (17), and betulin (18). The in vitro activity screening revealed that compounds 2, 3, 16—18 exhibited cytotoxicity in HepG2 and Hep3B cells, among which compound 2 was the most potent. compound 2 significantly increased the proportion of apoptotic cells and elevated the expression of apoptosis-related proteins such as Bax, decreased the expression of Bcl-2, all of which were statistically significant compared with control group (P < 0.001) at 10 μmol/L. Conclusion Compound 1 and 17—18 are triterpenoids; Compound 2 is a steroidal glycoside; compounds 3—6 are lignans, compounds 7—9 are anthrones, compounds 10—13 are phenolic acids, and compounds 14—16 are other types. Among them, compounds 2—5, 7—9, and 14—16 are isolated from the genus Buxus for the first time. In the anti-hepatocarcinoma activity assay, compound 2 demonstrated significant effects, with IC₅₀ values of 5.87 μnol/L and 6.42 μnol/L against HepG2 and Hep3B cells, respectively. Moreover, it effectively induced apoptosis in HepG2 cells.

Objective To prepare different polysaccharide fractions of Xiaoyao San (逍遥散, XYS) by graded ethanol precipitation and to clarify the anti-inflammatory activity, structural characteristics, and in vivo absorption and distribution behavior of the major enriched fraction. Methods Different polysaccharide fractions of XYS (40%, 60%, and 80% ethanol-precipitated fractions) were obtained using a water extraction-ethanol precipitation procedure, and the primary enriched fraction was screened based on yield comparison. Based on the inflammation-depression correlation, an LPS-induced microglial inflammation model was established, and anti-inflammatory activity was evaluated by measuring inflammatory markers including TNF-α, IL-1β, IL-6, and iNOS. The composition and structural features of the target polysaccharide were characterized using UV-Vis spectroscopy, FT-IR, and NMR analyses. Fluorescently labeled polysaccharides were further prepared for in vivo pharmacokinetic studies in mice to systematically assess exposure levels and tissue distribution characteristics. Results Significant differences in yield were observed among polysaccharide fractions obtained at different ethanol precipitation ratios. The 60% ethanol fraction (XYSP-60) was identified as the major enriched fraction, with an extraction recovery of 37.5%. In the LPS-induced microglial inflammation model, XYSP-60 significantly downregulated the expression levels of TNF-α, IL-1β, IL-6, and iNOS, demonstrating clear anti-inflammatory activity. Structural characterization indicated that the polysaccharide mainly consisted of galacturonic acid, glucose, and fructose, with relatively stable structural features. Pharmacokinetic results showed that XYSP-60 exhibited high exposure in the intestine but limited entry into systemic circulation. Conclusion The 60% ethanol-precipitated fraction represents the principal enriched polysaccharide fraction of XYS, with stable structural characteristics and definite anti-inflammatory activity. Its in vivo behavior is characterized by high intestinal exposure and limited systemic absorption, suggesting that this fraction may serve as one of the key material bases underlying the anti-inflammatory effects of XYS.

Objective To optimize the extraction and β-cyclodextrin (β-CD) inclusion process for the volatile oil from the classical formula Dihuang Yinzi (地黄饮子) based on the quality by design (QbD) concept and the analytic hierarchy process-entropy weight (AHP-entropy) method. Methods Failure mode and effects analysis (FMEA) was employed for risk identification in the volatile oil extraction process. Heating time, material-to-liquid ratio, and soaking time were determined as the critical process parameters (CPPs), while cinnamaldehyde content, β-asarone content, and volatile oil extraction yield were defined as the critical quality attributes (CQAs). On the basis of single-factor tests, the Box-Behnken design-response surface methodology (BBD-RSM) was used for process optimization. The AHP-entropy weight method was applied to calculate a comprehensive score for the CQAs, which was then used to establish and validate an optimized design space. The inclusion process of volatile oil was investigated using the saturated aqueous solution method. The inclusion conditions were comprehensively optimized through orthogonal experimental design combined with the AHP-entropy weight method for multi-index evaluation. Finally, the optimal inclusion process parameters were determined and validated. Results The optimized volatile oil extraction process was as follows: soaking for 30 to 45 min, adding 9- to 10-fold volume of water, and extracting for 3.0 to 3.5 h. The optimal inclusion process parameters were: inclusion time of 2.0 h, β-cyclodextrin to volatile oil ratio of 10:1, and inclusion temperature of 30 ℃. Conclusion The volatile oil extraction and inclusion processes optimized based on the QbD concept and the AHP-entropy weight method can reliably ensure a stable extraction yield and consistent content of key active components. The resulting inclusion complex exhibits excellent quality. This study provides reliable data support and a solid process foundation for the industrial production and development of related Chinese medicinal preparations, while also offering a feasible pathway for the modern dosage form development of classical formulas.

Objective To systematically analyze the differences in volatile components of Chenxiang (Aquilariae Lignum Resinatum) essential oil (AEO) from various origins and extraction methods using an electronic nose combined with chemometrics, aiming to establish a novel method for rapid identification of AEO origins and extraction processes. Methods A total of 38 batches of AEO samples were collected from seven major origins using two extraction methods. Their chemical compositions were analyzed using gas chromatography-mass spectrometry (GC-MS), while overall aroma fingerprint information was obtained via electronic nose. Principal component analysis (PCA), partial least squares-discriminant analysis (PLS-DA), and orthogonal partial least squares-discriminant analysis (OPLS-DA) were comprehensively applied for pattern recognition of multi-source data. Results GC-MS analysis revealed that the common major components in all samples were benzylacetone, agarospirol, dehydrofuranone, and 2-(2-phenylethyl)chromone. Seven key differential compounds, including 2-(2-phenylethyl)chromone and 6-methoxy-2-(2-phenylethyl)chromone, were screened through variable importance projection (VIP > 1). The PCA results of the electronic nose response values show a good correlation with the origin or extraction method of AEO samples. The established OPLS-DA discriminant model exhibited excellent performance: the origin discriminant model achieved R_X² = 0.839, R_Y² = 0.794, Q² = 0.572 > 0.500, and the extraction method discriminant model achieved R_X² = 0.790, R_Y² = 0.647, Q² = 0.633 > 0.500, which can effectively classify AEO samples. Conclusion This study successfully combined the rapid identification of electronic nose with GC-MS component analysis, which confirmed that the combined strategy could accurately identify the extraction method and geographical origins of AEO, and clarified its material basis, providing an efficient and reliable new method for the classification and identification of AEO.

Objective Based on the supramolecular “imprinting template” theory, this study investigates the autonomous interaction patterns of the component groups in Wuwei Xiaodu Yin (WXY, 五味消毒饮) during the preparation process from crude herbs to reference samples and elucidates the quantitative transfer law of its quality attributes. Methods Fifteen batches of WXY reference samples were prepared via water decoction. A UPLC fingerprint analysis method was established to identify key chromatographic peaks and determine the contents of chlorogenic acid, esculetin, cichoric acid, neochlorogenic acid, cryptochlorogenic acid, isochlorogenic acid A, isochlorogenic acid B, isochlorogenic acid C, glehinnalin, and linarin were determined at 240 nm. Parameters such as transfer rate, extract yield, total statistical moment, and information entropy were calculated for both the herbs and the reference samples. Results The fingerprint similarity of the 15 batches of reference samples was greater than 0.9. Fourteen chromatographic peaks were identified, with 10 characteristic peaks defined. The extract yield ranged from 43.27% to 53.43%. The transfer rates of chlorogenic acid, esculetin, cichoric acid, neochlorogenic acid, cryptochlorogenic acid, isochlorogenic acid A, isochlorogenic acid B, isochlorogenic acid C, glehinnalin, and linarin were 34.25%—42.72%, 51.52%—58.80%, 28.21%—32.04%, 56.26%—65.59%, 40.63%—53.89%, 22.35%—31.29%, 38.39%—46.22%, 34.02%—40.82%, 18.64%—20.96%, and 28.55%—32.63%, respectively, with no discrete data observed. The relative standard deviations (RSDs) of the information entropy for the UPLC fingerprints of the five herbs and the reference samples were all less than 10%. The RSDs of mean chromatographic retention time of total quantum (MCRT_T) and information entropy for WXY (crude herbs) were 3.90% and 2.25%, respectively. Conclusion Quality analysis of the reference samples based on the parameters of the supramolecular “imprinting template” provides a scientific basis for the quality control of WXY reference samples and the development of compound formulations.

Objective In response to the lack of objective standards for the nine-steaming and nine-drying process of Huangjing (Polygonati Rhizoma), this study quantified the dynamic changes in traits and components during processing, combined with zebrafish antioxidant activity experiments, to identify the optimal stage for comprehensive quality and provide a scientific basis for establishing modern quality control methods. Methods Using the decoction pieces of Polygonatum cyrtonema as the object of study, a colorimeter, texture analyzer, and electronic tongue were employed to quantify the color, texture, and taste of samples from different steaming cycles (S0—S9). Polysaccharide content, reducing sugars and amino acids was determined by UV-Vis, while 5-hydroxymethylfurfural (5-HMF) were measured using HPLC. Hierarchical cluster analysis (HCA) and principal component analysis (PCA) were used to identify patterns in the processing stages. Pearson correlation analysis, the CRITIC objective weighting method, and zebrafish antioxidant experiments were integrated for comprehensive evaluation. Results As steaming progressed, color parameters (E_ab^*, L^* and b^*) continuously decreased, texture parameters (hardness, chewiness, gumminess) significantly declined, and moisture content increased. In terms of taste, bitterness and astringency markedly decreased by the third steaming cycle (S3), while sweetness increased. Chemically, 5-HMF accumulated continuously, reducing sugars peaked at S3 (1.38%), and amino acid and polysaccharide contents stabilized after S3. The correlation network analysis revealed significant relationships among trait indicators, chemical components, and bioactivity (P < 0.05). Multivariate statistical analysis divided the processing into three stages, with the early stage (S1—S3) identified as the critical transition period for quality formation. The comprehensive evaluation using the Criteria importance through intercriteria correlation method indicated that sample S3 achieved the highest overall quality score (65.41). At this stage, the sample was characterized by moderate 5-HMF accumulation, peak reducing sugar conten, and and maintenance of amino acids at a high level. It exhibited blackish-brown color (a^* was 11.13), with a soft and flexible texture (springiness was 0.647), and a disappearance of the numbing sensation. Its taste was sweet with slight bitterness (sweetness value was 4.50, bitterness value was 5.55), accompanied by a significantly enhanced antioxidant capacity. Conclusion This study establishes the third steaming cycle (S3) as the optimized processing endpoint for the nine-steaming and nine-drying process of P. cyrtonema and established amulti-dimensional quantifiable quality control system centered on “appearance properties-intrinsic components-bioactivity”. These findings provide a scientific basis for the standardization and precise quality control of this processing method.