Chinese Traditional and Herbal Drugs

Chemical constituents from Dendrobium huoshanense

Chinese Traditional and Herbal Drugs. 2026, 57(4): 1228-1233.

Objective To study on the chemical constituents from Dendrobium huoshanense. Methods The chemical constituents were separated and purified by silica gel, Sephadex LH-20, semi-prepared HPLC and other chromatography techniques. Their structures were elucidated by MS, 1D and 2D NMR spectroscopic data. Results Eleven compounds (1—11) were isolated, and were identified as trans-ferulic acid nonadecyl ester (1), trans-p-hydroxycinnamic acid nonadecyl ester (2), 2,4,7-trihydroxy-9,10-dihydrophenanthrene (3), naringenin (4), 5-hydroxy-3,4′-dimethoxybibenzyl (5), 5-hydroxy-3-methoxybibenzyl (6), dendrogratiol A (7), amoenylin (8), methyl ferulate (9), protocatechuic acid (10), p-hydroxybenzaldehyde (11). At a concentration of 100 μmol/L, compounds 4 and 7 exhibited inhibitory rates of 39.0% and 38.3% against tyrosinase, respectively. Conclusion Compounds 1 and 2 are new compounds, named dendrohuoshanin A and dendrohuoshanin B. Compounds 3, 5, 7—9 were isolated for the first time from this plant. Compound 3 was the first to be separated and purified through phytochemical methods from this plant. Compounds 1, 2, and 9 belong to simple phenylpropanoids, compound 3 is a dihydrophenanthrene, compound 4 is a dihydroflavone, and compounds 5—8 are bibenzyls. Compounds 4 and 7 show potential skin-whitening effects.

Alkaloids from fruit of Lycium chinense and their hepatoprotective activity

Chinese Traditional and Herbal Drugs. 2026, 57(4): 1234-1241.

Objective To study the alkaloids from the fruit of Lycium chinense and their hepatoprotective activity. Methods The compounds were isolated and purified by silica gel column chromatography, D101 macroporous resin column chromatography, ODS column chromatography, and semi-preparative HPLC. Their structures were identified by¹H-NMR, ¹³C-NMR and mass spectrometry. The acetaminophen (APAP)-induced injury of human liver cancer HepG2 cells model was used to evaluate the hepatoprotective activity of these compounds. Results Sixteen alkaloids were isolated from the ethanol extract of fruit of L. chinense. Their structures were identified as lyciumamide P (1), lyciumamide Q (2), lyciumamide R (3), N-cis-grossamide (4), cannabisin E (5), cannabisin F (6), cannabisin G (7), cannabisin H (8), heliotropamide (9), N-malonyl-tryptophan (10), N-acetyltryptophan methyl ester (11), equisetinine A (12), nicotinamide (13), methyl-5-hydroxy-2-pyridinecarboxylate (14), thymidine (15), N¹,N¹⁰-di-dihydrocaffeoylspermidine (16). Conclusion Compounds 1—16 were isolated from L. chinense for the first time. Compounds 12, 13, 15 and 16 were isolated from Lycium for the first time. Compounds 5—7 and 10—16 showed significant hepatoprotective activity against APAP-induced injury of human liver cancer HepG2 cells at 10 μmol/L.

Allergen screening using LC-MS/MS analysis and molecular docking technology for Safflower Injection

Chinese Traditional and Herbal Drugs. 2026, 57(4): 1242-1250.

Objective Chemical composition analysis of Carthamus tinctorius injection and screening of allergenic components using molecular docking technology. Methods High performance liquid chromatography-ion trap-time-of-flight high resolution mass spectrometry (HPLC-IT-TOF-MS) was used to identify the chemical constituents of Safflower Injection, and molecular docking technology was used to further screen potential allergens.Results A total of 40 compounds were identified from the Carthamus tinctorius injection, including 26 chalcone C-glycosides, eight flavonoids, three alkaloids, and three other types of compounds. All compounds were identified in negative ion mode. These compounds were linked to human serum albumin (HSA), Mas-related G protein-coupled receptor X2 (MRGPRX2) and Ras homolog gene family member A (RhoA), among which six compounds docked with HAS and nine compounds docked with MRGPRX2. It was found that 6-hydroxykaempferol compounds and safflower quinone compounds were the main allergic components in safflower injection. Conclusion A method for allergen screening combining liquid chromatography-mass spectrometry and molecular docking was established. A total of 40 compounds were identified from Safflower Injection, and 6-hydroxykaempferols and safflower quinones were identified as potential allergens. This study provides important reference and data for allergen screening and sensitization mechanism research of Safflower Injection.

Effects of soluble excipients on disintegration behavior of traditional Chinese medicine extract tablets

Chinese Traditional and Herbal Drugs. 2026, 57(4): 1251-1263.

Objective To systematically evaluate the effects of soluble excipients on the disintegration behavior of Chinese medicine extract tablets prepared by different processes, thereby providing a scientific basis for the formulation design of Chinese medicine tablets. Methods A total of 11 representative Chinese medicine extract powders were selected, and the impacts of three processes (direct compression, dry granulation compression, and wet granulation compression) on tablet disintegration time and dissolution were compared. On this basis, Rougui (Cinnamomi Cortex) and Quɑnshen (Bistortae Rhizoma) extract tablets with poor disintegration performance were chosen for a factorial experimental design to investigate the modulating effects of soluble excipient type (sugar alcohols, lactose, and starch and its derivatives), proportion (10%, 20%, and 30%), and preparation process (dry granulation compression and wet granulation compression) on tablet disintegration. Results Except for Kushen (Sophorae Flavescentis Radix), the granulation process had minimal impact on the disintegration behavior of single Chinese medicine extract tablets, including Hujisheng (Visci Herba), Dɑnggui (Angelicae Sinensis Radix), Chuɑnxiong (Chuanxiong Rhizoma), Wumei (Mume Fructus), Fuchaocɑngzhu (Atractylodis Rhizoma stir-fried with bran), Zhiheshouwu (Polygoni Multiflori Radix Praeparata), Bohe (Menthae Haplocalycis Herba) with a disintegration time ≤ 30 min. However, for single extract tablets with slower disintegration (> 30 min), such as Xixin (Asari Radix et Rhizoma), Cinnamomi Cortex and Bistortae Rhizoma, granulation prolonged disintegration time and reduced dissolution rate. Under high drug-loading conditions (≥ 70%) sugar alcohols and lactose showed the most significant improvement in disintegration of Cinnamomi Cortex and Bistortae Rhizoma extract tablets, whereas starch and its derivatives exhibited limited effects but enhanced the dissolution of water-soluble components under wet granulation. Wet granulation was more suitable for Cinnamomi Cortex tablets, while dry granulation was preferable for Bistortae Rhizoma tablets. Conclusion In the formulation design of high drug-loading Chinese medicine extract tablets, selecting sugar alcohols or lactose as excipients and optimizing the granulation process based on material properties are effective strategies to enhance disintegration and dissolution. This study provides foundational data for the development of Chinese medicine tablets and related solid dosage forms.

Multidimensional evaluation of Asini Corii Colla formula granules based on transfer of critical quality attributes in process of decoction pieces-intermediates-finished products

Chinese Traditional and Herbal Drugs. 2026, 57(4): 1264-1274.

Objective To analyze variations in HPLC fingerprint profiles, characteristic constituents, and energy-related components during the preparation of Ejiɑo (Asini Corii Colla, ACC) decoction pieces, intermediates, and formulated granules. To investigate the transfer patterns of their critical quality attributes. And to establish a multidimensional quality control methodology tailored to the characteristics of ACC formulated granules. Methods HPLC fingerprint chromatograms for ACC decoction pieces, intermediates, and formulated granules were established using an indophenol post-column derivatisation-amino acid analyser method. Common peaks were assigned using reference substances. The quality variations across ten batches of ACC samples were analyzed by combining the fingerprint data with chemometric techniques. Furthermore, a method for the simultaneous quantification of six characteristic amino acids (aspartic acid, glutamate, glycine, alanine, arginine, proline) was developed. Conventional methods were employed to determine energy components, including protein and fat content. The production processes of ACC formulated granules were evaluated multi-dimensionally to construct a dynamic quality monitoring framework. Results Fingerprint chromatograms were established for ten batches of ACC, encompassing its decoction pieces, intermediates, and formulated granules. A total of 21 common peaks were identified, and the similarity among all batches were ≥ 0.990. The average transfer rate of the primary characteristic amino acids was 75.74%—92.09% from the decoction pieces to the intermediates, and 76.63%—94.84% from the intermediates to the formulated granules. The average transfer rate of energy components was 96.75% from the decoction pieces to the intermediates, and the average transfer rate of energy components was 43.26% from the intermediates to the formulated granules. Conclusion The indophenol post-column derivatization‑amino acid analyse method was used to construct HPLC fingerprints, determine multiple characteristic components, and measure energy components simultaneously, realizing a multidimensional evaluation of Ejiao decoction pieces‑intermediates‑finished products. A dynamic quality control method for the whole production process of Ejiao formula granules was established, providing a reference for its further research and development.

Optimization, characterization, and evaluation of myocardium-targeting CTP-modified tanshinone II_A micelles for cardioprotection

Chinese Traditional and Herbal Drugs. 2026, 57(4): 1275-1285.

Objective To construct and optimize tanshinone II_A (TS II_A)-loaded micelles modified with a cardiomyocyte-targeting peptide CTP (APWHLSSQYSRT) (CTP-Ms/TS II_A), optimize their formulation, and evaluate their physicochemical properties and cardioprotective effects in vitro. Methods CTP-Ms/TS II_A were prepared using the film hydration method. A Box-Behnken response surface design was applied to optimize formulation parameters (Soluplus concentration, TPGS₁₀₀₀ concentration, hydration temperature) with encapsulation efficiency as the evaluation index. Particle size, ζ potential, and morphology of micelles were characterized by dynamic light scattering and transmission electron microscopy (TEM). Critical micelle concentration (CMC) was determined using pyrene as a probe, and storage and serum stability were assessed. Cellular uptake was investigated in H9c2 cardiomyocytes by flow cytometry and fluorescence microscopy. In an isoproterenol-induced H9c2 injury model, intracellular reactive oxygen species (ROS), mitochondrial membrane potential, cell viability, and apoptosis were evaluated by DCFH-DA, JC-1, calcein/PI staining, and CCK-8 assays. Results The optimal preparation parameters were determined as: formulation volume 5 mL, Soluplus concentration 12 g/L, TPGS₁₀₀₀ concentration 5 g/L, and hydration temperature 40 ℃. The CTP-Ms/TS II_A prepared under these conditions (with membrane materials including TS II_A, Soluplus, TPGS₁₀₀₀, DSPE-PEG₂₀₀₀, and DSPE-PEG₂₀₀₀-CTP) achieved a high EE of (90.64 ± 1.01)% (n＝3). The micelles exhibited a particle size of (89.30 ± 0.76) nm, a ζ potential of (−0.033 ± 0.150) mV, and a critical micelle concentration of 42.8 μg/mL, with good stability. Compared with non-targeted micelles, CTP-Ms/TS II_A exhibited significantly enhanced uptake in H9c2 cells, more effective ROS scavenging, restoration of mitochondrial membrane potential, and improved cell survival. Conclusion CTP-Ms/TS II_A with stable physicochemical properties were successfully prepared, and their cardiac-targeting and cardioprotective potential were verified by in vitro experiments. This work provides a new experimental basis and potential delivery strategy for the application of TS II_A in the prevention and treatment of cardiovascular diseases.

Quality evaluation of reference substances of classical formula Tiaowei Chengqi Decoction based on HPLC fingerprint combined with multivariate statistical analysis

WANG Tongyun, MAO Wenyi, CHEN Rui, CAO Yan, ZHENG Guohua, LU Shan, GUO Yujie

Chinese Traditional and Herbal Drugs. 2026, 57(4): 1286-1296.

Objective The quality research system of the classic formula Tiaowei Chengqi Decoction (TCD, 调胃承气汤) was constructed by establishing HPLC fingerprinting and index component content determination methods, and the quantity value transfer law of its reference samples were explored. Methods Prepare TCD reference samples from 15 batches of herbal materials sourced from different regions using traditional methods. Establish fingerprint profiles via HPLC and evaluate batch-to-batch consistency using chemometric methods such as hierarchical cluster analysis (HCA) orthogonal partial least squares-discriminant analysis (OPLS-DA) and principal component analysis (PCA) to identify the batch-to-batch consistency and differential markers. Simultaneously, Hotelling’s T² and DModX were calculated based on the PCA model, with 95% and 99% confidence limits serving as the warning and control limits [T²_Crit (95%) = 31.49, T²_Crit (99%) = 54.15, D_Crit = 1.97] for batch consistency evaluation. A method was established to simultaneously determine the content of six target components gallic acid, glycyrrhizin, aloe-emodin, emodin, glycyrrhetic acid, and rhein in 15 batches of samples and their corresponding crude drug slices. The transfer rate of these components from crude drug slices to samples was calculated. Results A robust HPLC fingerprint profile of TCD was successfully established, allowing for the identification of 16 common peaks. Chemometric analysis confirmed effective batch-to-batch differentiation, with gallic acid and glycyrrhizic acid identified as key chemical markers contributing to the discrimination of batch variations. Quantitative analysis of six marker components across 15 batches revealed mass fractions ranging from 0.521 to 1.581 mg/g for gallic acid, 0.143 to 0.711 mg/g for glycyrrhizin, 0.025 to 0.071 mg/g for aloe-emodin, 0.016 to 0.182 mg/g for emodin, 0.487 to 2.740 mg/g for glycyrrhizic acid, and 0.007 to 0.039 mg/g for rhein. Furthermore, component tracking from crude drug to final sample demonstrated average transfer rates of 17.625%,2.878%,5.929%,5.159%,1.689% and 1.088% for these compounds, respectively. Conclusion Combined with multi-component quantitative analysis with chemometric methods to develop an HPLC fingerprint profile for TCD, systematically investigating the compositional variation patterns from herbal materials to reference samples. The findings provide a scientific foundation for quality evaluation research on TCD.

Quality consistency evaluation of intermediates and reference samples of classic formula Qingxin Lianzi Yin based on Bizhunziwei by electronic tongue and its application in optimization of pretreatment processes

Chinese Traditional and Herbal Drugs. 2026, 57(4): 1297-1310.

Objective Avoltammetric electronic tongue was applied to establish Bizhunziwei for evaluating the quality consistency between classical formulas Qingxin Lianzi Yin (QLY, 清心莲子饮) intermediate and explore its application in the pretreatment process optimization of QLY. Methods By comprehensively analyzing the precision of Euclidean distance (Ed), mean Euclidean distance (M-Ed), and standardized Euclidean distance (S-Ed) between the taste PCA score plots of intermediates and substance benchmark in combination with the discrimination index (DI), to construct the standard taste profile. The effects of the sample’s pH value, the salt ions and redox-active substances on Bizhunziwei were studied and the precision, repeatability and stability of Bizhunziwei were investigated. The application of Bizhunziwei in the pretreatment processes of QLY such as extraction and drying of classic famous prescriptions was explored and the correlation between Bizhunziwei and the similarity of fingerprint profiles was analyzed. Results The Bizhunziwei could be defined as “S-Ed*DI” which was the product of standardized Euclidean distance and the discrimination index of the taste PCA score plots. The RSD values for the precision, repeatability and stability of Bizhunziwei were 2.355%, 5.630%, 3.573%, respectively. The sample’s pH value, the salt ions and redox-active substances had a significant impact on Bizhunziwei (P < 0.05). The Bizhunziwei could distinguish the extraction and drying process parameters of QLY. The Bizhunziwei had a good correlation with the similarity of the fingerprint profile of QLY. Conclusion The Bizhunziwei provides a new approach for evaluating the quality consistency between intermediates and substance benchmark of QLY, and offers a new perspective for the development of classic famous prescriptions.

Qualitative and quantitative analysis of chemical constituents and quality evaluation of Tiaojing Cuyun Pills based on liquid chromatography-mass spectrometry combined with pattern recognition technology

Chinese Traditional and Herbal Drugs. 2026, 57(4): 1311-1324.

Objective To conduct qualitative and quantitative analysis of the chemical constituents in Tiaojing Cuyun Pills (TCP, 调经促孕丸) using high-resolution mass spectrometry and to evaluate its quality comprehensively. Methods Ultra-high performance liquid chromatography-quadrupole/electrostatic field orbitrap high-resolution mass spectrometry (UHPLC-Q-Exactive Orbitrap HRMS) was employed in this study. Combined with reference standard comparison, mass spectral fragmentation rule analysis and database retrieval, a method for identifying and analyzing the in vitro chemical constituents of TCP was established, and the key constituents were quantified. Multivariate statistical methods were applied to analyze the quantitative data for comprehensive quality evaluation of TCP. Results A total of 105 compounds were identified by collecting mass spectral data in Full-scan data-dependent MS/MS (Fullmass ddMS²) mode, covering various structural types such as flavonoids, organic acids, quinones, glycosides, terpenoids, alkaloids and others. Meanwhile, a quantitative analysis method was established for 24 key constituents in the drug using the full-scan accurate quasi-molecular ion mode to achieve precise content determination. Principal component analysis (PCA) and orthogonal partial least squares-discriminant analysis (OPLS-DA) analysis showed that the overall quality of 10 batches of drugs was stable, and catechin, tanshinone I, baohuoside I, daidzein, paeoniflorin and caffeic acid might be the key constituents affecting drug quality. Conclusion Based on high-resolution mass spectrometry technology, a variety of chemical components in TCP can be qualitatively and quantitatively analyzed in a systematic, accurate and rapid manner, which lays a foundation for the research on its pharmacodynamic material basis and quality control.

Effect and mechanism of bufotalin on growth of human head and neck squamous cell carcinoma

Chinese Traditional and Herbal Drugs. 2026, 57(4): 1325-1335.

Objective To investigate the effect and potential mechanism of bufotalin on growth of human head and neck squamous cell carcinoma (HNSCC). Methods The effect of bufotalin on viability and proliferation of Cal-27 and FaDu cells were observed by CCK-8 method and plate clone formation experiment. The effect of bufotalin on cell cycle distribution of Cal-27 and FaDu cells were detected by flow cytometry. Western blotting was used to detect the effect of bufotalin on expressions of cyclin-dependent kinase 4 (CDK4) and cyclin D1 in Cal-27 and FaDu cells. To further explore the anti-tumor effects of bufotalin in vivo, a xenograft tumor model of HNSCC was established in nude mice. Proteomics technology was applied to identify differentially expressed proteins in bufotalin-treated Cal-27 cells, and the associated signaling pathways underlying its anti-tumor effect were analyzed. Western blotting was performed to assess the expressions of protein kinase R-like endoplasmic reticulum kinase (PERK)/eukaryotic initiation factor 2α (eIF2α) signaling pathway related proteins. Results In vitro experimental results showed that bufotalin significantly reduced the viability of Cal-27 and FaDu cells (P < 0.01, 0.001), inhibited their proliferation (P < 0.01, 0.001), induced cell cycle arrest in G₀/G₁ phase (P < 0.05, 0.01, 0.001), down-regulated the protein expressions of CDK4 and cyclin D1 in FaDu cells (P < 0.05, 0.001), and down-regulated the protein expression of CDK4 in Cal-27 cells (P < 0.05). The in vivo experimental results showed that bufotalin could significantly inhibit the growth of tumors in tumor bearing mice (P < 0.01, 0.001). Proteomics and IPA analysis showed that bufotalin could induce endoplasmic reticulum stress and up-regulate the expression levels of p-PERK and p-eIF2α in Cal-27 and FaDu cells (P < 0.05, 0.001). Conclusion Bufotalin could induce endoplasmic reticulum stress, activate EIF2 signaling pathway, and induce the arrest of HNSCC cells in G₀/G₁ phase, thereby inhibiting tumor cell proliferation and tumor growth in tumor-bearing mice.