Chinese Traditional and Herbal Drugs

Processing, pharmacological activities and current application status of wine-processed Polygonati Rhizoma

WONG LI SOO, ZHANG Yizhong, SONG Xiankang, SONG Dawei, HUANG Qiubo, WANG Yuting, BAO Kangde, WANG Dan

Chinese Traditional and Herbal Drugs. 2026, 57(14): 5736-5748.

Wine-processed Huangjing (Polygonati Rhizoma) is one of the primary processed products of the Polygonati Rhizoma, its preparation technology has seen important progress in recent years. Literature research and the latest research results indicate that the chemical composition undergoes notable changes during the wine-processing of Polygonati Rhizoma, particularly generating substances that pose potential health risks to humans, such as 5-hydroxymethylfurfural, 2,3-dihydro-3,5-dihydroxy-6-methyl-4H-pyran-4-one, acrylamide. Following processing, the pharmacological activities such as immunomodulation, antioxidant, hypoglycemic, and hypolipidemic effects are markedly enhanced. Current research on wine-processed Polygonati Rhizoma faces challenges such as inconsistent processing standards, unclear process parameters and difficulties in quality control. This paper systematically summarizes research progress of wine-processed Polygonati Rhizoma, including the historical evolution, modern processing techniques, chemical composition, and pharmacological effects. Future research should focus on standardizing processing techniques, modernizing mechanism analysis, and applying technological innovations to further promote the comprehensive and rapid development of the wine-processed Polygonati Rhizoma industry.

Research progress on mechanisms of active ingredients in Gentianae Macrophyllae Radix and its compound prescriptions in treatment of rheumatoid arthritis

Chinese Traditional and Herbal Drugs. 2026, 57(14): 5749-5760.

Rheumatoid arthritis (RA) is an autoimmune disease characterized by chronic synovitis and progressive joint destruction. Current clinical therapy drugs are limited by significant adverse effects and the development of drug resistance. Qinjiao (Gentianae Macrophyllae Radix), a well-known herb for dispelling wind-dampness in traditional Chinese medicine, has been historically used to treat RA with confirmed efficacy. Phytochemical studies have identified iridoids, triterpenoids, and flavonoids as the primary anti-RA constituents, with gentiopicroside, swertiamarin, ursolic acid, and kaempferol serving as key active monomers. These compounds exert multifaceted pharmacological effects through modulation of core signaling pathways including nuclear factor--κB (NF-κB), Janus kinase (JAK)/signal transducer and activator of transcription (STAT), and nuclear factor erythroid 2-related factor 2 (Nrf2)/heme oxygenase-1 (HO-1), leading to anti-inflammatory activity, immune regulation, inhibition of fibroblast-like synoviocyte (FLS) proliferation and invasion, antioxidant effects, suppression of angiogenesis, and protection against bone destruction and cartilage damage. In clinical practice, Qinjiao is commonly combined with other botanicals such as Fangji (Stephaniae Tetrandrae Radix), Sangjisheng (Taxilli Herba), and Duhuo (Angelicae Pubescentis Radix) in composite formulas (e.g., Juanbi Tang and Compound Qixiong Granules), achieving synergistic multi-component and multi-target effects tailored to different TCM syndromes of RA. This review summarizes the comprehensive regulatory mechanisms through which Qinjiao intervenes in RA pathogenesis via multiple pathways, highlighting its promising therapeutic potential and providing a theoretical basis for further investigation of its pharmacodynamic material basis and clinical development.

Medicinal value of Gynostemma pentaphyllum and research progress in its marketed drugs

Chinese Traditional and Herbal Drugs. 2026, 57(14): 5761-5777.

Gynostemma pentaphyllum is a medicinal and edible plant belonging to the genus Gynostemma of the family Cucurbitaceae and has a long history of medicinal use. Its dried aerial parts are used medicinally. G. pentaphyllum is rich in various active components such as saponins, flavonoids and polysaccharides, and exhibits a wide range of pharmacological activities, such as lipid-regulating and hepatoprotective effects, adjuvant effects in cancer treatment, and amelioration of atherosclerosis.. This review systematically summarizes the research status and progress of marketed drugs containing G. pentaphyllum as the principal medicinal ingredient, with a focus on their pharmacological effects, basic research, clinical application and quality standards. It aims to provide theoretical support for the popularization, application and further development of G. pentaphyllum in clinical medicine, promote the development of the G. pentaphyllum industry towards standardization, modernization and internationalization, and support the inheritance and innovation of traditional Chinese medicine.

Exploration of digital-intelligent governance mechanism for quality evaluation of traditional Chinese medicinal materials

Chinese Traditional and Herbal Drugs. 2026, 57(14): 5778-5788.

Quality evaluation of traditional Chinese medicinal materials, a critical link in the inheritance and innovation of Traditional Chinese Medicine (TCM), is currently confronted with structural dilemmas including fragmented standard system, data silos, intergenerational talent gaps, and conflicts between technical and ethics. From the collaborative “humanities-science” perspective, this study systematically reviews the evolution and inherent contradictions of TCM medicinal materials quality evaluation from an experience-led paradigm to digital-intelligent governance. To address the prominent issues of “replacing quality with quantity” and the absence of value rationality, this study constructs a four-dimensional collaborative governance framework underpinned by digital-intelligent technologies, which encompasses the core dimensions of quality, yield, humanities, and ecology. Through such implementation paths as full industrial chain traceability, intelligent modeling, and human-machine collaborative processing, the framework facilitates the explicitization of tacit knowledge and the quantification of ecological and cultural values. This study argues that the quality evaluation system for traditional Chinese medicinal materials should shift from the monism of technical rationality to the dual parallel emphasis of both value rationality and technical rationality. It emphasizes that the application of relevant technologies should be guided and regulated by humanities, so as to advance the transformation of TCM medicinal materials quality evaluation towards digital-intelligent governance.

Trends in online detection and dynamic evaluation of traditional Chinese medicine solid preparations based on digital and intelligent technologies

Chinese Traditional and Herbal Drugs. 2026, 57(13): 4949-4963.

Traditional Chinese medicine (TCM) solid preparations represent the primary dosage form in the TCM industry, and their manufacturing model rapidly transitioning from traditional batch production to continuous manufacturing. The complex composition of TCM ingredients, significant variability in material properties, and highly nonlinear process characteristics pose substantial challenges for online monitoring and dynamic quality evaluation. This paper systematically examines the developmental bottlenecks currently faced by online monitoring and dynamic quality evaluation in the context of continuous manufacturing of TCM solid preparations, focusing on their technical features. It provides a comprehensive review of approaches such as the construction of multidimensional process-quality databases, integration of mechanistic models with data-driven models, application of process analysis techniques at critical stages, and the implementation of digital twin and closed-loop control platforms. Future research should further explore the deep integration of “data-model-control” frameworks to transform passive monitoring into proactive prediction and adaptive regulation, thereby establishing a dynamic quality evaluation system tailored to the unique characteristics of TCM. This will provide theoretical foundations and technical references for standardizing, intelligentizing, and enhancing the quality of TCM solid preparation manufacturing.

Two new diphenyl ethers from Cyperus rotundus

Chinese Traditional and Herbal Drugs. 2026, 57(13): 4964-4968.

Objective To investigate the chemical constituents and their antitumor activities isolated from Cyperus rotundus. Methods The isolates were isolated and purified by silica gel, Sephadex gel, reversed-phase C₁₈ column chromatography, and semi-preparative high-performance liquid chromatography (HPLC). The structures of the obtained compounds were elucidated by spectroscopic methods such as nuclear magnetic resonance (NMR) and mass spectrometry (MS). Finally, all compounds were subjected to MTT assays to evaluate their anti-tumor activities. Results Two new diphenyl ethers were obtained from C. rotundus, specifically as 2,3′-dihydroxy-5,2′,5′-trimethoxy diphenyl ether (1) and 2,3′-dihydroxy-4,2′,5′-trimethoxy diphenyl ether (2). Both compounds exhibited moderate inhibitory effects on human colon cancer cell line HCT116, with median inhibition concentration (IC₅₀) values of (24.20 ± 0.77) and (25.26 ± 0.65) μmol/L, respectively. Conclusion Compounds 1 and 2 are new compounds with anti-tumor potential, named cydipethers A (1) and B (2). Diphenyl ethers were identified from C. rotundus for the first time.

Chemical constituents of Euphorbia heterophylla and their antioxidant activity

WU Guonan, YUAN Zhenyi, ZOU Kun, WANG Lei, LIU Chengxiong

Chinese Traditional and Herbal Drugs. 2026, 57(13): 4969-4978.

Objective To study the chemical constituents and in vitro antioxidant activity of Euphorbia heterophylla. Methods Comprehensive separation and purification were performed using normal-phase silica gel column chromatography, Sephadex LH-20 gel column chromatography and semi-preparative HPLC. Their structures were elucidated by comprehensive spectroscopic analyses (1D NMR, 2D NMR, HRMS) combined with single-crystal X-ray diffraction. The in vitro antioxidant activities of the isolated compounds were evaluated by DPPH and ABTS methods. Results A total of 18 compounds were isolated from the ethanol extract of E. heterophylla, their structures were elucidated as (3R,5R,8R,9R,13S,14R,17R,18R,21R)-3-hydroxy-21-isopropyl-4,4,9,13,14,17-hexamethyl-cyclopenta[a]chrysen-1(10)-en-2-one (1), β-amyrin ferulate (2), stigmasterol-4-en-3-one (3), isoquercitrin (4), quercetin 3-O-α-L-rhamnoside (5), kaempferol-3-O-α-arabifuranoside (6), kaempferol-3-O-α-L-rhamnoside (7), multiflorin A (8), 4,6-dimethoxyphthalide (9), vanillin (10), p-hydroxybenzaldehyde (11), protocatechuic acid (12), vanillic acid (13), 3-hydroxy-1-(4-hydroxy-3-methoxyphenyl) propan-1-one (14), ferulic acid (15), diethylhexyl adipate (16), 13-propylheptacosane (17) and 1-n-decanoyl hydroxy-benzoic acid (18), respectively. Antioxidant activity evaluation revealed that compounds 5 and 15 exhibited potent DPPH radical scavenging activity, with half maximal inhibitory concentration (IC₅₀) values of (15.88 ± 0.84) μg/mL and (15.95 ± 0.75) μg/mL, respectively. Moreover, compound 15 also exhibited potent ABTS radical scavenging activity, with an IC₅₀ value of (2.54 ± 0.57) μg/mL, outperforming the positive control L-ascorbic acid [(IC₅₀ 12.25 ± 0.82) μg/mL]. Conclusion Compound 1 is a novel fernane-type triterpenoid and named as euheterophyllfernane A, compounds 2—3, 6—11, 14 and 16—18 are isolated from E. heterophylla for the first time.

Chemical constituents of Fissistigma bracteolatum

Chinese Traditional and Herbal Drugs. 2026, 57(13): 4979-4986.

Objective To investigate the chemical constituents of Fissistigma bracteolatum. Methods The 95% ethanol extract of F. bracteolatum was successively separated by solvent partitioning, macroporous resin, silica gel, MCI, Sephadex LH-20, ODS column chromatography, and semi-preparative HPLC to obtain individual compounds. Their structures were elucidated using modern spectroscopic techniques such as NMR and MS. An in vitro inflammatory model was established using lipopolysaccharide (LPS)-stimulated RAW264.7 macrophages to evaluate the anti-inflammatory activity of the isolated compounds. Results A total of 22 compounds were isolated from F. bracteolatum, comprising of 12 flavonoids, 8 amides, 1 lignan, and 1 lactone. These were determined as: 5,7-dihydroxy-6,8-dimethoxyflavone (1), 5-hydroxy-7,8-dimethoxyflavone (2), quercetin (3), rutin (4), 5,7,8-trimethoxydihydroflavone (5), 5,6,8-trimethoxy-7-hydroxydihydroflavone (6), 6,7-dimethoxy-8-hydroxydihydroflavone (7), (2S)-7-hydroxy-6,8-dimethoxydihydroflavone (8), dihydroquercetin (9), aromadendrin (10), 4,2',6'-trihydroxy-3',4'-dimethoxy- dihydrochalcone (11), 2',6'-dihydroxy-4'-methoxydihydrochalcone (12), N-trans-sinapoylmethoxytyramine (13), N-[2-(4-hydroxy-3-methoxyphenyl)ethyl]-3-phenyl-2-propenamide (14), (E)-3-(4-hydroxy-3-methoxyphenyl)-N-phenethyl-acrylamide (15), N-trans-feruloyltyramine (16), N-trans-p-coumaroyltyramine (17), N-cis-feruloyltyramine (18), cis-N-feruloyl-3-O-methyldopamine (19), cannabisin D (20), 3-caffeoyl-2-methyl-D-erythronic acid-1,4-lactone (21), and (-)-syringaresinol (22). Conclusion Compounds 1, 7, 9—11, 13—15, 17, 19, and 21 were isolated from the genus Fissistigma for the first time.The anti-inflammatory activity results demonstrated that compounds 5 , 9 , 13 , and 16 significantly inhibited the release of nitric oxide in LPS-induced RAW264.7 macrophages.

Identifying chemical constituents of Danggui Buxue Decoction and its tissue distribution in mice by UHPLC-Q-Exactive Orbitrap HRMS

Chinese Traditional and Herbal Drugs. 2026, 57(13): 4987-5001.

This study aimed to characterize the chemical profile of Danggui Buxue Decoction (DBD) and investigate the systemic exposure and tissue distribution of its constituents in mice following oral administration, using UHPLC-Q-Exactive Orbitrap high-resolution mass spectrometry (HRMS). Methods A total of 12 healthy male C57BL/6J mice were randomly divided into a blank control group (n = 3), administered purified water, and a DBD-treated group (n = 9), given a DBD extract at 16 g/kg by gavage. Serum and tissue samples were collected at 0.5, 1.5, and 3 h post-dose, pooled, and processed via protein precipitation. Chromatographic separation was performed on an ACQUITY UPLC BEH C₁₈ column (100 mm × 2.1 mm, 1.7 μm) using a gradient elution with 0.1% formic acid in water and methanol as the mobile phase. Mass spectrometric data were acquired in both positive and negative ion modes via full-scan MS¹/data-dependent MS² scanning. Compound identification was achieved by analyzing relative retention times and MS¹ fragment information using Xcalibur 4.2 software, with confirmation against reference standards, literature data, and databases. Results A total of 158 chemical compounds were identified in DBD, comprising 56 flavonoids, 44 saponins, 24 phthalides, 17 organic acids, 8 coumarins, 2 alkaloids, and 7 other constituents. The number of prototype compounds detected in mice after DBD administration varied over time. The abundance of these migrating components across tissues followed the order: ileum > liver > serum > lung > kidney > spleen > heart > brain. Key constituents identified in the serum and various tissues included 7,3'-dihydroxy-5'-methoxyisoflavone (pterocarpan E), calycosin-7-O-β-D-glucoside, methylnissolin, calycosin, oroxylin A, isomucronulatol, 3-butylidenephthalide, (6αR,11αR)-3,9-dimethoxy-10-hydroxypterocarpan and formononetin. Conclusion This study delineates the comprehensive chemical composition of DBD and in vivo absorption and tissue distribution patterns using HRMS, providing crucial insights for identifying the bioactive constituents of DBD and supporting further tissue pharmacokinetic investigations.

Construction of novel self-assembled nanoparticles loaded with Rhei Radix et Rhizoma-Moutan Cortex and its anti-colorectal cancer effect

Chinese Traditional and Herbal Drugs. 2026, 57(13): 5002-5016.

Objective Novel self-assembled nanoparticles (RMN-SAN) of Dahuang (Rhei Radix et Rhizoma) and Mudanpi (Moutan Cortex) were prepared by the micro-precipitation method, and their characterization, formation mechanism and anti-colorectal cancer (CRC) efficacy were investigated. Methods The process parameters were optimized through single-factor experiments, and characterization methods such as dynamic light scattering, ζ potential and transmission electron microscopy were performed. The core active components were identified by UPLC-Q-TOF-MS, and the self-assembly mechanism of RMN-SAN was revealed by FTIR and UV spectroscopy. The in vitro CT26 cell experiments and in vivo tumor-bearing mouse models were used to verify its anti-CRC efficacy. Results The optimized preparation method for RMN-SAN involves taking 10 g each of Rhei Radix et Rhizoma and Moutan Cortex, adding 10 times their volume of water, soaking for 30 min, and refluxing for 0.5 h, followed by filtration. The residue is then refluxed with 8 times its volume of 70% ethanol for 0.5 h and filtered again. The two extracts are combined, magnetically stirred at 600 r/min and 25 ℃ for 30 min, and the alcohol is removed by rotary evaporation at 60 ℃, concentrating to a final concentration of 0.2 g/mL. The solution is subjected to gradient centrifugation (4 ℃, 6 000, 8 000, and 10 000 r/min, each for 10 min), followed by dialysis (cut-off molecular weight 3 500) for 12 h, yielding the final product. The results showed that the average particle size of the optimized RMN-SAN was (109.30 ± 4.20) nm, the PDI was 0.353 ± 0.009, and the ζ potential was (-24.5 ± 1.3) mV, presenting a uniform spherical structure. Five core components such as rhein, aloe-emodin, sennoside B, paeonol, and paeoniflorin were identified, and their self-assembly was driven by hydrogen bonds and π-π stacking interactions, which was verified by molecular docking. The in vitro experiments confirmed that RMN-SAN could inhibit the proliferation of CT26 cells in a concentration-dependent manner, induce apoptosis and block the cell cycle at the G₁ phase. In the in vivo experiments, the tumor suppression effect of the high-dose RMN-SAN group (6.0 g/kg) was significantly higher than that of the traditional decoction group, and it could regulate the levels of immune and inflammatory factors more efficiently. Conclusion This study enabled the utilization of the therapeutic advantages of traditional Chinese medicine through modern processing, providing new ideas for the optimization of the preparation of self-assembled nanoparticles of traditional Chinese medicine, and also providing an efficient and stable new formulation for the treatment of CRC with traditional Chinese medicine.