1.Pharmacological Effect and Preparation Development of Geniposide: A Review
Yongmei GUAN ; Yidan LIU ; Hua ZHANG ; Haiyan ZHANG ; Zhenzhong ZANG
Chinese Journal of Experimental Traditional Medical Formulae 2026;32(1):317-326
Geniposide, the primary active component of the traditional Chinese medicine Gardeniae Fructus, is a water-soluble iridoid glycoside. Pharmacological studies have demonstrated that geniposide exhibits various biological activities, including hepatoprotective, anti-inflammatory, analgesic, neuroprotective, antidepressant effects, and inhibitory activity against ischemia-reperfusion injury. Recent research has revealed its promising potential in preventing and treating diseases such as atherosclerosis and osteoporosis, indicating broad application prospects. Numerous in vitro and in vivo studies indicate that the pharmacodynamic mechanisms of geniposide are primarily associated with the inhibition of inflammatory responses and oxidative stress, improvement of lipid metabolism, and regulation of apoptosis. However, due to its high water solubility and rapid metabolism in vivo, geniposide suffers from low oral bioavailability, which limits its therapeutic efficacy and clinical application. In recent years, various formulations, such as creams, cubic liquid crystals, hydrogels, and liposomes, have been developed to address its bioavailability issues. This article reviewed the latest research progress on the pharmacological activities and formulation development of geniposide by analyzing domestic and international literature from the past decade, aiming to provide a theoretical basis for further research, development, and utilization of geniposide and its formulations.
2.Preparation of Triptolide-Chuanxiong Rhizoma Extract Ethanol Transfersomes and Analysis on Its in Vitro Anti-inflammatory Mechanism
Ling TAO ; Zhiyan WAN ; Yidan LIU ; Zhe LI ; Zhenzhong ZANG ; Weifeng ZHU ; Yongmei GUAN
Chinese Journal of Experimental Traditional Medical Formulae 2026;32(10):210-218
ObjectiveTo prepare triptolide-Chuanxiong Rhizoma extract ethanol transfersomes(TP-CX@TESs), conduct its quality evaluation, and investigate its in vitro anti-inflammatory efficacy and the underlying mechanisms. MethodsTP-CX@TESs was prepared via the ultrasonic injection method. With encapsulation efficiency and particle size as evaluation indicators, Box-Behnken design-response surface methodology(BBD-RSM) was employed to optimize the formulation process. The TP-CX@TESs prepared under the optimal process was characterized and evaluated for in vitro transdermal performance. A lipopolysaccharide(LPS)-induced RAW264.7 cell inflammation model was established. After 24 h of drug intervention, the levels of inflammatory factors such as nitric oxide(NO), interleukin-6(IL-6), and tumor necrosis factor-α(TNF-α) in the cell supernatant were detected. Western blot was used to determine the protein expression levels of Janus kinase 2(JAK2), signal transducer and activator of transcription 3(STAT3), and α7 nicotinic acetylcholine receptor(α7nAChR), and real-time fluorescence quantitative polymerase chain reaction(Real-time PCR) was applied to measure the mRNA expression levels of JAK2, STAT3, the encoding gene of α7nAChR(CHRNA7), and nuclear transcription factor-κB(NF-κB). ResultsResults of BBD-RSM showed that the optimal formulation for preparing TP-CX@TESs was as follows:egg yolk lecithin content of 2.3%, ethanol volume fraction of 30%, and ratio of polysorbate-80 to egg yolk lecithin of 2∶5. Microscopic characterization revealed that TP-CX@TESs exhibited a spherical-like structure with a particle size of (105.60±3.85) nm, a polydispersity index of 0.19±0.03, and a Zeta potential of (-15.89±0.98) mV. The encapsulation efficiencies of triptolide, ferulic acid, and ligustilide were (76.88±4.40)%, (78.84±4.40)%, and (65.88±0.06)%, respectively. Both in vitro release and transdermal penetration of triptolide, ferulic acid, and ligustilide in TP-CX@TESs all followed the first-order kinetic model, showing a certain sustained-release property. Experimental results in RAW264.7 cells indicated that TP-CX@TESs significantly inhibited the release of NO, TNF-α, and IL-6(P<0.01), remarkably upregulated the protein expression levels of STAT3 and α7nAChR(P<0.01), increased the mRNA expression level of CHRNA7, and significantly downregulated the mRNA expression level of NF-κB(P<0.05, P<0.01). ConclusionThe optimized formulation process of TP-CX@TESs is simple and feasible, along with favorable in vitro release property, good transdermal permeability, and excellent in vitro anti-inflammatory activity, the mechanism is related to the inhibition of NF-κB.
3.Preparation of Triptolide-Chuanxiong Rhizoma Extract Ethanol Transfersomes and Analysis on Its in Vitro Anti-inflammatory Mechanism
Ling TAO ; Zhiyan WAN ; Yidan LIU ; Zhe LI ; Zhenzhong ZANG ; Weifeng ZHU ; Yongmei GUAN
Chinese Journal of Experimental Traditional Medical Formulae 2026;32(10):210-218
ObjectiveTo prepare triptolide-Chuanxiong Rhizoma extract ethanol transfersomes(TP-CX@TESs), conduct its quality evaluation, and investigate its in vitro anti-inflammatory efficacy and the underlying mechanisms. MethodsTP-CX@TESs was prepared via the ultrasonic injection method. With encapsulation efficiency and particle size as evaluation indicators, Box-Behnken design-response surface methodology(BBD-RSM) was employed to optimize the formulation process. The TP-CX@TESs prepared under the optimal process was characterized and evaluated for in vitro transdermal performance. A lipopolysaccharide(LPS)-induced RAW264.7 cell inflammation model was established. After 24 h of drug intervention, the levels of inflammatory factors such as nitric oxide(NO), interleukin-6(IL-6), and tumor necrosis factor-α(TNF-α) in the cell supernatant were detected. Western blot was used to determine the protein expression levels of Janus kinase 2(JAK2), signal transducer and activator of transcription 3(STAT3), and α7 nicotinic acetylcholine receptor(α7nAChR), and real-time fluorescence quantitative polymerase chain reaction(Real-time PCR) was applied to measure the mRNA expression levels of JAK2, STAT3, the encoding gene of α7nAChR(CHRNA7), and nuclear transcription factor-κB(NF-κB). ResultsResults of BBD-RSM showed that the optimal formulation for preparing TP-CX@TESs was as follows:egg yolk lecithin content of 2.3%, ethanol volume fraction of 30%, and ratio of polysorbate-80 to egg yolk lecithin of 2∶5. Microscopic characterization revealed that TP-CX@TESs exhibited a spherical-like structure with a particle size of (105.60±3.85) nm, a polydispersity index of 0.19±0.03, and a Zeta potential of (-15.89±0.98) mV. The encapsulation efficiencies of triptolide, ferulic acid, and ligustilide were (76.88±4.40)%, (78.84±4.40)%, and (65.88±0.06)%, respectively. Both in vitro release and transdermal penetration of triptolide, ferulic acid, and ligustilide in TP-CX@TESs all followed the first-order kinetic model, showing a certain sustained-release property. Experimental results in RAW264.7 cells indicated that TP-CX@TESs significantly inhibited the release of NO, TNF-α, and IL-6(P<0.01), remarkably upregulated the protein expression levels of STAT3 and α7nAChR(P<0.01), increased the mRNA expression level of CHRNA7, and significantly downregulated the mRNA expression level of NF-κB(P<0.05, P<0.01). ConclusionThe optimized formulation process of TP-CX@TESs is simple and feasible, along with favorable in vitro release property, good transdermal permeability, and excellent in vitro anti-inflammatory activity, the mechanism is related to the inhibition of NF-κB.
4.Combination of Components from Tripterygii Radix et Rhizoma-Chuanxiong Rhizoma Affects RA-FLSs by Regulating NF-κB, Nrf2/HO-1 Signaling Pathways and Bcl-2/Caspase-3 Expression
Yongmei GUAN ; Zhiyan WAN ; Shuhui WANG ; Weifeng ZHU ; Zhiyong LIU ; Cheng JIANG ; Zhenzhong ZANG
Chinese Journal of Experimental Traditional Medical Formulae 2025;31(2):17-26
ObjectiveTo investigate the effects of the combination of components from Tripterygii Radix et Rhizoma and Chuanxiong Rhizoma on rheumatoid arthritis fibroblast-like synoviocytes (RA-FLSs) and the underlying mechanism. MethodsRA-FLSs were grouped as follows: blank control, positive control (methotrexate), Tripterygii Radix et Rhizoma components, Chuanxiong Rhizoma components, and components from Tripterygii Radix et Rhizoma+Chuanxiong Rhizoma. The cell-counting kit-8 (CCK-8) assay was employed to the cell proliferation, invasion, and apoptosis. The levels of tumor necrosis factor (TNF)-α, interleukin (IL)-6, reactive oxygen species (ROS), and malondiadehyde (MDA) in cells were measured. Western blot was employed to determine the protein levels of nuclear factor erythroid 2-related factor 2 (Nrf2), heme oxygenase-1 (HO-1), nuclear factor-kappa B (NF-κB) p65, phosphorylated inhibitory subunit of NF-κBα (p-IκBα), cysteinyl aspartate-specific protease-3 (Caspase-3), and B-cell lymphoma 2 (Bcl-2). Real-time PCR was employed to determine the mRNA levels of Nrf2, HO-1, and NF-κB p65. ResultsThe cells in the groups of positive control, Tripterygii Radix et Rhizoma components, Chuanxiong Rhizoma components, and components from Tripterygii Radix et Rhizoma+Chuanxiong Rhizoma were treated with 2.50 mg·L-1 methotrexate, 0.20 mg·L-1 triptolide + 0.20 mg·L-1 celastrol, 5.00 mg·L-1 ferulic acid + 20.00 mg·L-1 ligustrazine, 0.20 mg·L-1 triptolide + 0.20 mg·L-1 celastrol + 5.00 mg·L-1 ferulic acid + 20.00 mg·L-1 ligustrazine, respectively. Compared with the blank control group, drug administration reduced the proliferation and invasion and increased the apoptosis of cells (P<0.01), lowered the levels of TNF-α, IL-6, ROS, and MDA (P<0.01), up-regulated the mRNA and protein levels of Caspase-3, Nrf2, and HO-1 (P<0.01), and down-regulated the mRNA and protein levels of Bcl-2, NF-κB p65, and p-IκBα (P<0.01). Compared with the Tripterygii Radix et Rhizoma components group, the combination of components from Tripterygii Radix et Rhizoma+Chuanxiong Rhizoma inhibited the proliferation and invasion (P<0.05) and promoted the apoptosis of RA-FLSs, up-regulated the mRNA levels of Nrf2 and HO-1 and protein levels of Nrf2 and Caspase-3 (P<0.05), and down-regulated the protein levels of NF-κB p65 and p-IκBα (P<0.05). ConclusionThe combination of components from Chuanxiong Rhizoma and Tripterygii Radix et Rhizoma can inhibit the proliferation and invasion and promote the apoptosis of RA-FLSs and alleviate oxidative stress and inflammation by inhibiting the NF-κB signaling pathway, activating the Nrf2/HO-1 pathway, and regulating the expression of Bcl-2/Caspase-3.
5.Expert consensus on the prevention and treatment of radiochemotherapy-induced oral mucositis.
Juan XIA ; Xiaoan TAO ; Qinchao HU ; Wei LUO ; Xiuzhen TONG ; Gang ZHOU ; Hongmei ZHOU ; Hong HUA ; Guoyao TANG ; Tong WU ; Qianming CHEN ; Yuan FAN ; Xiaobing GUAN ; Hongwei LIU ; Chaosu HU ; Yongmei ZHOU ; Xuemin SHEN ; Lan WU ; Xin ZENG ; Qing LIU ; Renchuan TAO ; Yuan HE ; Yang CAI ; Wenmei WANG ; Ying ZHANG ; Yingfang WU ; Minhai NIE ; Xin JIN ; Xiufeng WEI ; Yongzhan NIE ; Changqing YUAN ; Bin CHENG
International Journal of Oral Science 2025;17(1):54-54
Radiochemotherapy-induced oral mucositis (OM) is a common oral complication in patients with tumors following head and neck radiotherapy or chemotherapy. Erosion and ulcers are the main features of OM that seriously affect the quality of life of patients and even the progress of tumor treatment. To date, differences in clinical prevention and treatment plans for OM have been noted among doctors of various specialties, which has increased the uncertainty of treatment effects. On the basis of current research evidence, this expert consensus outlines risk factors, clinical manifestations, clinical grading, ancillary examinations, diagnostic basis, prevention and treatment strategies and efficacy indicators for OM. In addition to strategies such as basic oral care, anti-inflammatory and analgesic agents, anti-infective agents, pro-healing agents, and photobiotherapy recommended in previous guidelines, we also emphasize the role of traditional Chinese medicine in OM prevention and treatment. This expert consensus aims to provide references and guidance for dental physicians and oncologists in formulating strategies for OM prevention, diagnosis, and treatment, standardizing clinical practice, reducing OM occurrence, promoting healing, and improving the quality of life of patients.
Humans
;
Chemoradiotherapy/adverse effects*
;
Consensus
;
Risk Factors
;
Stomatitis/etiology*
6.Study on extraction technology of Sophora flavescens-Phellodendron chinense drug pair
Yongmei GUAN ; Ying TAO ; Chengyu ZOU ; Zhenzhong ZANG ; Lihua CHEN ; Lili LIU ; Limei CHEN ; Weifeng ZHU
China Pharmacy 2024;35(7):793-800
OBJECTIVE To study the extraction technology of Sophora flavescens-Phellodendron chinense drug pair and provide a reference for the development of new drugs for the treatment of anorectal diseases. METHODS Using the contents of total alkaloids of S. flavescens (matrine+oxymatrine), berberine hydrochloride and total flavonoid, and extract yield as evaluation indicators, analytic hierarchy process-entropy weight method was used to calculate the weight coefficient of each indicator, and was combined with Box-Behnken design-response surface method to study the extraction technology of S. flavescens-P. chinense drug pair and verify it. RESULTS The optimal extraction technology of S. flavescens-P. chinense drug pair was immersed in 12-fold amount of 58% ethanol for 30 minutes and extracted twice, each time for 120 minutes. The relative error between the verification experimental results and the predicted value was 1.88%. CONCLUSIONS The obtained extraction technology is stable and feasible and can provide reference for the application of S. flavescens-P. chinense drug pair and development of new drugs.
7.Key Components of Fishy Smell of Eupolyphaga Steleophaga by Head Space-Solid Phase Microextraction-GC-MS and Odor Activity Value
Hongyan MA ; Hong FAN ; Qian LIU ; Xue LI ; Hui YE ; Dingkun ZHANG ; Yongmei GUAN ; Ming YANG ; Houlin XIA
Chinese Journal of Modern Applied Pharmacy 2024;41(1):88-96
To determine the main components of the fishy smell of the Eupolyphaga Steleophaga, and to provide a theoretical basis for deodorizing the Eupolyphaga Steleophaga.
METHODS
Head space-solid phase microextraction-gas chromatography-mass spectrometry was used to identify the components of 10 batches of Eupolyphaga Steleophaga, and area normalization method and chemometrics method were used to analyze the smelly gas of different batches. Odor activity value(OAV) was used to evaluate the contribution of odor components and identify key odor components.
RESULTS
A total of 87 volatile odor components were identified, the key fishy smell compounds(OAV≥1) were m-methylphenol, dimethyltrisulfide, 4-methylphenol, 2-methyliso-borneol, 2-etzol, 4-methylvaleric acid, iso-valeric acid, etc. Modified fishy gas composition(0.1
8.Effect of volatile oil of Ligusticum chuanxiong on transdermal properties and cytotoxicity of triptolide in vitro
Cheng JIANG ; Zhenzhong ZANG ; Lihua CHEN ; Haiting ZHU ; Shihua FU ; Weifeng ZHU ; Wenting WU ; Wei SHI ; Yongmei GUAN
China Pharmacy 2024;35(4):413-418
OBJECTIVE To explore the effect of volatile oil of Ligusticum chuanxiong on the transdermal properties and cytotoxicity of triptolide in vitro. METHODS The chemical constituents of the volatile oil of L. chuanxiong were analyzed by gas chromatography-mass spectrometry. The lower abdominal skin of KM mice was separated and divided into triptolide group, triptolide in compatibility with volatile oil of L. chuanxiong groups at 1∶10, 1∶50, 1∶100 (hereinafter referred to as “compatibility 1∶10”“compatibility 1∶50”“compatibility 1∶100” groups). After the skin of mice in each group was fully exposed to 0.2 g of the corresponding cream for 24 h, the cumulative transdermal dose (Qn) of triptolide in the receiving solution of each group was determined by high-performance liquid chromatography, and the transdermal absorption rate (Jss) was calculated. Human immortalized keratinocytes (HaCat) were used as a model, the CCK-8 method was used to detect the cell survival rate of different concentrations of the volatile oil of L. chuanxiong and triptolide before and after compatibility. RESULTS A total of 62 chemical constituents of the volatile oil of L. chuanxiong were identified, including Z-ligustilide, senkyunolide, and β-selinene. The Qn (P< 0.01) and Jss of triptolide increased within 24 h in the compatibility 1∶10 and 1∶50 groups, while the Qn (P<0.05) and Jss decreased in the compatibility 1∶100 group as compared with the triptolide group. Compared with the triptolide group, the cell survival rate of HaCat was significantly increased in the compatibility 1∶10 and 1∶50 groups when the triptolide concentrations were 36, 72 and 144 ng/mL (P<0.05 or P<0.01); while the cell survival rate of HaCat was decreased in the compatibility 1∶100 group, but the difference was not statistically significant (P>0.05). CONCLUSIONS When the compatibility ratio of triptolide and volatile oil of L. chuanxiong was 1∶10 or 1∶50, it can promote the transdermal absorption of triptolide and reduce the cytotoxicity of triptolide to HaCat.
9.Analysis of Chemical Constituents in Puerariae Lobatae Radix Dispensing Granules by UPLC-Q-TOF-MS/MS
Meiqing CHEN ; Weifeng ZHU ; Yongmei GUAN ; Yulin FENG ; Yanli ZHANG ; Xiucun JING ; Wanqian PENG ; Hui OUYANG ; Qiong LI
Chinese Journal of Experimental Traditional Medical Formulae 2023;29(19):176-186
ObjectiveA rapid method for identification of chemical constituents in Puerariae Lobatae Radix dispensing granules was established in order to clarify the material basis. MethodThe chemical constituents of Puerariae Lobatae Radix dispensing granules was qualitatively analyzed by ultra-performance liquid chromatography-quadrupole-time-of-flight mass spectrometry(UPLC-Q-TOF-MS/MS) under positive and negative ion modes, and the chromatographic conditions were on an ACQUITY UPLC HSS T3 column(2.1 mm×100 mm, 1.8 μm) with 0.1% formic acid aqueous solution(A)-0.1% formic acid acetonitrile solution(B) as mobile phase for gradient elution(0-4 min, 5%-10%B; 4-10 min, 10%-15%B; 10-20 min, 15%-16%B; 20-27 min, 16%-31%B; 27-33 min, 31%-59%B; 33-42 min, 59%-95%B; 42-42.1 min, 95%-5%B; 42.1-45 min, 5%B), the flow rate was 0.35 mL·min-1, the column temperature was 40 ℃, the injection volume was 5 μL, and electrospray ionization(ESI) was selected. Then these chemical constituents were comprehensively identified based on PeakView 1.2, PubChem, ChemicalBook, ChemSpider, comparative control profiles and literature information. ResultA total of 128 chemical constituents were identified from the dispensing granules, including 60 flavonoids, 26 organic acids, 7 glycosides, 6 coumarins, 3 nucleosides and 26 other compounds. By focusing on the cleavage patterns of flavonoids, organic acids, glycosides, coumarins, nucleosides and other compounds, 12 compounds that have not been reported in Puerariae Lobatae Radix species were identified from the dispensing granules. ConclusionThe established method can systematically and rapidly identify the chemical constituents in Puerariae Lobatae Radix dispensing granules, and cleared it composition is mainly flavonoids and organic acids. Laying a foundation for the study of the material basis, mechanism of action and clinical application of the dispensing granules.
10.Progress of drug therapy for children with ulcerative colitis
Dexiu GUAN ; Yongmei ZHANG ; Jie WU
International Journal of Pediatrics 2023;50(9):584-589
Ulcerative colitis (UC) is a chronic, nonspecific inflammatory disease that affects the intestines.Drug therapy includes 5-aminosalicylic acid (5-ASA) drugs, glucocorticoids, immunomodulators, and biological agents, which can effectively induce and maintain remission and prevent complications.5-ASA is the first-line drug for inducing and maintaining remission in children with mild to moderate UC.Glucocorticoids are the first-line therapy for moderate to severe UC and the second-line remission inducing therapy for patients with mild to moderate UC who do not respond to 5-ASA.Immunomodulators(purine preparations)are suitable for maintenance remission therapy after steroid dependence, 5-ASA intolerance, frequent recurrence, and acute severe UC response to hormone-induced therapy.Calcineurin inhibitors and the biological agent infliximab can be used as second-line treatment for patients with acute severe UC who do not respond to glucocorticoids therapy.Vedolizumab and ustekinumab can be used as second-line biotherapy after failure of anti-tumor necrosis factor-α, but data are lacking in studies of pediatric UC.The purpose of this article is to review the progress of drug therapy for children with UC, and provide reference for clinical practice.


Result Analysis
Print
Save
E-mail