1.Study on secondary metabolites of Penicillium expansum GY618 and their tyrosinase inhibitory activities
Fei-yu YIN ; Sheng LIANG ; Qian-heng ZHU ; Feng-hua YUAN ; Hao HUANG ; Hui-ling WEN
Acta Pharmaceutica Sinica 2025;60(2):427-433
Twelve compounds were isolated from the rice fermentation extracts of
2.Molecular mechanism of verbascoside in promoting acetylcholine release of neurotransmitter.
Zhi-Hua ZHOU ; Hai-Yan XING ; Yan LIANG ; Jie GAO ; Yang LIU ; Ting ZHANG ; Li ZHU ; Jia-Long QIAN ; Chuan ZHOU ; Gang LI
China Journal of Chinese Materia Medica 2025;50(2):335-348
The molecular mechanism of verbascoside(OC1) in promoting acetylcholine(ACh) release in the pathogenesis of Alzheimer's disease(AD) was studied. Adrenal pheochromocytoma cells(PC12) of rats induced by β-amyloid protein(1-42)(Aβ_(1-42)) were used as AD models in vitro and were divided into control group, model group(Aβ_(1-42) 10 μmol·L~(-1)), OC1 treatment group(2 and 10 μg·mL~(-1)). The effect of OC1 on phosphorylated proteins in AD models was analyzed by whole protein phosphorylation quantitative omics, and the selectivity of OC1 for calcium channel subtypes was virtually screened in combination with computer-aided drug design. The fluorescence probe Fluo-3/AM was used to detect Ca~(2+) concentration in cells. Western blot analysis was performed to detect the effects of OC1 on the expression of phosphorylated calmodulin-dependent protein kinase Ⅱ(p-CaMKⅡ, Thr286) and synaptic vesicle-related proteins, and UPLC/Q Exactive MS was used to detect the effects of OC1 on ACh release in AD models. The effects of OC1 on acetylcholine esterase(AChE) activity in AD models were detected. The results showed that the differentially modified proteins in the model group and the OC1 treatment group were related to calcium channel activation at three levels: GO classification, KEGG pathway, and protein domain. The results of molecular docking revealed the dominant role of L-type calcium channels. Fluo-3/AM fluorescence intensity decreased under the presence of Ca~(2+) chelating agent ethylene glycol tetraacetic acid(EGTA), L-type calcium channel blocker verapamil, and N-type calcium channel blocker conotoxin, and the effect of verapamil was stronger than that of conotoxin. This confirmed that OC1 promoted extracellular Ca~(2+) influx mainly through its interaction with L-type calcium channel protein. In addition, proteomic analysis and Western blot results showed that the expression of p-CaMKⅡ and downstream vesicle-related proteins was up-regulated after OC1 treatment, indicating that OC1 acted on vesicle-related proteins by activating CaMKⅡ and participated in synaptic remodeling and transmitter release, thus affecting learning and memory. OC1 also decreased the activity of AChE and prolonged the action time of ACh in synaptic gaps.
Animals
;
Rats
;
Glucosides/administration & dosage*
;
Acetylcholine/metabolism*
;
Alzheimer Disease/genetics*
;
PC12 Cells
;
Phenols/chemistry*
;
Neurotransmitter Agents/metabolism*
;
Drugs, Chinese Herbal
;
Calcium-Calmodulin-Dependent Protein Kinase Type 2/genetics*
;
Humans
;
Phosphorylation/drug effects*
;
Calcium/metabolism*
;
Polyphenols
3."Component-effect" correlations in traditional Chinese medicine from holistic view: taking discovery of gintonin from ginseng as an example.
Xin-Ming YU ; Chen-Yu YU ; Hua-Ying WANG ; Wei-Sheng YUE ; Zhu-Bin ZHANG ; Wei WU ; Xiao-Bin JIA ; Bing YANG ; Liang FENG
China Journal of Chinese Materia Medica 2025;50(7):2001-2012
The holistic view is the key in the study of traditional Chinese medicine(TCM). The component structure theory is based on the holistic view to investigate the correlation between material basis and efficiency, which enriches the holistic "component-effect" research of TCM. Gintonin is a newly isolated non-saponin component of ginseng. Compared to ginsenosides, gintonin has many different pharmacological activities, and it provides new knowledge for the holistic research of ginseng. Thus, taking the discovery of gintonin from ginseng as an example, this paper explored the linkage between ginsenosides and gintonin from the perspective of "component-effect" correlations and systematically sorted out the similarities and differences between them in terms of structural characteristics, modes of action, and pharmacological activities. Starting from the collaborative interaction of TCM compounds, the study discussed the application and value of the holistic view in TCM "component-effect" research in the light of the component structure theory to provide new thoughts for the development of modern TCM research.
Panax/chemistry*
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Drugs, Chinese Herbal/pharmacology*
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Medicine, Chinese Traditional
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Humans
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Ginsenosides/pharmacology*
;
Animals
4.Exploration of evaluation criteria based on the biological variation in the external quality assessment for basic semen analysis in China.
Xi-Yan WU ; Jin-Chun LU ; Xin-Hua PENG ; Jing-Liang HE ; Dao WANG ; Cong-Ling DAI ; Wen-Bing ZHU ; Gang LIU ; Wei-Na LI
Asian Journal of Andrology 2025;27(5):621-626
This study explores whether the current external quality assessment (EQA) level and acceptable bias for basic semen analysis in China are clinically useful. We collected data of semen EQA from Andrology laboratories in the Hunan Province (China) in 2022 and searched for data in the published literature from January 2000 to December 2023 in China. On the basis of these data, we analyzed the coefficients of variation and acceptable biases of different quality control materials for basic semen analysis through robust statistics. We compared these findings with quality specifications based on biological variation from optimal, desirable, and minimum levels of bias to seek a unified and more suitable semen EQA bias evaluation standard for China's national conditions. Different sources of semen quality control material exhibited considerable variation in acceptable biases among laboratories, ranging from 8.2% to 56.9%. A total of 50.0% of the laboratories met the minimum quality specifications for progressive motility (PR), whereas 100.0% and 75.0% of laboratories met only the minimum quality specifications for sperm concentration and total motility (nonprogressive [NP] + PR), respectively. The Z value for sperm concentration and PR+NP was equivalent to the desirable performance specification, whereas the Z value for PR was equivalent only to the minimum performance specification. This study highlights the feasibility of operating external quality assessment schemes for basic semen analysis using quality specifications based on biological variation. These specifications should be unified among external quality control (EQC) centers based on biological variation.
Semen Analysis/standards*
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Humans
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China
;
Male
;
Quality Control
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Sperm Motility
;
Sperm Count/standards*
5.Three-dimensional (3D) printing-assisted freeze-casting of processed pyritum-doped β-tricalcium phosphate biomimetic scaffold with angiogenesis and bone regeneration capability.
Chenxu WEI ; Zongan LI ; Xiaoyun LIANG ; Yuwei ZHAO ; Xingyu ZHU ; Haibing HUA ; Guobao CHEN ; Kunming QIN ; Zhipeng CHEN ; Changcan SHI ; Feng ZHANG ; Weidong LI
Journal of Zhejiang University. Science. B 2025;26(9):863-880
Bone repair remains an important target in tissue engineering, making the development of bioactive scaffolds for effective bone defect repair a critical objective. In this study, β-tricalcium phosphate (β-TCP) scaffolds incorporated with processed pyritum decoction (PPD) were fabricated using three-dimensional (3D) printing-assisted freeze-casting. The produced composite scaffolds were evaluated for their mechanical strength, physicochemical properties, biocompatibility, in vitro pro-angiogenic activity, and in vivo efficacy in repairing rabbit femoral defects. They not only demonstrated excellent physicochemical properties, enhanced mechanical strength, and good biosafety but also significantly promoted the proliferation, migration, and aggregation of pro-angiogenic human umbilical vein endothelial cells (HUVECs). In vivo studies revealed that all scaffold groups facilitated osteogenesis at the bone defect site, with the β-TCP scaffolds loaded with PPD markedly enhancing the expression of neurogenic locus Notch homolog protein 1 (Notch1), vascular endothelial growth factor (VEGF), bone morphogenetic protein-2 (BMP-2), and osteopontin (OPN). Overall, the scaffolds developed in this study exhibited strong angiogenic and osteogenic capabilities both in vitro and in vivo. The incorporation of PPD notably promoted the angiogenic-osteogenic coupling, thereby accelerating bone repair, which suggests that PPD is a promising material for bone repair and that the PPD/β-TCP scaffolds hold great potential as a bone graft alternative.
Calcium Phosphates/chemistry*
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Animals
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Bone Regeneration
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Rabbits
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Tissue Scaffolds
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Printing, Three-Dimensional
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Humans
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Human Umbilical Vein Endothelial Cells
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Neovascularization, Physiologic
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Osteogenesis
;
Tissue Engineering/methods*
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Biomimetic Materials
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Cell Proliferation
;
Angiogenesis
6.Role of problem chain and course ideological and political cases teaching method in enhancing clinical medication ability research
Zhi-Hua QIN ; Long-Xi PENG ; Gao-Shuang LAN ; Xiao-Bin ZHANG ; Jiao-Jiao YANG ; Liang ZHU ; Xi-Long QIU ; Yun-Long CHEN
The Chinese Journal of Clinical Pharmacology 2024;40(11):1650-1653
Nowadays,with the continuous deepening and development of vocational education teaching reform,medical higher vocational education always takes moral education as the fundamental task.As an independent type of education,vocational education should always deepen the integration of industry and education and the integration of science and education.Through the teaching research of"problem chain+course ideological and political case",this study innovates the coordinated education team of drug nursing curriculum,the collaborative education method and the collaborative education evaluation,and improves the teaching effect.
7.Establishment and evaluation methods of a novel animal model of liver depression transforming into fire syndrome-related depression
Dan SU ; Jian LI ; Gen-hua ZHU ; Ming YANG ; Liang-liang LIAO ; Zhi-fu AI ; Hui-zhen LI ; Ya-li LIU ; Yong-gui SONG
Acta Pharmaceutica Sinica 2024;59(6):1680-1690
Through a compound induction method, combined with neurobehavioral, macroscopic characterization and objective pathological evaluation indicators, a murine depression model of liver depression transforming into fire syndrome was constructed and confirmed. The model was constructed using a combination of sleep deprivation, light exposure, and alternate-day food deprivation. Evaluation was conducted at three levels: face validity, constructs validity, and predictive validity. The establishment of the liver depression transforming into fire syndrome depression model was further validated through the counterproof of traditional Chinese medicine formulas. In terms of face validity, compared to the control group, mice in the model group exhibited typical depressive symptoms in neurobehavioral assessments; the general observation of the model group mice reveals disheveled and lackluster fur, along with delayed and easily agitated responses. Additionally, there is a substantial increase in water consumption. In the sleep phase detection of mouse, the model group showed a significant increase in the proportion of time spent in the wake phase during sleep, accompanied by a significant decrease in the proportions of time spent in both non-rapid eye movement (NREM) and rapid eye movement (REM) sleep phases. There are significant differences in physiological indicators such as average blood flow velocity, blood flow rate, tongue, urine, and claw color (r values) in the internal carotid artery. Structural validity demonstrated that levels of 5-hydroxytryptamine (5-HT), dopamine (DA), and
8.Effects of template and pore-forming agent method on the structure and drug delivery of porous maltodextrin
Zhe LI ; Xiao-sui LUO ; Wei-feng ZHU ; Qiong LI ; Yong-mei GUAN ; Zheng-ji JIN ; Li-hua CHEN ; Liang-shan MING
Acta Pharmaceutica Sinica 2024;59(8):2381-2395
This study using maltodextrin as raw material, 1%-5% polyvinylpyrrolidone K30 as template agent, 1%-5% ammonium bicarbonate as pore-forming agent, curcumin and ibuprofen as model drugs. Porous maltodextrin was prepared by template and pore-forming agent methods, respectively. The structure and drug delivery behavior of porous maltodextrin prepared by different technologies were comprehensively characterized. The results showed that the porous maltodextrin prepared by pore-forming agent method had larger specific surface area (6.449 4 m2·g-1) and pore size (32.804 2 nm), which was significantly better than that by template agent method (3.670 2 m2·g-1, 15.278 5 nm). The adsorption kinetics between porous maltodextrin prepared by pore-forming agent method and curcumin were suitable for quasi-first order adsorption kinetic model, and that between porous maltodextrin and ibuprofen were suitable for quasi-second order adsorption kinetic model. While the adsorption kinetics between porous maltodextrin prepared by template agent method and two model drugs were both suitable for the quasi-first order adsorption kinetic model. In addition, the dissolution behavior analysis showed that the porous maltodextrin prepared by the two technologies can significantly improve the dissolution behavior of insoluble drugs, and the drug release was both carried out by diffusion mechanism, which suitable for the Peppas kinetic release model, but the porous maltodextrin prepared by template agent method had a faster release rate. The change of nozzle diameter had no significant effect on the adsorption process and drug release behavior of porous maltodextrin. In conclusion, the porous maltodextrins prepared by two different technologies were both beneficial to the delivery of insoluble drugs, and the template agent method was the best for delivery of insoluble drugs. This study can provide theoretical basis for the preparation of porous particles, promote the application of porous particles in insoluble drugs, and improve the bioavailability of insoluble drugs.
9.Analysis of phenotype formation mechanism of a new variety of Lonicera japonica Flos "Huajin 6" at long bud stage
Run-zhu LI ; Cong-lian LIANG ; Zhen-hua LIU ; Jia LI ; Yong-qing ZHANG ; Hai-yan LIU ; Gao-bin PU
Acta Pharmaceutica Sinica 2024;59(2):476-481
Based on the long bud stage phenotype of a new
10.Two new dalbergiphenols from Zhuang medicine Dalbergia rimosa Roxb
Cheng-sheng LU ; Wei-yu WANG ; Min ZHU ; Si-si QIN ; Zhao-hui LI ; Chen-yan LIANG ; Xu FENG ; Jian-hua WEI
Acta Pharmaceutica Sinica 2024;59(2):418-423
Twelve compounds were isolated from the ethyl acetate fraction of the 80% aqueous ethanol extract of the roots and stems of

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