1.Design, synthesis and anti-Alzheimer's disease activity evaluation of cinnamyl triazole compounds
Wen-ju LEI ; Zhong-di CAI ; Lin-jie TAN ; Mi-min LIU ; Li ZENG ; Ting SUN ; Hong YI ; Rui LIU ; Zhuo-rong LI
Acta Pharmaceutica Sinica 2025;60(1):150-163
19 cinnamamide/ester-triazole compounds were designed, synthesized and evaluated for their anti-Alzheimer's disease (AD) activity. Among them, compound
2.The effect of rutaecarpine on improving fatty liver and osteoporosis in MAFLD mice
Yu-hao ZHANG ; Yi-ning LI ; Xin-hai JIANG ; Wei-zhi WANG ; Shun-wang LI ; Ren SHENG ; Li-juan LEI ; Yu-yan ZHANG ; Jing-rui WANG ; Xin-wei WEI ; Yan-ni XU ; Yan LIN ; Lin TANG ; Shu-yi SI
Acta Pharmaceutica Sinica 2025;60(1):141-149
Metabolic-associated fatty liver disease (MAFLD) and osteoporosis (OP) are two very common metabolic diseases. A growing body of experimental evidence supports a pathophysiological link between MAFLD and OP. MAFLD is often associated with the development of OP. Rutaecarpine (RUT) is one of the main active components of Chinese medicine Euodiae Fructus. Our previous studies have demonstrated that RUT has lipid-lowering, anti-inflammatory and anti-atherosclerotic effects, and can improve the OP of rats. However, whether RUT can improve both fatty liver and OP symptoms of MAFLD mice at the same time remains to be investigated. In this study, we used C57BL/6 mice fed a high-fat diet (HFD) for 4 months to construct a MAFLD model, and gave the mice a low dose (5 mg·kg-1) and a high dose (15 mg·kg-1) of RUT by gavage for 4 weeks. The effects of RUT on liver steatosis and bone metabolism were then evaluated at the end of the experiment [this experiment was approved by the Experimental Animal Ethics Committee of Institute of Medicinal Biotechnology, Chinese Academy of Medical Sciences (approval number: IMB-20190124D303)]. The results showed that RUT treatment significantly reduced hepatic steatosis and lipid accumulation, and significantly reduced bone loss and promoted bone formation. In summary, this study shows that RUT has an effect of improving fatty liver and OP in MAFLD mice.
3.Malaria elimination strategy and joint prevention and control of malaria across China-Myanmar border areas: an overview
Chun WEI ; Zurui LIN ; Zhonghua YANG ; Hongning ZHOU ; Xingwu ZHOU ; Rui YANG
Chinese Journal of Schistosomiasis Control 2025;37(1):19-23
Yunnan Province borders with Myanmar, Vietnam, and Laos, the China-Myanmar border area is the key area for prevention of re-establishment from imported malaria after the disease was eliminated in China. Since the malaria elimination action plan was launched in Yunnan Province in 2011, 129 counties (cities, districts) were classified into three categories according to malaria incidence and transmission risk, and different technical strategies and measures were implemented with adaptations to local circumstances. A total of 68 malaria consultation service stations were established on the Chinese side of the China-Myanmar border and 80 malaria prevention and control stations were established on the Myanmar side by Yunnan Province in 2014. Then, the “Three Lines of Defense” strategy was implemented for malaria elimination in the China-Myanmar border area in Yunnan Province during the period from 2015 to 2018, and this strategy was further refined and adjusted to the “3 + 1” strategy for prevention of re-establishment from imported malaria in 2019. Through decades of multifaceted efforts, the malaria elimination goal was achieved in Yunnan Province in June 2021. However, the number of imported malaria cases appeared a tendency towards a rise in Yunnan Province in 2023 and 2024, due to changes in the situation in Myanmar and the gradual resumption of international travel and border crossings following the adjustment of the COVID-19 prevention and control policy in China. The joint malaria prevention and control cooperation between China and Myanmar was initiated with the pilot project for joint malaria prevention and control in the China-Myanmar border area in 2005, and this project was progressed into the joint malaria and dengue fever prevention and control project in parts of the Greater Mekong Subregion border areas in 2010. The threat of overseas malaria epidemics to border areas in Yunnan Province was effectively reduced through implementation of coordination meetings with Myanmar health departments, establishment of efficient information exchange mechanisms, establishment of overseas surveillance sentinel sites, technical training, provision of material supports, joint propagation activities and joint responses to malaria epidemics. This project was incorporated into the Five-Year Plan of Action on Lancang-Mekong Cooperation (2018—2022) in China in 2018, with 5 liaison offices and 20 liaison workstations established in Myanmar, Laos, Vietnam, Cambodia, and Thailand, and 21 cross-border malaria surveillance sites assigned in border areas of Myanmar, Laos and Vietnam, and a long-term malaria prevention and control cooperation mechanisms was established through meetings, training, propagation, and joint investigations. Currently, Yunnan Province is poised to engage in more extensive and in-depth cooperation with neighboring countries, including malaria diagnosis and treatment techniques, drug and vaccine research and development, talent cultivation, information sharing, cross-border human health services, and health promotion, under the guidance of the Five-Year Plan of Action on Lancang-Mekong Cooperation (2023—2027).
4.Formulation Characteristics and Efficacy Classification of Chinese Patent Medicines for Cardiovascular and Cerebrovascular Diseases Based on Diagram of Tangye Jingfa Tu
Yuguang WANG ; Runtao ZHUANG ; Yanqing LIU ; Shen LI ; Xiaolan LIN ; Rui JIN
Chinese Journal of Experimental Traditional Medical Formulae 2025;31(12):224-233
ObjectiveChinese patent medicines for cardiovascular and cerebrovascular diseases are diverse and complex in their efficacy. The traditional classification method based on efficacy categories has certain limitations and cannot meet the clinical needs for individualized drug selection and variety comparison. This article, based on the formulation compatibility analysis technology of "Tangye Jingfa Tu", clarifies the composition and efficacy characteristics of common Chinese patent medicines used for cardiovascular and cerebrovascular diseases, providing support for the precise selection of these medicines. MethodsFifty-six representative Chinese patent medicines, covering all the efficacy subcategories of "stasis-resolving agents" in the National Basic Medical Insurance, Work Injury Insurance, and Maternity Insurance Drug Catalogue (2023) (more than 50% of the total), were selected for the study. Within the knowledge system of "Tangye Jingfa Tu", the compatibility structure of herbal flavors and the proportion structure of herbal quantities for each Chinese patent medicine were determined. The correlation between these structures and the efficacy categories was analyzed to identify the similarities and differences among the selected Chinese patent medicines. Additionally, the efficacy was reclassified and compared according to the theoretical framework of tonifying and purging methods of five Zang organs in the "Tangye Jingfa Tu". ResultsThe representative Chinese patent medicines included in the analysis were Shexiang Baoxin pills, Danshen tablets, Qili Qiangxin capsules, Breviscapine tablets, etc., covering all the efficacy subcategories of "stasis-resolving agents". Among the 56 representative Chinese patent medicines, salty flavor was the most common (48), followed by pungent (33), and sweet (26). According to the dominant herbal flavor, salty flavor was the most common (37), followed by pungent (9), and sour (5). According to the dominant herbal quantity, salty flavor was the most common (27), followed by sour (7), and pungent (5). Furthermore, Chinese patent medicines with different efficacy subtypes showed different flavor characteristics. For example, most Qi-invigorating and blood-activating agents contained sweet drugs for tonifying the spleen (9/10), most Qi-moving and blood-activating agents contained pungent drugs for tonifying the liver (7/8), and all kidney-invigorating and blood-activating agents contained bitter drugs for tonifying the kidneys (6/6). However, the efficacy classification of individual medicines did not always align with the compatibility characteristics of their formulas, as seen with Dengyin Naotong capsules. ConclusionThe formulations of Chinese patent medicines for cardiovascular and cerebrovascular diseases predominantly feature salty, sour, and pungent flavors, which largely conform to the therapeutic principles of "nourishing the heart with salt and soothing the heart with sour" and the liver-heart, heart-spleen mother-child treatment relationship shown in the "Tangye Jingfa Tu". Using the "Tangye Jingfa Tu" framework to conduct research on the structure and efficacy characteristics of Chinese patent medicines is objective and effective.
5.Mechanisms of Traditional Chinese Medicine in Prevention and Treatment of Stroke by Regulating Ferroptosis: A Review
Mingyan WEI ; Shanze LI ; Rui HAN ; Qingbi LI ; Xingyi SUN ; Han ZHANG ; Lin LI
Chinese Journal of Experimental Traditional Medical Formulae 2025;31(12):313-321
Stroke is one of the leading causes of death and disability worldwide, ranking as the second leading cause of mortality globally and the primary cause of adult disability. Its pathological process involves complex cascade mechanisms, with high incidence and disability rates, posing a major threat to human health. According to statistics from the World Health Organization, more than 13 million new cases of stroke occur globally each year, resulting in direct medical costs and socioeconomic burdens amounting to hundreds of billions of dollars. In recent years, breakthroughs in the study of programmed cell death mechanisms have provided new insights into stroke treatment. Among them, ferroptosis, a novel form of cell death driven by iron-dependent lipid peroxidation, has attracted widespread attention in the pathological process of stroke. Ferroptosis is closely associated with iron metabolism disorders, oxidative stress, and lipid peroxidation, and exhibits unique regulatory effects in key pathological processes of stroke, such as ischemia-reperfusion injury, disruption of the blood-brain barrier, and neuronal apoptosis. It plays an important role in post-stroke neurological damage. Chinese medicine, as an essential component of traditional Chinese medicine (TCM), has demonstrated advantages in modulating ferroptosis and exerting neuroprotective effects. This review systematically summarizes current research on the neuroprotective mechanisms of Chinese medicine compound formulas and monomers through the regulation of ferroptosis pathways in post-stroke conditions, aiming to provide a basis for optimizing clinical treatment strategies and exploring new therapeutic approaches, and to offer new strategies and approaches for stroke treatment.
6.Formulation Characteristics and Efficacy Classification of Chinese Patent Medicines for Cardiovascular and Cerebrovascular Diseases Based on Diagram of Tangye Jingfa Tu
Yuguang WANG ; Runtao ZHUANG ; Yanqing LIU ; Shen LI ; Xiaolan LIN ; Rui JIN
Chinese Journal of Experimental Traditional Medical Formulae 2025;31(12):224-233
ObjectiveChinese patent medicines for cardiovascular and cerebrovascular diseases are diverse and complex in their efficacy. The traditional classification method based on efficacy categories has certain limitations and cannot meet the clinical needs for individualized drug selection and variety comparison. This article, based on the formulation compatibility analysis technology of "Tangye Jingfa Tu", clarifies the composition and efficacy characteristics of common Chinese patent medicines used for cardiovascular and cerebrovascular diseases, providing support for the precise selection of these medicines. MethodsFifty-six representative Chinese patent medicines, covering all the efficacy subcategories of "stasis-resolving agents" in the National Basic Medical Insurance, Work Injury Insurance, and Maternity Insurance Drug Catalogue (2023) (more than 50% of the total), were selected for the study. Within the knowledge system of "Tangye Jingfa Tu", the compatibility structure of herbal flavors and the proportion structure of herbal quantities for each Chinese patent medicine were determined. The correlation between these structures and the efficacy categories was analyzed to identify the similarities and differences among the selected Chinese patent medicines. Additionally, the efficacy was reclassified and compared according to the theoretical framework of tonifying and purging methods of five Zang organs in the "Tangye Jingfa Tu". ResultsThe representative Chinese patent medicines included in the analysis were Shexiang Baoxin pills, Danshen tablets, Qili Qiangxin capsules, Breviscapine tablets, etc., covering all the efficacy subcategories of "stasis-resolving agents". Among the 56 representative Chinese patent medicines, salty flavor was the most common (48), followed by pungent (33), and sweet (26). According to the dominant herbal flavor, salty flavor was the most common (37), followed by pungent (9), and sour (5). According to the dominant herbal quantity, salty flavor was the most common (27), followed by sour (7), and pungent (5). Furthermore, Chinese patent medicines with different efficacy subtypes showed different flavor characteristics. For example, most Qi-invigorating and blood-activating agents contained sweet drugs for tonifying the spleen (9/10), most Qi-moving and blood-activating agents contained pungent drugs for tonifying the liver (7/8), and all kidney-invigorating and blood-activating agents contained bitter drugs for tonifying the kidneys (6/6). However, the efficacy classification of individual medicines did not always align with the compatibility characteristics of their formulas, as seen with Dengyin Naotong capsules. ConclusionThe formulations of Chinese patent medicines for cardiovascular and cerebrovascular diseases predominantly feature salty, sour, and pungent flavors, which largely conform to the therapeutic principles of "nourishing the heart with salt and soothing the heart with sour" and the liver-heart, heart-spleen mother-child treatment relationship shown in the "Tangye Jingfa Tu". Using the "Tangye Jingfa Tu" framework to conduct research on the structure and efficacy characteristics of Chinese patent medicines is objective and effective.
7.Mechanisms of Traditional Chinese Medicine in Prevention and Treatment of Stroke by Regulating Ferroptosis: A Review
Mingyan WEI ; Shanze LI ; Rui HAN ; Qingbi LI ; Xingyi SUN ; Han ZHANG ; Lin LI
Chinese Journal of Experimental Traditional Medical Formulae 2025;31(12):313-321
Stroke is one of the leading causes of death and disability worldwide, ranking as the second leading cause of mortality globally and the primary cause of adult disability. Its pathological process involves complex cascade mechanisms, with high incidence and disability rates, posing a major threat to human health. According to statistics from the World Health Organization, more than 13 million new cases of stroke occur globally each year, resulting in direct medical costs and socioeconomic burdens amounting to hundreds of billions of dollars. In recent years, breakthroughs in the study of programmed cell death mechanisms have provided new insights into stroke treatment. Among them, ferroptosis, a novel form of cell death driven by iron-dependent lipid peroxidation, has attracted widespread attention in the pathological process of stroke. Ferroptosis is closely associated with iron metabolism disorders, oxidative stress, and lipid peroxidation, and exhibits unique regulatory effects in key pathological processes of stroke, such as ischemia-reperfusion injury, disruption of the blood-brain barrier, and neuronal apoptosis. It plays an important role in post-stroke neurological damage. Chinese medicine, as an essential component of traditional Chinese medicine (TCM), has demonstrated advantages in modulating ferroptosis and exerting neuroprotective effects. This review systematically summarizes current research on the neuroprotective mechanisms of Chinese medicine compound formulas and monomers through the regulation of ferroptosis pathways in post-stroke conditions, aiming to provide a basis for optimizing clinical treatment strategies and exploring new therapeutic approaches, and to offer new strategies and approaches for stroke treatment.
8.Eucommia ulmoides promotes alveolar bone formation in ovariectomized rats
Lin ZHENG ; Wenjun JIN ; Shanshan LUO ; Rui HUANG ; Jie WANG ; Yuting CHENG ; Zheqing AN ; Yue XIONG ; Zipeng GONG ; Jian LIAO
Chinese Journal of Tissue Engineering Research 2025;29(6):1159-1167
BACKGROUND:Eucommia ulmoides has a certain osteogenic effect,which can promote the proliferation and differentiation of osteoblasts.However,it is unclear whether Eucommia ulmoides has effects on alveolar bone formation and Wnt/β-Catenin signaling pathway. OBJECTIVE:To investigate the mechanism by which Eucommia ulmoides promotes alveolar bone formation in ovariectomized rats based on the Wnt/β-Catenin signaling pathway. METHODS:Sixty female Sprague-Dawley rats were selected and randomly divided into five groups:blank control group,sham-operation group,model group,low-dose group Eucommia ulmoides group,and high-dose Eucommia ulmoides group,with twelve rats in each group.Osteoporosis animal models were constructed by bilateral oophorectomy in the model group and the low-dose and high-dose Eucommia ulmoides groups.The sham-operation group underwent the same method to remove adipose tissue of equal mass around the bilateral ovaries.Three months after surgery,the low-and high-dose Eucommia ulmoides groups were given 2.1 g/kg/d and 4.2 g/kg/d Eucommia ulmoides by gavage,respectively.The sham-operation group and model group were given the same amount of physiological saline by gavage.After 12 weeks of drug intervention,the changes in alveolar bone mass of rats in each group were observed through Micro-CT;hematoxylin-eosin staining was used to observe the pathological structural changes of alveolar bone in rats;enzyme linked immunosorbent assay was used to detect the expression levels of alkaline phosphatase and osteocalcin in the serum of rats;western blot was used to detect the expression levels of β-Catenin and Frizzled9 receptor proteins in the alveolar bone of rats;and real-time fluorescence quantitative PCR was used to detect the expression of osteocalcin,Runt-related transcription factor 2(Runx2),alkaline phosphatase,β-catenin,and frizzled9 mRNAs in alveolar bone tissues of rats. RESULTS AND CONCLUSION:Compared with the blank control group,bone volume fraction,trabecular number,trabecular thickness,and bone mineral density were reduced in the model group(P<0.05),and trabecular separation was elevated(P<0.05).Pathological observation showed that the arrangement of trabeculae was disordered and irregular,the trabeculae were thinned or broken,and the marrow cavity was enlarged in the model group,with a significant reduction in bone volume;the level of alkaline phosphatase in the serum was increased(P<0.05),and the level of osteocalcin was decreased(P<0.05);mRNA expression of alkaline phosphatase,osteocalcin,Runx2,β-catenin,and frizzled9 were decreased(P<0.05);protein expression of β-Catenin and Frizzled9 was decreased(P<0.05).Compared with the model group,the low-and high-dose Eucommia ulmoides groups showed an increase in bone volume fraction,trabecular number,trabecular thickness,and bone mineral density(P<0.05)and a decrease in trabecular separation(P<0.05).In the low-and high-dose Eucommia ulmoides groups,bone trabeculae were slightly aligned and thickened,with a significant increase in bone mass.Compared with the model group,the serum level of alkaline phosphatase was reduced(P<0.05)and the serum level of osteocalcin was elevated(P<0.05)in the low-and high-dose Eucommia ulmoides groups.Compared with the model group,the mRNA expression of alkaline phosphatase,osteocalcin,Runx2,β-catenin,and frizzled9 were increased in the low-and high-dose Eucommia ulmoides groups(P<0.05).Compared with the model group,the protein expression of Frizzled9 was increased in the low-dose Eucommia ulmoides group(P<0.05),while the protein expression of β-Catenin and Frizzled9 was increased in the high-dose Eucommia ulmoides group(P<0.05).Compared with the low-dose Eucommia ulmoides group,the high-dose Eucommia ulmoides group had a more significant improvement in the above indexes.To conclude,Eucommia ulmoides can effectively promote the alveolar bone formation,and its mechanism of action might be related to the activation of the Wnt/β-catenin signaling pathway.
9.Grounded theory, scientific connotation, and clinical application of aromatic immunity in traditional Chinese medicine.
Si-Rui XIANG ; Qin JIAN ; Qi XU ; Jun-Zhi LIN ; Ding-Kun ZHANG ; Ming YANG ; Chuan ZHENG
China Journal of Chinese Materia Medica 2025;50(5):1137-1145
Aromatic immunity in traditional Chinese medicine(TCM) is the medical knowledge accumulated in the process of people's struggling with diseases. It plays an important role in plague prevention, disease treatment, health preservation, and rehabilitation, and has profound TCM basic theoretical support and abundant modern scientific evidence. With the in-depth promotion of the Healthy China initiative and the succession of health needs in the post-COVID-19 era, how to practice the health concept of aromatic immunity in TCM and develop its health service resources with high quality has become an important proposition to be discussed urgently. This paper summarizes the cognitive process, puts forward the basic concept, discusses the scientific connotation and clinical application value, and looks forward to the future development trend of aromatic immunity in TCM, aiming to provide guidance for the development of great health products and promote the application of aromatic immunity in TCM in serving people's health.
Medicine, Chinese Traditional/methods*
;
Humans
;
COVID-19/immunology*
;
China
;
Drugs, Chinese Herbal/therapeutic use*
;
SARS-CoV-2
10.Color-component correlation and mechanism of component transformation of processed Citri Reticulatae Semen.
Kui-Lin ZHU ; Jin-Lian ZOU ; Xu-Li DENG ; Mao-Xin DENG ; Hai-Ming WANG ; Rui YIN ; Zhang-Xian CHEN ; Yun-Tao ZHANG ; Hong-Ping HE ; Fa-Wu DONG
China Journal of Chinese Materia Medica 2025;50(9):2382-2390
High-performance liquid chromatography(HPLC) was used to determine the content of three major components in Citri Reticulatae Semen(CRS), including limonin, nomilin, and obacunone. The chromaticity of the CRS sample during salt processing and stir-frying was measured using a color difference meter. Next, the relationship between the color and content of the salt-processed CRS sample was investigated through correlation analysis. By integrating the oil bath technique for processing simulation with HPLC, the changes in the relative content of nomilin and its transformation products were analyzed, with its structural transformation pattern during processing identified. Additionally, RAW264.7 cells were induced with lipopolysaccharides(LPSs) to establish an inflammatory model, and the anti-inflammatory activity of nomilin and its transformation product, namely obacunone was evaluated. The results indicated that as processing progressed, E~*ab and L~* values showed a downward trend; a~* values exhibited a slow increase over a certain period, followed by no significant changes, and b~* values remained stable with no significant changes over a certain period and then started to decrease. The limonin content remained barely unchanged; the nomilin content decreased, and the obacunone increased significantly. The changing trends in content and color parameters during salt-processing and stir-frying were basically consistent. The content of nomilin and obacunone was significantly correlated with the colorimetric values(L~*, a~*, b~*, and E~*ab), while limonin content showed no significant correlation with these values. By analyzing HPLC patterns of nomylin at different heating temperatures and time, it was found that under conditions of 200-250 ℃ for heating of 5-60 min, the content of nomilin significantly decreased, while the obacunone content increased pronouncedly. The in vitro anti-inflammatory activity results indicated that compared to the model group, the group with a high concentration of nomilin and the groups with varying concentrations of obacunone showed significantly reduced release of nitric oxide(NO)(P<0.01). When both were at the same concentration, obacunone showed better performance in inhibiting NO release. In this study, the obvious correlation between the color and content of major components during the processing of CRS samples was identified, and the dynamic patterns of quality change in CRS samples during processing were revealed. Additionally, the study revealed and confirmed the transformation of nomilin into obacunone during processing, with the in vitro anti-inflammatory activity of obacunone significantly greater than that of nomilin. These findings provided a scientific basis for CRS processing optimization, tablet quality control, and its clinical application.
Mice
;
Animals
;
Drugs, Chinese Herbal/pharmacology*
;
RAW 264.7 Cells
;
Limonins/chemistry*
;
Chromatography, High Pressure Liquid
;
Citrus/chemistry*
;
Color
;
Benzoxepins/chemistry*
;
Anti-Inflammatory Agents/chemistry*

Result Analysis
Print
Save
E-mail