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[Chemical constituents from Sageretia gracilis]. [牧尾草的化学成分]。
Q3 Pharmacology, Toxicology and Pharmaceutics Pub Date : 2025-12-01 DOI: 10.19540/j.cnki.cjcmm.20250818.201
Ke-Yu Liu, Xin-Li Chen, Tian-Ze Li, Yan-Mei Weng, Jia-Fen Qian, Li-Yuan Chen, Hui Wu

The water extract of the stem of Sageretia gracilis was separated and purified using Sephadex LH-20, RP-C_(18), silica gel column chromatography, and semi-preparative high performance liquid chromatography(HPLC). Based on physicochemical properties, modern spectroscopic techniques, and comparison with literature, 12 compounds were identified as methyl 4-hydroxylbenzoate 1-O-α-L-rhamnopyranosyl-(1→6)-β-D-glucopyranoside(1), 6-hydroxy-2,4-dimethoxyphenyl-1-O-β-D-furanopyranosyl-(1→6)-β-D-glucopyranosyl-4-hydroxybenzoic acid methyl ester(2), tachioside(3), 2,4,6-trimethoxyphenol-1-O-β-D-apiofuranosyl-(1→6)-β-D-glucopyronoside(4), methyl syringate-α-L-rhamnoside(5),(7R,8R)-Δ~(7')-3,3'-dimethoxy-4,7,9,9'-tetrahydroxy-8-O-4'-neolignan-7-O-β-D-glucopyranoside(6),(7S,8R)-dihydrodehydrodiconiferyl alcohol-4-O-β-D-glucopyranoside(7), 2,6-dimethoxy-4-(prop-2-enyl)phenyl-O-β-D-glu-(1→6)-β-D-glucoside(8), 5-hydroxy-2-[2-(4-hydroxyphenyl) acetyl]-3-methoxylbenzoic acid(9), icariside E_3(10), 5-(β-D-glucopyranosyloxy)-2-hydroxy benzoic methyl ester(11), and seco-dehydrodiconiferyl alcohol-4-O-β-D-glucopyranoside(12). Among them, compounds 1 and 2 are new compounds, named sagergracioside A and sagergracioside B, respectively. All compounds were obtained from S. gracilis for the first time.

采用Sephadex LH-20、RP-C_(18)、硅胶柱层析、半制备型高效液相色谱(HPLC)等方法对山艾草茎水提物进行分离纯化。根据理化性质、现代光谱技术和文献比较,鉴定出12个化合物为:4-羟基苯甲酸甲酯1- o -α- l-鼠李糖吡喃基-(1→6)-β- d -葡萄糖吡喃基-(1→6)-β- d -葡萄糖吡喃基-(1→6)- 1- o -β- d -呋喃吡喃基-(1→6)-β- d -葡萄糖吡喃基-4-羟基苯甲酸甲酯(2),桃核苷(3),2,4,6-三甲氧基苯酚-1- o -β- d -吡喃基-(1→6)-β- d -葡萄糖吡喃基-(4),甲基syringate -α-L-rhamnoside(5)、(7 r, 8 r) -Δ~ (7 ')3,3 ' -dimethoxy-4, 7, 9, 9“-tetrahydroxy-8-O-4”-neolignan-7-O——β-D-glucopyranoside (6), (7, 8 r) -dihydrodehydrodiconiferyl alcohol-4-O -β-D-glucopyranoside (7), 2, 6-dimethoxy-4 - (prop-2-enyl) phenyl-Oβ-D-glu -(1→6)β-D-glucoside (8), 5-hydroxy-2 - [2 - (4-hydroxyphenyl)乙酰基]3-methoxylbenzoic酸(9),icariside E_3(10), 5 -(β-D-glucopyranosyloxy)二羟基苯甲酸甲酯(11)和seco-dehydrodiconiferyl alcohol-4-O -β-D-glucopyranoside(12)。其中化合物1和2为新化合物,分别命名为蒿草苷A和蒿草苷B。所有化合物均为首次从该植物中分离得到。
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引用次数: 0
[Mechanism of Fufang E'jiao Jiang in ameliorating chemotherapy-associated muscle fatigue in 4T1 breast cancer-bearing mice based on metabolomics]. [基于代谢组学的复方阿娇江改善4T1乳腺癌小鼠化疗相关肌肉疲劳的机制]。
Q3 Pharmacology, Toxicology and Pharmaceutics Pub Date : 2025-12-01 DOI: 10.19540/j.cnki.cjcmm.20250911.403
Chao-Fan Zhao, Hui Sun, Yuan-Yuan Wang, Yi-di Jiang, Kun-Shuang Shen, Zhi-Gang Wang, Guang-Li Yan, Ling Kong, Xi-Jun Wang, Ning Zhang

The aim is to investigate the ameliorative effects and underlying mechanisms of Fufang E'jiao Jiang on chemotherapy-associated muscle fatigue in 4T1 breast cancer-bearing mice. A cancer-related fatigue model was established by orthotopic injection of 4T1 cells to induce breast cancer, combined with intraperitoneal injection of paclitaxel. The efficacy of Fufang E'jiao Jiang in ameliorating breast cancer-associated muscle fatigue was evaluated through multimodal pharmacodynamic indices, including behavioral tests, biochemical analyses, and histopathological examinations. Untargeted metabolomics was employed to characterize the metabolic profiles and identify biomarkers in a 4T1 breast cancer-bearing mouse model with chemotherapy-associated muscle fatigue. Subsequently, targeted investigations were conducted to determine the effects of Fufang E'jiao Jiang on these metabolic profiles and biomarkers. Finally, the expression of key metabolic enzymes was detected by Western blot. Based on the tumor volume measurements, Fufang E'jiao Jiang did not exert a significant inhibitory effect on tumor volume. Behavioral results showed that Fufang E'jiao Jiang could increase the grip strength, swimming exhaustion time, rotarod residence time, treadmill exercise distance and exercise time of mice with muscle fatigue. Biochemical analysis revealed that Fufang E'jiao Jiang significantly downregulated the level of creatine kinase(CK) and lactate(LAC). Hematoxylin and eosin staining indicated that Fufang E'jiao Jiang increased the cross-sectional area of gastrocnemius muscle fibers. Transmission electron microscopy results showed that Fufang E'jiao Jiang significantly increased the length and width of gastrocnemius muscle fibers in fatigued mice, and restored mitochondrial morphology towards normal. Metabolomics identified 20 biomarkers in the gastrocnemius muscle of 4T1 breast cancer-bearing mice with chemotherapy-associated muscle fatigue. Fufang E'jiao Jiang significantly restored the level of 17 biomarkers, including L-arginine(Arg), L-aspartic acid(Asp), homocarnosine, and α-ketoglutarate(AKG). Furthermore, Fufang E'jiao Jiang upregulated metabolic pathways such as arginine biosynthesis, alanine-aspartate-glutamate metabolism, and arginine-proline metabolism. The Western blot results indicated that Fufang E'jiao Jiang participated in arginine biosynthesis and metabolism by upregulating argininosuccinate synthase 1(ASS1) activity and downregulating arginase 1(ARG1) activity. This study demonstrates that Fufang E'jiao Jiang significantly ameliorates chemotherapy-associated muscle fatigue in 4T1 breast cancer-bearing mice. The underlying mechanism may involve modulation of Arg biosynthesis and metabolic pathways to maintain systemic arginine homeostasis. These findings provide a preliminary foundation for elucidating the mechanism of Fufang E'jiao Jiang in managing breast cancer chemotherapy-related muscle fatigue.

目的是探讨复方阿胶江对4T1乳腺癌小鼠化疗相关性肌肉疲劳的改善作用及其机制。采用原位注射4T1细胞诱导乳腺癌,联合腹腔注射紫杉醇建立肿瘤相关疲劳模型。通过行为学试验、生化分析和组织病理学检查等多模态药效学指标评价复方阿娇江改善乳腺癌相关性肌肉疲劳的疗效。采用非靶向代谢组学来表征化疗相关肌肉疲劳的4T1乳腺癌小鼠模型的代谢谱并鉴定生物标志物。随后,我们进行了有针对性的研究,以确定复方阿胶江对这些代谢特征和生物标志物的影响。最后用Western blot检测关键代谢酶的表达。根据肿瘤体积测量,复方阿胶江对肿瘤体积没有明显的抑制作用。行为学结果显示,复方阿胶江能增加肌肉疲劳小鼠的握力、游泳疲劳时间、旋转杆停留时间、跑步机运动距离和运动时间。生化分析显示,复方阿胶江显著下调了肌酸激酶(CK)和乳酸激酶(LAC)的水平。苏木精、伊红染色显示复方阿胶江使腓肠肌纤维横截面积增大。透射电镜结果显示,复方阿胶江明显增加疲劳小鼠腓肠肌纤维的长度和宽度,使线粒体形态恢复正常。代谢组学在患有化疗相关肌肉疲劳的4T1乳腺癌小鼠的腓肠肌中发现了20个生物标志物。复方阿胶江显著恢复了l -精氨酸(Arg)、l -天冬氨酸(Asp)、同型肌肽和α-酮戊二酸(AKG)等17种生物标志物的水平。此外,复方阿娇姜上调了精氨酸生物合成、丙氨酸-天冬氨酸-谷氨酸代谢和精氨酸-脯氨酸代谢等代谢途径。Western blot结果显示,复方阿胶姜通过上调精氨酸琥珀酸合成酶1(ASS1)活性和下调精氨酸酶1(ARG1)活性参与精氨酸的生物合成和代谢。本研究表明,复方阿胶江可显著改善4T1乳腺癌小鼠化疗相关肌肉疲劳。潜在的机制可能涉及调节精氨酸生物合成和代谢途径,以维持全身精氨酸稳态。本研究结果为阐明复方阿娇江治疗乳腺癌化疗相关性肌肉疲劳的机制提供了初步的基础。
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引用次数: 0
[Effects of Guben Zenggu Capsules on oxidative stress-mediated mitochondrial apoptosis and bone metabolism in bone tissue of postmenopausal osteoporosis rats]. [固本增骨胶囊对绝经后骨质疏松大鼠氧化应激介导的线粒体凋亡及骨组织骨代谢的影响]。
Q3 Pharmacology, Toxicology and Pharmaceutics Pub Date : 2025-12-01 DOI: 10.19540/j.cnki.cjcmm.20250812.501
Min Song, Hao-Nan Wen, Yong-Jia Song, Kai Wang, Yan-Long Gong, Xiao-Yu Liu, Rong-Wei Zhang

This study aims to investigate the protective effects of Guben Zenggu Capsules(GBZG) on oxidative stress and mitochondrial apoptosis in bone tissue of a rat model with postmenopausal osteoporosis(PMOP). Sixty female Wistar rats(three months old) were randomly allocated into sham group, model group, low-dose GBZG(GBZGL) group, medium-dose GBZG(GBZGM) group, high-dose GBZG(GBZGH) group, and estrogen group. Except for the rats in the sham group, all rats underwent bilateral ovariectomy to establish the PMOP model. After 12 weeks of continuous administration, BMD was measured using dual-energy X-ray absorptiometry. Bone microarchitecture and pathological changes were evaluated by micro-CT imaging. Bone metabolism indicators, including BGP, ICTP, PICP, and TRAP-5b, as well as oxidative stress indicators, such as MDA, SOD, and ROS, were determined by ELISA. The protein expression levels of Bcl-2, Bax, Cyt C, Caspase-3, and Caspase-9 in bone tissue were analyzed by Western blot. The mRNA expression levels of Bcl-2, Bax, Cyt C, Caspase-3, Caspase-9, and AIF were quantified by RT-qPCR. Immunofluorescence staining was used to evaluate the fluorescence intensity of Caspase-3 and AIF proteins. The results showed that the rats in the model group exhibited reduced BMD, deterioration of bone microarchitecture, elevated oxidative stress, increased pro-apoptotic factors, and abnormal bone metabolism. GBZGH group could significantly reverse these pathological changes, exhibiting superior efficacy than GBZGM group and GBZGL group and effects similar to the estrogen group. These findings suggest that GBZG can exert a therapeutic effect on PMOP by inhibiting oxidative stress, regulating mitochondrial apoptosis pathways, and restoring bone metabolic homeostasis.

本研究旨在探讨固本增骨胶囊(GBZG)对绝经后骨质疏松大鼠骨组织氧化应激和线粒体凋亡的保护作用。将60只3月龄雌性Wistar大鼠随机分为假手术组、模型组、低剂量GBZG(GBZGL)组、中剂量GBZG(GBZGM)组、高剂量GBZG(GBZGH)组和雌激素组。除假手术组大鼠外,其余大鼠均切除双侧卵巢建立PMOP模型。连续给药12周后,用双能x线吸收仪测量骨密度。显微ct成像评价骨微结构及病理改变。采用ELISA法测定骨代谢指标BGP、ICTP、PICP、TRAP-5b和氧化应激指标MDA、SOD、ROS。Western blot检测骨组织中Bcl-2、Bax、Cyt - C、Caspase-3、Caspase-9蛋白的表达水平。RT-qPCR检测Bcl-2、Bax、Cyt C、Caspase-3、Caspase-9、AIF mRNA表达水平。免疫荧光染色法检测Caspase-3和AIF蛋白的荧光强度。结果显示,模型组大鼠骨密度降低,骨微结构恶化,氧化应激升高,促凋亡因子增加,骨代谢异常。GBZGH组可明显逆转上述病理改变,疗效优于GBZGM组和GBZGL组,作用与雌激素组相似。上述结果提示,GBZG可能通过抑制氧化应激、调节线粒体凋亡途径、恢复骨代谢稳态等途径对ppu发挥治疗作用。
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引用次数: 0
[Multiscale regulation strategies for improving thermal stability of volatile oil components from Acorus tatarinowii]. [提高石竹挥发油组分热稳定性的多尺度调控策略]。
Q3 Pharmacology, Toxicology and Pharmaceutics Pub Date : 2025-12-01 DOI: 10.19540/j.cnki.cjcmm.20250916.303
Zhi-Chao Wang, Ya-Jun Shi, Fei Luan, Xiao-Fei Zhang, Lu Sun, Liang Feng, Jun-Bo Zou

Addressing the common challenge that the volatility and degradation of volatile oil components restrict pharmaceutical development, this study focuses on a cross-scale regulation strategy of "particle modification-emulsion stabilization" to enhance the stability of volatile oil components. To address the imbalance of surface hydrophilicity and hydrophobicity of the water-insoluble precipitate(WIP) from Arisaema cum Bile-Bombyx Batryticatus extract, WIP-cellulose composite functional particles were successfully prepared via hydroxypropylmethylcellulose E50-mediated solvent volatilization, increasing the contact angle to 78°. Based on this, an O/W Pickering emulsion system containing volatile oil components from Acorus tatarinowii was constructed. The emulsion process was optimized through multidimensional stability indicators, including particle size, zeta potential, emulsion stability index(ESI), and post-centrifugation cream layer height. Optimal system stability was achieved with 8 mg·mL~(-1) composite particles, a 55% oil phase ratio, and high-speed shearing(14 000 r·min~(-1), 2 min). Confocal laser scanning microscopy confirmed that the WIP-cellulose composite particles formed dense adsorption layers at the oil-water interface. Thermal stability studies at 60 ℃ demonstrated that the Pickering emulsion system provided exceptional component protection via mesoscale structural barriers. The retention rates of key components(α-asarone, β-asarone, γ-asarone, cis-methyl isoeugenol, and β-calacorene) increased compared to free volatile oil components, while maintaining stable quantitative relationships. This study provides a novel solution for enhancing the stability of volatile oil components in solid TCM preparations through the organic integration of particle interface modification, mesostructure stabilization, and macroscopic property regulation.

针对挥发油成分挥发性和降解制约药物开发的共同挑战,本研究重点研究了“颗粒改性-乳液稳定”的跨尺度调控策略,以提高挥发油成分的稳定性。摘要为解决天蚕提取物水不溶性沉淀(WIP)表面亲疏水性不平衡的问题,采用羟丙基甲基纤维素e50介导溶剂挥发法制备了WIP-纤维素复合功能颗粒,并将接触角提高到78°。在此基础上,构建了含金盏花挥发油组分的O/W Pickering乳液体系。通过粒径、zeta电位、乳状液稳定性指数(ESI)、离心后乳霜层高度等多维稳定性指标对乳化工艺进行优化。当复合颗粒为8 mg·mL~(-1),油相比为55%,高速剪切(14000 r·min~(-1), 2 min)时,体系稳定性最佳。激光共聚焦扫描显微镜证实,wip -纤维素复合颗粒在油水界面形成致密的吸附层。60℃下的热稳定性研究表明,皮克林乳液体系通过中尺度结构屏障提供了出色的组分保护。关键成分(α-细辛酮、β-细辛酮、γ-细辛酮、顺式甲基异丁香酚和β-角胶烯)的保留率较游离挥发油组分增加,同时保持稳定的定量关系。本研究通过颗粒界面修饰、介观结构稳定和宏观性质调控的有机结合,为提高中药固体制剂中挥发油组分的稳定性提供了一种新的解决方案。
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引用次数: 0
[Preparation of monoclonal antibodies against saikosaponin A and saikosaponin D and establishment of indirect competitive enzyme-linked immunosorbent assay]. [柴草皂苷A、D单克隆抗体的制备及间接竞争性酶联免疫吸附法的建立]。
Q3 Pharmacology, Toxicology and Pharmaceutics Pub Date : 2025-12-01 DOI: 10.19540/j.cnki.cjcmm.20250717.406
Wan-Ying Guo, Mei-Chen Zhou, Zhi-Lai Zhan, Li-Ping Kang, Yuan Yuan, Tie-Gui Nan

Saikosaponin A(SSA) and saikosaponin D(SSD) were conjugated with bovine serum albumin(BSA) and ovalbumin(OVA) via the periodate oxidation method to prepare immunogens(SSA/D-BSA) and coating antigens(SSA/D-OVA), respectively. BALB/c mice were immunized with SSA/D-BSA, and 15 monoclonal antibody(mAb) cell lines against SSA/D were screened. Among these, the mAb SD6 against SSD exhibited cross-reaction rates of 100.00%, 99.94%, 95.06%, 94.89%, 1.97%, 1.89%, and 0.93% with SSD, SSA, 6″-O-acetyl-saikosaponin A, 6″-O-acetyl-saikosaponin D, saikosaponin C(SSC), saikosaponin E(SSE), and hydroxysaikosaponin A, respectively. The cross-reactivity rates with saikosaponin F(SSF), saikosaponin B1(SSB1), saikosaponin B2(SSB2), and other compounds were all less than 0.10%. An indirect competitive enzyme-linked immunosorbent assay(icELISA) based on the selected mAb SD6 against SSD demonstrated an IC_(50) value of 32.68 ng·mL~(-1), a detection range from 6.4 to 159.12 ng·mL~(-1), a spiked recovery from 95.03% to 104.5%, and RSD from 2.7% to 4.0%. The developed icELISA was applied to determine the total content of SSA and SSD in 19 batches of Bupleurum chinense DC. The results were validated using ultra-high-performance liquid chromatography(UPLC), with a high correlation coefficient(0.994 7) shown between the two methods. This confirms that the established icELISA is reliable for rapid quantification of the total SSA and SSD content in B. chinense.

采用高碘酸氧化法将柴草皂苷A(SSA)和D(SSD)分别与牛血清白蛋白(BSA)和卵清蛋白(OVA)偶联,制备免疫原(SSA/D-BSA)和包被抗原(SSA/D-OVA)。用SSA/D- bsa免疫BALB/c小鼠,筛选出15株抗SSA/D单克隆抗体(mAb)细胞株。其中,SD6单抗与SSD、SSA、6″-O-acetyl-saikosaponin A、6″-O-acetyl-saikosaponin D、saikosaponin C(SSC)、saikosaponin E(SSE)、羟基saikosaponin A的交叉反应率分别为100.00%、99.94%、95.06%、94.89%、1.97%、1.89%和0.93%。与柴草皂苷F(SSF)、柴草皂苷B1(SSB1)、柴草皂苷B2(SSB2)等化合物的交叉反应率均小于0.10%。基于选定的抗SSD单抗SD6的间接竞争性酶联免疫吸附试验(icELISA)显示IC_(50)值为32.68 ng·mL~(-1),检测范围为6.4 ~ 159.12 ng·mL~(-1),加标回收率为95.03% ~ 104.5%,RSD为2.7% ~ 4.0%。采用建立的icELISA法测定了19批柴胡中SSA和SSD的总含量。采用超高效液相色谱(UPLC)对结果进行验证,两种方法的相关系数为0.994 7。这证实了建立的icELISA法能够快速定量测定中华白杨总SSA和SSD含量。
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引用次数: 0
[Construction and application of composite drug delivery system combining liquid self-microemulsifying and solid dispersed micro-tablets for tanshinone components]. 【丹参酮成分液体自微乳化与固体分散微片剂复合给药体系的构建与应用】。
Q3 Pharmacology, Toxicology and Pharmaceutics Pub Date : 2025-12-01 DOI: 10.19540/j.cnki.cjcmm.20250905.301
Xiao-Yan Ma, Jiang-Dong Dai, Shu-Qi Hu, Ben-Hong Li, Xi-Chao Zhao, Lu Sun, Zhi-Wei Xiong, Liang Feng

The low water solubility of tanshinone components(TSC) limits their quality and functionality. This study innovatively constructed a composite drug-loading system of TSC self-microemulsifying dispersed micro-tablets by integrating the solubilization advantages of self-microemulsions with the stability characteristics of solid preparations. First, based on solubility tests, compatibility experiments, and pseudo-ternary phase diagram analysis, a ternary self-microemulsion system composed of ethyl oleate, polyoxyethylene castor oil, and absolute ethanol was established, and the self-microemulsion formation process was optimized using a central composite design-response surface methodology. Under the optimal self-microemulsifying conditions, the equilibrium solubility of TSC increased to(58.65 ± 0.18) mg·mL~(-1), exhibiting excellent centrifugation and dilution stability. In vitro drug release studies demonstrated that the TSC self-microemulsifying system significantly improved drug release, achieving complete release within 48 h in HCl medium. Subsequently, the matrix formulation of the dispersed micro-tablets was determined through single-factor screening. The resulting micro-tablets exhibited good mechanical properties and rapid dispersion characteristics, while particle size distribution after dissolution and transmission electron microscopy images confirmed effective maintenance of the self-microemulsion structure. Fourier transform near-infrared spectroscopy, X-ray diffraction, and simultaneous thermal analysis indicated that TSC was successfully encapsulated within the self-microemulsifying dispersed micro-tablets, while also highlighting the need for temperature protection during production. This study successfully established a novel "liquid self-microemulsifying-solid dispersed micro-tablet" composite drug-loading system, providing a new approach for improving the bioaccessibility of TSC.

丹参酮成分(TSC)水溶性低,限制了其质量和功能。本研究结合自微乳的增溶优势和固体制剂的稳定性特点,创新性地构建了TSC自微乳化分散微片复合载药体系。首先,通过溶解度测试、配伍性实验和拟三元相图分析,建立了油酸乙酯、聚氧乙烯蓖麻油和无水乙醇三元自微乳体系,并采用中心复合设计-响应面法对自微乳形成过程进行了优化。在最佳自微乳化条件下,TSC的平衡溶解度提高到(58.65±0.18)mg·mL~(-1),具有良好的离心和稀释稳定性。体外释药研究表明,TSC自微乳化体系显著改善了药物的释药效果,在HCl介质中可在48 h内完全释药。通过单因素筛选确定分散微片的基质配方。所制得的微片具有良好的力学性能和快速分散的特点,溶出后的粒径分布和透射电镜图像证实了自微乳结构的有效维持。傅里叶变换近红外光谱、x射线衍射和同步热分析表明,TSC被成功地封装在自微乳化分散微片中,同时也强调了生产过程中温度保护的必要性。本研究成功建立了一种新型的“液体自微乳化-固体分散微片”复合载药体系,为提高TSC的生物可及性提供了新的途径。
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引用次数: 0
[Improvement of oxidative stability of volatile oil components of Acorus tatarinowii based on supramolecular structure Pickering emulsion]. [基于超分子结构Pickering乳状液提高石英树挥发油组分氧化稳定性]。
Q3 Pharmacology, Toxicology and Pharmaceutics Pub Date : 2025-12-01 DOI: 10.19540/j.cnki.cjcmm.20250913.301
Xiao-Xiao Lin, Jun-Bo Zou, Fei Luan, Xiao-Fei Zhang, Lu Sun, Liang Feng, Ya-Jun Shi

This study addresses the oxidative stability bottleneck of TCM preparations containing volatile oil components by innovatively constructing a Pickering emulsion system based on "protein-polysaccharide" supramolecular structures, enabling precise regulation of the oxidative stability of volatile oil components. Chitosan-mediated heterocoagulation technology was used to prepare "Saigae Tataricae Cornu-Chitosan" composite particles. Multi-dimensional characterization using Fourier transform infrared spectroscopy, scanning electron microscopy, elemental energy spectrum analysis, and contact angle measurement revealed the physicochemical basis of the composite particles as Pickering stabilizers: the contact angle increased from 53.00° to 87.67°, indicating enhanced interfacial wettability. Scanning electron microscopy and surface element analysis showed increased particle volume, with Saigae Tataricae Cornu particles adhering to the serrated surface of chitosan, while surface sulfur(S) and phosphorus(P) elements were significantly reduced, demonstrating effective compounding of Saigae Tataricae Cornu powder with chitosan. Based on this, a Pickering emulsion of volatile oil from Acorus tatarinowii Schott was successfully constructed using a high-speed shear method. Laser confocal microscopy confirmed that the composite particles formed a dense adsorption layer at the oil-water interface, with an average droplet size of(1.77±0.70) μm and a zeta potential increased to(32.50±0.50) mV, indicating an electrostatically dominated stabilization mechanism. In ozone-accelerated oxidation tests, the emulsion exhibited outstanding protective efficacy, significantly reducing the formation of peroxides and malondialdehyde in volatile oil components(P<0.05, P<0.01), while effectively slowing the oxidative degradation of key active components(α-asarone and γ-asarone) and maintaining their quantitative structure. This study presents a tripartite solution, "raw powder incorporation-interface regulation-system stabilization", establishing an ozone-resistant Pickering emulsion system and providing a distinctive TCM-based strategy for overcoming the stability challenges of solid preparations containing volatile oil components.

本研究通过创新构建基于“蛋白-多糖”超分子结构的Pickering乳剂体系,解决了含挥发油成分的中药制剂氧化稳定性瓶颈,实现了对挥发油成分氧化稳定性的精准调控。采用壳聚糖介导的异聚技术制备了“鹿茸-壳聚糖”复合颗粒。傅里叶变换红外光谱、扫描电镜、元素能谱分析和接触角测量等多维表征揭示了复合颗粒作为Pickering稳定剂的物理化学基础:接触角从53.00°增加到87.67°,表明界面润湿性增强。扫描电镜和表面元素分析结果表明,柴胡颗粒体积增大,颗粒粘附在壳聚糖的锯齿状表面,表面硫(S)和磷(P)元素明显减少,表明柴胡粉与壳聚糖的复配是有效的。在此基础上,采用高速剪切法制备了石竹挥发油皮克林乳状液。激光共聚焦显微镜观察发现,复合颗粒在油水界面形成致密的吸附层,平均粒径为(1.77±0.70)μm, zeta电位升高至(32.50±0.50)mV,表明复合颗粒的稳定机制以静电为主。在臭氧加速氧化试验中,乳化液表现出突出的保护作用,显著减少挥发油组分中过氧化物和丙二醛的形成(P<0.05, P<0.01),同时有效减缓关键活性成分(α-细辛酮和γ-细辛酮)的氧化降解,保持其定量结构。本研究提出了“原料粉掺入-界面调节-体系稳定”的三重解决方案,建立了抗臭氧皮克林乳液体系,并为克服含有挥发油成分的固体制剂的稳定性挑战提供了一种独特的基于中药的策略。
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引用次数: 0
[Pathogeneses and treatment of diabetes mellitus and its complications based on "Qi pathway-collateral axis" theory and trunk-branch coupling mechanism]. [基于“气经-络轴”理论和干支耦合机制的糖尿病及其并发症的病因与治疗]。
Q3 Pharmacology, Toxicology and Pharmaceutics Pub Date : 2025-12-01 DOI: 10.19540/j.cnki.cjcmm.20250724.502
Ya-Sheng Deng, Rong-Chang Zhang, Ming-Yue Zang, Jun-Quan Wei, Ye-Zhan Pang, Han-Dong Lin, Yu-Yan Huang, Jiang Lin, Tai-Jin Lan, Qiu Chen

Diabetes mellitus and its complications represent one of the most critical global public health challenges, with their pathogeneses involving complex multi-system and multi-level regulatory networks. Modern medical research confirms that diabetes mellitus not only manifests as glucose metabolism disorders characterized by insulin resistance and β-cell dysfunction but also involves progressive systemic pathological changes including microcirculation disorders(encompassing microvascular complications) and organ fibrosis(macrovascular complications). On the basis of the "Qi pathway-collateral axis" theory and the trunk-branch coupling mechanism, this study thoroughly investigates the pathogenesis and treatment of diabetes mellitus and its complications. Research findings demonstrate that Qi pathway, as the main channel for Qi and blood circulation, directly contributes to insulin resistance and β-cell dysfunction when its function is disrupted. Collaterals, as the finer branches of Qi and blood circulation, play a key pathological role in diabetic microvascular and macrovascular complications when being obstructed. Through the analysis of the trunk(Qi pathway)-branch(collateral vessel) coupling mechanism, this study reveals the intrinsic connection between central metabolic regulation and target organ damage. In terms of traditional Chinese medicine(TCM) treatment, an intervention system focusing on regulating Qi pathway to restore metabolic balance, dredging collateral vessels to improve microcirculation, and coordinating trunk-branch interactions to prevent complications has been established. This approach aims to restore the normal function of Qi pathway and collaterals while harmonizing the trunk-branch system, thereby providing new perspectives and methods for the prevention and treatment of diabetes mellitus and its complications. By constructing the "Qi pathway-collateral axis" theoretical framework, this study not only offers innovative TCM diagnostic and therapeutic insights for the management of diabetes mellitus but also paves new ways for the modernization and clinical application of TCM theory, providing unique theoretical foundations and practical guidance for improving the prevention and treatment of diabetes mellitus and its complications.

糖尿病及其并发症是全球最重要的公共卫生挑战之一,其发病机制涉及复杂的多系统、多层次调控网络。现代医学研究证实,糖尿病不仅表现为以胰岛素抵抗和β细胞功能障碍为特征的糖代谢障碍,而且还包括微循环障碍(包括微血管并发症)和器官纤维化(大血管并发症)等进行性全身病理改变。本研究以“气经-络轴”理论和干支耦合机制为基础,深入探讨糖尿病及其并发症的发病机制和治疗方法。研究发现,气通路作为气血循环的主通道,当其功能被破坏时,直接导致胰岛素抵抗和β细胞功能障碍。络作为气血循环的细分支,在糖尿病微血管和大血管病变受阻时起着关键的病理作用。本研究通过对干(气通路)-支(侧支血管)耦合机制的分析,揭示了中枢代谢调节与靶器官损伤之间的内在联系。在中医治疗方面,建立了以调节气路恢复代谢平衡、疏通侧支改善微循环、协调干支相互作用预防并发症为重点的干预体系。该方法旨在恢复气路和络的正常功能,协调干支系统,从而为糖尿病及其并发症的防治提供新的视角和方法。本研究通过构建“气经-络轴”理论框架,不仅为糖尿病的管理提供了创新的中医诊疗见解,而且为中医理论的现代化和临床应用开辟了新途径,为提高糖尿病及其并发症的防治水平提供了独特的理论基础和实践指导。
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引用次数: 0
[Quality improvement of traditional pediatric powder: taste enhancement and quality standard optimization of Lingzhu Powder]. 【传统小儿散的品质提升:灵珠散的口感增强与质量标准优化】。
Q3 Pharmacology, Toxicology and Pharmaceutics Pub Date : 2025-12-01 DOI: 10.19540/j.cnki.cjcmm.20250926.302
Wei-Lin Wang, Yan-Jun Yang, Mao-Mao Zhu, Zhong-Huan Qu, Zhou-Yang Qian, Wei-Ye Zhang, Lu Sun, Xiao-Bin Jia, Liang Feng

Good taste of the preparation and strict quality control standards are key factors in ensuring patient compliance, guaranteeing drug safety and efficacy, and enhancing market competitiveness, significantly impacting the quality of the preparation. Lingzhu Powder has noticeable undesirable tastes such as bitterness, fishy odor, and a gritty texture, which can cause resistance in taste-sensitive children and thus makes it difficult for them to take the medication. This study made a comprehensive analysis through volunteer sensory evaluation and found that the undesirable tastes of Lingzhu Powder originated from Bovis Calculus Artifactus(bitterness and fishy odor), Saigae Tataricae Cornu powder(fishy odor), and amber powder(gritty texture). Therefore, functional components, including flavoring agents, were used to improve the taste of Lingzhu Powder. A systematic study was conducted on the types, dosages, and ratios of these functional components, ultimately determining that the addition levels of stevioside, L-malic acid, xanthan gum, and honey peach flavoring should be 7%, 3%, 3%, and 5%, respectively, of the average total mass of the mixed powder of Lingzhu Powder. Meanwhile, to enhance the quality of the flavored Lingzhu Powder preparation and achieve precise quality control, it was proposed to incorporate microscopic identification of medicinal ingredients such as Cinnabaris, amber, Saigae Tataricae Cornu, Margarita, and Bovis Calculus Artifactus, TLC identification of Bovis Calculus Artifactus, Acori Tatarinowii Rhizoma oil, and Borneolum Syntheticum, and content determination of key pharmacodynamic components such as cholic acid and hyodeoxycholic acid into the quality standards for the flavored Lingzhu Powder. This will address the inadequacy of the original quality standards, which only included simple identification items, and ensure the safety of medication for children.

良好的制剂口感和严格的质量控制标准是保证患者依从性、保证药品安全有效性和增强市场竞争力的关键因素,对制剂质量有重要影响。灵珠散有明显的不良味道,如苦味、鱼腥味和砂砾质地,这可能导致味觉敏感的儿童产生抗药性,从而使他们难以服用药物。本研究通过志愿者感官评价进行综合分析,发现领珠散的不良味道来源于人工牛牙(苦味和鱼腥味)、鹿茸粉(鱼腥味)和琥珀粉(砂砾质地)。因此,通过添加调味剂等功能成分来改善灵珠粉的口感。对这些功能成分的种类、用量和配比进行了系统的研究,最终确定了甜菊糖苷、l -苹果酸、黄原胶和蜜桃香精的添加量分别为领珠粉混合粉平均总质量的7%、3%、3%和5%。同时,为提高香味灵珠散制剂的质量,实现精确的质量控制,提出了对朱砂、琥珀、石竹柏、玛格丽塔、牛牙等药用成分进行显微鉴别,对牛牙、石竹柏油、冰片进行薄层鉴别,并将胆酸、羟基去氧胆酸等关键药效成分的含量测定纳入调味灵珠粉的质量标准。这将解决原有质量标准的不足之处,该标准只包括简单的识别项目,并确保儿童用药的安全性。
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引用次数: 0
[Regulation of pyroptosis by traditional Chinese medicine compound formulas for prevention and treatment of ulcerative colitis: a review]. [防治溃疡性结肠炎中药复方对焦亡的调节作用综述]。
Q3 Pharmacology, Toxicology and Pharmaceutics Pub Date : 2025-12-01 DOI: 10.19540/j.cnki.cjcmm.20250915.702
Rui-Rui Wen, Si-Qi Li, Meng-Xin Li, Shu-Xia Li

Ulcerative colitis(UC) is a refractory inflammatory bowel disease with a high recurrence rate, characterized by inflammation and damage to the colonic mucosa, which severely impacts patients' quality of life. Current treatments for UC primarily rely on pharmacological interventions, including corticosteroids, aminosalicylates, biologics, and immunomodulators, but these approaches are limited by strong drug resistance and significant adverse effects. Pyroptosis, a highly inflammatory form of programmed cell death, can regulate the occurrence and progression of UC through multiple pathways by modulating diverse downstream targets, thereby providing a novel direction for UC therapy. Multiple studies have shown that pyroptosis can intervene in UC development by regulating the release of inflammatory cytokines, inflammasome activity, intestinal homeostasis, and the gut microbiota. Traditional Chinese medicine(TCM) has gained increasing attention due to its minimal adverse effects, personalized therapeutic strategies, and unique advantages in enhancing efficacy while reducing toxicity. Beyond traditional compound formulas, individual TCM herbs and extracts play a pivotal role owing to their more precise target specificity. Research indicates that TCM compound formulas classified as heat-clearing and dampness-eliminating, blood-activating and collaterals-unblocking, Qi-and blood-tonifying, or addressing cold-heat complex patterns can effectively alleviate inflammation by targeting pyroptosis. This is achieved through mechanisms such as maintaining intestinal homeostasis, regulating the gut microbiota, and inhibiting intestinal oxidative stress, thereby intervening in UC progression and offering new possibilities for precision therapy. Based on this, this paper discusses three aspects: an overview of pyroptosis, the relationship between pyroptosis and UC, and the regulatory mechanisms of TCM. It summarizes recent research findings in this field, aiming to provide a theoretical basis for future clinical treatment and drug development for UC.

溃疡性结肠炎(UC)是一种复发率高的难治性炎症性肠病,以炎症和结肠黏膜损伤为特征,严重影响患者的生活质量。目前UC的治疗主要依赖于药物干预,包括皮质类固醇、氨基水杨酸盐、生物制剂和免疫调节剂,但这些方法受到强耐药性和显著不良反应的限制。焦亡是一种高度炎症性的程序性细胞死亡形式,通过调节多种下游靶点,通过多种途径调节UC的发生和进展,为UC的治疗提供了新的方向。多项研究表明,焦亡可以通过调节炎症细胞因子的释放、炎症小体活性、肠道稳态和肠道微生物群来干预UC的发展。中医药以其不良反应小、治疗策略个性化、增效降毒等独特优势而受到越来越多的关注。除了传统的复方外,单个中药和提取物由于其更精确的目标特异性而发挥着关键作用。研究表明,清热湿散、活血通络、益气补血、冷热杂证等中药复方可通过针对焦亡有效缓解炎症。这是通过维持肠道内稳态、调节肠道微生物群和抑制肠道氧化应激等机制实现的,从而干预UC的进展,并为精准治疗提供了新的可能性。在此基础上,本文从焦亡的概述、焦亡与UC的关系、中医的调控机制三个方面进行了探讨。总结了近年来该领域的研究成果,旨在为UC的临床治疗和药物开发提供理论依据。
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引用次数: 0
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