Inflammation is a pathological process central to many chronic diseases. Conventional anti-inflammatories, including NSAIDs and corticosteroids, are limited by adverse effects and suboptimal efficacy with long-term use. Ginsenosides from Panax ginseng have emerged as promising multi-target candidates with favorable safety profiles. This review systematically summarizes recent advances in research on the anti-inflammatory pharmacological effects and molecular mechanisms of ginsenosides, with particular emphasis on Rg1, Rb1, Rd, Re, and Rg3. Recent literature was collected and analyzed, and network pharmacology and bioinformatics approaches were employed to predict therapeutic targets and regulatory networks. Core anti-inflammatory mechanisms include suppression of pro-inflammatory cytokines (TNF-α, IL-1β, and IL-6) and NF-κB signaling; modulation of TLR4/NF-κB and NLRP3 inflammasome activity; regulation of MAPK (ERK, JNK, and p38) phosphorylation; activation of Nrf2/HO-1 and Hippo-YAP/TAZ pathways; inhibition of COX-2 and iNOS expression; regulation of macrophage polarization; and modulation of membrane permeability and ion exchange. This study elucidates the association between ginsenosides and various inflammatory diseases, systematically consolidating their diverse molecular mechanisms underlying their treatment of typical inflammatory conditions. By integrating modern techniques such as network pharmacology and molecular docking, this review deepens our understanding of the efficacy of ginsenosides in the management of inflammatory diseases. It provides critical insights for further exploration of ginsenosides' pharmacological actions, the development of novel anti-inflammatory drugs, and the interpretation of the modern scientific basis underlying TCM concepts such as ginseng's "restorative and stabilizing" properties.
ETHNOPHARMACOLOGICAL RELEVANCE:Crataegus pinnatifida Bunge, a plant used traditionally in herbal medicine for digestive health, is known for its gut-protective properties. Orientin, a natural flavonoid compound abundant in this species, exhibits anti-inflammatory and gut-protective activities. AIM OF THE STUDY:This study examined the therapeutic potential of orientin against ulcerative colitis (UC) and aimed to elucidate its underlying molecular mechanisms. METHODS:This study established a DSS-triggered UC mouse model. RNA sequencing was carried out to identify key signaling pathways implicated in orientin's therapeutic effects. Disease activity, intestinal barrier integrity, inflammatory responses, ferroptosis, were systematically evaluated. To validate the role of GLUT1 in the pathogenesis of UC, GLUT1-knockdown mice were utilized. Additionally, LPS-stimulated primary intestinal epithelial cells (IECs) were employed to further confirm the protective effects of orientin in vitro. RESULTS:RNA sequencing revealed that orientin significantly modulated genes associated with inflammation, ferroptosis, and metabolic pathways. Orientin alleviated DSS-triggered colitis by boosting body weight, preserving colon length, reducing histological damage. GLUT1 deficiency exacerbated intestinal injury, whereas orientin treatment attenuated these effects by regulating the ROS/HIF-1α/GLUT1 signaling axis. Orientin also repressed pro-inflammatory cytokines, neutrophil infiltration, and oxidative stress, while inhibiting the ferroptosis pathway. Moreover, it normalized glycolytic reprogramming by targeting the ROS/HIF-1α/GLUT1 pathway. In vitro studies further confirmed orientin's protective effects on IECs by enhancing barrier function, reducing inflammation, and restoring metabolic homeostasis. CONCLUSIONS:This study underscores the pivotal role of the ROS/HIF-1α/GLUT1 axis and demonstrates the therapeutic potential of orientin in UC.
Inflammatory bowel disease imposes significant healthcare burdens, driving the search for natural therapeutic agents. This study investigated the protective effects of insect gall Methanol extract from Picea koraiensis Nakai (PK) against colitis. Using in vitro (H2O2-induced IEC-6 enterocytes) and in vivo (DSS-induced murine colitis) models, we assessed PK's impact on oxidative stress, inflammation, and apoptosis. In vitro, PK (0.6 mg/mL) significantly enhanced cell viability (∼40%) and key antioxidant enzyme activities, while reducing oxidative markers (MDA, LDH, ROS) by over 50%. It also suppressed apoptosis via caspase-3/9 inhibition and activated the Nrf2/HO-1 pathway. In vivo, PK ameliorated colitis severity, improved histopathology. Transcriptomic and molecular analyses confirmed the activation of the Nrf2/HO-1 pathway and inhibition of p53/p38-mediated apoptosis in colonic tissue. In conclusion, PK exhibits multimodal protection against colitis by alleviating oxidative stress, inflammation, and apoptosis, primarily via Nrf2/HO-1 activation. Future studies should focus on its pharmacokinetics and long-term safety.
This paper reviews the research progress of isoniazid electrochemical sensors in recent years. As an important anti-tuberculosis drug, the rapid and sensitive detection of isoniazid is of great significance for clinical treatment and drug quality control. This paper first introduces the basic properties and detection requirements of isoniazid, then elaborates on the working principle of electrochemical sensors and their application in isoniazid detection, with a focus on discussing isoniazid electrochemical sensors with different modified materials. Finally, the future development direction of isoniazid sensors is prospected, providing valuable insights for future research.
This investigation explored the hepatoprotective capabilities of Bruceine A (BA) and its underlying mechanisms in mitigating hepatic fibrosis. Hepatic stellate cells (HSCs) and mouse primary hepatocytes were treated with TGF-R and subsequently exposed to BA. To assess the effects of BA on the NR2F2-HMGB1 signaling cascade, these cells underwent transfection with a siRNA vector targeting NR2F2. The interaction between NR2F2 and the HMGB1 promoter was elucidated using a dual luciferase assay. In vivo, C57BL/6 mice were treated with thioacetamide (TAA) to induce liver damage, followed by administration of BA. The study found that BA moderated extracellular matrix (ECM) buildup, epithelial-mesenchymal transition (EMT), and inflammatory mediator levels, while concurrently reducing NR2F2 and HMGB1 expression in activated HSCs. Furthermore, BA lessened pyroptosis in hepatocytes, curtailing the inflammatory response. The absence of NR2F2 in HSCs or hepatocytes hindered BA's inhibitory effect on this pathway. It was demonstrated that NR2F2 binds directly to the HMGB1 promoter. Treatment with BA resulted in diminished serum levels of ALT and AST, mitigated damage in hepatic tissues, and decreased the ECM and neutrophil extracellular traps (NETs), thus protecting hepatocytes from fibrosis. Furthermore, BA suppressed the synthesis of inflammatory mediators such as NLRP3, caspase-1, and IL1R by blocking the NR2F2-driven HMGB1 pathway, markedly reversing hepatic fibrosis. These observations highlight the efficacy of BA as a viable therapeutic candidate for hepatic fibrosis.
Saponins, the major bioactive components of Panax ginseng C. A. Mey. (Renshen in Chinese), are gradually emerging as research hotspots owing to the possession of various pharmacological activities. This review updates the ginsenosides list from P. ginseng and the steam-processed ginseng (red ginseng and black ginseng) up to 271 by June of 2024, encompassing 241 saponins from different parts of P. ginseng (roots, stems, leaves, flowers, berries, and seeds), 103 from red ginseng, and 65 from black ginseng, respectively. Among 271 saponins, there are a total of 249 (1−249) dammarane type (with a−z subtypes) tetracyclic triterpene saponins reported from each part of P. ginseng and steam-processed ginseng, two (250−251) lanostane type tetracyclic triterpene saponins identified from red ginseng, 18 (252−269) oleanane type pentacyclic triterpenoid saponins discovered from each part of P. ginseng and steam-processed ginseng, and two (270−271) ursane type pentacyclic triterpenoid saponins reported from red ginseng. Overall, this review expounds on the chemical diversity of ginsenosides in multiple aspects, such as chemical structure, spatial distribution and subtype comparison, processed products, and transformation. This facilitates more in-depth research on ginsenosides and contributes to the future development of ginseng.
Picea koraiensis Nakai (PK) is an evergreen tree. It plays an important role in landscaping and road greening. Insect galls of PK are formed by parasitism of the adelgid Adelges laricis. Except for phenolics, other chemical constituents and biological activity of insect gall from PK are still unknown. Thus, here, we performed phytochemical and biological activity analyses of PK insect gall extracts, aiming to turn waste into treasure and serve human health. PK insect gall extracts were prepared using seven solvents. Antioxidant activities of the extracts were examined via antioxidant assays (radical and oxidizing substance quenching, metal chelating, and reducing power). The inhibitory activities of the extracts were determined toward the key human-disease-related enzymes α-glucosidase, α-amylase, cholinesterase, tyrosinase, urease, and xanthine oxidase. The content of numerous active constituents was high in the methanol and ethanol extracts of PK insect gall, and these extracts had the highest antioxidant and enzyme-inhibitory activities. They also showed excellent stability and low toxicity. These extracts have potential for use as stabilizers of olive and sunflower seed oils.
目的 建立清热化痰合剂质量标准.方法 采用薄层鉴别法定性鉴别该制剂中黄芩和桑白皮,采用高效液相色谱法测定麻黄中盐酸麻黄碱和盐酸伪麻黄碱含量.色谱柱:Hypersil BDS C18(4.6 mm× 200 mm,5 μm);流动相:乙腈-0.3%三乙胺0.02 mol·L-1磷酸二氢钾溶液(用磷酸调节至pH=3.0)(4∶96);流速:0.8 mL·min-1;柱温:25℃;检测波长:210 nm.结果 黄芩和桑白皮的薄层图斑点清晰,分离度好且阴性对照无干扰.盐酸麻黄碱和盐酸伪麻黄碱分别在0.4706~2.353 μg·mL-1和0.1519~0.7595 µg·mL-1范围内,线性关系良好,精密度、重复性及48h稳定性RSD均小于2.0%,平均加样回收率分别为102.87%、100.25%,RSD分别为1.09%和1.35%.结论 所建立的薄层鉴别法及高效色谱法稳定可靠、操作简单、结果准确,可以应用于该制剂的质量控制.
目的 检测蒸参水的主要化学成分和含量测定.方法 收集蒸参水,减压浓缩至一定浓度,加入适量乙醇得到沉淀的多糖部分,将去除多糖后的蒸参水用水饱和正丁醇萃取得到总皂苷部分,最后采用紫外可见分光光度法检测多糖与皂苷类成分并计算含量.结果 蒸参水中含有多糖和皂苷类成分含量分别为12.08 mg、2.77 mg.结论 经测定蒸参水中主要存在的化学成分为多糖和皂苷类,为人参扩大用药范围提供证据.
Three new organic-inorganic compounds based on polyoxometalates, [(CuCltpy)2( Cu2Cl2(tpy)2)(alpha-SiW12O40)]center dot 5H2O (1), [Cu4(tpy)4(H2O)4(alpha-P2W18O62)]center dot 4H2O (2), and [Cu(tpy)(Mo3O10)]center dot H2O (3) (tpy = 4 '-(pyrrol-3-yl)-2,2 ':6 ',2 ''- terpyridine), were facilely isolated by hydrothermal technique. Xray diffraction analysis shows that compound 1 with threedimensional (3D) supramolecular structure is featured by alpha-SiW12 clusters, {Cu2Cl2/tpy} dimers, and {CuCl/tpy} monomers. Compound 2 with zero-dimensional (0D) discrete structure is constructed from alpha-P2W18 clusters and four Cu/tpy units. The onedimensional (1D) infinite chain of 3 is stemmed from [Mo3O10]2- units and Cu/tpy motifs. Furthermore, we explored the bifunctional electrocatalytic activities of these three compounds for reduction and oxidation. The results show that the [Mo3O10]2-- type hybrid displays better difunctional electrocatalytic activities than heteropolyacids toward both reduction and oxidation. Significantly, the molecular electrostatic potential and the frontier molecular orbital were achieved by density functional theory calculations to analyze the electronic structure of three compounds. The natural bond orbital analysis was also carried out to interpret electron charge distribution.
目的 优化芎麻滴丸的制备工艺.方法 以基质与药物配比、药液温度、滴速为考察因素,采用Box-Behnken响应面分析法优化芎麻滴丸的制备工艺.结果 芎麻滴丸的最佳成型工艺中基质与药物比为4:6:1、药液温度为90℃、滴速为30 d/min.结论 经优化后的芎麻滴丸大小、颜色均匀且无粘连、拖尾.因此,优化后的芎麻滴丸制备工艺稳定可行.
目前,中药化学实验课学时较少,实验内容简单,教学模式为传授式,考核方式单一,且没有将思政元素融入教学中,本文针对中药化学实验课整体教学不利于培养学生自主性和创造性的问题,从增加实验课时,改进实验内容,引进新型教学模式,优化考核方式和挖掘课程思政元素五个方面进行改革,旨在提高中药化学实验课教学质量和培养学生的主观学习能力、自主创新意识和爱国情怀,真正落实立德树人的根本任务.
Three bimetallic organic-inorganic hybrids based on the [V2O6]2- building unit, [Cu(pty)(V2O6)]·H2O (1), [Cu(pty)(V2O6)] (2), [Cu(tpy)(V2O6)] (3), (pty = 4'-(4″-pyridyl)-2,2':6',2″-terpyridine, tpy = 2,2':6',2″-terpyridine), were synthesized via a one-pot method. Hybrid 1 has a 1D straight chain architecture with [V2O6]2- clusters and Cu-pty complexes; hybrids 2 and 3 possess a 2D sheet structure including 10-membered rings assembled from four [Cu(pty)]2+ motifs and six [V2O6]2- clusters in 2, and two [Cu(tpy)]2+ units and eight [V2O6]2- clusters in 3. Noteworthy, hybrids 1-3 can be employed as bifunctional electrocatalysts for electroreduction of nitrite and electrooxidation of ascorbic acid. Additionally, theoretical calculations including the molecular electrostatic potential and the frontier molecular orbital were performed to estimate the electronic structure of hybrids 1-3. The natural bond orbital analysis was also calculated to interpret the electron charge distribution.
In this work, upon subtle POMs variation, we reported on the assembly and performances of three new bimetallic component organic-inorganic hybrids, [Ag-2(bimpy)((V2O6)-O-V)](1), [Ag-3(bimpy)(2)(beta-(Mo8O26)-O-VI)](2), [Ag-4(bimpy)(2)(H2O)(2)(alpha-(SiW12O40)-O-VI)]center dot 2H(2)O (3) (bimpy = 3,5-bis(1-imidazoly) pyridine). Compound 1 with 3D framework structure is featured by {-V-O-V-}(n) helical chains, {Ag-3} clusters and {bimpy-Ag-bimpy} units. Compound 2 has a 3,3,6,6-connected 3D architecture with the (4(3))(4(3))(4(2)center dot 6(9)center dot 7 center dot 8(3))(4(6)center dot 5(2)center dot 6(4)center dot 7 center dot 8(2)) topology. Compound 3 has a 3,3,4-connected 2D layer with (6(2)center dot 8)(6(2)center dot 8)(6(6)) topology. The electrochemical and bifunctional electro-catalytic activities of three compounds have been conducted. The experimental results show that beta-[Mo8O26](4-) hybrid displays better electrocatalytic performance than [V2O6](2-) and Keggin-type hybrids for reduction of nitrite, while [V2O6](2-) hybrid exhibits better electrocatalytic activity than beta-[Mo8O26](4-) and Keggin hybrids towards oxidations of ascorbic acid. Furthermore, the molecular electrostatic potential and frontier molecular orbital were performed. (c) 2021 Elsevier Ltd. All rights reserved.
To develop effective anti-tumor and analgesic drugs, a series of novel 7-azaindole derivatives were designed and synthesized through a four-step reaction. 18 target compounds were obtained and characterized through Nuclear Magnetic Resonance and High Resolution Mass Spectrometry. Their anti-proliferative activities and analgesic effect were evaluated. When the 1-position was a methylsulfonyl group and the 5-position was a nitro group, compound 4f demonstrated the best activity. Furthermore, there was a dramatic difference between the IC50 values of compound 4f in tumor and in healthy cell line. The IC50 values of compound 4f in MCF7 breast cancer cell line was 5.781 μmol/L and 8.077 μmol/L in HepG2 hepatoma carcinoma cell line, but more than 100 μmol/L in HL7702 liver cell line. Preliminary results showed that compounds 3a, 3g and 4i had significant analgesic effects in mice, which were stronger than aspirin. These compounds have good prospects for new drug development.
目的 考察葛花水提物的抗疲劳作用.方法 将健康昆明种小鼠,随机平均分成4组,灌胃给葛花提取物的高、中、低三个浓度组及空白对照组.连续给药15d后分别进行疲劳转棒实验测试和负重游泳实验测定,并测定小鼠的肝糖原含量.结果 给药组较对照组均有增加运动耐力时间、游泳时间、肝糖原含量的作用.结论 葛花水提取物具有明显的抗疲劳作用.
以通化师范学院药学类专业为例,探讨"互联网+"背景下地方高校创新创业教育和专业教育互融的做法与经验,以进一步提升地方高校药学类专业人才综合创新能力,培育适应地方经济发展要求的高素质应用型人才.
In the present investigation, a series of dihydrotriazine derivatives-bearing 5-aryloxypyrazole moieties were synthesized and their structures were confirmed by different spectral tools. The biological evaluation in vitro revealed that some of the target compounds exerted good antibacterial and antifungal activity in comparison with the reference drugs. Among these novel hybrids, compound 10d showed the most potent activity with minimum inhibitory concentration values (MIC) of 0.5 µg/mL against S. aureus 4220, MRSA 3506 and E. coli 1924 strain. The cytotoxic activity of the compounds 6d, 6m, 10d and 10g was assessed in MCF-7 and HeLa cells. Growth kinetics study showed significant inhibition of bacterial growth when treated with different conc. of 10d. In vitro enzyme study implied that compound 10d exerted its antibacterial activity through DHFR inhibition. Moreover, significant inhibition of biofilm formation was observed in bacterial cells treated with MIC conc. of 10d as visualized by SEM micrographs. Twenty-nine target compounds were designed, synthesized and evaluated in terms of their antibacterial and antifungal activities.
"药理学"课程主要是研究药物与机体相互作用及作用规律的一门课程,属于药学类专业重要的专业核心课程之一.在"互联网+"背景下,将创新创业教育与"药理学"课程教学内容融合,是地方高校深化创新创业教育改革的重要实践.笔者从"药理学"课程教学实践出发,改革教学方法,结合"互联网+"教育模式、创业类课程教育及创新创业实践训练,有效提升了学生互联网思维、商科思维及实践能力、创新能力和科学研究能力.
C23H21NO6, triclinic, P1̄ (no. 2), a = 7.624(4) Å, b = 9.197(5) Å, c = 15.058(5) Å, α = 94.13(3)°, β = 102.27(3)°, γ = 106.72(3)°, V = 977.9(8) Å3, Z = 2, Rgt(F) = 0.0662, wRref(F2) = 0.1733, T = 296(2) K.