OBJECTIVE:To evaluate the anti-inflammatory activity and mechanism of Panaxadiol saponins (PDS), develop a PDS-based gel for periodontitis treatment, and evaluate its therapeutic efficacy using a rat model of periodontitis. METHODS:The anti-inflammatory effects of PDS were assessed using LPS-induced RAW264.7 cells. ELISA and RT-qPCR were performed to detect inflammatory factors; Western blotting analyzed MAPK/NF-κB pathway-related proteins. A single-factor experiment was used to examine the effects of the dosages of carbomer 940, propylene glycol, and triethanolamine on the properties of the PDS gel and to evaluate its in vitro release versus in vitro permeation and retention on oral mucosa. A rat periodontitis model was established by ligation plus high-sugar feeding, and the efficacy of PDS gel in ameliorating periodontitis in rats was evaluated using gingival index scoring, micro-CT, HE staining, ELISA, and RT-qPCR to assess the state of periodontal tissues and inflammatory responses, and salivary microbiota analysis using 16S rRNA sequencing. RESULTS:PDS significantly reduced NO, IL-6, IL-1β, and TNF-α release, inhibited their mRNA expression, and suppressed MAPK/NF-κB pathway-related proteins in LPS-induced RAW264.7 cells. The PDS gel exhibited good physicochemical properties, release performance, and mucosal permeability. PDS gel decreased gingival index, attenuated alveolar bone loss, reduced inflammatory cell infiltration, and lowered IL-6, IL-1β, TNF-α, and RANKL mRNA levels in serum and periodontal tissue. It also regulated and restored the balance of salivary flora. CONCLUSION:PDS gel can inhibit the MAPK/NF-κB pathway-mediated inflammatory response, reduce bone destruction, and regulate bacterial dysbiosis, demonstrating good therapeutic prospects for periodontitis.

INTRODUCTION:To overcome the poor oral bioavailability of Panax Notoginseng Saponins (PNS) caused by low permeability and acid instability, this study designed bioadhesive microspheres co-loaded with PNS and N-acetyl-L-cysteine (PNS-NAC-BMS). This system aims to protect PNS from gastric degradation and enhance its intestinal permeability and oral bioavailability. METHODS:PNS-NAC-BMS were fabricated via solvent evaporation and characterized for morphology, particle size, drug loading, encapsulation efficiency, mucoadhesion, and in vitro release. Permeability was assessed using Purified Mucin Intestinal Mucus (PIM), Artificial Intestinal Mucus (AIM), and Rat Native Intestinal Mucus (RIM). Oral bioavailability was assessed through rat pharmacokinetic studies. RESULTS:PNS-NAC-BMS exhibited spherical morphology with uniform particle sizes. They achieved high encapsulation efficiency (91.55%) and intestinal adhesion (94.83%), with sustained release. The system showed high apparent permeability coefficients across three models (PIM, AIM, RIM). Pharmacokinetic studies revealed prolonged release and a 2.6-fold increase in oral bioavailability versus PNS Active Pharmaceutical Ingredients (PNS APIs). DISCUSSION:Recently, patents (US 20230338448, CN 118873498) describe PNS delivery using nanocomposites and liposomes. However, none exist for NAC-modified adhesive microspheres, underscoring the novelty of this study. The BMS system significantly improves the oral bioavailability through combined mucoadhesion and NAC-mediated penetration. NAC promotes drug transport across the mucus barrier by cleaving mucin disulfide bonds and increasing lipid solubility. However, promising long-term stability, scalable production, and mucosal safety of NAC require further study. CONCLUSION:PNS-NAC-BMS significantly enhanced intestinal adhesion and sustained drug release, thereby synergistically improving intestinal mucus permeability and oral bioavailability, demonstrating potential as an effective oral drug delivery system.

Background: Acute lung injury (ALI) is a severe inflammatory condition characterized by dysregulated immune responses and high mortality rates, with limited effective therapeutic options currently available. Panax notoginseng saponins (PNS), bioactive compounds derived from Panax notoginseng, have shown promise in mitigating lipopolysaccharide (LPS)-induced ALI. However, the molecular mechanisms underlying their therapeutic effects remain poorly understood. Given the critical role of M2-like macrophage polarization in resolving inflammation and promoting tissue repair, we investigated whether PNS exerts its protective effects in ALI by modulating this process. Furthermore, we explored the specific involvement of the signal transducer and activator of transcription 6 (STAT6) pathway in mediating these effects. Methods: Chemical profiling of PNS was performed using ultra-performance liquid chromatography-quadrupole time-of-flight mass spectrometry (UPLC-Q-TOF-MS), followed by quantitative analysis of its major bioactive components via high-performance liquid chromatography (HPLC). To evaluate the therapeutic efficacy of PNS and its principal constituents, we established an ALI mouse model through intratracheal administration of LPS. Comprehensive assessments included lung field shadowing, oxygen saturation levels, pulmonary function, and systematic histopathological examination. The regulatory effects of PNS on macrophage polarization were examined in THP-1 cells and bone marrow-derived macrophages (BMDMs), with cellular phenotypes analyzed by flow cytometry. To elucidate the mechanistic role of STAT6 in PNS-mediated protection, experiments were conducted using Stat6-deficient BMDMs and Stat6 knockout mice. Results: UPLC-Q-TOF-MS and HPLC identified and quantified the principal components of PNS: Notoginsenoside R1, Ginsenoside Rg1, Ginsenoside Re, and Ginsenoside Rb1. PNS treatment dose-dependently reduced inflammatory responses in LPS-induced ALI mice, as evidenced by decreased cytokine levels. Each of the four major PNS components independently alleviated ALI symptoms in mice. Pathway analysis revealed 56 potential ALIrelated targets, with Kyoto Encyclopedia of Genes and Genomes (KEGG) enrichment suggesting that PNS exerts its protective effects by modulating inflammatory signaling pathways. In vitro studies demonstrated that PNS promoted STAT6 phosphorylation and nuclear translocation, enhancing M2-like macrophage polarization and interleukin-10 (IL-10) secretion in a STAT6-dependent manner. Genetic ablation of Stat6 partially reversed the protective effects of PNS on ALI, macrophage polarization, and IL-10 production, confirming the pivotal role of STAT6 in mediating PNS activity. Conclusion: This study demonstrates that PNS alleviates LPS-induced ALI by promoting STAT6-dependent M2-like macrophage polarization, highlighting its potential as a therapeutic agent for ALI. These findings provide mechanistic insights into the anti-inflammatory actions of PNS and underscore the importance of STAT6 signaling in its protective effects.

This study systematically analyzed the molecular mechanism and function of nuclear factor kappa B subunit 2 (NFKB2) in colorectal cancer (CRC) to investigate the potential of NFKB2 as a therapeutic target for CRC. Various experimental techniques, including RNA sequencing, proteome chip assays, and small molecule analysis, were used to obtain a deeper understanding of the regulation of NFKB2 in CRC. The results revealed that NFKB2 was upregulated in a significant proportion of patients with advanced hepatic metastasis of CRC. NFKB2 played an important role in promoting tumor growth through CD8+ T-cell exhaustion. Moreover, NFKB2 directly interacted with signal transducer and activator of transcription 2 (STAT2), leading to increased phosphorylation of STAT2 and the upregulation of programmed death ligand 1 (PD-L1). Applying a small molecule inhibitor of NFKB2 (Rg5) led to a reduction in PD-L1 expression and improved response to programmed death-1 blockade-based immunotherapy. In conclusion, the facilitated NFKB2-STAT2/PD-L1 axis may suppress immune surveillance in CRC and targeting NFKB2 may enhance the efficacy of immunotherapeutic strategies. Our results provide novel insights into the molecular mechanisms underlying the contribution of NFKB2 in CRC immune escape.

Ulcerative colitis (UC) is a chronic and non-specific inflammatory bowel disease that poses a serious threat to individuals' health and lives. Notoginsenoside R1 (R1) alleviates various symptoms caused by UC effectively. However, the application of R1 is somewhat restricted due to its low bioavailability and nontargeted delivery in vivo. Consequently, it is imperative to develop novel strategies to overcome the aforementioned limitations and enhance the efficacy of this drug. To enhance R1's efficacy and targeting ability, polyethylene glycol poly (lactic-co-glycolic acid) nanoparticles loaded with R1 (R1@PEG–PLGA NPs) modified by transferrin (Tf) were prepared in this study and named R1@Tf–PEG–PLGA NPs. R1@PEG–PLGA NPs and R1@Tf–PEG–PLGA NPs were prepared through nanoprecipitation, and the characterization methods were as follows: First, the surface morphology of the NPs was studied through transmission electron microscopy. Second, particle size, polydispersity index (PDI), and zeta potential were measured with a Malvern particle size analyzer, and the Tf grafting rate on the surface of the NPs was determined by using a bicinchoninic acid protein quantification kit. Third, high-performance liquid chromatography was used in determining the drug load (DL), entrapment efficiency (EE), and in vitro release of the prepared preparation. In addition, the fluorescence intensities of fluorescent-labeled NPs absorbed and ingested in Caco-2 cells were observed through in vitro experiments using fluorescence microscopy; the effects of incubation time, incubation temperature, and endocytosis inhibitors on the uptake of nanoparticles were compared; and the uptake-transport mechanism was explored. Finally, in vivo experiments were performed using the oxazolone (OXZ)-induced UC model in Sprague–Dawley (SD) rats to assess the pharmacodynamic effects and tissue distribution of the prepared NPs. The experimentally prepared R1@Tf–PEG–PLGA NPs were round particles with particle size and PDI of 153.50 ± 2.01 and 0.11 ± 0.01, respectively. In addition, the DL of R1@Tf-PEG-PLGA NPs was 24.26

Twenty-one previously undescribed compounds, including nineteen 3,4-seco-labdanes (nudiflopenes P-W, Y, AI-JI), one 3,4-seco-pimarane (nudiflopene X), and one labdane (nudiflopene Z), along with nine known compounds (one 3,4-seco-pimarane and eight 3,4-seco-labdanes) were isolated from the leaves of Callicarpa nudiflora Hook. Et Arn. The structures of these compounds were elucidated by high-resolution electrospray ionization mass spectrometry and one- and two-dimensional nuclear magnetic resonance spectroscopy. In addition, configurations of the isolated compounds were determined by electronic circular dichroism, DP4+ probability analysis, and single-crystal X-ray diffraction experiments. All undescribed compounds were evaluated for their cytotoxicity against HepG2 cells in vitro, among which compound 12 exhibited a moderate activity with an IC50 value of 27.8 μM.

目的 建立一测多评法同时测定肾康宁胶囊中丹参素、迷迭香酸、原儿茶醛、紫草酸、丹酚酸 B 的含量.方法 该药物 50%甲醇提取液的分析采用DIKMA Diamonsil Plus C18-A色谱柱(250 mm×4.6 mm,5 μm);流动相甲醇-乙腈-0.1%磷酸,梯度洗脱;体积流量 1.0 mL/min;柱温 30℃;检测波长 230 nm.以迷迭香酸为内标,计算其他4 种酚酸的相对校正因子,测定其含量.结果 5 种酚酸在各自范围内线性关系良好(r≥0.999 5),平均加样回收率98.29%～102.9%,RSD 0.11%～1.99%,一测多评法所得结果与外标法一致.结论 该方法简便稳定,重复性好,可用于肾康宁胶囊的质量控制.

In this work, self-double-emulsifying drug delivery system enteric-coated capsules (PNS-SDE-ECC) were used to enhance the oral bioavailability and anti-inflammatory effects of Panax notoginseng saponins (PNS), which are rapidly biodegradable, poorly membrane permeable, and highly water-soluble compounds. The PNS-SDEDDS formulated by a modified two-step method spontaneously emulsified to W/O/W double emulsions in the outer aqueous solution, which significantly promoted the absorption of PNS in the intestinal tract. The release study revealed that PNS-SDE-ECC exhibited sustained release of PNS within 24 h and the stability study indicated that PNS-SDE-ECC were stable at room temperature for up to 3 months. Furthermore, compared to PNS gastric capsules, the relative bioavailability of NGR1, GRg1, GRe, GRb1, and GRd in PNS-SDE-ECC was increased by 4.83, 10.78, 9.25, 3.58, and 4.63 times, respectively. More importantly, PNS-SDE-ECC significantly reduced OXZ-induced inflammatory damage in the colon by regulating the expression of TNF-α, IL-4, IL-13, and MPO cytokines. Overall, the prepared PNS-SDE-ECC may serve as a viable vehicle for increasing the oral bioavailability of PNS and its anti-inflammatory action on ulcerative colitis.

目的 通过前期建立的3种体外肠黏液渗透模型[纯化黏蛋白渗透模型(PIM)、人工肠黏液渗透模型(AIM)及大鼠肠黏液渗透模型(RIM)],研究三七中主要单体成分三七皂苷R1、人参皂苷Rg1和人参皂苷Rb1在肠黏液层的渗透作用,以期为三七皂苷类成分的口服吸收及应用提供实验依据.方法 采用高效液相色谱(HPLC)法建立三七皂苷R1、人参皂苷Rg1和人参皂苷Rb1的定量分析方法,并对其线性范围、精密度、稳定性、重复性、加样回收率进行考察;分别测定不同浓度三七皂苷R1、人参皂苷Rg1和人参皂苷Rb1溶液在3种肠黏液渗透模型上的表观渗透系数(Papp),分析比较其肠黏液渗透作用.结果 建立了三七皂苷R1、人参皂苷Rg1和人参皂苷Rb1的HPLC定量分析方法,精密度、稳定性、重复性、加样回收率均符合要求.3种皂苷成分在PIM、AIM、RIM模型的渗透性结果显示:三七皂苷R1、人参皂苷Rg1和人参皂苷Rb1在3种模型上的渗透作用随着药物浓度的升高均有不同程度的增加;在PIM中,与人参皂苷Rb1和人参皂苷Rg1相比,三七皂苷R1在不同浓度下的Papp均显著增加(P<0.05);在AIM中,20 g·L-1浓度下的Papp为三七皂苷R1>人参皂苷Rb1>人参皂苷Rg1(P<0.05);在RIM中,20 g·L-1浓度下的Papp为人参皂苷Rg1>三七皂苷R1>人参皂苷Rb1(P<0.05).结论 不同浓度的三七皂苷R1、人参皂苷Rg1和人参皂苷Rb1在3种肠黏液渗透模型中的稳定性、重现性较好,且随着药物浓度的上升渗透性也随之增加;水溶性较强且分子量相对较小的三七皂苷R1在脂类成分较少的PIM和AIM中渗透作用较强,而脂溶性较强的人参皂苷Rg1在RIM中渗透作用较强.

A phytochemical investigation of the dichloromethane soluble fraction of the ethanolic extract obtained from the roots of Marsdenia tenacissima led to the discovery of the sixteen undescribed pregnane C21 steroids (1-16) and isolation of eleven known C21 steroidal analogues (17-27). Their chemical structures were elucidated by one -and two-dimensional nuclear magnetic resonance spectroscopy and, high resolution-electrospray ionization mass spectrometry and their absolute configurations were determined using electronic circular dichroism or single-crystal X-ray diffraction. The in vitro anti-proliferative effects of 1-16 were evaluated against HepG2 (human hepatocellular cancer), A549 (lung cancer), and MCF-7 (human breast cancer) cell lines. Even though some of them showed moderate cytotoxic activities, marsectohexol derivative 12 exhibited significant cyto-toxicity against A549 cells with an IC50 value of 5.2 & mu;M.

Notoginsenoside R1 (R1), which originated from the rhizomes and roots of Panax notoginseng, is classified as a Biopharmaceutical Classification System class III drug with good solubility but poor oral absorption. Although R1 can alleviate the inflammation of dextran sulfate sodium (DSS)induced colitis in mice, the problem of acid degradation and low bioavailability limit its application. The purpose of this study was aimed to design one kind of pH-dependent solid dispersion for oral colon-targeted delivery of R1. Using Eudragit S100 (ES 100) and PEG 4000 as the pHdependent carriers, R1 solid dispersion (R1-SD) was fabricated by solvent evaporation method. Scanning electron microscopy, differential scanning calorimetry, and powder X-ray diffraction analysis indicated that R1-SD was completely formed, the surface was smooth surface and the strip crystal structure of R1 disappeared. The in vitro release profile of R1-SD (R1-ES 100-PEG 4000, 1:7:1, weight ratio) exhibited that R1-SD was not released in media simulating the gastric condition (pH 1.2), but better release characteristics of the drug could be obtained in media simulating the intestinal condition (less than 30% in pH 6.8 phosphate-buffered saline and more than 90% in pH 7.6 condition). The in vitro colon absorption test showed that the absorption rate and cumulative release of R1-SD were higher than those of R1. R1-SD and R1 had apparent protective effect on colon shortening, inflammatory infiltrating tissue injury, weight loss, diarrhea, blood stool in mice with ulcerative colitis induced by DSS, and the protective effect of R1-SD was better than that of R1, which indicated R1-SD has good practical application prospects.

Six new abietane diterpenoids (1-6) and five undescribed iridoids (7-11) have been isolated from the aerial parts of Caryopteris mongolica. The intricate structural characterization of these compounds was meticulously undertaken using an array of advanced spectroscopic techniques. This process was further enhanced by the application of DP4+ probability analyses and electronic circular dichroism (ECD) calculations. Following isolation and structural elucidation, the cytotoxicity of these compounds was evaluated. Among them, compound 3 stood out, displaying significant cytotoxic activity against HeLa cells with an IC50 value of 7.83 ± 1.28 μmol·L-1. Additionally, compounds 1, 2, 4, 9, and 10 manifested moderate cytotoxic effects on specific cell lines, with IC50 values ranging from 11.7 to 20.9 μmol·L-1.

This study describes the isolation and identification of two novel phenylethanoid glycosides, aureoglanduloside A (1) and aureoglanduloside B (2), as well as a newly discovered diterpene glycoside, aureoglanduloside C (29). Additionally, 31 known compounds were isolated from the n-butyl alcohol (BuOH) soluble fraction of Caryopteris aureoglandulosa whole dried plants. Their structures were characterized using various spectroscopic techniques and high-resolution electrospray ionization mass spectroscopy (HR-ESI-MS). Furthermore, the neuroprotective effects of all phenylethanoid glycosides were evaluated. Specifically, compounds 2 and 10-12 exhibited the ability to promote the phagocytosis of myelin by microglia, and compounds 2, 10-11, and 24 showed the ability to promote the phagocytosis of myelin by astrocytes.

ETHNOPHARMACOLOGICAL RELEVANCE:Diabetic retinopathy (DR) is a neurovascular disease that causes blindness in adults and is the most serious and common complication of diabetes mellitus. Retinal inflammation is an early stage of DR, and it is believed to play a crucial role in the development of DR. Panax notoginseng saponins (PNS) are the major active constituent in the main root of P. notoginseng, and they exhibit various biological activities, including anti-inflammatory, antioxidant, neuroprotective, and immunomodulatory functions. However, the protective effects and underlying mechanisms of PNS against DR remain unclear. AIM OF THE STUDY:This study aimed to investigate the alleviation effects of PNS on DR and the mechanisms involved. Furthermore, it intended to explore the major components that exert efficacy in vivo. MATERIALS AND METHODS:Streptozotocin (STZ) was administered intraperitoneally to Sprague Dawley rats, and PNS was administered orally for 1 month after 2 months of STZ injection. The morphological structure of the retina and retinal acellular capillaries were assessed via hematoxylin and eosin (H&E) staining assay. The disruption of the blood-retinal barrier (BRB) was detected through Evans blue dye leakage assay, and retinal leukocyte adhesion was achieved via fluorescein isothiocyanate-coupled concanavalin A lectin labeling assay. Immunofluorescence staining and Western blot assays were conducted to detect the expression of tight junction proteins, adhesion molecules, and the ionized calcium-binding adapter molecule-1 (Iba-1) in the retina. Enzyme-linked immunosorbent assay was performed to detect the levels of tumor necrosis factor (TNF)-α, interleukin (IL)-6, and IL-1β in serum. In addition, the protein expression levels of nuclear factor (NF)-κB p65, phosphorylated IκB kinase (p-IKK), phosphorylated NF-κB inhibitor (p-IκB), and phosphorylated NF-κB p65 (p-p65) were measured using Western blot assay. The ocular tissue distribution of PNS in normal and diabetic rats was determined through ultra-performance liquid chromatography-tandem mass spectrometry. The in vitro anti-inflammatory effects of PNS, notoginsenoside (NGR1), ginsenoside Rg1, Re, Rb1, and Rd (GRg1, GRe, GRb1, and GRd) were evaluated on human Müller (MIO-M1) cells. RESULTS:PNS increased the reduction in retinal inner nuclear layer thickness, reduced the increase in retinal acellular capillaries, and attenuated elevated BRB disruption by upregulating the decrease in protein expression of claudin-1 and occludin. Furthermore, PNS significantly abrogated microglial cell activation and reversed the increase in leukocyte adhesion by downregulating the increase in the protein expression of intercellular adhesion molecule-1 and vascular cell adhesion molecule-1. Moreover, PNS reduced the elevated levels of TNF-α, IL-6, and IL-1β in serum and inhibited the increased protein expression of p-IKK, p-IκB, and p-p65, and the nuclear translocation of p65. The tissue distribution results revealed that NGR1, GRg1, GRe, GRb1, and GRd were detected in the ocular tissue, while GRg1 and GRb1 were found at the highest levels compared with the other components. The cellular results showed that PNS, NGR1, GRg1, GRe, GRb1, and GRd suppressed the development of cellular inflammatory responses by inhibiting the activation of the NF-κB signaling pathway in MIO-M1 cells and that their anti-inflammatory effects were comparable. CONCLUSION:PNS suppressed retinal inflammation by inhibiting the activation of the NF-κB signaling pathway, alleviating DR. GRg1 and GRb1 may be the primary components that exert anti-inflammatory effects in vivo.

Notoginsenoside R1 (NGR1) is the main monomeric component extracted from the dried roots and rhizomes of Panax notoginseng, and exerts pharmacological action against myocardial infarction (MI). Owing to the differences in compound distribution, absorption, and metabolism in vivo, exploring a more effective drug delivery system with a high therapeutic targeting effect is crucial. In the early stages of MI, CD11b-expressing monocytes and neutrophils accumulate at infarct sites. Thus, we designed a mesoporous silica nanoparticle-conjugated CD11b antibody with loaded NGR1 (MSN-NGR1-CD11b antibody), which allowed NGR1 precise targeted delivery to the heart in a noninvasively manner. By increasing targeting to the injured myocardium, intravenous injection of MSN-NGR1-CD11b antibody nanoparticle in MI mice improved cardiac function and angiogenesis, reduced cell apoptosis, and regulate macrophage phenotype and inflammatory factors and chemokines. In order to further explore the mechanism of NGR1 protecting myocardium, cell oxidative stress model and oxygen-glucose deprivation (OGD) model were established. NGR1 protected H9C2 cells and primary cardiomyocytes against oxidative injury induced by H2O2 and OGD treatment. Further network pharmacology and molecular docking analyses suggested that the AKT, MAPK and Hippo signaling pathways were involved in the regulation of NGR1 in myocardial protection. Indeed, NGR1 could elevate the levels of p-Akt and p-ERK, and promote the nuclear translocation of YAP. Furthermore, LY294002 (AKT inhibitor), U0126 (ERK1/2 inhibitor) and Verteporfin (YAP inhibitor) administration in H9C2 cells indicated the involvement of AKT, MAPK and Hippo signaling pathways in NGR1 effects. Meanwhile, MSN-NGR1-CD11b antibody nanoparticles enhanced the activation of AKT and MAPK signaling pathways and the nuclear translocation of YAP at the infarcted site. Our research demonstrated that MSN-NGR1-CD11b antibody nanoparticle injection after MI enhanced the targeting of NGR1 to the infarcted myocardium and improved cardiac function. More importantly, our pioneering research provides a new strategy for targeting drug delivery systems to the ischemic niche.

目的:建立肾康宁胶囊中乌头类生物碱的含量测定方法.方法:采用Waters ACQUITY UPLC HSS T3色谱柱(2.1 mm×100 mm,1.8 μm),以0.1％甲酸水溶液(A)-乙腈(B)为流动相,梯度洗脱,流速0.3 mL·min-1,柱温40℃;质谱采用电喷雾离子化源(ESI),正离子模式下选择多反应监测(MRM)模式检测,建立同时测定肾康宁胶囊中乌头碱、新乌头碱、次乌头碱、苯甲酰乌头原碱、苯甲酰新乌头原碱、苯甲酰次乌头原碱、乌头原碱和新乌头原碱8个生物碱含量的固相萃取(SPE)辅助UPLC-MS/MS分析方法.结果:乌头碱、新乌头碱、次乌头碱、苯甲酰乌头原碱、苯甲酰新乌头原碱、苯甲酰次乌头原碱、乌头原碱、新乌头原碱分别在0.31～99.80、0.78～99.80、0.31～75.15、30.31～485.00、309.38～3 712.50、61.88～742.50、7.75～248.00、61.25～1 960.00 ng·mL-1的质量浓度范围内线性关系良好,精密度、重复性和稳定性的RSD均小于5％,加样回收率在80.6％～109.0％之间.12批胶囊中次乌头碱、苯甲酰乌头原碱、苯甲酰新乌头原碱、苯甲酰次乌头原碱、乌头原碱和新乌头原碱含量范围分别为0.002～0.041、1.163～1.758、9.300～16.446、2.070～3.112、0.166～0.319、1.243～3.067 μg·粒-1.结论:建立的方法稳定可靠,可用于肾康宁胶囊的质量控制.

目的 建立鲜百合质量控制方法.方法 采用TLC法对鲜百合进行定性鉴别,HPLC法测定王百合苷B含量;参照2015年版《中国药典》方法,测定水分、总灰分和浸出物含量.结果 TLC定性鉴别采用硅胶G板,以石油醚-二氯甲烷-乙酸乙酯-甲醇(7∶10∶7∶2)为展开系统,10％硫酸乙醇显色,365 nm下检视:鲜百合样品与对照药材在相同位置呈现相同颜色斑点,斑点清晰,重复性好;HPLC含量测定采用Agilent C18色谱柱(4.6 mm×250 mm,5 μm),在流动相乙腈-0.1％磷酸(17 ∶83)、检测波长312 nm、柱温25℃、流速1.0 mL/min、进样量20 μL条件下,王百合苷B在10.27～164.32 mg/L范围内线性关系良好(R2 = 0.999 7),平均加样回收率为100.08％(RSD为2.31％).20批样品中,王百合苷B含量0.62～4.71 mg/g;鲜百合粉末水分、总灰分和水溶性浸出物范围分别为7.53％～10.22％、2.63％～4.88％和23.07％～43.01％.结论 本研究建立的鲜百合质量控制方法准确稳定,重复性好,可用于鲜百合的质量控制.

目的:采用单因素试验与正交试验优化转铁蛋白(Tf)修饰的负载三七皂苷R1的PEG-PLGA纳米粒(R1@Tf-PEG-PLGA NPs)的制备工艺,并对其质量进行评价.方法:采用纳米沉淀法制备负载三七皂苷R1的PEG-PLGA纳米粒(R1@PEG-PLGA NPs),通过单因素试验与正交试验优选其最佳制备条件.将Tf共价偶联在纳米粒表面,制得R1@Tf-PEG-PLGA NPs.以Tf接枝率为指标,通过单因素试验优选其制备条件.采用激光粒度仪和透射电子显微镜对纳米粒进行形态表征及理化参数测定.采用透析法进行纳米粒体外释药研究,并对释药过程进行动力学模型拟合.结果:制得的R1@Tf-PEG-PLGA NPs形态圆整、分散性良好,粒径(153.50±2.01)nm,多分散指数0.11±0.01,Zeta 电位(-17.57±1.45)mV,包封率(50.32±0.86)％,载药量(24.26±0.18)％,蛋白接枝率(42.09±0.62)％.药物24 h累积释放率＞80％,体外释放过程符合Riger-Peppas动力学模型.结论:制得的R1@Tf-PEG-PLGA NPs粒径均一,包封率与载药量适宜,能够延缓药物的释放.

目的 建立超高效液相色谱-串联质谱(UPLC-MS/MS)法同时测定大鼠口服三七总皂苷后血浆中三七皂苷R1、人参皂苷Rg1、人参皂苷Re、人参皂苷Rb 1、人参皂苷Rd的含量.方法 以柴胡皂苷A为内标,蛋白沉淀法对血浆样品进行处理.色谱柱:ACQUITY BEH C18柱(100 mm×2.1 mm,1.7μm),流动相:乙腈-0.1％甲酸水溶液,梯度洗脱,流速:0.4 mL·min-1.采用电喷雾离子源,负离子模式及多反应监测模式.考察该方法的专属性、标准曲线与定量下限、精密度、提取回收率、基质效应和稳定性.结果 UPLC-MS/MS法检测三七皂苷R1、人参皂苷Rg1、人参皂苷Re、人参皂苷Rb1、人参皂苷Rd的标准曲线线性范围分别是2.01～1005.50,1.94～964.80,1.94～969.50,1.85～926.60,1.93～965.20 ng·mL-1,批内与批间精密度分别为0.96％～7.59％、0.77％～7.16％,提取回收率为85.01％～101.99％;基质效应为92.48％～105.81％;在设定的各种条件下稳定性良好.结论 建立的UPLC-MS/MS分析方法简便、快捷,适用于大鼠血浆中三七皂苷R1、人参皂苷Rg1、人参皂苷Re、人参皂苷Rb1、人参皂苷Rd的含量测定.