Peptide functionalization offers a way to improve nanocarrier transport across tissue and cellular barriers, but performance remains limited by competing interfacial requirements across the delivery cascade. Surface shielding supports circulation, whereas peptide exposure is needed for stromal access, membrane interaction, or endosomal escape. Cell-penetrating peptides (CPPs) and tissue-penetrating peptides (TPPs) contribute to different steps of delivery, and their function depends not only on peptide sequence but also on carrier architecture, ligand presentation, and the barrier being addressed. This review addresses membrane-associated entry of CPP-functionalized carriers, tissue-level transport mediated by TPPs, and dynamic surface designs that separate systemic stability from local activity. It also examines why commonly used experimental measurements do not provide equivalent evidence of delivery, and why accumulation, penetration, uptake, and functional intracellular access should be interpreted separately. Formulation heterogeneity, model dependence, reproducibility, and translational safety are discussed as practical constraints on the development of peptide-functionalized nanocarriers.

BCS Class II drugs, with low solubility and high permeability, face bioavailability challenges due to dissolution limitations. Improving solubility and generating supersaturation using amorphous forms is a promising approach, but amorphous systems are thermodynamically unstable and prone to recrystallization. This study evaluated the impact of four preparation methods including solvent evaporation (SE), melt cooling (MC), freeze-drying (FD), and hot-melt extrusion (HME) on the supersaturation stability and dissolution dynamics of felodipine (FEL)/copovidone (COP) amorphous solid dispersions (ASDs). SEM, PXRD, and DSC analyses showed similar amorphous properties of these ASDs, and HME resulted in the highest solubility but lower initial dissolution. "Spring-parachute" studies demonstrated that HME-based ASDs had superior supersaturation, including a 2.62-fold increase in Cmax and the longest supersaturation duration from AUCspring-parachute measurement. FT-IR analysis suggested that crystallization inhibition in HME-made ASD was due to the dense microstructure and rapid polymer swelling, rather than drug–polymer interactions. Collectively, this work establishes clear “preparation methods–performance” relationship and provides practical guidelines for adopting HME-based heat-driven process to design supersaturating FEL/COP ASDs with high supersaturation stability in practical pharmaceutical industry.

BCS Class II drugs, with low solubility and high permeability, face bioavailability challenges due to dissolution limitations. Improving solubility and generating supersaturation using amorphous forms is a promising approach, but amorphous systems are thermodynamically unstable and prone to recrystallization. The research clarified the impact of heat-driven and non-heat-driven processes on dissolution/solubility improvement and supersaturation extension of a particular amorphous supersaturating delivery system such as felodipine (FEL)/copovidone (COP) amorphous solid dispersions (ASDs). Heat-driven processes include melt cooling (MC) and hot-melt extrusion (HME), and non-heat-driven processes are associated with solvent evaporation (SE) and freeze-drying (FD). Scanning electron microscopy, powder X-ray diffraction, and differential scanning calorimetry analyses showed microscopic morphology and amorphous properties of these ASDs. MC-based and HME-based heat-driven processes caused the strongest dissolution and solubility improvement, respectively. FD-based and SE-based non-heat-driven process resulted in weakest dissolution and solubility improvement, respectively. In ASD made system by HME-based heat-driven process, the most remarkable crystallization inhibition effect was observed, and the inhibition depended on amount of COP polymer added. "Spring-parachute" studies demonstrated that ASD made by heat-driven processes had superior supersaturation extension, presenting the longer supersaturation duration from AUCspring-parachute measurement. FT-IR analysis strongly suggested the formation of significant molecular interactions between FEL and COP in the all FEL/COP ASD systems made by heat-driven process and non-heat-driven processes. In summary, this work clarified the impact of heat-driven and non-heat-driven processes on dissolution/solubility improvement and supersaturation extension of amorphous felodipine-copovidone supersaturating systems. It is also helpful to provide practical guidelines for adopting these heat-driven processes (esp. HME) to design a particular supersaturating delivery system (FEL/COP ASDs) with superior supersaturation extension ability in practical pharmaceutical industry.

Neurodegenerative diseases bring heavy burden to our society. Methylmercury (MeHg) is a potent neurotoxin and causes neurodegenerative diseases like Minamata Disease. Therefore, finding ways to combat MeHg-induced neurodegeneration may shed light on the treatment of neurodegenerative diseases. This study investigated the efficacy of bismuth selenide nanoparticles (Bi2Se3NPs, nBS) in treating MeHg-induced neurodegeneration. MeHg-poisoned rats were orally given nBS (4 mg/kg) every other day for 21 days and then sacrificed. It was found that nBS improved neurobehavioral performance, alleviated hippocampus damage and intestinal barrier damage, reduced Hg accumulation, and promoted MeHg demethylation in MeHg-poisoned rats. In addition, nBS up-regulated the abundance of gut microbes such as Faecalibacterium, Bifidobacterium and Akkermansiaceae, and increased the levels of butyric acid in feces while reduced the concentration of isobutyric acid in the brains. At the same time, nBS reduced the secretion of inflammatory factors IL-6 and TNF-α in the brains, guts and serum, and regulated AHR/IDO expression in the guts and brains. In all, nBS treatment improved the health status of MeHg-poisoned rats through enhancing Hg excretion and MeHg demethylation, reshaping gut microbiota, and reducing neuroinflammation. These findings suggested that nBS supplementation is a promising approach to treat MeHg-induced neurodegeneration, which may shed lights on the treatment of neurodegenerative diseases.

Bone tissue is a biological composite material with a complex hierarchical structure that could continuously adjust its internal structure to adapt to the alterations in the external load environment. The fluid flow within bone is the main route of osteocyte metabolism, and the pore pressure as well as the fluid shear stress generated by it are important mechanical stimuli perceived by osteocytes. Owing to the irregular multiscale structure of bone tissue, the fluid stimulation that lacunar-canalicular network (LCN) in different regions of the tissue underwent remained unclear. In this study, we constructed a multiscale conduction model of fluid flow stimulus signals in bone tissue based on the poroelasticity theory. We analyzed the fluid flow behaviors at the macro-scale (whole bone tissue), macro-meso scale (periosteum, interstitial bone, osteon and endosteum), and micro-scale (lacunar-osteocyte-canalicular) levels. We explored how fluid stimulation at the tissue level correlated with that at the cellular level in cortical bone and characterized the distributions of the pore pressure, fluid velocity and fluid shear stress that the osteocytes experienced across the entire tissue structure. The results showed that the initial conditions of intramedullary pressure had a significant impact on the pore pressure of Haversian systems, but had a relatively small influence on the fluid velocity. The osteocyte which were located at different positions in the bone tissue received very distinct fluid stimuli. Osteocytes in the vicinity of the Haversian Canals experienced higher fluid shear stress stimulation. When the permeability of the LCN was within the range from 10_21 m2 to 10_18 m2, the distribution of pressure, fluid velocity and fluid shear stress within the osteon near the periosteum and endosteum was significantly different from that in other parts of the bone. However, when the permeability was less than 10_ 22 m2, such a difference did not exist. Particularly, the flow velocity at the lacunae was markedly higher than that in the canaliculi. Meanwhile, the pore pressure and fluid shear stress were conspicuously lower than those in the canaliculi. In this study, we considered the interconnections of different biofunctional units at different scales of bone tissue, construct a more complete multiscale model of bone tissue, and propose that osteocytes at different locations receive different fluid stimuli, which provides a reference for a deeper understanding of bone mechanotransduction.

Artificial cultivation is indispensable for obtaining medicinal plants. However, numerous challenges persist in the practical cultivation of these plants. In recent years, the role of nanotechnology in promoting plant growth and improving soil quality has attracted increasing attention. In this study, focusing on the ginseng (Panax ginseng Mayer) cultivation system, the effects of hollow mesoporous silica nanoparticles (HM-SiO2 NPs) on ginseng growth, rhizosphere, and cultivated soil were comprehensively analysed. The results revealed that HM-SiO2 NPs did not exert a significant impact on ginseng growth but could enhance root activity and elicit responses from antioxidant enzyme systems. Specific concentrations of HM-SiO2 NPs alter the soil environment in the ginseng rhizosphere, thereby providing distinct habitats for soil microorganisms, enhancing microbial interactions, promoting the stability of microbial networks, and positively influencing nutrient cycling in the ginseng rhizosphere. Moreover, the extensive effects of HM-SiO2 NPs on the microbial and physicochemical properties of ginseng-cultivated soils were observed. Specifically, HM-SiO2 NPs reduced the abundance and diversity of bacterial communities in ginseng-cultivated soil and significantly altered the abundance of several dominant microbial taxa. The potential effects of HM-SiO2 on bacterial and fungal networks in ginseng-cultivated soil varied, with a reduction in the complexity of the bacterial network (particularly at low concentrations of HM-SiO2 NPs) and increase in the complexity of the fungal network. These findings offer insights into the complex effects of HM-SiO2 NPs on the "plant-soil-microbe" interaction system in medicinal plant cultivation, elucidate the potential applications of nanotechnology in this field, and provide a reliable basis for the development of environmentally friendly growth regulators or soil conditioners for medicinal plants.

Background: Supersaturating drug delivery systems (SDDSs) have gained significant attention as a promising strategy to enhance the solubility and bioabsorption of Biopharmaceutics Classification System (BCS) II drugs. To overcome challenges associated with polymer-based amorphous SDDS (aSDDS), coamorphous (CAM) systems have emerged as a viable alternative. Among them, “drug-drug” CAM (ddCAM) systems show considerable potential for combination drug therapy. However, many drugs in their pure amorphous forms are unstable at room temperature (RT), complicating their formation and long-term stability profiles. Consequently, limited knowledge exists regarding the behavior of ddCAMs containing RT-unstable components formed via quench cooling. Methods: In this study, we used naproxen (NAP), a RT-unstable amorphous drug, in combination with felodipine (FEL) or nitrendipine (NTP), two RT-stable amorphous drugs, to create “FEL-NAP” and “NTP-NAP” ddCAM pairs via quench cooling. Our work used a series of methods to perform a detailed analysis on the co-amorphization, dissolution, solubility, and stability profiles of ddCAMs containing RT-unstable drugs, contributing to advancements in co-amorphization techniques for generating SDDS. Results: This study revealed that the co-amorphization and stability profiles of ddCAMs containing RT-unstable components produced via a quench-cooling method were closely related to drug-drug pairing types and ratios. Both quench-cooling and incorporation into coamorphous systems improved the dissolution, solubility, and physical stability of individual APIs. Conclusions: Our findings provide deeper insight into the co-amorphization, dissolution, and stability characteristics of specific drug-drug coamorphous systems FEL-NAP and NTP-NAP, offering valuable guidance for developing new ddCAM coamorphous formulations containing some RT-unstable drugs.

Methylmercury (MeHg) can cause devastating neurotoxicity in animals and human beings. Gut microbiota dysbiosis has been found in MeHg-poisoned animals. Fecal microbiota transplantation (FMT) has been shown to improve clinical outcomes in a variety of diseases such as epilepsy, amyotrophic lateral sclerosis (ALS) and autism. The aim of this study was to investigate the effects of FMT on MeHg-poisoned rats. FMT treatment was applied to MeHg-poisoned rats for 14 days. The neurobehavior, weight changes, dopamine (DA), the total Hg and MeHg level were evaluated. Besides, the gut microbiota and metabolites change in feces were also checked. It was found that FMT helped weight gain, alleviated the neurological disorders, enhanced fecal mercury excretion and MeHg demethylation, reconstructed gut microbiome and promoted the production of gut-brain axis related-metabolites in MeHg-poisoned rats. This study elaborates on the therapeutic efficacy of FMT in treating of MeHg-poisoned rats, which sheds lights on the treatment of neurological diseases like Minamata Disease and even Parkinson's Disease.

Nanotherapies, valued for their high efficacy and low toxicity, frequently serve as antitumor treatments, but do not readily penetrate deep into tumor tissues and cells. Here we developed an improved tumor-penetrating peptide (TPP)-based drug delivery system. Briefly, the established TPP iNGR was modified to generate a linear NGR peptide capable of transporting nanotherapeutic drugs into tumors through a CendR pathway-dependent, neuropilin-1 receptor-mediated process. Although TPPs have been reported to reach intended tumor targets, they often fail to penetrate cell membranes to deliver tumoricidal drugs to intracellular targets. We addressed this issue by harnessing cell penetrating peptide technology to develop a liposome-based multibarrier-penetrating delivery system (mbPDS) with improved synergistic drug penetration into deep tumor tissues and cells. The system incorporated doxorubicin-loaded liposomes coated with nona-arginine (R9) CPP and cyclic iNGR (CRNGRGPDC) molecules, yielding Lip-mbPDS. Lip-mbPDS tumor-targeting, tumor cell/tissue-penetrating and antitumor capabilities were assessed using CD13-positive human fibrosarcoma-derived cell (HT1080)-based in vitro and in vivo tumor models. Lip-mbPDS evaluation included three-dimensional layer-by-layer confocal laser scanning microscopy, cell internalization/toxicity assays, three-dimensional tumor spheroid-based penetration assays and antitumor efficacy assays conducted in an animal model. Lip-mbPDS provided enhanced synergistic drug penetration of multiple biointerfaces for potentially deep tumor therapeutic outcomes. We co-modified R9 and iNGR on the liposome surface to obtain Lip-mbPDS. The penetration of Lip-mbPDS into multiple biointerfaces has enabled it to demonstrate good anti-tumor ability for CD13-positive HT1080 cells both in vivo and ex vivo.

Peptides and proteins, two important classes of biomacromolecules, play important roles in the biopharmaceuticals field. As compared with traditional drugs based on small molecules, peptide- and protein-based drugs offer several advantages, although most cannot traverse the cell membrane, a natural barrier that prevents biomacromolecules from directly entering cells. However, drug delivery via cell-penetrating peptides (CPPs) is increasingly replacing traditional approaches that mediate biomacromolecular cellular uptake, due to CPPs’ superior safety and efficiency as drug delivery vehicles. In this review, we describe the discovery of CPPs, recent developments in CPP design, and recent advances in CPP applications for enhanced cellular delivery of peptide- and protein-based drugs. First, we discuss the discovery of natural CPPs in snake, bee, and spider venom. Second, we describe several synthetic types of CPPs, such as cyclic CPPs, glycosylated CPPs, and D-form CPPs. Finally, we summarize and discuss cell membrane permeability characteristics and therapeutic applications of different CPPs when used as vehicles to deliver peptides and proteins to cells, as assessed using various preclinical disease models. Ultimately, this review provides an overview of recent advances in CPP development with relevance to applications related to the therapeutic delivery of biomacromolecular drugs to alleviate diverse diseases.

Despite the potential advantages of amorphism-induced supersaturation, the merit of new amorphization formation methods on the properties of the amorphous drug including the stability of the amorphous state, dissolution/solubility, supersaturation, and “spring-parachute” process is still poorly understood, particularly for certain amorphous supersaturating drug delivery systems (aSDDS). The present work aimed to explore the detailed merit of current attractive amorphization manufacturing methods (i. g., hot-melt extrusion (HME) technique) on the property improvement of aSDDS in form of amorphous solid dispersion microparticles by employing a model BCS II drug nitrendipine and a polyvinylpyrrolidone-based model polymer copovidone. Many aSDDS systems were developed by various methods, and their physicochemical properties were characterized by SEM, PXRD and DSC. HME-triggered amorphization induced superior supersaturation by the observation of the highest dissolution and solubility. HME induced the optimal supersaturation duration by the observed greatest extension of “spring-parachute” process (e. g., maximum AUCspring-parachute). HME technique is comparable with other techniques for the stabilization of amorphous state during storage. All aSDDS systems by HME and other methods showed improved long-term stability of the amorphous state in comparison to the pure amorphous drug. Fourier transformation infrared spectroscopy, Noyes-Whitney equation, nucleation theory and Gibbs free energy of transfer (ΔGto) were used to analyze the underlying mechanisms. Molecular mechanism studies indicated that HME caused a stronger crystallization inhibition effect in the aSDDS systems than other methods, but molecular interaction is not a dominant mechanism for property enhancement caused by HME. For the mechanism associated with the polymer itself (PVPVA64), it could inhibit the drug recrystallization, solubilize the drug spontaneously and cause the improved molecular interactions in all aSDDS systems. This study provided a deep insight into detailed advantage of HME-triggered supersaturation/amorphization and facilitated the applications of the technique both in the field of particuology and in pharmaceutical industry.

Amorphous solid-state dispersions that achieve supersaturation are often used to generate supersaturating drug delivery systems (SDDS). Relative to kinetic disordering approaches, thermodynamic disordering strategies utilizing currently popular self-micellizing amphiphilic polymers are better suited for industrial applications and can greatly improve supersaturating immediate-release of self-micellizing solid dispersion (SmSD) microcarrier delivery systems. However, the impact of thermodynamic disordering processes in different patterns (continuous and discontinuous) on the amorphization and supersaturating immediate-release of amorphous SmSD systems containing insoluble drugs is not clear. Here, we employed hot melt extrusion (HME) as a continuous thermodynamic disordering process, and two methods including solvent evaporation (SE) and microwave-quench cooling (MC) as discontinuous processes, to fabricate amorphous SmSD systems containing self-micellizing polymer Soluplus ® for the supersaturating delivery of a water-insoluble BCS II drug felodipine. Characterization of these amorphous SmSD systems was accomplished via scanning electron microscopy (SEM), powder X-ray diffraction (PXRD), and differential scanning calorimetry (DSC). HME-based continuous thermodynamic disordering process triggered a marked extension of supersaturating immediate-release by elevating solubility, enhancing dissolution and moving up “spring-parachute” processes as compared to discontinuous disordering processes. Molecular mechanisms contributing to internal stability of SmSD systems were explored through analyses of molecular interactions, crystallization inhibition effects and Gibbs free energy of transfer (ΔGtr°) values. This work indicates that HME-based continuous thermodynamic disordering process can be used in the development of superior amorphous SmSD microcarrier systems by triggering the generation of extended supersaturating immediate-release, and displays its further application potential in pharmaceutical industry.

The lack of effective rheumatoid arthritis (RA) therapies is a persistent challenge worldwide, prompting researchers to urgently evaluate traditional Chinese medicines (TCMs) as potential clinical RA treatments. The present investigation was conducted to evaluate the therapeutic effects and potential molecular mechanisms of the active components isolated from TCM Rhodiola sachalinensis Borissova from Baekdu Mountain (RsBBM) using an experimental adjuvant arthritis model induced by injection of rats with Freund's complete adjuvant. After induction of the adjuvant arthritis rat model, the extract-treated and untreated groups of arthritic rats were evaluated for RsBBM therapeutic effects based on comparisons of ankle circumferences and ELISA-determined blood serum inflammatory factor levels (TNF-α, IL-1β, and PGE2). In addition, the joint health of rats was evaluated via microscopic examination of hematoxylin-eosin-stained synovial tissues. Furthermore, to explore whether NF-κB and RANK/RANKL/OPG signaling pathways participated in observed therapeutic effects from a molecular mechanistic viewpoint, mRNA and protein levels related to the expression of nuclear factor kappa-B (NF-κB), osteoprotegerin (OPG), and receptor activator of nuclear factor kappa-Β ligand (RANKL) were analyzed via quantitative RT-PCR and Western blot analysis, respectively. Treatment of arthritic rats with the extract of RsBBM was shown to reduce ankle swelling, reduce blood serum levels of inflammatory factors, and alleviate arthritis-associated synovial inflammation and joint damage. Moreover, an RsBBM 50% ethanol extract treatment inhibited bone destruction by up-regulating OPG-related mRNA and protein expression and down-regulating RANKL-related mRNA and protein expression, while also reducing inflammation by the down-regulating of the NF-κB pathway activity. The results clearly demonstrated that the extract of RsBBM alleviated adjuvant arthritis-associated joint damage by altering activities of inflammation-associated NF-κB and the RANK/RANKL/OPG signaling pathways. Due to its beneficial effects for alleviating adjuvant arthritis, this RsBBM 50% ethanol extract should be further evaluated as a promising new therapeutic TCM treatment for RA.

The short-term immediate release of supersaturated drug-delivery systems (SDDSs) presents an interesting process that can be tailored to multi-stage release events including initial release after dosing and dissolution, evolved release over longer dissolution periods for biological absorption, and terminal release following the end of immediate release. However, although comprehensive analysis of these critical release behaviors is often ignored yet essential for understanding the supersaturable immediate-release events for supersaturable solid formations when employing new techniques or polymers matched to a particular API. Hot-melt extrusion (HME) has become a popular continuous thermodynamic disordering technique for amorphization. The self-micellizing polymer Soluplus® is reported to be a potential amorphous and amphiphilic graft copolymer frequently used in many nano/micro supersaturable formulations. Our current work aims to develop hypotensive supersaturating solid dispersion systems (faSDDSHME) containing the BCS II drug, felodipine, when coordinately employing the HME technique and self-micellizing Soluplus®, and to characterize their amorphization as well as immediate release. Other discontinuous techniques were used to prepare control groups (faSDDSSE and faSDDSQC). Tailored initial/evolved/terminal three-stage supersaturable immediate-release behaviors were identified and possible mechanisms controlling the release were explored. HME produced the highest initial release in related faSDDSHME. During the evolved-release period, highly extended "spring-parachute" process was found in HME-induced amorphization owing to its superior supersaturation duration. Due to the enhanced crystallization inhibition effect, faSDDSHME displayed the strongest terminal release as measured by solubility. For release mechanisms associated with HME, molecular interaction is not the likely dominant mechanism responsible for the improved properties induced by faSDDSHME. For release mechanisms involved with the polymer Soluplus® itself, they were found to inhibit drug recrystallization, spontaneously solubilize the drug and lead to improved molecular interactions in all SDDS systems, which were the factors responsible for the improved release. These mechanisms play an important role for the generation of an extended multi-stage immediate release produced via HME or self-micellizing polymer. This study provides a deeper understanding on amorphization and superior multi-stage supersaturable immediate-release behaviors for a particular hypotensive supersaturated delivery system combined with an HME-based continuous manufacturing technique and self-micellizing polymer strategy.

Hot melt extrusion (HME), a continuous manufacturing process for generating supersaturating amorphous self-micellizing solid dispersion systems (saSMSDs), holds promise for achieving amorphization of many pharmaceutical formulations. For saSMSDs generation, HME-triggered continuous processes offer advantages over traditional non-continuous processes such as fusion/quench cooling (FQC) and co-precipitation (CP). Here we employed HME, FQC, and CP to generate saSMSDs containing the water-insoluble BCS II drug nitrendipine (NIT) and self-micellizing polymer Soluplus®. Scanning electron microscopy, powder X-ray diffraction, and differential scanning calorimetry results revealed that saSMSDs formed when NIT–Soluplus® mixtures were subjected to the abovementioned amorphization methods. All saSMSDs outperformed crystalline NIT preparations and physical mixtures in achieving extended supersaturable immediate release states with superior solubility, “spring-parachute” process characteristics, and dissolution behaviors. Notably, Fourier transform-infrared spectroscopic results obtained for saSMSDs detected hydrogen bonding interactions between the drug and the carrier. Ultimately, our results revealed the advantages of HME-triggered amorphization as a continuous process for significantly improving drug dissolution, increasing solubility, and maintaining supersaturation as compared to traditional amorphization-based techniques.

Caco-2细胞来源于人体结肠癌细胞,可以参与药物的吸收、代谢、转运等过程,被看作分化的小肠上皮细胞,具有微绒毛等结构,并可分泌大量的小肠上皮细胞特有的蛋白、酶以及转运体.研究表明,Caco-2单层细胞模型可以用来探究不同条件因素对药物吸收转运的影响,对研究药物吸收机制有着重要的应用价值.

药学人才不仅需要丰富的专业知识、精湛的专业技术,更为重要的是需要具有优质的职业道德素养,可以工作中传达出对生命的尊重.在培养高水平、高素质的应用型药学人才的过程中,不仅需要遵循一般职业道德形成的规律,更要兼顾专业的特点,切实融入职业道德的内容与思考.

本试验用超声提取法提取长白山红景天黄酮组分,通过单因素变量法得到最佳提取条件;用AB-8大孔吸附树脂进行纯化,考察药液浓度、上样量、洗脱剂浓度及洗脱体积等因素,确定最佳纯化工艺;用ELISA法研究纯化后黄酮组分的抗炎活性.结果显示,长白山红景天黄酮组分的最佳提取工艺为:50％乙醇作为提取溶剂,料液比为1∶35,60C、200 W条件下超声提取35 min;最佳纯化工艺为:层析柱径高比为1∶16,药液中黄酮组分浓度为0.05 mg/mL,以2 BV/h的流量速度上样2 BV,再以50％乙醇洗脱2.5 BV,纯化后黄酮类成分纯度达到81.6％;纯化后黄酮组分能够显著地抑制小鼠巨噬细胞分泌促炎因子TNF-a(P＜0.01),明显提高抗炎性因子IL-10的分泌量(P＜0.05).由此可见,长白山红景天黄酮组分经提取纯化后具有良好的抗炎活性,可为其进一步开发和利用提供理论支持.

目的 建立液质联用检测方法分离鉴定藜芦主要化学成分,并比较各成分与不同比例南沙参配伍前后经Caco-2单层细胞模型吸收转运的变化情况,从吸收转运的角度分析南沙参对藜芦的"增毒"机制.利用Elisa法测定南沙参与不同比例藜芦配伍前后免疫调节作用的变化情况,从药效作用的角度分析藜芦对南沙参的"减效"机制.方法 液质条件为乙腈(A)和0.1％甲酸水溶液(v)作流动相,梯度洗脱,Acquity UPLC BEH C18(1.7 μm,2.1 mm×50 mm)色谱柱,柱温设置35℃;3200 QTRAPTM串联四级杆-线性离子阱质谱仪,采用电喷雾电离源,电喷雾电压为5.0 kV,透镜管电压为90 V,金属毛细管电压为40V、温度为250℃.结果 利用液质联用方法分离鉴定出8种生物碱成分,发现在一定配伍比例下南沙参可使藜芦中一些生物碱溶出和生物利用度提高,具有"增毒"作用.而藜芦的加入,使南沙参的免疫调剂作用降低,并随着藜芦用量的增加其药效作用降低明显,具有"减效"的作用.结论 该研究结果从化学成分含量变化、吸收转运和药效学改变的角度再次考察了中药"十八反"中南沙参"叛"藜芦的配伍禁忌原则,为深入研究中药十八反中藜芦-南沙参药对提供理论基础.

现代药理作用研究和临床应用表明,长白山红景天具有抗衰老、抗疲劳、抗缺氧、降血糖等作用.为了优化长白山红景天中多糖组分的提取纯化工艺,并探讨多糖组分对小鼠巨噬细胞的免疫调控作用,本试验用水提醇沉法提取长白山红景天多糖组分,并用Sevage法纯化多糖组分;通过设计正交试验精确调试Sevage试剂体积比、料液比、离心时间、离心次数等去除蛋白的最优条件;用MTT法与ELISA法研究纯化后多糖组分对小鼠巨噬细胞的增殖与免疫调节因子分泌的影响.结果显示,最佳纯化工艺为氯仿:正丁醇为5∶1;样品溶液:Sevage试剂为3:1;离心时间为15 min,离心次数为5次;得到提取纯化后多糖的含量占总溶液的68％.纯化后的长白山红景天多糖组分可显著促进小鼠巨噬细胞增殖(P＜0.05),增加巨噬细胞TNF-a和IL-1p分泌水平(P＜0.05).鉴于纯化后的长白山红景天多糖组分显示较好的免疫调节作用,极具进一步开发和利用的前景.