TRIACYLGLYCERINES OF Ruta graveolens GROWN in vivo AND in vitro

The composition of triacylglycerines (TAG) from photosynthetic tissues ofRuta graveolensL. (Rutaceae) grownin vivoandin vitrowas studied with respect to chain length and unsaturation. Esterification of sn-2-glycerol by unsaturated acids is less selective underin vitrothanin vivoconditions. TAG of thein vitroculture have an elevated content of forms with oleinic acid in the sn-2-position.     

STUDY ON in vitro SPERM CAPACITATION AND EGG-PENETRATION OF GIANT PANDA

A preliminary report on in vitro sperm capacitation and egg-penetration of giant panda is briefly presented. The panda spermatozoon consists of head, neck and tail, just like the spermatozoa of other animals. Before capacitation sperm heads clusterd together and dispersed after capacitation. They were then able to swim straight forwared. During the time of in vitro capacitation the plasm membrane of the sperm head was first expanded tov arious degrees, then disintegrated, and finally became detached. The electro-dense material in the acrosome appeared in small clumps with high density. Extensive vesiculation occurred between the bi-layered acrosome membranes and thus led to disintegration. Vesiculation in panda sperm differs from that reported in hamsters. When the capacitated panda spermatozoa came into contact with the hamster eggs, the region between the acrosome collar and postacrosome cap first fused with the egg membrane followed by the penetration of the nucleus into the cortex of the egg. Some o     

聚二氧杂环己酮合成可吸收缝合线体外降解研究

通过检测缝线的力学性能、分子量、失重、大分子取向和结晶度变化研究了聚二氧杂环己酮可吸收缝合线（ＰＤＳ）在体外的初期（４星期）降解过程。研究结果表明，本文工艺条件下研制的ＰＤＳ缝线在体外降解过程中随着分子量和大分子取向程度下降，力学性能明显下降，４星期时强度基本消失。分子量明显下降而失重变化很小的结果，证明ＰＤＳ缝线的酯水解在链中和链端等活性，水解的几率只与水分子的可及程度相关。ＷＡＸＤ和ＤＳＣ测试结果表明，随着体外降解进行，缝线原晶区基本保持不变，无定形区产生新的有序区，并且含量不断增加和完善。采用结晶高聚物微原纤结构模型解释ＰＤＳ缝线无定形区在水中的降解机理与研究结果相吻合。ＰＤＳ缝线的体外降解机理与聚羟基乙酸（ＰＧＡ）缝线基本相同     

高分子量聚对二氧环己酮体外降解研究

对高分子量(Mν=2.8×105)的聚对二氧环己酮条状样品在37℃磷酸缓冲溶液(PBS)中的降解行为进行了研究,通过定期观察其吸水率与质量损失,pH,特性黏数,降解过程中样品形态与晶体结构,热力学性能与机械性能的改化,发现此高分子量的聚对二氧环己酮在体外降解过程中质量损失与吸水率变化不大,但分子量下降明显,同时样品表面缺陷逐渐增加;结晶度与玻璃化温度随之改变,但其晶体结构基本保持不变;到第6周时,其力学强度基本消失.证明高分子量PPDO具有较慢的降解速度,显示出很好的稳定性.     

A STUDY OF STRUCTURE AND PROPERTY CHANGES OF BIODEGRADABLE POLYGLYCOLIDE AND POLY(GLYCOLIDE-co-LACTIDE)FIBERS DURING PROCESSING AND IN VITRO DEGRADATION*

Structure and properties of bioabsorbable polyglycolide (PGA) and poly(glycolide-co-lactide) (PGA-co-PLA)fibers were investigated during several industrial processing stages and in vitro degradation by means of wide-angle X-raydiffraction (WAXD), dynamic mechanical analysis (DMA) and mechanical property tests. In the orientation stage, the PGAfibers were found to have higher degrees of crystallinity than corresponding PGA-co-PLA samples produced under similarconditions. In the hot-stretching and post-annealing stages, after fibers were braided, PGA samples were found to gain morecrystallinity and higher T_g than PGA-co-PLA samples. The higher crystallinity in PGA fibers resulted in a slower rate ofdegradation. DMA results showed that a great deal of internal stress that was built during orientation and hot-stretchingstages was released in the post-annealing stage for a1l PGA and PGA-co-PLA samples. During earlier stages of in vitrodegradation, both PGA and PGA-co-PLA samples exhibited the typical cleavage-induced crystallization mechanism. Theheat shrinkage in the glass transition area was found to disappear after 6-8 days of degradation for all PGA and PGA-co-PLAsamples, indicating the amorphous portions of the polymers lost orientation after a short period in the buffer solution, mostlikely due to relaxation of the cleaved chains.     

FACTORS AFFECT THE RELEASE OF PSEUDOEPHDRINE HYDROCHLORIDE FROM THE UNCOATED CATION EXCHANGE RESIN—BASED DRUG DELIVERY SYSTEM IN VITRO

In this paper,it was investigated that the effect of parameters such as the ionic strength,pH.counter-ion type of release medium,particle size.and cross linkage of cation exchange resin on the release of model drug pseudoephedrine hydrochloride(PE) from uncoated drug-resin complex.The drug-resin complex was pepared by the reaction of PE with strongly acidic cation exchange resin(001×4,001×7,001×14） .The result showed that the loading of PE increased with the increase of temperatures.The release of PE from drug-resin complex at 37℃ was monitored in vitro.From the experiments,it was found that the release rate of PE depends on the pH.comosition of the releasing media,increased at lower pH media or with increase of ionic strength of media.Moreover,the release rate of PE was inversely proportional to the cross-linkage and particle size of the cation exchange resin.     

聚对二氧杂环己酮─乙交酯无规共聚物缝合线热处理及体外降解性能研究

本文研究了热处理对聚对二氧杂环己酮-乙交酯无规共聚物合成缝合线力学性能和体外降解性能影响。结果表明：60～80℃温度范围内定长热定型对缝线原有力学性能影响较小；体外降解性能表明，随着热定型温度提高，缝线强度下降速率减缓。DSC测试结果表明，热定型后缝线样品结晶度提高，体外降解过程样品结晶度也逐渐提高，其中，无热定型样品提高幅度最大，说明热定型可使缝线样品聚集态结构紧密，水解速度减慢。     

Synthesis and evaluation of in vitro anticancer activity of novel solasodine derivatives

<正>Solasodine 11 is a steroidal alkaloid with various biological activities.Herein,8 novel solasodine derivatives were synthesized and their effect on prostate cancer cell proliferation was assessed in vitro.Significant improvement in antiproliferative activity was achieved among some of the synthetic analogs.In particular,19 exhibited the most potent inhibitory effect against the proliferation of PC-3 cell line(IC_(50) = 3.91μmol/L).     

FACTORS AFFECT THE RELEASE OF PSEUDOEPHDRINE HYDROCHLORIDE FROM THE UNCOATED CATION EXCHANGE RESIN-BASED DRUG DELIVERY SYSTEM IN VITRO

1. INTRODUCTIONIn recent years increasing attention has been given to the controlled drug delivery system, which offer a potential advantage over conventional drug therapy. The advantages of a controlled drug release system included localized delivery of the drug to a particular region in the body. This lowers the systemic drug level, increases patient comfort and improves patient compliance. Ion exchange resins are functional polymers that have been used in purification of water, analyti…     

Metabolism of eupatilin in rats using liquid chromatography/electrospray mass spectrometry

Eupatilin (5,7-dihydroxy-3',4',6-trimethoxy flavone) is an active ingredient of an ethanol extract of Artemisia asiatica (DA-9601) that is used in the treatment of gastritis. In vitro and in vivo metabolism of eupatilin in the rats has been studied by LC-electrospray mass spectrometry. Rat liver microsomal incubation of eupatilin in the presence of NADPH and UDPGA resulted in the formation of four metabolites (M1-M4). M1, M2, M3 and M4 were tentatively identified as 3'- or 4'-O-demethyl-eupatilin glucuronide, eupatilin glucuronide, 6-O-demethyleupatilin and 3'- or 4'-O-demethyl-eupatilin, respectively. Those metabolites from in vitro study were also characterized in bile, plasma or urine samples after an intravenous administration of eupatilin to rats. In rat bile, plasma and urine samples, eupatilin glucuronide (M2) was a major metabolite, whereas M3, M4 and M4 glucuronide (M1) were the minor metabolites.     

新型仲钨酸盐-B化合物[Na_2(H_2O)_(10)][Cu_4(H_2O)_(12)(H_2W_(12)O_(42))]·15H_2O体外抗肿瘤活性研究

对化合物[Na_2(H_2O)_(10)][Cu_4(H_2O)_(12)(H_2W_(12)O_(42))]·15H_2O(简称Na_2Cu_4W_(12))进行了体外抗肿瘤活性研究.应用四甲基偶氮唑盐(3-[4,5-dimethylthiazo-2-y]-2,5-diphenyltetrazolium bromide,MTT)比色法分析Na_2Cu_4W_(12)对人肝癌细胞(Hep G2)、人神经母细胞瘤细胞(SHY5Y)增殖抑制活性.采用光学显微镜观察肿瘤细胞的凋亡形态变化,用流式细胞术分析细胞周期和细胞凋亡,计算各期细胞比例及细胞凋亡率.结果表明,Na_2Cu_4W_(12)对Hep G2和SHY5Y 2种肿瘤细胞增殖半数抑制浓度IC_(50)值分别为5.3和10.2μmol·L~(-1),且呈剂量依赖性.光学显微镜下处理组细胞出现皱缩、变圆、缩小等形态变化,不同浓度Na_2Cu_4W_(12)处理12h早期凋亡细胞所占的百分比显著增加且呈剂量依赖性.综上所述,Na_2Cu_4W_(12)能够抑制胞瘤细胞增殖,诱导细胞凋亡.     

In Vitro Ultrasound Influence on Cutaneous Permeation of Hyaluronidase

In vitro skin permeation of hyaluronidase enzyme and the ultrasound (US) effects on cutaneous permeation of this enzyme were investigated. Diffusion cell technique, porcine skins, buffer solution, and a hydrophilic gel + hyaluronidase (100 TUR/g), were used for study. The experimental groups were: gel + enzyme and gel + enzyme + US. The activity of permeated hyaluronidase was determined by turbydimetric method in spectrophotometer at 400 nm. Gel + enzyme group permitted a diffusion of 26.89 ± 3.82 TUR of hyaluronidase in the total time of 240 minutes. However, the other group did not produce significant differences (p < 0.05) in the same period (13.68 ± 5.35 TUR). Hyaluronidase permeation through the skin was verified; however US did not cause increase of this enzyme permeation.     

Recent Advances in the Antiproliferative and Proapoptotic Activity of Various Plant Extracts and Constituents against Murine Malignant Melanoma

Although conventional medicine, chemical drug synthesis and pharmaceutical research are advancing at a rapid pace, nature remains a major supplier of biological molecules. Natural bioactive compounds are studied closely especially as an alternative to the limitations of conventional therapy in many diseases, melanoma being one of them. Malignant melanoma is a highly aggressive type of cancer, and the current methods of treatment used are cryotherapy, external surgery, radiation therapy, chemotherapy, photodynamic therapy, biological therapy, and targeted drug therapy. Unfortunately, these treatment methods are often inefficient, extremely expensive and cause many side effects, which is why focusing on melanoma chemoprevention and adjuvant therapy with natural herbal phytoconstituents is an emerging strategy to prevent, cure or treat melanoma. This review aims to examine the latest discoveries in terms of potential natural bioactive compounds that possess important activity against the development and spread of murine melanoma cancer. In particular, the use of different phytochemicals such as phenolic acids, flavonoids, anthocyanins, terpenoids, essential oils and carotenoids in vitro and in vivo models will be discussed. These data are helpful in guiding researchers in the direction of studying phytonutrients with important effects in the prevention and treatment of melanoma.     

An Overview of Antifouling Strategies for Electrochemical Analysis

Fouling is a key issue which limits the practical applications of electrochemical sensors (ECSens) in both in vitro and in vivo analysis. The analytical sensitivity, limit of detection (LOD), selectivity, reproducibility and life-time of ECSens are all greatly affected by fouling. Although numerous methods and materials have been developed to minimize the fouling effect in past several decades, not all of them are suitable for constructing antifouling ECSens. In this paper we present an overview of surface antifouling strategies for ECSens. We begin with a short summary of sources and impacts of fouling under both in vitro and in vivo environments. Then the current surface antifouling strategies for ECSens are discussed, including self-assembled monolayers (SAMs), antifouling polymers, porous coating, in-situ electrochemical and photocatalytic cleaning. The antifouling mechanisms, advantages and challenges of each strategy are briefly summarized. The article ends up with a short conclusion and perspectives. We hope this article is helpful for constructing and designing ECSens with both outstanding antifouling performance and electrochemical activity for electrochemical analysis.     

Therapeutic Potential of Tuna Backbone Peptide and Its Analogs: An In Vitro and In Silico Study

Tuna backbone peptide (TBP) has been reported to exert potent inhibitory activity against lipid peroxidation in vitro. Since this bears relevant physiological implications, this study was undertaken to assess the impact of peptide modifications on its bioactivity and other therapeutic potential using in vitro and in silico approach. Some TBP analogs, despite lower purity than the parent peptide, exerted promising antioxidant activities in vitro demonstrated by ABTS radical scavenging assay and cellular antioxidant activity assay. In silico digestion of the peptides resulted in the generation of antioxidant, angiotensin-converting enzyme (ACE), and dipeptidyl peptidase-IV (DPPIV) inhibitory dipeptides. Using bioinformatics platforms, we found five stable TBP analogs that hold therapeutic potential with their predicted multifunctionality, stability, non-toxicity, and low bitterness intensity. This work shows how screening and prospecting for bioactive peptides can be improved with the use of in vitro and in silico approaches.     

生物材料用Mg-Y-Zn-Zr合金的微观结构及体外降解行为

通过向纯镁中添加微量的合金化元素（Y、Zn和Zr）,采用熔融浇铸法制备了名义成分为Mg1.5Y1.2Zn0.44Zr四元可降解镁合金生物材料,并对其进行了均匀化处理和挤压。 对这3种状态的镁合金进行了微观结构及在模拟体液(SBF)中体外降解行为的测试和分析,结果表明,合金主要由α-Mg基体和Mg12ZnY第二相组成;合金经过挤压后的组织得到了明显的细化;因此挤压后合金的降解性能得到明显改善;合金在模拟体液中生成的降解产物主要是含Ca和Mg的磷酸盐。     

Antifungal Properties of Essential Oils and Their Compounds for Application in Skin Fungal Infections: Conventional and Nonconventional Approaches

Essential oils (EOs) are known to have varying degrees of antimicrobial properties that are mainly due to the presence of bioactive compounds. These include antiviral, nematicidal, antifungal, insecticidal and antioxidant properties. This review highlights the potential of EOs and their compounds for application as antifungal agents for the treatment of skin diseases via conventional and nonconventional approaches. A search was conducted using three databases (Scopus, Web of Science, Google Scholar), and all relevant articles from the period of 2010–2020 that are freely available in English were extracted. In our findings, EOs with a high percentage of monoterpenes showed strong ability as potential antifungal agents. Lavandula sp., Salvia sp., Thymus sp., Citrus sp., and Cymbopogon sp. were among the various species found to show excellent antifungal properties against various skin diseases. Some researchers developed advanced formulations such as gel, semi-solid, and ointment bases to further evaluate the effectiveness of EOs as antifungal agents. To date, most studies on the application of EOs as antifungal agents were performed using in vitro techniques, and only a limited number pursued in vivo and intervention-based research.     

Antioxidant Activity of Acanthopanax senticosus Flavonoids in H2O2-Induced RAW 264.7 Cells and DSS-Induced Colitis in Mice

The redox reaction is a normal process of biological metabolism in the body that leads to the production of free radicals. Under conditions such as pathogenic infection, stress, and drug exposure, free radicals can exceed normal levels, causing protein denaturation, DNA damage, and the oxidation of the cell membrane, which, in turn, causes inflammation. Acanthopanax senticosus (A. senticosus) flavonoids are the main bioactive ingredients with antioxidant function. H₂O₂-treated RAW 264.7 cells and DSS-induced colitis in mice were used to evaluate the antioxidant properties of A. senticosus flavonoids. The results show that A. senticosus flavonoids can significantly downregulate the levels of ROS and MDA in H₂O₂-treated RAW 264.7 cells and increase the levels of CAT, SOD, and GPx. A. senticosus flavonoids can also increase the body weights of DSS-induced colitis mice, increase the DAI index, and ameliorate the shortening of the colon. ELISA experiments confirmed that A. senticosus flavonoids could reduce the level of MDA in the mouse serum and increase the levels of SOD, CAT, and GPx. Histopathology showed that the tissue pathological changes in the A. senticosus flavonoid group were significantly lower than those in the DSS group. The Western blot experiments showed that the antioxidant capacity of A. senticosus flavonoids was accomplished through the Nrf2 pathway. In conclusion, A. senticosus flavonoids can relieve oxidative stress in vivo and in vitro and protect cells or tissues from oxidative damage.     

自制微透析探针性能评价

以自制微透析探针为研究对象,通过体外芍药苷微透析实验,评估灌注液流速、人工细胞外液中药物浓度、回收率测定方法及半透膜性质对自制同轴型微透析探针取样回收率的影响。实验结果表明,自制探针的回收率随灌注液流速升高呈近似指数曲线降低。当灌注流速为8.0μL/min时,回收率表现出浓度依赖性。采用直接透析法或反向透析法所得同一探针回收率存在显著差异。回收率因探针不同而存在差异。探针在体内连续取样6h,半透膜的通量未见衰减。实验室自制探针性能稳定,可用于体内微透析研究。