目的:运用葡聚糖硫酸钠诱导的结肠炎小鼠模型评估山芝麻提取物对结肠炎的治疗作用,并探讨其中的分子机制.方法:对山芝麻提取物进行为期7天的急性毒性试验.给予小鼠加入3％(m/V)葡聚糖硫酸钠的饮用水自由饮用,诱导小鼠急性结肠炎模型.实验组小鼠灌胃给予山芝麻提取物200、400 mg/(kg·d),正常对照组及模型组给予等体积蒸馏水灌胃.采用疾病活动度指数对小鼠进行评分,并对小鼠结肠组织进行组织病理学分析,评价山芝麻提取物的治疗效果.ELISA检测小鼠结肠组织中IL-6、IL-1β、TNF-α和髓过氧化物酶水平.RT-qPCR测定结肠组织TNF-α、IL-1β、IL-6 mRNA的表达.Western blot检测结肠组织STAT3、p-STAT3、JAK1、JAK2、SOCS3蛋白表达.结果:葡聚糖硫酸钠水溶液的摄入可导致小鼠体质量严重下降和疾病评分升高,而山芝麻提取物可显著改善这些症状.组织病理学观察表明山芝麻提取物能减轻葡聚糖硫酸钠诱导的结肠形态学损害.与模型组比较,山芝麻提取物各组结肠组织TNF-α、IL-1β、IL-6水平及其mRNA表达和JAK1、JAK2、p-STAT3蛋白表达及髓过氧化物酶水平显著降低.结论:山芝麻提取物可通过抑制NF-κB和STAT3信号通路改善葡聚糖硫酸钠诱导的小鼠结肠炎.

随着我国鱼肉消费量的增加,大量的鱼类加工副产品也随之产生.内脏是鱼类加工中主要的副产品之一.本文综述了鱼类内脏中蛋白类物质的精深加工技术研究现状,并对其开发的产品,包括活性肽、细菌素、生物降解膜、蛋白胨、内脏酶等的理化及功能特性进行归纳总结,以期为鱼加工副产品——内脏潜在价值的开发利用提供研究思路.

The Janus kinases (JAKs) consist of four similar tyrosine kinases and function as key hubs in the signaling pathways that are implicated in both innate and adaptive immunity. Among the four members, JAK3 is probably the more attractive target for treatment of inflammatory diseases because its inhibition demonstrates the greatest immunosuppression and most profound effect in the treatment of such disorders. Although many JAK3 inhibitors are already available, certain shortcomings have been identified, mostly acquired drug resistance or unwanted side effects. To discover and identify new promising lead candidates, in this study, the structure of JAK3 (3LXK) was obtained from the Protein Data Bank and used for simulation modeling and protein-ligand interaction analysis. The ~36,000 Chinese herbal compounds obtained from TCM Database@Taiwan were virtually screened by AutoDock Vina docking program and filtered with Lipinski's Rules and ADME/T virtual predictions. Because of high occurrence of fake hits during docking, we selected 12 phytochemicals which have demonstrated modulating JAKs expressions among the top 50 chemicals from docking results. To validate whether these compounds are able to directly mediate JAK3 kinase, we have investigated the inhibitory activity using enzymatic activity assays, western blot, and HEK 293 cell STAT5 transactivity assays. The molecular analysis included docking and molecular dynamics (MD) simulations in order to investigate structural conformations and to explore the key amino acids in the interaction between JAK3 kinase and its putative ligands. The results demonstrated that Cryptotanshinone, Icaritin, and Indirubin exhibited substantial inhibitory activity against JAK3 kinase in vitro. The results also provide binding models of the protein-ligand interaction, detailing the interacting amino acid residues at the active ATP-binding domains of JAK3 kinase. In conclusion, our work discovered 3 potential natural inhibitors of JAK3 kinase and could provide new possibilities and stimulate new insights for the treatment of JAK3-targeted diseases.

热毒内蕴是结直肠癌的重要病因病机之一,清热解毒类中药在中医治疗结直肠癌中发挥了重要作用.通过中国知网(CNKD、PubMed数据库,检索出近20年与清热解毒类中药抗结直肠癌作用机制相关的研究并对其进行综述.结果 发现多种清热解毒类中药表现出良好的抗结直肠癌活性,机制与抑制肿瘤细胞增殖、促进肿瘤细胞凋亡、调控细胞内信号通道等作用相关.清热解毒类中药在抗结直肠癌方面具有良好的应用前景,但其作用机制尚未完全明确,需要更深入的研究.

JAK/STAT信号通路可以直接介导胞外细胞因子的信号与胞内的基因表达,可以引发和参与细胞生长、细胞分化、存活、编程性细胞死亡、有丝分裂发生、细胞周期控制和细胞运动性有关的一系列过程.近十年来,国内文献报道了许多中药通过JAK/STAT信号通路干预调控肿瘤、呼吸系统疾病、心血管疾病等的研究,但还未见系统的回顾和综述.文章对这些文献进行了系统地分析整理,旨在为该领域的研究工作提供系统的信息.

Colorectal cancer (CRC) is one of the most common malignancies and most frequent cause of cancer death worldwide. The activation of both NF-κB and STAT3 signaling and the crosstalk between them play an important role in colorectal tumor. Helicteres angustifolia L. is a type of commonly used Chinese medicinal herb and possesses a wide variety of biological activities. In the present study, we investigate the effects of three triterpenes from H. angustifolia (HT) such as helicteric acid (HA), oleanic acid (OA), and betulinic acid (BA), on inhibiting CRC progression. Our results showed that HT extracts could decrease proliferation and induce apoptosis in HT-29 colorectal cancer cells. Moreover, HT extracts could suppress LPS-triggered phosphorylation of IKK, IκB, and NF-κB, attenuate IL-6-induced phosphorylation of JAK2 and STAT3, and suppress the expression of c-Myc, cyclin-D1, and BCL-xL, the downstream gene targets of NF-κB and STAT3. Therefore, HT extracts showed potent therapeutic and antitumor effects on CRC via inhibiting NF-κB and STAT3 signaling.

Aiming to cultivate students of independent college with practical abilities, and to improve their innovative quality, application ability and job skills, exploration was performed on practical education innovation of Pharmaceutical Chemistry based on the sulfa drug synthesis. The computer aided drug design, chemical synthesis combined with quality inspection and biological effect testing, and professional training in practice bases were integrated into the practice teaching. Through the above practices, the qualities of students were improved, and their abilities were promoted.

目的 为更好地评价山芝麻药材的质量,建立RP-HPLC同时测定山芝麻药材的6个主要三萜类成分(山芝麻宁酸甲酯、山芝麻酸甲酯、山芝麻宁酸、山芝麻酸、白桦酯酸、齐墩果酸)含量的方法,建立紫外可见分光光度法测定山芝麻药材中总三萜含量的方法.方法 ①采用Waters Symmetry C18(4.6 mm× 250 mm,5μm)色谱柱,以乙腈-(0.2％)磷酸水溶液为流动相,采用二元梯度洗脱;流速:1.2ml/min;检测波长:230nm;柱温:35℃;②以齐墩果酸为对照,采用香草醛-高氯酸显色法在552nm测定山芝麻药材中总三萜的含量.结果 RP-HPLC方法中山芝麻药材的6个三萜类成分的回归方程具有良好的线性关系(相关系数为:r =0.9991～0.9996),紫外可见分光光度法测定山芝麻药材中总三萜含量的回归方程同样具有良好的线性关系(相关系数为:r=0.9998);不同产地的山芝麻药材各三萜类成分及总三萜的含量有一定的差异.结论 所建立的含量测定方法稳定性、精密度、重复性良好,适用于山芝麻药材及含山芝麻制剂的质量控制.

Objective:To develop a method for separation and purification of triterpenoids from Helicteres angustifolia by highspeed countercurrent chromatography( HSCCC).Methods:The ethyl acetate extract of Helicteres angustifolia were separated by two-step HSCCC. The structures of the target compounds were identified by ESI-MS and1H-NMR and characterized by FTIR.Results:Six compounds were isolated and prepared from ethyl acetate extract of Helicteres angustifolia,and identified as methyl helicterilate( 1),methyl helicterate( 2),helicterilic acid( 3),helicteric acid( 4),betulic acid( 5),oleanolic acid( 6). The purity of the chemical constituents were determined by HPLC,and the mass fraction was more than 95. 0%,respectively.Conclusion:This method is suitable for the separation and preparation of triterpenoids from Helicteres angustifolia,which is rapid,high purity and high yield.

OBJECTIVE:To optimize spray drying process for the raw fruits extract of Psidium guajava. METHODS:Based on single factor,the response surface method was designed to optimize spray drying process condition,using extract rate as index and mass concentration,sampling temperature and sampling speed as factors. The contents and transport rate of total flavones and total polyphenol were determined in each step. RESULTS:The optimal process was as follows as mass concentration of 100 g/L, sampling temperature of 170 ℃,sampling speed of 180 ml/h. Under this condition,the yield of 3 batches of product was(56.08± 0.58)%(RSD=1.04%,n=3). The difference value between test value and predict value was 0.25,without significant difference (P>0.05). The powder of the raw fruits of P. guajava had high contents of total flavones [(17.80 ± 0.09)%] and total polyphenol [(1.23 ± 0.06)%]. The transport rates of them were 87.7% and 25.7%. CONCLUSIONS:Optimized process is feasible to obtain qualified product,and can be used to make medicinal solid preparation.

目的 通过分子对接,探讨山芝麻中15种三萜化合物对5个溃疡性结肠炎(UC)靶蛋白的作用,从而阐释中药山芝麻抗UC的作用机制与分子基础.方法 植物化学成分的二维结构均从PubChem数据库中检索或使用Avogadro程序绘出,并采用Avogadro程序绘出它们的三维结构.从蛋白质数据库(PDB)提取靶蛋白(PPAR-gamma、JAK、TNF-alpha、IKK-beta and IL-2)的X-衍射晶体结构.分子对接研究采用AutoDock Vina软件.结果 通过与阳性药物相比较,山芝麻的三萜类化合物与靶蛋白的结合能较高(或相对较高),认为其与UC治疗相关的靶点蛋白有显著的结合亲和力,是它们的有效抑制剂.结论 分子对接研究显示山芝麻三萜类化合物对靶蛋白PPAR-gamma、JAK、TNF-alpha、IKK-beta and IL-2有抑制作用,预期其能有效防治溃疡性结肠炎.

OBJECTIVE:To investigate the effect of aqueous extract of Helicteres angustifolia (AEHA) on rats with ulcerative colitis (UC) and its mechanism.METHODS:SD rats were randomly divided into 6 groups normal control group, the model group, SASP group and 21.6, 10.8, 5.4 g/kg AEHA group with 10 rats in each group. UC was induced by clyster with 2, 4,6-trinitrobenzesulphonic acid (TN-BS) in rats. Rats were given AEHA by gavage for 3 weeks, and sacrificed at day 22nd to determine the expressions of IL-10, IL-6 and TNF-alpha in blood. Colon tissue pathological changes were investigated.RESULTS:Compared with the control group, the expression of IL-10 was increased, the expressions of IL-6 and TNF-alpha were decreased in AEHA treatment groups. The colon tissue damages and the symptoms of UC rats were improved.CONCLUSION:AEHA can keep balance of inflammatory factors in blood of UC rats, and improve it's colon tissue damages and symptoms.

<正>毒性中药在复方中药制剂中应用广泛,在长期的临床实践中发挥了重要的治疗作用。但是,长期受中药毒副作用小的观念影响,中药毒性的现代研究一直是一个比较薄弱的环节。参照化学药品毒性研究方法对毒性中药进行的毒性评价,主要还是集中在急性、亚急性和长期毒性实验,指标的选择主要集中在生化指标的检测和组织形态学的改变。这些方法为我们提出了毒性的

OBJECTIVE:To analyze the chemical components of volatile oil from Helicteres angustifolia by GC-MS.METHODS:The volatile oil was extracted from H.angustifolia by steam distillation.The chemical components of volatile oil were identified by GC-MS,the content of chemical components from volatile oil were determined by normalization method.RESULTS:There were 81 chemical components,accounting for 76.52% of total volatile oil.Main chemical components were monoterpenes,sesquiterpenes and their oxygenated derivatives and aliphatic compounds.CONCLUSION:The methods are reliable,stable and good repeatability.The methods can be applied to the analysis of chemical components of volatile oil from traditional Chinese medicine.

目的 探讨双黄连注射剂不良反应的一般规律和特点,以预防或避免其重复发生,促进临床合理用药.方法 用文献计量学方法对58例双黄连注射剂不良反应病例进行整理归纳与分析.结果 双黄连注射剂不良反应与性别、年龄无关,与药物自身因素、药物间配伍和临床医师中医诊疗水平等因素有关.不良反应发生时间主要集中于用药过程中的前30min,均引起患者不同程度的器官损害并死亡2例.结论 双黄连注射剂不良反应的相关因素很多,且后果严重,临床医务人员应引起重视,规范合理用药,避免或减少其不良反应的发生.

In the paper,experimental teaching of biochemistry in Zhongshan College of UEST as an example,discusses the drawbacks of traditional experimental teaching of personnel training on the application of the obstruction of an independent college.Status from the course,the experiment content,assessment methods were explored to adapt to the level of reform of the experiment,the experiment made better teaching results.

文章以电子科技大学中山学院生物化学实验教学为例,论述了传统实验教学的弊端对应用性人才培养的阻碍,从课程地位,实验内容,考核方式等方面探讨了适应于独立学院层次的实验改革方法,取得了较好的实验教学效果.

目的 对山芝麻近年来的研究概况作一综述.方法 分析山芝麻近年来的文献资料.结果与结论 应加强山芝麻的化学成分、药理作用和临床应用的研究,进一步对其进行制剂开发研究.

Objective:To study the effect of Huangzhi Oral Liquid on ATP binding cassette transporter A1 (ABCA1) expression in THP-1 macrophage-derived foam cells, and explore its effects on AC. Methods: The mean ABCA1 fluorescence intensity of THP-1 macrophage-derived foam cells was detected by flow cytometry. ABCA1 mRNA was determined by RT-PCR. Results: The results showed that Huangzi Oral Liquid markedly increased the ABCA1 expression in the THP-1 macrophage-derived foam cells, accompanied with the up-regulation of ABCA1 found with ox-LDL. Conclusion: The level of ATP binding cassette transporter A1 (ABCA1) expression in THP-1 macrophage-derived foam cells can be up-regulated by Huangzhi Oral Liquid.