木香降血糖有效部位及有效成分研究

目的筛选木香中降血糖活性部位及主要成分。方法制备木香乙醇提取物,乙醇提取物醋酸乙酯部位、正丁醇部位和水提取部位;用HepG2细胞消耗葡萄糖模型和四氧嘧啶致糖尿病小鼠模型测定各提取物的降血糖活性;降血糖活性强的醋酸乙酯部位用柱色谱法继续分离、精制,得2个化合物,经NMR等鉴定化合物结构;并对2个化合物进行降血糖活性研究。结果木香醋酸乙酯部位有较强的降血糖作用,从木香醋酸乙酯部位中分离得到木香烃内酯和去氢木香内酯,且两者均可降低四氧嘧啶所致糖尿病小鼠的血糖,并显示很好的抗氧化作用。结论木香烃内酯和去氢木香内酯可能是木香的降血糖活性成分,抑制氧化应激从而减轻胰岛素抵抗可能是其降血糖机制。     

In Vitro Cytotoxicity of Mokko Lactone in Human Leukemia HL-60 Cells: Induction of Apoptotic Cell Death by Mitochondrial Membrane Potential Collapse

We studied the effect of mokko lactone (ML) isolated from the roots of Saussurea lappa (Compositae), a plant that is used for medicinal purposes in Korea, on the induction of apoptosis in human leukemia HL-60 cells. ML was cytotoxic to HL-60 cells, and this cytotoxic effect of ML appears to be attributable to its induction of apoptotic cell death, as ML induced nuclear morphologic changes and internucleosomal DNA fragmentation and increased the proportion of Annexin V-positive cells and the activity of caspase-3. Further studies revealed that the induction of apoptosis by ML was associated with the loss of mitochondrial membrane potential. Collectively, our results suggest that apoptosis induced by ML in HL-60 cells was executed by a collapse of mitochondrial membrane potential followed by the activation of caspase-3. This is the first report on the mechanism of apoptosis-inducing effect of ML.     

螺内酯对老年充血性心力衰竭患者心率变异性的干预

目的探讨醛固酮受体拮抗剂螺内酯对老年充血性心力衰竭(CHF)患者心率变异性(HRV)的影响。方法比较52例老年CHF患者在螺内酯(20~40 mg/d)治疗前、第4、16周时HRV的时域指标及左室收缩功能的变化。结果螺内酯治疗4周时,左室收缩功能与治疗前相比差异无显著性意义(P>0.05),HRV的时域指标全部正常,R-R间期标准差(SDNN)、每5分钟R-R间期均值标准差(SDANN)及三角指数(TI)均有显著提高(P<0.05);治疗16周时,HRV上述时域指标进一步改善,同时左室收缩功能也有明显改善(P<0.05)。结论螺内酯可改善老年CHF患者的HRV,改善心功能。     

弯孢马利亚霉SIIA-F12361产生的新代谢产物研究

目的:对海洋生境来源菌株SIIA-F12361进行分类学鉴定以及次级代谢产物的化学研究.方法:采用形态学与18S rDNA序列分析对菌株进行分类学鉴定.通过硅胶柱层析、LH-20分子筛层析和反相制备HPLC诸方法,对新化合物进行分离纯化,并根据高分辨质谱、紫外、红外光谱和核磁共振数据对化合物SIIA-C12361进行结构鉴定.结果:鉴定菌株SIIA-F12361为弯孢马利亚霉,其产生的新次级代谢产物属于倍半萜烯内酯类化合物.结论:弯孢马利亚霉SIIA-F12361产生一新倍半萜烯内酯化合物.     

Anti-inflammatory activity of Eupatorium perfoliatum L. extracts, eupafolin, and dimeric guaianolide via iNOS inhibitory activity and modulation of inflammation-related cytokines and chemokines

Ethnopharmacological relevance

Eupatorium perfoliatum L. has been used traditionally for the treatment of fever, malaria and inflammation-associated diseases. Nowadays it is mostly used as immune activating remedy. The following study was performed to evaluate extracts with different polarity and defined lead-compounds from the herbal material on potential in vitro activities concerning immune cell activation, phagocytosis, and inflammation-related processes.

Materials and methods

MeOH-, EtOH-, and DCM extracts, beside several subfractions and isolated polysaccharides, sesquiterpene lactones and flavonoids were prepared and characterized analytically from the aerial parts of E. perfoliatum. Immunological activity was tested within lymphocyte transformation test on PBMC, test on enhancement of phagocytosis and of NO-production by murine RAW 264.7 macrophages. Anti-inflammatory effects were assessed from LPS-stimulated RAW 264.7 cells by NO/iNOS quantification, gene array, real-time PCR and ELISA.

Results

No stimulatory activity was found within lymphocyte transformation test, for phagocytic activity and NO formation in macrophages. MeOH-, EtOH- and DCM extracts showed anti-inflammatory activity against LPS-stimulated macrophages by inhibition of NO release (IC₅₀ > 100, 89, 19 μg/mL resp.) with eupafolin and a dimeric guaianolide having prominent NO inhibiting activity (IC₅₀ 6 resp. 16 μM). Anti-inflammatory activity was found on gene and protein level by significant down-regulation of cytokines CSF-3, IL-1α, IL-1β, and chemokines CCL2, CCL22 and CXCL10. Also TNF was down-regulated moderately (−17%).

Conclusions

Although the postulated immunostimulating properties of E. perfoliatum have not been confirmed, the anti-inflammatory effects can be seen as a verification of the traditional use against inflammatory diseases.     

丹参多酚酸提取物化学成分的分离与鉴定

目的研究丹参多酚酸提取物的化学成分。方法利用各种色谱技术进行分离纯化,利用光谱技术进行化合物结构解析。结果从丹参多酚酸提取物中分离得到7个化合物,分别鉴定为(2R)-2-[(7-羟基-2-羰基-2,3-二氢苯并呋喃基)-(4→3)-2-(2E)-烯丙酰氧基]-3-(3,4-二羟基苯基)-丙酸(1)、丹酚酸D(2)、原儿茶醛(3)、迷迭香酸(4)、紫草酸(5)、丹酚酸B(6)和丹酚酸Y(7)。结论化合物1为新化合物,命名为丹酚酸D内酯。     

A point mutation in a glutamate‐gated chloride channel confers abamectin resistance in the two‐spotted spider mite,Tetranychus urticae Koch

The molecular mechanisms and genetics of abamectin resistance mediated by target site insensitivity in the two‐spotted spider mite, Tetranychus urticae, were investigated by comparing two isogenic abamectin‐susceptible (AbaS) and abamectin‐resistant (AbaR) strains. Cloning and sequencing of full‐length cDNA fragments of γ‐amino butyric acid (GABA)‐gated chloride channel genes revealed no polymorphisms between the two strains. However, sequence comparison of the full‐length cDNA fragment of a T. urticae glutamate‐gated chloride channel gene (TuGluCl) identified a G323D point mutation as being tentatively related with abamectin resistance. In individual F₂ progenies obtained by backcrossing, the G323D genotype was confirmed to correlate with abamectin resistance. Bioassays using progeny from reciprocal crossings revealed that the abamectin resistance trait resulting from TuGluCl insensitivity is incompletely recessive.     

大孔吸附树脂纯化银杏叶提取物的工艺研究

目的:研究大孔吸附树脂分离纯化银杏叶提取物的工艺条件。方法:以银杏叶黄酮醇苷及银杏叶内酯为指标成分,考察大孔吸附树脂对有效成分的吸附和解析条件。结果:采用选用DA201作为纯化树脂,效果最好。结论:工艺成熟,产品质量达到较好水平,适合工业化生产。     

大鼠马桑内酯癫痫点燃模型P-170的表达

目的：探索大鼠马桑内酯癫痫点燃模型脑部星形胶质细胞及毛细血管内皮细胞P-170的表达。方法：用发作级数评分观察马桑内酯点燃大鼠，免疫组化法测定P-170蛋白的表达。结果：点燃大鼠脑部广泛区域的P-170表达较未点燃大鼠和正常大鼠显著增强，P-170的表达与马桑内酯（CL）的剂量无相关性（P〉0．05）。结论：SD大鼠马桑内酯癫痫点燃模型可用于建立一种耐药性癫痫模型。