Tissue factor inhibitory sesquiterpene glycoside from<Emphasis Type="Italic">Eriobotrya japonica</Emphasis>

Tissue factor (TF, tissue thromboplastin) is a membrane bound glycoprotein, which accelerates the blood clotting, activating both the intrinsic and the extrinsic pathways to serve as a cofactor for activated factor VII (Vlla). The TF-factor Vlla complex (TF/Vlla) proteolytically activates factors IX and X, which leads to the generation of thrombin and fibrin clots. In order to isolate TF inhibitors, by means of a bioassay-directed chromatographic separation technique, from the leaves ofEriobotrya japonica Lindley (Rosaceae), a known sesquiterpene glycoside (2) and ferulic acid (3) were isolated as inhibitors that were evaluated using a single-clotting assay method for determining TF activity. Another sesquiterpene glycoside (1) was also isolated but was inactive in the assay system. Compound3 was yielded by alkaline hydrolysis of compound2. The structures of compounds1, 2, and3 were identified by means of spectral analysis as 3-O-α-L-rhamnopyranosyl-(1→4)-α-L-rhamnopyranosyl-(1→2)-[α-L-rhamnopyranosyl-(1→6)]-β-D-glucopyranosyl nerolidol (1), 3-O-α-L-rhamnopyranosyl-(1→4)-α-L-rhamnopyr-anosyl-(1→2)-[α-L-(4-trans-feruloyl)-rhamnopyranosyl-(1→6)]-β-D-glucopyranosyl nerolidol (2) and ferulic acid (3), respectively. Compounds2 and3 inhibited 50% of the TF activity at concentrations of 2 and 369 μM/TF units, respectively.     

Flavonol glycosides from the aerial parts of<Emphasis Type="Italic">Aceriphyllum rossii</Emphasis> and their antioxidant activities

The methanol extract obtained from the aerial parts ofAceriphyllum rossii (Saxifragaceae) was fractionated into ethyl acetate (EtOAc),n-BuOH and H₂O layers through solvent fractionation. Repeated silica gel column chromatography of EtOAc andn-BuOH layers afforded six flavonol glycosides. They were identified as kaempferol 3-O-β-D-glucopyranoside (astragalin,1), quercetin 3-O-β-D-glucopyranoside (isoquercitrin,2), kaempferol 3-O-α-L-rhamnopyranosyl (1→6)-β-D-glucopyranoside (3), quercetin 3-O-α-L-rhamnopyranosyl (1→6)-β-D-glucopyrano-side (rutin,4), kaempferol 3-O-[α-L-rhamnopyranosyl (1→4)-α-L-rhamnopyranosyl (1→6)-β-D-glucopyranoside] (5) and quercetin 3-O-[α-L-rhamnopyranosyl (1→4)-α-L-rhamnopyranosyl (1→6)-β-D-glucopyranoside] (6) on the basis of several spectral data. The antioxidant activity of the six compounds was investigated using two free radicals such as the ABTS free radical and superoxide anion radical. Compound1 exhibited the highest antioxidant activity in the ABTS2,2-azinobis-(3-ethylbenzothiazoline-6-sulfonic acid) radical scavenging method. 100 mg/L of compound1 was equivalent to 72.1±1.4 mg/L of vitamin C, and those of compounds3 and5 were equivalent to 62.7±0.5 mg/L and 54.3±1.3 mg/L of vitamin C, respectively. And in the superoxide anion radical scavenging method, compound5 exhibited the highest activity with an IC₅₀ value of 17.6 ± 0.3 μM. In addition, some physical and spectral data of the flavonoids were confirmed.     

Urinary collagen metabolite excretion in amyotrophic lateral sclerosis

Collagen abnormalities of the spinal cord and the skin have been reported in patients with amyotrophic lateral sclerosis (ALS). The urinary concentrations of the hydroxylysine glycosides, i.e., glucosylgalactosyl hydroxylysine (glu-gal Hyl) and galactosyl hydroxylysine (gal Hyl), indicate the tissue origin of the collagen metabolites and the rate of the degradation of collagen. We measured the urinary levels of glu-gal Hyl and gal Hyl in 12 ALS patients, 10 diseased control subjects with other neurologic or muscular diseases (Control Group A), and 10 healthy control subjects (Control Group B). The urinary level of glu-gal Hyl in ALS patients was significantly lower than in the two control groups. In addition, a significant negative relationship between glu-gal Hyl urinary level and duration of illness was found in ALS patients. There was no marked difference in the urinary level of gal Hyl between ALS patients and the control groups. Our data suggest that the decreased urinary level of glu-gal Hyl may be useful in assessing the alteration in collagen metabolism in ALS and may have a relationship with the progression of ALS.     

黔岭淫羊藿化学成分的研究Ⅰ

 目的:对黔岭淫羊藿(Epimedium leptorrhizumStearm.)的化学成分进行分离,并鉴定其化学结构?方法:采用柱层析方法进行分离,用UV,IR,MS,¹H-NMR和¹³C-NMR等光谱技术鉴定化合物的结构?结果:从醋酸乙酯部分分离到4个化合物,经鉴定为:thalictoside(Ⅰ),2″-鼠李糖基淫-羊藿次苷Ⅱ[2″-O-rhamnosyl-icarisidⅡ(Ⅱ)],箭藿苷A[sagitatosideA(Ⅲ)],大花淫羊藿苷B[ikarisosideB(Ⅳ)]?结论:化合物Ⅰ为苯酚苷类化合物,化合物Ⅱ,Ⅲ,Ⅳ为8-异戊烯基黄酮苷类化合物,4个化合物均为首次从该植物中分离得到?     

A new lignan glycoside from Trigonostemon heterophyllus

Phytochemical investigation on the stems of Trigonostemonheterophyllus led to the isolation of a new lariciresinol-based lignan glycoside, trigonoheteran (1), together with a known lignan glycoside, aviculin (2). Their structures were elucidated by spectroscopic methods including 1D and 2D NMR (HMQC, ¹H–¹H COSY, HMBC, and NOESY).     

十三种洋地黄属强心甙成分的反相高效液相分离

洋地黄属强心甙系由玄参科洋地黄属植物中提取出的混合物,是重要的治疗心脏病药物。由于其成分复杂,分离其所含的各强心甙成分十分困难。本文采用反相高效液相色谱法,在传统用于分离洋地黄强心甙成分的乙腈—水流动相系统中加入一定量甲醇作改进剂,并进行凹形梯度洗脱,大大改进了结构极为近似的强心甙的分离,13种洋地黄属强心甙化合物得到了满意的分离。     

A Direct Comparison of the Anticancer Activities of Digitoxin MeON-Neoglycosides and O-Glycosides: Oligosaccharide Chain Length-Dependent Induction of Caspase-9-Mediated Apoptosis

Digitoxin is a cardiac glycoside currently being investigated for potential use in oncology. While a number of structure-activity relationship studies have been conducted, an investigation of anticancer activity as a function of oligosaccharide chain length has not yet been performed. We generated mono-, di-, and tri-O-digitoxoside derivatives of digitoxin and compared their activity to the corresponding MeON-neoglycosides. Both classes of cardenolide derivatives display comparable oligosaccharide chain length-dependent cytotoxicity toward human cancer cell lines. Further investigation revealed that both classes of compounds induce caspase-9-mediated apoptosis in non-small cell lung cancer cells (NCI-H460). Since O-glycosides and MeON-neoglycosides share a similar mode of action, the convenience of MeON-neoglycosylation could be exploited in future SAR work to rapidly survey large numbers of carbohydrates to prioritize selected O-glycoside candidates for traditional synthesis.     

山茱萸环烯醚萜苷对局灶性脑缺血模型大鼠神经功能和神经元损伤的影响

目的观察山茱萸环烯醚萜苷（CIG）对大脑中动脉阻塞法（MACO）致脑缺血再灌注模型大鼠神经功能和神经细胞的影响。方法用线栓法制备局灶性脑缺血大鼠模型，缺血2h再灌注24h。采用评分法检测神经功能改变，用尼氏染色的方法检测梗死灶神经元的变化。结果模型组与假手术组相比，神经症状评分明显升高，梗死灶神经元数量明显减少。与模型组相比，CIG灌胃口服能够明显降低模型大鼠神经症状评分，增加梗死灶神经元的存活数量。结论CIG对大鼠局灶性脑缺血有明显改善作用。     

Doehlert设计法优化紫珠中苯乙醇苷的提取工艺

目的:研究乙醇回流法提取枇杷叶紫珠中苯乙醇苷的优化工艺。方法:以料液比、提取时间、乙醇体积分数为3个考察因素,苯乙醇苷含量为指标,运用响应面分析法中的Doehlert设计法进行试验设计,并采用统计学和数学软件对试验数据进行分析,拟合出苯乙醇苷类的最优提取工艺条件。结果:优选的提取条件为以12倍量90%乙醇回流提取2次,每次2 h。结论:应用Doehlert设计的响应面优化法具有使用方便、预测性好的特点,值得推广应用。     

二苯乙烯苷对大鼠骨密度与骨强度的影响

目的：检测由何首乌中提取的有效成分2,3,5,4＇-四羟基二苯乙烯-2-O-β-D葡萄糖苷（二苯乙烯苷）,长期给药对大鼠骨密度及骨强度的影响。方法：大鼠分别按剂量150 mg/kg、300 mg/kg、600 mg/kg连续灌胃给药90 d,使用双能X线骨密度扫描仪测量大鼠骨密度后,处死取股骨测量骨9骼强度。结果：二苯乙烯苷各剂量组均能增加髂骨段的骨密度,增加髂骨段和肱骨段的骨矿重量和骨矿面积;显著增加骨折力与骨碎力。结论：二苯乙烯苷不仅能够增强骨密度,提高单位面积骨矿的含量及骨矿在组织中的含有面积,增强骨组织对于外力作用的抵抗能力,提高结构韧性与结构强度,为临床有效预防并改善骨质疏松症提供实验依据。