芩连四物汤化学物质基础及其抗凝血活性研究

目的:研究芩连四物汤的化学物质基础及其抗凝血生物效应。方法:采用水煎醇沉,醇溶液减压回收乙醇,用适量水溶解后,上D101大孔树脂采用不同浓度的乙醇梯度洗脱,各不同洗脱部位采用硅胶柱层析的方法分离,所得单体通过UV,IR,NMR及MS等方法确定其化学结构;将所得成分配成水溶液(100μmol·L^-1),采用体外法测定对血浆凝血酶时间(TT)的影响。结果:从芩连四物汤中分离并鉴定了5个黄酮类成分、1个生物碱、3个芳香酸、1个倍半萜类成分及2个其它类化合物。黄酮苷元、芳香酸、生物碱及倍半萜类化合物均能显著延长血浆凝血酶时间(TT)。结论:首次对芩连四物汤整方进行化学物质分离和结构分析研究,其中9个化合物,包括千层纸素A、汉黄芩素、6-甲氧基汉黄芩素、小檗碱、黄芩素、阿魏酸、香草酸、咖啡酸、地黄苦苷元显示了一定的体外抗凝血活性。     

Procyanidins extracted from the lotus seedpod ameliorate scopolamine‐induced memory impairment in mice

The major purpose of this study was to determine the effect of procyanidins extracted from the lotus seedpod (LSPC) on the learning and memory impairments induced by scopolamine (1 mg/kg, i.p.) in mice. The capacities of memory and learning were evaluated by the Morris water maze and the step‐down avoidance test. LSPC (50, 100, 150 mg/kg BW, p.o.) significantly reversed scopolamine‐induced learning and memory impairments in the Morris water maze test, as evaluated by shortened escape latency and swimming distance. In the step‐down avoidance test, LSPC (50, 100, 150 mg/kg BW, p.o.) treatment significantly reduced the number of errors and shortened latency compared with that of scopolamine. In addition, LSPC was also found to inhibit acetyl cholinesterase (AChE) activity. These results of this study suggest that LSPC may play a useful role in the treatment of cognitive impairment caused by AD and aging. Copyright © 2009 John Wiley & Sons, Ltd.     

Suppression of lipopolysaccharide-induced inflammatory responses in RAW 264.7 murine macrophages by aqueous extract of Clinopodium vulgare L. (Lamiaceae)

Ethnopharmacological relevance

The wild basil Clinopodium vulgare L. is commonly used in Bulgarian folk medicine for treatment of irritated skin, mastitis- and prostatitis-related swelling, as well as for some disorders accompanied with significant degree of inflammation (e.g. gastric ulcers, diabetes, and cancer).

Aim of study

To determine the effect of aqueous extract of Clinopodium vulgare L. on LPS-induced inflammatory responses of murine RAW 264.7 macrophages.

Materials and methods

Cell cytotoxicity was evaluated by MTT assay. Protein expression levels were monitored by Western blot analysis. Production of NO and PGE₂ was measured by the Griess colorimetric method and enzyme immunoassay, respectively. Activation of MMP-9 was visualized by gelatin zymography. Cytokine levels were determined by BioPlex assay. Intracellular ROS and free radical scavenging potential were measured by DCFH-DA and DPPH method, respectively. Xanthine oxidase activity was evaluated spectrophotometrically.

Results

The extract suppresses NF-κB activation by preventing Iκ-B phosphorylation and inhibits the phosphorylation of p38 and SAPK/JNK MAPKs. It down-regulates iNOS expression which manifests as a drastic decrease of NO production, inhibits MMP-9 activation, but does not affect COX-2 protein levels and reduces only slightly the released PGE₂. Secretion of IL-1β and Il-10 is greatly reduced, whereas suppression of TNF-α and GM-CSF production is less dramatic. The extract has strong free radical scavenging properties and exerts inhibitory effect on xanthine oxidase activity, which lowers the levels of intracellular ROS.

Conclusion

The study provides evidence for the anti-inflammatory potential of Clinopodium vulgare L. aqueous extract.     

高压脉冲电场对乳铁蛋白抑菌性能的影响

研究了高压脉冲电场(PEF)对乳铁蛋白(LF)的抑菌性能的影响。结果表明,LF质量浓度、电场强度、脉冲频率、脉冲数的增加,有利于LF抑菌能力的增强,而温度的升高会使之减弱。电场强度为35 kV/cm时,LF的抑菌能力达到最大值。LF的质量浓度越高,对电场强度的变化越敏感。当脉冲个数达到744时,LF的相对抑菌能力提高了34%。处理温度为15～55℃时,PEF处理的LF的相对抑菌性能增长了5%左右。当温度升高至65℃时,LF的相对抑菌能力下降显著,降低了约22%。     

人源性多肽pCM-19抗菌机制的初步研究

目的：初步分析人源性多肽pCM-19的抗菌作用机制。方法：利用荧光素掺入破损细胞膜的原理，采用流式荧光激活细胞分析（FACScan）和扫描电子显微镜分析pCM-19对靶菌膜的作用机制。结果：FACS分析法结果显示pCM-19处理后的大肠杆菌PI着染细菌比例明显高于未处理组，并且随作用时间的延长，PI着染BL-21菌比例增大，20min时达最高水平，20min以后反而降低；扫描电子显微镜观察到pCM-19处理后的大肠杆菌有明显的表面形态学的改变，如细菌体积缩小、细菌表面出现皱缩、凹陷似有孔洞形成。结论：人源性多肽pCM-19可能作用于细菌细胞壁和（或）细胞膜，通过改变其通透性而发挥杀菌作用。     

Flavocoxid is as effective as naproxen for managing the signs and symptoms of osteoarthritis of the knee in humans: a short-term randomized,double-blind pilot study

Flavocoxid (Limbrel), a proprietary mixture of flavonoid molecules (baicalin and catechin), was tested against a traditional nonsteroidal anti-inflammatory drug, naproxen, for the management of the signs and symptoms of moderate osteoarthritis (OA) in humans. Discomfort and global disease activity were used as the primary end points, and safety assessments were also taken for both treatments as a secondary endpoint. In this double-blind study, 103 subjects were randomly assigned to receive either flavocoxid [500 mg twice daily (BID)] or naproxen (500 mg BID) in a 1-month onset of action trial. Outcome measures included the short Western Ontario and McMaster University Osteoarthritis Index, subject Visual Analogue Scale for discomfort and global response, and investigator Visual Analogue Scale for global response and fecal occult blood. Both flavocoxid and naproxen showed significant reduction in the signs and symptoms of knee OA (P ≤ .001). There were no statistically detectable differences between the flavocoxid and naproxen groups with respect to any of the outcome variables. Similarly, there were no statistically detectable differences between the groups with respect to any adverse event, although there was a trend toward a higher incidence of edema and nonspecific musculoskeletal discomfort in the naproxen group. In this short-term pilot study, flavocoxid was as effective as naproxen in controlling the signs and symptoms of OA of the knee and would present a safe and effective option for those individuals on traditional nonsteroidal anti-inflammatory drugs or cyclooxygenase-2 inhibitors. A low incidence of adverse events was reported for both groups.     

Antioxidant and antiinflammatory activity of pine pollen extract in vitro

To determine the medicinal properties of pine pollen, the antioxidant and antiinflammatory activities of the ethanol extract of pine pollen extract (PPE) were investigated. PPE displayed a strong free radical scavenger activity on 1,1‐diphenyl‐2‐picrylhydrazyl radical and hydrogen peroxide. It was observed also that the antioxidant activity, measured by the ferric thiocyanate method, increased with the addition of PPE to the linoleic acid emulsion system. PPE was also found to inhibit significantly the amount of malondialdehyde and protein carbonyls formed from liver homogenate. Like the antioxidant activity, the reducing power of PPE was excellent. Thereafter, the study investigated the effects of PPE in modulating the production of pro‐inflammatory mediators in lipopolysaccharide (LPS)‐activated RAW 264.7 macrophages, and the effect of PPE on interleukin (IL)‐1β‐induced matrix metalloproteinases (MMPs) production and mitogen‐activated protein kinases (MAPKs) activation in the human synovial sarcoma cell line, SW982. PPE was found to inhibit the production of nitric oxide, tumor necrosis factor‐α, IL‐1 and IL‐6 in LPS‐activated macrophages. Treatment with PPE at 10 µg/mL significantly (p < 0.05) inhibited IL‐1β‐induced MMPs (MMP‐1 and ‐3) production in SW982 cells. IL‐1β‐induced JNK activation was inhibited by PPE (10 µg/mL), whereas p38 and ERK1/2 were not affected. These findings suggest that pine pollen is a potential antioxidant and beneficial for inflammatory conditions through down‐regulation of JNK and MMPs. Copyright © 2008 John Wiley & Sons, Ltd.     

Differentiation of Motor Activity of Normally Active and Hyperactive Boys in Schools: Some Preliminary Results

All non-task-related body movements during school hours were listed in 11 normally active and 12 hyperactive boys. The mean number of movements was 48 +/- 7 per 45 minutes in the normal actives and 79 +/- 16 per 45 minutes in the hyperactives. The rather monotonous increment and decrement of motor activity during the 4-hr registration period was noticed only in hyperactive boys. These results could be a consequence of a circadian rhythm, as there was independence of type of school hours and of teacher personality. The cyclical level of activity in hyperactive boys was sometimes in the range of the normal actives.     

Seasonal variation in the content of a febrifugine and isofebrifugine alkaloid mixture in aerial parts of <Emphasis Type="Italic">Hydrangea macrophylla</Emphasis> var. <Emphasis Type="Italic">Otaksa</Emphasis>, with special reference to its antimalarial activity

Febrifugine and isofebrifugine alkaloid mixtures extracted from the leaves and buds of Hydrangea macrophylla var. Otaksa, collected during different months, in Japan, were quantified using high-performance liquid chromatography. Leaves collected during the flowering season, namely from June to August, contained 0.16–0.31 mg/g of the alkaloid mixture, whereas those collected from September to December had less than 0.03 mg/g of the mixture. However, extracts of buds harvested from October to February contained a consistently larger amount (more than 0.49 mg/g) of the alkaloids. Hot-water extracts from the leaves and buds collected during different seasons were evaluated for antimalarial activity against Plasmodium yoelii 17XL in mice. The extract of leaves collected in August demonstrated high antimalarial activity, and all mice that received the extract survived the infection. In contrast, the extract of leaves collected in December showed little activity. The extract of buds collected in December cleared parasites, but with subsequent mortality to mouse. The present results show that the amount of antimalarial agent—febrifugine and isofebrifugine mixture—in H. macrophylla var. Otaksa is both part- and season-dependent, suggesting that the choice of plant parts and their harvesting season are important factors worth considering in the pharmacological use of medicinal plants.     

42例室性心动过速治疗的临床分析

本文介绍了42例室性心动过速的临床资料和特点,讨论了早期后除极与室性心动过速的关系,并探讨各型室速的治疗。