平糖舒目散治疗糖尿病的作用机制初探

目的：通过醛糖还原酶高通量模型对中药方剂平糖舒目散的筛选,探寻其治疗糖尿病的作用机制。方法：用高通量醛糖还原酶筛模型来筛选平糖舒目散,研究方剂平糖舒目散对醛糖还原酶的抑制作用。结果：平糖舒目散对醛糖还原酶有较强的抑制作用,其半数抑制浓度是0．8 g／L。结论：中药方剂平糖舒目散治疗糖尿病慢性并发症的作用机制之一是抑制醛糖还原酶活性。     

四种中草药对大鼠半乳糖性白内障相关酶活性的影响

本实验测定了中草药对大鼠半乳糖性白内障延缓及治疗中五种酶活性的影响。结果表明,在白内障晶状体中,醛糖还原酶的活性明显升高;多元醇脱氢酶,己糖激酶,6磷酸葡萄糖脱氢酶及过氧化氢酶的活性明显降低。在注射半乳糖的同时,分别用黄芩、石斛、菟絲子及玉蝴蝶四种中草药水煎剂灌胃,醛糖还原酶的活性没有明显升高,其余四种酶的活性均基本恢复到正常,表明这四种中草药对半乳糖所致的酶活性异常变化有抑制或纠正作用。     

四种中草药抗白内障形成中晶状体脂类过氧化水平及脂类含量的变化

我们观察了中草药防治大鼠半乳糖性白内障形成中脂类含量的变化及脂类过氧化水平。结果表明,与正常晶状体相比,白内障晶状体中总脂类的含量明显降低,总胆固醇的含量及脂类过氧化水平明显升高,总脂类与总胆固醇之比明显下降。而同时分别用黄苓、石斛、菟丝子及玉蝴蝶四种中草药水煎剂灌胃的大鼠晶状体中,总胆类与总胆固醇的含量基本恢复至正常;脂类过氧化水平虽仍高于正常晶状体,但也明显低于白内障晶状体,表明脂类过氧化参与了白内障的形成,上述四种中草药具有抑制脂类过氧化的作用。     

沙苑子酚类提取物的抗氧化能力研究

为有效开发利用沙苑子,探究其抗氧化特性为深加工提供理论依据和经验参数,本文主要从沙苑子酚类提取物的总还原能力,对超氧阴离子自由基和羟基自由基的清除能力,及对Fe2+诱导的脂质过氧化的抑制作用等四个方面进行了研究并比较了三种不同沙苑子酚类提取物的抗氧化性能。结果表明沙苑子酚类提取物均具有一定的抗氧化能力,在实验浓度范围内呈现一定的量效关系。     

绿木霉(Trichoderma virens)T43对四种重要林木病原菌的抑制效果及抑菌机理

通过对峙培养和非挥发性代谢产物对病原菌生长的抑制作用,开展了木霉菌株T43及其抑菌活性物质抑制樟子松枯梢病、杨树烂皮病和苗木立枯病3种病害的4种病原菌效果的研究。从菌株T43发酵液乙酸乙酯提取物对各病原菌的3种保护酶(CAT、POD和SOD)活力影响和对细胞渗透调节物质(可溶性蛋白、可溶性糖和丙二醛)的含量影响,探讨了提取物对病原菌的抑菌机理。结果表明:木霉菌株T43及其代谢产物对供试林木病原菌均有明显的抑制作用,菌株T43发酵液乙酸乙酯提取物对病原菌3种保护酶活性均有不同程度的影响,可导致病原菌3种保护酶活性降低,尤其是SOD活性下降的最为显著。该提取物可以显著降低菌丝体可溶性糖和蛋白含量,提高丙二醛含量,破坏细胞的完整性,这可能是绿木霉T43发酵液乙酸乙酯提取物抑制病原菌生长的机理之一。     

Cd2+ 、Zn2+单一及复合胁迫对凤眼莲根质膜3种氧化还原酶活性的影响

采用水培法研究了不同浓度Cd2+ 、Zn2+单一及复合胁迫(0.05和0.50 mmol·L-1 Cd2+,0.5和5.0 mmol·L-1 Zn2+)对凤眼莲[Eichhornia crassipes (Mart. ) Solms]幼苗根质膜3种氧化还原酶[NADH氧化酶、Fe(CN)63-还原酶和EDTA-Fe3+还原酶]活性的影响. 结果表明, Cd2+ 、 Zn2+单一及复合胁迫对凤眼莲根质膜NADH氧化酶、Fe(CN)63-还原酶及EDTA-Fe3+还原酶活性的影响效应有明显的差异.0.05或0.50 mmol·L-1 Cd2+单一胁迫处理20 h可使凤眼莲根质膜3种氧化还原酶活性均较对照显著降低(P≤0.05),0.5或5.0 mmol·L-1 Zn2+单一胁迫20 h可导致凤眼莲根质膜NADH氧化酶和EDTA-Fe3+还原酶活性也均较对照显著降低(P≤0.05).随胁迫时间的延长,Cd2+ 、 Zn2+单一及复合胁迫处理均可使凤眼莲根质膜氧化还原酶活性增强,胁迫处理20 d时凤眼莲根质膜3种氧化还原酶活性均高于胁迫20 h的活性.Cd2+-Zn2+复合胁迫对凤眼莲根质膜3种氧化还原酶活性的影响效应因作用时间和胁迫浓度的不同而有一定的差异;在胁迫20 h时,Cd2+与Zn2+之间对凤眼莲根质膜3种氧化还原酶活性的作用关系较复杂,因胁迫浓度的不同表现出协同或拮抗的关系;胁迫20 d时,Cd2+与Zn2+对凤眼莲根质膜3种氧化还原酶活性的复合影响表现出明显的拮抗关系.研究结果显示,Cd2+ 、 Zn2+对凤眼莲根质膜氧化还原酶的复合作用效应与Cd2+和Zn2+的浓度比例及胁迫时间均相关.     

中草药来源的醛糖还原酶抑制剂研究进展

糖尿病并发症严重威胁着糖尿病人的生存质量,阻断或减弱醛糖还原酶活性的药物可以用来预防或推迟糖尿病并发症的发生。由于目前可供临床使用的醛糖还原酶抑制剂依然很少,且大部分抑制剂多由人工合成。中草药作为天然产物,来源广泛且无明显不良反应,在有效阻止和延缓糖尿病并发症如:血管病变、糖尿病肾病、外周神经病变、视网膜病变、方面显示了良好的应用前景。本文综述了近几年中草药来源的醛糖还原酶抑制剂研究进展。     

石榴皮多酚提取物对醛糖还原酶的抑制作用

本文分别以丙酮、甲醇和水为溶剂对石榴皮中的多酚进行了提取,得到3种提取物,采用紫外分光光度法表征了其对AR的抑制作用及抑制类型.3种提取物对AR活性均表现出抑制作用,且其作用大小与浓度呈明显的剂量-效应关系.3种提取物中,丙酮提取物的抑酶活性最强,甲醇提取物次之,水提物最弱,其对AR的半数抑制浓度(IC50,μg/mL)分别为34.77、44.18和62.07.石榴皮的丙酮和甲醇提取物对AR均能产生反竞争性抑制;当浓度为0.033 mg/mL时,其对AR的抑制常数(Ki)分别为49和71 μg/mL.     

仙人掌多糖对蛋白质糖基化终产物和醛糖还原酶的抑制效应

以仙人掌为原料提取多糖产品,通过超滤浓缩和不同浓度乙醇分级沉淀,分别得到55%乙醇沉淀的多糖(OPMC I),进一步乙醇浓度增至80%沉淀的多糖(OPMCⅡ),以及一次性80%乙醇沉淀的多糖(OPMCⅢ)。比较了三种多糖对蛋白质非酶糖基化反应的终端产物(AGEs)和醛糖还原酶(AR)形成的抑制作用。结果表明,在对AGEs形成的抑制过程中,第四周时OPMC II的抑制作用较强,且强于同剂量的氨基胍;在对AR活性的抑制作用中,OPMC II在三种多糖样品中抑制作用最强,但明显低于阳性对照物依帕司他。     

蓝莓提取物对金黄色葡萄球菌的抑制作用研究

本文以四种栽培蓝莓为主要研究对象,通过与山梨酸钾抑菌效果的比较,研究了蓝莓提取物对金黄色葡萄球菌(AB91093)的抑制作用,并测定了蓝莓中总酚酸和还原糖的含量。结果表明,蓝莓对金黄色葡萄球菌具有显著的抑菌效果。四种蓝莓提取物中,Elliott和Darrow提取物对金黄色葡萄球菌的抑制效果显著,分别在300 mg/mL和350 mg/mL时可明显抑制金黄色葡萄球菌的生长,450 mg/mL时能完全杀死金黄色葡萄球菌。蓝莓的抑菌能力与其酚酸含量正相关,与还原糖含量负相关。而山梨酸钾对金黄色葡萄球菌的MIC和MBC分别为100 mg/mL和200 mg/mL。     

Antioxidative and free radical scavenging activities of selected medicinal herbs

The antioxidative and superoxide- and hydroxyl radical-scavenging activities and pro-oxidant effect of twelve selected medicinal herbs were studied. The aqueous extracts of Coptis chinensis, Paeonia suffruticosa, Prunella vulgaris and Senecio scandens exhibited the highest potency in inhibiting rat erythrocyte hemolysis and lipid peroxidation in rat kidney and brain homogenates. The aforementioned four herbs also demonstrated strong superoxide- and hydroxyl radical-scavenging activity, but exerted only a slight pro-oxidant effect.     

中草药浸提液对小列当种子发芽的影响

选用240种常用中草药,研究其蒸馏水和甲醇浸提液原液及其10倍、100倍和1 000倍稀释液对小列当种子发芽的影响.结果表明:小列当种子在蒸馏水浸提液刺激下发芽率超过70%的中草药有灯心草、降香和莲须,在甲醇浸提液刺激下发芽率超过70%的中草药有百部、桑椹、谷芽和萆薢;蒸馏水浸提液对小列当种子发芽抑制率超过50%的中草药有菊花、棕榈、苦杏仁和黄柏,甲醇浸提液对小列当种子发芽抑制率超过70%的有续断、地黄、肉豆蔻、地肤子、黄连、木贼和胡黄连.大部分中草药浸提液在10倍稀释液条件下对小列当种子发芽的刺激或抑制作用最明显.研究发现,一些参试中草药蒸馏水和甲醇浸提液能够刺激或抑制小列当种子萌发,并且其对种子萌发的影响程度随浸提液浓度的变化而异,不同中草药最佳处理浓度不同,而且用甲醇浸提液可筛选出更多种具有化感作用的中草药.     

Anti-acetylcholinesterase activities of traditional Chinese medicine for treating Alzheimer's disease

Alzheimer's disease (AD) is a neurodegenerative disease characterized by progressive memory loss and cognitive impairment. It is the most common type of dementia in the ageing population due to a severe loss of cholinergic neurons in selected brain area. At present, acetylcholinesterase inhibitors (AChEI) are the first group of drugs approved by the FDA to treat mild to moderate Alzheimer's disease. Most of these drugs such as huperzine and galanthamine are originally isolated from plants. In this study, the AChE inhibitory activities from extracts of Chinese medicinal herbs that have traditionally been prescribed to treat insomnia and brain function disorders were examined in a 96-well plate assay based on Ellman's method. Both ethanol and aqueous extracts of 26 traditional Chinese medicinal herbs were tested. Inhibitory effects were expressed as the percentage of inhibition. For the herbal extracts that were shown to exert a significant inhibition, dose-dependent inhibitory assays were also performed. Ethanol and aqueous extracts of six herbs were found to have high AChE inhibitory activities in a dose-dependent manner. The IC(50) of these herbal extracts on inhibition of AChE are at around 5-85mum/ml. The results of this study indicate that there is a great potential to search for novel usage of these medicinal herbs for the treatment of AD.     

Polyol pathway in tissues of spontaneously diabetic Chinese hamsters (Cricetulus griseus) and the effect of an aldose reductase inhibitor, ONO-2235

1. Sorbitol and fructose levels were significantly elevated in the lens, the sciatic nerve, the retina and the kidney of diabetic Chinese hamsters and inositol level was significantly decreased in the lens and sciatic nerve of diabetics. 2. The activity of an aldose reductase in the kidney was not different between normal and diabetic Chinese hamsters. 3. An aldose reductase inhibitor (ONO-2235) had no effect in sorbitol, fructose and inositol contents of all these tissues from diabetic Chinese hamsters. 4. These results suggest that diabetic Chinese hamsters produce polyol accumulation in tissues but that there is a clear species-specific difference to inhibition of aldose reductase.     

中草药提取物中单宁(鞣质)的选择性脱除

用牛皮为原料通过甲醛交联反应制备胶原纤维吸附材料,采用外加单宁的方法研究了这种吸附材料对双黄莲口服液、银黄注射液及中草药提取物中单宁的选择性吸附能力。结果表明,胶原纤维对单宁具有明显的竞争吸附能力和吸附选择性,在实验条件下单宁的去除率达到97％以上,而对有效成份吸附率很低。皮胶原纤维吸附材料为中药制剂工艺中单宁的高选择性脱除提供了一种新的、有效的方法。     

Investigation of the biosynthetic potential of endophytes in traditional Chinese anticancer herbs

Traditional Chinese medicine encompasses a rich empirical knowledge of the use of plants for the treatment of disease. In addition, the microorganisms associated with medicinal plants are also of interest as the producers of the compounds responsible for the observed plant bioactivity. The present study has pioneered the use of genetic screening to assess the potential of endophytes to synthesize bioactive compounds, as indicated by the presence of non-ribosomal peptide synthetase (NRPS) and polyketide synthase (PKS) genes. The total DNA extracts of 30 traditional Chinese herbs, were screened for functional genes involved in the biosynthesis of bioactive compounds. The four PCR screens were successful in targeting four bacterial PKS, six bacterial NRPS, ten fungal PKS and three fungal NRPS gene fragments. Analysis of the detected endophyte gene fragments afforded consideration of the possible bioactivity of the natural products produced by endophytes in medicinal herbs. This investigation describes a rapid method for the initial screening of medicinal herbs and has highlighted a subset of those plants that host endophytes with biosynthetic potential. These selected plants can be the focus of more comprehensive endophyte isolation and natural product studies.     

Chinese medicinal herbs modulate mutagenesis, DNA binding and metabolism of aflatoxin B1.

Oldenlandia diffusa (OD) and Scutellaria barbata (SB) have been used in traditional Chinese medicine for treating liver, lung and rectal tumors while Astragalus membranaceus (AM) and Ligustrum lucidum (LL) are often used as an adjunct in cancer therapy. In this study, we determined the effects of aqueous extracts of these four herbs on aflatoxin B1 (AFB1)-induced mutagenesis using Salmonella typhimurium TA100 as the bacterial tester strain and rat liver 9000 x g supernatant as the activation system. The effects of these herbs on [3H]AFB1 binding to calf-thymus DNA were assessed. Organosoluble and water-soluble metabolites of AFB1 were extracted and analyzed by high-performance liquid chromatography (HPLC). Mutagenesis assays revealed that all of these herbs produced a concentration-dependent inhibition of histidine-independent revertant (His+) colonies induced by AFB1. At a concentration of 1.5 mg/plate, SB and OD in combination exhibited an additive effect. The trend of inhibition of these four herbs on AFB1-induced mutagenesis was: SB greater than LL greater than AM. LL, OD and SB significantly inhibited AFB1 binding to DNA, reduced AFB1-DNA adduct formation, and also significantly decreased the formation of organosoluble metabolites of AFB1. Our data suggest that these Chinese medicinal herbs possess cancer chemopreventive properties.     

Antioxidant activity and phenolic compounds of 112 traditional Chinese medicinal plants associated with anticancer

Cancer prevention and treatment using traditional Chinese medicines have attracted increasing interest. This study characterizes antioxidant activity and phenolic compounds of traditional Chinese medicinal plants associated with anticancer, comprising 112 species from 50 plant families. The improved ABTS(*+) method was used to systematically assess the total antioxidant capacity (Trolox equivalent antioxidant capacity, TEAC) of the medicinal extracts. The TEAC values and total phenolic content for methanolic extracts of herbs ranged from 46.7 to 17,323 micromol Trolox equivalent/100 g dry weight (DW), and from 0.22 to 50.3 g of gallic acid equivalent/100 g DW, respectively. A positive, significant linear relationship between antioxidant activity and total phenolic content (all R(2) values>/=0.95) showed that phenolic compounds were the dominant antioxidant components in the tested medicinal herbs. Major types of phenolic compounds from most of the tested herbs were preliminarily identified and analyzed, and mainly included phenolic acids, flavonoids, tannins, coumarins, lignans, quinones, stilbenes, and curcuminoids. These medicinal herbs exhibited far stronger antioxidant activity and contained significantly higher levels of phenolics than common vegetables and fruits. Traditional Chinese medicinal plants associated with anticancer might be potential sources of potent natural antioxidants and beneficial chemopreventive agents.