头花蓼提取工艺的优化及其抗菌活性

目的优化头花蓼提取工艺,并评价其抗菌活性。方法在单因素试验基础上,以料液比、乙醇体积分数、提取温度、提取时间为影响因素,提取率为评价指标,采用响应面法优化提取工艺。然后,通过测定抑菌圈直径考察提取物对大肠杆菌、金黄色葡萄球菌的抑制作用。结果最佳条件为料液比25∶1,乙醇体积分数79%,提取温度80℃,提取时间1.5 h,提取率12.7%。在质量浓度为20 mg/mL时,提取物对金黄色葡萄球菌的抑菌圈直径为13 mm;在50 mg/mL时,对大肠杆菌的抑菌圈直径为11.5 mm。结论该方法稳定可靠,可用于提取头花蓼,并且该药材有较好的抗菌活性。     

连翘对金黄色葡萄球菌及表皮葡萄球菌的体外抗菌活性研究

[目的]观察连翘对金黄色葡萄球菌及表皮葡萄球菌的体外抗菌活性。[方法]用新的中药抑菌实验方法进行连翘对84株金葡菌和140株表皮葡萄球菌的体外抗菌活性的测定。[结果]连翘对金葡菌和表皮葡萄球菌能抑制50%菌株的最低细菌浓度(MIC50)均为0.122g/L,而能抑制90%菌株的最低抑菌浓度(MIC90)分别为0.98和0.244g/L。[结论]连翘对金黄色葡萄球菌和表皮葡萄球菌均有较好的体外抗菌效果。     

头花蓼化学成分及抗氧化活性研究

目的：对头花蓼的化学成分及其生物活性进行研究,为阐明有效成分提供依据。方法：利用硅胶、聚酰胺和Sephadex LH-20对其化学成分进行分离纯化,根据化合物的理化性质及光谱数据鉴定其结构。采用化学发光法测试化合物的抗氧化活性。结果：从该植物全草中分得10个化合物,分别鉴定为没食子酸（1）,原儿茶酸（2）,没食子酸乙酯（3）,山柰酚（4）,槲皮素（5）,槲皮苷（6）,阿魏酸二十四烷酯（7）,槲皮素-3-O-β-D-葡萄糖苷（8）,β-胡萝卜苷（9）和β-谷甾醇（10）。在药理活性研究中,化合物1～6在不同的药理模型中均显示了一定的抗氧化活性。结论：化合物3和7是从该属植物中首次分离得到,化合物2、4和9为该植物中首次分离得到。化合物1-6均具有一定的抗氧化作用,这也是首次对该植物的单体成分进行药理活性研究。     

头花蓼种子育苗技术研究

目的研究头花蓼种子育苗技术。方法头花蓼种子育苗选用肥沃疏松的沙质壤土或疏松肥沃的人工混合土做育苗基质,采用种子拌细土(1∶200)撒播,播种后厢面盖地膜再起塑料拱棚进行保温、保湿,并加强揭膜、浇水等田间管理。结果通过对育苗基质、覆土厚度、播种方法、播种后保温保湿措施等影响头花蓼种子育苗的因素进行系列试验研究,提出了头花蓼种子育苗的可行方法,并研究制订了种苗质量标准。结论头花蓼种子育苗技术可在头花蓼GAP基地建设中推广应用。     

头花蓼规范化种植密度研究

为了确定头花蓼规范化种植的最佳种植密度,提供制订头花蓼种植SOP的科学的数据,我们以不同株、行距组合成21种种植密度,采用方差法对其不同栽培密度下的药材产量进行了统计分析.结果表明,不同种植密度对头花蓼的产量存在显著影响.头花蓼规范化种植的最佳种植密度为20cm×20cm.     

9种蓼科植物抗菌活性

目的:研究9种蓼科植物的体外抗菌活性.方法:采用纸片扩散法和多孔板法研究9种蓼科植物的不同提取物对金黄色葡萄球菌(SA)、耐甲氧西林的金黄色葡萄球菌(MRSA)和β-内酰胺酶阳性的金黄色葡萄球菌(ESBLs-SA)的抑制活性.结果:四季红甲醇提取物和四季红乙酸乙酯提取物质量浓度在50 g·L-1对SA,MRSA和ESBLs-SA的抑菌圈直径较大,其中四季红乙酸乙酯提取物对3种菌均有抑制作用,MIC全部为0.062 5 g·L-1;多孔板法中,辣蓼乙酸乙酯提取物(IC50 0.45 g·L-1)活性最好.结论:实验证明蓼科植物提取物对SA,MRSA,ESBLs-SA有较好的抑制作用,尤其是四季红和辣蓼的抗菌活性较显著.     

头花蓼营养生长特性观察研究

目的：研究野生变家种头花蓼枝叶为主的营养生长特性。方法：采用固定植株跟踪观察法，研究观察其株高、主分枝数、主枝长、枝径、叶片大小和植株覆盖面，同时观察其根系生长状况。结果：6～8月中旬前为头花蓼的主要生长期，在此期间生长快速，而其主根、须根均不发达。结论：头花蓼具有以枝叶为主的营养生长特性，其主根、须根均不发达；6-8月中旬前为野生变家种头花蓼的主要生长期。     

头花蓼种子发芽生物学特性研究

目的研究头花蓼PolygonumcapitatumBuch.-Ham.exD.Don种子发芽的生物学特性。方法通过不同温度和黑暗条件下的发芽试验以及浸种处理发芽试验,观察统计其发芽所需时间、发芽持续时间、发芽势、发芽率。结果头花蓼种子在10～35℃下都能发芽;10～30℃下都能发芽完全;20℃、25℃时,观察的4项指标都无显著差异,并出现最短的发芽时间(4d)和最高发芽率(93.3%)。光照能使发芽时间缩短4天,发芽势提高50.6%,但不影响发芽率。浸种处理会降低头花蓼种子的发芽势和发芽率,特别是温水浸种达到极显著水平。结论20～25℃是头花蓼种子发芽的最适温度。发芽期间给予光照能极显著缩短发芽时间和提高发芽势。浸种处理对头花蓼种子的萌发没有促进作用。     

头花蓼种子发芽条件研究

目的:研究不同条件对头花蓼种子发芽的影响,为头花蓼种子发芽率检验及田间播种提供参考。方法:考察温度、培养方式以及盐胁迫对头花蓼种子发芽的影响,用培养皿法培养种子,统计发芽率。结果:头花蓼种子于15℃发芽率最高;在盐胁迫条件下,随着盐浓度的升高种子发芽率呈下降趋势,低盐条件下,发芽率与对照差异不显著;在同一温度条件下光培养比暗培养发芽率高,纸间比纸上发芽率高。结论:头花蓼种子发芽率检验时应选择15℃,有光照条件、双层滤纸纸间培养方式进行,在发芽试验进行20 d时,计算种子发芽势。头花蓼种子播种时,播种育苗田盐浓度不能高于1~2 g/L,过高影响头花蓼种子发芽。     

头花蓼酚酸类化学成分研究

目的 研究头花蓼Polygonum capitatum的酚酸类化学成分.方法 通过各种柱色谱技术对头花蓼进行分离纯化,根据理化性质、色谱性质和波谱数据进行结构鉴定.结果 从头花蓼地上部分中分离得到了13个化合物,分别鉴定为:丁香酸(4-hydroxy-3,5-dimethoxybenzoic acid;1);儿茶酚(catechol;2);5, 7-二羟基色原酮(5,7-dihydroxy-4H-chromen-4-one;3);3, 5-二羟基-4-甲氧基苯甲酸(3,5-dihydroxy-4-methoxybenzoic acid;4);原儿茶酸乙酯(ethyl protocatechuate;5);没食子酸乙酯(ethyl gallate;6);没食子酸(gallic acid;7);原儿茶酸(protocatechuic acid;8);槲皮素(quercetin;9);槲皮苷(quercitrin;10);陆地棉苷(hirsutine, quercetin-3-O-β-D-glucopyranoside;11);槲皮素-3-O-(2'-没食子酰基)-鼠李糖苷(quercetin-3-O-α-L-rhamnoside-2"-gallate;12);芦丁(rutin;13).结论 化合物1～4为首次从该植物中分离得到.     

Antibacterial activity of Curcuma longa L. against methicillin-resistant Staphylococcus aureus

Methicillin-resistant Staphylococcus aureus (MRSA) has been emerging worldwide as one of the most important hospital and community pathogens. Therefore, new agents are needed to treat MRSA associated infections. The present study investigated the antimicrobial activity of ethyl acetate, methanol and water extracts of Curcuma longa L. (C. longa) against MRSA. The ethyl acetate extract of C. longa demonstrated a higher antibacterial activity than the methanol extract or water extract. Since the ethyl acetate extract was more active than the other extracts, the study examined whether the ethyl acetate extract could restore the antibacterial activity of beta-lactams and alter the MRSA invasion of human mucosal fibroblasts (HMFs). In the checkerboard test, the ethyl acetate extract of C. longa markedly lowered the MICs of ampicillin and oxacillin against MRSA. In the bacterial invasion assay, MRSA intracellular invasion was significantly decreased in the presence of 0.125-2 mg/mL of C. longa extract compared with the control group. These results suggest that the ethyl acetate extract of C. longa may have antibacterial activity and the potential to restore the effectiveness of beta-lactams against MRSA, and inhibit the MRSA invasion of HMFs.     

广藿香精油对金黄色葡萄球菌的抑菌活性及机制研究

目的以金黄色葡萄球菌为供试菌,探讨广藿香精油的抑菌活性及其作用机制。方法通过测定广藿香精油对甲氧西林敏感金黄色葡萄球菌(MSSA)和耐甲氧西林金黄色葡萄球菌(MRSA)的抑菌活性,对金黄色葡萄球菌ATCC 25923的抑菌曲线、超微结构、细胞壁透性和肽聚糖的量、膜蛋白构象和离子渗漏的影响,来阐述广藿香精油的抑菌活性及作用机制。结果广藿香精油对受试菌的MICs为0.51 mg/mL;能明显延长受试菌生长的延迟期,抑制细菌的生长;破坏细胞的结构完整性,损伤胞膜;影响受试菌细胞壁透性,膜蛋白的构象;导致胞体K+、Mg2+的渗出;但在检测时间内对受试菌细胞壁肽聚糖的量无明显影响。结论广藿香精油对MSSA和MRSA有显著抑制作用,其抑菌机制与破坏细胞的结构完整性和损伤胞膜,影响细胞壁和细胞膜的通透性,改变膜蛋白构象有关。     

Antibacterial activity and synergistic antibiotic mechanism of trialdehyde phloroglucinol against methicillin-resistant Staphylococcus aureus

The emergence of methicillin-resistant Staphylococcus aureus (MRSA) has become a critical global concern. Identifying new anti-S. aureus agents or therapeutic strategies are urgently needed to treat S. aureus infection. The present study investigated the antibacterial activity of 16 phenolic compounds against MRSA, four of which exhibited antibacterial activity. Their antibacterial activities increased in a dose-dependent manner but showed different responses with the extension of treatment time. Trialdehyde phloroglucinol (TPG) and 2-nitrophloroglucinol (NPG) maintained stable antibacterial activity; however, that of dichlorophenol and myricetin decreased rapidly over 24 hr of treatment. Checkerboard and time-kill assays indicated that TPG and NPG exhibited strong synergistic antibacterial activities with penicillin or bacitracin. Microscopic observation and membrane integrity analysis showed that the combination of TPG and penicillin destroyed the MRSA cell membrane, resulting in the leakage of intracellular biomacromolecules, marked changes in surface zeta potential, and the collapse of membrane potential. Moreover, the combination significantly decreased penicillinase activity and penicillin-binding protein 2a mRNA expression, inhibiting MRSA growth. Taken together, these results demonstrated that the combination of the phloroglucinol derivative TPG and penicillin has significant synergistic anti-MRSA activity and can serve as a potential therapeutic strategy to treat MRSA infections.     

Antibacterial and anti-inflammatory effects of extracts and fractions from Polygonum capitatum

Aim of the study

This study was designed to investigate the antibacterial and anti-inflammatory activities of the extracts and the structure-based fractions from P. capitatum so as to provide the evidence for the traditional use of this plant in the treatment of urinary tract infections and to clarify the structural types that were responsible for the clinical use of the plant.

Materials and methods

The dry whole plant of P. capitatum was extracted with water and 70% aqueous ethanol and then separated, respectively, into a fraction enriched in polysaccharides and proteins (PP) and four other fractions enriched in gallic acid and its analogues (GAA), flavonoids (FV), tannins (TN), and triterpenoids and steroids (TS). UV spectral or chemical methods were used for the confirmation of the five fractions. The in vitro antibacterial activities of the aqueous (AE) and 70% aqueous ethanol (70EE) extracts as well as the fractions against gram-positive and gram-negative bacteria were initially evaluated by a disc diffusion test. The anti-bacterial potencies of the active extracts or fractions were then assessed in vitro by determining the MICs and MBCs. The anti-inflammatory activity was evaluated employing the xylene-induced mouse ear edema model.

Results

Except for fraction PP, AE, 70EE, and the four fractions (GAA, FV, TN, and TS) exhibited varying degrees of antibacterial and anti-inflammatory activities. The results of the minimal inhibition concentration (MIC) and minimal bactericidal concentration (MBC) indicated that the crude extracts or fractions FV and TN all possess bacteriostatic and bactericidal properties. Fractions FV and TS showed significantly anti-inflammatory activity (P < 0.01) with the inhibition rates of 86.15 and 73.71% at 0.6 g/kg, respectively, as compared to 76.93% of the positive control dexamethasone.

Conclusions

The overall results suggested that the traditional use of this plant for the treatment of urinary tract infections were attributed to the presence of antibacterial and anti-inflammatory agents. The results also provided evidence that the studied plant extracts, as well as some of the fractions obtained from this plant might be potential sources for antimicrobial and anti-inflammatory drug development.     

Antibacterial activity of flavanone isolated from Sophora exigua against methicillin-resistant Staphylococcus aureus and its combination with antibiotics

5,7,2′,4′-Tetrahydroxy-8-lavandulyl-flavanone, isolated from Sophora exigua, completely inhibited the growth of 21 strains of methicillin-resistant Staphylococcus aureus (MRSA) at concentrations of 3.13–6.25 μg/mL. The anti-MRSA effect was based on bactericidal action. In combinations of the flavanone with vancomycin, minocycline and rifampicin, the fractional inhibitory concentration indices were 0.90, 0.88 and 0.85, respectively, indicating partial synergistic effects with anti-MRSA antibiotics. The proposed flavanone would be a potent phytotherapeutic agent against MRSA infections.     

头花蓼质量标准的研究

目的建立头花蓼的质量标准。方法显微鉴别法、TLC法定性鉴别头花蓼;《中国药典》方法检查水分、总灰分、酸不溶性灰分;HPLC法测定没食子酸和槲皮苷的含有量。结果显微鉴别特征性强,多见腺毛、不定时气孔、草酸钙簇晶等;TLC图谱斑点清晰、分离度好、专属性强;23批样品水分、总灰分、酸不溶性灰分、50%乙醇浸出物含有量分别为7.75%～11.63%、4.04%～18.79%、0.14%～8.62%、15.49%～25.26%;没食子酸、槲皮苷含有量分别为0.470～1.856、0.160～4.199 mg/g。结论该方法合理可行,可用于头花蓼的质量控制。     

Antibacterial activity of sophoraflavanone G Isolated from the roots of Sophora flavescens against methicillin‐resistant Staphylococcus aureus

In this study, sophoraflavanone G obtained from Sophora flavescens was evaluated against 10 clinical isolates of methicillin‐resistant Staphylococcus aureus (MRSA), either alone or in combination with ampicillin or oxacillin, via checkerboard assay. At the end point of an optically clear well, the minimum inhibitory concentrations (MICs) ranged from 0.5 to 8 µg/ml for sophoraflavanone G, from 64 to 1024 µg/ml for ampicillin, and from 256 to 1024 µg/ml for oxacillin. The combination of sophoraflavanone G and ampicillin or oxacillin yielded a fractional inhibitory concentration index ranging from 0.188 to 0.375, thereby indicating a principally synergistic effect. The synergistic interaction was verified by time‐kill studies using sophoraflavanone G and/or antibiotics. Thirty minutes of treatment with sophoraflavanone G with ampicillin or oxacillin resulted in an increase in the rate of killing in units of CFU/ml to a greater degree than was observed with Sophoraflavanone G alone. These findings indicated that the application of the tested sophoraflavanone G alone or in combination with antibiotics might prove useful in the control and treatment of MRSA infections. Copyright © 2009 John Wiley & Sons, Ltd.     

不同栽培基质对头花蓼品质的影响

目的:以热淋清颗粒生产原料药头花蓼提取后的药渣为研究对象,探索头花蓼药渣回收利用的方式。方法:分析头花蓼药渣中的营养成分,并将药渣制成基质,用于头花蓼药材栽培,并对栽培的头花蓼药材进行质量检测。结果:药渣中含有丰富的营养成分,且pH适中。药渣基质栽培的头花蓼药材与头花蓼GAP基地土壤栽培的头花蓼药材在外观性状、定性、定量分析结果上相差不大,且符合药用要求。结论:将药渣作为基质栽培头花蓼药材,避免了土壤中重金属,农药残留等污染,为制药企业开辟了一条绿色中药材生产的循环经济发展道路。     

头花蓼总黄酮提取工艺研究

目的 探讨头花蓼总黄酮最佳提取工艺.方法 采用正交实验方法 进行优选,紫外分光光度法测定总黄酮含量.结果 乙醇浓度对总黄酮的提取有显著影响.结论 结合正交实验结果 和方差分析,确定12倍量55%乙醇提取3次,1h/次为最佳工艺.