Metal Complexes with 8-Hydroxyquinoline: Synthesis and <i>In Vitro</i>Antimicrobial Activity

In this paper, three complexes with 8-hydroxyquinoline (8-HQ) were synthesized, their spectral analysis was performed and the antimicrobial effect was examined in vitro. The stoichiometric ratio of the complex was determined conductometrically and spectrophotometrically. FTIR and UV/VIS spectroscopy were used for structural characterization. Antimicrobial activity was examined by diffusion technique on selected gram-positive and gram-negative bacteria, and C. albicans. Square planar and octahedral geometry complexes were synthesized by mixing in a molar ratio of 1:2 (M:L). Based on the spectral data, it is concluded that both oxygen and nitrogen atoms from 8-HQ are involved in the formation of the complex. The antimicrobial activity of the complexes is high, with zones of inhibition in the range of 15 - 28 mm. 8-HQ was shown to have a significantly higher ability to inhibit the growth of the tested microorganisms.

Fermented Herbal Decoction Selectively Targeting Human Cancer Cell Line and Human Pathogenic Microorganism

Introduction: Prolonged immuno-suppressed status promised to induce internal growth of malignant cell and infectious agent, yet, only a small part of affected individuals seek medical attention or berried by commercially over-flowed fake information. Several studies have described complementary and alternative medicine as effective strategies for improving anti-infectious agent including malignant cell. The purpose of this study was to investigate the effect of a fermented herbal decoction (FHD) both in vitro and in vivo to malignant cells and microorganism by regulating leukocyte subset proportioning FHD as dietary material. Methods: In this approach of alternative study, selective anti-cancer effect by fermented decoction was tried to show first in vitro system both, cancer cell and virus strain. The fermented herbal decoction consisting of 80 sorts of herbs and fruits. The selective toxicity was set up and then for immunological factors in animal and human. The most important factor is to reduce side effect for a normal cell. Results: First, FHD was proved as safe by animal test. FHD regulated also the proportion of granulocyte and lymphocyte ratio both animal and human. In vitro culture showed selective toxicity by FHD against human melanoma and leukemia cell line but reduced toxicity was showed by normal cell line. As for the anti-virus activity, anti-virus effect was tested on the feeder layer of human fibroblast cell, after 9 days of culture. Second, FHD inhibits colon cancer growth in 3-methylholanthrene induced cancer in rat. Conclusion: The present results suggest that our fermented herbal decoction showed selective anti-cancer activities and anti-virus activities, together with the regulative effect on the immune system.

Antioxidant Activities of Crude Phlorotannins from Sargassum hemiphyllum

Brown algae are well known as a source of biologically active compounds, especially those having antioxidant activities, such as phlorotannins. In this study we examined the antioxidant activities of crude phlorotannins extracts（CPEs） obtained from Sargassum hemiphyllum（SH） and fractionated according to the molecular weights. When CPEs were administrated at a dose of 30 mg/kg to Kunming mice pre-treated with carbon tetrachloride（CCl4）, the levels of oxidative stress indicators in the liver, kidney and brain were significantly reduced in vivo. All the components of various molecular weight fractions of CPEs exhibited greater scavenging capacities in clearing hydroxyl free radical and superoxide anion than the positive controls gallic acid, vitamin C and vitamin E. Particularly, the components greater than 30 k D obtained from ethyl acetate phase showed the highest antioxidant capacities. These results indicated that SH is a potential source for extracting phlorotannins, the algal antioxidant compounds.

Clarithromycin的体内抗菌作用研究

新的１４元大环内酯ｃｌａｒｉｔｈｒｏｍｙｃｉｎ（ＣＲＭ）与红霉素（ＥＭ）对金葡球菌、化脓链球菌、肺炎链球菌、嗜血流感杆菌感染小鼠体内保护作用结果显示：口服ＣＲＭ对金葡球菌、化脓链球菌及肺炎链球菌的体内抗菌作用优于ＥＭ６．３～８．６倍。尤其对金葡球菌耐药菌及嗜血流感杆菌感染小鼠的半数保护剂量作用有效于ＥＭ的保护作用１７及１８倍，ＣＲＭ在体内具有良好的抗菌作用。

Roxithromycin的药效学研究

报道国产ｒｏｘｉｔｈｒｏｍｙｃｉｎ（ＲＯＸ）对２０５株临床致病菌体内外抗菌活性及不同试验条件对抗菌活性的影响，并与进口产品及红霉素、麦迪霉素、柱晶白霉素、青霉素钾盐的抗菌活性进行比较。还进行了杀菌试验，结果表明，国产与进口ＲＯＸ及红霉素体外抗菌作用相似，对革兰氏阳性和阴性球菌有较好的抑制作用。另外，ＲＯＹ在偏碱性环境中抑菌效果较强，对１０５、１０７ｃｆｕ／ｍｌ细菌的ＭＩＣ基本一样。对感染金葡球菌的小鼠有很好的治疗保护作用，优于红霉素。

In Vitro and In Vivo Antibacterial Activity of Patchouli Alcohol from Pogostemon cablin

Objective:To investigate the antibacterial activity of patchouli alcohol(PA)against 127 bacteria strains,including the common bacteria and drug-resistant bacteria strains both in the in vitro and in vivo tests.Methods:For the in vitro trial,the antibacterial property of PA against 107 Gram-positive and 20 Gram-negative bacteria strains was screened by agar double dilution method.For the in vivo trial,specific pathogen free Kunming strain of both male and female white mice,were used to test the protective ability of PA after being injected with the median lethal dose of the tested strains.Results:PA possessed antibacterial activity against all the tested 127 strains.In the in vitro test,PA could inhibit both Gram-negative bacteria(25-768μg/m L)and Gram-positive bacteria(1.5-200μg/m L).Particularly,PA was active against some drug-resistant bacteria like methicillin-resistant Staphylococcus aureus(MRSA).PA also exhibited in vivo anti-MRSA activity in mice via intraperitoneal injection.PA could protect mice entirely infected with MRSA at 100 and 200 mg/kg,while 80% mice injected with MRSA could be protected at a low dose of 50 mg/kg.Conclusion:PA might be a potential antibacterial drug from natural sources and might be worthy to explore its mechanism and application in further study.

Synthesis and in vitro antimicrobial activity of N-arylquinoline derivatives bearing 2-morpholinoquinoline moiety

A new series of N-arylquinoline derivatives 5a-x bearing 2-morpholinoquinoline moiety has been synthesized by one pot base catalyzed cyclocondensation reaction of 2-morpholinoquinoline-3-carbaldehydes 2a-c,malononitrile 3 andβ-enaminones 4a-h. All the synthesized compounds were screened for their in vitro antimicrobial activity against six bacterial pathogens,namely Streptococcus pneumoniae,Clostridium tetani,Bacillus subtilis,Salmonella typhi,Vibrio cholerae,Escherichia coli and against two fungal pathogens,Aspergillus fumigatus and Candida albicans using broth microdilution MIC method.Of the compounds studied,majority of the compounds were found to active against C.tetani,B.subtilis and C.albicans as compared to first-line standard drugs.

Aqueous extract of Taxus Chinensis (Pilger) Rehd inhibits lung carcinoma A549 cells through the epidermal growth factor receptor/mitogen-activated protein kinase pathway in vitro and in vivo

OBJECTIVE:To explore the anticancer mechanismof aqueous extract of Taxus Chinensis (Pilger) Rehd (AETC).METHODS: The serum pharmacological method was used to avoid interference from administration of the crude medicinal herbs. Eight purebred New Zealand rabbits were used for preparation of serum containing various concentrations of AETC. Forty-eightBalb/c-nu mice were used for in vivo experiments. The effects of serum containing AETC on the proliferation of A549 cells and expression levels of the epidermal growth factor receptor/mitogen-activated protein kinase(EGFR/MAPK) pathway-related proteins in vitro were investigated. Additionally, the effects on the growth of A549 xenografts in nudemice,and expression levels of the EGFR/MAPK pathway-related proteins in the xenografts,were investigated.RESULTS: 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyl tetrazolium bromide(MTT) assay revealed that the serum containing AETC significantly decreased the viability of A549 cells in a dose-dependent manner.Western blot showed that the serum containing various concentrations of AETC strongly reduced the levels of phospho-Jun N-terminal kinase(p-JNK) and phospho-extracellular signal-regulated kinase1/2(ERK1/2) while it increased the level of p-p38. However, no significant effects on the expression levels of JNK, ERK1/2, and p38 MAPK were found. In addition, an anticancer effect from AETC was observed invivo in the Balb/c-nu mice bearing A549xenografts.CONCLUSION: AETC has significant effects on the growth of A549 xenografts and on the activity of the EGFR/MAPK pathway. Therefore, AETC may be beneficial in lung carcinoma treatment.

Trends in Antimicrobial Resistance against Enterobacteriaceae Strains Isolated from Blood： A 10-year Epidemiological Study in China's Mainland （2004-2014）

Background：Antimicrobial resistance is a serious problem that compromises the empirical treatment of infections,resulting in a lack of effective antibiotics and high medical expenses.Here,we aimed to monitor the trends in antimicrobial resistance among Enterobacteriaceae isolated from blood samples in China's Mainland.Methods：A total of 2240 Enterobacteriaceae isolates from blood were collected from hospitalized patients at 19 tertiary hospitals between October 2004 and June 2014.The minimum inhibitory concentrations of all isolates were determined using the agar dilution method according to the Clinical and Laboratory Standards Institute 2016 guidelines.Results：The most commonly isolated bacteria were Escherichia coli,compromising 47.0% （1053/2240） of the total isolates,followed byKlebsiella spp.（26.3%）,Sahnonella spp.（10.4%）,and Enterobacter spp.（9.2%）.The detection rates of extended-spectrum β-lactamases （ESBLs） among E.coli were 68.9% （2004-2005）,73.2% （2007-2008）,67.9% （2009-2010）,72.6% （2011-2012）,and 58.4% （2013-2014）,whereas those in ESBL-producing Klebsiellapneumoniae were slightly decreased （75.9%,50.0%,41.4%,40.2%,and 43.0%,respectively）.Carbapenems were the most potent agents against the Enterobacteriaceae isolates,followed by moxalactam,tigecycline,and amikacin.However,there was a decrease in the susceptibility rates for carbapenems in all species,particularly K.pneumoniae （decreased by 10.6% for imipenem） and Enterobacter aerogenes （decreased by 2 l.1% for imipenem）.Reviving antibiotics （tigecycline and polymyxins） showed good in vitro activity against Enterobacteriaceae.Conclusions：The activity of antibiotics against Enterobacteriaceae isolated from blood was decreased overall.Large proportions of ESBL-producing isolates were identified among E.coli and Klebsiella spp.Carbapenem-resistant isolates have become a major challenge in the treatment of infections.

Anthelmintic, antimicrobial, antioxidant and cytotoxic activity of Caltha palustris var. alba Kashmir, India

The methanolic extract obtained from the root portion of Caltha palustris var. alba was evaluated for its anthelmintic efficacy against gastrointestinal nematodes of sheep under both in vitro and in vivo conditions using worm motility inhibition(WMI) assay and fecal egg count reduction(FECR) assay, respectively. The extract was subjected to antimicrobial activity using agar-well diffusion method against different bacterial strains. In addition the extract was evaluated for cytotoxic and antioxidant activity against cultured THP-1(Leukemia), A-549(Lung), HCT-15(Colon), Cervix(HeLa) and PC-3(Prostrate) cell lines by SRB and DPPH radical scavenging assays. The extract used resulted in mean %WMI of 94.44%, as observed when the worms were put in lukewarm buffer for 30 min after exposure to different treatments. The mean mortality index of the sample was 0.95. The lethal concentration(LC50) was 0.11 mg·mL-1. Cell lines were exposed to concentration of 100 μg·mL-1 of extract for 48 h, which reduced the viability of these cell lines. The same plant extract also showed 55.58% DPPH radical scavenging activity.

Physicochemical properties,antimicrobial activity and oil release of fish gelatin films incorporated with cinnamon essential oil

Fish skin gelatin films incorporated with various concentrations of cinnamon essential oil(CEO)were prepared and characterized.The results showed that tensile strength(TS),elongation at break(EAB),and water content(WC)of the gelatin based film decreased with the increasing concentrations of CEO,but water vapor permeability(WVP)increased.Addition of CEO improved light barrier property of the film.The Scanning electron microscope(SEM)showed that the heterogeneous surface and porous formation appeared in gelatin-CEO films.Fourier transform infrared spectroscopy analyses(FTIR-ATR)spectra indicated the interactions existed between gelatin and CEO.The gelatin-CEO films exhibited good inhibitory effects against the tested microorganisms(Escherichia coli,Staphylococcus aureus,Aspergillus niger,Rhizopus oryzae,and Paecilomyces varioti)and their antifungal activity seemed to be more effective than the resistance to bacterial growth.In vitro release studies showed an initial burst effect of CEO release and that subsequently slowed down at 40℃,but the initial burst release was not obvious at 4℃.The obtained results suggested that incorporation of CEO as a natural antimicrobial agent into gelatin film has potential for developing as active food packaging.

黄秋葵抗氧化活性研究

目的研究黄秋葵果实不同极性部位提取物的体外和体内抗氧化能力,为黄秋葵的产品开发和利用提供依据。方法采用·DPPH清除能力、·ABTS^(+)清除能力、·OH清除能力、·O_(2)^(-)清除能力、FRAP法还原能力、TBARS法抗脂质过氧化能力体外抗氧化模型对黄秋葵果实95%乙醇提取物中不同极性部位进行抗氧化活性评价,并利用SPSS 19.0软件分析黄秋葵果实抗氧化活性与总黄酮含量之间的相关性。选择其具有体外抗氧化活性部位的提取物进行体内抗氧化活性研究。结果95%乙醇提取物中乙酸乙酯层和正丁醇层提取物表现出清除自由基能力、还原能力和抑制脂质过氧化能力,乙酸乙酯层和正丁醇层提取物的总黄酮含量高于其他各层提取物,总黄酮含量与抗氧化活性呈较强相关性。与模型组比较,给予乙酸乙酯层和正丁醇层提取物能够升高CCl_(4)肝损伤大鼠肝脏中SOD、CAT活性以及GSH水平,同时能够降低ALT活性和MDA水平。结论黄秋葵果实具有潜在的护肝作用,可为开展肝脏损伤保护研究提供重要依据。

域发喷剂敷料对糠秕马拉色菌体外抑菌活性的实验研究

目的采用琼脂平板扩散法(打孔法)和微量液基稀释法两种体外药敏实验方法,观察域发喷剂敷料及其主要成分(微生物源性抗菌肽)对头皮脂溢性皮炎常见的马拉色菌体外抑菌活性。方法不同浓度域发喷剂敷料、微生物源性抗菌肽为实验组,采乐洗剂(浓度2%酮康唑洗剂)、域发喷剂敷料空白溶剂为对照组,用琼脂平板扩散法(打孔法)和微量液基稀释法测试体外对马拉色菌的抑制作用,同时测定MIC(最小抑菌浓度)值。结果域发喷剂敷料、微生物源性抗菌肽、采乐洗剂均对马拉色菌有不同程度的体外抑制作用,其抑菌效果与药物浓度呈正相关。域发喷剂敷料的MIC值为0.977μL/mL、微生物源性抗菌肽的MIC值为3.907μL/mL。结论域发喷剂敷料安全性高,不易产生耐药性,副作用少,有较好地抑制马拉色菌作用,使用方便,可用于临床上头皮脂溢性皮炎的治疗。

瑞香狼毒总黄酮提取物的抗肿瘤作用

目的: 研究瑞香狼毒总黄酮提取物的抗肿瘤作用。方法:体外抗肿瘤活性研究采用MTT比色法和集落形成法测定,靶细胞采用人胃癌细胞SGC- 790 1、人肝癌细胞BEL- 74 0 2和人白血病细胞HL- 6 0 ;通过提取物对小鼠的移植性肿瘤S180和H2 2生长的影响来评价体内抗肿瘤作用。结果:瑞香狼毒总黄酮提取物对体外培养的肿瘤细胞有较强的抑制作用,体外抗肿瘤活性高于长春新碱;瑞香狼毒总黄酮提取物急性毒性较小,对小鼠移植性肿瘤S180和H2 2的生长也有显著的抑制作用,并和剂量正相关,高剂量组对小鼠移植性肿瘤S180的抑制率为4 5 . 6 4 % ,H2 2的为4 7 .5 9% ,与阳性对照组环磷酰胺的抑制率接近。结论:瑞香狼毒总黄酮提取物具有较强的体内和体外抗肿瘤作用。

藤茶多糖的抗氧化作用研究

目的: 探讨藤茶多糖的体内外抗氧化作用。 方法: (1)测定藤茶多糖(Ampelopsis Grossedentata polysaccharide,AGP)的还原能力;(2)测定AGP在化学模拟体系、体外血清的抗活性氧能力;(3)测定AGP对小鼠肝匀浆、小鼠肝线粒体MDA生成的影响;(4)用分光光度法测定H2O2诱导小鼠红细胞溶血和Fe2+-VC诱导的肝线粒体肿胀程度来研究AGP的抗氧化效果;(5)小鼠随机分成对照与AGP组,腹腔注射AGP 150mg/kg·bw·d 12d后,测定小鼠血清抗活性氧能力及肝组织MDA含量。 结果: AGP具有一定的还原能力,一定浓度范围内具有显著的体外抗活性氧能力并能抑制小鼠肝组织及肝线粒体MDA的生成,可减少红细胞诱导溶血和肝线粒体肿胀程度,对小鼠体内肝组织MDA生成的抑制作用显著。 结论: AGP一定浓度范围内具有抗氧化作用。

芦苇叶黄酮类提取物体内体外抗氧化性研究

研究醇提芦苇叶黄酮类提取物的体内体外抗氧化性。通过测定芦苇叶黄酮类提取物对体外大鼠肝组织匀浆、肝线粒体丙二醛(malondialdehyde,MDA)生成量及大鼠红细胞溶血的影响。结果表明:芦苇叶黄酮类提取物在0.5~10 mg/m L范围内能抑制大鼠肝组织匀浆及肝线粒体MDA的生成,抑制大鼠红细胞溶血,具有量效关系,表明芦苇叶黄酮类提取物具有体外抗氧化效果。随着剂量的增加,芦苇叶黄酮类提取物可提高S180荷瘤小鼠血清中谷胱甘肽过氧化物酶(glutathione peroxidase,GSH-Px)和超氧化物歧化酶(superoxide dismutase,SOD)活性,降低MDA含量,从而提高其体内抗氧化活性,当剂量达到300 mg/(kg·d)时,芦苇叶黄酮类提取物与10 m L/(kg·d)的氟尿嘧啶均可促进荷瘤小鼠体内抗氧化能力的提高,且二者间没有显著性差异。

头孢米诺和其他14种抗菌药物对产与不产超广谱β-内酰胺酶菌株抗菌活性比较

目的 测定头孢米诺和其他 14种抗菌药物对产与不产超广谱 β-内酰胺酶 (ESBL s)菌株的体外抗菌活性。方法 采用琼脂稀释法测定头孢米诺和其他 14种抗菌药物的最小抑菌浓度 (MIC) ,纸片确证法检测 ESBL s。结果 对 110株产 ESBL 的大肠埃希菌和肺炎克雷伯菌 ,未发现亚胺培南耐药的菌株 ,除亚胺培南外 ,头孢米诺比其他的 13种抗生素有较低的耐药性 ,其耐药率为 7.3% ,MIC50 和 MIC90 值范围分别为 0 .5～ 1mg/ L 和2～ 32 m g/ L;对 4 0株不产 ESBL s的大肠埃希菌和肺炎克雷伯菌、头孢米诺、头孢美唑、头孢他啶、头孢噻肟、头孢曲松、头孢哌酮、头孢吡肟及亚胺培南 ,有相似的体外抗菌活性 ,其敏感率均为 10 0 % ,MIC50 和 MIC90 值范围分别为 0 .0 32～ 0 .5 mg/ L和 0 .0 6 4～ 4 mg/ L。结论 对产 ESBL 的大肠埃希菌和肺炎克雷伯菌 ,未发现亚胺培南耐药的菌株 ,头孢米诺比其他 β-内酰胺类 ,庆大霉素和氟喹诺酮类有较高的体外抗菌活性 ;对不产 ESBL s的菌株 ,头孢米诺、头孢美唑、头孢他啶、头孢噻肟、头孢曲松、头孢吡肟及亚胺培南有相同的抗菌活性 ,没有耐药的菌株发现。