Quantification of Total Phenols, Total Flavonoids, Total Anthocyanins and Evaluation of Antioxidant and Antiradical Activities of Detarium Senegalense Extracts from Chad

The aim of the present work is to assess the value of Detarium Senegalense by determining the content of total phenols, total flavonoids and total anthocyanins, and by evaluating the free radical scavenging activity of Detarium Senegalense extracts. For this purpose, sequential extraction using solvents of increasing polarity was essential. The various extracts obtained underwent phytochemical and biochemical analyses. Phytochemical screening revealed the presence of flavonoids, alkaloids, tannins, polyphenols, anthocyanins and steroids/terpenes. Quantitative analysis of total polyphenols, total flavonoids and total anthocyanins yielded the following results: total flavonoids (0.803 ± 0029 mg EQ/100g P for acetone extract of roots and 0.871 ± 0.401 mg EQ/100g P for methanol extract of leaves);total polyphenols (23.298 ± 12.68 mg EAG/100g P for acetone extract of roots and 24.69 ± 0.49 401 mg EAG/100g P for methanol extract of leaves);total monomeric anthocyanins (44.697 ± 0.939 mg EC3G/100g P and 16.699 ± 0.193 mg EC3G/100g P respectively for acetone and methanol extracts of stem bark). DPPH free radical scavenging activity was 1.674 ± 0.023 mg/mL for the acetone extract and 0.934 ± 0.24 mg/mL for the methanol extract of roots. .

Synthesis and Anti-inflammatory Activity of 2-(E)-(4-Hy-droxy-3-methoxybenzylidene)-5-(N-Substituted aminomethyl)Cyclopentanones

本文合成了１５种２（Ｅ）（３甲氧基４羟基苯亚甲基）环戊酮杂环胺Ｍａｎｎｉｃｈ碱盐酸盐和芳胺Ｍａｎｎｉｃｈ碱，并进行了初步的抗炎活性筛选。所有化合物结构均经波谱分析和元素分析证实。药理试验结果表明：部分化合物对二甲苯致小鼠耳肿胀有较显著的抑制作用；苯胺取代基的变化对芳胺Ｍａｎｎｉｃｈ碱的抗炎活性有显著的影响。

Anti-diabetic and anti-cholesterolemic activity of methanol extracts of three species of Amaranthus

Objective:To investigate the anti-diabetic and anti-cholesterolemic activity of methanol extracts of leaves of Amaranthus caudatus,Amaranthus spinosus and Amaranthus viridis in normal and streptozotocin(STZ) induced diabetic rats.Methods:In this study,the anti-diabetic and anti-cholesterolemic activity of methanol extracts of leaves of all three plants was evaluated by using normal and STZ induced diabetic rots at a dose of 200 mg/kg and 400 mg/kg p.o.daily for 21 days.Blood glucose levels and body weight were monitored at specific intervals,and different biochemical parameters,serum cholesterol,serum triglyceride,high density lipoprotein, low density lipoprotein and very low density lipoprotein were also assessed in the experimental animals.Histology of pancreas was performed.Results:It was found that all the three plants at 400 mg/kg dose showed significant anti-diabetic and anti-cholesterolemic activity(P<0.01),while at 200 mg/kg dose less significant anti-diabetic activity(P<0.05) was observed.Concluslons: Methanol extracts of Amaranthus caudatus,Amaranlhus spinosus and Amaranthus viridis showed significant anti-diabetic and anti-cholesterolemic activity,which provides the scientific proof for their traditional claims.

The Anti-allergic Activity of Polyphenol Extracted from Five Marine Algae

Natural polyphenol has been widely believed to be effective in allergy remission. Currently, most of the natural polyphenol products come from terrestrial sources such as tea, grape seeds among others, and few polyphenols have been developed from algae for their anti-allergic activity. The aim of the study was to screen some commercial seaweed for natural extracts with anti-allergic activity. Five algae including Laminaria japonica, Porphyra sp., Spirulina platensis, Chlorella pyrenoidosa and Scytosiphon sp. were extracted with ethanol, and the extracts were evaluated for total polyphenol contents and anti-allergic activity with the hyaluronidase inhibition assay. Results showed that the total polyphenol contents in the ethanol extracts ranged from 1.67% to 8.47%, while the highest was found in the extract from Scytosiphon sp. Hyaluronidase inhibition assay showed that the extracts from Scytosiphon sp. had the lowest IC50, 0.67 mg m L-1, while Chlorella pyrenoidosa extract had the highest IC50, 15.07 mg m L-1. The anti-allergic activity of Scytosiphon sp. extract was even higher than the typical anti-allergic drug Disodium Cromoglycate(DSCG)(IC50 = 1.13 mg m L-1), and was similar with natural polyphenol from Epigallocatechin gallate(EGCG)(IC50 = 0.56 mg m L-1). These results indicated that the ethanol extract of Scytosiphon sp. contains a high concentration of polyphenol with high anti-allergic activity. Potentially Scytosiphon sp. can be developed to a natural anti-allergic compound for allergy remission.

PEGylation of Hirudin and Analysis of Its Antithrombin Activity in vitro

Hirudin 是在自然发现的大多数抗凝剂药，但是它的短浆液半衰期显著地禁止它的临床的申请。hirudin 的 PEGylation，最有希望的抗凝剂药，在这篇论文被执行。为 PEGylated hirudin 的最佳的反应条件被调查。PEGylation 反应什么时候在 10h 以后在 4 ° C 下面被进行，在在最适 PH 的硼酸盐缓冲区 8.5 与到 hirudin 的木钉的摩尔比率 250:1，更高的修正程度被完成。最后， PEGylated hirudin 的 bioactrvity 在 vitro 被测量。与未修改的 hirudin 相比， 26% 反凝血酵素活动被保留。

Content determination of benzyl glucosinolate and anti—cancer activity of its hydrolysis product in Carica papaya L.

Objective:To determine the content of benzyl glueosinolate（BG） in the pulp and the seed and investigate the anti-cuncer activity of its hydrolysis product in Curica papaya L.Methods: Determination of BG was performed on an Hypersil BDS C18 column at the wavelength of 214 nm with 0.1%trifluoroacelic acid（TFA） aqueous solution（A） and 0.1%TFA acelonilrile（B） as the mobile phase.In vitro activity test was adopted with cidtured human lung cancer H69 cell in vitro to investigate the inhibition rate of cell proliferation of benzyl isothiocyanale（BITC） againsl H69 cell.Results:The pulp has more BG before the maturation of papaya and it nearly disappeared after papaya matured,while the seed contains BG at every stage.Activity test demonstrated that the a higher concentration of BITC would have betler inhibition rate of cell proliferation on 1169 cell,and the IC50 was 6.5μmol/L.Conclusions:BG also can be produced in the pulp of papaya and it will be stored in the seed after the fruit has been matured.The hydrolysis product of BG has certain cancer-prevention anti-cancer activities for human.

Effect of chitosan on tobacco mosaic virus(TMV) accumulation, hydrolase activity, and morphological abnormalities of the viral particles in leaves of N. tabacum L. cv. Samsun

The effect of chitosan on the development of infection caused by Tobacco mosaic virus(TMV) in leaves of Nicotiana tabacum L. cv. Samsun has been studied. It was shown that the infectivity and viral coat protein content in leaves inoculated with a mixture of TMV(2 μg/mL) and chitosan(1 mg/mL) were lower in the early period of infection(3 days after inoculation), by 63% and 66% respectively, than in leaves inoculated with TMV only. Treatment of leaves with chitosan 24 h before inoculation with TMV also caused the antiviral effects, but these were less apparent than when the virus and polysaccharide were applied simultaneously. The inhibitory effects of the agent decreased as the infection progressed. Inoculation of leaves with TMV together with chitosan considerably enhanced the activity of hydrolases(proteases, RNases) in the leaves, in comparison with leaves inoculated with TMV alone. Electron microscope assays of phosphotungstic acid(PTA)-stained suspensions from infected tobacco leaves showed that, in addition to the normal TMV particles(18 nm in diameter, 300 nm long), these suspensions contained abnormal(swollen, "thin" and "short") virions. The highest number of abnormal virions was found in suspensions from leaves inoculated with a mixture of TMV and chitosan. Immuno-electron microscopy showed that "thin" virus particles, in contrast to the particles of normal diameter, lost the ability to bind to specific antiserum. It seems that the chitosan-induced activation of hydrolases stimulates the intracellular degradation of TMV particles and hence hydrolase activation may be considered to be one of the polysaccharide-mediated cellular defense mechanisms that limit virus accumulation in cells.

Anti-proliferative activity of phlorotannin extracts from brown algae Laminaria japonica Aresch

In this study,we evaluated the anti-proliferative activity of phlorotannins derived from brown algae Laminaria japonica Aresch extracts on the human hepatocellular carcinoma cell (BEL-7402) and on murine leukemic cells (P388) by MTT assay.Cells were incubated with 100 μg/mL of the phlorotannin extract (PE) for 48 h.The inhibitory rate of PE on BEL-7402 and P388 cells was 30.20±1.16% and 43.44±1.86%,respectively,and the half-inhibitory concentration of PE (IC50) on P388 and BEL-7402 cells was 120 μg/mL and >200 μg/mL,respectively.Microscopic observation shows that the morphologic features of tumor cells treated with PE and 5-fluorouracil are markedly different from the normal control group.The inhibitory rate of fraction A2 isolated from PE by sephadex LH-20 for BEL-7402 and P388 cells at the sample concentration of 70.42 μg/mL was 61.96±7.02% and 40.47±8.70%,respectively.The apoptosis peak for fraction A2 was the most profound of all fractions used in the flow cytometry assay.The results indicate that the anti-proliferative of this algal extract is associated with the total phlorotannin content.

Screening of flavonoid "quercetin" from the rhizome of Smilax china Linn.for anti-psoriatic activity

Objective:To assess anti-psoriatic activity of the methanol extract and the isolated flavonoid quercetin from the rhizome of Smilax china(S.china) Linn.Methods:Mouse tail test was used for the evaluation of anti-psoriatic activity.Methanol extract(100 and 200 mg/kg b.w.) and isolated flavonoid quercetin(25 and 50 mg/kg b.w.) were tested in Swiss albino mice.Parameters studied in the mouse tail test were changes in epidermal thickness and percentage orthokeratotic values.The anti-inflammatory role of the methanol extract and isolated flavonoid quercetin was evaluated using carrageenan-induced pleurisy in rats.In vitro antiproliferant assay on HaCaT cell lines was also carried out.Results:The isolated flavonoid quercetin from the rhizome of S.china produced significant orthokeratosis(P<0.01) in the mouse tail test.In epidermal thickness,a significant reduction with respect to control was observed in groups treated with retinoic acid and isolated flavonoid quercetin.The methanol extract(200 mg/kg) and isolated flavonoid quercetin(50 mg/kg) showed anti-inflammatory effect in terms of significant inhibition(P<0.001) in leukocyte migration.Maximum antiproliferant activity was shown by isolated flavonoid quercetin(IC_(50),62.42± 10.20 μg/mL).Conclusions:From the above data,the flavonoid quercetin shows significant orthokeratosis,anti-inflammatory and maximum antiproliferant activities.To our knowledge,this is the first report on the anti-psoriatic effect of the flavonoid quercetin which is promising for further investigations to prove its anti-psoriatic activity.

Estimation of total phenolic content,in-vitro antioxidant and anti-inflammatory activity of flowers of Moringa oleifera

Objective:To evaluate and compare the antioxidant potential and anti-inflammatory activity of ethanolic extract of flowers of Moringa oleifera(M.oleifera)grown in Oman.Methods:Flowers of M.oleiferawere collected in the month of December 2012 and identified by a botanist.Alcoholic extract of the dry pulverized flowers ofM.oleiferawere obtained by cold maceration method.The ethanolic flower extract was subjected to preliminary phytochemical screening as the reported methods.Folin-Ciocalteu reagent was used to estimate total phenolic content.DPPH was used to determinein-vitroantioxidant activity and anti-inflammatory activity of flowers was investigated by protein denaturation method.Results:Phytochemical analysis of extract showed presence of major classes of phytochemicals such as tannins,alkaloids,flavonoids,cardiac glycosidesetc.M.oleiferaflowers were found to contain 19.31 mg/g of gallic acid equivalent of total phenolics in dry extract but exhibited moderate antioxidant activity.The anti-inflammatory activity of plant extract was significant and comparable with the standard drug diclofenac sodium.Conclusions:The results of our study suggest that flowers ofM.oleiferapossess potent anti-inflammatory activity and are also a good source of natural antioxidants.Further study is needed to identify the chemical compounds responsible for their anti-inflammatory activity.

Assessing the anti-estrogenic activity of sodium pentachlorophenol in primary cultures of juvenile goldfish (Carassius auratus) hepatocytes using vitellogenin as a biomarker

Both pentachlorophenol and 2,3,7,8-tetrachlorodibenzo-p-dioxin （TCDD） had been studied widely because of their probable anti-estrogenic activity. Sodium pentachlorophenol （PCP-Na）, as a industrial product used in many fields, usually contains a trace of TCDD. The aim of this study was to assess the anti-estrogenic effect of PCP-Na in juvenile goldfish （Gurassius auratus） hepatocyte cultures using vitellogenin （VTG） as the biomarker. The ID50 of PCP-Na was investigated and then a series of concentrations （0.001 0.5 μg/ml） of PCP-Na were evaluated to estimate the anti-estrogenic activity. Results showed that PCP-Na was cytotoxic for hepatocytes even at very low concentration 〈1.21 μg/ml, and it could not induce VTG at any concentrations tested. Since it failed to stimulate VTG production, the possibility of its anti-estrogenic effect was tested, and a well-known anti-estrogenic compound-tamoxifen was used as positive control. PCP-Na caused a reduction in VTG synthesis in juvenile goldfish （Carassius auratus） hepatocytes at concentrations 〉0.1μg/ml when co-exposure with 1μg/ml 17β-estradiol （E2）, making its anti-estrogenic activity approximately as potent as tamoxifen. Our results indicate that PCP-Na can act as negative modulators of estrogenic function in juvenile goldfish （Carassius auratus） hepatocytes.

Synthesis and Anti-tumor Activity of Novel Amide Derivatives of Ursolic Acid

Ursolic acid was modified at C3 and C28 position to obtain fourteen derivatives including twelve novel compounds, and their chemical structures were characterized by IR, ^1H NMR and MS. Cell growth inhibitory effects of the derivatives against Hela cell were evaluated by MTT assay. All these derivatives were found to have stronger cell growth inhibitory than their parent compound, ursolic acid. The derivatives with a substituted acetyl group at C3 hydroxyl group show better activities than those with an unsubstituted hydroxyl group.

Synthesis of 6-sulfamoyl-4-oxoquinoline-3-carboxylic acid derivatives as integrase antagonists with anti-HIV activity

一系列新奇 6-sulfamoyl-4-oxoquinoline-3-carboxylic 酸衍生物为 HIV integrase 抑制活动被综合了并且屏蔽。他们的结构被 ESIMS 证实， 1 H NMR 和 13 C NMR。

3D-QSAR Studies on the Anti-tumor Activity of N-Aryl-salicylamide Derivatives

In the present work,comparative molecular field analysis(CoMFA)techniques were used to perform three-dimensional quantitative structure-activity relationship(3D-QSAR)studies on the anti-tumor activity(pHi,i=1,2,3,4)of N-aryl-salicylamide derivatives against four cancer cell lines,including A549,MCF-7,SGC-7901,and Bel-7402.12 compounds were randomly selected as the training set to establish the prediction models,which were verified by the test set of 5 compounds containing template molecule.The contributions of steric and electrostatic fields to pH1,pH2,pH3,and pH4 were 23.8% and 76.2%,20.1% and 79.9%,18.7% and 81.3%,and 14.3%and 85.7%,respectively.The cross-validation(Rcv 2)and non-cross-validation coefficients(R2)were 0.826 and 0.963 for pH1,0.867 and 0.974 for pH2,0.941 and 0.989 for pH3,and 0.797 and 0.961 for pH4,respectively.The CoMFA models were then used to predict the activities of the compounds,and it was found that the models had strong stability and good predictability.Based on the CoMFA contour maps,some key structural factors responsible for the anticancer activity of the series of compounds were revealed.The results provide some useful theoretical references for understanding the mechanism of action,designing new N-aryl-salicylamide derivatives with high anti-tumor activity,and predicting their activities.

Syntheses, Characterization and Anti-HIVActivity of Charge TransferHeteropolycomplexes

Each of Keggin type heteropolytungstosilicic and heteropolytungstogermanic acids reacted with 8-quinolinol, p-aminodimethylaniline and pyridine, respectively, yielding six charge trans- fer heteropolycomplexes (CTHPCs), which were purified and characterized by elemental analy- sis, IR, UV and 183W NMR. The anti-HIV-1 activities of CTHPCs were evaluated by ELISA of HIV-P24 antigen. The toxicity against MT-4 cells was measured by MTT. The results show that median inhibitory concentration (IC50) for each CTHPC to inhibit HIV-P24 antigen in cell culture was lower than 5 μg/mL, while median toxicity concentration (IC50) against MT-4 cells was higher than 268 μg/mL. The following mechanisms might be considered for their anti-HIV- 1 activity, namely, (1) inhibiting the penetration of HIV- 1 virus into target cells for it can blockade CD4 receptor of MT-4 cells and (2) inhibition of syncytium formation.

A Study on Anti-oxidative Activity of Soybean Peptideswith Linoleic Acid Peroxidation Systems

Soybean bioactive peptides（SBPs） were prepared from the isolated soybean protein by proteolysis with an alkaline protease, alcalase, at 50℃ and pH = 8.0. The dependence of hydrolysis time on hydrolysis degree and molecular weight distribution were examined. The hydrolysate was fractionated on a Sephadex G-25 column and the anti-oxidative activities of the fractions were detected by the method of pyrogallol auto-oxidation. The average chain length of soybean peptides that have anti-oxidative activity was estimated to be about 7. The anti-oxidative properties of the soy- bean peptide were also studied by using linoleic acid peroxidation systems. The optimal condition of the peroxidation system was set up, Vc/Cu^2 ＋ as the inducer at pH = 7.4 and 25 ℃. In addition, soybean peptides show higher antioxidative activity compared with GSH.

Total Synthesis of (±)-Calanolide A and Its Anti-HIV Activity

Anti-HIV agent (±)-calanolide A has been synthesized by a four-step approach startingfrom phloroglucinol, including the Pechmann reaction, Friedel-Crafts acylation, cyclization,chromenylation and Luche reduction.

Anti-Insect Activity of the Methanol Extracts of Fern and Gymnosperm

With environmental and food safety issues becoming one of the greatest concerns of the public, active plant compounds play more and more important roles in pest controlling. Fern to their particular status in plant taxology and co-evolution are of great significance for application as new pesticides due with insects. In this study, methanol extracts were distilled from wild fern and gymnosperm of 54 species of 22 families collected from Shiwandashan Mountain in Guangxi Zhuang Autonomous Region of China. Insecticidal activities of the methanol extracts were assayed on both adult house fly （Musca domestica） and mosquito （Aedes albopictus）. Significant insecticidal activities were exhibited in the methanol extracts of five species, Cupressusfunebris （leaves and stems）, Cycas acuminatissima （roots）, Keteleeria fortunei （leaves and stems）, Onychium japonicum （whole plant）, and Pinus taiwanensis var. Darning shanensis （leaves and stems）. Applications of the extracts of these plants resulted in higher than 50% mortalities in 4th instar larvae of A. albopictus at 24 h after treatment. The methanol extracts from 13 species possessed insecticidal activities against the adult of M. domestica at 48 h after treatment with higher than 90% mortalities. The extensive screening results showed that these fern and gymnosperm were highly potential to be botanical insecticides. The findings provide a feasible and valuable basis for further investigation.

Evaluation of anti-resistant activity of Auklandia(Saussurea lappa) root against some human pathogens

Objective:The antimicrobial activity of the ethanol extract of the Auklandia(Saussurea lappa)root plant was investigated to verify its medicinal use in the treatment of microbial infections.Methods:The antimicrobial activity of the ethanol extract was tested against clinical isolates ofsome multidrug-resistant bacteria using the agar well diffusion method.Commercial antibioticswere used as positive reference standards to determine the sensitivity of the clinical isolates.Results:The extracts showed significant inhibitory activity against clinical isolates of methicillinresistantStaphylococcus aureus,Pseudomonas aeruginosa,Escherichia coli,Klebsiella pneumonia,Extended Spectrum Beta-Lactemase,Acinetobacter baumannii.The minimum inhibitory concentration values obtained using the agar dilution test ranged from 2.0μg/μL-12.0μg/μL.In the contrary the water extract showed no activity at all against the tested isolates.Furthermore,theresults obtained by examining anti-resistant activity of the plant ethanolic extract showed thatat higher concentration of the plant extract(12μg)all tested bacteria isolates were inhibited with variable inhibition zones similar to those obtained when we applied lower extract concentrationusing the well diffusion assay.Conclusion:The results demonstrated that the crude ethanolicextract of the Auklandia(Saussurea lappa)root plant has a wide spectrum of activity suggestingthat it may be useful in the treatment of infections caused by the above clinical isolates(humanpathogens).

Anti-inflammatory Activity of Polysaccharide Isolated from Thamnolia Subuliformis

The present study aimed at isolating,purifying,characterizing the structure and estimating the anti-inflammatory activity of a polysaccharide named THSA which was obtained from Thamnolia subuliformis(Ehrh.) W.Culb(T.subuliformis).A newheteroglycan THSA was gained by hot water extraction and further continuously purification through Sephadex G-75 and Superdex 200 column chromatography.The structural characteristics of THSA were primarily investigated by molecular mass estimation,monosaccharide composition analysis and Fourier transforminfrared spectroscopy(FT-IR).The anti-inflammatory effects of THSA was also estimated in lipopolysaccharide(LPS)-stimulated mouse macrophages cell line RAW264.7 through the method of reverse transcription polymerase chain reaction(RT-PCR) and quantitative real-time PCR.The results indicate that THSA is composed of Glc,Gal,Man in the ratio 1:2.1:6.16,with average molecular weight of about 12.4 k Da,and significantly inhibits the mRNA expression of tumor necrosis factor alpha(TNF-α),IL-6 at100 or 1 000 μg/m L and increases the anti-inflammatory cytokine level of IL-10 at 100 μg/m L.It indicates that polysaecharide THSA has strong anti-inflammatory activity.