<i>Fusarium lini</i>Potential for the Biotransformation of Norandrostenedione and Evaluation of Urease and Chymotrypsin Properties of the Transformed Products

Several androgenic steroids have been biotransformed by fungi into metabolites with numerous biological properties. Incubation of norandrostenedione (1) with Fusarium lini NRRL 2204 was carried out for the first time, yielding two new metabolites, 3,7β-dihydroxy-19-norandrost-1,3,5-trien-17-one (3) and 6α,10β,17β-trihydroxy-19-nor-4-androsten-3-one (4), along with three known compounds, 3-hydroxy-19-norandrost-1,3,5-trien-17-one (2), 10β, 17β-dihydroxy-19-nor-4-androsten-3-one (5) and 10β-hydroxy-19-nor-4- androsten-3,17-dione (6). Their structures were elucidated by extensive spectroscopic analyses, including 1D-, 2D-NMR, and HR-MS experiments. Substrate 1 and its derivatives 2-6 were evaluated in vitro for their urease and chymotrypsin inhibitory properties. Compounds 2 and 3 were found to have strong urease activity with IC50 = 23.7 ± 0.17 and 10.2 ± 0.28 μm, respectively, as compared to the standard drug thiourea (IC50 = 21.6 ± 0.12 μm). Compounds 4, 5 and 6 showed good chymotrypsin activity with IC50 values of 6.4 ± 0.19, 15.6 ± 0.46 and 18.4 ± 0.65 μm, respectively, as compared to standard chymostatin with IC50 = 5.7 ± 0.14 μm. These transformed metabolites may form the basis for the future development of new drugs against ulcer, inflammation, bacterial and viral diseases.

GC/GCMS analysis of the petroleum ether and dichloromethane extracts of Moringa oleifera roots

Objective:To explore the phytochemical constituents from petroleum ether and diehloromethane extracts of Moringa oleifera(M.oleufera)roots using GC/GC—MS.Methods:A total of 5.11 kg fresh and undried crashed root of M.oleifera were cut into small pieces and extracted with petroleum ether and diehloromethane(20 L.each) at room temperature for 2 d.The concentrated extracts were subjected to their GC—MS analysis.Results:The GC-MS analysis of the petroleum ether and diehloromethane extracts of M.oleifern roots,which showed promising biological activities,has resulted in the identification 102 compounds.These constituents belong to 15 classes of compounds including hydrocarbons,fatty acids,esters,alcohols,isolhioeyanate.thiocyanale,pyrazine,aromalics.alkamides.cyanides,steroids,halocompounds.urea and N-hydroxyimine derivatives,unsaturated alkenamides.alkyne and indole.GC/GC-MS studies on petroleum ether extraet of the roots revealed that it contained 39 compounds,belonging to nine classes.Cyclooctasulfur S8 has been isolated as a pure compound from the extract.The major compounds identified from petroleum ether extract were trans-13-clocosene(37.9%).nonacosane(32.6%).cycloartenol(28.6%) nonadecanoic acid(13.9%) and cyclooctasulfur S8(13.9%).Dichloromethane extract of the roots was composed of 63 compounds of which nasimizinol(58.8%) along with oleic acid(46.5%),N—benzyl-N-(7—cyanato heptanamide(38.3%),N—benzyl-N—(1—chlorononyl) amide(30.3%),bis[3—benzyl prop-2-ene]-1-one(19.5%) and N.N-dibeuzyl—2-ene pent 1.5—diamide(11.6%) were the main constituents.Conclusions:This study helps to predict the formula and structure of active molecules which can be used as drugs.This result also enhances the traditional usage of M.oleifera which possesses a number of bioactive compounds.

In vivo sedative and muscle relaxants activity of Diospyros lotus L

Objective: To evaluate the sedative effect of Diospyros lotus L(D. lotus) extract in mice using the open field and Rota rod tests.Methods: For the sedative and muscle relaxants activities of extract/fractions of the plant, invivo open field and phenobarbitone-induced sleeping time were used, while the Roda rod test was employed in animals for the assessment of muscle relaxant activity.Results: Results from this investigation revealed that the extracts of D. lotus have exhibited significant sedative effect in mice(45.98%) at 100 mg/kg i.p. When the extract was partitioned with different solvents, the n-hexane fraction was inactive whereas the chloroform fraction was the most active with 82.67% sedative effect at 50 and 100 mg/kg i.p. On the other hand,the ethyl acetate and n-butanol fractions displayed significant sedative effects(55.65% and40.87%, respectively) at 100 mg/kg i.p. Among the tested extract/fractions, only chloroform and ethyl acetate fractions showed significant(P < 0.05) muscle relaxant activity in the Rota rod test.Conclusions: In short, our study provided scientific background to the traditional uses of D.lotus as sedative.

Acylhydrazide and Isatin Schiff Bases as Alternate UV-Laser Desorption Ionization (LDI) Matrices for Low Molecular Weight (LMW) Peptides Analysis

Matrix-assisted laser desorption/ionization (MALDI) is a preferred and widely used mass spectrometric technique for the analysis of macromolecules. Limited UV-LDI matrices are available for the analysis of biomolecules due to the restricted structural features to serve in the laser desorption/ionization mechanism with a problem of background signals appearing in the low mass region. This paper describes the application of Schiff base derivatives of acylhydrazide and isatin as alternate UV-LDI matrices for the analysis of peptides with significantly low background signals. Thirty one compounds have been successfully employed as matrices for the analysis of low molecular weight (LMW) peptides (α-Cyano-4-hydroxycinnamic acid (HCCA), a preferred choice for peptide analysis.

In vitro antiplasmodial and antioxidant activities of bisbenzylisoquinoline alkaloids from Alseodaphne corneri Kosterm

Objective:To study antiplasmodial and antioxidant activities of the isolation of alkaloids from the active dichloromcthanc extract of Alseodaphne corneri.Methods:Phytochemical studies of the crude extract led to the isolation of six alkaloids using recycle high performance liquid chromatography and preparative thin layer chromatography.The antiplasmodial activity of the isolated compounds was evaluated usingthe histidinc-rich protein II assay.The isolated alkaloids were also tested for their antioxidant activity using three different assays:DPPH.ferric reducing ability of plasma and metal chelating assays.Results:Malaria infection caused the formation of free radicals which subsequently led to oxidative stress and apoplosis.The antioxidant properties of the alkaloids under investigation revealed that in addition to the aniiplasmodial activity,the alkaloids could also prevent oxidative stress.(+)-laurotetanine and(+)-norstephasubine exhibited strong antiplamodial activities with IC_(50) values of 0.189 and 0.116 μM.respectively.Conclusions:Interestingly,the two most potent compounds that exhibit aniiplasmodial activity also exhibit good antioxidant activities.The crude dichloromcthanc extract and the isolated compounds exert substantial aniiplasmodial and antioxidative activities which in turn suppress oxidative stress and cause less damage to the host.

In vitro modulation of oxidative burst via release of reactive oxygen species from immune cells by extracts of selected tropical medicinal herbs and food plants

Objective:To evaluate in vitro immunomodulating properties and potential cytotoxicity of six tropical medicinal herbs and food plants namely Antidesma madagascariense(Euphorbiaceae) (AM),Erylhroxylum macrocarpum(Erythroxylaceae)(EM),Faujasiopsis flexuosa(Asteraceae) (FF),Pittosporum senacia(Pittosporaceae)(PS),Momordica charantia(Cucurbitaceae)(MC) and Orimum tenuiflorum(Lamiaceae)(Of).Methods:Initially,the crude water and methanol extracts were probed for their capacity to trigger immune cells’ NADPH oxidase and MPO-dependent activities as measured by lucigenin- and luminol-amplified chemiluminescence,respectively; as compared to receptor-dependent(serum opsonised zymosan- OPZ) or receptor-independent phorbol myristerate acetate(PMA).Results:Preliminary screening on whole human blood oxidative buret activity showed significant and concentration-dependent immunomodulating properties of three plants AM,FF and OT.Further investigations of the fractions on isolated human polymorphonuclear cells(PMNs) and mice monocytes using two different pathways for activation of phagocytic oxidative burst showed that ethyl acetate fraction was the most potent extract. None of the active samples had cell-death effects on human PMNs,under the assay conditions as determined by the trypan-blue exclusion assay.Since PMA and OPZ NADPH oxidase complex is activated via different transduction pathways,these results suggest that AM,FF and OT does not affect a specific transductional pathway,but rather directly inhibit a final common biochemical target such as the NADPH oxidase enzyme and/or scavenges ROS.Conclusions:Our findings suggest that some of these plants extracts/fractions were able to modulate significantly immune response of phagocytes and monocytes at different steps,emphasizing their potential as a source of new natural alternative immunomodulatory agents.

TGA-DSC: A Screening Tool for the Evaluation of Hydrocracking Catalyst Performance

DSC-TGA was used for screening of commercially available and synthesized catalyst for the degradation of polypropylene (PP). In this study, all the runs were performed with 50% load of the catalyst and the results were compared with those of PP + 50% pure silica having no catalytic activity. The degradation behavior of PP using catalyst Zeolyst-713 exhibited much higher degradation activity among the other catalysts used in this study. Moreover, it contributed to lowering of initial stage temperature showing a shape-selective effect. DSC-TGA tools such as Ton, Tmax, T99%, activation energy, enthalpy change in the process and coke content were used for screening. It was concluded that the pore construction and unique acid properties of the Zeolyst-713 as well as proper reaction temperatures were significant influential factors to fully exert this effect. In this work, kinetics of catalytic thermogravimetric degradation of PP used for domestic purposes was investigated using Alumino-silicate catalyst. Zeolyst-713 was observed to lower activation energy and enhances degradation activity in comparison with thermal degradation without a catalyst.

Simple Quantitation of Flucytosine in Low Volume Serum Samples and Evaluation of Common Endogenous Interferences by HPLC-UV

5-Fluorocytosine (5-FC) is used for the treatment of several infections. It is extremely important to monitor blood level concentration for maximum activity to avoid its side effects. A simple, faster, and more accurate analytical method is developed and validated using high-performance liquid chromatography with UV detection in a very low-volume serum sample. Exactly 50 μL of serum was precipitated with 5% trichloroacetic acid. After mixing and centrifugation, 20 μL of supernatant was injected into the HPLC column. Detection was performed at 280 nm. The method is very specific and free from interfering substances due to different drugs and their different circulating metabolites. The limit of detection (LOD) and limit of quantification (LOQ) were found to be 0.50 μg/L and 1.0 μg/L, respectively. The method was linear in the range of 5 - 150 μg/L in the serum sample. In method comparison, the correlation coefficient r2 was 0.999 and the percentage recovery was 90% - 105% on four levels of the quality control samples. Within run and between run precision was found to be less than 2.2% at four different concentrations (5, 25, 50, and 100 μg/L). A simple, faster, and more accurate HPLC-UV method is developed which is very useful for monitoring 5-FC concentration in low volume serum samples without evaporation step and ion exchange chromatography within minutes.

Reversal of multidrug resistance and antitumor promoting activity of 3-oxo-6β-hydroxy-β-amyrin isolated from Pistacia integerrima

The bioactive triterpenoid 3-oxo-6-β-hydroxy-β-amyrin(1)has been isolated from multiple plant sources.In this study,chloroform fraction of Pistacia integerrima extract was processed for the isolation of the compound.The compound identity was confirmed by advanced spectroscopy technique.X-ray crystallography was applied for molecular structure confirmation.In addition,compound 1 was screen for its activity on reversal of MDR(multidrug resistance)mediated by P-gp(P-glycoprotein).This was accomplished by using rhodamine123 exclusion on multidrug-resistant human ABCB1 gene transfected mouse T-lymphoma cell line.Outcomes revealed that MDR reversing effect was comparable to verapamil as positive control in vitro.Treatment of TPA-induced tumor promotion with 3-oxo-6β-hydroxy-β-amyrin led to reduction in the applied anti-tumor promotion experiment.The chemo-preventive effect of 3-oxo-6β-hydroxy-β-amyrin was comparable to curcumin as positive control based on the reduction of immediate early tumor antigen expression.Molecular docking by applying Autodock Vina 1 and i-GEMDOCK v 2.1 tools indicated that compound 1 gives good docking results,as determined by their fitness score and specificity.Moreover,results showed that compound 1 isolated from Pistacia integerrima precisely attached to a region where co-crystallized ligand for receptor previously existed.Our findings may explain the use of Pistacia integerrima plant extracts as an anticancer agent in folk medicine.

NO-cGMP-K channel-dependent anti-nociceptive activities of methanol stem bark extract of Piptadeniastrum africanum(Mimosaceae) on rats

Objective: To explore anti-hyperalgesic properties of methanol extract of Piptadeniastrum africanum stem bark(PAME) and it possible action mechanism. Methods: PAME was tested on carrageenan ?induced hyperalgesia using plantar test(thermal) and analgesymeter(mechanical) in rats, on prostaglandin E_2(PGE_2) induced mechanical hyperalgesia and vincristine induced neuropathic pain in rat, both with analgesymeter. Modulators of NO/cG MP/K^+ channel pathway and endogenous opioids receptor antagonists and/or agonists were used to determine the possible action mechanism of PAME. Results: PAME significantly decreased carrageenan induced thermal and mechanical hyperalgesia, as well as PGE_2 induced mechanical hyperalgesia. PAME significantly protected the animals against the installation of neuropathic pain. Anti-nociception activity produced by PAME was significantly blocked in animals pre?treated with all the antagonists(naloxone, NW-nitro-L-arginine methyl ester(L-NAME), methylene blue and glibenclamide). Conclusions: Results of this study reveal that, PAME administrate orally, can induce anti-hyperalgesic action against installation of inflammatory pain as well as neuropathic pain. The mechanism underlying PAME antihyperalgesic effect could probably be associated with an activation of opioid receptors and NO/cG MP/K^+ channel pathway.

Efficient Removal of Reactive Orange 107 Dye from Aqueous Media by Shrimp Shell Derived Chitosan Functionalized Magnetic Nanoparticles

In present work chitosan functionalized magnetic nanoparticles (CMNPs) were successfully prepared and investigated for the removal of Reactive Orange 107 dye (RO 107) from water. The chitosan was extracted from shrimp shells (Penaeus merguiensis) and was characterized by solubility test and fourier transform infrared spectroscopy (FTIR). Degree of deacetylation of chitosan was examined by 1H-NMR and potentiometric titration method. Thereafter, the chitosan was used for synthesis of CMNPs. The synthesized CMNPs were characterized by FTIR, scanning electron microscopy-energy dispersive spectroscopy (SEM-EDS), thermal gravimetric analysis (TGA) and atomic force microscopy (AFM). Effects of various variables such as contact time, pH, stirring speed, adsorbent dosage, temperature, and concentration of electrolyte on extraction efficiency were evaluated. Freundlich isotherm model fits better that shows the removal of RO 107 with CMNPs by multilayer adsorption behaviour. Furthermore, kinetic study showed that adsorption process followed pseudo-second order kinetic model regulated by chemisorption. Thermodynamic analysis explained that adsorption of RO 107 onto CMNPs was endothermic as well as spontaneous. The developed CNMPs were applied to environmental remediation of spiked RO 107 treated waste water samples with 96.20% removal potential, hence, offered an effective sorbent for removal of RO 107 contaminated water samples.

肾脏衰老的代谢谱变化及黄精多糖对D-半乳糖诱导的衰老小鼠的保护作用

目的基于超高效液相色谱-四级杆静电场轨道阱质谱(UPLC-Q-Exactive MS/MS)研究D-半乳糖诱导衰老小鼠肾脏衰老的代谢轨迹,以及黄精多糖对D-半乳糖诱导衰老小鼠肾脏衰老的影响。方法将36只C57BL/6J小鼠随机分为6组:对照组(CON)、模型组(MOD)、黄精多糖低剂量组(PSP-L)、中剂量组(PSP-M)、高剂量组(PSP-H)和阳性药物组(VC)。为建立衰老模型,除对照组外,其他各组小鼠均往腹腔注射D-半乳糖。模型建立后,给予相应的中药[PSP,PSP-L:150 mg/(kg·d),PSP-M:300 mg/(kg·d),PSP-H:600 mg/(kg·d)]或阳性药物[抗坏血酸,300 mg/(kg·d)]进行干预。测定各组小鼠尿液和血清中肾功能的关键指标,如肌酐(Crea)、尿素氮(BUN)和尿酸(UA)水平,以及血清和肾脏中氧化应激的关键指标,包括超氧化物歧化酶(SOD)、过氧化氢酶(CAT)、丙二醛(MDA)和谷胱甘肽过氧化物酶(GSH-Px),以验证肾脏衰老模型的成功建立,并评价黄精多糖的影响。苏木精-伊红(HE)染色、过碘酸雪夫(PAS)染色和β-半乳糖苷酶染色用于评估肾脏病理变化。采用UPLC-Q-Exactive MS/MS分析了对照组、模型组和黄精多糖高剂量组血清、肾脏和尿液样本的代谢谱,并利用模式识别方法研究肾脏衰老的代谢轨迹和特征代谢物的鉴定。结果与年龄有关的小鼠肾组织病理学改变和肾功能受损与氧化应激指标有关。给予黄精多糖[PSP-H:600 mg/(kg·d)]后,与衰老相关的病理指标被调整到正常水平,衰老小鼠的肾功能和氧化应激得到改善,并显著改善了肾脏病理损伤。同时,通过UPLC-Q-Exactive MS/MS分析鉴定了潜在的生物标志物,并进一步以P<0.05为临界值分析形成了相关的代谢通路。结果表明,嘌呤代谢、鞘脂代谢、甘油磷脂代谢、色氨酸代谢和核黄素代谢是衰老相关的主要代谢通路。给予黄精多糖后,这些病理指标恢复到正常水平,与衰老过程相关的生物标志物,如单磷酸腺苷(AMP)、色氨酸和5-羟色氨酸,也在一定程度上表现出反向调节(促进合成)作用。结论基于UPLC-Q-Exactive MS/MS和多元统计分析的代谢组学方法可用于建立衰老小鼠的代谢谱。黄精多糖可通过干扰肾脏中的嘌呤代谢,鞘脂代谢,甘油磷脂代谢,色氨酸代谢和核黄素代谢,显示出对肾脏衰老的保护作用。

Kadsura coccinea:A rich source of structurally diverse and biologically important compounds

Kadsura coccinea belongs to medicinally important genus Kadsura from the Schisandraceae family.It has been used in traditional Chinese medicine(TCM)for the treatment of rheumatoid arthritis and gastroenteric disorders.The initial phytochemical work focused on the identification of some structurally novel and diverse natural products,which turned the attention of many researchers towards this plant.Thus far,202 compounds have been reported in this plant.Lignans and terpenoids were found as the main chemical constituents of this plant.Some of the triterpenoids and sesquiterpenoids with novel structures are of particular interest for natural product researchers.The isolated compounds of this plant have shown different bioactivities including anti-tumor,anti-HIV,anti-inflammatory,nitric oxide(NO)production inhibitory and other pharmacological effects.This review systematically summarizes all the phytochemical and pharmacological work done so far on K.coccinea,and can be used as a reference for future research on this plant.

山银花化学成分与其生物活性的研究进展（英文）

山银花作为中国传统中药,在中国有数千年历史。目前,山银花在湖南省有广泛栽培,主要作为清热药和消毒药应用。山银花主要包括咖啡酸衍生物、挥发油、黄酮类化合物、环烯醚萜苷和萜类化合物,主要有抗炎、抗肿瘤、抗氧化、抗过敏、免疫调节及抗菌活性等。本文通过查阅相关文献,对山银花的化学成分及其生物活性进行了全面的系统总结。

南五味子属植物三萜类化合物及其药理作用研究进展（英文）

五味子科南五味子属植物在民间治疗类风湿性关节炎和胃肠疾病具有悠久历史,研究表明其主要活性成分为木脂素和三萜类化合物。三萜类化合物是五味子科五味子属和南五味子属植物的主要差异性化学成分。本文对近三十年(1987-2017年)南五味子属植物中的214种三萜类化合物的结构分类及其药理活性的研究进展进行了系统综述,以期为进一步的研究提供理论参考。

Bioassay-guided isolation of novel and selective urease inhibitors from Diospyros lotus

Two new dimeric naphthoquinones, 5′,8′-dihydroxy-6,6′-dimethyl-7,3′-binaphthyl-1,4,1′,4′-tetraone(1; Di-naphthodiospyrol D) and 5′,8′-dihydroxy-5,8-dimethoxy-6,6′-dimethyl-7,3′-binaphthyl-1,4,1′,4′-tetraone(2; Di-naphthodiospyrol E), along with known naphthoquinones diospyrin(3) and 8-hydroxy diospyrin(4) were isolated from the chloroform fraction of extract of Diospyros lotus roots. Their structures were elucidated by advanced spectroscopic analyses, including HSQC, HMBC, NOESY, and J-resolved NMR experiments. The fractions and compounds 1-4 were evaluated for urease activity and phosphodiesterase-Ⅰ, carbonic anhydrase-Ⅱ and α-chymotrypsin enzyme inhibitory activities. Compounds 1 and 2 and their corresponding fractions showed significant and selective inhibitory effects on urease activities. The IC_(50) values of 1 and 2 were 260.4 ± 6.37 and 381.4 ± 4.80 μmol·L-1, respectively, using thiourea(IC_(50) = 21 ± 0.11 μmol·L^(-1)) as the standard inhibitor. This was the first report demonstrating that the naphthoquinones class showed urease inhibition.

Metabolic engineering of Yarrowia lipolytica for scutellarin production

Scutellarin related drugs have superior therapeutic effects on cerebrovascular and cardiovascular diseases.Here,an optimal biosynthetic pathway for scutellarin was constructed in Yarrowia lipolytica platform due to its excellent metabolic potential.By integrating multi-copies of core genes from different species,the production of scutellarin was increased from 15.11 mg/L to 94.79 mg/L and the ratio of scutellarin to the main by-product was improved about 110-fold in flask condition.Finally,the production of scutellarin was improved 23-fold and reached to 346 mg/L in fed-batch bioreactor,which was the highest reported titer for de novo production of scutellarin in microbes.Our results represent a solid basis for further production of natural products on unconventional yeasts and have a potential of industrial implementation.

Microwaves spark emission spectroscopy for the analysis of cations:A simple form of atomic emission spectroscopy

为阳离子分析的一个新奇方法被调查。分析基于在在一个石墨房间放以后在微波炉发出火花金属的盐。石墨房间吸收微波并且生产把盐变换成射出种类的光的高温度。然而，光的颜色在阳离子的性质上被发现到依赖者射出的光的紧张被发现除了盐的集中正在取决于石墨集会的形式和形状。这通讯为所有这些观察并且为介绍解释系统并且定量分析使用微波火花排放技术。

New antiglycation and enzyme inhibitors from Parmotrema cooperi

Lichens are unique individuals which have been widely used in traditional medicines.This study was focused on the bioassay-guided phytochemical investigation,and bioactivity evaluation on a lichens species,Parmotrema cooperi.This first bioassay-directed chemical study on P.cooperi has led to the isolation of ethyl heamatomate(1),atraric acid(2),ethyl orsellinate(3),orsellinic acid(4),lecanoric acid(5),gyrophoric acid(6),and licanorin(7).The structures of 1-7 were mainly elucidated from spectroscopic methods including 1D,and 2D NMR spectroscopy,and mass spectrometry.These compounds were evaluated for their antiglycation,urease,α-chymotrypsin,and β-glucoronidase inhibitory activities.Few of the phenolic compounds showed significant,while most of them showed good inhibition of protein glycation,and urease activities.