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.

Optimization Conditions of the Preparation of Activated Carbon Based Egusi (<i>Cucumeropsis mannii</i>Naudin) Seed Shells for Nitrate Ions Removal from Wastewater

Egusi seed shells (ESS) were used as precursor for the preparation of two activated carbons (ACs) following H3PO4 and ZnCl2 activation. The effect of factors controlling the preparation of ACs such as chemical activating agent concentration (2 - 10 M), activation temperature (400°C - 700°C) and residence time (30 - 120 min) were optimized using the Box-Behnken Design (BBD). The optimized activated carbons based H3PO4 (ACP) and ZnCl2 (ACZ) were characterized by N2 adsorption, elemental analysis, atomic force microscopy (AFM), Boehm titration and Fourier transformed infrared (FTIR) techniques. The specific surface area was found to be 1053.91 and 1009.89 m2·g-1 for ACP and ACZ respectively. The adsorbents had similar surface functionalities and were both microporous. The effect of various parameters such as initial pH, concentration, and contact time on the adsorption of nitrate ions on ACP and ACZ in aqueous solution was studied. ACZ demonstrated better adsorption capacity (8.26 mg·g-1) compared to ACP (5.65 mg·g-1) at the same equilibrium time of 20 min. The adsorption process was governed by a “physical interactions” phenomenon for both adsorbents.

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.

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.

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.

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.

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.

<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.

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.

Isolation and characterization of xanthine oxidase inhibitory constituents of Pyrenacantha staudtii

Six compounds have been isolated from the leaves of Pyrenacantha staudtii, two of which are new compounds. The new compounds have been characterized as kaempherol 3-O-β-rhamnopyranosyl (1→6)-β-D-glucopyranoside (1) and 4-β-glucopyranosyl-(2-furyl)-5-methy-l,2-glucopyranoside phenylmethanone (2). The known compounds are 3-pyridinecarboxylic acid (3), β-sitosterol (4), sitosterol 3-O-β-glucopyranoside (5) and taraxerol (6). Their structures were determined by spectroscopic and chemical evidences. The two new compounds together with 3-pyridinecarboxylic acid showed significant in vitro xanthine oxidase inhibitory activity. To the best of our knowledge, this is the first report of these compounds from this plant.

Urinary metabolomics analysis of the anti-depressive effects of Hemerocallis citrina extracts in a simulated microgravity-induced rat model of depression

We investigated the antidepressant-like activity of Hemerocallis citrine Baroni extract(HCE)in a simulated microgravity(SMG)-induced rat model of depression using a metabolomics method.A rat model,generated via 14 d of SMG induction,was validated from the reduced sucrose preference and the enhanced immobility time in the forced swimming test.HCE and paroxetine reversed certain metabolite profiles.Anti-depressant effects of HCE might involve the regulation of several metabolic pathways,such as phenylalanine,glutamic acid,and tryptophan metabolism and changes in energy metabolism.5-Hydroxytryptophan,hippuric acid,phenylacetylglycine,citric acid,3-hydroxykynurenine,cyclic AMP,and L-DOPA profiles were altered upon HCE and paroxetine administration.Furthermore,glutamic acid was only regulated in the HCE group,while xanthurenic acid and deoxyuridine were reversed in the positive group,suggesting differences in the mechanisms between the positive drugs and HCE in improving glutamic acid metabolism.This study provided a theoretical foundation for the application of HCE in depression therapy.

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.

Structural basis of AimP signaling molecule recognition by AimR in Spbeta group of bacteriophages

Dear Editor,Quorum sensing(QS)is a widespread phenomenon in bacteria which enables them to participate in cell-to-cell communication by producing and responding to small signal molecules,thus synchronously altering their behavior depending on population density(Singh et al.,2000;Miller and Bassler,2001).Through QS,bacteria coordinate processes such as expression of virulenee factors(Slamti and Lereclus,2002),biofilm formation(Parashar et al.,2011),sporulation(Perego et al.,1996),conjugation(Kozlowicz et al.,2006),antibiotic synthesis(Miller and Bassler,2001;Whiteley et al.,2017)etc.

Tsc1/Tsc2 complex: A molecular target of capsaicin for protection against testicular torsion induced injury in rats

Objective: The detailed knowledge about protective effects of capsaicin(cap) and involved mechanisms against testicular torsion(TT) is still not available completely.Methods: Male Wistar rats were assigned into four major cohorts:(i) sham,(ii) TT,(iii) three subgroups subjected to TT and different doses of cap(100, 500, and 1000 μg/mL), and(iv) three subgroups of healthy animals subjected to various concentrations of cap. The animals were decapitated at 24 h after reperfusion, and the evaluation of protein expression was performed by Western blotting assay. At 72 h after reperfusion, apoptotic cell death and tissue injury were evaluated by TUNEL nuclear and H&E staining,respectively.Results: The results showed that cap administration following TT significantly increased the expression of tuberous sclerosis proteins 1 and 2(Tsc1/Tsc2) in a dose-dependent manner(P < 0.05). Cap decreased cell apoptosis at highest dose. Likewise, cap contributed to the preservation of tubular morphology and decreased tissue injury at the highest tested concentration(1000 μg/m L).Conclusion: Collectively, our findings demonstrate the validity of cap as a therapeutic agent against TT through targeting Tsc1/Tsc2 in a dose-dependent manner.

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

A novel method for the cation analysis was investigated. The analysis is based on the sparking of the salts of metals in a microwave oven after placing in a graphite cell. The graphite cell absorbs microwaves and produces high temperature which converts the salt into light emitting species. The colour of light was found to dependent on the nature of cation, however, the intensity of the emitted light was found to be depending upon the form and shape of the graphite assembly in addition to the concentration of the salt. This communication presents explanation for all these observations and for the systematic and quantitative analysis using microwave spark emission technique.

Anti-diabetic related health food properties of traditional rice(Oryza sativa L.)in Sri Lanka

Objective:To evaluate a range of anti-diabetic related properties and some consumer preferred physicochemical properties of selected Sri Lankan traditional rice varieties.Methods:Sudu Heeneti,Goda Heeneti,Masuran and Dik Wee varieties were used in this study.Anti-diabetic related properties of bran extracts of selected varieties were studied for methylglyoxal mediated protein glycation inhibition,acetyl and butyryl-cholinesterase inhibition in vitro and anti-hyperglycemic activity in vivo.Further,selected varieties were studied for starch hydrolysis rate in vitro.Physicochemical properties including grain color,size,shape,crude protein,crude fat,ash,dietary fiber and total carbohydrate contents were studied.Results:Brans of selected varieties had significant(P<0.05)and dose dependent methylglyoxal mediated protein glycation inhibition[IC_(50):(174.77±6.65)to(342.87±0.43)μg/mL]and acetyl[IC_(50):(37.00±0.68)to(291.00±3.54)μg/mL]and butyryl-cholinesterase[IC_(50):(18.50±0.60)to(96.60±0.56)μg/mL]inhibitory activities.Further,Sudu Heeneti,Masuran and Dik Wee had low starch digestion rate(52.40±1.44 to 53.76±1.19)indicating that these varieties may be low glycemic index rices.Brans of Masuran tested in rat model showed anti-hyperglycemic activity.Physicochemical properties studied showed that selected varieties were red in color and grain size and shape were mostly medium and bold respectively.Moisture,crude protein,crude fat,ash and total carbohydrate contents varied significantly(P<0.05)among the varieties.Conclusions:It is concluded that selected varieties could be promoted as physicochemically sound rices with a range of anti-diabetic related properties in the management of diabetes and its complications.

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 bioassayguided phytochemical investigation, and bioactivity evaluation on a lichens species, Parmotrema cooperi. This first bioassaydirected 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, a-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.

Parmotrema cooperi中的新型抗醣化物质和酶抑制剂

地衣是被广泛用于传统药物中的独特个体.本文对一类地衣,Parmotrema cooperi,进行了生物测定引导的植物化学研究和生物活性评价.对该类地衣的首次生物测定引导的化学研究分离出了化合物ethyl heamatomate(1),atraric acid(2),ethyl orsellinate(3),orsellinic acid(4),lecanoric acid(5),gyrophoric acid(6)以及licanorin(7).化合物1～7的结构主要通过一维、二维核磁共振谱和质谱等谱学方法判定.对这些化合物还进行了抗醣化活性以及尿素酶、α-胰凝乳蛋白酶、β-葡萄糖醛酸苷酶抑制活性的评价.这些苯酚化合物没有显示特别好的活性,但其中大部分对蛋白质醣化和尿素酶活性具有较好的抑制作用.