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Purpose: To study the antimicrobial and cytotoxic potential of a novel 3,9-peroxsesquiterpene-15-Oglucoside from Cyperus rotundus rhizomes, against HeLa cell line and selected strains of microorganisms. Methods: The rhizomes were macerated with methanol and fractionated with n-hexane, chloroform, ethyl acetate and butanol. High-performance liquid chromatography (HPLC) was performed together with chemical analysis of the fractions. The 3,9-peroxysesquiterpene-15-O-glucoside was purified through column chromatography of the ethyl acetate fraction, and its purity was determined via reversephase HPLC. Structural elucidation was done with Infrared (IR), proton-nuclear magnetic resonance (HNMR), carbon-13 nuclear magnetic resonance (13C NMR), and mass spectrometry (MS) spectroscopic analyses. Results: The isolated compound exhibited bactericidal and fungicidal activities against S. aureus and C. albicans at concentration, respectively, in the range of 32 – 100 μg/mL, while MTT assay results showed the cytotoxicity of the compound against eukaryotic (HeLa) cell line (IC50, 88.32 μg/mL). Conclusion: The isolated metabolite from the methanol extract of C. rotundus rhizome exhibits bactericidal, fungicidal, and cytotoxic potential. However, further studies are required to ascertain its suitability for use as a therapeutic agent. Keywords: Terpenoids, Column chromatography, Spectroscopy, Antimicrobial, Cytotoxicity, Cyperus rotundus

Awsaj (Lycium barbarum) is a plant belong to family Solanaceae serves as a good source of bioactive compounds like phytosterols which have many important biological activity. Literature survey available so far revealed that there was no studies about Iraqi wild Awsaj phytosterols especially B-sitosterol, there for the objective of this study was to examine the efficiency of ultrasound assisted extraction (probe and bath) as compared to the conventional (Soxhlet) extraction method for extraction of phytosterols especially B-sitosterol from fruits, leaves, stems and roots of Iraqi wild Awsaj plant. This goal was achieved by comparing the extraction mass yield, also by a quick and easy approach for identification and quantification of bioactive B-sitosterol in four parts of Awsaj using high performance thin layer chromatography (HPTLC) which confirm the presence of B-sitosterol in four parts of Iraqi Awsaj plant and the results clarify that the root part of Iraqi Awsaj plant extracted by probe UAE give the highest concentration (0.610 mg/ml) of B-sitosterol followed by fruits (0.465mg/ml), leaves(0.405mg/ml) and the least was stems(0.275mg/ml); according to these; isolation and purification of B-sitosterol from petroleum ether fraction of Awsaj roots was done by preparative HPLC. The isolated compound (B-sitosterol) was identified by measuring melting point, FT-IR, TLC and preparative HPLC. Key words: Awsaj, ultrasound assisted extraction (UAE), B-sitosterol, high performance thin layer chromatography (HPTLC), preparative high performance liquid chromatography (PHPLC).

A small number of researches were done in the design and synthesis of enkephalin analogues that are able to resist degradation effect of proteolytic enzymes with good bioavailability and half-lives.Through studying structure activity relationships we tried to incorporate phthalyl group, tryptophan and lysine amino acids in different positions in the basic backbone structure of the naturally occurring opioid Leu5- and Met5- enkephalin, in the hope that such insertion of these amino acids could induce interesting addition in the biological activity of these analogues with enhancement of their bioavailability, in addition to decrease side effects as addiction liability. These synthesized peptides are: Analogue I: phthalyl-tyrosyl-glycel-tryptophan methyl ester. Analogue II: Boc-tyrosyl-glycyl-phenylalanyl-lysine ethyl ester. HBr. According to the designed structures, the analogues were synthesized following the conventional solution method and they were identified using the following techniques: melting point, optical rotation, thin layer chromatography (TLC), infrared spectroscopy (IR), elemental analysis (CHN) and amino acid analysis. Key words: peptide, phthalyl, opoioid analgesics

Background: Coumarin is quite extend in plants including various vegetables, flavors, foods. Coumarin has various significant medicinal activities such as anti-inflammatory, anti-oxidant, anti-viral, anti-microbial, anti-cancer and has been indicated to increase central nervous system activity. Methods: The syntheses of tailor-made coumarins, which are highly compelling for medical applications due to their structurally interesting antioxidant activity, were report in this manuscript. Coumarins were synthesized successfully through the modification of 4-hydroxycoumarin by different reaction steps. The molecular structures of the coumarins were characterized by the Fourier transformation infrared and Nuclear magnetic resonance (NMR) spectroscopies. The antioxidant efficiency of the 4-hydroxycoumarins were evaluated by typical spectroscopic method, using radicals DPPH• and H2O2. Results: The new coumarins synthesized in this work exhibited an excellent antioxidant compared to the free vitamin C. Molecular modelling studies using DFT (Density Functional Theory) calculations showed that there is a high correlation between dipole moment, Ionization potential (IP), Electron affinity (EA), Hardness (η), Softness (S), Electro negativity (μ), energy gap, HOMO (Highest Occupied Molecular Orbital) and LUMO (Lowest Unoccupied Molecular) energies and antioxidant activity. Conclusion: New coumarin derivatives were successfully synthesized using chemical methods. The characterized of these coumarins were done by using different spectroscopic techniques (FT-IR and NMR) and micro-elemental analysis (CHNS). The antioxidant activity of these coumarins were determined by using DPPH and hydrogen peroxide assays. Results indicated that the new coumarins possess higher scavenging activity than vitamin C.

Burdock ( Arctium lappa), is among the most popular plants in traditional medicine and it is associated with several biological effects. Literature survey revealed the presence of phenylpropanoid compounds .The most widespread are hydroxycinnamic acids ( mainly caffeic acid and chlorogenic acid) and lignans (mainly arctiin and arctigenin). This work will confirm the presence of these compounds in Arctium lappa, cultivated in Iraq, in both root and leaf samples. The dried plant samples were extracted by soxhlet with 80% methanol then separated the main constituents by thin layer chromatography (TLC) and high performance liquid chromatography (HPLC). Identification of the isolated compounds was carried out by UV, IR, and compared with reference standards using TLC, HPLC and HPTLC. Keywords: Actium lappa, hydroxycinnamic acid, Lignan, Phytochemical.

Ammi species belong to the family Umbellifereae that provide a host of bioactive compounds (mainly coumarins and flavonoids) of important biological activities, like prevention and treatment of heart and vascular disease and some types of cancer. Literature survey revealed that there was no study concerning Ammi flavonoids in Iraq. Ammi majus and Ammi visnaga, which are wildly grown in Iraq, were chosen for this study. This study concerned with extraction, identification, isolation, and purification of some biologically important flavonols quercetin and kaempferol from the fruits of Ammi majus and Ammi visnaga. Extraction of these flavonols was carried out using 85% methanol and 90% ethanol. Identification of these flavonols quercetin and kaempferol was done using thin Layer chromatography (TLC) where different solvent systems had been tried. Ultra violet (UV) Light and iodine vapor where used for detection. This identification was further augmented by using high performance Liquid chromatography (HPLC) and then these flavonols were isolated and purified. The most suitable extraction, isolation and purification procedures of flavonols were fully described in this study. The identification of isolated flavonols (quercetin & kaempferol) was carried out using melting point (M.P.), Thin Layer chromatography (TLC), and infrared spectroscopy (IR).This study confirms the presence of quercetin and kaempferol in Ammi majus & an Ammi visnaga fruit, the percentage of quercetin was higher in Ammi visnaga than Ammi majus, while the percentage of kaempferol was higher in Ammi majus than Ammi visnaga. Key words : Ammi majus , Ammi visnaga , quercetin , kaempferol .

Plumbago (Plumbaginaceae) is a genus of 10-20 species of flowering plants used in traditional Indian medicine, native to warm temperature to tropical regions of the world. The roots of Plumbago europaea, the Iraqi species of Plumbago, have been used for the treatment of cancer, rheumatoid arthritis, and dysmenorrhea. The main active constituents from dried powdered leaves and roots of Plumbago europaea were extracted by Soxhlet apparatus using ethyl acetate, the main active constituent was characterized by spectroscopic analysis (IR, 1H NMR, and 13C NMR) as plumbagin. Quantitative and qualitative study of plumbagin in the roots and leaves extracts was carried out by HPLC technique using analytical column (Eurospher 100, C18, 5 µm, 250 x 4.6 mm) with 10% solvent (B) isocratic elution of methanol (solvent A) and water (solvent B) at flow rate 0.75 ml/min and detection wave length of 270 nm. The percentage of plumbagin in the root and leaf extracts was recorded to be (1.9 %) and (1.5 %) respectively. Keywords: Plumbago europaea, plumbagin, HPLC

A series of new coumarin and N-amino-2-quinolone derivatives have been synthesized. The reaction of coumarin (1) with excess of Hydrazine hydrate 98% yielded 1-amino-2-quinolone (2), Compound (2) was reacted with different Sulfonyl chloride to yield Sulfonamides [ N-(2-oxoquinolin-1(2H)-yl) methane sulfonamide (3), N-(2-oxoquinolin-1(2H)-yl) Benzene sulfonamide (4) and 4-methyl-N-(2-oxoquinolin-1(2H)-yl) benzene sulfonamide (5) ], while reaction of 2-(4-methyl-2-oxo-2H-chromen-7-yloxy) acetic acid (8) with different amines yielded compounds [ 2-(4-methyl-2-oxo-2H-chromen-7-yloxy)-N-(2-oxoquinolin-1(2H)-yl) acetamide (9) and N-(5-methyl-1,3,4-thiadiazol-2-yl)-2-(4-methyl-2-oxo-2H-chromen-7-yloxy)acetamide (10) ] through amide linkage.The reactions and purity of the products were checked by TLC. The structures of the final compounds and their intermediates were confirmed by their melting points, IR spectroscopy, and elemental microanalysis.The coumarin and N-amino-2-quinolone derivatives were evaluated for their anti bacterial and antifungal activity. Key words: coumarin , 1-amino-2-quinolone, sulfonamide, amide, biological activity.

This study concerned with phytochemical investigation and methods of extraction and separation of active constituents from Valeriana officinalis plant cultivated in Iraq. Due to the large number of active constituents in Valeriana officinalis, it was necessary to make analytical study of its constituents to determine the chemical nature of these constituents and then determine the main classes (terpenes and iridoids) using chemical reagents specific for each class. Different organic solvents like ethanol (70%) used in soxhlet apparatus and hexane, ethyl acetate and methanol were used separately to extract the main active constituents by maceration. Through comparison between these solvents using thin layer chromatography (TLC), it has been found that hexane was best suited to extract most of the active constituents from the plant by maceration method. Analytical study showed that terpens was separated and purified using preparative TLC and preparative HPLC. Identification of isolated component (valtrate) from roots of plant was obtained using HPLC and PHPLC also depending on some material-specific constants such as infrared spectroscopy (FTIR). Results of analysis showed that Valeriana officinalis cultivated in Iraq is a good source of many constituents with different important pharmacological activities. The pharmacological study showed that the total organic plant extract has sleep induction effect when injected I.P. to experimental mice. Key wards: Valeriana officinalis, Valepotriate, Insomnia.

Coumarins are important and useful compounds with diverse pharmacological properties. New coumarin derivatives namely N-aminoquinoline-2-one 1, 1-((4-hydroxy-6-methyl-2-oxo-2H-pyran-3-yl)methyleneamino)quinolin-2(1H)-one 2 and 1,1′-(1E,1′E)-(1,4-phenylenebis(methan-1-yl-1-ylidene))bis(azan-1-yl-1-ylidene)diquinolin-2(1H)-one 3, were synthesized and characterized by UV–Vis, FT-IR, and NMR spectra in addition of elemental analysis. The synthesized compounds (2 and 3) show considerable anticancer activity against HEp-2 cell line. Synthesized compounds (2 and 3) were tested against selected types of microbial organisms and showed significant activities. The free-radical scavenging activity of synthesized compounds (2 and 3) have been determined by their interaction with the stable free-radical 1,1-diphenyl-2-picrilhydrazyl (DPPH) and all the compounds have shown encouraging antioxidant activities.

Problem statement: The studied dihydropyridone was synthesized for the first time via the microwave assisted reaction of curcumin and methylamine and it is important to support the mechanism by the crystal structure. Approach: The crystal structure of the title compound was determined using high resolution x-ray diffraction. PowderSolve program was used to solve the structure while the refinement was done in material studio Reflex module. Results: The findings obtained with high-resolution x-ray powder diffraction and molecular location methods based on simulated annealing algorithm after Rietveld refinement showed that the monoclinic unit cell was a = 13.4925 A b = 12.8162 A, c = 11.5231 A, α = 90.000°, β= 99.0401°,γ = 90.000°; cell volume = 1967.85A3 and space group P 21/a with 4 molecules in a unit cell. Conclusion/Recommendations: Powder diffractometry could be a powerful tool for determining crystal structures for organic molecules.

The search for new peptides to be used as analgesics in place of morphine has been mainly directed to develop peptide analogues to have higher biological stability and receptor selectivity. Therefore extensive researches have been carried out on naturally occurring and synthetic opiates in order to enhance the analgesic potency, so we intended to prepare opioiod peptide analogue linked to estrone which may increase the analgesic effect of this compound. Steric hindrance clearly will be produced by estrone may affect the enzymatic activity on the synthesized analogue and this in turn may enhance the bioavailability of the analogue itself, meanwhile estrone may affect physicochemical properties of the analogue by increasing its lipophilicity and so facilitate its passage through the biological barriers, also estrone may affect receptor binding selectivity of this analogue and decrease the side effect of the original opioid peptide. The designed analogue is (estrone-3-O-acyl-tyr-gly-gly-phe-met-OH), where this opioid peptide synthesized following the conventional solution method, then linked to estrone by amide linkage and it was characterized using: thin layer chromatography (TLC), melting point, infrared spectroscopy (IR), elemental microanalysis(CHN), optical rotation, amino acid analysis, and hydrogen-nuclear magnetic resonance( 1 H-NMR).

Problem statement: Pyridones are known to have variety of biological activities like antitumor, antibacterial, anti-inflammatory and antimalarial activities. This study presents antiviral evaluation of dihydropyridones derived from curcumin, as well as curcumin for comparison. Approach: The compounds evaluated for their in vitro antiviral activities against the viruses: HIV-1, Bovin viral Diarrhea, Yellow Fever, Reovirus 1, Herpesvirus 1, Vaccinia, Vescular Stomatitis, Coxackie virus B2, Poliovirus 1 and Respiratory Syncytial viruses by using Microculture Tetrazolium assay (MTT) method. The method was based on the metabolic reduction of 3-(4,5-dimethylthiazol-2- yl)-2,5-diphenyltetrazolium bromide. Results: Antiviral biological activities represented as CC50 were within the range >100-26 for BHK-21, while they were within the range >90-≥13 against Respiratory Syncytial Virus when represented as EC50 for example. Both CC50 and EC50 values were found to increase with increasing chain length of the substituent on the nitrogen atom. Conclusion: The in vitro antiviral activities of the tested dihydropyridones can be enhanced by increasing chain length of the substituent on the nitrogen atom.

Dihydropyridones were prepared by microwave-assisted reaction between curcumin and primary amines or their acetates in the presence of Montmorillonite (K-10) as a catalyst. The reaction was complete within a few minutes and the yield depends on the amine used.

Dihydropyridones were prepared by microwave-assisted reaction between curcumin and primary amines or their acetates in the presence of Montmorillonite (K-10) as a catalyst. The reaction was complete within a few minutes and the yield depends on the amine used.