Search

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.

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).

Alteration in the backbone structure of the endogenously released opioid peptides Leu5/Met5 enkephalins may result in compounds having comparable profile of pharmacological activity but with different physicochemical properties and side effects. Phthalyl amino acid and phthalyl esters are among the derivatives that have been synthesized and evaluated for their antibacterial and antifungal activities.This study was conducted to evaluate the possible analgesic activity of phthalyl-tyrosyl-glycin sodium that has been recently synthesized by our team.The study was carried out on 24 albino mice using hot plate method. The animals were allocated in to three groups; the first group received saline and represent a control group; the second group received morphine HCl as a standard drug; and the third group received phthalyl-tyrosyl-glycin sodium. The onset with which the animal lift his forearm and the number of jumps per 25 seconds were recorded for each group. The results of this study showed that phthalyl-tyrosyl-glycin sodium resulted in significant improvement (P0.05) was observed in analgesia score but with significant delay in induced hyperalgesia.The results obtained in this study provide experimental evidences for the effectiveness of the prepared compound as analgesic with comparable effect to that of morphine. Key words: Phthalyl-tyrosyl-glycin sodium, phthalyl group, analgesia

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

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

So far synthesis of Gonadotropin Releasing Hormone (GnRH) analogues reported in the literature has clarified some aspects of structural activity of the naturally released GnRH. As a part of continuing efforts for further understanding of this relationship, the present investigation was undertaken which involved synthesis and biological evaluation of two GnRH analogues, firstly, by replacement of the amino acid L-Argenine in the 8th position at the backbone structure of the natural hormone by the amino acid D-Alanine; and secondly, by replacement of the amino acid L-Glycine in the 10th position by D-Alanine also at the backbone structure of the nature hormone, to obtain the following analogues respectively: PGlu-His-Trp-Ser-Tyr-Gly-Leu-DAla-Pro-Gly-NH2 (Analogue I: D-Alanine8 GnRH), PGlu-His-Trp-Ser-Tyr-Gly-Leu-Arg-Pro-DAla-NH2 (Analogue II: D-Alanine10 GnRH), which were synthesized by applying conventional solution method. Peptides were purified by several recrystallization using appropriate solvent and proved to be homogenous. Conformity of the synthetic procedure was achieved by applying different physico-chemical analyses including Melting Point (mp), Thin Layer Chromatography (Tlc.), Infrared Spectroscopy (IR), Elemental Analysis (CHN), Amino Acid Analysis (AAA), and Nuclear Magnetic Resonance (H1NMR).Preliminary biological activity of the two analogues was determined by testing their effects of parenteral administration on ascorbic acid depletion from the ovary of pseudopregnant mice and compared with that of natural GnRH hormone. Analogue II showed significant ascorbic acid depletion as compared to the native hormone while the percentage in ascorbic acid depletion after administration of analogue I were not significant as compared to the native hormone. Key Words: Gonadotropine releasing hormone, Peptide synthesis, Biological activity of GnRH

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.

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.

This study includes synthesis of some nitrogenous heterocyclic compounds linked to amino acid esters or heterocyclic amines that may have a potential activity as antimicrobial and/or cytotoxic. Quinolines are an important group of organic compounds that possess useful biological activity as antibacterial, antifungal and antitumor .8-Hydroxyquinoline (8-HQ) and numerous of its derivatives exhibit potent activities against fungi and bacteria which make them good candidates for the treatment of many parasitic and microbial infection diseases. These pharmacological properties of quinolones aroused our interest in synthesizing several new compounds featuring heterocyclic rings of the quinoline derivatives linked to amino acid ester or heterocyclic amine with the aim of obtaining a pharmacologically active compounds.O-alkylation has been done on( 8-hydroxyquinoline ) to get (O-alkylated ester) derivatives which are deesterfied to get acetic acid derivatives, then coupled with amino acid that have protected carboxyl group (amino acid esters) or heterocyclic amine by using conventional solution method for peptide synthesis as a coupling method. The proposed analogues were successfully synthesized and the processing of the reactions confirmed by TLC ,the synthesized analogues with the proposed structures as they were characterized and proved by melting point, infrared spectroscopy (IR) and elemental microanalysis. The tested analogues showed cytotoxic activity on the HEp-2 cell line (tumor of larynx) with inhibitory concentration percent of (IC %) range (32.43 % - 49.55%) and showed that the tested compounds had variable antimicrobial activities against selected bacteria and yeast when compared with selected standard drugs. Keywords: Quinolones, 8-hydroxyquinoline , N-heterocycles biological activity.

A series of coumarin derivatives linked to amino acid ester side chains were synthesized and evaluated of their antibacterial and antifungal activity. The coumarin derivatives was alkylated by the ethyl bromoacetate and then using potassium carbonate to get alkylated hymecromone. Conventional solution method for amide bond formation was used as a coupling method between the carboxy-protected amino acids with acetic acid side chain of coumarin derivatives. The DCC/ HOBt coupling reagents were used for peptide bond formation. The proposed analogues were successfully synthesized and their structural formulas were consistent with the proposed structures as they were proved and characterized by thin layer chromatography (TLC), melting point, infrared spectroscopy (IR), and elemental microanalysis (CHN). Key words: coumarin, amino acid, coumarin antimicrobialal 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.