M. CHERIET Thamere

abstract

a

From folk medicinal uses to phytochemical and biological studies, Linaria species
(Plantaginaceae) have been extensively studied. Moreover, it is important to note that the main
reason behind placing Linaria species in the category of a subject of interest is their ability to
contain different bioactive molecules. A suitable example is pectolinarin, and its derivatives,
which are well known for their powerful biological effects. Therefore, this study came with the
objective to compare the effect of extraction methods (Maceration, Soxletation, Sonication, and
Infusion) on the yield and polyphenol_flavonoid contents of Linaria gharbensis. The
phytochemical study was carried on two parts; the first one was about the qualitative analysis
that revealed a strong presence of flavonoids and a remarkable presence of triterpenoids and
cardiac glycosides. Whereas, the second part was about the quantitative analysis, evaluating the
contents of flavonoids and polyphenols. The results were shown that the sonication and
soxhletation with MeOH gave higher polyphenol content (34.350 ± 5.873, 28.649 ± 8.911 μg
GAE/mg EE respectively). Higher flavonoid contents were observed for Sonication and
soxhletation with MeOH as well (34.013 ± 4.365, 29.674 ± 2.395 μg QE/mg EE respectively).
The antibacterial evaluation of the extracts obtained by different methods of extraction has
displayed no activity against three available bacterial strains E. coli, S. aureus, and P.
aeruginosa, this result is quietly in accordance with the literature. (This study affords the first
preliminary phytochemical investigation and antibacterial property of Linaria gharbensis).
Keywords: Linaria gharbensis, Extraction methods, Soxhletation, Sonication, Total phenolic,
Flavonoid contents.

ce polycopié comporte les notions essentielles des méthodes et stratégies en synthèse organique. Ce document est destiné principalement aux étudiants de Master I en
chimie organique. Le but de ce polycopié est de fournir à l’étudiant les bases nécessaires, permettant de faire introduire les étudiants aux notions de bases de la synthèse
organique, et par la suite les différentes réactions de synthèse qui sont indispensables dans la production des molécules bioactifs très utilisées dans le domaine pharmaceutique. Ce
polycopié comprend six chapitres, le premier est consacré aux notions de stratégies de synthèse (protection fonctionnelle, rétrosynthèse et planification, réactions tandem et multi
composants), le second chapitre traitera création des liaisons carbone-carbone, en utilisant les différents méthodes de synthèse (chimie des énolates et azaénolates; alkylation, βhydroxyalkylation et réactions apparentées; acylation, aldolisation-crotonisation; additions de Michael; alkylidénation; cycloadditions - réactions concertées). Le troisième chapitre
concerne la création des liaisons carbone-hétéroatome (oxydation et réduction). Le quatrième chapitre est sur la chimie aromatique et comment créer des liaisons carbone-carbone et
carbone-hétéroatome (X). Le cinquième chapitre rassemble les différentes méthodes de synthèse et réactivité en série hétérocyclique aromatique pour synthétiser pyridine,
quinoléine, furane, thiophène, pyrrole, indole et bis-1H-indole, alors que le dernier chapitre offre une démonstration sur la synthèse multi-étapes des molécules complexes de produits
naturels et de nouvelles molécules organiques.
L’auteur remercie à l’avance les lecteurs qui voudront bien lui faire part des remarques et critiques que leur a inspirés la lecture de ce polycopié et souhaite que ce polycopié pourra
fournir à l’étudiant les informations nécessaires pour l’étude de méthodes et stratégies en synthèse organique.

The ficus genus is one of the largest genera of the mulberry family (Moraceae) are known for their ethno pharmacological,therapeutic importance and have been used in traditional medicine as a cure against malaria ,diabetes ,cancer ,diarrhea ,ulcer and tract infection. The objective of this study was to determine the total phenolic and flavonoid content of the ethyl acetate and nbutanol extracts from the ficus species by in vitro chemical analyses using the Folin-Ciocalteu (FCR) and the Aluminium Chloride (AlCl) method. The most significant total phenolic content was (303,47 ± 1,90 µg GAE/mg) to the ethyl acetate extract and the greatest flavonoid content was observed with n-butanol extract (155,07 ± 2,35µg QE/mg).
Key words: Moraceae, Mulberry, phenolic content, flavonoid content, FCR

This work concerned the phytochemical study of a plan from Lavandula genus many species of
this genus are known for their biological activities. the studied plant was extracted with ethanol
using ultra-sound method the obtained ethanolic extract was screened for different secondary
metabolites using standard methods and it was also tested for both total flavonoid and
polyphenol content the results showed the presence of different chemical groups such as
flavonoids, terpenoides and sterols while the TPC and TFC tests showed the presence of a
considerable amount of both plolyphenols and flavonoids
Mots clés : phytochemical screening, TPC , TFC , Lavandula

Plant secondary metabolism constitutes a large reservoir of natural chemical diversity that encompasses an enormous range of compounds. The requirement for secondary metabolites to have highly diverse biological activities has led plants to accumulate a vast number of compounds. Because plants cannot escape from their biotic and abiotic stressors, being linked to the ground by means of their root system, and therefore they must stay and protect themselves. Plants, as sessile organisms, evolve and exploit metabolic systems to create a rich repertoire of complex natural products that hold adaptive significance for their survival in challenging ecological niches on earth. The production of chemicals that deter or kill pests and pathogens represents one mean of self-protection. Plants produce a large number of secondary metabolites, which are classified into several groups according to their biosynthetic routes and structural features. The most known groups using by plants in defense are iridoids and flavonoids. This two classes are knowing as chemotaxonomic markers of the Scrophulariaceae family. The genus Linaria belongs to the Scrophularioideae˗Antirrhineae tribe of the Scrophulariaceae family comprises about 200 species, widely distributed throughout the northern hemisphere with its center of distribution in the Mediterranean basin and eastern Asia. Several Linaria species were used in folk medicine as tonics, antiscorbutics, laxatives, antidiabetics, and diuretics, as well as for the treatment of wounds, hemorrhoids, and vascular disorders. This genus is presented by 39 spices and subspecies in Algeria. One of these spices named L. reflexa Desf. and known as traditional plat « Oum lajrah » used for treatment of skin scar. The biological investigation proved the anti-proliferative action of several flavones and the acetyl cholinesterase inhibition of extracts and flavones isolated from the aerial parts of L. refelaxa. These results have courage as to continue the research for other bioactive compounds. For now we have isolate five compounds witch three are new for the spice, the two knowing compounds are bioactive compounds (pectolinarin & linariin).

The ethanol extract from aerial parts of Ranunculus were investigated for its chemical composition by LC-ESI-MS/MS technique, which allowed to identify a series of glycosylated flavonoids and one phenolic acid. RBEE extract showed acetyl-cholinesterase inhibition higher than the reference compound Galantamine at a concentrationof 200 µg/mL. A moderate antibacterial activity of the extract was also obtained against Staphylococcus aureus ATCC43300, Citrobacter freundii ATCC8090, and Proteus vulgaris ATCC29905 at a concentration 100 µg. Additionally, a good reduction in plasma coagulation time at 200 μL was also observed for RBEE

e profil phytochimique obtenu à partir de l'analyse LC-ESI-MS/MS de l' extrait de n- butanol (BEHL) de la plante endémique d'Afrique du Nord Hyacinthoides lingulata (Poir.) Rothm. a permis l'identification de dix dérivés glycosylés de l'apigénine et des flavones de lutéoline. Pour le même extrait végétal, anti-inflammatoire in vitro (test d'hémolyse induite par hypotonie et d'hémolyse induite par la chaleur) et antioxydant (DPPH et β-Carotène) ont été évaluées en observant une inhibition inflammatoire élevée en protégeant la stabilité membranaire des érythrocytes à la fois dans l'hémolyse induite par la chaleur (84,70 ± 0,24%) et l'hypotonie (79,45 ± 0,12%). Un effet hémostatique remarquable a également été établi en mesurant le temps de coagulation (15,95 ± 1,05 s à la dose de 1 mg/mL) de plasma décalcifié lié à son contenu phytochimique. Il s'agit du premier rapport sur les composants chimiques combinés et l'évaluation biologique de cette plante spécifique.

Hyacinthoides is a genus of perennial bulbous plants, belonging to the Asparagacae family. This genus is distributed in the western Mediterranean–Atlantic region and the Northern
African (Morocco to Tunisia) mountains. Previously published studies on this genus revealed its richness with phytochemicals that shown crucial biological effects. Precisely, Hyacinthoides lingulata (Poir.) Rothm. [Syn: Scilla lingulata Poir.], is one of the Algerian endemic species of this genus which is named in the Arabic language "Becal el far".
Therefore, in the present study, we investigate the chemical composition of the n-butanol extract obtained from the whole H. lingulata plant (bulbs, leaves, stems and flowers) by using
LC-ESI-MS/MS technique. The analysis of retrieved spectrum data in both negative and positive ionization modes led to the identification of ten glycosylated flavones (apigenin and
luteolin derivatives), among them nine compounds were firstly reported from the genus Hyacinthoides. The ESI/MS identification method was based on the search of the main
molecular ions and also on some of the useful observed fragmentations. The fragmentation pathway proposition of the elucidated compounds was established in this study.
Keywords: Hyacinthoides lingulata, glycosylated flavones, LC-ESI-MS/MS, fragmentation.

Plant secondary metabolism constitutes a large reservoir of natural chemical diversity that encompasses an enormous range of compounds. The requirement for secondary metabolites to have highly diverse biological activities has led plants to accumulate a vast number of compounds. Because plants cannot escape from their biotic and abiotic stressors, being linked to the ground by means of their root system, and therefore they must stay and protect themselves. Plants, as sessile organisms, evolve and exploit metabolic systems to create a rich repertoire of complex natural products that hold adaptive significance for their survival in challenging ecological niches on earth. The production of chemicals that deter or kill pests and pathogens represents one mean of self-protection. Plants produce a large number of secondary metabolites, which are classified into several groups according to their biosynthetic routes and structural features. The most known groups using by plants in defense are iridoids and flavonoids. This two classes are knowing as chemotaxonomic markers of the Scrophulariaceae family. The genus Linaria belongs to the Scrophularioideae˗Antirrhineae tribe of the Scrophulariaceae family comprises about 200 species, widely distributed throughout the northern hemisphere with its center of distribution in the Mediterranean basin and eastern Asia. Several Linaria species were used in folk medicine as tonics, antiscorbutics, laxatives, antidiabetics, and diuretics, as well as for the treatment of wounds, hemorrhoids, and vascular disorders. This genus is presented by 39 spices and subspecies in Algeria. One of these spices named L. reflexa Desf. and known as traditional plat « Oum lajrah » used for treatment of skin scar. The biological investigation proved the anti-proliferative action of several flavones and the acetyl cholinesterase inhibition of extracts and flavones isolated from the aerial parts of L. refelaxa. These results have courage as to continue the research for other bioactive compounds. For now we have isolate five compounds witch three are new for the spice, the two knowing compounds are bioactive compounds (pectolinarin & linariin).

Flavonoids are metabolites widely distributed in plants and commonly present in foods, such as fruits and vegetables. Pectolinarin, which belongs to the flavone subclass, has attracted considerable attention due to its presence in many medicinal plants. It has turned out to be a good biological agent especially due to its antioxidant, anti-inflammatory, antidiabetic, and antitumor activities, evaluated both in vitro and in vivo. Its aglycone, the metabolite pectolinarigenin, is also known for a series of biological properties including anti-inflammatory and antidiabetic effects. In the first overview on the two metabolites here presented, their collection, isolation and the results of their biological evaluation are reported.

The genus Linaria belongs to the Scrophularioideae˗Antirrhineae tribe of the Scrophulariaceae family comprises about 200 species, widely distributed throughout the northern hemisphere with its center of distribution in the Mediterranean basin and eastern Asia. This genus is very well presented in Algeria with the presence of 39 species and subspecies. Previous study on L. reflexa proved the importance of their flavones especially pectolinarin, linariin and pectolinarigenin with good cytotoxic and acetyl-cholinesterase inhibition activities. In the folk medicine of North Africa, L. reflexa Desf. is knowing for the treatment of certain skin diseases. To continue the previous research made on the phytochemical analysis of the genus Linaria, this present research present the identification of constituents of the MeOH extract of L. reflexa Desf., using the LC-MS. This research leads the detection of sixteen compounds and the determination of 8 flavonoids. These identified constituents were determinate after isolation with NMR 1 & 2D and mass spectra or with mass spectra comparing with literature data. The other constituents will identified after isolation using the HPLC in continuation of this research.

Keywords: LC-MS, Flavonoids, Linaria reflexa Desf., Scrophulariaceae.

The work presented here was aimed to investigate the in vivo anti-inflammatory and in vitro hemostatic activities of Linaria reflexa extract and to establish the relationship between its bioactivity and chemical composition. Twenty-three secondary metabolites were identified, most of them are good anti-inflammatory agents, in line with data by carrageenin-induced rat paw edema assays of the n-butanol extract showing high anti-inflammatory inhibition (63.90%) of edema swelling in the rat paw at the dose 200 mg/kg after 4 h. Furthermore, both extent of inflammatory response and tissue injury were prevented keeping the levels of rate myeloperoxidase (60.16%) and of malondialdehyde, which is the final product of lipid peroxidation generated by free radicals (58.58%). The same extract showed also a remarkable hemostatic effect established by measuring the coagulation time of decalcified plasma (45 s), related to its flavonoid glycosides content.

The study was performed on the dichloromethane (DCM), ethyl acetate (EAc) and n-butanol (Bu) fractions (F) obtained from the 80% ethanol extract of Linaria scariosa Desf. aerial parts, collected in the North Eastern region of Algeria. Remarkable total phenolic and flavonoid contents were obtained, mainly for EAcF. These results were in accordance with the antioxidant activity of EAcF against DPPH, ABTS, CUPRAC and reducing power tests. DCMF and BuF exhibited significant cholinesterase activity inhibition of BChE and AChE. Moreover, EAcF displayed only moderate antibacterial activities, especially against S. aureus. The biological results were correlated to the chemical components, deduced by both GC-MS analysis of the fractions and the isolation of hemipholin, pectolinarigenin, antirride, antirrinoside, pectolinarin and linariosise, some of which known to exhibit potent effects on the tested biological activities. The study provides the first biological and chemical investigation on Linaria scariosa Desf (unresolved name)

The phytochemical investigation of both chloroform and ethyl acetate extracts of Centaurea microcarpa Coss. & Dur. led to the isolation of a new cyanogenic glucoside 6’-methacrylate prunasin (3) together with seven known compounds: hydroxy-11b, 13-dihydro onopordaldehyde (1), b-sitosterol (2), daucosterol (4), nepetin (5), prunasin (6), astragalin (7) and 7-O-b-D-glucopyranosyl centaureidin (8). Their structures were established by spectral analysis, mainly UV, IR, ESI-MS, 1D & 2D-NMR experiments (COSY, HSQC, HMBC and ROESY)

The study was performed to assess the antioxidant properties of the n-butanol extract of the Algerian endemic specie Linaria tingitana Boiss. and Reut., using different tests (DPPH• radical, β-carotene-linoleic acid, ferric-reducing power and ferrous-chelating ability). The phytochemical investigation was based on total phenolic and flavonoids contents together with the HPLC analysis which led us to identify twelve constituents (gallic acid 1, chlorogenic acid 2, hydroxycafeic acid 3, caffeic acid 4, vanillic acid 5, syringic acid 6, rutin 7, luteolin 8, ferulic acid 9, coumaric acid 10, quercetin 11 and chrysin 12). Results showed that the n-BuOH extract exhibited an antioxidant activity as reflected by the DPPH• scavenging effect, ferric reducing power, and ferrous-chelating ability,(IC50: 122.26, 19.39 and 113.13 µg/mL, respectively) and β-carotene inhibition (59.358%). In addition, the quantity of the compounds (total phenolic and flavonoids contents) confirmed the obtained data. These results indicate that L. tingitana can be used as functional products

The aim of this study is the phytochemical and biological investigations of the endemic species Linaria tingitana Boiss. & Reut. (Plantaginaceae). The anti-arthritic activity of n-butanol extract of Linaria tingitana (BELT) showed that it exhibited a concentration dependent stabilisation of HRBC membrane, inhibition of protein denaturation and nitric oxide scavenging effect in the in vitro process; this might be believed to be influenced by the synergistic action of the above isolated compounds. The analysis of the BELT by High performance liquid chromatography equipped with diode array detection and electrospray ionozation mass spectrometry (HPLCDAD–ESI/MS) allowed the identification of four iridoids structurally confirmed by NMR and ESI–MS/MS extensive experiments data. The present study suggests that BELT would serve as a source for the discovery of novel anti-inflammatory agents