POTENTIAL ROLE OF MILK THISTLE SEED AND ITS OIL EXTRACTS AGAINST HEART AND BRAIN INJURIES INDUCED BY γ-RADIATION EXPOSURE

Objective: This study aimed to investigate the protective effect of Silybum marianum (S. marianum) seeds extract its oil fraction against damage effect of γ-radiation in female albino rats.Methods: Ultrasonic-assisted extraction was used for the extraction of S. marianum seeds. Lipid patterns of S. marianum seeds oil were elucidated using gas chromatography-mass spectrometry (GC-MS). S. marianum seeds extract was analyzed using high-performance liquid chromatography (HPLC). Malondialdehyde (MDA), reduced glutathione (GSH) and metallothionein (MT) were estimated in heart and brain tissues of the examined rats. Lactate dehydrogenase (LDH) and creatine kinase-MB (CKMB) were measured in the serum of the examined rats, and the brain biomarkers; dopamine and serotonin were also measured.Results: The oil was found to be rich in linoleic acid (58.20%) and arachidic acid (23.38%). S. marianum seeds extract revealed the presence of taxifolin and six main active constituents of silymarin, including silydianin, silychristin, silybin A, silybin B, isosilybin A and isosilybin B. Treatment of γ-radiation damage effect using S. marianum seeds extract and its oil fraction led to a significant reduction of MDA levels in heart (139.6 and 165.5 nmol/g, respectively) and brain (158.5 and 135.2 nmol/g, respectively) tissues, however, significant increase of GSH levels in heart (316.4 and 293 mg/g, respectively) and brain (210.4 and 227 mg/g, respectively) tissues was observed, also a significant increase of dopamine levels (85.27 and 65.74 ng/g, respectively) and MT levels of heart tissues (108.5 and 70.52 mg/g, respectively) was observed.Conclusion: S. marianum seeds extract and its oil fraction showed a protective effect against γ-radiation-induced damage in heart and brain.Â

Chemical Investigation of Some Capparis Species Growing in Egypt and their Antioxidant Activity

Capparis cartilaginea and C. deserti growing in Egypt were investigated for their glucosiolates and rutin content. From Capparis cartilaginea four isothiocynates were isolated and identified using GC and EI/MS techniques. These compounds were butyl isothiocyanate (1), 6-methylsulphonylhexyl isothiocyanate (2), 7-methylsulphonylheptyl isothiocyanate (3) and 5-benzylsulphonyl-4-pentenyl isothiocyanate (4). In addition to compounds (1) and (2), two other compounds were isolated and identified from Capparis deserti. These compounds are 3-methylthiopropyl isothiocyanate (5) and [11-(2-butenylthio)6-undecenyl isothiocyanate] (6). Compounds (1), (2), (5) and (6) are reported in this study for the first time from Capparis deserti. The main flavonoid component in the studied species was isolated and identified as rutin by comparing the data with those reported. Also, quantitative evaluation of rutin in the two species was carried out by TLC-densitometric analysis. The antioxidant activity was done using diphenylpicrylhydrazyl (DPPH) radical scavenging method. The butanol fraction from C. cartilaginea and C. deserti showed the highest antioxidant properties

COMPARATIVE ANALYSIS OF BIOLOGICAL ACTIVITY OF SILYBUM MARIANUM L. FOOD SUPPLEMENTS AVAILABLE ON MARKET: INVITRO STUDY

Objective: Silybum marianum L. Food Supplements that contain silymarin is widely used as a therapeutic agent in liver diseases. Many brands are available on the market in USA, Egypt, Europe and other countries. The objective of this study was to compare the biological activity in different preparations of silymarin available on the market in USA and Egypt using paracetamol-induced oxidative stress injury on primary cultured rat hepatocytes. Methods: Forty four silymarin samples available on the market were collected from USA (24) and Egypt (20) and tested for hepat protective antioxidant effects on primary cultured rat hepatocytes. Cytotoxicity was measured by MTT [3-(4, 5-dimethyl-thiazol-2)-2,5-diphenyl tetrazolium bromide] assay and lactate dehydrogenase (LD) leakage into culture medium. Antioxidant effects were determined by glutathione reductase (GR), and Nitric oxide (NO) assays in silymarin, pretreated rat hepatocytes for 2 h followed by incubation with 25 mM paracetamol over a period of 1 h. Therapeutic index was calculated for each tested sample for comparative analysis. Results: Silymarin preparations significantly decreased toxicity induced by paracetamol in rat hepatocytes, decreased lactate dehydrogenase leakage and prevented GSH depletion (P<0.01) and returned NO to basal levels in rat hepatocytes. The therapeutic index was 80, 40 and 20 for samples No. 20, 19 and 5 respectively. Conclusions: The 44 different silymarin preparations tested in this study exhibited variation in antioxidant capacity and in reducing nitric oxide produced as a result of paracetamol injury. This variation in biological activity did not always correspond to the amount of silymarin recorded on samples

Targeting multidrug resistance in cancer by natural chemosensitizers

Abstract Background Statistics on cancer incidence and mortalities indicate that this disease still has a fatal outcome for a majority of patients due to non-sufficient treatment. The options available for cancer treatment include chemotherapy, which still commands a leading position in clinical oncology. A major obstacle to successful chemotherapy is the development of cellular resistance to multiple structurally unrelated anticancer drugs. This phenomenon has been termed multidrug resistance (MDR), which occurs in a majority of cancer patients. MDR is mainly due to the overexpression of ABC transporters which extrude chemotherapeutic drugs outside of cancer cells. A plethora of synthetic chemosensitizers have been described during the past decades that block ABC transporter function to reverse their MDR. However, none of them reached clinical routine application as of yet. In this review, we highlight the potential of natural products derived from plants, marine organisms, fungi, and other sources as chemosensitizers to the targeted major ABC transporters (ABCB1, ABCC1, and ABCG2). Conclusion Natural compounds may serve as lead compounds for the development of novel ABC transporter inhibitors with improved pharmacological features that can be used as adjuvant therapy to enhance the efficacy of chemotherapeutic drugs against MDR

INVESTIGATION OF THE LIPID AND CARBOHYDRATE CONTENTS OF GREWIA TENAX FORSSK. FRUITS & EVALUATION OF HEPATOPROTECTION ACTIVITY

Objective: Grewia tenax Forssk. is represented in Egypt and known for its edible fruits which are nutritionally balanced and rich in iron and calcium. This work was to investigate the Lipid and Carbohydrate Contents of Grewia tenax Forssk. fruits and evaluation of Hepatoprotection activity.Methods: Investigation of carbohydrate contents of Grewia tenax Forssk. fruits were carried out using HPLC. The lipids content of Grewia tenax Forssk. fruits were analyzed by GLC. Also, the hepatoprotective activity on rat hepatocytes monolayer culture was studied.Results: The HPLC analysis of free sugars of Grewia tenax Forssk. fruits revealed the presence of stachyose, sucrose, glucose and fructose. While the HPLC analysis of the polysaccharide hydrolysate from Grewia tenax Forssk. fruits showed the presence of glucuronic acid, glucose, galactose and arabinose.GLC of the unsaponifiable matter of hexane extract of Grewia tenax Forssk. fruits revealed the presence of a mixture of a series of n-alkanes (63%) and a series of sterols (9.9%). A series of hydrocarbons ranging from C10-C26 in addition to cholesterol, campasterol, stigmasterol and β-Sitosterol and six fatty acids among which Linoleic acid (C18:2) was the major one (55.5 %) was identified. Also, the hepatoprotective activity study of the extracts of Grewia tenax Forssk. fruits (80% MeOH extract of defatted powder) and water extract indicated that they exhibited hepatoprotection at (25 μg/ml and 50 μg/ml) and (12.5 μg/ml to 100 μg/ml); respectively.Conclusion: Our study was the first record of carbohydrate and lipid fraction contents of Grewia tenax Forssk. fruits. From the obtained results, the highly nutritive and medicinal values of Grewia tenax Forssk. fruits should be considered. Furthermore, and due to the high hepatoprotection effects of the plant extracts, further investigation and studies should be done to isolate the bioactive compounds. Â

Lipophilic Constituents of Rumex vesicarius L. and Rumex dentatus L.

Rumex dentatus L. and Rumex vesicarius L., of the family Polygonaceae, are edible herbs growing wild in Egypt. Their lipoid constituents were examined by both liquid chromatography/mass spectrometry (LC/MS) and by gas chromatography/mass spectrometry (GC/MS). Their essential oil compositions consisted mainly of thujene, limonene, fenchon, estragole, and anethole but at largely different concentration. Fatty acid compositions were similar among the two species and consisting of palmitic, oleic, linoleic and linolenic acids, with R. vesicarius containing much higher level of omega-3-fatty acids. Both of the crude lipid extracts of the two species showed strong antioxidant activity as a radical quenching agent against 2,2-diphenyl-1-picrylhydrazyl (DPPH) systems. Antioxidant activities were mostly associated with the polar lipid fractions. High performance thin layer chromatography (HPTLC), both in the normal and reversed phase,as well as liquid chromatography/mass spectrometry (LC/MS) in the positive and negative electrospray ionization (ESI), showed unique chemical profile for each species that can be useful for species identification and quality control of herbal drug formulations. R. vesicarius was characterized by abundances of flavonoids and R. dentatus was abundant in anthraquinones and chromones

Euphosantianane A–D: Antiproliferative Premyrsinane Diterpenoids from the Endemic Egyptian Plant Euphorbia Sanctae-Catharinae

Euphorbia species are rich in diterpenes. A solvent extraction of Euphorbia sanctae-catharinae, a species indigenous to the Southern Sinai of Egypt, afforded several premyrsinane diterpenoids (1–4) as well as previously reported metabolites (5–13) that included three flavonoids. Isolated compounds were chemically characterized by spectroscopic analysis. Identified compounds were bioassayed for anti-proliferative activity in vitro against colon (Caco-2) and lung (A549) tumor cell lines. Compound 9 exhibited robust anti-proliferative activity against A549 cells (IC50 = 3.3 µM). Absolute configurations for 8 versus 9 were determined by experimental and TDDFT-calculated electronic circular dichorism (ECD) spectra