Browsing by Author "Ezzat, Shahira M"

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Acovenoside A as a novel therapeutic approach to boost taxol and carboplatin apoptotic and antiproliferative activities in NSCLC: Interplay of miR-630/miR- 181a and apoptosis genes
(Academic Press Inc., 2023-07) Aborehab, Nora M; Abd-Elmawla, Mai A; ElSayed, Abeer M; Sabry, Omar; Ezzat, Shahira M; Abd-Elmawla, Mai A; ElSayed, Abeer M; Sabry, Omar
The aim of the present study is to explore the potential anticancer effect of the cardenolide; 2 acovenoside A against non-small cell lung cancer, understand its molecular mechanism in inducing 3 apoptosis and show the effect of its combination with carboplatin and taxol. MTT assay showed that the 4 combination of acovenoside A with taxol and carboplatin caused 78.9% cytotoxicity reflecting the 5 synergistic effect. The triple combination showed the best growth inhibition efficiency where the 6 number of cells at the G2/M phase was decreased and boosted up apoptotic and necrotic activity. The 7 combination also showed the most remarkable increase in gene expression of Bax and p53 and the least 8 level of Bcl2. The gene expression of miRNA181a and miRNA630 was significantly upregulated in cell 9 lines treated with the combination. The present study has proven that the underlying mechanism of 10 acovenoside A is partially attributed to the upregulation of miR-630 and miR-181a gene expressions 11 which in turn targets the intrinsic apoptosis genes as p53, Bax and Bcl2 as well as caspase 3. The present 12 study is the first to address the valuable effect of using acovenoside A together with carboplatin and 13 taxol in the treatment of NSCLC via exerting apoptotic, antiproliferative, and cytotoxic ef
Acovenoside A Induces Mitotic Catastrophe Followed by Apoptosis in Non-Small-Cell Lung Cancer Cells
(American Chemical Society, 2017) El Gaafary M.; Ezzat, Shahira M; El Sayed A.M.; Sabry O.M.; Hafner S.; Lang S.; Schmiech M.; Syrovets T.; Simmet T.; Department of Pharmacognosy; College of Pharmacy; Cairo University; Giza; 11562; Egypt; Pharmacognosy Department; Faculty of Pharmacy; October University for Modern Sciences and Arts (MSA); Cairo; 11562; Egypt; Institute of Pharmacology of Natural Products and Clinical Pharmacology; Ulm University; Ulm; D-89081; Germany
We investigated the cytotoxic potential of the cardenolide glycoside acovenoside A against non-small-cell lung cancer cells. Lung cancer is the leading cause of cancer-related mortality and the second most common cancer diagnosed. Epidemiological studies revealed a direct correlation between the regular administration of cardiac glycosides and a lower incidence of various cancers. Acovenoside A, isolated from the pericarps of Acokanthera oppositifolia, potently inhibited proliferation and induced cytotoxicity in A549 non-small-cell lung cancer cells with an IC 50 of 68 � 3 nM after 48 h of exposure. Compared to the antineoplastic agent doxorubicin, acovenoside A was more potent in inhibiting the viability of A549 cancer cells. Moreover, acovenoside A exhibited selectivity against cancer cells, being significantly less toxic to lung fibroblasts and nontoxic for peripheral blood mononuclear cells. Analysis of the cell cycle profile in acovenoside A-treated A549 cells revealed mitotic arrest, due to accumulation of the G 2 /M regulators cyclin B 1 and CDK1, and cytokinesis failure. Furthermore, acovenoside A affected the mitochondrial membrane integrity and induced production of radical oxygen species, which resulted in induction of canonical apoptosis, manifested by caspase 3 activation and DNA fragmentation. Based on our results, acovenoside A warrants further exploration as a potential anticancer lead. � 2017 The American Chemical Society and American Society of Pharmacognosy.
Aloe Species as Valuable Sources of Functional Bioactives
(Springer, 2020-06) Egbuna, Chukwuebuka; Gupta, Ena; Ezzat, Shahira M; Jeevanandam, Jaison; Mishra, Neha; Akram, Muhammad; Sudharani, N.; Adetunji, Charles Oluwaseun; Singh, Priyanka; Ifemeje, Jonathan Chinenye; Deepak, M; Walag, Angelo Mark; Ansari, Rumaisa; Adetunji, Juliana Bunmi; Laila, Umme; Olisah, Michael Chinedu; Onyekere, Peculiar Feenna
Herbal medicines occupy distinct position right from the primitive period to present day. In every ethnic group, there exists a traditional health care system, which is culturally patterned. In rural communities, health care seems to be the first and fore- most line of defence. The WHO has already recognized the contribution of tradi- tional health care in tribal communities. These medicines have fewer side effects and are easily accessible to mankind in the nature. It has been a source of medicinal
Angiotensin-converting enzyme and renin inhibition activities, antioxidant properties, phenolic and flavonoid contents of Cuphea ignea A. DC
(Wolters Kluwer Medknow Publications, 2020-06) Ismail, W.M; Ezzat, Shahira M; Michel, H; El Deeb, K; El-Fishawy, A
Cuphea ignea A. DC. is an ornamental plant belonging to family Lythraceae distributed in the tropics and temperate zones. Some Cuphea members are traditionally used in treatment of hypertension. The aim of this research was to study the antihypertensive activity of the plant by applying a bio-guided fractionation scheme of the leaves, stems, and flowers using in vitro angiotensin-converting enzyme (ACE) and renin inhibition assays to identify the active organ and its respective active fractions. The aqueous extract and the n-butanol fraction of the leaves showed the highest ACE inhibition activity with IC50values 0.491 and 0.084 mg/mL, respectively. The renin inhibition activity showed that the alcoholic extract of the leaves had the highest percentage of inhibition (94.82%). Meanwhile, the methylene chloride fraction of the stems showed the highest renin inhibition activity (98.14%) followed by the ethyl acetate fraction of the leaves (93.09%). The antioxidant activity was tested using the 2,2-diphenyl-1-picrylhydrazyl and oxygen radical absorbance activity assays. Correlation studies of the antioxidant activity showed moderate correlation with the phenolic content and strong correlation with the flavonoid content. The renin inhibition activity showed significant positive correlation with the phenolic and flavonoid contents with r values (0.777 and 0.629, respectively). © 2020 Wolters Kluwer Medknow Publications. All rights reserved
Anti-acetylcholinesterase activity of essential oils and their major constituents from four Ocimum species
(De Gruyter, 2016) A Farag, Mohamed; Ezzat, Shahira M; M Salama, Maha; Tadros, G; AT Serya, Rabah
Ocimum is a genus of considerable importance in traditional medicine worldwide. The goal of this study was to examine the anti-acetylcholinesterase activity of Ocimum essential oils and to correlate the activity with their chemical profiles using a metabolome based GC-MS approach coupled to chemometrics. Further, molecular docking was adopted to rationalize the activity of some essential oil isolates. Essential oil prepared from the four species O. basilicum, O. africanum, O. americanum, and O. minimum exhibited significant anti-acetylcholinesterase activity with (IC50 0.22, 0.175, 0.57 and 0.152 mg/mL, respectively) comparable to that of physostigmine (IC50 0.27 mg/mL). The phenylpropanoids (i.e. estragole) constituted the most dominant chemical group in O. basilicum (sweet basil) and O. minimum, whereas camphor (a ketone) was the most abundant in O. africanum and O. americanum. Supervised and unsupervised multivariate data analyses clearly separated O. africanum and O. americanum from other accessions, with estragole, camphor and, to less extent, β-linalool contributing to species segregation. Estragole was found the most active AchE inhibitor (IC50 0.337 µM) followed by cineole (IC50 2.27 µM), camphor (IC50 21.43 µM) and eugenol (IC50 40.32 µM). Molecular docking revealed that these compounds bind to key amino acids in the catalytic domain of AchE, similar to standard drugs
Anti-acetylcholinesterase potential and metabolome classification of 4 Ocimum species as determined via UPLC/qTOF/MS and chemometric tools
(Elsevier, 2016) Ezzat, Shahira M; Farag, MA; Salama, MM; Tadros, MG
Ocimum (sweet basil) is a plant of considerable commercial importance in traditional medicine worldwide as well as for the flavor and food industry. The goal of this study was to examine Ocimum extracts anti-acetylcholinesterase activity and to correlate the activity with their secondary metabolites profiles via a metabolome based ultraperformance liquid chromatography-mass spectrometry (UPLC–MS) approach coupled to chemometrics. The metabolomic differences in phenolics from leaves derived from 4 Ocimum species: Ocimum basilicum, Ocimum africanum, Ocimum americanum and Ocimum minimum were assessed. Under optimized conditions, 81 metabolites were identified including 21 hydroxy cinnamic acids, 4 benzoic acid conjugates, 14C/O flavonoid conjugates, 2 alcohols, 5 acyl sugars, 4 triterpenes and 12 fatty acids. Several salviolanic acid derivatives including salviolanic acid A, B, C & I found in Salvia, were found in Ocimum herein for the first time. Unsupervised principal component analysis (PCA) and supervised orthogonal projection to latent structures-discriminant analysis (OPLS-DA) were further used for comparing and classification of samples. A clear separation among the four investigated Ocimum species was revealed, with O. africanum samples found most enriched in hydroxy cinnamates conjugates (HC) and flavonoids. To the best of our knowledge, this is the first report for compositional differences among Ocimum leaves via a metabolomic approach revealing that among examined species O. africanum leaves present a better source of Ocimum bioactive metabolites. The anticholinesrase activity of examined species was further assessed with a potent IC50 values for O. americanum, O. africanum, O. basilicum ranging from 2.5 to 6.6 mg/ml, whereas O. minimum was least active with IC50 of 31.4 mg/ml. Furthermore, major HC i.e., caftaric, chlorogenic and rosmarinic acids identified in extracts via UPLC–MS analysis exhibited IC50 values of 24, 0.5 and 7.9 mg/ml respectively, suggesting that HCs are likely to mediate for the anticholinesterase effect in Ocimum extracts.
Anti‑estrogenic and anti‑aromatase activities of citrus peels major compounds in breast cancer
(Nature, 2021-03) El‑Kersh, Dina M; Ezzat, Shahira M; Salama, Maha M; Mahrous, Engy A; Attia, Yasmeen M; Ahmed, Mahmoud Salama; Elmazar, Mohey M
Estrogen signaling is crucial for breast cancer initiation and progression. Endocrine-based therapies comprising estrogen receptor (ER) modulators and aromatase inhibitors remain the mainstay of treatment. This study aimed at investigating the antitumor potential of the most potent compounds in citrus peels on breast cancer by exploring their anti-estrogenic and anti-aromatase activities. The ethanolic extract of diferent varieties of citrus peels along with eight isolated favonoids were screened against estrogen-dependent breast cancer cell lines besides normal cells for evaluating their safety profle. Naringenin, naringin and quercetin demonstrated the lowest IC50s and were therefore selected for further assays. In silico molecular modeling against ER and aromatase was performed for the three compounds. In vivo estrogenic and anti-estrogenic assays confrmed an anti-estrogenic activity for the isolates. Moreover, naringenin, naringin and quercetin demonstrated in vitro inhibitory potential against aromatase enzyme along with anticancer potential in vivo, as evidenced by decreased tumor volumes. Reduction in aromatase levels in solid tumors was also observed in treated groups. Overall, this study suggests an antitumor potential for naringenin, naringin and quercetin isolated from citrus peels in breast cancer via possible modulation of estrogen signaling and aromatase inhibition suggesting their use in pre- and post-menopausal breast cancer patients, respectively.
Anti-inflammatory activity of the lipophilic metabolites from Scolymus hispanicus L
(ELSEVIER, 2020) A Kandil, Zeinab; Esmat, Ahmed; Salah El-Din, Reham; Ezzat, Shahira M
The golden thistle, Scolymus hispanicus L. (Asteraceae), is a prickly perennial herb that is widely grown in Mediterranean and in Southeastern Europe. The aim of current study was to isolate and identify the constituents of S. hispanicus L. chloroform fraction, and assess their anti-inflammatory activity in-vitro. Chemical investigation led to isolation of one new guaianolide sesquiterpene; namely iso-japonicolactone (4), three tritepenes namely lupeol acetate (1), lupeol (2), and oleanolic acid (5), and the sterol stigmasterol (3). The isolated compounds demonstrated free radical scavenging activity against DPPH with compound 4 being able to scavenge more than 90% of DPPH radical at 100 µM. Treatment of the peripheral blood mononuclear cells (PBMC) stimulated with phytohaemagglutinin (PHA) with the isolated compounds resulted in a decrease in nuclear factor kappa (NFκB) p65 content in a dose-dependent manner. Compound 4 was the most efficient in decreasing NFκB p65 at the lowest concentration (1 µM), followed by compound 5. In addition, cell treatment with isolated compounds resulted in dose-related reduction of interleukins (IL-6 and IL-1β), and tumor necrosis factor (TNF-α). To the best of our knowledge this is the first report for the isolation of iso-japonicolactone and the detailed study of its anti-inflammatory activity. The potent anti-inflammatory compounds in this study could be considered as a nucleus for developing anti-inflammatory drugs through further biological studies on the molecular level.
Anti-Obesity Effect of a Tea Mixture Nano-Formulation on Rats Occurs via the Upregulation of AMP-Activated Protein Kinase/Sirtuin-1/Glucose Transporter Type 4 and Peroxisome Proliferator-Activated Receptor Gamma Pathways
(Multidisciplinary Digital Publishing Institute (MDPI), 2023-07) Salem, Mohamed A.; Aborehab, Nora M.; Abdelhafez, Mai M.; Ismail, Sameh H.; Maurice, Nadine W.; Azzam, May A.; Alseekh, Saleh; Fernie, Alisdair R.; Salama, Maha M.; Ezzat, Shahira M
White, green, and oolong teas are produced from the tea plant (Camellia sinensis (L.) Kuntze) and are reported to have anti-obesity and hypolipidemic effects. The current study aims to investigate the anti-obesity effects of a tea mixture nano-formulation by targeting the AMPK/Sirt-1/GLUT-4 axis in rats. In vitro lipase and α-amylase inhibition assays were used to determine the active sample, which was then incorporated into a nanoparticle formulation subjected to in vivo anti-obesity testing in rats by measuring the expression level of different genes implicated in adipogenesis and inflammation using qRT-PCR. Moreover, metabolomic analysis was performed for each tea extract using LC/ESI MS/MS coupled to chemometrics in an attempt to find a correlation between the constituents of the extracts and their biological activity. The in vitro pancreatic lipase and α-amylase inhibition assays demonstrated more effective activity in the tea mixture than the standards, orlistat and acarbose, respectively, and each tea alone. Thus, the herbal tea mixture and its nanoparticle formulation were evaluated for their in vivo anti-obesity activity. Intriguingly, the tea mixture significantly decreased the serum levels of glucose and triglycerides and increased the mRNA expression of GLUT-4, P-AMPK, Sirt-1, and PPAR-γ, which induce lipolysis while also decreasing the mRNA expression of TNF-α and ADD1/SREBP-1c, thereby inhibiting the inflammation associated with obesity. Our study suggests that the tea mixture nano-formulation is a promising therapeutic agent in the treatment of obesity and may also be beneficial in other metabolic disorders by targeting the AMPK/Sirt-1/Glut-4 pathway.
ANTI-WRINKLE ACTIVITY AND UPLC-MS/MS METABOLIC PROFILING OF POMEGRANATE AND GRAPE SEEDS EXTRACTS
(INT JOURNAL PHARMACEUTICAL SCIENCES, 08/01/2020) Odah, Sally M.; Salama, Maha M.; Aziz, Wafaa M.; El-Alfy, Taha S.; Ezzat, Shahira M
UV irradiation is one of the main causes of what is known as photoaging characterized by loss of skin elasticity and the appearance of wrinkles. In this study, the anti-wrinkle activity of grape seed extract (GSE) and Pomegranate seed extract (PSE) was studied through evaluation of their in-vitro antioxidant, anti-tvrosinase and in-vivo anti-wrinkle activity in UVB-irradiated mice through topical application of PSE and GSE at 50 mg/kg/twice a week for 15 weeks. The total phenolic content of PSE and GSE was 2.1375 and 5.9625 mg GAE/g extract, respectively. PSE and GSE also showed DPPH scavenging activity with IC50 of 37.9 and 29.9 mu g/mL, respectively. PSE and GSE showed anti-tyrosinase activity with IC50 of 115 and 107.75 mu g /mL, respectively, while that of Kojic acid is 17.45 mu g /mL. In UVB-irradiated mice, the increased expression of metaloproteinase (MMP-2) was significantly inhibited by PSE and GSE where their activities exceeded that of the standard turmeric extract (TME). The topical application of PSE, GSE, and TME of the UVB radiated groups prevented the increase in the thickness of the epidermis induced by UVB. UPLC-MS/MS profiling of both extracts led to the identification of 43 phenolic compounds of different classes. We can conclude that the anti-wrinkle activity of both extracts was attributed to their high phenolic content and the antioxidant potential of both extracts. Therefore, the seeds of pomegranate and grapes, which are considered as waste products, could be incorporated in cosmeceutical skincare products after further clinical trials
ANTIBACTERIAL ACTIVITY OF THE ETHANOLIC EXTRACTS OF ALLIUM SATIVUM L. BULBS AND ZINGIBER OFFICINALE ROSCOE RHIZOMES AS IRRIGATING SOLUTIONS
(World Journal of Pharmacy and Pharmaceutical Sciences, 2014) A. Alrazhi, Basma; H. Diab, Alaa; A. Essa, Somaia; M. Ahmed, Geraldine; Ezzat, Shahira M
Irrigation of the root canals with antibacterial solutions is a mandatory step to reduce or eliminate micro-organisms. The aim of this study was to evaluate the efficacy of garlic and ginger as irrigating solutions. The ethanolic extracts of garlic bulbs, ginger rhizomes and 2% solution of CHX were prepared. Forty single rooted teeth canal were divided into 3 groups according to the irrigant used, in addition to the positive control group where the roots were irrigated with sterile distilled water and a negative control group in which the roots were uninfected with E. faecalis. The teeth were filled with 30 μl of E. faecalis suspension and incubated for 1 week at 37ºC. They were prepared mechanically using protaper rotary files both shaper and finisher, each root was irrigated successively with 1 ml of the tested irrigant after each file and then 3 ml as a final flush. After chemo- mechanical preparation, samples were evaluated for antibacterial evaluation using brain heart infusion agar method. The components of the ethanolic extracts of garlic bulbs and ginger rhizomes were identified using LC/ESI-MS analysis. The highest antibacterial activity was observed in ginger extract followed by 2% CHX solution, and garlic extract. Zingerone, gingerol and [6]-shogaol were the major components determined in ginger extract using LC/ESI-MS, while garlic extract was rich in di-2-propenyldisulfide, methyl-2-propenyl trisulfide, 3-vinyl-1,2-dithiocyclohex-4-ene and di-2-propenyltrisulfide. The ethanolic extracts of both garlic bulbs and ginger rhizomes can be used as endodontic irrigants during the root canal treatment for their antimicrobial effects.
Antibacterial, antioxidant, and topical antiinflammatory activities of Bergia ammannioides: A wound-healing plant
(Informa Healthcare, 2015) Ezzat, Shahira M; A. Choucry, Mouchira; A. Kandil, Zeinab
Context: Despite the traditional use of Bergia ammannioides Henye ex Roth. (Elatinaceae) for the treatment of wounds in India, there is a scarcity of scientific data supporting this use. Objective: The objective of this study is to assess wound-healing potentiality of the plant, to study pharmacological activities that may contribute in eliminating wound complications, and to investigate the biologically active fractions. Material and methods: The ethanolic extract (EtOH) of the aerial parts was fractionated to obtain n-hexane (HxFr), chloroform (ClFr), ethyl acetate (EtFr), and n-butanol (BuOH) fractions. EtOH and its fractions were formulated in strength of 5 and 10% w/w ointment and tested for wound-healing activity using the excision model. The topical anti-inflammatory, in vitro antioxidant, and antibacterial activities were evaluated. HxFr and EtFr were chemically investigated to isolate their constituents. Results: Application of EtOH, HxFr, and EtFr (10% w/w ointments) leads to 71.77, 85.62, and 81.29% healing of the wounds with an increase in the collagen content. HxFr had the strongest anti-inflammatory (64.5% potency relative to Voltaren) and antibacterial activity (MIC ¼ 104 mg/ml against Staphylococcus aureus), while EtFr showed the strongest antioxidant activity against DPPH, ABTS+ , and super oxide radical with an IC50 value of 10.25 ± 0.01, 66.09 ± 0.76, and 167.33 ± 0.91 mg/ml, respectively. b-Sitosterol, lupeol, cyclolaudenol, and cycloartenol were isolated from HxFr. Quercetin, ellagic acid, kaempferol-3-O-a-L-rhamnoside, and quercetin-3-O-a-L-rhamnoside were isolated from EtFr. Discussion and conclusion: Our study presents scientific evidence for the efficacy of B. ammannioides in enhancing wound healing, and the first isolation of cyclolaudenol and cycloartenol from Bergia
Anticancer potentiality of lignan rich fraction of six Flaxseed cultivars
(Nature Publishing Group, 2018) Ezzat, Shahira M; Shouman S.A.; Elkhoely A.; Attia Y.M.; Elsesy M.S.; El Senousy A.S.; Choucry M.A.; El Gayed S.H.; El Sayed A.A.; Sattar E.A.; El Tanbouly N.; Pharmacognosy Department; Faculty of Pharmacy; Cairo University; Kasr El-Einy Street; Cairo; 11562; Egypt; Department of Pharmacognosy; Faculty of Pharmacy; October University for Modern Science and Arts (MSA); 6th October; 12566; Egypt; Cancer Biology Department; National Cancer Institute; Cairo University; Cairo; Egypt; Pharmacology and Toxicology Department; Faculty of Pharmacy; Helwan University; Helwan; Egypt
The objective of our study is to highlight the therapeutic effect and mechanism of action by which purified Flaxseed hydrolysate (PFH) which is a lignan rich fraction exerts its anticancer activity on a human breast cancer cell line (T47D) and in mice bearing tumor. HPLC analysis of PFH of six flaxseed cultivars had shown that PFH of the cultivar Giza 9 (PFH-G9) contains the highest concentration of SDG (81.64 mg/g). The in vitro cytotoxic potentiality of PFH's of six flaxseed cultivars was screened against a panel of human cancer cell lines. PFH -G9 showed the most significant cytotoxic activity against ER-receptor positive breast cell lines MCF7 and T47D with IC50 13.8 and 15.8 ?g/ml, respectively. Moreover, PFH-G9 reduced the expression of the metastasis marker, 1-?, metalloproteinases and vascular endothelial growth factor (VEGF), one of the most potent stimulators of angiogenesis, while it increased the caspase-3 dependent apoptosis. Our study also showed that dietary intake of 10% of Giza 9 Flaxseeds (FS), fixed oil (FSO) or Flax meal (FSM) twice daily for 3 weeks in mice-bearing solid Ehrlich ascites carcinoma (EAC) resulted in reducing the tumor volume, the expression of estrogen, insulin growth factor, progesterone, VEGF and MMP-2, but enhanced expression of caspase-3. � 2018 The Author(s).
Antidepressant-Like Effect of Selected Egyptian Cultivars of Flaxseed Oil on a Rodent Model of Postpartum Depression
(Hindawi Limited, 2017) El Tanbouly N.; El Sayed A.M.; Ali Z.Y.; Abdel Wahab S.; El Gayed S.H.; Ezzat, Shahira M; El Senousy A.S.; Choucry M.A.; Abdel-Sattar E.; Department of Pharmacognosy; College of Pharmacy; Cairo University; Cairo; 11562; Egypt; Department of Biochemistry; National Organization for Drug Control and Research; Giza; 12553; Egypt; Department of Pharmacognosy; College of Pharmacy; October University for Modern Sciences and Arts; 6th of October12566; Egypt
Flaxseed (Linum usitatissimum L.) is a multipurpose crop with health promoting potential. This study was undertaken to investigate the fatty acid profile and yield of fixed oil of six Egyptian flaxseed cultivars. The selected cultivars with the highest content of polyunsaturated fatty acids (PUFAs) (G9 and G10) were assessed for their antidepressant-like effect in rat model of postpartum depression (PPD) induced by hormone-simulated pregnancy followed by hormone withdrawal and compared to fluoxetine. As compared to control group, administration of G9 and G10 (270 mg/kg/day, p.o) for two weeks during the postpartum period can alleviate anxiety and depressive-like behaviors and biochemical changes in PPD-induced rats. This was confirmed by evaluation of anxiety-like behaviors (elevated plus maze, open field test, and forced swim test tests), in addition to biochemical analysis (brain monoamine oxidase-A, corticosterone level, proinflammatory cytokines, and hippocampal redox state). In conclusion, flaxseed oil of Egyptian cultivars G9 and G10 exhibited significant antidepressant-like effect in rat model of PPD without affecting locomotor activity. At the treatment doses, the antidepressant-like activity of Giza 9 oil is comparable to fluoxetine. � 2017 Nebal El Tanbouly et al.
Antifibrotic effects of gallic acid on hepatic stellate cells: In vitro and in vivo mechanistic study
(National Taiwan University, 2019) El-Lakkany N.M.; El-Maadawy W.H.; Seif el-Din S.H.; Saleh S.; Safar M.M.; Ezzat, Shahira M; Mohamed S.H.; Botros S.S.; Demerdash Z.; Hammam O.A.; Department of Pharmacology; Theodor Bilharz Research Institute; Warak El-Hadar; Imbaba P.O. Box 30; Giza; 12411; Egypt; Department of Pharmacology and Toxicology; Faculty of Pharmacy; Cairo University; Cairo; 11562; Egypt; Department of Pharmacognosy; Faculty of Pharmacy; Cairo University; Cairo; 11562; Egypt; Department of Immunology; Theodor Bilharz Research Institute; Warak El-Hadar; Imbaba P.O. Box 30; Giza; 12411; Egypt; Department of Pathology; Theodor Bilharz Research Institute; Warak El-Hadar; Imbaba P.O. Box 30; Giza; 12411; Egypt; Department of Pharmacology and Biochemistry; Faculty of Pharmacy; The British University in Egypt; Suez Desert Road; P.O. Box 43; ElSherouk City; Cairo 11837; Egypt; Department of Pharmacognosy; Faculty of Pharmacy; October University for Modern Sciences and Arts (MSA); 6th of October; Giza; 12566; Egypt
Few studies reported the antifibrotic effects of gallic acid (GA) despite its known hepatoprotective and antioxidant activities. Accordingly, this study investigated the antifibrotic effects of GA through clarifying its mechanisms on hepatic stellate cells� (HSCs) activation, proliferation and/or apoptosis. In vitro effects of GA on HSC-T6 activation/proliferation, morphology and safety on hepatocytes were assessed. In vivo, hepatic fibrosis was induced via chronic thioacetamide (TAA)-intoxication. TAA-intoxicated rats were treated with silyamrin or GA. At end of experiment, liver functions, hepatic MDA, GSH, PDGF-BB, TGF-?1, TIMP-1 and hydroxyproline were determined. Histological analysis and Sirius red staining of hepatic sections, expressions of alpha-smooth muscle actin (?-SMA), proliferating cellular nuclear antigen (PCNA) and caspase-3 were examined. In vitro, GA resulted in a concentration and time-dependent inhibition in HSCs activation, proliferation (IC50= 45 and 19 ?g/mL at 24 and 48 h respectively); restored the quiescent morphology of some activated HSCs plus its safety on hepatocytes. In vivo, GA reduced ALT, AST, MDA, PDGF-BB levels, collagen deposition and fibrosis score (S1 vs S4); increased caspase-3 expression and restored GSH stores, TGF-?1 level, ?-SMA and PCNA expressions. In conclusion, GA counteracted the progression of hepatic fibrosis through reduction of HSCs proliferation/activation mutually with their apoptosis induction. � 2018 Center for Food and Biomolecules, National Taiwan University
Antihyperglycemic Activity and Standardization of the Bioactive Extract of Cleome droserifoliaGrowing in Egypt
(Pharmacognosy Journal, 2014) Abdel Motaal, Amira; Ezzat, Shahira M; El-Askary, Hesham
Cleome droserifolia herb is well known in the Egyptian folk medicine for the treatment of diabetes. However, a standardized active extract of the herb was never prepared for incorporation into a pharmaceutical dosage form.
Antihyperglycemic and antihyperlipidemic effects of the methanol extracts of Cleome ramosissima Parl., Barleria bispinosa (Forssk.) Vahl. and Tribulus macropterus Boiss.
(Faculty of Pharmacy, Cairo University, 2014) Ezzat, Shahira M; Abdel-Sattar, Essam; M. Harraz, Fathalla; A. Ghareib, Salah
The antihyperglycemic and antihyperlipidemic effects of the methanolic extracts of the aerial parts of Cleome ramosissima Parl. (Cleomaceae), Barleria bispinosa (Forssk.) Vahl. (Acanthaceae) and Tribulus macropterus Boiss. (Zygophyllaceae) were evaluated in streptozotocin (STZ) induced diabetic rats at a dose of 500 mg/kg bw. The reduction in fasting blood glucose level (BGL) was observed in the following order C. ramosissima, B. bispinosa and T. macropterus at the 4th week of administration. C. ramosissima and T. macropterus also showed significant increase in plasma insulin by 100.6% and 189.9%, respectively. The studied plant extracts induced an increase in both utilization and tolerance of glucose in diabetic rats. The hypolipidemic effect of C. ramosissima and T. macropterus was demonstrated by a significant reduction in plasma total cholesterol (TC) (42.6% and 37.2%, respectively) and low density lipoprotein cholesterol (LDL-C) (48.0% and 42.1%, respectively) and the increase of high density lipoprotein cholesterol (HDL-C) by 81.0% and 91.9%, respectively. B. bispinosa decreased the blood levels of LDL-C
Antileishmanial Potentials of Phytochemicals
(Wiley & Sons, Inc., 2022) Ezzat, Shahira M; Salem, Mohamed A; Zayed, Ahmed
Leishmaniasis is a neglected tropical disease that causes severe morbidity and mortality. It has an estimated worldwide incidence of 15 million infected people and 350 million at risk, living in tropical and subtropical areas of 88 endemic countries in America, Europe, Africa, Middle East, and Asia. Current treatment of leishmaniasis relies on chemotherapy. No vaccine exists for leishmaniasis and most of the antileishmanial drugs currently in use, have disadvantages, such as severe side effects or parasite resistance. Amphotericin B and its lipid-carrier formulations have been successfully applied, while the first line drugs were no longer effective due to drug resistance. Nevertheless, very high costs of these drugs prevent their widespread use. Alternatively, many plants and plant constituents have been used over the past years for controlling such disease. In this chapter, emphasis was made on the different plants, plant extracts as well as natural lead molecules that were proved to have antileishmanial activity. © 2022 John Wiley & Sons, Inc.
Antiprotozoal activity of major constituents from the bioactive fraction of Verbesina encelioides
(Taylor & Francis, 2017) Ezzat, Shahira M; M Salama, Maha; A Mahrous, Engy; Maes, Louis; Pan, Cheol-Ho; Abdel-Sattar, Essam
The bioactive petroleum ether fraction of Verbesina encelioides, previously studied by the authors, was chosen for the isolation of antiprotozoal metabolites. Pseudotaraxasterol-3β-acetate (1), benzyl 2,6-dimethoxy benzoate (2), 16β-hydroxy-pseudotaraxasterol-3β-palmitate (3) and pseudotaraxasterol (4), in addition to β-sitosterol glucoside (5) and β-sitosterol galactoside (6) were isolated and identified based on one-dimensional and two-dimensional spectral analysis. This is the first report describing (3) and (6) in genus Verbesina. The isolated compounds were tested in vitro against Plasmodium falciparum, Trypanosoma brucei, Trypanosoma cruzi and Leishmania infantum. Cytotoxicity was evaluated on MRC-5 cells. Compound 1 showed moderate to weak activity against L. infantum T. brucei and P. falciparum and was inactive against T. cruzi. Compound 3 showed moderate activity against L. infantum, compound 4 revealed weak activity against T. cruzi, while 5 and 6 were inactive against all tested protozoa. All compounds were non-cytotoxic. The isolated constituents showed less antiprotozoal activity than the crude fraction.
Application of a comprehensive metabolomics approach for the selection of flaxseed varieties with the highest nutritional and medicinal attributes
(6/15/2021) Salem, Mohamed A; Ezzat, Shahira M; Giavalisco, Patrick; Abdel Sattar, Essam; El Tanbouly, Nebal
Flaxseed is considered an indispensable generally recognized as safe (GRAS) source of polyphenolic lignans, poly- unsaturated fatty acids (PUFA), fibers as well as minerals and vitamins. The metabolite content of flaxseed reflects its nutritional and medicinal value. Therefore, the selection of flaxseed variety for food industry is dependent on its metabolome. A metabolomics approach based on liquid or gas chromatography coupled to mass spectrometry has been applied to discriminate different flaxseed cultivars that are commercially available in Egypt. The available Sakha cul- tivars were subjected to a comprehensive metabolomics and lipidomics approach for investigation of their metabolomes. Our results showed that among the screened cultivars, Sakha 6, with its yellow-colored testa, showed marked metabolic discrimination. This yellow cultivar showed high accumulation of essential amino acids. Additionally, the oil of this cultivar accumulated the highest content of the two essential PUFA: alpha-linolenic acid (an u-3 fatty acid) and linoleic acid (an u-6 fatty acid). Interestingly, the content of the main antinutritional cyanogenic glycosides such as linustatin and neolinustatin was lower, while, the content of medicinally-important secondary metabolites was higher in Sakha 6 cultivar. These results support the use of this cultivar for human consumption owing to its high nutritional and me- dicinal value