ETHANOL EXTRACT AND ACTIVE FRACTION  EFFECT OF  Moringa Oleifera. Lam IN INHIBITING COX-2 ACTIVITY ON MCF-7 CELL

The expression of COX-2 is involved in carcinogenesis through the proliferative process, angiogenesis and inhibition of apoptosis. Moringa oleifera has been shown to function as an anti-oxidant, anti-inflammatory, anti-microbial and anticancer. Moringa leaf extraction was done by percolation method, and continued to liquid-liquid extraction to obtain nonpolar, semipolar, and polar fractions using n-hexane and ethylacetate solvent.The aim of this study was to determine the effect of ethanol extract and the fraction of n-Hexane of Moringa oleifera leaf in decreased MCF-7 breast cancer cell and COX-2 expression. This study used true experimentation in vitro design using MCF-7 cells. MTT Assay was performed using a therapeutic dose 6,125-1000 μg / ml to determine IC50 in MCF-7 cells. IC50 of ethanol extract was obtained 94.44 μg / ml and 97.60 μg / ml for n-Hexane fraction. Selectivity index of both samples was 3.95 μg / ml and 2.87 μg / ml. The expression of COX-2 was tested qualitatively with immunocytochemical methods and showed that ethanol extract and n-hexane fraction of Moringa oleifera leaf were able to suppress COX-2 enzyme expression on MCF-7 cells depending on concentration. Keywords: Moringa leaf, cancer cells MCF-7, Apoptosis and COX-2

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In Vitro Inhibitory Effects of Moringa oleifera Leaf Extract and Its Major Components on Chemiluminescence and Chemotactic Activity of Phagocytes

Natural Product Communications ◽

10.1177/1934578x1300801115 ◽

2013 ◽

Vol 8 (11) ◽

pp. 1934578X1300801 ◽

Cited By ~ 5

Author(s):

Boonyadist Vongsak ◽

Wandee Gritsanapan ◽

Yuvadee Wongkrajang ◽

Ibrahim Jantan

Keyword(s):

Chlorogenic Acid ◽

Oxidative Burst ◽

Moringa Oleifera ◽

Ethanol Extract ◽

Boyden Chamber ◽

Inhibitory Effects ◽

Chemotactic Migration ◽

Human Polymorphonuclear Leukocytes ◽

Moringa Oleifera Lam

The ethanol extract of Moringa oleifera Lam. leaves and its major constituents, crypto-chlorogenic acid, quercetin 3- O-glucoside and kaempferol 3- O-glucoside, were investigated on the respiratory burst of human whole blood and isolated human polymorphonuclear leukocytes (PMNs) using a luminol-based chemiluminescence assay. The chemotactic migration of PMNs was also investigated using the Boyden chamber technique. The ethanol extract demonstrated inhibitory activities on the oxidative burst and the chemotactic migration of PMNs. Quercetin 3- O-glucoside, crypto-chlorogenic acid, and kaempferol 3- O-glucoside, isolated from the extract, expressed relatively strong inhibitory activity on the oxidative burst of PMNs with IC50 values of 4.1, 6.7 and 7.0 μM, respectively, comparable with that of aspirin. They also demonstrated strong inhibition of chemotatic migration of PMNs with IC50 values of 9.5, 15.9 and 18.2 μM, respectively. The results suggest that M. oleifera leaves could modulate the immune response of human phagocytes, linking to its ethnopharmacological use as an anti-inflammatory agent. The immunomodulating activity of the plant was mainly due to its major components.

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New Ferrocene Compounds as Selective Cyclooxygenase (COX-2) Inhibitors: Design, Synthesis, Cytotoxicity and Enzyme-inhibitory Activity

Anti-Cancer Agents in Medicinal Chemistry ◽

10.2174/1871520617666171003145533 ◽

2018 ◽

Vol 18 (2) ◽

pp. 295-301 ◽

Cited By ~ 8

Author(s):

Shabnam Farzaneh ◽

Elnaz Zeinalzadeh ◽

Bahram Daraei ◽

Soraya Shahhosseini ◽

Afshin Zarghi

Keyword(s):

Cell Lines ◽

Inhibitory Activity ◽

Fibroblast Cell ◽

Breast Cancer Cell Lines ◽

Ferrocene Derivatives ◽

Cox 2 ◽

Cytotoxicity Effects ◽

Cox 2 Inhibitors ◽

Mcf 7

Background: Due to the astonishing properties of ferrocene and its derivatives, it has a broad application in diverse areas. Numerous ferrocene derivatives demonstrated anti-proliferative activity. Also COX-2, as a key isoenzyme for production of prostaglandins, is frequently overexpressed in various cancers. It is now recognized that COX-2 over expression promotes tumorigenic functions which can be suppressed by COX-2 inhibitors, a phenomenon useful for the preventing of tumor progression. The combination of COX-2 inhibitors with other anti-cancer or cancer prevention drugs may reduce their side effects in future cancer prevention and treatment. Objective: Owing to high anticancer potential of ferrocene derivatives and considerable COX-2 inhibitory and cytotoxicity effects of our previously synthesized chalcones, we decided to incorporate the ferrocenyl moiety into appropriate COX-2 inhibitor chalcone based scaffold, to evaluate COX-2 inhibitory activity as well as anticancer activities. Methods: Chalcones were synthesized via clasien-schmidt condensation of methylsulfonyl aldehyde and acetyl ferrocene. Further different amines with solvent free and ultra sound condition were reacted with chalcones to have different 1-ferrocenyl-3-amino carbonyl compounds. Docking study was carried out with Auto Dock vina software. All the newly-synthesized compounds were evaluated for their cyclooxygenase-2 (COX-2) inhibitory activity using chemiluminescent enzyme assays as well as cytotoxicity activity against MCF-7 and T47D and fibroblast cell lines by MTT assay. Results: In vitro COX-1/COX-2 inhibition studies demonstrated that all compounds were selective inhibitors of the COX-2 isozyme with IC50 values in the highly potent 0.05-0.12 µM range, and COX-2 selectivity indexes (SI) in the 148.3-313.7 range. These results indicated that either potency or selectivity of COX-2 inhibitory activity was affected by the nature and size of the substituents on C-3 of propane-1-one. Also anti-proliferative and toxicity activities of synthesized compounds against breast cancer cell lines MCF-7 and T47D and fibroblast cell lines showed that the synthesized compounds had mild to moderate cytotoxicity against MCT7 and T47D breast cancer cell lines at 10 µM concentration. In vitro COX-1/COX-2 inhibition studies and anticancer activity against MCF-7, identified 1-ferrocenyl-3-(4-methylsulfonylphenyl) propen-1-one as a potent compound (IC50 COX-2 = 0.05 µM, MCF-7: % inhibition (at concentration of 10 µM) = 32.7%), and also 1-ferrocenyl-3- (propan-1-amine)-3-(4-methylsulfonylphenyl) propan-1-one showed the most selectivity on COX-2 inhibition (selectivity index= 313.7). Conclusion: A novel group of ferrocene compounds, possessing a methyl sulfonyl COX-2 pharmacophore were synthesized to investigate the effect of different substituents on selectivity and potency of COX-2 inhibitory activity and their cytotoxicity effects. This study indicates that 1-ferrocenyl-3-amino carbonyl compounds having ferrocene motif and methyl sulfonyl COX-2 pharmacophore is a suitable scaffold to design COX-2 inhibitors and anti-cancer agents.

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In Vitro Cytotoxic Effects of Secondary Metabolites Present in Sarcopoterium Spinosum L.

Applied Sciences ◽

10.3390/app11115300 ◽

2021 ◽

Vol 11 (11) ◽

pp. 5300

Author(s):

Jozef Hudec ◽

Jan Mojzis ◽

Marta Habanova ◽

Jorge A. Saraiva ◽

Pavel Hradil ◽

...

Keyword(s):

Mammary Gland ◽

Ethyl Acetate ◽

Cytotoxic Activity ◽

Cell Lines ◽

Benzalkonium Chloride ◽

Ethanol Extract ◽

Cytotoxic Activities ◽

Sarcopoterium Spinosum ◽

Mcf 7

Sarcopoterium spinosum (L.) is a medicinal plant traditionally used for the treatment of various diseases including cancer in the Near- and Middle East. The fractions and constituents of the ethanol extract of S. spinosum were screened for in vitro cytotoxic activities on Jurkat (acute T-lymphoblastic leukemia), HeLa (cervical adenocarcinoma), MCF-7 (mammary gland adenocarcinoma), Caco-2 (human colorectal adenocarcinoma), and MDA-MB-231 (mammary gland adenocarcinoma) cell lines using the MTT (3-(dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide) assay. The ethanol extract was subsequently re-extracted with ethyl acetate and in its sub-fraction obtained by column chromatography three compounds (stachydrine, benzalkonium chloride and rutine) were the first time identified by nuclear magnetic resonance (NMR) analyses. The most active subfraction showed cytotoxic activity against HeLa, MCF-7, and Caco-2 cell lines. The three compounds mentioned, as standards of high-performance liquid chromatography (HPLC) quality, were studied individually and in combination. Cytotoxic activity observed might be due to the presence of benzalkonium chloride and rutin. Benzalkonium chloride showed the strongest growth suppression effect against HeLa cells (IC50 8.10−7 M) and MCF-7 cells (IC50 5.10−6 M). The mixture of stachydrine and benzalkonium chloride allowed a synergistic cytotoxic effect against all tested cancer and normal cells to be obtained. Anti-cancer activity of the plant extract of S. spinosum remains under-investigated, so this research describes how the three major compounds identified in the ethyl acetate extract can exert a significant dose dependent in vitro cytotoxicity.

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Bioaccessibility, antioxidant activity and modulation effect on gut microbiota of bioactive compounds from Moringa oleifera Lam. leaves during digestion and fermentation in vitro

Food & Function ◽

10.1039/c9fo00793h ◽

2019 ◽

Vol 10 (8) ◽

pp. 5070-5079 ◽

Cited By ~ 9

Author(s):

Zuman Dou ◽

Chun Chen ◽

Xiong Fu

Keyword(s):

Antioxidant Activity ◽

Gut Microbiota ◽

Bioactive Compounds ◽

Moringa Oleifera ◽

Modulation Effect ◽

Gastrointestinal Digestion ◽

Colonic Fermentation ◽

Moringa Oleifera Lam

This study aims to investigate the bioaccessibility, bioactivity and gut microbiota modulation effect of Moringa oleifera Lam. leaves after in vitro gastrointestinal digestion and colonic fermentation.

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Development of mouthwash with Rosmarinus officinalis extract

Brazilian Journal of Pharmaceutical Sciences ◽

10.1590/s1984-82502014000400020 ◽

2014 ◽

Vol 50 (4) ◽

pp. 851-858 ◽

Cited By ~ 1

Author(s):

Isabela Moreira Baumgratz de Paula ◽

Flávia Costa Moraes ◽

Orlando Vieira de Souza ◽

Célia Hitomi Yamamoto

Keyword(s):

Sodium Fluoride ◽

Inhibitory Activity ◽

Raw Materials ◽

Ethanol Extract ◽

Inhibitory Effect ◽

Rosmarinus Officinalis ◽

Hexane Fraction ◽

Diffusion Method ◽

Oral Infections

Rosmarinus officinalis, which belongs to the Lamiaceaefamily, is a species of medicinal flora with therapeutic properties. In order to exploit the benefits of these properties, a mouthwash formulation was developed, with careful selection of raw materials to meet pharmacotechnical requirements. Extracts of the plant were incorporated into a mouthwash, which was shown to have inhibitory action in vitro against the micro-organisms commonly found in periodontics. Controls for assessing the quality of the drugs were carried out, quantifying phenols and flavonoids as chemical markers. Mouthwash solutions were formulated containing 0.1, 5 and 10% ethanol extract of R. officinalis; and 0.05, 5 and 10% of the hexane fraction of R. officinalis. In order to evaluate synergism, ethanol extract and hexane fraction were also added to formulations containing 0.05% sodium fluoride and 0.12% chlorhexidine digluconate. These formulations were assessed for inhibitory effect against the specific microorganisms involved in the process of bacterial plaque formation, S. mutans(ATCC25175) and C. albicans(ATCC 10231), frequently found in cases of oral infections. The agar diffusion method was used to evaluate the inhibitory activity of extracts and formulations. All mouthwash solutions displayed inhibitory activity having higher sensitivity to S. mutansfor the 5% ethanol extract+0.05% sodium fluoride, and greater sensitivity to C. albicansfor the 10% hexane fraction. Results were characterized by the appearance of a growth inhibition halo, justifying the utilization and association of extracts of R. officinalis.

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Uji Aktivitas Antioksidan Ekstrak Air dan Ekstrak Etanol Daun Kelor (Moringa Oleifera LAM)

Jurnal Akademika Kimia ◽

10.22487/j24775185.2017.v6.i2.9244 ◽

2017 ◽

Vol 6 (2) ◽

pp. 125

Author(s):

Rizkayanti Rizkayanti ◽

Anang Wahid M. Diah ◽

Minarni Rama Jura

Keyword(s):

Vitamin C ◽

Moringa Oleifera ◽

Water Extract ◽

Ethanol Extract ◽

Positive Control ◽

Negative Control ◽

Ic50 Value ◽

Antioxidant Potency ◽

Ethanol Extracts ◽

Moringa Oleifera Lam

Moringa (moringa oleifera Lam) leaves contains many molecules as inhibitors for free radicals such as phenolic compounds (phenolic acids, flavonoids, quinones, coumarins, lignans, stilbenes, tannins), nitrogen compounds (alkaloids, amines, betalain), vitamins, terpenoids (including carotenoids), and several other endogenous metabolites as antioxidants. This study aimed to determine the antioxidant potency of water and ethanol extracts of moringa (moringa oleifera Lam) leave obtained by maceration and dekok. The concentration of free radical 1,1-diphenyl-2-picrylhydrazyl (DPPH) was analyzed using UV-Vis spectrophotometer after addition of various concentrations of Moringa leaves extracts. Various concentrations of moringa leave extracts used were 20 ppm, 40 ppm, 60 ppm and 80 ppm. Vitamin C solutions as the positive control were prepared on similar various concentrations. The negative control was prepared using DPPH solutions dissolved in absolute ethanol. The results indicated that the ethanol extract of moringa leaves prepared by maceration method showed the antioxidant potency with an IC50 value of 22.1818 ppm, but the IC50 value of water extract of moringa leaves prepared by dekok was 57.5439 ppm. While, the IC50 value of Vitamin C was 8.8084 ppm. Based on the IC50 data it can be concluded that Vitamin C is a stronger antioxidant than moringa leaves extracts.

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