SECONDARY METABOLITES FROM RICE CULTURE OF ASPERGILLUS SP. ISOLATED FROM MELALEUCA SUBULATA (CHEEL) CRAVEN LEAVES AND THEIR ANTICANCER ACTIVITY

2020 ◽  
pp. 52-61
Author(s):  
HAITHAM ALI IBRAHIM ◽  
REHAM RAGAEI IBRAHIM ◽  
REEM ALAA KAMEL ◽  
SHAHENDA METWALLY EL-MESSERY ◽  
FATMA ABDELKADER MOHARRAM
Keyword(s):  
Secondary Metabolites ◽  
Ethyl Acetate ◽  
Anticancer Activity ◽  
Ethyl Acetate Extract ◽  
Moderate Activity ◽  
Hep G2 ◽  
Rice Culture ◽  
Aspergillus Sp ◽  
Hsp 90 ◽  
Mcf 7

Objective: Aspergillus fungus is a rich source of natural products with broad biological activities. This study was conducted to identify secondary metabolites from the rice culture of Aspergillus species isolated from Melaleuca subulata leaves and evaluated their anticancer activity. Methods: Ethyl acetate extract was fractionated on silica gel and Sephadex columns. Structures of the compounds were established using physical and chemical methods. Cytotoxic activities of the extract and pure compounds against two human cancer cell lines (Mcf-7and Hep G2) were evaluated using microculture tetrazolium assay as well as the mode of the cytotoxicity was evaluated. Molecular docking studies have been performed using the Hsp 90 enzyme as an anticancer target. Results: Methyl linoleate (1), arugosin C (2), ergosterol (3), sterigmatocystin (4), diorcinol (5), alternariol-5-O-methyl ether (6), averufin (7), averufanin (8), and alternariol (9) were identified from ethyl acetate extract. All tested compounds exhibit week activity against MCF-7 and Hep G2 cell lines but a mixture of compounds 7 and 8 is considered to be more active towards both MCF-7 and Hep G 2 in comparison to other compounds. Compound 4 exhibits moderate activity against Hep G2 only as well as the ethyl acetate extract exerts moderate activity against MCF-7 cell line Moreover, compound 4 and a mixture of 7 and 8 caused a decrease in the number of Hep G2 cancer cells due to apoptotic and necrotic processes. Most active anticancer candidates 7 and 8 showed binding to the active site similar to geldanamycin reference ligand. Conclusion: Secondary metabolites identified from Aspergillus sp. and their anticancer activity were evaluated. Molecular docking suggested active candidates as Hsp 90 inhibitors.

scholarly journals CYTOTOXICITY OF METABOLITES PRODUCED BY ENDOPHYTIC FUNGUS CLADOSPORIUM SP. ISOLATED FROM MARINE MACROALGAE ON IN­VITRO MCF­7, HELA, AND DU-145 CELL LINES

2018 ◽  
Vol 10 (8) ◽  
pp. 72
Author(s):  
Asri Peni Wulandari ◽  
R. R. Indry Noviarin Examinati ◽  
Madihah . ◽  
Desi Harneti Putri Huspa ◽  
Poniah Andayaningsih ◽  
...  
Keyword(s):  
Ethyl Acetate ◽  
Anticancer Activity ◽  
Cell Line ◽  
Cell Lines ◽  
Ethyl Acetate Extract ◽  
In Vitro Cytotoxicity ◽  
Marine Macroalgae ◽  
Morphological Alteration ◽  
Mcf 7

Objective: To investigate the in vitro cytotoxicity effect of the crude ethyl acetate extract of Cladosporium sp. on MCF-7, HeLa, and DU-145 cell lines.Methods: In vitro cytotoxicity was evaluated by tetrazolium reduction assay. The percentage of cell inhibition was analyzed using probit analysis to obtain 50% inhibitory concentration (IC50). Morphological alteration of the cell lines after exposure with extract was observed under an inverted microscope.Results: The ethyl acetate extract of the metabolite performed an anticancer activity for cancer cell line MCF-7, HeLa, and DU-145 with IC50 respectively 8.46 μg/ml; 9.87 μg/ml; and 98.03 μg/ml. The extract shows greater the anticancer activity and has strong antiproliferative on MCF-7 and HeLa cell line than DU-145. Confirmation morphological were observed under the inverted microscope showed a morphological change in cancer cells when incubated with the extract.Conclusion: From the performed assay, the crude extract of Cladosporium sp. exhibit cytotoxic activity against MCF-7, HeLA, and DU-145.

Study on Chemical Constituents and Cytotoxic Activities of Salacia chinensis Growing in Vietnam

2010 ◽  
Vol 65 (10) ◽  
pp. 1284-1288 ◽  
Author(s):  
Tran Thi Minh ◽  
Nguyen Thi Hoang Anh ◽  
Vu Dao Thang ◽  
Tran Van Sung
Keyword(s):  
Spectral Analysis ◽  
Ethyl Acetate ◽  
Cell Lines ◽  
Cancer Cell ◽  
Ethyl Acetate Extract ◽  
Chemical Constituents ◽  
Cytotoxic Activities ◽  
Good Activity ◽  
Hep G2 ◽  
Mcf 7

Two new triterpenoids, named 7α,21α-dihydroxyfriedelane-3-one (1) and 7α,29-dihydroxyfriedelane- 3-one (2) have been isolated from the ethyl acetate extract of the stems of Salacia chinensis besides the known triterpenoid 21α,30-dihydroxyfriedelane-3-one (3). The structures of the isolated compounds were elucidated on the basis of spectral analysis. Eight triterpenoids from this plant have been tested against the four cancer cell lines Hep-G2, LU, KB, and MCF-7. The new compound 1 showed good activity against all four tested cell lines.

scholarly journals Synthesis, characterization, molecular docking and in vitro anticancer activity of 3-(4-methoxyphenyl)-5-substituted phenyl-2-pyrazoline-1- carbothioamide

2021 ◽  
Vol 12 (2) ◽  
pp. 1648-1658
Author(s):  
Benupani Sahu ◽  
Rajapandi R ◽  
Avik Maji ◽  
Abhik Paul ◽  
Tanushree Singha ◽  
...  
Keyword(s):  
Molecular Docking ◽  
Liver Cancer ◽  
Anticancer Activity ◽  
Cell Lines ◽  
Breast Adenocarcinoma ◽  
Moderate Activity ◽  
Hep G2 ◽  
Molegro Virtual Docker ◽  
Mcf 7

In the present study, eight numbers of new 3- (4-methoxy phenyl)-5-substituted phenyl-2-pyrazoline-1-carbothioamide (5a-h) have been synthesized from 1- (4-methoxy phenyl)-3- (substituted phenyl)-prop-2-en-1-one (3a-h) and structurally characterized by using FT-IR, 1H NMR, 13C NMR, Mass and Elemental analysis. The synthesized molecules were biologically evaluated for their in vitro anticancer activity against human breast adenocarcinoma (MCF-7), liver cancer (Hep-G2) and leukaemia cancer (K-562) cell line using Sulforhodamine B (SRB) bioassay technique. From the all synthesized compounds 5a, 5c, 5d, and 5e exhibited potent anticancer activity (GI50= <10µg/ml) as compared to the controlled drug 5-Fluorouracil (5-FU) (GI50=44.5µg/ml) and Adriamycin (ADR) (GI50= <10µg/ml) on MCF-7 cell lines. Besides this, all the synthesized compounds have exhibited moderate activity against human liver cancer (Hep-G2) and leukaemia cancer (K-562) cell lines. In addition, molecular docking studies were also explored in order to study the probable binding specificity into the active site of Epidermal Growth Factor Receptor tyrosine kinase (EGFR) (PDB ID: 1M17) using Molegro Virtual Docker Evaluation 2013 6.0.1 (MVD). Based on the molecular docking result, it was found that compound 5a exhibited the best interaction with the above target (i.e., EGFR) by interacting with specific amino acid residues such as: Thr 766, Gin 767, Thr 830, Cys 575, Ala 719 and Met 769.

Synthesis of novel amide and Schiff’s base functionalized novel pyrido[1,2-a] pyrimidin-4-one derivatives and their anticancer activity studies.

2021 ◽  
Vol 18 ◽  
Author(s):  
Sailu Betala ◽  
Chiranjeevi Abba ◽  
Hanumandlu Racha
Keyword(s):  
Anticancer Activity ◽  
Hydrazine Hydrate ◽  
Human Cancer ◽  
Aromatic Aldehydes ◽  
Human Cancer Cell ◽  
Hep G2 ◽  
Schiff’S Base ◽  
Human Cancer Cell Lines ◽  
Amide Derivatives ◽  
Mcf 7

Abstract: A series of novel amide and Schiffs base functionalized novel pyrido[1,2-a]pyrimidin-4-one derivatives were prepared starting from 6-(thiophene-2-yl)/phenyl-4-(trifluoromethyl) pyridin-2-amine 1a and 1b. These compounds on reaction with EMME, to afford compounds 2a and 2b, followed by cyclization to afford compounds 3a and 3b. Treatment of compound 3a and 3b with hydrazine hydrate to get compounds 4a and 4b, compounds 4a and 4b on reaction with different substituted aromatic aldehydes to get Schiff’s base derivatives 5a-j, in another way compounds 3a, 3b on reaction with aliphatic amines to get amide derivatives 6a-f. All the compounds 5a-j and 6a-f were screened against four human cancer cell lines (HeLa, COLO205, Hep G2, and MCF 7), among all the derivatives, compounds 5c, 5e, 6a, and 6b showed promising anticancer activity.

scholarly journals GCMS ANALYSIS OF ENDOPHYTIC FUNGI CURVULARIA AERIA MTCC-12847 ISOLATED FROM TRIBULUS TERRESTRIS L.

2019 ◽  
pp. 26-32
Author(s):  
Kamana Sahani ◽  
DEEPENDRA THAKUR
Keyword(s):  
Mass Spectrometry ◽  
Gas Chromatography ◽  
Secondary Metabolites ◽  
Ethyl Acetate ◽  
Endophytic Fungi ◽  
Active Compound ◽  
Ethyl Acetate Extract ◽  
Gas Chromatography Mass Spectrometry ◽  
Tribulus Terrestris ◽  
Chromatography Mass Spectrometry

Objective: The objective of the present investigation was to perform the Gas Chromatography-mass spectrometry (GCMS) analysis of endophytic fungi Curvularia aeria MTCC-12847 isolated from Tribulus terrestris L. to find out the active compound present in the extract. Methods: The endophytic fungi were isolated from the plant Tribulus Terrestris L., leaf which was cultivated in optimized media for the production of secondary metabolites and was extracted using ethyl acetate. Ethyl acetate extract was used for the Gas Chromatography-mass spectrometry (GCMS) analysis. Results: GC-MS analysis of ethyl acetate extract of endophytic fungi revealed the presence of various secondary metabolites, the highest amount present was Palmitic acid (24.54%) and Lowest was Dimethyl 1-phenyl-7-methyl-1-hydroxy-1,4-dihydronaphthalene-2,3-dicarboxylate (5.76%). Conclusion: The endophytic fungal Curvularia aeria MTCC-12847 extract isolated from the Tribulus terrestris L. shows the presence of various bioactive compounds.

scholarly journals Cytotoxic Stilbenes and Canthinone Alkaloids from Brucea antidysenterica (Simaroubaceae)

Molecules ◽  
2019 ◽  
Vol 24 (23) ◽  
pp. 4412 ◽  
Author(s):  
Yves Salomon Makong ◽  
Gervais Mouthé Happi ◽  
Judith Liliane Djouaka Bavoua ◽  
Jean Duplex Wansi ◽  
Lutfun Nahar ◽  
...  
Keyword(s):  
Secondary Metabolites ◽  
Ethyl Acetate ◽  
Propionic Acid ◽  
2D Nmr ◽  
Spectroscopic Methods ◽  
Phytochemical Study ◽  
Methanolic Extracts ◽  
New Compounds ◽  
Soluble Fractions ◽  
Mcf 7

A phytochemical study of the root and bark of Brucea antidysenterica J. F. Mill. (Simaroubaceae) afforded three new compounds, including a stilbene glycoside bruceanoside A (1), and two canthinone alkaloids bruceacanthinones A (3) and B (4), along with ten known secondary metabolites, rhaponticin (2), 1,11-dimethoxycanthin-6-one (5), canthin-6-one (6), 1-methoxycanthin-6-one (7), 2-methoxycanthin-6-one (8), 2-hydroxy-1,11-dimethoxycanthin-6-one (9), β-carboline-1-propionic acid (10), cleomiscosin C (11), cleomiscosin A (12), and hydnocarpin (13). The structures of all the compounds were determined using spectrometric and spectroscopic methods including 1D and 2D NMR, and HRSEIMS. The identities of the known compounds were further confirmed by comparison of their data with those reported in the literature. The root and bark methanolic extracts, the dichloromethane and ethyl acetate soluble fractions, and the isolated compounds (3–13), were assessed for their cytotoxicity against the cancer cell lines A-549, MCF-7, and PC-3. The results suggested that compounds in the extracts might possess a synergic action in their cytotoxicity.

scholarly journals CYTOTOXIC AND ANTIOXIDANT ACTIVITIES OF SECONDARY METABOLITES FROM PULICARIA UNDULATA

2016 ◽  
Vol 8 (9) ◽  
pp. 150 ◽  
Author(s):  
Taha A. Hussien ◽  
Sayed A. El-toumy ◽  
Hossam M. Hassan ◽  
Mona H. Hetta
Keyword(s):  
Antioxidant Activity ◽  
Secondary Metabolites ◽  
Antioxidant Activities ◽  
Structure Activity Relationship ◽  
Activity Relationship ◽  
Hep G2 ◽  
Structure Activity ◽  
Dpph Method ◽  
Mcf 7

<p><strong>Objective:</strong><strong> </strong>To evaluate the <em>in vitro</em> cytotoxicity, antioxidant activities and structure-activity relationship of secondary metabolites isolated from <em>Pulicaria undulata</em>.</p><p><strong>Methods: </strong>The methylene chloride-methanol (1:1) extract of the air-dried aerial parts of <em>Pulicaria undulata</em> was fractionated and separated to obtain the isolated compounds by different chromatographic techniques. Structures of the isolated compounds were determined on the basis of the extensive spectroscopic analysis, including 1D and 2D NMR and compared with the literature data. The crude extract and the isolated compounds were evaluated for <em>in vitro</em> antioxidant activity using the 2,2 diphenyl dipicryl hydrazine (DPPH) method and cytotoxic assay using human breast cancer (MCF-7) and hepatoma (Hep G2) cell line.</p><p><strong>Results: </strong>Nine secondary metabolites were isolated from <em>Pulicaria undulata</em> in this study. Of which two terpenoidal compounds; 8-epi-ivalbin and 11β, 13-dihydro-4H-xanthalongin 4-<em>O</em>-β-D-glucopyranoside firstly isolated from the genus <em>pulicaria</em> and three flavonoids; eupatolitin, 6-methoxykaempferol, and patulitrin firstly isolated from <em>P. undulata</em>. 6-methoxykaempferol (IC<sub>50</sub> 2.3 µg/ml) showed the most potent antioxidant activity. The highest cytotoxic effect against MCF-7 and Hep G2 cells was obtained with eupatolitin (IC<sub>50</sub> 27.6 and 23.5 µg/ml) respectively. The structure-activity relationship was also examined and the findings presented here showed that 3, 5, 7, 4' and 3, 5, 4', 5'-hydroxy flavonoids were potent antioxidant and has cytotoxic activity.</p><p><strong>Conclusion: </strong><em>Pulicaria undulata</em> is a promising medicinal plant, and our study tends to support the therapeutic value of this plant as antioxidant drug and in the treatment of cancer.</p>

In Vitro Tracing of Cytotoxic Compounds in Jarak Cina Stem Bark (Jatropha Multifida Linn.)

2020 ◽  
Vol 20 (1) ◽  
Author(s):  
Sista Werdyani ◽  
Annisa Fitria ◽  
Sari Rakhmawati
Keyword(s):  
Ethyl Acetate ◽  
Cytotoxic Activity ◽  
Cancer Cells ◽  
Cancer Cell ◽  
Ethyl Acetate Extract ◽  
Soxhlet Extraction ◽  
Ethanol Extract ◽  
Jatropha Multifida ◽  
Mcf 7

Cancer remains one of the diseases with increasing number of sufferers, but research on compounds that act as anti-cancer is also ongoing. Terpenoids have been known as a compound that can inhibit the proliferation of cancer cells. One of the medical plants that produce terpenoids is Jarak cina (Jatropha multifida Linn.). Therefore, the possibility of Jarak cina (Jatropha multifida Linn.) to have an cytotoxic activity on cancer cell proliferation is reasonably high. This study was conducted to determine the cytotoxic activity of Jarak cina (Jatropha multifida Linn.) bark extracts against cancer cell MCF-7. Jarak cina bark was extracted using the multilevel soxhlet extraction method with n-hexane, ethyl acetate, and ethanol as the solvents. All the three extracts were then tested against MCF-7 cancer cells using MTT (3-(4,5-dimethylthiazol-2-yl) - 2,5-diphenyltetrazolium bromide) method. Data analysis was performed for IC50 (ppm) parameter. The results showed that the IC50 of n-hexane extract was 313.21 ppm, while the ethyl acetate extract reached 258.38 ppm of IC50, and the IC50 of ethanol extract was 418.51 ppm. The highest potential of cytotoxicity was found in the ethyl acetate extract, so further testing would be required to optimize the proliferation inhibitory activity.

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