scholarly journals 13α–Hydroxylucilactaene and Other Metabolites of an Endophytic Strain of Fusarium acuminatum

2007 ◽  
Vol 2 (5) ◽  
pp. 1934578X0700200 ◽  
Author(s):  
Bharat P. Bashyal ◽  
Stanley H. Faeth ◽  
A. A. Leslie Gunatilaka
Keyword(s):  
Spectroscopic Data ◽  
Metastatic Prostate Cancer ◽  
Human Cancer ◽  
Small Cell ◽  
Small Cell Lung ◽  
Human Cancer Cell Lines ◽  
Fusarium Acuminatum ◽  
Relative Stereochemistry ◽  
Normal Human ◽  
Mcf 7

A liquid fermentation culture of Fusarium acuminatum, endophytic in the root of Larrea tritentata, afforded a new furanopyrrolidone, 13α–hydroxylucilactaene (1), together with four known metabolites, NG–391 (2), NG–393 (3), enniatin A (4), and enniatin B (5). The structure and relative stereochemistry of 1 was established by extensive NMR spectral analysis and the known compounds 2 – 5 were identified by comparison of their spectroscopic data with those reported in the literature. The cytotoxicity of all compounds was evaluated in a panel of five human cancer cell lines [NCI–H460 (non-small cell lung), MCF–7 (breast), SF–268 (CNS glioma), MIA Pa Ca–2 (pancreatic carcinoma), PC-3M (metastatic prostate cancer)] and normal human fibroblast (WI–38) cells, and only enniatins A (4) and B (5) were shown to have significant cytotoxic activity.

scholarly journals A New Optical Biflavonoid, (2″R)-2″,3″-Dihydrorobustaflavone 7,4′-Dimethyl Ether, and Other Constituents from Selaginella trichoclada Alsto

2019 ◽  
Vol 14 (12) ◽  
pp. 1934578X1988788
Author(s):  
Peng Yang ◽  
Mei-Long Lu ◽  
Ke Li ◽  
Qun Zhou
Keyword(s):  
Dimethyl Ether ◽  
Spectroscopic Data ◽  
High Performance ◽  
Human Cancer ◽  
Ethanol Extract ◽  
Racemic Compound ◽  
Chiral Phase ◽  
Human Cancer Cell Lines ◽  
First Time ◽  
Mcf 7

A new optical biflavonoid, (2” R)-2″,3″-dihydrorobustaflavone 7,4′-dimethyl ether (1), and 6 known compounds (2-7) were isolated for the first time from the 70% ethanol extract of Selaginella trichoclada Alsto. The structures of the compounds were confirmed by extensive spectroscopic data analyses. Racemic compound 1 was separated by chiral-phase high-performance liquid chromatography, and the absolute configurations of (±)-1 were defined by circular dichroism spectroscopic data. Compound 1 exhibited moderate cytotoxicity against MCF-7, A549, and HepG2 human cancer cell lines.

scholarly journals Synthesis and Anticancer Evaluations of Novel Thiazole Derivatives Derived from 4-Phenylthiazol-2-amine

2021 ◽  
Vol 68 (3) ◽  
pp. 604-616
Author(s):  
Amira E. M. Abdallah ◽  
Rafat M. Mohareb ◽  
Maher H. E. Helal ◽  
Germeen J. Mofeed
Keyword(s):  
Anticancer Agents ◽  
Human Cancer ◽  
Human Cell Line ◽  
Breast Adenocarcinoma ◽  
Small Cell Lung ◽  
Thiazole Derivatives ◽  
Human Cancer Cell Lines ◽  
Chemical Reagents ◽  
Cns Cancer ◽  
Mcf 7

Many novel thiazole derivatives were designed and synthesized using 4-phenylthiazol-2-amine. The reactivity of the latter compound toward different chemical reagents was studied. The structure of the newly synthesized compounds was established based on elemental analysis and spectral data. Furthermore, twenty compounds of the synthesized systems were selected and evaluated in (μM) as significant anticancer agents towards three human cancer cell lines [MCF-7 (breast adenocarcinoma), NCI-H460 (non-small cell lung cancer), and SF-268 (CNS cancer)] and normal fibroblasts human cell line (WI-38). The results showed that compounds 9 and 14a displayed higher effeciency than the reference doxorubicin.

scholarly journals Two New Triterpenes from Basidiomata of the Medicinal and Edible Mushroom, Laetiporus sulphureus

Molecules ◽  
2021 ◽  
Vol 26 (23) ◽  
pp. 7090
Author(s):  
Khadija Hassan ◽  
Blondelle Matio Kemkuignou ◽  
Marc Stadler
Keyword(s):  
Secondary Metabolites ◽  
Spectroscopic Data ◽  
Human Cancer ◽  
Edible Mushroom ◽  
Mouse Fibroblast ◽  
Human Cancer Cell ◽  
Mucor Hiemalis ◽  
Natural Sources ◽  
Human Cancer Cell Lines ◽  
Mcf 7

In the search for novel anti-infectives from natural sources, fungi, in particular basidiomycetes, have proven to still harbor so much potential in terms of secondary metabolites diversity. There have been numerous reports on isolating numerous secondary metabolites from genus Laetiporus. This study reports on two new triterpenoids, laetiporins C and D, and four known triterpenes from the fruiting body of L. sulphureus. The structures of the isolated compounds were elucidated based on their 1D and 2D nuclear magnetic resonance (NMR) spectroscopic data in combination with high-resolution electrospray mass spectrometric (HR-ESIMS) data. Laetiporin C exhibited weak antifungal activity against Mucor hiemalis. Furthermore, the compounds showed weak antiproliferative activity against the mouse fibroblast L929 and human cancer cell lines, including KB-3-1, A431, MCF-7, PC-3 and A549.

scholarly journals Flavonoids from Twigs of Millettia pubinervis

2014 ◽  
Vol 9 (12) ◽  
pp. 1934578X1400901
Author(s):  
Zhi Na ◽  
Qi-Shi Song ◽  
Hua-Bin Hu
Keyword(s):  
Cell Lines ◽  
Cancer Cell ◽  
Spectroscopic Data ◽  
Human Cancer ◽  
Data Interpretation ◽  
2D Nmr ◽  
Human Cancer Cell ◽  
Human Cancer Cell Lines ◽  
Phytochemical Investigation ◽  
Mcf 7

A new flavone, 3-methoxy-5-hydroxy-[2”,3”:7,8] furanoflavone, pubinerone (1), was isolated from the twigs of Millettia pubinervis Kurz, together with ten known flavonoids, karanjin (2), kanjone (3), 3,6-dimethoxy-[2”,3”:7,8] furanoflavone (4), pongaglabrone (5), pongapin (6), pongaflavone (7), 3,6-dimethoxy-6”,6”-dimethylchromene-[2”,3”:7,8] flavone (8), pongachromene (9), 3,6-dimethoxy-3′,4′-methylenedioxy-6”,6”-dimethylchromene-[2”,3”:7,8] flavone (10) and demethoxykanugin (11). This is the first phytochemical investigation of this plant. The structure of compound 1 was elucidated on the basis of spectroscopic data interpretation, including 1D and 2D NMR and HREIMS analysis. The cytotoxicity of 1 against five human cancer cell lines, HL-60, SMMC-7721, A-549, MCF-7 and SW480, was evaluated, but it was inactive (IC50>40μM).

scholarly journals Teratopyrones A–C, Dimeric Naphtho-γ-Pyrones and Other Metabolites from Teratosphaeria sp. AK1128, a Fungal Endophyte of Equisetum arvense

Molecules ◽  
2020 ◽  
Vol 25 (21) ◽  
pp. 5058
Author(s):  
Ya-Ming Xu ◽  
A. Elizabeth Arnold ◽  
Jana M. U′Ren ◽  
Li-Jiang Xuan ◽  
Wen-Qiong Wang ◽  
...  
Keyword(s):  
Human Breast Cancer ◽  
Spectroscopic Data ◽  
Fungal Endophyte ◽  
Small Cell ◽  
Potato Dextrose Agar ◽  
Equisetum Arvense ◽  
Human Breast ◽  
Small Cell Lung ◽  
Bioassay Guided Fractionation ◽  
Mcf 7

Bioassay-guided fractionation of a cytotoxic extract derived from a solid potato dextrose agar (PDA) culture of Teratosphaeria sp. AK1128, a fungal endophyte of Equisetum arvense, afforded three new naphtho-γ-pyrone dimers, teratopyrones A–C (1–3), together with five known naphtho-γ-pyrones, aurasperone B (4), aurasperone C (5), aurasperone F (6), nigerasperone A (7), and fonsecin B (8), and two known diketopiperazines, asperazine (9) and isorugulosuvine (10). The structures of 1–3 were determined on the basis of their spectroscopic data. Cytotoxicity assay revealed that nigerasperone A (7) was moderately active against the cancer cell lines PC-3M (human metastatic prostate cancer), NCI-H460 (human non-small cell lung cancer), SF-268 (human CNS glioma), and MCF-7 (human breast cancer), with IC50s ranging from 2.37 to 4.12 μM while other metabolites exhibited no cytotoxic activity up to a concentration of 5.0 μM.

scholarly journals Mutation analysis of Rad18 in human cancer cell lines and non small cell lung cancer tissues

2009 ◽  
Vol 28 (1) ◽  
pp. 106 ◽  
Author(s):  
Tadahiko Nakamura ◽  
Shinji Ishikawa ◽  
Yoshikatsu Koga ◽  
Youhei Nagai ◽  
Yu Imamura ◽  
...  
Keyword(s):  
Lung Cancer ◽  
Small Cell Lung Cancer ◽  
Cell Lines ◽  
Cancer Cell ◽  
Human Cancer ◽  
Small Cell ◽  
Human Cancer Cell ◽  
Small Cell Lung ◽  
Human Cancer Cell Lines ◽  
Cancer Tissues

scholarly journals Semi-Synthesis and Cytotoxicity Evaluation of Pyrimidine, Thiazole, and Indole Analogues of Argentatins A–C from Guayule (Parthenium Argentatum) Resin

2021 ◽  
Author(s):  
Chandrashekhar Madasu ◽  
Ya-Ming Xu ◽  
E. M. Kithsiri Wijeratne ◽  
Manping X. Liu ◽  
István Molnár ◽  
...  
Keyword(s):  
Human Cancer ◽  
Value Added ◽  
Breast Adenocarcinoma ◽  
Cytotoxic Activities ◽  
Human Cancer Cell Lines ◽  
Potential Applications ◽  
Normal Human ◽  
Indole Analogues ◽  
Mcf 7 ◽  
Value Added Products

Abstract Argentatins A–C (1–3), the major cycloartane-type triterpenoids of guayule resin, a byproduct of commercial rubber production, were converted into their pyrimidine (7–12), thiazole (13–15), and indole (16–18) analogues by a molecular hybridization approach. The cytotoxic activities of these fused heterocyclic analogues 7–18 were compared with those of argentatins A–C (1–3) against a panel of three sentinel human cancer cell lines [NCI-H460 (non-small cell lung), MCF-7 (breast adenocarcinoma), and SF-268 (central nervous system glioma)], and normal human fibroblast (WI-38) cells. The cytotoxicity data suggest that the pyrimidine analogues 7 and 8 (derived from 1), 9 and 10 (derived from 2), and 12 (derived from 3 ) had significantly enhanced activity compared to the parent compounds or their thiazole (13–15) and indole (16–18) analogues. These findings indicate that triterpenoid constituents of guayule resin may be exploited to obtain value-added products with potential applications in anticancer drug discovery.

Novel 1,2,3-Triazole-functionalized pyrido[3',2':4,5]furo[3,2-d]pyrimidin- 4(3H)-one Derivatives: Synthesis, Anticancer Activity, CoMFA and CoMSIA Studies

2020 ◽  
Vol 17 (12) ◽  
pp. 969-978
Author(s):  
Balakishan Vadla ◽  
Sailu Betala
Keyword(s):  
Anticancer Activity ◽  
Cell Line ◽  
Normal Cell ◽  
Rational Design ◽  
Human Cancer ◽  
Strong Basis ◽  
Hek 293 ◽  
Normal Cell Line ◽  
Human Cancer Cell Lines ◽  
Mcf 7

A series of novel triazole functionalized pyrido [3',2':4,5] furo[3,2-d] pyrimidin-4 (3H)-one derivatives 7a-p were prepared from ethyl furo[2,3-b]pyridine-2-carboxylate 3 on reaction with ammonia to afford furo[2,3-b]pyridine-2-carboxamide 4. This compound, on reaction with triethyl orthoformate TEOF, gave compound 5. Compound 5 on propargylation, followed by a reaction with substituted aryl azides under Sharpless reaction conditions, furnished triazole tagged pyrido [3',2':4,5]furo[3,2-d] pyrimidin-4(3H)-one derivatives. All the products 7a-p were screened against four human cancer cell lines, such as HeLa - Cervical cancer (CCL-2), COLO 205- Colon cancer (CCL-222), HepG2- Liver cancer (HB-8065), and MCF7 - Breast cancer (HTB-22) and one normal cell line (HEK 293). Compounds 7b, 7n, 7o and 7p, which showed promising anticancer activity, were identified and found to be non-toxic to normal cell line. Studies for HeLa, COLO205, HepG2, and MCF-7 using CoMFA and CoMSIA were carried out . Models from 3D-QSAR provided a strong basis for future rational design of more active and selective HeLa, COLO205, HepG2, and MCF-7 cell line inhibitors.

scholarly journals Discovery of New Pyrazolopyridine, Furopyridine, and Pyridine Derivatives as CDK2 Inhibitors: Design, Synthesis, Docking Studies, and Anti-Proliferative Activity

Molecules ◽  
2021 ◽  
Vol 26 (13) ◽  
pp. 3923
Author(s):  
Adel A.-H. Abdel-Rahman ◽  
Amira K. F. Shaban ◽  
Ibrahim F. Nassar ◽  
Dina S. EL-Kady ◽  
Nasser S. M. Ismail ◽  
...  
Keyword(s):  
Cell Lines ◽  
Cancer Cell ◽  
Human Cancer ◽  
Cancer Cell Lines ◽  
Human Cancer Cell ◽  
Molecular Docking Study ◽  
Human Cancer Cell Lines ◽  
Hct 116 ◽  
Mcf 7

New pyridine, pyrazoloyridine, and furopyridine derivatives substituted with naphthyl and thienyl moieties were designed and synthesized starting from 6-(naphthalen-2-yl)-2-oxo-4-(thiophen-2-yl)-1,2-dihydropyridine-3-carbonitrile (1). The chloro, methoxy, cholroacetoxy, imidazolyl, azide, and arylamino derivatives were prepared to obtain the pyridine-−C2 functionalized derivatives. The derived pyrazolpyridine-N-glycosides were synthesized via heterocyclization of the C2-thioxopyridine derivative followed by glycosylation using glucose and galactose. The furopyridine derivative 14 and the tricyclic pyrido[3′,2′:4,5]furo[3,2-d]pyrimidine 15 were prepared via heterocyclization of the ester derivative followed by a reaction with formamide. The newly synthesized compounds were evaluated for their ability to in vitro inhibit the CDK2 enzyme. In addition, the cytotoxicity of the compounds was tested against four different human cancer cell lines (HCT-116, MCF-7, HepG2, and A549). The CDK2/cyclin A2 enzyme inhibitory results revealed that pyridone 1, 2-chloro-6-(naphthalen-2-yl)-4-(thiophen-2-yl)nicotinonitrile (4), 6-(naphthalen-2-yl)-4-(thiophen-2-yl)-1H-pyrazolo[3,4-b]pyridin-3-amine (8), S-(3-cyano-6-(naphthaen-2-yl)-4-(thiophen-2-yl)pyridin-2-yl) 2-chloroethanethioate (11), and ethyl 3-amino-6-(naphthalen-2-yl)-4-(thiophen-2-yl)furo[2,3-b]pyridine-2-carboxylate (14) are among the most active inhibitors with IC50 values of 0.57, 0.24, 0.65, 0.50, and 0.93 µM, respectively, compared to roscovitine (IC50 0.394 μM). Most compounds showed significant inhibition on different human cancer cell lines (HCT-116, MCF-7, HepG2, and A549) with IC50 ranges of 31.3–49.0, 19.3–55.5, 22.7–44.8, and 36.8–70.7 μM, respectively compared to doxorubicin (IC50 40.0, 64.8, 24.7 and 58.1 µM, respectively). Furthermore, a molecular docking study suggests that most of the target compounds have a similar binding mode as a reference compound in the active site of the CDK2 enzyme. The structural requirements controlling the CDK2 inhibitory activity were determined through the generation of a statistically significant 2D-QSAR model.

scholarly journals Antioxidants, Phytochemicals, and Cytotoxicity Studies onPhaleria macrocarpa(Scheff.) Boerl Seeds

2014 ◽  
Vol 2014 ◽  
pp. 1-13 ◽  
Author(s):  
Ma Ma Lay ◽  
Saiful Anuar Karsani ◽  
Behrooz Banisalam ◽  
Sadegh Mohajer ◽  
Sri Nurestri Abd Malek
Keyword(s):  
Human Cancer ◽  
Cytotoxic Effects ◽  
Nutritional Values ◽  
Water Fraction ◽  
Human Cancer Cells ◽  
Fiber Protein ◽  
Cytotoxicity Studies ◽  
Normal Human ◽  
Lung Cell Line ◽  
Mcf 7

In recent years, the utilization of certain medicinal plants as therapeutic agents has drastically increased.Phaleria macrocarpa(Scheff.) Boerl is frequently used in traditional medicine. The present investigation was undertaken with the purpose of developing pharmacopoeial standards for this species. Nutritional values such as ash, fiber, protein, fat, and carbohydrate contents were investigated, and phytochemical screenings with different reagents showed the presence of flavonoids, glycosides, saponin glycosides, phenolic compounds, steroids, tannins, and terpenoids. Our results also revealed that the water fraction had the highest antioxidant activity compared to the methanol extract and other fractions. The methanol and the fractionated extracts (hexane, chloroform, ethyl acetate, and water) ofP. macrocarpaseeds were also investigated for their cytotoxic effects on selected human cancer cells lines (MCF-7, HT-29, MDA-MB231, Ca Ski, and SKOV-3) and a normal human fibroblast lung cell line (MRC-5). Information from this study can be applied for future pharmacological and therapeutic evaluations of the species, and may assist in the standardization for quality, purity, and sample identification. To the best of our knowledge, this is the first report on the phytochemical screening and cytotoxic effect of the crude and fractionated extracts ofP. macrocarpaseeds on selected cells lines.

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