Biological Evaluation of Curcumin and Related Diarylheptanoids

2006 ◽  
Vol 61 (9-10) ◽  
pp. 625-631 ◽  
Author(s):  
Faridah Abas ◽  
Lim Siang Hui ◽  
Syahida Ahmad ◽  
Johnson Stanslas ◽  
D. A. Israf ◽  
...  
Keyword(s):  
Free Radical ◽  
Cell Line ◽  
Cancer Cell ◽  
Radical Scavenging Activity ◽  
Radical Scavenging ◽  
Cancer Cell Line ◽  
Biological Evaluation ◽  
Free Radical Scavenging ◽  
Lung Cancer Cell Line ◽  
Cytotoxic Activities

AbstractNine derivatives of three natural diarylheptanoids, curcumin, demethoxycurcumin and bisdemethoxycurcumin, were prepared. Their antioxidant, free radical scavenging, nitric oxide (NO) inhibitory and cytotoxic activities were evaluated and compared with those of the respective natural compounds. Curcumin (1), demethoxycurcumin (2), demethyldemethoxycurcumin (C3), diacetyldemethoxycurcumin (AC2) and triacetyldemethylcurcumin (AC5) exhibited higher antioxidant activity than quercetin while products from demethylation of 1 and 2 exhibited higher free radical scavenging activity. Compounds AC2 and AC5 were found to be most active in inhibiting breast cancer cells (MCF-7) proliferation with IC50 values of 6.7 and 3.6 μм, respectively. The activity of AC2 is almost doubled and of AC5 almost tripled as compared to curcumin. Their selectivity towards different cell lines is also more noticeable. Compounds AC2 and AC5 also showed increased activity against a human prostate cancer cell line (DU-145) and non-small lung cancer cell line (NCI-H460) with IC50 values of 20.4, 16.3 and 18.3, 10.7 μм, respectively.

scholarly journals Two New Cyclobutane Dimers from Diospyros macrocarpa

2017 ◽  
Vol 12 (8) ◽  
pp. 1934578X1701200
Author(s):  
Charlotte Thieury ◽  
Rémy Le Guével ◽  
Gaëtan Herbette ◽  
Valérie Monnier ◽  
Nicolas Lebouvier ◽  
...  
Keyword(s):  
Cancer Cell ◽  
New Caledonia ◽  
Radical Scavenging Activity ◽  
Radical Scavenging ◽  
Cancer Cell Line ◽  
Cytotoxic Activities ◽  
Endemic Plant ◽  
Leaf Extracts ◽  
Phytochemical Study ◽  
Cyclobutane Dimers

A biochemical and phytochemical study of Diospyros macrocarpa Hiern, an endemic plant of New Caledonia, was realized. Indeed, bark and leaf extracts were tested for their cytotoxic and antibiotic activities as well as for their radical scavenging properties. Methanol extracts showed promising radical scavenging activity with an IC50 value of 5.6 ± 0.9 μg/mL for the leaves and 8.1 ± 1.4 μg/mL for the barks. The ethyl acetate extract from the barks showed strong and selective activity against NCI-H727 cancer cell line with an IC50 value of 9.5 ± 0.6 μg/mL.. Two new cyclobutane dimers: macrocarpasin A (1) and B (2) (figure 1) together with six known compounds: yangonin (3), betulinic acid (4), α-amyrin (5), β–amyrin (6), loliolide (7) and oleanderolide (8) were isolated from leaf extracts. Their structures were established by 1D and 2D NMR along with HRMS analyses. Cytotoxic activities of isolated compounds were also evaluated. None of them showed interesting cytotoxicity against the seven tested cancer cell lines.

Development and Biological Evaluation of Imidazothiazole propenones as Tubulin Inhibitors that Effectively Triggered Apoptotic Cell Death in Alveolar Lung Cancer Cell Line

2017 ◽  
Vol 2 (22) ◽  
pp. 6480-6487 ◽  
Author(s):  
Ibrahim Bin Sayeed ◽  
Koteswara Rao Garikapati ◽  
Venkata Krishna Kanth Makani ◽  
Apoorva Nagarajan ◽  
Mohd Adil Shareef ◽  
...  
Keyword(s):  
Lung Cancer ◽  
Cell Death ◽  
Cell Line ◽  
Cancer Cell ◽  
Apoptotic Cell ◽  
Cancer Cell Line ◽  
Biological Evaluation ◽  
Lung Cancer Cell Line ◽  
Lung Cancer Cell ◽  
Tubulin Inhibitors

scholarly journals Antioxidant, Membrane Stabilizing and Cytotoxic Activities of Cissus adnata (Roxb.)

2016 ◽  
Vol 15 (1) ◽  
pp. 69-71 ◽  
Author(s):  
Ridwan Bin Rashid ◽  
Farhan Nur Towsif ◽  
Farhana Ahmed Bushra ◽  
Faiza Tahia
Keyword(s):  
Free Radical ◽  
Soluble Fraction ◽  
Radical Scavenging Activity ◽  
Radical Scavenging ◽  
Free Radical Scavenging ◽  
Cytotoxic Activities ◽  
Hypotonic Solution ◽  
Lc50 Value ◽  
Whole Plant ◽  
Vincristine Sulphate

The methanol extracts of whole plant of Cissus adnata (Roxb.) and their organic and aqueous soluble partitioning materials were evaluated for antioxidant, cytotoxic and membrane stabilizing properties. In the DPPH free radical scavenging assay, the aqueous extract of whole plant of C. adnata displayed the highest free radical scavenging activity with IC50 value of 4.17 ?g/ml, while the pet ether soluble fraction showed significant lethality to brine shrimps having LC50 value of 1.02 ?g/ml, as compared to the standard vincristine sulphate (LC50 value of 0.44 ?g/ml). In the evaluation for membrane stabilizing property, the pet ether soluble fraction of methanol extract of the whole plant inhibited 67.43 % and 56.60 % hypotonic solution- and heat-induced haemolysis of RBCs, respectively.Dhaka Univ. J. Pharm. Sci. 15(1): 69-71, 2016 (June)

The anticancer and free radical scavenging potential of the Unani medicine Agaricus albus L.

2021 ◽  
Vol 0 (0) ◽  
Author(s):  
Mohd Nazir Mannan ◽  
Mohammad Zakir ◽  
Tasleem Ahmad ◽  
Kuna Lahari ◽  
Munawwar Husain Kazmi
Keyword(s):  
Free Radical ◽  
Cell Line ◽  
Cytotoxic Effect ◽  
Radical Scavenging Activity ◽  
Antioxidant Properties ◽  
Radical Scavenging ◽  
Free Radical Scavenging ◽  
Breast Cancer Cell Lines ◽  
Unani Medicine ◽  
Mcf 7

Abstract Objectives Traditional Unani medicine plays a major role in maintaining health in developing countries. For ages, Unani physicians have described many Classical Unani Formulations (CUF) for their anti-cancerous action (Dāfiʻ-i-saraṭān) in the human population. These formulations contain various individual drugs which also have anticancer activity. The present study was designed to screen and compare cytotoxic and antioxidant properties of different extracts of Agaricus albus L. (A. albus), a drug used in the Unani system of medicine on human breast cancer cell lines (MCF-7). Methods Cytotoxic effect was assessed using MTT assay kit and free radical scavenging activity was done by using DPPH assay. Aqueous, hydro-ethanol and methanolic extracts were used at different concentrations. Results All extracts were shown good antioxidant and cytotoxic activity. Among all extracts, maximum cytotoxic effect was observed in methanolic extract and aqueous extract at the concentration of 1,000 μg against MCF-7 cell line in comparison to paclitaxel. The maximum antioxidant activity was observed in the hydroethanolic extract at the concentration of 1,000 μg against the MCF-7 cell line in comparison to ascorbic acid. Conclusions The present study advocates, the anticancer and antioxidant property of A. albus and suggests that this drug may be used as a potential drug for cancer treatment after a successful and detailed preclinical study and clinical trial.

scholarly journals Synthesis, Biological Evaluation and Docking Study of Etodolac-Triazole Conjugate

2020 ◽  
pp. 35-51
Author(s):  
Papigani Neeraja ◽  
Suryapeta Srinivas ◽  
Venkanna Banothu ◽  
Khagga Mukkanti ◽  
Pramod Kumar Dubey ◽  
...  
Keyword(s):  
Cell Line ◽  
Cancer Cell ◽  
Cancer Cell Line ◽  
Triazole Ring ◽  
Docking Study ◽  
Biological Evaluation ◽  
Lung Cancer Cell Line ◽  
Human Lung Cancer ◽  
High Yield ◽  
Diffusion Method

A new set of 15 compounds containing etodolac moiety and triazole ring were prepared by CuAAC reaction in moderate to high yield. All the synthesized compounds were purified by chromatographic techniques and characterized by spectral data IR, 1H and 13C NMR and mass spectrometry. The newly derived compounds were screened for their anti-bacterial activities against one gram-positive (S. aureus) and two gram-negative (E. coli, K. pneumoniae) bacteria using an agar-well diffusion method. Most of the compounds showed good to moderate antibacterial activities. Especially compound 4e having good activities against all the strains. The compound 4e displayed significant inhibitory potential with MIC 25 µg/mL against all the strains. The potential DNA gyrase inhibitory activity of this compound was investigated by using molecular docking studies carried out using Autodock Vina software. The compound 4e showed the lowest ΔGbind results (-7.7 Kcal/mol, -7.9Kcal/mol). The cytotoxic activity of the obtained compounds was determined using A549 cancer cell line by a MTT assay. They displayed promising activity against the human lung cancer cell line. Especially 4o, 4b, 4d shown lowest IC50 values.

scholarly journals Synthesis of Analogues of Dicoumarol and Their Biological Evaluation

2018 ◽  
Vol 10 (3) ◽  
pp. 1 ◽  
Author(s):  
Julie Obi ◽  
Tagbo Ezenwa
Keyword(s):  
Lung Cancer ◽  
Cell Line ◽  
Cancer Cell ◽  
Cancer Cell Line ◽  
Biological Evaluation ◽  
Lung Cancer Cell Line ◽  
Lung Cancer Cell ◽  
Inhibitory Potency ◽  
One Pot ◽  
Microwave Assisted

Both symmetrical (1a-f) and asymmetrical (2a-f) analogues of dicoumarol were synthesized in 20 – 86% yield by using microwave assisted one-pot protocol. Their ability to inhibit NAD (P)H:oxidorectase quinone 1 (NQO1) and cytotoxicity towards A549 small lung cancer cell line were evaluated. Interestingly, (E)-3-(2-hydroxynaphthalen-1-y)chroman-2,4-dione (2d) showed not only moderate inhibitory potency (IC50 = 20 ± 6 nM) towards NQO1 but also was toxic (IC50 = 9.2 ± 0.2 µM) towards the A549 small lung cancer cell line.

scholarly journals LC-ToF-ESI-MS Patterns of Hirsutinolide-like Sesquiterpenoids Present in the Elephantopus mollis Kunth Extract and Chemophenetic Significance of Its Chemical Constituents

Molecules ◽  
2021 ◽  
Vol 26 (16) ◽  
pp. 4810
Author(s):  
Gabin Thierry M. Bitchagno ◽  
Jean Garba Koffi ◽  
Ingrid Konga Simo ◽  
Donald Ulrich K. Kagho ◽  
Augustin Silvere Ngouela ◽  
...  
Keyword(s):  
Cell Line ◽  
Cancer Cell ◽  
Chemical Constituents ◽  
Radical Scavenging Activity ◽  
Sesquiterpene Lactones ◽  
Radical Scavenging ◽  
Cancer Cell Line ◽  
Flash Chromatography ◽  
Ongoing Research ◽  
Esi Ms

A total of nine sesquiterpenoid lactones together with phenolic compounds and other terpenes were identified from the crude methanol extract of Elephantopus mollis Kunth. Compounds were isolated using different chromatographic techniques and their structures were determined by NMR and IR spectroscopy as well as mass spectrometry. The structures of some detected compounds were assigned based on LC-ToF-ESI-MS screening of main fractions/subfractions from flash chromatography and comparison with isolated analogues as standards. The findings revealed not only the in-source loss of water as the base peak in hirsutinolides but also the in-source loss of corresponding alcohol when the oxygen at position 1 is alkylated. The present study also draws up a complement of data with respect to hirsutinolide-like sesquiterpene lactones whose LC-MS characteristics are not available in the literature. The chemophenetic significance is also discussed. Some of the isolated compounds were reported for the first time to be found in the species, the genus as well as the plant family. The medium-polar fractions of the crude extract, also containing the larger amount of sesquiterpenoid lactones, exhibited activity both against a cancer cell line and bacterial strains. Isolated lactones were also active against the cancer cell line, while the chlorogenic derivatives also valuable in Elephantopus genus showed potent radical scavenging activity. This is the first report of cytotoxic and antibacterial activities of our samples against the tested strains and cell line. The present study follows the ongoing research project dealing with the characterization of taxa with antibacterial and antiparasitic activities from Cameroonian pharmacopeia.

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