Synthesis of Novel 5-Substituted Phenyl-3-(P-Isopropylpheny1)-1-Phenylformazan and Their Biological Activities

Novel 1-substituted 3-(p-isopropylphenyl)-5-phenylformazans (3a-g) were synthesized and characterized by elemental analysis, H-1 NMR, and FT-IR techniques and UV-visible spectroscopy. Antiproliferative activities of 3a-g against HeLa and C6 cells were determined using the BrdU cell proliferation ELISA assay. 5-Florouracil was used as the positive control. The effects of substituents (-H, -CH3, and A) and their positions (ortho, meta, and para) on the antiproliferative activities were evaluated. The results of the assay indicate that I substituent exhibited higher activity against the cells at the meta and para positions than -CH3 and -H substituents. 3a-g exhibited both high antiproliferative activities against C6 cells and noncytotoxicity. 3a-g may be anticancer drug candidates.Wo

Phytochemical Content of Centaurea polypodiifolia boiss. var. polypodiifolia

Various solvents including hexane, CHCl3, EtOAc, and MeOH were used to extract the aerial parts of C. polypodiifolia Boiss. var. polypodiifolia. Hexane extract was analyzed by GC-MS and nonacosane and octacosane were determined as the main constituents. HPLC-TOF/MS analyses were carried out on CHCl3, EtOAc, and MeOH extracts. The main constituents of CHCl3 extract were detected as 4-hydroxybenzoic acid, vanilic acid, and gentisic acid. Gentisic acid, fumaric acid, chlorogenic acid, and vanilic acid were determined as the main compounds of EtOAc extract. Finally, main constituents of MeOH extract were found as fumaric acid, chlorogenic acid, quercetin-3-β-D-glucoside, gentisic acid and diosmin

Antimicrobial Activity of Essential Oil Components and Antiproliferative Activity of Trans-Tiliroside Compound from an Endemic Desert Species Thymelaea microphylla Coss. et Dur

ABSTRACT Essential oil components of the aerial parts of Thymelaea microphylla was subjected to evaluate the antimicrobial activity by disc diffusion method and tested against Gram-positive and Gram-negative bacteria and showed a high antibacterial activity against E.coli and Staphylococcus aureus at 2000μg /ml. The antiproliferative activity of fractio

Phytochemical analysis, antiproliferative and antioxidant activities of Chrozophora tinctoria: a natural dye plant

Context: Chrozophora tinctoria (L.) A. Juss. (Euphorbiaceae) is known as ‘dyer’s-croton’ and used to obtain dye substances. Recently, natural antioxidants and colorants have been of interest because of their safety and therapeutic effects. Objective: This study investigates the antiproliferative and antioxidant activities of the various extracts and fractions from C. tinctoria and analyzes their phytochemical contents. Materials and methods: The aerial parts of C. tinctoria were extracted with water, ethyl acetate, n-butanol, and methanol/chloroform. Phenolic compounds and other constituents of the extracts were analyzed by HPLC/TOF-MS. The ethyl acetate extract (EA) was fractionated by flash chromatography. The extracts, fractions, and major phenolic compounds were investigated for their antiproliferative activities on human cervical adenocarcinoma (HeLa) cell line at the concentrations of 5–100 μg/mL by using BrdU ELISA assay during 24 h of incubation. DPPH radical scavenging activities (5–150 μg/mL) and total phenolic contents of the samples were also evaluated. Results: 4-Hydroxybenzoic acid (268.20 mg/kg), apigenin-7-glucoside (133.34 mg/kg), and gallic acid (68.92 mg/kg) were the major components of EA. CT/E-F6 (IC50 = 64.59 ± 0.01 μg/mL) exhibited the highest antiproliferative activity. CT/E-F2 (IC50= 14.0 ± 0.0 μg/mL) and some fractions displayed higher radical scavenging activity compared to synthetic antioxidant BHT (IC50 = 23.1 ± 0.0 μg/mL). Among the main phenolics, gallic acid exhibited the highest antiproliferative and radical scavenging abilities (IC50 < 5 μg/mL). Conclusion: In this study, we have determined the biologically active fractions and their high effects may be attributed to the presence of gallic acid

Synthesis and biological evaluation of novel urea, thiourea and squaramide diastereomers possessing sugar backbone

Bulut, Adnan/0000-0001-9322-0325WOS:000537685900004PubMed: 32259705A series of novel chiral 14 urea, thiourea and squaramide stereoisomers possessing carbohydrate backbones as well as amide functional groups was synthesized and characterized by their, H-1 NMR, C-13 NMR, FT-IR, HRMS, optical rotation, and melting points. Their antiproliferative activities were investigated against HeLa and PC3 cell lines. The compounds 9, 11 and 12 showed better activities at 25 mu M against PC3 cell line with respect to the standard 5-fluorouracil (5-FU). Especially, the compounds 9 and 11 showed higher activities than the standard 5-FU even at low concentration (5 mu M) against HeLa cell line. IC50 results also confirm these activities. The compounds 9, 10 and 11 have the IC50 values of 1.10 mu M, 1.51 mu M and 1.02 mu M, respectively while 5-FU has 2.51 mu M. Moreover, their cytotoxicity tests have proven that their viabilities were in between 50% and 100%.Scientific Research Projects Coordination Unit of Kirikkale UniversityKirikkale University [2017/060]This work was supported by Scientific Research Projects Coordination Unit of Kirikkale University. Project number: 2017/060

Phytochemical analysis, antiproliferative and antioxidant activities of Chrozophora tinctoria: a natural dye plant

Context: Chrozophora tinctoria (L.) A. Juss. (Euphorbiaceae) is known as `dyer's-croton' and used to obtain dye substances. Recently, natural antioxidants and colorants have been of interest because of their safety and therapeutic effects. Objective: This study investigates the antiproliferative and antioxidant activities of the various extracts and fractions from C. tinctoria and analyzes their phytochemical contents. Materials and methods: The aerial parts of C. tinctoria were extracted with water, ethyl acetate, n-butanol, and methanol/chloroform. Phenolic compounds and other constituents of the extracts were analyzed by HPLC/TOF-MS. The ethyl acetate extract (EA) was fractionated by flash chromatography. The extracts, fractions, and major phenolic compounds were investigated for their antiproliferative activities on human cervical adenocarcinoma (HeLa) cell line at the concentrations of 5-100 mu g/mL by using BrdU ELISA assay during 24 h of incubation. DPPH radical scavenging activities (5-150 mu g/mL) and total phenolic contents of the samples were also evaluated. Results: 4-Hydroxybenzoic acid (268.20 mg/kg), apigenin-7-glucoside (133.34 mg/kg), and gallic acid (68.92 mg/kg) were the major components of EA. CT/E-F6 (IC50 = 64.59 +/- 0.01 mu g/mL) exhibited the highest antiproliferative activity. CT/E-F2 (IC50 = 14.0 +/- 0.0 mu g/mL) and some fractions displayed higher radical scavenging activity compared to synthetic antioxidant BHT (IC50 = 23.1 +/- 0.0 mu g/mL). Among the main phenolics, gallic acid exhibited the highest antiproliferative and radical scavenging abilities (IC50< 5 mu g/mL). Conclusion: In this study, we have determined the biologically active fractions and their high effects may be attributed to the presence of gallic acid

Antiproliferative and Antioxidant Activities of Two Extracts of the Plant Species Euphorbia dendroides L.

Background: These days, the desire for naturally occurring antioxidants has significantly increased, especially for use in foodstuffs, cosmetics, and pharmaceutical products, to replace synthetic antioxidants that are regularly constrained due to their carcinogenicity. Methods: The study in hand aimed to appraise the antioxidant effect of two Euphorbia dendroides extracts using reducing power, anti-peroxidation, and DPPH (1,1 Diphenyl 2 Pycril Hydrazil) scavenging essays, in addition to the anticancer activity against two tumor cell lines, namely C6 (rat brain tumor)cells, and Hela (human uterus carcinoma)cell lines. Results: The results indicated that the ethyl acetate extract exhibited antiradical activity of 29.49%, higher than that of n-butanol extract (18.06%) at 100 &micro;g/mL but much lower than that of gallic acid (78.21%).The ethyl acetate extract exhibits better reducing capacity and lipid peroxidation inhibitory activity compared to n-butanol extract but less than all tested standards. Moreover, the ethyl acetate extract was found to have an antiproliferative activity of more than 5-FU (5-fluoro-Uracil) against C6 cells at 250 &micro;g/mL with IC50 and IC75 of 113.97, 119.49 &micro;g/mL, respectively, and good cytotoxic activity against the Hela cell lines at the same concentration. The HPLC-TOF-MS (high performance liquid chromatography-Time-of-flight-Mass Spectrometry) analyses exposed the presence of various compounds, among which Gallic and Chlorogenic acids functioned as major compounds. Conclusions: The two extracts exhibited moderate anticancer abilities and behaved somewhat as average antioxidant agents. Based on the total phenolics and flavonoids contents, as well as HPLC results, it could be concluded that antiproliferative and antioxidant activities depend upon the content of different phenolics and flavonoids

Chemical constituents, in vitro antioxidant and antiproliferative activities of Perralderia coronopifolia Coss. subsp. eu-coronopifolia M. var. typica M. extract

Phytochemical investigations of extracts from the aerial parts (leaves and flowers) of Perralderia coronopifolia Cosson resulted in the isolation of nine secondary metabolites corresponding to three flavonoids: rhamnazin, chrysosplenol D, and (2R, 3R) taxifolin, two monoterpene glycosides: myrtenol- β-Dglucopyranoside- 6'-O-acetate and myrtenol β-D-glucopyranoside, a disaccharide: sucrose and three di-Ocaffeoylquinic acid derivatives : methyl 3, 5-di-O-caffeoyl quinate and methyl 3,4-di-O-caffeoyl quinate as a mixture and 1,5-di-O-caffeoylquinic acid. The structures were identified by spectroscopic methods such as 1H and 13C NMR, COSY, HSQC and HMBC experiments, HRESI-MS and comparison with literature data. Myrtenol-β-Dglucopyranoside-6'-O-acetate was isolated in pure and native state for the first time. The other compounds are new for the genus Perralderia Cosson. The ethyl acetate extract showed a high antioxidant effect, especially DPPH radical scavenging activity with IC50=7.01±0.28µg/mL) compared to ascorbic acid (IC50= 5±0.1µg/mL. This extract also showed antiproliferative activity against HeLa (human cervix carcinoma) and C6 (rat brain tumor) cells.Peer Reviewe