ABSTRACT
Evaluation of antioxidant and anticancer activities were screened by various Saururus chinensis root extracts. Four solvents (ethyl acetate, methanol, ethanol, and water) extracts were investigated for their total flavonoids, phenol contents and their antioxidant activity of DPPH (2,2-diphenyl-1-picrylhydrazyl), NO (nitric oxide), H2O2 (hydrogen peroxide), ABTS 2,2'-azino-bis(3-ethylbenzothiazoline-6-sulfonicacid)diammonium assays, FRAP (ferric reducing ability of plasma) assays and anticancer activity. The total phenolic and flavonoid content of extracts were determined by using FC (Folin-Ciocalteu) and AlCl3 colorimetric assay method. Total flavonoid content in these plants ranged from 24.7 to 72.1 mg g-1 and amount of free phenolic compounds was between 11.2 and 67.1 mg g-1 extract. The all extracts have significant levels of phenolics and flavonoids content. Anticancer activity was screened for MCF-7 breast cancer cell line. Ethanol extract shows significant of antioxidant activity and water extract shows significant of anticancer activity compared with standard (BHT) butylated hydroxy toluene. These ethanol and water extracts could be considered as a natural source for using antioxidant, and anticancer agents compared to commercial available synthetic drugs.
ABSTRACT
A new series of 1,4-dihydropyridine derivatives (2a-h, 3a-e, and 4a-e) were systematically designed and synthesized via ultrasound irradiation methods with easy work-up and good yields. Compounds structures were confirmed by IR, 1H NMR, 13C NMR, and mass spectra. The synthesized compounds were screened for both antimicrobial and anticoagulant activities. Compound 2e (MIC: 0.25⯵g/mL) was highly active against Escherichia coli and compound 2c (MIC: 0.5⯵g/mL) was also highly active against Pseudomonas aeruginosa compared with ciprofloxacin. (MIC: 1⯵g/mL) The antifungal activity of 2c (MIC: 0.5⯵g/mL) against Candida albicans was high relative to that of clotrimazole (MIC: 1⯵g/mL). Anticoagulant activity was determined by activated partial thromboplastin time (APTT) and prothrombin time (PT) coagulation assays. Compound 4-(4-hydroxyphenyl)-2,6-dimethyl-N3,N5-bis(5-phenyl-1,3,4-thiadiazol-2-yl)-1,4-dihydropyridine-3,5-dicarboxamide 3d (>1000â¯s in APTT assays) was highly active in anticoagulant screening compared with the reference of heparin. Cytotoxicity was evaluated using HepG2 (liver), HeLa (cervical), and MCF-7 (breast) cancer cell lines, with high toxicities observed for 2c (GI50â¯=â¯0.02⯵m) against HeLa cell line and 2e (GI50â¯=â¯0.03⯵m) equipotant against MCF-7 cell line. Therefore, the compounds 2e, 2c and 3d can serve as lead molecules for the development of new classes of antimicrobial and anticoagulant agent.
ABSTRACT
A simple and convenient one-pot four-component synthesis of morpholine-connected pyrazolidine derivatives 2a-f and 4a-f was developed using direct metal-free catalysis, with the identities of the synthesized compounds confirmed by IR, NMR (1H and 13C), mass spectrometry, and elemental analysis. The prepared compounds were inspected for antimicrobial, antioxidant, and cytotoxic activities. Antimicrobial and antifungal activities against five bacterial and four fungal pathogens, respectively, were investigated using the disc diffusion technique. In antibacterial activity, compounds 2d and 2f (MIC=2µg/mL) exhibited significantly higher activity than the standard ciprofloxacin. The results of antifungal assay showed that the activity of compound 4a (MIC=0.5µg/mL) was significantly higher than the standard clotrimazole. Antioxidant activity was screened based on ABTS+ radical scavenging and linoleic acid peroxidation performance. Compound 4a showed substantial antioxidant (91.3%) activities, as compared with the Trolox standard. Cytotoxicity was evaluated using HepG2 (liver), HeLa (cervical), and MCF-7 (breast) cancer cell lines, with high toxicities observed for 2b (GI50=12.2µm) and 4a (GI50=07.8µm).
