METHODS: Samples of leaves, stems, flowers and roots from E. hirta were tested for total phenolic content, and flavonoids content and in vitro antioxidant activity by diphenyl-1-picrylhydrazyl (DPPH) assay and reducing power was measured using cyanoferrate method.
RESULTS: The leaves extract exhibited a maximum DPPH scavenging activity of (72.96±0.78)% followed by the flowers, roots and stems whose scavenging activities were (52.45±0.66)%, (48.59±0.97)%, and (44.42±0.94)%, respectively. The standard butylated hydroxytoluene (BHT) was (75.13±0.75)%. The IC(50) for leaves, flowers, roots, stems and BHT were 0.803, 0.972, 0.989, 1.358 and 0.794 mg/mL, respectively. The reducing power of the leaves extract was comparable with that of ascorbic acid and found to be dose dependent. Leaves extract had the highest total phenolic content [(206.17±1.95) mg GAE/g], followed by flowers, roots and stems extracts which were (117.08±3.10) mg GAE/g, (83.15±1.19) mg GAE/g, and (65.70±1.72) mg GAE/g, respectively. On the other hand, total flavonoids content also from leave had the highest value [(37.970±0.003) mg CEQ/g], followed by flowers, roots and stems extracts which were (35.200±0.002) mg CEQ/g, (24.350±0.006) mg CEQ/g, and (24.120±0.004) mg CEQ/g, respectively. HPTLC bioautography analysis of phenolic and antioxidant substance revealed phenolic compounds. Phytochemical screening of E. hirta leaf extract revealed the presence of reducing sugars, terpenoids, alkaloids, steroids, tannins, flavanoids and phenolic compounds.
CONCLUSIONS: These results suggeste that E. hirta have strong antioxidant potential. Further study is necessary for isolation and characterization of the active antioxidant agents, which can be used to treat various oxidative stress-related diseases.
OBJECTIVES: Based on the multitargeted biological activities approach of ligustrazine based chalcones, in current study 18 synthetic ligustrazine-containing α, β-unsaturated carbonyl-based 1, 3-Diphenyl-2-propen-1-one derivatives were evaluated for their inhibitory effects on growth of five different types of cancer cells.
METHODS: All compounds were evaluated for anticancer effects on various cancer cell lines by propidium iodide fluorescence assay and various other assays were performed for mechanistic studies.
RESULTS: Majority of compounds exhibited strong inhibition of cancer cells especially synthetic compounds 4a and 4b bearing 1-Pyridin-3-yl-ethanone as a ketone moiety in main structural backbone were found most powerful inhibitors of cancer cell growth. Most active 9 compounds among whole series were selected for further studies related to different cancer targets including EGFR TK kinases, tubulin polymerization, KAF and BRAFV600E.
CONCLUSION: Synthetic derivatives including 4a-b and 5a-b showed multitarget approach and showed strong inhibitory effects on EGFR, FAK and BRAF while three compounds including 3e bearing methoxy substitution, 4a and 4b with 1- pyridin-3-yl-ethanone moiety showed the inhibition of tubulin polymerization.
MATERIALS AND METHODS: Total phenolic content (TPC) and ascorbic acid equivalent antioxidant capacity (AEAC) were assessed using the Folin-Ciocalteu and 2,2-diphenyl-1-picrylhydrazyl (DPPH) assays, respectively. Minimum inhibitory dose (MID) against Gram-positive Micrococcus luteus, Staphylococcus aureus, and Bacillus cereus, and Gram-negative. Escherichia coli, Salmonella typhi, and Pseudomonas aeruginosa was assessed using the disc-diffusion method. Teas were extracted with hot water successively three times for one hour each time. The extracts were fractionated using Sephadex LH-20 column chromatography to obtain the NP and PT constituents.
RESULTS: Extraction yields ranged from 12 to 23%. Yields of NP fractions (70-81%) were much higher than those of PT fractions (1-11%), suggesting that the former are the major tea components. Ranking of antioxidant properties of extracts was green tea>black tea>herbal tea. For all six teas, antioxidant properties of PT fractions were significantly higher than extracts and NP fractions. Extracts and fractions of all six teas showed no activity against the three Gram-negative bacteria. Green teas inhibited all three Gram-positive bacteria with S. aureus being the least susceptible. Black and herbal teas inhibited the growth of M. luteus and B. cereus, but not S. aureus. The most potent were the PT fractions of Boh Cameron Highlands and Ho Yan Hor with MID of 0.01 and 0.03 mg/disc against M. luteus.
CONCLUSION: Results suggested that NP constituents are major contributors to the antioxidant and antibacterial properties of teas of C. sinensis. Although PT constituents have stronger antioxidant and antibacterial properties, they constitute only a minor component of the teas.