3 research outputs found
Antioxidant Activity, Total Phenolic and Flavonoid Content and LC–MS Profiling of Leaves Extracts of Alstonia angustiloba
No full textPlants have a wide range of active compounds crucial in treating various diseases. Most people consume plants and herbals as an alternative medicine to improve their health and abilities. A. angustiloba extract showed antinematodal activity against Bursaphelenchus xylophilus, antitrypanosomal action against Trypanosoma brucei and anti-plasmodial activity against the chloroquine-resistant Plasmodium falciparum K1 strain. Moreover, it has demonstrated growth inhibitory properties towards several human cancer cell lines, such as MDA-MB-231, SKOV-3, HeLa, KB cells and A431. DPPH and ABTS assays were carried out to determine the antioxidant activity of the aqueous and 60% methanolic extract of A. angustiloba leaves. Moreover, total phenolic and flavonoid contents were quantified. The presence of potential active compounds was then screened using liquid chromatography coupled with a Q-TOF mass spectrometer (LC–MS) equipped with a dual electrospray ionisation (ESI) source. The EC50 values measured by DPPH for the 60% methanolic and aqueous extracts of A. angustiloba leaves were 80.38 and 94.11 µg/mL, respectively, and for the ABTS assays were 85.80 and 115.43 µg/mL, respectively. The 60% methanolic extract exhibited the highest value of total phenolic and total flavonoid (382.53 ± 15.00 mg GAE/g and 23.45 ± 1.04 mg QE/g), while the aqueous extract had the least value (301.17 ± 3.49 mg GAE/g and 9.73 ± 1.76 mg QE/g). The LC–MS analysis revealed the presence of 103 and 140 compounds in the aqueous and 60% methanolic extract, respectively. It consists of phenolic acids, flavonoids, alkaloids, amino acids, glycosides, alkaloids, etc. It can be concluded that the therapeutic action of this plant is derived from the presence of various active compounds; however, further research is necessary to determine its efficacy in treating diseases
Synthesis, characterization, cytotoxicity evaluation and molecular docking study of new bis-chalcone, fused-pyrimidine and fused-pyrazoline derivatives
No full text251-264Chemotherapeutic drug resistance and high-risk side effects are common limitations in cancer treatment. Thus, the
continuous development of new drugs that target only the cancer cell without affecting the normal cells is needed. The simple
structure of the chalcone and the ease of its synthesis showed promising functions. Such compounds have been reported to
exhibit diverse pharmacological activities, particularly anticancer. This study involves the design of chalcones 1 and 2 which
have been synthesized via Claisen-Schmidt condensation. Further cyclo-condensation reactions of these chalcone compounds
has formed five pyrazoline and three pyrimidine derivatives. All the desired derivatives are characterised by FT-IR, 1H-NMR,
and 13C-NMR. These derivatives are tested for cytotoxicity against breast cancer cell lines (MCF-7 and MD-MB-231) and
normal breast cell lines (MCF-10A). The results emphasized that pyrazoline compounds 1Aii and 1Aiii are showing the
minimum inhibition against MCF-7 with the IC50 values of56.73±3.3 μM and 37.74±1.32 μM, respectively, after 24 h of
exposure, which are comparable to Tamoxifen, as reference anticancer drug (IC50 = 42.66±2.19 μM)
Synthesis, characterization, cytotoxicity evaluation and molecular docking study of new bis-chalcone, fused-pyrimidine and fused-pyrazoline derivatives
Get PDFChemotherapeutic drug resistance and high-risk side effects are common limitations in cancer treatment. Thus, the continuous development of new drugs that target only the cancer cell without affecting the normal cells is needed. The simple structure of the chalcone and the ease of its synthesis showed promising functions. Such compounds have been reported to exhibit diverse pharmacological activities, particularly anticancer. This study involves the design of chalcones 1 and 2 which have been synthesized via Claisen-Schmidt condensation. Further cyclo-condensation reactions of these chalcone compounds has formed five pyrazoline and three pyrimidine derivatives. All the desired derivatives are characterised by FT-IR, 1H-NMR, and 13C-NMR. These derivatives are tested for cytotoxicity against breast cancer cell lines (MCF-7 and MD-MB-231) and normal breast cell lines (MCF-10A). The results emphasized that pyrazoline compounds 1Aii and 1Aiii are showing the minimum inhibition against MCF-7 with the IC50 values of56.73±3.3 µM and 37.74±1.32 µM, respectively, after 24 h of exposure, which are comparable to Tamoxifen, as reference anticancer drug (IC50 = 42.66±2.19 µM)
