Extraction and Isolation of Phenolic compounds from Sweet lime and Evaluation of Anticancer potentiality followed by Molecular docking against Topoisomerase II

The main aim and objective of the present research work was the isolation of some novel bioflavanoids from methanolic extract of peels of sweet lime (MEE-PSWL) and evaluation of in vitro anticancer activity followed by molecular docking against target protein topoisomerase II. The extraction was done by reflux condensation method and preliminary phytochemical screening of MEE-PSWL was carried out for the evaluation of bioactive molecules, the bioflavanoids present in MEE-PSWL was confirmed by spectral analysis such as ESI-MS-MS and FTIR. Molecular docking of isolated compounds was carried out against target protein Topoisomerase II with PDB id 1ZXM by Auto dock program and the best dock pose was selected based on the interaction study analysis. In vitro anticancer activity MEE-PSWL was evaluated by SRB assay toward human colon adenocarcinoma cell line SW620 and the test was carried out at different concentrations. A preliminary screening displayed that the MEE-PSWL was able to inhibit the proliferation of more than 60% of human colon adenocarcinoma SW620 cells. The maximum growth of inhibition was found to be at 125µg/ml (IC50 4.5µg/ml) and the standard drug doxorubicin was found to inhibit the maximum proliferation at concentration 75µg/ml (IC50 3µg/ml).

STRUCTURAL AND BIOLOGICAL CHARACTERISTICS OF SELF-ORGANISING CHITOSAN HYDROGELS

Creating innovative methods of treatment and regeneration of damaged tissues or organs is a key challenge of the twenty-first century. The aim of this study was to determine the possibility of producing and characterising the properties of self-organising chitosan hydrogels prepared with the use of chitosan lactate/chloride and disodium hydrogen phosphate dodecahydrate as a cross-linking agent. The structure and supramolecular architecture of the biomaterials were evaluated by Fourier-transform infrared spectroscopy and polarised optical microscopy. Biological studies assessed cytotoxicity by contact with a human colon adenocarcinoma cell line. The colourimetric resazurin assay showed that the obtained chitosan hydrogels are non-cytotoxic materials. Thus, self-organising biomaterialshold great promise for application in tissue engineering.

New Hybrids Based on Curcumin and Resveratrol: Synthesis, Cytotoxicity and Antiproliferative Activity against Colorectal Cancer Cells

We synthesized twelve hybrids based on curcumin and resveratrol, and their structures were elucidated by spectroscopic analysis. The chemopreventive potential of these compounds was evaluated against SW480 human colon adenocarcinoma cells, its metastatic derivative SW620, along with the non-malignant CHO-K1 cell line. Among the tested compounds, hybrids 3e and 3i (for SW480) and 3a, 3e and 3k (for SW620) displayed the best cytotoxic activity with IC50 values ranging from 11.52 ± 2.78 to 29.33 ± 4.73 µM for both cell lines, with selectivity indices (SI) higher than 1, after 48 h of treatment. Selectivity indices were even higher than those reported for the reference drug, 5-fluorouracil (SI = 0.96), the starting compound resveratrol (SI = 0.45) and the equimolar mixture of curcumin plus resveratrol (SI = 0.77). The previous hybrids showed good antiproliferative activity.

Triterpenes and Phenolic Compounds from the Fungus Fuscoporia torulosa: Isolation, Structure Determination, and Biological Activity

Investigation of the methanol extract of the poroid fungus Fuscoporia torulosa resulted in the isolation of a novel triterpene, fuscoporic acid (1), together with inoscavin A and its previously undescribed Z isomer (2 and 3), 3,4-dihydroxy-benzaldehide (4), osmundacetone (5), senexdiolic acid (6), natalic acid (7), and ergosta-7,22-diene-3-one (8). The structures of fungal compounds were determined on the basis of NMR and MS spectroscopic analyses, as well as molecular modeling studies. Compounds 1, 6–8 were examined for their antibacterial properties on resistant clinical isolates, and cytotoxic activity on human colon adenocarcinoma cell lines. Compound 8 was effective against Colo 205 (IC50 11.65 ± 1.67 µM), Colo 320 (IC50 8.43 ± 1.1 µM) and MRC-5 (IC50 7.92 ± 1.42 µM) cell lines. Potentially synergistic relationship was investigated between 8 and doxorubicin, which revealed a synergism between the examined compounds with a combination index (CI) at the 50% growth inhibition dose (ED50) of 0.521 ± 0.15. Several compounds (1 and 6–8) were tested for P-glycoprotein modulatory effect in Colo 320 resistant cancer cells, but none of the compounds proved to be effective in this assay. Fungal metabolites 2–5 were evaluated for their antioxidant activity using the oxygen radical absorbance capacity (ORAC) and DPPH assays. Compounds 4 and 5 were found to have a considerable antioxidant effect with EC50 0.25 ± 0.01 (DPPH) and 12.20 ± 0.92 mmol TE/g (ORAC). The current article provides valuable information on both the chemical and pharmacological profiles of Fuscoporia torulosa, paving the way for future studies with this species.

Antiproliferative Activity on Human Colon Adenocarcinoma Cells and In Vitro Antioxidant Effect of Anthocyanin-Rich Extracts from Peels of Species of the Myrtaceae Family

There is a significant indication of the beneficial health effects of fruit rich diets. Fruits of native plant species have noticeably different phytochemicals and bioactive effects. The aim of this work was to characterize and compare the constituents of jabuticaba (Myrciaria jaboticaba, MJ), jamun-berry (Syzygium cumini, SC), and malay-apple (Syzygium malaccense, SM) extracts and their influence on antioxidant activity in vitro and antiproliferative effects on human colon adenocarcinoma cells. According to the results, dried peel powders (DP) have a high anthocyanin content, phenolic compounds, and antioxidant activity when compared to freeze dried extracts (FD). M. jaboticaba dried peel powder extract had a higher total anthocyanin and phenolic compounds content (802.90 ± 1.93 and 2152.92 ± 43.95 mg/100 g, respectively). A reduction in cell viability of HT-29 cells after treatment with M. jaboticaba extracts (DP-MJ and FD-MJ) was observed via MTT assay. Flow cytometry showed that the treatment with the anthocyanin-rich extracts from MJ, SC, and SM had an inhibitory impact on cell development due to G2/M arrest and caused a rise in apoptotic cells in relation to the control group. The findings of this study highlight the potential of peel powders from Myrtaceae fruits as an important source of natural antioxidants and a protective effect against colon adenocarcinoma.