Intensification of resveratrol cytotoxicity, pro-apoptosis, oxidant potentials in human colorectal carcinoma HCT-116 cells using zein nanoparticles.

Resveratrol (RSV), a non-flavonoid stilbene polyphenol, possesses anti-carcinogenic activities against all the major stages of cancer. Zein nanoparticles (ZN NPs) have been utilized successfully in delivery of variant therapeuticals by virtue of their histocompatible nature. The goal of this work was to comparatively explore the antiproliferative, pro-apoptotic and oxidative stress potentials of RSV-ZN NPs versus RSV against human colorectal carcinoma HCT-116 cells. ZN-RSV NPs were developed and assayed for particle size analysis and RSV diffusion. The selected formula obtained 137.6 ± 8.3 nm as mean particle size, 29.4 ± 1.8 mV zeta potential, 92.3 ± 3.6% encapsulation efficiency. IC50 of the selected formula was significantly lower against HCT-116 cells versus Caco-2 cells. Also, significantly enhanced cellular uptake was generated from RSV-ZN NPs versus free RSV. Enhanced apoptosis was concluded due to increased percentage cells in G2-M and pre-G1 phases. The pro-apoptotic potential was explained by caspase-3 and cleaved caspase-3 increased mRNA expression in addition to NF-κB and miRNA125b decreased expression. Biochemically, ZN-RSV NPs induced oxidative stress as demonstrated by enhanced reactive oxygen species (ROS) generation and endothelial nitric oxide synthase (eNOS) isoenzyme increased levels. Conclusively, ZN-RSV NPs obtained cell cycle inhibition supported with augmented cytotoxicity, uptake and oxidative stress markers levels in HCT-116 tumor cells in comparison with free RSV. These results indicated intensified chemopreventive profile of RSV due to effective delivery utilizing ZN nano-dispersion against colorectal carcinoma HCT-116 cells.

Potential Apoptotic Activities of Hylocereus undatus Peel and Pulp Extracts in MCF-7 and Caco-2 Cancer Cell Lines.

There is a huge demand for novel anticancer agents with fewer side effects compared to current therapies. Pitaya, or dragon fruit, is a reservoir of potent anticancer compounds. This research aimed to analyze the phytochemical components of Hylocereus undatus pulp and peel extracts using LC-MS and GC-MS, and to investigate the in vitro effects of both extracts against cancer (breast, MCF-7, and colon, Caco-2) and normal (lung; WI-38 and breast; MCF-10A) cell proliferation using the MTT assay. The apoptosis potential of the anticancer effects was also evaluated using flow cytometry, RT-PCR, and Western blot. The total phenolic and flavonoid contents in the peel extract were significantly higher than those in the pulp extract. Compared to the flavonoid and phenolic acid standards, the LC-MS analysis revealed the presence of nine compounds, which were represented as 84.32 and 5.29 µg/g of the flavonoids and 686.11 and 148.72 µg/g of the phenolic acids in the peel and pulp extracts, respectively. Among the identified compounds, chlorogenic acid, caffeic acid, ferulic acid, and rutin were found at the highest concentration in both plant extracts. Both extracts displayed cytotoxic activity against MCF-7 and Caco-2 cancer cells after 48 h of treatment at IC50 values ranging from 14 to 53 µg/mL with high selective indices against normal WI-38 and MCF-10A cell lines. The increase in apoptosis was revealed by the overexpression of p53, BAX, and caspase-9 and the downregulation of antiapoptotic Bcl-2 mRNA and protein expressions. The results indicate that H. undatus extracts can be a plant source for cancer therapy.

Phenolic profile, anti-inflammatory, antinociceptive, anti-ulcerogenic and hepatoprotective activities of Pimenta racemosa leaves.

BACKGROUND: Pimenta racemosa tree has many traditional uses where its leaves are used as herbal tea for treatment of flatulence, gastric disorder, osteoarthritis, colds and fever in addition to its analgesic and anti-inflammatory activities. So, this study aimed to isolate phenolic constituents of 80% aqueous methanol extract (AME) of leaves and evaluate its biological activities. METHODS: The defatted AME was chromatographed and structures of the isolated compounds were elucidated using UV, NMR spectroscopy and UPLC-ESI-MS analysis. Antioxidant activity was investigated using 2, 2-diphenyl-1-picrylhydrazyl (DPPH) radical scavenging capacity. Anti-inflammatory activity was evaluated using carrageenan - induced paw oedema, while antinociceptive activity was determined by chemical and thermal stimuli. Anti-ulcerogenic effect of AME against gastric damage induced by ethanol in Wister male albino rats was evaluated. Also, hepatoprotective activity was investigated through determination of alanine aminotransferase (ALT) and aspartate aminotransferase (AST) following oral administration of paracetamol. Both of Anti-ulcerogenic and hepatoprotective activities (125, 250 and 500 mg/kg b.wt.) were supported by histopathological examinations. RESULTS: Gallic acid (1), methyl gallate (2), avicularin (3), quercetin 3-O-ß-D-arbinopyranoside (4), quercetin 3-O-ß-D-glucopyranoside (5), quercetrin (6), cynaroside (7), strictinin (8), castalagin (9), grandinin (10) quercetin (11) and ellagic acid (12) were isolated. AME showed significant radical scavenging activity (SC50 = 4.6 µg/mL), promising anti-inflammatory effect through inhibition of oedema and antinociceptive activity by reduction in number of writhes after acetic acid injection and prolongation of reaction time towards the thermal stimulus. AME reduced the gastric mucosal lesions compared with ethanol control and ranitidine groups, ALT at the three doses and AST only at 125 and 250 mg/kg b.wt., when compared with paracetamol group. The results were confirmed by histopathological studies. CONCLUSION: P. racemosa leaves are rich in phenolic compounds and showed significant biological activities.