Cis-trimethoxystilbene, exhibits higher genotoxic and antiproliferative effects than its isomer trans-trimethoxystilbene in mcf-7 and mcf-10a cell lines

Stilbenes are a class of natural compounds with a wide variety of biological effects, such as antitumor activity. The best-known stilbene is resveratrol, whose clinical application is limited due to its low bioavailability. Methoxylated derivatives of this stilbene, including cis-trimethoxystilbene (cis-TMS) and trans-trimethoxystilbene (trans-TMS) have demonstrated more pronounced cytotoxic and anti-proliferative effects than resveratrol. Thus, the objective of this study is to evaluate and compare the cytotoxicity and antiproliferative effects of cis-and trans-TMS in MCF-7 and its normal counterpart MCF-10A. Both compounds were cytotoxic, genotoxic, and induced G2-M accumulation and cell death in the two cell lines. These results suggested that the genotoxicity of cis-and trans-TMS is involved in the reduction of cellular proliferation of MCF-7 and MCF-10A cells, but notably, such antiproliferative effects are more pronounced for cis-than trans-TMS

Synthesis of benzonaphthofuroquinones and benzoylnaphthindolizinediones by reactions of flavonoids with dichlone under basylous, oxygenous and aqueous conditions: Their cytotoxic and apoptotic activities

© 2020 The Royal Society of Chemistry. Using flavonoids and dichlone as substrates, benzonaphthofuroquinones (1, 2, 3, 5, 6, novel; 4 new) and benzoylnaphthindolizinediones (7, 8, known; 9, new) were synthesized through common base-catalyzed method and a new method of combining base-catalyzed with O2/H2O exposing. The possible reaction mechanisms may involve the process like isomerization, hydration, oxidation, decomposition and intermolecular condensation. Benzonaphthofuroquinones (2, 3, 4, 5) were found to exhibit potent cytotoxicity against carcinoma cell lines and low toxicity to normal cell lines. The compounds 4 and 5 not only expressed a significant late-stage-apoptosis against human leukemia and melanoma, but also promoted the cleavage of caspase-3 and PARP in human leukemia, which suggested that the late-stage-apoptosis and caspase-3 pathway may be responsible for the cytotoxicities of these benzonaphthofuroquinones. The replacement of the furan ring with pyrrole system in benzoylnaphthindolizinediones (7, 8, 9) resulted in the loss of anticancer activity

Coal Consumption: An Alternate Energy Resource to Fuel Economic Growth in Pakistan

This study is an attempt to revisit the causal relationship between coal consumption and economic growth in case of Pakistan. The present study covers the period of 1974-2010. The direction of causality between the variable is investigated by applying the VECM Granger causality approach. Our findings have exposed that there exists bidirectional Granger causality between economic growth and coal consumption. The Cumulative Sum (CUSUM) and Cumulative Sum of Square (CUSUMSQ) diagrams have not found any structural instability over the period of 1974-2010

Utility of fatty acid profile and in vitro immune cell activation for chemical and biological standardization of Arthrospira/Limnospira

Corresponding author (NCNPR): Jin Zhang, [email protected]://egrove.olemiss.edu/pharm_annual_posters_2022/1021/thumbnail.jp

Computational Tools to Expedite the Identification of Potential PXR Modulators in Complex Natural Product Mixtures – A Case Study with Five Closely Related Licorice Species

Corresponding author (NCNPR): Pankaj Pandey, [email protected]://egrove.olemiss.edu/pharm_annual_posters_2022/1014/thumbnail.jp

In search for potential antidiabetic compounds from natural sources: docking, synthesis and biological screening of small molecules from Lycium spp. (Goji)

© 2019 Current clinical antidiabetic drugs, like rosiglitazone 1, have been implicated in some serious side effects like edema, weight gain, and heart failure, making it necessary to find alternative agents. Partial agonists of peroxisome-proliferator activated receptor-gamma (PPARγ) were determined to possess improved insulin sensitivity without undeseirable side-effects when compared to full agonists of PPARγ, like rosiglitazone 1. The traditional Chinese medicine (TCM) plants, Goji (Lycium barbarum and Lycium chinense) are widely used for treating symptoms related to various diseases including diabetes and hypertension. Twenty-seven reported compounds from Goji were docked into both partial- and full-agonist binding sites of PPARγ. Amongst the docked compounds, phenylethylamide-based phytochemicals (5–9) (termed as tyramine-derivatives, TDs) were found to possess good docking scores and binding poses with favorable interactions. Synthesis of 24 TDs, including three naturally occuring amides (6, 8, 9) were synthesized and tested for PPARγ gene induction with cell-based assay. Three compounds showed similar or higher fold induction than the positive control, rosiglitazone. Among these three active TDs, trans-N-feruloyloctopamine (9) and tyramine derivatives-enriched extract (TEE) (21%) of the root bark of L. chinense were further studied in vivo using db/db mice. However, both TEE as well as 9 did not show significant antidiabetic properties in db/db mice. In vivo results suggest that the proposed antidiabetic property of Lycium species may not be due to tyramine derivatives alone. Further studies of tyramine derivatives or enriched extract(s) for other bioactivities like hypocholesterolemic activities, and studies of novel isolated compounds from Goji will enable a more complete understanding of their bioactivities

Available Bandwidth Measurement in 4G Networks

Existing available bandwidth estimation tools were mainly designed for fixed IP backbone networks and desktops with assumption of First In First Out(FIFO) Principle. While LTE supports high data rates of 100 Mbps, challenge is to adapt available bandwidth algorithms for quick and non-intrusive measurements on an Android OS based device supporting different MIMO configurations.This Master thesis presents real time, two way available bandwidth measurement tool using Two Way Active Measurement Protocol(TWAMP) for Android OS based devices to measure high speed LTE networks. The tool performance is verified against FTP throughput measurement with effect of variation in constant bit rate UDP cross traffic and load on the server on end-to-end measurements. The results from emulation and tests in a commercial LTE network show that we can achieve available bandwidth estimations on both the uplink and downlink in real time. This opens up wide possibility to include various existing available bandwidth techniques and tools in mobile application to be used over a wireless link. Further, possible suggestions to achieve better available bandwidth estimations with native application development has been proposed.Validerat; 20130917 (global_studentproject_submitter

Design, synthesis and biological evaluation of benzoxazolinone-containing 1,3,4-thiadiazoles as TNF-α inhibitors

A library of nineteen benzoxazolinone-based 1,3,4-thiadiazoles has been synthesized and screened for their anti-inflammatory activity. The compound 1f exhibited a potent anti-inflammatory activity with an inhibition of 65.83% and 32.50% after 3 h and 5 h respectively. It also exhibited a significant in vitro (p < 0.01), TNF- α inhibitory activity with 51.44 % inhibition. The compound 1f showed hydrogen bonding with GLN 61 and interactions with TYR 119, TYR 151 and GLY 121. The histopathology report showed that none of the compounds caused gastric ulceration. The results from the in vivo &amp; in vitro antiinflammatory activity along with In Silico studies exhibit that benzoxazolinone-based 1,3,4-thiadiazoles may be used in the future development of anti-inflammatory drugs