In vitro evaluations of biomolecular interactions, antioxidant and anticancer activities of Nickel(II) and Copper(II) complexes with 1:2 coordination of anthracenyl hydrazone ligands

2021 ◽  
pp. 120419
Author(s):  
K.S. Neethu ◽  
S. Sivaselvam ◽  
M. Theetharappan ◽  
J. Ranjitha ◽  
N.S.P. Bhuvanesh ◽  
...  
2020 ◽  
Vol 26 (45) ◽  
pp. 5783-5792
Author(s):  
Kholood Abid Janjua ◽  
Adeeb Shehzad ◽  
Raheem Shahzad ◽  
Salman Ul Islam ◽  
Mazhar Ul Islam

There is compelling evidence that drug molecules isolated from natural sources are hindered by low systemic bioavailability, poor absorption, and rapid elimination from the human body. Novel approaches are urgently needed that could enhance the retention time as well as the efficacy of natural products in the body. Among the various adopted approaches to meet this ever-increasing demand, nanoformulations show the most fascinating way of improving the bioavailability of dietary phytochemicals through modifying their pharmacokinetics and pharmacodynamics. Curcumin, a yellowish pigment isolated from dried ground rhizomes of turmeric, exhibits tremendous pharmacological effects, including anticancer activities. Several in vitro and in vivo studies have shown that curcumin mediates anticancer effects through the modulation (upregulation and/or downregulations) of several intracellular signaling pathways both at protein and mRNA levels. Scientists have introduced multiple modern techniques and novel dosage forms for enhancing the delivery, bioavailability, and efficacy of curcumin in the treatment of various malignancies. These novel dosage forms include nanoparticles, liposomes, micelles, phospholipids, and curcumin-encapsulated polymer nanoparticles. Nanocurcumin has shown improved anticancer effects compared to conventional curcumin formulations. This review discusses the underlying molecular mechanism of various nanoformulations of curcumin for the treatment of different cancers. We hope that this study will make a road map for preclinical and clinical investigations of cancer and recommend nano curcumin as a drug of choice for cancer therapy.


2012 ◽  
Vol 3 (12) ◽  
pp. 1310 ◽  
Author(s):  
Haifang Xiao ◽  
Yutang Wang ◽  
Qisen Xiang ◽  
Chunxia Xiao ◽  
Li Yuan ◽  
...  

Pharmaceutics ◽  
2021 ◽  
Vol 13 (4) ◽  
pp. 498
Author(s):  
Mariaevelina Alfieri ◽  
Antonietta Leone ◽  
Alfredo Ambrosone

Plants produce different types of nano and micro-sized vesicles. Observed for the first time in the 60s, plant nano and microvesicles (PDVs) and their biological role have been inexplicably under investigated for a long time. Proteomic and metabolomic approaches revealed that PDVs carry numerous proteins with antifungal and antimicrobial activity, as well as bioactive metabolites with high pharmaceutical interest. PDVs have also been shown to be also involved in the intercellular transfer of small non-coding RNAs such as microRNAs, suggesting fascinating mechanisms of long-distance gene regulation and horizontal transfer of regulatory RNAs and inter-kingdom communications. High loading capacity, intrinsic biological activities, biocompatibility, and easy permeabilization in cell compartments make plant-derived vesicles excellent natural or bioengineered nanotools for biomedical applications. Growing evidence indicates that PDVs may exert anti-inflammatory, anti-oxidant, and anticancer activities in different in vitro and in vivo models. In addition, clinical trials are currently in progress to test the effectiveness of plant EVs in reducing insulin resistance and in preventing side effects of chemotherapy treatments. In this review, we concisely introduce PDVs, discuss shortly their most important biological and physiological roles in plants and provide clues on the use and the bioengineering of plant nano and microvesicles to develop innovative therapeutic tools in nanomedicine, able to encompass the current drawbacks in the delivery systems in nutraceutical and pharmaceutical technology. Finally, we predict that the advent of intense research efforts on PDVs may disclose new frontiers in plant biotechnology applied to nanomedicine.


ChemMedChem ◽  
2021 ◽  
Author(s):  
Vijaykumar D. Nimbarte ◽  
Julia Wirmer-Bartoschek ◽  
Santosh L. Gande ◽  
Islam Alshamleh ◽  
Marcel Seibert ◽  
...  

Author(s):  
Changhong Li ◽  
Kui Zhang ◽  
Guangzhao Pan ◽  
Haoyan Ji ◽  
Chongyang Li ◽  
...  

Abstract Background Dehydrodiisoeugenol (DEH), a novel lignan component extracted from nutmeg, which is the seed of Myristica fragrans Houtt, displays noticeable anti-inflammatory and anti-allergic effects in digestive system diseases. However, the mechanism of its anticancer activity in gastrointestinal cancer remains to be investigated. Methods In this study, the anticancer effect of DEH on human colorectal cancer and its underlying mechanism were evaluated. Assays including MTT, EdU, Plate clone formation, Soft agar, Flow cytometry, Electron microscopy, Immunofluorescence and Western blotting were used in vitro. The CDX and PDX tumor xenograft models were used in vivo. Results Our findings indicated that treatment with DEH arrested the cell cycle of colorectal cancer cells at the G1/S phase, leading to significant inhibition in cell growth. Moreover, DEH induced strong cellular autophagy, which could be inhibited through autophagic inhibitors, with a rction in the DEH-induced inhibition of cell growth in colorectal cancer cells. Further analysis indicated that DEH also induced endoplasmic reticulum (ER) stress and subsequently stimulated autophagy through the activation of PERK/eIF2α and IRE1α/XBP-1 s/CHOP pathways. Knockdown of PERK or IRE1α significantly decreased DEH-induced autophagy and retrieved cell viability in cells treated with DEH. Furthermore, DEH also exhibited significant anticancer activities in the CDX- and PDX-models. Conclusions Collectively, our studies strongly suggest that DEH might be a potential anticancer agent against colorectal cancer by activating ER stress-induced inhibition of autophagy.


Molecules ◽  
2021 ◽  
Vol 26 (9) ◽  
pp. 2433
Author(s):  
Nesren Elsayed ◽  
Hatem Sharaf El-Din ◽  
Ammar B. Altemimi ◽  
Hanaa Y. Ahmed ◽  
Anubhav Pratap-Singh ◽  
...  

In this study, Egyptian beebread (EBB) was investigated for its nutritive value, chemical composition, antioxidant properties, antimicrobial and antitumor activities. Results indicated that EBB was a good source of protein (23.58 ± 0.183 g/100 g BB), total free sugar (20.266 ± 0.930) and potassium (290.202 ± 2.645 mg/100 g). Additionally, 14 fatty acids were identified in EBB, wherein polyunsaturated and monounsaturated fatty acids represented 51.06% ± 0.09% and 9.86% ± 0.01%, respectively. The EBB extract exhibited almost 400% better antiradical activity than BHT, with IC50 of EBB extract being 10.7 µg/mL compared to 39.5 µg/mL for BHT. EBB exhibited higher inhibitory activity than the reference compound against Staphylococcus aureus and Escherichia coli, followed by Bacillus subtilis. No inhibitory activity was observed against Aspergillus Niger. Additionally, the highest inhibitory activity was recorded against Caco-2 cells, followed by PC3 and HepG-2 cancer cell lines with IC50 values 262, 314 and 386 μg/mL, respectively. These findings establish the potential of EBB as an antioxidant, antimicrobial and antitumor agent, with possible applications as natural food supplements and natural preservatives.


Nanomaterials ◽  
2021 ◽  
Vol 11 (3) ◽  
pp. 808
Author(s):  
Ahmed Al Saqr ◽  
El-Sayed Khafagy ◽  
Ahmed Alalaiwe ◽  
Mohammed F. Aldawsari ◽  
Saad M. Alshahrani ◽  
...  

Green synthesis of gold nanoparticles (GNPs) with plant extracts has gained considerable interest in the field of biomedicine. Recently, the bioreduction nature of herbal extracts has helped to synthesize spherical GNPs of different potential from gold salt. In this study, a fast ecofriendly method was adopted for the synthesis of GNPs using fresh peel (aqueous) extracts of Benincasa hispida, which acted as reducing and stabilizing agents. The biosynthesized GNPs were characterized by UV–VIS and Fourier transform infrared spectroscopy, transmission electron microscopy (TEM), and dynamic light scattering. In addition, the in vitro antibacterial and anticancer activities of synthesized GNPs were investigated. The formation of gold nanoparticles was confirmed by the existence of a sharp absorption peak at 520 nm, corresponding to the surface plasmon resonance (SPR) band of the GNPs. TEM analysis revealed that the prepared GNPs were spherical in shape and had an average particle size of 22.18 ± 2 nm. Most importantly, the synthesized GNPs exhibited considerable antibacterial activity against different Gram-positive and Gram-negative bacteria. Furthermore, the biosynthesized GNPs exerted remarkable in vitro cytotoxicity against human cervical cancer cell line, while sparing normal human primary osteoblast cells. Such cytotoxic effect was attributed to the increased production of reactive oxygen species (ROS) that contributed to the damage of HeLa cells. Collectively, peel extracts of B. hispida can be efficiently used for the synthesis of GNPs, which can be adopted as a natural source of antimicrobial and anticancer agent.


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