scholarly journals Eruca sativa L-A promising source of drug lead for antimicrobial, neuroprotective and anticancer treatment regimens: Pharmacological properties of medicinal plant “Eruca sativa”

2019 ◽  
pp. 17-21
Author(s):  
Waseem Mohammed Abdul ◽  
Syed Shoeb Razvi
Keyword(s):  
Human Cancer ◽  
Biological Effects ◽  
Bacterial Species ◽  
Eruca Sativa ◽  
Human Cancer Cell Lines ◽  
Plant Parts ◽  
Synthetic Drugs ◽  
Treatment Regimens ◽  
Epigenetic Modulation ◽  
Promising Source

Rocket (Eruca sativa) is a low-calorie leafy vegetable of the family Brassicaceae under the genera Eruca mostly consumed raw in salads. It has been used since ancient times from food to medicine and cosmetics without any knowledge of the mechanism or the targets involved. However, presently, the production and cultivation of rocket have significantly increased owing to its different biological effects. Erucin and Sulforaphane are the most commonly studied isothiocyanates obtained from the plant parts of Eruca sativa. Over time, with continuous usage of conventional and synthetic drugs, the drug resistant and off-target toxicities rapidly increase, which necessitates for alternative medicine with increased specificity and minimal detrimental effects. It is interesting to note that many previous studies have reported the antimicrobial impact of E. sativa against the pathogenic bacterial species like Escherichia coli, Staphylococcus aureus, Salmonella typhimurium, etc. Moreover, Erucin obtained from E. sativa has shown significant inhibitory and protective effect against different human cancer cell lines and xenograft animal models. The present review gives a brief overview of the antimicrobial, neuroprotective and anticancer effects of the various plant parts of E. sativa and the most bioactive isothiocyanates. It is exciting to note that epigenetic modulation of gene expression has also been reported in some studies which could be a new direction of research on the path of naturopathy.

scholarly journals 13-Ethylberberine Induces Apoptosis through the Mitochondria-Related Apoptotic Pathway in Radiotherapy-Resistant Breast Cancer Cells

Molecules ◽  
2019 ◽  
Vol 24 (13) ◽  
pp. 2448 ◽  
Author(s):  
Hana Jin ◽  
Young Shin Ko ◽  
Sang Won Park ◽  
Ki Churl Chang ◽  
Hye Jung Kim
Keyword(s):  
Breast Cancer ◽  
Human Cancer ◽  
Biological Effects ◽  
Bacterial Species ◽  
Extrinsic Pathway ◽  
Apoptotic Pathway ◽  
Septic Mouse ◽  
Human Cancer Cell Lines ◽  
Apoptotic Genes ◽  
Anti Inflammatory

Berberine is reported to have multiple biological effects, including antimicrobial, anti-inflammatory, and antitumor activities, and 13-alkyl-substituted berberines show higher activity than berberine against certain bacterial species and human cancer cell lines. In particular, 13-ethylberberine (13-EBR) was reported to have anti-inflammatory effects in endotoxin-activated macrophage and septic mouse models. Thus, in this study, we aimed to examine the anticancer effects of 13-EBR and its mechanisms in radiotherapy-resistant (RT-R) MDA-MB-231 cells derived from the highly metastatic MDA-MB-231 cells. When we compared the gene expression between MDA-MB-231 and RT-R MDA-MB-231 cells with an RNA microarray, RT-R MDA-MB-231 showed higher levels of anti-apoptotic genes and lower levels of pro-apoptotic genes compared to MDA-MB-231 cells. Accordingly, we examined the effect of 13-EBR on the induction of apoptosis in RT-R MDA-MB-231 and MDA-MB-231 cells. The results showed that 13-EBR reduced the proliferation and colony-forming ability of both MDA-MB-231 and RT-R MDA-MB-231 cells. Moreover, 13-EBR induced apoptosis by promoting both intracellular and mitochondrial reactive oxygen species (ROS) and by regulating the apoptosis-related proteins involved in the intrinsic pathway, not in the extrinsic pathway. These results suggest that 13-EBR has pro-apoptotic effects in RT-R MDA-MB-231 and MDA-MB-231 cells by inducing mitochondrial ROS production and activating the mitochondrial apoptotic pathway, providing useful insights into new potential therapeutic strategies for RT-R breast cancer treatment.

scholarly journals Comprehensive Evaluation of Biological Effects of Pentathiepins on Various Human Cancer Cell Lines and Insights into Their Mode of Action

2021 ◽  
Vol 22 (14) ◽  
pp. 7631
Author(s):  
Lisa Wolff ◽  
Siva Sankar Murthy Bandaru ◽  
Elias Eger ◽  
Hoai-Nhi Lam ◽  
Martin Napierkowski ◽  
...  
Keyword(s):  
Oxidative Stress ◽  
Cell Lines ◽  
Cancer Cell ◽  
Human Cancer ◽  
Biological Effects ◽  
Cancer Cell Lines ◽  
Biological Evaluation ◽  
Human Cancer Cell ◽  
Strand Breaks ◽  
Human Cancer Cell Lines

Pentathiepins are polysulfur-containing compounds that exert antiproliferative and cytotoxic activity in cancer cells, induce oxidative stress and apoptosis, and inhibit glutathione peroxidase (GPx1). This renders them promising candidates for anticancer drug development. However, the biological effects and how they intertwine have not yet been systematically assessed in diverse cancer cell lines. In this study, six novel pentathiepins were synthesized to suit particular requirements such as fluorescent properties or improved water solubility. Structural elucidation by X-ray crystallography was successful for three derivatives. All six underwent extensive biological evaluation in 14 human cancer cell lines. These studies included investigating the inhibition of GPx1 and cell proliferation, cytotoxicity, and the induction of ROS and DNA strand breaks. Furthermore, selected hallmarks of apoptosis and the impact on cell cycle progression were studied. All six pentathiepins exerted high cytotoxic and antiproliferative activity, while five also strongly inhibited GPx1. There is a clear connection between the potential to provoke oxidative stress and damage to DNA in the form of single- and double-strand breaks. Additionally, these studies support apoptosis but not ferroptosis as the mechanism of cell death in some of the cell lines. As the various pentathiepins give rise to different biological responses, modulation of the biological effects depends on the distinct chemical structures fused to the sulfur ring. This may allow for an optimization of the anticancer activity of pentathiepins in the future.

scholarly journals Antibacterial, Antihemolytic, Cytotoxic, Anticancer, and Antileishmanial Effects of Ajuga bracteosa Transgenic Plants

Plants ◽  
2021 ◽  
Vol 10 (9) ◽  
pp. 1894
Author(s):  
Samina Rubnawaz ◽  
Mohammad K. Okla ◽  
Nosheen Akhtar ◽  
Imdad Ullah Khan ◽  
Muhammad Zeeshan Bhatti ◽  
...  
Keyword(s):  
Neglected Tropical Diseases ◽  
Human Cancer ◽  
Conventional Polymerase Chain Reaction ◽  
Rol Genes ◽  
Human Cancer Cell Lines ◽  
Traditional Medicines ◽  
Synthetic Drugs ◽  
Rolb Gene ◽  
Transgenic Lines

Herbal and traditional medicines can play a pivotal role in combating cancer and neglected tropical diseases. Ajuga bracteosa, family Lamiaceae, is an important medicinal plant. The genetic transformation of A. bracteosa with rol genes of Agrobacterium rhizogenes further enhances its metabolic content. This study aimed at undertaking the molecular, phytochemical, and in vitro biological analysis of A. bracteosa extracts. We transformed the A. bracteosa plant with rol genes and raised the regenerants from the hairy roots. Transgenic integration and expression of rolB were confirmed by conventional polymerase chain reaction (PCR) and qPCR analysis. The methanol: chloroform crude extracts of wild-type plants and transgenic regenerants were screened for in vitro antibacterial, antihemolytic, cytotoxic, anticancer, and leishmanial activity. Among all plants, transgenic line 3 (ABRL3) showed the highest expression of the rolB gene. Fourier transform infra-red (FTIR) analysis confirmed the enhanced number of functional groups of active compounds in all transgenic lines. Moreover, ABRL3 exhibited the highest antibacterial activity, minimum hemolytic activity (CC50 = 7293.05 ± 7 μg/mL) and maximum antileishmanial activity (IC50 of 56.16 ± 2 μg/mL). ABRL1 demonstrated the most prominent brine shrimp cytotoxicity (LD5039.6 ± 4 μg/mL). ABRL3 was most effective against various human cancer cell lines with an IC50 of 57.1 ± 2.2 μg/mL, 46.2 ± 1.1 μg/mL, 72.4 ± 1.3 μg/mL, 73.3 ± 2.1 μg/mL, 98.7 ± 1.6 μg/mL, and 97.1 ± 2.5 μg/mL against HepG2, LM3, A549, HT29, MCF-7, and MDA-MB-231, respectively. Overall, these transgenic extracts may offer a cheaper therapeutic source than the more expensive synthetic drugs.

Synthesis and Characterization of Some Metal Complexes of 4,5-Diazafluoren-9-one and their Biological Effects on Human Carcinoma Cells

2008 ◽  
Vol 61 (12) ◽  
pp. 975 ◽  
Author(s):  
Guo-Liang Lu ◽  
Cheuk-Lam Ho ◽  
Qiwei Wang ◽  
Wai-Yeung Wong ◽  
Chung-Hin Chui ◽  
...  
Keyword(s):  
Metal Complexes ◽  
Cell Lines ◽  
Cancer Cell ◽  
Human Cancer ◽  
Biological Effects ◽  
Cancer Cell Lines ◽  
Inhibitory Effect ◽  
Ambient Conditions ◽  
Human Carcinoma ◽  
Human Cancer Cell Lines

Three new transition metal complexes of 4,5-diazafluoren-9-one, [(DAFO)PdCl2], [(DAFO)PtCl2], and [(DAFO)ZnCl2], were prepared in good yields by the reactions between appropriate metal chloride precursors and 4,5-diazafluoren-9-one under ambient conditions. The structures of these metal complexes were established by spectroscopic (Fourier-transform IR, NMR, and fast-atom bombardment mass spectrometry) techniques. The possible biological activity of these compounds on three human cancer cell lines including Hep3B, MDAMB-231, and SKHep-1 was investigated. The results obtained showed that both zinc- and platinum-containing compounds exhibit a similar growth inhibitory effect on these three cancer cell lines when compared with the prototypical cis-platin. In contrast, the corresponding palladium congener is virtually biologically inactive in these trials.

scholarly journals Genistein Derivatives Regioisomerically Substituted at 7-O- and 4′-O- Have Different Effect on the Cell Cycle

2013 ◽  
Vol 2013 ◽  
pp. 1-12 ◽  
Author(s):  
A. Byczek ◽  
J. Zawisza-Puchalka ◽  
A. Gruca ◽  
K. Papaj ◽  
G. Grynkiewicz ◽  
...  
Keyword(s):  
Cell Cycle ◽  
Cell Lines ◽  
Cancer Cell ◽  
Human Cancer ◽  
Biological Effects ◽  
Cancer Cell Lines ◽  
Dna Lesions ◽  
Hydroxyl Group ◽  
Human Cancer Cell Lines

Our previous studies on antiproliferative properties of genistein derivatives substituted at C7 hydroxyl group of the ring A revealed some compounds with antimitotic properties. The aim of this work was to synthesize their analogues substituted at the 4′-position of the ring B in genistein and to define their antiproliferative mechanism of action in selected cancer cell linesin vitro. C4′-substituted glycoconjugates were obtained in a three-step procedure: (1) alkylation with anω-bromoester; (2) deacylation; (3) Ferrier-type rearrangement glycosylation with acylated glycals. Biological effects including antiproliferative effects of the compounds, cell cycle, DNA lesions (ATM activation, H2A.X phosphorylation, and micronuclei formation), and autophagy were studied in human cancer cell lines. Some of the tested derivatives potently inhibited cell proliferation. The presence of a substituent at the 4′-position of the ring B in genistein correlated to a p53-independent G1 cell-cycle arrest. The derivatives substituted at C4′ did not induce DNA lesions and appeared to be nongenotoxic. The tested compounds induced autophagy and caused remarkable decrease of cell volume.

scholarly journals The prohibitin-binding compound fluorizoline affects multiple components of the translational machinery and inhibits protein synthesis

2020 ◽  
Vol 295 (29) ◽  
pp. 9855-9867 ◽  
Author(s):  
Xin Jin ◽  
Jianling Xie ◽  
Michael Zabolocki ◽  
Xuemin Wang ◽  
Tao Jiang ◽  
...  
Keyword(s):  
Endoplasmic Reticulum ◽  
Protein Synthesis ◽  
Cancer Cell ◽  
Human Cancer ◽  
Biological Effects ◽  
Cellular Protein ◽  
Initiation Factor ◽  
Marked Rise ◽  
Human Cancer Cell Lines ◽  
Translational Machinery

Fluorizoline (FLZ) binds to prohibitin-1 and -2 (PHB1/2), which are pleiotropic scaffold proteins known to affect signaling pathways involved in several intracellular processes. However, it is not yet clear how FLZ exerts its effect. Here, we show that exposure of three different human cancer cell lines to FLZ increases the phosphorylation of key translation factors, particularly of initiation factor 2 (eIF2) and elongation factor 2 (eEF2), modifications that inhibit their activities. FLZ also impaired signaling through mTOR complex 1, which also regulates the translational machinery, e.g. through the eIF4E-binding protein 4E-BP1. In line with these findings, FLZ potently inhibited protein synthesis. We noted that the first phase of this inhibition involves very rapid eEF2 phosphorylation, which is catalyzed by a dedicated Ca2+-dependent protein kinase, eEF2 kinase (eEF2K). We also demonstrate that FLZ induces a swift and marked rise in intracellular Ca2+ levels, likely explaining the effects on eEF2. Disruption of normal Ca2+ homeostasis can also induce endoplasmic reticulum stress, and our results suggest that induction of this stress response contributes to the increased phosphorylation of eIF2, likely because of activation of the eIF2-modifying kinase PKR-like endoplasmic reticulum kinase (PERK). We show that FLZ induces cancer cell death and that this effect involves contributions from the phosphorylation of both eEF2 and eIF2. Our findings provide important new insights into the biological effects of FLZ and thus the roles of PHBs, specifically in regulating Ca2+ levels, cellular protein synthesis, and cell survival.

scholarly journals Antiproliferative and Enzyme Docking Analysis of Engleromycin from Engleromyces goetzei

Molecules ◽  
2019 ◽  
Vol 24 (1) ◽  
pp. 166 ◽  
Author(s):  
Yongli Zhang ◽  
Guilin Chen ◽  
Hong Ma ◽  
Mingquan Guo
Keyword(s):  
Antiproliferative Activity ◽  
Topoisomerase Ii ◽  
Antitumor Agents ◽  
Human Cancer ◽  
Biological Effects ◽  
A549 Cells ◽  
Human Cancer Cell Lines ◽  
Ic50 Values ◽  
Ht 29

Engleromyces goetzei P. Henn. (E. goetzei) has been widely used as a traditional herb for many years in Kenya due to its diverse biological effects. Although engleromycin was first isolated from E. goetzei in 1980, its pharmacological activity is still unknown. In this study, engleromycin from E. goetzei was identified by spectroscopic analyses, and subsequently examined for its antiproliferative activity using human cancer cell lines of SGC-7901, HT-29, HeLa and A549. As a result, it was revealed that engleromycin strongly inhibited the growth of SGC-7901, HT-29, HeLa and A549 cells with IC50 values at 26.77 ± 1.69 µM, 7.73 ± 0.18 µM, 7.00 ± 0.12 µM and 3.14 ± 0.03 µM, respectively. The results of topoisomerase II (Top II) inhibition assay in vitro implied that engleromycin might be a Top II inhibitor. Further insights into the potential mechanism of antiproliferative activity displayed that engleromycin could dock into the binding pockets of Top II, like the clinical inhibitor doxorubicin, and then inhibit the biological activity of Top II. Taken together, our findings suggest that engleromycin has an anticancer potential, and may serve as a leading compound for the development of antitumor agents.

scholarly journals Phytochemicals Derived from Catharanthus roseus and Their Health Benefits

Technologies ◽  
2020 ◽  
Vol 8 (4) ◽  
pp. 80
Author(s):  
Hong Ngoc Thuy Pham ◽  
Quan Van Vuong ◽  
Michael C. Bowyer ◽  
Christopher J. Scarlett
Keyword(s):  
Bioactive Compounds ◽  
Catharanthus Roseus ◽  
Anticancer Agents ◽  
Human Cancer ◽  
Biological Activities ◽  
Health Benefits ◽  
Traditional Use ◽  
Human Cancer Cell Lines ◽  
Promising Source

Catharanthus roseus (C. roseus) is an important medicinal plant distributed in many countries. It has attracted increasing attention due to it being shown to possess a range of phytochemicals with various biological activities such as antioxidant, antibacterial, antifungal, antidiabetic and anticancer properties. Remarkably, vinblastine and vincristine isolated from this plant were the first plant-derived anticancer agents deployed for clinical use. Recently, new isolated indole alkaloids from this plant including catharoseumine, 14′,15′-didehydrocyclovinblastine, 17-deacetoxycyclovinblastine and 17-deacetoxyvinamidine effectively inhibited human cancer cell lines in vitro. Moreover, vindoline, vindolidine, vindolicine and vindolinine isolated from C. roseus leaf exhibited in vitro antidiabetic property. These findings strongly indicate that this plant is still a promising source of bioactive compounds, which should be further investigated. This paper provides an overview of the traditional use and phytochemical profiles of C. roseus, and summarises updated techniques of the preparation of dried material, extraction and isolation of bioactive compounds from this plant. In addition, purported health benefits of the extracts and bioactive compounds derived from this plant were also addressed to support their potential as therapeutic agents.

scholarly journals Proinsulin Binds with High Affinity the Insulin Receptor Isoform A and Predominantly Activates the Mitogenic Pathway

Endocrinology ◽  
2012 ◽  
Vol 153 (5) ◽  
pp. 2152-2163 ◽  
Author(s):  
Roberta Malaguarnera ◽  
Antonella Sacco ◽  
Concetta Voci ◽  
Giuseppe Pandini ◽  
Riccardo Vigneri ◽  
...  
Keyword(s):  
Insulin Receptor ◽  
Metabolic Activity ◽  
Human Cancer ◽  
Biological Effects ◽  
Similar Degree ◽  
Human Cancer Cell Lines ◽  
Cell Proliferation And Migration ◽  
Igf I ◽  
And Migration ◽  
Proliferation And Migration

Proinsulin is generally regarded as an inactive prohormone because of its low metabolic activity. However, proinsulin appears to regulate embryo development in animal models. In this study, we evaluated whether proinsulin may differentially bind to and activate the two insulin receptor (IR) isoforms (IR-A and IR-B), because IR-A is a relatively low-specificity receptor that is prevalent in fetal and cancer cells and is able to mediate the growth effects of IGF-II. Mouse R− fibroblasts devoid of IGF-I receptor (IGF-IR) and stably transfected with cDNA encoding either human IR-A or IR-B (R− /IR-A and R− /IR-B cells) were used. Three human cancer cell lines were also studied. We found that proinsulin stimulated phosphorylation of IR-A with an EC50 of 4.5 ± 0.6 nm and displaced [125I]insulin from IR-A with a similar EC50. In contrast, proinsulin EC50 values for stimulation of IR-B phosphorylation and for [125I]insulin displacement from IR-B were approximately 7-fold higher. Proinsulin did not bind or activate IGF-IR or IR/IGF-IR hybrids. Via IR-A, proinsulin activated the ERK/p70S6K pathway to a similar degree as insulin but elicited a weaker Akt response. Despite its low metabolic activity, proinsulin was almost equipotent as insulin in inducing cell proliferation and migration in cells expressing various IR-A levels. In conclusion, proinsulin is a selective IR-A ligand and may induce biological effects through this IR isoform.

scholarly journals Design, Synthesis and Structural Confirmation of a Series of 2-(Thiophen-2-yl)- 4H-chromen-3-yl-sulfonate Derivatives and Preliminary Investigation of Their Antioxidant and Anticancer Potentials

2021 ◽  
Author(s):  
Jialin Zang ◽  
Ming Bu ◽  
Jifang Yang ◽  
Lu Han ◽  
Zhen Lv
Keyword(s):  
Cell Lines ◽  
Cancer Cell ◽  
Human Cancer ◽  
Biological Effects ◽  
Cancer Cell Lines ◽  
Positive Control ◽  
Cytotoxic Activities ◽  
Spectroscopic Techniques ◽  
Human Cancer Cell ◽  
Human Cancer Cell Lines

A series of novel 2-(thiophen-2-yl)-4H-chromen-3-yl-sulfonate derivatives (4a-4n) were synthesized and investigated for their in vitro free radical scavenging potential as well as cytotoxic efficacies against selected cancer cell lines. The cytotoxicity of the 4H-chromene derivatives (4a‑4n) was evaluated according to three human cancer cell lines (HepG2, A549, HeLa) by utilizing a 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide (MTT) assay. Accordingly, part of the results exhibited better cytotoxic activities than that of the positive controls (4H-chromen-4-one and apigenin). Among them, compounds 4c-4g exhibited better training to the positive control against the three human cancer cell lines (half maximal inhibitory concentration (IC50) = 3.87 ± 0.12 to 21.38 ± 0.52 μM). Moreover, the extract of the 4H-chromene derivatives (4a‑4n) showed better activity against 2,2-diphenyl-1-picrylhydrazyl (DPPH) and 2,2’-azino-bis-3‑ethylbenzothiazoline-6-sulfonic acid (ABTS) in antioxidant assays compared to that of the positive control ascorbic acid (IC50 = 12.72 ± 0.27, 5.09 ± 0.21 μg mL-1). Thus, it can be confirmed from the bioassay results that the overall structural design, as well as proper substitution, is crucial in delivering anticipated biological effects. In this regard, spectroscopic techniques such as 1H nuclear magnetic resonance (NMR), 13C NMR, and high-resolution mass spectrometry (HRMS) were also carried out to confirm the final structures.

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