Evaluation of Insecticidal Potentials of Five Plant Extracts against the Stored Grain Pest, Callosobruchus maculatus (Coleoptera: Bruchidae).

Plant based insecticides are considered among the most economic and ecofriendly chemicals for the protection of plants and stored grains. The cowpea weevil (Callosbruchus maculatus) causes more than 90% damage to sored grains in three to six months. The current study investigates insecticidal potentials of five selected botanicals: Melia azedarach, Nicotiana rustica, Azadirachta indica, Nicotiana tabacum and Thuja orientalis. They are explored at six different concentrations (0.5, 1.0, 1.5, 2.0, 2.5 and 3.0%) against C. maculatus and compared to effects of distilled water which is used as a control. Toxicities of 3%(V/V) extracts of N. tabacum, N. rustica, A. indica and T. orientalis against C. maculatus were 100%, 86.11%, 80.56% and 72.22%, respectively. Maximum mortality was caused by N. tabacum and N. rustica (100%), followed by A. indica (82%), whereas minimum mortality was observed in T. orientalis (64%) at 2.5%. Several phytochemicals, alkaloids, saponins, diterphenes, phytosterol, flavonoids and phenols were identified in N. tabacum and N. rustica, while few were present in A. indica. Phytosterol was present in greatest abundance. Saponins were only detected in aqueous extracts of N. rustica and N. tabacum. Taken together, these results indicate the utility of N. tabacum, N. rustica and A. indica as potential botanicals to control pest beetle and cowpea weevil.

Recent Developments and Anticancer Therapeutics of Paclitaxel: An Update.

Plants are a source of diverse classes of secondary metabolites with anticancer properties. Paclitaxel (Taxol) is an anticancer drug isolated from various Taxus species and is used as a chemotherapeutic agent against various cancers. The biosynthesis of paclitaxel is a complex pathway, making its total chemical synthesis commercially non-viable; hence, alternative novel sources - like plant cell culture and heterologous expression systems, are being investigated to overcome this issue. Advancements in the field of genetic engineering, microbial fermentation engineering, and recombinant techniques have significantly increased the achievable yields of paclitaxel. Indeed, paclitaxel selectively targets microtubules and causes cell cycle arrest in the G2/M phase, inducing a cytotoxic effect in a concentration and time-dependent manner. Innovative drug delivery formulations, like the development of albumin-bound nanoparticles, nano-emulsions, nano-suspensions, liposomes, and polymeric micelles, have been applied to enhance the delivery of paclitaxel to tumor cells. This review focuses on the production, biosynthesis, mechanism of action, and anticancer effects of paclitaxel.

Seroprevalence of Anti-tTg-IgA among Symptomized Celiac Disease Patients and Their Correlation with Rotavirus Infection.

Celiac disease (CD) is a chronic inflammatory disorder in the intestinal tract as a response to the use of gluten in genetically predisposed individuals. It is a worldwide problem, with a high prevalence rate in North America. This is a descriptive cross-sectional study involving 1090 samples collected from different hospitals of Rawalpindi and Islamabad, Pakistan, from January 2019 to December 2019. In this study, 1090 blood samples screened for seroprevalence of anti-tTG antibodies in CD symptomatic patients via ELISA (enzyme-linked immunosorbent assay). 1090 fecal samples from the same CD patients were collected and tested for the presence of rotavirus (RV) via ELISA and RT-PCR. Of the 1090 patients tested for seroprevalence of anti-tTG antibodies, 112/1090 (10.3%) were found to be positive. Of the 112 anti-tTG-positive patients, 78/112 (70%) were positive for RV via ELISA and 74/112 (66.1%) were RV positive via RT-PCR. A statistically significant association was reported between rotavirus infection and celiac disease (p˂0.05). Anti-tTG antibodies were higher in age group 6 (12-18 years) patients (18.4%) and at minimum in age group 3 (1-3 years) patients (4.8%). However, there was a statistically insignificant relationship between group age and CD prevalence (p > 0.05). The highest CD prevalence was noted during winter season (19.6%) and the lowest (3.0%) during fall/autumn. Our study findings demonstrate that Pakistan has a high prevalence of CD compared to other studies. Further studies in the fields of environmental risk factors and treatment with more advanced serological and histopathological studies are needed in the future.

Biorational Control of Callosobruchus maculatus (Coleoptera: Buchidae) in Stored Grains with Botanical Extracts.

Globally, around 2000 plant species are used against pest control. The utilization of botanicals is considered the most economic and biodegradable methods for the control of stored grains pests. Therefore, the current study was carried out to investigate the repellency potential of five botanicals against Callosbruchus maculatus F. in Haripur, Pakistan. The concentrations of Azadirachta indica L., Nicotiana tabacum L., Melia azedarach L., Nicotiana rustica L., and Thuja orientalis L. were, i.e., 0.5, 1.0, 1.5, 2.0, 2.5, and 3.0% in four replicates to establish contact effects. The data were recorded after 1, 2, 3, 6, 24, 48, 72, and 96 hours. The repellency effect of these plant species against C. maculatus were increased in both the time- and dose-dependent manner, and highest effect was observed at 72 h. In addition, the repellency effect was 91% for A. indica (class: V), 86% M. azedarach, 82%, N. tabacum (class: V), 79% N. rustica (class: IV), and 75% T. orientalis (class: IV) at 3% concentration against C. maculatus. Furthermore, following 96 hours' exposure to treatment the sensitivity response of insects decreases as the time interval increases, i.e., 86% A. indica (class: V) was followed by 71% M. azedarach (class: IV), 65% N. tabacum (class: IV), 61% N. rustica (class: IV), and T. orientalis 57% (class: III) repellency at highest concentration of 3%. The current study concluded that A. indica and M. azedarach can be incorporated for the management of C. maculatus and these plant species might be helpful in the productions of new biopesticides.

Development, Molecular Docking, and In Silico ADME Evaluation of Selective ALR2 Inhibitors for the Treatment of Diabetic Complications via Suppression of the Polyol Pathway.

Diabetic complications are associated with overexpression of aldose reductase, an enzyme that catalyzes the first step of the polyol pathway. Osmotic stress in the hyperglycemic state is linked with the intracellular accumulation of sorbitol along with the depletion of NADPH and eventually leads to oxidative stress via formation of reactive oxygen species and advanced glycation end products (AGEs). These kinds of mechanisms cause the development of various diabetic complications including neuropathy, nephropathy, retinopathy, and atherosclerotic plaque formation. Various aldose reductase inhibitors have been developed to date for the treatment of diabetic complications, but all have failed in different stages of clinical trials due to toxicity and poor pharmacokinetic profiles. This toxicity is rooted in a nonselective inhibition of both ALR2 and ALR1, homologous enzymes involved in the metabolism of toxic aldehydes such as methylglyoxal and 3-oxyglucosazone. In the present study, we developed a series of thiosemicarbazone derivatives as selective inhibitors of ALR2 with both antioxidant and antiglycation potential. Among the synthesized compounds, 3c exhibited strong and selective inhibition of ALR2 (IC50 1.42 µM) along with good antioxidant and antiglycative properties. The binding mode of 3c was assessed through molecular docking and cluster analysis via MD simulations, while in silico ADME evaluation studies predicted the compounds' druglike properties. Therefore, we report 3c as a drug candidate with promising antioxidant and antiglycative properties that may be useful for the treatment of diabetic complications through selective inhibition of ALR2.

Phytochemical Analysis and In Vitro and In Vivo Pharmacological Evaluation of Parthenium hysterophorus Linn.

The main aim of this research was to explore Parthenium hysterophorus Linn phytochemically and pharmacologically. Phytochemical screening is important for the isolation of active compounds before bulk extraction. The crude extracts and their fractions were screened for enzyme (urease, α-glycosidase, and phosphodiesterase) inhibition assays, in vivo analgesic, anti-inflammatory, and sedative effects. Results indicated the presence of steroids, flavonoids, etc. The crude extracts such as methanol, hexane, aqueous, ethyl acetate, chloroform, and butanol exhibited excellent urease inhibitory activities with IC50 = 43.1 ± 1.24, 31.9 ± 2.21, 31.9 ± 2.21, 57.3 ± 1.27, 49.2 ± 2.16, and 35.3 ± 1.12, respectively, as compared to standard acetohydroxamic acid (20.3 ± 0.43). The extracts (methanol, hexane, aqueous, ethyl acetate, chloroform, and butanol) also showed promising α-glycosidase potency with IC50 = 13.1 ± 0.34, 21.2 ± 1.16, 23.1 ± 0.12, 84.2 ± 2.17, 118.6 ± 3.07, and 840 ± 1.73, respectively against acarbose (840 ± 1.73). The phosphodiesterase activity of the mentioned extracts was also excellent with IC50 = 131.1 ± 2.41, 197.2 ± 3.16, 24.2 ± 0.11, 62.4 ± 2.21, 152.4 ± 1.81, and 55.3 ± 2.15, respectively, against the standard (265.5 ± 2.25). Furthermore, butanol (14.96 ± 1.78), ethyl acetate (18.98 ± 1.71), and methanol (16.87 ± 1.00) showed dose-dependent analgesic effects with a maximum inhibition of acetic acid-induced writhes. Whereas, methanolic and butanol extracts exhibited maximum inhibition of inflammation in the carrageenan paw edema test. The aqueous (p < 0.01) and butanol (p < 0.01) extracts exhibited maximum a sedative effect followed by chloroform (p < 0.05), ethyl acetate (p < 0.05), and methanolic (p < 0.05) fractions as compared to the standard drug. The current research concluded that Parthenium hysterophorus Linn has important phytochemical constituents having inhibitory effects on urease, α-glycosidase, and phosphodiesterase enzymes. Furthermore, the plant has analgesic, anti-inflammatory, and sedative effects. The P. hysterophorus needs to further be explored for the candidate molecules responsible for the abovementioned activities.

Appraisal of novel azomethine-thioxoimidazolidinone conjugates as ecto-5'-nucleotidase inhibitors: synthesis and molecular docking studies.

Purinergic signaling is regulated by a group of extracellular enzymes called ectonucleotidases. One of its members i.e., ecto-5'-nucleotidase (h-e5'NT) is involved in the final step of the enzymatic hydrolysis cascade that is the conversion of adenosine monophosphate (AMP) to adenosine and therefore, involves the regulation of adenosine level in extracellular space. The overexpression of h-e5'NT has been observed in various pathological conditions such as hypoxia, inflammation and cancers, and led to various complications. Hence, the identification of a potent as well as selective inhibitor of h-e5'NT is of greater importance in therapeutic treatment of various diseases. Azomethine-thioxoimidazolidinone derivatives were studied for their inhibition potential against e5'NT enzyme along with cytotoxic potential against cancer cell lines possessing overexpression of e5'NT enzyme. The derivative (E)-3-((4-((3-methoxybenzyl)oxy)benzylidene)amino)-2-thioxoimidazolidin-4-one (4g) displayed selective and significant inhibition towards h-e5'NT with an IC50 value of 0.23 ± 0.08 µM. While two other derivatives i.e., (E)-3-(((5-bromothiophen-2-yl)methylene)amino)-2-thioxoimidazolidin-4-one (4b) and 2-thioxo-3-((3,4,5-trimethoxybenzylidene)amino)imidazolidin-4-one (4e), exhibited non-selective potent inhibitory behavior against both human and rat enzymes. Moreover, these derivatives (4b, 4e and 4g) were further investigated for their effect on the expression of h-e5'NT using quantitative real time polymerase chain reaction. Additionally, molecular docking and DFT studies were also performed to determine the putative binding mode of potent inhibitors within the enzyme active site. HOMO, LUMO, ΔE, and molecular electrostatic potential maps were computed by DFT and the charge transfer regions within the molecules were identified to find out the regions for electrophilic and nucleophilic attack.

Development and exploration of novel substituted thiosemicarbazones as inhibitors of aldose reductase via in vitro analysis and computational study.

The role of aldose reductase (ALR2) in causing diabetic complications is well-studied, with overactivity of ALR2 in the hyperglycemic state leading to an accumulation of intracellular sorbitol, depletion of cytoplasmic NADPH and oxidative stress and causing a variety of different conditions including retinopathy, nephropathy, neuropathy and cardiovascular disorders. While previous efforts have sought to develop inhibitors of this enzyme in order to combat diabetic complications, non-selective inhibition of both ALR2 and the homologous enzyme aldehyde reductase (ALR1) has led to poor toxicity profiles, with no drugs targeting ALR2 currently approved for therapeutic use in the Western world. In the current study, we have synthesized a series of N-substituted thiosemicarbazones with added phenolic moieties, of which compound 3m displayed strong and selective ALR2 inhibitory activity in vitro (IC50 1.18 µM) as well as promising antioxidant activity (75.95% free radical scavenging activity). The target binding modes of 3m were studied via molecular docking studies and stable interactions with ALR2 were inferred through molecular dynamics simulations. We thus report the N-substituted thiosemicarbazones as promising drug candidates for selective inhibition of ALR2 and possible treatment of diabetic complications.

Nucleotide pyrophosphatase/phosphodiesterases (NPPs) including NPP1 and NPP2/ ATX as important drug targets: A patent review (2015-2020).

INTRODUCTION: Ectobucleotidases are a broad class of extracellular nucleotide and nucleoside hydrolyzing enzymes. Since they play a crucial role in mediating purinergic cell signalling, they are promising therapeutic targets for treatment of a range of disorders, including fibrosis, tumor metastasis, inflammation, multiple sclerosis, and autoimmune diseases. Hence selective inhibtors of ectonulceotidases are of great interest for therapeutic intervention. AREA COVERED: Many compounds have demonstrated promising inhibitory potential against ecto-nucleotide pyrophosphatase/phosphodiesterases (NPPs). The chemistry and clinical applications of NPP inhibitors patented between 2015 and 2020 are discussed in this review. EXPERT OPINION: In recent years, there has been a lot of effort towards finding effective and selective inhibitors of NPPs. Even though a number of inhibitors are known, only a few in vivo investigations have been published. In addition to IOA-289, which has passed Phase Ia clinical trials, potent NPP2/ATX inhibitor compounds such as BLD-0409, IPF and BBT-877 have been placed in phase I clinical studies. Some of the most promising NPP2/ATX inhibitors in recent years are closely related analogs of previously known inhibitors, such as PF-8380. Knowledge of the structure activity relationship of such promising inhibitors can potentially translate into the discovery of more potent and effective inhibitors of NPP.

Feasible regeneration and agro bacterium-mediated transformation of Brassica juncea with Euonymus alatus diacylglycerol acetyltransferase (EaDAcT) gene.

In the present study an effort has been made to optimize the in vitro regeneration protocol for Agrobacterium-mediated transformation of Brassica juncea, because of its importance as oilseed crops. The highest callus induction frequency of 87% was observed on MS (Murashige and Skoog, 1962) medium supplemented with 4 µM 6-benzyladenine (BA) after four weeks of culture period. Subculturing of organogenic calli in MS media with a similar hormonal composition resulted in shoot organogenesis after six weeks of culture cultivation. The highest shoot induction frequency (92%) was recorded on MS medium containing 4 µM BA in combination with 1 µM of α-naphthalene acetic acid (NAA). Further, well-developed roots were formed in MS media augmented with 6 µM of Indole acetic acid (IAA) in combination with 1 µM Kinetin (Kn). Cotyledon explants were exploited in vitro for the successful transformation of B. juncea. A binary vector comprised of the Euonymus alatus diacylglycerol acetyltransferase (EaDAcT) gene under the transcriptional control of a glycinin promoter and with a basta selection marker was introduced into A. tumefaciens strain GV3101 via electroporation. EaDAcT gene is responsible for unusual triacylglycerol's production where the sn-3 position is esterified with acetate instead of the long-chain fatty acid found in the triacylglycerol's. The highest regeneration frequency (100%) of transgenic shoots was observed on MS medium supplemented with 4 µM BA plus 1 µM NAA in the presence of 25 mg l-1 basta and 160 mg l-1 timintin. The efficiency of stable transformation was found to be approximately 7% in the transgenic plants. Moreover, the transformed regenerated shoots were confirmed by PCR analysis using EaDAcT gene-specific primers.

Arsenic in a groundwater environment in Bangladesh: Occurrence and mobilization.

Groundwater with an excessive level of Arsenic (As) is a threat to human health. In Bangladesh, out of 64 districts, the groundwater of 50 and 59 districts contains As exceeding the Bangladesh (50 µg/L) and WHO (10 µg/L) standards for potable water. This review focuses on the occurrence, origin, plausible sources, and mobilization mechanisms of As in the groundwater of Bangladesh to better understand its environmental as well as public health consequences. High As concentrations mainly was mainly occur from the natural origin of the Himalayan orogenic tract. Consequently, sedimentary processes transport the As-loaded sediments from the orogenic tract to the marginal foreland of Bangladesh, and under the favorable biogeochemical circumstances, As is discharged from the sediment to the groundwater. Rock weathering, regular floods, volcanic movement, deposition of hydrochemical ore, and leaching of geological formations in the Himalayan range cause As occurrence in the groundwater of Bangladesh. Redox and desorption processes along with microbe-related reduction are the key geochemical processes for As enrichment. Under reducing conditions, both reductive dissolution of Fe-oxides and desorption of As are the root causes of As mobilization. A medium alkaline and reductive environment, resulting from biochemical reactions, is the major factor mobilizing As in groundwater. An elevated pH value along with decoupling of As and HCO3- plays a vital role in mobilizing As. The As mobilization process is related to the reductive solution of metal oxides as well as hydroxides that exists in sporadic sediments in Bangladesh. Other mechanisms, such as pyrite oxidation, redox cycling, and competitive ion exchange processes, are also postulated as probable mechanisms of As mobilization. The reductive dissolution of MnOOH adds dissolved As and redox-sensitive components such as SO42- and oxidized pyrite, which act as the major mechanisms to mobilize As. The reductive suspension of Mn(IV)-oxyhydroxides has also accelerated the As mobilization process in the groundwater of Bangladesh. Infiltration from the irrigation return flow and surface-wash water are also potential factors to remobilize As. Over-exploitation of groundwater and the competitive ion exchange process are also responsible for releasing As into the aquifers of Bangladesh.

Steroidal alkaloids efficient aromatase inhibitors with potential for the treatment of postmenopausal breast cancer.

Plant-derived natural products are of great interest due to their diversity in modern drug discovery. Sarcococca saligna has been used for the treatment of different diseases. The present study was aimed at isolating phytochemical constituents including Alkaloid-C (a), Dictyophlebine (b), Sarcovagine-D (c) and Saracodine (d) Holaphylline (e) from Sarcococca saligna to investigate the anticancer effect of these compounds. These compounds were evaluated for inhibition of aromatase enzyme of breast cancer in assistance by molecular docking simulations to understand molecular interaction between the enzyme and ligands. The IC50 values of compound 1 and 5 were found 138.27 ± 0.01 µl and 12.91 ± 0.01 µl, respectively, and both were found active due to their bulky structures in comparison to the active site of aromatase enzyme. The standard drug exemestane showed potent activity in comparison with the test compounds, having IC50 values of 0.052 ± 0.01 µl. Both compounds showed favorable electrostatic interactions with the active site of aromatase enzyme but the shape and steric bulk of the compounds was the limiting factor in their inhibitory effects. New lead compounds could be generated after extensive modifications guided by computational and experimental tools as a possible anticancer agents by targeting aromatase enzyme.

Integration of poultry manure and phosphate solubilizing bacteria improved availability of Ca bound P in calcareous soils.

A laboratory incubation experiment was executed to examine the role of phosphate solubilizing bacteria (with PSB and without PSB) and poultry manure (4, 8 and 12 t PM ha-1) in improving P mobilization/mineralization under four different lime regimes (4.78, 10, 15 and 20% CaCO3 M/M) for 56 days using three factorial complete randomized design (CRD) with triplicates. Phosphorus availability progressively increased over time irrespective of PSB inoculation, PM and lime levels. The PSB and PM (4-12 t ha-1) addition into soil significantly increased Olsen P at all incubation intervals. Post incubation PSB survival increased by 12 and 9% with inoculation and 12 t PM ha-1 over control and 4 t PM ha-1, respectively. Liming ominously reduced P mobilization/mineralization by 1.3, 2.6 and 10.5% and PSB population by 6.6, 7.3 and 16.3% at 10, 15 and 20% (lime), respectively, over control at day 56. However, PSB and PM addition (with increasing rate) into soil significantly counterbalanced these ill effects of lime. Thus, the application of PSB and PM is a promising measure to enhance P availability in calcareous soils and shall be practiced.

High arsenic contamination and presence of other trace metals in drinking water of Kushtia district, Bangladesh.

Drinking water with excessive concentration levels of arsenic (As) is a great threat to human health. A hydrochemical approach was employed in 50 drinking water samples (collected from Kushtia district, Bangladesh) to examine the occurrence of geogenic As and the presence of trace metals (TMs), as well as the factors controlling As release in aquifers. The results reveal that the drinking water of shallow aquifers is highly contaminated by As (6.05-590.7 µg/L); 82% of samples were found to exceed the WHO recommended limit (10 µg/L) for potable water, but the concentrations of Si, B, Mn, Sr, Se, Ba, Fe, Cd, Pb, F, U, Ni, Li, and Cr were within safe limits. The Ca-HCO3-type drinking water was identified as having high contents of As, pH and HCO3-, a medium-high content EC, and low concentrations of NO3-, SO42-, K+, and Cl-. The significant correlation between As and NO3- indicates that NO3- might be attributed to the use of phosphate fertilizers and a factor responsible for enhancing As in aquifers. The study also reports that the occurrence of high As and the presence of TMs in drinking water may be a result of local anthropogenic activities, such as irrigation, intensive land use and the application of agrochemicals. The insignificant correlation between As and SO42- demonstrated that As is released from SO42- minerals under reducing conditions. An elevated pH value along with decoupling of As and HCO3- plays a vital role in mobilizing As to aquifer systems. Moreover, the positive relationship between As and Si indicated that As is transported in the biogeochemical environment. The reductive suspension of Mn(IV)-oxyhydroxides also accelerated the As mobilization process. Over exploitation of tube-well water and the competitive ion exchange process are also responsible for the release of As in aquifers.

Host Selection Behavior of the Green Peach Aphid, Myzus persicae, in Response to Volatile Organic Compounds and Nitrogen Contents of Cabbage Cultivars.

Plants emit volatile organic compounds (VOCs) in response to herbivore attack. VOCs emitted from the Chinese cabbage cultivars in response to the damage by the green peach aphid, Myzus persicae, were unknown. Using a solid-phase microextraction-based headspace collection method, we investigated and compared the emissions of VOCs from seven Chinese cabbage cultivars (Qibao, Qingan 80, Lvlong, Yuanbao, Qingan 70, Jinlv, and Lvqiu 66) in response to M. persicae attack. Our results showed that the VOCs emitted from the cultivars Qingan 80 and Yuanbao differed significantly from the other cultivars in response to the attraction of wingless M. persicae. Most importantly, out of the 27 detected compounds, α-caryophyllene was detected only in Qingan 80 and Qibao, but not in the other five cultivars. Among the compounds detected, 2 monoterpene and 12 terpenes were predominant in all cabbage cultivars. Furthermore, the wingless M. persicae showed preference to Qingan 80 while it had the highest nitrogen content among the tested cultivars. Moreover, we found a remarkable relationship among M. persicae attraction, plant nitrogen content, and total volatile emissions. Nitrogen content of the plants has a significant impact on volatile emission and preference behavior of M. persicae. Our results indicate that the wingless M. persicae were efficient in their interspecific host selection with an ability to distinguish plant cultivar differences by leaf nitrogen content. This study will be helpful in understanding aphid host selection, and sets a stage to further study the attractant-based integrated aphid management programs.

Suppressing photorespiration for the improvement in photosynthesis and crop yields: A review on the role of S-allantoin as a nitrogen source.

Environmental variations resulting in biotic and abiotic stresses demand adaptive changes in the photosynthetic machinery. To cope with these challenges, plant scientists are constantly striving to enhance photosynthetic activity. The photorespiration pathway, which fixes O2 and releases CO2 in C3 plants, competes with photosynthesis. One method to increase yield would be to enhance photosynthesis by engineering the photorespiratory pathway. To date, three engineered photorespiratory pathways have been produced, of which two have been proven experimentally in the model plant, Arabidopsis thaliana. These approaches might be helpful in enhancing crop resilience to future environmental challenges. In partially photorespiratory suppressed plants, it is hypothesized that a gene cluster may have formed between bacterial glycolate dehydrogenase (GDH), glyoxylate carboligase (GCL), and tartronic semi aldehyde (TSR) genes with Arabidopsis allantoin degradation genes like Arabidopsis allantoinase (AtALN) to utilize S-allantoin as a source of nitrogen. Observations of the use of allantoin as an exclusive source of nitrogen or energy by Arabidopsis and Escherichia coli led us to propose a genetic switch control model between nitrogen assimilation and energy producing pathways in partially photorespiratory suppressed plants.

Luteolin, a flavonoid, as an anticancer agent: A review.

Many food-derived phytochemicals and their derivatives represent a cornucopia of new anti-cancer compounds. Luteolin (3,4,5,7-tetrahydroxy flavone) is a flavonoid found in different plants such as vegetables, medicinal herbs, and fruits. It acts as an anticancer agent against various types of human malignancies such as lung, breast, glioblastoma, prostate, colon, and pancreatic cancers. It also blocks cancer development in vitro and in vivo by inhibition of proliferation of tumor cells, protection from carcinogenic stimuli, and activation of cell cycle arrest, and by inducing apoptosis through different signaling pathways. Luteolin can additionally reverse epithelial-mesenchymal transition (EMT) through a mechanism that involves cytoskeleton shrinkage, induction of the epithelial biomarker E-cadherin expression, and by down-regulation of the mesenchymal biomarkers N-cadherin, snail, and vimentin. Furthermore, luteolin increases levels of intracellular reactive oxygen species (ROS) by activation of lethal endoplasmic reticulum stress response and mitochondrial dysfunction in glioblastoma cells, and by activation of ER stress-associated proteins expressions, including phosphorylation of eIF2α, PERK, CHOP, ATF4, and cleaved-caspase 12. Accordingly, the present review article summarizes the progress of recent research on luteolin against several human cancers.

Anticancer potential of quercetin: A comprehensive review.

Diet plays a key role to maintaining healthy life. Many natural products present in our diet, such as flavonoids, can prevent the progression of cancer. Quercetin, a distinctive bioactive flavonoid, is a dietary component that has attracted the attention of dietitians and medicinal chemists due to its numerous health-promoting effects. It is an outstanding antioxidant that has a well-documented role in reducing different human cancers. Quercetin exhibits direct proapoptotic effects on tumor cells and thus can inhibit the progress of numerous human cancers. The anticancer effect of quercetin has been documented in numerous in vitro and in vivo studies that involved several cell lines and animal models. On the other hand, the high toxic effect of quercetin against cancer cells is accompanied with little or no side effects or harm to normal cells. Accordingly, this review presents an overview of recent developments on the use of quercetin against different types of cancer along with mechanisms of action. In addition, the present review summarizes the literature pertaining to quercetin as an anticancer agent and provides an assessment of the potential utilization of this natural compound as a complimentary or alternative medicine for preventing and treating cancer.