Beneficial effects of thymoquinone and omega-3 on intestinal ischemia/reperfusion-induced renal dysfunction in rats

Intestinal ischemia–reperfusion (II/R) is a complex phenomenon causing local and remote tissue destruction and multiple-organ dysfunction. The technique has been used by many authors to produce certain organ dysfunctions. This study is to investigate the possible beneficial effects of thymoquinone and omega-3 separately in II/R-induced renal dysfunction in rats. Sixty-four Wistar albino rats were randomly allocated into four experimental groups namely sham control, II/R control, thymoquinone and omega-3 each group pre-treated separately. II/R model was established by clamping the superior mesenteric artery (SMA) for 30 min followed by 60 min reperfusion. Serum level of creatinine was measured. Renal tissue contents of malodialdehyde (MDA) and reduced glutathione (GSH) as well as myeloperoxidase (MPO), tumor necrosis factor alpha (TNF-α) and superoxide dismutase (SOD) activities were measured. Apoptosis in renal tissue cells was determined by immunohistochemical analysis of caspase-3. Renal histopathological examination was carried out. II/R elevated serum creatinine level. In-addition, renal tissue content of GSH and SOD activity were decreased. However renal tissue content of MDA and MPO activity were increased. Immunohistochemical analysis showed remarkable activation of caspase-3 in renal tissue. Histopathological examination revealed definite alterations after II/R. Pre-treatment with thymoquinone and omega-3 resulted in increased renal tissue content of GSH and SOD activity. The results revealed significant decrease in renal tissue content of MDA as well as MPO activity. Test drugs decreased the activity of caspase-3 through immunohistochemical examination. Thymoquinone and omega-3 corrected the reported histopathological changes induced by II/R. Depending on the obtained results in the present study it could be concluded that thymoquinone and omega-3 have beneficial effects on II/R-induced renal dysfunction in rats. The protective potential could be attributed to the antioxidant, antiapoptotic and anti-inflammatory effects of test drugs

Dihydromyricetin Modulates Nrf2 and NF-κB Crosstalk to Alleviate Methotrexate-Induced Lung Toxicity

Background: Methotrexate (MTX) is an effective anticancer, anti-inflammatory, and immunomodulatory agent. However, it induces a serious pneumonitis that leads to irreversible fibrotic lung damage. This study addresses the protective role of the natural flavonoid dihydromyricetin (DHM) against MTX-induced pneumonitis via modulation of Nrf2/NF-κB signaling crosstalk. Methods: Male Wistar rats were divided into 4 groups: control, which received the vehicle; MTX, which received a single MTX (40 mg/kg, i.p) at day 9 of the experiment; (MTX + DHM), which received oral DHM (300 mg/kg) for 14 days and methotrexate (40 mg/kg, i.p) on the 9th day; and DHM, which received DHM (300 mg/kg, p.o) for 14 days. Results: Lung histopathological examination and scoring showed a decline in MTX-induced alveolar epithelial damage and decreased inflammatory cell infiltration by DHM treatment. Further, DHM significantly alleviated the oxidative stress by decreasing MDA while increasing GSH and SOD antioxidant levels. Additionally, DHM suppressed the pulmonary inflammation and fibrosis through decreasing levels of NF-κB, IL-1β, and TGF-β1 while promoting the expression of Nrf2, a positive regulator of antioxidant genes, and its downstream modulator, HO-1. Conclusion: This study identified DHM as a promising therapeutic target against MTX-induced pneumonitis via activation of Nrf2 antioxidant signaling while suppressing the NF-κB mediated inflammatory pathways

Development of New Iso-Cytoplasmic Rice-Restorer Lines and New Rice Hybrids with Superior Grain Yield and Grain Quality Characteristics by Utilizing Restorers’ Fertility Genes

This research was carried out at the Experimental Farm of Sakha Agricultural Research Station, Sakha, Kafr El-Sheikh, Egypt, during the 2018–2020 rice-growing seasons to develop and evaluate four iso-cytoplasmic rice-restorer lines: NRL79, NRL80, NRL81, and NRL82, as well as Giza 178, with ten new hybrids in order to estimate genotypic coefficient, phenotypic coefficient, heritability in a broad sense, and advantage over Giza 178 as a check variety (control) of new restorer lines. This study also estimated combining ability, gene action, better-parent heterosis (BP), mid-parents heterosis (MP), and standard heterosis (SH) over Egyptian Hybrid one (IR69A × Giza 178) as a check hybrid (control) for grain yield, agronomic traits, and some grain quality characters in restorer lines and hybrids. The percentage of advantage over commercial-variety Giza 178 (check) was significant, and highly significant among the newly developed restorer fertility lines for all the studied traits. This indicates that the selection is a highly effective factor in improving these traits. New restorer fertility lines showed highly significant positive values over commercial restorer for grain yield; the values ranged from 51% for NRL80 to 100.4% for NRL82, respectively. Meanwhile, in regard to the grain shape of paddy rice, three lines of the promising lines showed highly significant negative desirable values compared with Giza 178; the values ranged from −7.7% for the NRL80 to −15.2% for NRL79, respectively. Based on the superiority of the new lines, the new lines can be used as new restorer fertility lines to breed promising new hybrids and new inbred rice lines or varieties. From the results of the testcross experiment, the four promising lines were identified as effective restorer fertility lines for two cytoplasmic male sterile (CMS) lines. Moreover, the six rice hybrids showed values for SH heterosis of grain yield/plant of more than 15% over the check hybrid variety, with high values of 1000-grain weight and desirable grain shape; these hybrids were G46A × NRL81 (125.1%), G46A × NRL80 (66.9%), IR69A × NRL79 (47.2%), G46A × NRL79 (24.6%), IR69A × NRL81 (23.4%), and IR69A × NRL82 (16.2%)

Combining Ability and Gene Action Controlling Agronomic Traits for Cytoplasmic Male Sterile Line, Restorer Lines, and New Hybrids for Developing of New Drought-Tolerant Rice Hybrids

This study aimed to identify new rice lines and hybrids that are tolerant to water deficit and produce high yields under water stress conditions. A line × tester mating design was used to study the lines and testers’ general combining ability (GCA) effects. The specific combining ability (SCA) of the hybrid rice combinations was measured under three different irrigation regimes; 6, 9, and 12 days. The study was carried out at the experimental farm of Sakha Agricultural Research Station, Sakha, Kafr El-Sheikh, Egypt, during the 2018 and 2019 rice growing seasons. Due to the genotypes and their partitions to the parents and the crosses, the mean squares were highly significant for all studied traits under the three irrigation regimes. The additive gene effects play an important role in expressing most of the studied traits. Therefore, the selection procedures based on the accumulation of the additive effect would be successful at improving these traits and the grain yield. The cytoplasmic male sterile (CMS) line G46A (L1) was the best combiner for most yield component traits in the three irrigation regimes. The newly devolved restorer lines T11, T1, T2, T5, T4, and T3, as well as the new hybrids L2 × T10, L2 × T6, L1 × T7, L1 × T5, L1 × T3, L2 × T7, L2 × T9, L2 × T8, L2 × T4, L1 × T4, L2 × T2, L1 × T8, L1 × T9, and L2 × NRL 10, showed good, desirable values of the studied traits such as earliness of flowering, short plant height, number of panicles/plant, panicle length, number of spikelets/panicle, number of filled grains/panicle, panicle weight, 1000-grain weight, hulling percentage, milling percentage, head rice percentage, and grain yield under the irrigation regimes of 6, 9, and 12 days. The hybrids L2 × T10, L2 × T6, L1 × T7, and L1 × T5, showed significant positive SCA effects for grain yield, under all three irrigation regimes

Assessment of Genetic Variability and Bran Oil Characters of New Developed Restorer Lines of Rice (Oryza sativa L.)

Rice is one of the most important crops in Egypt. Due to the gap between the demand and the availability of the local edible oils, there is need to raise the nutritional value of rice and, therefore, to improve the nutritional value of the consumer. This research was carried out at the Experimental Farm of Sakha Agricultural Research Station, Sakha, Kafr El-Sheikh, Egypt, during the 2019 and 2020 seasons. Five newly developed genotypes of rice, namely NRL 63, NRL 64, NRL 65, NRL 66, and Giza 178 as check variety (control), were used to evaluate the analytical characterization of raw rice bran and rice bran oil from rice bran, study the genetic variability and genetic advance for various quantitative and qualitative traits in rice as well as, rice bran oil. The genotypes were evaluated in a randomized complete block design (RCBD) with three replications. Analysis of variance revealed highly significant variations among the genotypes for all the studied characters. Data revealed that high estimates of the phenotypic coefficient of variance (PCV%) and genotypic coefficient of variance (GCV%) were observed for amylose content percentage, peroxide value (meq/kg oil), myristic C14:0, and arachidic C20:0, indicating that they all interacted with the environment to some extent. The line NRL66 and NRL64 showed the highest and high values of mean performance for grain yield (t/h), grain type (shape), amylose content percentage, crude protein, ether extract and ash of milled rice, crude protein, ether extract, ash, phosphorus, magnesium, manganese, zinc, and iron of stabilized rice bran oil. Genetic advance as a percentage of mean was high for most of the studied traits. It indicates that most likely, the heritability is due to additive gene effects, and selection may be effective. The percentage of advantage over the Giza 178 as the commercial variety was significant and highly significant among the genotypes for all the characters studied in the two years, indicating that the selection is effective in the genetic improvements for these traits

Development of New Restorer Lines Carrying Some Restoring Fertility Genes with Flowering, Yield and Grains Quality Characteristics in Rice (<em>Oryza sativa</em> L.)

This study was carried out using 22 promising restorer lines of rice and their parental lines to study genetic variability and genetic advance for yield and yield-associated grain quality traits and floral traits. These genotypes are evaluated in a replicated trial using Randomized Complete Block Design (RCBD) with three replications at the Experimental Farm of Sakha Agricultural Research Station, Sakha, Kafr El-Sheikh, Egypt, during the seasons from 2012 to 2020. Analysis of variance revealed that highly significant variations were observed among the genotypes for all the studied characters. Both GCV% and PCV% were high for the number of spikelets per panicle, the number of filled grains per panicle, and panicle weight. The genetic advance in the percentage of mean was high for days to plant height, panicle length, number of spikelets per panicle, number of filled grains per panicle, panicle weight, grain yield per plant, anther length, anther breadth, duration of floret opening, and head rice percentage. Mean performance of the rice genotypes indicated that the genotypes NRL 59, NRL 55, NRL 62, NRL 63, NRL 66, and NRL 54-2 were promising for grain yield and associated desirable traits. Thus, some of these promising lines can be promoted as a new rice variety and could be used as a source for developing new hybrid combinations in hybrid rice breeding programs. The percentage of advantage over better parent and Giza 178 as the commercial variety was significant and there were highly significant desirable values among the genotypes for all the studied traits in the two years, indicating that the selection is effective in the genetic improvements for these traits

Benzimidazole Bearing Thiosemicarbazone Derivatives Act as Potent &alpha;-Amylase and &alpha;-Glucosidase Inhibitors; Synthesis, Bioactivity Screening and Molecular Docking Study

Diabetes mellitus is one of the most chronic metabolic diseases. In the past few years, our research group has synthesized and evaluated libraries of heterocyclic analogs against &alpha;-glucosidase and &alpha;-amylase enzymes and found encouraging results. The current study comprises the evaluation of benzimidazole-bearing thiosemicarbazone as antidiabetic agents. A library of fifteen derivatives (7&ndash;21) was synthesized, characterized via different spectroscopic techniques such as HREI-MS, NMR, and screened against &alpha;-glucosidase and &alpha;-amylase enzymes. All derivatives exhibited excellent to good biological inhibitory potentials. Derivatives 19 (IC50 = 1.30 &plusmn; 0.20 &micro;M and 1.20 &plusmn; 0.20 &micro;M) and 20 (IC50 = 1.60 &plusmn; 0.20 &micro;M and 1.10 &plusmn; 0.01 &micro;M) were found to be the most potent among the series when compared with standard drug acarbose (IC50 = 11.29 &plusmn; 0.07 and 11.12 &plusmn; 0.15 &micro;M, respectively). These derivatives may potentially serve as the lead candidates for the development of new therapeutic representatives. The structure&ndash;activity relationship was carried out for all molecules which are mainly based upon the pattern of substituent/s on phenyl rings. Moreover, in silico docking studies were carried out to investigate the active binding mode of selected derivatives with the target enzymes