The auxin transporter OsAUX1 regulates tillering in rice(Oryza sativa)

Tillering is an important agronomic trait of rice(Oryza sativa)that affects the number of effective panicles,thereby affecting yields.The phytohormone auxin plays a key role in tillering.Here we identified the high tillering and semi-dwarf 1(htsd1)mutant with auxin-deficiency root characteristics,such as shortened lateral roots,reduced lateral root density,and enlarged root angles.htsd1 showed reduced sensitivity to auxin,but the external application of indole-3-acetic acid(IAA)inhibited its tillering.We identified the mutated gene in htsd1 as AUXIN1(OsAUX1,LOC_Os01g63770),which encodes an auxin influx transporter.The promoter sequence of OsAUX1 contains many SQUAMOSA PROMOTER BINDING PROTEIN-LIKE(SPL)binding sites,and we demonstrated that SPL7 binds to the OsAUX1 promoter.TEOSINTE BRANCHED1(OsTB1),a key gene that negatively regulates tillering,was significantly downregulated in htsd1.Tillering was enhanced in the OsTB1 knockout mutant,and the external application of IAA inhibited tiller elongation in this mutant.Overexpressing OsTB1 restored the multi-tiller phenotype of htsd1.These results suggest that SPL7 directly binds to the OsAUX1 promoter and regulates tillering in rice by altering OsTB1 expression to modulate auxin signaling.

Metal-Free Photocatalytic[4+2]Annulation of Acrylamides with 2-Benzyl-2-bromocarbonyls to Assemble Tetralin-1-carboxamides

Tetralin-1-carboxamides are frequently incorporated in myriad medicinally important molecules.However,their existing synthetic routes not only suffer from some drawbacks such as tedious procedures,harsh reaction conditions,narrow substrate scope,low yields,and environmental problems,but are also based upon the elaboration of uneasily available non-linear tetralin derivatives.Herein,we describe a metal-and additive-free visible light-induced[4+2]annulation of two simple linear starting materials,namely acrylamides and 2-benzyl-2-bromocarbonyls,through a cascade C(sp^(3))-Br/C(sp^(2))-H bond cleavage,double C-C bond formation,and aromatization sequence.The developed protocol provides a convenient,efficient,and green approach to a variety of tetralin-1-carboxamide derivatives with good functional group compatibility.Importantly,the resulting products could also undergo the Licl-mediated mono-decarboxylative cyclization process to further furnish the architecturally novel bridged polycyclic imides with excellentcis-diastereoselectivities.

Regeneration Function Analysis of GmESR1 in Transgenic Soybean

ENHANCER OF SHOOT REGENERATION(ESR1)is an important regulator of plant regeneration in vitro,which promotes regeneration of plant.In this study,transgenic positive plants with normal expression of proteins were screened by molecular assay.Through the study of the transgenic plants and the control Dongnong 50,the difference between immature embryo-induced callus and induced shoot bud was observed.The increase in callus weight indicated that GmESR1 gene accelerated the formations of shoot buds.By measuring the changes of hormone in the process of induction callus of transgenic plants,it was found that the contents of indole-3-acetic acid(IAA)and zeatin(ZT)in transgenic lines were significantly increased.It could be concluded that GmESR1 gene promoted the accumulation of hormone and affected regeneration process.In addition,this study also verified the interaction between GmBIM1 gene and GmESR1 gene by bimolecular fluorescence complementation(BiFC).

Regioselective Synthesis and Base Catalyzed Transacylation of Substituted 1H-Pyrazole-4-carboxamides

New type of substituted 1H-pyrazole-4-carboxamides were obtained byregioselective synthesis under the catalysis of different bases. The structures of the titlecompounds were confirmed by elemental analysis, ~1H NMR, IR, MS and X-ray crystallography. Compounds1 were transacylated into their corresponding amides 3 in the presence of sodium hydride.Preliminary bioassays indicated that some compounds showed fungicidal activities against Rhizoctoniasolani and Sclerotinia sclerotiorum.

Indole-3-propionic Acid-aggravated CCl_(4)-induced Liver Fibrosis via the TGF-β1/Smads Signaling Pathway

Background and Aims:The pathogenesis of liver fibrosis involves liver damage,inflammation,oxidative stress,and intestinal dysfunction.Indole-3-propionic acid(IPA)has been demonstrated to have antioxidant,anti-inflammatory and anticancer activities,and a role in maintaining gut homeostasis.The current study aimed to investigate the role of IPA in carbon tetrachloride(CCl4)-induced liver fibrosis and explore the underlying mechanisms.Methods:The liver fibrosis model was established in male C57BL/6 mice by intraperitoneal injection of CCl4 twice weekly.IPA intervention was made orally(20 mg/kg daily).The degree of liver injury and fibrosis were assessed by serum alanine aminotransferase(ALT),aspartate aminotransferase(AST),and histopathology.Enzyme-linked immunosorbent assay and quantitative real-time polymerase chain reaction(qPCR)were used to detect the inflammatory cytokines.The malondialdehyde(MDA),glutathione,glutathione peroxidase,superoxide dismutase,and catalase were determined via commercial kits.Hepatocyte apoptosis was detected by terminal deoxynucleotidyl transferase-mediated dUTP nick end labeling assay.The expression of mRNA and protein was assayed by qPCR,Western blotting,or immunohistochemical staining.Results:After IPA treatment,the ALT and AST,apoptotic cells,and pro-inflammatory factor levels were enhanced significantly.Moreover,IPA intervention up-regulated the expression of collagen I,α-smooth muscle actin,tissue inhibitor of matrix metalloproteinase-1,matrix metalloproteinase-2,transforming growth factor-β1(TGF-β1),Smad3,and phosphorylated-Smad2/3.Additionally,IPA intervention did not affect the MDA level.Attractively,the administration of IPA remodeled the gut flora structure.Conclusions:IPA aggravated CCl_(4)-induced liver damage and fibrosis by activating HSCs via the TGF-β1/Smads signaling pathway.

Multi-walled carbon nanotube as a solid phase extraction adsorbent for analysis of indole-3-butyric acid and 1-naphthylacetic acid in plant samples

In this work, a new sample pretreatment method prior to HPLC separations was developed for the determination of auxins in plant samples, Owing to its large surface area and high adsorption capacity, multi-walled carbon nanotube （MWCNT） was chosen as the adsorbent for the extraction of auxins from plant samples. In this study, two important auxins were selected as model analytes, namely indole-3- butyric acid （IBA） and 1-naphthylacetic acid （NAA）. They could be extracted and concentrated due to their π-π stacking interactions with MWCNT. Then HPLC-UV was introduced to detect IBA and NAA after sample pretreatment. Factors that may affect the enrichment efficiency were investigated and optimized. Comparative studies showed that MWCNT was superior to CI 8 for the extraction of the two analytes. Validation experiments showed that the optimized method had good linearity （0.9998 and 0.9960）, high recovery （81.4%-85.4%）, and low detection limits （0.0030 mg/L and 0.0012 mg/L）. The results indicated that the novel method had advantages of convenience, good sensitivity, high efficiency, and it was feasible for the determination of auxins in plant samples.

Design, synthesis and insecticidal activities of novel 1-substituted-5-(trifluoromethyl)-1H-pyrazole-4-carboxamide derivatives

A series of novel 5-（trifluoromethyl）-1H-pyrazole-4-carboxamide derivatives（6a–6n, 7a, 7b, and 8a-8f）were synthesised by placing the amide bond at the 4-position of the pyrazole ring. These derivatives differed from the structure of chlorantraniliprole analogues with the amide bond at the 5-position of the pyrazole ring. Preliminary bioassay results revealed that a few title compounds exhibited good insecticidal activities against lepidopteran pests, such as Plutella xylostella, Mythimna separate, Heliothis armigera, and Ostrinia nubilalis. Some title compounds also elicited broad-spectrum insecticidal activities against dipterous insects including Culex pipiens pallens after altering the amide position. Similar to pyrazole-5-carboxamide analogues, compounds 6b and 6e showed 100% insecticidal activity against P. xylostella, C. pipiens pallens, and M. separate at concentrations of 200, 2, and 200 mg/m L, respectively.This finding suggested that 5-（trifluoromethyl）-1H-pyrazole-4-carboxamide derivatives are potential alternative insecticides for management of agriculture pests.

In <i>Vitro</i>Clonal Propagation from Adult Material of a Savannah Species of Socio-Economic Importance: <i>Annona senegalensis</i>Pers.

Annona senegalensis (Pers.) or Annone from Senegal is a species found in the West African savannah and para-littoral sands. It offers real possibilities of socio-economic use, particularly in the medical, nutritional, ecosystem conservation and poverty alleviation fields. However, this wild species remained not fully exploited despite its potentialities. As a result, there is a need to regenerate this species;therefore, the in vitro propagation from adult material was undertaken. For this purpose, axillary nodes from plant regrowth taken from elderly subjects were aseptically introduced into different media enriched or not with phytohormones. Among the 3 culture media tested, that of Murashige and Skoog (MS, 1962) was the most reactive and made it possible to develop a micropropagation protocol for adult material of A. senegalensis. Thus, the introduction of these explants in media containing cytokinins (BAP and Kinetin) significantly increased the reactivity compared to media without hormones. If the best average numbers of shoots (2.3) and nodes (5.3) are obtained in MS + BAP 2 mg·L−1, with a reactivity of 91.66%, the addition of 0.1 mg·L−1 NAA gave the best average length (8.25 cm) of vitroplants. An induction time of 3 days into darkness with IBA at 50 mg·L−1, followed by a transfer to hormone-free expression medium (MS/2) under light, resulted in a rooting rate of 58.33%. After the gradual weaning of the young plants in a mini-greenhouse, under shade for 3 weeks, 50% of the plants survived. This in vitro regeneration protocol can therefore be adopted for the clonal propagation of adult material of A. senegalensis. However, the rooting rate can be improved by trying other hormonal combinations based on auxins or by considering ex-vitro rooting during shade weaning.

<i>In Vitro</i>Clonal Propagation from Juvenile and Different Explant Types of Two Edible <i>Annonaceae</i>Species: <i>Annona muricata</i>L. and <i>Annona squamosa</i>L.

Annona muricata L. and Annona squamosa L. are tropical species whose fleshy fruit is edible. They offer real possibilities for socio-economic use, particularly in the fields of medicine, nutrition, ecosystem conservation and the poverty alleviation. This study was set up to evaluate different methods of micropropagation from juvenile material for the regeneration of these species. Thus, MS medium supplemented with [BAP 2 mg·L-1] i.e. M2 produced 2.87 newly formed shoots from the cotyledonary nodes of A. muricata. For the terminal apices of A. squamosa, it was MMS medium supplemented with [BAP 2 mg·L-1] i.e. MM2 that was most conducive to new shoot formation (3.12). The addition of 0.1 and 0.2 mg·L-1 of NAA in the M2 medium, made it possible to have the best elongations and average number of nodes for the new shoots from cotyledonary nodes of A. muricata (9.11 cm for 5.62 nodes). With A. squamosa, MM7 medium [MMS + BAP 1 mg·L-1 + KIN 1 mg·L-1] resulted in an average length of 9.05 cm with 5.62 nodes on average for the apical shoots. A 3-day rhizogenic induction period in the dark with [IBA 50 mg·L-1] and 2 g·L-1 of activated charcoal gave a rooting rate of 66.67% for shoots originating from the cotyledonary nodes of A. squamosa;while with vitroplants from cotyledonary nodes of A. muricata, a better rooting rate (83.33%) was obtained following a 5-day rhizogenic induction. After 30 days of acclimatization, the survival rate reached 83.33% for plants from the tips of A. muricata, whereas for A. squamosa, it was plants grown from cotyledonary nodes that had the same survival rate.

Synthesis and biological evaluation of indole-3-carboxamide derivatives as antioxidant agents

Oxidative stress results in various pathologies and as consequence antioxidant agents have attracted uninterrupted attention.In this paper,a novel series of indole-3-carboxamide derivatives(6 a-61) were designed and synthesized based on the melatonin structure as novel antioxidants.All of them were evaluated for the antioxidant activities in vitro against human neuroblastoma SH-SY5 Y cell line using H2 O2 radical scavenging assay.The target compounds 6 a,6 f and 6 i indicated better activities than the positive control,ascorbic acid,and 6 a exhibited the best antioxidant activity.In addition,the structureactivity relationships of the target compounds were also preliminarily summarized based on the obtained experimental data.

Synthesis, Reactions and Antimicrobial Activity of Some New 3-Substituted Indole Derivatives

Reaction of indole-3-carboxaldehydes 4 with hydrazine derivatives and different substituted acid hydrazides afforded the corresponding hydrazine derivatives 5a-c and acid hydrazide derivatives 7-11 respectively. Condensation of indole-3-carboxaldehydes 4 with phenacyl bromide and thiourea gives 1,3-thiazol-2-amine derivative 18. On the other hand, reaction 4 with 3-acetylchromene-2-one afforded chalcone derivative 19. Compound 4 undergoing Knoevenagel condensation with cyanoacetamide, ethyl cyanoacetate, benzimidazol-2-ylacetonitrile, rhodanine-3-acetic acid, 2,3-dihydropyrimidin-4-one derivative and 2,4-dihydropyrazol-3-one afforded the compounds 20a,b, 22, 23, 27 and 28 respectively. The structure of the newly synthesized compounds has been confirmed by elemental analysis and spectra data. The antimicrobial activities of the some newly synthesized compounds were measured and showed that most of them have high

The Dependence of <i>N</i>-Malonyltryptophan Formation in Plants on Water Deficit (Review)

Drought stress in plants is accompanied by several metabolic changes. One of them is the appearance of N-malonyltryptophan (MT) during leaf wilting of many species, but there is a significant number of plant species in which the appearance of MT did not occur. Plants of some species were able to synthesize also N-acetyltryptophan (AT). Excised tomato leaves incubated with D-amino acids (including D-Trp) transform them into malonyl- and acetyl-derivatives even without water deficit. However, MT which appeared during water deficit has been shown to contain L-Trp. Amino acid—1-amino-cyclopropane-1-carboxylic acid (ACC) is also malonylated during water deficit, but other L-amino acids were not malonylated. N-malonyl transferases specific for Trp and ACC have been found in several plants. The existence of N-malonyltransferase specific to L-Trp and appeared during water deficit in plants forming MT is supposed, but clear experimental proof has not been obtained yet. Plants can transform MT applied exogenously into Trp and further to indole-3-acetic acid (IAA). But no evidence has been appeared up to now that endogenous MT may be a source of IAA. It is unknown till now why it is necessary for plants of many species to malonylate only Trp during water deficit. How MT metabolized in animals and if it affects them is also unknown. The necessity to use molecular-genetic approaches for the elucidation of the physiological significance of MT formation during water deficit is underlined.

Micropropagation from Juvenile Material of Annona senegalensis Pers.

Annona senegalensis is a savannah species present in the wild in tropical and sub-tropical African regions. It is used by the local populations for its many economic, pharmacological, nutritional and ecological interests. However, the strong pressure exerted on this species as well as the increasing degradation of the ecosystems, in which it evolves, seriously compromise its sustainability and development. Conventional methods of vegetative propagation are not sufficient to ensure its durable regeneration and the renewal of endemic populations in Senegal. In this context, it was undertaken in vitro propagation, from 30 days old juvenile seedlings. Thus, axillary, cotyledonary and apical nodes were in vitro cultured in Murashige and Skoog (1962) medium (MS), with different concentrations of cytokinins and/or auxins. BAP used alone at 2 mg•L−1 proved to be more beneficial for micropropagation of different types of explants compared to Kinetin used alone or in combination with BAP, especially for axillary and cotyledonary nodes. The BAP-NAA combination allowed to have a better elongation of newly formed shoots. For shoots of apical and cotyledonary nodes origin, a rhizogenic induction of 5 days, with IBA at 25 mg•L−1, resulted in a better rooting rate with, respectively, 75% (for 2.22 roots) and 66.67% (for 4.17 roots). For newly formed shoots of axillary origin, a 24-hour rooting induction with IBA at 50 mg•L−1 gave a rooting rate of 58.33% (for 2.4 roots). After 30 days of acclimatization, the survival rate was 75% for the young plants from the apices and 83.33% for those originating from the cotyledonary and axillary nodes. This protocol can therefore be adopted for the in vitro clonal propagation of A. senegalensis juvenile material.

Bactericidal bissulfone B7 targets bacterial pyruvate kinase to impair bacterial biology and pathogenicity in plants

The prevention and control of rice bacterial leaf blight(BLB)disease has not yet been achieved due to the lack of effective agrochemicals and available targets.Herein,we develop a series of novel bissulfones and a novel target with a unique mechanism to address this challenge.The developed bissulfones can control Xanthomonas oryzae pv.oryzae(Xoo),and 2-(bis(methylsulfonyl)methylene)-N-(4-chlorophenyl)hydrazine-1-carboxamide(B_(7))is more effective than the commercial drugs thiodiazole copper(TC)and bismerthiazol(BT).Pyruvate kinase(PYK)in Xoo has been identified for the first time as the target protein of our bissulfone B_(7).PYK modulates bacterial virulence via a CRP-like protein(Clp)/two-component system regulatory protein(reg R)axis.The elucidation of this pathway facilitates the use of B_(7)to reduce PYK expression at the transcriptional level,block PYK activity at the protein level,and impair the interaction within the PYK-Clp-reg R complex via competitive inhibition,thereby attenuating bacterial biology and pathogenicity.This study offers insights into the molecular and mechanistic aspects underlying anti-Xoo strategies that target PYK.We believe that these valuable discoveries will be used for bacterial disease control in the future.

Two homologous INDOLE-3-ACETAIVHDE (IAM) HYDROLASE genes are required for the auxin effects of IAM in Arabidopsis

Indole-3-acetamide(IAM)is the first confirmed auxin biosynthetic intermediate in some plant pathogenic bacteria.Exogenously applied IAM or production of IAM by overexpressing the bacterial iaaM gene in Arabidopsis causes auxin overproduction phenotypes.However,it is still inconclusive whether plants use IAM as a key precursor for auxin biosynthesis.Herein,we reported the isolation IAM HYDROLASE 1(IAMH1)gene in Arabidopsis from a forward genetic screen for IAM-insensitive mutants that display normal auxin sensitivities.IAMH1 has a close homolog named IAMH2 that is located right next to IAMH1on chromosomeⅣin Arabidopsis.We generated iamh1 iamh2 double mutants using our CRISPR/Cas9gene editing technology.We showed that disruption of the IAMH genes rendered Arabidopsis plants resistant to IAM treatments and also suppressed the iaaM overexpression phenotypes,suggesting that IAMH1 and IAMH2 are the main enzymes responsible for converting IAM into indole-3-acetic acid(IAA)in Arabidopsis.The iamh double mutants did not display obvious developmental defects,indicating that IAM does not play a major role in auxin biosynthesis under normal growth conditions.Our findings provide a solid foundation for clarifying the roles of IAM in auxin biosynthesis and plant development.