Same allocation proposed by an individual or a group elicits distinct responses: Evidence from event-related potentials and neural oscillation.

People tend to perceive the same information differently depending on whether it is expressed in an individual or a group frame. It has also been found that the individual (vs. group) frame of expression tends to lead to more charitable giving and greater tolerance of wealth inequality. However, little is known about whether the same resource allocation in social interactions elicits distinct responses depending on proposer type. Using the second-party punishment task, this study examined whether the same allocation from different proposers (individual vs. group) leads to differences in recipient behavior and the neural mechanisms. Behavioral results showed that reaction times were longer in the unfair (vs. fair) condition, and this difference was more pronounced when the proposer was the individual (vs. group). Neural results showed that proposer type (individual vs. group) influenced early automatic processing (indicated by AN1, P2, and central alpha band), middle processing (indicated by MFN and right frontal theta band), and late elaborative processing (indicated by P3 and parietal alpha band) of fairness in resource allocation. These results revealed more attentional resources were captured by the group proposer in the early stage of fairness processing, and more cognitive resources were consumed by processing group-proposed unfair allocations in the late stage, possibly because group proposers are less identifiable than individual proposers. The findings provide behavioral and neural evidence for the effects of "individual/group" framing leading to cognitive differences. They also deliver insights into social governance issues, such as punishing individual and/or group violations.

Investigation on the near-field cutoff effect in a subwavelength plasma shell with near-zero permittivity.

Although the plasma-induced receiving and radiating near-field cutoff phenomena in the subwavelength regime are found of crucial importance in electromagnetic (EM) signal transmissions and plasma property studies, their mechanisms to a large extent remain unclear and undistinguished. In this paper, in the perspective of field and energy transfer, it is demonstrated that the cutoff in the near-field regime is completely different from that in the geometric optical regime. Results show that, for the receiving mode, epsilon-near-zero (ENZ) plasmas can be treated as a nearly ideal EM fluid, and thus, EM waves are restricted into the plasma channel. For the radiating mode, on the other hand, it is the destructive interference between the electric dipole fields of the antenna and the ENZ plasma that results in vanishing far-field radiation. As an important supplement to the existing cutoff theories, our results not only offer clearer physical insights into the near-field cutoff effect but also provide a helpful reference for cutoff-related practical applications in various frequency bands.

Recombinant Klotho attenuates IFNγ receptor signaling and SAMHD1 expression through blocking NF-κB translocation in glomerular mesangial cells.

Interferon gamma (IFNγ) is a cytokine implicated in the pathogenesis of autoimmune diseases. SAM and HD domain-containing protein 1 (SAMHD1) is an IFNγ-inducible protein that modulates cellular dNTP levels. Mutations in the human SAMHD1 gene cause Aicardi-Goutières (AG) syndrome, an autoimmune disease sharing similar clinical features with systemic lupus erythematosus (SLE). Klotho is an anti-inflammatory protein which suppresses aging through multiple mechanisms. Implication of Klotho in autoimmune response is identified in rheumatologic diseases such as SLE. Little information exists regarding the effect of Klotho in lupus nephritis, one of the prevalent symptoms of SLE. The present study verified the effect of IFNγ on SAMHD1 and Klotho expression in MES-13 glomerular mesangial cells, a special cell type in glomerulus that is critically involved in lupus nephritis. IFNγ upregulated SAMHD1 expression in MES-13 cells through the Janus kinase-signal transducer and activator of transcription 1 (JAK-STAT1) and the nuclear factor kappa B (NFκB) signaling pathways. IFNγ decreased Klotho protein expression in MES-13 cells. Treatment of MES-13 cells with recombinant Klotho protein inhibited SAMHD1 expression by blocking IFNγ-induced NFκB nuclear translocation, but showed no effect on JAK-STAT1 signaling. Collectively, our findings support the protective role of Klotho in attenuating lupus nephritis through the inhibition of IFNγ-induced SAMHD1 expression and IFNγ downstream signaling in MES-13 cells.

Maternal Variability of Amplitudes of Frequency Fluctuations Is Related to the Progressive Self-Other Transposition Group Intervention in Autistic Children.

The self-to-other model of empathy (SOME) states that a key reason for the empathic deficiency in autistic individuals is the imbalance of the self-other switch. The existing interventions of theory of mind contain training of self-other transposition ability but combined with other cognitive trainings. The self-other distinction brain areas of autistic individuals have been revealed, but the brain areas of the self-other transposition ability and its intervention have not been investigated. There are normalized amplitudes of low-frequency fluctuations (mALFFs) within 0.01-0.1 Hz and many normalized amplitudes of frequency fluctuations (mAFFs) within 0-0.01, 0.01-0.05, 0.05-0.1, 0.1-0.15, 0.15-0.2, and 0.2-0.25 Hz. Therefore, the current study established a progressive self-other transposition group intervention to specifically and systematically improve autistic children's self-other transposition abilities. The transposition test with a three mountains test, an unexpected location test, and a deception test was used to directly measure autistic children's transposition abilities. The Interpersonal Responsiveness Index Empathy Questionnaire with perspective-taking and fantasy subscales (IRI-T) was used to indirectly measure autistic children's transposition abilities. The Autism Treatment Evaluation Checklist (ATEC) was used to measure autistic children's autism symptoms. The experiment was designed with two (intervention: experimental group vs. control group) independent variables and two (test time: pretest vs. posttest or tracking test) × three (test: transposition test vs. IRI-T test vs. ATEC test) dependent variables. Furthermore, it used eyes-closed resting-state functional magnetic resonance imaging to investigate and compare the relevant maternal mALFFs and average energy rank and energy rank variability of mAFFs of autistic children's transposition abilities, autism symptoms, and intervention effects. The results showed the following: (1) There were many improvements (pretest vs. posttest or tracking test) greater than chance 0 in the experimental group, such as the three mountains, lie, transposition, PT, IRI-T, PT tracking, cognition, behavior, ATEC, language tracking, cognition tracking, behavior tracking, and ATEC tracking improvements. However, there was no improvement greater than chance 0 in the control group. (2) The maternal mALFFs and maternal average energy rank and energy rank variability of mAFFs could predict the autistic children's transposition abilities, autism symptoms, and intervention effects with some overlap and some difference in maternal self-other distinction, sensorimotor, visual, facial expression recognition, language, memory and emotion, and self-consciousness networks. These results indicated that the progressive self-other transposition group intervention successfully improved autistic children's transposition abilities and reduced their autism symptoms; the intervention effects could be applied to daily life and last up to a month. The maternal mALFFs, average energy rank, and energy rank variability of mAFFs were three effective neural indictors of autistic children's transposition abilities, autism symptoms, and intervention effects, and the average energy rank and energy rank variability of mAFFs were two new neural indictors established in the current study. The maternal neural markers of the progressive self-other transposition group intervention effects for autistic children were found in part.

Achieving tunable Kerker-type invisibility for a radiation-enhanced electrically small antenna.

Low-temperature gaseous plasmas exhibit great potential in designing tunable and reconfigurable electromagnetic devices. In this paper, based on an overdense-underdense core-shell plasma structure, tunable Kerker-type invisibility for a radiation-enhanced electrically small antenna is achieved, where dominant scattering direction can be mutated between backward and forward while omnidirectional invisibility and signal enhancement are maintained. Moreover, by electromagnetic multipole decompositions, it is shown that the underdense outer plasma with a negative polarizability is able to weaken the strength and modulate the phase of the electric dipolar scattering component (a_{1}), while the magnetic dipolar term (b_{1}) nearly remains unchanged. Consequently, quasi-first and -second Kerker conditions are fulfilled near the cutoff band of a_{1}.

Luteolin alleviates ulcerative colitis by restoring the balance of NCR-ILC3/NCR+ILC3 to repairing impaired intestinal barrier.

Ulcerative colitis (UC) is a multifactorial, refractory chronic inflammatory disease. The primary factor leading to prolonged ulcerative colitis is the imbalance of the group 3 innate lymphoid cells (ILC3) subgroup resulting in the delayed reconstruction of damaged intestinal barrier. Previous studies show that luteolin had efficacy on UC, however, the potency of luteolin on restoring the balance of NCR-ILC3/NCR+ILC3 to repairing impaired intestinal barrier remains unclear. In this study, to investigate the potential mechanism of luteolin on ILC3 subgroup, we first evidenced that luteolin could promote transformation NCR-MNK3 to NCR+MNK3 in vitro. Then, a UC model was established in C57BL/6J mice to assess the efficacy of luteolin in restoring ILC3 subgroup balance and repairing intestinal barrier in chronic UC. Finally, the experiments in vitro validated the potential mechanism of luteolin in regulating ILC3 plasticity. The results showed that luteolin significantly alleviated the symptoms of DSS-induced UC in mice, including preventing body weight loss and decreasing the disease activity index (DAI) and intestinal damages. Additionally, luteolin increased NCR+ILC3 levels, promoted the production of IL-22 and decreased the levels of IL-17a and INF-γ in the intestine, and encourage intestinal barrier function recovery in UC mice by promoting the expression of ZO-1 and Occludin. Experiments in vitro revealed that luteolin facilitated the transformation of NCR-MNK3 to NCR+MNK3 and promoted the secretion of IL-22, which was linked to the Notch pathway. All results revealed that luteolin restored the balance of NCR-ILC3/NCR+ILC3 and contributed to repair of injured intestinal epithelium to alleviate ulcerative colitis.

Study on the Regulation Effect of Optogenetic Technology on LFP of the Basal Ganglia Nucleus in Rotenone-Treated Rats.

Background: Parkinson's disease (PD) is a common neurological degenerative disease that cannot be completely cured, although drugs can improve or alleviate its symptoms. Optogenetic technology, which stimulates or inhibits neurons with excellent spatial and temporal resolution, provides a new idea and approach for the precise treatment of Parkinson's disease. However, the neural mechanism of photogenetic regulation remains unclear. Objective: In this paper, we want to study the nonlinear features of EEG signals in the striatum and globus pallidus through optogenetic stimulation of the substantia nigra compact part. Methods: Rotenone was injected stereotactically into the substantia nigra compact area and ventral tegmental area of SD rats to construct rotenone-treated rats. Then, for the optogenetic manipulation, we injected adeno-associated virus expressing channelrhodopsin to stimulate the globus pallidus and the striatum with a 1 mW blue light and collected LFP signals before, during, and after light stimulation. Finally, the collected LFP signals were analyzed by using nonlinear dynamic algorithms. Results: After observing the behavior and brain morphology, 16 models were finally determined to be successful. LFP results showed that approximate entropy and fractal dimension of rats in the control group were significantly greater than those in the experimental group after light treatment (p < 0.05). The LFP nonlinear features in the globus pallidus and striatum of rotenone-treated rats showed significant statistical differences before and after light stimulation (p < 0.05). Conclusion: Optogenetic technology can regulate the characteristic value of LFP signals in rotenone-treated rats to a certain extent. Approximate entropy and fractal dimension algorithm can be used as an effective index to study LFP changes in rotenone-treated rats.

The effect of comprehensive rehabilitation program plus chemotherapy on quality of life in patients with postoperative non-small-cell lung cancer: study protocol of a multicenter randomized clinical trial.

BACKGROUND: Comprehensive rehabilitation therapy based on traditional Chinese medicine (TCM) has been widely applied in various cancer treatments in China. Thus far, Chinese herbal medicine (CHM) has been shown effective in reducing the adverse effects of chemotherapy and improving the quality of life (QoL) during chemotherapy. The purpose of the present study is to compare the effects of CHM plus Liu Zi Jue (LZJ) exercises with CHM plus rehabilitation education and with placebo plus rehabilitation education in patients who have undergone complete resection for nonsmall-cell lung cancer (NSCLC) followed by postoperative adjuvant chemotherapy. METHODS AND DESIGN: A multicenter, randomized clinical trial will be performed with 354 stage Ib-IIIa NSCLC patients in five centers in China. Patients satisfying the inclusion criteria will be randomly divided into three groups according to a 1:1:1 ratio: intervention group A (IGA), intervention group B (IGB), and control group (CG). Each group will receive adjuvant platinum-based doublet chemotherapy for a total of four cycles. IGA participants will receive chemotherapy combined with CHM and LZJ exercises, IGB participants will receive chemotherapy combined with CHM and rehabilitation education, and CG participants will receive chemotherapy combined with placebo and rehabilitation education. The herbal treatment patients will be given granules daily and LZJ exercises will be performed four times per week during chemotherapy. The primary outcome is QoL, which will be assessed with the European Organization for Research and Treatment of Cancer (EORTC)-QLQ-C43 scale in each cycle. The secondary outcomes include the 2-year disease-free survival rate, disease-free survival, TCM symptoms, tumor markers, safety, and adverse events. After treatment, the patients will be followed up every 3 months within 2 years and every 6 months after 2 years until disease recurrence and/or metastasis. DISCUSSION: Our previous study reported that CHM in combination with chemotherapy could lower the overall incidence of adverse events but increased digestive and gastrointestinal side effects compared with chemotherapy alone in postoperative NSCLC patients. This study will lay a foundation for the effectiveness of chemotherapy with or without a comprehensive rehabilitation program for QoL in patients with postoperative NSCLC. TRIAL REGISTRATION: ClinicalTrials.gov, NCT03372694. Retrospectively registered on 17 December 2018.

Adjuvant Chemotherapy with Chinese Herbal Medicine Formulas Versus Placebo in Patients with Lung Adenocarcinoma after Radical Surgery: a Multicenter, Randomized, Double-Blind, Placebo-Controlled Trial.

BACKGROUND: The toxicity and side effects caused by adjuvant chemotherapy (ACT) after radical surgery for lung adenocarcinoma (LAC) lead to early termination frequently. This study was conducted to provide an objective basis for the effect of Chinese herbal medicine formulas (CHMFs) combined with chemotherapy in reducing toxicity and enhancing efficacy of ACT. METHOD: From February 17th, 2012 to March 20th, 2015, 233 patients from 7 hospitals diagnosed with LAC in IB~IIIA stage were randomly assigned into ACT + CHMF group (116 patients) and ACT + placebo group (117 patients). CHMF was taken orally until the end of chemotherapy. Chemotherapy-related toxic, side effects were investigated as the primary outcome. Disease-free survival (DFS) and overall survival (OS) were used as the secondary outcome. RESULTS: At one week following chemotherapy, the incidence of dry mouth, diarrhea and thrombocytopenia significantly decreased in CHMF group (P = 0.017, P = 0.033, P = 0.019, respectively). At two weeks following chemotherapy, fatigue and diarrhea were more obvious in the placebo group (P = 0.028, P = 0.025, respectively). In addition, patients in the CHMF group showed an increase in median DFS from 37.1 to 51.5 months compared with placebo group although there was no statistical significance (P = 0.16). In the stage IB subgroup, the CHMF group had a significantly better DFS (HR (95% CI) = 0.53 (0.28-0.99), P = 0.046). There was no significant difference in OS between the groups (P = 0.72). CONCLUSION: For patients with LAC, ACT combined with CHMF after radical surgery can prolong the DFS time especially in the early stage, and reduces the chemotherapy-related toxic and side effects. TRIAL REGISTRATION: NCT01441752. Registered 14 July, 2011.

Total Synthesis of (-)-Gardmultimine A.

The first total synthesis of Gardneria oxindole alkaloid (-)-gardmultimine A has been achieved in 19 steps from d-tryptophan in a fully stereocontrolled manner. This synthesis features (1) an Ir-catalyzed regioselective C-H borylation/oxidation sequence to introduce the C12 methoxyl group, (2) a stereocontrolled oxidative rearrangement of indole to construct the spirooxindole motif, and (3) an Au(I)-catalyzed transannular Conia-ene-type 6-exo-dig cyclization to establish the azabicyclo[2.2.2]octane skeleton and the exocyclic E-alkene with exclusive stereoselectivity.

A Strategy to Construct cis-Hydrocarbazole via Nickel/Lewis Acid Dual-Catalyzed Arylcyanation.

A strategy for the synthesis of cis-hydrocarbazole with a C3 quaternary carbon center has been developed through nickel/Lewis acid dual-catalyzed arylcyanation. A wide array of cis-hydrocarbazoles was accessed with high diastereoselectivities and atom economies in a good yield. The rich chemistry of the installed nitrile group was demonstrated in the preparation of tryptamine- and tryptophol-derived cis-hydrocarbazoles.

Total Synthesis of (-)-Pepluanol†B: Conformational Control of the Eight-Membered-Ring System.

The first total synthesis of the Euphorbia diterpenoid pepluanol B in both racemic and enantioenriched form involves 20 steps from a known bicyclic diol. This synthesis features an unprecedented bromo-epoxidation to control the eight-membered-ring conformation. In addition, salient reactions for the construction of the tetracyclic backbone include a sterically challenging aldol reaction to establish the quaternary center, a ring closing metathesis (RCM) to forge the eight-membered ring, and a diastereoselective cyclopropanation to assemble the embedded cyclopropane motif.

Enhancement of thermoelectric performance across the topological phase transition in dense lead selenide.

Alternative technologies are required in order to meet a worldwide demand for clean non-polluting energy sources. Thermoelectric generators, which generate electricity from heat in a compact and reliable manner, are potential devices for waste heat recovery. However, thermoelectric performance, as encapsulated by the figure of merit ZT, has remained at around 1.0 at room temperature, which has limited practical applications. Here, we study the effects of pressure on ZT in Cr-doped PbSe, which has a maximum ZT of less than 1.0 at a temperature of about 700 K. By applying external pressure using a diamond anvil cell, we obtained a room-temperature ZT value of about 1.7. From thermoelectric, magnetoresistance and Raman measurements, as well as density functional theory calculations, a pressure-driven topological phase transition is found to enable this enhancement. Experiments also support the appearance of a topological crystalline insulator after the transition. These findings point to the possibility of using compression to increase not just ZT in existing thermoelectric materials, but also the possibility of realizing topological crystalline insulators.

Synthesis and insecticidal activity studies of novel phenylpyrazole derivatives containing arylimine or carbimidate moiety.

Phenylpyrazole insecticides are successful for crop protection and public hygiene by blocking gamma-aminobutyric acid (GABA)-gated chloride channels and glutamate-gated chloride (GluCl) channels. A series of novel phenylpyrazoles containing arylimine or 1-methoxyaryl groups were designed and synthesized. The addition reaction of methanol to the imines 1-11 was investigated and the cayno addition products 13-15 were obtained. The compounds 1-15 were confirmed by 1H NMR and elemental analysis. The results of bioassay indicated that some compounds exhibited comparable bioactivity to fipronil against a broad spectrum of insects such as bean aphid (Aphis craccivora), mosquito (Culex pipiens pallens), diamondback moth (Plutella xylostella) and Oriental armyworm (Mythimna separata). Especially, the foliar contact activity against bean aphid of compound 7 at 10 µg mL-1 was 68%, the larvacidal activity against mosquito of compounds 5, 13 and 15 at 0.0025 µg mL-1 was 100%, the larvacidal activity against diamondback moth of compounds 9 and 11 at 0.05 µg mL-1 was 100%, the larvacidal activity against Oriental armyworm of compound 9 at 1 µg mL-1 was 100%. The 3-cayno moiety on pyrazole ring was essential for the high insecticidal activities against bean aphid, diamondback moth and Oriental armyworm, while the 3-carbimidate moiety on pyrazole ring was crucial to the excellent high insecticidal activities against mosquito.

Chinese Herbal Medicine Combined With EGFR-TKI in EGFR Mutation-Positive Advanced Pulmonary Adenocarcinoma (CATLA): A Multicenter, Randomized, Double-Blind, Placebo-Controlled Trial.

Background: To determine the clinical activity and safety of Chinese herbal medicine (CHM) combined with epidermal growth factor receptor tyrosine kinase inhibitors (EGFR-TKI) in patients with advanced pulmonary adenocarcinoma (ADC) and the ability of CHM combined with EGFR-TKI to activate EGFR mutations. Methods: Three hundred and fifty-four patients were randomly assigned to EGFR-TKI (erlotinib 150 mg/d, gefitinib 250 mg/d, or icotinib 125 mg tid/d) plus CHM (TKI+CHM, N = 185) or EGFR-TKI plus placebo (TKI+placebo, N = 169). Progression-free survival (PFS) was the primary end point; the secondary end points were overall survival (OS), objective response rate (ORR), disease control rate (DCR), quality of life [Functional Assessment of Cancer Therapy-Lung (FACT-L) and Lung Cancer Symptom Scale (LCSS)], and safety. Results: The median PFS was significantly longer for the TKI+CHM group (13.50 months; 95% CI, 11.20-16.46 months) than with the EGFR-TKI group (10.94 months; 95% CI, 8.97-12.45 months; hazard ratio, 0.68; 95% CI, 0.51-0.90; P = 0.0064). The subgroup analyses favored TKI+CHM as a first-line treatment (15.97 vs. 10.97 months, P = 0.0447) rather than as a second-line treatment (11.43 vs. 9.23 months, P = 0.0530). Patients with exon 19 deletion had a significantly longer PFS than with 21 L858R. The addition of CHM to TKI significantly improved the ORR (64.32% vs. 52.66%, P = 0.026) and QoL. Drug-related grade 1-2 adverse events were less common with TKI+CHM. Conclusions: TKI+CHM improved PFS when compared with TKI alone in patients with EGFR mutation-positive advanced non-small-cell lung cancer (NSCLC). Clinical Trial Registration: www.ClinicalTrials.gov, identifier NCT01745302.

Selective Photooxidation of Amines and Sulfides Triggered by a Superoxide Radical Using a Novel Visible-Light-Responsive Metal-Organic Framework.

Photocatalysis is an efficient and sustainable approach to convert solar energy into chemical energy, simultaneously supplying valuable chemicals. In this study, a novel metal-organic framework (MOF) compound is constructed from anthracene-based organic linkers, which shows visible-light absorption and efficient photoinduced charge generation property. It was applied for triggering photooxidation of benzylamines and sulfides in the presence of environmental benign oxidants of molecular oxygen or hydrogen peroxide. Results show that it is a highly selective photocatalyst for oxidation reactions to produce valuable imines or sulfoxides. We further investigate the underlying mechanism for these photocatalytic reactions by recognizing reactive oxygen species in the reactions. It has been demonstrated that the superoxide radical (O2•-), generated by electron transfer from a photoexcited MOF to oxidants, serves as the main active species for the oxidations. The work demonstrates the great potential of photoactive MOFs for the transformation of organic chemicals into valuable complexes.

Maintenance Chemotherapy With Chinese Herb Medicine Formulas vs. With Placebo in Patients With Advanced Non-small Cell Lung Cancer After First-Line Chemotherapy: A Multicenter, Randomized, Double-Blind Trial.

Background: Chinese Herb Medicine Formulas (CHMF) was reported to improve the quality of life (QoL) in advanced NSCLC patients. The present study was designed to investigate whether maintenance chemotherapy plus CHMF in patients would improve QoL and progression-free survival (PFS). Methods: Seventy-one patients were enrolled from 8 medical centers in China, and were randomly assigned to a maintenance chemotherapy plus CHMF group (n = 35) or a maintenance chemotherapy plus placebo group (n = 36). The outcome measures included PFS, Karnofsky performance status (KPS) scores, QoL (assessed with the lung cancer symptom scale (LCSS) questionnaire), and adverse events (AEs). Results: Patients in the CHMF group showed significant improvements in median PFS (HR = 0.55, 95% CI 0.28-0.88, P = 0.019), KPS scores (P = 0.047), fatigue (cycle [C] 3: P = 0.03), interference with daily activities (C3: P = 0.04) and dyspnea (C2: P = 0.03) compared with patients in the placebo group. Compared with the placebo group, the incidence of AEs decreased in the CHMF group, including loss of appetite (C2: P = 0.011, C4: P = 0.004) and dry mouth (C4: P = 0.011). Conclusion: The essential finding of our study is that maintenance chemotherapy combined with CHMF may prolong PFS, relieve symptoms, improve QoL and alleviate the side effects.

Investigation of Novel Pesticides with Insecticidal and Antifungal Activities: Design, Synthesis and SAR Studies of Benzoylpyrimidinylurea Derivatives.

In order to find pesticides with insecticidal and antifungal activities, a series of novel benzoyl pyrimidinylurea derivatives were designed and synthesized. All target compounds were identified by ¹H-NMR spectroscopy and HRMS. Insecticidal and antifungal activity of these compounds were evaluated and the structure-activity relationships (SAR) were clearly and comprehensively illustrated. Compound 7, with low toxicity to zebrafish (LC50 = 378.387 µg mL-1) showed 100% inhibition against mosquito (Culex pipiens pallens) at 0.25 µg mL-1. Both compounds 19 and 25 exhibited broad-spectrum fungicidal activity (>50% inhibitory activities against 13 phytopathogenic fungi), which were better than those of the commercial pesticide pyrimethanil (>50% inhibitory activities against eight phytopathogenic fungi). Furthermore, compounds 19 and 25 exhibited protective activity against Sclerotinia sclerotiorum on leaves of Brassica oleracea L. during in vivo experiments.

Natural Product-Based Pesticide Discovery: Design, Synthesis and Bioactivity Studies of N-Amino-Maleimide Derivatives.

Natural products are an important source of pesticide discovery. A series of N-amino-maleimide derivatives containing hydrazone group were designed and synthesized based on the structure of linderone and methyllinderone which were isolated from Lindera erythrocarpa Makino. According to the bioassay results, compounds 2 and 3 showed 60% inhibition against mosquito (Culex pipiens pallens) at 0.25 µg·mL−1. Furthermore, the results of antifungal tests indicated that most compounds exhibited much better antifungal activities against fourteen phytopathogenic fungi than linderone and methyllinderone and some compounds exhibited better antifungal activities than commercial fungicides (carbendazim and chlorothalonil) at 50 µg·mL−1. In particular, compound 12 exhibited broad-spectrum fungicidal activity (>50% inhibitory activities against 11 phytopathogenic fungi) and compounds 12 and 14 displayed 60.6% and 47.9% inhibitory activity against Rhizoctonia cerealis at 12.5 µg·mL−1 respectively. Furthermore, compound 17 was synthesized, which lacks N-substituent at maleimide and its poor antifungal activity against Sclerotinia sclerotiorum and Rhizoctonia cerealis at 50 µg·mL−1 showed that the backbone structure of N-amino-maleimide derivatives containing hydrazone group was important to the antifungal activity.