Prediction of the global occurrence of maize diseases and estimation of yield loss under climate change.

Background: Climate change significantly impacts global maize production via yield reduction, posing a threat to global food security. Disease-related crop damage reduces quality and yield and results in economic losses. However, the occurrence of diseases caused by climate change, and thus crop yield loss, has not been given much attention.

Triphenylphosphonium-linked derivative of hecogenin with enhanced antiproliferative activity: Design, synthesis, and biological evaluation.

Hecogenin (HCG), a steroidal sapogenin, possesses good antitumor properties. However, the application of HCG for cancer treatment has been hindered primarily by its moderate potency. In this study, we incorporated triphenylphosphonium cation (TPP) at the C-3 and C-12 positions through different lengths of alkyl chains to target mitochondria and enhance the efficacy and selectivity of the parent compound.

Targeting the Nrf2-dependent mechanism of b-Ecdysterone in attenuating the motor dysfunction in the MPTP/Pro-induced Parkinson's disease mice model.

Oxidative stress is a pivotal stimulating factor in neurocyte apoptosis and has been involved in the pathogenesis of Parkinson's disease (PD). In this study, we have demonstrated that the improvement in the motor disorder of 1-methyl-4-phenyl-1,2,3,6-tetrahydropyridine (MPTP)/Pro-induced mice caused by b-Ecdysterone (b-Ecd) treatment is due to its antioxidant properties. Using open field, rotarod, and pole climbing tests, we have found that b-Ecd alleviates motor disorder in MPTP/Pro-induced mice and ultimately reduces the impairment of tyrosine hydroxylase (TH)-positive dopaminergic neurons in the substantia nigra (SN).

Study on the influence of COVID-19 on the growth of China's small and medium-sized construction enterprises.

The outbreak of COVID-19 at the beginning of 2020 had a significant impact on China's economy, society, and citizens; it also had a negative impact on the development of the construction industry. In particular, small and medium-sized construction enterprises with low ability to withstand risk have been strongly impacted, aggravating a crisis of survival among these firms. The focus of this study is to analyze the impact of COVID-19 on the growth of small and medium-sized construction companies.

Design, synthesis and biological evaluation of novel diosgenin-benzoic acid mustard hybrids with potential anti-proliferative activities in human hepatoma HepG2 cells.

To discover new lead compounds with anti-tumour activities, in the present study, natural diosgenin was hybridised with the reported benzoic acid mustard pharmacophore. The cytotoxicity of the resulting newly synthesised hybrids (-, -, and -) was then evaluated in three tumour cells (HepG2, MCF-7, and HeLa) as well as normal GES-1 cells. Among them, possessed the most potential anti-proliferative activity against HepG2 cells, with an IC value of 2.

Synthesis and biological evaluation of celastrol derivatives as potential anti-glioma agents by activating RIP1/RIP3/MLKL pathway to induce necroptosis.

Celastrol, a quinone methide triterpenoid, possesses potential anti-glioma activity. However, its relatively low activity limit its application as an effective agent for glioma treatment. In search for effective anti-glioma agents, this work designed and synthesized two series of celastrol C-3 OH and C-20 COOH derivatives 4a-4o and 6a-6o containing 1, 2, 3-triazole moiety.

Novel diosgenin-amino acid-benzoic acid mustard trihybrids exert antitumor effects via cell cycle arrest and apoptosis.

In discovering new powerful antitumor agents, two series of novel diosgenin-amino acid-benzoic acid mustard trihybrids (7a-7 g and 12a-12 g) were designed and synthesized. The antiproliferative activities were tested against five human tumor cell lines and one normal cell line using CCK-8 assays. Among the trihybrids, 12e was the most promising compound, which inhibited T24 cells with IC value of 6.

DG-8d, a novel diosgenin derivative, decreases the proliferation and induces the apoptosis of A549 cells by inhibiting the PI3k/Akt signaling pathway.

Unlabelled: Lung neoplasm has a relatively poor prognosis, and the clinical efficacy of targeted medicine remains unsatisfactory. Therefore, the development of novel efficient anti-lung cancer drugs is urgently needed. In our previous study, we showed that a novel diosgenin derivative 8d (DG-8d), which contained 5-(3-pyridyl)-1,3,4-thiadiazole moiety, had significant cytotoxic activity on human tumor cells, especially the A549 cells.

Design and synthesis of diosgenin derivatives as apoptosis inducers through mitochondria-related pathways.

Diosgenin (DSG) has attracted attention recently as a potential anticancer therapeutic agent due to its profound antitumor activity. To better utilize DSG as an antitumor compound, two series of DSG-amino acid ester derivatives (3a-3g and 7a-7g) were designed and synthesized, and their cytotoxic activities against six human cancer cell lines (K562, T24, MNK45, HepG2, A549, and MCF-7) were evaluated. The results obtained showed that a majority of derivatives exhibited cytotoxic activities against these six human tumor cells.

Alkaloids constituents from the roots of (Cav.) Trin. ex Steud. with their cytotoxic activities.

Two new alkaloids, phranisines AB (), along with two known compounds, N-p-Coumaroyl serotonin () and N-p-coumaroyl-tryptamine (), were isolated from the roots of . The structures of were established on the basis of extensive spectroscopic. The absolute configuration of compounds were identified through quantum-chemical electronic circular dichroism (ECD) calculation compared with their experimental CD.

Novel diosgenin derivatives containing 1,3,4-oxadiazole/thiadiazole moieties as potential antitumor agents: Design, synthesis and cytotoxic evaluation.

Diosgenin, a naturally occurring steroidal saponin, has been confirmed to possess potent anticancer properties. In the current work, two series of novel diosgenin derivatives bearing 1,3,4-oxadiazole (6a-6e and 7a-7e) or 1,3,4-thiadiazole (8a-8e and 9a-9e) moieties were designed, synthesized and evaluated for their cytotoxicities in four human cancer cell lines (HepG2, A549, MCF-7 and HCT-116) and normal human gastric epithelial cells (GES-1) using the MTT assay in vitro. The results showed that compounds 8d and 9d exhibited significant cytotoxic activities against the HepG2 and A549 cells, being more potent than their parent compound diosgenin.

Glutathione Conjugation and Protein Adduction Derived from Oxidative Debromination of Benzbromarone in Mice.

Benzbromarone (BBR), a uricosuric agent, has been known to induce hepatotoxicity, and its toxicity has a close relation to cytochrome P450-mediated metabolic activation. An oxidative debromination metabolite of BBR has been reported in microsomal incubations. The present study attempted to define the oxidative debromination pathway of BBR in vivo.

Preparation and Evaluation of mPEG-PLGA Block Copolymer Micelles Loaded with a Sarsasapogenin Derivative.

Sarsasapogenin derivative 5n (SGD 5n) is a new compound with potent antitumor efficacy, but the low solubility severely affects its absorption and bioavailability. Therefore, the SGD 5n-loaded mPEG-PLGA block copolymer micelles were developed to improve the value of SGD 5n in clinical application. The polymeric micelles were prepared by an organic solvent evaporation method, and the encapsulation efficiency (EE), drug loading (DL), critical micelle concentrations (CMC), morphology, particle size, and zeta potential were determined.

Novel sarsasapogenin-triazolyl hybrids as potential anti-Alzheimer's agents: Design, synthesis and biological evaluation.

Sarsasapogenin, an active ingredient in Rhizoma anemarrhenae, is a promising bioactive lead compound in the treatment of Alzheimer's disease. To search for more efficient anti-Alzheimer agents, a series of novel sarsasapogenin-triazolyl hybrids were designed, synthesized, and evaluated for their Aβ aggregation inhibitory activities. Most of these new hybrids displayed potent Aβ aggregation inhibition.

and induction of the apoptotic effects of oxysophoridine on colorectal cancer cells via the Bcl-2/Bax/caspase-3 signaling pathway.

Oxysophoridine (OSR) is a major active alkaloid extracted from L. The aim of the present study was to investigate the induction of the apoptotic effects of OSR on colorectal cancer cells and . The results of the MTT and colony formation assays demonstrated that the proliferation of HCT116 cells was inhibited by OSR .

Synthesis of new sarsasapogenin derivatives with antiproliferative and apoptotic effects in MCF-7 cells.

Sarsasapogenin, a kind of mainly effective component of Anemarrhena asphodeloides Bunge, possesses good antitumor properties. Two series of new sarsasapogenin derivatives were synthesized and evaluated for their cytotoxicities against three human cancer cell lines (HepG2, A549, MCF-7) using the MTT assay. The structure-activity relationship revealed that the N, N-dimethylamino, pyrrolidinyl, and imidazolyl substituted at the C26 position could increase the antitumor efficacy of the 3-oxo sarsasapogenin series of compounds.

Metabolic Epoxidation Is a Critical Step for the Development of Benzbromarone-Induced Hepatotoxicity.

Benzbromarone (BBR) is effective in the treatment of gout; however, clinical findings have shown it can also cause fatal hepatic failure. Our early studies demonstrated that CYP3A catalyzed the biotransformation of BBR to epoxide intermediate(s) that reacted with sulfur nucleophiles of protein to form protein covalent binding both in vitro and in vivo. The present study attempted to define the correlation between metabolic epoxidation and hepatotoxicity of BBR by manipulating the structure of BBR.

Synthesis and evaluation of 26-amino acid methyl ester substituted sarsasapogenin derivatives as neuroprotective agents for Alzheimer's disease.

Sarsasapogenin, extracted from Anemarrhena asphodeloides Bunge., has been reported to protect neurons from HO-induced damage. In the current study, four series of 26-amino acid methyl ester substituted sarsasapogenin derivatives (5a-5e, 5f-5j, 6a-6e and 7a-7e) were synthesized and tested for neuroprotective activity by evaluating their neuroprotective ratio against SH-SHY5Y cell lines.

A novel structural class of coumarin-chalcone fibrates as PPARα/γ agonists with potent antioxidant activities: Design, synthesis, biological evaluation and molecular docking studies.

A series of structurally interesting coumarin-chalcone fibrates were synthesized and evaluated for their PPARα/γ agonist activities and antioxidant activities. Among these compounds, compounds 5a, 5d, and 7a were identified as potent PPARα and γ dual agonists, and their PPARα agonist activities were found to be more potent than that of Fenofibrate. Furthermore, the results of antioxidant investigations revealed that compounds 5d and 6a-6d had greater potency than Trolox with IC values ranging from 9.

Synthesis of new sarsasapogenin derivatives with cytotoxicity and apoptosis-inducing activities in human breast cancer MCF-7 cells.

Based on the fact that Timosaponin A-III, a saponin isolated from the rhizome of Anemarrhena asphodeloides, is a promising bioactive lead compound in the treatment of cancer, structural modification at the C3 and C26 positions of sarsasapogenin has always been the focus of our structure-activity investigations. In this paper, we describe the synthesis of a range of new derivatives 5a-5o and the evaluation of their antitumor activities in a panel of six human cancer cell lines using the MTT assay in vitro. The results obtained showed that compounds 5h, 5i, and 5n exhibited significant cytotoxic activities against the six cell lines, being more potent than their parent compound sarsasapogenin.

How do the substrate reaction forces acting on a gecko's limbs respond to inclines?

Locomotion is an essential character of animals, and excellent moving ability results from the delicate sensing of the substrate reaction forces (SRF) acting on body and modulating the behavior to adapt the motion requirement. The inclined substrates present in habitats pose a number of functional challenges to locomotion. In order to effectively overcome these challenges, climbing geckos execute complex and accurate movements that involve both the front and hind limbs.