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1.
Article in English | MEDLINE | ID: mdl-35805404

ABSTRACT

As the most important driving force for ensuring the effective supply of grain in the country, the production stability of the major grain-producing areas directly concerns the national security of China. In this paper, considering the "water-soil-energy-carbon" correlation, water, soil and energy resource factors, and carbon emission constraints were included in an index system, and the global common frontier boundary three-stage super-efficient EBM-GML model was used to measure the grain production resource utilization efficiency of the major grain-producing areas in China from 2000 to 2019. This paper also analyzed the static and dynamic spatiotemporal characteristics and the restrictions of utilization efficiency. The results showed that, under the measurement of the traditional data envelopment analysis model, the grain production resource utilization efficiency in the major producing areas is relatively high, but there is still room to improve by more than 20%, and grain production still has enormous growth potential. After excluding external environmental and random factors, it was found that the utilization efficiency of grain production resources in the major producing areas decreased, and the efficiency and ranking of provinces changed significantly. External factors inhibit pure technical efficiency and expand the scale efficiency. The utilization efficiency of Northeast China was much higher than that of the Huang-Huai-Hai region and the middle and upper reaches of the Yangtze River region, and its grain production resource allocation management had obvious advantages. The total factor productivity index of food production resources showed an upward trend as a whole, and its change was affected by both technological efficiency and technological progress, of which technological progress had the greater impact. Therefore, reducing the differences in the external environment of different regions while making adjustments in accordance with their own potential is an effective way to further improve the utilization efficiency of food production resources.


Subject(s)
Carbon , Efficiency , Carbon/analysis , China , Economic Development , Edible Grain/chemistry , Soil , Water
2.
ChemistryOpen ; 7(4): 302-309, 2018 Apr.
Article in English | MEDLINE | ID: mdl-29721402

ABSTRACT

Complexity-generating chemical transformations that afford novel molecular scaffolds enriched in sp3 character are highly desired. Here, we present a highly stereoselective scaffold diversity synthesis approach that utilizes cascade double-annulation reactions of diverse pairs of zwitterionic and non-zwitterionic partners with 3-formylchromones to generate highly complex tetracyclic benzopyrones. Each pair of annulation partners adds to the common chroman-4-one scaffold to build two new rings, supporting up to four contiguous chiral centers that include an all-carbon quaternary center. Differently ring-fused benzopyrones display different biological activities, thus demonstrating their immense potential in medicinal chemistry and chemical biology research.

3.
Bioorg Med Chem ; 22(18): 5110-6, 2014 Sep 15.
Article in English | MEDLINE | ID: mdl-24530033

ABSTRACT

Natural products represent compound classes with high chemical and structural diversity and various biological activities. Libraries based on natural products are valuable starting point in the search for novel biologically active substances. Here we report on the identification of the natural product podoverine A from the plant Podophyllum versipelle Hance as a novel tubulin-acting agent. A natural product compound collection was subjected to a high-content screen that monitors changes in cytoskeleton and DNA and podoverine A was identified as inhibitor of mitosis. This natural product causes mitotic arrest and inhibits microtubule polymerization in vitro and in cells by targeting the vinca binding site on tubulin.


Subject(s)
Antineoplastic Agents, Phytogenic/pharmacology , Biological Products/pharmacology , Flavones/pharmacology , Microtubules/drug effects , Podophyllum/chemistry , Tubulin Modulators/pharmacology , Animals , Antineoplastic Agents, Phytogenic/chemistry , Antineoplastic Agents, Phytogenic/isolation & purification , Biological Products/chemistry , Biological Products/isolation & purification , Cell Cycle/drug effects , Cell Line , Cell Proliferation/drug effects , Chlorocebus aethiops , Dose-Response Relationship, Drug , Drug Screening Assays, Antitumor , Flavones/chemistry , Flavones/isolation & purification , HeLa Cells , Humans , MCF-7 Cells , Microtubules/metabolism , Molecular Structure , Polymerization/drug effects , Structure-Activity Relationship , Tubulin Modulators/chemistry , Tubulin Modulators/isolation & purification
4.
Angew Chem Int Ed Engl ; 52(1): 410-4, 2013 Jan 02.
Article in English | MEDLINE | ID: mdl-23080551

ABSTRACT

A Prins cyclization between a polymer-bound aldehyde and a homoallylic alcohol served as the key step in the synthesis of tetrahydropyran derivatives. A phenotypic screen led to the identification of compounds that inhibit mitosis (as seen by the accumulation of round cells with condensed DNA and membrane blebs). These compounds were termed tubulexins as they target the CSE1L protein and the vinca alkaloid binding site of tubulin.


Subject(s)
Cellular Apoptosis Susceptibility Protein/metabolism , Pyrans/chemical synthesis , Pyrans/pharmacology , Tubulin/metabolism , Animals , Binding Sites , Cellular Apoptosis Susceptibility Protein/chemistry , HeLa Cells , Humans , MCF-7 Cells , Mitosis/drug effects , Mitosis Modulators , Pyrans/chemistry , Tubulin/chemistry , Tubulin Modulators/chemical synthesis , Tubulin Modulators/chemistry , Tubulin Modulators/pharmacology
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