Chromium Picolinate Regulates Bone Metabolism and Prevents Bone Loss in Diabetic Rats.

Diabetic osteoporosis (DOP) is an abnormal metabolic disease caused by long-term hyperglycemia. In this study, a model rat of streptozotocin (STZ)-induced diabetes was established, and chromium picolinate (5 mg·kg-1) was given; the changes in blood glucose and body weight were detected before and after administration; and bone mineral density (BMD), bone morphology, bone turnover markers, inflammatory cytokines, and oxidative stress indicators were observed in each group. We found that after chromium picolinate (CP) intervention for 8 weeks, the blood glucose level was decreased; the BMD, the bone histomorphology parameters, and the pathological structure were improved; the expression of bone resorption-related proteins was downregulated; and the expression of bone formation-related proteins was upregulated. Meanwhile, serum antioxidant activity was increased, and inflammatory cytokine levels were decreased. In conclusion, CP could alleviate DOP by anti-oxidation, inhibition of bone turnover, anti-inflammation, and regulation of the OPG/RANKL/RANK signaling pathway. Therefore, CP has important application values for further development as a functional food or active medicine in DOP treatment.

Chromium Picolinate Protects against Testicular Damage in STZ-Induced Diabetic Rats via Anti-Inflammation, Anti-Oxidation, Inhibiting Apoptosis, and Regulating the TGF-ß1/Smad Pathway.

Chromium picolinate (CP) is an organic compound that has long been used to treat diabetes. Our previous studies found CP could relieve diabetic nephropathy. Thus, we speculate that it might have a positive effect on diabetic testicular injury. In this study, a diabetic rat model was established, and then the rats were treated with CP for 8 weeks. We found that the levels of blood glucose, food, and water intake were reduced, and body weight was enhanced in diabetic rats after CP supplementation. Meanwhile, in CP treatment groups, the levels of male hormone and sperm parameters were improved, the pathological structure of the testicular tissue was repaired, and testicular fibrosis was inhibited. In addition, CP reduced the levels of serum inflammatory cytokines, and decreased oxidative stress and apoptosis in the testicular tissue. In conclusion, CP could ameliorate testicular damage in diabetic rats, as well as being a potential testicle-protective nutrient in the future to prevent the testicular damage caused by diabetes.

The stereoselective conversion of epimerized alkoxyl phosphine-borane to P,C, axial-stereogenic tertiary phosphine via cleavage of P-O bond.

The P-O bond of epimerized alkoxyl phosphine-borane was cleaved by naphthalene-lithium, to form two diastereomers of P-anions in a ratio of 86 : 14, which was then converted to secondary phosphine-borane via acidification, and to tertiary phosphines with alkyl halides with enhanced 96 : 4 dr. The isolated tertiary phosphine containing hydroxyl (in >99 : 1 dr) was converted to multi-stereogenic tertiary phosphines via O-alkylation with alkylene dihalides.

ZnO-Co3O4/N-C Cage Derived from the Hollow Zn/Co ZIF for Enhanced Degradation of Bisphenol A with Persulfate.

The zeolitic imidazolate framework (ZIF)-67 microcrystal was employed as a precursor to synthesize the hollow ZIF-8/ZIF-67 composite via the epitaxial growth of ZIF-8 on ZIF-67, in situ self-sacrifice, and excavation of ZIF-67. The hollow ZIF-8/ZIF-67 composite was successfully transformed to the ZnO-Co3O4/N-C cage by thermal treatment, which was further used as the catalyst for the oxidative degradation of bisphenol A (BPA) in the presence of potassium persulfate (PS). In comparison with the Co3O4/N-C and Co3O4 obtained from pure ZIF-67 and cobalt nitrate, the ZnO-Co3O4/N-C cage demonstrated a more than four fold-higher activity and robust reusability. Based on structural analysis, the enhanced catalytic performance could be ascribed to the small, highly dispersed cobalt oxide particles, the hollow structure that facilitated the transportation of the molecules, and the synergistic effect between cobalt oxide and nitrogen-doped carbon in the composite. Besides, the effect of dosage of PS, BPA, and the co-existing components such as chloride ion, methanol, and t-butyl alcohol was carefully investigated to propose the possible mechanism. This study would give new insights into the design of functional composite materials from metal organic frameworks and the development of their application in environmental pollution disposal.

The construction of benzimidazo[2,1-a]isoquinolin-6(5H)-ones from N-methacryloyl-2-phenylbenzoimidazoles through radical strategies.

Benzimidazo[2,1-a]isoquinolin-6(5H)-one constitutes a structurally unique class of tetracyclic N-heterocycles that are found throughout a myriad of biologically active natural products, pharmaceutical compounds, and functional materials. Various synthetic routes for the preparation of benzimidazo[2,1-a]isoquinolin-6(5H)-ones have been reported. In particular, the use of N-methacryloyl-2-phenylbenzoimidazoles to construct benzimidazo[2,1-a]isoquinolin-6(5H)-ones through various radical strategies have attracted widespread attention due to the versatility and simple preparation of raw materials, as well as the step-economy and mild reaction conditions. Using representative examples, we highlight significant progress in the synthesis of benzimidazo[2,1-a]isoquinolin-6(5H)-ones, including the selection of the catalytic system, substrate scope, mechanistic understanding, and applications. The contents of this review focus on the development of C-, S-, P-, and Si-centered radical addition-intramolecular cyclization strategies.

Recent progress in the radical α-C(sp3)-H functionalization of ketones.

The direct use structurally simple ketones as α-ketone radical sources for α-C(sp3)-H functionalization is a sustainable and powerful approach for constructing complex and multifunctional chemical scaffolds with diverse applications. The reactions of α-ketone radicals with alkenes, alkynes, enynes, imides, and imidazo[1,2-a]pyridines have broadened the structural diversity and complexity of ketones. Through chosen illustrative examples, we outline the recent progress in the development of methods that enable the radical α-C(sp3)-H functionalization of ketones, with an emphasis on radical initiation systems and possible mechanisms of the transformations. The application of these strategies is illustrated by the synthesis of several biologically active molecules and drug molecules. Further subdivision is based on substrate type and reaction type.

Selective divergent radical cyclization of 1,6-dienes with alkyl nitriles.

An efficient, selective, and step economical radical cyclization of 1,6-dienes with alkyl nitriles initiated by α-C(sp3)-H functionalization under the Sc(OTf)3 and Ag2CO3 system is described here. The selective divergent cyclization relies on the substitution effect at the α-position of the acrylamide moiety and nitriles, which is terminated by hydrogen abstraction, direct cyclization with the aryl ring, or further cyclization with the CN bond and hydrolysis, respectively.

An Integrated Mission Planning Framework for Sensor Allocation and Path Planning of Heterogeneous Multi-UAV Systems.

Mission planning is the guidance for a UAV team to perform missions, which plays the most critical role in military and civil applications. For complex tasks, it requires heterogeneous cooperative multi-UAVs to satisfy several mission requirements. Meanwhile, airborne sensor allocation and path planning are the critical components of heterogeneous multi-UAVs system mission planning problems, which affect the mission profit to a large extent. This paper establishes the mathematical model for the integrated sensor allocation and path planning problem to maximize the total task profit and minimize travel costs, simultaneously. We present an integrated mission planning framework based on a two-level adaptive variable neighborhood search algorithm to address the coupled problem. The first-level is devoted to planning a reasonable airborne sensor allocation plan, and the second-level aims to optimize the path of the heterogeneous multi-UAVs system. To improve the mission planning framework's efficiency, an adaptive mechanism is presented to guide the search direction intelligently during the iterative process. Simulation results show that the effectiveness of the proposed framework. Compared to the conventional methods, the better performance of planning results is achieved.

Oxidize Amines to Nitrile Oxides: One Type of Amine Oxidation and Its Application to Directly Construct Isoxazoles and Isoxazolines.

A facile oxidative heterocyclization of commercially available amines and tert-butyl nitrite with alkynes or alkenes leading to isoxazoles or isoxazolines is described. The unprecedented strategy of the oxidation of an amine directly to a nitrile oxide was used in this cyclization process. This reaction is highly efficient, regiospecific, operationally simple, mild, and tolerant of a variety of functional groups. Control experiments support a nitrile oxide intermediate mechanism for this novel class of oxidative cyclization reactions. Moreover, synthetic applications toward bioactive molecular skeletons and the late-stage modification of drugs were realized.

Stereoselective preparation of P,axial-stereogenic allenyl bisphosphine oxides via chirality-transfer.

P,C-Stereogenic propargyl alcohols RC-3/SC-3' were prepared by the addition of (L)-menthyl-derived SPOs to propynals, which were converted to P,axial-stereogenic allenyl bisphosphine oxides. The chirality transfer was controlled by α-carbon via syn [2,3]-sigmatropic rearrangement. For SC-3' linking weak WDG on the alkynyl moiety, the chirality on the axis depended on stereogenic phosphorus.

Solving the Multi-Functional Heterogeneous UAV Cooperative Mission Planning Problem Using Multi-Swarm Fruit Fly Optimization Algorithm.

The complexity of unmanned aerial vehicle (UAV) missions is increasing with the rapid development of UAV technology. Multiple UAVs usually cooperate in the form of teams to improve the efficiency of mission execution. The UAVs are equipped with multiple sensors with complementary functions to adapt to the complex mission constraints. Reasonable task assignment, task scheduling, and UAV trajectory planning are the prerequisites for efficient cooperation of multi-functional heterogeneous UAVs. In this paper, a multi-swarm fruit fly optimization algorithm (MFOA) with dual strategy switching is proposed to solve the multi-functional heterogeneous UAV cooperative mission planning problem with the criterion of simultaneously minimizing the makespan and the total mission time. First, the multi-swarm mechanism is introduced to enhance the global search capability of the fruit fly optimization algorithm. Second, in the smell-based search phase, the local search strategies and large-scale search strategies are designed to drive multiple fruit fly swarms, and the dual strategy switching method is presented. Third, in the vision-based search stage, the greedy selection strategy is adopted. Finally, numerical simulation experiments are designed. The simulation results show that the MFOA algorithm is more effective and stable for solving the multi-functional heterogeneous UAV cooperative mission planning problem compared with other algorithms.

Competing Dehalogenation versus Borylation of Aryl Iodides and Bromides under Transition-Metal-Free Basic Conditions.

In this work, selectivity-controllable base-promoted transition-metal-free borylation and dehalogenation of aryl halides are described. Under the conditions of borylation, the dehalogenation which emerges as a competitive side reaction has been well-controlled by carefully controlling the borylation conditions. On the other hand, the dehalogenation using benzaldehyde as a hydrogen source has also been accomplished. The applications of direct radical borylation and dehalogenation of aryl halides demonstrate their synthetic practicability in pharmaceutical-oriented organic synthesis. Based on the experimental evidences, the tBuOK/1,10-Phen-triggered radical nature of both competitive reactions has been revealed.

Cyclodextrin-Assisted Synthesis of Pd/Co/C Nanopolyhedra by ZIF-67 as a Highly Acid Tolerant Catalyst for Hexavalent Chromium Reduction.

The palladium/cobalt/carbon (Pd/Co/C) nanopolyhedra were synthesized by calcinating the precursor prepared by a cyclodextrin (CD) modified palladium acetylacetonate loaded on ZIF-67, hydroxypropyl-ß-cyclodextrin (HP-ß-CD)-[Pd(acac)2]/ZIF-67. On one hand, the HP-ß-CD was used to increase the solubility of Pd(acac)2 by supramolecular interactions, and on the other hand, ZIF-67 was employed to provide the Co/C as the magnetic support. The Pd/Co/C nanopolyhedra obtained with the assistance of HP-ß-CD have high activity and reusability for the reduction of the dichromate ion in the presence of formic acid without using any buffer solution, and no significant leaching of metallic Co of the catalyst was observed. This could be ascribed to the fact that the presence of HP-ß-CD could lead to a more homogeneous distribution of metallic Pd in the Pd/Co/C nanopolyhedra, which could prevent the dissolution of metallic Co by formic acid.

Phytochemicals Content, Antioxidant and Antibacterial Activities of Sophora viciifolia.

The objective of this study is to compare the efficacy of ethanol extracts from different parts of Sophora viciifolia. The content of polyphenols, flavonoids, alkaloids, and antioxidant capacity, antimicrobial activity were investigated, and individual polyphenols and alkaloids were analyzed and quantified by ultra-high performance liquid chromatography (UPLC). The microdilution method was used to determine the antimicrobial activity of extracts from S. viciifolia on six strains. The results for extracts from the different parts (flowers, leaves, and fruit) were compared in varying concentrations to determine whether one extract source is superior to another. Testing verified that extracts from the different parts of S. viciifolia did vary, as expected. For example, extract from the leaves had the best antimicrobial activity against pathogenic Candida albicans, but all extracts had good antimicrobial activity against the six tested strains. These results reveal that the active substances in S. viciifolia are abundant and have good antioxidant and antimicrobial activities, which can provide theoretical support for the subsequent development and utilization of S. viciifolia extracts.

Baseflow estimation for catchments in the Loess Plateau, China.

Baseflow is the portion of streamflow that originates from groundwater. It is pivotal to groundwater supply as well as the interactions between groundwater and surface water. In the Loess Plateau of China, the baseflow plays a fundamental role in sustaining the aquatic ecosystem. Rational estimation of baseflow is of critical importance for understanding the functioning of the groundwater system and informing management of regional water resources. In this study, a two-well parameterised digital filter was used to separate baseflow from observed daily total streamflow on the Weihe River Basin. Two parameters (maximum baseflow index (BFImax) and the recession constant) of this filter were estimated using UKIH and a recession analysis with physical meaning, respectively. The results show that the baseflow index increased from the upstream to downstream (0.27-0.32) of the Weihe River, and the baseflow of the river is summer dominant. In general, the baseflow has been increasing gradually owing to the implementation of soil conservation measures. This study provides an understanding of baseflow response to seasonal variability and water environmental management in basin scale.

Icariin Prevents Diabetes-Induced Bone Loss in Rats by Reducing Blood Glucose and Suppressing Bone Turnover.

Diabetic Osteoporosis (DOP) is a common metabolic bone disease, characterized by decreased bone mineral density (BMD) and destruction of bone microstructure. It has been reported that icariin is beneficial for estrogen deficiency-induced osteoporosis, and alcohol-induced osteoporosis; whether icariin has protective effects on diabetes-induced osteoporosis has not been reported. In this study, a rat model of diabetic osteoporosis was established by streptozotocin injection, the bone protective effects and potential mechanism of icariin on diabetes-induced bone loss was observed. Thirty 8-week-old female Sprague Dawley rats were divided into control group (vehicle treatment), T1DM (diabetic) group and T1DM-icariin (ICA) group (diabetic rats treated with icariin), 10 rats in each group. The bone histomorphometry parameters, bone mineral density (BMD), serum bone turnover markers, and bone marrow adipogenesis were analyzed after 8 weeks of icariin administration. The results showed consumption of icariin at a doses of 100 mg kg-1 decreased blood glucose, and increased the BMD of diabetic rats. Icariin effectively decreased serum bone turnover marker levels, including CTX-1, ALP, TRACP 5b, osteocalcin, and PINP. Meanwhile, the bone histomorphometry parameters, the number of osteoclasts per bone perimeter were turned to be normal level, and the icariin treatment suppressed bone marrow adipogenesis. The runt-related transcription factor 2 (RUNX 2), as well as the osteoprotegerin (OPG)/receptor activator of nuclear factor-κ B ligand (RANKL) ratio in serum and bone tissues were increased significantly after icariin treatment in diabetic rats. All of the above indicate that oral administration of icariin can prevent diabetic osteoporosis; the effect is mainly related to its ability to reduce blood glucose, inhibit bone turnover and bone marrow adipogenesis, as well as up-regulate bone RUNX 2, and OPG expression.

Salidroside Improves Bone Histomorphology and Prevents Bone Loss in Ovariectomized Diabetic Rats by Upregulating the OPG/RANKL Ratio.

Postmenopausal diabetic women have a high risk of fractures. Salidroside has preventive effects on estrogen deficiency-induced osteoporosis and has hypoglycemic effects on diabetes in rats. However, whether salidroside inhibits bone loss in postmenopausal diabetic patients is still unknown. Here, we established a rat model of osteoporosis to investigate the protective effects of salidroside on bone loss induced by ovariectomy combined with diabetes, also investigating the underlying mechanisms. Two-month-old female Sprague-Dawley rats were divided into three equal groups (10 rats in each group): control group (with sham operation, treated with drug vehicle); OVX/T1DM group (ovariectomized diabetic rats); OVX/T1DM-SAL group, comprising ovariectomized diabetic rats treated with salidroside (20 mg/kg body weight) by gavage. The results showed that after 60 consecutive days of treatment, the bone mineral density (BMD) of OVX/T1DM-SAL increased significantly compared with the OVX/T1DM group (p < 0.01). The level of serum bone turnover markers, including alkaline phosphatase (ALP), cross linked c-telopeptide of type I collagen (CTX-1), osteocalcin, N-terminal propeptide of type I procollagen (PINP), and tartrate-resistant acid phosphatase 5b (TRACP 5b) were all increased in the OVX/T1DM group compared with the control (p < 0.01), and those were decreased by salidroside treatment. Meanwhile, the bone histopathological changes were also attenuated, and the bone marrow adipogenesis was inhibited in salidroside treated rats. Moreover, protein and mRNA ratio of bone osteoprotegerin (OPG)/receptor activator of nuclear factor-κB ligand (RANKL) was upregulated in ovariectomized diabetic rats by salidroside treatment. The results above indicated that the protective effect of salidroside on bone loss induced by ovariectomy and diabetes was mainly due to its ability to suppress bone turnover, inhibit bone marrow adipogenesis, and up-regulate the OPG/RANKL ratio.

Pharmaceutical-Oriented Selective Synthesis of Mononitriles and Dinitriles Directly from Methyl(hetero)arenes: Access to Chiral Nitriles and Citalopram.

A pharmaceutical-oriented, transition-metal-free, cyanide-free one-step direct transformation of methylarenes to aryl nitriles is described. For the dimethylarenes, the selectivity can be well-controlled to form mononitriles or dinitriles. Enantioenriched nitriles can also be synthesized by this method. As a pharmaceutically practical method, the antidepressant drug citalopram was synthesized from cheap and commercially abundant m-xylene on a gram scale in high yield, avoiding transition-metal residues and toxic cyanides.

Addition of optically pure H-phosphinate to ketones: selectivity, stereochemistry and mechanism.

Aromatic methyl ketones and cyclic asymmetric ketones underwent hydrophosphorylation with P-stereogenic H-P species in the presence of potassium carbonate to produce P,C-stereogenic tertiary α-hydroxyl phosphinates in excellent yields with up to 99 : 1 dr. The diastereoselectivity was induced by a reversible conversion of less stable stereomer of product to that of a more stable one via an equilibrium, which was confirmed by aldehyde/ketone exchanging reaction. Toward the exchange, aliphatic or aldehyde carbonyl were more active than aromatic or ketone carbonyls, respectively. The stability difference between the two diastereomers was controlled by the sizes of substituents linking to phosphorus or α-carbon.

Divergent determinants on interannual variability of terrestrial water cycle across the globe.

Intensifying variability in precipitation under a changing climate is projected to amplify fluctuation in terrestrial hydrological cycle, leading to more severe water-related disasters. The connections between interannual variability of hydrological components and factors influencing these connections have not been clearly defined yet. Based on terrestrial water budget from Climate Data Record, we identify dominant factors influencing partitioning interannual variability of precipitation (P) into that of evapotranspiration (E), runoff (Q), and water storage deviation (ΔS) across the globe by employing geographical detector model (GDM). Sensitivities of the variability partitioning to dominant factors are quantified for different hydroclimate regions by linear regression model and law of total differential. Results show that dominant factors influencing precipitation variability partitioning (VP) are different across distinct hydroclimate conditions. Comparing the statistical index (q value) of the GDM, it can be seen that surface air temperature (Ta), snow water equivalent (SWE) and water storage capacity (Smax) are dominant factors of VP in humid, semi-arid and arid regions, respectively. Changes in P variability largely can transfer into Q variability in humid region. The P variability partitioned into Q variability is dramatically reduced in semi-arid region with SWE decreasing, while P variability partitioned into ΔS variability increases with Smax increasing in arid region. Joint effects of Ta and coefficient of variation of precipitation (Pcv) are found to be the most important interaction in determining VP across the globe. Furthermore, warmer temperatures in humid region cause >90 % of the change in precipitation variability to be transferred to Q variability change. In semi-arid region with snowfall, decreased SWE has strong effect on changes in ΔS (30-40 %) and Q (20-40 %) variability. Our findings imply a changing VP and more severe impacts of hydrological extremes under future climate, where intensive changes in Ta, SWE and land cover are projected.